Sustained release solid dispersion of a BCS class II Drug

Abstract

The present study aims to develop a sustained-release solid dispersion (SRSD) of a Biopharmaceutical Classification System (BCS) Class II drug by employing a blend of polymers. The SRSD was prepared by kneading technique, followed by solvent evaporation using rotary evaporator. After conducting an equilibrium solubility study, SRSD (F5) was found to be the optimal formulation. The dissolution profiles of SRSD (F5) were examined at different pH values. Since Carvedilol exhibits pH dependent solubility, the drug release from SRSD (F5) was limited at pH 6.8 and increased at pH 1.2. The structural characteristic of SRSD (F5) was examined by using powder X-ray diffraction (PXRD), which shows a change in drug crystallinity to an amorphous form. The results obtained from the dissolution study suggest that SRSD (F5) could be a promising approach for developing sustained-release oral dosage form of Carvedilol, thereby reducing the dosing frequency and improving the oral bioavailability.