Technical Note: Using Biorelevant Media with Different Types of Orally Administered Formulations

Abstract

One of the most important aims of formulation development for a poorly soluble new chemical entity (NCE) or active pharmaceutical ingredient (API) is to enhance bioavailability. For orally administered compounds, this can be broadly assessed by knowing the solubility and the permeability of a compound. The Biopharmaceutical Classification System (BCS) proposed by Amidon et.al in 1995 (1) uses these two parameters to classify an NCE. If a compound is to be administered orally, the solubility in small intestinal fluids is particularly important because most compounds are absorbed in this region of the gastrointestinal tract. Therefore, information on how a formulation potentially enhances performance can be assessed by testing its solubility or dissolution rate in biorelevant media (2–4). The use of biorelevant media such as Fed State Simulated Intestinal Fluid (FeSSIF) and Fasted State Simulated Intestinal Fluid (FaSSIF) is particularly important for poorly water-soluble compounds because they simulate the solubilizing environment of mixed micelles. They comprise a bile salt and lecithin, which are responsible for the emulsification and absorption of dietary fats in humans and animals. This note reviews how biorelevant media can be used to assess the performance of different formulations for poorly water-soluble compounds.