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色谱和电迁移技术中的手性分离原理。

Chiral separation principles in chromatographic and electromigration techniques.

作者信息

Gübitz Gerald, Schmid Martin G

机构信息

Institute of Pharmaceutical Sciences, Department of Pharmaceutical Chemistry, Karl-Franzens University, Universitätsplatz 1, A-8010 Graz, Austria.

出版信息

Mol Biotechnol. 2006 Feb;32(2):159-80. doi: 10.1385/MB:32:2:159.

Abstract

Almost half of the drugs in use today are chiral. It is well established that the pharmacological activity is mostly restricted to one of the enantiomers (eutomer). There can be qualitative and quantitative differences in the activity of the enantiomers. In many cases, the inactive enantiomer (distomer) shows unwanted side effects or even toxic effects. Even if the side effects are not that drastic, the distomer has to be metabolized and this represents an unnecessary burden for the organism. Therefore, the development of methods for the separation of enantiomers, both on analytical and preparative scale, has become increasingly important. Chromatographic techniques such as thin layer chromatography (TLC), gas chromatography (GC), supercritical fluid chromatography (SFC), and above all high-performance liquid chromatography (HPLC) have been used for enantiomer separation for about two decades. More recently, electromigration techniques, such as capillary electrophoresis and capillary electrochromatography, have been shown to be powerful alternatives to chromatographic methods. This review gives a short overview of different chiral separation principles and their application. Several new developments are discussed.

摘要

如今使用的药物中几乎有一半是手性的。众所周知,药理活性大多局限于其中一种对映体(优映体)。对映体的活性在性质和数量上可能存在差异。在许多情况下,无活性的对映体(劣映体)会表现出不良副作用甚至毒性作用。即使副作用不那么严重,劣映体也必须进行代谢,这对生物体来说是一种不必要的负担。因此,开发用于分析和制备规模对映体分离的方法变得越来越重要。诸如薄层色谱法(TLC)、气相色谱法(GC)、超临界流体色谱法(SFC),尤其是高效液相色谱法(HPLC)等色谱技术已经用于对映体分离约二十年了。最近,电迁移技术,如毛细管电泳和毛细管电色谱,已被证明是色谱方法的有力替代方法。本文综述简要概述了不同的手性分离原理及其应用。还讨论了一些新进展。

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