手性拆分抗疟药物的毛细管电泳法：使用中性和负电荷环糊精。

Enantiomeric separation of antimalarial drugs by capillary electrophoresis using neutral and negatively charged cyclodextrins.

机构信息

Institute of Biomolecular Chemistry, Chemical Research Center, Hungarian Academy of Sciences, H-1025 Budapest, Pusztaszeri út 59-67, Hungary.

出版信息

J Pharm Biomed Anal. 2011 Feb 20;54(3):475-81. doi: 10.1016/j.jpba.2010.09.020. Epub 2010 Sep 19.

DOI:10.1016/j.jpba.2010.09.020

PMID:20943339

Abstract

Capillary electrophoresis (CE) methods for chiral resolution of five antimalarial drugs (primaquine, tafenoquine, mefloquine, chloroquine and quinacrine) were developed by using a wide selection of neutral and anionic cyclodextrin (CD) derivatives. The use of sulfobutyl-β-CD and carboxymethyl-β-CD (CMBCD) resulted in good resolution of quinacrine and tafenoquine, respectively. New results are presented for resolutions of chloroquine and mefloquine. Application of carboxyalkyl- and sulfobutyl-CD derivatives provided improved resolution for primaquine. The impurity in primaquine sample detected by CE was identified as quinocide by MS and NMR. CMBCD provided not only the best separation of primaquine from quinocide but also the simultaneous complete resolution of both compounds.

摘要

毛细管电泳（CE）方法用于手性拆分 5 种抗疟药物（伯氨喹、他非诺喹、甲氟喹、氯喹和奎宁），使用了广泛的中性和阴离子环糊精（CD）衍生物。使用磺丁基-β-CD 和羧甲基-β-CD（CMBCD）分别得到了奎宁和他非诺喹的良好分离。本文还报道了氯喹和甲氟喹的拆分新结果。羧烷基和磺丁基-CD 衍生物的应用为伯氨喹提供了更好的分辨率。CE 检测到的伯氨喹样品中的杂质通过 MS 和 NMR 鉴定为喹喔啉。CMBCD 不仅提供了伯氨喹与喹喔啉的最佳分离，还实现了两种化合物的完全同时拆分。