A simple, safe, and environmentally friendly method of FaSSIF and FeSSIF preparation without methylene chloride

Abstract

Biorelevant dissolution media were designed and proposed based on physiological and physicochemical properties of the small intestine luminal contents in the fasted- and fed-state conditions. Biorelevant dissolution media have proved to be an excellent in vitro tool for predicting the in vivo performance of formulations in fasted- and fed-state conditions. Taurocholic acid and lecithin are surfactants used in biorelevant dissolution media to solubilize the drugs in dissolution media, which mimics the solubilization process of drugs in vivo. Preparation of biorelevant dissolution media is tedious and complex; it involves the emulsification of lecithin with methylene chloride followed by evaporation of methylene chloride under vacuum. In this work, an attempt was made to simplify biorelevant media preparation by applying high-speed stirring without methylene chloride. Biorelevant dissolution media prepared by the stirring method were clear and transparent. The performance of the media was compared by a dissolution study of two formulations in FaSSIF and FeSSIF media prepared by both the proposed method and a conventional method. The results of the dissolution test were comparable. The proposed method of biorelevant dissolution media preparation is simple, safe, reproducible, and less time consuming.