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首过效应:非线性概念,包含米氏方程积分的显式解。

First-pass effect: nonlinear concept comprising an explicit solution of integrated Michaelis-Menten equation.

作者信息

Keller F, Scholle J

出版信息

J Pharm Sci. 1981 Feb;70(2):195-8. doi: 10.1002/jps.2600700221.

DOI:10.1002/jps.2600700221
PMID:7205226
Abstract

The first-pass effect results from metabolism during the first liver passage of a drug given by mouth. The metabolism is described by the Michaelis-Menten equation, but the integrated form of the Michaelis-Menten equation has no explicit solution for concentration and its handling requires a computer. However, the presented nonlinear equation of the first-pass effect is an explicit integration of the Michaelis-Menten equation and involves only general mathematics. However, the problem of evaluating the Michaelis-Menten constants Vm and Km is not resolved. Therefore, linear equations are also derived, which correspond to previous clearance models.

摘要

首过效应源于口服给药后药物在肝脏首次通过时的代谢。这种代谢由米氏方程描述,但米氏方程的积分形式没有关于浓度的显式解,其处理需要计算机。然而,所提出的首过效应非线性方程是米氏方程的显式积分,只涉及一般数学。然而,评估米氏常数Vm和Km的问题尚未解决。因此,还推导了与先前清除模型相对应的线性方程。

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引用本文的文献

1
Theoretical considerations in the calculation of bioavailability of drugs exhibiting Michaelis-Menten elimination kinetics.具有米氏消除动力学特征的药物生物利用度计算中的理论考量
J Pharmacokinet Biopharm. 1984 Aug;12(4):437-50. doi: 10.1007/BF01062667.