【摘要】 目的比较在毛细管电泳中不同中性环糊精(CD)及其衍生物对氧氟沙星对映体的手性拆分能力,并提出可能的手性识别机制.方法分别以α-CD,β-CD,γ-CD,HP-β-CD和DM-β-CD为手性选择剂,采用毛细管电泳法研究CD种类及其浓度、分离电压、温度对氧氟沙星对映体分离的影响.结果在50mmol/L磷酸缓冲液(pH3.0),15kV分离电压、柱温25℃的基本优化条件下,分别以25mmol/L DM-β-CD或50mmol/L HP-β-CD+25mmol/Lγ-CD为手性选择剂,氧氟沙星对映体得到基线分离,分离度(Rs)分别达2.0和1.7.结论CD空腔大小和空腔边缘作用对于手性识别有重要选择性,该毛细管电泳法操作简单方便,手性分离效果良好,可用于氧氟沙星对映体药物的分离.更多还原

【Abstract】 AIM: To compare the separation ability of different neutral cyclodextrins (CD) and their derivatives on ofloxacin enantiomer by capillary electrophoresis (CE) and to explore the possible mechanisms of chiral separation. METHODS: The effects of concentration and type of neutral CD, buffer pH, running voltage and capillary temperature on the enantioseparation were investigated by CE using α-CD, β-CD, γ-CD, hydropropyl-β-CD (HP-β-CD) and dimethyl-β-CD (DM-β-CD) respectively. RESULTS: Under the optimized CE conditions (50 mmol/L phosphate buffer at pH=3.0, capillary temperature 25℃, separation voltage 15 kV using 25 mmol/L DM-β-CD or by the combination of 50 mmol/L HP-β-CD and 25 mmol/L γ-CD), ofloxacin enantiomer was completely separated with resolution as high as 2.0 and 1.7 respectively. CONCLUSION: Inclusion-complexation mechanism is based on the cavity size and function of the rim of CDs. The proposed method was simple and rapid with high separation efficiency and can be used for enantioseparation of ofloxacin drug.更多还原