Abstract

ENHANCEMENT OF DISSOLUTION PROPERTIES OF REPAGLINIDE BY SOLID DISPERSION TECHNIQUE USING SYLYSIA AS CARRIER

Bharathi Arigela*, Roja Sali, Aswini Priya Vaida, Anusha Nadikatla, Priyanka Garikapati

ABSTRACT

Solid dispersions in water soluble carriers have attracted considerable interest as a means of improving the dissolution rate, and hence possibly bioavailability of a range of hydrophobic drugs. The present study was aimed to enhance and evaluate the dissolution rate of Repaglinide (REP) by solid dispersion technique using various grades of sylysia (SYL) for better absorption. The poor solubility of REP leads to poor dissolution and hence variation in bioavailability. The solid dispersions were prepared by solvent evaporation and kneading methods in two different mass ratios 1:1 and 1:2 w/w and effect of the methods on improvement REP dissolution as also investigated. Physicochemical characterisation of disperse systems was carried out using differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction studies (XRD). The in- vitro drug release studies were carried out in 0.1N HCl up to 2 hrs and data was evaluated on the basis of cumulative percentage drug release. The prepared solid dispersions were also evaluated for REP content. Based on the in-vitro drug release profiles, 1:2 ratio kneaded systems prepared by SYL 430 showed better drug release (99.84%) compared to dispersions prepared by solvent evaporation method. Mathematical treatment of the in vitro drug release data suggests that, all the solid dispersion compacts fitted into first order release kinetics. Physicochemical characterisation results suggested that REP existed in amorphous form in all dispersion systems which show that dissolution can be enhanced.

Keywords: Dissolution, Kneading method, Repaglinide, Solvent evaporation method, Solid dispersions, Sylysia.