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World Journal of Pharmaceutical Sciences
ISSN (Print): 2321-3310; ISSN (Online): 2321-3086
Published by Atom and Cell Publishers © All Rights Reserved
Available online at: http://www.wjpsonline.org/
Editorial
Solid dispersions: A feasible technique to improve the aqueous solubility of poorly
soluble drugs
Dr. D. Nagasamy Venkatesh
M. Pharm., Ph.D.,
Assistant Professor, Department of Pharmaceutics,
JSS College of Pharmacy,
(A Constituent College of Jagadguru Sri Shivarathreeswara University, Mysuru),
Udhagamandalam – 643 001. Tamil Nadu. India.
Phone: 00-91-423-2443393 (Ext-216); Fax: 00-91-423-2442937
Mobile: 08903123467, E-mail: nagasamyvenkatesh@rediffmail.com
ABSTRACT
Solid dispersion technology deals with dispersing one or more active ingredients in an inert matrix in the solid
state in order to achieve enhanced dissolution rate and stability. Upon increasing the dissolution rate in the
gastro intestinal tract, the rate of absorption is increased as long as the dissolution rate is still the rate-limiting
step. Various carriers have been used in the formation of solid dispersion, which can facilitate in improving the
dissolution rate of poorly soluble drugs to improve better bioavailability.
Key words: Solid dispersion, carriers, dissolution enhancement and applications.
INTRODUCTION
A drug must possess some aqueous solubility to
exert its therapeutic effect
1
. Due to the
advancement in chemistry lead to the effective
discovery of new drugs. However, 35-40% of these
newly discovered drugs suffer from poor aqueous
solubility
2-3
. The solubility behavior of a drug is
key determinant to its oral bioavailability, and rate-
limiting step in absorption of drugs from gastro
intestinal tract
4-6
. Poor aqueous solubility of drugs
leads to low bioavailability, increase in the dosage
and variability in blood concentrations. It is a
unique approach to present a poorly soluble drug in
an extremely fine state of subdivision in
gastrointestinal fluids. This dispersion consists of a
microcrystalline dispersion of a poorly soluble drug
in a matrix consisting of physiologically inert,
readily soluble carrier
7-10
. Exposure of this type of
solid dispersion to the gastro intestinal fluids
results in dissolution of water soluble carrier and
exposes the dispersed poorly soluble drug. The
solubility characteristics of the drug may be altered
by reduction in particle size. Several insoluble
drugs have been shown to improve their dissolution
character when incorporated into solid dispersion.
It releases the drug through different mechanisms,
and the rate of release of drug to the surrounding
fluid is mainly dependent on the type of solid
dispersion formed
11-13
. Solid dispersion technique
has been widely employed to improve the
dissolution rate, solubility and oral adsorption of
poorly water soluble drug’s
15-16
. The advantages of
solid dispersion system includes:
An increase in aqueous solubility of the
drug because of its extremely small
particle size.
Possible solubilization effect on the drug
by the carrier in the surrounding diffusion
layer.
Reduction or absence of agglomeration of
drug particles.
Excellent wettability and dispersibility of
the exposed drug particles in the gastro
intestinal fluids.
Formation of metastable polymorphic
forms.
However, solid dispersion does have certain
disadvantages which include change in crystallinity
and decrease in dissolution rate on aging. Moisture
and temperature have more detoriating effect on
these systems and handling is not easy due to
tackiness.