左旋氨氯地平拆分技术研究进展  

Study on the resolution method of Levamlodipine

作　　者：赵明蕊 刘阳 闫青青 罗明錦 郭亭玉 施秀芳[2] ZHAO Mingrui;LIU Yang;YAN Qingqing;LUO Mingjin;GUO Tingyu;SHI Xiufang(College of Pharmacy,Henan Medical College,Henan,Zhengzhou 451191,China;School of Pharmaceutical Sciences,Zhengzhou University,Henan,Zhengzhou 450000,China)

机构地区：[1]河南医学高等专科学校药学系,河南郑州451191 [2]郑州大学药学院,河南郑州450000

出　　处：《中国医药科学》2022年第19期47-51,126,共6页China Medicine And Pharmacy

基　　金：河南省高层次人才国际化培养资助项目(豫科〔2020〕22号);郑州大学大学生创新创业训练计划项目(2021cxcy335)。

摘　　要：氨氯地平是一种强效的第三代二氢吡啶钙通道拮抗剂,临床上用其消旋体和左旋异构体,其中左旋氨氯地平的降压活性是消旋体的2倍。通过文献调研,本文以左旋氨氯地平的研发为主线,简要介绍左旋氨氯地平的发现、构型确定过程以及我国科研工作者自主创新完成苯磺酸左旋氨氯地平片(施慧达)的生产转化。同时,本研究从化学拆分、毛细管电泳拆分、色谱拆分、分子印迹拆分及手性萃取拆分等技术在左旋氨氯地平拆分过程中的应用进行简要介绍,并对酶定向化技术在左旋氨氯地平拆分方面的开发潜力进行探讨。随着各种拆分新技术的应用,绿色高效的高纯度左旋氨氯地平的制备技术指日可待。Amlodipine is the third-generation Calcium channel antagonist of dihydropyridine,which belongs to the first-line antihypertensive drug in clinic and used as race mate and levoisomer.The antihypertensive effection of levamlodipine is twice as much as that of race mate.Based on the discovery and resolution of Levamlodipine,this paper introduces the discovery and determination of the configuration of Levamlodipine,as well as the production transformation of Levamlodipine besylate tablets(Shi Huida)by Chinese researchers.At the same time,the applications of chemical resolution,Capillary electrophoresis resolution,chromatography resolution,molecular imprinting resolution and chiral extraction resolution in the resolution of Levamlodipine are introduced,the potential of enzyme-oriented technology in the resolution of Levamlodipine was also discussed.With the application of various new resolution technologies,the preparation technology of highpurity Levamlodipine with green and high efficiency is expected soon.

关 键 词：降压药 左旋氨氯地平 手性化合物 化学拆分 分子印迹拆分 

分 类 号：TQ463[化学工程—制药化工]