Volker Bühler

Generic Drug Formulations

Fine Chemicals
(4th edition 2001)

1 Introduction
1.1 Preface
A selection of more than 500 formulations of human and veterinary drugs
are presented in this booklet. They
have all been developed in the last 22
years in the Applications Laboratories
of BASF AG and are in solid, liquid,
and semi-solid form. However, emphasis is placed on tablets. Human
and veterinary medicines have not
been dealt with in separate chapters,
because the technologies and excipients are the same.

BASF Pharma Ingredients Generic Drug Formulations 2001

1.2 List of all formulations aranged alphabetically

A
Aceclofenac Gel-Cream (1.5 %)
Aceclofenac Instant Granules (50 mg)
Acetylcysteine Effervescent Tablets
(600 mg)
Acetylsalicylic Acid + Paracetamol
(= Acetaminophen) + Caffeine
Tablets (250 mg + 250 mg + 50 mg)
Acetylsalicylic Acid + Paracetamol
(= Acetaminophen) + Caffeine Tablets (400 mg + 100 mg + 30 mg)
Acetylsalicylic Acid + Paracetamol
(= Acetaminophen) Tablets (250 mg
+ 250 mg)
Acetylsalicylic Acid + Vitamin C Effervescent Tablets (400 mg + 250 mg)
Acetylsalicylic Acid + Vitamin C Tablets
(325 mg + 250 mg)
Acetylsalicylic Acid + Vitamin C Tablets
(400 mg + 250 mg)
Acetylsalicylic Acid Tablets (400 mg)
Acetylsalicylic Acid Tablets (500 mg)
Aciclovir Oral Suspension
(2 % = 200 mg/10 ml)
Adhesive Buccal Tablets
(Basic Formulation)
Albendazole Dry Syrup or Instant
Granules (200 mg)
Albendazole Tablets, (100 mg)
Alginic Acid + Aluminium Hydroxide +
Magnesium Silicate Tablets
(500 mg + 100 mg + 25 mg)
Aloe Vera Gel
Alpha-Bisabolol Aqueous Mouth Wash
Solution (0.2 %)
Alpha-Bisabolol Buccal or Topical
Solution (0.1%)
Alpha-Bisabolol Mouth Wash Solution
(0.5 %)
Alpha-Methyldopa Tablet Cores
(250 mg), DC
Alpha-Methyldopa Tablet Cores
(250 mg), WG

Alpha-Methyldopa Tablets
(500 mg), DC
Alpha-Methyldopa Tablets
(500 mg), WG
Alprazolam Tablets (0.5 mg)
Aluminium Acetylsalicylate Tablets
(250 mg)
Aluminium Hydroxide + Magnesium
Carbonate Dry Syrup
(12.5 % + 12.5 %)
Aluminium Hydroxide + Magnesium
carbonate/oxide + Simethicone
Tablets (150 mg + 250 mg + 90 mg)
Aluminium Hydroxide + Magnesium
Hydroxide + Simethicone Suspension (8 % + 8 % + 0.8 %)
Aluminium Hydroxide + Magnesium
Hydroxide Chewable Tablets
(200 mg + 200 mg)
Aluminium Hydroxide + Magnesium
Hydroxide Suspension (4 % + 4 %)
Aluminium Hydroxide + Magnesium
Silicate Chewable Tablets
(120 mg + 250 mg)
Ambroxol Tablets (30 mg)
Aminophylline Tablets (90 mg)
Aminophylline Tablets (100 mg), DC
Aminophylline Tablets, WG (100 mg)
Amitryptylline Tablets
(10 mg and 25 mg)
Amoxicillin Dry Syrup
(5 % = 500 mg/10 ml)
Amoxicillin Lyophylisate for Injection
(250 mg)
Amoxicillin Tablets (125 mg)
Ampicillin + Cloxacillin Oily Suspension
(1.5 % + 4.0 %)
Ampicillin Dry Syrup
(5 % = 500 mg/10 ml)
Ampicillin Tablets (250 mg)
Ampicillin Tablets (500 mg)
Anise Oil Solution (1%)
Asparagus Extract + Parsley Extract
Tablets (200 mg + 200 mg)

BASF Pharma Ingredients Generic Drug Formulations 2001

Aspartame Effervescent Tablets
(20 mg)
Aspartame Tablets (25 mg), DC
Aspartame Tablets (25 mg), WG
Atenolol Tablets (90 mg)
Azithromycin Dry Syrup
(5 % = 500 mg/10 ml)
Azithromycin Suspension
(5 % = 500 mg/10 ml)
Azulene solution (1%)
B
Barium Sulfate Oral Suspension (23 %)
Basic Cream for Different Active
Ingredients
Benzhexol Tablets (5 mg)
Benzoyl Peroxide + Alpha-Bisabolol
Gel (5.0 % + 0.2 %)
Benzyl Benzoate Solution (10 %)
Benzylpenicilline + Dihydrostreptomycin Injectable Suspension
(200,000 units + 200 mg/ml)
Berberine Tablets (5 mg)
Beta Carotene + Vitamin C + Vitamin E
Chewable Tablets (3 mg + 50 mg +
25 mg)
Beta Carotene + Vitamin C + Vitamin E
Chewable Tablets (10 mg + 500 mg
+ 250 mg)
Beta Carotene + Vitamin C + Vitamin E
Effervescent Tablets (12 mg +
150 mg + 25 mg)
Beta Carotene + Vitamin C + Vitamin E
Tablets (6 mg + 100 mg + 30 mg)
Beta Carotene + Vitamin C + Vitamin E
Tablets (7 mg + 60 mg + 25 mg)
Beta Carotene + Vitamin C + Vitamin E
Tablets (12 mg + 250 mg + 125 mg)
Beta Carotene Effervescent Tablets
(7 mg)
Beta Carotene Tablets (15 mg)
Betamethasone + Neomycin
Gel-Cream (0.1% + 0.6 %)
Betamethasone Cream (0.1%)
Betamethasone Gel (0.1%)
Bifonazole Cream (1%)

BASF Pharma Ingredients Generic Drug Formulations 2001

Bran Tablets (250 mg), WG
Bran Tablets (250 mg), DC
Bromhexine Tablets (8 mg)
Bromocriptine Tablet Cores (6 mg)
C
Calcium Carbonate Tablets (500 mg)
Calcium Chewable Tablets (200 mg Ca)
Calcium Effervescent Tablets
(250 mg Ca)
Calcium Gluconate Tablets (350 mg)
Calcium Glycerophosphate Tablets
(200 mg)
Calcium Glycerophosphate Tablets
(500 mg)
Calcium Phosphate Tablets for Cats
and Dogs (400 mg)
Captopril Tablet Cores (25 mg)
Carbamazepine Oral Suspension
(2 % = 100 mg/5 ml)
Carbamazepine Sustained Release
Tablets (200 mg) DC
Carbamazepine Sustained Release
Tablets (200 mg) WG
Carbamazepine Tablets (200 mg)
Carbonyl Iron + Copper Sulfate +
Manganese Sulfate Tablets
(24 mg + 0.16 mg + 3.5 mg)
Carnitine + Coenzym Q Solution
(4.0 % + 0.1%)
Caroate Dispersible Cleaning Tablets
(880 mg)
Caroate Effervescent Cleaning Tablets
(650 mg)
Cetylpyridinium Lozenges (2.5 mg)
Charcoal Tablets I (250 mg)
Charcoal Tablets II (250 mg)
Chloramphenicol Ophthalmic Solution
(3 %)
Chloramphenicol Palmitate Oral or
Topical Emulsion
(2.5 % = 250 mg/10 ml)
Chloramphenicol Palmitate Oral or
Topical Emulsion
(5.0 % = 500 mg/10 ml)

Chlorhexidine Gel (2 %)
Chlorhexidine Lozenges (5 mg)
Chloroquine Tablets (250 mg)
Choline Theophyllinate Tablets (100 mg)
Chymotrypsine Tablets (27 mg)
Cimetidine Effervescent Tablets
(400 mg)
Cimetidine Tablets (200 mg)
Cimetidine Tablets (280 mg)
Cimetidine Tablets (400 mg)
Clenbuterol Tablets (20 µg)
Clobazam Tablets (10 mg)
Clomifen Citrate Tablets (50 mg)
Closantel Veterinary Injectable Solution
(12 – 20 g/100 ml)
Clotrimazole Cream (1%)
Clotrimazole Topical Solution (3 %)
Crospovidone Effervescent Tablets
(1000 mg)
Crospovidone Oral Suspension
(2000 mg/10 ml)
Crospovidone Water Dispersible
Tablets (1000 mg)
Cyproheptadine Tablet (4 mg)

Doxazosin Mesylate Tablets
(1 mg and 4 mg)
E
Enteric Film Coating of Acetylsalicylic
Acid Crystals (Aqueous)
Enteric Film Coating of Pellets
(Aqueous)
Enteric Film Coating of Soft Gelatin
Capsules (Aqueous, colourless)
Enteric Film Coating of Tablets
(Aqueous) I
Enteric Film Coating of Tablets
(Aqueous) II
Erythromycin Gel (1%)
Ethambutol Tablets (400 mg), DC
Ethambutol Tablets (400 mg), WG
Ethambutol Tablets (800 mg)
Etophylline + Theophylline Tablets
(100 mg + 22 mg), DC
Etophylline + Theophylline Tablets
(100 mg + 22 mg), WG
Eucalyptol Solution (8 %)

D

F

Dexpanthenol Gel-Cream (5 %)
Diazepam Injectable Solution
(2.5 mg/ml)
Diazepam Tablet (10 mg)
Diclofenac Gel (1%)
Diclofenac Gel-Cream (1%)
Diclofenac Injectable Solution
(75 mg/3 ml)
Diclofenac Oral Solution (1.5 %)
Diclofenac Spheronized Pellets for
Sustained Release Coating (30 %)
Diclofenac Sustained Release Tablets
(100 mg)
Diclofenac Tablet Cores (50 mg)
Diclofenac Tablets (50 mg)
Diltiazem Tablets (50 mg)
Dimenhydrinate Tablet Cores (100 mg)
Dimenhydrinate Tablets (50 mg), DC
Dimenhydrinate Tablets (50 mg), WG
Dipyrone see Metamizol

Famotidine Tablets (40 mg)
Ferrous Fumarate Tablets (200 mg)
Ferrous Sulfate + Manganese Sulfate +
Copper Sulfate Tablets
(65 mg + 3.5 mg + 0.16 mg)
Ferrous Sulfate Tablets (200 mg)
Fir Needle Oil Solution (3 %)
Fluoxetine Tablets (20 mg)
Folic Acid Tablets (5 mg)
Furaltadone Injectable Solution
(50 mg/ml)
Furosemide Tablets (40 mg)
Furosemide Tablets (200 mg)
Fusidic Acid Tablet Cores (125 mg)
G
Garlic Extract + Thyme Extract Tablets
Cores with Vitamin C
(300 mg + 25 mg + 100 mg)

BASF Pharma Ingredients Generic Drug Formulations 2001

Garlic Tablets Cores (100 mg)
Gemfibrozil Tablets (600 mg)
Ginkgo Extract Tablets (40 mg)
Glibenclamide (Glyburide) Tablets
(5 mg)
Glutaminic Acid Tablets (550 mg)
Gramicidin Ophthalmic Solution
(1.3 mg/10 ml)
Griseofulvin Tablets (125 mg)
Griseofulvin Tablets (500 mg)
H
Heparin Gel-Cream (300 i.u./g)
Horsetail Extract Tablets (450 mg)
Hydrochlorothiazide + Potassium Chloride Tablet Cores (50 mg + 300 mg)
Hydrochlorothiazide Tablets
(50 mg), DC
Hydrochlorothiazide Tablets
(50 mg), WG
Hydrocortisone Aqueous Gels (1%)
Hydrocortisone Cream (1%)
Hydrocortisone Ethanolic Gel (0.5 %)
I
Ibuprofen Gel-Cream (5 %)
Ibuprofen Gels (5 %)
Ibuprofen Solution (2 %)
Ibuprofen Suspension
(4 % = 400 mg/10 ml), I
Ibuprofen Suspension
(4 % = 400 mg/10 ml), II
Ibuprofen Tablets (400 mg), DC
Ibuprofen Tablets (400 mg), WG
Ibuprofen Tablets (600 mg), DC
Indomethacin Gel (1%), I
Indomethacin Gel (1%), II
Indomethacin Powder for Hard Gelatin
Capsules (160 mg)
Indomethacin Suppositories (50 mg)
Indomethacin Sustained Release
Tablets (75 mg)
Indomethacin Tablets (50 mg), DC
Indomethacin Tablets (50 mg), WG
Indomethacin Tablets (100 mg)

BASF Pharma Ingredients Generic Drug Formulations 2001

Inosin Tablet Cores (200 mg)
Isosorbide Dinitrate Tablets (5 mg)
K
Khellin Tablets (25 mg)
L
Labetalol Tablets (50 mg)
Levamisole Tablets (150 mg)
Levothyroxine Tablets (0.05 mg)
Lidocain Gel (2 %)
Lidocain Gel-Cream (5 %)
Lisinopril Tablets (10 mg)
Lycopene Tablet Cores (6 mg)
M
Magaldrate Chewable Tablets (500 mg)
Magaldrate Chewable Tablets
(1000 mg)
Magaldrate Dispersible Tablets
(700 mg)
Magaldrate Instant Powder or Dry
Syrup (800 mg)
Magaldrate Suspension (10 %)
Magnesium Carbonate Tablets
(260 mg)
Mebendazole Suspension
(2 % = 200 mg/10 ml)
Mebendazole Tablets (100 mg)
Mefenamic Acid Tablets (250 mg)
Meprobamate + Phenobarbital Tablets
(400 mg + 30 mg), DC
Meprobamate + Phenobarbital Tablets
(400 mg + 30 mg), WG
Meprobamate Tablets (400 mg), DC
Meprobamate Tablets (400 mg), WG
Metamizol Tablets (500 mg)
Metformin Tablets (500 mg)
Methyl Cysteine Tablets (100 mg)
Methyl Salicylate + Menthol Gel
(11% + 5 %)
Metoclopramide Tablets (10 mg)
Metronidazole Effervescent Vaginal
Tablets (500 mg)

Metronidazole Injectable Solution
(500 mg/10 ml)
Metronidazole Tablet Cores (400 mg)
Metronidazole Tablets (200 mg)
Metronidazole Tablets (500 mg)
Metronidazole Vaginal Gel (1.2 %)
Miconazole Cream (2 %)
Miconazole Injectable Solution (1%)
Miconazole Mouth Gel (2 %)
Mint Mouth Wash Solutions
Mint Oil Solution (3.5 %)
Mitonafide Tablets (60 mg)
Multivitamin + Calcium + Iron Tablets
(1 RDA of Vitamins)
Multivitamin + Calcium Syrup
(1 RDA of Vitamins/20 ml)
Multivitamin + Carbonyl Iron Tablets
(1 – 2 RDA of Vitamins)
Multivitamin + Minerals Tablets with
Beta Carotene (1 RDA of Vitamins)
Multivitamin + Minerals Tablets with
Beta Carotene (2 RDA of Vitamins)
Multivitamin Chewable Tablets for
Children
Multivitamin Effervescent Granules
(1 RDA of Vitamins)
Multivitamin Effervescent Tablets with
Beta Carotene, Food
(1 – 2 RDA of Vitamins)
Multivitamin Effervescent Tablets I, DC
(1 – 2 RDA of Vitamins)
Multivitamin Effervescent Tablets II, DC
(3 – 4 RDA of Vitamins)
Multivitamin Effervescent Tablets, WG
Multivitamin Injectables for Veterinary
Application
Multivitamin Instant Granules
(2 – 4 RDA of Vitamins)
Multivitamin Oral Gel
Multivitamin Oral Gel with Linoleic Acid
and Linolenic Acid
Multivitamin Syrup, I (1 – 2 RDA/20 ml)
Multivitamin Syrup, II
Multivitamin Tablets, DC
(1 – 2 RDA of Vitamins)
Multivitamin Tablets, WG
(1 – 2 RDA of Vitamins)

Multivitamin Tablet Cores with BetaCarotene (1 – 2 RDA of Vitamins)
Multivitamin Tablets for Dogs
Multivitamin Tablets with Beta
Carotene (1 – 2 RDA of Vitamins)
Multivitamin Tablets with Copper and
Zinc
Multivitamin Two Chamber Ampules
N
Nalidixic Acid Tablets (500 mg)
Naproxen Tablets (250 mg)
Naproxen Tablets (450 mg)
Neomycin Gel (0.05 %)
Neomycin Tablets (250 mg)
Nicotinamide see Vitamin B3
Nicotinic Acid (= Niacin) Tablets
(200 mg)
Nifedipine Tablet Cores (10 mg)
Nitrendipine Tablets (25 mg)
Nitrofurantoin Tablet Cores (100 mg)
Nitrofurantoin Tablets (100 mg)
Norephedrine Syrup (40 mg/10 g)
Nystatin Suspension (100,000 i.u./ml)
Nystatin Tablet Cores (200 mg)
Nystatin Tablets (50 mg and 100 mg)
O
Omega Fatty Acids Tablet Cores
(10 mg EPA + DHA)
Oxytetracycline Injectable Solution for
i. m. + i. v. Veterinary Application
(500 mg/10 ml)
Oxytetracycline Sustained Release
Injectable for i. m. Veterinary
Application (2.2 g / 10 ml)
Oxytetracycline Tablets (250 mg)
P
Pancreatin Tablet Cores (30 mg)
Pancreatin Tablet Cores (130 mg)
Pancreatin Tablet Cores (300 mg)
Paracetamol (= Acetaminophen) +
Caffeine Tablets (500 mg + 50 mg)

BASF Pharma Ingredients Generic Drug Formulations 2001

Paracetamol (= Acetaminophen) +
Doxylamine + Caffeine Effervescent
Granules (500 mg + 5 mg +
33 mg/2.1 g)
Paracetamol (= Acetaminophen) +
Ibuprofen + Orphenadrin Tablets
(250 mg + 200 mg + 100 mg)
Paracetamol (= Acetaminophen) +
Norephedrine + Phenyltoloxamine
Tablets (300 mg + 25 mg + 22 mg)
Paracetamol (= Acetaminophen)
+ Phenprobamat Tablets
(200 mg + 200 mg)
Paracetamol (= Acetaminophen)
Chewable Tablets (300 mg)
Paracetamol (= Acetaminophen)
Effervescent Tablets (500 mg) DC
Paracetamol (= Acetaminophen)
Effervescent Tablets (500 mg) WG
Paracetamol (= Acetaminophen)
Instant Granules (250 mg or 500 mg)
Paracetamol (= Acetaminophen)
Suppositories (150 mg and 500 mg)
Paracetamol (= Acetaminophen)
Suspension (5 % = 500 mg/10 ml)
Paracetamol (= Acetaminophen) Syrup
(5 % = 500 mg/10 g)
Paracetamol (= Acetaminophen) Syrup
for Children (2.5 % = 250 mg/10 ml)
Paracetamol (= Acetaminophen) Tablet
Cores (500 mg)
Paracetamol (= Acetaminophen)
Tablets (500 mg)
Paracetamol (= Acetaminophen)
Tablets for Children (200 mg)
Phendimetrazin Tablets (35 mg)
Phenindione Tablets (50 mg)
Phenolphthalein Tablet Cores (200 mg)
Phenytoin Oral Suspension (5 %)
Phenytoin Sodium Tablets
(100 mg), DC
Phenytoin Sodium Tablets
(100 mg), WG
Phenytoin Tablets (100 mg)
Piroxicam + Dexpanthenol Gel
(0.5 % + 5.0 %)

BASF Pharma Ingredients Generic Drug Formulations 2001

Piroxicam Water Dispersible Tablets
(20 mg)
Placebo Tablets
Polidocanol Wound Spray (0.5 %)
Povidone-Iodine + Lidocain Gel (10 %)
Povidone-Iodine Bar Soap (5 %)
Povidone-Iodine Bar Soaps (5 %)
Povidone-Iodine Concentrates for
Broilers and Cattles (20 %)
Povidone-Iodine Cream (10 %)
Povidone-Iodine Effervescent Vaginal
Tablets (350 mg)
Povidone-Iodine Foam Spray (10 %)
Povidone-Iodine Gargle Solution
Concentrate (10 %)
Povidone-Iodine Mouth Wash and Gargle Solution Concentrate (7.5 %)
Povidone-Iodine Gel-Cream (10 %)
Povidone-Iodine Gels (10 %)
Povidone-Iodine Glucose Ointment
(2.5 %)
Povidone-Iodine Lipstick or After
Shave Stick (10 %)
Povidone-Iodine Liquid Spray (10 %)
Povidone-Iodine Lozenges (5 mg)
Povidone-Iodine Mastitis Cream for
Cattles (10 %)
Povidone-Iodine Ophthalmic Solutions
(0.4 % + 1.0 %)
Povidone-Iodine Powder Spray
Povidone-Iodine Pump Spray (1%)
Povidone-Iodine Seamless Solutions
(10 %)
Povidone-Iodine Shampoo (7.5 %)
Povidone-Iodine Soft Gel (1%)
Povidone-Iodine Solution (10 %), I
Povidone-Iodine Solution (10 %), II
Povidone-Iodine Surgical Scrubs
(7.5 %), I
Povidone-Iodine Surgical Scrubs
(7.5 %), II
Povidone-Iodine Teat-Dip Solution
for Cattles (3 %)
Povidone-Iodine (+ Lidocain)
Thermo-Gelling Solution (10 %)
Povidone-Iodine Transparent Ointment
(10 %)

Povidone-Iodine Vaginal Douche
Concentrate (10 %)
Povidone-Iodine Vaginal Ovula
(5 % and 10 %)
Povidone-Iodine Viscous Solution (1%)
Povidone-Iodine Wash Solution (5 %)
Prazosin Tablets (5 mg)
Prednisolone Tablets (20 mg)
Prednisone Tablets (10 mg)
Probenecid Tablets (500 mg)
Procain Penicillin Injectable
Suspension (300 mg/ml)
Propanidide Injectable Solution
(50 mg/ml)
Propanolol Spheronized Pellets for
Sustained Release Coating
(20 % and 30 %)
Propranolol Sustained Release Tablets
(160 mg)
Propranolol Tablet Cores (40 mg)
Propranolol Tablets
(10 mg, 50 mg and 100 mg)
Protective Film Coating with Ethyl
Cellulose + Kollidon VA 64
Protective Film Coating with Hydroxypropyl Cellulose + Kollidon VA 64
Protective Film Coating with
Hypromellose + Kollidon VA 64
Protective Film Coating with
Kollidon VA 64
Protective Film Coating with Polyvinyl
Alcohol + Kollidon VA 64
Protective Film Coating with Shellac +
Kollidon 30
Pseudoephedrine Tablets (60 mg)
Pyrazinamide Tablets (500 mg), DC
Pyrazinamide Tablets (500 mg), WG
Pyridoxin see Vitamin B6
R
Ranitidine Tablet Cores (150 mg)
Ranitidine Tablet Cores (300 mg)
Rifampicin Tablets (450 mg)

S
Saccharin Effervescent Tablets (15 mg)
Saccharin Tablets (15 mg)
Selegiline Tablets (5 mg)
Serratio Peptidase Tablets (10 mg)
Silimarin Tablets (35 mg)
Simethicone Chewable Tablets (70 mg)
Simethicone Chewable Tablets (80 mg)
Simethicone Instant Granules
(60 mg and 120 mg)
Sobrerol Injectable Solution
(75 mg/5 ml)
Sodium Fluoride Tablets (0.5 mg)
Sodium Fluoride Tablets (1.3 mg)
Spironolactone Tablets (25 mg)
Spirulina Extract Chewable Tablets
(250 mg)
Subcoating for Core Protection
Sucralfate + Sodium Alginate Tablets
(500 mg + 20 mg)
Sugar Coating, automatic
Sugar Coating, manual
Sugar Film Coating
Sulfadiazin Tablets (450 mg)
Sulfadiazine + Trimethoprim Veterinary
Concentrated Oral Suspension
(40 % + 8 %)
Sulfadimethoxine Veterinary Injectable
Solution (2.5 % = 250 mg/10 ml)
Sulfadimidine Tablets (500 mg)
Sulfadoxine + Pyrimethamine Tablets
(500 mg + 25 mg)
Sulfadoxine + Trimethoprim Veterinary
Injectable Solution (1000 mg +
200 mg/10 ml)
Sulfadoxine Solution (2 % = 20 mg/ml)
Sulfamethoxazol + Trimethoprim Dry
Syrup (400 mg + 80 g/10 ml)
Sulfamethoxazole + Trimethoprim Oral
Suspension (400 mg + 80 mg/5 ml)
Sulfamethoxazole + Trimethoprim
Tablets (400 mg + 80 mg)
Sulfamoxole + Trimethoprim Veterinary
Injectable Solution
(400 mg + 80 mg/10 ml)
Sulfathiazole Tablets (250 mg)

BASF Pharma Ingredients Generic Drug Formulations 2001

Sulfathiazole Veterinary Injectable and
Oral Solutions (0.8 % = 8 mg/ml)
Sustained Release Coating of Caffeine
Pellets
Sustained Release Coating of
Diclofenac Pellets
Sustained Release Coating of
Propanolol Pellets I
Sustained Release Coating of
Propanolol Pellets II
Sustained Release Coating of
Theophylline Pellets
Sustained Release Coating of
Verapamil Pellets
T
Tannin-Crospovidone Complex Tablets
(55 mg + 230 mg)
Terazosin Tablets (1 mg and 5 mg)
Terfenadine Suspension
(1.2 % = 60 mg/5 ml)
Terfenadine Tablets (60 mg)
Tetracycline Tablets (125 mg)
Tetracycline Tablets (250 mg)
Tetrazepam Tablets (50 mg)
Theophylline Injectable Solution
(4 % = 200 mg/5 ml)
Theophylline Sustained Release
Tablets (400 mg), WG
Theophylline Sustained Release
Tablets (500 mg) DC
Theophylline Tablets (100 mg)
Thiamine see Vitamin B1
Tramadol Sustained Release Tablets
(100 mg)
Tretinoin + Alpha Bisabolol Gel
(50 mg + 100 mg/100 g)
Tretinoin + Dexpanthenol Gel
(50 mg + 2,500 mg/100 g)
Tretinoin Cream (50 mg/100 g)
Tretinoin Gel (50 mg/100 g)
Tretinoin Solution (50 mg/100 g)
Triamcinolone Tablets (4 mg)
Trifluoperazine Tablets (5 mg)
Trihexylphenidyl see Benzhexol

BASF Pharma Ingredients Generic Drug Formulations 2001

U
Ultrasonic Adhesive Gel
V
Valeriana Extract + Passiflora Extract
Tablet Cores (44 mg + 30 mg)
Valproate Sodium Tablets (500 mg)
Verapamil Spheronized Pellets for
Sustained Release Coating (48 %)
Verapamil Sustained Release Tablets
(220 mg)
Verapamil Tablets (120 mg), DC
Verapamil Tablets (120 mg), WG
Vitamin A + Vitamin B6 + Vitamin E
Tablets
(40,000 i. u. + 40 mg + 35 mg)
Vitamin A + Vitamin C + Vitamin E
Tablets
(1,200 i. u. + 60 mg + 30 mg)
Vitamin A + Vitamin D3 + Calcium +
Magnesium Injectable Solution
(33,000 i.u. + 6,000 i. u. + 100 mg +
200 mg/g i.u.)
Vitamin A + Vitamin D3 + Vitamin C
Chewable Tablets for Children
(2,000 i. u. + 200 i. u. + 30 mg)
Vitamin A + Vitamin D3 + Vitamin E +
Beta Carotene Veterinary Injectable
Solution (100,000 i.u. + 20,000 i.u.
+ 10 mg + 8 mg/g)
Vitamin A + Vitamin D3 + Vitamin E
Aqueous Injectable Emulsion for
Cattles (500,000 i.u. + 75,000 i.u. +
50 mg/ml with Cremophor EL)
Vitamin A + Vitamin D3 + Vitamin E
Aqueous Injectable Emulsion for
Cattles (500,000 i.u. + 75,000 i.u. +
50 mg/ml with Solutol HS 15)
Vitamin A + Vitamin D3 + Vitamin E
Concentrates, Water-miscible
(120,000 i.u. + 60,000 i.u. +
40 mg/ml)

Vitamin A + Vitamin D3 + Vitamin E
Injectable Solution in Organic
Solvents for Cattles (500,000 i.u. +
75,000 i.u. + 50 mg/ml)
Vitamin A + Vitamin D3 Concentrate,
Water-miscible
(120,000 i.u. A + 12,000 i.u. D/g)
(100,000 i.u./A + 20,000 i.u./D3/ml)
Vitamin A + Vitamin D3 Drops
(30,000 i.u. + 3,000 i.u./g)
Vitamin A + Vitamin D3 Injectable
Solutions (30,000 i.u. A
+ 5,000 or 10,000 i.u. D3/ml)
Vitamin A + Vitamin D3 Syrup
(30,000 i.u. + 10,000 i.u. /ml)
Vitamin A + Vitamin E Drops
(25,000 i. u. + 50 mg/ml)
Vitamin A + Vitamin E Injectable Solution for Sheeps (250,000 i.u. +
25 mg/ml)
Vitamin A + Vitamin E Tablets
(33,000 i. u. + 70 mg)
Vitamin A Chewable Tablets
(100,000 i. u.)
Vitamin A Concentrate, Water-miscible
(100,000 i. u./ml)
Vitamin A Drops (50,000 i. u./ml)
Vitamin A Suppositories (150,000 i.u.)
Vitamin A Tablet Cores (50,000 i. u.)
Vitamin A Tablets (25,000 i. u.)
Vitamin A Tablets (50,000 i. u.)
Vitamin B Complex + Amino Acid +
Magnesium Effervescent Granules
(Sugar-free)
Vitamin B Complex + Carnitine Tablet
Cores
Vitamin B Complex + Minerals +
Linoleic/Linolenic Acid Syrup
Vitamin B Complex + Vitamin C
+ Calcium Effervescent Tablets
Vitamin B Complex + Vitamin C
+ Ferrous Sulfate Tablets
Vitamin B Complex + Vitamin C
Effervescent Tablets
Vitamin B Complex + Vitamin C Instant
Granules (2 RDA of Vitamins)

Vitamin B Complex + Vitamin C
Syrup, I (2 – 3 RDA/10 g)
Vitamin B Complex + Vitamin C
Syrup, II
Vitamin B Complex + Vitamin C Tablets
Vitamin B Complex Injectable Solution
Vitamin B Complex Syrup
Vitamin B Complex Tablets, I
Vitamin B Complex Tablets, II
Vitamin B Complex Tablets, III
Vitamin B Complex Tablets, IV
Vitamin B1 (Thiamine) Tablets
(50 mg), I
Vitamin B1 (Thiamine) Tablets
(50 mg), II
Vitamin B1 (Thiamine) Tablets
(100 mg), DC
Vitamin B1 (Thiamine) Tablets
(100 mg), WG
Vitamin B1 + Caffeine Tablets
(500 mg + 100 mg)
Vitamin B1 + Vitamin B2 + Vitamin B3
+ Vitamin B6 Injectable Solution
(100 mg + 6 mg + 40 mg + 4 mg/2 ml)
Vitamin B1 + Vitamin B6 + Vitamin B12
Tablets (100 mg + 200 mg + 100 µg)
Vitamin B1 + Vitamin B6 + Vitamin B12
Tablets (100 mg + 10 mg + 100 µg)
Vitamin B12 (Cyanocobalamin)
Tablets, Coloured (50 µg)
Vitamin B2 (Riboflavin) Tablets (3 mg)
Vitamin B2 (Riboflavin) Tablets (10 mg)
Vitamin B2 (Riboflavin) Tablets (75 mg)
Vitamin B2 (Riboflavin) Tablets (100 mg)
Vitamin B3 (Nicotinamide) Tablets
(300 mg)
Vitamin B5 (Calcium D-Pantothenate)
Tablets (100 mg)
Vitamin B5 (Calcium D-Pantothenate)
Tablets (300 mg)
Vitamin B6 (Pyridoxine) Tablets
(40 mg), DC
Vitamin B6 (Pyridoxine) Tablets
(40 mg), WG
Vitamin B6 (Pyridoxine) Tablets
(100 mg)

BASF Pharma Ingredients Generic Drug Formulations 2001

Vitamin B6 (Pyridoxine) Tablets
(250 mg)
Vitamin C + Calcium Carbonate Effervescent Tablets (500 mg + 300 mg)
Vitamin C + Vitamin E Chewable
Tablets or Lozenges
(500 mg + 20 mg)
Vitamin C + Vitamin E Lozenges
(100 mg + 50 mg)
Vitamin C (Ascorbic acid) Chewable
Tablets (100 mg, 500 mg, 1,000 mg)
Vitamin C (Ascorbic Acid + Ascorbate)
Chewable Tablets (500 mg)
Vitamin C (Ascorbic acid) Chewable
Tablets with Dextrose (100 mg)
Vitamin C (Ascorbic Acid) Chewable
Tablets with Fructose (120 mg)
Vitamin C (Ascorbic acid) Chewable
Tablets with Sucrose (500 mg)
Vitamin C (Ascorbic acid) Effervescent
Tablets (100 mg and 1000 mg)
Vitamin C (Ascorbic Acid) Effervescent
Tablets (500 mg)
Vitamin C (Ascorbic Acid + Ascorbate)
Lozenges
(250 mg and 500 mg)
Vitamin C (Ascorbic Acid) Tablets
(100 mg)
Vitamin C (Ascorbic Acid) Tablets
(200 mg)
Vitamin E + Selenium Veterinary
Injectable Solution
(60 mg E + 3 mg Se/ml)
Vitamin E Chewable Tablets (100 mg), I
Vitamin E Chewable Tablets (100 mg), II
Vitamin E Chewable Tablets (150 mg)
Vitamin E Chewable Tablets (200 mg)
Vitamin E Chewable Tablets (400 mg)
Vitamin E Concentrate, Water-miscible
(10 % = 100 mg/ml)
Vitamin E Gel-Cream (10 %)
Vitamin E Tablets (50 mg)
Vitamin K1 (= Phytomenadione)
Injectable Solution
(10 mg and 20 mg/ml)

BASF Pharma Ingredients Generic Drug Formulations 2001

Chapter 2.4). Most of the vitamins used and many of the excipients are from the BASF range. propranolol. scale-up for production must therefore be checked and revised. It is only in very exceptional cases that the formulations have been optimized by a systematic study involving a comparison between different excipients or by varying the amounts of excipients. as necessary. ephedrine.4 Active substances The active substances are almost exclusively generic. caffeine.1. theophylline. the formulations are merely suggestions that require further optimization. Thus.3 Size and optimization of the formulations All the formulations were developed exclusively on a laboratory scale of the order of 1 kg maximum . ibuprofen. The reason for this is that the difference in physical properties may exert a strong effect particularly on solid drugs (cf. tretinoin and verapamil. norephedrine. 1. Significant differences in the properties of the preparations may occur if the same active substance is used.g. fluoxetin. it unfortunately cannot be listed here. but has a different grain size or originates from another manufacturer. They were mostly supplied free of charge as samples by pharmaceutical companies. prazosin. Since the manufacturer's name was mostly not mentioned. BASF Pharma Ingredients Generic Drug Formulations 2001 . selegiline. PVP-iodine. e. For this reason. crospovidone M. oxymetazoline. pancreatin.

capsules and granules. oral solubilizers. Kollidon CL-M Micronized crospovidone as a stabilizer for oral and topical suspensions and for improving the release of active substances from tablets. Excipient Description Kollidon® grades The Kollidon grades are soluble and/or insoluble polyvinylpyrrolidones of various molecular weights and particle sizes and a vinylpyrrolidone/vinyl acetate copolymer 6+4. BASF Pharma Ingredients Generic Drug Formulations 2001 . The corresponding pharmacopoeial names are Povidone. film-formers.Kollidon 30 Povidone of medium molecular weight (M w 28000 – 34000 and 44000 – 54000). enzyme stabilizers. dispersants for pigments. Kollidon 17 PF Low-molecular-weight povidone (M w 2000 – 3000 and 7000 –11000) of pyrogen-free quality for use as solubilizer. The following list gives a brief description of the functions of the individual excipients in the BASF range. Crospovidone and Copovidone Kollidon 12 PF.5 BASF excipients and their functions = [1] The range of BASF excipients for the pharmaceutical industry contains more than 50 different pharmacopoeiagrade sales products that are used in practically all dosage forms. Kollidon 90 F High-molecular-weight povidone (M w 1000000 – 1500000) as a highly effective binder. capsules. Examples of use are binders in tablets. Kollidon CL Crospovidone for use as tablet disintegrant and for improving the release of active substances from tablets. and hydrophilizer and pore former in medicinal plastic materials. stabilizer for oral and topical suspensions. Kollidon 25. and bioavailability enhancers. thickener. crystallization inhibitor. suspension stabilizer and lyophilization agent in injections and ophthalmic preparations. capsules and granules.1. stabilizers in oral suspensions. and granules.

.Excipient Description Kollidon VA 64 Copovidone for use as a dry binder in tablets. Eur. BASF Pharma Ingredients Generic Drug Formulations 2001 . JPE) for the sustained release coating of pellets and for sustained release matrix tablets.Eur. Kollicoat EMM30D Ethyl acrylate/Methyl methacrylate copolymer (2+1) in the form of a 30 % aqueous dispersion (Ph. film-former in topical sprays. and as a binder in wet granulation.) for enteric coatings on tablets and capsules Kollicoat MAE100P Methacrylic acid/ethyl acrylate copolymer (1+1) in powder form for the suspension in water to prepare enteric coatings on tablets and capsules. and Kollidon CL for use as an all-purpose direct compression excipient that fulfills the functions of filler. capsules and granules. Kollidon SR Research product: Physical mixture of 80 % polyvinyl acetate and 20 % povidone (Kollidon 30) as matrix former for the direct compression of sustained release tablets. Kollicoat SR30D Polyvinyl acetate in form of a 30 % aqueous dispersion stabilized with povidone and sodium lauryl sulfate for the sustained release coating of pellets and for sustained release matrix tablets. chewable and effervescent tablets Kollicoat® MAE30DP Methacrylic acid/ethyl acrylate copolymer (1+1) in the form of a 30 % aqueous dispersion (USP. and flow improver. Ludipress is suitable for active substances and vitamins in all dosage forms Ludipress LCE Direct compression granules consisting of lactose monohydrate and Kollidon 30 for lozenges. disintegrant. Ludipress® Custom-produced granules consisting of lactose monohydrate. Ph. binder. Kollidon 30. film-former in tablet coatings and subcoatings.

Cremophor EL is used to solubilize vitamins. though water-in-oil preparations are also feasible Macrogol-25-cetostearyl ether (PhEur) prepared by ethoxylation of 1 mole of cetostearyl alcohol with 25 moles of ethylene oxide. HLB value 15 –17. HLB value 10 –12. and essential oils in water or mixtures of water and alcohol. The product also contains some free fatty alcohol. topical and parenteral preparations. and other hydrophobic substances Cremophor ELP Purified Cremophor ELP for injectables Solutol HS 15 Macrogol-15 hydroxystearate produced by reacting 15 moles of ethylene oxide with 1 mole of 12-hydroxystearic acid. Nonionic solubilizer in paste form for use in human and veterinary injections Cremophor grades as emulsifiers Cremophor A 6 Cremophor A 25 Macrogol-6-cetostearyl ether (Ph. Cremophor RH 40 is used to solubilize vitamins. Nonionic solubilizer and emulsifier in liquid form for oral.Excipient Cremophor® grades and Solutol® HS 15 as solubilizers Cremophor RH 40 Description Polyoxyl 40 Hydrogenated Castor Oil (PhEur/USP-NF) produced by ethoxylation of hydrogenated castor oil.Eur.) produced by ethoxylation of 1 mole of cetostearyl alcohol with 6 moles of ethylene oxide. Nonionic solubilizer and emulsifier for oral and topical preparations. Cremophor A 6 is intended for the production of ointments and creams mainly in the form of oil-in-water emulsions. water-insoluble active substances. It features a very faint taste and odour in aqueous solution. Cremophor A 25 is intended for the production of ointments and creams based on oil-in-water emulsions BASF Pharma Ingredients Generic Drug Formulations 2001 . water-insoluble active substances. Cremophor EL Poloxyl 35 Castor Oil (PhEur/USP-NF) produced by ethoxylation of castor oil. and to improve bioavailability in solid dosage forms.

thickener and solubilizer in buccal and topical solutions and as a stabilizer in topical suspensions BASF Pharma Ingredients Generic Drug Formulations 2001 . solubilizer. It has an average molecular weight of 8600. as a plasticizer.g. It allows more rapid absorption of active substances on topical application 1.Eur. They are widely used in the production of pharmaceuticals and are therefore marketed in pharmaceutical quality under the tradename Lutrol F Lutrol F 68 Poloxamer 188 (DAC.) as solvent for human and veterinary oral. topical and parenteral dosage forms. USP-NF) is a block polymer consisting of 73 % of polyethylene glycol and 27 % polypropylene glycol with an average molecular weight of 12000. The main applications for Lutrol F 127 are as a gel former. USP-NF) is a block polymer consisting of 81% of polyethylene glycol and 19 % of polypropylene glycol. and for enhancing the bioavailability in solid preparations Lutrol F 127 Poloxamer 407 (DAC. Macrogol (PhEur) and polyethylene glycol (USP-NF) Lutrol E 600 of average molecular weight (300. Lutrol E 400. Ph.2-Propylene glycol (USP. topical and parenteral preparations Lutrol F grades The two Lutrol F grades are poloxamers in an extensive line of block polymers. topical and parenteral drugs The Lutrol E grades are liquid polyethylene glycols (macrogol) of various molecular weights with different fields of application Lutrol E 300. e. 400 and 600). and suspension stabilizer in liquid oral.Excipient Soluphor® P and other solvents Soluphor P Propylene Glycol Lutrol® E grades Description 2-Pyrrolidone as solvent for veterinary injections. Pluronic ® products. Lutrol F 68 is primarily intended as an emulsifier. The main application is as solvents for oral.

3 Azorubine 85 E 122 Amaranth 85 E 123 Patent Blue 80 E 131 FD & C Blue No.Excipient Description Sicovit® colorants The Sicovit colorants (formerly Sicopharm) are divided into two separate product lines: dyes and pigments. 1 Indigotin 85 E 132 Brilliant Black 80 E 151 Sicovit pigments Iron oxide Yellow 10 E 172 Iron oxide Red 30 E 172 Iron oxide Brown 70 E 172 Iron oxide Brown 75 E 172 Iron oxide Black 80 E 172 Iron oxide Black 85 E 172 Titanium dioxide White P 77891 A BASF Pharma Ingredients Generic Drug Formulations 2001 . 10 Cochineal Red 70 E 124 Erythrosine 85 E 127 FD & C Red No. They conform to the EEC and FAO Directives and are therefore used in various dosage forms Sicovit dyes Quinoline Yellow 70 E 104 Tartrazine 85 E 102 Sunset Yellow 85 E 110 D&C Yellow No.

MO 63134. powder [7] Mallincrodt Inc. Rue Pierre Pays B. Germany Sorbitol. crystalline Talc Stearic acid [10] BASF Pharma Ingredients Generic Drug Formulations 2001 .6 Excipients from other suppliers Supplier and address Excipients [2] Bärlocher GmbH 80992 Munich.1. Box 5439 675 McDonnel Boulevard St. Germany Polyethylene glycol 6000. P. USA Stearic acid [8] Meggle Milchindustrie GmbH Postfach 40 83512 Wasserburg. Germany Calcium arachinate Magnesium stearate [3] Cerestar GmbH Düsseldorferstrasse 191 47809 Krefeld. USA Avicel ® products Ac-Di-Sol ® [6] Hüls AG Postfach 45674 Marl. Germany Lactose Monohydrate D 20 Tablettose ® [9] Rhône-Poulenc 15. Food + Pharmaceutical Products 735 Market Street Philadelphia. CaHPO 4 (= DI-TAB ® ) Riedel-de-Haen AG Wunstdorferstrasse 40 30926 Seelze. 52 69660 Collonges-au Mont d'Or. Louis. Germany Potato starch Corn starch [4] Degussa AG GB Industry + Fine Chemicals Postfach 1345 63457 Hanau. Germany Aerosil ® 200 [5] FMC Corp. France Dicalcium phosphate.P.O. PA 19103.

The reasons are as follows. or a stress test lasting one year or more. Thus the final formulation must always be checked by the producer. BASF Pharma Ingredients Generic Drug Formulations 2001 . The formulations are practically always modified to meet the requirements of industrial-scale production. Physical stability data are also given for a number of the formulations. and b. c.g. The stability of the preparation may change as a result of points a. Chemical stability data are often available for sensitive materials.1. a. It is not possible for us to determine the long-term stabilities of the large number of formulations presented here. They mostly determined from either storage at room temperature (20 – 25 °C) over a period of one year. Aromas and colorants are often added to the formulations in amounts depending on the particular taste of the target group. PVP-iodine or vitamins.7 Stability data It is only in exceptional cases or when certain groups of active substances are present that data are given on the chemical and/or the physical stability of the formulations. e. b.

Even substances such as ascorbic acid that are hardly suitable for direct compression.2 Direct compression The technology involved in direct compression assumes great importance in the tablet formulations.g. Plasticity. or starch.g. Two important alternatives. e. Ludipress grades and Kollidon VA 64. The beneficial properties of Kollidon VA 64 can BASF Pharma Ingredients Generic Drug Formulations 2001 . and a disintegrant. can be found in the BASF line of pharmaceutical excipients for direct compression. Ludipress grades Ludipress is a speciality derived from lactose. This limit may be shifted upwards by special direct compression auxiliaries. in particular. many analgetics. Chapter 2. particularly in the production of generics. viz. 2. and Kollidon CL. can normally be directly pressed into tablets at concentrations of 30 – 40 %. e. 1. this technique is not as suitable if the content of ascorbic acid is higher. By virtue of its versatility. the amounts weighed out in the formulations correspond to the amount in the tablets multiplied by a factor of 1. Ludipress. behave very differently with Ludipress when the dosage is extremely high. Kollidon 30. B. that the active substance permits. this property of Kollidon VA 64 is not adversely effected by increasing the pressure. Acetylsalicylic acid and metamizole can be pressed when little Ludipress has been added. microcrystalline cellulose. It thus combines the properties of a filler. and the fraction of Ludipress required in the tablets is too large for paracetamol (= acetaminophen). calcium phosphate. lactose. No other dry binder has a binding power and plasticity comparable to those of Kollidon VA 64.1 Size of formulations The formulations were developed on a laboratory scale in which case 200 –1. because it is often the cheapest means. This combination even allows 500 mg of paracetamol to be pressed into good tablets with a weight of 700 mg. It can also be combined with almost all active substances with the exception of those that enter into a chemical interaction with lactose (Maillard reaction).g. Normally.000. binder. The limiting factors are the physical properties of the active substance and its concentration in the tablets (cf. Active substances. e. Kollidon CL. However. ibuprofen requires a larger amount. and flow agent and also often acts as a release accelerator. e. disintegrant.g. Kollidon VA 64 An alternative to the Ludipress grades is the outstanding dry binder Kollidon VA 64 together with excipients. is an important parameter in direct compression. As can be seen in Fig. formulations containing it are usually very simple. owing to the friability of their crystals.2 Tablets obtained by direct compression 2. A.4).000 g of the mixtures to be tabletted were used.

5 % binder + 0.5 0. Kollidon VA 64 and Ludipress can also be combined with one another.4 Kollidon VA 64 Kollidon 30 Mc.5 Effect of the physical properties of the excipients Characterization of the physical properties of excipients is also important because the influences can be similar as mentioned for active ingredients. BASF Pharma Ingredients Generic Drug Formulations 2001 Fig.9 0. Cellulose HPMC 11000 Plasticity = plastic energy/total energy Fig.Eur.7 0. This particularly concerns the particle size and the flowability. 1 Plasticity of dry binders in tablets (99.Plasticity 1. but when the active substance consists of crystals of two different sizes (crystalline = > 150 µm. 2.4 Effect of the physical properties of the active substance In the manufacture of tablets it is important to define and appreciate the physical properties of the active substance. Obviously.5 % magnesium stearate) also be exploited for the production of concentrated active substance that is subsequently used for direct tabletting.0 Force: 18 kN Force: 25 kN 0. 2. powder = < 150 µm).3 Tablet press All the formulations were devised on rotary tabletting presses that were fitted with 10 – 20 punches. disintegration.8 0. 2 shows the difference that can occur when ascorbic acid tablets of the same composition are produced at the same pressure. or USP. dissolution) are contained the Pharmacopoeiae Ph. the disintegration time is measured in . friability.6 0. 2.6 Methods of measuring the properties of tablets The general instructions for the determination of the corresponding properties of tablets (hardness. If it is not stated to the contrary. 2.

BASF Pharma Ingredients Generic Drug Formulations 2001 . The dissolution is determined by the conditions laid down in the corresponding monographs for the tablets (usually USP) and in the prescribed medium. 5 % Kollidon VA 64) artificial gastric juice.Tablet Hardness (N) 140 120 100 80 60 40 crystalline grade Compression force: 25 kN powder grade Fig. 2. This is particularly the case when the active substance is sufficiently soluble or when the formulation was developed in a time when this parameter was not yet demanded. these data cannot be given for all formulations. 2.8 Formulations The formulations in this chapter have been arranged in the alphabetic order of their active substances. Unfortunately.7 Information on dissolution of active substance Nowadays it is standard practice and/or laid down that the in-vitro release of active substance be checked. 2 Direct compression of different types of ascorbic acid (40 % ascorbic acid.

........ powder [6]..............................97 N Disintegration................20 mm Form ....1% BASF Pharma Ingredients Generic Drug Formulations 2001 ..........450 g Tartaric acid..............400 g Sodium bicarbonate ...... 2.......biplanar Hardness..... crystalline (Merck)... pass through a sieve and press with medium compression force at a maximum of 30 % of relative atmospheric humidity..........1........ Manufacturing (Dir ect compression) Mix all components.....................1975 mg Diameter ......................................................................................... 3...................75 g Apartame (Searle) .......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Acetylcysteine Effervescent Tablets (600 mg) Formulation Acetylcysteine........................q................................................. Tablet properties Weight.... powder .........s..................................................600 g Ludipress LCE [1] ..........................................2 – 3 min Friability ........................................2.350 g Polyethylene glycol 6000........25 g Orange flavour (Dragoco) .

....................................5 g g g g g g g 2............................30 Stearic acid [7] .....20 Polyethylene glycol 6000..........400 Paracetamol.....100 Caffeine (BASF) ..........................................................30 Ludipress [1] .................0........................... 3...2...................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Acetylsalicylic Acid + Paracetamol (= Acetaminophen) + Caffeine Tablets (400 mg + 100 mg + 30 mg) Formulation Acetylsalicylic acid. crystalline ................................................................... Manufacturing (Dir ect compression) Mix all components...........116 N Disintegration................3 % BASF Pharma Ingredients Generic Drug Formulations 2001 ....... Tablet properties Weight .............1 – 2 min Friability.............biplanar Hardness ... crystalline (BASF) .....683 mg Diameter ................................................... pass through a sieve and press with low compression force........................... powder [6].....12 mm Form ................................100 Kollidon CL [1] .................................

. Tablet properties Weight .......0...........250 Paracetamol...biplanar Hardness................................ Manufacturing (Dir ect compression) Pass all components through a 0.....................01% 6 Months 12 Months 100 % 100 % 100 % 96 % < 0...........2.....................................90 N Disintegration .......01% < 0..............................25 g g g g g 2.......8 mm sieve..605 mg Diameter ...01% BASF Pharma Ingredients Generic Drug Formulations 2001 ...15 Kollidon CL [1] ............7 % 4.01% < 0...................................< 1 min Friability................. 2 (20–25 °C.......250 Avicel PH 101 [5] ....... Chemical stability of formulation No................................. crystalline (Merck) ...60 Kollidon 30 (or Kollidon VA 64) [1] .....12 mm Form ...........................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Acetylsalicylic Acid + Paracetamol (= Acetaminophen) Tablets (250 mg + 250 mg) Formulation Acetylsalicylic acid.............................. crystalline (BASF) . closed) 0 Months Acetylsalicylic acid Vitamin C Free acetic acid Free salicylic acid 100 % 100 % < 0...... 3.. mix and press with medium compression force.............................................................

.............250 Ludipress LCE [1] ............................... Tablet properties No.........................2........................ 1 No..400 Ascorbic acid...........................................600 Ctitric acid......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Acetylsalicylic Acid + Vitamin C Effervescent Tablets (400 mg + 250 mg) 1..................... 1 Acetylsalicylic acid (Synopharm) .......................................................biplanar biplanar Hardness...........................1 min 35 sec 1 min 22 sec Friability ...............66 % 0.................white white BASF Pharma Ingredients Generic Drug Formulations 2001 ............ 3................. Manufacturing (Dir ect compression) Pass all components through a 0..........20 mm 20 mm Form ...................... crystalline (BASF) ..300 Sodium bicarbonate ........... crystalline ............145 N 125 N Disintegration ........ Formulations No.................... 2 400 250 500 400 600 90 g g g g g g 2.........8 mm sieve.........0............................. 2 Weight ..........................600 Lutrol E4000F [1]...........2251 mg 2244 g Diameter .............90 g g g g g g No................................. mix and press with high compression force..............................86 % Colour ..................

. Manufacturing (Dir ect compression) Pass all components through a 0................................................................. 2 325 g 250 g – 100 g 12 g 30 g 3g 2. 3................. powder (BASF).2 g g g g g g g No.....................2 min Friability ........................ crystalline [10] ............................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Acetylsalicylic Acid + Vitamin C Tablets (325 mg + 250 mg) 1............120 Avicel PH 101 [5] .....325 Ascorbic acid................ 1 Acetylsalicylic acid.........................1% 726 mg 12 mm biplanar 100 N < 1 min 1% BASF Pharma Ingredients Generic Drug Formulations 2001 .................40 Kollidon VA 64 [1] .250 Sorbitol......8 mm sieve. 2 Weight ..........................................2.............. Tablet properties No..................biplanar Hardness .................... 1 No.................92 N Disintegration .......................20 Magnesium stearate [2] ............................... crystalline (Merck) .....790 mg Diameter ........................................... Formulations No............25 Kollidon CL [1] .....................................................12 mm Form ................................................ mix and press with medium/high compression force......

2 (20–25 °C) 0 Months Acetylsalicylic acid Vitamin C Free acetic acid Free salicylic acid 100 % 100 % < 0.01% < 0.Acetylsalicylic Acid + itamin V CT ablets (325 mg + 250 mg) 4. Chemical stability of formulation No.01% < 0.01% BASF Pharma Ingredients Generic Drug Formulations 2001 6 Months 12 Months 100 % 100 % 100 % 96 % < 0.01% page 2 .

.. Tablet properties Weight . Manufacturing (Dir ect compression) Pass all components through a 0.... crystalline (Merck) ........................................ 3...3 g g g g g 2...0......120 N Disintegration .................841 mg Diameter ........................20 Macrogol 6000 powder [6] ......100 Kollidon CL [1] ...............................................8 mm sieve.................................... Formulation Acetylsalicylic acid...........biplanar Hardness ......................01% Free salicylic acid ..........................12 mm Form ......................<1 min Friability..................... mix and press with medium compression force..............<0.................2........................................................0............................................1% Colour ....400 Ascorbic acid......white BASF Pharma Ingredients Generic Drug Formulations 2001 ...........4 % Free acetic acid .....................................................................250 Ludipress [1] .......................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Acetylsalicylic Acid + Vitamin C Tablets (400 mg + 250 mg) 1....... powder (BASF) ..

..Acetylsalicylic Acid + itamin V CT ablets (400 mg + 250 mg) 4........................130 N Disintegration .......................................................<0......................................0...........................1% Colour of the tablets ...............white BASF Pharma Ingredients Generic Drug Formulations 2001 page 2 ............0.................................... closed) Hardness ......................................8 % Acetylsalicylic acid ..........01% Free salicylic acid ............................ Stability after 12 months (20–25 °C....100 % Free acetic acid .............................<1 min Friability....100 % Ascorbic acid ....

.............................biplanar Hardness..............................0 % 100..... Tablet properties Weight ...........................................99 Stearic acid [7] .....2...............................8 mm sieve and press with low compression force.......4 % Dissolution....................84 % 30 min ....................................... 3............0 % The content of free salicylic acid remained always below 0............................<1 min Friability......... 15 min....................4 % 100..................2 %................15 g g g g 2........0 % 98...........................516 mg Diameter ......0 % 100................... BASF Pharma Ingredients Generic Drug Formulations 2001 ...400 Ludipress [1] ................... pass through a 0......................90 N Disintegration .......0 % 100... Formulation Acetylsalicylic acid.... Manufacturing (Dir ect compression) Mix all components.......0....... crystalline (Merck) .............. Chemical stability Storage time RT 40 °C 0 months 6 months 12 months 100..............12 mm Form ..8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Acetylsalicylic Acid Tablets (400 mg) 1.........97 % 4...............1 Kollidon CL [1]...................

..... mix and press with low compression force....................................12 mm Form ................7 % BASF Pharma Ingredients Generic Drug Formulations 2001 ....707 mg Diameter ............................................ Manufacturing (Dir ect compression) Pass all components through a 0..........................8 mm sieve.........................25 Magnesium stearate [2] ....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Acetylsalicylic Acid Tablets (500 mg) 1..............................................3 g g g g g 2..................................................... 3..15 Kollidon CL [1] ..................... Formulation Acetylsalicylic acid (Merck) ............0.<1 min Friability............200 Kollidon 30 [1] ..................500 Avicel PH 101 [5] .................... Tablet properties Weight .................................61 N Disintegration ............................................................................biplanar Hardness.................2..

........1% BASF Pharma Ingredients Generic Drug Formulations 2001 ................................ Formulation Albendazole ..............................................................................................288 Magnesium stearate [2] ..........................2 min Friability ... Manufacturing (Dir ect compression) Mix all components....................................4 Aerosil 200 [4] ..................8 mm sieve and press with low compression force......................................................biplanar Hardness..............100 Ludipress [1] ...... pass through a 0........................... (100 mg) 1....................8 g g g g 2..99 N Disintegration .............. 3...... Tablet properties Weight ........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Albendazole Tablets.12 mm Form ...............................................................0.....2.......400 mg Diameter ...................

............... crystalline [10] ...............5 g g g g g g g g g g 2...2.........................biplanar Hardness ..900 Kollidon VA 64 [1] .500 Aluminium hydroxide dried gel (Giulini) ..............................................................................................170 Sorbitol.......8 mm sieve.....50 Vanillin ..........................................627 Ludipress [1] ........................................ 3.........1. Formulation Alginic acid ........................70 Magnesium stearate [2].......... mix and press with high compression force..........160 Sucrose.....2...20 mm Form ................3 % BASF Pharma Ingredients Generic Drug Formulations 2001 .............. Manufacturing (Dir ect compression) Pass all components through a 0.................................120 N Friability.........................................................................100 Magnesium trisilicate ...... crystalline ......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Alginic Acid + Aluminium Hydroxide + Magnesium Silicate Tablets (500 mg + 100 mg + 25 mg) 1....................................................... Tablet properties Weight ....25 Sodium bicarbonate...................................................55 g Diameter ....................................

..........................................98 % 4.......... Manufacturing (Dir ect compression) Mix all components. DC 1...................11 mm Form .................................5 % Dissolution (10 min) .............................6 min Friability....... Tablet properties Weight ................... pass through a 0................91% (20 min) ..........................620 mg Hardness ......620 mg Diameter ................... 3.....biconvex Hardness ................91% (20 min).............................. 20–25 ºC) Weight .........................100 % BASF Pharma Ingredients Generic Drug Formulations 2001 .................................350 g Stearic acid [7] ............................................123 N Disintegration ...................8 mm sieve and press with low compression force.................................... Formulation Alpha-Methyldopa .......15 g 2..............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Alpha-Methyldopa Tablet Cores (250 mg)...........................................2.................................................................................7 min Friability...........................115 N Disintegration ................2 % Dissolution (10 min) ................................... Physical stability (20 months.......0.....................................0....................250 g Ludipress [1] ..........................

........................................................4 % Dissolution. 3...<1 min Friability .........................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Alpha-Methyldopa Tablets (500 mg)....................... 1 No.86 % 16 min .........12 mm Form ......– 500 g 200 30 20 8 1 g g g g g – 1g 2............. DC 1... 2 Weight ........................................................ 1) and low compression force (Formulation No........................20 g Kollidon CL [1] ......7 g Magnesium stearate [2] ................................................ 2)......................500 g (Alpha Chemicals) Avicel PH 101 [5] ............... mix and press with high compression force (Formulation No......... 1 No.........................................................biplanar Hardness ..............54 g Kollidon VA 64 [1] .................5 mm sieve.............. Tablet properties No.......80 N Disintegration . Formulations No......................................... Manufacturing (Dir ect compression) Pass magnesium stearate trough a 0..................2 g Calcium arachinate [2] ........................693 mg Diameter .....................2.... 2 Alpha-Methyldopa ..................90 g Aerosil 200 [4]...............92 % 750 mg 12 mm biplanar 113 N 1 – 2 min 0...8 % – – BASF Pharma Ingredients Generic Drug Formulations 2001 ................20 g Talc [10] .................................2 mm sieve and the other components through a 0............................0.............................................................. 4 min ..

Remark In the case of formulation No. BASF Pharma Ingredients Generic Drug Formulations 2001 . 1 it was not possible to press tablet cores of a biconvex form because some capping effect was observed.Alpha-Methyldopa T ablets (500 mg). DC page 2 4.

......... BASF Pharma Ingredients Generic Drug Formulations 2001 .............................1 g 2....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Alprazolam Tablets (0............<0.....158 mg Diameter .....8 mm Form .......................148 g Magnesium stearate [2] ....................................3 min Friability ...............106 N Disintegration ............................................... Formulation Alprazolam...........................................................8 mm screen and press with low compression force..........biplanar Hardness .... Manufacturing (Dir ect compression) Mix all components.1% 4. sieve through a 0................................................. Remark If the content uniformity does not meet the requirements it would be recommended to prepare a premix of the active ingredient with a small part of the Ludipress or with lactose monohydrate before mixing with the other components of the formulation................................................ 3.............2..0............5 mg) 1.............5 g Ludipress [1] ...................... Tablet properties Weight ...

..232................0 Magnesium trisilicate ... Manufacturing (Dir ect compression) Mix all components........... Tablet properties Weight .............0 Ludipress [1] .................................................biplanar Hardness..........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Aluminium Hydroxide + Magnesium Silicate Chewable Tablets (120 mg + 250 mg) 1..0 Aerosil 200 [4] ................................ 3........................................640 mg Diameter ..1...... pass through a 0..................................................250....6....... Formulation Aluminium hydroxide dried gel (Giulini) ..................................2..........................................6.16 mm Form .................5 g g g g g g g 2.... Remarks Due to the poor flowability of the powder the tabletting machine should be equipped with a special technical device providing a continuous and homogenous filling of the dies.............0 Cyclamate sodium .......... BASF Pharma Ingredients Generic Drug Formulations 2001 .......120...............................0 Magnesium stearate [2].......8 mm sieve and press with a compression force of 20 kN.........83 N 4..............12.0 Menthol ....

..........................7 min Friability....82 % BASF Pharma Ingredients Generic Drug Formulations 2001 .........................................................115 N Disintegration .......... 3.....biplanar Hardness ....................................................................2................................................0 g Ludipress [1] ...8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Ambroxol Tablets (30 mg) 1.. 30 min ...........0.......8 mm Form .....8 mm sieve and press with low compression force...................30............. pass through a 0.....................2 % Dissolution...............................5 g 2..........250 mg Diameter ........... Formulation Ambroxol hydrochloride .................5 g Magnesium stearate [2]............................217....... Manufacturing (Dir ect compression) Mix all components......................... Tablet properties Weight ..2....

..........................biplanar Hardness ................................................... Manufacturing (Dir ect compression) Mix all components..............................................97 N Disintegration ........................................................100 % 318 mg 12 mm biplanar 124 N 1 – 2 min 0............... Tablet properties No................0........................................................ sieve and press on a rotary press to tablets with low compression force....– Magnesium stearate [2] .2..................2 g Aerosil 200 [4]............................2 g 100 g – 200 g 6g 2g 12 g 2................................................. 2 Weight ................. 2 Aminophylline powder (BASF)........2 % – – BASF Pharma Ingredients Generic Drug Formulations 2001 .......10 min Friability ................... Formulations No................................8 mm Form ............. DC 1....... 3........150 g Avicel PH 200 [5].. 1 No...............................................87 % 15 min: .................. 1 No....100 g Ludipress [1] .................................................................................2 % Dissolution 10 min:.............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Aminophylline Tablets (100 mg)...........– Kollidon VA 64 [1]....254 mg Diameter ........

BASF Pharma Ingredients Generic Drug Formulations 2001 . 2 Due to the reduced flowability the tabletting machine should be equipped with a special technical device providing a continuous and homogenous filling of the molds. 1 After 2 weeks at room temperature no change of the colour of the tablets was observed but the long term compatibility between aminophylline and lactose should be controlled. Colour stability of Formulation No.Aminophylline ablets T (100 mg) page 2 4. Remark for Formulation No. 5.

.......................10 mg Ludipress [1] ..70 N Disintegration.... Formulations No...........................................................139 mg Magnesium stearate [2] ...3 % 157 mg 8 mm biplanar 92 N 3 min 0......................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Amitryptylline Tablets (10 mg and 25 mg) 1................. 2 Weight ........................8 mm Form ..............................................2.................1 g 25 mg 124 mg 1 mg 2............................................................... mix intensively and press with low compaction force (8 kN).... 1 No..............................152 mg Diameter ...................................biplanar Hardness ............8 mm sieve........0... 2: 25 mg Amitryptylline.1 – 2 min Friability .................... Tablet properties No.............2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........ 3....... Manufacturing (Dir ect compression) Pass all components through a 0............... 1: 10 mg No......

............................... Manufacturing (Dir ect compression) Mix all components.84 N Disintegration ....................................................2.......0..............250 g Magnesium stearate [2]..................biplanar Hardness................................................. Formulation Ampicillin trihydrate ...... Tablet properties Weight ...................................4 min Friability.............................................................................................10 g 2.... 3............. pass through a sieve and press with low compression force.........................4 % BASF Pharma Ingredients Generic Drug Formulations 2001 .250 g Ludipress [1] ..............500 mg Diameter ......12 mm Form .......................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Ampicillin Tablets (250 mg) 1............

......... Manufacturing (Dir ect compression) Pass all components through a 0...4 g g g g g g 2..200 Sorbitol......................................................................................................2.......................................... mix and press with low compression force............................ crystalline [10] ............................................0 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..........20 Kollidon CL [1]...................636 mg Diameter ......200 Kollidon VA 64 [1] .......................biplanar Hardness...9 min Friability ................ Formulation Asparagus extract. 3.......................... Tablet properties Weight .........................10 Magnesium stearate [2] ............................49 N Disintegration .........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Asparagus Extract + Parsley Extract Tablets (200 mg + 200 mg) 1............... powder ................200 Parsley extract....8 mm sieve... powder .............................12 mm Form .............................

.......................7 Kollidon 25 [1] .4 Tartaric acid..0.....................................25 N Disintegration .......... powder ........1...3 Sodium bicarbonate.......0 Sorbitol..... Tablet properties Weight ..20....1.......................................... Manufacturing (Dir ect compression) Mix .........66 mg Diameter ....... powder [6] ............10..................................biplanar Hardness.............................14.............7 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........... 3..............6 mm Form .....................18..................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Aspartame Effervescent Tablets (20 mg) 1............2. crystalline [10] .....................................................<1 min Friability...7 Polyethylene glycol 6000...........5 mm sieve and press to tablets........................ Formulation Aspartame ................. pass through a 0............................1 g g g g g g 2..................................

