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手性药物:概述

Chiral drugs: an overview.

作者信息

Nguyen Lien Ai, He Hua, Pham-Huy Chuong

机构信息

Department of Pharmacy, Lucile Salter Packard Children's Hospital, Stanford University Medical Center, 725 Welch Road, Palo Alto, USA;

出版信息

Int J Biomed Sci. 2006 Jun;2(2):85-100.

Abstract

About more than half of the drugs currently in use are chiral compounds and near 90% of the last ones are marketed as racemates consisting of an equimolar mixture of two enantiomers. Although they have the same chemical structure, most isomers of chiral drugs exhibit marked differences in biological activities such as pharmacology, toxicology, pharmacokinetics, metabolism etc. Some mechanisms of these properties are also explained. Therefore, it is important to promote the chiral separation and analysis of racemic drugs in pharmaceutical industry as well as in clinic in order to eliminate the unwanted isomer from the preparation and to find an optimal treatment and a right therapeutic control for the patient. In this article, we review the nomenclature, pharmacology, toxicology, pharmacokinetics, metabolism etc of some usual chiral drugs as well as their mechanisms. Different techniques used for the chiral separation in pharmaceutical industry as well as in clinical analyses are also examined.

摘要

目前使用的药物中约一半以上是手性化合物,近90%的上市新药是以由两种对映体等摩尔混合物组成的外消旋体形式销售的。尽管它们具有相同的化学结构,但大多数手性药物的异构体在药理学、毒理学、药代动力学、代谢等生物活性方面表现出显著差异。还解释了这些性质的一些机制。因此,在制药行业和临床中促进外消旋药物的手性分离和分析非常重要,以便从制剂中去除不需要的异构体,并为患者找到最佳治疗方法和正确的治疗控制。在本文中,我们综述了一些常见手性药物的命名、药理学、毒理学、药代动力学、代谢等及其机制。还研究了制药行业和临床分析中用于手性分离的不同技术。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7ab/3614593/96a4bde3e211/IJBS-2-85_F1.jpg

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