Journal
CURRENT DRUG METABOLISM
Volume 8, Issue 7, Pages 676-684Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/138920007782109733
Keywords
first-pass metabolism; gut metabolism; CYP3A; P-glycoprotein; drug transport; well-stirred model
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Despite a lower content of many drug metabolising enzymes in the intestinal epithelium compared to the liver (e.g. intestinal CYP3A abundance in the intestine is 1% that of the liver), intestinal metabolic extraction may be similar to or exceed hepatic extraction. Modelling of events on first-pass through the intestine requires attention to the complex interplay between passive permeability, active transport, binding, relevant blood flows and the intrinsic activity and capacity of enzyme systems. We have compared the predictive accuracy of the well-stirred gut model with that of the Q(Gut) model. The former overpredicts the fraction escaping first-pass gut metabolism; the latter improves the predictions by accounting for interplay between permeability and metabolism.
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