...........3 g g g g g 2..................................<1 min Friability .....8 mm sieve and press to tablets with low compression force..........................8 mm Form ......... 3............................................................................................2..................................................................12 Magnesium stearate [2] ....0.....................1 Lutrol F 68 [1] ................biplanar Hardness........................................ Manufacturing (Dir ect compression) Mix all components........................................120 mg Diameter ................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Aspartame Tablets (25 mg)..............76 Kollidon CL [1]......27 Ludipress [1] .......... Formulation Aspartame ................. DC 1.............1% BASF Pharma Ingredients Generic Drug Formulations 2001 .... pass through a 0..65 N Disintegration ....................... Tablet properties Weight ...........

......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Atenolol Tablets (90 mg) 1..........2......................2 – 3 min Friability ...............287..52....................................93.. Manufacturing (Dir ect compression) Mix all components..................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ..............2 Aerosil 200 [4] ......................0 Ludipress [1].................436 mg Diameter .................................0 Magnesium stearate [2]...............................biplanar Hardness................................................................. Tablet properties Weight ....................................85 N Disintegration........................ 3..12 mm Form ....................2...........0...................................9 g g g g g 2.......0 Kollidon CL [1]................... Formulation Atenolol (Stober)..................... pass through a 0.............8 mm sieve and press to tablets with low compression force...<0...

...5 g g g g 2.......0 g Corn starch [3] ..120 mg Diameter .......................................... Formulations No..................– Magnesium stearate [2] ....................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Benzhexol Tablets (5 mg) 1..5 mm Form ...................... Tablet properties No.....................4 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...2....5 0.120 N Disintegration ........ 1 No.biplanar Hardness............................................... 3....7 min Friability ................. 2 Weight .06 % 121 mg 5 mm biplanar 113 N 3 min 0..........< 0......................... Manufacturing (Dir ect compression) Mix all components for 10 minutes in a turbula mixer and press with low compression force............................... 1 No............. 2 Benzhexol chloride ..............5 1................................................................114....................................0.....– 5.......................................................6 g Aerosil 200 [4]......0 g 100........................5.......................................0 g (= trihexylphenidyl hydrochloride) Ludipress [1]....0 14........

.............................. Formulation Berberine sulfate ...........2................7 Lactose monohydrate [8].................1 Ludipress [1] ........1..............................115 mg Diameter ....biplanar Hardness...............1 min Friability ...............54......2 g g g g 2........54............ 3.........40 N Disintegration ......... Tablet properties Weight..............1% BASF Pharma Ingredients Generic Drug Formulations 2001 ....8 mm sieve and press with low compression force................................................ Manufacturing (Dir ect compression) Mix all components....................6 mm Form ............... pass through a 0.8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Berberine Tablets (5 mg) 1....................1 Magnesium stearate [2].............0.............................................................................................................5......

....1% BASF Pharma Ingredients Generic Drug Formulations 2001 ................................... 2 Betavit ® Dry Powder 10 % (BASF.............12 mm Form .......................17 min Friability............................... Tablet properties No......... 3.............................................. pass through a sieve and press with high compression force..................... 1 No....biplanar Hardness.....................– Magnesium stearate [2] ............ 1 No................126 N Disintegration (water).....1% 506 mg 12 mm biplanar 167 N 8 min 0................................5 g 30 g 50 g 50 g – 335 g 30 g 5g 2........... cryst..........................................0................................................. Manufacturing (Dir ect compression) Mix all components................................ 2 Weight .......... Formulations No.................... [10] .50 g Dry Vitamin E acetate 50 % DC (BASF) ..50 g Ludipress LCE [1] ....30 g Ascorbic acid...........................2.......– Kollidon VA64 [1].................................. powder (BASF)...........365 g Sorbitol...503 mg Diameter ....................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Beta Carotene + Vitamin C + Vitamin E Chewable Tablets (3 mg + 50 mg + 25 mg) 1......

.........2.0.............122 N Disintegration (water) ................................... Formulation Beta Carotene dry powder 10 % ..350 Polyethylene glycol 6000..4 % BASF Pharma Ingredients Generic Drug Formulations 2001 . crystalline [10] ......................... powder [6]..........................600 mg Diameter .................. Manufacturing (Dir ect compression) Mix all components............................20 mm Form ................ crystalline.......500 (BASF) Sorbitol...................................100 Ascorbic acid..................... Tablet properties Weight ......biplanar Hardness ............250 Sodium ascorbate................. crystalline (BASF) ..........................500 Fructose ............50 g g g g g g g g 2.....................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Beta Carotene + Vitamin C + Vitamin E Chewable Tablets (10 mg + 500 mg + 250 mg) 1...............280 Vitamin E acetate dry powder SD 50 ..................2.................600 Ludipress [1] .............................. 3.................15 – 20 min Friability....................... pass through a sieve and press with high compression force............

..........705 Kollidon VA64 [1] ..................... Manufacturing (Dir ect compression) Mix all components........................ powder [10] ...............................2....................................... 3..............50 Ludipress LCE [1] .....................20 mm Form .....95 N Disintegration (water) ...8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Beta Carotene + Vitamin C + Vitamin E Effervescent Tablets (12 mg + 150 mg + 25 mg) 1...............120 Ascorbic acid...................................3 min Friability....9 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...........2045 mg Diameter ................................50 Citric acid................................... crystalline (BASF) ........0....................75 Orange flavour (Dragoco) .................................450 Sodium bicarbonate ...............150 Dry Vitamin E acetate 50 % DC (BASF) .......... Formulation Lucarotene Dry Powder 10 % CWD G/Y (BASF) .............................. Tablet properties Weight .......................................50 Aspartame (Searle) ......biplanar Hardness...............30 g g g g g g g g g g 2........................320 Polyethylene glycol 6000.................. anhydrous ................ pass through a sieve and press with high compression force at a maximum of 30 % of relative atmospheric humidity....................

... Manufacturing (Dir ect compression) Pass all components through a 0.... crystalline (Merck) ............................... 1 No....– Magnesium stearate [2] ............................ 3.....65 g Ascorbic acid................................ 1 No........ 2 Betavit ® dry powder 10 % (BASF) ..................................60 g Ludipress [1] .............599 mg Diameter ..........................................– Kollidon CL [1] .8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Beta Carotene + Vitamin C + Vitamin E Tablets (6 mg + 100 mg + 30 mg) 1....................................... Tablet properties No........................2...........369 g Sorbitol..100 g Vitamin E acetate dry powder 50 % ...............6 g 65 g 100 g 60 g – 233 g 30 g 8g 4g 2..............2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...................................12 mm Form .............................8 mm sieve...................................... Formulations No...60 N Disintegration (water) ...............................0..... mix and press with medium or high compression force...........................................7 min Friability ......................biplanar Hardness .........– Kollidon VA64 [1].................. powder (BASF) ................. 2 Weight ...................................3 % 502 mg 12 mm biplanar 59 N 7 min 0.....

1 could be commercialized in Europe as dietary food because all components are allowed for this application.0 mg 7. Remarks A colourant pigment should be added to obtain a homogeneous appearance of the tablets.Beta Carotene + Vitamin C + Vitamin E T ablets (6 mg + 100 mg + 30 mg)page 2 4. 1 (40 °C.8 mg Beta carotene/tablet 5. Chemical stability of be ta carotene in Formualtion No. closed) 0 weeks 15 weeks 8. The tablets of Formulation No. BASF Pharma Ingredients Generic Drug Formulations 2001 .

................5 g g g g g g 2.......................................................... Tablet properties Weight ..............................................1% 4.........................< 0......................................................... mix and press with low compression force......... 3............55 N Disintegration ........... These tablets could be commercialized in Europe as dietary food because all components are allowed for this application..8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Beta Carotene + Vitamin C + Vitamin E Tablets (7 mg + 60 mg + 25 mg) 1...................................8 min Friability .......12 mm Form ......... Remarks A colourant pigment should be added to obtain a homogeneous appearance of the tablets.............................8 mm sieve.................. Manufacturing (Dir ect compression) Pass all components through a 0.................. powder (BASF) .. Formulation Betavit® dry powder 10 % (BASF) ............60 Vitamin E acetate dry powder 50 % ............... crystalline [10] .75 Ascorbic acid.biplanar Hardness......2........50 Sorbitol...............240 Kollidon CL [1] .... BASF Pharma Ingredients Generic Drug Formulations 2001 ....................497 mg Diameter ....30 Magnesium stearate [2] .......

...... pass through a sieve and press with medium compression force....biplanar Hardness.......................15 Sodium cyclamate .......10 g g g g g g g g 2............... crystalline (BASF) .............................790 mg Diameter ... Formulation Beta Carotene dry powder 10 % ..50 N Disintegration ............................ Tablet properties Weight ...1% BASF Pharma Ingredients Generic Drug Formulations 2001 ..5 Orange flavour (FDO) .... Manufacturing (Dir ect compression) Mix all components........ crystalline [10] ........................................ crystalline (BASF)................. 3.......< 0. powder [10] .141 Vitamin E acetate dry powder SD 50 ......2..................125 Ascorbic acid............................................125 Sodium ascorbate.........................12 mm Form .................................not tested Friability ...119 Polyethylene glycol 6000...................................250 (BASF) Ludipress [1] or Sorbitol.......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Beta Carotene + Vitamin C + Vitamin E Tablets (12 mg + 250 mg + 125 mg) 1................................................

......................20 Polyethylene glycol 6000............ powder [6]................ Manufacturing (Dir ect compression) Pass all components through o 0.....biplanar Colour................................45 sec Friability ...............................................................8 mm sieve....................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 .......2.................. 3...............................................0....................12 mm Form .............................................81 N Disintegration (water) ........... Tablet properties Compression force 18 kN 26 kN Weight ..........113 Citric acid..30 g g g g g g g g g 2..................................4 % 605 mg 12 mm biplanar brown 108 N 50 sec 0..................120 Sodium carbonate ........... Formulation Lucarotin ® dry powder 10 % CWD (BASF) ....................................15 Orange flavour ................................602 mg Diameter ...........................................................................................brown Hardness .............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Beta Carotene Effervescent Tablets (7 mg) 1.............................................12 Sodium cyclamate . anhydrous ..20 Aspartame .......................... mix and press with medium or high compression force at maximum 30 % of relative atmospheric humidity.70 Ludipress [1]......200 Sodium bicarbonate...........

..........– 5 % Kollidon 30 Avicel PH 101 [5]........................0 g Aerosil 200 [4]....2...5 20............................. 1 No.........................0 g – 175.........1% 502 mg 12 mm biplanar 57 N 1 min 0% BASF Pharma Ingredients Generic Drug Formulations 2001 ... Tablet properties No.................. pass through a 0....... 1 No............................– Kollidon CL [1] .................– Magnesium stearate [2] .........................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Beta Carotene Tablets (15 mg) 1............................................. Manufacturing (Dir ect compression) Mix all components..biplanar Hardness ..........................................2.......0...... granulated with ....................12 mm Form ................... 2 Weight ............... 2 Beta carotene dry powder 10 % ......0 2..................................– Talc [10] .59 N Disintegration ............0 5...................................400 mg Diameter ..........8 mm sieve and press with a medium compression force......160.......................12 min Friability.0 g 150............................................................6...................– Calcium arachinate [2] ..... Formulation No....0 g 100..........0 2............240........................ 3..................5 g g g g g – 2..0 g Ludipress [1] .......0 g Dicalcium phosphate [9].......................................................

15 % 4% 59 N 7 min 0.16 % 6 Months 12 Months Loss of beta carotene BASF Pharma Ingredients Generic Drug Formulations 2001 < 8% 9% . 2: 3% 60 N 9 min 0. Chemical and physical stability (20–25 °C) Formulation No.Beta Carotene Tablets (15 mg) page 2 4. 1: 6 Months 12 Months Loss of beta carotene Hardness Disintegration Friability Formulation No.

................................................0..200 Kollidon 30 [1] .......2............................................................4 % 4............ These tablets could be commercialized in Europe as dietary food because all components are allowed for this application...................................................................4 Magnesium stearate [2] .......................................... Tablet properties Weight . BASF Pharma Ingredients Generic Drug Formulations 2001 ...... Formulation Bran wheat (milled <1 mm).....................biplanar Hardness.....................................52 N Disintegration ...12 mm Form ...............5 Aerosil 200 [4] .......250 Ludipress [1] ...... DC 1..........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Bran Tablets (250 mg)...............................3 min Friability....4 g g g g g 2...................................... the hardness of tablet is higher but the content uniformity is less.........477 mg Diameter ... Remark If the bran is not milled......... Manufacturing (Dir ect compression) Mix all components......................... pass through a sieve and press with medium compression force...................... 3.....

...........................0...........2 % BASF Pharma Ingredients Generic Drug Formulations 2001 .. Manufacturing (Dir ect compression) Pass all components through a 0..................................................................................... 1 No..........1 g 8g – 190 g – – 1g 2........................ Formulations No........– Kollidon VA 64 [1]................................. 3.....................2 % 202 mg 8 mm biplanar 70 N 1 – 2 min 0...5 g Magnesium stearate [2] ..............70 N Disintegration ........... mix and press with low/ medium compression force...................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Bromhexine Tablets (8 mg) 1..........8 mm sieve......2.7 g Kollidon CL [1] .............................................biplanar Hardness ........................204 mg Diameter . 2 Bromhexine ...... 2 Weight .......... Tablet properties No.......179 g Ludipress [1] ............................................................... 1 No.............8 g Dicalcium phosphate [9].........< 1 min Friability ..............................8 mm Form ............................................................................................................

......... Tablet properties Weight ................9 mm Form ............4 min Friability..... Manufacturing (Dir ect compression) Mix all components....7 % Dissolution (10 min...........88 N Disintegration ................ Formulation Bromocriptine mesylate ..6...............6 % BASF Pharma Ingredients Generic Drug Formulations 2001 .............................................................2......................................0........................................................) .................... 3................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Bromocriptine Tablet Cores (6 mg) 1...................5 g Magnesium stearate [2]...................95..biconvex Hardness............ pass through a 0........8 mm sieve and press with high compression force....................................................2........1 g Ludipress [1] ......214 mg Diameter ......205..............2 g 2......

. mix and press with high compression force.0 g Orange flavour (Dragoco) .....0 g (Jungbunzlauer) Polyethylene glycol 6000............................201 N Friability..........0 g Aerosil 200 [4]..............2 % BASF Pharma Ingredients Generic Drug Formulations 2001 .845....................................0 g Calcium citrate (Merck) .... Tablet properties Weight...........0 g Ludipress LCE [1] ..biplanar Hardness.................500.. potassium (Searle) ...................... Aspartame.....297...8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Calcium Chewable Tablets (200 mg Ca) 1..............0 g 2..........0.....................20 mm Form ..................8 mm sieve...80........100.............................................0 g....5 g Citric acid anhydrous............................5..................... Manufacturing (Dir ect compression) Pass all components through a 0.............. Formulation Calcium gluconate (Merck) .....2................... powder [6]...17..................2417 mg Diameter ............... fine granular .. 3........................30.......

......200.............................5 g Aerosil 200 [4] ...................................biplanar Hardness ..................8 mm sieve.............................0 g Ludipress [1].... Manufacturing (Dir ect compression) Pass all components through a 0..............5 g Magnesium stearate [2].s.............2.............................470 mg Diameter .....................................q..........................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ................0...... 2................. Formulation Calcium glycerophosphate ....... Tablet properties Weight .................................297..........................................131 N Disintegration ...8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Calcium Glycerophosphate Tablets (200 mg) 1.12 mm Form ..................... mix and press with high compression force....2...........7 min Friability ......................... 3.........

...............8 mm Hardness......................................................................................................................... Manufacturing (Dir ect compression) Mix all components...91 Kollidon CL [1] .... pass through a 0...........8 mm sieve and press with medium compression force..............2................2 Magnesium stearate [2] ............. Tablet properties Weight .................................49 N Disintegration .......122 mg Diameter .............25 Ludipress [1] ......1 min Friability.....................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 .....0..........................2 g g g g 2........................................................................ 3....................... Formulation Captopril.8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Captopril Tablet Cores (25 mg) 1.................

...........................................................12 mm Hardness..........140 N Friability ........0 2..502. Tablet properties A B Weight .....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Carbamazepine Sustained Release Tablets (200 mg) DC 1............2..100...... Sintetica) ... blended for 10 min in a Turbula mixer and the compressed with high compression force.................. Formulations A Carbamazepine (Fabrica ital............200........14 % 472.........................0 20.......0 g Ludipress LCE [1] ................................................– Magnesium stearate [2] .......0 g Kollidon CL-M [1] ................. Manufacturing (Dir ect compression) All ingredients were passed through a 0.......5 g B 200.5 g g g g g 2.................06 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...0 100...............5 mg 12 mm 164 N 0..200.......8 mm sieve........... 3..............0 g Kollidon SR [1]...............0 150........................5 mg Diameter ..............0......2...............

Carbamazepine Sustained Release ablets T (200 mg) DT page 2 released drug [%] 4. Dissolution of Carbamazepine 100 Formulation B 80 60 Formulation A 40 20 0 0 2 4 6 8 10 time [h] BASF Pharma Ingredients Generic Drug Formulations 2001 12 14 16 18 .

......................2..12 mm Form ..................... 3.......... pass through a 0............................... Tablet properties Weight .....3 % Dissolution 10 min:....1 min Friability.......................................................................................................200 g Ludipress [1] ............................................................................................................................83 % 60 min: ......300 g Magnesium stearate [2] .......75 % 30 min: .......................................... Formulation Carbamazepine .................................. Manufacturing (Dir ect compression) Mix all components....0........................128 N Disintegration .....................8 mm sieve and press with low compression force...................496 mg Diameter ..8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Carbamazepine Tablets (200 mg) 1.2 g 2..........biplanar Hardness ..................86 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......

.. Tablet properties Weight .............2 – 3 min Friability...................................................... 3.......................0..........0 Copper sulfate ..8 mm Form ............ Manufacturing (Dir ect compression) Pass all components through a 0............0 g g g g g 2...........................5 Ludipress [1] ..........16 mg + 3............................16 Manganese sulfate .......3..............0 Magnesium stearate [2].2.......100..........0........... mix and press with medium compression force....................................................................................95 N Disintegration.... Formulation Carbonyl iron OF (BASF) ...3 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..............................131 mg Diameter .......5 mg) 1..........................................5 mm sieve........2........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Carbonyl Iron + Copper Sulfate + Manganese Sulfate Tablets (24 mg + 0............................biplanar Hardness...24.............

.................0 Polyethylene glycol 6000...................20.......................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ...................................10 mm Form .... pass through a 0..................................................>10 min Friability .................................................... Manufacturing (Dir ect compression) Mix all components......402 mg Diameter ..370........... crystalline.8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Cetylpyridinium Lozenges (2......0 Aspartame......5 Ludipress LCE [1] .............biplanar Hardness.2........... 3....5 g g g g g 2............ powder [6]....80 N Disintegration..5 mg) 1............8 mm sieve and press with low compression force..............................< 0.........2.....0 Menthol.......................... Formulation Cetylpyridinium chloride (Merck) ..................... potassium (Searle) ............. Tablet properties Weight ........1.6.......

.........1................................... crystalline ..................150..............0..... Formulation Chlorhexidine (Sigma) .......0 g g g g g g g g g 2...........................2................................................ Tablet properties Weight .... crystalline............ potassium .....8 mm sieve and press with medium compression force..5............................2..................0 Eucalyptol...3 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........... sodium ... Manufacturing (Dir ect compression) Mix all components......................................5......................................................8 mm Form ..175 mg Diameter ....0 Saccharin.............1.........................................0 Magnesium stearate [2]....1 Aerosil 200 [4] ..0 Sorbitol................................0...>10 min Friability..............................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Chlorhexidine Lozenges (5 mg) 1........biplanar Hardness....63 N Disintegration........ pass through a 0.5.............................. crystalline [10] ............ 3.................................0 Aspartame...5..........0 Menthol......0 Kollidon VA64 [1] ......................

...< 0...............................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Choline Theophyllinate Tablets (100 mg) 1........ Tablet properties Weight ..........5 mm sieve mix and press with very low compression force.................................................biplanar Hardness.......................................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ...............2..................4 min Friability ....................70 N Disintegration ....................100 g Ludipress [1] ........................................350 mg Diameter ......6 g 2.......................... 3.............. Formulation Choline theophyllinate .......... Manufacturing (Dir ect compression) Pass all components through a 0..........................................244 g Magnesium stearate [2] ..........8 mm Form ........................................

......... pass through a 0.........8 mm Form ...............................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Chymotrypsine Tablets (27 mg) 1...............................6 min Friability ....5 g Magnesium stearate [2]....71........67 N Disintegration ........8 mm screen and press with low compression force.. 3.........5 g Ludipress [1] .......27.................. Formulation Chymotrypsine .........100 mg Diameter ............................................... Tablet properties Weight .................0 g 2........................2.. Manufacturing (Dir ect compression) Mix all components...................................biplanar Hardness.1...........................................................< 0.................................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ............................................

... Formulations No.........................biplanar Hardness.........4 min Friability .....................1..............0 % 1780 mg 16 mm biplanar 195 N < 2 min 1..680 g Sodium bicarbonate ..............8 mm screen and press with medium compression force at a maximum of 30 % of relative atmospheric humidity................................... powder [6] .s................ 2.q..s................. Manufacturing (Dir ect compression) Pass the mixture through a 0........................................................................................................... 3....................... 1 No......30 g Polyethylene glycol 6000..0 % BASF Pharma Ingredients Generic Drug Formulations 2001 .......................................................................................450 g Citric Acid.............. Tablet properties No..............20 mm Form .....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Cimetidine Effervescent Tablets (400 mg) 1..............................................90 g Orange flavour (Dragoco) .2...... 400 g 400 g 500 g – 400 g 27 g 75 g q................. 1 No.......– Aspartame (Searle) ......................................2250 mg Diameter ............................. 2 Weight .............................................400 g Ludipress LCE [1] ..........107 N Disintegration (water) .....600 g Tartaric Acid... 2 Cimetidine ......................

..........................1 min Friability............ Formulation Cimetidine................................................88 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..... 3..8 mm screen and press with low compression force.............. Tablet properties Weight .........................200 g Ludipress [1] ............................5 g 2........................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Cimetidine Tablets (200 mg) 1.........................biplanar Hardness..................12 mm Form .....510 mg Diameter ................2 % Dissolution (15 min) ...92 N Disintegration ...............................................................................................................295 g Magnesium stearate [2] .................................... Manufacturing (Dir ect compression) Pass the mixture through a 0...0.....2................

.......... Tablet properties Weight ............. 3...........3 min 4......................2...............................00 g 2.......... Formulation Clenbuterol hydrochloride ................................0..........................................1.............99.....75 N Disintegration .................................8 mm Form ........02 g Ludipress [1] ........................... Remark If the content uniformity does not meet the requirements it would be recommended to prepare a premix of clenbuterol hydrochloride with a small part of the Ludipress before mixing with the other components of the tabletting mixture.......................00 g Magnesium stearate [2]..................... Manufacturing (Dir ect compression) Mix all components in a turbula mixer and press to tablets with a compression force of 20 kN.....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Clenbuterol Tablets (20 µg) 1.. BASF Pharma Ingredients Generic Drug Formulations 2001 .....biplanar Hardness..100 mg Diameter ...........................

............. DI-TAB [9] ............... Tablet properties Weight ...................8 mm sieve and press with medium compression force (15 kN).......................165 mg Diameter .... pass through a 0....7..1.......................................... Formulation Clobazam...............................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Clobazam Tablets (10 mg) 1..........135........44 N Disintegration ......0 Kollidon CL [1].........0 Magnesium stearate [2]...0 Kollidon VA 64 [1] ...........biplanar Hardness......0 Dicalcium phosphate...........7..........................< 0.........................................< 1 min Friability .............8 mm Form ..........................1% BASF Pharma Ingredients Generic Drug Formulations 2001 .2........... 3...................................... Manufacturing (Dir ect compression) Mix all components.............10.................................................................5 g g g g g 2................

................ 3.......................................................................................biplanar Hardness...................2.. Manufacturing (Dir ect compression) Mix all components..................... sieve and press with low compression force.................6 min Friability ............50 mg Ludipress [1].................................100 mg Magnesium stearate [2]....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Clomifen Citrate Tablets (50 mg) 1.............................................0......................13 % Dissolution (60 min) .......100 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...1 mg 2.......................... Formulation Clomifen citrate .....................8 mm Form ..........................82 N Disintegration ......... Tablet properties Weight ..........154 mg Diameter ...........................................................

........... 3..............0...............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Cyproheptadine Tablet (4 mg) 1.. Remark If the content uniformity does not meet the requirements it would be recommended to prepare a premix of the active ingredient with a small part of the Ludipress or with lactose monohydrate before mixing with the other components of the formulation..8 mm sieve................... Mix and press with very low compression force (4 kN).................................5 % 4.............biplanar Hardness....2 g 2..................................... BASF Pharma Ingredients Generic Drug Formulations 2001 ..........................................................................................202 mg Diameter ............................................. Formulation Cyproheptadine ......... Tablet properties Weight .............................................194 g Magnesium stearate [2] .4 g Ludipress [1] ..........46 N Disintegration ............2............................... Manufacturing (Dir ect compression) Pass all ingredients through a 0........8 mm Form ...... 3 min Friability...........

... Formulation Diazepam..10 g Ludipress . Tablet properties Weight .100 % BASF Pharma Ingredients Generic Drug Formulations 2001 .................1% Dissolution (10 min) ............................2....................... 3........8 mm sieve and press with medium compactation force...................biplanar Hardness ...............................................................................0........................according to the formulation Form ..........< 0.........................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Diazepam Tablet (10 mg) 1........< 5 min Friability ... Manufacturing (Dir ect compression) Mix all components...................110 – 490 mg ......... pass through a 0..............100 – 480 g Magnesium stearate .............................................5 – 2..0 g 2...........> 100 N Disintegration ...........................................................

......................................206.................100...................4 g g g g 2.. Tablet properties Weight ..3....8 mm Hardness .......... Formulation Diclofenac sodium (Ivotec).8 40 20 0 0 2 4 6 8 10 time [h] BASF Pharma Ingredients Generic Drug Formulations 2001 12 14 16 18 ..............4 Magnesium stearate [2].............................. blended for 10 min in a Turbula mixer and then compressed with medium compression force......100.........................................0..............................4 mg Diameter ............09 % released drug [%] 4.8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Diclofenac Sustained Release Tablets (100 mg) 1..8 mm sieve...........195 N Friability.......0 Silicon dioxide....................................... colloidal [4] ..2... 3.3......0 Kollidon SR [1].. Manufacturing (Dir ect compression) All ingredients were passed through a 0....... Dissolution of Diclofenac-sodium 100 80 60 50 rpm medium: phosphate buffer pH 6.............

...............10.............99 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..........77 % (30 min).................biplanar Hardness..........58 % (15 min) ......72 N Disintegration ....0 Kollidon CL [1] ........8 mm sieve and press with low compression force....................1.............. Manufacturing (Dir ect compression) Mix all components.150.......50.....................0 Magnesium stearate [2].......................0 g g g g g 2..8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Diclofenac Tablets (50 mg) 1.... pass through a 0.........................0 Ludipress [1] ... Formulation Diclofenac sodium .........226 mg Diameter ........................ 3.....................................................<0.. powder [6] ...........15..........16 min Friability ...........................................2..............................8 mm Form ........................1% Dissolution (10 min) ....5 Polyethylene glycol 6000...................... Tablet properties Weight ...........................................................................................................................

............................................................8 mm Form ....................................1 g g g g g 2.......215 mg Diameter .....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Diltiazem Tablets (50 mg) 1.............................. Tablet properties Weight ....... 3.........................................6 min Friability .......... Formulation Diltiazem .................5 Aerosil 200 [4] ...........0...........60 Ludipress [1] .....> 100 N Disintegration ........1% BASF Pharma Ingredients Generic Drug Formulations 2001 ................................................................................................biplanar Hardness ....................... powder [6]....... Manufacturing (Dir ect compression) Mix all components............................... pass through a sieve and press with low compression force.........................1 Magnesium stearate [2] ........................2.........141 Polyethylene glycol 6000..............

.................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Dimenhydrinate Tablets (50 mg)............................2..............................0 Ludipress [1] ..............3 min Friability ... DC 1............................................................. Formulation Dimenhydrinate ....4........................................5 g g g g g 2....................8 mm Form ...........................1...................... 15 min .....50 Aerosil 200 [4] .......1% Dissolution in water (USP................... add the other components.......76 N Disintegration ................2................0 Magnesium stearate [2]................................................... sieve and press with low compression force............................. Manufacturing (Dir ect compression) Mix dimenhydrinate with Aerosil 200................... 3..94 % BASF Pharma Ingredients Generic Drug Formulations 2001 .........93 % 45 min ........202 mg Diameter .............140 Kollidon CL [1] ......................<0...............91% 30 min ...biplanar Hardness...................... Tablet properties Weight ...............

85 % 10 min.............. Formulations 1 mg 4 mg Doxazosin mesylate ......98 g Magnesium stearate [2] ................................... Tablet properties 1 mg 4 mg Weight .........................................1 g Ludipress [1] ...................................2.........................1 g 4g 95 g 1g 2...........1% Dissolution in water (USP).........................biplanar Hardness .........3 min Friability.65 N Disintegration ......................................< 0..................100 mg Diameter ..................................... sieve and press with low compression force.................. Manufacturing (Dir ect compression) Mix all components.................... 3......................100 % 102 mg 6 mm biplanar 66 N 3 min < 0.........................6 mm Form ......................................1% 67 % 100 % BASF Pharma Ingredients Generic Drug Formulations 2001 .... 5 min .......................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Doxazosin Mesylate Tablets (1 mg and 4 mg) 1.............................

......620 mg Diameter ............ pass through a 0..................... Formulation Ethambutol ...........12 mm Form ...........biplanar Hardness.8 % BASF Pharma Ingredients Generic Drug Formulations 2001 .............20 Kollidon CL [1]...................................................... crystalline [10] ................................................... 3..................................10 g g g g g 2.............. DC 1..........................400 Sorbitol....... Manufacturing (Dir ect compression) Mix all components...............10 min Friability.........................................0................82 N Disintegration........200 Kollidon VA 64 [1] ...........2.....8 mm sieve and press with medium/high compression force...8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Ethambutol Tablets (400 mg)...........................10 Magnesium stearate [2]................................................... Tablet properties Weight ..............................................

.....2 % 4...53 Magnesium stearate [2] ................... 3............................101 Theophylline.............. DC 1..2/0................1 Aerosil 200 [4] .23 Ludipress [1] ...............................................102 N Disintegration .......2 g g g g g 2..................................7 – 8 min Friability........... powder ..175 mg Diameter .0............................ Formulation Etophylline..... Manufacturing (Dir ect compression) Mix all components...................2.................................................................................. Tablet properties Weight .....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Etophylline + Theophylline Tablets (100 mg + 22 mg)............7 (BASF) ............8 mm Form .. Remark To enhance the flowability of the tabletting mixture the amount of Aerosil 200 could be increased.. anhydrous 0.............................. BASF Pharma Ingredients Generic Drug Formulations 2001 ......... pass through a 0......biplanar Hardness ................................................8 mm sieve and press to tablets with low compression force...........

............. Formulations No..............105 g Magnesium stearate [2] ....3 g Stearic acid [7] ............ Tablet properties No.........................................8 mm Form ......................... 2 Famotidine........................ 1 No....................4 g 40 g 104 g – 2g 4g 2..................................................74 N Disintegration (gastric juice).....................149 mg Diameter ...........................– Aerosil 200 [4].....................3 min Friability............................................ 3.............1% Dissolution (10 min)................<0....... Manufacturing (Dir ect compression) Mix all components...........95 % 148 mg 8 mm biplanar 49 N 1 min 0..................................8 mm sieve and press with low compression force................................2...................... pass through a 0..........3 % not tested not tested BASF Pharma Ingredients Generic Drug Formulations 2001 ..........................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Famotidine Tablets (40 mg) 1.....................................40 g Ludipress [1] ..................................................biplanar Hardness .......... 2 Weight ....................63 % (30 min) ....... 1 No....

......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Ferrous Fumarate Tablets (200 mg) 1....................................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ....... pass through a 0..................................................................................12 mm Form ............................. Tablet properties Weight .......................................................................295 g Magnesium stearate [2] ........1 min Friability...............5 g 2..509 mg Diameter ..............................biplanar Hardness. Formulation Ferrous fumarate ........200 g Ludipress [1] .........................2...8 mm sieve and press with low compression force............................ 3.........................0......92 N Disintegration ..................... Manufacturing (Dir ect compression) Mix all components.......

...8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Ferrous Sulfate + Manganese Sulfate + Copper Sulfate Tablets (65 mg + 3........... 3........3 – 4 min Friability.........5 Copper sulfate .....149 mg Diameter ............0 Aerosil 200 [4] ..........0......................... anhydrous ....8 mm Form .............................................10.... mix and press with high compression force......................0 Kollidon 30 [1] .. Formulation Ferrous sulfate.....................................biplanar Hardness................3...... Tablet properties Weight ................... Manufacturing (Dir ect compression) Pass all components through a 0.........................3.................................2.........................16 mg) 1.........................0 Magnesium stearate [2].................5 mg + 0...16 Ludipress [1] ...................0.........................................4 % BASF Pharma Ingredients Generic Drug Formulations 2001 .............................70....65......5 mm sieve.........................0 Manganese sulfate .28 N Disintegration ..........................2............0 g g g g g g g 2...........................

.8 mm sieve and press to tablets with medium compression force.............3 g g g g g g 2...4 Talc [10] ..........................110 N Disintegration................ Manufacturing (Dir ect compression) Mix all components.................... pass through a 0.....2............................15 Magnesium stearate [2] ................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...0................................................... 3................13 min Friability............................................................ anhydrous .413 mg Diameter ............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Ferrous Sulfate Tablets (200 mg) 1...................8 mm Form ..............................185 Kollidon VA 64 [1] ..........biplanar Hardness ...................................................................................................................... Formulation Ferrous sulfate................4 Aerosil 200 [4] ......................203 Ludipress [1] ..................................... Tablet properties Weight ..........

...................................................0..............0 g Magnesium stearate [2]............5 min Friability .......2...........................................76 N Disintegration .176....... Formulation Fluoxetine HCl (BASF)....................... pass through a 0.........205 mg Diameter ..........8 mm sieve and press to tablets with low compression force......... Tablet properties Weight .......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Fluoxetine Tablets (20 mg) 1.................biplanar Hardness.....22. 3..1% BASF Pharma Ingredients Generic Drug Formulations 2001 ..... Manufacturing (Dir ect compression) Mix all components..............................................................................................4 g Ludipress [1]...........1.........................8 mm Form .............6 g 2.....................................

..............0 g Magnesium stearate [2].........biplanar Hardness..........213 mg Diameter .............................2..............1% 4.......195.........................8 mm sieve and press to tablets with medium compression force...0 g Ludipress [1] ....8 mm Form ........................ Formulation Folic acid ..........1........................................................................... pass through a 0...... 3.......7 min Friability ....................................5............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Folic Acid Tablets (5 mg) 1..5 g 2...................... Remark If the content uniformity does not meet the requirements it would be recommended to prepare a premix of the active ingredient with a small part of the Ludipress or with lactose monohydrate before mixing with the other components of the formulation...........................205 N Disintegration ................................... Tablet properties Weight ......... BASF Pharma Ingredients Generic Drug Formulations 2001 .......< 0................... Manufacturing (Dir ect compression) Mix all components.............

........................................................8 mm sieve and press with low compression force......81 N Disintegration .biplanar Hardness...........2 min Friability .......................................................40 g Ludipress [1] .......................... Formulation Furosemide .. Tablet properties Weight .8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Furosemide Tablets (40 mg) 1.8 mm Form ...............205 mg Diameter ............................. Manufacturing (Dir ect compression) Mix all components........................................................................... 3............................2 g 2................................................................ pass through a 0.........................158 g Magnesium stearate [2] ......0................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ....2.

..................... Tablet properties Weight ............................................................................ Formulation Furosemide .............................................. 3.....12 mm Form .................2. Manufacturing (Dir ect compression) Mix all components.......................................159 N Disintegration ................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Furosemide Tablets (200 mg) 1..............................biplanar Hardness ............618 mg Diameter ..........................388 Magnesium stearate [2] .6 g g g g 2........8 mm sieve and press with low compression force......................... pass through a 0......200 Ludipress [1] .6 Aerosil 200 [4] ....................................0...............................................3 – 4 min Friability.............................

..........100 Kollidon CL [1].........................8 mm sieve and press to tablets with medium compression force............................. 3................... powder (Aflopa) ... Tablet properties Weight.. Formulation Garlic extract. Manufacturing (Dir ect compression) Mix all components....... crystalline (BASF)...........714 mg Diameter .............................................0 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Garlic Extract + Thyme Extract Tablets Cores with Vitamin C (300 mg + 25 mg + 100 mg) 1........2.......................biconvex Hardness.............268 Magnesium stearate [2] ....9 min Friability ............................7 g g g g g g 2........25 Ascorbic acid............................................................................................. granulated (Aflopa)..........14 Ludipress [1] ..12 mm Form ...300 Thyme extract......................................... pass through a 0.........................................................50 N Disintegration .........

....1 Kollidon CL [1] .............. Tablet properties Weight ..... 3.... add the other components.................................................. dry powder ........254 mg Diameter ......203 Magnesium stearate [2] ...............................................................81 N Disintegration .........< 0....................................................................................................... Formulation Ginkgo biloba extract.......................2 g g g g g 2...8 mm sieve and press to tablets with low compression force........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Ginkgo Extract Tablets (40 mg) 1.. Manufacturing (Dir ect compression) Mix the Ginkgo extract with Aerosil 200................8 min Friability....... pass through a 0...........................................................2.............1% BASF Pharma Ingredients Generic Drug Formulations 2001 ........................8 mm Form ......240 (Biogen) Aerosil 200 [4] .........................4 Ludipress [1] ..........................................biplanar Hardness ..........

........2-3 min Friability .......biplanar Hardness ........120.....7 mm Form ....1% – – – BASF Pharma Ingredients Generic Drug Formulations 2001 .... Tablet properties No.......5.8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Glibenclamide (Glyburide) Tablets (5 mg) 1..........125 mg Diameter ..................................................... 2 Weight .. 2 Glibenclamide micronized (Guidotti).......................................75 % 201 mg 8 mm biplanar 107 N 3 – 4 min < 0................................................5 g – 5..0 g 194............... 3.............................< 0............4) (10 min) .8 mm sieve and press with low compression force (about 10 kN)......................– Ludipress [1] ........... Manufacturing (Dir ect compression) Mix all components........0 g Magnesium stearate [2] .................................................0 g Glibenclamide ................................ 1 No........0 g 2............80 N Disintegration ...... 1 No............ pass through a 0.............69 % (60 min) ..............0 g 1.....................................50 % (30 min) ......2 % Dissolution (pH 7..................2.............0............................. Formulation No..................

1% Compression force 10 kN 20 kN 107 N 3 – 4 min < 0.Glibenclamide (Glyburide)ablets T (5 mg) page 2 4. 2) Property Hardness Disintegration Friability 5 kN 47 N 2 – 3 min < 0.1% . Influence of the compr ession force on the physical table t properties (Formulation No.1% 25 kN 191 N 5 min < 0.1% BASF Pharma Ingredients Generic Drug Formulations 2001 158 N 3 – 4 min < 0.

................. Formulation Griseofulvin..............................88 % 60 min .............................................79 N Disintegration ........ micronized (Aldrich) ..................2...250 Polyethylene glycol 6000.................. powder [6] .................................. Remark The flowability of the tabletting mixture should be increased by higher amounts of Ludipress or/and Aerosil 200............5 mm sieve...............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Griseofulvin Tablets (125 mg) 1..........................................92 % 4................. BASF Pharma Ingredients Generic Drug Formulations 2001 ..... 20 min ................1 min Friability.............367 mg Diameter ..0........19 g g g g 2.................................................................................................... mix and press with low compression force applying a vibrating hopper........78 % 40 min .............3 % Dissolution...biplanar Hardness........ Manufacturing (Dir ect compression) Pass all components through a 0....12 mm Form ... 3...............................10 Aerosil 200 [4] ............... Tablet properties Weight .....................125 Ludipress [1] ..........

.................89 % 10 min BASF Pharma Ingredients Generic Drug Formulations 2001 ................................... mix and press............................biconvex Hardness.... Formulation Hydrochlorothiazide...............................................................300 Kollidon CL [1]....... Tablet properties Weight ..< 1 min Dissolution of hydrochlorothiazide.............2 g g g g g 2......................................15 Aerosil 200 [4] ........2 Magnesium stearate [2] .......9 mm Form ........................................... Manufacturing (Dir ect compression) Pass all components through a 0..................2........................369 mg Diameter ....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Hydrochlorothiazide + Potassium Chloride Tablet Cores (50 mg + 300 mg) 1..................... ............88 N Disintegration .......... 3....................................................8 mm sieve...............................50 Potassium chloride ..........

...........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Hydrochlorothiazide Tablets (50 mg).........................................8 mm sieve and press with low compression force.................................0.3 min Friability ........................................................................... pass through a 0...1% BASF Pharma Ingredients Generic Drug Formulations 2001 .2 g 2..............280 g Magnesium stearate [2] ........8 mm Form ........................................70 N Disintegration ...........................2........ Tablet properties Weight ....... 3........................328 mg Diameter ........ Manufacturing (Dir ect compression) Mix all components................biplanar Hardness................... Formulation Hydrochlorothiazide..................... DC 1............................................50 g Ludipress [1] ..........

.................... Formulations Ibuprofen (Francis) ............................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Ibuprofen Tablets (400 mg)................. 10 min 20 min BASF Pharma Ingredients Generic Drug Formulations 2001 – – – 85 % 87 % 8 Months 12 Months 121 N 2 – 3 min 0................................................... Manufacturing (Dir ect compression) Pass ibuprofen and magnesium stearate through a 200 µm sieve........... 3.........2 % 89 % 88 % ..8 Magnesium stearate [2] .........................400 Aerosil 200 [4] ..................4 % Dissolution.......................... Physical stability (20–25ºC) 6 Months Hardness Disintegration Friability Dissolution...........112 N Disintegration ........0. Tablet properties Weight ....2 – 3 min Friability ..............82 % 15 min....................752 mg Diameter ....342 Kollidon CL [1] ..........................................2..16 mm Hardness ...................................................8 g g g g g 2.. 10 min ..............................4 % – 91% 120 N – 0.............91% 4.. 4 Ludipress [1] ................................................................................. mix with the other components and press with medium compression force.......... DC 1..............................................

.27 Macrogol 6000 powder [6] ...........................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Ibuprofen Tablets (600 mg)..... add the other components and press with low compression force...........................................108 Kollidon VA 64 [1] ....6 2.... Tablet properties Weight ......50 Kollidon CL [1] ..600 Aerosil 200 [4] .................................... 3.............................. Formulations Ibuprofen 50 (BASF) ......................9 Avicel PH 200 [5] .........793 mg Diameter ....16 mm Hardness......2...............................<1 min Friability.......80 N Disintegration ......0............. DC 1..8 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......................................................................................... g g g g g g Manufacturing (Dir ect compression) Mix ibuprofen with Aerosil 200........................................................................................................................

page 2 Dissolution (Storage 20-25°C) 100 10 min 15 min 80 30 min 60 40 20 0 0 3 6 Months BASF Pharma Ingredients Generic Drug Formulations 2001 9 12 . DC drug released [%] 4.Ibuprofen Tablets (600 mg).

................ Manufacturing (Dir ect compression) All ingredients were passed through a 0........ blended for 10 min in a Turbula mixer and then compressed with medium compression force...100 Silicon dioxide.....................163 N Friability .... Tablet properties Diameter . 3..................................................................01% released drug [%] 4.....5 g g g g g 2.10 mm Weight .................................8 mm sieve.....5 Magnesium stearate [2].........................2......1..125 Ludipress LCE [1] ............303 mg Hardness ...........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Indomethacin Sustained Release Tablets (75 mg) 1............2 20 0 0 2 4 6 8 10 time [h] 12 14 16 18 BASF Pharma Ingredients Generic Drug Formulations 2001 .... Formulation Indomethacin (Synopharm) .0...1.................................................................... Dissolution of Indome thacin 100 80 60 40 75 rpm medium: phosphate buffer pH 6....75 Kollidon SR [1]....... colloidal [4] ..........................................

..........................3 min Friability..........20 Magnesium stearate [2] ............................................... Tablet properties Weight ..227 Kollidon CL [1] .......................... Formulation Indomethacin ...........biplanar Hardness ....................... 3....................................................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..............3 g g g g 2.......................................................................................................... DC 1..............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Indomethacin Tablets (50 mg)....2..........................8 mm Form .8 mm sieve and press with medium compression force....................0... pass through a 0....50 Ludipress [1] ..................... Manufacturing (Dir ect compression) Mix all components.........................303 mg Diameter ................176 N Disintegration .........

Manufacturing (Dir ect compression) Mix all components.................................. pass through a 0..................biplanar Hardness..3 g 2...........................61 N Disintegration ............................5 min Friability... BASF Pharma Ingredients Generic Drug Formulations 2001 ... Formulation Indomethacin .......................... 3.....4 % 4...............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Indomethacin Tablets (100 mg) 1................0............................500 mg Diameter ..........8 mm sieve and press with low compression force...................100 g Ludipress [1] .........................397 g Magnesium stearate [2] ...........12 mm Form .........................................................2..................................... Tablet properties Weight ...... Remark If the flowability of indomethacin is not good it should be mixed with a low percentage of Aerosil 200...............................................

...........................4 Kollidon CL [1] .............2.......1 Kollidon 30 [1] ....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Isosorbide Dinitrate Tablets (5 mg) 1........5....9.........5 Lactose monohydrate [8] ...........................152........................................................................0 Magnesium stearate [2]......................................... Tablet properties Weight .................0 g g g g g 2...................... 3...........45 N Disintegration ............................8 mm Form ....................................... Formulation Isosorbide dinitrate + Lactose (4+6) ....12..< 1 min Friability ....................................... pass through a 0.................... Manufacturing (Dir ect compression) Mix all components.8 mm sieve and press with low compression force..............184 mg Diameter ..........biplanar Hardness.......1.....1% BASF Pharma Ingredients Generic Drug Formulations 2001 ......0..........

................ mix intensively and press with low compression force (10 kN).....65 N Disintegration .... Formulation Khellin .........................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Khellin Tablets (25 mg) 1...................................... Tablet properties Weight ........124 g Magnesium stearate [2] .....................25 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..about 1 min Friability.......................................8 mm sieve.....0.2. Manufacturing (Dir ect compression) Pass all components through a 0.................................................................................... 3.................8 mm Form ......1 g 2.......................................25 g Ludipress [1] .........150 mg Diameter ..........................biplanar Hardness........................................

..................... 3..........................................................2...............6 % 15 min ..2 % Dissolution (gastric juice......1 min Friability.....8 Magnesium stearate [2]...8 mm Form ..............4 Aerosil 200 [4] ....................150 mg Diameter ...0......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Labetalol Tablets (50 mg) 1........................ Formulation Labetalol....100 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...0 Ludipress [1] ..... 50 rpm) 10 min..biplanar Hardness ................0..................96..8 g g g g 2.....71 N Disintegration ................................................. Manufacturing (Dir ect compression) Mix all components....50..... fine powder (Joy Sun)......................... sieve through a 0... paddle................................................................................0.....8 mm screen and press with low compression force............... Tablet properties Weight .................98..........................

......................458 mg Diameter .............3 – 4 min Friability...............................80 N Disintegration .....biplanar Hardness.......8 mm sieve and press with low compression force....................2....................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Levamisole Tablets (150 mg) 1..... Tablet properties Weight ............................................................................. 3...... Manufacturing (Dir ect compression) Mix all components.2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..0.........300 g Magnesium stearate [2] ..........4 g 2.......................... pass through a 0.....................................12 mm Form .... Formulation Levamisole hydrochloride ........................................................................150 g Ludipress [1] ..........................

.................................... The effectiveness was not controlled in this formulation..1..0..................6 mm 6 mm Form .........................00 1........... Levothyroxine sodium ........ 1 No........biplanar biplanar Hardness .........05 10.....– Magnesium stearate .................... II.............. Remarks If the content uniformity of formulation No.......99..05 mg) 1.......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Levothyroxine Tablets (0...............................52 N 45 N Disintegration......8 mm sieve......05 g Citric acid.............................00 g No.......... Mix and press with low compression force.....................0............ 2 0............00 89.............00 g g g g 2........... 3.........1 – 2 min 4 min Friability.......... 1 I...................... Tablet properties No....... BASF Pharma Ingredients Generic Drug Formulations 2001 ..1% <0......00 g Ludipress [1] .. The function of citric acid in formulation No......1% Content uniformity not controlled 4...... 1 does not meet the requirements it would be recommended to add a small part of Ludipress (= part II) to the premix I..............103 mg 101 mg Diameter ............................... Formulations No.... anhydrous.............. Manufacturing (Dir ect compression) Prepare premix I. 2 is the stabilization of the active ingredient............... add II and pass the mixture thorugh a 0.....2..................... 2 Weight ......

........1 g 2...............................................94 N Disintegration.............0................139 g Magnesium stearate [2] ......................... Tablet properties Weight .......8 mm Form ................. Manufacturing (Dir ect compression) Pass all components through a 0..............biplanar Hardness...............................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Lisinopril Tablets (10 mg) 1..............................8 mm sieve.............2........2 – 3 min Friability.................................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......... Formulation Lisinopril ......................152 mg Diameter .........10 g Ludipress [1] ...................... 3................................................................ mix intensively and press with low compactation force (10 kN)..................................

...... Formulation LycoVit 10 % dry powder....................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Lycopene Tablet Cores (6 mg) 1..........8 mm screen and press with medium to high compression force................................... 3............. sieve through a 0.....2......1% BASF Pharma Ingredients Generic Drug Formulations 2001 .........................330 Kollidon CL [1] .........................................<0............................11 mm Form .400 mg Diameter ................................................60 Ludipress [1] .............................................4 min Friability .................biconvex Hardness..................................... Manufacturing (Dir ect compression) Mix the LycoVit dry powder with the other components.............................. Tablet properties Weight ...80 N Disintegration ...........4 g g g g 2..6 Magnesium stearate [2] ...........................................................

.....180 III..............1% Taste .....60 min Friability .............................................................................................500 Lactose monohydrate [8] .............< 0........................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Magaldrate Chewable Tablets (500 mg) 1........ Manufacturing (W et granulation) Granulate mixture I with solution II...............6 Cocos flavour (FDO) . pass through a 0.........................72 N Disintegration (water) .............16 mm Form .............................. 3......................................... Magaldrate USP ....................................biplanar Hardness.......................... dry.... Formulation I........................................1 Water ...................... Kollidon 90 F [1] ..........................3 g g g g g g g g g g 2.2............................................ Tablet properties Weight.......................1000 mg Diameter .............................................6 Saccharin sodium.........8 mm sieve....................................................... Aerosil 200 [4] ....50 II......... mix with III and press with low compression force......5 Magnesium stearate [2] ............400 Orange flavour (FDO) ....good BASF Pharma Ingredients Generic Drug Formulations 2001 ..............................20 Banana flavour (FDO)....................................

...........1% BASF Pharma Ingredients Generic Drug Formulations 2001 ............................................... mix and press with medium compression force..........10 g Peppermint flavour .. Formulation Magaldrate (Reheis) ......................... potassium (Searle) .. 3................q.........60 g Aspartame.................................... 2...biplanar Hardness.....1000 g Ludipress LCE [1] ................2...>250 N Friability .........................................................................000 mg Diameter .................................... Tablet properties Weight ..2........930 g Lutrol E4000F [1] ............s............................8 mm sieve...............................<0...... Manufacturing (Dir ect compression) Pass all components through a 0..20 mm Form ...............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Magaldrate Chewable Tablets (1000 mg) 1................

.....................50 Magnesium stearate [2] ........0................................................. Formulation Magaldrate............................. 3..16 mm Form ......................................................125 N Disintegration (water)......10 Kollidon CL [1] ..2...................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Magaldrate Dispersible Tablets (700 mg) 1............................. Manufacturing (Dir ect compression) Pass all components through a 0...........1..........................25 sec Friability .....................biplanar Hardness .........200 mg Diameter ...................... Tablet properties Weight ............435 Kollidon 90 F [1] .....1% BASF Pharma Ingredients Generic Drug Formulations 2001 ..........700 Lactose monohydrate [8] ....................................................5 g g g g g 2....................... mix and press with low compression force (4 – 6 kN)...........................8 mm sieve..............................

. Formulation Magnesium carbonate USP .................................2.................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ...................12 mm Form ..... pass through a 0................biplanar Hardness .. Tablet properties Weight ..........4 g 2.............................................................. Manufacturing (Dir ect compression) Mix all components................................................................262 g Ludipress [1] ...................499 mg Diameter .......................1 min Friability ....168 N Disintegration .........8 mm sieve and press with medium compression force.238 g Magnesium stearate [2] ...........< 0.......................... 3................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Magnesium Carbonate Tablets (260 mg) 1....................................................

................100 g Ludipress [1] .....5 % BASF Pharma Ingredients Generic Drug Formulations 2001 .........biplanar Hardness.........................2......................8 mm sieve and press with low compression force..................0........196 g Magnesium stearate [2] ................................................................................. Formulation Mebendazole......................... Tablet properties Weight ...................73 N Disintegration .... Manufacturing (Dir ect compression) Mix all components........................... pass through a 0........................... 3......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Mebendazole Tablets (100 mg) 1........................4 g 2.......................294 mg Diameter ......................................................12 mm Form ......2 min Friability.................

.87 N Disintegration ................................................................8 mm sieve..................21 Talc [10] ...............................................1 g g g g g g g g 2.................................. Manufacturing (Dir ect compression) Pass all components through a 0......... mix and press with low compression force..< 1 min Friability.............8 Aerosil 200 [4] ...............biplanar Hardness......13 Kollidon CL [1] .............. Tablet properties Weight ............. Formulation Meprobamate.................2......................1 Calcium arachinate [2] .....................................................................551 mg Diameter ..............................................................12 mm Form ........0.............................76 Kollidon VA 64 [1] ............................30 Avicel PH 101 [5] ........9 % BASF Pharma Ingredients Generic Drug Formulations 2001 ............................................................400 Phenobarbital............................... DC 1............................... 3..........................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Meprobamate + Phenobarbital Tablets (400 mg + 30 mg).......

...............................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Meprobamate Tablets (400 mg).......20 Talc [10] ......biplanar Hardness.........90 N Disintegration.........................6 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..................... Manufacturing (Dir ect compression) Mix all components...........................................................................................................................3 g g g g g g g 2.............................................................................................. 3...........< 10 min Friability .8 mm sieve and press with high compression force (20 KN). Tablet properties Weight ................................80 Corn starch [3] ......................30 Kollidon VA 64 [1] ........7 Magnesium stearate [2] ..... Formulation Meprobamate.. pass through a 0.............................................20 Kollidon CL [1] .........2......... DC 1.....................................0.400 Avicel PH 101 [5] .....560 mg Diameter ................................12 mm Form ...............

.....................................................................................................................10 g Magnesium stearate [2]......................................................– Kollidon 30 [1].........................................................625 mg Diameter ......5 g Talc [10] ....... pass through a 0..............................biplanar Hardness........10 g Aerosil 200 [4]....................... 2 Weight .........3 % 654 mg 12 mm biplanar 62 N 2 min 1% BASF Pharma Ingredients Generic Drug Formulations 2001 . 2 Metamizol sodium .............100 g Avicel PH 101 [5].....................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Metamizol Tablets (500 mg) 1......– 500 g – 100 g 15 g 25 g – 1g 8g 1g 2................... Formulations No...0.......... 1 No....– Calcium arachinate [2] .......5 min Friability ..........................12 mm Form ............................................... Tablet properties No...................5 mm sieve and press with low compression force............................ 1 No...................2.......120 N Disintegration ....... Manufacturing (Dir ect compression) Mix all components............................................ 3..................– Kollidon CL [1] ........................................500 g (= Dipyrone) Ludipress [1] .........................................................................................

307 mg Diameter ...................... 20–25 ºC) Weight ........................................... 3....................8 mm sieve and press with low compression force.................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Methyl Cysteine Tablets (100 mg) 1.............................................. Tablet properties Weight ..................................0.......biplanar Hardness..........100 g Ludipress [1] ............................................................... Physical stability (12 months..........3 % 4.....8 mm Form .......3 mg Menthol ...........................2 – 3 min Friability............4 mg 2............................55 N Disintegration... Formulation Methyl cysteine hydrochloride .................................85 N Disintegration.........2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......................... pass through a 0.......................2.........2 – 3 min Friability............0.......................307 mg Hardness. Manufacturing (Dir ect compression) Mix all components.................................................................................................200 g Magnesium stearate [2]...........

...10....................................................................100 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...2... 3............................ Tablet properties Weight .....0 g Ludipress [1] ..................... Physical stability (18 months..0.... Formulation Metoclopramide hydrochloride ..........8 mm sieve and press with medium compression force........................35 N Disintegration (gastric juice) .................................................3 min Friability ...............100 mg Diameter ...........1% Dissolution (15 min) .......100 mg Hardness...................................6 mm Form ............................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Metoclopramide Tablets (10 mg) 1................35 N Disintegration (gastric juice) ..100 % 4.............................................................................biplanar Hardness........ 20–25 ºC) Weight ...............5 g Magnesium stearate [2]........89.0..................................... pass through a 0.3 min Friability .....0...................................... Manufacturing (Dir ect compression) Mix all components.......................1% Dissolution (15 min) .......5 g 2..........................

..... pass through a 0...............biconvex Hardness. 3..............645 mg Diameter ................................................ Tablet properties Weight ................................. Manufacturing (Dir ect compression) Mix all components..1% BASF Pharma Ingredients Generic Drug Formulations 2001 .................................25 Kollidon CL [1]..< 0...........15 Aerosil 200 [4] ..................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Metronidazole Tablet Cores (400 mg) 1...........................2...87 N Disintegration.............................5 Polyethylene glycol 6000................................50 g g g g g g 2............................................................................400 Avicel PH 102 [5] ................ Formulation Metronidazole ......1 – 2 min Friability ..........12 mm Form .... powder [6]............................................150 Kollidon VA 64 [1] .........8 mm sieve and press with high compression force (25 – 30 kN)....................................

.......................... pass through a 0..... Manufacturing (Dir ect compression) Mix all components..............................8 mm sieve and press with high compression force (25 – 30 kN).......1% BASF Pharma Ingredients Generic Drug Formulations 2001 ......................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Metronidazole Tablets (200 mg) 1............................................................................. Tablet properties Weight ..................1 – 2 min Friability ......................................6 Kollidon CL [1].........................................2......< 0........................................5 Magnesium stearate [2] ...........10 Aerosil 200 [4] ..200 Kollidon 30 [1] .................................5 g g g g g g 2.................................................133 N Disintegration...............................................biplanar Hardness ..........................200 Avicel PH 101 [5] ..426 mg Diameter ................................ 3.12 mm Form .............. Formulation Metronidazole .....

/g (BASF) Vitamin D dry powder ............0 Dibasic calcium phosphate [9]..............................000 i..../g (BASF) Thiamine mononitrate (BASF) ......8 Nicotinamide .1...2 Riboflavin (BASF).....0 Ferrous fumarate .......................0 (BASF) Ascorbic acid........12...............2........3 % BASF Pharma Ingredients Generic Drug Formulations 2001 ............................. Tablet properties Weight ..........60..............................4..0 Vitamin E acetate dry powder SD 50 .....0 granulated with 5 % Kollidon 30 [1] Calcium carbonate...... u.......11 mm Form ..................50... powder (BASF) ...................5 g g g g g g g g g g g g 2.......biplanar Hardness........................ 3.......................75 N Disintegration (water).......2 – 3 min Friability....000 i............. Manufacturing (Dir ect compression) Mix all components........500 mg Diameter ...........45............. pass through a sieve and press to tablets.................0 100.....0 500......1..........................1...5.200.................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin + Calcium + Iron Tablets (1 RDA of Vitamins) 1..................0 Aerosil 200 [4] .......0 Avicel PH 101 [5] ..................................................... Formulation Vitamin A acetate dry powder ..................... u.....................0.. .......................125..................................................2............

.........12 mm Form ............2...................0 g Thiamine mononitrate (BASF) ...............8 mm sieve......0 g Magnesium stearate [2].. pass through a 0...............000 i......3......................2.......0 g Orange flavour.................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........5 g Calcium D-pantothenate (BASF) .......10.2. Manufacturing (Dir ect compression) Mix all ingredients.............................2 g Nicotinamide .....2......12 min Friability.........16.............31.......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin + Carbonyl Iron Tablets (1–2 RDA of Vitamins) 1.. powder (BASF) ........................ 3......10...............0 g Ascorbic acid.. Ludipress [1]...../g (BASF) ............................... Tablet properties Weight ..6...500 mg Diameter ......................2 g Saccharin sodium.............................................................................1% .....................................0....................0 g Carbonyl iron powder OF (BASF) ................................ mix and press with high compression force (20 kN)............. dry powder 0..0 g (BASF)..........311..............2 g Cyanocobalamin...................69 N Disintegration..............2 g Riboflavin (BASF)....0 g Vitamin E acetate dry powder SD 50 ............. Formulation Vitamin A acetate dry powder 500...11..........................biplanar Hardness...........85..................................................7................................5 g 2........2............... u..5 g Pyridoxine hydrochloride (BASF)....

..........0 Pyridoxine hydrochloride (BASF) ....................... 3.......0 Magnesium stearate [2] .........0 Avicel PH 102 [5] ......................................6.....22..... Manufacturing (Dir ect compression) All ingredients were passed through a 0.......1......60.............0 Croscarmellose [5] .....165..........7 Riboflavin (BASF).............................................12 mm Form ...6...6...............biplanar Hardness ... cryst...... Formulation Beta carotene dry powder......0........ high density type ......................... powder (Merck) ....9 Zink oxide (Merck) .......................................................0 Calcium D-pantothenate (BASF) ...0 Vitamin E acetate dry powder 50 % (BASF) ..... Tablet properties Weight ................................16.......12.........72...1% BASF Pharma Ingredients Generic Drug Formulations 2001 ....0 g g g g g g g g g g g g g g g g g g g g 2...9 Nicotinamide (Degussa) ........2...............................2 Ascorbic acid..................0 Syloid ® 244 FP (Grace) ...............0 Stearic acid [7] ............76.....54.18..........32...............1..8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin + Minerals Tablets with Beta Carotene (1 RDA of Vitamins) 1...................1193 mg Diameter ..550.....................112 N Friability ........2...........66................8 mm sieve..... blended in a Turbula mixer and then compressed with medium to high compression force......7 Magnesium oxide.....3 Dicalium phosphate............. (BASF).................5 Manganese sulfate (Merck) ............2..........8 (Merck) Copper II oxide......................6.......7 Potassium chloride (Baker) .............. DI-TAB [9] .................................................................................5 (BASF) Thiamine mononitrate (BASF) .... Betavit 20 % ...........0 Ferrous fumarate ..................................................

% 90 80 70 20-25∞C 40∞C/75% r. 60 50 0 20 40 Weeks BASF Pharma Ingredients Generic Drug Formulations 2001 60 . Stability of be ta carotene Because beta carotene may be the most sensitive vitamin in this formulation it’s stability at room temperature and at 40°C/75 % relative humidity was determined 100 Beta carotene content.h.Multivitamin + Mineralsablets T with Beta Carotene (2 RDA of iVtamins) page 2 4.

........0 Calcium D-pantothenate (BASF) .0 22....................0 80..0 No.........0 Thiamine mononitrate (BASF) ...0 2...0 50......12.........9 Pyridoxine hydrochloride (BASF) ....... 1 Beta carotene dry powder 10 % ........................0 3...2.......................2................................ Manufacturing (Dir ect compression) Mix all components....0 6................................ Formulation No.............5....0 3......................0 5...........0 Cupric sulfate.82. BASF Pharma Ingredients Generic Drug Formulations 2001 ....13.........8 Potassium chloride ....22..5 Riboflavin (BASF)....0 14..... pass through a 0......0 g g g g g g g g g g g g g g g g g g 550..................2...........8 mm sieve and press with high compression force.0 Ferrous fumarate .......0 3.......37................................150.2 Zinc sulfate ..........................2...110....550......0 160.0 Ascorbic acid for direct compression .......57........0 50....................0 37...57........5 Manganese sulfate ............................. dibasic [9] ..........0 100.......................0 Avicel PH 102 [5] ...... 2 g g g g g g g 50........50.........0 12..0 g g g g g g g g g g g 2....................2................5....166..0 Magnesium oxide .....7 Magnesium stearate [2] .........................0 (Roche) Calcium phosphate..................................0 Kollidon CL [1] ......0 Nicotinamide .....0 60.....0 Stearic acid [7] .......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin + Minerals Tablets with Beta Carotene (2 RDA of Vitamins) 1...........

........... 1 No..94 N Disintegration (water) ...........................................Multivitamin + Mineralsablets T with Beta Carotene (2 RDA of iVtamins) page 2 3.............................................................1% 1205 mg 16 mm biplanar 88 N < 1 min < 0.......................... 2 (20–25°C) Storage time Beta Carotene B1 B2 B5 B6 6 Months 12 Months 100 % 92 % 98 % 96 % 98 % 92 % 100 % 97 % 99 % 96 % 5.......... Chemical stability of formulation No........................ Remark These tablets could be commercialized in Europe as dietary food because all components are allowed for this application... 2 Weight ........... BASF Pharma Ingredients Generic Drug Formulations 2001 C 95 % 94 % ..................................................1% 4.....< 1 min Friability .......16 mm Form ...................1300 mg Diameter ....biplanar Hardness ..................... Tablet properties No.................

...... crystalline [10] ................1.. dry powder.............7...000 i....../g (BASF) .. BASF Pharma Ingredients Generic Drug Formulations 2001 ........... crystalline................3........0 Cyclamate sodium .... dry powder ............... powder (BASF) ..............0 Aerosil 200 [4] ..............1% dry powder .......60...................0 Sucrose............................... u..1.........2...... u..200...2 Riboflavin (BASF)...................30.0 Raspberry flavour....5 (BASF) Ascorbic acid............1........ Formulation Vitamin A acetate dry powder.....5.6........... Manufacturing (Dir ect compression) Mix all ingredients........0 g g g g g g g g g g g g g g g g g 2............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin Chewable Tablets for Children 1........... dry powder......./g (BASF) Thiamine mononitrate (BASF) ......2.................31.............................................0 Pyridoxine hydrochloride (BASF)......20...8 mm sieve and press with medium to high compression force (20 kN)............ pass through a 0....000 i.......2 Nicotinamide .............0 dry powder SD 50 (BASF) Sorbitol...........0 Kollidon VA 64 [1] ...0 Passion fruit flavour.....0 500........1.......8 Cyanocobalamin 0..6....0 Vitamin D 3 acetate dry powder 100.0 Orange flavour.0 Vitamin E acetate .............200.....20..........

..................................0....................100 N Disintegration ....................................................................................12 mm Form ..............2 % BASF Pharma Ingredients Generic Drug Formulations 2001 page 2 ..............7 min Friability.....Multivitamin Chewableablets T for Childr en 3............................................................................... Tablet properties Weight ....................................biplanar Hardness ....575 mg Diameter .

.............91 N Disintegration (water) ... Tablet properties Weight.biplanar Hardness..............0 Sodium bicarbonate ....... mix and press with high compression force at a maximum of 30 % of relative atmospheric humidity............0 Ascorbic acid.20 mm Form .......85....40....... powder (BASF) ......0 CWD G/Y (BASF) Dry Vitamin E acetate 50 % DC (BASF)..........6........600...22.0 Pyridoxine hydrochloride (BASF).....................6 % BASF Pharma Ingredients Generic Drug Formulations 2001 . powder [6] .....................................0 Thiamine mononitrate (BASF) ...........0 Calcium D-pantothenate (BASF) ..........0...........1850 mg Diameter ......................2...........................8 mm sieve.2..................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin Effervescent Tablets I..............................0 Riboflavin C (BASF) .......2........477............................60.......0 Tartaric acid ........0 Orange flavour (Dragoco) .............0 Nicotinamide ..1% dry powder ...... DC (1 – 2 RDA of Vitamins) 1.......0 Ludipress LCE [1] ...........90.....23............400............................................0 g g g g g g g g g g g g g g g 2...........11.....................0 Cyanocobalamin 0.......... Manufacturing (Dir ect compression) Mix all components........2............ Formulation Lucarotene Dry Powder 10 % ..........................0 Polyethylene glycol 6000............30....0 Apartame (Searle) ..........................1 min Friability ................... 3............... pass through a 0...........................

