PHYSICOCHEMICAL

CHARACTERISTIC OF DRUG

Group 1
Habibie Deswilyaz Giffari (1311011039)
Nadia Putri Inanta (1411011001)
Annisa Fitri Febrianti (1411011004)
Stefany Faula Rendy Putri (1411011007)
Wira Wahyudi Nandayasa (1411011009)

What is

Biopharmaceutical?

Biopharmaceutics Definition
Biopharmaceutics is the science that examines

this interrelationship of the physicochemical

properties of the drug, the dosage form in
which the drug is given, and the route of
administration on the rate and extent of
systemic drug absorption (Shargel et al., 2004).

Biopharmaceutics involves factors that influence :

(1)the stability of the drug within the drug product,

(2)the release of the drug from the drug product,
(3)the rate of dissolution/release of the drug at the
absorption site,
(4)the systemic absorption of the drug
(Shargel et al., 2004).

 The aim of biopharmaceutics is to adjust the

delivery of drug from the drug product in

such a manner as to provide optimal
therapeutic activity and safety for the
patient (Shargel et al., 2004).

Route of Administration
Local activity only

Intramuscular or
Subcutaneous
Injection

Oral
Gastrointestinal
tract

Tissue Depots
DRUG

DRUG
DRUG
DRUG

Topical
Administration

Intravenous
Injection

DRUG

Systemic circulation
Drug

Serum Albumin

First
Pass
Effect

Lipid
Membranes

Drug Metabolites

Drug Metabolites
Enterohepatic
Recirculation

Primarily the Liver

produces Drug
Metabolites

Route of
Metabolism

Bile
Duct

Intestinal
Tract
Feces

Kidney

Urine: Drug &

Drug Metabolite

Route of Elimination

Receptors
for desired
effects

Receptors
for undesired
effects

Pharmacology

Pharmaceutical Dosage
Form

Dosage forms are the means (or the form) by which drug molecules
are delivered to sites of action within the body.
The need for dosage forms:
1. Accurate dose.
2. Masking taste and odour.
3. Placement of drugs within body tissues.
4. Controlled release medication.
5. Optimal drug action.
6. Insertion of drugs into body cavities (rectal, vaginal)
(Damodharan, 2010).

They are classified according to:

Route of administration
Oral - Vaginal
Topical - Inhaled
Rectal - Ophthalmic
Parenteral - Otic

Physical form
Solid
Semisolid
Liquid
Gaseous
(Damodharan, 20xx).

ORAL DOSAGE FORMS

A.

Tablet
Tablet is hard, compressed medication in round, oval or
square shape. Solid dosage form containing unit dose of one
or more medicament.

(Damodharan, 2010).

B. Capsule
Capsule is a medication in a gelatin container. Capsule is a solid dosage form. The
advantage is mask the unpleasant taste of its contents. There is two mainty pesof capsules
are: Hard-shelled capsules,which are normally used for dry, powdered ingredients, and
soft-shelled capsules, primarily used for oils and for active ingredients that are dissolved or
suspended in oil.

(Damodharan, 2010).

C. Emulsion
Oral emulsions are stabilized oil-in-water dispersions, either or
both phases of which may contain dissolved solids either oil is
dispersed in finely divided form in water or vice versa.

(Damodharan, 2010).

D. Suspension
Liquid preparations for oral use containing one or more active
ingredients suspended in a suitable vehicle. May show a
sediment which is readily dispersed on shaking to give a
uniform suspension which remains sufficiently stable to enable
the correct dose to be delivered.

(Damodharan, 2010).

D. Syrup

It is a concentrated aqueous solution of a sugar, usually

sucrose to which medicaments are added. Flavored syrups
are a convenient form of masking disagreeable tastes.

(Damodharan, 2010).

E. Elixir
It is pleasantly flavored clear liquid oral preparation of potent or
nauseous drugs. The vehicle may contain a high proportion of ethanol
or sucrose together with antimicrobial preservatives which confers the
stability of the preparation.

(Damodharan, 2010).

TOPICAL DOSAGE FORMS

A.

Ointments
Ointments are semi-solid, greasy preparations for application to the skin,rectumor
nasal mucosa. The base is usually anhydrous and immiscible with skin secretions.
Ointments may be used as emollients or to apply suspended or dissolved
medicaments to the skin

(Damodharan, 2010).

B. Pastes
Pastes are basically ointments into which a high percentage of insoluble solid
has been added. The extraordinary amount of particulate matter stiffens the
system.

(Damodharan, 2010).

PARENTERAL DOSAGE
FORMS
There are several methods of injection, including:
A. Intravenous injection:
It is a liquid administered directly into the bloodstream via a vein. It is advantageous when a rapid onset of action is
needed.
B. Intramuscular injection:
It is the injection of a substance directly into a muscle. Many vaccines are administered intramuscularly. Depending on
the chemical properties of the drug, the medication may either be absorbed fairly quickly or more gradually.
C. Subcutaneous injection:
Subcutaneous injections are given by injecting a fluid into the subcutis,the layer of skin directly below the dermis and
epidermis. Subcutaneous injections are highly effective in administering vaccines and such medications as insulin
(Damodharan, 2010).

