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MODULE 5: PHARMACEUTICS (17.

5%)
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- Ease of administration
Drug Delivery System o Cosmetics
- Any substance/ preparation intended to be
place and contact with the external parts of
I. Introduction
the human body or with the teeth and mucous
o Drug- it is an agent intended for use in the diagnosis,
membrane of the oral cavity.
mitigation, treatment, cure, prevention of disease in
- Main used: Clean, Perfume, Changing the
humans/ animals.
appearance, Correcting Body Odor, To
o Dosage form- containing the following: API and
protect and for keep in good condition.
Excipient/ adjuncts/ additives.
o Compounding- preparation, mixing, packaging, or
Excipient/ Adjuncts/ Additives
labelling of a drug to prepare an individualized drug
- Inert (should have no reaction with the API,
treatment for a patient.
maintain the stability of drug)
II. Solid Dosage Forms and Solid Modified-Release Drug
o Drug Delivery System- is a system that is used as a
Delivery System
medium or carrier for administering a Pharmaceutical
Powders
product to a patient.
Granules
o Reasons for formulating dosage form:
Tablets
1. To protect the drug substance from
Capsules
destructive influences of atmospheric oxygen/
A. Powders
humidity
- Intimate mixtures of dry, finely divided drugs
2. To protect the drug substance from
and or chemicals that may be intended for
destructive influences of gastric acid after oral
“internal or external”
administration.
- Advantages:
3. To conceal the bitter, salty or offensive taste or
o Flexibility in Compounding
odor of a drug substance.
o Good Chemical Stability
4. To provide rate-controlled drug action.
o Rapid dispersion of ingredient
5. To provide liquid preparation of substance that
- Disadvantages:
are either insoluble/ unstable in the desired
o Inaccuracy of dose
vehicle.
o Not suitable for dispensing
To sum it up: unpleasant fasting, deliquescent or
hygroscopic drugs.
- Improve palatability Deliquescent- absorb moisture and
- Appearance liquefy (e.g. Naphthalene balls)
- Stability
- Solubility
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Hygroscopic drugs- absorb moisture - Not for potent substances


and doesn’t liquefy (e.g. dry ice, d. Geometric Dilution
silica gel) - For potent substance
1. Comminution of Drug - Addition of an equal volume of diluent
- Processes of reducing particle size. to a potent substance
Methods of Particle Size - Example:
a. Trituration 1g potent substance + 1g diluent (2 g
- Mortar and Pestle mixture)
b. Pulverization by Intervention - + 2g diluent
- For gummy substances which resist e. Tumbling- a process of mixing powders in a
grinding large container rotated by a motorized process.
- Addition of volatile oils
USP Standard for Powders of Animal and Vegetable Drugs
- Example: Camphor + Alcohol, Iodine
All particles pass through Type of Powder
Crystal + Ether #8 Very Coarse
c. Levigation #20 Coarse
- Forming a paste by addition of a #40 Moderately Coarse
#60 Fine
levigating agent. #80 Very Fine
- Example: Mineral oil, Glycerin
2. Blending of Powders USP Standard for Powders of Chemicals
a. Trituration (grind)- Mortar and Pestle All particles pass through Type of Powder
Types of Mortar and Pestle #20 Coarse
#40 Moderately Coarse
1) Glass #80 Fine
- Smooth, Non-porous surface; #120 Very Fine
Simple admixture (blend)
- For chemicals that stain Types of Powders
I. Bulk Powder
2) Porcelain- Rough inner surface; used if
- Dispensed in “large quantities”
comminution is desired. - Packaging: Sifter cans, Aerosol cans, Widemouth Bottle
3) Wedge Wood - Example:
a) Oral Powders
- Rough inner surface
- Suspended/ dissolved in water or mixed with soft foods prior to
- Used for crystalline substances administration
b. Spatulation - For Non-potent substances
b) Dentifrices- Powders that contain a soap; mild abrasive and anti-
- Use of spatula cariogenic agent (prevents tooth decay).
- Not for potent substances c) Dusting Powder
c. Sifting - Locally applied non-toxic powders with no systemic action.
- Example: foot powders
- Use of sifters resulting in a light product d) Douche Powder- Intended to be dissolved, in warm water prior to use
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as cleaning agent and antiseptic. - Process: Powder → Tablet Molder → Slug (flat
e) Insufflation- Powders blown into a body cavity using an insufflator
(powder blower).
face and about 2.5 cm (1 in) in
f) Triturations- Dilution of potent powdered drugs. (1:10 dilution) (10% diameter)→Granulator→Granules
dilution)
II. Divided Powder
- a.k.a. “Chartulae”
- Example: Effervescent Granule
- Dispensed in individual doses usually in folded papers (Chartula) - Dissolve in water before use
- Block and Divide Method where CO2 gas (has something to
Types of Powder Papers
a) White Bond Paper
do with the taste buds) is released
- Opaque paper with no moisture resistance to mask the unpleasant taste of
b) Glassine the drug.
- Glazed, transparent
- Moisture resistant - Components: (Incorporate all to
c) Vegetable Parchment balance)
- Thin, Semi-opaque with moisture resistant paper a. Sodium Bicarbonate-
d) Waxed Paper
- Transparent undergo neutralization
- Waterproof paper suitable for deliquescent (absorb b. Citric Acid- sticky
moisture and liquefy) and hygroscopic powders (does c. Tartaric Acid- crumble easily
not absorb moisture and liquefy)
- ↓ Photodegradation C. Tablets
- A solid dosage form prepared by “Compression” or
B. Granules “Molding”
- Are prepared agglomerates of smaller particles of - Excipients:
powder. o Diluent/ fillers- add a necessary bulk
- #14-#12 Sieve Size Range o Binders/ adhesive- promote adhesion
- Advantage: o Disintegrant- promote break-up of the tab
o Flowability after oral administration
o More stable to humidity o Antiadherent, glidants (powder)- enhance
o Wettability flow of material (Machine and powder)
o Less tendency to cake/ hardens - Types of Tablets:
- Methods in preparation of Granules: 1) Tablets for Oral ingestion:
1) Wet Method/ Wet Granulation a) Compressed Tablet
- Most common method which produced - Formed by compression
tablet of best quality - Scored (line in the middle of the
- Process: Powder + Solvent= Wet Mass tablet)
→Sieve #4→Oven (60 ℃)→Granules b) Multiple Compressed Tablet
2) Dry Method/ Dry Granulation 1. Layer tablets
- For Moisture and heat sensitive materials
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- Incompatible drugs/ - Dissolve slowly (4 hours