............ Manufacturing (Dir ect compression) Mix all components.... powder [6].. crystalline .8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin Effervescent Tablets II.......2.......5 6...............0 g Vitamin A palmitate dry powder 325000 i...600....0 g 0.................0 200...............0 g 200.....200............30..0 g Ludipress [1] ..6....0 g No.....500.........0 g Vitamin E acetate dry powder 50 % ...5..............................0 g 2......0 g 50..0 g Cyanocobalamin 0....5 g Riboflavin (BASF).............................................5...5 g 40................0 g Flavours (Firmenich) ..........0 g 200.0 30..5 60........0 g 500... powder (BASF) ..5 g Nicotinamide ....0 g Fructose ................5 5....0 g Ascorbic acid........... sieve through a 0....... BASF Pharma Ingredients Generic Drug Formulations 2001 ................0 g 70...0 g Calcium D-pantothenate (BASF).....200.... 2 5....... powder .... powder ...........110....100......0 g Polyethylene glycol 6000.................70.0 g 100....0 g 500..30................... u...5 g Pyridoxine hydrochloride (BASF) ...........0...0 g Citric acid.0 g Sucrose.....40....0 g – 500..– Tartaric acid....... 1 Thiamine mononitrate (BASF) .. DC (3–4 RDA of Vitamins) 1............8 mm screen and press with high compression force at maximum 30 % relative atmospheric humidity......5 g Cyclamate sodium./g CWD (BASF)....................200.............0 g Saccharin sodium ........ Formulations No......................0 g g g g g g g 30.0 g Sodium bicarbonate .....20.....400......60...........0 20..........................................................1% dry powder .......

...................................93 % Vitamin B 6 ....Multivitamin Ef fervescent T ablets II.. Chemical stability of formulation No.1.. 2 Weight ...............................................2200 mg Diameter ........................1 – 2 min Friability ..........98 N Disintegration (water)............................................................................. DC (3–4 RDA ofitamins) V page 2 3....... 1 No..................... HPLC) Vitamin B 1 ................................................................................88 % Vitamin A ..........................> 95 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..................89 % Vitamin B 12 ......................................biplanar Hardness .................. Tablet properties No..................4 % 4.................................................. 1 (after 12 months at 20–25 ºC...20 mm Form ......................................................0 % 2495mg 20 mm biplanar 197 N 2 min 0.......79 % All other vitamins ................

B 2 ...........conform to DAB BASF Pharma Ingredients Generic Drug Formulations 2001 .......................11 mm Form ................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin Tablet Cores with Beta-Carotene (1–2 RDA of Vitamins) 1. Formulation Vitamin mixture (BASF...........0 % Content uniformity of Vitamin B 1 ............................ B 6 and folic acid ...3.......................................270.....................................biconvex Hardness....1 g Magnesium stearate [2]........................3 g 2.................................8 mm sieve.......................................... 3............................. mix and press with high compression force....2. see “Remark”).......13 min Friability .....69............459 mg Diameter ...97 N Disintegration (water)............2 g Ludipress [1] ....................... Tablet properties Weight .......... Manufacturing (Dir ect compression) Pass all components through a 0......

..19 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..........50 % Thiamine mononitrate.......15 % Cyanocobalamin gelatin coated 1% ...............91% Folic acid .....1.....................40 % Phytomenadione dry powder 5 % GFP.............../g .........................1.11.28...1...24 % Riboflavin ..........11............. u........0......50 % Calcium D-pantothenate ........................000 i....../g Beta carotene dry powder BetaVit 10 % ......................Multivitamin a Tblet Cores with Beta-Carotene (1–2 RDA of itamins) V page 2 4.............38.............09 % Ascorbic acid..1.......86 % D-Biotin....20 % Vitamin D 3 dry powder 100...................000 i..........91% Pyridoxine hydrochloride ............. 1% trituration .............. Remark The used vitamin mixture had the following composition: Vitamin A acetate dry powder ........96 % Nicotinamide..1.... u.........................0............................................0.................27 % 500.....0....2.76 % Vitamin E acetate dry powder 50 DC...

............2 2.– Magnesium stearate [2] .11... DC (1–2 RDA of Vitamins) 1......................2 6... u......– (Rettenmaier) Kollidon VA 64 [1]..................../g (BASF) ......321............................000 i....0 g Orange flavour ..0 85.......................2 g Ribolfavin (BASF).......0 g 21..........0 g 500..0 31.....2 2....... Thiamine mononitrate (BASF) .........0 g Ascorbic acid...2 g Nicotinamide .....5 2.....................1% dry powder .... pass through a 0.......... 1 No....5 g Calcium D-pantothenate (BASF) .16.........2....0 g (BASF) Ludipress [1] .................................85............0 3..............5 g g g g 2. Vitacel ® ..2......0 g 2.........2.......0 g Microcrystalline cellulose.............................5 g 10..................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin Tablets................. Manufacturing (Dir ect compression) Mix all components.........0 g Vitamin E acetate dry powder SD 50 ......2................................3........2 16....5 11.............2 g Saccharin sodium ..... Formulation No...2...........7....... mix and press with medium compression force (15 kN)........2 g Cyanocobalamin 0... powder (BASF)....................6.... BASF Pharma Ingredients Generic Drug Formulations 2001 .5 g Pyridoxine hydrochloride (BASF) ...........31... 2 Vitamin A acetate dry powder .......0 7..10..8 mm sieve....0 g g g g g g g g – 300.....

.............. Chemical stability of formulation No......................................88 % Vitamin B 6 ............ DC (1–2 RDA of itamins) V page 2 3.....12 mm Form ... Tablet properties No............................................................................ All other vitamins ..........................0..............94 % Calcium D-pantothenate ......2 % 501 mg 12 mm biplanar 195 N 6 min < 0..................................................... 1 (after 12 months at 20–25 ºC) Vitamin A ............... 2 Weight ..................92 % Vitamin B 12 ...............Multivitamin a Tblets. 1 No.......68 N Disintegration (water) ......................................................................................................................1% 4.........500 mg Diameter .............biplanar Hardness ..............> 95 % BASF Pharma Ingredients Generic Drug Formulations 2001 90 % ..................................................5 min Friability ..........................

...5.............. mix and press with low compression force..........7 Nicotinamide ................5 Riboflavin (BASF)....0 Pyridoxine hydrochloride (BASF)......0 (BASF) Ludipress [1] ..........000 i........20......................7 min Friability ...............0.....................4.8 mm Form ..............0 % BASF Pharma Ingredients Generic Drug Formulations 2001 .................1.........5 (BASF) Folic acid ..............0......................biplanar Hardness............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin Tablets for Dogs 1.......2....../g (BASF) Thiamine mononitrate (BASF) ..........20.................. 3...........................................8 mm sieve..........................................2........... Tablet properties Weight .0 Vitamin E acetate dry powder SD 50 ....... u........................0 Magnesium stearate [2]..............0...0......................................... Formulation Vitamin A + D 3 dry powder ................5 Cyanocobalamin gelatin coated 1% ........0 500.......0 Calcium D-pantothenate (BASF)......................................196................05 Choline bitartrate .....................0..........................................000 + 50................250 mg Diameter ....0 g g g g g g g g g g g g 2...... Manufacturing (Dir ect compression) Pass all components through a 0..77 N Disintegration (water) ..........

..0 g Saccharin sodium .....0 g Riboflavin (BASF)..........................................2 6....2.....85.... Manufacturing (Dir ect compression) Mix all components..........2...0 7..0 g Pyridoxine hydrochloride (BASF) ...7.....2....0 g Nicotinamide ...1% dry powder ............0 85......... 1 No.....321.......0 g Kollidon VA 64 [1]....................0 g Vitamin E acetate dry powder SD 50 ..10......0 g g g g g g g g 210....2............0 g Ascorbic acid.0 2..........2.... Beta Carotene dry powder 10 % ..– Magnesium stearate [2] ................5 2..................................... BASF Pharma Ingredients Generic Drug Formulations 2001 ..16..0 32.............0 g Cyanocobalamin 0......0 3..0 g 2..3...0 g (BASF) ......................8 mm sieve.............2 2........................ pass through a 0............11..5 11......... 2 Beta Carotene dry powder 10 % Betavit ® ....................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin Tablets with Beta Carotene (1–2 RDA of Vitamins) 1..................5 g g g g g 2............................31.............6..0 g Orange flavour ............. Formulations No...........0 g – 70..... mix and press with medium compression force............................0 g Calcium D-pantothenate (BASF) ...... powder (BASF)..........2 6...............0 7......– Pharma (BASF) Thiamine mononitrate (BASF) ................0 g (BASF) Ludipress [1] ...........

............. Tablet properties Weight Diameter Form Hardness Disintegration Friability No................biplanar .....................5 min .. 1 could be commercialized in Europe as dietary food because all components are allowed for this application........12 mm ...... 1 No.....................................1% 449 mg 12 mm biplanar 47 N 10 min 0............. 2 .< 0...... BASF Pharma Ingredients Generic Drug Formulations 2001 .................................. Chemical stability of vitamins in formulation No....72 N (water) .........................................508 mg . 1 (20–25 °C... Remark Formulation No...15 % 4.............................................Multivitamin a Tblets with Beta Carotene (1–2 RDA of itamins) V page 2 3. HPLC) Storage time Beta Carotene B1 B2 6 Months 12 Months 100 % 100 % 100 % 90 % 98 % 87 % B5 B6 100 % 98 % 100 % 97 % C 96 % 94 % 5.........

............................25 Magnesium stearate [2].. mix and press with high compression force...................... Tablet properties Weight .................................................1000 Aerosil 200 [4] .5 Ludipress [1] ................................. Formulation Vitamin mixture (BASF................. see “Remark”) ........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Multivitamin Tablets with Copper and Zinc 1.150 Avicel PH102 [5] ..16 mm Form ............biplanar Hardness...............................................................................................................................1350 mg Diameter ..............10 g g g g g g g 2.......0 % BASF Pharma Ingredients Generic Drug Formulations 2001 .......................... Manufacturing (Dir ect compression) Pass all components through a 0...........................62 N Disintegration (water) ....................1..........................................2... 3..............8 mm sieve....3 min Friability....................................................10 Talc [10] ..........................120 Kollidon VA64 [1] ..

........0...9 % Riboflavin 100 ..................................2 % Cyanocobalamin gelatin coated 0...............................2..................................9...10...............................................1% Calcium D-pantothenate .....................3 % Zinc sulphate .....9 % Pyridoxine hydrochloride .....0............3......1% Ascorbic acid fine powder ..............4 % Nicotinamide .....2..4 % Vitamin E acetate dry powder 500 SD .........1% ..................1....... Remark The used vitamin mixture had the following composition: Thiamine mononitrate.6....6 % Folic acid .1% Cupper oxide......Multivitamin a Tblets with Copper and Zinc 4..63...............................0 % BASF Pharma Ingredients Generic Drug Formulations 2001 page 2 .....0......................................

................6 Aerosil 200 [4] ........10 g g g g 2........12 mm Form ............. Tablet properties Weight ...........................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Neomycin Tablets (250 mg) 1.........biplanar Hardness........................................................................76 N Disintegration.......... Manufacturing (Dir ect compression) Mix all componnents...........334 Magnesium stearate [2] ...................600 mg Diameter ............. pass through a 0.......0............... 3......................................14 min Friability...2....250 Ludipress [1] ..............................................................................................8 mm-sieve and press to tablets with low compression force............8 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......... Formulation Neomycin sulfate ................................................

.........................5........ Formulation Nicotinic acid (Lonza)..............................................................5 Aerosil 200 [4] ............................5 mm sieve........2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...................419 mg Diameter ..........................2.....................0 Polyethylene glycol 6000.......................0 Kollidon CL [1] ......................1...............................................12 mm Form ........................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Nicotinic Acid (= Niacin) Tablets (200 mg) 1.............10.........................................3.............0 Magnesium stearate [2] .............................. Manufacturing (Dir ect compression) Pass all componts through a 0...biplanar Hardness......0 Ludipress [1] ................200..................0 g g g g g g 2.................... 3................................. powder [6]..... Tablet properties Weight .....200...1 min Friability ..... mix and press with very low compression force....0...144 N Disintegration ..

......53..........................................................biplanar Hardness..............5 g g g g 2..........................................< 1 min Friability...0 Kollidon CL [1] ............26...........0 Ludipress [1] ..................0.................5 Magnesium stearate [2].............................2.................... 3....... Tablet properties Weight ...........63 N Disintegration .............................................1.........................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Nitrendipine Tablets (25 mg) 1........0........ Manufacturing (Dir ect compression) Pass all components through a 0..................6 mm Form .........82 mg Diameter ..3 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........... Formulation Nitrendipine...............................................................5 mm sieve................ mix and press with low compression force.......

...............85 N Disintegration.............................................biplanar Hardness.............................. 3.307 mg Diameter ....................................2 Aerosil 200 [4] ...................2......................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Nitrofurantoin Tablets (100 mg) 1.................... pass through a 0. Manufacturing (Dir ect compression) Mix all components.............100 Ludipress [1] ....................................................................................8 mm sieve and press with low compression force...........................................1 – 2 min Friability... Formulation Nitrofurantoin .....................200 Magnesium stearate [2] .................................. Tablet properties Weight .....0....12 mm Form ...........3 g g g g 2...............................5 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..................

..8 mm sieve and press with very low compression force.........................8 mm Form .............................biplanar Hardness ..............0........0 2..........110............3 g g g g 100 mg 110........ Tablet properties 50 mg 100 mg Weight .............1....................................................................0 220..................6 % 339 mg 10 mm biplanar 66 N 9 min 0..........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Nystatin Tablets (50 mg and 100 mg) 1....................1...........................................................0 Aerosil 200 [4] ..........................................175 mg Diameter . Manufacturing (Dir ect compression) Mix the components........................................0 Magnesium stearate [2] ...................0 2.10 min Friability ............5 g g g g 2...................54 N Disintegration ...............................2.............55.... Formulations 50 mg Nystatin ....... pass through a 0...........0 Ludipress [1]..........3 % BASF Pharma Ingredients Generic Drug Formulations 2001 ....... 3...

............71 N Friability ..289 mg Diameter ....... BASF Pharma Ingredients Generic Drug Formulations 2001 ..................................2........ – These tablet cores could be coated with an enteric coating of Kollicoat MAE 30 D [1] (see chapter 3).......140.. 3...................2....biconvex Hardness .........0 Kollidon VA 64 [1] .. This fish oil consists of about 30 % EPA+DHA............................ Remarks – The dry powder Omega Fatty Acids Dry N-3 contains 25 % fish oil.< 0..............9 mm Form .......0 g g g g 2.4 Magnesium stearate [2]... Tablet properties Weight .........0 Avicel PH 101 [5] ....8 mm sieve..................................................................................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Omega Fatty Acids Tablet Cores (10 mg EPA + DHA) 1............. Formulation Omega Fatty Acids Dry N-3 (BASF) ............................ mix and press with high compression force..........8.... Manufacturing (Dir ect compression) Pass all components through a 0.....140........................15 4.

............. Tablet properties Weight ...........2........... pass through a 0...........0.......4 min Friability .................12 mm Form ...................................................................................................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Oxytetracycline Tablets (250 mg) 1.............. 3.....................................8 mm sieve and press with very low compression force............6 g 2......................86 N Disintegration .......................230 g Magnesium stearate [2] ...................... Formulation Oxytetracycline hydrochloride . Manufacturing (Dir ect compression) Mix all components..............................250 g Ludipress [1] ......biplanar Hardness....495 mg Diameter .......................................

........................8 mm sieve and press with low compression force..........355 mg Diameter ..< 0........................................... Enteric coating See Chapter 3.............................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Pancreatin Tablet Cores (30 mg) 1...10 Magnesium stearate [2] ............................ Tablet properties Weight ............4 – 5 min Friability ...............................308 Kollidon CL [1]...biconvex Hardness................................ Manufacturing (Dir ect compression) Mix the components..................................................................30 Ludipress [1] .....8 mm Form ................................................1% 4....76 N Disintegration ................. BASF Pharma Ingredients Generic Drug Formulations 2001 .. 3............................... pass through a 0.......... Formulation Pancreatin (BASF) ......2 g g g g 2...2.......................................

........................................................9 mm Form ........... Formulation Pancreatin (BASF).. 3.......56 Magnesium stearate (Merck) ................. Manufacturing (Dir ect compression) Mix the components and press with high compression force...........177 N Friability ................127 Lactose monohydrate [8] ..............1% 4............................ Properties of the cor es Weight .............................................................. BASF Pharma Ingredients Generic Drug Formulations 2001 ........................< 0........324 mg Diameter ...................................... Enteric coating See Chapter 3...............3 g g g g g g 2.............................................biconvex Hardness .2 Avicel PH 101 [5] .....130 Cholic acid...............................2 Aerosil 200 [4] ........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Pancreatin Tablet Cores (130 mg) 1......................................................2...................

.......... Tablet properties Weight .......... 3................... BASF Pharma Ingredients Generic Drug Formulations 2001 ...............................615 mg Diameter .................................................................biconvex Hardness......................11mm Form .2.. Enteric coating See Chapter 3......... Formulation Pancreatin (BASF) ........300 Ludipress [1] ....................................................3 g g g g 2............................290 Kollidon CL [1] ......... pass through a 0.....................25 Magnesium stearate [2] .8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Pancreatin Tablet Cores (300 mg) 1...................... Manufacturing (Dir ect compression) Mix the components..............1% 4....................................................74 N Friability .....< 0........8 mm sieve and press to tablets with low compression force..................

....................... granulated with 3 % of povidone ..........1.... 1 No.............................................................. 3.................................................................................2.....– Citric acid................ fine granules (Jungbunzlauer) ........................................... Manufacturing (Dir ect compression) Mix all components............. 1 Paracetamol................................500 g Sodium bicarbonate (Merck)........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Paracetamol (= Acetaminophen) Effervescent Tablets (500 mg) DC 1............................... Tablet properties Weight Diameter Form Hardness Disintegration Friability No...8 % 4......600 g Ludipress LCE [1] . 2 ..................125 N ..............500 g Paracetamol........ BASF Pharma Ingredients Generic Drug Formulations 2001 ..............20 mm ..........1-2 min ...... Formulations No.............. Remark The sedimentation of paracetamol after the dissolution of the tablet in water is much better using the povidone granulated paracetamol................................ add the lubricant and press with high compression force of 25-30 kN........................................... granular (BASF) .700 g Lutrol E4000 F [1] ... 2 525 500 600 600 100 – g g g g g 2.. pass through a 0............................8 mm sieve..........biplanar ..................2 % 2340 mg 20 mm biplanar 153 N 1-2 min 0....80 g No....2384 mg ....

..........8 mm and press with high compression force......biplanar Hardness....... powder [6] ....................................683 mg Diameter ..56 N Disintegration ...............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Paracetamol (= Acetaminophen) + Caffeine Tablets (500 mg + 50 mg) 1...500 Caffeine (BASF) ........................................................................12 mm Form ...................... Tablet properties Weight ...50 Avicel PH 101 [5] ...... 3.... Manufacturing (Dir ect compression) Mix all components.....2........... Remark If the flowability of the powder mixture for tabletting is not high enough some Aerosil 200 [4] should be added..........< 1 min Friability.... 15 min ...............9 % Dissolution....20 Polyethylene glycol 6000.................... BASF Pharma Ingredients Generic Drug Formulations 2001 .................................. crystalline (BASF) ............10 g g g g g g 2.................................10 Kollidon CL [2] ...0....................................................................... Formulation Paracetamol............ pass through a sieve of 0..........................90 Kollidon 30 [1] ............................................91% 4......................................

...................................... powder < 300 µm .......................................................................................0...........................................7 % BASF Pharma Ingredients Generic Drug Formulations 2001 ....250 Ibuprofen ....................12 mm Form .......................... 3.....biplanar Hardness..................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Paracetamol (= Acetaminophen) + Ibuprofen + Orphenadrin Tablets (250 mg + 200 mg + 100 mg) 1....5 Aerosil 200 [4] .... Manufacturing (Dir ect compression) Pass all components through a 0............100 Ludipress [1] ....................200 Magnesium stearate [2] ...................................................2............... Tablet properties Weight ....................................................5 g g g g g g 2.......761 mg Diameter ............6 min Friability..............200 Orphenadine hydrochloride .................. Formulation Paracetamol...5 mm sieve.......................74 N Disintegration ......... mix and press with high compression force...................

................................54 N Disintegration ........5 g Aerosil 200 [4] ..................................................................12 mm Form ....................8 mm sieve..........................< 1 min Friability.....0...................................... 2...465 mg Diameter ..........................200 g Phenprobamat .....35 g Kollidon VA 64 [1] .........5 mm ....................q..8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Paracetamol (= Acetaminophen) + Phenprobamat Tablets (200 mg + 200 mg) 1.........biplanar Hardness.......... Manufacturing (Dir ect compression) Pass all components through a 0................................................... Formulation Paracetamol..................200 g Avicel PH 101 [5] ............................ powder < 0................................................s........ mix and press with high compression force.......................................20 g Kollidon CL [1].........8 % BASF Pharma Ingredients Generic Drug Formulations 2001 .. 3......10 g Magnesium stearate [2] ...........................2......................... Tablet properties Weight .........

.............7 % Dissolution......................35 g Kollidon CL [1] .............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Paracetamol (= Acetaminophen) Tablets (500 mg) 1.6 min Friability .................. 1 No................................................500 g (Synopharm) Avicel PH 102 [5] ................ pass through a 0........... 2 Weight .....................................biplanar Hardness ....................................... Formulations No.....................................................60 N Disintegration ............... powder [6] .. Tablet properties No.2..............4 % 73 % 86 % BASF Pharma Ingredients Generic Drug Formulations 2001 . 10 min ............................................................ 1 No....................98 % 703 mg 12 mm biplanar 87 N 1 min 0.......4 g 500 g 150 g 20 g 15 g – 15 g 2g 2........ crystalline ..3 g Polyethylene glycol 6000.......... mix all other components....– Aerosil 200 [4] .............................21 g Magnesium stearate [2] ... Manufacturing (Dir ect compression) Pass the lubricant through a 200 µm sieve.......137 g Kollidon VA 64 [1] ... 3.................12 mm Form ......................8 mm sieve..699 mg Diameter ................. add the lubricant and press with high compression force of 25 – 30 kN... 2 Paracetamol......................................................0........................................84 % 30 min .................

8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Paracetamol (= Acetaminophen) Tablets for Children (200 mg) 1...........4 % BASF Pharma Ingredients Generic Drug Formulations 2001 ....................13 Kollidon CL [1] .................................................0................ Formulation Paracetamol (BASF) ......................................2 g g g g g 2.............65 N Disintegration ...........401 mg Diameter ......168 Kollidon VA 64 [1] ...... mix and press with medium compression force.....................................................................6 Magnesium stearate [2] ..........210 Avicel PH 101 [5] ..2.....8 mm sieve................................................................. Tablet properties Weight .......................................................................< 1 min Friability..........................biplanar Hardness......... 3................ Manufacturing (Dir ect compression) Pass all components through a 0.........................12 mm Form ...........

...8 mm sieve....................................................................................... BASF Pharma Ingredients Generic Drug Formulations 2001 .........................................................12 mm Form .......... mix and press with medium compression force........................> 3 Aerosil 200 [4] .604 mg Diameter ...................0.......281 Magnesium stearate [2] ..................... Manufacturing (Dir ect compression) Pass all components through a 0..................................................................... Remark The amount of Ludipress and/or corn starch could be reduced......2...........146 N Disintegration (water).......2 % 4.........................................35 Ludipress [1] ..................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Phendimetrazin Tablets (35 mg) 1..........biplanar Hardness ...> 3 g g g g g 2..................................... Tablet properties Weight ..........281 Corn starch [3] .......... Formulation Phendimetrazin ..........3 – 4 min Friability....... 3..........

.............................15 min Friability ..................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Phenindione Tablets (50 mg) 1........................biplanar Hardness .........2..............................2 g 2..................165 g Magnesium stearate [2] ......... Manufacturing (Dir ect compression) Mix all components........8 mm Form .............................. pass through a 0............0....................................................................... 3...........8 mm sieve and press with low compression force............................................... Tablet properties Weight ........................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ....50 g Ludipress [1] ....................193 N Disintegration..................230 mg Diameter ............ Formulation Phenindione ........................

..............................................57 % 30 min ..... Manufacturing (Dir ect compression) Mix all components......................................346 mg Diameter ..............................100 Ludipress [1] .................................. Tablet properties Weight ............................... 10 min.......................................................9 min Friability..............5 g g g g g 2................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Phenytoin Sodium Tablets (100 mg)...................................................235 Magnesium stearate [2].....8 mm sieve and press with low compression force.......... pass through a 0..12 mm Form ................. Formulation Phenytoin sodium (Sigma) ..............................................2..2 % Dissolution................... DC 1........82 N Disintegration ............0............................8 Aerosil 200 [4] .10 Kollidon CL [1] ..............biplanar Hardness....................................... 3...89 % BASF Pharma Ingredients Generic Drug Formulations 2001 ................

................................................ Formulation Phenytoin base (Fluka) ..........................8 mm sieve and press with low compression force...... Tablet properties Weight .................100 Ludipress [1] ...biplanar Hardness....12 mm Form ....8 Aerosil 200 [4] ....0.......................................................................................... pass through a 0...........5 g g g g g g 2..........................351 mg Diameter ............................235 Magnesium stearate [2] ....1 min Friability............................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Phenytoin Tablets (100 mg) 1.......................................81 N Disintegration ... Manufacturing (Dir ect compression) Mix all components......................................................................................................2 Stearic acid [7] .........2 Kollidon CL [1] .................................. 3.............................4 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...................2.

..............2............................biplanar Hardness..1 – 2 g g g g g g 2.............................. pass through a 0...8 Polyethylene glycol 6000 powder [6] ...57 sec Friability .................. 3...................................66 N Disintegration (water)...8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Piroxicam Water Dispersible Tablets (20 mg) 1............. Manufacturing (Dir ect compression) Mix all components..........10 Aerosil 200 [4] ......8 mm Form .................................................... Formulation Piroxicam..............................................8 mm sieve and press with low to medium compression force.......50 Kollidon CL [1] ......1% BASF Pharma Ingredients Generic Drug Formulations 2001 ........150 Ludipress [1] .................20 Corn starch [3] ..................................................0. Tablet properties Weight .........................................................238 mg Diameter ..............................................................................................................

Manufacturing (Dir ect compression) Mix the components........99............ sieve and press...05 % ...05 % BASF Pharma Ingredients Generic Drug Formulations 2001 22 kN 160 N 3 – 4 min < 0........9 % Magnesium stearate [2] ..........0...............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Placebo Tablets 1...05 % 15 kN 110 N 2 – 3 min < 0......... Formulation Ludipress [1].1% 2. 3...... Influence of the compr ession force on the table t properties (300 mg table t weight) compression force Property Hardness Disintegration Friability 7 kN 45 N 1 min 0..2.

............................................19 Calcium arachinate [2] ....................... Tablet properties Weight ..................... Formulation I............ Application The tablet is dissolved in water to obtain a vaginal douche solution.....7 min Friability.............................20 mm Form ................2 mg mg mg mg mg mg mg 2...................................................2..............................................2 Aerosil 200 [4] ....................1...... Manufacturing (Dir ect compression) Dry the mixture II for 4 hours at 60 °C........450 Tartaric acid .....................biplanar Hardness.............360 Ludipress [1]........ mix with I and III and press to tablets...........2................................................. BASF Pharma Ingredients Generic Drug Formulations 2001 ......9 % 4........... II..............265 III....0.............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Povidone-Iodine Effervescent Vaginal Tablets (350 mg) 1....200 N Disintegration in water................................... PVP-Iodine 30/06 M 10 (BASF) ........ 3.............................5 g Diameter ...360 Sodium bicarbonate.... Talc [10] .........................

....... Manufacturing (Dir ect compression) Mix all components................1....................>10 min Friability.................... Formulations PVP-Iodine 30/06 M 10 (BASF) ....... Tablet properties Weight ..0.......0 – 3..... crystalline .............0 Menthol.....2 % 4....0 – 5......0 Eucalyptol.................4..............................2...........176 mg Diameter .............0 Magnesium stearate [2]........................150........................... potassium (Searle) .biplanar Hardness ............................ Chemical stability (14 days at 52°C) The loss of available iodine was 16 %....................................... [10]....2.............1 Aerosil 200 [4] .100 N Disintegration in water . BASF Pharma Ingredients Generic Drug Formulations 2001 .... sodium ........8 mm Form .......8 mm sieve and press with medium compression force........0 g g g g g g g g 2..1.......4...5................0 Sorbitol.............................. 3................ crystalline .. pass through a 0..........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Povidone-Iodine Lozenges (5 mg) 1.......... cryst............0 Aspartame..................................0 Saccharin..0...0 – 5......................

...................... Manufacturing (Dir ect compression) Mix all components.................. 3..........................109 mg Diameter .............1 g – 6g 93 g 1g 2.............94 g Magnesium stearate [1] .. 2 Prazosin hydrochloride........8 mm Form ...................................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 .............2 min Friability ............................................................ anhydrous (BASF)....................... polyhydrate (BASF) ...2................– Ludipress [1] ......... pass through a 0............76 N Disintegration ..2 % 103 mg 8 mm biplanar 74 N 3 min 0..................................biplanar Hardness ......................0.....................5 g Prazosin hydrochloride........................8 mm sieve and press with high compression force... Tablet properties Weight . Formulations No.............. 1 No.........................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Prazosin Tablets (5 mg) 1....

............................................20 Lactose monohydrate [8]......... Manufacturing (Dir ect compression) Mix all components.............................................................................................10 Kollidon CL [1] ................... Formulation Prednisolone .......................................................................................5 Aerosil 200 [4] ....... pass through a 0.........8 mm sieve and press with low compression force................ 3..< 1 min Friability...............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Prednisolone Tablets (20 mg) 1............2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........155 Kollidon VA 64 [1] .................212 mg Diameter ..............2 g g g g g g 2...............0..............8 mm Form ...........63 N Disintegration ..............2............................................ Tablet properties Weight ............................................................8 Magnesium stearate [2] ..biplanar Hardness...............

...........................................8 mm Form .................................................. Manufacturing (Dir ect compression) Mix all components............................................2..................................70 N Disintegration ........................2 g 2...........82 % BASF Pharma Ingredients Generic Drug Formulations 2001 ................................................... 3.....................................78 % 30 min .................. pass through a sieve and press with low compression force....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Prednisone Tablets (10 mg) 1..........................223 mg Diameter .........................0................ Tablet properties Weight ..............15 min......208 g Magnesium stearate [2] ..biplanar Hardness...............10 g Ludipress [1] ........... Formulation Prednisone....................................4 min Friability.................2 % Dissolution............

.........8 mm sieve and press with medium compression force...............0 Magnesium stearate [2]..........................4 g g g g 2..... Formulation Propanolol hydrochloride.....325 mg Diameter ......0 Kollidon SR [1]..8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Propranolol Sustained Release Tablets (160 mg) 1...... Manufacturing (Dir ect compression) Mix all components.......biplanar Hardness (Compression force 10 kN/16 kN/ 25 kN).............................3...........................160...1......... Tablet properties Weight ......................................................................................................................6 Aerosil 200 [4] .....0.190 N/269 N/270 N Friability .. pass through a 0...160...........................2...............10 mm Form ...... 3...................1% BASF Pharma Ingredients Generic Drug Formulations 2001 .

Propranolol Sustained Releaseablets T (160 mg) page 2 carbamazepin release [%] 4. Drug release 100 80 60 40 20 0 0 2 4 6 8 10 12 14 time [%] BASF Pharma Ingredients Generic Drug Formulations 2001 16 18 20 22 24 .

.................... 3.2 % BASF Pharma Ingredients Generic Drug Formulations 2001 .............0 Magnesium stearate [2]......................3 min Friability.............................3 Stearic acid [7] ............0...................................... pass through a 0...............4 g g g g 2....................0 Ludipress [1] ... Formulation Propranolol ........biconvex Hardness.........................0...........................75 N Disintegration . Tablet properties Weight ..................................................................................150 mg Diameter ...............8 mm Form ......... Manufacturing (Dir ect compression) Mix all components....2.....0.................................................................108................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Propranolol Tablet Cores (40 mg) 1....40........8 mm sieve and press with high compression force................

........2 min Friability ........10 g Ludipress [1] .2............... 50 mg and 100 mg) 1....... 1 or No.......0........... 1: 10 mg No................. 1 No..........112 N Disintegration .. Remarks – In the case of formulation No..........8 mm sieve and press with low compression force.........2 % 505 mg 12 mm biplanar 101 N 3 min 0..... 3: 100 mg Propranolol hydrochloride ...... 2 No.......... Tablet properties No..1% 496 mg 12 mm biplanar 86 N 2 min 0.1% 4......... BASF Pharma Ingredients Generic Drug Formulations 2001 . 2 the amount of Ludipress and the tablet weight could be reduced................. 3 Weight . Formulation No.... 2: 50 mg No......514 mg Diameter . 3. pass through a 0...12 mm Form ...... – These formulations can be used for tablet cores..........2....................5 g 50 g 450 g 2......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Propranolol Tablets (10 mg. too...5 g 100 g 400 g 2.......................biplanar Hardness............ Manufacturing (Dir ect compression) Mix all components....5 g 2.............490 g Magnesium stearate [2] ...............

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Pyrazinamide Tablets
(500 mg), DC

1. Formulation
Pyrazinamide........................................500.0
Ludipress [1] ........................................134.5
Kollidon CL [1] ........................................12,0
Aerosil 200 [4] ..........................................3.5

g
g
g
g

2. Manufacturing (Dir
ect compression)
Mix all components, sieve through a 0.8 mm screen and press with
medium compression force.
3. Tablet properties
Weight .................................................652 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardness..................................................96 N
Disintegration ................................45 seconds
Friability.................................................0.36 %
Dissolution, 45 min ...................................89 %

BASF Pharma Ingredients Generic Drug Formulations 2001

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Ranitidine Tablet Cores
(150 mg)

1. Formulation
Ranitidine .............................................150 mg
Ludipress [1].........................................147 mg
Magnesium stearate [2].............................3 mg
2. Manufacturing (Dir
ect compression)
Mix all components, pass through a 0.8 mm screen and press with low
compression force.
3. Tablet properties
Weight .................................................305 mg
Diameter .................................................8 mm
Form ..................................................biconvex
Hardness..................................................61 N
Disintegration .....................................2 – 3 min
Friability...................................................0.5 %
4. Remark
If the flowability of the tabletting mixture is not sufficient about 1%
Aerosil 200 [4] could be added.

BASF Pharma Ingredients Generic Drug Formulations 2001

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Ranitidine Tablet Cores
(300 mg)

1. Formulation
Ranitidine................................................300
Ludipress [1] ...........................................295
Magnesium stearate [2] ...............................5
Aerosil 200 [4] .............................................5

g
g
g
g

2. Manufacturing (Dir
ect compression)
Mix all components, pass through a 0.8 mm screen and press with low
compression force.
3. Tablet properties
Weight .................................................600 mg
Diameter ...............................................12 mm
Form ..................................................biconvex
Hardness..................................................72 N
Disintegration .........................................5 min
Friability ..................................................0.6 %
Dissolution, 45 min ...................................95 %

BASF Pharma Ingredients Generic Drug Formulations 2001

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Saccharin Effervescent Tablets
(15 mg)

1. Formulation
Saccharin sodium ......................................15
Tartaric acid ..............................................10
Sodium bicarbonate ..................................14
Kollidon VA 64 [1] ........................................2
Polyethylene glycol 6000, powder [6]............2

g
g
g
g
g

2. Manufacturing (Dir
ect compression)
Dry saccharin sodium and tartaric acid 1 hour at 100°C. Mix all components, pass through a 0.8 mm sieve and press with low compression
force.
3. Tablet properties
Weight ...................................................42 mg
Diameter .................................................5 mm
Form ...................................................biplanar
Hardness..................................................23 N
Disintegration (45 °C, water) .....................1 min
Friability ..................................................0.6 %

BASF Pharma Ingredients Generic Drug Formulations 2001

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Saccharin Tablets
(15 mg)

1. Formulations
No. 1
Saccharin sodium (Roth) ..............................15.0 g
Ludipress [1] ...............................................31.0 g
Kollidon CL [1] ..............................................2.0 g
Magnesium stearate [2] .................................0.3 g
Polyethylene glycol 6000, powder [6] .............2.0 g
Lutrol F 68 [1], milled < 100 µm............................–

No. 2
15.0
31.0
2.0
0.3

g
g
g
g

2.0 g

2. Manufacturing (Dir
ect compression)
Mix all components, pass through a 0.8 mm sieve and press with
medium compression force.
3. Tablet properties
Weight ........................................................51 mg
Diameter ......................................................5 mm
Form ........................................................biplanar
Hardness ......................................................33 N
Disintegration (water) .................................< 2 min
Friability .......................................................0.2 %

51 mg
5 mm
biplanar
29 N
< 2 min
0.2 %

BASF Pharma Ingredients Generic Drug Formulations 2001

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Selegiline Tablets
(5 mg)

1. Formulation
Selegiline HCI (BASF) ..................................5 g
Ludipress [1] .............................................94 g
Magnesium stearate [2] ...............................1 g
2. Manufacturing (Dir
ect compression)
Mix all components intensively, pass through a 0.8 mm sieve and press
with low compression force.
3. Tablet properties
Weight ...................................................99 mg
Diameter .................................................6 mm
Form ...................................................biplanar
Hardness..................................................81 N
Disintegration .....................................3 – 4 min
Friability ................................................< 0.1%

BASF Pharma Ingredients Generic Drug Formulations 2001

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Serratio Peptidase Tablets
(10 mg)

1. Formulation
Serratio peptidase .....................................10 g
Ludipress [1] ...........................................228 g
Magnesium stearate [2] ...............................2 g
2. Manufacturing (Dir
ect compression)
Pass all components through a 0.8 mm sieve, mix intensively and press
with low compactation force (6 kN).
3. Tablet properties
Weight .................................................238 mg
Diameter .................................................8 mm
Form ...................................................biplanar
Hardness..................................................80 N
Disintegration .....................................3 – 4 min
Friability ...............................................< 0.2 %

BASF Pharma Ingredients Generic Drug Formulations 2001

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Silimarin Tablets
(35 mg)

1. Formulation
Silimarin .................................................35.5 g
Ludipress [1] ........................................410.5 g
Magnesium stearate [2].............................4.5 g
2. Manufacturing (Dir
ect compression)
Mix all components, pass through a 0.8 mm sieve and press with low
compression force (about 10 kN).
3. Tablet properties
Weight .................................................458 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardnes...................................................0.1%
Disintegration ..........................................3 min
Friability ................................................< 0.1%

BASF Pharma Ingredients Generic Drug Formulations 2001

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Sodium Fluoride Tablets
(0.5 mg)

1. Formulation
Sodium fluoride (Merck) ..........................0.55
Sorbitol, crystalline [10] .........................56.25
Dicalcium phosphate, DI-TAB [9] ...........56.25
Kollidon VA 64 [1] ...................................2.20
Magnesium stearate [2]...........................0.50

g
g
g
g
g

2. Manufacturing (Dir
ect compression)
Mix all components, pass through a 0.8 mm sieve and press with high
compression force.
3. Tablet properties
Weight..................................................116 mg
Diameter .................................................6 mm
Form ...................................................biplanar
Hardness ................................................144 N
Disintegration .....................................8 – 9 min
Friability ................................................< 0.1%
4. Remark
If the content uniformity is not sufficient a premix of sodium fluoride and
sorbitol or dicalcium phosphate should be prepared separately before
mixing with the rest of the excipients.

BASF Pharma Ingredients Generic Drug Formulations 2001

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Sodium Fluoride Tablets
(1.3 mg)

1. Formulation
Sodium fluoride (Merck) ............................1.3 g
Ludipress [1] ..........................................76.7 g
Magnesium stearate [2].............................0.4 g
2. Manufacturing (Dir
ect compression)
Mix all components, pass through a 0.8 mm sieve and press with low
compression force.
3. Tablet properties
Weight ...................................................78 mg
Diameter .................................................5 mm
Form ...................................................biplanar
Hardness..................................................82 N
Disintegration ..........................................4 min
Friability ................................................< 0.1%
4. Remark
If the content uniformity does not meet the requirements it would be
recommended to prepare a premix of the active ingredient with a small
part of the Ludipress or with lactose monohydrate before mixing with the
other components of the formulation.

BASF Pharma Ingredients Generic Drug Formulations 2001

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Spironolactone Tablets
(25 mg)

1. Formulation
Spironolactone .......................................25.0 g
Ludipress [1].........................................175.0 g
Magnesium stearate [2].............................1.5 g
2. Manufacturing (Dir
ect compression)
Mix all components, pass through a sieve and press with medium
compression force.
3. Tablet properties
Weight .................................................197 mg
Diameter .................................................8 mm
Form ...................................................biplanar
Hardness ................................................153 N
Disintegration.........................................13 min
Friability ................................................< 0.1%

BASF Pharma Ingredients Generic Drug Formulations 2001

2.8 Formulations of ablets
T
Obtained by Dir
ect Compression (Lab Scale)

Spirulina Extract Chewable Tablets
(250 mg)

1. Formulation
Spirulina extract, powder ........................250
Ludipress [1] ...........................................245
Polyethylene glycol 6000, powder [6]..........25
Aerosil 200 [4] .............................................5

g
g
g
g

2. Manufacturing (Dir
ect compression)
Mix all components, pass through a 0.8 mm sieve and press with
medium compression force.
3. Tablet properties
Weight .................................................495 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardness ................................................149 N
Disintegration (water).........................not tested
Friability...................................................0.2 %

BASF Pharma Ingredients Generic Drug Formulations 2001

.. mix intensively and press with low compression force (10 kN)...................2.6 mm Hardness ...............97 % 20 min .....................98.. Manufacturing (Dir ect compression) Pass all components through a 0........ 3......................................................................100 % 97.. 5 min .....1.....................0.....5 min Friability....0 g 5...0 g 1...........................1% 41% 97 % 100 % 4.............................1 g Ludipress [1] .......1 mg Diameter ..........................98.............1........... Remark If the content uniformity does not meet the requirements it would be recommended to prepare a premix of the active ingredient with a small part of the Ludipress or with lactose monohydrate before mixing with the other components of the formulation...................94 N Disintegration ............................1% Dissolution..........................................59 % 10 min ..5 g 94....... Tablet properties Weight ...... BASF Pharma Ingredients Generic Drug Formulations 2001 .......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Terazosin Tablets (1 mg and 5 mg) 1.......0 g 2..... Formulations 1 mg 5 mg Terazosin hydrochloride (BASF) .......................6 mg 6 mm 105 N 5 min < 0..................8 mm sieve.............0 g Magnesium stearate [2] .....................................

..................... 3..............183 N Disintegration ...................................................301 mg Diameter ..................................< 0...235 Kollidon CL [1]........................6 Magnesium stearate [2]............5 min Friability ........... Manufacturing (Dir ect compression) Mix all components...................................2.............1% BASF Pharma Ingredients Generic Drug Formulations 2001 ..............1 mg mg mg mg 2... Formulation Terfenadine ............................biplanar Hardness ........................60 Ludipress [1] ........... pass through a 0................................................................................ Tablet properties Weight .......................8 mm Form .......................8 mm sieve and press with very low compressive force.....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Terfenadine Tablets (60 mg) 1.....................

............................................................8 mm sieve and press to tablets with very low compression force...................................64 N Disintegration. 3...............biplanar Hardness.................................................... Tablet properties Weight ................278 mg Diameter .........biplanar Hardness................... Manufacturing (Dir ect compression) Mix all components................. Formulation Tetracycline hydrochloride (Welding) ..................................... Physical stability (12 months...125 Ludipress [1] ................2......< 0..................................................................< 0...........................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Tetracycline Tablets (125 mg) 1...............................8 mm Form ......................... 20–25 °C) Weight ........278 mg Diameter ...................................42 Magnesium stearate [2] ......................................................1 – 2 min Friability .......................1 – 2 min Friability .................................... pass through a 0......................100 Avicel PH 101 [5] .............3 g g g g 2...........8 mm Form ................1% 4..63 N Disintegration..............1% BASF Pharma Ingredients Generic Drug Formulations 2001 ...................................

..........28.....biplanar Hardness..............250....12 mm Form ......................................15..2............................505 mg Diameter .....................175..... add the mixture II and press with low compression force.....................5 Calcium arachinate [2] .......0 Talc [10] ..0 Kollidon 30 [1] .......0 Aerosil 200 [4] ...........3.........................5 g g g g g g g 2...........................25............5 % BASF Pharma Ingredients Generic Drug Formulations 2001 .........................................62 N Disintegration .......................5 mm sieve....0 Kollidon CL [1]..................................................................... II.......0.3 min Friability................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Tetracycline Tablets (250 mg) 1.......... 3.0 Lactose monohydrate D 20 [8]................................. Manufacturing (Dir ect compression) Pass the components I through a 0...................................... Tablet properties Weight .. Tetracycline hydrochloride ................. Formulation I...................3.........................

.................... Tablet properties Weight .106 N Disintegration............2 g g g g g 2..................................208 mg Diameter ..........................................................................50 Avicel PH 101 [5]...........2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..... Formulation Tetrazepam ..8 mm Form ........0....................................................................1 – 2 min Friability.......5 mm sieve and press with low compression force.............................................2.........biplanar Hardness .............................30 Kollidon VA 64 [1] ......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Tetrazepam Tablets (50 mg) 1..... Manufacturing (Dir ect compression) Pass the components through a 0................................113 Starch 1500 (Colorcon) ............................................................. 3....5 Magnesium stearate [2] ...............................................

...........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Theophylline Sustained Release Tablets (500 mg) DC 1................225 Magnesium stearate [2] .........223 N Friability .................... granular type (BASF) ..........5 mm Form .......................................................... 3..................................................2..........................................................................8 mmand press with medium compression force....................... pass through a sieve of 0........................ Formulation Theophylline..............3 g g g g 2............................. Football shape Hardness .....125 Ludipress LCE [1] .....................................................500 Kollidon SR [1].......................19 x 8..................................853 mg Diameter ....................................<0.. Manufacturing (Dir ect compression) Mix all components................................................ Tablet properties Weight ...1% BASF Pharma Ingredients Generic Drug Formulations 2001 .............Amer.........

Drug e r lease 100 80 60 40 50 rpm medium: 0.08 N HCl (0-2 h) phosphate buffer pH 6.8 (2-12) 20 0 0 2 4 6 8 time [h] BASF Pharma Ingredients Generic Drug Formulations 2001 10 12 14 16 .Theophylline Sustained Release ablets T (500 mg) DT page 2 released drug [%] 4.

................. 3...... Tablet properties Weight ..........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Theophylline Tablets (100 mg) 1...........................2 min Friability ................................................................15 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......0........1/0....................biplanar Hardness................................147 g Magnesium stearate [2] ..........8 mm Form ....................................................83 N Disintegration .......... Formulation Theophylline granules 0...............2..........................3 g 2.........4 mm (BASF) ....................................... pass through a sieve and press with low compression force. Manufacturing (Dir ect compression) Mix all components............247 mg Diameter ....100 g Ludipress [1] .......

.......2............150....100. Tablet properties Diameter ... 3..8 mm sieve............................... blended for 10 min in a Turbula mixer and then compressed with medium compression force........254 mg Hardness .....5 Magnesium stearate [2]...0 Kollidon SR [1].......... colloidal ................. Formulation Tramadol-HCI (Chemagis).................8 (2-16) 20 0 0 2 4 6 8 10 time [h] BASF Pharma Ingredients Generic Drug Formulations 2001 12 14 16 18 ..........2.................................. Manufacturing (Dir ect compression) All ingredients were passed through a 0... Dissolution of ramadol-HCI T 100 80 60 40 50 rpm medium: 0............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Tramadol Sustained Release Tablets (100 mg) 1..0 Silicon dioxide...................................211 N Friability .10 mm Weight ..........................5 g g g g 2......1..................................08 N HCl (0-2 h) phosphate buffer pH 6.......................0 % released drug [%] 4........................

................................................................................8 mm Form ...............................191 Kollidon CL [1] ......2 g g g g 2............2 Magnesium stearate [2] ...................................... pass through a sieve and press with low compression force.............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Triamcinolone Tablets (4 mg) 1................................ Remark If the content uniformity does not meet the requirements it would be recommended to prepare a premix of the active ingredient with a small part of the Ludipress or with lactose monohydrate before mixing with the other components of the formulation........................................ Tablet properties Weight ................................206 mg Diameter .biplanar Hardness.....0............................................2 % 4......2 min Friability.................... Formulation Triamcinolone..4 Ludipress [1] .. 3.............2............ BASF Pharma Ingredients Generic Drug Formulations 2001 ............................... Manufacturing (Dir ect compression) Mix all components............................45 N Disintegration ..................

........194 g Magnesium stearate [2] ...................2........... Formulation Trifluoperazine hydrochloride................. Tablet properties Weight ....................3 min Friability .15 % 4..................... pass through a sieve and press with very low compression force..... Remark If the content uniformity does not meet the requirements it would be recommended to prepare a premix of the active ingredient with a small part of the Ludipress or with lactose monohydrate before mixing with the other components of the formulation......... 3...............0........8 mm Form ..............................5 g Ludipress [1] .....204 mg Diameter ..........................................biplanar Hardness.................................................................1 g 2..................... BASF Pharma Ingredients Generic Drug Formulations 2001 ................................................. Manufacturing (Dir ect compression) Mix all components..........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Trifluoperazine Tablets (5 mg) 1...........65 N Disintegration ...............................

........0 Avicel PH 101 [5] ...........120.....................7................... Manufacturing (Dir ect compression) Pass all components through a 0..............biconvex Hardness.. powder......................0 Kollidon CL [1] ........ 3.....36...................................................................9 mm Form .49 N Disintegration..2..............................3 % BASF Pharma Ingredients Generic Drug Formulations 2001 ....................................0 Aerosil 200 [4] .....0 Passiflora extract....................3 g g g g g g 2..231 mg Diameter ............10 min Friability.................................... Formulation Valeriana extract...........................................................6 Magnesium stearate [2] ..0.......... mix and press with low compression force...........3......................11..............44..............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Valeriana Extract + Passiflora Extract Tablet Cores (44 mg + 30 mg) 1.............8 mm sieve.......... powder................ Tablet properties Weight .......

......2.....5 g g g g g g 2......75.....................................12 mm Form ..................75 % BASF Pharma Ingredients Generic Drug Formulations 2001 ................................628 mg Diameter ............... pass through a 0......1% Mass uniformity (s rel....)...........................................................................................................75.......................................0 Ludipress LCE [1] .....8 mm sieve and press with low compression force using a vibrating hopper...................240............. Formulation Verapamil hydrochloride .0............. Tablet properties Weight .........................0 Magnesium stearate [2]....................................0 Talc .5..........2.............................0 Methocel K15M (Dow).biplanar Hardness .........0 Aerosil 200 [4] ...........100 N Friability ............. 3. Manufacturing (Dir ect compression) Mix all components.....230.............1.8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Verapamil Sustained Release Tablets (220 mg) 1......................

8) 100 80 60 40 20 0 0 4 8 12 time [h] BASF Pharma Ingredients Generic Drug Formulations 2001 16 20 24 .Verapamil Sustained Releaseablets T (220 mg) page 2 released drug [%] 4. Dissolution (2h gastric juice. then pH 6.

.. pass through a 0.....biplanar Hardness .........3 Aerosil 200 [4] ........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Verapamil Tablets (120 mg).......374 mg Diameter ...............................................................................................108 N Disintegration....5 – 6 min Friability.................................2.............................................4 % 4................................................................... 3......... Formulation Verapamil hydrochloride (BASF) ....270 Magnesium stearate [2] ... BASF Pharma Ingredients Generic Drug Formulations 2001 ...8 mm sieve and press with medium compression force using a vibrating hopper..................12 mm Form ........................120 Ludipress [1] ...........0.... Manufacturing (Dir ect compression) Mix all components.3 g g g g 2........................ Remark The tablet weight should be increased to about 400 mg........... DC 1.............. Tablet properties Weight ..............................

.............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin A + Vitamin B6 + Vitamin E Tablets (40.2........395 Magnesium stearate [2] . mix and press with high compression force.................................. Manufacturing (Dir ect compression) Pass all components through a 0...........1% BASF Pharma Ingredients Generic Drug Formulations 2001 ................................ 3.............../g (BASF) Pyridoxine hydrochloride (BASF).................13 min Friability ............................................< 0.............. + 40 mg + 35 mg) 1.............. Tablet properties Weight .........................40 Vitamin E acetate dry powder SD 50 . u......................................................... Formulation Vitamin A acetate dry powder ...........................000 i..89 N Disintegration.12 mm Form ..........................583 mg Diameter ...8 mm sieve....4 Aerosil 200 [4] ...75 (BASF) Ludipress [1] ...80 500.................. u.........biplanar Hardness.......................................................000 i..........5 g g g g g g 2..................

..........60.......................0 g 2............... powder (BASF).......5...........0 g 2.........200 i...............20....................................30........................................4 g 500.......... Formulations No..................105......53 N Disintegration .......2..................0 g Avicel PH 101 [5] .........4 g 60.....0 g 5....– Lactose monohydrate [8] ............................................0 g Kollidon VA 64 [1]....................... u............1.....................................0 g Kollidon 25 [1] ............. mix and press with medium compression force...........................................................................15 min Friability.0 g 5..8 mm sieve................. Manufacturing (Dir ect compression) Pass all components through a 0............8 mm Form ......0 g – 30..1% BASF Pharma Ingredients Generic Drug Formulations 2001 ......– Kollidon CL [1] .... 2 Vitamin A acetate dry powder .000 i.....2..................................< 0..........285 mg Diameter .................0 g Aerosil 200 [4] ............... u.......60.................... 1 No.... 1 No.......................0 g 100............0 g Vitamin E acetate dry powder 50 % ./g (BASF) Ascorbic acid...0 g 60...............0 g – 20.... + 60 mg + 30 mg) 1......1% 279 mg 8 mm biplanar 67 N 6 min < 0....................... Tablet properties No.0 g Mannitol .8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin A + Vitamin C + Vitamin E Tablets (1........................................... 2 Weight .................– Talc [10] .... 3.....................biplanar Hardness ...0 g 1....

33............................16 mm Form ..300....................4../g (BASF) Ascorbic acid..............0 Saccharin sodium .................300..................0 Mannitol . u.....................0 Sucrose..300...............0 500............. 3......................107 N Disintegration ......000 + 50....................000 i........... crystalline.................0 Sorbitol.................... crystalline [10] ..20.....0 Stearic acid [7] ................ Formulation Vitamin A + D 3 dry powder ...................0. + 200 i..0......1................30........ Manufacturing (Dir ect compression) Pass all components through a 0................biplanar Hardness .......8 mm sieve.......................30.0 Polyethylene glycol 6000...........7 min Friability... mix and press with high compression force................. + 30 mg) 1...........5......300...................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin A + Vitamin D3 + Vitamin C Chewable Tablets for Children (2............................................................................0 Ludipress [1] .......000 i............ Tablet properties Weight ..............290 mg Diameter ......0 Flavour mixture (Firmenich)...... powder [6]........0 g g g g g g g g g g g 2.......... u........... powder (BASF) .1 Cyclamate sodium ..............................2...4 % BASF Pharma Ingredients Generic Drug Formulations 2001 ................. u...

pass through a 0.......... u...17 g g g g 2..............biplanar Hardness....................................... 3........2...............................................12 mm Form .....69 500.......... Manufacturing (Dir ect compression) Mix all components.........146 of Kollidon 30 Kollidon CL [1] .......................< 0............ + 70 mg) 1.......000 i............. Formulation Vitamin A acetate dry powder ...../g (BASF) Vitamin E acetate dry powder.............................. granulated with 10 % ........................................8 mm sieve and press with high compression force..8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin A + Vitamin E Tablets (33.........................................38 N Disintegration.............1% BASF Pharma Ingredients Generic Drug Formulations 2001 ......................000 i.........14 min Friability ....... Tablet properties Weight ..........70 SD 50 (BASF) Mannitol...300 mg Diameter . u....................

................24 min Friability ..350 Kollidon VA 64 [1] ................25 Magnesium stearate (Merck) ................................................................< 0......... u. Manufacturing (Dir ect compression) Mix all components.750 mg Diameter ......1% BASF Pharma Ingredients Generic Drug Formulations 2001 .12 mm Form ..................................................... u............ pass through a 0....... Formulation Vitamin A acetate dry powder......111 N Disintegration .....2......................biplanar Hardness ............/g (BASF) Mannitol....................................................000 i........................................ Tablet properties Weight .............5 Aerosil 200 [4] ...................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin A Chewable Tablets (100....350 325.............000 i...........) 1..........................3 g g g g g 2. 3...........................................................8 mm sieve and press with medium compression force...

......................5 Aerosil 200 [4] ..............................................................) 1.......< 0......... 3....................................231 mg Diameter ...........................2.......................biconvex Hardness..2 min Friability ... u..............100 Kollidon VA 64 [1] ..................... mix and press with low compression force...................64 N Disintegration ..1 g g g g g 2............................000 i.............000 i.......... Formulation Vitamin A acetate dry powder ........... Manufacturing (Dir ect compression) Pass all components through a 0...........1% BASF Pharma Ingredients Generic Drug Formulations 2001 ..../g (BASF) Avicel PH 102 [5] .................. u.......................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin A Tablet Cores (50......110 500......................................9 mm Form .8 mm sieve...........10 Kollidon CL [1] ..... Tablet properties Weight ............................

... Formulation Vitamin A acetate dry powder........................4 Aerosil 200 [4] .2.................... Manufacturing Granulate the dicalcium phosphate with Kollidon 30.............0 Kollidon CL [1] .........0 granulated with 3 % of Kollidon 30 [1] Polyethylene glycol............680 mg Diameter ...........0 500..............................biplanar Hardness.......... powder [6] ..........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin A Tablets (25................... 3......5....55.............................................6 g g g g g 2............2 min Friability.......................28... u................... Tablet properties Weight ......000 i............................... dissolved in isopropanol or water and pass through a 0... ............40 N Disintegration .........5 mm screen.............12 mm Form ./g (BASF) Dicalcium phosphate (DI-TAB) [9]...................) 1................ sieve and press with high compression force using a vibrating hopper. Mix the obtained dried granules with the other components.......4 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...........0.19......... u......572.....000 i..............

....................../g (BASF) Ludipress[1] ....... Formulation No..) 1....................biplanar Hardness .....51 N Disintegration ..................1% BASF Pharma Ingredients Generic Drug Formulations 2001 .......................– Kollidon CL [1] .............................. u...189 g Avicel PH 101 [5] .. 2 No... 1 No.........000 i... 3 Vitamin A acetate dry powder.............– Magnesium stearate (Merck) .1 g Aerosil 200 [4] ..2....< 0..................8 mm sieve and press with low compression force. 1 No..............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin A Tablets (50............– Kollidon VA 64 [1] ........ 3................306 mg Diameter............. 2 No.............. u.8 mm Form ....................... Manufacturing (Dir ect compression) Mix all components..110 g 500...1% 277 mg 8 mm biplanar 119 N < 1 min < 0.............– 120 g 110 g 120 g 10 g – – 1g 1g – 154 g 10 g 4g – 1g 2.....3 min Friability . pass through a 0...............000 i... Tablet properties No......1% 250 mg 8 mm biplanar 106 N 7 min 0..... 3 Weight ..................................................

0 g – – 100........150............5..........................................0......0 g – 10.............5.......– Riboflavin (BASF).30...........0 g – 25....4 g Kollidon VA 64 [1] .....2........0 g Folic acid ....................................................0 g Pyridoxine hydrochloride (BASF) ................0 g Thiamine hydrochloride (BASF) ...........0 g 5.0 g Ascorbic acid... pass through a 0...........20.................................................................... Press the mixture with medium/low compression force. 1 No.0 g Stearic acid [7] ..– – 15..................0 g Magnesium stearate [2] ...........................0 g 2...– Niacin ..........2........1 g Calcium D-pantothenate (BASF) ................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B Complex + Vitamin C Tablets 1........... BASF Pharma Ingredients Generic Drug Formulations 2001 .............0 g Nicotinamide.........5 g Choline bitartrate ..........................................0 g 2.5......................10.....0 g 220........................ Manufacturing (Dir ect compression) Weigh all ingredients in.......0................0 g – – 8...8 mm-sieve and mix...172..... 2 Thiamine mononitrate (BASF) ................................................ ..– Biotin (Merck) ............................. Formulations No.................0 g crystalline/powder (BASF) Ludipress [1] .................

................Vitamin B Complex + itamin V CT ablets page 2 3........................ 2.....3 – 4 min Friability....400 mg Diameter .................. 2 Weight ....................................biplanar Hardness ..................................10 mm Form ......................0......3 % 4......1% 411 mg 12 mm biplanar 69 N 5 min 0...............................95 N Disintegration ................................ BASF Pharma Ingredients Generic Drug Formulations 2001 ............................ 1 No..................................... Tablet properties No................... Remark For stability reasons it would be better to substitute thiamine hydrochloride by thiamine mononitrate in formulation No.....

...............25 g Nicotinamide ........................< 1 min Friability ......1% (BASF)....................................................................................................16 g Aerosil 200 [4]............................. 3...............— Riboflavin (BASF)........... Tablet properties No............................8 % BASF Pharma Ingredients Generic Drug Formulations 2001 .......... 1 No......40 g Pyridoxine hydrochloride (BASF)...........3 g — 25 g 25 g 80 g 40 g 16 g 16 g 282 g 16 g 3g 2......... 1 No.............. Manufacturing (Dir ect compression) Pass all component through a 0................282 g Kollidon 30 [1] ............................ Formulations No....................................................16 g Cyanocobalamin gelatin coated 0................ 2 Weight ......513 mg Diameter ....2...........0...8 mm sieve................16 g Avicel PH 101 [5] ...biplanar Hardness ............................. 2 Thiamine mononitrate (BASF) .............80 g Calcium D-pantothenate (BASF).................... I 1....................25 g Thiamine hydrochloride (BASF) ...12 mm Form .................................... mix and press with medium to high compression force.................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B Complex Tablets................................................4 % 504 mg 12 mm biplanar 68 N < 1 min 0.......73N Disintegration .......................................

Vitamin B Complex ablets. closed) 0 Month Formulation No. 2 100 % 100 % 6 Months 12 Months 83 % 32 % 72 % 11% Result: Thiamine hydrochloride is not suitable in this formulations. Chemical stability of vitamin B1 (40 °C. BASF Pharma Ingredients Generic Drug Formulations 2001 . T I page 2 4. 1 Formulation No.

.............................0 Saccharin sodium ....314 mg Diameter .......2.... Manufacturing (Dir ect compression) Pass all component through a 0.76 N Disintegration .....6 Nicotinamide .................................................................3 Riboflavin (BASF).2............0.......4 (BASF) Ludipress [1] ....................6 min Friability. BASF Pharma Ingredients Generic Drug Formulations 2001 .......................................................biplanar Hardness ..............................................2.......4........... Formulation Thiamine mononitrate (BASF) ..................3 Calcium D-pantothenate (BASF)...............................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B Complex Tablets.7 Cyanocobalamin gelatin coated 0..... 3........... II 1......0.............1% ..............................0 g g g g g g g g g g g 2.................2.14..............................2 Pyridoxine hydrochloride (BASF).................................... Tablet properties Weight .....0 Magnesium stearate [1]............ mix and press with low compression force..... Remark These tablets could be commercialized in Europe as dietary food because all components are allowed for this application.............1% 4........................................0 Flavour (Firmenich).8 mm sieve......280....................2...8 mm Form ................05 Cyclamate sodium ........2.............................................2..5................

..........................................................biplanar Hardness ............ Formulation Vitamin premix BASF (see Remark)..........2 g g g g 2............ Manufacturing (Dir ect compression) Mix the vitamin premix with Aerosil 200........................... III 1.............................................................0.......2 Ludipress [1] .....................2......1% 4....................... Tablet properties Weight ....6 min Friability......8 mm sieve..........................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B Complex Tablets............................................33 Aerosil 200 [4] ......................46 N Disintegration ........................ Remark The vitamin premix BASF had the following composition: Thiamine mononitrate Riboflavin Pyridoxine hydrochloride Nicotinamide Calcium D-panthothenate BASF Pharma Ingredients Generic Drug Formulations 2001 20 % 6% 7% 57 % 10 % .. 3.... add the other components...................232 mg Diameter .......... mix and press with low compression force..8 mm Form ..............200 Magnesium stearate [1] .......................... pass through a 0................................

............... Remark The vitamin premix BASF had the following composition: Thiamine mononitrate (BASF) Riboflavin 100 (BASF) Pyridoxine hydrochloride (BASF) Nicotinamide......10 mm Form ............................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B Complex Tablets........................ Manufacturing (Dir ect compression) Mix the vitamin premix with the other components...................biplanar Hardness ..............................4-5 min Friability . mix and press with low compression force...139 g Ludipress [1] ...........................57 N Disintegration ...............................................................8 mm sieve......233 g Magnesium stearate [2] ............... Tablet properties Weight ..............................3 g 2..................0..................... 3...........................................2 % 4..... fine granules (Degussa) Calcium D-panthothenate (BASF) 17 % 12 % 10 % 39 % 22 % BASF Pharma Ingredients Generic Drug Formulations 2001 ................... IV 1..... Formulation Vitamin premix BASF (see Remark) .........2.........372 mg Diameter ........ pass through a 0...............

.. 2 Weight ...5 g Aerosil 200 [4].........................5 mm sieve..........................................................2 – 3 min Friability...................... 1 No....... 1 Thiamine hydrochloride (BASF) .........110 N Disintegration ...................................... Manufacturing (Dir ect compression) Pass all components through 0.............................biplanar Hardness .............50 g Thiamine mononitrate (BASF) ...........................0..........................2 g No.............. 3........357 mg Diameter .................. mix and press with medium compression force............................293 g Magnesium stearate [2] ...........2.........12 mm Form ...........1% BASF Pharma Ingredients Generic Drug Formulations 2001 ...............1% 347 mg 12 mm biplanar 108 N 7 min < 0....... I 1..........................– Ludipress [1] ...................................... 2 50 293 5 2 – g g g g 2.........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B1 (Thiamine) Tablets (50 mg)................. Formulation No................................. Tablet properties No.............

......150 g Avicel PH 101 [5] .......... closed) Formulation No.......................2 g No............................................ 3................150 N Disintegration .................................................5 mm sieve....... 1 Thiamine hydrochloride (BASF) ...biplanar Hardness.............. mix and press with high compression force........................ 2 0 Months 3 Months 100 % 100 % 98 % 100 % 6 Months 12 Months 90 % 96 % 97 % 97 % BASF Pharma Ingredients Generic Drug Formulations 2001 .......344 mg Diameter .. 1 Formulation No........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B1 (Thiamine) Tablets (50 mg).......... 2 Weight ..........2 min Friability......12 mm Form ....................................... 1 No.....................1% 4. II 1.. Manufacturing (Dir ect compression) Pass all components through 0...............................0......2......................150 g Kollidon CL [1] ................................ 2 50 150 150 15 2 g g g g g 2.....................50 g Thiamine mononitrate (BASF) ........................15 g Aerosil 200 [4].............. Chemical stability of thiamine (40 °C........ Formulation No................................– Lactose monohydrate [8] .............................. Tablet properties No..............1% 373 mg 12 mm biplanar 150 N < 1 min < 0........................

