SOLUBILITY AND BIOAVAILABILITY ENHANCEMENT AND MODIFIED RELEASE FORMULATION OF POORLY WATER SOLUBLE DRUG GLICAZIDE

Anuja A. Malgunde* and Apeksha V. Masal

ABSTRACT

A drug with poor bioavailability is one with poor aqueous solubility, slow dissolution rate in biological fluids, poor stability of dissolved drug at physiological pH, poor permeation through biomembrane and extensive presystemic metabolism. Glicazide is practically insoluble in water and having limited bioavalability. To enhance the dissolution rate and oral bioavailability. The present study was aimed Solubility and Bioavailability Enhancement and Modified release formulation of poorly water soluble drug Gliclazide by using β –Cyclodextrin as a water soluble polymer using different methods physical mixture(PF1 – PF3), spray drying(SF1- SF3) and kneading method(KF1-KF3). The interaction of a pure drug with polymer was studied by Fourier Transformation-Infrared Spectroscopy and Differential Scanning Calorimetry. Formulated batches were characterized for physicochemical properties like drug content, dissolution studies. Pharmacokinetic studies of optimized formulation (KF3) were compared with pure drug. The dissolution rate of pure drug and tablet prepared by kneading method with ratio of polymer (1:3) showed 38.14% and 100.5% in the phosphate buffer pH 7.4 at 30 min. From above study it concluded that kneading method is an effective in increasing solubility and bioavailability of poorly water soluble drug.

Keywords: Gliclazide, Enhancement, Bioavailability.