HPLC-FLD法同时测定丁酸氯维地平及其代谢物

发布时间：2018-04-03 23:21

  本文选题：丁酸氯维地平　切入点：氯维地平酸　出处：《中国药科大学学报》2015年03期

【摘要】：研究丁酸氯维地平脂微球(CDB-LM)注射液在小鼠体内的药代动力学过程,探讨丁酸氯维地平(CDB)在体内的代谢规律。采用HPLC-FLD法同时测定CDB及其代谢物氯维地平酸(MI)在小鼠全血样品中的浓度。色谱柱Waters C18(4.6 mm×150 mm,5μm);流动相:乙腈-甲醇-磷酸盐缓冲液(2∶1∶2);FLD检测波长:激发波长358 nm,发射波长440 nm。采用DAS 2.0软件分析计算出CDB和MI的药代动力学参数,所得参数采用PASW Statistics 18软件进行统计分析。结果表明,CDB和MI的半衰期分别在4 min和20 min左右。低剂量组和高剂量组的药代动力学参数依次为:CDB的CL为4.21和2.72 L·min-1·kg-1,AUC0-t为3.86和6.43 mg/L·min,MRT0-t为7.09和6.17 min。MI的CL为0.34和0.22 L·min-1·kg-1,AUC0-t为52.23和74.90 mg/L·min,MRT0-t为201.24和217.33 min。采用乙腈沉淀蛋白法处理全血样品,操作简单快速,全血中内源性杂质无干扰,方法准确可靠。体内研究结果表明,建立的HPLC-FLD法简便、灵敏,可同时测定CDB和MI的血药浓度。高、低两剂量组的血药浓度-时间曲线趋势相同,CDB在体内迅速代谢为MI。
[Abstract]:To study the pharmacokinetic process of clonvedipine butyrate (CDB-LM) injection in mice and to study the metabolism of clonvedipine butyrate (CDB) in vivo.The concentration of CDB and its metabolite chlorvedipine in whole blood samples of mice was determined by HPLC-FLD.The mobile phase consisted of acetonitrile-methanol-phosphate buffer (2: 1: 2), the detection wavelength was 358 nm and the emission wavelength was 440 nm.The pharmacokinetic parameters of CDB and MI were calculated by DAS 2.0 software, and the parameters were analyzed by PASW Statistics 18 software.The results showed that the half-life of CDB and MI were about 4 min and 20 min, respectively.浣庡墏閲忕粍鍜岄珮鍓傞噺缁勭殑鑽�浠ｅ姩鍔涘�﹀弬鏁颁緷娆′负:CDB鐨凜L涓，

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