substances disintegration)
- Modify the release of the API - Example: Buccal Progesterone
- Prepared by compressing a tablet
tablet granulation against a
previously compressed tablet. c) Sublingual Tablets
2. Compression Coated tablets - Tablets which allow absorptive after
- Prepared by compressing an dissolution “under the tongue”
outer shell around a - Dissolve rapidly (2-3 minutes)
previously compressed tablet. - Used for emergency cases
c) Sugar-coated Tablets (Shiny) - Example:
- Tablet with water soluble o Nitroglycerin (Nitrostat)
- Sucrose-based coating - For acute angina attack
- Reasons: Protection, Palatability, o Isosorbide Dinitrate (Isordil)
Appearance - Prevents Angina
d) Film-coated tablet d) Rapidly/ Orally Disintergrating
- Tablets which are coated with a thin - Tablet which liquefy on the tongue
layer of polymer material. and patient swallows the liquid
e) Enteric Coated tablet - Example:
- Tablets which disintegrate only in o Resperidone (Respiridal)
the small intestine. - Anti-psychotic
- Reason: Protection of a drug e) Lozenges
destroyed by an acidic environment, - Dissolves slowly in the mouth for
increase absorption, Prevent gastric local effects
irritation - Example:
2) Tablets used in the Oral Cavity o (Strepsils)
a) Chewable Tablets - Amylmetacresol
- Tablets which disintegrate when - Dichlororbenzyl
chewed - Alcohol
- No disintegrants o Difflam
- Diluents: “Mannitol” or “Xylitol” - Use: For Sore Throat
b) Buccal Tablets - Types of Lozenges:
- Allow absorption after dissolution in a) Troche
the buccal cavity/ pouch - Compressed
lozenges
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- Hard o Type B: Base Hydrolysis- Bovine bones