..... mix and press with medium compression force.............2 min Friability ......................................... Tablet properties No.biplanar Hardness ..........................................................................2...........................2 g – 100 g – 100 g 100 g 9g 1g – 2..........302 mg Diameter ............. 2 Thiamine hydrochloride (BASF) ....5 mm sieve..............................................................................2 % 320 mg 8 mm biplanar 150 N < 1 min 0....................................... 1 No.........110 g Thiamine mononitrate (BASF) ........................8 mm Form .......................3 g Magnesium stearate [2] ............................– Avicel PH 101 [5]...... 2 Weight .......................................... Manufacturing (Dir ect compression) Pass all components through 0...– Ludipress [1] ..190 g Lactose monohydrate [8] ................................................................– Aerosil 200 [4]..................... 3..................... Formulations No............... DC 1.....– Kollidon CL [1] ...8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B1 (Thiamine) Tablets (100 mg)................. 1 No........................................0..................114 N Disintegration .........2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ....

....... 3...............................................................63 N Disintegration .......8 mm sieve............................................. Formulation Thiamine hydrochloride (BASF) ..............0..............10 Ludipress [1] ...............10 Cyanocobalamin...394 mg Diameter .......2..................... Tablet properties Weight ...........................biplanar Hardness .......... Manufacturing (Dir ect compression) Pass all components through a 0................................... gelatin coated 1% (BASF) ................ mix and press with low compression force......................................................................4 min Friability .....................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B1 + Vitamin B6 + Vitamin B12 Tablets (100 mg + 10 mg + 100 µg) 1........................3 g g g g g 2.......100 Pyridoxine hydrochloride (BASF)..........12 mm Form ................277 Magnesium stearate [2] .3 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...........

................. powder [6] ..........................250 Polyethylene glycol 6000................................................10 Ludipress [1] ................................8 mm sieve and press with low compression force.................................................................200 Cyanocobalamin gelatin coated 1% (BASF) .......................... Tablet properties Weight ....102 N Disintegration ...............100 Pyridoxine hydrochloride (BASF)..............................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 .....................................biplanar Hardness........0..........................................5 g g g g g g 2............. Formulation Thiamine mononitrate (BASF) ............................................2. Manufacturing (Dir ect compression) Mix all components...........12 mm Form ...................45 Aerosil 200 [4]....... pass through a 0.............609 mg Diameter ..8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B1 + Vitamin B6 + Vitamin B12 Tablets (100 mg + 200 mg + 100 µg) 1....... 3...5 min Friability ..................

. orange BASF Pharma Ingredients Generic Drug Formulations 2001 ... 3......................80 N Disintegration .............................. Coloured (50 µg) 1..... Tablet properties Weight ....................0 (BASF) Ludipress [1] ...........2................................................... Manufacturing (Dir ect compression) Prepare the premix II............. Cyanocobalamin gelatin coated 0...................150.................homogeneous..< 0................1% Colour ....0 Yellow orange lake ............. II... pass through a 0...........8 mm Form .........................................10 min Friability..................3.209 mg Diameter ......5 mm sieve and press with low compression force.... Formulation I...2... add to mixture I....................................................5 Quinoline yellow lake .....0 Magnesium stearate [2] ........................1%......................................................biplanar Hardness .........................1.......................................0 g g g g g 2..............50.8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B12 (Cyanocobalamin) Tablets...

.............................. Tablet properties Weight ................................ Manufacturing (Dir ect compression) Pass all components through a 0...........1 g g g g 2........1% Content uniformity: meets the requirements of DAB 4...............97 N Disintegration ....3 Ludipress [1] ....................... If the content uniformity does not meet the requirements it would be recommended to prepare a premix of the active ingredient with a small part of the Ludipress or with lactose monohydrate before mixing with the other components of the formulation....................................202 mg Diameter ......................2 Aerosil 200 [4]..............................0....8 mm Form .....................................................................................................................biplanar Hardness .... Remarks These tablets could be commercialized in Europe as dietary food because all components are allowed for this application.............2....... mix and press with very low compression force (4 kN)................3 – 4 min Friability..............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B2 (Riboflavin) Tablets (3 mg) 1..................................8 mm sieve.......195 Magnesium stearate [2] ................. Formulation Ribolfavin C (BASF) ......................... BASF Pharma Ingredients Generic Drug Formulations 2001 ...... 3.............................

...........5 % BASF Pharma Ingredients Generic Drug Formulations 2001 ............................... 3................biplanar Hardness........................23 Magnesium stearate [2] ........... Manufacturing (Dir ect compression) Pass all components through a 0.................................................. mix and press with low compression force.2..........................................................................................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B2 (Riboflavin) Tablets (75 mg) 1........... Tablet properties Weight ......12 g g g g g 2.... crystalline [10]........................12 mm Form .8 mm sieve....................75 Sorbitol....4 Aerosil 200 [4] .. Formulation Riboflavin (BASF)................................................................................................................................375 Kollidon VA 64 [1] ........100 N Disintegration .....10 min Friability ......493 mg Diameter .....0.......................................

........................ Manufacturing (Dir ect compression) Pass all components through a 0............................ Tablet properties Weight ......biplanar Hardness ................................... Formulation Riboflavin .......................................................2...........384 mg Diameter .............7 min Friability .............................5 Aerosil 200 [4] .......3 % BASF Pharma Ingredients Generic Drug Formulations 2001 .............100 Sorbitol.................. crystalline [10]................ 3.....53 N Disintegration ................10 g g g g g 2.................250 Kollidon VA 64 [1] ....................... mix and press with medium compression force...............................19 Magnesium stearate [2] ....................................0.......................................................................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B2 (Riboflavin) Tablets (100 mg) 1...............8 mm sieve..12 mm Form ......................................

...320 Avicel PH 101 [5] ....................2..........................................................................< 1 min Friability ........................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 .....................................3 g g g g g 2............89 N Disintegration .........................................160 Kollidon VA 64 [1] ........ Manufacturing (Dir ect compression) Pass all components through a 0...........506 mg Diameter ..8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B3 (Nicotinamide) Tablets (300 mg) 1.......0.....................3 Aerosil 200 [4]...........................................................................................16 Magnesium stearate [2] ................... mix and press with medium compression force....................................................biplanar Hardness ..................... Tablet properties Weight ...................... Formulation Nicotinamide (Degussa) ..8 mm sieve. 3.....................................12 mm Form ......................

..............................................................252 mg Diameter ...........10 Magnesium stearate [2] ..150 Kollidon CL [1] ......................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B5 (Calcium D-Pantothenate) Tablets (100 mg) 1..............6 min Friability. Manufacturing (Dir ect compression) Mix all components..................................................... pass through a 0......8 mm Form ................................3 g g g g 2....... Tablet properties Weight .... Formulation Calcium D-Pantothenate (BASF).............................................................................196 N Disintegration ..................biplanar Hardness.................100 Ludipress [1] ...........................................................................................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ........................2...... 3...8 mm sieve and press to tablets with medium compression force......................< 0.....

...8 mm sieve and press to tablets with medium/low compression force....25 g Talc [10] .................. 1 No.8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B5 (Calcium D-Pantothenate) Tablets (300 mg) 1........................................................ pass through a 0..60 g Corn starch [3] ..................................50 g Sorbitol....biplanar Hardness ...– 305 g – – 75 g 70 g – 15 g – – – 25 g 2......6 g Polyethylene glycol 6000..........................................................................................................62 N Disintegration.................. 2 Calcium D-Pantothenate (BASF) ................. 3.............– Avicel PH 101 [5] ..... powder [6] ....11 min Friability ..... 1 No.............................. Manufacturing (Dir ect compression) Mix all components.....8 % 488 mg 12 mm biplanar 135 N 5 min < 0...................................................................12 mm Form ...............................100 g Kollidon VA 64 [1] ........ Formulations No.............2...................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ..................................... 2 Weight ................ crystalline [10] ...................................................0......52 g Calcium arachinate [2] ................300 g Lactose Monohydrate [8] ........... Tablet properties No......................12 g Kollidon CL [1] ...........................................................................................................6 g Aerosil 200 [4]....................604 mg Diameter ........

............................. 2 Weight .............2 min Friability.................1% 340 mg 12 mm biplanar 81 N 2 min 0...............................................1 g g g g g g g No..................................................2. mix and press with high compression force......................< 0..150 Kollidon VA 64 [1] ........................... closed) Vitamin B 6 0 Months 3 Months 6 Months 100 % 100 % 100 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........................5 mm sieve.......................... Chemical stability of Formulation No... 2 40 g 150 g 150 g – – 1g 1g 2.....15 Kollidon CL [1] ..12 mm Form ............................biplanar Hardness................................................................ Manufacturing (Dir ect compression) Pass all components through a 0........ 3............... 1 (40°C. 1 No....40 Lactose monohydrate [8] ....361 mg Diameter ..2 4..............................................10 Magnesium stearate [2] ............ 1 Pyridoxine hydrochloride (BASF) ...................................1 Aerosil 200 [4]..............................140 N Disintegration ........... Formulations No...................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B6 (Pyridoxine) Tablets (40 mg)..150 Avicel PH 101 [5] ........................ Tablet properties No....................... DC 1......

....................12 mm Form .. 2 Weight ...........biplanar Hardness ............1% BASF Pharma Ingredients Generic Drug Formulations 2001 .... 2 Pyridoxine hydrochloride .............2........– Avicel PH 101 [5]....................100 g Tabletlose [8].....................................................................................< 1 min Friability ...............3 g Magnesium stearate [2] ............................0....2 % 360 mg 12 mm biplanar 61 N < 1 min < 0......10 g Kollidon CL [1] ........ mix and press with medium compression force..............1 g 100 g – 150 g 83 g 10 g 3g 1g 1g 2.............................................1 g Aerosil 200 [4].................– Kollidon VA 64 [1] .........................................8 mm sieve................... 3................................. 1 No...................... 1 No.............................................................................................................363 mg Diameter ...........200 g Lactose monohydrate [8] .74 N Disintegration ..................................... Formulations No.....................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B6 (Pyridoxine) Tablets (100 mg) 1.......... Manufacturing (Dir ect compression) Pass all components through a 0................................................. Tablet properties No.......

.............................................................2 – 3 min Friability.............< 0............................................361 mg Diameter ....................2.............12 Magnesium stearate [2] ...................53 N Disintegration ..................... 3.8 mm sieve............12 mm Form ..................................................biplanar Hardness .8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin B6 (Pyridoxine) Tablets (250 mg) 1...........................................................100 Kollidon VA 64 [1] ............... Manufacturing (Dir ect compression) Pass all components through a 0..........................250 Avicel PH 101 [5] .. mix and press with high compression force............. Tablet properties Weight ...................................................................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ...5 g g g g 2...... Formulation Pyridoxine hydrochloride (BASF)...............

.............. dry powder 50 % DC ........................ 3.4 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......................... powder [6] .......2. powder (BASF).16 mm Form .... pass through a 0..20 g g g g g g g g 2...........139 N Friability .......................840 Macrogol 6000............ Manufacturing (Dir ect compression) Mix all components........................................................biplanar Hardness. Tablet properties Weight .......25 Aspartame (Nutrasweet) ..........................................................................142 Vitamin E acetate.......................500 mg Diameter .30 Orange flavour (Dragoco) .......................25 Mango flavour (Dragoco)...................... Formulation Ascorbic acid....1...40 (BASF) Ludipress LCE [1] ................................................................................................0....8 mm sieve and press with high compression force....................................... (BASF) . cryst......8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin C + Vitamin E Chewable Tablets or Lozenges (500 mg + 20 mg) 1..............375 Sodium ascorbate...

......2 % Microcristalline cellulose. powder (BASF) .0 % Sucrose.........3 % e........ BASF Pharma Ingredients Generic Drug Formulations 2001 .2......000 mg) 1.......2 % Saccharin sodium ......... Formulation Ascorbic acid.........1% 1250 mg 15 mm biplanar > 100 N > 15 min 0........................ Tablet properties Vitamin C content / Tablet 100 mg 500 mg 1000 mg Weight Diameter Form Hardness Disintegration (water) Friability 250 mg 8 mm biplanar 157 N 15 min < 0. Manufacturing (Dir ect compression) Mix all components....42................. ................. 1. powder [6] .13...6 % 4.....0 % Orange flavour + strawberry flavour (2+1)...........2 % Aerosil 200 [4] ......... Deutscher Apothekerverlag............ 500 mg.........0......... 1988... 3.....8 % 2500 mg 20 mm biplanar > 150 N 14 min 0..2... crystalline.....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin C (Ascorbic acid) Chewable Tablets (100 mg.........0.......... Remark This formulation also is mentioned in “Standardzulassungen für Fertigarzneimittel”........ pass through a 0.....................0 % Kollidon VA 64 [1] .. powder ...4 % Cyclamate sodium ...........28...8 mm sieve and press to tablets with medium to high compression force....... Avicel PH 101 [5] Sucrose.......2.....2............................8..4 % Polyethylene glycol 6000.......1......g......................1% 2...

........................20 mm Form .. crystalline [10] .....biplanar Hardness.......– Dextrose ..... 1 Ascorbic acid...... 3......295 mg 16 mm biplanar 126 N 0..................................... crystalline (BASF) ............2............... 2 Weight ... powder................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin C (Ascorbic Acid + Ascorbate) Chewable Tablets (500 mg) 1.......– Sucrose............................. 2 100 450 264 200 200 60 3 4 1 20 g g g g g – g g g g – g 2......................................10 g Orange flavour ..................... 1 No..........– Cyclamate sodium ............ mix and press with medium to high compression force..10 g Aerosil 200 [4] . Manufacturing (Dir ect compression) Pass all components through a 0......................................................500 g Sodium ascorbate.................300 g Polyethylene glycol 6000............................................................................. powder [6].8 mm sieve.....1.> 150 N Friability ......2..........................– Sorbitol......... Tablet properties No...................7 % 1............................100 g Sucrose..........................30 g No........................0.. crystalline .10 g Saccharin sodium ....................................100 g Magnesium stearate [2]................................................. Formulations No........................7 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........080 mg Diameter ............ crystalline (BASF) ...................................

.............. powder (BASF) ...........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin C (Ascorbic Acid) Chewable Tablets with Fructose (120 mg) 1.................120 Fructose ...........................................8 mm sieve.......................................0 % BASF Pharma Ingredients Generic Drug Formulations 2001 ................................................................................... mix and press with high compression force..................... 3.....................4 Polyethylene glycol 6000.....100 Kollidon VA 64 [1] .......................................................... Manufacturing (Dir ect compression) Pass all components through a 0........................ powder [6] .. Tablet properties Weight ............35 g g g g g g g 2.........................................9 min Friability .biplanar Hardness....... Formulation Ascorbic acid........2........................970 mg Diameter ..........................................500 Ludipress [1] ...................................................................................222 N Disintegration (water) ......15 Aerosil 200 [4].........................12 mm Form ..200 Avicel PH 101 [5] ....

........................ Formulation Ascorbic acid (BASF) ...........15 g g g g g 2.................................................500 Sucrose......................................5 % BASF Pharma Ingredients Generic Drug Formulations 2001 ............................................................ crystalline .........60 Magnesium stearate [2] ............ Manufacturing (Dir ect compression) Pass all components through a 0....................20 mm Form ..... Tablet properties Weight ............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin C (Ascorbic acid) Chewable Tablets with Sucrose (500 mg) 1..........biplanar Hardness.....> 20 min Friability .................. 3............2...............................130 N Disintegration .............. mix and press with medium compression force.......................................................850 Avicel PH 101 [5] ........575 Kollidon VA 64 [1] .............................2.................000 mg Diameter ...........8 mm sieve....................0...........................................

........– Sorbitol Instant (Merck) .................1 g – 1000 g 800 g – 150 g 660 g 80 g q............................... powder [6] .........1% BASF Pharma Ingredients Generic Drug Formulations 2001 No......s..................... 2 1000 mg Ascorbic acid............ anhydrous .....1000 g Sodium bicarbonate ..........................................s.......8 % ............. 1 100 mg No.......................s...2...... q................65 g Lemon flavour ......< 0.........biplanar Hardness...................................... 2............................587 g Polyethylene glycol 6000. Manufacturing (Dir ect compression) Dry the sodium bicarbonate during 1 hour at 100 °C... pass all through a 0......... crystalline (BASF) .....2050 mg Diameter ......................... q..............10 g Cyclamate sodium........... 1 Weight .112 g Ascorbic acid.........2 – 3 min Friability.......... Tablet properties No.......................................– Sorbitol........... crystalline [10] ..............................................25 g Saccharin sodium .................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin C (Ascorbic acid) Effervescent Tablets (100 mg and 1000 mg) 1............... 2 2......690 mg 20 mm biplanar 174 N 2 – 3 min 0.......... powder (BASF) ............ Formulation No..........150 N Disintegration (water) .................................... mix with the other components....... 3.....200 g Citric acid........................20 mm Form ....8 mm sieve and press with high compression force at maximum 30 % of relative atmospheric humidity.................

........................2.................................3 Aerosil 200 [4]......... pass through a 0.........1% 500 mg 1010 mg 16 mm biplanar 116 N 5 min 0.................. Tablet properties 250 mg Weight .........6 Saccharin sodium ........................................................................................3 g g g g g g g 500 mg 140 416 392 28 12 6 6 g g g g g g g 2......biplanar Hardness ...................................... powder (BASF)........................................70 Sodium ascorbate .........................................8 % 4.......12 mm Form .....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin C (Ascorbic Acid + Ascorbate) Lozenges (250 mg and 500 mg) 1. Remark These tablets could be commercialized in Europe as dietary food because all components are allowed for this application..............................................................................92 N Disintegration ....... Manufacturing (Dir ect compression) Mix all components...................................208 Ludipress LCE [1] .....14 Orange flavour ......................... 3.................. BASF Pharma Ingredients Generic Drug Formulations 2001 ...........................................8 mm sieve and press with high compression force................5 min Friability ...............................196 Stearic acid [7] ......................... Formulations 250 mg Ascorbic acid..505 mg Diameter ................

.232 g Magnesium stearate [2] ..........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin C (Ascorbic Acid) Tablets (100 mg) 1...............05 % 22 kN 83 N 2 – 3 min < 0................. powder (BASF) . Influence of the compr ession force on the table t properties compression force Property Hardness Disintegration Friability 7 kN 20 N 1 min 0............05 % 4....... Manufacturing (Dir ect compression) Mix all components....... BASF Pharma Ingredients Generic Drug Formulations 2001 ... 3......... Formulation Ascorbic acid...1 g 2..100 g Ludipress [1] ......... sieve and press to tablets of 335 mg weight...06 % 15 kN 55 N 1 – 2 min < 0.2........... Remark These tablets could be commercialized in Europe as dietary food because all components are allowed for this application.........

...................0.................0 Kollidon CL [1]..25...2....................................................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin C (Ascorbic Acid) Tablets (200 mg) 1....200. Manufacturing (Dir ect compression) Mix all components........2 Magnesium stearate [2] .................> 90 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........15......................0 Ludipress [1]............2...............................0 Aerosil 200 [4] ..5 g g g g g g 2...........0 Kollidon VA 64 [1] ...............499 mg Diameter .....................0 – 256...... Formulation Ascorbic acid.............. 30 min .1................ 3.....8 mm screen and press with medium compression force (18 kN)............................................12 mm Form .....4 % Dissolution............ pass through a 0................................. powder (BASF) ...................... Tablet properties Weight ....................................................................231..........................biplanar Hardness ..2 min Friability ..............................................................73 N Disintegration ...............

Substitution of KollidonAV64 by other dry binders .Vitamin C (Ascorbic Acid)ablets T (200 mg) page 2 80 Hardness Friability 70 60 50 40 Kollidon VA 64 Kollidon 30 BASF Pharma Ingredients Generic Drug Formulations 2001 HP MC 11000 10 9 8 7 6 5 4 3 2 1 0 Friability [%] Hardness [kN] 4.

..............................35 g Aerosil 200 [4]................. powder [6] ..2...... 3...................... Tablet properties No................................. I 1.......... Manufacturing (Dir ect compression) Pass all components through a 0.......... Formulations No...........................................................1% BASF Pharma Ingredients Generic Drug Formulations 2001 .... 1 No..................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin E Chewable Tablets (100 mg)..... 2 Vitamin E acetate dry powder SD 50 (BASF) .biplanar Hardness ......... 2 Weight ......87 N Friability.........................200 g Ludipress [1] ....– Ludipress LCE [1] .......... 1 No............................ mix and press with high compression force............1% 727 mg 12 mm biplanar 102 N < 0....8 mm sieve......................10 mm Form ......................7 g 200 g 493 g – – 7g 2........................................< 0....................258 g Polyethylene glycol 6000.................500 mg Diameter ...........

................................. 3............................................ crystalline [10]..........biplanar Hardness.............. Tablet properties No..................– Kollidon 30 Aerosil 200 [4]........ II 1...200 g Sorbitol..................... granulated with 5 % .....0 % 624 mg 12 mm biplanar 68 N 17 min 0% BASF Pharma Ingredients Generic Drug Formulations 2001 .. 2 Weight...............................8 mm screen and press with high compression force...............................................12 mm Form ............. pass through a 0.....7 g Magnesium stearate [2] ...................2.............................................3 g 200 g – – 400 g 4g – 2.........390 g Mannitol.......711 mg Diameter .... Manufacturing (Dir ect compression) Mix all components............................ Formulations No.................................106 N Disintegration ..................... 1 No............................................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin E Chewable Tablets (100 mg).............. 1 No........ 2 Vitamin E acetate dry powder SD 50 (BASF) ...........12 min Friability .....100 g Dicalcium phosphate [9]...............

......................biplanar Hardness.......................... mix and press with high compression force........8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin E Chewable Tablets (150 mg) 1........12 mm Form ..........................300.. 3.6........0 Saccharin sodium..............8 mm sieve.................300......0 g g g g g 2.................1% 4...............................6..........> 30 min Friability ........ Formulation Vitamin E acetate dry powder .................................................................................. Tablet properties Weight ......................2..........................0 Aerosil 200 [4] ............. BASF Pharma Ingredients Generic Drug Formulations 2001 ..................... Remark These tablets could be commercialized in Europe as dietary food because all components are allowed for this application........ Manufacturing (Dir ect compression) Pass all components through a 0.......................0.....0 SD 50 (BASF) Sorbitol [10]...........80 N Disintegration (water) ....................2 Magnesium stearate [2].........620 mg Diameter ....< 0.....

........ Formulation Vitamin E acetate dry powder ..................400... BASF Pharma Ingredients Generic Drug Formulations 2001 ....biplanar Hardness...................................................... Tablet properties Weight ..0 SD 50 (BASF) Ludipress [1] ............ 3.....................................10. Manufacturing (Dir ect compression) Mix all components......0.......12 mm Form ... Remark These tablets could be commercialized in Europe as dietary food because all components are allowed for this application...............200......................... pass through a 0..............0 Saccharin sodium .............................................> 30 min Friability .............8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin E Chewable Tablets (200 mg) 1................8 mm sieve and press with high compression force...67 N Disintegration (water) .....0 % 4.........0 Aerosil 200 [4] ....................................................................................610 mg Diameter ....1 g g g g 2.............................2......

...... Formulation Vitamin E acetate dry powder..................q..................................................108 N Disintegration (water) ..2....................20 mm Form .......0 % 4.................... 2..........790 g Aerosil 200 [4] ........800 g SD 50 (BASF) Ludipress [1] ....... Remark These tablets could be commercialized in Europe as dietary food because all components are allowed for this application... BASF Pharma Ingredients Generic Drug Formulations 2001 .................. 3.........> 30 min Friability ...................665 mg Diameter ........... Tablet properties Weight .....8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin E Chewable Tablets (400 mg) 1..biplanar Hardness .......................................................................................................s. mix and press with high compression force.......20 g Flavours ..1........................5 mm sieve................................................................... Manufacturing (Dir ect compression) Pass all components through a 0.......................

...........8 mm sieve.........................1% BASF Pharma Ingredients Generic Drug Formulations 2001 .............2 g Aerosil 200 [4] .140 g Tablettose [8] .................................................. Manufacturing (Dir ect compression) Pass all components through a 0......– Mannitol..................................... crystalline (Merck) ..................... 3....... 2 Vitamin E acetate dry powder. 2 Weight ..biplanar Hardness ..... mix and press with high compression force...........................34 N Desintegration ...................................140 g Kollidon VA 64 [1] ................100 g SD 50 (BASF) Sorbitol........10 g 100 g 300 g – – – 3g 3g 2................................. Formulations No...15 g Magnesium stearate [2] .................12 mm Form ....................................................2....................8 Formulations of ablets T Obtained by Dir ect Compression (Lab Scale) Vitamin E Tablets (50 mg) 1.... 1 No.....................................< 0................................. Tablet properties No........................................................................410 mg Diameter .................................................9 min Friability............1% 413 mg 12 mm biplanar 70 N 11 min < 0..... 1 No...............

g. however. the amounts weighed out in the formulations correspond to the amount in the tablets multiplied by a factor of 1.2 Wet granulation technology Great significance is still attached to wet granulation. The example of a placebo tablet illustrated in Fig. eliminates all problems in wet granulation.000. The granules for tabletting were mostly produced by traditional means. moistening. Substituting Kollidon 25 or Kollidon 30 by Kollidon 90 F would be particularly interesting for obtaining greater hardness without increasing the pressure. screening. 3.e. 3 shows that tablets of twice the hardness of those obtained by Kollidon 25 can be achieved by using Kollidon 90 F at low pressures. Fluidized-bed granulation was resorted to only in exceptional cases in view of the amounts needed. Various alternatives to wet granulation in general are offered by BASF pharmaceutical excipients: – granulation with a Kollidon solution – granulation of a dry mixture of the active substance and (filler and) Kollidon with water/solvent Other alternatives consist of using different grades of Kollidon. drying. Even if the active substance is sensitive to hydrolysis. and again screening. the disintegration and the release are also affected. In practice. there would be some point in changing over from Kollidon 90 F to Kollidon 25 or 30 if the viscosity of the solution used in granulation is too high. To a certain extent. e. in a fluidized bed.3 Effect of the physical properties of the excipients Characterization of the physical properties of excipients is also important.3 Tablets obtained by wet granulation – granulation in which some of the Kollidon is mixed with the active substance and the rest of Kollidon is dissolved in the solution used for granulation 3.000 g of the mixtures to be tabletted were used. Normally. Tablets of greater hardness are obtained if fine instead of coarse Povidone K 90 is taken. Conversely. modern equipment. BASF Pharma Ingredients Generic Drug Formulations 2001 . This is demonstrated in Table 2 in the light of the example of hydrochlorothiazide.1 Size of formulations The last the of the three alternatives is preferred if the amount of liquid required for granulation is restricted and therefore does not suffice to obtain a solution of reasonable viscosity with all of the Kollidon. i. The formulations were developed on a laboratory scale in which case 200 –1. the same hardness is usually achieved by increasing the amount of Kollidon. because direct compressing is not the most suitable technology for many active substances that are in high dosages or in fine powder form. 3.

............. 422..... 37..........................0 Povidone K 90 ........... 50......5 Lactose monohydrate ....5 Magnesium stearate .... 7.............................5 mg mg mg mg mg Tablet properties Binder Hardness Disintegration time Dissolution (30 min) Povidone K 90 95 % > 250 µm 66 N 18 min 23 % Povidone K 90 15 % > 250 µm 97 N 22 min 19 % BASF Pharma Ingredients Generic Drug Formulations 2001 .....5 Water ...Hardness N Kollidon 25 Kollidon 30 Kollidon 90 F 90 80 70 60 50 40 4 6 8 10 12 Compression force kN 14 16 Fig. 2. 3 Hardness of lactose tablets containing various Kollidon products (wet granulation) Table 2 Influence of the particle size of Povidone K 90 on the properties of hydrochlorothiazide tablets (solvent granulation) Formulation I II III Hydrochlorothiazide ...

3. or USP. BASF Pharma Ingredients Generic Drug Formulations 2001 . If it is not stated to the contrary. disintegration.6 Formulations The formulations in this chapter have been arranged in the alphabetic order of their active substances. 3. friability.Eur. Unfortunately.5 Information on dissolution of active substance Nowadays it is standard practice and/or laid down that the in-vitro release of active substance be checked. the disintegration time is measured in artificial gastric juice.3. This is particularly the case when the active substance is sufficiently soluble or when the formulation was developed in a time when this parameter was not yet demanded. The release is determined by the conditions laid down in the corresponding monographs for the tablets (usually USP) and in the prescribed medium. dissolution) are contained the Pharmacopoeiae Ph. these data cannot be given for all formulations.4 Methods of measuring the properties of tablets The general instructions for the determination of the corresponding properties of tablets (hardness.

...................................................................... Physical stability (12 months.........................0.........q....9 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..........................50 g Isopropanol ................... 3........250 g Paracetamol................250 g Caffeine (BASF) ...........................biplanar Diameter ......... III............. add the components III and press with high compression force.................................670 mg Hardness............65 N Disintegration .................. dry and sieve through a 0..................................................... crystalline (Merck) ............... crystalline (Merck) .....6 min Friability........3...............................................50 g II.......... Magnesium stearate [2] ........6 Tablet formulations obtained by we t granulation (Lab Scale) Acetylsalicylic Acid + Paracetamol (= Acetaminophen) + Caffeine Tablets (250 mg + 250 mg + 50 mg) 1....45 N Disintegration ............670 mg Form ..... Formulation I.....5 g Kollidon CL [1]........ s............. Manufacturing (W et granulation) Granulate mixture I with solution II.....................7 % 4............................12 mm Hardness................................................ 20–25 °C) Weight .............................4 min Friability...8 mm screen......................................16 g 2................. Tablet properties Weight . Kollidon 90 F [1] ................ Acetylsalicylic acid..................0........................

. 3......................................................5 mm sieve..................................... 1: about 7 N Formulation No...................1% 4... Magnesium stearate [2] .. 2 Active Ingredient ..................8 mm sieve........ Ethanol 96 % .................................... dry. Lactose monohydrate ..3.... 1 No...............................1 g q........ 2...................... – Kollidon VA64 [1] .. Buccal adhesive str ength (in vitr o) One drop of human saliva was given to a glass plate and a tablet was put on this drop...15 g III........ After 7 min the force (N) was measured needed to separate the tablet vertically from the glas plate: Formulation No............ Manufacturing (W et granulation) Mix intensively the components I...................................... 76 g – 4g 19 g 10 g 1g I... sieve again through a 0.......... pass through a 0....s................................................ 2: about 3 N BASF Pharma Ingredients Generic Drug Formulations 2001 ........6 Tablet formulations obtained by we t granulation (Lab Scale) Adhesive Buccal Tablets (Basic Formulation) 1............................s..........q...200 mg Hardness.. granulate mixture I with ethanol II...........>30 min Friability.. Formulations No...8 mm Weight .................................76 g Carbopol ® 934 (Goodrich) .......4 g Carbopol 980/981 1+1 (Goodrich).........>180 N Disintegration ............................. mix with the component III and press with medium compression force to tablets... Tablet properties Diameter ...........19 g II.........<0........

.....15 g Isopropanol ......... pass through a sieve................ 2....................................................................... dibasic [9] .6 Tablet formulations obtained by we t granulation (Lab Scale) Alpha-Methyldopa Tablet Cores (250 mg)........... 1 No........................82 % (30 min) ...............................5 min Friability..............2 g 275 g – 55 g 15 g 80 ml 8g 2g I.....................275 g Lactose monohydrate [8] ............................... mix the dry granules with III and press with medium compression force......1% 55 % 90 % 98 % BASF Pharma Ingredients Generic Drug Formulations 2001 ............11 mm Hardness ......80 ml III.....55 g Calcium phosphate....45 % (20 min) ...... 2 Alpha-Methyldopa .....<0....... 3............ Kollidon CL [1] ....... Formulations No.............................................................................................1% Dissolution (10 min)..............................................361 mg Diameter ............................................. WG 1... Tablet properties No.......................90 % 362 mg 11 mm 156 N 4 min <0.. 2 Weight ......................... Manufacturing (W et granulation) Granulate mixture I with solution II.........3............................ Kollidon 30 [1] ...........8 g Magnesium stearate [2] ...118 N Disintegration ..................... 1 No............................................– II.......................

..0.......................................... mix with III and press with low/medium compression force.............80 N Disintegration .........................790 mg Diameter ..............– II...................12 mm Form ..35 ml III............................ Kollidon 30 [1]........................biplanar Hardness ........................................5 g Magnesium stearate [2] . pass through a 0...........................................................................................– 500 g – 200 g – 10 g q.5 % 696 mg 12 mm biplanar 95 N 4 min 0....– Isopropanol .................................30 g Kollidon 90 F [1] ......................20 g Talc [10] ............... 1 No..................... 2 Alpha-Methyldopa .. 3...........8 mm sieve..... Tablet properties No.........................– Aerosil 200 [4]..98 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...................................... Formulations No....................... 15 g 8g 2g – 2g I....................................................................... 2 Weight ....................... 2.......................... Kollidon CL ...................................s.....500 g Lactose monohydrate [8] ........200 g Corn starch [3] ................. WG 1............................8 g Calcium arachinate [2] .................................6 Tablet formulations obtained by we t granulation (Lab Scale) Alpha-Methyldopa Tablets (500 mg)................... 1 No............. Manufacturing (W et granulation) Granulate the mixture I with solution II....................................................3............5 min Friability .....

WG page 2 4. BASF Pharma Ingredients Generic Drug Formulations 2001 . Remark For the production of tables cores for coating purposes the oblong form would be better.Alpha-Methyldopa T ablets (500 mg).

.........23 Magnesium stearate [2] .............213 Corn starch [3] .....................................................................6 Tablet formulations obtained by we t granulation (Lab Scale) Aluminium Acetylsalicylate Tablets (250 mg) 1......................3.5 g g g g g g g g 2..10 Lutrol E 6000 [1]....................... mix with III and press with medium compression force........... Tablet properties Weight ..............1 – 2 min Friability................................4 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...........................110 N Disintegration...................................................................... Formulation I..... Kollidon CL [1] ...............about 50 III......................................................5 Isopropanol .....................................12 mm Form .............0....255 Mannitol ....................................8 mm sieve.........................28 II..biplanar Hardness ................ dry...............540 mg Diameter ................... Aluminium acetylsalicylate ............................................... pass through a 0.......... Kollidon 90 F [1] .......... 3. Manufacturing (W et granulation) Granulate mixture I with solution II....

......9 Saccharin sodium....................97 Kollidon 90 F [1] ................1 Talc [10] ......................................................... dry..... Menthol ........... Manufacturing (W et granulation) Granulate mixture I with the simethicone suspension II.................................... suspension 30 % ......130 N Disintegration ..............................................................576 Aluminium hydroxide................................. Sucrose .....................................0........................ Formulation I....................................... Properties of the table ts pressed with two dif ferent diameters 12 mm 20 mm Weight .......13 g g g g g g g g g g g 2..............................................biplanar Hardness.............................................. add III and press with high compression force............160 Magnesium oxide ....................... sieve through a 0....................3.......8 mm screen...........................22 II............1% 1295 mg biplanar 55 N 7 min 0....45 Aerosil 200 [4] ..........7 % BASF Pharma Ingredients Generic Drug Formulations 2001 ............. Simethicone.......30 min Friability....................1200 mg Form ......... 3...................49 Magnesium stearate [2].........157 Magnesium carbonate ..........................6 Tablet formulations obtained by we t granulation (Lab Scale) Aluminium Hydroxide + Magnesium carbonate/oxide + Simethicone Tablets (150 mg + 250 mg + 90 mg) 1..................300 III................

.. Tablet properties Weight........0...............6 Magnesium stearate [2] .....................................................315 Sorbitol..........30 Water........................ Sucrose.................... 3............................... Formulation I.............100 II.............. Kollidon VA 64 [1] ..................................... powder [6].................................................................biplanar Hardness ........................................ pass through a 0......................27 min Friability....1013 mg Diameter ........... crystalline..60 Aerosil 200 [4] .........6 g g g g g g g g g g g 2................. crystalline (Merck) ..200 Magnesium hydroxide (Rorer) ......6 Tablet formulations obtained by we t granulation (Lab Scale) Aluminium Hydroxide + Magnesium Hydroxide Chewable Tablets (200 mg + 200 mg) 1......100 Polyethylene glycol 6000... add III and press with high compression force (20 kN)......12 Talc [10] ................3....260 III....................................8 mm sieve........................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 .131 N Disintegration ..... Manufacturing (W et granulation) Granulate mixture I with solution II................................................... dry...200 Lactose monohydrate [8]......................16 mm Form ....................................................................... Aluminium hydroxide (Rorer).

....... Formulations No.... pass through a 0.............................6 Tablet formulations obtained by we t granulation (Lab Scale) Aminophylline Tablets (90 mg) 1..............8 mm sieve..3 – 4 min Friability ............................ powder [6] ......1 g Talc [10] ....80 N Disintegration ..... Manufacturing (W et granulation) Granulate mixture I with solution II.80 g Corn starch [3] ................................... hydrous powder (BASF) ...3.........................3 g II......5 mm sieve and press to tablets with medium compression force....... dry............ pass through a 0..............0........... Kollidon VA 64 [1].......................................... Tablet properties No........................4 % 180 mg 8 mm biplanar 72 N 6 – 7 min 0.......... 1 No...........3 g Water ...... 3...............4 g Polyethylene glycol 6000.................. Magnesium stearate [2] ..– 90 g – 74 g 3g 3g 27 g – – 10 g I.......................................– Kollidon VA 64 [1]........4 % BASF Pharma Ingredients Generic Drug Formulations 2001 . 2 Aminophylline....................................30 g III.....................90 g Potato starch [3] ....................................................................... mix with III..........................................................biplanar Hardness ..... 1 No............8 mm Form .179 mg Diameter ....................................................... 2 Weight ............................................ 2.................

...................................................0 Corn starch ..0 g g g g g g 2.....8 mm sieve.......6 Tablet formulations obtained by we t granulation (Lab Scale) Aminophylline Tablets....................... Magnesium stearate [2]..............................200 mg Hardness...... dry..........................................................1..........6...0 III....... Aminophylline..............................22...0....3 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...... Tablet properties Diameter .8 mm Weight ........................... mix with the components III and press with low compression force to tablets........0 Kollidon 30 [1] ...............3...... fine powder (BASF)..........100....................... 3.............69 N Disintegration ............... WG (100 mg) 1..100... Manufacturing (W et granulation) Granulate mixture I with water II.. pass through a 0.5 Talc [10] ..........................0 II............4-5 min Friability....... Formulation I.......... Water.......................3.....................................

............................ sieve and mix with III..............................3.. Kollidon 30 [1] .................62 N Disintegration ......... Tablet properties Weight ....125 Corn starch [3] ..................... Press with low compression force............................4 min Friability...............6 Tablet formulations obtained by we t granulation (Lab Scale) Amoxicillin Tablets (125 mg) 1.......2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ....................................................................................... Manufacturing (W et granulation) Granulate mixture I with solution II........... dry............about 60 III.............................................9 Water ................297 mg Diameter .. Kollidon CL [1]..................12 mm Form ...................... Amoxicillin ..................................... Formulation I..................biplanar Hardness..........................15 Magnesium stearate [2] ...................148 II...................3 g g g g g g 2..................0............. 3...............................

...... 1 No................6 Tablet formulations obtained by we t granulation (Lab Scale) Ampicillin Tablets (500 mg) 1..................0..................170 N Disintegration ................. dry.................– II.... 2......2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..5 min Friability .s................... Kollidon VA 64 [1] ................................ Formulations No.......................... crystalline [10] .... Manufacturing (W et granulation) Granulate mixture I with solution II....... Tablet properties No.........................8 mm sieve................... 3......................16 mm Hardness ..25 g Isopropanol or water ................. s..... pass through a 0.....................798 mg Diameter ................................8 g 500 g – 242 g 25 g q..10 g Aerosil 200 [4] .......................... Kollidon CL [1] .......500 g Corn starch [3] ..........................242 g Sorbitol......................... 12 g 10 g 8g I............................................. 2 Weight ....................4 % 822 mg 16 mm 154 N 11 min 0.................................3.................... 2 Ampicillin trihydrate ..................... III...... 1 No.....12 g Magnesium stearate [2]............. mix with III and press with high/medium compression force.q.................................

......................... Water...5 mm Form .. WG 1................................................................................... Tablet properties Weight .........60 mg Diameter .................. Kollidon CL [1] ................... 3..biplanar Hardness.....................3 Polyethylene glycol 6000................25 Kollidon VA 64 [1] ......................3.............10 III.................. mix with III and press to tablets.. powder [6]....................25 Dibasic calcium phosphate [9].60 N Disintegration ............................................6 Tablet formulations obtained by we t granulation (Lab Scale) Aspartame Tablets (25 mg)......... Aspartame ...................................8 mm sieve..... Manufacturing (W et granulation) Granulate the mixture I with II................................................................3 II...................................1% BASF Pharma Ingredients Generic Drug Formulations 2001 . Formulation I.......3 g g g g g g 2...........1 min Friability ................... pass through a 0.............< 0.........

.200 g II............ Kollidon 90 F [1] .......biplanar Hardness................. mix with III and press with medium compression force.......... pass through a sieve.q.............. 3.....................................4 g 2..............................3............6 Tablet formulations obtained by we t granulation (Lab Scale) Bran Tablets (250 mg)...........................................4 % BASF Pharma Ingredients Generic Drug Formulations 2001 .............s...................................467 mg Diameter .... Manufacturing (W et granulation) Granulate mixture I with solution II............................................3 min Friability...............70 N Disintegration .. WG 1.....12 g Water ........... Bran wheat (milled <1 mm)................3 g III.. powder [6]..............................12 mm Form ......................................... Tablet properties Weight ...................................... Magnesium stearate [2] ........250 g Dibasic calcium phosphate [9] ................ Polyethylene glycol 6000...... Formulation I....0............

................3............... Calcium carbonate................. Manufacturing (W et granulation) Granulate mixture I with the water II..... Water............................120 N Disintegration........................ 3.............. mix the dry granules with III and press with low compression force............. Formulation I...................................................97 III............................. pass through a sieve.......32 Ludipress [1] ..................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ..12 mm Form .......................... Tablet properties Weight ...53 g g g g g 2.......656 mg Diameter .....10 min Friability ............ precipitated ...............................biplanar Hardness ....0.........................................500 Kollidon 30 [1] .................................................................. Kollidon CL [1] ................65 II..................6 Tablet formulations obtained by we t granulation (Lab Scale) Calcium Carbonate Tablets (500 mg) 1.................................

.........................6 Tablet formulations obtained by we t granulation (Lab Scale) Calcium Effervescent Tablets (250 mg Ca) 1....... powder [6].... Kollidon 30 [1] .................. Tablet properties Weight ............................................2560 mg Diameter ........... Formulation I................................650 g Calcium gluconate .... mix with III and press with low compression force.....20 mm Form ......... dry.....................12 g Isopropanol ..................................................s....................................................s..2 – 3 min Friability. Manufacturing (W et granulation) Granulate mixture I with solution II........................................... 3....100 g Polyethylene glycol 6000..................190 g Sodium bicarbonate..480 g Kollidon 30 [1] .............................................. III........................................................................ sieve..............................48 g II.........410 g Tartaric acid . Kollidon CL [1] .................................0...............................48 g Flavour ..3....5 % BASF Pharma Ingredients Generic Drug Formulations 2001 ............. Calcium lactate ......625 g Calcium carbonate... 2........................................................biplanar Hardness ..193 N Disintegration (water)........................q....................q..........

............12 mm Form .......118 N Disintegration (water)..................3......................................biplanar Hardness ......... powder...........117 II..................... Formulation I.........500 mg Diameter ...............8 mm sieve........ mix with III and press with high compression force...11 Isopropanol......6 Tablet formulations obtained by we t granulation (Lab Scale) Calcium Gluconate Tablets (350 mg) 1.......................................................................................... Kollidon CL [1] ......... dry....................... Manufacturing (W et granulation) Granulate mixture I with solution II............ Tablet properties Weight ...................................2 g g g g g g 2.................................................................90 III............. 3.. Calcium gluconate.....................25 Magnesium stearate [2] ... Kollidon 30 [1] .................. pass through a 0.............< 0...........360 Lactose monohydrate [8] ...............16 min Friability ..1% BASF Pharma Ingredients Generic Drug Formulations 2001 ..........

..........15.....................................15.........0 Magnesium stearate [2].............0 Water................................................... Tablet properties Weight .......... sieve and mix with III..117.......... Kollidon 90 F [1] . Kollidon CL [1] ............220 N Disintegration ... 3........................6 Tablet formulations obtained by we t granulation (Lab Scale) Calcium Glycerophosphate Tablets (500 mg) 1..........650 mg Diameter ..........5 II.....................3............0 III................ Calcium glycerophosphate .500...................0 Corn starch [3] ........................................................................................12 mm Form ........... dry...........7 min Friability .................................5 g g g g g g 2...0.......2................. Press with medium to high compression force.........................60.....1% BASF Pharma Ingredients Generic Drug Formulations 2001 ........ Formulation I.................................. Manufacturing (W et granulation) Granulate mixture I with solution II........biplanar Hardness...

..12 mm Form ......q........................150 g III...............................s.............................biplanar Hardness................................................................. Kollidon 30 F [1] ...........................................6 Tablet formulations obtained by we t granulation (Lab Scale) Calcium Phosphate Tablets for Cats and Dogs (400 mg) 1... Magnesium stearate [2] ...... dry and pass through a 0......................................... add III and press with medium to high compression force (20 kN)................100 g Citric acid crystalline ...1% BASF Pharma Ingredients Generic Drug Formulations 2001 .....30 g Water.................0................180 N Disintegration .... Manufacturing (W et granulation) Granulate mixture I with solution II...................................... II..8 – 9 min Friability............8 mm sieve....................................................... Formulation I....... Tablet properties Weight . 3..................................................800 mg Diameter ...........................................262 g Flavours.............400 g Wheaten flour.................. Dicalcium phosphate [9] .3.........................................................4 g 2...................1 g Lactose monohydrate [8] ...............................................

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Carbamazepine Sustained Release Tablets
(200 mg) WG

1. Formulation
I

II
III

Carbamazepine (Sintetica)........................200
Granulac 140 [8] ......................................148
Kollidon CL-M [1] ......................................20
Kollicoat SR30D [1] ...................................99
Aerosil 200 [4] .............................................2
Magnesium stearate [2] ...............................2

g
g
g
g
g
g

2. Manufacturing (W
et granulation)
Granulate the mixture I with Kollicoat SR30D (II) in a fluidized bed, mix
with the components of III and press with medium compression force.
3. Tablet properties
Weight .................................................407 mg
Diameter ...............................................11 mm
Form ..................................................biconvex
Hardness ................................................136 N
Disintegration ..........................................1 min
Friability ................................................< 0.1%

BASF Pharma Ingredients Generic Drug Formulations 2001

Carbamazepine Sustained Release
ablets
T
(200 mg) WG

page 2

carbamazepin release [%]

4. Release of carbamezepine (0-2
h: 0.08N HCl, 2-24
h: pH 6.8)
100
80
60
40
20
0
0

2

4

6

8

10

12
14
time [%]

BASF Pharma Ingredients Generic Drug Formulations 2001

16

18

20

22

24

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Caroate Dispersible Cleaning Tablets
(880 mg)

1. Formulation
I.
II.

Sodium chloride ......................................884 g
Kollidon VA 64 [1] ......................................47 g
Ethanol or Isopropanol................................q.s.
III. Caroate...................................................884 g
Kollidon CL [1] ..........................................93 g
Polyethylene glycol 6000, powder ..............93 g
2. Manufacturing (W
et granulation)
Granulate I with soluton II, pass through a 0.8 mm sieve, dry, mix with
the components III and press to tablets.
3. Tablet properties
Weight ..............................................2,000 mg
Diameter ...............................................20 mm
Form ...................................................biplanar
Hardness ................................................130 N
Disintegration (water)...........................< 30 sec
Friability ................................................< 0.1%

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Caroate Effervescent Cleaning Tablets
(650 mg)

1. Formulation
I.
II.

Sodium chloride ......................................488 g
Kollidon VA 64 [1] ......................................49 g
Ethanol or Isopropanol................................q.s.
III. Caroate...................................................650 g
Tartaric acid ............................................325 g
Sodium bicarbonate ................................407 g
Polyethylene glycol 6000, powder ..............81 g
2. Manufacturing (W
et granulation)
Granulate I with soluton II, pass through a 0.8 mm sieve, dry, mix with
the components III and press to tablets.
3. Tablet properties
Weight ..............................................2,000 mg
Diameter ...............................................20 mm
Form ...................................................biplanar
Hardness ................................................140 N
Disintegration (water) ...............................2 min
Friability...................................................0.3 %

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Charcoal Tablets I
(250 mg)

1. Formulation
I.

Activated charcoal ..................................250
Kollidon VA64............................................50
Sorbit, crystalline [10] ...............................110
II. Acacia gum ...............................................50
Water .....................................................275
III. Lutrol E4000F [1].........................................2

g
g
g
g
g
g

2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, pass through a 0.8 mm sieve, dry
until the relative powder humidity of 40 – 50 % is reached, pass again
through a 0.8 mm sieve, mix with III and press with high compression
force.
3. Tablet properties
Weight .................................................447 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardness .................................................27 N
Disintegration ..........................................7 min
Friability...................................................0.5 %

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Charcoal Tablets II
(250 mg)

1. Formulation
I.

Activated charcoal ..................................250 g
(Carbo medicinalis, Merck)
Bolus alba (Merck) ...................................150 g
II. Kollidon 25 [1] ...........................................28 g
Acacia gum ...............................................38 g
Water + isopropanol (10 + 3)...................575 ml
III. Cremophor EL [1] ......................................15 g
Isopropanol ...........................................300 ml
2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, pass through a 1 mm sieve, dry until
the relative powder humidity of 90 % is reached, add solution III and pass
again through a sieve. Dry the granules and press with low compression
force. Dry the obtained tablets.
3. Tablet properties
Weight .................................................481 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardness..................................................55 N
Disintegration ..........................................1 min

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Chloroquine Tablets
(250 mg)

1. Formulation
I.

Chloroquine diphosphate .........................250
Dicalcium phosphate, DI-TAB [9] ..............100
II. Kollidon 30 [1] ...........................................10
Isopropanol...............................................83
III. Kollidon CL [1]...........................................10
Aerosil 200 [4] .............................................2
Talc [10] ......................................................3

g
g
g
g
g
g
g

2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, dry, pass through a 0.8 mm sieve,
add the mixture III and press with low compression force.
3. Tablet properties
Weight .................................................361 mg
Diameter .................................................8 mm
Form ...................................................biplanar
Hardness................................................202 N
Disintegration ..........................................8 min
Friability ................................................< 0.1%

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Cimetidine Tablets
(280 mg)

1. Formulation
I.

Cimetidine...............................................288
Corn starch [3] ........................................122
II. Kollidon 30 [1] ...........................................14
Water........................................................72
III. Magnesium stearate [2] ...............................2

g
g
g
g
g

2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, pass through a 0.8 mm sieve, add III
and press to tablets with low compression force.
3. Tablet properties
Weight .................................................427 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardness ................................................108 N
Disintegration ..........................................3 min
Friability...................................................0.2 %

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Cimetidine Tablets
(400 mg)

1. Formulation
I.

Cimetidine...............................................400
Corn starch [3] ........................................170
II. Kollidon VA 64 [1] ......................................20
Water ......................................................100
III. Magnesium stearate [2] ...............................3

g
g
g
g
g

2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, pass through a 0.8 mm sieve, add III
and press to tablets with low compression force.
3. Tablet properties
Weight .................................................601 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardness..................................................91 N
Disintegration ..........................................4 min
Friability...................................................0.5 %
Dissolution (10 min) ...................................62 %
(20 min) ...................................91%
(30 min) .................................100 %

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Crospovidone Effervescent Tablets
(1000 mg)

1. Formulation
I.

Crospovidone, micronized ......................1000 g
(Kollidon CL-M, BASF)
Citric acid................................................150 g
Aerosil 200 [4] ...........................................25 g
II. Sucrose, crystalline..................................100 g
Saccharin sodium........................................1 g
Water.........................................................q.s.
III. Magnesium stearate [2] ...............................5 g
Sodium bicarbonate.................................125 g
Flavour mixture..........................................65 g
2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, pass through a sieve, mix the dry
granules with III and press with medium compression force.
3. Tablet properties
Weight ...............................................1590 mg
Diameter ...............................................20 mm
Form ...................................................biplanar
Hardness ................................................111 N
Disintegration ..........................................1 min
Friability...................................................0.4 %
4. Remark
The dosage may be increased to 2000 mg crospovidone by increasing
the tablet weight to 3200 mg.

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Crospovidone Water Dispersible Tablets
(1000 mg)

1. Formulation
I.

Crospovidone M (BASF) .........................1000
Aerosil 200 [4] ...........................................50
II. Sucrose, crystalline .................................250
Saccharin sodium........................................5
Flavours ..................................................2-3
Water......................................................380
III. Magnesium stearate [2] ...............................5

g
g
g
g
g
g
g

2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, pass through a sieve, mix the dry
granules with III and press with low compression force.
3. Tablet properties
Weight ...............................................1280 mg
Diameter ...............................................20 mm
Form ...................................................biplanar
Hardness ................................................103 N
Disintegration......................................1 – 2 min
Friability ..................................................0.6 %
4. Remark
The dosage may be increased to 2000 mg Crospovidone by increasing
the tablet weight to 2600 mg.

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Diclofenac Tablet Cores
(50 mg)

1. Formulation
I.

Diclofenac sodium (Chemag)......................50 g
Calcium phosphate, dibasic [9].................132 g
Kollidon 30 [1] .............................................6 g
II. Ethanol 96 % ..............................................q.s.
III. Kollidon CL [1]...........................................10 g
Magnesium stearate [2] ...............................2 g
2. Manufacturing (W
et granulation)
Granulate mixture I with solvent II, pass through a 0.8 mm sieve, add III
and press with low compression force.
3. Tablet properties
Weight .................................................209 mg
Diameter .................................................8 mm
Form ..................................................biconvex
Hardness..................................................72 N
Disintegration ..........................................7 min
Friability...................................................0.4 %

BASF Pharma Ingredients Generic Drug Formulations 2001

........................... mix with III and press with low compression force........................9 mm Form .......6 Tablet formulations obtained by we t granulation (Lab Scale) Dimenhydrinate Tablet Cores (100 mg) 1.........................................27 N Disintegration ..... Formulation I.............................................. Manufacturing (W et granulation) Granulate mixture I with solution II..........14 Talc [10] .......................... 3........100 Lactose monohydrate [8] ............................................................3......2 Calcium arachinate [2] ....................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ........................................ Kollidon CL [1]..................................................................... pass through a 0....6 II........................biconvex Hardness .........40 Kollidon 90 F [1] ................................... Dimenhydrinate ............40 Corn starch [3] .......2 g g g g g g g g g 2........210 mg Diameter ...8 mm sieve...... dry...............................< 1 min Friability................................................. Tablet properties Weight ..............................................16 Aerosil 200 [4] .............................30 III................... Isopropanol.

.......3 min Friability .........3....................5 g 2...........................................8 mm sieve......... 1 I...0 Kollidon CL [1] ...5 g g g g g g g g No................1............60 N Disintegration ............0 II..............209 mg Diameter ................ 2 Weight .....15...........5 g 1...... mix with III and press with low compression force.......................................0 Lactose monohydrate D 20 [8] .2....... WG 1........................0 Magnesium stearate [2] .............0 g 1....98 % 202 mg 8 mm biplanar 48 N 1 min 0............. 2 50....................... 1 No.... Formulations No......0 g -130....................4 % 83 % 93 % 96 % BASF Pharma Ingredients Generic Drug Formulations 2001 .....69 % 30 min .................8 mm Form ... Dimenhydrinate .. dry....................0 III...................5 g 3..................2...........biplanar Hardness ............................50..................0 g 15.15 min ...............0 g 1.................... Kollidon CL [1] ..80.....6 Tablet formulations obtained by we t granulation (Lab Scale) Dimenhydrinate Tablets (50 mg)......3..................... Ethanol .....................................................................91% 45 min ............ pass through a 0.......... 3................50...................0 Corn starch [3] .0 Kollidon VA 64 [1] ......... Tablet properties No............... Manufacturing (W et granulation) Granulate mixture I with the solvent II............25 % Dissolution in water (USP)........0...................

.... pass through a 0...............4 % BASF Pharma Ingredients Generic Drug Formulations 2001 ............. IV....................................................................10 g 2..........s............8 mm sieve.............40 g II..... Tablet properties Weight ...........9 min Friability..... mix with the components I and IV and press with high compression force....12 mm Form ........................97 N Disintegration ........3.....400 g Kollidon CL [1] ...................................... dry.............. WG 1..........6 Tablet formulations obtained by we t granulation (Lab Scale) Ethambutol Tablets (400 mg).............................................. Manufacturing (W et granulation) Granulate mannitol II with solution III..................... Mannitol................................... 3.................................... Formulation I..............biplanar Hardness........7 g Water.... Kollidon 30 [1] ..........0.........................622 mg Diameter .........................200 g III............................................... Magnesium stearate [2].................................... Ethambutol .......q....

..................... pass through a 0.......................................................................oblong Hardness...........200 g II. Formulation I...............................15 g 2...s... Kollidon CL [1] ......................................1.. Ethambutol (Helm) ..78 N Disintegration .6 Tablet formulations obtained by we t granulation (Lab Scale) Ethambutol Tablets (800 mg) 1...............................................................................800 g Dicalcium phosphate.................................................. 3...........2 min Friability ............... add III and press with high compression force..... DI-TAB [9] .112 mg Diameter ........8 mm sieve..............................20 mm Form ..............50 g Magnesium stearate [2].... dry....................q.... Kollidon 30 [1] ............... Tablet properties Weight ............3.......30 g Isopropanol ..............1% BASF Pharma Ingredients Generic Drug Formulations 2001 ................. Manufacturing (W et granulation) Granulate mixture I with solution II....... III.....................1..

............................................... Formulation I........................8 mm Form ........... Etophylline..... anhydrous 0........3 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......8 mm sieve.. mix with III.......0..................... Manufacturing (W et granulation) Granulate mixture I with solution II............92 N Disintegration ......................................biplanar Hardness....3..................7 (BASF) ........................183 mg Diameter ..........1 Talc [10] ......50 Kollidon VA 64 [1] ......................35 III.......2/0... Kollidon VA 64 [1] .....23 Corn starch or potato starch ..........................4 Water............................................................ 3. powder .................. Magnesium stearate [2] . pass through a 0......... WG 1.................................. dry.100 Theophylline.............6 Tablet formulations obtained by we t granulation (Lab Scale) Etophylline + Theophylline Tablets (100 mg + 22 mg)......... Tablet properties Weight .............5 g g g g g g g g 2.................................................5 mm sieve and press with medium compression force............3 – 4 min Friability............3 II......... pass through a 0..........................................

............................... BASF Pharma Ingredients Generic Drug Formulations 2001 ........... pass through a 0......... Formulation I..........63..............................3.2..55 N Disintegration ..... Tablet properties Weight .....0 g II......biconvex Hardness..... DI-TAB [9] ... Kollidon 90 F [1] ............... 3............ Manufacturing (W et granulation) Granulate mixture I with solution II.......................................2 g Aerosil 200 [4] .....6 Tablet formulations obtained by we t granulation (Lab Scale) Fusidic Acid Tablet Cores (125 mg) 1.............200 mg Diameter ..........................................8 mm sieve.........125............ sodium salt ..3.0 g 2....................................3 g Magnesium stearate [2]............. Remark To accelerate the disintegration the amount of Kollidon 90 F should be reduced and Kollidon CL should be applied in intra.................................30 ml III......................... Fusidic acid..........6............. add the mixture III and press with low compression force..............9 mm Form ..5 g Isopropanol ..........0 g Dicalcium phosphate.0 % 4..and extragranular form................... dry..................................................1.................25 min Friability ............. Kollidon CL [1] .....................

...3....................... Tablet properties Weight ... Dried garlic powder ....... BASF Pharma Ingredients Generic Drug Formulations 2001 ...................6 Tablet formulations obtained by we t granulation (Lab Scale) Garlic Tablets Cores (100 mg) 1...............................................................................9 Water... add III and press with low compression force...............100 Magnesium stearate [2] ........ Kollidon 30 [1] ..... Calcium phosphate..2 g g g g g g 2......... pass through a 0........................................................ Manufacturing (W et granulation) Granulate mixture I with solution II...................95 Lactose monohydrate [8] ........23 min Friability...25 III.0..................94 II....................312 mg Diameter .........biconvex Hardness.............................98 N Disintegration .....8 mm sieve...3 % 4.........................9 mm Form ................. Remark These tablets could be commercialized in Europe as dietary food because all components are allowed for this application........... Formulation I............................. dibasic [9] ................................................................. 3.....................

.... mix..... Spray conditions: Inlet temperature .........s..... Talc ................4...........about 100 min BASF Pharma Ingredients Generic Drug Formulations 2001 ..................45 psi Spray time .......................................................................2..........0..8 % Prepare the two suspensions separately.......0 % Sicovit Iron Oxide Red.... II............................................0.....2 % Water ........................................................................................25..............................................Garlic Tablet cores (100 mg) page 2 5............... Masking of the garlic smell To mask the smell of the tablets the following coating formulation could be applied: I.............. Kollicoat MAE 30DP ...........................38-40 ml/min Pan speed ..............5 % Sicovit Titanium Dioxide .....................55-60°C Outlet temperature .......... pass through a colloid mill and spray onto the tablet cores in a perforated coating pan (e.........5 % Vanilline .....10 % of the cores ist obtained...50..........g....32-34°C Spray rate ..........................q...................... Accela Cota 24 inch) until a weight gain of 8 ...0 % Water........................................0 % Triacetin ....................................................17....about 11 rpm Atomizing air pressure .......

..............................200 Kollidon CL [1] ...................................................................................40 Magnesium stearate [2] .......16 mm Form ........8 g g g g g g g g g g 2................. 28 kN) to tablets 3.. USP (paddle)................ 10 min...............84 % 30 min ..............86 % BASF Pharma Ingredients Generic Drug Formulations 2001 .......................20 Aerosil 200 [4] ...................... Press with high compression force (e.............10 Talc [10] .... Tablet properties Weight ...............................about 72 Kollidon CL [1] ....................................................................................... dry..........................................................40 Ethanol 96 % .................. Formulation I II III Gemfibrozil.. pass through a 0......2 min Friability......biplanar Hardness ......950 mg Diameter ........................70 % 20 min ........0........................................8 mm sieve and mix with the components III...7 % Dissolution...............................600 Corn starch [3] ..g......... powder [6] ......................30 Kollidon VA64 [1] ...3...................................................................151 N Disintegration ....... Manufacturing (W et granulation) Granulate mixture I with ethanol II..................20 Polyethylene glycol 6000......6 Tablet formulations obtained by we t granulation (Lab Scale) Gemfibrozil Tablets (600 mg) 1...............

.................................. Kollidon CL [1] ....................................biplanar Hardness .....12 mm Form . crystalline [10] .......................... Formulation I.115 g II........... III...........s......6 min Friability....................................6 Tablet formulations obtained by we t granulation (Lab Scale) Glutaminic Acid Tablets (550 mg) 1................. dry.......573 g Sorbitol............................................2 g 2...............2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........................................q..............17 g Water............. Glutaminic acid ............ Manufacturing (W et granulation) Granulate mixture I with solution II...........3..... Kollidon 30 [1] ........8 mm sieve and mix with III..................................11 g Magnesium stearate [2] .......... Press with low compression force to tablets.................. pass through a 0..719 mg Diameter ...0..........138 N Disintegration ................................ Tablet properties Weight............................................................ 3.........................

.5 % BASF Pharma Ingredients Generic Drug Formulations 2001 .... Griseofulvin .....6 Tablet formulations obtained by we t granulation (Lab Scale) Griseofulvin Tablets (500 mg) 1.............. Manufacturing (W et granulation) Dissolve mixture I in the solvent II.........................7...2 min Friability..........500 III..... Kollidon CL [1] ................................. Formulation I...........................75 Magnesium stearate [2] .......0..... 3........5 mm sieve............12 mm Form ............................751 mg Diameter ............................................................................................................... pass the obtained coprecipitate through a 0......100 II.............5 Aerosil 200 [4] ..............5 g g g g g g g 2...........................75 Lactose monohydrate [8] .............................................................. evaporate to dryness.........3......................... Dimethyl formamide ...........biplanar Hardness.........................62 N Disintegration ........................ Tablet properties Weight ...............500 Kollidon VA 64 [1] ..................... mix with III and press with low compression force...........

...................2 – 3 min Friability............12 mm Form ....75 N Disintegration.....................................456 g Kollidon VA 64 [1] ...2 % BASF Pharma Ingredients Generic Drug Formulations 2001 .................. Horsetail extract............3....... Tablet properties Weight ...... mix with III and press with high compression force......................14 g Lutrol F 68 [1] ........... dry..............................q..................0...... 3..................6 Tablet formulations obtained by we t granulation (Lab Scale) Horsetail Extract Tablets (450 mg) 1...............................14 g Magnesium stearate [2]...............5 g Isopropanol ............................................... Formulation I............................biplanar Hardness......................... powder ......... 2.......s.......8 mm sieve........... pass through a 0.................... Kollidon CL [1]..about 120 g III.......489 mg Diameter ..................... II.......................................... Manufacturing (W et granulation) Granulate the extract I with solution II.........................

..........3........................................biplanar Hardness.................................. Tablet properties Weight ....................2 g 2..< 1 min Friability ........................................................ WG 1.......................... 2-Propanol ....< 0. Formulation I........422 g Kollidon 90 F [1] .......... Manufacturing (W et granulation) Granulate mixture I with solution II.8 mm sieve........................................................... Hydrochlorothiazide (Chemag).. Kollidon CL [1]....... pass through a 0...............55 N Disintegration ..... add III and press with low compression force..............15 g Magnesium stearate [2] ..........................495 mg Diameter ..............100 % BASF Pharma Ingredients Generic Drug Formulations 2001 .................................................1% Dissolution (30 min).........12 mm Form ..........................6 Tablet formulations obtained by we t granulation (Lab Scale) Hydrochlorothiazide Tablets (50 mg)...................38 ml III............8 g II...................50 g Lactose monohydrate [8] ............................................................... 3.............92 % (60 min) .........

.........................................8 g – 289 g 15 g q.12 mm Form ........................................................4 % Dissolution (30 min) ................ Dissolution stability of formulation No..........................................................85 % 741 mg 12 mm biplanar 177 N 1-2 min 0. Manufacturing (W et granulation) Granulate mannitol or dicalcium-phosphate with solution II............................. 1 (3 months.....– II......90 N Disintegration ............................................................................ Tablet properties No............................. III....s................774 mg Diameter ...........3 % – 4....... 20–25 ºC) Dissolution (30 min)................. add III and press with low compression force..8 mm sieve.......... 2 Weight ........12 g Water ....................................400 g Kollidon CL [1] ..16 g Aerosil 200 [4].......... WG 1................ 1 No...biplanar Hardness ..................... 3..........................81% BASF Pharma Ingredients Generic Drug Formulations 2001 .... 2 Mannitol ......................................0......q..... Formulations No.....................8 g Magnesium stearate [2] .................... Kollidon 30 [1] ..... Ibuprofen (BASF) ......................... pass through a 0................. 1 No.............................s................................................................................ 400 g 38 g I...................2 min Friability ........6 Tablet formulations obtained by we t granulation (Lab Scale) Ibuprofen Tablets (400 mg)..330 g Dicalcium phosphate [9] ......... 8g 2..3..

