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药代动力学概述。

Overview of pharmacokinetics.

作者信息

Aimone Lisa D, de Lannoy Inés A M

机构信息

Teva Pharmaceuticals, Malvern, Pennsylvania.

InterVivo Solutions, Toronto, Ontario, Canada.

出版信息

Curr Protoc Pharmacol. 2014 Sep 2;66:7.1.1-7.1.31. doi: 10.1002/0471141755.ph0701s66.

Abstract

In addition to having selective potency against the molecular target(s), a compound must be able to reach its intended site of action in vivo in sufficient quantity and for the appropriate duration of time to exert a biological effect. The fate of a compound after in vivo administration depends upon its absorption, distribution, metabolism, and excretion (ADME), as well as its target residence time. The concentration of the compound in the blood, plasma, and other tissues represents the sum of all of these processes. Described in this unit are protocols for administering a compound by various routes to rats and for collecting the appropriate samples to determine the pharmacokinetics profile. The basic terms used in pharmacokinetics studies are defined, and representative examples are given to illustrate important variables to consider.

摘要

除了对分子靶点具有选择性效力外,化合物还必须能够以足够的量并在适当的时间内到达其体内的预期作用部位,以发挥生物学效应。化合物在体内给药后的命运取决于其吸收、分布、代谢和排泄(ADME),以及其靶点停留时间。化合物在血液、血浆和其他组织中的浓度代表了所有这些过程的总和。本单元描述了通过各种途径给大鼠给药化合物以及收集适当样本以确定药代动力学特征的方案。定义了药代动力学研究中使用的基本术语,并给出了代表性示例来说明需要考虑的重要变量。

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