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Multiple dose pharmacokinetics of artemisinin in rats by high performance liquid chromatography-tandem mass spectrometry
关键词：时间依赖性　　药代动力学　　青蒿素　　液相色谱-质谱分析法
Aim To investigate the pharmacokinetics of the antimalarial artemisinin in rats after single and multiple oral doses. Methods Six male Wistar rats were orally given a single dose of artemisinin 40 mg·kg-1(Group 1). Another six rats were orally given artemisinin at the same dose once daily for 5 consecutive days(Group 2). Artemisinin plasma concentrations，after single dose or after 5 consecutive doses，were determined by high performance liquid chromatography-tandem mass spectrometry(LC/MS/MS). Results The artemisinin pharmacokinetic parameters of Group 1 were compared with that of Group 2. The areas under the plasma concentration-time curve(AUC0-8)decreased from 126.53 h·ng·mL-1 of Group 1 to 39.91 h·ng·mL-1 of Group 2(p0.05). Conclusions The optimized LC/MS/MS method was successfully applied to the pharmacokinetic study of artemisinin in rats after single and multiple oral doses. The results suggested that artemisinin exhibits time-dependent pharmacokinetics.
单剂量口服盐酸环丙沙星胃漂浮片人体药代动力学及相对生物利用度研究
关键词：盐酸环丙沙星胃漂浮片药代动力学相对生物利用度 RP-HPLC
目的以市售盐酸环丙沙星普通片为参比制剂进行盐酸环丙沙星胃漂浮片的人体药代动力学及相对生物利用度研究。方法采用二周期交叉试验方法,以RP-HPLC法测定环丙沙星血浓度,采用DAS程序计算环丙沙星约动学参数并进行生物等效性评价。结果单剂口服给药试验制剂和参比制剂环丙沙星时间-浓度曲线下面积(AUC0-t)分别为10.889±1.385 μg ·h·ml-1和12.406±1.384 μg ·h ·ml-1;AUC0-∞分别10.889±1.385 μg ·h·ml-1和12.406±1.384 μg·h·ml-1; Cmax分别为1.026±0.247 μg·ml-1和3.093±0.452 μg·ml-1,Tmax分别为5.4±1.1h,1.5±0.46h;试验制剂相对于普通制剂单剂给药的生物利用度(F)为87.79%±5.61%。结论盐酸环丙沙星胃漂浮片与盐酸环丙沙星普通片AUC无显著性差异,但Cmax 和Tmax有显著性差异,提示盐酸环丙沙星缓释片具有明显的缓释特征。

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