蒿甲醚贴剂小鼠体内药代动力学研究

Studies on pharmacokinetics of artemether patch in rats

目的:建立高效液相.质谱法测定小鼠血浆中蒿甲醚(ARM)及代谢产物双氢青蒿素(DHA)浓度的方法,比较蒿甲醚口服与经皮给药主要药代动力学参数。方法:按平行设计方法,小鼠随机分为2组(经皮给药组和口服给药组),测定给药后血浆中蒿甲醚及代谢产物双氢青蒿素的浓度,并用DAS2.0软件进行数据处理,并进行统计。结果:蒿甲醚贴剂的C_(max),T_(max),AUC_(0-t),MRT与口服制剂存在显著性差异(P<0.05)。结论:蒿甲醚贴剂有达峰时间长和体内维持时间长的特点,具有长效缓释的作用。

Objective： To establish a HPLC-MS-MS determination method of artemether （ARM） and active derivatives DHA, and compare the pharmacokinetic parameters of ARM after transdermal and oral administration. Method： The mice were divided two groups （ transdermal and oral） by parallel design. ARM and active derivatives DHA in plasma of mice at different sampling time were determined. The pharmacokinetic parameters were calculated by DAS 2.0 and by statistic analysis. Result：compare oral administration, the pharmacokinetic parameters of ARM after transdermal, Cmax, Tmax, AUC0-1, MRT, had significant difference （P 〈 0.05 ）. Conclusion： The artemrther patch has long-releasing property.