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[肾上腺素能β受体阻滞剂——一类手性药物:β受体阻滞剂中的对映体拆分]

[Adrenergic beta-receptor blockers--a group of chiral drugs: enantioseparation in the group of beta-blockers].

作者信息

Cizmáriková R, Valentová J, Hutta J A

机构信息

Katedra chemickej teórie lieciv Farmaceutickej fakulty Univerzity Komenského, Bratislava.

出版信息

Ceska Slov Farm. 2004 Jan;53(1):9-17.

Abstract

The preparation of pure individual enantiomers represents a topical problem from the standpoint of efficacy and safety of drugs. This paper continues in the preceeding review of the blockers of beta-adrenergic receptors as a group of chiral drugs, which is concerned with different pharmacodynamic, pharmacokinetic, and toxicological effects of individual enantiomers of this group. The review paper pays attention to the problems of enantioseparation of this group of chiral drugs, listing individual examples of the methods of enantioseparation, such as crystallization, biocatalysis, chromatographic methods (HPLC, GC, TLC), capillary electrophoresis, and the method of nuclear magnetic resonance (NMR). The individual methods of enantioseparation including enantioseparation in biological material (urine, serum) are illustrated on examples on beta-blockers used in clinical practice (e.g., propranolol, atenolol, metoprolol) as well as potential agents of this group of drugs.

摘要

从药物的有效性和安全性角度来看,制备纯的单一对映体是一个热门问题。本文延续了之前对β-肾上腺素能受体阻滞剂这一手性药物组的综述,该综述涉及该组单一对映体不同的药效学、药代动力学和毒理学效应。这篇综述文章关注了这组手性药物的对映体拆分问题,列举了对映体拆分方法的个别实例,如结晶法、生物催化法、色谱法(高效液相色谱法、气相色谱法、薄层色谱法)、毛细管电泳法以及核磁共振法。包括生物材料(尿液、血清)中的对映体拆分在内的各种对映体拆分方法,通过临床实践中使用的β-阻滞剂(如普萘洛尔、阿替洛尔、美托洛尔)以及该组药物的潜在制剂的实例进行了说明。

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