Abstract

DESIGN AND DEVELOPMENT OF CONTROLLED RELEASE TABLETS OF BOSENTAN

Ch. Taraka Ramarao* and Kagupati Sridevi

Abstract

The present investigation attempt has been made to formulate controlled release matrix tablets of Bosentan using HPMC K15M, HPMC E-15 and Xanthan gum are rate controlling polymer, PVP K-30 used as binder, microcrystalline cellulose as filler. The prepared tablets were prepared by conventional wet granulation method and evaluated for pre compression and post compression parameters with different ratios. All the evaluated parameters of the formulations showed compliance with pharmacopoeial standards. The effect of polymer loading in in-vitro drug release and the mechanism of release was studied by different mathematical models. This could be retarded or maintained by the proper choice of controlling agent in order to achieve the desired release profile. The o p t i m i z e d formulation (F5) were subjected to stability studies as per ICH guidelines at different temperature and humidity conditions. It can be concluded that among all the formulations and the combinations of HPMC K15M, HEC & Metolose SR considered as the optimized formulations in the present research work. The optimized formulations follow zero order release kinetics and super case II transport release mechanism.

Keywords: Bosentan, HPMC K15M, HPMC E-15, Xanthan gum, Avicel PH102, PVP K-30 and Magnesium stearate.