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药物在外周组织中的单次通过平均驻留时间:一个反映药物组织亲和力的内在分布参数。

Single pass mean residence time in peripheral tissues: a distribution parameter intrinsic to the tissue affinity of a drug.

作者信息

Veng-Pedersen P, Gillespie W R

出版信息

J Pharm Sci. 1986 Dec;75(12):1119-26. doi: 10.1002/jps.2600751202.

DOI:10.1002/jps.2600751202
PMID:3559920
Abstract

The single pass mean residence time in peripheral tissues, tp1, is a characteristic constant of linear pharmacokinetic systems and nonlinear systems with linear distribution kinetics. It is descriptive of distribution kinetics in such systems and is not dependent on elimination kinetics as are other related parameters, e.g., mean residence time in peripheral tissues, tp. Equations are derived which permit estimation of tp1 from experimental data for systems in which no peripheral elimination occurs. The type of data required are systemic drug levels resulting from iv administration. The probability density function for single pass residence time in peripheral tissues is derived. It is shown that tp1 is related to the amount of drug in the peripheral tissues at steady state according to (Ap)ss = CLdCsstp1, where CLd is the distribution clearance, and Css is the steady-state systemic drug level. Values of tp1 are presented for several drugs.

摘要

外周组织中的单次通过平均驻留时间tp1是线性药代动力学系统以及具有线性分布动力学的非线性系统的一个特征常数。它描述了此类系统中的分布动力学,并且不像其他相关参数(例如外周组织中的平均驻留时间tp)那样依赖于消除动力学。推导了一些方程,这些方程允许从无外周消除发生的系统的实验数据中估算tp1。所需的数据类型是静脉给药后的全身药物水平。推导了外周组织中单次通过驻留时间的概率密度函数。结果表明,根据(Ap)ss = CLdCsstp1,tp1与稳态时外周组织中的药量相关,其中CLd是分布清除率,Css是稳态全身药物水平。给出了几种药物的tp1值。

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