....1% BASF Pharma Ingredients Generic Drug Formulations 2001 ............372 mg Diameter ............................................................1% Dissolution..........................................................................50 Lactose monohydrate [8] ... 3......................... pass through a 0.......................... Kollidon CL [1]...............1% 0...........75 % 20 min . Manufacturing (W et granulation) Granulate mixture I with solution II....................... Kollidon 30 [1] .......0......................2 g g g g g g g 2................................................. Indomethacin ........<1 min Friability ................................................... WG 1.12 Aerosil 200 [4] .............3.................... Tablet properties Weight ........... 10 min..............8 mm sieve....10 Water.....72 N Disintegration ....300 II......2 Magnesium stearate [2] ...biplanar Hardness......12 mm Form ................................................. Formulation I..........................................................6 Tablet formulations obtained by we t granulation (Lab Scale) Indomethacin Tablets (50 mg).....30 III.......... Physical stability (20–25°C) Storage time Hardness Disintegration Friability 6 Months 12 Months 70 N 55 N <1 min <1 min 0........................ add III and press with low compression force.....................................88 % 4...

............................................... Tablets properties Weight ......................... 3.51 g Kollidon 90 F [1] .........0 % BASF Pharma Ingredients Generic Drug Formulations 2001 .................6 Tablet formulations obtained by we t granulation (Lab Scale) Inosin Tablet Cores (200 mg) 1.......6 g II....... pass through a 0.............. Formulation I.............................................3 g 2.3 – 4 min Friability ..............10 g Magnesium stearate [2] ..60 ml III.......270 mg Diameter .............. dry..............55 N Disintegration ..................................200 g Lactose monohydrate [8] ............................ add the components III and press with low compression force................ Manufacturing (W et granulation) Granulate mixture I with the solvent II..................biconvex Hardness................ Kollidon CL [1]....................3................................. Russia) .................................... Isopropanol ............9 mm Form ....... Inosin (Ribaxin.........................................8 mm sieve.................................

.....1000 mg Diameter . Tablet properties Weight...................................................50 II.................. Aerosil 200 [4] ................good BASF Pharma Ingredients Generic Drug Formulations 2001 ....................................16 mm Form .............................20 Banana flavour (FDO)..........................................72 N Disintegration (water) ............................................................3..................................................................................biplanar Hardness......................................................................................................500 Lactose monohydrate [8] ....................60 min Friability ...........................6 Saccharin sodium................. dry............ Magaldrate USP ...... Manufacturing (W et granulation) Granulate mixture I with solution II.......... 3.6 Tablet formulations obtained by we t granulation (Lab Scale) Magaldrate Chewable Tablets (500 mg) 1......3 g g g g g g g g g g 2................................5 Magnesium stearate [2] .. pass through a 0........180 III..................8 mm sieve.................... Kollidon 90 F [1] ..................1% Taste ........................< 0... mix with III and press with low compression force......1 Water ................400 Orange flavour (FDO) ..............6 Cocos flavour (FDO) .......... Formulation I.......

.................................................................. sieve........2 min Friability....5 g Isopropanol .............. 3............................ Tablet properties Weight .................................................biplanar Hardness.......................8 % BASF Pharma Ingredients Generic Drug Formulations 2001 . Kollidon CL [1]...........................................3.......................s..........................5 g 2.70 N Disintegration ...0........................................................... Mefenamic acid ...............404 mg Diameter ..6 Tablet formulations obtained by we t granulation (Lab Scale) Mefenamic Acid Tablets (250 mg) 1.............250 g Corn starch [3] ................. add mixture III and press with medium compression force....................... dry...............................................40 g II................................85 g Magnesium stearate [2] ... Formulation I...............q.. Kollidon 90 F [1] ........12 g Avicel PH 101 [5] .................... III................................12 mm Form .... Manufacturing (W et granulation) Granulate mixture I with solution II........

...........q................................... 3.....................................s.............4 % BASF Pharma Ingredients Generic Drug Formulations 2001 .......... Manufacturing (W et granulation) Granulate mixture I with solution II...........1 g 2. pass through a 0.........................................................................................3.... Formulation I................6 Tablet formulations obtained by we t granulation (Lab Scale) Meprobamate + Phenobarbital Tablets (400 mg + 30 mg)..................1 g Calcium arachinate [2] ...............21 g Corn starch [3] ........................................... Tablet properties Weight ................................ Meprobamate...... III............. WG 1.......8 mm sieve............. mix with III and press with low compression force.12 mm Form .....................13 g Isopropanol ................................................8 g Aerosil 200 [4] ........................60 g Talc [10] ................30 g II..........400 g Phenobarbital................................ Kollidon CL [1] ....................... dry........< 1 min Friability............biplanar Hardness ...................................................559 mg Diameter .......................... Kollidon VA 64 [1] ..................50 g Avicel PH 101 [5] ..................................131 N Disintegration ..............................0.

..........3.. 2 Meprobamate.... Talc [10] ......s...............0 g 0.........................12 mm Form ....................................0............ 2......2 g Calcium arachinate [2] ........................ 2............................ 1 No......... Kollidon 25 [1] .....4.....................0 g – 15............biplanar Hardness .......................8 mm sieve.....0 g Corn starch [3] ........................................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ..............................95 N Disintegration ............................0 g – q........................................400............................3 g I.0....... 1 No...............................................0 g II...q..........15...5 % 500 mg 12 mm biplanar 88 N 3 – 4 min < 0....................0 g Aerosil 200 [4] ........................6 Tablet formulations obtained by we t granulation (Lab Scale) Meprobamate Tablets (400 mg).......5 min Friability ................– Lutrol E 400 [1] ..................3 g 400.........0 g 100..2 g 0................. Manufacturing (W et granulation) Granulate the mixture I with solution II................................................2.....100......s.0.. pass through a 0.............. III.......0 g Kollidon VA 64 [1]...... Tablet properties No...... add III and press...... 2 Weight . 3..........5 g Isopropanol.................. WG 1.................520 mg Diameter ......................... Formulations No....

.......................8 Isopropanol...........................................> 200 N Disintegration ..... Kollidon 90 F [1] ..................8 mm sieve and press with medium compression force..........................biplanar Hardness......3 % 4.... pass through a 0..500 Dicalcium phosphate...................... powder [6] ...................15 II.............. Remark Due to the high hardness the amount of Kollidon 90 F could be reduced.........................0..............650 mg Diameter ............. 3........ Tablet properties Weight .................... Manufacturing (W et granulation) Granulate the mixture I with solution II.......12 mm Form .....................5 Polyethylene glycol 6000...................15 g g g g g g g 2.. Metformin hydrochloride ...................... DI-TAB [9] ........................6 Tablet formulations obtained by we t granulation (Lab Scale) Metformin Tablets (500 mg) 1............. mix with III.......................................................................100 Kollidon 90 F [1] ..... Kollidon CL [1] ............... BASF Pharma Ingredients Generic Drug Formulations 2001 . Formulation I.......90 III..6 min Friability....3..................................................

.................. Metronidazole ..............................................................50 g 2........................ Kollidon 30 [1] .... powder [6]...................................3........................16 mm Form ......500 g Polyethylene glycol 6000..............................30 g II..............8 % BASF Pharma Ingredients Generic Drug Formulations 2001 .... mix with III and press............................................................ 3..........................................8 mm sieve.............. Manufacturing (W et granulation) Granulate I with solution II........... crystalline.............4 min Friability........113 N Disintegration ......500 g Sodium bicarbonate ..6 Tablet formulations obtained by we t granulation (Lab Scale) Metronidazole Effervescent Vaginal Tablets (500 mg) 1......1.........................10 g Isopropanol ...........................biplanar Hardness ..........................................600 g Kollidon 30 [1] ...... Tartaric acid............ pass through a 0.......................150 ml III.....1700 mg Diameter ......... Tablet properties Weight... Formulation I.......

.................20 Talc [10] ....................220 II............................................. Manufacturing (W et granulation) Granulate mixture I with solution II.......6 min Friability .......................755 mg Diameter .............0... crystalline [10] .....10 Ethanol 96 %............................. 3.........16 mm Form ................... dry................. Kollidon CL [1].................................................................. mix with III and press with medium compression force.....................3.............178 N Disintegration ................... Formulation I...................6 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...500 Sorbitol........0...................................... Tablet properties Weight .6 Tablet formulations obtained by we t granulation (Lab Scale) Metronidazole Tablets (500 mg) 1...........5 mg mg mg mg mg mg mg mg 2..........ca.. 75 III....8 mm sieve................ pass through a 0...............................0.5 Calcium arachinate [2] ....... Metronidazole...................................biplanar Hardness ......4 Aerosil 200 [4] ................................................................... Kollidon 90 F [1] ...............

.........................7 II.. Formulation I.......21.............8.......2....0 Lactose monohydrate [8] ............................................8 g g g g g g g 2..................... 69..... mix with III and press to tablets..........................0..........5 Water ... sieve........................... Manufacturing (W et granulation) Granulate mixture I with solution II........9 min Friability....3.............................7 Magnesium stearate [2]...3 Corn starch [3] ................. 101 –105) 1..2 % Dissolution (12 min) ................... Corn starch [3] .............53 N Disintegration .........58............. 3................172 mg Diameter ..... Pharm..................... Acta Helv..................... dry.......................................biplanar Hardness.......... Mitonafide .............................7 mm Form ...................... 1994............. Tablet properties Weight ......about 18 III...........................6 Tablet formulations obtained by we t granulation (Lab Scale) Mitonafide Tablets (60 mg) (according to A......8........... Torres et al....I..................0..... Kollidon 30 [1] ...............70 % BASF Pharma Ingredients Generic Drug Formulations 2001 ............................................

............1 min Friability.. 3.....................................................600 g Flavours ................... Corn starch [3] ......................................................s...............9 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..................22 g Calcium D-pantothenate (BASF) ........ Manufacturing (W et granulation) Granulate mixture I with solution II prepared at 70 ºC........................................................... powder (BASF) .................400 g Lactose monohydrate [8] .........q.........1630 mg Diameter ......................85 g Vitamin E acetate dry powder 50 % ...........3 g Water........biplanar Hardness ...........................2 g Nicotinamide .... Formulation I......... Food (1–2 RDA of Vitamins) 1...2 g Pyridoxine hydrochloride (BASF).............................1% (BASF) ..... Tablet properties Weight ........................................4 mm sieve and press with high compression force at maximum 30 % of relative atmospheric humidity............................23 g Cyanocobalamin... add III................................ dry and sieve................. pass through a 0..6 g Ascorbic acid.....50 g III.....0......11 g Tartaric acid powder .....100 g II...........................................................................................................300 g Corn starch [3] ....... powder 0........ Beta carotene dry powder 10 % CWD Food grade (BASF) .........3......................6 Tablet formulations obtained by we t granulation (Lab Scale) Multivitamin Effervescent Tablets with Beta Carotene............80 g Saccharin sodium.......................2 g Riboflavin (BASF)......40 g Sodium bicarbonate .16 mm Form .......107 N Disintegration (water) .... 2............................................................. Thiamine mononitrate (BASF) ................

BASF Pharma Ingredients Generic Drug Formulations 2001 .Multivitamin Ef fervescent T ablets with Beta Carotene. Food page 2 4. Remark All components of this formulation are allowed in Europe for food application.

...12 Vitamin E acetate dry powder 50 % .......550 Cyanocobalamin 0.......17 Tartaric acid..............80 Kollidon CL [1] .................................................140 N Disintegration (water) ..550 Sucrose..5 Isopropanol ............................................biplanar Hardness ...66 Calcium D-pantothenate (BASF) ........................6 Ascorbic acid.about 80 III................................. WG 1.........300 Sucrose...........................................360 Sodium bicarbonate..................................... crystalline..4 Pyridoxine hydrochloride (BASF) ...................6 Tablet formulations obtained by we t granulation (Lab Scale) Multivitamin Effervescent Tablets...... 3........................... powder ......./g dry powder CWD (BASF) .................100 mg mg mg mg mg mg mg mg mg mg mg mg mg mg mg mg mg mg mg 2.20 Vitamin A palmitate 250000 I............ Kollidon 30.............................................20 mm Form .........................60 Polyethylene glycol 6000... dry at 60 ºC with vacuum....... Thiamine mononitrate (BASF) ...........1% dry powder .............11 Nicotinamide .........................................................................35 II...............U............................ powder (BASF) ..............3.. Formulation I.......1 – 2 min Friability..........................................................13 Riboflavin (BASF) ...........2500 mg Diameter ........ Manufacturing (W et granulation) Granulate the mixture I with solution II.........................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ........... mix with III and press with high compression force......................300 Kollidon 30 [1] .... powder ..... Tablet properties Weight ....... Riboflavin (BASF) .................... powder [6] .

0 % 5.6 % 105 N < 2 min 2. Remark The high loss of vitamin A is caused by the strong hardness of the the tablets. The compression force should be reduced to minimize the expression of vitamin A from the dry powder and to increase its stability by this manner. Chemical and physical stability (20-25 ºC) Ascorbic acid Cyanocobalamin Vitamin A All other vitamins Hardness Disintegration (water) Friability 6 Months 12 Months 100 % 91% 80 % > 94 % 92 % 92 % 69 % > 94 % 114 N < 2 min 1. BASF Pharma Ingredients Generic Drug Formulations 2001 . WG page 2 4.Multivitamin Ef fervescent T ablets.

..........................2...........560 mg Diameter .....................< 0..........11.... 3.............. Vitamin A acetate + Vitamin D 3 dry powder 500.................................. crystalline (BASF) .............11............................................. pass through a 0...........................................................1 – 2 min Friability.............................2 Mannitol ......0 Cyanocobalamin gelatin coated 0....0 Avicel PH 101 [5] .........................31..........2....................0 Ascorbic acid.....................................0 Isopropanol ......................................65...................................20...20........0 Magnesium stearate [2].......100 N Disintegration (water).............................................2 Riboflavin (BASF) ..................... Kollidon 30 [1] or Kollidon VA 64 [1] ....................... Thiamine mononitrate (BASF) .......................12 mm Form ....................... WG (1–2 RDA of Vitamins) 1........... Tablet properties Weight .. Manufacturing (W et granulation) Granulate mixture I with solution II.........................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ...............2............0 Pyridoxine hydrochloride (BASF).............................2 Calcium D-pantothenate (BASF) ....biplanar Hardness............................................0 II...........................................................0 Nicotinamide .....................................................3.................................000 i........ca... u.300.......1% (BASF) .............................0 Vitamin E acetate dry powder SD 50 (BASF) .6..............................................2................................................6 Tablet formulations obtained by we t granulation (Lab Scale) Multivitamin Tablets..........0 Orange flavour........../g (BASF) . Formulation I...............0 Saccharin sodium...........80...................................................000 + 50. mix with the components III and press with medium compression force.............................3............... dry....7.......... 80 III...............................................8 mm sieve..............................0 g g g g g g g g g g g g g g g g 2....

u. WG (1–2 RDA of itamins) V page 2 4./g = 92 % Vitamin C 85 mg = 106 % 82 mg = 102 % 77 mg = 96 % BASF Pharma Ingredients Generic Drug Formulations 2001 . u. u./g = 100 % 15. Chemical stability of vitamins A and C (20–25°C.Multivitamin a Tblets.300 i.500 i.500 i./g = 100 % 14. closed) 0 Months 3 Months 6 Months Vitamin A 15.

....25 Magnesium stearate [2] .............................500 Kollidon 30 [1] ..................545 mg Diameter ...............................................................0............................................................. 3................. Kollidon CL [1] ................................8 mm-sieve.................................. pass again through a 0.............................. Nalidixic acid .... mix during 10 minutes.............104 N Disintegration (water) .............1 min Friability.15 Water .4 % Dissolution (30 min)...............8 mmsieve and press with low compression force (10 kN). Manufacturing (W et granulation) Granulate I with the solution II............................ II...................................6 Tablet formulations obtained by we t granulation (Lab Scale) Nalidixic Acid Tablets (500 mg) 1...................5 g g g g g 2....59 % (60 min).............. dry and pass through a 0....... Formulation I................. add the mixture III..................biplanar Hardness ................ Tablet properties Weight ..........73 % BASF Pharma Ingredients Generic Drug Formulations 2001 .....125 III..............12 mm Form ......................3...............................

. add III and press with low compression force......6 II...................................441 mg Diameter .......... Kollidon 90 F [1] ................. 3..........1 AcDiSol [5] .................. Naproxen (Midas) .........................41 III.....................................................12 mm Form .........................4 Water......5 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......................................3........................................ dry.... Tablet properties Weight .................................................................................................. Tablettose [8]...biplanar Hardness...................................250 Kollidon 90 F [1] ............................................................10 g g g g g g g g g g 2...............................1 Polyethylene glycol 6000... Formulation I.......8 mm sieve............2 min Friability..........10 Magnesium stearate [2] ....4 Cremophor RH 40 [1] .................6 Tablet formulations obtained by we t granulation (Lab Scale) Naproxen Tablets (250 mg) 1............................................. Manufacturing (W et granulation) Granulate mixture I with solution II....................... pass through a 0....................150 Stearic acid [7] ...47 N Disintegration .0................... powder [6] ............

.....8 mm sieve........................................................................9 % 94.....................................100 N Disintegration ....5 g – 25.............5 g Kollidon CL [1].......................95...................0.3 % 86.........0 g 90....5 g Kollidon CL [1] ................................. Magnesium stearate (Merck) . 1 No.... 1 No..5 g 10... Tablet properties No.........0 g III.......................12 mm Form . pH 7.......................... Manufacturing (W et granulation) Granulate mixture I with solution II..90................... 2.......85.0 g Water ..25..........3..............4 min Friability .... 2 Weight ....– 457.......................... pass through a 0.......457........... 2 Naproxen (Syntex) ....................10..... Formulations No.....................biplanar Hardness................6 Tablet formulations obtained by we t granulation (Lab Scale) Naproxen Tablets (450 mg) 1......3 % Dissolution...............4 (10 min) . 3...........496 mg Diameter ......................................5 % (30 min) .........................................0 g II..........2.3 % BASF Pharma Ingredients Generic Drug Formulations 2001 .......0 g I................0 g 2........ add III and press to tablets with low compression force....................... Kollidon 30 [1] ....................2 % 511 mg 12 mm biplanar 95 N 3 min 0........

........................25...... Nifedipine .......223 mg Diameter .. Formulation I................................< 0................................................ Microcrystalline Cellulose [5].... Methylene chloride...............4 g g g g g g g 2...... add IV and press with low to medium compression force...............430...................................20...................180.................................0 Kollidon 25 [1] .................. 3..about 10 min Friability .........................40........ Manufacturing (W et granulation) Dissolve mixture I in II...... Patent 0078.........................................................................0 II.....8 mm Form .............0 Kollidon CL [1]....................105........0.............Eur.........biconvex Hardness ............ sieve. dry the obtained coprecipitate....10..............90 % BASF Pharma Ingredients Generic Drug Formulations 2001 .......................... Granulate mixture III with solution I/II..1% Dissolution (20 min).. Magnesium stearate .............0 III.......................6 Tablet formulations obtained by we t granulation (Lab Scale) Nifedipine Tablet Cores (10 mg) (According to Ph............0 IV..... Tablet properties Weight ......... 1982) 1.3..........0 Corn starch [3] ...132 N Disintegration ..

.....................38 g II......... 1631 – 38................................................................ sieve. Pharm 20(9)..............100 g Corn starch [3] ....................M...........78 % (120 min) ............. Kollidon 30 [1] ........1 g 2.......q.. Formulation I..... Nitrofurantoin .................biconvex Disintegration .................8 mm Form .................... 1994) 1.180 mg Diameter ................ Ahmed.....................5 g Corn starch [3] ................5 min Dissolution (60 min)......................... Tablet properties Weight .................... mix with III and press.....6 Tablet formulations obtained by we t granulation (Lab Scale) Nitrofurantoin Tablet Cores (100 mg) (According to E...........3 g Magnesium stearate [2] ............................s................................S...8 g Talc [10] .........10 g Water.... III.........20 g Lactose [8] ........ Drug Dev....................93 % BASF Pharma Ingredients Generic Drug Formulations 2001 ................................................ Manufacturing (W et granulation) Granulate mixture I with solution II........ 3.................................... A...................... dry...........3.............Hosny...........A......... Ind............. Kollidon CL [1] ............................................................

....6 Tablet formulations obtained by we t granulation (Lab Scale) Nystatin Tablet Cores (200 mg) 1....... Kollidon CL [1]......................... dry...................................................3 g 2.........8 mm sieve....10 g Magnesium stearate [2] ...........270 mg Diameter ......................... add the components III and press with medium compression force................................................14 min Friability ..............40 N Disintegration....................0 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..............................................................................9 mm Form ...........3.... Tablet properties Weight .................................. Formulation I.........51 g II...........40 ml III..................... pass through a 0.............................................biconvex Hardness.....................................200 g Lactose monohydrate [8] ................ Isopropanol ...... Nystatin ...... Manufacturing (W et granulation) Granulate mixture I with the solvent II.. 3...

....................................25 g Ethanol 96 % .s... Manufacturing (W et formulation) Granulate mixture I with solution II.. Paracetamol............. add III and press with high compression force..................0................601 mg Diameter ....... Formulation I.......... dry...................8 mm sieve..300 g Norephedrine hydrochloride (BASF) .................................. Kollidon 30 [1] ............. pass through a 0.................................97 N Disintegration....25 g Magnesium stearate [2] ..................q....6 Tablet formulations obtained by we t granulation (Lab Scale) Paracetamol (= Acetaminophen) + Norephedrine + Phenyltoloxamine Tablets (300 mg + 25 mg + 22 mg) 1......................................................................................12 mm Form ...................200 g II.......................................................................... Tablet properties Weight ........................ Kollidon CL [1] ... III........ crystalline (BASF) .22 g Corn starch [3] ............................................. 3...............1 – 2 min Friability.3............25 g Phenyltoloxamine ................7 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......................biplanar Hardness.........5 g 2...

........................60 Ethanol 96 % .....300 Sucrose............................1..........6 Tablet formulations obtained by we t granulation (Lab Scale) Paracetamol (= Acetaminophen) Chewable Tablets (300 mg) 1...........biplanar Hardness ..........................................................30 Kollidon 30 [1] .................................................. BASF Pharma Ingredients Generic Drug Formulations 2001 .................................. milled (Hoechst) ...............................30 Strawberry flavour (FDO) ....... Taste on chewing of the table ts Sweet.........................1% 4... II............................... Paracetamol..27 min Friability..............20 mm Form .. 3..about 425 g g g g g g g 2.......................................... fruity and only very slightly bitter..................620 mg Diameter ..........600 Kollidon CL-M [1]. Formulation I.. pass through a sieve and press with medium compression force...................................................111 N Disintegration ..3.. Tablet properties Weight ...........550 Orange flavour (FDO) ................................... milled............ Manufacturing (W et granulation) Granulate mixture I with solution II..........

.....................4 min Friability.............6 Tablet formulations obtained by we t granulation (Lab Scale) Paracetamol (= Acetaminophen) Effervescent Tablets (500 mg) WG 1.............. powder [6].. powder .........8 mm sieve................. pass through a 0....................biplanar Hardness ..................................100 ml III. powder < 300 µm .................16 mm Form ....................7 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........................150 N Disintegration ............ Kollidon 30 [1] ............700 mg Diameter ................................................1.............................................430 g Dextrose ...20 g Isopropanol ..... Tablet properties Weight ........................................... Formulation I..........500 g Tartaric acid...............60 g 2................500 g Sodium bicarbonate ........................200 g Flavouring II... Manufacturing (W et formulation) Granulate the mixture I with solution II.. Paracetamol.................. 3.... add III..............0.....3................................... mix and press to tablets........ Polyethylene glycol 6000............

..................................... 3........................12 Kollidon VA 64 [1] ........................................6 Tablet formulations obtained by we t granulation (Lab Scale) Paracetamol (= Acetaminophen) Tablet Cores (500 mg) 1.....10 g g g g g g g g 2.............................. dry..biconvex Hardness .. Formulation I................... powder [6] ..< 1 min Friability ................12 Polyethylene glycol..................................................157 N Disintegration ........... Kollidon CL [1]..............10 Ethanol 96 %....11 mm Form ............. Press with high compression force of 25 – 30 kN..................... 70 III.......20 II......500 Dicalcium phosphate [9] .................88 % 30 min ............................................... Paracetamol... Manufacturing (W et granulation) Granulate mixture I with solution II..........587 mg Diameter ......................................................30 Kollidon CL [1].........................................97 % BASF Pharma Ingredients Generic Drug Formulations 2001 . 10 min..3........................................... powder (RPR) ........................ Kollidon 90 F [1] .............. Tablet properties Weight ................................ sieve and mix with III..max.......1% Dissolution.........................< 0............

.q.......................................200 g Dibasic calcium phosphate [9] ..................biconvex Hardness.........................2 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......................................................... Kollidon 30 [1] .............. Formulation I.........................385 mg Diameter ................ III.......... pass through a 0.......0........................................................3....... Kollidon CL [1].. mix with III....... Tablet properties Weight ......................8 sieve and press with low compression force...< 1 min Friability.......................150 g II............ Phenolphthalein.. s.......280 N Disintegration (water) ........................9 mm Form .......................19 g Magnesium stearate [2] .............6 Tablet formulations obtained by we t granulation (Lab Scale) Phenolphthalein Tablet Cores (200 mg) 1.................11 g Isopropanol or ethanol 96 % ............................3 g 2........ Manufacturing (W et granulation) Granulate mixture I with solution II.............. 3.......

5 Magnesium stearate [2] ...... mix with III and press with high compression force......209 mg Diameter .......................................2 g g g g g g g 2.................................30 III..0.........................10 Isopropanol + Ethanol (1 + 1) ................................................................................................................8 mm Form ...... 3...........50 Sucrose...3 min Friability................................. Manufacturing (W et granulation) Granulate mixture I with solution II......... Kollidon 25 [1] .... Kollidon CL [1] ................biplanar Hardness..................................................................45 II....................................... Formulation I......... WG 1....60 N Disintegration .............8 mm sieve..................6 Tablet formulations obtained by we t granulation (Lab Scale) Phenytoin Sodium Tablets (100 mg)......... pass through a 0....................3............5 % BASF Pharma Ingredients Generic Drug Formulations 2001 ... Tablet properties Weight ........ Phenytoin sodium ........ crystalline ..... dry........100 Dicalcium phosphate [9] ...................

.......................8 mm sieve....... pass through a 0................................................ 3.............................biplanar Hardness........3......................................................674 mg Diameter ....................................................54 N Disintegration ....12 mm Form ....... Manufacturing (W et granulation) Granulate mixture I with solution II...3 g Magnesium stearate [2] ................. 5 min ......................................3 % Dissolution...............................0..500 g Corn starch [3] .......130 g II.................. add III and press with low compression force.....................................3 g 2...............................................................................................70 ml III.............. Probenecid .........10 g Ethanol 96 % ............................................6 Tablet formulations obtained by we t granulation (Lab Scale) Probenecid Tablets (500 mg) 1.... Kollidon 30 [1] ...........100 % BASF Pharma Ingredients Generic Drug Formulations 2001 .....................9 min Friability.................... Kollidon CL [1] ........ Formulation I...........25 g Aerosil 200 [4] ...................43 % 60 min........... Tablet properties Weight ............

......2 g 2....3 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........................ (+) Pseudoephedrine hydrochloride (BASF) ... 3....8 mm sieve......0............. powder [6].........................8 mm Form ............ add IV and press with low compression force...........................6 Tablet formulations obtained by we t granulation (Lab Scale) Pseudoephedrine Tablets (60 mg) 1......... pass through a 0.............................. mix with I...............82 N Disintegration ................. Tablet properties Weight .biplanar Hardness..... dry.3......... Formulations I.......... Manufacturing (W et granulation) Granulate dicalcium phosphate II with solution III........ Dicalcium phosphate................192 mg Diameter .......................q.....95 g III......................................s........................ DI-TAB [9] ................... IV........4 min Friability............5 g Water...................60 g II.....................20 g Aerosil 200 [4] ......... Kollidon 30 [1] .............................. Polyethylene glycol 6000................................

..................................................... Formulation I............... 200 ml III............ Kollidon CL [1] ............78 % 30 min ...........(5-) 10 g Magnesium stearate [2] ... 3.........12 mm Form ..................... Kollidon 30 [1] ........20 g Ethanol 96 % ........3.......................... Manufacturing (W et granulation) Granulate mixture I with solution II...6 g 2............................................................................................................25 % Dissolution. mix with III and press with low compression force.....3 min Friability......500 g Corn starch [3] .8 mm sieve............................................................50 g II..........96 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......................................6 Tablet formulations obtained by we t granulation (Lab Scale) Pyrazinamide Tablets (500 mg)............ 15 min...605 mg Diameter ..............approx...0.... pass through a 0.................... Pyrazinamide........................................................................................ Tablet properties Weight ........ WG 1..131 N Disintegration ...........biplanar Hardness ......................

................. 3.............3.................................................450 g Corn starch [3] ..................................................................................50 ml III....550 mg Diameter .... Formulation I...........15 g Stearic acid [7] ....................................... sieve and mix with the components of III and press with low compression force to tablets................................................................................. Tablets properties Weight ...2 g 2...............10 g Magnesium stearate [2] ...........................................................................6 Tablet formulations obtained by we t granulation (Lab Scale) Rifampicin Tablets (450 mg) 1............1 – 2 min Friability . Manufacturing (W et granulation) Granulate mixture I with solution II..............95 N Disintegration ...........9 g Isopropanol or ethanol 96 % .....................................................................................................2 g Aerosil 200 [4] .........................58 g II...... Kollidon CL [1]........ dry.. Rifampicin ........6 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...... Kollidon 90 F [1] .....0.........12 mm Form ....biplanar Hardness....

................s. powder .. pass through a 0.. Tablet properties Weight ...............q...............biplanar Hardness.... mix throroughly...... 3............. III...........2.....8 g 2.280... add mixture III....................................... Formulation I.......> 30 min Friability .6 Tablet formulations obtained by we t granulation (Lab Scale) Simethicone Chewable Tablets (70 mg) 1..........................0 g Sucrose.. and press with high compression force....... Manufacturing (W et granulation) Granulate mixture I with solution II.....................40 N Disintegration ....8 g Magnesium stearate [2].............................442 mg Diameter ..........2.................................. Kollidon 90 F [1] ...... Aerosil 200 [4] .............1% BASF Pharma Ingredients Generic Drug Formulations 2001 ............................8 mm sieve..12 mm Form ...........0 g Kollidon 90 F [1] ..5 g Isopropanol ................................................................0 g II................< 0.............7................ Simethicone dry powder 25 % .........3........................................158...........3............................ dry....................

............................... pass through a 0.. Simethicone (Wacker Siliconoil S 184) ....... add mixture III................ powder ........... Tablet properties Weight .................... Ludipress [1] ....biplanar Hardness..80 Sorbitol..........................1% BASF Pharma Ingredients Generic Drug Formulations 2001 .... Manufacturing (Granulation) Mix the components II with the simethicone oil I........6 Tablet formulations obtained by we t granulation (Lab Scale) Simethicone Chewable Tablets (80 mg) 1..........400 Aerosil 200 [4] .................................. II................................................................................... mix thoroughly......2 Magnesium stearate [2] ...81 N Friability .............8 mm sieve and press with high compression force.................20 III... pass again through a 0................................870 mg Diameter .................. crystalline [10] ............. 3..................................390 Menthol.......< 0..................8 g g g g g g 2...3...............16 mm Form .....8 mm sieve.. Formulation I..........

...............................12 mm Form .........20 g Ethanol 95 % .............90 N Disintegration ................................................. Kollidon CL [1] ......................................3...........biplanar Hardness..... Formulation I................. mix the dry granules with III and press with low compression force..........................20 g Corn starch [3] ..................................................80 ml III........................ pass through a sieve........................................... Kollidon 30 [1] ..660 mg Diameter .. Sucralfate ......3 % BASF Pharma Ingredients Generic Drug Formulations 2001 . Manufacturing (W et granulation) Granulate mixture I with solution II.......... Tablet properties Weight ............70 g II.............................................................................0.............................30 g Magnesium stearate [2] .......................................................................................6 Tablet formulations obtained by we t granulation (Lab Scale) Sucralfate + Sodium Alginate Tablets (500 mg + 20 mg) 1......3 – 4 min Friability......3 g 2...... 3..500 g Sodium alginate .......................

..................... Kollidon CL [1].......................... dry......465......23..............2 Calcium arachinate [2] .....................3.........8 mm sieve.... Kollidon 30 [1] ..... 10 min........77 % 20 min ............. Formulation I.........4 Talc [10] ..................................93............................8 Aerosil 200 [4] ...................................0 II...152 N Disintegration ..........602 mg Diameter ............. Manufacturing (W et granulation) Granulate mixture I with solution II.........89 % BASF Pharma Ingredients Generic Drug Formulations 2001 ..........................0 III......................3 min Friability ............... pass through a 0..................................................... add mixture III and press with low compression force..........................................87 % 30 min .........0 Lactose monohydrate D 20 [8] ........6 Tablet formulations obtained by we t granulation (Lab Scale) Sulfadiazin Tablets (450 mg) 1.........................biplanar Hardness ..........................0 Water ...........< 0..........0..................0...............................14. Tablet properties Weight .............. 3......1% Dissolution......................................1..... Sulfadiazin ...........200..................................12 mm Form .........2 g g g g g g g g 2.......................................

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Sulfadimidine Tablets
(500 mg)

1. Formulation
I.

Sulfadimidine (Cilag) .............................500.0
Lactose monohydrate [8].......................100.0
II. Kollidon 30 [1] ........................................15.0
Water ...................................................200.0
III. Kollidon CL [1]........................................25.0
Talc [10] ...................................................2.4
Aerosil 200 [4] ..........................................0.3
Calcium arachinate [2] ..............................0.3

g
g
g
g
g
g
g
g

2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, dry, pass through a 0.8 mm sieve,
mix with III and press.
3. Tablet properties
Weight .................................................610 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardness ................................................120 N
Disintegration......................................2 – 3 min
Friability...................................................0.7 %

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Sulfadoxine + Pyrimethamine Tablets
(500 mg + 25 mg)

1. Formulation
I.

Sulfadoxine ..........................................500.0
Pyrimethamine .......................................25.0
II. Kollidon 30 [1] ........................................20.0
2-Propanol ...........................................167.0
III. Magnesium stearate [2].............................6.0
Kollidon CL [1]........................................25.0
Aerosil 200 [4] ..........................................3.0

g
g
g
g
g
g
g

2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, dry, pass through a 0.8 mm sieve,
mix with the components III and press with medium compression force
to tablets.
3. Tablet properties
Diameter ...............................................10 mm
Weight .................................................607 mg
Hardness ................................................126 N
Disintegration......................................1 – 2 min
Friability...................................................0.4 %

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Sulfamethoxazole + Trimethoprim Tablets
(400 mg + 80 mg)

1. Formulation
I.

Sulfamethoxazole ....................................400 g
Trimethoprim .............................................80 g
II. Kollidon 30 [1] ...........................................15 g
Isopropanol ...............................................q.s.
III. Kollidon CL [1] ..........................................24 g
Talc [10] ......................................................2 g
Magnesium stearate [2] ...............................8 g
2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, pass through a 0.8 mm sieve, dry,
add III and press with low compression force.
3. Tablet properties
Weight .................................................546 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardness ................................................115 N
Disintegration ..........................................9 min
Friability ..................................................0.6 %

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Sulfathiazole Tablets
(250 mg)

1. Formulations
No. 1

No. 2

Sulfathiazole ................................................250 g
Lactose monohydrate [8] ..............................237 g
Dicalcium phosphate [9] ......................................–
Kollidon 30 [1] ................................................12 g
II. Water .............................................................q.s.
III. Kollidon CL [1] ...............................................12 g
Magnesium stearate [2] ...............................2 – 3 g

250 g

237 g
12 g
q.s.
12 g
2–3 g

I.

2. Manufacturing (W
et granulation)
Granulate mixture I with solvent II, pass through a 0.8 mm sieve, dry,
add III and press with low compression force.
3. Tablet properties
Weight ......................................................504 mg
Diameter ....................................................12 mm
Form ........................................................biplanar
Hardness .....................................................115 N
Disintegration ...............................................1 min
Friability .......................................................0.2 %
Dissolution, 10 min ........................................80 %
20 min ........................................96 %

BASF Pharma Ingredients Generic Drug Formulations 2001

512 mg
12 mm
biplanar
154 N
< 1 min
0.2 %
69 %
90 %

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Tannin-Crospovidone Complex Tablets
(55 mg + 230 mg)

1. Formulation
I.

Tannic acid.............................................55.0
Water ...................................................230.0
II. Crospovidone (Kollidon CL) [1] ..............230.0
III. Avicel PH 101 [5] ....................................33.0
Talc [10] ...................................................2.6
Aerosil 200 [4] ..........................................0.3
Calcium arachinate [2] ..............................0.3

g
g
g
g
g
g
g

2. Manufacturing
Prepare solution I, suspend II and filtrate the formed insoluble tannincrospovidone complex. Wash with water until the water is clear, pass the
solids through a 0.8 mm sieve and dry. Add the components III and
press with low compression force.
3. Tablet properties
Weight .................................................323 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardness..................................................40 N
Disintegration .......................................< 1 min
Friability...................................................0.8 %

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Theophylline Sustained Release Tablets
(400 mg), WG

1. Formulations

I
II
III

No. 1

No. 2

Theophylline, powder (BASF) ........................400 g
Granulac 140 [8]...........................................337 g
Kollicoat SR30D [1] ......................................198 g
Kollicoat EMM30D [1] ..........................................–
Aerosil 200 [4]..................................................4 g
Magnesium stearate [2] ....................................4 g

400 g
356 g

132 g
4g
4g

2. Manufacturing (W
et granulation)
Granulate the mixture I with Kollicoat SR30D or Kollicoat EMM30D (II) in
a fluidized bed (inlet temperature 45-55 °C, outlet temperature 2125 °C, nozzle 0.8 mm, spray pressure 1.5-2.0 bar, spray rate 10 g/min),
mix with the components of III and press to tablets with medium compression force.
3. Tablet properties
Percent of Kollicoat (solid polymer)............7.4 %
Weight .................................................797 mg
Diameter .......................................19 x 8.5 mm
Form .....................................................oblong
Hardness................................................276 N
Friability ...................................................0.1%

5.0 %
811 mg
19 x 8.5 mm
oblong
228 N
<0.1%

BASF Pharma Ingredients Generic Drug Formulations 2001

Theophylline Sustained Release
ablets
T
(400 mg) WG

page 2

released drug [%]

4. Release of theophylline (0-2 h: 0.08N HCI, 2-24 h: pH 6.8)
100
80
Kollicoat EMM30D
60
40
Kollicoat SR30D
20
0
0

4

8

12
time [h]

BASF Pharma Ingredients Generic Drug Formulations 2001

16

20

24

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Valproate Sodium Tablets
(500 mg)

1. Formulation
I.

Valproate sodium.....................................500 g
Corn starch [3] ..........................................80 g
II. Kollidon 30 [1] ...........................................20 g
Isopropanol .............................................60 ml
III. Kollidon CL [1] ............................................5 g
Magnesium stearate [2] ...............................5 g
2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, pass through a sieve, mix the dry
granules with III and press with low compression force.
3. Tablet properties
Weight .................................................607 mg
Diameter ...............................................12 mm
Form ...................................................biplanar
Hardness ................................................162 N
Disintegration ..........................................7 min
Friability ...................................................0.1%
4. Remark
The powder mixture was electrostatic.

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Verapamil Tablets
(120 mg), WG

1. Formulation
I.

Verapamil HCl (BASF)............................120.0
Lactose Monohydrate [8].......................160.0
II. Kollidon 30 [1] ........................................12.0
Ethanol 96 % ..........................................30.0
III. Magnesium stearate [2].............................1.5
Kollidon CL [1] .........................................9.0

g
g
g
g
g
g

2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, dry, pass through a 0.8 mm sieve,
mix with the components III and press with low compression force to
tablets.
3. Tablet properties
Diameter .................................................9 mm
Weight .................................................300 mg
Hardness ................................................105 N
Disintegration .......................................5-6 min
Friability...................................................0.2 %
Dissolution (USP 24), 10 min ......................82 %
20 min ......................97 %

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Vitamin B Complex + Carnitine Tablet Cores

1. Formulation
I.

Thiamine mononitrate (BASF) ..................95.0
Riboflavin (BASF) ....................................20.0
Nicotinamide (Degussa).........................100.0
Calcium D-pantothenate (BASF) ..............50.0
Folic acid (Knoll) .......................................2.0
Biotin.......................................................0.2
Cyanocobalamin, gelatin coated 1%..........0.5
(BASF)
Carnitine hydrochloride ...........................50.0
Inositol .................................................100.0
Adenosine phosphate ...............................2.0
II. Kollidon 30 [1] ........................................15.7
Isopropanol ............................................70.0
III. Kollidon CL [1]........................................26.0
Lactose monohydrate [8].......................122.0
Polyethylene glycol 6000, powder [6] .......14.0

g
g
g
g
g
g
g
g
g
g
g
g
g
g
g

2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, dry, pass through a 0.8 mm sieve,
mix with III and press with low compression force.
3. Tablet properties
Weight .................................................708 mg
Diameter ...............................................13 mm
Form ..................................................biconvex
Hardness..................................................88 N
Disintegration......................................1 – 2 min
Friability ...................................................0.1%

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Vitamin B Complex + Vitamin C
+ Calcium Effervescent Tablets

1. Formulation
I.

Thiamine mononitrate (BASF) .......................7 g
Riboflavin (BASF).........................................5 g
Nicotinamide .............................................25 g
Pyridoxine hydrochloride (BASF).................20 g
Calcium D-pantothenate (BASF) .................12 g
Calcium carbonate ....................................75 g
Calcium glycerophosphate .......................164 g
Sodium bicarbonate ................................400 g
Tartaric acid, powder ...............................300 g
Sucrose, crystalline .................................400 g
Sucrose, powder .....................................350 g
Kollidon 30 [1] ...........................................50 g
II. Kollidon 30 [1] ...........................................10 g
Isopropanol ................................................q.s.
III. Ascorbic acid, powder (BASF) ..................550 g
Riboflavin (BASF).........................................2 g
Cyanocobalamin gelatin coated 0.1%...........5 g
(BASF).............................................................
Polyethylene glycol 6000, powder [6]..........40 g
Kollidon CL [1] ..........................................50 g
2. Manufacturing (W
et granulation)
Granulate mixture I with solution II, dry at 60 °C with vacuum, mix with III
and press with medium to high compression force.
3. Tablet properties
Weight ..............................................2,500 mg
Diameter ...............................................20 mm
Form ...................................................biplanar
Hardness ................................................150 N
Disintegration ..........................................2 min
Friability...................................................0.9 %

BASF Pharma Ingredients Generic Drug Formulations 2001

3.6 Tablet formulations obtained by we
t granulation (Lab Scale)

Vitamin B Complex + Vitamin C
+ Ferrous Sulfate Tablets

1. Formulation
I.

Ferrous sulfate (1H20)..............................300 g
Kollidon 30 [1] ...........................................15 g
II. Kollidon 30 [1] .............................................6 g
2-Propanol .................................................q.s.
III. Thiamine mononitrate (BASF) .....................45 g
Riboflavin (BASF) .......................................10 g
Pyridoxine hydrochloride (BASF).................82 g
Nicotinamide .............................................69 g
Ascorbic acid, powder (BASF) ..................470 g
Ludipress [1] ...........................................690 g
Polyethylene glycol 6000, powder [6]..........50 g
Aerosil 200 [4] .............................................9 g
2. Manufacturing (W
et granulation)
Granulate the mixture I with solution II, pass through a 0.8 mm sieve, mix
with III and press with high compression force (25 – 30 kN).
3. Tablet properties
Weight ..............................................1,750 mg
Diameter ...............................................20 mm
Form ...................................................biplanar
Hardness ................................................120 N
Disintegration ..........................................6 min
Friability...................................................0.9 %

BASF Pharma Ingredients Generic Drug Formulations 2001

315 mg Diameter ..................... crystalline . pass through a 0................... 3................................... Isopropanol .... Formulation I..................0........................... Tablet properties Weight ................................10 g Orange flavour....................................2..........10 g Nicotinamide ..q............... III.... crystalline (BASF) .141 N Disintegration ..............1% .......................50 g 2....................................................................s............. Ascorbic acid.....................4 g Pyridoxine hydrochloride (BASF) ..................................... Manufacturing (W et granulation) Granulate mixture I with the solvent II.................................... Thiamine mononitrate (BASF) ......8 mm sieve.....10 g Saccharin sodium...33 g Riboflavin (BASF)............3...........20 mm Form ...500 g Riboflavin.................... powder [6]...5 g Polyethylene glycol 6000....6 Tablet formulations obtained by we t granulation (Lab Scale) Vitamin B Complex + Vitamin C Effervescent Tablets 1......................................................................................9 % BASF Pharma Ingredients Generic Drug Formulations 2001 ......................................................biplanar Hardness ......... dry................750 g Kollidon 30 [1] ....................... powder ...............................350 g Sodium bicarbonate .......66 g Calcium D-pantothenate (BASF) ...............30 g II......2 g Cyclamate sodium............ mix with II and press with high compression force at maximum 30 % of relative atmospheric humidity...............2 min Friability....17 g Tartaric acid.................3 g Cyanocobalamin gelatin coated 0...........................450 g Sucrose................

.............. Kollidon 30 [1] ...................100 Lactose monohydrate [8] ..........................................................10 Isopropanol................................. 3..................7 min Friability ....9 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........0..... Kollidon CL [1] .............................................................1 g g g g g g g 2.............................6 Tablet formulations obtained by we t granulation (Lab Scale) Vitamin B1 (Thiamine) Tablets (100 mg)..................200 II................... Formulation I...........3..................................... Tablet properties Weight ........................330 mg Diameter .............................8 mm screen.............................2 Aerosil 200 [4]................................8 mm Form ............... WG 1.........................................10 Magnesium stearate [2] ....................60 III....... Thiamine hydrochloride (BASF) ......................... dry and sieve through a 0.174 N Disintegration ................. mix with III and press to tablets........................... Manufacturing (W et granulation) Granulate mixture I with solution II............biplanar Hardness .....

...........5 % BASF Pharma Ingredients Generic Drug Formulations 2001 ....30 g Kollidon VA 64 [1] .......biplanar Hardness..................... Polyethylene glycol 6000........ powder [6] .................................................. Kollidon VA 64 [1] . mix with III and press with low compression force......q............. dry.................. 3....2 min Friability .....16 mm Form ........... III.s............................................... Formulation I......20 g II........................698 mg Diameter .................... sieve.........................35 g 2.............................0..................................100 g Corn starch [3] ..............................101 N Disintegration ................................................3.................. Tablet properties Weight .......500 g Caffeine (BASF) ...................................................................6 Tablet formulations obtained by we t granulation (Lab Scale) Vitamin B1 + Caffeine Tablets (500 mg + 100 mg) 1........... Manufacturing (W et granulation) Granulate mixture I with solution II...15 g Ethanol 96 % ...................................................... Thiamine hydrochloride (BASF)..............

.....................75......... Formulation I................................................1 – 2 min Friability..8 mm Form ..........< 0........................0 Lactose monohydrate [8] ............1.......... Kollidon 30 [1]....3...........6 Tablet formulations obtained by we t granulation (Lab Scale) Vitamin B2 (Riboflavin) Tablets (10 mg) 1...............biplanar Hardness ....8 Talc [10] ...............15................ pass through a 0.. Riboflavin (BASF) ..............................................2..........8 mm sieve......... Tablet properties Weight ...................................................................................0 Corn starch [3] ........ 3.................1% BASF Pharma Ingredients Generic Drug Formulations 2001 ...........................20......... dry........... Aerosil 200 [4] ..........................25 III...134 mg Diameter ....0...........................5 Hydrogenated castor oil (Henkel)..0 II.....................................................................................................5 Water ......................0 Avicel PH 101 [5] .......................................10.......................7 g g g g g g g g g 2....82 N Disintegration...................... mix with II and press with low compression force............ Manufacturing (W et granulation) Granulate mixture I with solution II...............

.. 3.................................40 Corn starch [3] ........ closed) Vitamin B 6 0 Months 3 Months 6 Months 100 % 100 % 100 % BASF Pharma Ingredients Generic Drug Formulations 2001 ................................................................ Kollidon 30 [1] .........................354 mg Diameter ............ Manufacturing (W et granulation) Granulate mixture I with solution II........................biplanar Hardness ................... pass through a 0..............2 g g g g g g 2...6 Tablet formulations obtained by we t granulation (Lab Scale) Vitamin B6 (Pyridoxine) Tablets (40 mg)......0..........80 III..... dry..............................70 N Disintegration . Chemical stability (40°C............. WG 1............1% 4......................................300 II.................... mix with III and press with high compression force......3......................... Magnesium stearate [2] ............................3 min Friability................ Formulation I................... Pyridoxine hydrochloride (BASF) .. Tablet properties Weight ......................................12 mm Form ..............15 Water + Isopropanol (1+1) .......................................................8 mm sieve.......................1 Aerosil 200 [4].

.......... Add IV and press with a high compression force at maximum 30 % of relative atmospheric humidity..2 % BASF Pharma Ingredients Generic Drug Formulations 2001 .........100 N Disintegration .... Calcium carbonate ........................................ Sucrose crystalline .............2.........450 Tartaric acid........................2 min Friability ............60 g g g g g g g g g g 2......10 Isopropanol....500 mg Diameter .....................................................................................400 IV...................600 Kollidon 30 [1]...................315 Sodium bicarbonate ................................... 3.................. Tablet properties Weight ....200 III......................................20 mm Form ...................6 Tablet formulations obtained by we t granulation (Lab Scale) Vitamin C + Calcium Carbonate Effervescent Tablets (500 mg + 300 mg) 1................ Formulation I....120 Polyethylene glycol 6000........................... crystalline (BASF) ..............................................................................35 II......550 Kollidon CL [1]. powder ....... Kollidon 30 [1] .......................................... mix with III and dry............3................biplanar Hardness................ Manufacturing (W et granulation) Granulate mixture I with solution II........................................... powder [6] .................................... Ascorbic acid...................................

......................61 N Friability............6 Tablet formulations obtained by we t granulation (Lab Scale) Vitamin C + Vitamin E Lozenges (100 mg + 50 mg) 1.................100 Dextrose .. Isopropanol.................... crystalline (BASF) ............ mix with III and press with high compression force....................... Manufacturing (W et granulation) Granulate mixture I with isopropanol...........< 0... BASF Pharma Ingredients Generic Drug Formulations 2001 ..3........... 3....................... pass through a 0..........................................................................................400 Kollidon 90 F [1] ...600 mg Diameter ........ Formulation I.....................................1% 4.............6 g g g g g g 2........................... Ascorbic acid.................... Tablet properties Weight .8 mm sieve......................12 mm Form ....................................biplanar Hardness ..................... Polyethylene glycol 6000. Stability of appearance No change of the tablet colour during 3 months at 30 °C and 70 % relative humidity..........25 III........4 II..100 Vitamin E acetate dry powder SD 50 (BASF) .......... dry. powder [6] .........

.....................................105 g Ascorbic acid... 2..........3....... crystalline ...................5 % (Merck).....6 Tablet formulations obtained by we t granulation (Lab Scale) Vitamin C (Ascorbic acid) Chewable Tablets with Dextrose (100 mg) 1.......... 3...............< 0...................500 g II.. Polyethylene glycol 6000.. powder [6] ..................10 min Friability.....1% BASF Pharma Ingredients Generic Drug Formulations 2001 ............................................................... Kollidon 90 F [1] ..... 1 No..........4 g Water and/or isopropanol... sieve....................................... EC coated 97.................biplanar Hardness..12 mm Form .......150 N Disintegration ......620 mg Diameter ... Tablet properties No.......................................... 1 No.. Formulations No....... 2 Ascorbic acid................6 g — 110 g 500 g 4g 30 – 50 g 6g I......................1% 620 mg 12 mm biplanar > 100 N not tested 0.................... add III and press with high compression force....... 2 Weight ................................. Manufacturing (W et granulation) Granulate mixture I with solution II (in a fluidized bed)........30 – 50 g III......................– Dextrose ..................................

Chemical stability (40 °C. 2. closed) Formulation No. If no fluidized bed is available water should be avoided as granulation solvent. Remarks 1. 1 Formulation No. BASF Pharma Ingredients Generic Drug Formulations 2001 page 2 .Vitamin C (Ascorbic acid) Chewable ablets T with Dextr ose (100 mg) 4. The use of coated ascorbic acid does not increase the stability. 2 0 Months 3 Months 6 Months 100 % 100 % 100 % 92 % 100 % 93 % 5.

.3.................. Dry mixture III also at 60 °C and mix together with I/II and IV................................................ and dry at 60 °C............. Sodium hydrogen carbonate ................20 mm Form .................... Polyethylene glycol 6000............................300 mg Diameter ................... Formulation I.....................................................6 Tablet formulations obtained by we t granulation (Lab Scale) Vitamin C (Ascorbic Acid) Effervescent Tablets (500 mg) 1..........67 g Dextrose........................... 3........1 g 2... At maximum 30 % relative atmospheric humidity.... powder.................................200 ml III........................5 mm-sieve.............. pass through a 0.......... powder [6] .................660 g IV........................... Ascorbic acid...... Tablet properties Weight ..biplanar Hardness...............................................................67 g Orange flavour ..........430 g II......5 mm) .. crystalline (BASF) .......... Manufacturing (W et granulation) Granulate mixture I with solution II........8 g 2-Propanol ..............10 g Saccharin sodium ....500 g Tartaric acid ...........100 N Disintegration (water) .................... Kollidon 25 [1]........2.............................. press to effervescent tablets.....550 g Sucrose (<0......2 min BASF Pharma Ingredients Generic Drug Formulations 2001 ..................................................

4. 4. 1 kg of spray solution or spray suspension and 5 kg of tablet cores.3 Conditions for spraying Whenever they are of importance. for which the minimum amount of cores is 5 kg. BASF Pharma Ingredients Generic Drug Formulations 2001 . In a few cases. The batches usually consisted of ca. the conditions for processing the formulations on a given scale have been quoted.4 Colour additives Normally the colorants added were Sicovit pigments. 4. 4. the fluidized-bed granulator WSG Glatt 15 or a traditional coating pan was used.5 Formulations The formulations in this chapter have been arranged in the alphabetic order of their function.2 Equipment The tests were mostly performed in the Accela-Cota 241.1 Size of formulations and amounts used The formulations were developed on a laboratory scale.4 Coating of tablets and capsules 4.

.......5 g Talc [10] .......0 g II................... 2 Pigment suspension: Sicovit titanium dioxide [1] .............. 2) Add the pigment suspension I to the well stirred polymer suspension II........... 1) or suspend Kollicoat MAE100P in water.. 1 I..............................250...20...161..........11............... 2.........5 52.......... Manufacturing of the suspension I Suspend the pigments and talc in the well stirred water and homogenize in a disk mill or in a colloid mill...0 g 500....3 g Total I + II:............................ Formulations No. stir 2-3 hours and add the propylene glycol (=No..................2..................0 2.......5 g g g g 2........ II Separately suspend Kollicoat MAE30DP in the mixture of water and propylene glycol (=No.........................5 g Polymer suspension: Kollicoat MAE30DP [1] .........0 g Kollicoat MAE100P [1] .4................2 g 326..........5 g Water.3 g – 75...... BASF Pharma Ingredients Generic Drug Formulations 2001 .– Propylene glycol [1]...........5 20.. Stir the obtained suspension during the entire coating process.................. No.......................0 g Sicovit Iron oxide Red [1] .........2...52...5 Coating formulations (Lab Scale) Enteric Film Coating of Acetylsalicylic Acid Crystals (Aqueous) 1.2 g Water ...500.....0 g 11.................................

..................................0............................500 g Quantity of solids applied per cm 2 ...... Coating procedure (Fluidized bed...............................0 mm Quantity of suspension applied................1 bar Inlet air temperature..... Release of the ace tylsalicylic acid 100 0-120 min: 0........................... 100 min Drug dissolved [%] 4.......................... Aer omatic® Strea1) Acetylsalicylic acid crystals loading..................................continuous Spraying pressure ....................60 °C Outlet air temperature ........................about 6 mg Quantity of film-forming agent applied per cm 2 .....................3-1.......................500 g Size of the crystals ....................1N HCl 120-200 min: Buffer pH 6....... about 4 mg Type of spraying ............ 35 °C Spraying time ............................................................................Enteric Film Coating of Ace tylsalicylic Acid Crystals (Aqueous) page 2 3.....8 80 60 40 20 0 0 20 40 60 80 100 120 Time [min] BASF Pharma Ingredients Generic Drug Formulations 2001 140 160 180 200 ......................................

.........500 g II... 1) or suspend Kollicoat MAE100P in water................ 2 mg Type of spraying .. Formulations No......................45 g Talc [10] .......4.435 g – 675 g 67 g 3.......................................3 mg Quantity of film-forming agent applied per cm 2 ......010 g Total I + II:............0.....8-1............................500 g 4......... Stir the obtained suspension during the entire coating process................................................................................. 2) Add the pigment suspension I to the well stirred polymer suspension II.............................2...................................1..................500 g Polymer suspension: Kollicoat MAE30DP [1] ............. 100 min Spraying rate ......180 g Kolidon 30 [1] ..............................continuous Inlet air temperature......................................................45 g/min BASF Pharma Ingredients Generic Drug Formulations 2001 .........2 mm Quantity of suspension applied ................................. 2 Pigment suspension: Sicovit titanium dioxide [1] ..................500 g Quantity of solids applied per cm 2 .................................................................................................. 1 I........................250 g Kollicoat MAE100P [1] ....................... Coating procedure (Hüttlin Kugelcoater HKC 5 TJ) Pellet loading........ stir 2-3 hours and add the propylene glycol (=No...........4......5 Coating formulations (Lab Scale) Enteric Film Coating of Pellets (Aqueous) 1.......... 3..................................................................– Propylene glycol [1] ............................ Manufacturing of the suspension I Suspend the pigments and talc in the well stirred solution of Kollidon 30 and homogenize in a disk mill or in a colloid mill.....................................................5 kg Pellet size............................60 °C Outlet air temperature ..........................................67 g Water......23 g Water.......... 45 180 23 500 g g g g 2... 32-35 °C Spraying time ................ II Separately suspend Kollicoat MAE30DP in the mixture of water and propylene glycol (=No........4.. No.

.....101 g Water....................... Manufacturing of the suspension No. colourless) 1....... Add the propylene glycol. 1: Dissolve the propylene glycol in the water and suspend the Kollicoat MAE dispersion in this well stirred solution.... 70 min Spraying rate .......12 mg Quantity of film-forming agent applied per cm 2 ...................... Stit the obtained suspension during the entire coating process...........795 g Total ...400 g 2..................... Coating procedure (Accela Cota 24 ) Soft gelatin capsules loading ................2....................................................................................................1.. 10 mg Spraying pressure ............. No.............................. 2: Suspend Kollicoat MAE100P in water and stir for 2-3 hours until a homogeneous dispersion is obtained....................................................30-35 g/min BASF Pharma Ingredients Generic Drug Formulations 2001 .........................................................................680 g Kollicoat MAE100P [1] .....50 °C Temperature of the capsules ........................4................... 2 Kollicoat MAE30DP [1].............................– Propylene glycol [1] .....................................continuous Inlet air temperature.............................2.......5 kg Quantity of suspension applied .....................................619 g – 504 g 101 g 1...................................2 bar Type of spraying .....................5 Coating formulations (Lab Scale) Enteric Film Coating of Soft Gelatin Capsules (Aqueous.... 3......400 g 2...400 g Quantity of solids applied per cm 2 ............................................. 1 No. Formulations No.30-32 °C Spraying time...............

...............15 Water........500 g Propylene glycol [1] ...............5 g Talc [10] .............4................................. BASF Pharma Ingredients Generic Drug Formulations 2001 .................. 2 Pigment suspension: Sicovit titanium dioxide [1] ..............................................100 g Polymer suspension: Kollicoat MAE30DP [1]................... Add the pigment suspension I to the well stirred polymer suspension II....................................20 g Sicovit Iron oxide Red 30 [1] .............– Triethyl citrate (Merck).......................5 g Kollidon 30 [1].. No.........................................350 g 600 g 18 g – 396 g Total I + II: .. 1 I....................... Stir the obtained suspension during the entire coating process...5 Coating formulations (Lab Scale) Enteric Film Coating of Tablets (Aqueous) I 1.................................................................................. Manufacturing of the suspension I Suspend the pigments and talc in the well stirred solution of Kollidon 30 and homogenize in a disk mill or in a colloid mill.....5 g Water................ 6 48 6 6 120 g g g g g 2....... II Separately suspend Kollicoat MAE30DP in the solution of propylene glycol or triethyl citrate........................1000 g 1200 g II..... Formulations No......

.........approx............9 mm convex Quantity of suspension applied .8 mm Spraying pressure .......12 rpm .....................................0 bar ..............approx......... 30 g/min .................................1.......continuous Inlet air temperature ...... Coating procedure (Accela Cota 24 ) Tablet core loading .......5 kg Core size.......continuous .........................................................4 mg Speed of the coating pan .................... approx.......................200 g Quantity of solids applied per cm 2 .. 30 min Spraying rate ........................................2....0 bar Type of spraying .......................12 rpm Spray nozzle ....0..................0..approx.50 °C .... 60 min .............9 mm convex............9 mg .........5 kg .............................. approx............7 mg Quantity of film-forming agent applied per cm 2 ..2.....................Enteric Film Coating ofablets T (Aqueous) I page 2 3... 40 °C Spraying time ............ 30 °C...........................................1.............60 °C Outlet air temperature ...............................800 g ........................ 6 mg ...............40 g/min BASF Pharma Ingredients Generic Drug Formulations 2001 ..........................8 mm ..........

..... 3...9 mm convex Quantity of suspension applied.............2..................0............4.....0 bar Type of spraying ............................................................................5 Coating formulations (Lab Scale) Enteric Film Coating of Tablets (Aqueous) II 1.................40 g/min BASF Pharma Ingredients Generic Drug Formulations 2001 ....................................... Formulations I............................... Pigment suspension: Sicovit titanium dioxide [1] .........990 g Quantity of solids applied per cm 2 .......5 kg Core size ..................... stir for 2-3 hours and add the propylene glycol........ II.............................................23 Water......990 g 2.............................................................................. Stir the obtained suspension during the entire coating process........... Coating procedure (Accela Cota 24 ) Tablet core loading .............................................................8 mm Spraying pressure ..........40 Sicovit Iron oxide Red 30 [1] ...............................continuous Inlet air temperature.....................................................................5 Talc [10] ....12 rpm Spray nozzle.........................................................................................6 mg Quantity of film-forming agent applied per cm 2 . 25-30 min Spraying rate ..............60 °C Outlet air temperature ..........................................665 g g g g g g g Total I + II: ..... II Separately suspend Kollicoat MAE100P in 665 g of water.................................................. 32-35 °C Spraying time .........................................................................................................149 Propylene glycol [1] ......................................103 Polymer suspension: Kollicoat MAE100P [1] ............................... 4 mg Speed of the coating pan ............................ Manufacturing of the suspension I Suspend the pigments and talc in 103 g of well stirred water and homogenize in a disk mill or in a colloid mill........5 Water... Add the pigment suspension I to the well stirred polymer suspension II.....................................

......................... II................. Coating procedure (Fludized bed) Tablet core loading ....3 bar Spraying time.......2 min Quantity of film forming agent/cm 2 .....................................................98 g Water.140 g Water............................5 kg Inlet air temperature ......... Isopropanol.....13 g Sicovit Iron oxide [1] ...........................59 g Isopropanol ..............................................................1 mg BASF Pharma Ingredients Generic Drug Formulations 2001 ...q............................................................................Positon 4 Spraying pressure ....................................... Kollidon VA 64 [1] ........ Formulation I...........5 Coating formulations (Lab Scale) Protective Film Coating with Ethyl Cellulose + Kollidon VA 64 1............................................... Manufacturing of the suspension Dissolve Ethocel and Kollidon VA 64 in isopropanol.Position 10 Outlet flap..38 °C Inlet flap ........................... s................60 g 2...................20 g Talc......40 °C Outlet air temperature ......................... add the water and suspend the colorants and the talc............. 3.....15 min Final drying....................5 g Ethocel ® 20 (Dow) ...............................4........................................... Pass this mixture through a colloid mill and add solution II......................................5 g Sicovit Titanium dioxide [1] ............................................................

5 s Drying phase (warm air) ......................20 g Klucel ® EF (Hercules) .............1 mg 5–6 h BASF Pharma Ingredients Generic Drug Formulations 2001 ...............< 800 g Spray phase............. Formulations No............. – 740 g 2..............................6 s Interval ............. 3.. Coating procedure (Sugar coating pan) No............... Pass this mixture through a colloid mill.......................– Sicovit Iron oxide [1] ......... 1 Loading of tablet cores (9 mm.......................................................2 s Nozzle (Walther WA XV) ......................8 mm 6.......................25 g Quantity of solids applied on each tablet core < 3....................s...............– 20 g 20 g 20 g q..... surface 3 cm 2 ).....................5 Coating formulations (Lab Scale) Protective Film Coating with Hydroxypropyl Cellulose + Kollidon VA 64 1... biconvex...................5 s 6s 2s 0....................................760 g Water ........... 2 (Final coating) Kollidon VA 64 [1] ................................<1 h Total coating time ...8 mm Quantity of sprayed suspension / min .....4...............<1 h No....................0.......................................2 kg Amount of coating suspension .. 2 2 kg 800 g 3s 0.........................20 g Talc ..........................................6 s Interval...... s................. 1 (Subcoating No............................................ Manufacturing of the suspension Dissolve Klucel and Kollidon VA 64 in isopropanol or water and suspend the colorants and the talc..........8 g 3...............0..2 mg.. Isopropanol..q..................

.............................36 Sicovit Iron oxide Red 30 [1].....................34 min Final drying.........................................................12 HPMC 6 mPa · s ........2......................................2 kg Inlet air temperature ........................60 °C Outlet air temperature .. Pharmacoat ® 606..4.....0 bar Spraying rate ..........216 1200 g g g g g g g g g 2.... Suspend the pigments and talc in 216 ml of water and pass this mixture through a colloid mill............. g................... To obtain the final coating suspension mix solution I with suspension II............................54 Water ............... II..... Manufacturing of the suspension Dissolve Lutrol E6000 and Kollidon VA 64 in 732 ml of water.....40 °C Nozzle.....0 kg Core size ......9 mm biconvex Amount of coating suspension applied.............. Kollidon VA 64 [1] ..............5 min at 60 °C Quantity of film former applied...................18 Talc [10] ..........5 Coating formulations (Lab Scale) Protective Film Coating with Hypromellose + Kollidon VA 64 1................ Formulation I........ Shin-etsu) Water.......................... Coating procedure (Accela Cota 24 ) Tablet core loading ...5.....732 Sicovit Titanium dioxide [1] .............................. 3.....14 mg/cm 2 BASF Pharma Ingredients Generic Drug Formulations 2001 ..........2 min Drying after spraying......................................................53 Lutrol E6000 [1] ......................12 rpm Spraying pressure ...........1................................................................79 (e.............................................. add HPMC and stirr 45 min avoiding the formation of too much of air bubbles...3..........50 g/min Spraying time (continuously) .............0 mm Rotation speed of the pan .................1................

Viscosity of the coating spray suspension Viscosity [mPa·s] The combination of HPMC with Kollidon VA64 reduced the viscosity of the spray suspension and therefore the spraying rate was increased: 1000 800 HPMC alone 600 HPMC + Kollidon VA64 (4+6) 400 Limit 200 0 0 3 6 9 12 Polymer concentration in water [%] BASF Pharma Ingredients Generic Drug Formulations 2001 15 18 .Protective Film Coating with Hydr oxypropylmethyl Cellulose + KollidonAV64 page 2 4.

