Abstract

SOLUBILITY ENHANCEMENT OF POORLY SOLUBLE DRUG BY VARIOUS TECHNIQUES

Sandip A. Bandgar*, Sardar S. Shelake and Shitalkumar S. Patil

ABSTRACT

Oral route is the easiest and convenient route but it may be produce problem when the drug molecules which shows poor aqueous solubility. These are classified as Class II drugs Biopharmaceutical Classification System (BCS-II) i.e. drugs with poor solubility and high permeability. So by using various methods a solubility of drug is get increases. In this present study we developed a tablet of poorly water soluble drug Ezetimibe by preparing solid dispersion of it. Solid dispersions are one of the most promising strategies to improve the oral bioavailability of poorly water soluble drugs. The purpose of this study was to increase solubility of Ezetimibe by solid dispersion (SDs) technique with Kolliphor P 237 in aqueous media. The Ezetimibe - Kolliphor P 237 solid dispersion was prepared by solvent evaporation method. It was characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), Fourier transformation infra-red spectroscopy (FT-IR), scanning electron microscopy (SEM) and in vitro dissolution studies. The prepared solid dispersion was found to have higher dissolution rates as compared to intact Ezetimibe. During formulation of solid dispersion crystalline to amorphous transition has been observed. By using solid dispersed powder of Ezetimibe, prepared tablet showed greater drug release (98.47±1.13%) as compared with conventional tablet.

Keywords: Solubility Enhancement, BCS-II, Poorly Soluble Drug, Solid Dispersion, Spherical Crystallization, Ezetimibe.