AN APPROACH FOR IMPROVEMENT OF THE WATER SOLUBILITY OF GLICLAZIDE IN SOLID DISPERSION WITH PEG 4000Abstract
Gliclazide is a second-generation hypoglycaemic sulfonylurea that is useful in the treatment of Type 2 diabetes mellitus. It shows low aqueous solubility and dissolution rate and often shows low and irregular bioavailability after oral administration. This paper describes an approach to improve the Solubility of gliclazide by using solid dispersions (SDs) in polyethylene glycol 4000 (PEG 4000). Solid dispersions were prepared by a solvent-melting method and Solubility determinations were performed in triplicate according to the method of Higuchi and Connors. The solubility of gliclazide is 0.86 mg/ml in water but after the addition of different concentration of PEG 4000, the solubility of gliclazide is increased maximum 3.07 mg/ml at 20%w/v of PEG 4000, was observed. The main conclusion of this article is that the solubility of gliclazide can be enhanced in Solid Dispersion with PEG 4000. The solubilization effect of PEG 4000, reduction of particle aggregation of the drug, absence of crystallinity, increased wettability and dispersibility, and alteration of surface properties of the drug particles may be responsible for the enhanced solubility of gliclazide from its Solid Dispersion.