..................000 g g g g g g g 2.....2 bar Spraying time...... Formulation Kollidon VA 64 [1] .........................45 °C Temperature at outlet............... Manufacturing A 500-g sample of this suspension was passed through a disk mill and sprayed under the following conditions: Sugar-coating pan Spray gun .........................................................................15 Sicovit Titanium dioxide [1] ......................Walther WAXV with 0............................................8-mm nozzle Temperature at inlet ......4.................................................................................6 sec Pause................................................................. 50 min BASF Pharma Ingredients Generic Drug Formulations 2001 ...........5 Sicovit Iron oxide [1] ........50 Lutrol E 6000 [1]...........................30 Talc [10] .............................ad 1..........................................................................38 °C Spraying pressure .......................5 Coating formulations (Lab Scale) Protective Film Coating with Kollidon VA 64 1.............40 Glycerol ............50 Water ....................................................5 sec Dry air .............3 sec Accela Cota 24 (continuous spraying) Spray gun ......................................3 sec Pause....Walther WAXV with 1-mm nozzle Spraying time .........0...........................

BASF Pharma Ingredients Generic Drug Formulations 2001 . Remark If the film is to sticky a certain part of Kollidon VA 64 should be substituted by hypromellose or sucrose.Protective Film Coating with Kollidon AV 64 page 2 3.

. To obtain the final coating suspension mix solution I with suspension II.........12 Polyvinyl alcohol (Mowiol® 8-88......................................................................840 Sicovit Titanium dioxide [1] .......................................................... Coating procedure (Accela Cota 24’ ’) Loading of tablet cores ..5 min Quantity of film former .....5 Coating formulations (Lab Scale) Protective Film Coating with Polyvinyl Alcohol + Kollidon VA 64 1..2.................................................83 min Final drying.......168 .. about 3 cm 2 ) Amount of coating suspension.......... 3....4....18 Talc .......5......................................... add the polyvinyl alcohol and stirr 45 min avoiding the formation of too much of air bubbles...0 kg (9 mm..about 3 mg/cm 2 applied BASF Pharma Ingredients Generic Drug Formulations 2001 ..................................... Manufacturing of the suspension Dissolve Lutrol E6000 and Kollidon VA 64 in 840 ml of water....46 °C Nozzle........................37 Sicovit Iron oxide Red [1] ...................................26 kg Inlet air temperature ...........50 Lutrol E6000 [1] .1.................................................................................1257 g g g g g g g g g 2................. Kollidon VA 64 [1] ...........0 bar Spraying rate .............. biconvex............. II... Formulation I...................................76 Water...............15 rpm Spraying pressure ...........0 mm Rotation speed of the pan ......15 g/min Spraying time (continuously) ..1....................................59 °C Outlet air temperature ........ Suspend the pigments and talc in 168 ml of water and pass this mixture through a colloid mill....... Hoechst)................................56 Water .....................

...............20 Sicovit Titanium dioxide [1] ......... Formulation Shellac ........................... Application of the coating suspension About 50 g suspension were applied to 1 kg of tablet cores in a conventional coating pan or in a Accela Cota pan (1 – 2 mg film formers/cm 2 ) BASF Pharma Ingredients Generic Drug Formulations 2001 ................... talc and the iron oxide and mix in the colloid mill...............185 Talc .....................458 g g g g g g g g 2.....................................................177 Kollidon 25 or 30 [1] .....15 Sorbitane trioleate ...................................30 Sicovit Iron oxide [1] .................5 Coating formulations (Lab Scale) Protective Film Coating with Shellac + Kollidon 30 1...... 3.............65 Cetyl alcohol ...............50 Isopropanol or ethanol ...... Add titanium dioxide.............................................4... Manufacturing of the coating suspension Dissolve shellac and sorbitane oleate in the warm solvent and then Kollidon and cetyl alcohol................

...100 g Ethanol or isopropanol . The amount of 0.4.........4 mg/cm 2 tablet surface is sufficient for a good subcoating protection...................... BASF Pharma Ingredients Generic Drug Formulations 2001 ..900 g 2.. Remark No plastisizer is needed in this formulation due to the plasticity of Kollidon VA 64.... Manufacturing (Accela Cota) Spray the solution onto the warm tablet cores (30 – 40 °C) for few minutes before to continue with the aqueous main coating procedure.... 3...........5 Coating formulations (Lab Scale) Subcoating for Core Protection 1... Formulation Kollidon VA 64 [1] ............

....................... Drying phase (warm air) ...................4........290 g Sicovit Iron oxide [1] .... Coating procedure 4 kg of tablet cores with a weight of 420 mg were sprayed with 2...............80 g Sicovit Titanium dioxide [1] ..16 h BASF Pharma Ingredients Generic Drug Formulations 2001 ...............................................................................10 min...................................................5 Coating formulations (Lab Scale) Sugar Coating................ than mix with glycerol................ 3.....90 g Talc ......5 s Interval .................................................................. Formulation of the coating suspension Sucrose ... s............................................... dissolve Kollidon 30 and suspend the other components...........q...5 kg of the above suspension in a conventional coating pan under the following conditions: Spray phase ............................90 g Calcium carbonate ....... automatic 1... Manufacturing of the coating suspension Dissolve the sucrose in the hot water...630 g 2............... Glycerol ..................................................40 g Water.760 g Kollidon 30 [1] ......... Total coating time ................................10 min.

.................3.. 2 continue with the same procedure until homogeneous coloured sugar coated tablets are obtained.... 3.3 g Sicovit Titanium dioxide [1] .................. 1 by means of the manual sugar coating procedure during some hours........5..........4.......... Polysorbate or Cremophor and sucrose in the water and suspend the other components in this solution.............16.................70 g Sicovit Iron oxide [1] ..................0 g Polysorbate or Cremophor RH 40 [1] ..................... Mix in a colloid mill.............................8 g Carmelose sodium........ Formulations No...3 3. After changing to formulation No....8 14............10.14...7 81......6 10...– Sucrose ............. manual 1.............5 Coating formulations (Lab Scale) Sugar Coating..7 g Talc ..............135 1..............0 17.......135 g Water... BASF Pharma Ingredients Generic Drug Formulations 2001 ...6 g Aerosil 200 [4] ......... 2 Coloured 16........1........................ 4........... Remark The polishing can be done by means of a solution of beeswax or polyethylene glycol 6000.....................0 5.......81..........3 115...................650 g g g g g g g g g 2.... Manufacturing of the coating suspensions Dissolve Kollidon... Application of the coating suspension Start with formulation No.. 1 White Kollidon 30 [1] ...................650 g No..

....4 mg/cm 2 BASF Pharma Ingredients Generic Drug Formulations 2001 .....................2.................................15 rpm Spraying pressure .0 bar Spraying time (continuously) ......................................................................... 3.8 mm Rotation speed of the pan ..................0............ Formulation of the coating suspension Sucrose ................................36 °C Nozzle..........4.30 Sicovit Iron oxide [1] ......2 kg Inlet air temperature ...................1.................................................................................... Pass through a colloid mill....50 Water ........0 kg Amount of coating suspension ....................200 Kollidon VA64 [1] ...............45 °C Outlet air temperature ........................15 Macrogol 4000 ... Coating procedure (Accela Cota 24’ ’) Tablet core loading ............... Manufacturing of the coating suspension Dissolve the sucrose...................................5...........................50 min Quantity of film former applied ...............5 Coating formulations (Lab Scale) Sugar Film Coating 1...........................40 Talc ..... Kollidon VA64 and Macrogol 4000 in the water and suspend the other components.........................50 Sicovit Titanium dioxide [1] .ad 1200 g g g g g g g 2.............

............3 g III Caffeine spheronized pellets 10 %....................... Stir the obtained suspension during the entire coating process...............1 Water....................5 Coating formulations (Lab Scale) Sustained Release Coating of Caffeine Pellets 1................................14......1 Talc [10] ....100....2........ BASF Pharma Ingredients Generic Drug Formulations 2001 ...2.................500 g 2..................................4........................506...200... suspend the pigments and talc and homogenize in a colloid mill..2..................................5 Sicovit iron oxide Red [1]... Formulation of the coating suspension I Polymer Suspension: Kollicoat SR30D [1]...........3. Add the pigment suspension II to the well stirred polymer suspension I..................1 Sicovit Titanium dioxide [1].... Manufacturing of the coating suspension I Mix propylene glycol with water and suspend slowly Kollicoat SR30D.........0 g 1....9 g g g g g Total I + II: ............................ II Dissolve Kollidon 30 in water..................3 g Water ................75...2-Propylene glycol [1] ..0 g II Pigment suspension: Kollidon 30 [1] ....

...............................400 g = 3 mg/cm 2 Nozzle .......................3 g/min Drying time after coating (45 °C).8 mm Spraying pressure ........ 2-24 h: pH 6........................8) 100 80 60 40 20 0 0 2 4 6 8 10 12 14 time [h] BASF Pharma Ingredients Generic Drug Formulations 2001 16 18 20 22 24 ............................................35 °C Spray rate ..............................................................Sustained Release Coating of Caf feine Pelle ts page 2 3.......................................... Coating procedure (Fluidized bed Aer omatic Strea-1) Loading of caffeine pellets 10 % (III) .................500 g Quantity of spray suspension applied ..................................................................08N HCI........... Release of caf feine (0-2 h 0..................1 bar Inlet temperature........0..........................................................................5 min [%] 4..................................60 °C Outlet temperature .............................

................... 3.................. Manufacturing of the suspension Add the talc suspension II to the well stirred polymer suspension I...........50 °C Outlet temperature ..........1 g II Talc Suspension: Talc [10] .............................4................1.........................................................................................5 Coating formulations (Lab Scale) Sustained Release Coating of Diclofenac Pellets 1.............2 g Solid Content I+II:...80 m 3 /h Spray rate ........................5 g (=20 %) III Diclofenac sodium spheronized pellets 30 % (see Chapter 5..........................4 mg/cm 2 Nozzle .1 bar Inlet temperature........................35 min Drying time ...........................3 g Water ..................................... top spray (Fluidized bed Aer omatic Strea-1) Loading of diclofenac pellets..................................................................................... Coating procedure.....................482 g Quantity of solids applied ..............0............97 g Quantity of polymer applied.................................................4) ..........482..................................5 min (45 °C) BASF Pharma Ingredients Generic Drug Formulations 2001 ....500 g 2....................................................14 g/min Spray pressure..................8 g Total I + II: ..............500 g Quantity of spray suspension applied ................................228..................29.........33 °C Air volume......................................................2 bar Spray time.................................................................................................... Stir the obtained suspension during the entire coating process....................................................... Formulation I Polymer Suspension: Kollicoat EMM30D [1]............................................96........................................224........................................................................8 mm Spraying pressure ......

Release of diclofenac sodium (0-2 h 0.Sustained Release Coating of Diclofenac Pelle ts page 2 drug release [%] 4.8) 100 80 60 40 20 0 0 2 4 6 8 10 12 14 time [h] BASF Pharma Ingredients Generic Drug Formulations 2001 16 18 20 22 24 . 2-24 h: pH 6.08 N HCI.

4 g 1......................249............ Manufacturing of the suspension I Mix propylene glycol with water and suspend slowly Kollicoat SR30D..................2-Propylene glycol [1] ................................. Stir the obtained suspension during the entire coating process.7.5 g Water ...................44...................174...............506..29.............................9 g Total I + II: .................................. II Suspend the talc in water and homogenize in a colloid mill..... BASF Pharma Ingredients Generic Drug Formulations 2001 .500 g 2......9 g Water....3 g III Propanolol HCI spheronized pellets 20 % (See chapter 5......................................5 Coating formulations (Lab Scale) Sustained Release Coating of Propanolol Pellets I 1............ Add the talc suspension II to the well stirred polymer suspension I. Formulation I Polymer Suspension: Kollicoat SR30D [1].....4) .................4.6 g II Talc Suspension: Talc [10] ...

Sustained Release Coating of opanolol Pr Pelle ts I page 2 3......................0..........................................35 °C Spray rate ...................................................................................8) 100 80 60 40 20 0 0 2 4 6 8 10 12 14 time [h] BASF Pharma Ingredients Generic Drug Formulations 2001 16 18 20 22 24 ......................................................................1 bar Inlet air ................................................... Release of pr opanolol HCI (0-2 h 0........500 g Quantity of spray suspension applied ...................................................................506 g = 3 mg/cm 2 Nozzle ....08N HCI......................................................................... Coating procedure (Fluidized bed Aer omatic Strea-1) Loading of propanolol pellets 20 % (III) ............................................. 2-24 h: ph 6.............................................5 min propranol release [%] 4..................................................................1............................................39 min Drying time after coating (45 °C)................60 °C Pellet temperature ........2 bar Spray time........3 g/min Spray pressure.................................................8 mm Spraying pressure ....................36 °C Outlet temperature .................................................................80 m3 /h Inlet temperature....

.......9 Water ...................................... Stir the obtained suspension during the entire coating process..................246 g III Propanolol HCI spheronized pellets 30 % (See chapter 5...............................60 g 2..............................5.....................257........................................... Add the pigment suspension II to the well stirred polymer suspension I....393....1000 g Solid Content I+II:.........0 g Water .. II Dissolve Kollidon 30 in water..........5 Coating formulations (Lab Scale) Sustained Release Coating of Propanolol Pellets II 1... suspend the iron oxide pigment and talc and homogenize in a colloid mill.....221................................. Then add Pharsil 21046 VP............1000 g IV Antitack suspension: Aerosil 200 [4] .. BASF Pharma Ingredients Generic Drug Formulations 2001 .....................70. Formulation I Polymer Suspension: Kollicoat EMM30D [1] ......4) .......1 g Water....6 g g g g g Total I + II: ............4...........0 Talc [10] ...........................0 Sicovit Iron oxide Red 30 [1]...........3 g II Pigment Suspension: Kollidon 30 [1] ..2 Pharsil 21046 VP [Wacker] ............... Manufacturing of the suspension I Dilute the Kollicoat suspension with water.................................5............................................47...................

..............................................................8 mm Spraying pressure ......................................61 g propranol release [%] 4....40-45 °C Pellet temperature.......28-30 °C Spray rate ........................................................................................................28-31 °C Outlet temperature ..... 2-24 h: ph 6............................7-11 g/min Drying time after coating .........................5 min Antitack suspension after coating .........................................................100-120 m 3 /h Inlet temperature.........................................................1 bar Inlet air .............. Coating procedure (Fluidized bed Aer omatic MP-1) Loading of propanolol pellets (III) ..............................08N HCI.......................................Sustained Release Coating of opanolol Pr Pelle ts II page 2 3............................ Release of pr opanolol HCI (0-2 h 0..............................8) 100 80 60 40 20 0 0 2 4 6 8 10 12 14 time [h] BASF Pharma Ingredients Generic Drug Formulations 2001 16 18 20 22 24 ....................................0.....................................................................................1 kg Nozzle ........

........6....223......................15............... Stir the obtained suspension during the entire coating process........4...... II Dissolve Kollidon 30 in water.2-Propylene glycol [1] ....2 Sicovit Titanium dioxide [1].................44..............2 Talc [10] ...5 Coating formulations (Lab Scale) Sustained Release Coating of Theophylline Pellets 1.7 g Water .......................2....3 g III Theophylline pellets Sperofillin ® (BASF) 2..........2...................................447......... suspend the iron oxide and titaniom dioxide pigments and talc and homogenize in a colloid mill...............................................................9 g II Pigment Suspension: Kollidon 30 [1] ......7 g g g g g Total I + II: . Add the pigment suspension II to the well stirred polymer suspension I..149...7 Water.... BASF Pharma Ingredients Generic Drug Formulations 2001 .......2.. Formulation I Polymer Suspension: Kollicoat SR30D [1]................... Manufacturing of the suspension I Mix propylene qlycol with water and suspend slowly Kollicoat SR30D....................7 g 1..........................2 Sicovit Iron oxide Red 30 [1]..........

..............1 bar Inlet air .........5 g/min Spray time for 448 g suspension ......................................................5 min theophylline rerlease [%] 4..11...............................................................0.....38 °C Outlet temperature ...................08N HCI.........................................60 °C Pellet temperature ................8) 100 1 mg/cm3 80 60 40 2 mg/cm3 20 0 0 2 4 6 8 10 12 14 time [h] BASF Pharma Ingredients Generic Drug Formulations 2001 16 18 20 22 24 .............................................. 224 g = 1 mg solids/cm 2 Nozzle ...........................................80 m3 /h Inlet temperature........... Coating procedure (Fluidized bed Aer omatic Strea-1) Loading of Sperofillin pellets .........................................................................................................................................................Sustained Release Coating of Theophylline Pelle ts page 2 3................................... Release of theophylline (0-2 h 0.....................39 min Drying time after coating (45 °C).....................................................................500 g Quantity of spray suspension applied ...........................8 mm Spraying pressure .....................................................................448 g = 2 mg solids/cm 2 . 2-24 h: ph 6...........37 °C Spray rate ..........................................

............. suspend the iron oxide pigment and talc and homogenize in a colloid mill......238.1000 g Solid content: .........5...........5 Water ...39..4) .................. Formulation I II Polymer Suspension: Kollicoat EMM30D [1] ........214.................................5.......... Then add Pharsil 21046 VP.................0 Pharmacoat 603 [Shin-Etsu]...58...... Add the pigment suspension II to the well stirred polymer suspension I................................5 g g g g Pigment Suspension: Kollidon 30 [1] ..1 g Water.......60 g 2...............................................3........5 Coating formulations (Lab Scale) Sustained Release Coating of Verapamil Pellets 1...................................................................8 Water ................................... II Dissolve Kollidon 30 in water....2 g g g g g Total:........ Stir the obtained suspension during the entire coating process...............1000 g IV Antitack suspension: Aerosil 200 [4] ........1 g III Verapamil HCI spheronized pellets 48 % (See chapter 5....................4........................325........45.......... suspend Avicel PH105 and add slowly Kollicoat EMM30D....0 Talc [10] ...........0 Avicel PH105 [5] .....0 Sicovit Iron oxide Red 30 [1]............... Manufacturing of the suspension I Dissolve Pharmacoat 603 in water............0 Pharsil 21046 VP [Wacker] .....280.............. BASF Pharma Ingredients Generic Drug Formulations 2001 ..................................................

.28-31 °C Outlet temperature .................................................................................... Coating procedure (Fluidized bed Aer omatic MP-1) Loading of verapamil HCI pellets (III) ......................................................................................................................................................................... Release of verapamil HCI (0-2 h 0...............................................................08N HCI........................................................61 g verapamil release [%] 4........141 g = 2........................................5 min Antitack suspension after coating ...........7-11 g/min Drying time after coating (45 °C)..................................Sustained Release Coating oferapamil V Pelle ts page 2 3......1 bar Inlet air ..8 mm Spraying pressure ...28-30 °C Spray rate .........................100-120 m 3 /h Inlet temperature...................................................................... 2-24 h: ph 6..............8) 100 80 60 40 20 0 0 2 4 6 8 10 12 14 time [h] BASF Pharma Ingredients Generic Drug Formulations 2001 16 18 20 22 24 ................0....40-45 °C Pellet temperature..........1 kg Quantity of solids applied.............................................................4 mg/cm 2 Nozzle ..

5. Normally the amounts used were those required for a trial of 50 – 500 g. drying. e. powders. in fluidized-bed granulation.e. Fluidized-bed granulation was resorted to only in exceptional cases in view of the amounts needed. and again screening.1 Size of formulations and amounts used The formulations were developed on a laboratory scale. Consequently. the properties of the suspension thus formed were assessed. i. moistening.5 Granules. 5.g. BASF Pharma Ingredients Generic Drug Formulations 2001 .3 Assessment of the properties of the granules Most of the cases concerned granules that were suspended in water before the administration. dry syrups and lyophilisates 5. See Chapter 5.2 Methods of granulation The granules were mostly produced by traditional means. were only resorted to in exceptional cases. Larger batches.4 Formulations The formulations in this chapter have been arranged in alphabetical order of their active substances. The parameters that attracted most attention were the relative sediment volume (volume of sediment/total volume) and the redispersability. screening.3 for details on the suspensions. 5.

.......... water dispersible granules having almost no bitter taste.. Properties of the granules Free flowing...................4 Cremophor RH 40 [1] ...... Fill 3........ Formulation (granules) I...... II.................... dry and sieve again..............4.......about 50 g g g g g g 2...................... Manufacturing Granulate mixture I with solution II..........6 Lutrol F 68 [1]............ dry syrups and Iyophylisates (Lab scale) Aceclofenac Instant Granules (50 mg) 1. 3..................8 mm screen..... Aceclofenac ....................................................4..........5...................4 Water ..3 Orange flavour ...... BASF Pharma Ingredients Generic Drug Formulations 2001 ......4 Formulation of granules...3 Sorbitol .4..9 g in sachets corresponding to 50 mg aceclofenac....85.... pass through a 0.....1...

......... Instant granules (200 mg albendazole sachet): Suspend 5 g of the granules (= 200 mg albendazol) in a glass of water........88 Ethanol 96 % ...2 g g g g g g 2. dry syrups and Iyophylisates (Lab scale) Albendazole Dry Syrup or Instant Granules (200 mg) 1......5................... Albendazole . II..... pass through a 0.... Formulation I... Manufacturing Granulate mixture I with solution II.......... crystalline [10].............. Fill 50 g of the granules in a 100 ml flask (= dry syrup) or 5 g in sachets (= instant granules) 3...................................4 Citric acid ........................... The obtained suspension has no bitter taste....................................... BASF Pharma Ingredients Generic Drug Formulations 2001 ........ The suspension has no bitter taste..22 Lutrol F 68 [1] ..............3 Sodium citrate.8 mm screen............ Administration forms Dry syrup (200 mg albendazole /10 ml): Fill the flask containing 50 g of granules with water to the 100 ml mark........ dry and sieve again.....................4 Formulation of granules............................3 Sorbitol..

..0... Formulation I....25. Aluminium hydroxide dry gel (Giulini) ... dry syrups and Iyophylisates (Lab scale) Aluminium Hydroxide + Magnesium Carbonate Dry Syrup (12..........25...about 36.................... 3.................5%) 1......4 Formulation of granules....0 Kollidon 30 [1] ................5...... – Redispersibility very easy.........................0....0 g g g g g g g g g g g 2.0 Kollidon CL-M [1].4 Banana flavour .......5...................25....5 Saccharin sodium...............0 Basic Magnesium carbonate ..0............................ Properties of the suspension – Homogeneous and without sedimentation during more than 24 h........ BASF Pharma Ingredients Generic Drug Formulations 2001 .....5% + 12...................10........................1 .. 4.................................... crystalline [10] ............ II..................6 Orange flavour .............................0...... pass through a sieve and dry.......... Manufacturing Granulate mixture I with solution II...5 Water............0 Coconut flavour.......29... Preparation of the suspension for administration Shake 58 g of the granules with 100 ml of water............................0 Sorbitol.

5%)page 2 Relative sediment volume after 24 h [%] 5.Aluminium Hydr oxide + Magnesium Carbonate Dry Syrup (12.5% + 12. Influence of the amount of Kollidon Cl-M on the sedimentation of the obtained suspension 100 80 60 40 20 0 0 4 8 Kollidon CL-M in the administration form [%] BASF Pharma Ingredients Generic Drug Formulations 2001 12 .

.5 Lemon flavour ....................4 Formulation of granules.9....... Formulation Amoxicillin trihydrate...............40..................................5.. Properties of the suspension The pH of the suspension is about 4.......0 Citric acid.....0 Sodium citrate....5...... 3............6....0........ BASF Pharma Ingredients Generic Drug Formulations 2001 ..........................5..........1 Sodium gluconate .......................... Preparation of the suspension for administration To 66 g of the powder add water to fill to a total volume of 100 ml shaking very well......... dry syrups and Iyophylisates (Lab scale) Amoxicillin Dry Syrup (5% = 500 mg/10 ml) 1.......2.................0 Sorbitol crystalline [10] .......5... crystalline ......0............. No sedimentation could be observed during more than 24 hours..........0 Orange flavour ..4 g g g g g g g g g 2...... The redispersibility is very easy after 2 weeks.............5 Saccharin sodium.........1...............................0 Kollidon CL-M [1] ........ 4................ Manufacturing Mix all components and fill in a flask......

Influence of the amount of Kollidon CL-M on the sedimentation of the obtained suspension 100 90 80 70 60 50 0 0 4 6 2 Kollidon CL-M in the administration form [%] BASF Pharma Ingredients Generic Drug Formulations 2001 8 .Amoxicillin Dry Syrup (5% = 500 mg/10 ml) page 2 Relative sediment volume after 24 h [%] 5.

. Patent 0....50 g Water for injections .................... the dry content of an ampoule is mixed with 1..... Formulation Amoxicillin sodium ... Administration Prior to administration.495 + 0. 1979...7.....6.....5.012.... Beecham) 1.............. BASF Pharma Ingredients Generic Drug Formulations 2001 .00 ml 2....... fill 500-mg-portions of the dry lyophilisate into ampoules....496...9 ml of water to give a clear injection solution..... dry syrups and Iyophylisates (Lab scale) Amoxicillin Lyophylisate for Injection (250 mg) (according to Eur..25 g Kollidon 12 PF [1] .......add 100....012...4 Formulation of granules... Manufacturing Dissolve the active ingredient in the well stirred solution of Kollidon 12 PF and after freeze-drying. 3....

........... 3..................... No sedimentation could be observed during more than 24 hours...4 Formulation of granules............1 Sodium gluconate .9.................1.......................0 Sodium citrate............ Formulation Ampicillin trihydrate ..... Preparation of the suspension for administration To 66 g of the powder add water to fill to a total volume of 100 ml shaking very well...... The redispersibility is very easy after 2 weeks...........5 Saccharin sodium.....5........0 Citric acid.. Properties of the suspension The pH of the suspension is about 4..................2..........5 Lemon flavour ................... Manufacturing Mix all components and fill in a flask.5............. 4...... BASF Pharma Ingredients Generic Drug Formulations 2001 ...0 Kollidon CL-M [1] .6.....0 Sorbitol crystalline [10] . dry syrups and Iyophylisates (Lab scale) Ampicillin Dry Syrup (5% = 500 mg/10 ml) 1..0 Orange flavour .............4 g g g g g g g g g 2.........................................40.....5...0...................................5.....0........................ crystalline ..........

Influence of the amount of Kollidon CL-M on the viscosity of the obtained suspension 80 60 40 20 0 0 2 4 6 Kollidon CL-M in the suspension [g/100 ml] BASF Pharma Ingredients Generic Drug Formulations 2001 8 .Ampicillin Dry Syrup (5% = 500 mg/10 ml) page 2 Viscosity [mPa·s] 5.

. 3........0 mm sieve and dried at room temperature..2....... II... crystalline...0 Sodium citrate................. Remark See also “Sustained Release Coating of Diclofenac Pellets” BASF Pharma Ingredients Generic Drug Formulations 2001 ... dry syrups and Iyophylisates (Lab scale) Azithromycin Dry Syrup (5% = 500 mg/10 ml) 1.............5......0.......... Azithromycin dihydrate ....9.0............5 Kollidon CL-M [1] ..................................................................... Formulation I..............5............................. The obtained granules are passed through a 1............60...............................9.3 g g g g g g g g g 2......0.......................0 Sodium cyclamate ...........5 Cremophor RH 40 [1] ....0 Sucrose ...................... Manufacturing The mixture I is granulated with the solution II...4 Formulation of granules.............0 Menthol.............0 Ethanol ... Fill 83 g of the granules in a 100 ml flask.....0 Citric acid .....5...........................

. Dry the pellets in a fluidizedd bed at 70°C....... dry syrups and Iyophylisates (Lab scale) Diclofenac Spheronized Pellets for Sustained Release Coating (30%) 1....................... II... Diclofenac sodium ...........300 Avicel PH101 [5] ................about 580 g g g g g 2.... BASF Pharma Ingredients Generic Drug Formulations 2001 ..........................4 Formulation of granules............ Manufacturing Granulate the mixture (I) in a Diosna granulator with water (II) and press the humid granules through a sieve of 1................... Form pellets in a spheronizer during 10 min with the rotation speed of 380-420 rpm........237 Kollidon VA64 [1] .....5 mm.............. Formulation I..................5..........438 Granulac 230 [8].................25 Water ...........

..160 g Kollidon CL [1].q.......... Dissolution 100 80 with Kollidon CL 60 40 20 without Kollidon CL 0 0 15 30 45 60 75 Minutes 90 105 120 BASF Pharma Ingredients Generic Drug Formulations 2001 ...........4 Formulation of granules........5............ 2......... Indomethacin dissolved [%] 3.......................... dry syrups and Iyophylisates (Lab scale) Indomethacin Powder for Hard Gelatin Capsules (160 mg) 1................. Formulation Indomethacin ..... Manufacturing Mix the components for about 10 min and fill in hard gelatin capsules to obtain 160 mg indomethacin in each capsule.......s.........................320 g Aerosil 200 [4] ...

50.................................. BASF Pharma Ingredients Generic Drug Formulations 2001 .......... Administration • Instant granules in sachets: Suspend 2 g (= 1 sachet) in a glass of water (= 800 mg Magaldrate) • Dry syrup: Fill the flask with drinking water until the mark of 100 ml and shake well............ Formulation I......80........ 3.0.....0 g Saccharine sodium ...............8 mm sieve to obtain free-flowing granules...0 g Kollidon CL-M [1]................5.........................4 Formulation of granules....... Manufacturing Granulate mixture I with solution II and pass through a 0......... Fill 2 g in sachets or 20 g in a 100 ml flask.......about 70 ml 2.1..................................0 g Banana flavour ............0 g Coconut flavour ...0 g Sorbitol.10...... II.....1.100........10.. dry syrups and Iyophylisates (Lab scale) Magaldrate Instant Powder or Dry Syrup (800 mg) 1........... 10 ml of the suspension correspond to 800 mg Magaldrate.....................................................................0 g Orange flavour ............... Magaldrate USP .......0 g Kollidon 90 F [1] .........2 g Water . crystalline [10] ...........

..............1............ pass through a 0.... dry well and mix with III........10 Pyridoxine hydrochloride (BASF) .....66 coated 0.U..................... Vitamin A acetate dry powder 325...0.............00 III....2.00 Fructose ..20....0.00 Flavours .................00 Citric acid ............1............ powder (BASF) ..................................... Kollidon VA 64 [1] ......0.......... Formulation I...................................0...25......50.0..... dry syrups and Iyophylisates (Lab scale) Multivitamin Effervescent Granules (1 RDA of Vitamins) 1...................................10 II.......... Manufacturing Granulate mixture I with solution II................................... Thiamin hydrochloride (BASF)...000 I............1.5................50 Vitamin D 3 dry powder 100....00 Cyclamate sodium ...........26 Riboflavin (BASF) ..2..........00 Saccharine sodium ..15... BASF Pharma Ingredients Generic Drug Formulations 2001 ..........000 I.........80.........40............30 Nicotinamide ....../g CWD (BASF) ...........00 Kollidon CL-M [1]..............10 Cyanocobalamin gelatin ............................25 Calcium D-pantothenate (BASF) ......80 Vitamin E acetate dry powder 50 %....................1% (BASF) Sodium bicarbonate .......130......35..U...........4 Formulation of granules............/g CWD (BASF) ............00 Sucrose ...........20..............0.........50 Ascorbic acid.........00 g g g g g g g g g g g g g g g g g g g g 2......... Fill 3 – 4 g in sachets.....................00 Isopropanol ..........8 mm sieve.............

Administration 3 – 4 g of the granules (= 1 sachet) correspond to about 1 RDA of the vitamins BASF Pharma Ingredients Generic Drug Formulations 2001 . Properties of the granules Colour: Flowability: Dispersibility: Yellow granules Very good 4 g disperse homogeneously in water after about 40 seconds.Multivitamin Ef fervescent Granules (1 RDA ofitamins) V page 2 3. 4.

......1................... E and B 12 should be added after the granulation of the other components..............33 g Nicotinamide ............000 g Kollidon CL-M [1].............approx..... Administration Suspend 6 –12 g (= 1 sachet) in a glass of water corresponding to 2 – 4 RDA of vitamins..........000 g Kollidon VA 64 [1] ............. 7 l 2....../g CWD (BASF) ................. 3..... the dry powders of vitamin A..5.....................2....1%.... dry syrups and Iyophylisates (Lab scale) Multivitamin Instant Granules (2–4 RDA of Vitamins) 1..........................26 g Riboflavin (BASF).150 g Cyanocobalamin 0............4 Formulation of granules......210 g SD 50 (BASF) Sucrose........22 g Calcium D-pantothenate (BASF) .. Formulation I.................000 I......................66 g gelatin coated (BASF) Ascorbic acid powder (BASF) ..000 + 50.000 g Ethanol or Isopropanol ... Vitamin A+D dry powder 250..................................... Manufacturing Pass mixture through a 0.5........110 g Pyridoxine hydrochloride (BASF)....... finely ground . BASF Pharma Ingredients Generic Drug Formulations 2001 ......U...20................ Fill 6 –12 g of the granules in sachets...1..................... If the technology of a fluidized bed is not available.....8 mm sieve and granulate with solution II in the fluidized bed.....000 g Orange flavour.....200 g Thiamine mononitrate (BASF) ...........150 g Vitamin E acetate dry powder ................ II..

.............................. HPLC) Vitamin C.........Multivitamin Instant Granules (2–4 RDA of itamins) V page 2 4.... Stability (after 12 months........... The uniform.....not tested All other vitamins ......91% Calcium pantothenate ....... Properties of the suspension The multivitamin suspension is prepared prior to application by shaking the granules with water. The redispersibility is very easy.............. 5.. 20–25 °C.......> 95 % BASF Pharma Ingredients Generic Drug Formulations 2001 ............ yellow suspension thus obtained shows no sedimentation over a period of some hours.........

......... BASF Pharma Ingredients Generic Drug Formulations 2001 ....... dry at 60°C under vacuum conditions.....5 g Caffeine (BASF) ................ 4.............. Fill 2................... Kollidon 30 [1] ................. Remark If the solvent insopropanol is replaced by water the granulation should be done in a fluidized bed..................30 g Sugar .... Manufacturing Granulate mixture I with solution II.... 3... Formulation I...........................391 g Sodium hydrogen carbonate ..............1 g in sachets at maximum 30 % of relative atmospheric humidity.....5. III......33 g Tartaric acid ............................ Paracetamol......417 g II..............q.6 g Isopropanol (or Ethanol) .......................707 g 2...... Properties Free flowing granules........s............. powder....... Sodium citrate.........................................4 Formulation of granules............500 g Doxylamine succinate ......1 g) 1..... dry syrups and Iyophylisates (Lab scale) Paracetamol (= Acetaminophen) + Doxylamine + Caffeine Effervescent Granules (500 mg + 5 mg + 33 mg/2... sieve and mix with III....................

...50 g Sucrose.........0 g in sachets......5 g 500 mg paracetamol) in a glass of Formulation No.................... Formulation No................ dry syrups and Iyophylisates (Lab scale) Paracetamol (= Acetaminophen) Instant Granules (250 mg or 500 mg) 1..............5 g or 3.............75 g 50 g – 130 g 50 g 7g 5g 5g 3g 3g – 8g 50 g 2.................. and pass through a 0.....128 g Sorbitol Instant (Merck)............ BASF Pharma Ingredients Generic Drug Formulations 2001 .... 1 No.......12 g Kollidon 90 F [1] ........ Manufacturing (W et granulation) Granulate mixture I with solution II.......... fine powder ......... 2: Fill 1....– Citric acid ......................– Kollidon CL-M [1] ....... No.............. 1: Fill 1... 3....... or 2.............................. Properties of the granules The free flowing granules are very well dispersible in cold water......... fine powder..... 1: Suspend 1.............. Formulations I................................................ 2 Paracetamol.......– Ethanol 96 %.............. 2: Suspend 1..... II.................5 g Strawberry flavour ..........................................................5 g Sodium citrate .. Administration Formulation No........................3 g 500 mg paracetamol) in a glass of or 3........8 mm sieve......5......– Kollidon 30 [1] .0 g of the granules (= 250 mg or water.................... Formulation No...............6 g in sachets......7 g Orange flavour ..........6 g of the granules (= 250 mg or water.....................................3 g or 2.. 4...4 Formulation of granules........................90 g Aspartame ........

BASF Pharma Ingredients Generic Drug Formulations 2001 . 6. 1) No loss of paracetamol after 2 months at 60 °C. milky appearance with a sweet and fruity taste. No sedimentation within two hours. Properties of the suspensions Yellowish. Chemical stability of the granules (Formulation No.Paracetamol (= Acetaminophen) Instant Granules (250 mg or 500 mg) page 2 5.

...0 Maize PO 4 Aerosol (Hauser) . dry syrups and Iyophylisates (Lab scale) Povidone-Iodine Powder Spray 1.........1...50.................22.. Isopropyle myristate ............................. 1+3 ... Formulation I..25....5 Dow Corning 344 Fluid (DOW) . PVP-Iodine 30/06 M 10 (BASF)............ Manufacturing Suspend PVP-Iodine and Maize-PO4-Aerosol (I) in the liquid mixture II and fill in aerosol cans with the propellants III........ Propane + butane........................ III....25........5...0 Pentane ......10......... BASF Pharma Ingredients Generic Drug Formulations 2001 .......0 II.0 g g g g g g 2...............4 Formulation of granules.........

7 mm sieve to eliminate the fine particles...5 mm.................................4 Formulation of granules...... Manufacturing Granulate the mixture (I) in a Diosna granulator with water (II) and press the humid granules through a sieve of 1.....517 Granulac 230 [8] .about 500 30% Pellets g g g g g 300 467 208 25 540 g g g g g 2..................... Formulations 20% Pellets I II Propanolol HCI............ Form pellets in a spheronizer with the rotation speed of 200-400 rpm............... 3.......... Dry the pellets in a fluizid bed and sieve through a 0..25 Water .... dry syrups and Iyophylisates (Lab scale) Propanolol Spheronized Pellets for Sustained Release Coating (20% and 30%) 1...........................................200 Avicel PH101 [5] ............5.... Remark See also “Sustained Release Coating of Propanolol Pellets” BASF Pharma Ingredients Generic Drug Formulations 2001 .................................258 Kollidon VA64 [1] ..............................

......10................ Manufacturing Introduce solution II into the mixture I.....g.......... 1 to 2 g) in 100 ml of drinking water..0 Ethanol ...... 4..... dry syrups and Iyophylisates (Lab scale) Simethicone Instant Granules (60 mg and 120 mg) 1..................... – 98 % coarser than 50 µm.. g g g g g g g g 2........... Goldschmidt) . Administration Take the content of one sachet (1 g = 60 mg simethicone or 2 g = 120 mg simethicone) as powder or disperse the recommended amount (e.... Properties of the granules – Free flowing white granules.......... crystalline (Merck) ..............0 III.... Kollidon VA 64 [1] ..0 Orange flavour (Dragoco) .....4 Formulation of granules.......0 Kollidon CL-M [1].3....0 Fructose (Merck) .5.........50. Fill 1 or 2 g in sachets.............0 Cremophor RH 40 [1] .... dry and pass through a 1 mm sieve........ 3......................0...... Formulation Simethicone (Abil ® 200...........................5 I... Sorbitol...............50.5. BASF Pharma Ingredients Generic Drug Formulations 2001 .... Granulate the powder mixture III with the well stirred mixture I/II.....0 II. – Easily dispersible in cold water without any physical separation during 30 min...50........40....

.....................................0 Sodium gluconate ..0. crystalline [10] ...............8 Sorbitol.30.................5.......... 3.................4 Formulation of granules..............1 Saccharin sodium ....0 Sodium citrate........0 Vanillin ................................0...1 g g g g g g g g g g 2.0... 4....... The redispersibility is very easy after 2 weeks......... Formulation Sulfamethoxazol ..........1 Sodium benzoate ...1 Chocolate flavour ..... BASF Pharma Ingredients Generic Drug Formulations 2001 ... Fill 55 g of the mixture in a 100 ml flask.............. dry syrups and Iyophylisates (Lab scale) Sulfamethoxazol + Trimethoprim Dry Syrup (400 mg + 80 g/10 ml) 1............... Preparation of the administration form Shake 55 g of the powder with 100 ml of water until a homogeneous suspension is obtained... Properties of the obtained suspension No sedimentation during more than 24 hours......................5........................0.....5....................10.4.............................. Manufacturing Mix all components and sieve for administration...0 Kollidon CL-M [1]..................0................................................0 Trimethoprim ......

.. dry syrups and Iyophylisates (Lab scale) Verapamil Spheronized Pellets for Sustained Release Coating (48%) 1...........20 Aerosil 200 [4] ...............................5..................... Dry the pellets in a fluidized bed and sieve through a 0..........................................4 Formulation of granules.... Remark See also “Sustained Release Coating of Verapamil Pellets” BASF Pharma Ingredients Generic Drug Formulations 2001 ...........7 mm sieve to eliminate the fine particles....25 Talc [10] .....................480 Avicel PH101 [5] ........................ 3......400 g 2.300 Kollidon VA64 [1] .........5 mm..... Manufacturing Granulate the mixture (I) in a Diosna granulator with water (II) and pass the humid granules through a sieve of 1.......................... Formulation I Verapamil HCI (BASF) ...... Form pellets in a spheronizer with the rotation speed of 300-400 rpm................................175 g g g g g II Water.........

.........350 g Citric acid...........s...... Fill 2.. 3........2 g Pyridoxine hydrochloride (BASF)..................................... Manufacturing Mix the components I.... Formulation I......50 g III.. Thiamin hydrochloride (BASF) ...q..................................80 g 2...1 g of the granules in sachets.............500 g Magnesium L-aspartate ....2 g Cyanocobalamin dry powder 0............... anhydrous .......... add the mixture II.......1% (BASF) .....1 g disperse homogeneously in 100 ml of water in about 60 seconds....... DL-Carnitine hydrochloride............600 g Sodium bicarbonate (Merck)...5 g L-Glutamine .......... dry well and mix with III............5.20 g Inositol ....... BASF Pharma Ingredients Generic Drug Formulations 2001 ...................... granulate mixture I+II with the liquid III................ Isopropanol.. pass through a 0..........500 g Flavours .....4 Formulation of granules......................................... Properties of the granules Colour: Flowability: Dispersibility: Yellow granules Very good 2.................8 mm sieve............. 4..............10 g II....... dry syrups and Iyophylisates (Lab scale) Vitamin B Complex + Amino Acid + Magnesium Effervescent Granules (Sugar-free) (1 RDA of vitamins + 500 mg carnitine + 20 mg glutamine) 1.............10 g Potassium L-aspartate ...............1 g of the granules correspond to about 1 RDA of the vitamins and 500 mg of carnitine and 20 mg of glutamine............................... Kollidon VA 64 [1] . Administration 2..

.... 3...5.................................... Properties of the granules Yellow homogeneous granules dispersible in cold water......... dry syrups and Iyophylisates (Lab scale) Vitamin B Complex + Vitamin C Instant Granules (2 RDA of Vitamins) 1...... dry and pass through a 0...9 g Nicotinamide (Degussa) . Thiamine hydrochloride (BASF).... 4................8 mm sieve..... (or 10 g in 100 ml flaks as dry syrup)...1..0 g Ethanol ....0 g coated 0..0 g Kollidon 30 [1] ......17...60 ml 2..... Manufacturing Mix the components I....15.....1...2 g Riboflavin phosphate sodium ..........1% (BASF) Ascorbic acid......1.... II.......241..........4 Formulation of granules..............0 g Pyridoxine hydrochloride (BASF)...... powder (BASF) .......... Formulation I.0 g Sucrose ....5 g Cyanocobalamin.................... gelatin .......... Fill 1 g of the granules in sachets.5. BASF Pharma Ingredients Generic Drug Formulations 2001 ............................ Administration About 1 g of the granules (= 1 sachet) correspond to two daily vitamin B and vitamin C requirements of adults.... granulate with soluiton II.....................50.........

Vitamin B Complex + itamin V C Instant Granules (2 RDA of itamins) V page 2 5. Remark Due to the high loss of riboflavin phosphate sodium it should be substituted by riboflavin. Chemical stability of the granules (20–25 °C) Vitamin After production 4 Months 6 Months B1 B2 B3 B6 B 12 C 100 % 100 % 100 % 100 % 100 % 100 % 93 % 80 % 98 % 97 % 100 % 97 % 100 % 93 % 100 % 100 % 100 % 100 % 6. BASF Pharma Ingredients Generic Drug Formulations 2001 .

and there is also a restriction on the amount to be used for each dose administered in intramuscular application. Micelle formation is certainly of minor significance. B Formation of complexing compounds The soluble Kollidon products form reversible complexes with many hydrophobic active substances. and etherian oils or fragrances.6 Liquid preparations 6. The batches were of 50 –1. BASF Pharmaceutical Excipients offer several possibilities and mechanisms.000 g size. antimycotics of the miconazole type. Cremophor EL. This may be affected by the molecular weight. It is laid down in many countries that the K-value must not exceed 18. A Microemulsions Cremophor RH 40. The mechanism is probably based. There are also restrictions on the use of this auxiliary in human parenterals. In practice. on the principle of hydrophilization. BASF Pharma Ingredients Generic Drug Formulations 2001 . 6. C Hydrophilization Active substances can also be solubilized by Lutrol F 68 in addition to the Cremophor and Kollidon products. The micelle that envelops the active substance is so small that it is invisible or perhaps visible in the form of an opalescence. this effect was mostly exploited for the solubilization of antibiotics in human and veterinary medicine. and clear solutions in water are thus obtained. mouth disinfectants. e. 6.g. if it exists at all. the stronger is the solubility effect and thus the greater the solubility that can be obtained by the active substance. for the most part. Details are given in the book “Kollidon – Polyvinylpyrrolidone for the pharmaceutical industry”.3 Stabilizing suspensions Various BASF pharmaceutical excipients with different functions can be used for stabilizing suspensions.1 Size of formulations and amounts used The formulations were developed on a laboratory scale. and Solutol HS 15 act as surfaceactive solubilizers in water and form the structures of micelles.2 Solubilization of insoluble active substances In order to solubilize insoluble lypophilic or hydrophobic active substances in an aqueous medium. hexiditin. Typical fields of application are oilsoluble vitamins. The longer the chains or the higher the K-value of the Kollidon type. Solutol HS 15 is recommended for parenteral use of this solubilizing system and has been specially developed for this purpose.

6. e. Kollidon CL-M The use of Kollidon CL-M as a suspension stabilizer has nothing whatever to do with the principle of increasing the viscosity. B. Soluble Kollidon products Low concentrations. 4 Effect of Kollidon 90 F on the volume of sediment in a crospovidone suspension (7. Kollidon CL. 5 that a relative volume of sediment of normal micronized crospovidone of high bulk density (= Crospovidone M) is less and more compact that of Kollidon CL-M.). but strongly reduces the rate of sedimentation and facilitates the redispersability. an effect that is consistent with the low viscosity.g. i. 2 – 5 %. The addition of 5 – 9 % has practically no effect in changing the viscosity. of Kollidon 90 F suffice to stabilize aqueous suspensions.e. One of the reasons for this Kollidon CL-M effect is its low (bulk) density. It can be combined with all conventional suspension stabilizers (thickeners.5% in water) BASF Pharma Ingredients Generic Drug Formulations 2001 . A.1 Oral and topical suspensions The following groups of products can be offered for stabilizing oral and topical suspensions. which is only half of that of conventional crospovidone. surfactants. Relative sediment volume (24 h). which undergoes hardly any sedimentation. 4 demonstrates that it can completely prevent sedimentation. Fig. in particular. a number of formulations for made-up suspensions or extemporaneous suspensions produced from instant granules or dry syrups 100 50 0 without Povidone with 5% Kollidon 90 F Fig. The example taken was a crospovidone suspension. etc. It can clearly be seen from Fig. A combination consisting of 2 % of Kollidon 90 F and 5 – 9 % of Kollidon CL-M has proved to be an effective system for stabilizing suspensions.3. % Kollidon 30 is also used for this purpose. In this book.

4 Aromas and dyes Aromas and dyes are quoted in only exceptional cases. in the amounts used for this purpose. 5 Volume of sediment of various micronized crospovidone types (7.g. Examples are given in Chapter 3. exerts practically no influence on the viscosity. 6. BASF Pharma Ingredients Generic Drug Formulations 2001 . the preservative system i. It reduces the sedimentation rate and improves the dispersability. % 100 80 60 40 20 0 Kollidon CL-M Crospovidone M Fig. They also do not increase the viscosity when used in these amounts and can be combined with all other conventional suspension stabilizers. should be the subject of accurate research.. in concentrations of 2 – 5 %. 6. preservatives have been already integrated in the formulations.3 Dispersions for tablet coating C Lutrol F products Kollidon 25 or Kollidon 30 are particularly suitable for stabilizing pigment suspensions. Kollidon 17 PF. The polyoxamers. 6. antiacid suspensions with a pH more than 7. penicillin ampoules.3. e.Relative sediment volume after (24 h). e. They can be included in the formulations if this is wished. Lutrol F 68 and Lutrol F 127.5% in water + 5% Lutrol F 127) (see Chapter 4) illustrate the use of Kollidon CL-M.e. In difficult cases. Solutol HS 15 can also be used.2 Parenteral suspensions Kollidon 17 PF is eminently suitable for improving the wetability of the active substance in parenteral suspensions.3. expressed in terms of the final weight of the suspension.4. because they depend strongly on the taste of the target group concerned and are often specific for a particular country.5 Preservation In a few cases. bacteria-free or low-bacteria production. offer a further opportunity of stabilizing suspensions.g. 6.

and this corresponds to at least one year at room temperature.7 Chemical stability Data on the chemical stability at room temperature have been compiled almost exclusively for vitamins.8 Formulations The formulations mentioned in this chapter are arranged in alphabetical order of their active substances. 6. 6.6 Physical stability The most important parameters for the physical stability of suspensions are the relative volume of sediment (= volume of sediment/total volume) and the redispersability. BASF Pharma Ingredients Generic Drug Formulations 2001 . A stress test was almost always performed for PVP-iodine preparations.6. They are tested after 1 – 4 weeks have elapsed.

......0 g Kollidon CL-M [1] ..................6.............................................8 Liquid Formulations (Lab scale) Aciclovir Oral Suspension (2% = 200 mg/10 ml) 1............... – The substitution of citric acid by sodium citrate impairs strongly the redispersibility.... BASF Pharma Ingredients Generic Drug Formulations 2001 ....................0 g Kollidon 30 [1] .0.. Remarks – The substitution of Kollidon 30 by Kollidon 90F gives a more compact sediment........96 % Redispersibility after 14 days....easy 4............. Water........................white Relative sediment volume after 14 days ........2........ Manufacturing Suspend aciclovir and Kollidon CL-M in the solution of the other components under vigorous stirring........ Formulation Aciclovir .......................................................q.. – The deletion of citric acid gives a much more compact sediment............s..3..0 g Sorbitol [10] ...........28...................6................ 3......0 g Citric acid ..............................5 g Preservative ................................... Properties of the solution Colour ...............................60....5 g 2...........

0......2%) 1..............................1 g Preservative .................8 Liquid Formulations (Lab scale) Alpha-Bisabolol Aqueous Mouth Wash Solution (0.. Properties of the solution Clear........................q.......... BASF Pharma Ingredients Generic Drug Formulations 2001 .....0........ Formulation I... natural (BASF) ..0 g Saccharin sodium .. 3....q..92....... II........5.... Water..............6......................................................................s Cremophor RH 40 [1] .............. Alpha-Bisabolol........... colourless liquid having a low viscosity......... Manufacturing Heat mixture I to about 60 °C and add slowly the warm solution II (60 °C).......................5 g Glycerol ...........s..........2...2 g 2.2 g Flavour ...........

..6............. Chemical stability (40 °C) No loss of alpha-Bisabolol after 3 months.12 g Cremophor RH 40 [1]...............99 g 2........ II..0. Alpha-Bisabolol.1.......1%) 1...s. racemic (BASF)...00 g Butylhydroxytoluene ....q... stirr well and add slowly the warm solution II... BASF Pharma Ingredients Generic Drug Formulations 2001 ......... A clear solution is obtained..........01 g Preservative ........................ Formulation I........................ Manufacturing Heat mixture I to about 60 °C.............................8 Liquid Formulations (Lab scale) Alpha-Bisabolol Buccal or Topical Solution (0...... Water.............0.......... 3....

..... Formulation I...0 g Ethanol 96 % ....... Remark The neutralisation to pH 5 – 7 would be recommended..0 g Flavour ... natural (BASF)..10.................................. 4.....0 g Water.........................0..5 g Lutrol F 127 [1] ..5 g 2..54.......... Propylene glycol [1]......6...... Manufacturing Prepare solution I and add slowly the water.........s.............5.....................5%) 1....8 Liquid Formulations (Lab scale) Alpha-Bisabolol Mouth Wash Solution (0. II............... 3.... Properties of the solution The clear colourless solution had got the pH 8.30.q............ BASF Pharma Ingredients Generic Drug Formulations 2001 ........................ (-)Alpha-Bisabolol......................................

...............White Aspect: ...8..0................... Mix Cremophor RH 40 with simethicone.......0 g Water ............. Manufacturing I..6....... heat to about 50 °C stirring well and add the warm water... Formulation I.......99 % BASF Pharma Ingredients Generic Drug Formulations 2001 ................0 g Banana flavour ............ III................... Properties of the suspension Colour: ..8 Liquid Formulations (Lab scale) Aluminium Hydroxide + Magnesium Hydroxide + Simethicone Suspension (8% + 8% + 0........3... to adust pH 9 2.......... II..............0 g Kollidon CL-M [1] ...........10...........ad 100 ml III.....1 g Water.......... magnesium hydroxide and Kollidon CL-M..........2....................8%) 1. milky Relative sediment volume (1 day):......0 g Sorbitol............ 3... Citric acid ...................... Add emulsion I to the stirred suspension II and adjust the pH to about 9 with citric acid if needed....................8..........................................4 g Coconut flavour.................................0 g II...............0..................7 g Cremophor RH 40 [1] .....q........ s..Homogeneous...........0....7................ Aluminium hydroxide dry gel (Giulini) ................5 g Saccharin sodium ..................... Dissolve the flavours and saccharin in water and suspend aluminium hydroxide........ crystalline [10] ...... Simethicone 30 % ........8 –10..................................................................0 g Magnesium hydroxide.

....1 Kollidon CL-M [1]......4....... add the water and suspend the solid substances..9 g g g g g g 2.............. Properties of the suspension There was only a slow sedimentation during storage and the redispersibility after weeks was excellent..........6...0 Silicon oil DC 200 (Serva) ...........................5.....10..0 Magnesium hydroxide.................... 3....................8 Liquid Formulations (Lab scale) Aluminium Hydroxide + Magnesium Hydroxide Suspension (4% + 4%) 1...................76................. Manufacturing Mix Cremophor RH 40 well with the silicon oil.....4.0 Water................................... BASF Pharma Ingredients Generic Drug Formulations 2001 .0........0 Cremophor RH 40 [1] ....... Formulation Aluminium hydroxide ..........

... BASF Pharma Ingredients Generic Drug Formulations 2001 ................. Lutrol F 68 [1].... Remark The castor oil should not be heated to more than 50 °C because at higher temperature a strong thickening effect was observed... Formulation I...5 g Cloxacillin sodium....5 g 2..8 Liquid Formulations (Lab scale) Ampicillin + Cloxacillin Oily Suspension (1..1......... Antioxidant.5% + 4......3.................... 4....... Ampicillin sodium ................0 g II....... Castor oil ................ Manufacturing Heat the mixture III to 50 °C and dissolve II..................6..91...................4... s. 3.......... Properties of the suspension A homogeneous suspension was obtained.......... Add the components I and stir during cooling to room temperature........................q........0 g III...........0%) 1.......

.....34. colourless liquid....7 g Ethanol ...3 g 2............. Anise oil .. 3.........................................8 Liquid Formulations (Lab scale) Anise Oil Solution (1%) 1..........q.................. heat to about 65 °C. Manufacturing Mix the anise oil with Cremophor RH 40...63...........s........... stir strongly and add slowly the hot solution II........................................1.. Water.................. BASF Pharma Ingredients Generic Drug Formulations 2001 ....0 g Cremophor RH 40 [1] ...6...........1........................... Properties Clear or slightly opalescent... II...0 g Preservatives....... Formulation I........

........ BASF Pharma Ingredients Generic Drug Formulations 2001 ....0 g II..........................0 g Sodium citrate.0.......................... Water..6........ Properties of the suspensions Light-brown suspension showing no sedimentation during 24 hours and good redispersibility...................2..9......5 g Chocolate flavour .......8 Liquid Formulations (Lab scale) Azithromycin Suspension (5% = 500 mg/10 ml) 1..0 g Citric acid ............................ Formulations I........ Azithromycin dihydrate .......................................5...................................... Cremophor RH 40 [1] .....10.........0..............2 g Water ...... 3......... The bitter taste of Azithromycin is almost completely masked.............ad 100 ml 2.........0 g Kollidon CL-M [1] .............. Manufacturing Add the mixture I to the solution II and fill with water to a total volume of 100 ml shaking very well...................................................................5..0 g Sucrose .60..............0 g III.....

...3........8 Liquid Formulations (Lab scale) Azulene solution (1%) 1........ Manufacturing Mix azulene and Cremophor RH 40 and heat to about 60 °C.. Add slowly the water (60 °C) and cool to room temperature 3....ad 100 ml 2.. Formulation Azulene................ Properties A clear solution was obtained..................... BASF Pharma Ingredients Generic Drug Formulations 2001 ...................0 g Cremophor RH 40 [1] ...0 g Water...............................1.6......................

............ Formulation Barium sulfate . s..0 g Carboxymethylcellulose sodium ..........0 g 2............................. Properties of the suspension White homogeneous suspension having a viscosity of about 160 mPa · s.......0..........5 g Preservatives....100.......0 g Kollidon 90 F [1] ..............5................... In the obtained clear solution suspend barium sulfate.......4 g Sodium bisulfite....... 3........8 Liquid Formulations (Lab scale) Barium Sulfate Oral Suspension (23%) 1.........................6... Water ........< 0....320..... BASF Pharma Ingredients Generic Drug Formulations 2001 ....................q........................... Manufacturing Dissolve the preservatives and the carboxy methylcellulose sodium in the hot water and add Kollidon 90 F and sodium bisulfite............

.....6.... colourless liquid...........22 Ethanol 96 % .27 g g g g 2...10 Cremophor RH 40 [1] .............41 Water ......................... stir strongly and add slowly the water.. Benzyl benzoate ..............................8 Liquid Formulations (Lab scale) Benzyl Benzoate Solution (10%) 1............ 3........ Manufacturing Heat the mixture of benzyl benzoate and Cremophor RH 40 to about 60 °C............................... Properties of the solution Clear.... BASF Pharma Ingredients Generic Drug Formulations 2001 ................. Finally add the ethanol.......... Formulation I.......

.......0..0 g Dihydrostreptomycin sulfate ... Properties A white homogeneous suspension was obtained.. add the components I to the well stirred solution II and pass through a colloid mill......5 g Sodium citrate..... 3........0. Water for injectables ..........................................8 Liquid Formulations (Lab scale) Benzylpenicilline + Dihydrostreptomycin Injectable Suspension (200.... 4......................20..000 units + 200 mg/ml) 1...s......0 g Kollidon 12 PF [1] ................ Manufacturing Prepare solution II...5 g Carboxymethyl cellulose sodium .... II................. Remark To prevent of discolouration of Kollidon in the solution during storage 0. Formulation I.ad 100 ml 2.... Procain benzylpenicilline ..6 g Parabene .. BASF Pharma Ingredients Generic Drug Formulations 2001 ..........2 to 0.................20.5 % of cysteine could be added as antioxidant..............q..................6.............0..

.......41..................... no crystals Very low BASF Pharma Ingredients Generic Drug Formulations 2001 . Dissolve sorbitol in this mixture and add Kollidon CL-M to the well stirred suspension to obtain a homogeneous suspension..........Not needed Structure of the sediment ................. Manufacturing Stirr the mixture of carbamazepine and propylene glycol at least during 2 hours...............0 1....... ....................no crystals Viscosity ...........3....20....................1 Sodium citrate........ crystalline .0 Kollidon 90F [1] ............7. saccharine...........6..2-Propylene glycol [1] ..................0....................................Very fine particles....... 3...8 Liquid Formulations (Lab scale) Carbamazepine Oral Suspension (2% = 100 mg/5 ml) 1..............0 Water...................... sodium citrate and the water and stirr again until these components are dissolved..........Very low Milky white 98 % Very easy Very fine particles............... Properties of the suspension After 1 day After 1 month (RT) Colour:............................................1........... add Kollidon 90F......................Milky white Relative sedimentation volume .....................................9 g g g g g g g g 2.....0 Sorbitol.........25........2........0 Saccharine sodium ..............100 % Redispersibility ...................................0 Kollidon CL-M [1]. Formulation Carbamazepine (Flavine) ...........................

... Properties of the solution Clear.........0% + 0...................... Carnitine .....4 g II.95.4...............0..0.......................0 g 2. 4..................8 Liquid Formulations (Lab scale) Carnitine + Coenzym Q Solution (4.........6..... Physical stability (6–8 °C) No change of clarity after one month.........1 g Cremophor RH 40 [1] ......... Water....... 3...... Cool and dissolve III.......1 g Lutrol E 400 [1]..4 g III.. BASF Pharma Ingredients Generic Drug Formulations 2001 ............q.................... colourless liquid.1%) 1...................... Preservative ......s.................................. Formulation I........................ Manufacturing Heat the mixture I to 60 °C.... stir well and add solution II (60 °C).... Coenzym Q 10 .0...

.........................0 g Preservative ..............6... cool.....0 g 2...q.. add chloramphenicol and stir until a clear solution is obtained..... 4..............8 Liquid Formulations (Lab scale) Chloramphenicol Ophthalmic Solution (3%) 1.......0 g Kollidon 25 [1] ............s........15..2 to 0.........add 100....... Remark To prevent of discolouration of Kollidon in the solution during storage 0........................ BASF Pharma Ingredients Generic Drug Formulations 2001 ......... Properties Clear colourless solution having a low viscosity............. dissolve Kollidon 25...5 % of cysteine could be added as antioxidant... Water .3. Formulation Chloramphenicol .......... 3..... Manufacturing Dissolve the preservative in hot water...

..... Manufacturing Mix components I at 70°C to obtain a clear solution..............................5 g Lutrol E 400 [1].........................5% = 250 mg/10 ml) 1...0 g Cremophor RH 40 [1] .................8 Liquid Formulations (Lab scale) Chloramphenicol Palmitate Oral or Topical Emulsion (2..... Formulation I.ad 100 ml 2...............40...... homogeneous emulsion without foam formation..0 g III..4.4... Chloramphenicol palmitate..... Water.....0 g II............ 3..............0 g Water.... crystalline ......6......................... Fill up with III to 100 ml............. Properties White.2..........40.... Cool to 40 °C and add this solution slowly to the well stirred solution II................ BASF Pharma Ingredients Generic Drug Formulations 2001 ........ Sucrose...........

............45 g 2........... crystalline ............. 3.q.. Properties White.................................... II........ Physical Stability After 3 weeks at room temperature and at 45 °C no change of appearance and viscosity was observed.................................4 g Sucrose......8 Liquid Formulations (Lab scale) Chloramphenicol Palmitate Oral or Topical Emulsion (5......6............5 g Lutrol E400 [1] ......6 g Cremophor RH 40 [1] ... Manufacturing Mix components I at 70°C to obtain a clear solution and cool to about 40 °C...... Chloramphenicol palmitate............ milky emulsion 4.... Add the warm solution II slowly to the well stirred solution I........... BASF Pharma Ingredients Generic Drug Formulations 2001 ..0% = 500 mg/10 ml) 1... Water..40 g Preservative .......s.................................... Formulation I...........................

.........04 Water for injectables ...........0.....0 Sodium hydroxide...g...9.. Closantel .... Properies of the solution Clear yellow solution 4.... II..........ca...........01 – 0...0 – 20... Remarks The function of Kollidon 12 PF or Kollidon 17 PF is to reduce strongly the local side effects (e...... BASF Pharma Ingredients Generic Drug Formulations 2001 ......0 Kollidon 12 PF or Kollidon 17 PF [1] .... The sterilisation can be done by heating (120 °C. formation of oedemas) and to increase the retention time in the tissue..2.... Sodium bisulfite . Formulation I........ 50 % in water .12... 20 g g g g g g 2.....0 –12...6......5 – 3.0 Propylene glycol [1] . Manufacturing Dissolve Closantel in solution II and add solution III...ca.................. 20 min) 3.............. 60 III..8 Liquid Formulations (Lab scale) Closantel Veterinary Injectable Solution (12–20 g/100 ml) 1.

II..8 Liquid Formulations (Lab scale) Clotrimazole Topical Solution (3%) 1........30.6....3............. Manufacturing Dissolve Clotrimazole in Cremophor RH 40 at about 60 °C............... BASF Pharma Ingredients Generic Drug Formulations 2001 ............. s.............. colourless.............................. 3..... Clotrimazole ............ stir strongly and add slowly the hot solution II.........0 g Cremophor RH 40 ......................... Properties Clear.....q..........34 g Water.. viscous liquid..........0 g Preservative .. Formulation I.............................33 g 2..... Ethanol 96 % ............................

...... Kollidon 90F........0 g Sorbitol.... add Kollidon CL-M and homogenize by shaking. Formulation Kollidon CL-M [1]......q...................... milky suspension showing no sedimentation during 24 hours............................. Manufacturing Dissolve sorbitol.0 g Preservatives................. 3.. Physical stability after 4 weeks at oom r temperatur e Sediment volume: Redispersibility: 98 % Very easy... Properties of the suspensions White..............q.. Water........s......10..................................8 Liquid Formulations (Lab scale) Crospovidone Oral Suspension (2000 mg/10 ml) 1......2..................... crystalline [10] ........s..6.ad 100 ml 2...........20...... 4.................... BASF Pharma Ingredients Generic Drug Formulations 2001 ..... the preservatives and the flavours in the water......... Flavour ..............0 g Kollidon 90F [1] .....

.... Properties of the solution A clear colourless solution of very low viscosity was obtained...................... 2.......5 mg/ml) 1............ 3. stirr well and add very slowly the hot solution II...6..............q..... Formulation I..4.......4.............................................00 g Water for injectables . BASF Pharma Ingredients Generic Drug Formulations 2001 ............................ad 100 ml Preservative ................8 Liquid Formulations (Lab scale) Diazepam Injectable Solution (2.........s... Diazepam.. II.0.........00 g Lecithin .............................25 g Solutol HS 15 [1] . Manufacturing Heat mixture I to 60 – 70 °C.

................................................6.2 µm)........ add diclofenac sodium and stir until a clear solution is obtained........... Formulation Diclofenac sodium ...12.0 g Kollidon 17 PF [1] ...... benzyl alcohol and water. The sterilisation could be made by aseptic filtration (0..........5 g Propylene glycol [1] ..... Manufacturing Dissolve Kollidon 17 PF in the mixture of propylene glycol.......5.50...................8 Liquid Formulations (Lab scale) Diclofenac Injectable Solution (75 mg/3 ml) 1..0 g Water for injectables...................7.........to 300 ml 2..........0 g Benzyl alcohol .............. BASF Pharma Ingredients Generic Drug Formulations 2001 ..........

..........– Sucrose....................40.......... 3.. Manufacturing Dissolve diclofenac sodium in the aqueous solution of the auxiliaries. Physical stability There was no crystallisation after the storage of 2 weeks at 6 °C...........................5%) 1.... 2 1.5 g Kollidon 30 [1]............... 1 Diclofenac sodium..........5 0............. crystalline .........6.......................................2.....5 g Cremophor RH 40 [1] ..5 g g g g g 2... Formulations No....0 g Water ............................0 g No...8 Liquid Formulations (Lab scale) Diclofenac Oral Solution (1..............5 40....56.. BASF Pharma Ingredients Generic Drug Formulations 2001 ...5 1.......0 56..1......

............................0 g Cremophor RH 40 [1] ....... II................4.... Properties of the solution Clear or slightly opalescent.0 g Preservative ....8 Liquid Formulations (Lab scale) Eucalyptol Solution (8%) 1.. Eucalyptol .........q.........................8..... Formulation I. stir well and add slowly the warm solution II........ 3................ BASF Pharma Ingredients Generic Drug Formulations 2001 . Manufacturing Mix eucalyptol and Cremophor at 65 °C.ad 100 ml 2...s............................... Water............. colourless liquid.......6.......

