摘要
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 in situ intestinal absorption kinetics of baicalin contained in Tiangou Jiangya capsules, and the effect of different intestinal segments, pH value, drug concentration and P-gp inhibitor on the absorption. Method： The in situ intestinal perfusion test was adopted, and HPLC method was used to determine the content of baicalin in samples at different time points. Ultra-violet （UV） speetrophotometry was used to determine the content of phenol red in samples at different time points. Result： When pH value was at 5.0, 6. 5, 7.4, the absorption of baicalin was not impacted. P-gp inhibitor verapamil could enhance the absorption of baicalin. When the quality concentration of the test solution ranged between 5-20 g. L - l , the linearity of the absorption amount of ba- iealin increased. The absorption kinetic equation of baicalin was Y = - 0. 073 7X ＋ 0. 118 7 （ r = 0. 994 8 ） , Ka 0. 073 7 h, t/2 9.40 h. Conclusion： Baiea]in is mainly absorbed in colon. The absorption of baicalin shows the first-order kinetics process, with the ab- sorption mechanism of passive diffusion. Baicalin is a substrate for P-gp.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2013年第6期894-898,共5页
China Journal of Chinese Materia Medica
基金
国家"重大新药创制"科技重大专项(2012ZX09102201-004)
关键词
天钩降压胶囊
黄芩苷
在体肠灌流
吸收动力学
吸收机制
Tiangou Jiangya capsules
baicalin
in situ intestinal perfusion
absorption kinetics
absorption mechanism
