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  • 沈意翔,李珍,黄文龙,林梅,胡晋红,范国荣.氯苄律定对映体的毛细管电泳分离及其在家兔体内手性药代动力学研究*[J].第二军医大学学报,1999,20(1):    [点击复制]
  • 沈意翔,李珍,黄文龙,林梅,胡晋红,范国荣.Separation of chlorobenzyltetrahydroberberine enantiomers by capillary electrophoresis and their chiral pharmacokinetic studies in rabbits[J].Acad J Sec Mil Med Univ,1999,20(1):   [点击复制]
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氯苄律定对映体的毛细管电泳分离及其在家兔体内手性药代动力学研究*
沈意翔,李珍,黄文龙,林梅,胡晋红,范国荣
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摘要:
目的:建立氯苄律定(CBTHB)对映体的毛细管电泳分离方法,研究家兔体内CBTHB的手性药代动力学特征。方法:通过羧甲基环糊精手性识别作用和其他电泳条件的比较,确定CBTHB对映体毛细管电泳体内分析方法,由统计矩方法计算家兔口服CBTHB后的药代动力学参数。结果:CBTHB两个对映体获得理想分离。家兔口服150 mg/kg CBTHB后体内过程存在着立体选择性差异,其中R-CBTHB与S-CBTHB的平均血浆浓度比值为(1.43±0.21)。两个对映体血浆浓度之间存在非常显著性差异(t = 4.14,P<0.01 ),R-CBTHB的AUC0?τ 和AUC0?∞也明显大于S-CBTHB(P<0.05)。结论:手性毛细管电泳分析方法成功地应用于CBTHB对映体的药代动力学研究。
关键词:  氯苄律定、毛细管电泳、对映体分离、药代动力学,手性
DOI:
基金项目:
Separation of chlorobenzyltetrahydroberberine enantiomers by capillary electrophoresis and their chiral pharmacokinetic studies in rabbits
沈意翔,李珍,黄文龙,林梅,胡晋红,范国荣
()
Abstract:
Objective: To establish a capillary electrophoresis method for the separation and determination of chlorobenzyltetrahydroberberine (CBTHB)enantiomers and to investigate their chiral pharmacokinetics in rabbits. Methods: Racemic CBTHB was separated optimally and measured successfully by capillary electrophoresis, based on comparison of chiral recognition capabilities of carboxymethylated cyclodextrins and selection of other electrophoretic conditions.The plasma concentration data were handled with theory of statistical moment and the pharmacokinetic parameters were obtained. Results: CBTHB enantiomers in rabbit plasma samples were separated under optimal chiral conditions. After a single oral dose of 150 mg/kg racemic CBTHB in six rabbits, plasma level of R-enantiomer was always higher than that of S-enantiomer. The ratio of R-to S-enantiomer was (1.43±0.21), resulting in more significant differences between the plasma concentrations of R-enantiomer and those of S-enantiomer(t = 4.14,P<0.01). Furthermore, it was found that AUC0?τ and AUC0?∞ of R-enantiomer were significantly greater than those of S-enantiomer. Conclusion:The new chiral capillary electrophoresis method proves to be suitable for studies on CBTHB enantiomers pharmacokinetics.
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