4.0 Camphora............. Properties of the solution Clear or slightly opalescent liquid....................0 Ethanol 96 % .................................................... Add the ethanol and slowly the warm water to the well stirred solution. Manufacturing Mix the active ingredients with Cremophor RH 40 and heat to 50 – 60 °C.........7 g g g g g 2.........6.....................40..... BASF Pharma Ingredients Generic Drug Formulations 2001 ...45.......................3.........................0 Cremophor RH 40 [1] ..... Formulation Fir needle oil (Frey & Lau) ...... 3. Remark The needed amount of Cremophor RH 40 depends on the type of fir needle oil....8 Liquid Formulations (Lab scale) Fir Needle Oil Solution (3%) 1........3 Water....6...5..

.................5..6...........2 to 0.. Remark To prevent of discolouration of Kollidon in the solution during storage 0.00 g Tartaric acid .........8 Liquid Formulations (Lab scale) Furaltadone Injectable Solution (50 mg/ml) 1.... Formulation Furaltadone.... Manufacturing Dissolve the solid substances in water at about 50 °C..... 20 min)............25 g Kollidon 12 PF [1] ...00 g Water of injectables ............... The sterilisation can be made by aseptic filtration or by heating (120 °C..............................5 % of cysteine could be added as antioxidant.... BASF Pharma Ingredients Generic Drug Formulations 2001 ............ad 100 ml 2.1.............25. 3...............

.........8 Liquid Formulations (Lab scale) Gramicidin Ophthalmic Solution (1...... Formulation I.................. Manufacturing Mix gramicidin and Cremophor RH 40...................13 mg Cremophor RH 40 [1].............0......... Gramicidin.. Water................................1 g Ethanol 96 % .8 g 2...3 mg/10 ml) 1..6.... heat to about 65 °C.............................. BASF Pharma Ingredients Generic Drug Formulations 2001 .................0 g Preservatives.......q...... stir and add slowly the heat solution II......... s........... II..........1... Properties Clear solution.... 3.98.....................

...........................6.. Physical stability The solution remained clear more than one week at 6 °C..............................20 g Preservatives............... II.................2 g Cremophor RH 40 [1] ........ Water.... BASF Pharma Ingredients Generic Drug Formulations 2001 ....q.78 g 2........... s.... Ibuprofen (BASF) ............. 3.... Formulation I..........8 Liquid Formulations (Lab scale) Ibuprofen Solution (2%) 1..................... Manufacturing Suspend Ibuprofen in the hot Cremophor RH 40 (about 60 °C) and add slowly the hot solution II..............

...... sediment volume ..................low Rel..................... sediment volume ..............8 Liquid Formulations (Lab scale) Ibuprofen Suspension (4% = 400 mg/10 ml).......................100 % (after 1 day) Rel............... Manufacturing Dissolve sucrose............ Suspension pr operties Color .....8 g Kollidon 90 F [1] .........................very easy (after 4 weeks) BASF Pharma Ingredients Generic Drug Formulations 2001 ...............................................................................................................................ad 100 ml 2............ I 1.......................................................... suspend Kollidon CL-M and ibuprofen in this solution by stirring and add the rest of water................ Kollidon 90 F and sodium citrate in about 40 ml of water....25 g Kollidon CL-M [1] .................white Aspect ................ 3............................................................... Formulation Ibuprofen (BASF) ....Homogeneous Viscosity.................2 g Water................2 g Sodium citrate....................4 g Sucrose .94 % (after 4 weeks) Redispersibility.....6........

I page 2 Relative sediment volume.Ibuprofen Suspension (4% = 400 mg/10 ml). 4 weeks [%] 4. Influence of the amount of Kollidon CL-M on the sedimentation 100 90 80 70 60 50 40 30 20 10 0 2 4 6 Kollidon CL-M [%] BASF Pharma Ingredients Generic Drug Formulations 2001 8 10 .

............. II 1.................6........4..10.............................0 g Lutrol F 68 [1]........s...0 g Preservative ...................5.... BASF Pharma Ingredients Generic Drug Formulations 2001 .............................8 Liquid Formulations (Lab scale) Ibuprofen Suspension (4% = 400 mg/10 ml)..... Water.... II... Manufacturing Dissolve Lutrol F 68 and the preservative in water II and ibuprofene in Cremophor RH 40 (I). The viscosity is low........ Add the solution II slowly to the ibuprofeneCremophor RH 40 mixture I whilst stirring........0 g Cremophor RH 40 [1] ............................. Formulation I..... 3...81 g 2....... Properties of the suspension The redispersibility of the suspension is very easy after 14 days at room temperature..... Ibuprofen (BASF) .............q........

.. Manufacturing Dissolve or suspend all the solids in water under aseptic conditions..........................0 g Coconut flavour .....................................0.........s.................... 3..................05 g Banana flavour .8....................15...8 Liquid Formulations (Lab scale) Magaldrate Suspension (10%) 1..........................0 g Orange flavour ....ad 100 ml 2.............10.. – Very easy to redisperse by shaking after the storage of more than 2 weeks.1.......0 g Kollidon 90 F [1].0...............6..................02 g Preservatives..........2............................... BASF Pharma Ingredients Generic Drug Formulations 2001 ................ Properties of the suspension – White homogeneous suspension practically without sedimentation during 24 hours.......0 g Kollidon CL-M [1] ...................0..08 g Saccharine sodium .............q.................0 – 3............... Water....................... Formulation Magaldrate USP .... – pH about 9.0 g Sucrose ...................................

Magaldrate Suspension (10%) page 2 Number of shakings needed to homogenize 4. Influence of the Kollidon 90 F concentration on the edispersibility r after 7 days 25 20 15 10 5 0 0 2 1 Kollidon 90 F [%] BASF Pharma Ingredients Generic Drug Formulations 2001 3 .

............................... Formulation Mebendazole .....8 Liquid Formulations (Lab scale) Mebendazole Suspension (2% = 200 mg/10 ml) 1.................................3 Methylparaben........... After cooling to room temperature add Lutrol F 127 whilst stirring........................................... After some weeks of storage at room temperature some sedimentation occurred but the redispersibility was very easy.ad 100 g g g g g 2.......................0...18 Propylparaben..........................6............... When the Lutrol F 127 is completely dissolved suspend Mebendazole in the solution....2 Lutrol F 127 [1]......02 Water ............0.. 3... BASF Pharma Ingredients Generic Drug Formulations 2001 ... Properties of the suspension After one day of storage at room temperature no sedimentation could be observed....... Manufacturing Dissolve the parabens in water at 80 °C...

...0 g Kollidon 12 PF [1] ........... It can be diluted with water without precipitation............ Manufacturing Suspend I in the solution II.0 g Lutrol E 400 [1]....20...... 3..........s.........0 g Water for injectables ......4 with III and heat until metronidazol is dissolved..............25...6. Hydrochloric acid 0............... BASF Pharma Ingredients Generic Drug Formulations 2001 .. 4................0 g Propylene glycol [1] ... Remark To prevent of discolouration of Kollidon in the solution during storage 0.1 N ....25........ 2...0 g III.............2 to 0.q........... adjust pH 4...................25.................8 Liquid Formulations (Lab scale) Metronidazole Injectable Solution (500 mg/10 ml) 1.......5 % of cysteine could be added as antioxidant. Formulation I..... Metronidazole .... II....5........... Properties of the solution A clear solution was obtained.........

. BASF Pharma Ingredients Generic Drug Formulations 2001 ....... 3...........6........ while they are still hot.......1.q. stir well and add slowly the hot solution II........... to eliminate any separation of the phases that may have occurred...... they should be shaken for a short time.......................... II....s..0 g Cremophor EL [1] ...... After the ampoules have been heat-sterilized... Manufacturing Heat mixture I to about 65 °C......... Formulation I. Sterilization can also be performed by membrane filtration under pressure.........ad 100 ml 2..12...... Miconazole ..........8 Liquid Formulations (Lab scale) Miconazole Injectable Solution (1%) 1....0 g Parabenes ...... Water for injectables ................ Properties of the solution Clear colourless liquid having a low viscosity..................

..0 g 1................... Formulations I..................8 Liquid Formulations (Lab scale) Mint Mouth Wash Solutions 1.. Water .0 g Salicylic acid .....0...02 g 5............. 3..................................0.............0 g 0..........10 g Sorbitol....50 g Sodium fluoride................ 2 Mint oil ...............21.........................................................45 g Sodium citrate..................5..... Prepare solution II..............0 g – – – 6.................0..– Glycerol ..0 g – 4.. II.....20 g 0.....0...4 g – 1.............6 g Sicovit colorant [1]..... heat to about 60 °C and add it slowly to the well stirred mixture I..................06 g Cremophor RH 40 [1] ..........0 g Menthol ................– Thymian oil .................1 g 2................................ Properties of the solutions Clear............ s............... crystalline [10] .................................. Manufacturing Mix the components I and heat to about 60 °C........0...48........... 80......2....................................................................q.... coloured liquids having a fresh mint taste......................... No...0... s.....................0................20 g Citric acid .....................0.......06 g Benzoic acid .5 g Ethanol 96 % ...................... 1 No........................7 g q....17............. BASF Pharma Ingredients Generic Drug Formulations 2001 ...............4.............0 g 5.......................– Lutrol F 127 [1]...........50 g 0..................0 g Saccharin sodium....................6..........0 g 1...........09 g alpha-Bisabolol (BASF) .................04 g Eucalyptus oil.........45 g 0..............................

............52...8 Liquid Formulations (Lab scale) Mint Oil Solution (3....5 Cremophor RH 40 [1] .............. stir well and add slowly ethanol and water.............. BASF Pharma Ingredients Generic Drug Formulations 2001 .30..................7 g g g g 2. Manufacturing Mix the peppermint oil with Cremophor RH 40...........8 Ethanol 96 % ........3..6.........................0 Water..... colourless liquid of low viscosity. 3.............. Formulation Peppermint oil .................13... Properties of solution Clear.........5%) 1...................

.............25....45.0 g Total amount ................10.......0 – 4.............80...................... Water ....15.......................0 mg Riboflavin 5’-phosphate sodium..........................05 mg Vitamin E acetate (BASF) .0 mg Butylhydroxytoluene ..............9...............................0................................... Saccharose .......6 g Calcium gluconate ....15.....0 g III................... Formulation I.....................4................... Manufacturing Heat I and II separately to about 60 °C and mix slowly well stirring to obtain a clear solution.....2..... Glycerol ..... Vitamin A palmitate ............ crystalline (BASF).................0 mg IV. III/IV and V and adjust the pH value to 4....6.........5..1..........................15...... Dissolve III in the hot solution IV to obtain a clear solution....../g........................................100.........................200.8 Liquid Formulations (Lab scale) Multivitamin + Calcium Syrup (1 RDA of Vitamins/20 ml) 1......100...... Pass during 10 min nitrogen through the solution and fill in flasks under nitrogen.. i..........10.0 g Methyl parabene ....................... Mix the cool solutions I/II..0 g V.....0 mg Nicotinamide ..55..../g (BASF) Vitamin D 40 Mio................... i.....7 Mio........0 mg Propylene glycol Pharma [1] .......0 mg 1.......... u..0 mg Pyridoxine hydrochloride (BASF) .........100 g 2.70 mg Water..........5 g II........ Thiamine hydrochloride (BASF) .........300....................0 mg Ascorbic acid..0 mg Sorbic acid ..................0 mg Citric acid.............0 mg Cremophor RH 40 [1] ................u.... BASF Pharma Ingredients Generic Drug Formulations 2001 ......

HPLC thods) me The following stability data were obtained with the same syrup but without calcium gluconate: Vitamin Vitamin Vitamin Vitamin A B1 B2 C BASF Pharma Ingredients Generic Drug Formulations 2001 (9 months) (12 months) 86 % 88 % 96 % 78 % 73 % 83 % 92 % 77 % .Multivitamin + Calcium Syrup (1 RDA of itamins/20 V ml) page 2 3. Chemical stability (20–25 °C.

.....1...6....5 Mio...........1 g Thiamine hydrochloride. Prepare solution III and add to the cool mixture I/II.............0...0 g q.........1 g Butylhydroxytoluene ...........8 Liquid Formulations (Lab scale) Multivitamin Injectables for Veterinary Application 1...........10 mg Water .................0. ad 90 ml 1....6....................0 g Solutol HS 15 [1] ...5 g 1....................... i....... 1 Emulsion No....................27 mg 40 Mio.......100 ml 100 ml I...s.........1 g 0..........1.................2..........................s..0.... i..6 g 0..4....../g Vitamin E acetate (BASF) ............0................... BASF Pharma Ingredients Generic Drug Formulations 2001 ....................ad 90 ml III.................5 g Dexpanthenol..5 g 2................0 g II................../g (BASF) Vitamin D 3 (Cholecaciferol) .................. 27 mg 2...............................................ad 10 ml 4. stir well and add very slowly the hot solution II...................0..... u........................................ Water for injectables .....5 g 2........... Nicotinamide ................. 2 Solution Vitamin A propionate ..1 g 0...6 g 10 mg ad 10 ml Total amount......6 g Riboflavin phosphate sodium ............................................. Formulations No.......................... u.....0 g 22..............1 g 0....5 g 0..5 g Benzyl alcohol.................................6 g EDTA sodium . Preservative ..... Manufacturing Heat mixture I to about 65 °C....q.......1 g Pyridoxine hydrochloride......

Solution (formulation No. BASF Pharma Ingredients Generic Drug Formulations 2001 .5.1. 2) A clear yellow solution was obtained having a viscosity of about 7 mPa · s and a pH of 4. 1) A yellow milky emulsion was obtained having a viscosity below 5 mPa · s and a pH of 4.Multivitamin Injectables foreterinary V Application page 2 3. Properties Emulsion (formulation No.

........ III/IV and V and adjust the pH value to 4....0 mg Cremophor RH 40 [1] ..0 g III.... Manufacturing Heat I and II separately to about 60 °C and mix slowly well stirring to obtain a clear solution....25..................0 mg Riboflavin 5’-phosphate sodium.15........5 g II..0 mg Sorbic acid ............. BASF Pharma Ingredients Generic Drug Formulations 2001 ......300...100....................................0 mg Pyridoxine hydrochloride (BASF) ..... Water .........0 mg Citric acid....u..............4.................. Vitamin A palmitate ...............................45......... Mix the cool solutions I/II.0 g Total amount ............ Glycerol ............................. crystalline (BASF).......................................................0 mg IV..15........... Formulation I...........2.....................6 g Water.. Pass during 10 min nitrogen through the solution and fill in flasks under nitrogen......05 mg Vitamin E acetate (BASF) ......6......100................. Dissolve III in the hot solution IV to obtain a clear solution................0 mg Nicotinamide .........55...................2.0 mg Ascorbic acid.... I (1–2 RDA/20 ml) 1....... u........... Vitamin D 40 Mio......................0 mg Propylene glycol [1] ...80...............................................7 Mio..............10.......0 g Methyl parabene ....15........0 mg Butylhydroxytoluene ..........0 g V...... i../g (BASF) ..9...100 g 2..............0 – 4.......5..200..........8 Liquid Formulations (Lab scale) Multivitamin Syrup...............0......./g.........10...................... Thiamine hydrochloride (BASF) ...0 mg 1.. Saccharose ..................... i.........

Chemical stability (20–25 °C. I (1–2 RDA/20 ml) page 2 3.Multivitamin Syrup. HPLC thods) me Vitamin Vitamin Vitamin Vitamin A B1 B2 C BASF Pharma Ingredients Generic Drug Formulations 2001 (9 months) (12 months) 86 % 88 % 96 % 78 % 73 % 83 % 92 % 77 % .

............3. Mix with solution III and add the syrup IV...... yellow viscous liquid.....17..............0..0.......... II 1. Manufacturing Heat mixture I to about 65 °C...........5 g IV................00 g III.. 4. Sugar syrup USP........... stir well and add very slowly the warm solution II (65 °C)......00 g II..............ad 100 ml 2.0...............................................02 g Ascorbic acid...............u...........0. crystalline (BASF) ...........1 mg Butylhydroxytoluene ....................... Vitamin A palmitate ....../g (BASF) Vitamin D 3 40 Mio i.......0 mg 1........ BASF Pharma Ingredients Generic Drug Formulations 2001 ........10 g Water ............17...... Thiamine hydrochloride (BASF) ................7 Mio i....................0...............0 mg Cremophor RH 40 [1].......0.... Parabenes ....8 Liquid Formulations (Lab scale) Multivitamin Syrup....05 g Riboflavin phosphate sodium .../g ............ Physical stability (20–25 °Cotected pr from light) No change of the appearance after 3 months.25 g Water .... Properties of the syrup Clear.. 3...........02 g Pyridoxine hydrochloride (BASF) .... Formulation I..6....... u.....1....

...... 0.... add slowly the water of the same temperature and mix with solution III.300 mg Folic acid ...............18 mg Citric acid...... solution 1 molar ....... The pH-value is about 4./g..... keep it during 5 min under nitrogen bubbles.30...................... pass nitrogen through the solution and fill in ampules under nitrogen............../g (BASF) Vitamin E acetate (BASF).......... Water.................6..6 mg Butylhydroxyanisol ............................... Vitamin A palmitate ..................4...9......40 mg 1....6 ml 2..............2 g Dexpanthenol (BASF) ........44 mg II........u......... Adjust the pH to about 7.....1 molar .........8 mg Propylene glycol [1] ................. Parabenes . Formulations Chamber 1: I.. BASF Pharma Ingredients Generic Drug Formulations 2001 ......4 ml Hydrochloric acid...0 ml Chamber 2: I..............2.... filter through a 0............110 mg Riboflavin phosphate sodium.............................0 ml Water for injectables ..................................................................................................................70.0 g II................4 mg Solutol HS 15 [1] ... i... i..7 Mio.......2...8 Liquid Formulations (Lab scale) Multivitamin Two Chamber Ampules 1....0..................1.66 mg Nicotinamide ........... Chamber 2: Dissolve the mixture I in the buffer solution II........2 mg Butylhydroxytoluene ....... Manufacturing Chamber 1: Heat mixture I to 60 °C.....0....0 g Lutrol E 400 [1].................. Thiamine hydrochloride (BASF) ..440 mg Pyridoxine hydrochloride (BASF) ........2...........................................2..........8.....200 mg Vitamin D 2 40 Mio...........u............ Sterilize at 120 °C during 10 min...........0 g III...................2 µm membrane and fill in ampules under nitrogen.... Sodium ascorbate crystalline .........252 mg Sodium hydroxide.....

.........................Multivitamin w T o Chamber Ampules page 2 3.................................................................................................. Chemical stability (V itamin contents after 12 months at 20–25 °C.......90 % Nicotinamide:.....................................75 % Dexpanthenol: .......... HPLC) Vitamin A: ....................100 % Vitamin B 6 :.......................97 % Vitamin C: ...not determined Folic acid:.............91% Vitamin B 1 :.............94 % BASF Pharma Ingredients Generic Drug Formulations 2001 .....................................93 % Vitamin B 2 :........................................................................

.......0 g g g g g g 2.................... add the sorbitol............1 to 0... Manufacturing Dissolve the parabenes in the hot water............8 Liquid Formulations (Lab scale) Norephedrine Syrup (40 mg/10 g) 1................. 3...... Properties of the syrup Appearance ............... BASF Pharma Ingredients Generic Drug Formulations 2001 ..1 Saccharin sodium...........................................46............0............................. Remarks To prevent of discolouration of Kollidon in the solution during storage 0................5 Kollidon 90 F [1] ......5 % of cysteine could be added as antioxidant.................clear solution Taste .................. Merck) Water...... Formulation DL-Norephedrine hydrochloride..0.....0......................4 Parabenes (Nipa) .............reasonable 4.........50.. Flavours should be added to adjust the required taste... cool to room temperature and dissolve the other components..6.....3.0 (Karion ® F liquid....0 Sorbitol solution ............

..............................8 Liquid Formulations (Lab scale) Nystatin Suspension (100.............64. Properties of the suspension Colour ........... Kollidon 90 F is added slowly in small portions under vigorous stirring.....0..6............................25 Kollidon CL-M [1].......2................000 i...............................80 Citric acid ..../ml) 1...70 g g g g g g 2..........24.....easy BASF Pharma Ingredients Generic Drug Formulations 2001 ....50 Water ........................ Formulation Nystatin ....................... Kollidon CL-M......................................................not observed after one week Redispersibility ... 3..5.........2.........75 Kollidon 90 F [1] ...... Manufacturing Nystatin...................... sorbitol and citric acid are suspended in water...................60 mPa · s Sedimentation .u........yellow Viscosity (25 °C) .......................................................00 Sorbitol [10].....

............... Magnesium oxide .......... Ethanolamine ..6. Rongalite ® C.......5........0 g Reducing agent .... The function of Kollidon 17 PF not only is the solubilisation of oxytetracycline but also the reduction of its local toxicity.. Formulation I.... pass continously nitrogen through the solution to avoid oxidation and add slowly I to the well stirred solution. 3..0.............. Remarks The absence of oxygen during manufacturing and in the final packaging and a good quality of oxytetracycline HCl are essential to avoid the oxidation (= dark solution).... Veterinary Application (500 mg/10 ml) 1.8 2......8 Liquid Formulations (Lab scale) Oxytetracycline Injectable Solution for i............. BASF) Water for injectables .. m.................. Properties of the solution Yellow clear solution...5 g (e.46 g IV....... 4..to adjust pH 8............. Manufacturing Suspend III in solution II....0. II..... The reducing agent must be selected in accordance with the legislation of the corresponding country.... BASF Pharma Ingredients Generic Drug Formulations 2001 .....7 g Kollidon 17 PF [1] .ad 100 ml III.....10..... + i.... Adjust the pH with IV......................... Oxytetracycline hydrochloride ..g.. v........

.......6...............3.................2 g / 10 ml) (According to US-Patent 4... Manufacturing Mix the water and the Soluphor P..........................5 with aminoethanol..00 g Kollidon 17 PF [1] ..00 g Sodium formaldehyde sulfoxylate .. After the solution has cooled.1..8 Liquid Formulations (Lab scale) Oxytetracycline Sustained Release Injectable for i.................44 g 2-Aminoethanol ......... Formulation Oxytetracycline.92 g Soluphor P [1] ..s.. and dissolve the Kollidon 17 PF in the mixture. ad 100......018.... Heat the solution to 75 °C............... sodium formaldehyde sulfoxylate (Rongalite‚ C...........5........... m...........00 ml 2.. The reducing agent e.g.......40.. After the magnesium oxide has been suspended..84 g Water of injectables.... BASF) must be selected in accordance with the legislation of the corresponding country.65 g Magnesium oxide .q..... set to pH 8.... Veterinary Application (2.. 3.889 (1976) 1. BASF Pharma Ingredients Generic Drug Formulations 2001 ............ Remarks The quality of the oxytetracycline and the complete absence of oxygen during the manufacturing and packaging of the solution is essential to obtain a acceptable chemical stability and no dark colour. Add the sodium formaldehyde sulfoxylate and stir until dissolved................0....... slowly stir in the oxytetracycline until a clear solution is obtained...22.....

........0 Water..0 Orange flavour.................. sodium citrate.......0...5............0... powder ................ 3.............58.....5. Formulation Paracetamol.....0 Citric acid.................. A white.. Kollidon CL-M and paracetamol.........0.......... Manufacturing Prepare the solution of dextrose in water and add the other solid ingredients with stirring in the following sequence: citric acid.. stable suspension showing almost no sedimentation during 24 hours and good redispersibility (easily to homogenize by shaking twice to 3 times).......1 Dextrose .. Properties of the suspension Practically tasteless..... powder ..30.............. BASF Pharma Ingredients Generic Drug Formulations 2001 .............. homogeneous suspension is obtained.....8 Liquid Formulations (Lab scale) Paracetamol (= Acetaminophen) Suspension (5% = 500 mg/10 ml) 1........5 Sodium citrate...........5 Kollidon CL-M [1] ........................................................................9 g g g g g g g 2.........6.......... orange flavour.................

............ To prevent of discolouration during storage 0.................. Chemical stability (HPLC) No loss of paracetamol was found during 3 months at 40 °C......... 4..............20....0 Cyclamate sodium .................... 3.20..... Properties of the syrup Clear solution of certain viscosity having only a slightly bitter taste.............. 5....5....0 Strawberry flavour . Physical stability The solution remained clear during more than 1 week at 6 °C and during more than 3 months at 25 °C and 40 °C........0 Sorbitol. crystalline [10]...... BASF Pharma Ingredients Generic Drug Formulations 2001 ...............................0 Glycerol ................5 % of cysteine could be added as antioxidant...................0 g g g g g g g g 2.0 Water.1 Kollidon 25 [1] ...5................4...............0. Manufacturing Dissolve first Kollidon 25 and then the other solid components in the solvent mixture of glycerol....................... propylene glycol and water.......0 1...6.....................8 Liquid Formulations (Lab scale) Paracetamol (= Acetaminophen) Syrup (5% = 500 mg/10 g) 1..15...2 to 0.. Formulation Paracetamol (BASF) ............. The colour of the solution changed only a little during 3 months at 25 °C and 40 °C.31.......................2-Propylene glycol [1] ......

.................6..0........ heat to 50 °C and stir to obtain a clear solution.0 Glycerol .................5 g g g g g g g 2... Dissolve the flavours and mix with glycerol.....................5 Kollidon 25 or Kollidon 30 [1] .....30.8 Liquid Formulations (Lab scale) Paracetamol (= Acetaminophen) Syrup for Children (2.... Manufacturing Dissolve Kollidon in water........................ clear sweet and only slightly bitter liquid......... crystalline (BASF) ........< 0................2........ BASF Pharma Ingredients Generic Drug Formulations 2001 ..................0 Sodium cyclamate ...4........ 3.6........57......................................... Properties of the syrup The obtained syrup is a viscous......... Formulation Paracetamol.. add paracetamol and cyclamate......2 Water ....1 Raspberry flavour .....................0 Orange flavour...5% = 250 mg/10 ml) 1...

............8 Liquid Formulations (Lab scale) Phenytoin Oral Suspension (5%) 1......................................................................... Formulation Phenytoin ................6............................. Content uniformity of phenytoin in the suspension mg Phenytoin/ml after 1 h after 24 h 60 50 40 30 20 10 0 low area medium area Fractions of the suspension BASF Pharma Ingredients Generic Drug Formulations 2001 high area .....s...................... 3....... Water.q.. Manufacturing Dissolve the preservative and Kollidon 90 F in water and suspend Kollidon CL-M and phenytoin.......................5 g Kollidon CL-M [1] .....1 g Preservative .....................86 g 2................8 g Kollidon 90 F [1] ............

1 Kollidon VA 64 [1] ......................... II...........5%) 1...................10 Lutrol E 400 [1] ...8 Liquid Formulations (Lab scale) Polidocanol Wound Spray (0..........10 Ethocel ® 20 (Dow) ..135 Isopropanol............ BASF Pharma Ingredients Generic Drug Formulations 2001 ... g......... Polidocanol ................................................................ Manufacturing of the spray Fill the solution into spray cans with the necessary quantity of propellant (e.........6....................... propane/butane) or in a mechanical pump bottle.... 3................................ Formulation I..................4 Ethyl acetate ............ Manufacturing of the solution Dissolve the components I in the solvent mixture II........40 g g g g g g 2....

............3 g Ethanol 96 % ... II................... 1 No.. diluted ............... Formulations No. 2 PVP-Iodine 30/06 (BASF).......................... 4... 3....10...................................... Properties of the solutions Brown transparent liquids having a pH of about 1....ad 100 g 20........ Tartaric acid ........7...... Administration as pr eventive desinfectant Dilute about 3 ml of the concentrate with 1 l of water...............0 g – 7........................3 g 10.......... BASF Pharma Ingredients Generic Drug Formulations 2001 .0 g 5...3 g 4.................0 g Texapon ® K 12 (Henkel) ..........0 g Water .4...... Manufacturing Dissolve the surfactant II in solution III and add slowly PVP-Iodine I........................6.....– Nonoxinol 14..........................5........ 2.......8 Liquid Formulations (Lab scale) Povidone-Iodine Concentrates for Broilers and Cattles (20%) 1......3 g Sulfuric acid.....0 g ad 100 g I.....0 g III.......20.

........0........ Manufacturing Dissolve PVP-Iodine in the solution of Cremophor A 25 in water........ 52 °C) The content of available iodine dropped to 98 %.................0 g Cremophor A 25 [1] . Formulation PVP-Iodine 30/06 (BASF) ..8 Liquid Formulations (Lab scale) Povidone-Iodine Foam Spray (10%) 1. Chemical stability (14 days...10.........................6................... Fill the aerosol cans with 90 parts of this solution and 10 parts of propane + butane (1+3)....... 3.......... BASF Pharma Ingredients Generic Drug Formulations 2001 ..ad 100 g 2..01 g Water ...

.........0 Water.....6.................................................10. Manufacturing Dissolve the PVP-Iodine in the solvent mixture....... Properties of the concentrate Brown transparent liquid......... BASF Pharma Ingredients Generic Drug Formulations 2001 ..... Formulation PVP-Iodine 30/06 (BASF) .......... 4..8 Liquid Formulations (Lab scale) Povidone-Iodine Gargle Solution Concentrate (10%) 1.......0 Ethanol 96 % .........1.....80. 3....9....... Administration Dilute 10 ml of the concentrate with about 100 ml of water...............0 g g g g 2...................0 Propylene glycol [1] ....

..0 Menthol .......15......0.........0 Ethanol 96 % ........5 Water .....1 Lutrol E 400 [1] ..... Formulation I....... Chemical stability (20–25 °C) 0 Months Available iodine Loss of iodine 0.2 % 0.8 Liquid Formulations (Lab scale) Povidone-Iodine Mouth Wash and Gargle Solution Concentrate (7...................................5 Saccharin sodium....... PVP-Iodine 30/06 (BASF) ........ 1+1 .89 % 2. 4................0..........6......... II.. A brown liquid is obtained having a fresh taste..........................50. Manufacturing Dissolve PVP-Iodine and saccharin in water and mix with solution II............. Properties of the concentrate Brown transparent liquid having a fresh odour..0 g g g g g g g 2............ Administration Dilute 10 – 20 ml with a glass of water................ 3..............0.......5%) 1..........82 % 2...............2 Anise oil + eucalyptus oil..15............... BASF Pharma Ingredients Generic Drug Formulations 2001 .......7........91% – 6 Months 12 Months 0..2 % 5....

..... 2 PVP-Iodine 30/06 ....... Fill in aerosol cans with propellants like propane+butane or with manual valves.............................. 3......0 g 2... 1 No.6.....75....10................................. Manufacturing Dissolve Kollidon VA 64 in the mixture of solvents and add slowly PVPIodine to the well stirred solution...................0 g – 75......0 g n-Propanol..0 g Ethanol .0 g Kollidon VA 64 [1] ....................... Formulations No.0 g 15...... BASF Pharma Ingredients Generic Drug Formulations 2001 ... Chemical Stability The obtained solutions showed no loss of iodine after the storage of 15 days at 60 °C.15..........................8 Liquid Formulations (Lab scale) Povidone-Iodine Liquid Spray (10%) 1.........– 10..................

... 1 = 0......0...4% No... 4.............7 0..11 g – – 98..............0%) 1...... Properties of the solutions Clear..0.................. 0........6.......................6 % 1..01 molar ....9 ppm BASF Pharma Ingredients Generic Drug Formulations 2001 .......8 mg Sodium chloride ..........6.50 g 0.........0% PVP-Iodine 30/06 ...........0..56 g 1.. 3..............00 g 0................. 2 = 1......0...... Manufacturing Dissolve PVP-Iodine slowly in the solution of the salts...............2 Available iodine ................................................... 1 ess (Str test at 52 °C) Initial After 14 days pH........1......................4% + 1....................... brown liquid of low viscosity.............9 ppm 6........... Formulation No....74 g Sodium hydroxide solution.05 g Water ................1..........– Free iodine ...39 g 2.........053 % 3....40 g Potassium iodide...........055 % Loss of iodine .................20 g Potassium iodate.........44.97..................8 Liquid Formulations (Lab scale) Povidone-Iodine Ophthalmic Solutions (0.............. Chemical stability of formulation No.................

.....1.........................................9 ppm 7.....3 Available iodine ......– Free iodine ..... Chemical stability of formulation No....................Povidone-Iodine Ophthalmic Solutions (0....................2 0....0%) page 2 5...........................................0..........6..........4% + 1.... 2 ess (Str test at 52 °C) Initial After 14 days pH.2 ppm BASF Pharma Ingredients Generic Drug Formulations 2001 .........16 % 0% 2...15 % Loss of iodine ...................................

............ warm up to 40 °C and dissolve xylitol.....10 Peppermint oil double rect............................ Chemical stability After storage of 15 hours at 80 °C a loss on iodine of about 7 % has been determined....... Formulation PVP-Iodine 30/06 (BASF) .10. 3... At room temperature dilute with propylene glycol..... Manufacturing Dissolve potassium iodide in water...00 Potassium iodide .0..1...10............................................... dissolve PVPIodine and add the flavours.........10 Xylitol ..78.........75 Menthol.............00 Propylene glycol [1] . crystalline ..... 4......00 Water .........05 g g g g g g g 2...... BASF Pharma Ingredients Generic Drug Formulations 2001 ......... Properties of the solution Clear brown liquid with a sweet refreshing taste........... .....................6........0......................0.......8 Liquid Formulations (Lab scale) Povidone-Iodine Pump Spray (1%) 1...........

.....– Sodium biphosphate solution 0.....1 molar...85............... 1 molar solution.........6 g 10................2 g 59... 2 PVP-Iodine 30/06 (BASF) ...... add Texapon and slowly dissolve the PVP-Iodine......– Water ... Formulations No.... 1: Dissolve Lutrol F 127 and than Natrosol in the water..5 g 28............0 g Natrosol ® HR 250 (Hercules) .... Adjust the pH with the sodium hydroxide solution to about 3...........0... clear solutions having a certain viscosity and a pH of 3 – 4.....2 molar..................10...6... Formulation No..– Citric acid solution 0....................................... 2: Dissolve Tylose M 300 in the mixture of the citric acid and sodium biphosphate solutions.........2 g Tylose ® M 300 (Hoechst).. 1 No............1........5.... Properties of the solutions Brown..........3....2 g Sodium hydroxide..0 g Lutrol F 127 [1].......... Manufacturing Formulation No.0 g 0...................... As soon as both are dissolved add slowly the PVP-Iodine to the well stirred solution.................3 g – 2...... 3..8 Liquid Formulations (Lab scale) Povidone-Iodine Seamless Solutions (10%) 1...................0 g – – – 2..– Texapon K 12 (Henkel) ..................... BASF Pharma Ingredients Generic Drug Formulations 2001 .

.. The viscosity can be changed by modification of the amount of Natrolsol 250 HR...8 Liquid Formulations (Lab scale) Povidone-Iodine Shampoo (7.... BASF Pharma Ingredients Generic Drug Formulations 2001 .... Chemical stability In the stress test (14 days..............4....0 Super Amide ® L 9 (Onyx) ................ After cooling incorporate Neutronyx... 52 °C) the loss of available iodine was about 12 %.......5 – 0...... Properties of the shampoo Brown.............7 Water ..... Formulation PVP-Iodine 30/06 (BASF) ...........................ad 100 g g g g g 2.. 4. 3........25......... clear solution....0..0 Natrosol ® 250 HR (Hercules) ...7.5%) 1...5 Neutronyx ® S 60 (Onyx) .6...... Manufacturing Dissolve Super Amide and Natrosol in hot water (about 60 °C) and then dissolve PVP-Iodine........

. 1 PVP-Iodine 30/06 (BASF) ...4 .0 g g g g g 2.... 2 (52 °C........ 2 10.... 1 (20–25 °C.....1 molar solution . I 1..............– Citric acid 0..... 3......1 96 % 4.......6. Chemical stability Formulation No.......2 46.....5 43..0 0. Manufacturing Dissolve the PVP-Iodine (and Lutrol F 127) in the mixture of the buffer solutions (and Lutrol E 400)...8 Liquid Formulations (Lab scale) Povidone-Iodine Solution (10%)..... 4...........4 Formulation No. 14 days) Loss of available iodine 6.. Properties of the solutions Brown clear solutions having a low viscosity and pH of about 4....10......... 1 year) 0 Month Available iodine pH 100 % 4......3 0....2 molar solution ..43.............3 % BASF Pharma Ingredients Generic Drug Formulations 2001 6 Months 12 Months 100 % 4.46...............5....– Lutrol E 400 [1] ............0 g Lutrol F 127 [1] ..........6 g Na 2 HPO 4 · 12H 2 O 0.........4 g No........ Formulations No.

..0............ PVP-Iodine 30/06 (BASF) ...........42 g g g g g g g 2.6 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...............5 Available iodine ..86....0.............03 Sodium hydroxyde solution........... Properties of the solution Brown transparent liquid having a pH of 4............– 3...... II 1....00 Water ...............03 % 4.............08 % Loss of iodine .....2...................................5 1.........8 Liquid Formulations (Lab scale) Povidone-Iodine Solution (10%)....03 III..00 II......... 1 molar .................... Manufacturing Dissolve Texapon K 12 (II) in solution III and add slowly PVP-Iodine to the well stirred solution............ 3..........................1...6........0...... Texapon K 12 (Henkel) ........... Sodium biphosphate (Na 2 HPO 4 ) ...08 Glycerol .. Chemical stability After production After 14 days/52 °C pH .............10...........4....... Formulation I...14 Sodium citrate ...........5.......1..... 4........

...... Water ....... 1 is about 3.......6 ......6..............5 g 7. dissolve PVPIodine and add Neutronyx or Lutensit..................................... 2 PVP-Iodine 30/06 (BASF) ..0 g 4....................5 g Neutronyx S 60 (Onyx) .....3 87 % 4................. clear viscous solution.. I 1... cool.0 g – q........ 63..0 g Floral Bouquet .25.. s..........4 4.............. The pH of formulation No...... Chemical stability of formulation No.. Manufacturing Dissolve Super Amide or Monoamide in hot water..– Super Amide L 9 (Onyx) ..63.7.. 1 No................0 g Lutensit ® AES (BASF) ..........5 g – 25..... 3.......5 g 2.4...................q... s........ Properties of the scrub Brown.5%).........– Monoamide ® 150 MAW (Mono) ......8 Liquid Formulations (Lab scale) Povidone-Iodine Surgical Scrubs (7.......................... 1 (20–25 °C) 0 Month Available iodine pH 100 % 3......6 BASF Pharma Ingredients Generic Drug Formulations 2001 6 Months 12 Months 99 % 4... Formulations No.

...5 g – – 20..... 3 Loss of available iodine .....7 g – 7..................12.9 % 10............0 g 46....8 Liquid Formulations (Lab scale) Povidone-Iodine Surgical Scrubs (7.....2 g 25.......15..7........ 1 No......... 3 PVP-Iodine 30/06 (BASF)..............6.........0 g Lutensit A-ES (BASF) ..73... 4............ 3....5 g 7.. Properties of the scrubs Brown.. Formulations No....0 g 4...4. 2 No.......2 % 13.– Fenopon ® CO 436 ............ 1 No.5%)........... II 1.– (Rhône-Poulenc) Super Amide L 9 (Onyx)..8 g 1.– Water ..... 2 No.5 g Texapon K 12 (Henkel) .. clear viscous solution....8 % BASF Pharma Ingredients Generic Drug Formulations 2001 ........0 g – 68......... Stability (14 days at 52 °C) No....3 g 2.....0 g Glycerol..5 g – 18. Manufacturing Dissolve the surfactants in hot water (add glycerol) and incorporate the PVP-Iodine...

..................3..................... BASF Pharma Ingredients Generic Drug Formulations 2001 .......................... 4...00 Glycerol .0..8 Liquid Formulations (Lab scale) Povidone-Iodine Teat-Dip Solution for Cattles (3%) 1.................ad 100..... Chemical stability After the storage at 52 °C during 14 days the loss of available iodine was 11..00 Glacial acetic acid .......3..5 %... 3...........80 Sodium hydroxide solution.......35 Water ......... 50 % ... Formulation PVP-Iodine 30/06 (BASF) ........0 g g g g g 2............0........ Manufacturing Mix all liquid components and dissolve PVP-Iodine......6. Properties of the solution Brown transparent liquid having a pH of 4...8........

.....0 1.. 1 molar.....................0 g Lidocain hydrochloride ....... Manufacturing Dissolve the solids (I) in water (IV)................... cool to about 6 °C.........7 % 2.......6 g with lidocain 10.........1 g g g g g g 2...... Stability (14 days............... PVP-Iodine 30/06 (BASF) .....7 15...4 g IV....2..9 20 % BASF Pharma Ingredients Generic Drug Formulations 2001 ...............6.... Lutrol F 127 [1] ........ 3......4......5 Loss of available iodine . Properties of the gels Viscosity at room temperature ....................0 g III...........– Sodium chloride ................................ Formulations without lidocain I.........4...........69.........1.gels pH value (20 % in water) ..........0 4.............0 g II..........9........8 Liquid Formulations (Lab scale) Povidone-Iodine (+ Lidocain) Thermo-Gelling Solution (10%) 1. Sodium hydroxide solution.....15..........8 4....2 69..10..viscous solutions (20 – 25 °C) Viscosity on the skin (35 – 37 °C) .................. dissolve Lutrol F 127 (II) and adjust the pH value with the sodium hydroxide solution (III)............................. Water ..... 52 °C) without lidocain with lidocain pH value (20 % in water) ........0 0.................

2 is mainly provided for the production and use in hospitals. BASF Pharma Ingredients Generic Drug Formulations 2001 . Remark Since the stability of the combination of Povidone-Iodine with lidocaine is limited the formulation No.Povidone-Iodine (+ Lidocain) Thermo-Gelling Solution (10%) page 2 5.

10.. Formulation PVP-Iodine 30/06 (BASF) .................. 0. Properties of the solution Brown..............6......3................2 molar solution ...3 Citric acid...0........2 Na 2 HPO 4 · 12H 2 O. clear solution having a low viscosity and a pH of about 4.......43.....5 Lutrol F 127 [1] ....46.......0 g g g g g 2..0..1 molar solution ... 0....8 Liquid Formulations (Lab scale) Povidone-Iodine Vaginal Douche Concentrate (10%) 1...... 3...0 Lutrol E 400 [1].... Manufacturing Dissolve PVP-Iodine and Lutrol F 127 in the mixture of the buffer solutions with Lutrol E 400........... BASF Pharma Ingredients Generic Drug Formulations 2001 ................

....... BASF Pharma Ingredients Generic Drug Formulations 2001 ..........8 Liquid Formulations (Lab scale) Povidone-Iodine Viscous Solution (1%) 1..........5 g (Buffer.97..1............... Formulation PVP-Iodine 30/06 (BASF) .....6.......... Viscosity (Brookfield): 7....) Water .................................3 % and no change of the appearance was observed......5 g 2.................s......500 mPa · s 4... 3.................... Manufacturing Dissolve PVP-Iodine and Natrosol in the well stirred water.... Properties of the solution Clear brown viscous liquid..q.... Chemical and physical stability In a stress test (15 hours at 80 °C) the loss of iodine was 13........0 g Natrosol 250 HR (Hercules) ..1....

0.............. 1 molar .00 Neutronyx S60 (Onyx......8 Liquid Formulations (Lab scale) Povidone-Iodine Wash Solution (5%) 1......... clear solution having a pH of 5............. USA) ......20 Natrosol 250 HR (Hercules) ..5..........5..15 Water ....6........ad 100 g g g g g g g g 2......0......... Properties of the wash solution Brown..................2... Germany) .00 Monamide 150 MW (Mona..00 Sodium hydroxyde solution. Formulation PVP-Iodine 30/06 (BASF) ...5 4........ Chemical stability In the stress test (14 days.....1..27 Potassium iodate ...........30 Softigen ® 767 (Hüls.....1.........6........... USA) ........... 3...... BASF Pharma Ingredients Generic Drug Formulations 2001 .............. Manufacturing Dissolve all components in the given order in water. 52 °C) there was no loss of available iodine and the pH only increased to 5........

...........0......s............................................. Water of injectables ..15 g Sodium citrate . II.........0......................... Preservative .........0.............homogeneous Redispersibility ...................57 g Antioxidant...............q..........................0 g Kollidon 17 PF [1] .......5 % of cysteine could be added as antioxidant........8 Liquid Formulations (Lab scale) Procain Penicillin Injectable Suspension (300 mg/ml) 1........................................30.... Manufacturing Suspend procain penicillin G in the well stirred solution II.... 3.4 g Carboxymethyl cellulose................................q.......ad 100 ml 2. BASF Pharma Ingredients Generic Drug Formulations 2001 .....easy 4.. Properties of the suspension Aspect ... Procain Penicillin G .... Remark To prevent of discolouration of the dissolved Kollidon during storage 0........................s........6...........2 to 0..... Formulation I.............

.ad 100 ml 2. Cremophor EL could be substituted by Solutol HS 15 [1]........................ BASF Pharma Ingredients Generic Drug Formulations 2001 ... Manufacturing Mix propanidide with the warm Cremophor EL (60 °C) and add slowly the warm solution II.......20............ s.. Shaking of the ampoules during cooling gives homogeneous clear solutions............ 4. The sterilisation can be done by filtration or heat.q...... Water for injectables ..........0 g Cremophor EL [1] ........ Propanidide ..................0 g Preservatives...... Formulation I........6... Properties of the solution A clear colourless solution was obtained...... Remarks – To reduce the viscosity and the side effects...... II...... 3.5....... – During the heat sterilisation a separation of two layers can be observed......8 Liquid Formulations (Lab scale) Propanidide Injectable Solution (50 mg/ml) 1.......... – In Germany Cremophor EL must be declared on the package of injectables......

. BASF Pharma Ingredients Generic Drug Formulations 2001 ..........1 to 0..........5 % of cysteine could be added as antioxidant......1.........................0 g Water for injectables .......6... Formulation Sobrerol.....................................................2 µm filter...........................6..........100.. 3.. Remark Preservatives could be added if it is needed. Properties Appearance . The sterilisation can be done by filtration through a 0.......5 g Kollidon 17 PF [1] ...clear Viscosity........................0 ml 2..very low 4....8 Liquid Formulations (Lab scale) Sobrerol Injectable Solution (75 mg/5 ml) 1..... Manufacturing Dissolve sobrerol slowly in the well stirred solution of Kollidon 17 PF....... To prevent of discolouration of Kollidon in the solution during storage 0..............

............................. Properties of the suspension A homogeneous white suspension was obtained................2 Water... Formulation Sulphadiazine.......................... It showed some sedimentation after 7 days but the redispersibility was very easy...................................................8 Sodium hydroxide ........... BASF Pharma Ingredients Generic Drug Formulations 2001 ..........44 g g g g g 2.....6 Kollidon CL-M [1] ..................... Manufacturing Dissolve sodium hydroxide in water and suspend the active ingredients and Kollidon CL-M......8 Liquid Formulations (Lab scale) Sulfadiazine + Trimethoprim Veterinary Concentrated Oral Suspension (40% + 8%) 1.............40 Trimethoprim ......6...................... The pH was 12. 3...............

.................. s. Water for injectables ............................40 ml Propylene glycol [1].......clear pH...........70 g Antioxidant.very low 4............................................ Properties of the solution Appearance ............5 g Ethanol 96 % ......................................... Manufacturing Mix solution I slowly with solution II at 60 °C and cool........2 to 0.......... II............q. 3..... Sulfadimethoxine........ Formulation I...............40 ml Kollidon 12 PF [1] ....7 Viscosity........ Physical stability (20–25 °C) No recrystallisation after some weeks.............6........ ad 200 ml 2......... s.............. BASF Pharma Ingredients Generic Drug Formulations 2001 .......................8 Liquid Formulations (Lab scale) Sulfadimethoxine Veterinary Injectable Solution (2.......5% = 250 mg/10 ml) 1..............5 % of cysteine could be added as antioxidant.... Remark To prevent of discolouration of Kollidon in the solution during storage 0.. 5.......................q...............................................

... colourless pH....2...5 with sodium hydroxide..................... s..................................0 g Soluphor P [1] ....8.........29.... Manufacturing Disolve sulfadoxine and trimethoprim in Soluphor P............8 Liquid Formulations (Lab scale) Sulfadoxine + Trimethoprim Veterinary Injectable Solution (1000 mg + 200 mg/10 ml) 1.......................................... 2......... Formulation Sulfadoxine ....6................... and set to pH 8......................0 g Sodium hydroxide ... add the water.....0 g Trimethoprim .................5 BASF Pharma Ingredients Generic Drug Formulations 2001 .0 g Water for injectables ..............10....... Properties of the solution Appearance ......clear....................................56......q... 3................

................. colourless solution of low viscosity was obtained..... Sulfadoxine .... Properties of the solution A clear... BASF Pharma Ingredients Generic Drug Formulations 2001 ............ 3............. Formulation I.. Water........................8 Liquid Formulations (Lab scale) Sulfadoxine Solution (2% = 20 mg/ml) 1..... II........................0 g 2.... 4................30.........0 g Preservative ... s............ Heat the solution II to the same temperature and mix slowly with solution I.68....6....................q.. Physical stability No change of the clarity after 2 weeks stored at 6 °C and at 20 – 25 °C........2.........0 g Lutrol E 400 [1]... Manufacturing Prepare solution I at 60 °C..

... 1 No.... Properties of the suspensions No...........very easy beige very low very few easy BASF Pharma Ingredients Generic Drug Formulations 2001 .....s...... Vanillin ............... I... 2 Colour:...0 g II..........0 g Trimethoprim......4 g q.....6 g Kollidon CL-M [1] ..77............................... suspend in solution II and add the flavours III..0 g III..........0 g Lutrol F 127 or Lutrol F 68 [1].................... 1 No..beige Viscosity: .very low Sedimentation after 2 weeks: ..................... 2 Sulfamethoxazole . Sucrose ........................................ Manufacturing Sieve the components I............3......1.............. q...................not observed Redispersibility after 2 months: ...0...................................... 2................................................ Formulations No....................................s...0 g 1.6..8 Liquid Formulations (Lab scale) Sulfamethoxazole + Trimethoprim Oral Suspension (400 mg + 80 mg/5 ml) 1.....2 g 8.. 3.........0 g 82.....0..............– Water...........8.....................................2 g Chocolate flavour ................................0 g 3................................6 g – 5.10.........

...................... 3.............. Manufacturing Dissolve Kollidon........................... Remark The use of sodium sulfite in injectables is not allowed in all countries...4..8 Kollidon 12 PF [1] .....44.............2 Sodium sulfite or cysteine ................. add the active ingredients and stir until they are dissolved................0 Trimethoprim ..............6 Ethanol ....................... parabene.......... Formulation Sulfamoxole ..........0.... cool and sterilize......10.....0 Parabene . sodium sulfite (or cysteine) in the mixture of water und propylene glycol....................10... BASF Pharma Ingredients Generic Drug Formulations 2001 .............. 4...............0........... Add ethanol.........0 Water for injectables ..............6....4 Propylene glycol [1].......30.... heat..................0..8 Liquid Formulations (Lab scale) Sulfamoxole + Trimethoprim Veterinary Injectable Solution (400 mg + 80 mg/10 ml) 1. Properties of the solution A clear solution was obtained..........0 g g g g g g g g 2...........

.........12....1 g q.............................. Manufacturing Dissolve Kollidon and sulfathiazole at 70 °C in water and cool slowly to room temperature... 3..................... BASF Pharma Ingredients Generic Drug Formulations 2001 ....... Remark To prevent of discolouration of the solution during storage 0......0..................2 to 0............6....s...100........................– Sodium sulfite .......................................< 0.....0 g 2.......very low 4.........– Water (for injectables) .0 g 0................clear Viscosity ..................8 Liquid Formulations (Lab scale) Sulfathiazole Veterinary Injectable and Oral Solutions (0................................8 g – 22..... Formulations Injectable Oral solutions Sulfathiazole ...... Sterilisation of the injectable solution can be done by filtration through a 0........5 g < 0....2 filter................5 g Kollidon 25 [1].............5 % of cysteine could be added as antioxidant instead of sodium sulfite.................8% = 8 mg/ml) 1...............8 g Kollidon 12 PF or Kollidon 17 PF [1] ........... Properties of the solution Appearance... 100.....1 g Preservative .

......... Water.....2 g 2.92... 3.......... 4......2% = 60 mg/5 ml) 1....3........................ Physical stability After 7 days of storage at room temperature almost no sedimentation of the terfenadine was observed but the redispersibility by shaking (2 times) was very easy. Formulation Terfenadine .............6 g Preservative .............q........ BASF Pharma Ingredients Generic Drug Formulations 2001 .3..................1....................................s........... Manufacturing Dissolve Lutrol F 127 and Cremophor RH 40 in water at 40 °C..................6....2 g Lutrol F 127 [1] ... Whilst stirring slowly add the terfenadine.....8 Liquid Formulations (Lab scale) Terfenadine Suspension (1...................0 g Cremophor RH 40 [1] .......... Properties of the suspension A tasteless milky suspension was obtained.............

....5 % of cysteine could be added as antioxidant....................ad 50 g 2. Formulation Theophylline (Knoll) ...... Manufacturing Dissolve Kollidon 12 PF and the preservative/antioxidant in water and add theophylline to the well stirred solution 3................. Properties of the solution The obtained clear and somewhat yellowish solution had got the pH value 5.....6.....2 and did not recrystallize in a short term test.8 Liquid Formulations (Lab scale) Theophylline Injectable Solution (4% = 200 mg/5 ml) 1....q............... Antioxidant.. 4............. Remarks To prevent of discolouration of Kollidon in the solution during storage 0...2 to 0.......................... Water for injectables .......s..s................15 g Propylene glycol [1] ...... BASF Pharma Ingredients Generic Drug Formulations 2001 ...........................2 g Kollidon 12 PF [1] ......................10 g Preservative .....................q...........................

........................15. 3......... BASF Pharma Ingredients Generic Drug Formulations 2001 .......05 g Alpha Bisabolol nat.........8 Liquid Formulations (Lab scale) Tretinoin Solution (50 mg/100 g) 1......0.....0 g Propylene glycol [1].......s...otected pr from light) Months Tretinoin content 0 3 6 9 12 0...1 g Water.............0.....0 g Butylhydroxytoluene ......... 2...0......q. Chemical stability (20–25 °C..14.....0 g Parabenes/sorbic acid .70.......044 % = 96 % 5.045 % 0...046 % 0. Introduce this warm solution slowly in solution II............. 4... It forms a clear yellow solution..... II..... Properties of the solution Clear yellow liquid......05 g Cremophor RH 40 [1] ...... (BASF).................046 % = 100 % 0..6... Tretinoin (BASF).. Formulation I....................... Remark It is very important to protect this formulation from light to avoid the isomerization and degradation of tretinoin................... Manufacturing Heat mixture I to 40 – 50 °C to obtain a clear solution...044 % 0...............................

............ i... 5..13........./g15 mg Solutol HS 15 [1]... Cool to room temperature and dissolve the components III.........0 g Vitamin D 3 (Cholecalciferol) 40 Mio.....2. After the ampoules have been heat-sterilized. Vitamin A palmitate 1....8 Liquid Formulations (Lab scale) Vitamin A + Vitamin D3 + Calcium + Magnesium Injectable Solution (33. + 6.../g (BASF) . Calcium gluconate ..0 g III.. u... Water for injectables .. to eliminate any separation of the phases that may have occurred.otected pr from light) No change of the clarity after some days...... 4. u.. 3.. Properties of the solutions A clear yellow solution was obtained.. they should be shaken for a short time................. while they are still hot.... Sterilization can also be performed by membrane filtration under pressure..... Physical stability (20–25 °C...... + 100 mg + 200 mg/g i......1..1...7 Mio i... Remark Perhaps it would be recommendable to use an other magnesium salt instead of the sulfate to avoid any precipitation of calcium sulfate during storage..000 i. Formulation I.. BASF Pharma Ingredients Generic Drug Formulations 2001 .u.) 1....6..........1 g Magnesium sulfate .. Manufacturing Heat mixture I and the water (II) separated to about 65 °C.....000 i.0 g II.u...............0 g 2.85.. Add the water very slowly to the well stirred mixture I..... u......

After the ampoules have been heat-sterilized.... BASF Pharma Ingredients Generic Drug Formulations 2001 .....000 i........... while they are still hot... Heat the water II to 65 °C and add it slowly to the heated mixture I.............. Manufacturing Heat mixture I to 65 °C...........u.... to eliminate any separation of the phases that may have occurred..u......9......4 Cremophor EL [1] .............6.u... clear solution.................0 IV...... Heat the mixture III to 180 °C....8 g g g g g g g g g 2.....72......5 Mio i..........000 i.....< 9.. When the temperature is reached add the beta-carotene IV.... Beta-Carotene crystalline (BASF)..... they should be shaken for a short time...... Let cool under continuous stirring of about 30 minutes......u.8 Liquid Formulations (Lab scale) Vitamin A + Vitamin D3 + Vitamin E + Beta Carotene Veterinary Injectable Solution (100..0......... + 10 mg + 8 mg/g) 1.. A clear solution is formed..........0./g./g (BASF) Vitamin D 3 40 Mio i...............05 Benzyl alcohol ...... Vitamin A propionate .4........ Properties of the solution Dark red-brown... hold for 3 min at this temperature and then add Mixture I/II slowly during the next 4 minutes.0.... Remark In Germany Cremophor EL must be declared on the package of injectables.1.. 3....... Formulation I. 4.0 II........ Sterilization can also be performed by membrane filtration under pressure............. + 20.............................. A clear solution is formed (= Mixture I/II)....3 III.. Vitamin E acetate .0 Butylhydroxytoluene .............1... Water for injectables ...4 2.0 Cremophor EL [1] ...................

butylhydroxytoluene and benzyl alcohol are mixed together at around 60 °C.. they should be briefly shaken whilst they are still hot....................ad 100 ml 2..u................ BASF Pharma Ingredients Generic Drug Formulations 2001 ..u... 3......... Formulation Vitamin A propionate .................... u.2 g Vitamin E acetate (BASF) .................8 Liquid Formulations (Lab scale) Vitamin A + Vitamin D3 + Vitamin E Aqueous Injectable Emulsion for Cattles (500.5 Mio i...0 g Water for injectables ........... Cremophor EL. Chemical stability of vitamin A (Str ess test at 40°C) Vitamin A content 1 Month 2 Months 3 Months 92 % 86 % 81% 5.. 4..... + 50 mg/ml with Cremophor EL) 1....000 i......22.0 g Cremophor EL [1] ....1..6.... Manufacturing The vitamins.000 i. After the ampoules have been sterilized... Properties of the emulsion Pale yellow milky.... + 75. and water at 60 °C is slowly incorporated with vigorous stirring.. stable emulsion with a viscosity of less than 30 mPa · s......../g (BASF) Vitamin D 3 (Cholecalciferol)..............0..........5..... Remark In Germany Cremophor EL must be declared on the package of injectables...5 g Benzyl alcohol . to eliminate any separation of the phases............................0 g Butylhydroxytoluene .0.0 g 2.......................10.....

+ 50 mg/ml with emophor Cr EL) page 2 Vitamin A found in the liver [%] 6.u. Bioavailability of vitamin A inoilers br after 7 days (intramuscular application) 80 60 40 20 0 Aqueous emulsion Organic solution for comparison BASF Pharma Ingredients Generic Drug Formulations 2001 Oily solution for comparison . + 75.000 i.u.Vitamin A + Vitamin D3 + V itamin E Aqueous Injectable Emulsion for Cattles (500.000 i.

....8 Liquid Formulations (Lab scale) Vitamin A + Vitamin D3 + Vitamin E Aqueous Injectable Emulsion for Cattles (500.. i...........0 g Water for injectables ............... and then add the water (60 °C) slowly and with vigorous stirring.............2 g Vitamin E acetate (BASF) .... 3............. pale yellow emulsion.... Manufacturing Mix the vitamins.. + 75......000 i...../g (BASF) Vitamin D3 40 Mio...... butylhydroxytoluene and benzyl alcohol at approx.5 g Solutol HS 15 [1]...... BASF Pharma Ingredients Generic Drug Formulations 2001 .5 Mio i..........u..5 g Butylhydroxytoluene .............6..... to eliminate any separation of the phases that may have occurred...... u.....0. Sterilization can also be performed by membrane filtration under pressure.........u.........000 i...../g .. Properties of the emulsion Aspect: Milky... Physical stability (20–25 °C.. Viscosity: Less than 20 mPa · s 4......0......... they should be shaken for a short time....5.1. Formulation Vitamin A propionate ...ad 100 ml 2.22.......... – After the ampoules have been heat-sterilized..otected pr from light) No change of the appearance during 2 years.......... u............0 g Benzyl alcohol .. 60 °C... Solutol HS 15... + 50 mg/ml with Solutol HS 15) 1.15........0 g 2.. while they are still hot..............

16 % loss after 2 years.000 = 20–25 ∞ C =6∞ C 500. Chemical stability of vitamin A (2 years.u. + 75.000 i.000 400. 700. + 50 mg/ml with Solutol HS 15) 5. otected pr from light) i.000 600.000 0 3 6 9 BASF Pharma Ingredients Generic Drug Formulations 2001 12 Months 15 18 21 24 .000 i.u./g Room temperature: 9 % loss after 1 year.Vitamin A + Vitamin D3 + V itamin E Aqueous Injectable Emulsion page 2 for Cattles (500. u.

......50 g Preservative ............ 3......... u........06 g 29. 2 Vitamin A palmitate 1............5 Mio i.0.20 g Butylhydroxytoluene ..10 g (BASF) Vitamin A propionate 2. Water-miscible (120.... i...... miscible with water... Formulations I.000 i.. No................... 1: Formulation No...........4...... stir well and add very slowly the warm solution II (65 °C).....s../g ..................................ad 100 ml – 4.......... clear viscous liquids........ + 40 mg/ml) 1........– (BASF) Vitamin D 3 40 Mio i.. + 60..0 g Glycerol ..06 g Cremophor EL [1] ...........0 g 6..50 g q.. Clarity: Formulation No.8 Liquid Formulations (Lab scale) Vitamin A + Vitamin D3 + Vitamin E Concentrates.....u....... Water .... 2: 28 FTU 32 FTU BASF Pharma Ingredients Generic Drug Formulations 2001 .....6......s..30.......7 Mio.u...7......000 i.... Properties of the solutions Yellow................../g .. II............. u... Manufacturing Heat mixture I to about 65 °C...........0......................./g.......6......... ad 100 ml 2..............q..... 1 No...15 g 4.....u.............15 g Vitamin E acetate (BASF) ..80 g 0...20 g 0..

.............u..../g in arachis oil ...... Properties of the solution Yellow clear liquid.......u..u...........0 1...........0 Mio i..7 Mio i.../g (BASF) Vitamin D 3 2. 5.......6. Chemical stability (str ess test at 40 °C) 3 – 4 % loss of vitamin A per month...............4.. + 50 mg/ml) 1...1.5 Miglyol ® 812 (Dynamit-Nobel) .....................000 i...........u.5.... 4... Manufacturing Mix all components at about 60 °C and cool..........5 DL-alpha Tocopherol (BASF) .......... + 75............... 3.7 Benzyl alcohol .......2.....0 Benzyl benzoate ............................... Remark In Germany Cremophor EL must be declared on the package of injectables....000 i.8 g g g g g g g g g 2.10...2......35......0.............. BASF Pharma Ingredients Generic Drug Formulations 2001 . Formulation Vitamin A palmitate...37.5 Cremophor EL [1] .......8 Liquid Formulations (Lab scale) Vitamin A + Vitamin D3 + Vitamin E Injectable Solution in Organic Solvents for Cattles (500...5 Butylhydroxyanisole .....................5 Vitamin E acetate (BASF) .......

... A + 12....u...000 i. D/ml Vitamin A palmitate ...000 i.0 g q.........7 Mio i..u......./g....... Formulations No... u.03 g Butylhydroxytoluene ....... 3.. u. yellow liquid...u.. miscible with water (Clarity: 34 FTU)........u.....2 g 2.. u.........000 i..000 i... D/g) (100... u....6.3 g 26..0..u.......000 i..... D/g I..........014 g/ml 25 mPa · s The concentrate is miscible with water and can be processed further to liquid pharmaceuticals...5 g 55 mg 0.8 Liquid Formulations (Lab scale) Vitamin A + Vitamin D3 Concentrate......0...7..... No. II..ad 100. Water ...s.. with vigorous stirring...... BASF Pharma Ingredients Generic Drug Formulations 2001 .s.. 1 Slightly opalescent.. A + 20....... D/ml) 1..........25.0 g Preservative . 2 Clarity: Density (25°C): Viscosity (25°C): Clear (27 FTU) 1./g (BASF) Vitamin D 3 40 Mio i.....000 i..000 i. 2 100.10 g 1.000 i.u. 67. Formulation No.. A + 12.......q...... Properties of the solutions Formulation No.... Water-miscible (120. Manufacturing Heat the mixture I to about 65 °C.... A + 20... add very slowly the warm solution II (65 °C).......15 g Cremophor RH 40 [1] .....0 g 6........... 1 120...

....0 g Parabene ........u..6... BASF Pharma Ingredients Generic Drug Formulations 2001 ..10..................... + 3. II...... i...7............................. Vitamin A palmitate.8 g Sorbic acid ....2 g Water.................... 3... Manufacturing Heat mixture I and solution II to about 65 °C and add II slowly to the well stirred mixture I...8 g 2....................../g (BASF) Vitamin D 3 40 Mio....74......7 Mio i........0..8 Liquid Formulations (Lab scale) Vitamin A + Vitamin D3 Drops (30.........1..........9 g 1....................0..........000 i... u...........................0.3 g Lutrol E 400 [1] ........5 mg Cremophor RH 40 [1] ......./g) 1..0 g Butylhydroxytoluene ....................000 i.......u....... Formulation .... Properties of the solution Yellow clear or slightly opalescent liquid.... u...............12...................../g ..........

u.000 i.u. Chemical stability of vitamin A (about 23 °C) 30. u.000 i.000 88% 84% 20./g 4./g) page 2 i. + 3.000 0 0 3 BASF Pharma Ingredients Generic Drug Formulations 2001 6 Months 9 12 .Vitamin A + V itamin D3 Dr ops (30.000 25.

..otected pr from light) No change was observed during 1 year. Formulation 30.u...s.. A + 5.6..000 i.u...ad 100 ml 1.. Heat the solution of the preservative in water to the same temperature and add it slowly to the well stirred vitamin mixture..... A + 5...013 g Butylhydroxytoluene..... After the ampoules have been heat-sterilized.....000 i...u....0 g q./g (BASF) Vitamin D 3 40 Mio i. D3 30. to eliminate any separation of the phases that may have occured...... ad 100 ml 2...... D3 Vitamin A palmitate ..1 g Solutol HS 15 [1] .u....0. Water for injectables ..s.. while they are still hot......0 g Preservative ..9 g 0.. 3.000 i........u...7 Mio i..1 g 10.9 g 1./g .000 i......q... Sterilization can also be performed by membrane filtration under pressure.....0 –10........... Properties of the solutions Clear yellow solutions where obtained...u.......000 i..... 4................u......0. BASF Pharma Ingredients Generic Drug Formulations 2001 ...............9.u.. A + 10....000 or 10............ they should be shaken for a short time....026 g 0... Manufacturing Heat the mixture of the vitamins with butylhydroxytoluene and Solutol HS 15 to about 65 °C... D3/ml) 1..8 Liquid Formulations (Lab scale) Vitamin A + Vitamin D3 Injectable Solutions (30...1..000 i... Physical stability (20–25 °C....