b) Pastilles o HMPC/ Hydroxypropyl Methylcellulose
- Molded lozenges (Hypromellose)
- Soft - Alternative to gelatin from pig
- Example: (Cotch) - Not animal source
3) Tablets used to prepare solutions: - Types of Capsules:
- This is dissolved in water prior to 1. Hard Gelatin Capsules
administration - Dry filled or two-piece capsule
a) Effervescent Tablet (Capsule body, capsule cap)
- Prepared by compressing - Components of Hard Gelatin: Gelatin,
granular effervescent salts sugar, water (+colorant), opacifying
that release gas when in (titanium dioxide), 0.15% sulfur
contact with water. dioxide (to prevent decomposition)
- Example: (Fluimucil) - Moisture content: 12-16%/ 13-16%
b) Dispensing Tablet o <12- brittle and crumble
- a.k.a. “Compounding o >16- distorbed and lose their
Tablet” rigid shape
- Contain large amount of - Capsule size: 000 (largest), 00, 0, 1, 2, 3,
highly, potent drugs which 4, 5 (smallest)
is used for compounding - Method of compounding: Punch
multiple dosing unit. Method
c) Hypodermic Tablet 2. Soft Gelatin Capsules
- Used by physician to - One-piece capsule
prepare parenteral - Use for: water-immiscible volatile and
solutions. non-volatile liquids, ↓ Vegetable and
d) Molded Tablet Aromatic oils
- a.k.a. “Tablet Triturates” - Water-miscible and non-volatile
- Prepared by molding liquids: Propylene glycol
D. Capsules - Water-miscible and relatively non-
- API’s/ excipients enclosed in a small shell of Gelatin volatile compounds: Propylene glycol
Gelatin- obtained by partially hydrolysis of - Preservative: Methylparaben,
collagen (Skin, white connective tissue, bones of Propylparaben
animals) - Components: Gelatin, Glycerin/
- Types of Gelatin: Polyhydric alcohol ((Sorbitol), for
o Type A: Acid Hydrolysis- Porcine Skin elasticity and plasticity)
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- Moisture content: 6-10%


- Methods of Compounding: Plate
process, Rotary die process
Time
b) Delayed Release- drug release is other than the
time of administration. Example: Enteric coated
Solid Modified-Release Drug Delivery System tablet
c) Repeat Action- contains 2 single doses of
- Concern Problem: Dose Dumping= ↑ Dose, ↑ Adverse
medication one for immediate release and another
effect
for the delayed release or second dose. Example:
- Drug release features are based on time, coarse and
Two-layer tablet
location.
d) Targeted Release
- Reasons: to prolong the action of the drug, to decrease
- Drug release is isolated in a specific body
frequency of administration (commonly feature in
organ or tissue for absorption and
extended release)
metabolism
- Types of Solid Modified Release:
III. Semi-Solid Dosage Form and Transdermal Drug Delivery
a) Extended Release
System
- Provides a prompt desired effect followed
- Intended for topic administration: Ointments,
by a gradual release of the remaining
Creams, Gels, Pastes, Plaster, Glycerogelatin,
amount.
Poultices/ Cataplasm
- Reason: for drugs which are not inherently
A. Ointments
long lasting, for drugs which require multiple
- Are semi-solid preparation intended for external
dosing
application to the skin or mucous membrane.
- Types of Extended Release:
- Type of ointment:
1. Controlled Release
o Medicated- API’s
- Constant concentration
o Non-medicated
2. Sustained Release
- used for protectants, emollients or lubricants
- Gradual release is not
- vehicle, base for preparing medicated
constant
ointment.

Classification of Ointment bases according to USP


1. Oleaginous - a.k.a. “Hydrocarbon bases”
Therapeutic base - used as an emollient and occlusive
effects
Range - most difficult to wash off with water
a) Petrolatum, USP
- a.k.a. “Yellow Petrolatum/
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Petroleum Jelly” decolorized


- It is purified mixture of semi- - Melts between 36-42℃
solid hydrocarbons - 2 types of Lanolin
obtained from petroleum. 1) Anhydrous
- Example: Vaseline - 0.25% moisture
b) White Petrolatum, USP 2) Hydrous
- a.k.a. “White Petrolatum - 25% moisture
Jelly” 3) Water Removable base
- Wholly/ nearly decolorized - a.k.a. “Water
vallow petrolatum washable base”
- Example: White vaseline - Oil-in-water emulsion
c) Yellow ointment, USP - Easily washed from
- Contains yellow wax (50 g) the skin
+ Petrolatum (950 g) = - Absorb serous
Yellow ointment/ Simple discharges
ointment - Example:
- Yellow wax- a purified wax Hydrophilic
obtained from the Ointment, USP
honeycomb of the bee 4) Water Soluble base
(Apis mellifera) - Do not contain
d) White ointment, USP oleaginous
- White wax (50 g) + White components
Petrolatum (950 g) = White - Completely water
ointment washable
- White wax- bleached and - “Greaseless”
purified yellow wax - Example:
2. Absorption - Water-in-oil (W/O) emulsion a) Polyethylene
bases - May permit incorporation of small Glycol
amounts of water/ aqueous solution Ointment
- Less degree of emollient (soften the - PEG 3350 (400
skin) and occlusive effects (absorb g)- solid + PEG
moisture) 400 (600 g)-
- Not easily washed off with water liquid = PEG
- Examples: Ointment, USP
a) Hydrophilic Petrolatum, USP
- Formula:
o Cholesterol 30 g B. Creams
o Stearyl alcohol 30 g
o White wax 80 g - Are semisolid preparation containing one or
o White Petrolatum 865 g more agents dissolved or dispersed in either a
- Example: Aquaphor
“water-in-oil” or “oil-in-water”- emulsion
b) Lanolin, USP
- Obtained from the wool of - Examples:
the sheep (Ovis aries) a) Vanishing Cream
- It is a purified wax-like
- Is an O/W emulsion
substance that has been
cleaned, deodorized and
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- Contain large % of water and stearic - Employed to absorb serous discharges


