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使用羧甲基环糊精通过毛细管电泳对手性碱性药物进行拆分。

Chiral separation of basic drugs by capillary electrophoresis with carboxymethylcyclodextrins.

作者信息

Zukowski Janusz, De Biasi Vern, Berthod Alain

机构信息

GlaxoSmithKline, Analytical Chemistry, New Frontiers Science Park (North), Harlow, Essex CM19 5AD, UK.

出版信息

J Chromatogr A. 2002 Mar 1;948(1-2):331-42. doi: 10.1016/s0021-9673(01)01473-x.

DOI:10.1016/s0021-9673(01)01473-x
PMID:12831209
Abstract

Capillary electrophoresis (CE) with carboxymethylated beta- or gamma-cyclodextrins was used to achieve the rapid enantiomeric separation of a set of basic drugs. The enantiomers of 12 chiral amino-containing pharmaceutical compounds belonging to various therapeutic categories were analyzed by CE using an uncoated 60 cm x 75 microm I.D. silica capillary. Several experimental parameters such as the nature, concentration and pH of the buffer, nature and concentration of the anionic cyclodextrin and temperature were studied in order to optimize the enantiomeric separation. The variation of the solute partition coefficient for the chiral selector, the enantioselectivity and resolution factors are used to assess the quality of the chiral separation. It is shown that the solute affinity for the chiral selector is not related to its enantioresolution factor. None of the two cyclodextrin selectors used was able to separate the whole set of basic drugs.

摘要

采用羧甲基化的β-或γ-环糊精进行毛细管电泳(CE),以实现一组碱性药物的快速对映体分离。使用未涂层的60 cm×75 μm内径的石英毛细管,通过CE分析了12种属于不同治疗类别的含手性氨基药物化合物的对映体。研究了缓冲液的性质、浓度和pH值、阴离子环糊精的性质和浓度以及温度等几个实验参数,以优化对映体分离。使用手性选择剂的溶质分配系数变化、对映选择性和分离度因子来评估手性分离的质量。结果表明,溶质对手性选择剂的亲和力与其对映体分离度因子无关。所使用的两种环糊精选择剂均无法分离整个碱性药物组。

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