2004•Zhongguo linchuang yaolixue yu zhiliaoxueRequires access
Impact of CYP3A4 and P-glycoprotein on drug disposition in intestine
Hua‐Wen Xin
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Abstract
Intestinal CYP3A4-mediated biotransformation and active efflux of absorbed drug by P-glycoprotein are major determinants of bioavailability of orally administered drugs. The expression of CYP3A4 and P-glycoprotein in the intestine is not co-ordinately regulated. However, synergistic actions of CYP3A4 and P-glycoprotein in intestinal drug disposition have been confirmed by in vitro and animal studies. Further understanding of this interaction would be potentially useful to improve oral bioavailability of CYP3A4/P-glycoprotein substrates.