Abstract

COMPARATIVE STUDIES ON SOLUBILITY ENHANCEMENT OF IRBESARTAN BY USING COMPLEXATION AND SOLID DISPERSION TECHNIQUES

M. Raj Kumar*, Y. Rama Ruchitha, B. Hari Priya, Y. Shanmmuukha, D. Murthujavali and G. Chidananda

ABSTRACT

The objective of the present investigation was to enhance the solubility and dissolution rate of poorly soluble drug irbesartan by preparing it as inclusion complexes and solid dispersions and formulating it as fast-dissolving tablets (FDTs) and compared formulated tablet invitro dissolution studies with marketed AVAPRO 75mg tablets. Irbesartan is poorly soluble in water, and this low aqueous solubility in addition to its poor wettability leads to poor bioavailability of the drug. Inclusion complexes were prepared by using HP-β-Cyclodextrin and Solid dispersions were prepared using PVP and PEG 4000, as carriers. The dispersions were prepared using the kneading methods in a 1:1, 1:2, 1:3 ratio of drug and carrier. These formulations were characterized for solid state properties using X-ray powder diffraction and Fourier transform infrared spectroscopy spectral studies. Formulations were further evaluated for dissolution. The aqueous solubility of irbesartan in inclusion complex was improved by the presence of HP-β-Cyclodextrin when compared with solid dispersion developed from other carriers. Solid state characterization indicated that irbesartan was inserted as guest into the Host carrier. This was due to efficient entrapment of the drug in polymer. Thus, the complexes prepared with HP-β-Cyclodextrin would be useful for delivering poorly soluble irbesartan with enhanced solubility and dissolution rate. Furthermore, the inclusion complex that were formulated as FDTs using super disintegrants showed faster drug release with increased dissolution rate. FDTs containing irbesartan inclusion complex prepared using the kneading method and sodium starch glycolate as super disintegrant showed faster disintegration and increased dissolution rate.

Keywords: Fast dissolving, irbesartan, Inclusion complex, HP-?-Cyclodextrin.