左金丸配伍意义药物代谢动力学分析.docVIP

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左金丸配伍意义药物代谢动力学分析.doc

左金丸配伍意义药物代谢动力学分析

左金丸配伍意义药物代谢动力学分析   [摘要] 目的 研究左金丸在SD大鼠体内的药代动力学,为临床应用提供参考。 方法 将左金丸及黄连、吴茱萸制成水煎液,对SD大鼠进行灌胃,HPLC法测定并计算小檗碱、吴茱萸次碱的药代动力学参数。 结果 左金丸组的小檗碱的t1/2延长,tmax缩短,Cmax增大,AUC(0-∞)增加,代谢较缓慢;吴茱萸次碱tmax缩短,Cmax增大,AUC(0-∞)增加。 结论 左金丸中黄连∶吴茱萸为6∶1时,能很好地发挥作用。   [关键词] 左金丸;小檗碱;吴茱萸次碱;药代动力学   [中图分类号] R965 [文献标识码] A [文章编号] 1674-4721(2012)02(b)-0019-02      Pharmacokinetic analysis based Zuojinwan compatibility of significance   NI Jianxin1 LIN Yuehong1 CHEN Miaozhu2   1.Department of Pharmacy, the People′s Hospital of Baoan District of Shenzhen City in Guangdong Province, Shenzhen 518101, China; 3.Department of Community Health, the People′s Hospital of Baoan District of Shenzhen City in Guangdong Province, Shenzhen 518101, China   [Abstract] Objective To study the pharmacokinetic parameters of Zuojinwan in SD rat′s, provide a reference for clinical application. Methods A HPLC method was used to detect the pharmacokinetic parameters of berberine and rutaecarpine in SD rats which were administrated with Zoujinwan, berberine, rutaecarpine separately. Results The t1/2, Cmax, AUC(0-∞) of berberine were increased in the rats administrated with Zuojinwan and their tmax was shorter, metabolic state was slower, the Cmax and AUC(0-∞) of rutaecarpine were increased and tmax was shorter. Conclusion Zuojinwan is effective when Coptis:Evodia=6:1, can be a very good effect.   [Key words] Zuojinwan; Berberine; Rutaecarpine; Pharmacokinetic      左金丸由黄连、吴茱萸(6∶1)组成,是消化系统常用中药[1]。方中黄连的活性成分主要为小檗碱,吴茱萸的活性成分主要为吴茱萸次碱[2]。本研究采用SD大鼠,给予左金丸及黄连、吴茱萸后取其血浆,进行药物代谢动力学比较,为左金丸的临床使用提供参考。   1 材料与方法   1.1 实验材料   药品与试剂:黄连、吴茱萸饮片;小檗碱、吴茱萸次碱标准品;甲醇、乙醚、甲酸、重蒸馏水。仪器:LC-2010C高效液相色谱仪(岛津),电子分析天平,高速离心机,DAS2.0药代动力学???据处理软件。动物:SD大鼠,92只,雌雄均可,体重180~210 g。   1.2 方法   1.2.1 药液制备 黄连组:取黄连300 g,加水2 000 mL;吴茱萸组:取吴茱萸50 g,加水400 mL;左金丸组:取黄连300 g,吴茱萸50 g,加水2 000 mL。分别煎煮2 h后收集煎煮液,再加入等量水后煎煮1 h,合并煎煮液。浓缩成相当于含黄连2.0 g/mL或者含吴茱萸0.33 g/mL的药液。HPLC含量测定结果为:黄连组含小檗碱36.5 mg/mL;吴茱萸组含吴茱萸次碱1.6 mg/mL;左金丸组含小檗碱31.8 mg/mL,含吴茱萸次碱1.3 mg/mL。   1.2.2 给药 取SD大鼠92只随机分成3组:黄连组(22只),吴茱

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