TITLE

Solid dispersion a novel technique for solubility enhancement of poorly water soluble drug gliclazide

AUTHOR(S)
Shep, Santosh G.; Vinayak, Mundhe; Shep, Sachin G.; Chandewar, A. V.
PUB. DATE
March 2012
SOURCE
Journal of Pharmacy Research;2012, Vol. 5 Issue 3, p1706
SOURCE TYPE
Academic Journal
DOC. TYPE
Article
ABSTRACT
The aim of this study is to develop a novel sustained-release system for poorly water-soluble drugs by applying solid dispersion technique for improving the solubility. Solubility is an important determinant in drug liberation and absorption and hence plays a key role in its bioavailability. For a drug to be absorbed, it must be present in the form of an aqueous solution at the site of absorption. Solubility of a drug candidate is an important aspect for the formulation development. Thus poor aqueous solubility is a very challenging problem in drug formulation. "A dispersion of one or more active ingredients in an inert carrier or matrix at solid state prepared by the melting (fusion), solvent, or melting-solvent method is called as solid dispersion" Solid dispersion is one of the most promising approach for solubility enhancement. A combination of solid dispersion and sustained release technique is one of the attractive approaches since supersaturation of drugs can be achieved by solid dispersion. Gliclazide is an oral hypoglycemic (anti-diabetic drug) and is classified as a sulfonylurea. Gliclazide is used for control of hyperglycemia in gliclazide-responsive diabetes mellitus of stable, mild, non-ketosis prone, maturity-onset or adult type. It is used when diabetes cannot be controlled by proper dietary management and exercise or when insulin therapy is not appropriate. The principal action of sulfonylureas is on B-cells, stimulating insulin secretion and thus reducing plasma glucose. High affinity receptors for sulfonylureas are present on the K-ATP channels in B-cells plasma membranes and the binding of various sulfonylureas parallels their potency in stimulating insulin release. The drug reduce the k+ permeability of B-cells by blocking K-ATP channels, causing depolarization, ca2+ entry and insulin secretion.
ACCESSION #
87543413

 

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