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[利用环糊精进行毛细管电泳对药物对映体的分离]

[Enantiomeric separation of drugs with capillary electrophoresis with cyclodextrins].

作者信息

Fillet M

出版信息

Bull Mem Acad R Med Belg. 2001;156(6 Pt 2):311-7.

PMID:11928221
Abstract

General strategies for the development of capillary electrophoretic methods for the enantiomeric separation of basic, acidic or neutral drugs have been developed. For all kinds of compounds the use of a buffer made of 100 mM phosphoric acid adjusted to pH 3 or 5 with triethanolamine, containing cyclodextrin (CD) derivatives as chiral selectors, is recommended. Five b-cyclodextrin derivatives were found to be particularly useful for enantioseparations: dimethyl-beta-CD (DMCD), trimethyl-beta-CD (TMCD), hydroxypropyl-beta-CD (HPCD), carboxymethyl-beta-CD (CMCD) and sulfobutyl-beta-CD (SBCD). Two different strategies are proposed, depending on the acidic or basic character of the analytes. Using these strategies, 96% of the 50 drugs examined as model compounds could be fully enantioseparated, which confirmed the usefulness of capillary electrophoresis in order to obtain complete enantiomeric separation as quickly as possible and with a minimum consumption of chiral selector.

摘要

已经开发出用于碱性、酸性或中性药物对映体分离的毛细管电泳方法的一般策略。对于所有类型的化合物,建议使用由100 mM磷酸制成的缓冲液,用三乙醇胺将其pH值调节至3或5,并含有环糊精(CD)衍生物作为手性选择剂。发现五种β-环糊精衍生物对映体分离特别有用:二甲基-β-环糊精(DMCD)、三甲基-β-环糊精(TMCD)、羟丙基-β-环糊精(HPCD)、羧甲基-β-环糊精(CMCD)和磺丁基-β-环糊精(SBCD)。根据分析物的酸性或碱性特征,提出了两种不同的策略。使用这些策略,作为模型化合物检测的50种药物中有96%能够实现完全对映体分离,这证实了毛细管电泳在尽快获得完全对映体分离且手性选择剂消耗最少方面的实用性。

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