基于共晶技术的手性药物拆分研究进展  

Recent Advances in Resolution of Chiral Drugs Based on Cocrystallization

作　　者：曹阳 朱冉冉 区杏君 宋利星 吴范宏 CAO Yang;ZHU Ranran;OU Xingjun;SONG Lixing;WU Fanhong(School of Chemical and Environmental Engineering,Shanghai Institute of Technology,Shanghai 201418;Shanghai Engineering Research Center of Green Fluoropharmaceutical Technology,Shanghai 201418)

机构地区：[1]上海应用技术大学化学与环境工程学院,上海201418 [2]上海绿色氟代制药工程技术研究中心,上海201418

出　　处：《中国医药工业杂志》2023年第10期1420-1428,共9页Chinese Journal of Pharmaceuticals

基　　金：上海市浦江人才计划项目(22PJ1412700)。

摘　　要：手性是药物中广泛存在的一种特性,单一对映体药物较其外消旋体往往表现出更高的活性、更低的不良反应,因此制备高纯度手性单体具有十分重要的研究意义。结晶拆分法是制药工业中获取手性单体的重要途径,共晶作为一种新颖的结晶技术,因适用性广而备受关注。该文重点介绍了共晶拆分法的发展历程,并按照外消旋药物的共晶结构特征进行分类,综述了近年来共晶拆分法的研究进展。此外,对共晶拆分法面临的主要挑战进行了总结和展望。Chirality is a widely existing property in pharmaceuticals.In general,the chiral enantiomers show higher activity and lower adverse reaction than their racemates.Therefore,the manufacturing of pure chiral enantiomer is of great scientific significance.Crystallization resolution method is an important technique in pharmaceutical industry to achieve the separation of enantiomers.As a novel crystallization technique,cocrystal has attracted much attention due to its broad applicability.In this paper,the history and development of chiral resolution based on cocrystallization are briefly introduced.Meanwhile,the recent progress in this field is classified and summarized according to the structural characteristics of cocrystals formed by racemic drugs.In addition,the main challenges of chiral resolution based on cocrystallization are summarized and prospected.

关 键 词：共晶 手性拆分 对映体选择性共晶 非对映体共晶 共晶聚集体 

分 类 号：O652.6[理学—分析化学]