acid or other oleaginous - Example: Lassar’s Plain Zinc Paste
components - a.k.a. “Zinc oxide paste”
- Residue film- Retard loss of moisture - containing 25% each of zinc
b) Cold Cream oxide and starch with white
- Is a W/O emulsion petrolatum
- Examples: E. Plasters
a) Rose Water Ointment - Solid/ semisolid adhesive masses spread on a
- Components: backing of paper, fabric, moleskin or plaster.
o Spermaceti - Example: Salicylic Acid Plaster
o Almond oil - a.k.a. “Corn Plaster”
o White wax - Contains 10-40% Salicylic Acid
b) Petrolatum Rose Water Ointment - Used for the removal of corns by
- Components: the keratolytic action of Salicylic
o Spermaceti Acid
o Mineral oil F. Glycerogelatin
o White wax - Plastic masses applied to the skin with a “fine
- a.k.a. “Cold Cream” brush”
C. Gels - Component: Gelatin (15%), Glycerin (40%),
- a.k.a. “Jellies” Water (35%), API (10%)
- Semisolid system consisting of dispersions of - Example: Zinc Gelatin
small/ large molecules in aqueous liquid - a.k.a. “Zinc Gelatin Boot”
vehicle rendered jellylike by the addition of - Treatment of varicose ulcer
“Gelling Agent” G. Poultices/ Cataplasm
- Characteristics: Thixotropy- revisable gel-sol - One of the ancient class of pharmaceutical
formation preparation
D. Pastes - Examples: Meal, Herbs, Seeds, etc.
- Are semisolid preparation intended for - Applied Hot in Cloth
application to the skin - Examples: Kaolin Poultice
- They generally contain larger proportion of - For boils and inflammation
solid material (25%)
- Stiffer than ointment
- They remain in place after application
- Not suited for application to hairy parts of the
body. Transdermal Drug Delivery System
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A. TTDS c) TD Clonidine
- Is a controlled release delivery system/ patches - Catapress TTS (Transdermal Therapeutic System)
which facilitate the passage of therapeutic - First TDDS for hypertension
quantities of drug substance through the skin d) TD Fentanyl
(Stratum corneum) and into general circulation - Good analgesic (Chronic pain)
for systemic effects. e) TD Estradiol
- Nitropatch - (Estraderm)
- Hormone Replacement Therapy
f) TD Testosterone
- (Testoderm), (Androderm)
- Hormone Replacement Therapy

II. Pharmaceutical Inserts

A. Suppositories
1. Occlusive backing - Solid dosage forms intended for insertion into
- Film- prevents loss of water from the body orifices where they melt, soften or dissolve
skin or prevents drug loss from the and exert local or systemic effects.
matrix. - Types:
2. Drug Reservoir/ Drug Matrix System o Rectal
- It is where the system drug is store o Vaginal/ Pessaries
and release. o Urethral/ Bougies
3. Adhesive layer
- Ensure TDDS are kept in place after Features Rectal Vaginal Urethral
a.k.a. Pessaries Bougies
application to the skin. Sex Both Female Both
4. Protective linear/ Release liner Age Adults/ Children Adults Adults
- Remove before application to the Shape Pencil-like Globular, Pencil-shaped
shaped Oviform,
skin. Cone shaped
- Examples of TDDS: Weight Adults: 2 g 3 grams Male: 4 g
a) Transdermal Drug (TD) Scopolamine Children: 1 g Female: 2 g
Size Adults: 32 mm Varies Male: 140 mm
- First TDDS to receive FDA approval Children: ½ Female: 70 mm
- Used for motion sickness Intended use Local and Local local
- a.k.a. “Transderm scop” systemic
Commonly used Cocoa butter Glycerenated
b) TD Nitroglycerin
based gelation
- Nitro-Dur, Transderm-Nitro B. Oleaginous Base
- For prophylactic treatment of angina - Example:
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a) Cocoa Butter - AGI is impregnated into a material and is release


