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目的:考察葛根素自微乳在大鼠体内的血药浓度经时过程,评价葛根素自微乳的药代动力学及相对生物利用度。方法:单剂量给予大鼠葛根素自微乳和葛根素混悬液,采用HPLC测定血浆中葛根素质量浓度,检测波长250 nm,流动相甲醇(A)-0.1%磷酸水溶液(B)梯度洗脱(0~30 min,20%~25%A;30~40 min,25%~40%A;40~50 min,40%A),运用DAS2.1.1程序拟合药物浓度-时间曲线,计算药代动力学参数及生物利用度。结果:葛根素自微乳和混悬液的tmax分别为0.71,1.1 h,Cmax分别为2.052,1.120 mg·L-1,AUC0-24 h依次为2.901,2.013 mg·h·L-1,葛根素自微乳相对于混悬液的生物利用度144.11%。结论:与葛根素混悬液相比,葛根素自微乳能显著提高葛根素在大鼠体内的生物利用度。
OBJECTIVE: To investigate the pharmacokinetics and relative bioavailability of puerarin self-microemulsions in rats during the course of plasma concentration over time. Methods: The single-dose administration of puerarin and puerarin suspension in rats was used to determine the concentration of puerarin in plasma. The detection wavelength was 250 nm and the mobile phase consisted of methanol (A) -0.1% phosphoric acid solution (B) (0-30 min, 20% -25% A; 30-40 min, 25-40% A; 40-50 min, 40% A). The DAS2.1.1 program was used to fit the drug concentration- Pharmacokinetic parameters and bioavailability. Results: The tmax of puerarin self-microemulsion and suspension were 0.71,1.1 h, Cmax were 2.052,1.120 mg · L-1, AUC0-24 h were 2.901,2.013 mg · h · L-1, The bioavailability of verapamil relative to the suspension was 144.11%. CONCLUSION: Compared with puerarin suspension, puerarin self-microemulsion can significantly improve the bioavailability of puerarin in rats.