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目的:京尼平苷酸(GPA)具有利胆作用,研究该成分在胆汁淤积病理模型状态下体内代谢过程的差别。方法:大鼠随机分为正常组和α-萘异硫氰酸酯(ANIT剂量100 mg·kg-1)诱导胆汁淤积模型组,给予不同剂量GPA(高、中、低剂量分别为100,50,25 mg·kg-1)。采用蛋白沉淀法对大鼠血浆进行处理,建立以绿原酸为内标的HPLC-UV检测方法,流动相乙腈-0.5%冰乙酸(28∶72),检测波长238 nm,利用Stata12.0软件拟合房室模型并计算各组大鼠的药动学参数。结果:ANIT造胆汁淤积模型成功率>95%。与正常组相比,胆汁淤积模型降低了GPA在体内的消除速率常数(Ke),延长了在体内的平均驻留时间(MRT0-t)和半衰期(t1/2),提高了药时曲线下面积AUC0-t和AUC0-∞。结论:该分析方法满足了京尼平苷酸体内药物分析的要求,胆汁淤积模型可降低京尼平苷酸的消除和排泄。
OBJECTIVE: Geniposidic acid (GPA) has the function of gallbladder and studies the difference of the metabolic process of this component in the pathological model of cholestasis. Methods: The rats were randomly divided into normal group and α-naphthalene isothiocyanate (ANIT dose 100 mg · kg-1) induced cholestasis model group, given different doses of GPA (high, medium and low doses were 100,50 , 25 mg · kg-1). HPLC-UV method was developed for the determination of chlorogenic acid in rat plasma using protein precipitation method. The mobile phase was acetonitrile-0.5% glacial acetic acid (28:72). The detection wavelength was 238 nm. Stata12.0 software was used Amalgam model and calculate the pharmacokinetic parameters of rats in each group. Results: The success rate of ANIT-made cholestasis model was> 95%. Compared with the normal group, the cholestasis model reduced the elimination rate constant (Ke) of GPA in vivo, prolonging the mean residence time (MRT0-t) and half-life in vivo (t1 / 2) Area AUC0-t and AUC0-∞. CONCLUSIONS: This assay meets the requirements for in vivo pharmacokinetics of geniposidic acid. Cholestasis models reduce the elimination and excretion of geniposidic acid.