- Widely used for rectal slowly into the body
suppository - Example: Progesterone implants
- Fat obtained from the seed of - Leuprolid Acetate (Viadur)
Theobroma cocoa - Treatment: Prostate Cancer
- It melts at 30-36℃
V. Liquid Dosage Form
- Polymorphism- existence in
several crystalline form o Solution
- Crystalline forms: o Dispersed System
o Alpha Crystals A. Solutions
o Beta Crystals- most - Liquid preparations
stable - Containing 1 or more chemical substances
o Beta Prime Crystals dissolved in a suitable solvent.
o Gamma Crystals - Advantage/s:
b) Wecobee- derived coconut o Homogenous doses
c) Witepsol o Immediate availability for absorption
- Saturated fatty acid from C-12 to C- and distribution flexible (easy to
18 swallow and easy to adjust dose)
- Major component: Lauric acid - Disadvantage/s:
d) Glyceryl Monopalmitate o Degrade rapidly (Prone to microbial
C. Water-Soluble/ Water-miscible base contamination)
a) Glycerinated Gelatin o Bulkier
- Most commonly used base for pessaries Water- most common vehicle or solvent for drug solutions
b) Polyethylene Glycol Descriptive Terms for Solubility
III. Vaginal Tablets Descriptive terms Parts of solvent required for 1 part of
- a.k.a. “Vaginal Inserts” solute

- ovoid tablet which are formed by compression Very soluble <1


Freely soluble 1 - 10
intended to be inserted into the vagina using
Soluble 10 - 30
plastic inserter
Sparingly soluble 30 - 100
- Content: Anti-microbials Slightly Soluble 100 - 1,000
- Example: Mycelex-G (Clotrimoxazole) 500 mg Very slightly soluble 1, 000 - 10, 000
- Candida infections Insoluble >10, 000

IV. Implants and Devices Types of Solution


1. Aqueous a) Aromatic water (Medicated Waters)
- Used to control drug delivery solution - Are clear, aqueous solutions saturated
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(Solvent- with volatile oils, other aromatic or naphthalene like odor.


water) volatile substance. - Component: 20% Coal Tar +
- Use: Flavoring or perfuming vehicle 5% Polysorbate 80
aqueous phase in emulsion or d) Antibacterial Topical Solution
suspension. - Examples:
- Method of Preparation: 1. Hydrogen Peroxide (H2O2)
o Distillation - “Agua oxinada”
- Not practical, economical - 3%= 10 volume- wound
for most products antiseptic
- Only method for: - 6%=20 volume- bleaching
 Strong Rose Water agent
 Orange Flower Water 2. Povidone-Iodine Topical Solution
- Simple solution - Betadine
- can use dispersant (ex. Talc) - 10% complex of Iodine and
- Example: Peppermint water, Polyvinylpyrolidone
USP 3. Thimerosal Topical Solution
b) Diluted Acids - a.k.a. “Merthiolate”
- Aqueous solutions prepared by - 0.1% Thimerosal- Mercurial
dissolving concentrated acids in antibiotic
“purified water” e) Douche
- Concentration - Aqueous solutions directed into a body
o Strong acid: 10% w/v cavity used as a cleansing agent and
o Acetic acid: 6% w/v antiseptic
- Example: Diluted Hydrochloric Acid- - Examples:
treatment for achlorhydria (taken with 1. Eye Douche
straw) - Removes foreign
c) Astringents particles
- Aqueous solutions that precipitate 2. Pharyngeal Douche
proteins - Prepares interior of throat
- Constriction of the skin (pores) 3. Vaginal Douche
1. Aluminum Acetate Topical - Most common type
Solution - Maintains acid pH of
- a.k.a. “Burrow’s Solution” vagina
- Used as wet dressing in - May contain
contact dermatitis (Poison antimicrobial
ivy) - Example: pH care
2. Calcium Hydroxide Topical (Chlorhexidine
Solution gluconate)
- a.k.a. “Lime water or liquor f) Enemas
calcis” - Two types:
- more soluble in cold water o Evacuation Enema
3. Coal Tar Topical Solution - Rectal injection employed to
- Used as a local anti- evacuate the bowel
eczematic - Example: Fleet Enema (Sodium
- Coal Tar- nearly black Phosphate Enema, USP)
viscous liquid with a sharp o Retention Enema
burning taste and - Influence general system by
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adsorption or to affect a local those injured by heat


