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一种用于估算经肝代谢和肾排泄以外途径消除的药物量以及口服给药后到达“首过”的药物分数的简便方法。

A convenient method for estimating the quantity of drug eliminated by the routes other than hepatic metabolism and renal excretion and the fraction of drug that reaches the "first pass" after oral administration.

作者信息

Berezhkovskiy Leonid M

机构信息

Roche Palo Alto LLC, Palo Alto, California 94304, USA.

出版信息

J Pharm Sci. 2006 Apr;95(4):828-33. doi: 10.1002/jps.20479.

DOI:10.1002/jps.20479
PMID:16489605
Abstract

The comparison of routine pharmacokinetic data obtained after intravenous and oral drug administration allows to figure out that some quantity of drug, which reached the systemic circulation, was eliminated from the body by routes other than hepatic metabolism and renal excretion. This quantity is equal or exceeds the certain minimum value, which can be calculated from a simple equation obtained in the article. If the minimum value is equal to zero, then the maximum possible fraction of orally administered drug, that is, absorbed into the gut wall and gets through it unchanged, can be calculated. The examples considered indicate that the quantity of drug eliminated not by liver metabolism or kidney excretion could be quite substantial (exceeds half of the dose that reached the circulation).

摘要

静脉注射和口服给药后获得的常规药代动力学数据的比较表明,一些进入体循环的药物是通过肝代谢和肾排泄以外的途径从体内消除的。这个量等于或超过某个最小值,该最小值可以从文章中得到的一个简单方程计算得出。如果最小值等于零,那么就可以计算出口服给药药物的最大可能分数,即吸收到肠壁并原样通过肠壁的分数。所考虑的例子表明,非肝脏代谢或肾脏排泄所消除的药物量可能相当可观(超过进入循环剂量的一半)。

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