Colesevelam hydrochloride is a high-capacity bile acid-binding molecule, which is a non-absorbed, polymeric, lipid-lowering and glucose-lowering agent, initially marketed as Welchol.  As generic versions of marketed colesevelam tablet products are being developed for release in the market, equivalence between the generic and innovator products must be established to satisfy the FDA guidance for this class of product.  To compare the bile acid-binding activity of these products, the equilibrium and kinetic binding profiles of colesevelam hydrochloride must be compared for both the generic and innovator products.  An HPLC method with UV detection has been developed and validated to detect free bile acids (glycocholic acid, glycochenodeoxycholic acid, and taurodeoxycholic acid) in simulated intestinal fluid (SIF).  This method also accommodates conducting binding studies both with and without acid pre-treatment of the products, with no matrix interference observed.  The key parameters of the study, as well as the method will be discussed.

Method development for equilibrium and kinetic binding in vitro bioequivalence of colesevelam hydrochloride in simulated intestinal fluid (SIF)

243rd National Meeting (2012)

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