disease. 3) Percolation
- Example: Sulfasalazine Enema - Preferred method for Ipecac
(Treats Ulcerative colitis) Syrup, NF
g) Gargles - Percolator
- Aqueous solution used for treating the - Rate: 1 mL/minute
“pharynx” and “nasopharynx” - Rapid flow may cause
- Used by foaming air from the lungs oxidation
through the solution which is held in the 4) Reconstitution
throat - Addition of sugar to
h) Mouthwashes medicated liquids or vice
- Aqueous solution used by swishing the versa.
liquid in the oral cavity to cleanse the b) Honeys
mouth. - Thick liquid preparation somewhat
2. Sweet and a) Syrups allied to syrups but using “Honey” as the
Viscid - Concentrated solutions or nearly base.
Aqueous saturated solutions of “sucrose” or other c) Mucilage
solution sugars in water or aqueous liquid - Thick, viscid, adhesive liquid
- Types: - From vegetable source
1. Simple Syrup, NF - Method of preparation:
- 85% w/v, 65% w/w 1. Dispersion of gums in water
- Sp. Gr. 1.313 2. Extraction of mucilaginous
- Self-preserving >65% principles from vegetable
2. Flavored Syrup substances
- Syrup + Flavor/ Juice - Example:
- Example: Cherry Syrup, o Acacia Mucilage, NF
Orange Syrup- for drugs that o Tragacanth Mucilage, NF
requires acidic medium, d) Jellies
Cocoa Syrup- mask bitter - Class of gels in which the structural
taste, Raspberry Syrup- for coherent matrix contains high portion of
salty or sour taste, Ora- water, having a jelly like consistency.
sweet- for extemporaneous - Used as lubricant for: surgical gloves,
compounding rectal thermometer, catheter
3. Medicated Syrup - Example: Lidocaine HCl Jelly (Topical
- Simple syrup/ Flavored Syrup anesthetic)
+ API 3. Hydroalcoholic a) Elixir
- Methods of Preparation: solutions - Are clear, sweetened hydroalcoholic
1) Solution with heat solutions intended for oral use
- Fastest method - Self-preserving: 10-12% of alcohol
- Used when components are - Alcohol content: 5-40%
neither volatile nor injured by - Method of Preparation:
heat. o Simple Solution
- Overheating- sucrose inversion - Addition of API with solvent with
“caramelization” the aid of heat
2) Solution without heat - Admixture of 2 or more medicated
- To prevent sucrose inversion liquids
- For volatile components and - Types of Elixir:
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1) Medicated Elixir - Distilled


