色谱法拆分β-受体阻滞剂的进展。
Progress in the Enantioseparation of β-Blockers by Chromatographic Methods.
机构信息
Institute of Pharmaceutical Engineering, College of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310027, China.
Institute of Zhejiang University-Quzhou, Quzhou 324000, China.
出版信息
Molecules. 2021 Jan 17;26(2):468. doi: 10.3390/molecules26020468.
β-adrenergic antagonists (β-blockers) with at least one chiral center are an exceedingly important class of drugs used mostly to treat cardiovascular diseases. At least 70 β-blockers have been investigated in history. However, only a few β-blockers, e.g., timolol, are clinically marketed as an optically pure enantiomer. Therefore, the separation of racemates of β-blockers is essential both in the laboratory and industry. Many approaches have been explored to obtain the single enantiomeric β-blocker, including high performance liquid chromatography, supercritical fluid chromatography and simulated moving bed chromatography. In this article, a review is presented on different chromatographic methods applied for the enantioseparation of β-blockers, covering high performance liquid chromatography (HPLC), supercritical fluid chromatography (SFC) and simulated moving bed chromatography (SMB).
β-肾上腺素能拮抗剂（β-受体阻滞剂）具有至少一个手性中心，是一类非常重要的药物，主要用于治疗心血管疾病。历史上已经研究了至少 70 种β受体阻滞剂。然而，只有少数几种β受体阻滞剂，如噻吗洛尔，作为光学纯对映异构体在临床上上市。因此，在实验室和工业中分离β受体阻滞剂的外消旋体都是必不可少的。为了获得单一的手性β受体阻滞剂，已经探索了许多方法，包括高效液相色谱、超临界流体色谱和模拟移动床色谱。本文综述了用于β受体阻滞剂对映体拆分的不同色谱方法，包括高效液相色谱（HPLC）、超临界流体色谱（SFC）和模拟移动床色谱（SMB）。
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