Introduction to Pharmaceutical Dosage Form

23/05/2011
.. 2510
1)

(USP:The United States

Pharmacopeia,BP: British Pharmacopeia )

2)

3)
4) ( )

( )

(
photolysis:
, oxidation:, hydrolysis: )

Bioavailability ( )

F (
)

AUC (Area Under

Curve)
bioavailability

bioavailability

1)

Particle size :


Particle size
bioavailability

Freeze modified

Bulk (
)

Freeze-modified

Tablet

Granules

small particles

USP ,BP

, 0.1 normal HCl (

) , pH 6.8 ( ileum )

bioavailability

y
x

bulk product :
20
60 %

modified freeze
modified freeze bioavailability bulk
product

2)

Enzyme

Enzyme

propranolol Hydrochloride

 Cytochrome P450s
bioavailability
Enzyme

portal vein

phase I oxidation cytochome P450 s ,Phase II
conjugation polar from

()
enzyme
3)

GI tract Environment :

Losec Omeprazole


bioavailability enteric

coated (delayed release) (enteric coated

: Omeprazole
NaHco3
Omeprazole Enteric-coated

 : Omeprazole NaHCO3 Bioavailability

Omeprazole Enteric-coated

: Omeprazole
NaHCO3
Omeprazole
: NaHCO3
Omeprazole
Bioavailability

prazole

protron pump inhibitor enteric

coated

 enantiomer R S Isomer
Omeprazole R-

Isomer

S- Isomer S- Isomer

R-

Isomer

S- Isomer
Esomeprazole Losec

4)

Efflux pump (P GP)

P GP : Preglycoprotien

P GP

Bioavailability

Noral Cyclosporin A 2
1.

Cyclosporin

2.

solf Gelatin capsule

SEDDS(self emulsified drug delivery system) 4

emulsion
Bioavailability

4 class class 1
Class 2
Class 3
Class 4

2 4
,
Class 2

,
,

SEDDS

,
Efflux pump cremophor EL pump

,

Class 4

Probucol class 4 Efflux pump

cremophor EL

probucol cremophor EL Bioavailability

 Bioavailability
1. Particle size

2. Enzyme

3. GI tract Environment

4. Efflux pump (P GP)

Dosage from
Liquid dosage from : oral

solution

homogeneous system (homogenous system

)

sterile
sterile sterile

1)

Active gradients >> /

2)

Sweetener >> sorbital

3)

Preservative >> methyl paraben , sodium bensoate

4)

Coloring /flavoring agent >>

5)

Antioxidant >> sodium metabisulfite

ascorbic acid

(A,D,E,K)
oxidation
6)

Buffering >> ascorbic acid

pH

7)

Thickner >>
cellulose hydroxyl methylcellulose

8)

Solvent >> propyleneglycal

1)

Benadryl

dose

2)

Calpal

3)

Atarax

Phenobarbital Elixir ()
1)

Phenobarbital (therapeutic agent)>>

2)

Orange oil (flavour) >>

3)

Propylene glycal ( co-solvent) >>

Phenobarbital

4)

Alcohol >>

5)

Sorbital solution (sweetener) >>

6)

Colour >>

7)

Purified water >>

Theophylline Elixir ()
1)

Theophyline (therapeutic agent)>>

2)

Citric acid (pH regulation) >> pH

3) Liquid glucose (sweetening agent)

4)

Syrup (sweetening agent)

5) Sacharin sodium (sweetening agent)

6)

Glycerin(co-solven)
Sorbital solution( co-solven)

7)

Theophyline

8)

Alcohol >>

9) Lemon oil (flavor)

10)

FDC yellow no. 5 (colour)

11)

Purified water >>

glycerin, Alcohol, sorbital solution, propylene glycal

Dispersed system: Suspension

Suspension

1)

Active gradients >> /

2)

Sweetener >> sorbital

3)

Preservative >> methyl paraben , sodium bensoate

4)

Coloring /flavoring agent >>

5)

Antioxidant >> sodium metabisulfite

ascorbic acid

(A,D,E,K)
oxidation
6)

Buffering >> ascorbic acid

pH

7)

Thickner >>
cellulose hydroxyl methylcellulose
suspension

8)

