Enhancement of Dissolution profile of poorly water soluble drug using Water Soluble Carriers

Abstract

Teneligliptin Hydrobromide is a long-acting, orally bioavailable, pyrolidone anti-diabetic activity with a solubility of 1.7mg/ml in water which also depends upon the pH and temperature of the solvent. So, Solid dispersion of drug with different polymers an attempt was made to improve dissolution of teneligliptin hydrobromide. The aim of this study was to prepare, characterize and compare solid dispersions of poorly water soluble anti diabetic drug by using PVP and HPMC for enhancing the dissolution rate of the drug. The solid dispersions were prepared by physical mixing method and kneading method at 1:1, 1:2 and 2:1 ratios of drug to polymer. The drug-excipient interaction study showed that the drug and polymers were compatible with each other. The formulations were evaluated for percent drug content, micromeritics and in-vitro dissolution studies. In the present study it was seen that there was an increase in in-vitro drug release for solid dispersion as compared to the pure drug taken alone. Based on the pattern of drug release, the kneading method showed more drug release as compared to physical mix method. In physical mix method, the rate of dissolution of teneligliptin hydrobromide was increased in teneligliptin and Polyvinylpyrrolidone (PVP) with the proportion of (1:2) when compared to the other formulations. In kneading method, the rate of dissolution of teneligliptin hydrobromide was increased in drug and Hydroxypropylmethylcellulose (HPMC) with the proportion of (1:2) when compared to the other formulations. Finally, solid dispersion containing HPMC, as a carrier, gave faster dissolution rates among all the formulations and was selected as the optimized formulation inthis study.