CYP3A4 和P 糖蛋白与药物的肠道处置

摘要/Abstract

摘要： 肠CYP3A4 介导的生物转化和P 糖蛋白介导的药物主动泵出肠细胞是决定口服药物生物利用度的主要因素。有证据显示CYP3A4 和P 糖蛋白在小肠不是共同调节的, 但两者在药物肠道处置中的协同作用已得到体外试验和动物体内试验的证实。进一步了解两者的相互作用有助于改善CYP3A4 /P 糖蛋白底物的生物利用度。

关键词: CYP3A4, P 糖蛋白, 药物代谢, 肠道, 肝脏首过代谢, 生物利用度, 相互作用

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 /-glycoprotein substrates.

Key words: CYP3A4, P-glycoprotein, drug metabolism, intestine, liver, first-pass metabolism, bioavailability, drug interaction

中图分类号:

R969.1

辛华雯. CYP3A4 和P 糖蛋白与药物的肠道处置[J]. 中国临床药理学与治疗学, 2005, 10(7): 721-725.

XIN Hua-wen. Impact of CYP3A4 and P-glycoprotein on drug disposition in intestine[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2005, 10(7): 721-725.

参考文献

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