..... pH 6. Formulation I.25 mg Cremophor RH 40 .... Properties of the syrup Clear.....7 Mio i...............7..1......... Vitamin A palmitate......... II........u... + 10.............6../g.........000 i......9 g 1.......u.... /ml) 1.8 Liquid Formulations (Lab scale) Vitamin A + Vitamin D3 Syrup (30...... yellow liquid...0 g Sugar syrup 50 % ....000 i....../g (BASF) Vitamin D 3 40 Mio i.... stir well and add slowly the syrup II. 3.ad 100 ml 2. 4.. Chemical stability of vitamin A (20-25 °C) Vitamin content After production 3 Months 6 Months 100 % 99 % 97 % BASF Pharma Ingredients Generic Drug Formulations 2001 .... Manufacturing Heat mixture I to about 45 °C..u...........u..2..

viscous liquids....... u. 2 Vitamin A palmitate 1../g (BASF) Vitamin E acetate (BASF) ..... II...... 1 No..8 Liquid Formulations (Lab scale) Vitamin A + Vitamin E Drops (25...........0 g DL-alpha-Tocopherol (BASF) ............71..s....s...q...........7 Mio........0 g Preservative ...0 g Cremophor RH 40 [1] ...... yellow.7 Mio i.1............. with stirring.5 g 5............... 3....5.. Formulations I. Manufacturing Mix the vitamins with Cremophor RH 40 (and DL-alpha-tocopherol) at 60 °C and then add solution II (at 37 °C) slowly. + 50 mg/ml) 1....... u.......6... No..... BASF Pharma Ingredients Generic Drug Formulations 2001 ..........................5 g 2. i..1.... Properties of the solutions Clear../g ..u....0 g 20................................... Water.21..0 g – q........ 72......5 g 1...........5 g 1......000 i.

2 100 90 23 ∞ C 80 70 40 ∞ C 0 3 BASF Pharma Ingredients Generic Drug Formulations 2001 6 Months 9 12 .000 i. + 50 mg/ml) page 2 Vitamin A content [%] 4. Chemical stability of vitamin A in Formulation No. u.Vitamin A + V itamin E Dr ops (25.

... 3....... II. + 25 mg/ml) 1............. Vitamin A propionate.............2.... to eliminate any separation of the phases that may have occured............57..../g (BASF) Vitamin E acetate (BASF) .30.....3 g 2...5 Mio i...3 yellow 45 mPa · s BASF Pharma Ingredients Generic Drug Formulations 2001 .q...2 g Solutol HS 15 [1] .......000 i.0 g Preservative (e.............6.................5 g Butylhydroxytoluene .... while they are still hot..... Water for injectables .. Properties of the solution Clarity: pH: Colour: Viscosity: clear to slightly opalescent 6............... benzyl alcohol) .......0. Manufacturing Heat mixture I to 70 °C... stir well and add slowly the warm solution II.. Formulation I....... Sterilization can also be performed by membrane filtration under pressure.. they should be shaken for a short time....u........ After the ampoules have been heat-sterilized....0 g 2..........10.8 Liquid Formulations (Lab scale) Vitamin A + Vitamin E Injectable Solution for Sheeps (250.........g..s.....u..

....2 g Cremophor RH 40 [1].............................0......6....s. Manufacturing Heat the mixture I to about 65 °C.u../ml) 1........../g (BASF) ........ Water-miscible (100..............8 Liquid Formulations (Lab scale) Vitamin A Concentrate........... Physical stability (20–25 °C) No change of appearance after 3 months........ Vitamin A palmitate 1..000 i.... II. miscible with water. Water...0 g Preservative ... BASF Pharma Ingredients Generic Drug Formulations 2001 .... u......21...5 g Butylhydroxytoluene . Formulation I..........7 Mio i.... yellow liquid... stir well and add very slowly the warm solution II (65 °C)........6.q.. Properties of the solution Clear.....ad 100 ml 2........ 4...... 3..............

1 g Water .......3.... 1 I... BASF Pharma Ingredients Generic Drug Formulations 2001 ...0 g Lutrol E 400 [1] . II......0 g Cremophor RH 40 [1]............ Manufacturing Heat the mixture I to about 65 °C.......1 81.. Formulations No. 2 3..– Butylhydoxytoluene (BHT) ... Vitamin A palmitate 1....... u......./g (BASF)..........000 i................11..9 g No. 4.........9 g g g g g 2. stir very well and add slowly the hot water (65 °C).... Physical stability (20–25 °C.85.........6.0 0......0.................0 5. Properties of the solutions Yellow clear or slightly opalescent solutions of low viscosity....otected pr from light) No change of clarity and colour after 1 year.......8 Liquid Formulations (Lab scale) Vitamin A Drops (50. u.................../ml) 1.7 Mio.... 3...............0 10............... i.

u. Chemical stability (20–25 °C.Vitamin A Dr ops (50./ml) page 2 Vitamin A [%] 5.otected pr from light) 100 Formulation 2 90 Formulation 1 80 70 0 3 6 Months BASF Pharma Ingredients Generic Drug Formulations 2001 9 12 .000 i.

6.8 Liquid Formulations (Lab scale)

Vitamin B Complex + Minerals +
Linoleic/Linolenic Acid Syrup

1. Formulation
I.

Evening primrose oil (see Remark) ...........5.0 ml
Cremophor RH 40 [1]..............................20.0 g
II. Water.....................................................41.0 g
III. Ferric citrate ...........................................60 mg
Manganese phosphate...........................300 µg
Thiamine hydrochloride (BASF) ..................3 mg
Riboflavin (BASF) ......................................4 mg
Cyanocobalamin, crystalline .....................10 µg
Nicotinamide ..........................................50 mg
Kollidon CL-M [1] .....................................5.0 g
Sucrose .................................................25.0 g
Citric acid ................................................0.5 g
Vanilla-flavour (Gunther) ............................0.2 g
Cyclamate sodium ....................................1.0 g
Saccharin sodium ...................................20 mg
IV. Kollidon 90 F [1] .......................................2.5 g
2. Manufacturing
Mix the primrose oil with Cremophor RH 40 heat to 60 °C and add
slowly the warm water II. Add the components III to the well stirred
solubilisate I/II. Finally add Kollidon 90 F to the obtained suspension
portionwise with stirring.
3. Properties
Appearance: ......Viscous yellow suspension (syrup)
pH:..................................................................3.3
Viscosity (25 °C): ...............16,000 –17,000 mPa · s
Rel. sediment volume: ................85 % after 1 week
Redispersibility:..............................................easy

BASF Pharma Ingredients Generic Drug Formulations 2001

Vitamin B Complex + Minerals + Linoleic/Linolenic Acid Syruppage 2
4. Remark
5 ml of Evening Primrose oil (Epopure‚, Prima Rosa, South Africa)
contain 3.5 g linoleic acid + 0.45 g gamma linolenic acid

BASF Pharma Ingredients Generic Drug Formulations 2001

6.8 Liquid Formulations (Lab scale)

Vitamin B Complex + Vitamin C Syrup, I
(2–3 RDA/10 g)

1. Formulation
I.

II.

Thiamine hydrochloride (BASF) ................60 mg
Riboflavin phosphate sodium...................55 mg
Nicotinamide ........................................250 mg
Dexpanthenol (BASF) ............................120 mg
Pyridoxine hydrochloride (BASF) ..............55 mg
Ascorbic acid, crystalline (BASF)............900 mg
Orange flavour .......................................25 mg
EDTA sodium ...........................................5 mg
Propyl gallate .........................................50 mg
Sorbic acid...........................................200 mg
Kollidon 25 [1] .............................................5 g
Sorbitol, crystalline [10] ..............................10 g
Glycerol ......................................................9 g
1,2-Propylenglycol [1] ................................10 g
Water .........................................................5 g
Sugar syrup DAB ......................................60 g
(sucrose + water, 64 g + 36 g)
Total amount ...........................................100 g

2. Manufacturing
Mix solution I with sugar syrup II. Adjust the clear solution to about
pH 4,2. Use nitrogen as an inert gas in the final packaging.

BASF Pharma Ingredients Generic Drug Formulations 2001

Vitamin B Complex + itamin
V
C Syrup, I (2–3 RDA/10 g)

page 2

3. Chemical stability (20–25 °C, dark)
The following vitamin contents were determined by HPLC.
Vitamin

B1
B2
Nicotinamide
Dexpanthenol
B6
C

0 Months

6 Months

9 Months

12 Months

100 %
100 %

100 %
100 %
92 %
95 %
100 %
94 %

95 %
100 %
96 %
88 %
100 %
90 %

87 %
90 %
92 %
90 %
100 %
not determined

100 %

BASF Pharma Ingredients Generic Drug Formulations 2001

82 %
92 %

88 %

6.8 Liquid Formulations (Lab scale)

Vitamin B Complex + Vitamin C Syrup, II

1. Formulation
I.

Thiamine hydrochloride (BASF) ................27 mg
Riboflavin phosphate sodium ..................27 mg
Nicotinamide ........................................125 mg
Dexpanthenol (BASF) ..............................55 mg
Pyridoxine hydrochloride (BASF) ..............27 mg
Ascorbic acid, crystalline (BASF)............400 mg
Orange aroma ........................................50 mg
EDTA sodium..........................................10 mg
II. Propylene glycol [1] ...................................30 g
+ water (2 + 1)
III. Parabene .............................................250 mg
Sorbitol, crystalline [10] ..............................15 g
Sucrose, crystalline..................................100 g
Water........................................................70 g
Total amount ...........................................216 g
2. Manufacturing
Dissolve the components I in mixture II. Prepare solution III by heating,
cool and mix with solution I/II. Adjust to pH 4,2 – 4,5. Use nitrogen as
inert gas during packaging.
3. Properties of the solution
Yellow clear taste full solution having a density of 1.23 g/ml (25 °C).

BASF Pharma Ingredients Generic Drug Formulations 2001

Vitamin B Complex + itamin
V
C Syrup, II

page 2

4. Chemical stability (20–25 °C, dark)
The following vitamin contents were determined by HPLC.
Vitamin

B1
B2
Nicotinamide
Dexpanthenol
B6
C

0 Months

6 Months

100 %
100 %
100 %
100 %
100 %
100 %

85 %
91%
100 %
88 %
100 %
89 %

BASF Pharma Ingredients Generic Drug Formulations 2001

9 Months 12 Months

85 %
91%
100 %
86 %
96 %


87 %
100 %
86 %
96 %
88 %

6.8 Liquid Formulations (Lab scale)

Vitamin B Complex Injectable Solution

1. Formulation
I.

II.

Thiamine hydrochloride (BASF) ...........1,100 mg
Riboflavin phosphate sodium.................660 mg
Nicotinamide .....................................4,400 mg
Pyridoxine hydrochloride (BASF) ............440 mg
Cyanocobalamin ....................................880 µg
EDTA, disodium salt................................20 mg
Propyl gallate .........................................50 mg
Kollidon 17 PF [1] ......................................10 g
Parabenes ............................................160 mg
Citric acid..........................................2,270 mg
Sodium hydroxide solution 1 molar ........21.6 ml
Hydrochloric acid 0.1 molar ...................72.0 ml
Propylene glycol [1] ...............................20.0 ml
Water for injectables .............................86.4 ml
Total amount ................................about 200 ml

2. Manufacturing
Dissolve the mixture I in the buffer solution II, keep it during 5 min under
nitrogen bubbles, filter through a 0.2 µm membrane and fill the clear
yellow solution in ampoules of 2 ml under nitrogen. The pH-value is about
4.
3. Stability (20-25 °C, dark)
The following vitamin losses were determined by HPLC.
Vitamin
B1
B2
Nicotinamide
B6

9 Months

12 Months

8%
6%
0%
9%

11%
10 %
0%
9%

BASF Pharma Ingredients Generic Drug Formulations 2001

6.8 Liquid Formulations (Lab scale)

Vitamin B Complex Syrup

1. Formulation
Thiamine hydrochloride (BASF) .............60.0 mg
Riboflavin 5-phosphate sodium ............55.0 mg
Nicotinamide .....................................250.0 mg
Dexpanthenol (BASF) .........................120.0 mg
Pyridoxine hydrochloride (BASF) ...........55.0 mg
Sorbic acid ........................................200.0 mg
EDTA sodium ........................................5.0 mg
Vanilline.............................................225.0 mg
Sucrose .................................................46.5 g
Kollidon 25 [1] ..........................................2.5 g
Glycerol ...................................................9.0 g
Propylene glycol [1].................................10.0 g
Water.....................................................31.0 g
2. Manufacturing
Dissolve the sucrose in the heat mixture of glycerol, propylene glycol and
water, cool to room temperature and dissolve the other components to
obtain a clear solution.
3. Stability (r
oom temperatur
e, HPLC)
Vitamin

Content after 1 year

B1
B2
B6
Nicotinamide
Dexpanthenol

BASF Pharma Ingredients Generic Drug Formulations 2001

80 %
75 %
97 %
97 %
92 %

6.8 Liquid Formulations (Lab scale)

Vitamin B1 + Vitamin B2 + Vitamin B3 +
Vitamin B6 Injectable Solution
(100 mg + 6 mg + 40 mg + 4 mg/2 ml)
1. Formulation
I.

II.

Thiamine hydrochloride (BASF) ................11.0 g
Riboflavin-5’-phosphate, sodium ...............6.6 g
Nicotinamide ..........................................44.0 g
Pyridoxine hydrochloride (BASF)................4.4 g
Parabene .................................................1.8 g
Citric acid ..............................................25.2 g
Sodium hydroxide solution, 1 molar ........240 ml
Hydrochloric acid, 0.1 molar ...................800 ml
Water for injectables ..............................960 ml

2. Manufacturing
Prepare solution II by heating and allow to cool before dissolving the
components of I in it. Flush 5 –10 min. with nitrogen, filter through a
0.22 µm membrane and fill into 2-ml ampoules under nitrogen.
3. Properties of the solution
A clear yellow solution was obtained having a pH of a about 4.0.
4. Chemical stability (20–25°C)
Vitamin
B1
B2
B3
B6

Content after 1 year (HPLC)
93 %
90 %
100 %
97 %

Vitamin B 12 was not stable in this formulation

BASF Pharma Ingredients Generic Drug Formulations 2001

6.8 Liquid Formulations (Lab scale)

Vitamin E + Selenium Veterinary Injectable
Solution (60 mg E + 3 mg Se/ml)

1. Formulation
I.
II.

Vitamin E acetate (BASF) ..........................6.0 g
Cremophor EL or Solutol HS 15 [1] ..........22.0 g
Preservative ...............................................q.s.
Sodium selenite......................................0.33 g
Water for injectables ..........................ad 100 ml

2. Manufacturing
Heat mixture I to about 60 °C, stir well and add very slowly the hot
solution II (60 °C).
After the ampoules have been heat-sterilized, they should be shaken for
a short time, while they are still hot, to eliminate any separation of the
phases that may have occurred. Sterilization can also be performed by
membrane filtration under pressure.
3. Properties of the solution
Clear or slightly opalescent, colourless liquid.
4. Remark
In Germany Cremophor EL must be declared on the package of
injectables.

BASF Pharma Ingredients Generic Drug Formulations 2001

6.8 Liquid Formulations (Lab scale)

Vitamin E Concentrate, Water-miscible (10%
= 100 mg/ml)

1. Formulation
I.
II.

Vitamin E acetate (BASF).........................10.5 g
Cremophor RH 40 [1]..............................25.0 g
Preservative ..............................................q. s.
Water................................................ad 100 ml

2. Manufacturing
Heat the mixture I and solution II separately to about 65 °C and add
mixture I slowly to the well stirred solution II (or solution II slowly to
mixture I).
3. Properties of the solution
Clear colourless liquid, miscible with water.
4. Physical stability (20–25 °C)
No change of appearance after 3 months.

BASF Pharma Ingredients Generic Drug Formulations 2001

6.8 Liquid Formulations (Lab scale)

Vitamin K1 (= Phytomenadione) Injectable
Solution (10 mg and 20 mg/ml)

1. Formulation
No. 1

No. 2

Phytomenadione ...........................................1.0 g
Solutol HS 15 or Cremophor EL [1].................6.5 g
Preservatives ..................................................q.s.
Water for injectables ....................................93.0 g

2.0 g
11.0g
q.s.
87.0 g

2. Manufacturing
Dissolve phytomenadione in Solutol HS 15 heated to about 60 °C and
add slowly the warm water. The sterilisation can be done by heat at
120 °C or by filtration. After the ampoules have been heat-sterilized, they
should be shaken for a short time, while they are still hot, to eliminate
any separation of the phases that may have occurred.
3. Properties of the solution
A clear colourless solution of low viscosity was obtained.
4. Physical stability (Formulation No. 1)
Stored at 40 °C and protected from light the heat sterilized solution did
not show any change of the clarity and colour after 12 weeks.
Stored at 20 – 25°C in the day light the heat sterilized solution did not
show any change of the clarity and colour after 12 weeks.
5. Remark
In Germany Cremophor EL must be declared on the package of injectables.

BASF Pharma Ingredients Generic Drug Formulations 2001

Cremophor A 6 and Cremophor A 25 are the most suitable in the BASF line of excipients for the development of macroemulsions with the appearance and the consistency of a cream. 7. with the result that care must be exercised in scaling up from a laboratory to a production scale. and Macrogol 6000.7 Semi-solid drugs (gels. Macrogol 1500. The size of the batch was usually 100 g. 7. They allow the production of physically stable formulations when they are used in low concentrations in the vicinity of 1 – 4 %. suppositories and ovula) 7. are intended as water-soluble base for suppositories and ovula. BASF Pharma Ingredients Generic Drug Formulations 2001 . Lutrol E 400. Macrogol 4000.2 Emulsifying agents in pharmaceutical creams The Cremophor types.1 Size of formulations and amounts used The formulations were developed on a laboratory scale. creams.3 Excipients as a base for suppositories and ovula In the formulations presented here. mixtures of the polyethylene glycols.

7 Formulations The formulations given in this chapter have been arranged in alphabetical order of their active substances. Data on the chemical stability are scanty. viscosity [mPa·s] 7. Rel. on applying heat at 45 °C. a gel reversibly exists whose consistency depends on the concentration of the Lutrol F 127.6 Stability The physical stability. No neutralization whatever is necessary. this point must be worked out in the final formulation. 6 that the gels are liquid at low temperatures i. 250 rpm) BASF Pharma Ingredients Generic Drug Formulations 2001 . In between these two values. in which case a stress test was always performed whose results represent a period of much more than 12 months at room temperature (20 – 25 °C). Preparations with PVP-iodine as disinfectant are an exception. Preservatives and fragrances were not always added. 7. 6 Influence of the temperature on the consistency of 20% Lutrol F 127 in water (rotary viscometer. in contrast to pastes and creams. A feature of these gels is their thermoreversible consistency. It is apparent from Fig. C Fig. gels are growing in importance in the pharmaceutical industry.4 Gel formers 7. deg. it can be visually ascertained that the active substance is dissolved. It allows the production of gels whose structures are stable in a pH range of 4 – 8.2 % sorbic acid is recommended. Consequently. the polyoxamer Lutrol F 127. was mainly determined on creams.e. This is often coupled with a guarantee of superior absorption. 2500 2000 Gel 1500 1000 500 0 10 15 20 Liquid 25 30 35 40 45 50 55 60 65 70 75 80 85 90 Temperature. because.5 Preservatives and fragrances At the present time. viz. For the gels based on Lutrol F 127 the addition of 0. The BASF line of pharmaceutical excipients includes a gel former.7. below 15 °C and at temperatures above 75 °C.

..............................64..19..... Add slowly Lutrol F 127 and continue stirring until Lutrol F 127 is dissolved. firm gel was obtained..........1.......9......... Lutrol F 127 [1] .... Maintain cool until the air bubbles escaped. Formulation I................................................. Properties of the gel A milky...... Water....... 3..9 Lutrol E 400 [1].5 Miglyol ® 812 (Dynamit-Nobel) .........0 III...... BASF Pharma Ingredients Generic Drug Formulations 2001 .....9 II...4........7 Formulations of semi-solid drugs (Lab scale) Aceclofenac Gel-Cream (1... Aceclofenac ... Manufacturing Mix the components I with water and cool to about 5 °C..........7 g g g g g 2............5%) 1...7....................

....4 g Propylene glycol [1] ......1. Cremophor RH 40 [1].......73.5........1 g Perfume ............. Aloe vera extract 200 fold .................................... 3. Lutrol F 127 [1] ... Properties of the gel Appearance Viscosity pH Physical stability clear · about 60 Pa · s about 5.......5 no change of appearance after 4 weeks at room temperature BASF Pharma Ingredients Generic Drug Formulations 2001 ........... Formulation I...............7 Formulations of semi-solid drugs (Lab scale) Aloe Vera Gel 1.......7.............s................................... Cool this mixture to < 10 °C (or heat to 70 – 80 °C) and dissolve III............ Water............ Manufacturing Prepare the solutions I and II separtely and add I onto II..........s....0 g 2.............q.6 g II.............. III............ Maintain the temperature until the air bubbles escaped.....q....0 g Preservative .....20....0........................................

.............. This basic cream was tested with different active ingredients soluble in 1....... Propylene glycol [1] ..............7 Formulations of semi-solid drugs (Lab scale) Basic Cream for Different Active Ingredients 1... Properties White cream.............0 Cremophor A 6 [1] ......7......0...12. Heat III until the active ingredient is dissolved...... Cetylstearyl alcohol............................0 Active ingredient .. BASF Pharma Ingredients Generic Drug Formulations 2001 ............ Add the water II to the obtained solution I with rigorous stirring...1 – 2. 4.....5 Cremophor A 25 [1] ........ Water ..................... mix with I/II and continue to stir during cooling to room temperature...................67.................... Formulation I.... Physical stability No change of appearance were observed during 6 weeks at 45 °C.....1...........7 III.2 II....2-propylene glycol.........0 g g g g g g g g 2..8..5 Liquid paraffin ......................... Manufacturing Heat the mixture I and the water II separately to about 80 °C.1.0........................................8 – 69. 3.........0 Parabene(s).............7......

....... Formulation I....0% + 0..............7 Formulations of semi-solid drugs (Lab scale) Benzoyl Peroxide + Alpha-Bisabolol Gel (5........................6......... Add III.....................2%) 1................3..................0 Water........... Manufacturing Prepare suspension II and let swell during one hour....7.... 3....................... natural (BASF) ..........0 Triethanolamine ......0 Water......................0 g g g g g g g g g 2............0 Cremophor RH 40 [1] .1.. BASF Pharma Ingredients Generic Drug Formulations 2001 ...0 Kollidon 30 [1] ............1...........0 III................2 Propylene glycol [1] .......... Carbopol 940 (Goodrich) ....5...0............. Properties of the gel Colourless transparent gel......................40..............3... Add this suspension to the well stirred solution I........................ Alpha-Bisabolol....8 II........40.. Benzoyl peroxide .

.10.00 Lutrol F 127 [1] .............. Maintain cool until the air bubbles disappeared.13 Neomycin sulfate . Formulation Betamethasone valerate .......................65 Lutrol E 400 [1] ....... Manufacturing Dissolve betamethasone valerate in the mixture of Lutrol E 400 and Miglyol 812... Dissolve Lutrol F 127 and neomycin sulfate in water at 5 –10°C.....00 g g g g g g 2...20.......0..............ad 100............6%) 1.....7............. BASF Pharma Ingredients Generic Drug Formulations 2001 .... 3...........7 Formulations of semi-solid drugs (Lab scale) Betamethasone + Neomycin Gel-Cream (0..........00 Water ...0..00 Miglyol ® 812 (Dynamit-Nobel) ..............1% + 0.15.......... Mix both solutions.................... Properties of the gel-cr eam A milky white soft gel-cream is obtained............................

.... 5...... Water............7..5 Liquid paraffin .............0 Betamethasone ....................................7 Formulations of semi-solid drugs (Lab scale) Betamethasone Cream (0..1%) 1..... BASF Pharma Ingredients Generic Drug Formulations 2001 ................5 Cremophor A 25 [1] ..... Properties White cream....0. 4.0 Cremophor A 6 [1] ................. Add the water II to the obtained solution I with rigorous stirring......... Formulation I......0..... 3.. Manufacturing Heat the mixture I and the water II separately to about 80 °C....................7 III..............7............1 g g g g g g g g 2..........................69.............2 II.....1....................... Heat III until the active ingredient is dissolved............ Remark This formulation could be used for other active ingredients too....8......... Physical stability No change of appearance or crystallization were observed during 6 weeks at 45 °C.12................... Propylene glycol [1] ...0 Parabene(s).1...... Cetylstearyl alcohol......... mix with I/II and continue to stir during cooling to room temperature.....................

........ Betamethasone valerate ..1 Ethanol 96 % ..... 4....... Maintain the temperature until the air bubbles disappeared...... 3......20.......... Remark Perhaps a certain amount of propylene glycol could be substituted by water.......0 Propylene glycol [1] ... Formulation I............0.......... BASF Pharma Ingredients Generic Drug Formulations 2001 ..0 g g g g g 2... II.......47.........................0 Water ....22.......................... Manufacturing Prepare the solution I at room temperature and solution II at about 6 °C (or at > 70 °C)............1%) 1.........7......10............ Mix both solutions.... Properties of the gel The obtained gel is clear and colourless.........7 Formulations of semi-solid drugs (Lab scale) Betamethasone Gel (0......0 Lutrol F 127 [1] ...........

...........5 Cremophor A 25 [1] ......0 Cremophor A 6 [1] ......7 Formulations of semi-solid drugs (Lab scale) Bifonazole Cream (1%) 1...........1...................... Formulation I............1...............12...........8.0 Bifonazole ....... Propylene glycol [1] ........... Water............ 5.................. 3............. 4..2 II.1............ Add the water II to the obtained solution I with rigorous stirring......................0 Parabene(s)......68.7.....0.... Manufacturing Heat the mixture I and the water II separately to about 80 °C........................ Heat III until the active ingredient is dissolved.............. Physical stability No change or appearance or crystallization were observed during 6 weeks at 45 °C...... mix with I/II and continue to stir during cooling to room temperature.7................................8 III......................................... Properties White cream......5 Liquid paraffin .. Cetylstearyl alcohol.... Remark This formulation could be used for other active ingredients too... BASF Pharma Ingredients Generic Drug Formulations 2001 ........0 g g g g g g g g 2.

........ Physical stability (4 months............ Properties of the gel A clear colourless gel is obtained....................................... stir well and add slowly Lutrol F 127 and water..30 Lutrol F 127 [1] ....7 Formulations of semi-solid drugs (Lab scale) Chlorhexidine Gel (2%) 1.. 4............2-Propylene glycol [1] .7.....22 Water.... 3.........................46 g g g g 2...........2 1............. Formulation Chlorhexidine diacetate . Manufacturing Dissolve chlorhexidine diacetate in propylene glycol at > 70 °C.. Maintain the temperature until the air bubbles escaped.......... BASF Pharma Ingredients Generic Drug Formulations 2001 ......... 40 °C) No change of the appearance...........

.......................... Cetylstearyl alcohol....2 II.........7.......1..............0 Parabene(s)............7 Formulations of semi-solid drugs (Lab scale) Clotrimazole Cream (1%) 1. Heat III until the active ingredient is dissolved........1.........8.................0............... Formulation I.......................................... Properties White cream............0 Cremophor A 6 [1] ........8 III....0 g g g g g g g g 2... Propylene glycol [1] ..................68............ 4.0 Clotrimazole ...5 Cremophor A 25 [1] ....7............. mix with I/II and continue to stir during cooling to room temperature.......... Manufacturing Heat the mixture I and the water II separately to about 80 °C..... Add the water II to the obtained solution I with rigorous stirring.......5 Liquid paraffin ......1....................... 5.............. Water... Physical stability No change of appearance or crystallization were observed during 6 weeks at 45 °C..12....... 3. Remark This formulation could be used for other active ingredients too.......................... BASF Pharma Ingredients Generic Drug Formulations 2001 ..

.... Manufacturing Dissolve dexpanthenol and Lutrol E 400 in water.... Add slowly Lutrol F 127 and stir until it is dissolved. Physical stability (3 months............. 4..................18 Water...... 40 °C) No change of the appearance and viscosity................................................. add liquid paraffin and stir heating to 60 – 70°C........ Properties of the gel Soft turbid gel-cream..........5 Liquid paraffin ...52 g g g g g 2.............7 Formulations of semi-solid drugs (Lab scale) Dexpanthenol Gel-Cream (5%) 1......15 Lutrol F 127 [1] ................ BASF Pharma Ingredients Generic Drug Formulations 2001 ........................... Cool to room temperature stirring continously when the air bubbles disappeared....................... 3.......7.... Formulation Dexpanthenol (BASF)..............10 Lutrol E 400 [1].....

........................ BASF Pharma Ingredients Generic Drug Formulations 2001 ..............1 Propylene glycol [1] ............................................57 g g g g 2.22 Water.........7 Formulations of semi-solid drugs (Lab scale) Diclofenac Gel (1%) 1..............20 Lutrol F 127 [1] ..... Manufacturing Dissolve Lutrol F 127 in water at 4 – 6 °C (or at > 70 °C) and mix with the solution of diclofenac sodium in propylene glycol. Properties Colourless clear gel...... Formulation Diclofenac sodium ........... 3.........7............................ Maintain the temperature until the air bubbles disappeared..............

.... 3..... Properties White................. BASF Pharma Ingredients Generic Drug Formulations 2001 ......................15 Miglyol 812 (Dynamit-Nobel) .......... Maintain the temperature until the air bubbles escaped..... add the mixture of water and Miglyol 812.......... Manufacturing Dissolve diclofenac sodium in propylene glycol.............. turbid gel-cream..................54 g g g g g 2....20 Water.........7.7 Formulations of semi-solid drugs (Lab scale) Diclofenac Gel-Cream (1%) 1...................................... Formulation Diclofenac sodium .......................10 Lutrol F 127 [1] ................. Dissolve Lutrol F 127 in this well stirred mixture at 4 – 6 °C (or at > 70 °C).1 Propylene glycol [1] ........

................ BASF Pharma Ingredients Generic Drug Formulations 2001 ... Manufacturing Heat solution I to about 70 °C.....1 Lutrol E 400 [1]...... 3... mix with III and cool when the air bubbles escaped..........7 Formulations of semi-solid drugs (Lab scale) Erythromycin Gel (1%) 1................ Properties of the gel A clear soft gel is obtained....20 III........................7.........20 II... Water.................................................. dissolve II..............39 g g g g g 2.................20 Propylene glycol [1] .................... Lutrol F 127 [1] .................... Erythromycin base..... Formulation I.

.....7.......... stir and cool to 6 °C..7 Formulations of semi-solid drugs (Lab scale) Heparin Gel-Cream (300 i.............. Heat to room temperature when the air bubbles escaped. add Lutrol E 400 and liquid paraffin.......................23 g Water ...................ad 100 g 2....... Add slowly Lutrol F 127 and stir until it is dissolved./g) 1......... Formulation Heparin sodium ....................u.186 mg Lutrol E 400 [1]... BASF Pharma Ingredients Generic Drug Formulations 2001 ...............10 g Lutrol F 127 [1] ............................ Manufacturing Dissolve heparin sodium in water......................................15 g Liquid paraffin ..........................

... Continue to stir until the gel is cool. Properties Clear colourless gels...5 g Water ......... Formulations No..7 Formulations of semi-solid drugs (Lab scale) Hydrocortisone Aqueous Gels (1%) 1..... Triethanolamine .......... Carpopol 940 (Goodrich) .7...................................7...0 g – – I..........0 g III....................1........2 g 1....... 1: Suspend I in the mixture II at 70 °C.0....0........................5 g IV..s.......................8 g Water.............q...... Manufacturing Formulation No.0 g V..........s............................................. Preservative ........5........49..................0 g Lutrol E 400 [1]..... 3..................................... dilute with the solution IV.................. 2: Suspend I in the mixture II at 70 °C.....0 g Cremophor A 25 [1] ................. Add solution V and continue to stir until the gel is cool....0 g 20...... Prepare solution IV..................... heat to 70 °C.. II........... heat to 70 °C and add slowly to the hot mixture I/II. 1 No.... 2 Hydrocortisone acetate ... Formulation No............ Prepare solution II. 64....0 g – 15.................. 2.0 g – – q...........– Cremophor RH 40 [1] .............. Water ........ and add slowly to the hot mixture I/II...10.........26... BASF Pharma Ingredients Generic Drug Formulations 2001 ...

....1.. Properties White cream.... BASF Pharma Ingredients Generic Drug Formulations 2001 .........7 Formulations of semi-solid drugs (Lab scale) Hydrocortisone Cream (1%) 1........ 3............... 5.....................5 Liquid paraffin .......................... Physical stability No change of appearance or crystallization were observed during 6 weeks at 45 °C............1.........................68...... Formulation I.1.0 Parabene(s).......... Add the water II to the obtained solution I with rigorous stirring............0...7....8 III........ Cetylstearyl alcohol........7........ mix with I/II and continue to stir during cooling to room temperature................0 Cremophor A 6 [1] ......0 Hydrocortisone... Propylene glycol [1] ..........................................2 II....... Remark This formulation could be used for other active ingredients too....8.......................5 Cremophor A 25 [1] .............. Water... 4...... Heat III until the active ingredient is dissolved..................12.... Manufacturing Heat the mixture I and the water II separately to about 80 °C.0 g g g g g g g g 2..........

....0.....5 Water................. 3...9 Water ......5 g g g g g g g 2........5 Cremophor RH 40 [1] .............7......0 Carbopol 940 (Goodrich) .......60................ colourless gel............6 Ethanol 96 % ...... II..........................................6...............0................................... Properties Clear............................5%) 1................. Hydrocortisone acetate......7 Formulations of semi-solid drugs (Lab scale) Hydrocortisone Ethanolic Gel (0............ BASF Pharma Ingredients Generic Drug Formulations 2001 .....7...0 Triethanolamine ...0............ Manufacturing Prepare solution II and mix slowly with solution I.. Formulation I..24.........

...... Die Creme wird bis zum Erkalten gerührt und das verdampfte Wasser ersetzt...................50 Teile Teile Teile Teile Teile In das auf dem Wasserbad auf etwa 70 °C erwärmte Gemisch von Polysorbat 60............................44 IV.............................................. Maintain cool until the air bubbles escaped.... Lutrol F 127 [1] ......7 Formulations of semi-solid drugs (Lab scale) Ibuprofen Gel-Cream (5%) 1.......... Formulation I................................................ Water...... Nonionic hydrophilic Cream (DAB 1996)*.............................. Die Creme kann mit 0............. Cetylstearylalkohol und Weißem Vaselin wird die auf gleiche Temperatur erwärmte Mischung der übrigen Bestandteile in Anteilen eingearbeitet..12 III.......... *Nichtionische hydr ophile Creme (DAB 1996) Polysorbat 60 .................... Manufacturing Prepare solution I and coll to about 8°C.......1 Prozent Sorbinsäure konserviert werden.................... Das für die Herstellung verwendete Wasser soll vor Gebrauch frisch aufgekocht werden........7....... BASF Pharma Ingredients Generic Drug Formulations 2001 .5 Cetylstearylalkohol ......................10 Glycerol 85 % ........................................10 Weißes Vaselin.....5 Propylene glycol [1] ............12 II........................................25 Wasser.15 g g g g g g 2.. Dissolve II and add III and IV.......................12 Isopropanol . Ibuprofen (BASF) ......

......... The gel of formulation No......7......... 2 is less sticky than formulation No........ Formulations No...........s....7 Formulations of semi-solid drugs (Lab scale) Ibuprofen Gels (5%) 1...5 g Ethanol 96 % . Isopropyl myristate .... Lutrol F 127 [1].. 1................. Properties of the gel A colourless clear gel was obtained..................................................... 3............ 4....... cool to 40°C and add solution I.– Preservative .s....20 g II...................................q.......... 2.................... 59 g I.... BASF Pharma Ingredients Generic Drug Formulations 2001 .................. Remark The function of isopropyl myristate is the reduction of the stickness....... 1 No...... Water ..................43 g 5g 10 g 10 g 15 g 1g q................... 2 Ibuprofen (BASF).........10 g Propylene glycol [1] .................................. Manufacturing Dissolve II in III at 70°C under vacuum.......22 g III........................

... 40 °C) No change of appearance......................74 g g g g 2......... 4...1 Cremophor RH 40 [1]....... Cool to room temperature.... add slowly the water (60 – 70°C) stirring well the mixture and dissolve Lutrol F 127... Manufacturing Dissolve indomethacin in Cremophor RH 40 at 60 – 70°C.................................................. I 1.......10 Lutrol F 127 [1] .15 Water.. Formulation Indomethacin ... Properties of the gel A clear soft gel was obtained.... BASF Pharma Ingredients Generic Drug Formulations 2001 .... 3.......7..................7 Formulations of semi-solid drugs (Lab scale) Indomethacin Gel (1%)......... Physical stability (4 weeks..................................

0 g II.20..0 g – 15..0 g 39.............0 g 23...21......0 g Ethanol 96 %.. 1 No.........7 Formulations of semi-solid drugs (Lab scale) Indomethacin Gel (1%)..............0 g 22.....................0 g I. 2. Water . 1: No change during 1 year at room temperature. Lutrol F 127 [1].– Lutrol E 400 [1] ...0 g Propylene glycol [1] ..... Formulation No....................20.... Physical stability Formulation No....................................38.............. 2 Indomethacin ... 3...... mix with III and cool................... II 1....7.....................................1. 2: No change during 12 weeks at 40 °C........0 g 1.. BASF Pharma Ingredients Generic Drug Formulations 2001 ....... Formulations No........ 23 °C and 6 °C........... dissolve II well stirring about 30 minutes.................. Manufacturing Heat solution I to about 70°C....................... It forms a clear yellow gel.0 g III......

pH in both Pluronic and aqueous solutions. No. the rates of hydrolysis of indomethacin (Sigma-Chem.“ BASF Pharma Ingredients Generic Drug Formulations 2001 . Suec.. The degradation of indomethacin followed 1st order kinetics. with linear plots of the 1st order rate constant vs. II page 2 4.Indomethacin Gel (1%). 2.) were considerably slower in Pluronic F 127 (BASF) gels than in buffer alone. Kiryu S. 25. allowing prediction of the time required for degradation of indomethacin.: Acta Pharm. Chemical stability Lutrol F 127 (= Pluronic ® F 127) stabilizes indomethacin against hydrolisis as shown in the following publication summary: Hydrolysis of Indome thacin in Plur onic F 127 Gels Tomida H. Kuwada N.. 87 – 96 (1988) „In drug stability studies.

......7..... 3........................................s..................slightly yellowish BASF Pharma Ingredients Generic Drug Formulations 2001 .......... Manufacturing Prepare solution II............0 g Macrogol 6000 ..................................... Properties of the suppositories Weight: ..............3 mg Water.........141........ II....q............................................................0 g Butylhydroxytoluene ......................... mix with the melted mixture I and fill into the moulds of suppositories........... Indomethacin ................7 Formulations of semi-solid drugs (Lab scale) Indomethacin Suppositories (50 mg) 1......14............................ Macrogol 4000 .........0 g 2..6 g Colour:......1..0 g EDTA ...............16......... Formulation I.....5..3.....

... Formulation I......7............22 g g g g 2.. Lidocain hydrochloride... heat to 70 °C or cool to 6 °C and add slowly II to the well stirred solution until it is dissolved....................2 Water................... Properties of the gel A clear colourless gel was obtained...... 20–25 °C) No change was observed..................7 Formulations of semi-solid drugs (Lab scale) Lidocain Gel (2%) 1................... II.......56 Propylene glycol [1] ... Physical stability (3 months........... 4.... BASF Pharma Ingredients Generic Drug Formulations 2001 ... 3............................. Manufacturing Prepare solution I at room temperature......... Maintain the temperature until the air bubbles escaped...20 Lutrol F 127 [1] ...

.................... Lutrol F 127 [1] ......... BASF Pharma Ingredients Generic Drug Formulations 2001 ....... Heat to 70 °C or cool to 6 °C and add slowly III to the well stirred solution until it is dissolved. Manufacturing Prepare solution I at room temperature and mix with II........... Maintain cool until the air bubbles escaped..... Lidocain hydrochloride..........................7 Formulations of semi-solid drugs (Lab scale) Lidocain Gel-Cream (5%) 1......................... 3.....5 Water... Physical stability (3 months. Liquid paraffin ...15 II.........50 Propylene glycol [1] .............. Formulation I..........10 III..............7......................... 20–25 °C) No change was observed............................20 g g g g g 2......

.11 Menthol ....................... Remark Reducing the concentration of the active ingredients the amount of Lutrol F 127 could be reduced too and the consistency of the gel will be normal.... Manufacturing Dissolve II in solution I and mix with III........ Water........ BASF Pharma Ingredients Generic Drug Formulations 2001 ....... Properties of the gel Due to the high concentration of the active ingredients and of Lutrol F 127 the consistency of the colourless clear gel is extremely hard..7 Formulations of semi-solid drugs (Lab scale) Methyl Salicylate + Menthol Gel (11% + 5%) 1...5 Lutrol E 400 [1]................... Lutrol F 127 [1] ...................... 3..............................7 II.................................................................................6 Propylene glycol [1] ............................ 4.......19 g g g g g g g 2...................... Methyl salicylate ..........7......32 III.............. Formulation I...20 Cremophor RH 40 [1] .................. The clear gel can be diluted with water..

....... Formulation I.....8 g g g g 2......7...................................2 Lutrol F 127 [1] .... 3....0 Water .... Metronidazole ..........................2%) 1.37.......40...... BASF Pharma Ingredients Generic Drug Formulations 2001 . Properties of the gel A clear colourless gel was obtained............... Manufacturing Heat mixture I to 70 – 80 °C and slowly add the water heated to about 70 °C........... II........1..............0 Lutrol E 400 [1].. Maintain the temperature until the air bubbles disappeared.......21......7 Formulations of semi-solid drugs (Lab scale) Metronidazole Vaginal Gel (1...................

..8.......5 Liquid paraffin ..... 3..0..............12........... Remark This formulation could be used for other active ingredients too...................1 II..1..........0 Parabene(s) . Water ...... Cetylstearyl alcohol.. Propylene glycol [1] ....................5 Cremophor A 25 [1] ..............................7................... Manufacturing Heat the mixture I and the water II separately to about 80 °C....0 g g g g g g g g 2....... Formulation I........ mix with I/II and continue to stir during cooling to room temperature........7......... Add the water II to the obtained solution I with rigorous stirring.................7 Formulations of semi-solid drugs (Lab scale) Miconazole Cream (2%) 1.......1...................... BASF Pharma Ingredients Generic Drug Formulations 2001 ....................8 III....... 4.. Physical stability No change of appearance or crystallization were observed during 6 weeks at 45 °C...... Properties White cream..................0 Miconazole nitrate .. Heat III until the active ingredient is dissolved....0 Cremophor A 6 [1] ...2.....................67. 5.......................

.......1 II................0 III. Formulation I........52.......................... Let cool to room temperature when the air bubbles escaped.............. Kollidon 90 F [1] .....0 Saccharine sodium ..........3 Water....0 Cremophor RH 40 [1] . clear and soft gel was obtained having a orange like taste and a slightly bitter after taste............2.0........10.......7.... 3...........6 g g g g g g g g 2.................... Miconazole nitrate (Sigma) ...............20...........5..0 Orange flavour........... Lutrol F 127 [1] ....................7 Formulations of semi-solid drugs (Lab scale) Miconazole Mouth Gel (2%) 1........0 Propylene glycol [1].....0................... Manufacturing Dissolve I in the molten mixture II..................... BASF Pharma Ingredients Generic Drug Formulations 2001 ............ Properties of the gel A colourless....10............ Heat solution III to 90 °C and mix slowly with I/II.....................

.............35 mg (BASF) Nicotinamide .........353 mg Folic acid ............................................................ Formulation I.................. Manufacturing Heat mixture I to about 60 °C to obtain a clear solution..........about 1000 g 2.....1..........177 mg Cyanocobalamin gelatin coated 1% .................... add V and stirr until all Lutrol F 127 is dissolved.............. cool to about 6 °C.........................438 mg Manganese chloride (4 H 2 O) ....7.................300 mg Ferrous sulfate (7 H 2 O) ...20 g II........ BASF Pharma Ingredients Generic Drug Formulations 2001 ............... add slowly the water II to the well stirred solution I................................................7 Mio......110 mg 1...............353 mg EDTA sodium................./g (BASF) Vitamin E acetate (BASF)...................... Thiamine hydrochloride (BASF) ..... Water......725 g III...355 mg Riboflavin (BASF) ............ Kollidon 90 F [1] ... i................................100 g V Lutrol F 127 [1] ........060 mg Butylhydroxytoluene.................. dissolve III and IV in this mixed solution at room temperature......... Vitamin A palmitate ..........100 g Total amount: .............35 mg Dexpanthenol (BASF) ..................................................................u...500 mg Cremophor RH 40 [1] ..................7 Formulations of semi-solid drugs (Lab scale) Multivitamin Oral Gel 1......... Maintain the cool temperature until the air bubbles escaped.............50 g Lutrol F 127 [1] ............638 mg Potassium iodide .........35 mg Pyridoxin hydrochloride (BASF) .................................................115 mg IV..

.....................opalescent pH-value.......................Multivitamin Oral Gel 3.... Properties of the gel Colour .....3 Consistency...................4.........yellow-orange Clarity ...........................semi-solid BASF Pharma Ingredients Generic Drug Formulations 2001 page 2 .......................................................................

.........0 g I.u......30 mg 1..about 100 g 2.................7 Formulations of semi-solid drugs (Lab scale) Multivitamin Oral Gel with Linoleic Acid and Linolenic Acid 1......... i.... Properties A clear yellow gel was obtained.........50 mg Ascorbic acid......7 Mio.....3 mg Riboflavin (BASF) ........u............. crystalline (BASF) ...............150 µg Cremophor RH 40 [1]...... Total amount: .......0 g Lutrol F 127 [1] ..............................19 mg Vitamin D 3 40 Mio i......... crystalline .... Thiamine hydrochloride (BASF) .5............................0 g II..0 ml Vitamin A palmitate ......55....... Dissolve at 20 – 25 °C the components III in this clear solution I/II... Manufacturing Prepare mixture I and heat to about 65 °C........................................ Lutrol F 127 [1] .3 mg Pyridoxin hydrochloride (BASF) ........15 mg Cyanocobalamin.............................5....0 g III............20..7.... BASF Pharma Ingredients Generic Drug Formulations 2001 ...... Cool the obtained solution to about 5 °C and dissolve the rest of Lutrol F 127 (= IV)............... Formulation Evening Primrose Oil (Epopure ® ............1.....0 g IV.. Add the warm water II (65 °C) slowly to the well stirred mixture I.......... Water..............10 mg Nicotinamide .................. 3........................../g ...... Prima Rosa/SA) ................... Maintain the cool temperature until the air bubbles escaped.................................10 µg Calcium D-pantothenate (BASF) .......14..................../g (BASF) Vitamin E acetate (BASF)...........

BASF Pharma Ingredients Generic Drug Formulations 2001 .Multivitamin Oral Gel with Linoleic Acid and Linolenic Acid page 2 4.45 g gamma-linolenic acid.5 g linoleic acid and 0. Remark 5 ml of Evening Primrose Oil Epopure contains 3.

..........05 Propylene glycol [1] . Formulation Neomycin sulfate ... cool to 5-10 °C........20........ add the propylene glycol and dissolve neomycin sulfate.......................74..0..7..... Properties of the gel A clear semisoft gel was obtained.................... 4......... Cool to room temperature when the air bubbles escaped.. dissolve Lutrol F 127............5 Lutrol F 127 [1] .. add propylene glycol and dissolve neomycin sulfate........ 3..05%) 1................................... Yellowish at 45 °C... Manufacturing Dissolve the parabenes and Lutrol F 127 in water heated to about 80 °C......................0 Water..7 Formulations of semi-solid drugs (Lab scale) Neomycin Gel (0...5 g g g g g 2...5....... Physical stability (6 weeks) No change at 6 °C and 23 °C......0 Parabenes ...............0..... BASF Pharma Ingredients Generic Drug Formulations 2001 ....... Alternative: Dissolve parabenes in hot water... Maintain the cool temperature until the air bubbles escaped....

..........0 g 2.......... 3..2 g Lutrol E 400 [1] ..... fine powder .................7 Formulations of semi-solid drugs (Lab scale) Paracetamol (= Acetaminophen) Suppositories (150 mg and 500 mg) 1...............4 g Aerosil 200 [4] ........................................15.........7............. 20 °C or 40 °C..... No... BASF Pharma Ingredients Generic Drug Formulations 2001 ............0........ 1 150 mg No...... Fill the molten mass in the moulds of suppositories......................................0 g 80. Properties of the suppositories Weight ......................129...... Formulations I......... 1) No crystallisation after the storage of 6 weeks at 6 °C...............0 g – 10. Physical stability (Formulation No..... II.colourless 4.2...............easy Colour .. Manufacturing Melt the mixture II and suspend the mixture I............0 g Macrogol 4000 ....– Macrogol 1500 .0 g 60............0 g Solubility in water ....................................4 g 50.................. 2 500 mg Paracetamol...............55.....

.5 1..........5% + 5... cool to room temperature when the air bubbles escaped and adjust the pH to about 8................0 Ethanol 96 % .......... add the rest of the water........ Formulation Piroxicam (Sigma)... 3.................... adjust the pH with triethanolamine to about 7......7.0%) 1..........2-Propylene glycol [1] ...........0 Triethanolamine... Properties of the gel A clear colourless gel was formed having a pH of about 8...25.......................... Maintain the cool temperature until the air bubbles escaped........0... add ethanol and Lutrol F 127.........................7 Formulations of semi-solid drugs (Lab scale) Piroxicam + Dexpanthenol Gel (0....46. Alternative mode of preparation: Dissolve piroxicam in propylene glycol.......about 0.. Remark The addition of ethanol is not essential because it reduces the viscosity.......0 g g g g g g g 2.......... Manufacturing First mode of preparation: Prepare the solution of piroxicam in propylene glycol and dexpanthenol at 70 – 80°C..... BASF Pharma Ingredients Generic Drug Formulations 2001 ................ 4...... Cool the mixture of Lutrol F 127 and water to about 5 °C and mix with the piroxicam solution................5.. Stirr the highly viscous mixture.5.. Add the ethanol.... dexpanthenol and triethanolamine...............0 Water.23..........0 Dexpanthenol (BASF)...4 Lutrol F 127 [1] ............ add 50 % of the hot water (70°C).

........2..................7................000 mPa · s pH value (20 % in water) .. Stability (14 days.. Lutrol F 127 [1] ..............51......15.......9 IV.61....0 Sodium chloride .. Formulation I.54...7....... PVP-Iodine 30/06 (BASF) .... Manufacturing Dissolve the solids (I) in water (IV)...s pH value (20 % in water) ....20...... Sodium hydroxide solution...............7 4.....1 g g g g g g 2........................4......7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine + Lidocain Gel (10%) 1..000 mPa... 23 °C)....10. cool to about 6 °C....................1.0 Lidocain hydrochloride..... Maintain the cool temperature until the air bubbles escaped....1............4 Loss of available iodine.....................0 II......0 III................. 23 °C)...... 3.5 % BASF Pharma Ingredients Generic Drug Formulations 2001 .................... 1 molar ..... Properties of the gels Viscosity (Brookfield.... dissolve Lutrol F 127 (II) and adjust the pH value with the sodium hydroxide solution (III)........... 52 °C) Viscosity (Brookfield........ Water ....................

......................... mix the solution with the fragrance and the syndet base...10 Water.......................... Heat the area of the 2 disks is to 50 °C by a heating collar..7.. Pass the blend 4 x through a three-roller mill... 3..75 Syndet base (see Remark) ............. Remark Composition of the syndet base (sequence of concentration): Disodium lauryl sulfosuccinate Sodium lauryl Sulfate Cetylstearyl alcohol Paraffin Glycerol stearate Water Titanium dioxide BASF Pharma Ingredients Generic Drug Formulations 2001 ........... Formulation PVP-Iodine 30/06 (BASF) . Give the blend 3 times through a plodder with a narrow sieve hole disk...............50 Fragance....... Cut the bar in pieces on a Lab stamper..........................940 g g g g 2......... Pass the blended material through a wide sieve hole disk combined with a mouth hole disk..... Manufacturing Dissolve PVP-Iodine in water..........7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine Bar Soap (5%) 1.........

...............19......................0 g 15........3 g Glycerol monostearate.............. 3..........7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine Bar Soaps (5%) 1....... 2 PVP-Iodine 30/06 (BASF) ..0 g Texapon K 12 (Henkel) ....48..........5 % BASF Pharma Ingredients Generic Drug Formulations 2001 .. Manufacturing Heat mixture II to 75 – 80 °C and cool to about 50 °C well stirring..0 g Paraffin (56 – 58 °C) . Chemical stability (40 °C during 4 weeks) No..45.............1% 11....1 (Wilco) ........3 g Emcol ® 4400..... Pass the blend four times through a three-roller mill and let dry over night at room temperature........0 19.– Cetylstearyl alcohol ..29.............. 2 Loss of available iodine ............2 g 10................ II.......... Formulations I............... 1 No.................................... Add solution I and let cool to room temperature continuously stirring.......3 g 48. 1 No............... Cut the bar in pieces on a Lab stamper.........3 45..............0 g 48....... No.48..15...................0 g Water............2 – g g g g 2..........9...............3 29...3 g Setacin ® F special paste (Zschimmer + Schwarz) .10..7..

..2.................1 Na 2 HPO 4 solution 0.....10...............2..... BASF Pharma Ingredients Generic Drug Formulations 2001 ..............2 % During this stress test at 52 °C the emulsion was separated into two phases...7...............0 Liquid paraffin.0 Cetylstearyl alcohol.........5.. II...................2 molar ............36..1 molar ... 3................ PVP-Iodine 30/06 (BASF) .....24......0 Cremophor A 25 [1] ....... Properties of the cr eam Brown cream having a pH of 4.......10.......... Formulation I. Stir in the PVP-iodine dissolved in the buffer solutions (I)...0 g g g g g g g g 2........7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine Cream (10%) 1..............1 0.....99 % 9...5 1. Chemical stability pH Available iodine Loss of iodine After production After 14 days/52 °C 4....... Manufacturing Prepare a basic cream from the emulsifying agents and the fatty substances (II)..... 4................9 Cremophor A 6 [1] .........5...0 Citric acid solution 0.09 % – 4..................0 Glycerol ....10............

. Lutrol F 127.........0 g g g g g g g 2......0 III.0 V.....0 Citric acid solution.....................4 Available iodine 1.....5.95 % 5% 122......1 Lutrol E 400 [1].15.. mix with III and dissolve IV at about 20 °C.......7....0 IV.... PVP-Iodine 30/06 (BASF) .........000 mPa · s 3..... Properties Brown turib gel... 0......0 % Loss of iodine – Viscosity (Brookfield) 113......1 0........ Formulation I. II.... Maintain cool until all air bubbles disappeared...... 3.........9 NA 2 HPO 4 · 12H 2 O solution.. Cool to 5 – 8 °C and dissolve V..... 0............1 molar .... Liquid paraffin...1 0..... Lutrol F 127............18.7.....2 molar ......... Chemical stability (20–25 °C) 0 Months 3 Months 6 Months pH 3..........35..10........99 % 1% 124..... Manufacturing Dissolve I in solution II..... 4......7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine Gel-Cream (10%) 1......000 mPa · s 3.........000 mPa · s BASF Pharma Ingredients Generic Drug Formulations 2001 .....10..........

.......... Properties of the gels No.....2 4... Sodium hydroxide solution.....000 mPa · s 1.................. 1 I..– II.– IV...0 g Sodium chloride ...................... 52 °C) Viscosity (Brookfield........ 2 4.. 1 No......... 1 molar .0 20....10.......0 7.. 2 61..7 8.0 1..20. Manufacturing Dissolve the solids (I) in water (IV)...... dissolve Lutrol F 127 (II) and adjust the pH value with the sodium hydroxide solution (III).....9 10.9 61..000 mPa · s 54....7... 23 °C) pH value (20 % in water) Loss of available iodine 58...000 mPa · s 2....... Maintain cool until all air bubbles escaped...0 g No....... PVP-Iodine 30/06 (BASF) .0 % BASF Pharma Ingredients Generic Drug Formulations 2001 ....70. cool to about 6 °C.........6 No....... Formulations No.......000 mPa · s 45..0 g III.... 3..7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine Gels (10%) 1.1 g g g g g 2...2 % 2. Lutrol F 127 [1] . 1 Viscosity (Brookfield.. Stability (14 days........ 2 10.. 23 °C) pH value (20 % in water) No.... Water............

............. 5 – 7) 1.. 1987.... Properties of the ointment Brown viscous and turbid paste..................287 % 1.................5%) (According to R.... Chemical stability After After production 14 days/52 °C Available iodine Loss of iodine 0.4 % 5....4 Glycerol .............0...0... II......84.9 Macrogol 4000 .....3..... 3....7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine Glucose Ointment (2.6 Water......... Remark A similar formulation using sucrose instead of glucose is mentioned in the European Patent 0258761 (Kowa)..... M......Asanger.......7.................291% – 0.............................................Dolder. Formulation I...................6 g g g g g g 2......... Manufacturing Dissolve macrogol 4000 in the hot mixture of glycerol and water and add the glucose warmed to 60 – 80 °C....... 4.6 Ethanol 96 % ......................... PVP-Iodine 30/06 (BASF) .........2.............3..5 Glucose .4.. Febr..... Incorporate solution (I) in the obtained paste.. APV-Pharmazie in der Praxis No.... BASF Pharma Ingredients Generic Drug Formulations 2001 ....

.......................... Formulation I...............23 Solid paraffin (mp.............. II........................... 50/55 °C) ... Luvitol EHO [1] .............22 Cetyl alcohol ........15 Cremophor RH 40 [1] ...7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine Lipstick or After Shave Stick (10%) 1.... PVP-Iodine 30/06 M 10 (BASF)........18 Sicovit Titanium dioxide [1] ..................6 III............7.... 3.... Manufacturing Melt the mixture III at 60°C............................................5 Bees wax ................................. stir it into the suspension II and finally add I.......10 White Mineral Oil .................................. Properties Brown homogeneous sticks BASF Pharma Ingredients Generic Drug Formulations 2001 .... When a homogeneous suspension has been obtained cast the sticks in preformed moulds..1 g g g g g g g g 2........

Stability (52 °C.............................. Propylene glycol [1] ................................................................................ Manufacturing Dissolve PVP-Iodine I in the solvents III....................................2 Cremophor A 25 [1] ............7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine Mastitis Cream for Cattles (10%) 1.................. II..........10 Cetylstearyl alcohol........... BASF Pharma Ingredients Generic Drug Formulations 2001 .......53 – 56 g g g g g g g g 2.........................10 Liquid paraffin ..................... stir the solution I/III in the molten mixture II and cool by stirring.... 3.... Mix the components II by heating.............2 III....5 – 8 Cremophor A 6 [1] .. Formulation I..7. 14 days) The cream is physically stable and shows no loss of iodine.............. PVP-Iodine 30/06 (BASF) ...........................5 Water ..10 Vaseline .......

...........96...........31....2............... Formulation PVP-Iodine 30/06 (BASF) .... Viscosity (Brookfield.........500 mPa · s BASF Pharma Ingredients Generic Drug Formulations 2001 ..........5 g 2....... Properties of the gel Appearance................................7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine Soft Gel (1%) 1.. Manufacturing Dissolve PVP-Iodine and Natrosol HR 250 in the well stirred water........ 3.5 g Water.... 23°C)...Clear brown gel.....................0 g Natrosol 250 HR (Hercules) ...1....7..

.. 52 °C) The content of available iodine dropped only to 99 % and the pH to 3..4 Macrogol 4000 .6 Water.0 g g g g g 2..................7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine Transparent Ointment (10%) 1..... 4...10...........0..60. PVP-Iodine 30/06 (BASF) ............0 Sodium hydroxide.......0 Lutrol E 400 [1]...........7..6..... Manufacturing Prepare solution I......................... Properties Transparent ointment like a gel having a ph of 4.... Miscible and washable with water......25............ 1 molar solution .... BASF Pharma Ingredients Generic Drug Formulations 2001 ... Stability (14 days..... II..................4.. incorporate II stirring very well and cool to room temperature.. 3.............. heat to about 60 °C... Formulation I.........

.... 3.... Properties Homogeneous brown coloured ovula..............– Macrogol 4000 ....................... Stir in the micronized PVP-Iodine product in small portions into the melt. 4..... pour it into polyethylene moulds to produce suppositories. each of 2 g weight.................. Chemical stability In a stress test (14 days/52 °C) and at room temperature (one year) no loss of available Iodine were measured.. Formulations 5% PVP-Iodine 30/06 M 10 (BASF) .......................... BASF Pharma Ingredients Generic Drug Formulations 2001 ...........85 g 10% 10 5 50 35 g g g g 2.... Manufacturing Melt the macrogols by gentle heating.........7 Formulations of semi-solid drugs (Lab scale) Povidone-Iodine Vaginal Ovula (5% and 10%) 1..... After a uniform suspension has been obtained...................7............10 g Macrogol 1500 ..5 g Lutrol E 400 [1]....

..... 3....................................... Tretinoin (BASF)................................. 4...04 g (-)alpha-Bisabolol............... Heat to about 50 °C and dissolve about 14 g of III in the combined solution I/II..5 g 2......3 g Preservatives..18.....0 g Butylhydroytoluene ........... Maintain cool until the air bubbles escaped.. BASF Pharma Ingredients Generic Drug Formulations 2001 ...0....... III......... Cool to about 6 °C and dissolve the rest of III.0 g Cremophor RH 40 [1] ............. Properties of the gel A clear yellowish gel was obtained.............................0..5......q......7. Formulation I...................1 g II.. Water....... Chemical stability (20–25 °C. Lutrol F 127 [1] ........0..s...........................6. dark) 0 Months Tretinoin content 100 % 6 Months 12 Months 100 % 96 % There was no loss of alpha bisabolol during these 12 months.... Remark It is important to protect this formulation against light to avoid the isomerization and degradation of tretinoin........7 Formulations of semi-solid drugs (Lab scale) Tretinoin + Alpha Bisabolol Gel (50 mg + 100 mg/100 g) 1.. 5.... Manufacturing Add solution II slowly to the clear solution I at about 40 °C................70.05 g Lutrol E 400 [1]........... natural (BASF) ..........

....0 mg Lutrol E 400 [1]......... 23 °C....0 g Cremophor RH 40 [1] ....18.. dark) Tretinoin Dexpanthenol 96 % 100 % 5............ Manufacturing Add II slowly to the clear solution I at about 40 °C............50...... Maintain cool until the air bubbles escaped. Cool to about 6 °C and dissolve the rest of III........................5. Chemical stability (12 months.....4 g Dexpanthenol (BASF).7........68....................... Formulation I.............. Tretinoin (BASF) ... BASF Pharma Ingredients Generic Drug Formulations 2001 ....... Remark It is important to protect the gel against light to avoid the isomerization and degradation of tretinoin........ 3.............. Water......500 mg/100 g) 1................6.. 4..................0 g Butylhydroytoluene .........0 g 2...........2.................. Properties of the gel A clear yellowish gel was obtained..................5 g III..............40 mg II...7 Formulations of semi-solid drugs (Lab scale) Tretinoin + Dexpanthenol Gel (50 mg + 2......... Lutrol F 127 [1] .. Heat to about 50 °C and dissolve about 4 g of III in I/II.

......7.....3.............................76.......0 II..........................................................3....................05 Luvitol EHO [1] .5 Perfumes ..............0.. then mixture III and cool by stirring. Manufacturing Separately prepare solution I and mixture II by heating to about 75 °C.......0 Cremophor A 25 [1] .. Cremophor A 6 [1] ..04 Propylene glycol [1] ....8.......0 Cetyl alcohol ...046 % 0..........5 Glycerol monostearate ...................0.............047 % 0% 0% 0% 0% Analytical method: Spectrophotometric at 358 nm in chloroform + 2-propanol 1+1 (E 1%/1 cm = 1....... 3........................... Chemical stability (20–25 °C....................480) BASF Pharma Ingredients Generic Drug Formulations 2001 ...........4..047 % 0..... Tretinoin (BASF)......047 % 0............. Heat mixture III until a clear solution is formed........046 % 0..........1................. Formulation I.............5 III..........2 Water........................... dark) Months Tretinoin content Loss of tretinoin 0 3 6 9 12 0.0...7 Formulations of semi-solid drugs (Lab scale) Tretinoin Cream (50 mg/100 g) 1......................0.....0 Preservatives .... To the warm mixture II add solution I..............0 Tegiloxan ® 100 (Goldschmidt)..3................. Butylhydroxytoluene ...........2 g g g g g g g g g g g g 2............0......

Remark It is important to protect the gel against light to avoid the isomerizationand degradation of tretinoin.Tretinoin Cream (50 mg/100 g) page 2 4. BASF Pharma Ingredients Generic Drug Formulations 2001 .

....0........ 4.... dark) No loss of tretinoin was measured after 1 year.. 3................... Tretinoin (BASF)....... Butylhydroxytoluene .....05 g Ethanol .....6...............0.6 g 2............ Chemical stability (20–25 °C....0 g Cremophor RH 40 [1] ................. When a clear mixture is formed add solution I.......................5 g Water.......................................q...........76....7....................... Carbopol 940 (Goodrich) ...... Triethanolamine ..0...........0.1.0 g Perfume ................ Properties A clear yellowish gel was obtained..15................... Remark It is important to protect the gel against light to avoid the isomerization and degradation of tretinoin. Formulation I....04 g II................7 Formulations of semi-solid drugs (Lab scale) Tretinoin Gel (50 mg/100 g) 1...s...................................................................0 g III.........7 g Water.... 5.................... BASF Pharma Ingredients Generic Drug Formulations 2001 ................ Manufacturing Prepare suspension II and add solution III to the well stirred suspension.

............. 3..6 III.0 g g g g g g 2.....2.................5 Water. Sodium hydroxide solution 10 % .7 Formulations of semi-solid drugs (Lab scale) Ultrasonic Adhesive Gel 1..............4 II.................... Formulation I..75... Preservative (e.........0 IV........1...............0....... 4.. Properties of the gel A clear colourless adhesive gel was obtained.. Carbopol 940 (Goodrich) .......................0........................5 Water.... Add the solutions III and IV... Kollidon 30 [1] ... Parabenes) ..7. Remark The addition of salts like sodium chloride would be possible but the consistency could be changed by such modification................. BASF Pharma Ingredients Generic Drug Formulations 2001 .. Manufacturing Prepare solution I by heating and add II slowly to obtain a homogeneous suspension.......20.......g.................

......... add Cremophor and mix with the molten macrogols.7 Mio i....7 Formulations of semi-solid drugs (Lab scale) Vitamin A Suppositories (150.........Homogeneously yellow Drop point:......... 3....................u.....0 g Colour: .........40 Macrogol 1500 .......... Formulation Vitamin A palmitate 1............................7.....................54 °C Disintegration in water: .............) 1............................................u.........................1 Cremophor RH 40 [1] ............................./g (BASF) ........80 Macrogol 4000 ........ Properties of the suppositories Weight: . Fill into moulds of suppositories to obtain the weight of 2 g.000 i...22 min (emulsion) BASF Pharma Ingredients Generic Drug Formulations 2001 ....9 Butylhydroxytoluene ............................. Manufacturing Dissolve butylhydroxytoluene in the warm vitamin A......50 g g g g g 2.........2...

7 Formulations of semi-solid drugs (Lab scale) Vitamin E Gel-Cream (10%) 1............000 mPa · s....... After cooling to about 6 °C dissolve slowly Lutrol F 127 in the well stirred mixture. Viscosity at 25 °C about 120............. Maintain cool until the air bubbles escaped.... 4...55 g g g g 2.................................. Manufacturing Mix vitamin E acetate with propylene glycol and add the water................ BASF Pharma Ingredients Generic Drug Formulations 2001 ............7.... Properties of the gel-cr eam Turbid white gel at temperatures between 20 – 50 °C......... Formulation Vitamin E acetate (BASF) ..20 Water..................10 Propylene glycol [1] ... 3.........15 Lutrol F 127 [1] ...................... Physical stability After 2 weeks at 40 °C no changes of aspect or viscosity were observed....

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