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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 establish a method for the quantitative analysis of puerarin in canine plasma and to determine the pharmacokinetics and relative bioavailability of puerarin self-microemulsion in dogs by measuring its serum concentration over time. Methods: The crossover design was used. The puerarin and puerarin suspension of Beagle dogs were administrated in a single dose. The concentration of puerarin in plasma was determined by HPLC. The drug concentration-time curve was fitted by DAS 2.1.1 program. Pharmacokinetic parameters and bioavailability were calculated. RESULTS: The pharmacokinetic parameters of puerarin self-microemulsions and suspensions were as follows: Tmax was 3.0 h and 2.0 h, Cmax was 2.14 mg / L and 1.061 mg / L, AUC0-24 was 10.642 mg.h / L and 3 mg.h / L, the bioavailability of puerarin compared with the suspension was 354.73%. CONCLUSION: Puerarin compared with puerarin suspension can significantly improve the bioavailability of puerarin in Beagle dogs.