Simplified biorelevant media for screening dissolution performance of poorly soluble drugs

Abstract

Selected media containing synthetic surfactants with physicochemical properties similar to those of FaSSIF and FeSSIF were identified. These can be used to replace biorelevant test media for screening formulations if it can be shown that solubility and dissolution of the drug in these simplified media are similar to the profiles in biorelevant media prepared with bile components. Validation of the correspondence of results in media containing synthetic surfactants with those containing bile components is necessary on a case-by-case basis. In cases where results are similar, the simplified media represent a very promising approach to designing both formulation screening and quality control tests that are relevant to in vivo conditions, while retaining the cost and time efficiencies associated with use of synthetic surfactants. In particular, when taking into account several additional physiological parameters (i.e., pH, buffer capacity, and osmolality) in the fasted and fed small intestine, the results generated with these media should be more reliable in predicting the in vivo release behavior of a formulation than those generated with commonly used surfactant systems.