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肝脏和肝外器官清除的药物及代谢物的代谢物曲线下面积。其对前体药物给药途径的依赖性。

The area under the curve of metabolites for drugs and metabolites cleared by the liver and extrahepatic organs. Its dependence on the administration route of precursor drug.

作者信息

Klippert P J, Noordhoek J

出版信息

Drug Metab Dispos. 1985 Jan-Feb;13(1):97-101.

PMID:2858385
Abstract

The venous equilibrium model (or well-stirred model) is used to determine the area under the blood concentration vs. time curve of a metabolite formed from a precursor drug. It will be shown that the AUC of a metabolite will change according to the route of precursor drug administration(whether intraarterially, intravenously, via the portal vein, or orally) when the drug and/or metabolite is eliminated by more than one organ. Elimination includes hepatic and extrahepatic metabolism and renal excretion. The validity of the model is probed by using literature data for drug and metabolite areas. Finally, the use of metabolite areas for evaluating the complete/incomplete absorption or orally administered precursor drug is discussed.

摘要

静脉平衡模型(或充分搅拌模型)用于确定由前体药物形成的代谢物的血药浓度-时间曲线下面积。当药物和/或代谢物由不止一个器官消除时,将表明代谢物的AUC会根据前体药物的给药途径(无论是动脉内、静脉内、经门静脉还是口服)而变化。消除包括肝脏和肝外代谢以及肾脏排泄。通过使用药物和代谢物面积的文献数据来探究该模型的有效性。最后,讨论了使用代谢物面积来评估口服前体药物的完全/不完全吸收情况。

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The area under the curve of metabolites for drugs and metabolites cleared by the liver and extrahepatic organs. Its dependence on the administration route of precursor drug.肝脏和肝外器官清除的药物及代谢物的代谢物曲线下面积。其对前体药物给药途径的依赖性。
Drug Metab Dispos. 1985 Jan-Feb;13(1):97-101.
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引用本文的文献

1
A review of metabolite kinetics.代谢物动力学综述。
J Pharmacokinet Biopharm. 1985 Dec;13(6):633-62. doi: 10.1007/BF01058905.
2
Primary, secondary, and tertiary metabolite kinetics.初级、次级和三级代谢物动力学。
J Pharmacokinet Biopharm. 1988 Oct;16(5):493-527. doi: 10.1007/BF01062382.
3
Physiological modeling of drug and metabolite: disposition of oxazepam and oxazepam glucuronides in the recirculating perfused mouse liver preparation.药物及代谢物的生理模型:奥沙西泮及其葡糖醛酸苷在再循环灌注小鼠肝制备物中的处置
J Pharmacokinet Biopharm. 1990 Oct;18(5):423-48. doi: 10.1007/BF01061703.
4
Absolute bioavailability of clarithromycin after oral administration in humans.克拉霉素口服给药后在人体内的绝对生物利用度。
Antimicrob Agents Chemother. 1992 May;36(5):1147-50. doi: 10.1128/AAC.36.5.1147.