目的:研究大鼠静脉注射黄连生物碱提取物后,小檗碱在大鼠小肠和胆汁中的药代动力学特性。方法:用高效液相色谱(HPLC)检测大鼠小肠和胆汁样品中小檗碱的浓度。结果:黄连生物碱中小檗碱在静脉给药后0.25~4 h,B/P(胆汁中浓度/血浆中浓度)为69.1-497.9,属于胆汁清除率高的药物。胆汁引流实验表明,小肠中绝大部分的小檗碱来自胆汁。引流胆汁后,给大鼠静脉给药,在小肠中仍能检测到小檗碱,推测这一部分小檗碱来自于血浆中的小檗碱,其转运方向是从侧底膜(basolateral membrane)向顶侧膜(apical membrane)转运至小肠中。结论:实验从整体动物水平上证明了小檗碱在血液中可以逆向转运至小肠中,其转运机理涉及P-糖蛋白(P-glycoprotein,P-gp)。
Objective: To investigate the pharmacokinetics of berberine in Coptidis Rhizoma extract in rat intestinal and bile. Method: A simple and accurate high-performance liquid chromatography method was used to determine the concentration of berberine in the rat intestinal and bile samples. Result: Following the intravenous administration of Coptidis Rhizoma extract, B/P (concentration in the bile/ concentration in the plasma) of berberine was determined to be 69.1-497.9 from 0. 25 h to 4 h. Bile excretion was one of the main excretion ways for rats to eliminate berberine of Coptidis Rhizoma alkaloids. Most of berberine in the intestinal was from the bile. While bile was discharged from rats, berberine still could be determined in the intestinal. Conclusion: The results proved that berberine could be transported from blood to intestinal in the animal model with a direction from basolateral membrane to apical membrane. P-glycoprotein is involved in the transport mechanism.