Solvent >> propyleneglycal

Powder for reconstitution

Flueknil
Thickner

Amoxicillin
Amoxicillin hydrolysis
capsule tablet
tablet
Powder for reconstitution

suspension Ibuprofen suspension , para suspension

milk of magnesia sodium
hydroxide

Thixotropic
(3
4)
suspention

Dispersed System : Ointment

penicillin

emulsion emulsion
hydrolysis emulsion 2

 ointment

base 4
1 Hydrocarbon base
2. Absorption base
3. Water-removable base
4. Water-soluble base
Water-removable base Water-soluble base
emulsion ointment Hydrocarbon
base

DISPERSED SYSTEM : GELS organic inorganic

inorganic
Aluminum Hydroxide Gel ( )
Aluminium Hydroxide 2
1.

Dry powder 100%

2.

Dry gel

% Aluminium Hydroxide Dry

powder Aluminium Hydroxide 100% Dry gel Aluminium
Hydroxide30%
Organic
carbomer tragacanth

 single phase gel

carbomer carbomer
carbomer
cellulose
plastic flow

DISPERSED SYSTEM: PASTES

ointment ointment
pastes
Zinc Oxide Paste
TRINOLONE

OCULAR DOSAGE FORMS

 pyrogen free bacteria

1.Active ingredient chloramphenical

2.Solvent
3.Antioxidant
4.Isotonicity value hypertonic hypotonic
Isotonic
5.Preservative


Hydrolysis
1
suspension ointment ointment
suspension ointment chloramphenical



ointment
Hydrolysis

Parenteral Formulations ()
2
Large volume parenteral 100 cc

Small volum parenteral 100 cc

emulsion solution suspension

pyrogen

free

omiprazol
1 Active ingredient
2 Buffering agents pH
3 Solvent
4 Antioxidant or inert gas
5 Isotonicity value
6 Preservative
7 Sterility
8 Pyrogen free

Rectal Dosage Form

dulcolax

Respiratory Dosage Forms

beta2agonists
First pass metabolism

Bioavailability

1.Inhalions
ventrolin
Suspension
compressor
compressor

2. Metered-Dose Inhalars (MDI)

 Inhalions
Suspension Solutions Ventrolin



Inhale

r adaptor

3.Drypowder Inhalers

Mouthpiece

White Wheel

SOLID-DOSAGE FORMS:TABLETS

4
1)

Wet granulation

2)

Dry granulation (slugging)

3) Direct compression
4) Roller compaction
(active ingradient)
(Powder excipients) Lactose
Mixer
granule granule



( Compression force)





Nippon


Mixing
time
roller roller


granule

High speed
400-600

granule


Fluidized-Bed

 5-6

Fig.Fluidized-Bed

2
1.
2.

granule

12 compacter
roller 2 granule

enteric coat

 spray

TABLETS
1) Active ingredients
2) Diluents lactose
,starch
3) Binder starch , povidone
4) Disintegrants starch, sodium starch glycolate.
5) Lubricants
magnesium steraten, stearic acid.
6) Glidants silicon dioxide.
7) Retard-materials polyvinyl acetate,
carbomer.
8) Coated materials
sugar,hydroxypropryl methyl cellulose, methacrylic acid co-polymer,
cellulose acetate phthalate(delayed release)
4 TABLETS 2

1)

Extended Release tablets

polymer coat
Tylinol 8 hour 3 Tylinol
8

 4-6

Extended Release tablets
1.
2.
3.

2)

Delayed Release tablets

Enteric

coat Methacrylic acid copolymer Cellulose acetate catalase.
Enteric coat Dulcolax

Voltaren

CHEWABLE TABLETS

1


air-x
antacil

EFFERVESCENT TABLETS


mucinac,CDR(Calcium-D-Redoxon)

SOLID-DOSAGE FORMS : CAPSULES

2
1)Soft gelatin
2)Hard gelatin


starch, hydroxypropylmethyl - cellulose
hard gelatin

penicillin hydrolysis
NSAIDs

soft gelatin

gelatin
gelatin

roller
roller gelatin roller

Delayed-release and extended-release ?

Delayed-release = enteric coat

polymer methacrylic acid copolymer cellulose acetate phthalated
extended-release


polymer
Tylinol ,Diclofenac

Creams and ointments ?

hydrogen base

Powder for reconstitution ?

penicillin,
Cephalosporins,Ampicilin
>>>>>>>>>>>>>>>>>>>>>>>>
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