杜迎翔, 陈建民, 郑朝华. 多聚乙酰神经氨糖酸毛细管电泳拆分新药马来酸氨氯地平对映体及手性分离机制J. 药学学报, 2004, 39(9): 734-737.
引用本文: 杜迎翔, 陈建民, 郑朝华. 多聚乙酰神经氨糖酸毛细管电泳拆分新药马来酸氨氯地平对映体及手性分离机制J. 药学学报, 2004, 39(9): 734-737.
DU Ying-xiang, CHEN Jian-min, ZHENG Zhao-hua. Enantioseparation of amlodipine maleate by capillary electrophoresis using colominic acid as a chiral selector and the mechanism of chiral recognitionJ. Acta Pharmaceutica Sinica, 2004, 39(9): 734-737.
Citation: DU Ying-xiang, CHEN Jian-min, ZHENG Zhao-hua. Enantioseparation of amlodipine maleate by capillary electrophoresis using colominic acid as a chiral selector and the mechanism of chiral recognitionJ. Acta Pharmaceutica Sinica, 2004, 39(9): 734-737.

多聚乙酰神经氨糖酸毛细管电泳拆分新药马来酸氨氯地平对映体及手性分离机制

Enantioseparation of amlodipine maleate by capillary electrophoresis using colominic acid as a chiral selector and the mechanism of chiral recognition

  • 摘要: 目的将多聚乙酰神经氨糖酸用作分离双氢吡啶类药物对映体的毛细管电泳手性选择剂,建立新药马来酸氨氯地平对映体的拆分方法。方法考察了手性选择剂浓度、运行缓冲液pH值、毛细管温度、工作电压和多糖分子量等因素对手性分离的影响。结果马来酸氨氯地平两对映体得到了完全分离,分离度为2.20,并研究了多聚乙酰神经氨糖酸对马来酸氨氯地平的手性识别机理。结论本法操作简便,可用于该新药对映体的分离分析。

     

    Abstract: AimColominic acid, a novel chiral selector, was applied to enantioseparation of dihydropyridine derivative by capillary electrophoresis. A new method was developed for enantioseparation of amlodipine maleate, a novel calcium channel blocking therapeutic agent. The chiral recognition mechanism of colominic acid to amlodipine maleate was studied. MethodsCapillary electrophoresis was performed, and the effects of separation conditions on chiral separation were examined, including concentration of chiral selector, buffer pH, capillary temperature, applied voltage and molecular mass of colominic acid. ResultsThe optimum conditions were additive concentration of 8.0%, buffer pH at 3.00, capillary temperature at 15 ℃, 12 kV for applied voltage and 3×104 for molecular mass of colominic acid. Under optimum conditions complete separation was achieved between the enantiomers of amlodipine maleate with resolution as high as 2.20. ConclusionThe cliral separation was based on the multipoint recognition between colominic acid and amlodipine maleate. It is recommended that this simple, rapid and selective method be used for enantioseparation of amlodipine maleate. As far as polysaccharides were concerned, colominic acid was first used for enantioseparation of amlodipine maleate.

     

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