- Example: Digoxin, Phenobarbital, grapes/
Diphenhydramine HCl, fermented
Dexamethasone grapes
2) Non-medicated Elixir o Whisky
- Example: Aromatic Elixir, NF- 22% - Spiritus frumenti
alcohol - Fermented malt
- Provides sufficient alcohol content grain
to dissolve drugs d) Fluid Extracts
b) Tinctures - Are hydroalcoholic solution from
- Are hydroalcoholic solutions prepared vegetable drug prepared by
from soluble constituents of vegetable percolation
drugs or from chemical substances - Too potent and bitter
- Strength: 10% w/v - Methods of Preparation:
- Methods of preparation: 1. Process A
1. Process P (Percolation)- - Must be assayed
Example: Belladonna tincture 2. Process E
2. Process M (Maceration) - Alternative to process
3. Simple Solution 3. Process D
- Example: - Boiling water as menstruum
o Iodine Tincture (2%Iodine, - Example: Cascara
50% Alcohol) Sagrada Fluid Extract
o Opium Tincture, USP/ (Cathartic)
Laudanum 4. Non-aqueous a) Liniments
o Paregoric, USP/ solution - a.k.a. “Embrocation”
Camphorated Opium - are alcoholic/ oleaginous (massage)
Tincture solutions or emulsions of various
o Compound Benzoin Tincture medicinal substance intended to be
(74-80% Alcohol) “rubbed on the skin”
c) Spirits/ Essences - Types of Liniments:
- Are hydroalcoholic solutions of volatile o Alcoholic- useful when
substances rubefacient counterirritant and
- 80-90% penetrating action is desired.
- Methods or Preparation: o Oleaginous- if massage is
1. Simple solution desired
- Example: Aromatic b) Collodions
Ammonia Spirit - Is a clear/ slightly opalescent viscous
2. Solution with Maceration liquid prepared by dissolving pyroxylin
- Example: Peppermint (4% w/v) in a 3:1 mixture of ether and
Spirit alcohol.
3. Chemical Reaction o Pyroxylin
- Example: Ethyl Nitrite - a.k.a. “Soluble gun cotton,
Spirit Collodion Cotton,
4. Distillation Nitrocellulose”
- Example: - Obtained by the action of a mixture of
o Brandy Nitric and Sulfuric Acid on Cotton
- Spiritus vini vitti (consist of cellulose tetranitrate)
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3 Ether consistency
- No intention of
removing the solvent
2.Pilular/ Solid Extract
- Plastic consistency
(Cellulose tetranitrate) 1 Alcohol - An intention of
Nitric and Sulfuric removing nearly all
- Use of Collodion: intended for solvent
external use as an occlusive 3.Powder Extracts
protective to the skin. - Prepared to be dry by
- Types of Collodion: removing all solvent
1. Flexible Collodion
- Prepared by adding:
o 2% Camphor: B. Disperse System
makes the product 1) Suspension
“waterproof”
o 3% Castor oil:
- Is a preparation containing finely divided
renders the drug particles (suspensoid) distributed
product “flexible” uniformly throughout a vehicle
2. Salicylic Acid Collodion
- 10% Salicylic acid in
- Example of suspension:
flexible collodion o Gels
- Used for its keratolytic - semisolid system consisting of
effects.
dispersions made up of either
c) Extracts small inorganic particles or
- Concentrated preparations of large organic molecules.
vegetable or animal drugs.
- Method of extraction: - Characteristics of Gels:
o Maceration- soaking for 3 days a. Imbibition
with frequent agitation - Taking up of liquid
o Digestion- maceration with
gentle heat without an increase
o Percolation- meaning to strain, in size or volume.
a process in which a b. Swelling
comminuted drug is extracted
of its soluble constituents by - Taking up of liquid
the slow passage of suitable but with an increase
solvent through a column of
in size or volume.
the drug.
o Decoction- boiling in water for c. Synerersis
15 minutes - Liquid comes out of
o Infusion- maceration in hot/
cold water
the gel and the gel
- Three forms of Extracts: shrinks.
1. Semisolid Extracts d. Thixotropy
- Liquid/ syrup
MODULE 5: PHARMACEUTICS (17.5%)
15

- Reversible gel-sol - Example: Bentonite Magma


formation. 2) Emulsion
e. Xerogel - A two-phase system prepared by
- The liquid is combining two immiscible liquids.
removed from a gel - One of which is dispensed throughout the
and only the other in the form of small droplets.
framework remains. - O/W
o Lotions External Phase Internal Phase
- “Dispersing medium” - “Dispersed Phase”,
- A suspension intended for
- Continuous phase “Discontinuous
external application to the Phase”
body.
- 2 Methods of Preparation Types of Emulsion
1. Oil-in-water (O/W) Oleaginous internal
1. Trituration Emulsion phase and aqueous
- With the aid of external phase.
mortar and pestle 2. Water-in-oil (W/O) Aqueous internal
Emulsion phase and
- Example: oleaginous external
o Calamine Lotion phase.
- Zinc oxide + 3. Multiple Emulsion W/O/W or O/W/O
Ferric oxide
(pink
coloration)
- Used as anti- - Preparation of Emulsion:
pruritic o Emulsifying agent
- Used to promote and maintain
2. Chemical Reaction dispersion of finely subdivided
- Example: particles of drug in a vehicle in
o White Lotion which it is immiscible.
- Components: - Examples:
Zinc sulfate + o Natural- Acacia,
Sulfurated Tragacant
Potash o Anionic- Sodium Lauryl
o Magma Sulfate
- A gel mass consists of o Cationic- Benzalkonium
floccules of small, distinct Chloride
particles.
MODULE 5: PHARMACEUTICS (17.5%)
16

o Non-ionic- Spans and - Surfactant- lowers tension between


Tweens surface.
HLB System (Hydrophil-Lipophil Balance) 3) Aerosol
Activity HLB-Value
- A preparation in which a solid or liquid
Anti-foaming 1-3
W/O Emulsifier 3-6 medicinal agent is disperse in a gaseous
Wetting agent 7-9 phase.
O/W emulsified 8-18
Detergents 13-16
Solubilizer 15-20

