BASIC PRINCIPLE OF

PHARMACEUTICAL DOSAGE
FORM
PHARMACEUTICS DEPARTMENT
PHARMACY STUDY PROGRAM FACULTY OF MEDICINE
BRAWIJAYA UNIVERSITY

OUTLINE
DRUG RESEARCH & DEVELOPMENT
VARIOUS PHARMACEUTICAL DOSAGE FORM
CONSIDERATIONS OF PHARMACEUTICS, BIOPHARMACEUTICAL & PHARMACOKINETICS IN
DESIGNING DOSAGE FORM

HISTORY OF DRUGS
DIGOXIN

1785

HISTORY OF DRUGS
CALCITONIN

THE PROCESS OF
DRUG DISCOVERY
AND DEVELOPMENT
IS COMPLEX.

Chemical &
physical

Mechanism of
action

Pharmacokinetic

Toxicologic

Metabolic
degradation

PHARMACEUTICS

The general area of study concerned with the formulation,

manufacture, stability, and effectiveness of pharmaceutical
dosage forms

THE PROPER DESIGN AND FORMULATION OF A DOSAGE FORM REQUIRES CONSIDERATION OF

THE PHYSICAL, CHEMICAL, AND BIOLOGIC CHARACTERISTICS
THE DRUG AND PHARMACEUTICAL MATERIALS MUST BE COMPATIBLE

DRUG PRODUCT THAT IS STABLE, EFFICACIOUS, ATTRACTIVE, EASY TO ADMINISTER, AND SAFE.

PHARMACEUTICAL DOSAGE FORM

Choose the route......

Oral

Table, Capsule,
Solution, Emulsion,
Suspension

Rectal

Suppositories

Parenteral

Injection

Topical

Ointments, Gel,
Cream

Routes of
administration

Other routes : nasal, otic,

opthalmic, etc

ROUTES OF
DRUG ADMINISTRATION

ROUTE OF ADMINISTRATION
AND DELIVERY SYSTEM OF PRIMARY
DOSAGE FORMS

CONSIDERATION OF CHOSING THE ROUTE

NEONATES, CHILDREN, ADULTS, GERIATRICS,
WEIGHTS
STATES OF ILLNESS

It has been said that the only difference between a drug and a poison is the dose

PRODUCT OF APPLICATION OF THE

PHARMACEUTICAL SCIENCES

Development

Design

Production
Use

PHARMACEUTICAL FORMULATION

Active Therapeutic Ingredients

Nontherapeutic/pharmaceutical ingredients
Filler, thickener, solven, suspending agent
Penetration enhancer, flavor, colorants, sweetener

THE NEED FOR DOSAGE FORMS

Protect from the destructive
influences

Coated tablet
Sealed ampuls

Conceal the bitter, salty or

offensive taste/odor

Capsule, coated tablet

Flavoured syrup

Liquid preparations of
substances insoluble/unstable
in the desired vehicle

Provide clear liquid dosage

forms

suspensions

Syrups, solutions

Provide for insertion of

a drug into one of the
bodys orifice
Drugs directly in the
bloodtream or body
tissues

Rectal
Vaginal suppositories

Injections

Optimal drug action to

the certain sites

inhalants & inhalation aerosols

Topical : ointment, cream, patch
Ophtalmic, ear, nasal

Provide rate-controlled
drug action

various controlled-release tablets, capsules, and suspensions

GENERAL CONSIDERATIONS
IN DOSAGE FORM DESIGN
DETERMINE THE DESIRED PRODUCT TYPE
DRUG RELEASE PROFILE, BIOAVAILABILITY, CLINICAL EFFECTIVENESS
THE MANNER IN WHICH IT IS TREATED (LOCALLY OR THROUGH SYSTEMIC)

THE AGE
THERAPEUTIC SITUATIONS

PHARMACEUTICS CONSIDERATIONS

PREFORMULATION STUDIES
PHYSICAL DESCRIPTION
MICROSCOPIC EXAMINATION
HEAT OF VAPORIZATION AEROSOL DOSAGE FORMS
MELTING POINT DEPRESSION PURITY
THE PHASE RULE
PARTICLE SIZE
POLYMORPHISM
SOLUBILITY

PHYSICAL DESCRIPTION
SOLID MATERIALS, CRYSTALLINE OR AMORPHOUS CONSTITUTION.
THE PURITY IDENTIFICATION AND FOR EVALUATION OF ITS CHEMICAL, PHYSICAL, AND BIOLOGIC
PROPERTIES.
CHEMICAL PROPERTIES : STRUCTURE, FORM, AND REACTIVITY.
PHYSICAL PROPERTIES : PHYSICAL DESCRIPTION, PARTICLE SIZE, CRYSTALLINE, STRUCTURE, MELTING
POINT, AND SOLUBILITY
VOLATILITY
STABILITY

MICROSCOPIC EXAMINATION
IT GIVES AN INDICATION OF PARTICLE SIZE AND SIZE RANGE OF THE RAW MATERIAL ALONG
WITH THE CRYSTAL STRUCTURE.
SOLID DRUG POWDERS : SPHERICAL AND OVAL POWDERS FLOW MORE EASILY THAN NEEDLESHAPED POWDERS AND MAKE PROCESSING EASIER

