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目的:研究天钩降压胶囊中黄芩苷在大鼠肠道的吸收动力学及不同肠段、pH、药物浓度、P-gp抑制剂对吸收的影响。方法:采用大鼠在体肠灌流试验,用HPLC测定不同时间点样品中黄芩苷的含量,用紫外-可见分光光度法测定不同时间点样品中酚红的含量。结果:在pH 5.0,6.5,7.4时不影响黄芩苷的吸收;P-gp抑制剂维拉帕米可增加黄芩苷的吸收;在供试液质量浓度5～20 mg·L-1,黄芩苷吸收量线性增加;吸收动力学方程为Y=-0.073 7X+0.118 7(r=0.994 8),Ka0.073 7 h-1,t1/29.40 h。结论:黄芩苷主要在结肠吸收,呈一级动力学过程,吸收机制为被动扩散;黄芩苷为P-糖蛋白的底物。
OBJECTIVE: To study the absorption kinetics of baicalin in Tian hookjiangya capsule and the effects of different intestinal segments, pH, drug concentration and P-gp inhibitors on the absorption. Methods: Rat intestinal perfusion test was used to determine the content of baicalin in different time points by HPLC. The content of phenol red in samples at different time points was determined by UV-Vis spectrophotometry. Results: The absorption of baicalin was not affected at pH 5.0,6.5,7.4; Verapamil of P-gp inhibitor could increase the absorption of baicalin. When the concentration of test solution was 5 ~ 20 mg · L-1, baicalin Absorption increased linearly. The absorption kinetics equation was Y = -0.073 7X + 0.118 7 (r = 0.994 8), Ka0.073 7 h-1, t1 / 29.40 h. CONCLUSION: Baicalin is mainly absorbed in the colon, showing a first-order kinetic process and its absorption mechanism is passive diffusion. Baicalin is a substrate of P-glycoprotein.