葛根素自微乳在Beagle犬体内的药代动力学及生物利用度研究

Pharmacokinetics and Bioavailability of Puerarin Self-microemulsion in Beagle Dogs

目的：建立犬血浆中葛根素的定量分析方法,测定其在犬体内的血药浓度经时过程,评价葛根素自微乳的药动学及相对生物利用度。方法：采用交叉试验设计,分别单剂量给予Beagle犬葛根素自微乳和葛根素混悬液,用HPLC法测定血浆中葛根素的浓度,用DAS 2.1.1程序拟合药物浓度-时间曲线,计算药动学参数和生物利用度。结果：葛根素自微乳和混悬液的药动学参数分别为：Tmax为3.0 h和2.0 h,Cmax为2.14 mg/L及1.061 mg/L,AUC0~24为10.642 mg.h/L和3 mg.h/L,葛根素自微乳相对于混悬液的生物利用度为354.73%。结论：葛根素自微乳相对于葛根素混悬液,能显著提高葛根素在Beagle犬体内的生物利用度。

Objective：To estabolish a quantitative analysis method for pharmacokinetics and bioavailability of Puerarin self-microemulsion in Beagle dogs.Methods：A crossover design was use to detect the pharmacokinetic parameters of Puerarin self-microemulsion and suspension in Beagle dogs.The concentration of Puerarin in plasma was determined with HPLC,the pharmacokinetics parameters and bioavailability was calculated with DAS 2.1.1programs.Results：Tmax of Puerarin self-microemulsion and suspension were 3.0 h and 2.0 h,Cmax were 2.14 mg/L and 1.061 mg/L,AUC0~24 were 10.642 mg·h/L and 3 mg·h/L,respectively.The bioavailability of Puerarin self-microemulsion relative to Puerarin suspension were 354.73%.Conclusion：Puerarin self-microemulsion can significantly improve the bioavailability in Beagle dogs.