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使用环糊精添加剂通过毛细管区带电泳对手性碱性药物进行拆分

Chiral separation of basic drugs by capillary zone electrophoresis with cyclodextrin additives.

作者信息

Bechet I, Paques P, Fillet M, Hubert P, Crommen J

机构信息

Institute of Pharmacy, University of Liège, Belgium.

出版信息

Electrophoresis. 1994 Jun;15(6):818-23. doi: 10.1002/elps.11501501115.

DOI:10.1002/elps.11501501115
PMID:7982405
Abstract

The enantiomers of a series of basic drugs were separated in capillary zone electrophoresis (CZE) in phosphate buffers, pH 3, containing beta-cyclodextrin or one of its derivatives as chiral selectors and uncoated fused silica capillaries thermostated at 15 degrees C. The nature of the cationic component of the background electrolyte was found to have a significant influence on achiral resolution and peak symmetry. The best results were obtained with triethanolamine, which was then used to adjust the buffer pH in all further experiments. The effects on chiral resolution of the nature and concentration of cyclodextrin, of the addition of methanol, and of capillary temperature were studied. Maximum resolution was obtained at a particular cyclodextrin concentration for each analyte, depending on the affinity of the analyte for this cyclodextrin. On the basis of the results, the effects of methanol addition and temperature on enantiomeric resolution could be explained and predicted. Numerous chiral separations are presented and suggestions for the rapid optimization of CZE enantioseparations with cyclodextrin additives are given.

摘要

在含有β-环糊精或其衍生物之一作为手性选择剂的pH 3磷酸盐缓冲液中,于15℃恒温的未涂层熔融石英毛细管中,采用毛细管区带电泳(CZE)法分离了一系列碱性药物的对映体。发现背景电解质阳离子成分的性质对非手性拆分和峰对称性有显著影响。使用三乙醇胺获得了最佳结果,随后在所有进一步实验中都用其调节缓冲液pH。研究了环糊精的性质和浓度、甲醇的添加以及毛细管温度对手性拆分的影响。对于每种分析物,在特定的环糊精浓度下可获得最大拆分度,这取决于分析物对该环糊精的亲和力。基于这些结果,可以解释和预测甲醇添加和温度对映体拆分的影响。给出了众多手性拆分实例,并针对使用环糊精添加剂快速优化CZE对映体拆分提出了建议。

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[Enantiomeric separation of drugs with capillary electrophoresis with cyclodextrins].[利用环糊精进行毛细管电泳对药物对映体的分离]
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