- Method of Preparation:
a) Dry gum or “continental method”
- a.k.a. “4:2:1 method”
- 4:2:1 (oil: water: gum)
- Oil + Gum → Trituration → Add
water (all at once)
b) Wet gum or English method
- Same proportion as in dry gum
method (4:2:1) Basic parts and components
Propellant/API - Supplies the necessary force to expel
- Water + Gum→ Trituration → Add oil product and some save as the solvent or
in portion diluent.
c) Forbes bottle method - Types of Propellant:
o Liquefied gases
- For volatile oils and less viscous oil - Saturated hydrocarbon
- Oil + Gum in bottle → Shake → Add (propane)
- Chlorofluorocarbon
water in proportion (2:2:1 (oil:
(CFC’s) - degrades zone
water: gum) layer
d) Lu situ soap method - Hydrofluorocarbon- more
accepted
- Oil + Aqueous Alkali’s solution o Compressed gases:
(calcium hydroxide) - CO2
- Emulsifying agent: salt of free fatty - Nitrogen
Container for a) Tin-plated steel
acid Aerosol - Most widely used for
e) Microemulsion metal container for
- Are thermodynamically stable, aerosols.
b) Actuator
optically transparent isotropic - Is the button the user
mixtures of a biphasic o/w system presses to activate the
stabilized with surfactants. emission of the product
MODULE 5: PHARMACEUTICS (17.5%)
17

c) Valve of suitable vehicles yield


- Where the contents are solutions.
emitted. - Example: Cefuroxime for
d) Dip tube injections
- Conveys the liquid from 3. Injectable emulsion - Drug substance dispersed in
the bottom of the a suitable emulsion medium.
container to the - Example: Propofol, USP
dispensing value. 4. Injectable suspension - Liquid preparation of solid
suspended in a suitable liquid
medium.
4) Suspension - Example: Methylprednisolone
Acetate Suspension, USP
VI. Sterile Dosage Form 5. For injectable suspension - Dry solids that upon addition
of suitable vehicles yield
A.) Injections- are sterile, pyrogen-free preparations solutions
intended to be administered parenterally. - Example: Imipenem and
Cilastatin for Injectable
B.) Parenteral Routes of Administration
Suspension, USP
1. Intra-articular - Joints
2. Intra-synovial - Joint fluid area
3. Intraspinal - Spinal column D.) Solvents and vehicles for injection
4. Intrathecal - Spinal fluid 1. Water for Injection - Purified by: Distillation or
5. Intra-arterial - Arteries reverse osmosis
6. Intracardiac - Heart - Must be pyrogen free
7. Intravenous - Veins 2. Purified water - Purified by: Distillation or
- Most common % bioavailability reverse osmosis
8. Intramuscular - Muscle - Ion exchange
- Deltoid or glutes maximus: 3. Sterile water for injection - Packaged in a single dose
vaccines container
- Volume: n.m.t. 5 mL (9-45 for o Single dose container/
dengue vaccine) single unit
9. Intradermal - Skin - Contains a single
- Most superficial of the skin layer dose
- Volume: n.m.t. 0.4 mL - No antimicrobial
- Example: Skin test agent
10. Subcutaneous - Under the skin - USP limit: not larger
- Volume: n.m.t. 1.3 mL than 1 L or 1000 mL
11. Epidural - Near or outside the dura matter of - Example: ampules
the CNS 4. Bacteriostatic water for - Is a sterile water for injection
- During childbirth injection containing one or more
suitable antimicrobial agents.
- Not used for neonates
C.) Official Types of injection because it contains benzyl
1. Injection - Liquid preparations that are alcohol which can cause
drug substances or solutions. “gasping syndrome or multi-
- Example: Insulin injection, USP organ failure”.
2. For injection - Dry solids that upon addition - Container: multiple unit
MODULE 5: PHARMACEUTICS (17.5%)
18

- Contains
multiple dose
- USP limit: not
larger than 30
mL
5. Bacteriostatic Sodium - Is a sterile water for injection
Chloride Injection containing one or more
antimicrobial agent.
6. Ringer’s injection - Contents in water for injection:
NaCl, KCl, CaCl

E.) Non-aqueous vehicle


1. Fixed Vegetable oils
- Used as vehicle for (IM injection):
- Mnemonics: CoCoPeSe
Co Corn oil
Co Cottonseed oil
Pe Peanut oil
Se Sesame oil
2. Others
o Glycerin
o Polyethlene glycol
o Propylene glycol
o Alcohol
- Less often used agents:
o Ethyl oleate
o Isopropyl myristate
o Dimethyl Acetamide

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