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胃肠道中口服药物的损失。

Loss of orally administered drugs in GI tract.

机构信息

Dept. of Pharmaceutics, Govt. College of Pharmacy, Karad (MS), India.

出版信息

Saudi Pharm J. 2012 Oct;20(4):331-44. doi: 10.1016/j.jsps.2012.03.005. Epub 2012 Apr 20.

DOI:10.1016/j.jsps.2012.03.005
PMID:23960808
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3744959/
Abstract

The aim of this review is to provide a broad perspective on intestinal absorption and the impact of intestinal first-pass metabolism on both clearance and drug-drug interaction prediction along with its historical perspectives. The review also considers abilities to bridge the gap between the increasing amount of intestinal in vitro data and the importance of intestinal first-pass metabolism in vivo. The significance of efflux transporters on the intestinal absorption is also discussed.

摘要

本次综述旨在提供一个广泛的视角，讨论肠道吸收以及肠道首过代谢对清除率和药物相互作用预测的影响，同时回顾其历史发展。本文还考虑了如何弥合肠道体外数据量不断增加与体内肠道首过代谢重要性之间的差距。本文还讨论了外排转运体对肠道吸收的重要性。

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P-glycoprotein efflux inhibition by amphiphilic diblock copolymers: relationship between copolymer concentration and substrate hydrophobicity.两亲性二嵌段共聚物对P-糖蛋白外排的抑制作用：共聚物浓度与底物疏水性之间的关系。
Mol Pharm. 2008 Jul-Aug;5(4):643-53. doi: 10.1021/mp7001347. Epub 2008 Apr 2.
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Strategies to in vitro assessment of major human CYP enzyme activities by using liquid chromatography tandem mass spectrometry.利用液相色谱串联质谱法对主要人细胞色素P450酶活性进行体外评估的策略。
Curr Drug Metab. 2008 Jan;9(1):12-9. doi: 10.2174/138920008783331112.
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Inhibitory effect of docosahexaenoic acid (DHA) on the intestinal metabolism of midazolam: in vitro and in vivo studies in rats.二十二碳六烯酸（DHA）对咪达唑仑肠道代谢的抑制作用：大鼠的体外和体内研究
Int J Pharm. 2008 Mar 3;351(1-2):133-43. doi: 10.1016/j.ijpharm.2007.09.037. Epub 2007 Oct 5.
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Tofisopam inhibits the pharmacokinetics of CYP3A4 substrate midazolam.托非索泮抑制CYP3A4底物咪达唑仑的药代动力学。
Eur J Clin Pharmacol. 2008 Jan;64(1):93-4. doi: 10.1007/s00228-007-0397-y. Epub 2007 Nov 8.
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Intestinal first-pass metabolism: bridging the gap between in vitro and in vivo.肠道首过代谢：弥合体外与体内之间的差距
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