Comparison of in vitro intestinal and hepatic metabolism of diltiazem by ultra-performance liquid chromatography accurate mass spectrometry

摘要

Diltiazem metabolite profiles were established for liver and intestinal microsomes from human and rat. Major metabolites observed were formed by heteroatom dealkylation, hydroxylation and ester hydrolysis or a combination thereof. Relative metabolite abundance across test systems known for differential carboxylesterase expression implicated CE1 as the carboxylesterase predominantly responsible for diltiazem hydrolysis.