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PHARMACOLOGY - Microsoft OneNote Online

DOSAGE FORMS

I. Introduction

Pharmaceutical Dosage Forms

Drug product or preparing containing the:

Drug/active ingredient
Excipients/additive/adjuncts

Drug

Any article or agent that is used for the diagnosis, mitigation, treatment, prevention & cure of disea
ses in man
and animals

Agents used to affect the structure & any function of the body of man & other animals

Excipients

Agents that are used to solubilize, suspend, thicken, dilute, emulsify, stabilize, preserve, c
olor, &
flavor medicinal agents into appealing & efficacious dosage forms

Cosmetics

Any substance or preparation intended to be placed in contact with the external parts of the human
body
(epidermis, hair system, nails, lips, & external genitals) or with the teeth & the mucous membrane
of the oral
cavity with a view exclusively or mainly to clean, perfume, changing their appearance, correcting b
ody odors
&/or protecting them or keeping them in good condition

Reasons for formulating Dosage Forms :

Stability
Improved solubility
Improved appearance
Ease of administration
Palatability

SOLID DOSAGE FORMS

A.

Powders

Intimate mixture of finely divided drugs or chemicals, which are intended for external & inter

nal use
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Advantages
flexibility in compounding
devoid of mixture
relatively stable

Disadvantages
Inaccuracy of dose
Not easily wetted (low absorption)
Not suitable for dispensing
Some powders are hygroscopic and deliquescent

> Hygroscopic absorbs moisture but does not liquefy

> Deliquescent absorbs moisture & liquefies

PARTICLE SIZE ANALYSIS

Obtain quantitative data for size, shape, & distribution of drug particles & other components
to be
used in the formulation

FACTORS INFLUENCED BY PARTICLE SIZE

1. Dissolution

Particle size
Rate of dissolution
ex. Micronization

1. Suspendability

Important for redispersing suspenoids in suspensions

Sedimentation volume, the better the suspension

2. Uniformity

Content uniformity
Weight variation

3. Penetrability

Important for inhalational

Particle size, faster penetration

4. Feel

Particle size, better skin feel

Prevent grittiness

> Comminution process of particle size reduction

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SMALL SCALE METHODS

Trituration use mortar & pestle

3 types

1. Glass smooth, nonporous surface, solutions, suspensions, & ointments colored

stances.

5. Wedgewood crystals

6. Porcelain soft aggregate crystals

a. Levigation
Forming a paste by the addition of a nonsolvent (levigating paste)
Lowers the particle size but does not dissolve the powder
Ex. Mineral oil & glycerins

a. Pulverization by Intervention
Addition of a nonvolatile substance
Ex. Camphor + Mineral Oil
Iodine crystals + Ether

LARGE SCALE METHODS

7. Mechanical pulverizers Large mills

8. Blending process of mixing powdered materials

9. Tumbling materials are enclosed in a constantly rotating chamber (large scale)
10. Spatulation use of spatula, small scale; if powders are nonpotent
11. Sifting use of sifters; nonpotent powders
12. Geometric Dilution addition of an EQUAL volume of diluent to a potent substance

Types of Powders
13. Bulk powders large quantities of oral powders
a. Dentrifices mild abrasive, anticariogenic
b. Dusting powders locally applied, nontoxic
c. Douche powders starting material for vaginal douche
d. Insufflations blown into body cavity by the use of insufflator (ex. for ears, nose)
e. Triturations 10% of active ingredient

14. Divided powders small quantities; aka chartulae or individualized powders

Types of paper

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sub

A. Bond paper: no moisture resistance

B. Glassine: glazed transparent paper; moisture resistant

Disadvantage doesnt protect product from photodegredation

C. Vegetable parchment: thin, semiopaque, moisture resistant
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Waxed paper: suitable for hygroscopic & deliquescent powders, waterproof

D.

Granules

B.

Prepared agglomerates of powders

Sieve size: No 412
For tablet preparation: No 1220
Methods of Preparation
Wet granulation: most common; uses granulating fluids such as water, ethanol, & isopropy
l alcohol
** drying step (dry inside the oven)
Dry granulation: used if material is moisturesensitive &/or heat labile
a. Slugging produces slugs
** slugs large flat tablets about 1 inch in diameter which are broken down into g
ranules
b. Roller compaction: produces sheets

Effervescent Granules
Releases CO2 to mask the disagreeable taste of drug
Components:
NAHCO3
Citric acid (C6H8O7) if alone, it yields a sticky mixture
Tartaric acid (C4H4O6) if alone, it easily crumbles
** Should have both citric & tartaric

C.

Tablets
Solid dosage forms that are prepared by molding or compression.

TYPES OF TABLETS:
1.
2.

Molded tablets Soft

Compressed tablets Hard

Compresses Tablets 1 layer

MultiCompressed tablet 2 or more layers
C. Sugar coated tablets Used to mask the disagreeable taste of the drug
A.

B.

Disadvantages:
Adds bulk to the formulation (>50%)
Time consuming

Requires expertise
D.

Film Coated Tablets Involves the application of a thin plastic like material on the tablet

.
Advantages:
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Does not form bulk to the formulation

Less timeconsuming
More durable and pliable
E.

Enteric Coated Tablets

Meant to disintegrate in the small intestine wherein the PH is greater than the PH of the

gastric
mucosa.
Reasons:
To increase absorption of a drug
To prevent gastric irritation
To offer protection for drugs destroyed by acid.
F.

Chewable Tablets
For those who have difficulty in swallowing
Does not need disintegrants
Usual diluents are Mannitol and Xylitol (SugarFree preparations)

G.

Effervescent Tablets
When in contact with water, It will release CO2

H.

Buccal Tablets
Tablets placed in the buccal cavity (Between the cheeks & gums)
Disintegration time: 4 hours

I.

Sublingual Tablets
Tablets placed under the tongue
Fast disintegration time
Used for emergency drugs : Clonidine (Catapress)
ISMN (Imdur)
ISDN (Isordil)

J.

Rapidly Disintegrating Tablets (RDT)

For patients with difficulty in swallowing
EX: Risperidone (AntiPsychotics)

K.
L.

Extended Release / Modified Release Tablets

Vaginal Tablets / Inserts

METHODS OF MANUFACTURING TABLETS :

Wet Granulation
Dry Granulation
3. Direct Compression From Powder to Tablet
For materials with excellent flow property and cohesive proper
1.
2.

ty
EX: NaCl, KCl
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