The AAPS Journal

, Volume 15, Issue 4, pp 1043–1050 | Cite as

Impact of Osmotically Active Excipients on Bioavailability and Bioequivalence of BCS Class III Drugs

  • Mei-Ling Chen
  • Nakissa Sadrieh
  • Lawrence Yu
Regulatory Note


The Biopharmaceutics Classification System (BCS), based on aqueous solubility and intestinal permeability, has been widely used to predict drug absorption during pharmaceutical development (1). Recently, the system has also been employed in regulatory practice to determine if waiver of in vivo bioavailability or bioequivalence studies (i.e., biowaivers) can be granted for an immediate-release solid oral dosage form (2). In this regard, the US Food and Drug Administration (FDA) currently allows biowaivers for BCS class I (highly soluble and highly permeable) drugs formulated in immediate release, rapidly dissolving drug products (2). Since the publication of the FDA Guidance on BCS in 2000, however, there has been continued interest in the possible extension of BCS-based biowaivers, particularly for class III drugs that exhibit high solubility and low permeability (3, 4, 5).

One of the major challenges to the allowance of biowaivers for BCS class III drugs is related to the...

Key words

BCS bioavailability/bioequivalence drug absorption excipient osmotic potential 


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Copyright information

© American Association of Pharmaceutical Scientists 2013

Authors and Affiliations

  1. 1.Center for Drug Evaluation and Research, Food and Drug AdministrationSilver SpringUSA

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