Dry Process Induced Phase Transited Drug Delivery System: A Means for Delivery of a GI Irritant Drug

Abstract

An in-situ formed phase transited, nondisintegrating, controlled release, asymmetric membrane capsular system for the poorly water soluble model drug ketoprofen was developed and evaluated in vitro to assess for osmotic and controlled release and in vivo to assess the ability of the fabricated dosage form to control GI disturbances caused by the drug. In situ formed asymmetric membrane capsule (AMC) was made by dry
method via precipitation of asymmetric membrane of ethylcellulose on the walls of hard gelatin capsule. Effect of varying osmotic pressure (created by osmogen-sodium chloride) of the dissolution medium on drug release was studied. Acute toxicity studies and histomorphological analyses were conducted in rats. Membrane characterization by scanning electron microscopy showed an outer dense region with less pores
and an inner porous region for the prepared asymmetric membrane. In vitro release studies for all the prepared formulations were done (n = 3). Statistical test was applied for in vitro drug release at P >0.05. The drug release was found to be independent of the pH but dependent on the osmotic pressure of the dissolution medium. In vivo studies lent favourable support to the fabricated system in preventing gastric
disturbances.

Keywords: in situ, phase transited, asymmetric membrane capsule, ketoprofen, ethylcellulose

Ethiopian Pharmaceutical Journal Vol. 25 (2) 2007: pp. 121-130