(Damodharan, 20xx).

INHALED DOSAGE FORMS

A.

Inhaler

Inhalers ares olutions,suspensions or emulsion of drugs in a mixture of inert

propellants heldunder pressure in an aerosol dispenser. Insome types, the valve is
actuated by finger pressure,the valve is actuated by the patient breathing in through
the mouth piece. It is commonly used to treat as asthma respiratory problems.

(Damodharan, 2010).

OPHTHALMIC DOSAGE
FORMS
A.

Eyes-Drop
Eye drops are saline-containing drops used as a vehicle to
administer medication in the eye.

(Damodharan, 2010).

OTIC DOSAGE FORMS

A.

Ears-Drop

Ear drops are solutions, suspensions or emulsions of drugs that are instilled
into the ear with a dropper. It is used to treator prevent ear infections,
especially infection soft ear canal.

(Damodharan, 2010).

Physical and Chemical

Characteristic Of Drug

Chemical Characteristic Of Drug

1.

pKa

.The ionizability of a compound is indicated by pKa.

.Ionizability

is

major

determinant

of

solubility

and

permeability.
.When pH=pKa, the concentrations of ionized and neutral

molecules in solution are equal.

.Basicity of bases increases as pKa increases; acidity of acids

increases at pKa decreased (Kerns & Di, 2008).

The Henderson-Hasselbach equation is a useful relationship for

discovery.

For acids:

pH = pKa+logA/HA or HA/A = 10pKapH

For bases:

pH = pKa +logB/HB+ or BH+/B = 10pKapH

(Kerns & Di, 2008).

2.

Permeability

.Permeability is the velocity of molecule passage through a

membrane barrier.
.Permeability is a determinant of intestinal absorption and oral

bioavailability.
.Optimizing passive diffusion is productive because it is the

predominant mechanism for absorption of most commercial drugs.

. Permeability is increased by removing ionizable groups, and

decreasing size and polarity

(Kerns & Di, 2008).

Physical Characteristic Of Drug

1. Solubility
Solubility is the maximum dissolved concentration under given

solution conditions.
Solubility is a determinant of intestinal absorption and oral

bioavailability.
Solubility is increased by adding ionizable groups.
Salt forms increase dissolution rate
(Kerns & Di, 2008).

2. Lipophilicity
The lipophilicity of a compound is commonly estimated using Log P from

octanol/water partitioning.
Lipophilicity is a major determinant of many ADME/Tox properties.
Lipophilicity is a property that has a major effect on absorption, distribution,

metabolism, excretion, and toxicity (ADME/Tox) properties as well as

pharmacological activity.
Lipophilicity can be quickly measured or calculated. Lipophilicity has been

correlated to many other properties, such as solubility, permeability,

metabolism, toxicity, protein binding, and distribution.
(Kerns & Di, 2008).

 The relationship between the physical and chemical properties of

drug is about the biological activity of the drug itself.

Ionization is closely associated with the process of drug

penetration into biological membranes and bind to the receptor.

And to be able to make biological activity, usually in the form of

non-ionized drugs

(Kerns & Di, 2008).

On a weak acidic drug, with increasing pH, ionization properties

grew large, unionized forms become smaller, so that the amount

of drugs that penetrate biological membranes is getting smaller.
Consequently the possibility of drugs to interact with receptors

will be lower and the drug wouldnt provide therapeutic effects

(Kerns & Di, 2008).

Classification Of Drug
Molecule Based On BCS

According to the BCS, drug substances are

classified as follows:
Class I - High Permeability, High Solubility
Class II - High Permeability, Low Solubility
Class III - Low Permeability, High Solubility
Class IV

- Low Permeability, Low Solubility

(Shargel, 1988).

Provisional BCS Classification

Fig. 1. The Biopharmaceutics Classification System as
defined by
Amidon et al.(5). The BCS classifies drugs by their
solubility and
permeability properties in order to stand for the most
fundamental

CLASS BOUNDARIES
A drug substance is considered HIGHLY SOLUBLE when the highest dose

strength is soluble in < 250 ml water over a pH range of 1 to 7.5.

A drug substance is considered HIGHLY PERMEABLE when the extent of

absorption in humans is determined to be > 90% of an administered dose, based

on mass-balance or in comparison to an intravenous reference dose.

A drug product is considered to be RAPIDLY DISSOLVING when > 85% of the

labeled amount of drug substance dissolves within 30 minutes using USP

apparatus I or II in a volume of < 900 ml buffer solutions.

(Shargel, 1988).

References
Damodharan,N. (2010). Dosage Form Unit. SRM College Of Pharmacy
Edward KH, Li D. (2008). Drug Like Properties: Concept, Structure, Design
and Methods, from ADME to Toxicity Optimization. Elsevier : London.
Shargel,L., Andrew

B.C.,

Susanna

WuPong.

(2004).

Applied

Biopharmaceutics and Pharmacokinetics 5th edition. Department of

Pharmaceutics.Virginia Commonwealth University
Shargel,L.(1988). Applied Biopharmaceutics and Pharmacokinetics 3rd
edition. Department of Pharmaceutics.Virginia Commonwealth University

THANK YOU