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目的:建立黄芩素在血浆中的高效液相色谱法检测方法,并研究大鼠灌胃黄芩素后的体内药动学。方法:采用Agi-lent1200高效液相色谱系统,Zorbax SB-C18色谱柱(250mm×4.6mm,5μm),流动相0.1%pH2.0甲酸-乙腈溶液(60:40),流速1.0mL·min-1,进样量20μL,检测波长276nm,室温检测。大鼠按黄芩素75mg.kg-1灌胃给药后,测定给药后不同时间的原型药物和酶解后药物在血浆中的浓度,并用Win Nolin软件计算药动学参数。结果:大鼠灌胃给药后,血浆中酶解后黄芩素总量的AUC0-24和Cmax均显著高于黄芩素原型,前者分别是后者的2.67倍和2.59倍,且黄芩素总量的达峰时间tmax明显迟于黄芩素原型。结果说明,大鼠灌胃给药黄芩素后首过效应严重,大部分在体内被代谢成葡萄糖醛酸、硫酸结合物。无论原型还是Ⅱ相代谢结合物在体内的消除过程都比较缓慢。结论:此方法简便、稳定、准确,可用于黄芩素的体内药动学研究。
Objective: To establish a HPLC method for the determination of baicalein in plasma and to study the pharmacokinetics of baicalein in rats. Methods: Agi-lent1200 HPLC system was used. The mobile phase consisted of Zorbax SB-C18 column (250 mm × 4.6 mm, 5 μm), mobile phase 0.1% 1, injection volume 20μL, detection wavelength 276nm, room temperature detection. The rats were administered with baicalein 75mg.kg-1. After administration, the concentrations of the prototype drug and the drugs in the plasma after the drug administration were measured at different times after administration, and the pharmacokinetic parameters were calculated by Win Nolin software. Results: After intragastric administration, the total AUC0-24 and Cmax of baicalein in plasma were significantly higher than those of baicalein, the former were 2.67 and 2.59 times of the latter respectively, and the total amount of baicalein The peak time tmax was significantly later than the baicalein prototype. The results showed that, after oral administration of baicalein in rats first-pass effect serious, most of the metabolism in the body into glucuronic acid, sulfuric acid conjugates. Either the prototype or Phase II metabolic conjugates in the body to eliminate the more slowly. Conclusion: This method is simple, stable and accurate and can be used for in vivo pharmacokinetics of baicalein.