1.

6 BCS CLASSIFICATION
The biopharmaceutical classification system (BCS) (by Amidon and coworkers
kers in
in 1995)
new concept in the field of pharmaceutical science and technology. This is a valuable to
1995) i
l for
the formulation scientists, for the selection and design of the formulation of anv

substance. It is an experimental model that measures permeability and solubility drug

ty unde
und
prescribed conditions. The recent developments have also enabled us t o predict the
solubility and permeability characteristics of the drug molecule in the early developmerthe
stages so that the necessary structural changes can be made to the molecule in order
ment
to
optimize the pharmacokinetic parameters. This system is mostly utilized in developmento
of
oral drug delivery since the majority of drugs are and remain orally dosed.

BCS system classifies drugs in to 4 categories on the basis of solubility and permeability
A
drug substance is considered soluble" when the highest clinical dose strength
strength is
"highly
soluble in 250 mL or less of aqueous media over a pH range of 1-7.5 at 37 °C. A
7 °C. A drue
substance is considered to be "highly permeable" when the extent of the absorption (parens
drug
drug plus metabolites) in humans is determined to be 290% of an administered dose basea
on a mass balance determination in comparison
or to an intravenous reference dose
Class I: Drugs having high solubility as well as permeability are placed in class first. These
dissolution and absorption
drugs show fast dissolution and rapid bioavailability. Since the
studies are unnecessary for
of class I drugs is very fast, bioavailability and bioequivalence
candidates for controlled drug delivery.
the products of such drugs. These drugs are good
in this case.
Gastric emptying is often the rate governing parameter

Class II: Drugs having low solubility and high permeability

belongs to this class; hence, the
These drugs exhibit variable
dissolution rate becomes limiting factor for bioavailability.
different methods for
the dissolution rate by
bioavailability and need enhancement in release drug delivery.
also suitable for controlled
improvement in bioavailability. These are
in this class.
but low permeability are placed
Class III: Drugs which shows high solubility
forms the rate-determining step for these
Permeation through the intestinal membrane
is independent of drug
is permeation rate limited, bioavailability
drugs. Since absorption exhibit low bioavailability and
release from the dosage form. These drugs generally
These drugs are problematic for controlled
enhancement is generally required.
permeability
release development. have poor
class show less solubility
and permeability. These drugs
Class IV: Drugs of this
several factors such as
The overall bioavailability is governed by
and variable bioavailability.
emptying etc. These drugs are generally
intestinal permeability, gastric
rate of dissolution, such as
or else s o m e special drug delivery technologies
not suitable for oral drug delivery
be needed.
nanosuspensions will
 Table 1.1:
Biopharmaceutical Classification System (BCS)
Sr.
Class Solubility
No. Permeabilily Absorption/ IVIVC Example

1. High High Well absorbed. Good Metoprolol,

VIVC Verapamil

II Low | Glibenclamide,
2 High Dissolution is rate limiting.
IVIVC with high dose Aceclofenac

3. II High Low Permeability is rate limiting.| Cimetidin,

No IVIVC Captopril

dissolution/ No Chlorothiazide,
IV Low Low No
absorption. No IVIVC Taxol, Bifonazol

Significance of BCS classification

characteristics of a drug then
i. If formulator is aware of the solubility and permeability
that to get the optimum
drug
he can easily decide drug delivery technology for
pharmacokinetic characteristics.
of the drug, so one can
ii. The BCS provides a clue about the pharmacokinetic properties
as to optimize the
in the chemical structure of the drug entity
so
manipulate and
of the lead molecule for desired drug delivery
physicochemical parameters
targeting characteristics.
under which IVIVCs
ii. BCS provides basic information for determining the conditions
are expected.
both time as well as money.
iv. It can bypass the BA/BE studies saving for efficient
tremendous tool
information it can prove a
V. When integrated with other
drug development.
and clinical drug development process.
vi. It is applicable in both pre-clinical becomes
and permeability of class I drugs targeted delivery
vii. Due to high solubility and
include both the control of release rate
difficult. Formulation approaches
of the drug.
properties of drugs like the pH-solubility profile
physiochemical
vii. The dosage forms containing class II drugs are require micronization, lyophilizas zation,
and microemulsion systeme
addition of surfactants, and formulation as emulsions
of complexing agents like cyclodextrins etc approaches to improve solubility use ns,
or
dissolution.
ix address the fundamental limitass.
Class II drugs are required for technologies that ations
of absolute permeability. Peptides and proteins constitute, solely, the
cl
or regional
delivery.
lass
drugs; these are now the center of focus for research drug
l
in

The class IV drugs present a major challenge for the development

of drug delivos
systems and the route of choice, due to their poor solubility and permeability
ery
with the formulaio
characteristics. These are often administered by parenteral route n
containing solubilityenhancers.