化学学报 ›› 1998, Vol. 56 ›› Issue (1): 87-92. 上一篇    下一篇

研究论文

毛细管区带电泳对手性药物盐酸美西律和盐酸异博定的对映体分离

王志;黄爱今;孙亦梁;孙曾培   

  1. 北京大学化学系;中国药品生物制品检定所
  • 发布日期:1998-01-15

Enantiomeric separation of mexiletine and verapamil by cyclodextrin-mediated capillary zone electrophoresis

WANG ZHI;HUANG AIJIN;SUN YILIANG;SUN ZENGPEI   

  • Published:1998-01-15

应用环糊精-毛细管区带电泳体系对手性药物盐酸美西律和盐酸异博定的对映体分离进行了研究。结果表明, 在所研究的手性选择剂α-环糊精, β-环糊精, 二甲基-β-环糊精, 羟丙基β-环糊精和γ-环糊精中, 羟丙基β-环糊精对所研究的手性药物分离效果较好。对盐酸美西律和盐酸异博定的最佳羟丙基-β-环糊精浓度分别为30mmol/L和9mmol/L, 最佳缓冲溶液浓度为100mmol/L Tris-H3PO4(pH2.3)。向缓冲溶液中加入0.05%羟丙基纤维素(HPLC)可改善分离。盐酸美西律获得了接近基线的手性分离, 而盐酸异博定亦获得了较好的分离。

关键词: 分离, 环糊精, 对映体, 毛细管区带电泳, 盐酸美西律, 盐酸异博定

The enantiomeric separation of chiral drugs mexiletine and verapamil was investigated using cyclodextrins added buffers at acidic conditions in capillary zone electrophoresis. The results show that the type and concentration of chiral selector, buffer concentration etc, influence the separation. Among the five cyclodextrins (CDs) investigated, i.e., α-CD, β-CD, Heptakis(2, 6-di-O-methyl)-β-CD (DM-β-CD), Hydroxypropyl-β-CD(HP-β -CD) and γ-CD, HP-β-CD gave the best separation of verapamil and mexiletine is at 9 and 30 mmol/L, respectively and the optimal Tris-H3PO4 (pH 2.3) buffer concentration at 100 mmol/L. The separation was improved by the addition of 0.05% hydroxypropyl cellulose (HPC) to the buffer. Under the optimized separation conditions, near baseline enantiomeric separation was achieved for mexiletine and enantiomers of verapamil were also fairly well separated.

Key words: SEPARATION, CYCLODEXTRIN, ENANTIOMORPH, CAPILLARY ZONE ELECTROPHORESIS

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