Provisional BCS Classification of the Leading Oral Drugs on the Global Market

Abstract

In the early 1990s, a collaborative research effort between academia and the U.S. Food and Drug Administration (FDA) was initiated to establish a database of human jejunal permeabilities based on a Biopharmaceutics Classification System (BCS). The BCS broadly allowed the prediction of human absorption, Fraction absorbed ( F abs ) and the rate‐limiting step in the intestinal absorption process of drugs following oral administration. The BCS classified compounds into one of four biopharmaceutical classes according to water solubility and membrane permeability characteristics. Today, the BCS has generated remarkable impact on the global pharmaceutical sciences arena, in drug discovery, development and regulation, and an extensive validation/discussion of the BCS is continuously published in the literature. BCS has been effectively implanted by drug regulatory agencies around the world, and widely practiced by the pharmaceutical industry. The aim of this chapter is to present the BCS and its scientific basis, to describe its impact on regulatory practice of oral drug products, and to access the BCS classification of the top drugs on the global market. Finally, current and future directions in BCS related extensions, and their impact on the pharmaceutical industry, will be discussed.

A Formulation Strategy for Gamma Secretase Inhibitor ELND006, a BCS Class II Compound: Development of a Nanosuspension Formulation with Improved Oral Bioavailability and Reduced Food Effects in Dogs

“…Poor aqueous solubility and slow dissolution are rate limiting factors in the GIT absorption of compounds that are considered BCS Class II molecules 5–8. Such compounds exhibit not only poor and erratic bioavailability but also significant fed–fasted state variability when formulated into a conventional dosage form, such as a tablet or a powder‐filled capsule 9–12.…”