THE PHASE RULE

PROVIDE A VISUAL PICTURE OF THE EXISTENCE AND EXTENT OF THE PRESENCE OF SOLID AND
LIQUID PHASES IN BINARY, TERNARY, AND OTHER MIXTURES

I Solid A + solid B
II Solid A + melt
III Solid B + melt
IV Melt

PARTICLE SIZE
AFFECTS :
DISSOLUTION RATE, BIOAVAILABILITY, CONTENT UNIFORMITY, TASTE, TEXTURE, COLOR, AND
STABILITY

FLOW CHARACTERISTICS AND SEDIMENTATION RATES

PARTICLE SIZE SIGNIFICANTLY INFLUENCES THE ORAL ABSORPTION PROFI LES OF CERTAIN
DRUGS, INCLUDING GRISEOFULVIN, NITROFURANTOIN, SPIRONOLACTONE, AND PROCAINE
PENICILLIN

POLYMORPHISM
DIFFERENT PHYSICOCHEMICAL PROPERTIES, INCLUDING MELTING POINT AND SOLUBILITY
AMORPHOUS FORM OF A COMPOUND IS ALWAYS MORE SOLUBLE THAN A CORRESPONDING
CRYSTAL FORM

SOLUBILITY
DRUG MUST POSSESS SOME AQUEOUS SOLUBILITY FOR THERAPEUTIC EFFICACY
EXERT A THERAPEUTIC EFFECT, IT MUST FIRST BE IN SOLUTION.
MODIFI CATION OF THE DRUG INTO SALT OR ESTER FORMS IS FREQUENTLY USED TO INCREASE
SOLUBILITY.
ADJUSTMENT OF THE PH OF THE SOLVENT TO ENHANCE SOLUBILITY
IT IS DESIRABLE TO USE COSOLVENTS OR OTHER TECHNIQUES SUCH AS COMPLEXATION,
MICRONIZATION, OR SOLID DISPERSION TO IMPROVE AQUAEOUS SOLUBILITY

DOSAGE FORM DESIGN: BIOPHARMACEUTICAL &

PHARMACOKINETIC CONSIDERATIONS

BIOPHARMACEUTICS
PHARMACOKINETICS

The area of study embracing this relationship

between the physical, chemical, and biologic
sciences as they apply to drugs, dosage
forms, and drug action

The area of study that elucidates the time course

of drug concentration in the blood and tissues. It
is the study of the kinetics of absorption,
distribution metabolism, and excretion (ADME) of
drugs and their corresponding pharmacologic,
therapeutic, or toxic effects in animals and man.

ABSORPTION

DOSAGE AND KINETICS OF NITROGLYCERIN IN

VARIOUS DOSAGE FORMS

CRYSTAL OR AMORPHOUS
DRUG FORM
NOVOBIOCIN AND CHLORAMPHENICOL PALMITATE, ARE ESSENTIALLY INACTIVE WHEN
ADMINISTERED IN CRYSTALLINE FORM, BUT WHEN THEY ARE ADMINISTERED IN THE
AMORPHOUS FORM, ABSORPTION FROM THE GASTROINTESTINAL TRACT PROCEEDS RAPIDLY,
WITH GOOD THERAPEUTIC RESPONSE
THE CRYSTALLINE FORMS OF PENICILLIN G AS THE POTASSIUM SALT OR SODIUM SALT ARE
CONSIDERABLY MORE STABLE THAN THE ANALOGOUS AMORPHOUS FORMS

SALT FORMS
THE ADDITION OF THE ETHYLENEDIAMINE MOIETY TO THEOPHYLLINE INCREASES THE WATER
SOLUBILITY OF THEOPHYLLINE FIVEFOLD
DIMINISHED THE NEED TO USE HYDROALCOHOLIC MIXTURES SUCH AS ELIXIRS

SOME FACTORS THAT

INFLUENCE BIOAVAILABILITY
OF ORAL DRUGS

DRUG STANDARDS
AS THE SCIENTIFIC BASIS FOR DRUGS AND DRUG PRODUCTS DEVELOPED, SO DID THE NEED
FOR UNIFORM STANDARDS TO ENSURE QUALITY.
MONOGRAPHS AND REFERENCE BOOKS CONTAINING SUCH STANDARDS TO BE USED BY
THOSE INVOLVED IN THE PRODUCTION OF DRUGS AND PHARMACEUTICAL PRODUCTS.
ORGANIZED SETS OF MONOGRAPHS OR BOOKS OF THESE STANDARDS ARE CALLED
PHARMACOPEIAS OR FORMULARIES.

THE UNITED STATES PHARMACOPEIA AND THE NATIONAL FORMULARY

HANDBOOK OF PHARMACEUTICAL EXCIPIENTS (HOPE)

ALL ABOUT EXCIPIENTS
CONCENTRATION, STABILITY, COMPATIBILITY, INTERACTIONS, SOLUBILITY

Any Question?