Dong Yu, Zhang Yingfeng, Yang Qing, Li Yujie, Zhu Xiaoxin
Institute of Chinese Materia Medica, Guang'anmen Hospital, Beijing 100053, China.
Zhongguo Zhong Yao Za Zhi. 2009 Apr;34(7):884-8.
To research the intestinal absorption characteristics of paeoniflorin in extractive Radix Paeoniae Alba in the different intestinal segment, and the interaction with P-glycoprotein.
Paeoniflorin, a representative component in extractive Radix Paeoniae Alba, on the intestinal absorption was studied in vitro using everted gut sacs model and detected by HPLC method. The absorption characteristics was evaluated by the absorption parameter.
The absorption of paeoniflorin was linearity at different intestine segment and dose, and the square of regrees correlation coefficient exceed 0.9 (R2 > 0.9), which consistent with zero order rate process. The Kalpha of paeoniflorin showed a dose-dependent increase along with the raised dose of extractive Radix Paeoniae Alba, indicated it was a mechanism of passive absorption. The absorption rate was jejunum > ileum > colon. Verapamil (100 micromol x L(-1)), a inhibitor of the P-glycoprotein, can remarkable increase the absorption of the paeoniflorin in ileum (P < 0.05). After administer the extractive Radix Paeoniae Alba for 5 days, the extraction of Rho123 is significantly increase in ileum (P < 0.01).
The intestinal absorption of paeoniflorin is zero order rate process and passive absorption. Paeoniflorin is a substrate of P-glycoprotein, and extractive Radix Paeoniae Alba could induce the expression of the P-glycoprotein.
研究白芍提取物中芍药苷在不同肠段的肠道吸收特性及其与P-糖蛋白的相互作用。
以白芍提取物中的代表性成分芍药苷为研究对象，采用外翻肠囊模型体外研究其肠吸收情况，并用高效液相色谱法进行检测。通过吸收参数评价吸收特性。
芍药苷在不同肠段及不同剂量下的吸收呈线性，回归相关系数平方均大于0.9（R2>0.9），符合零级速率过程。芍药苷的Ka值随白芍提取物剂量增加呈剂量依赖性升高，表明其为被动吸收机制。吸收速率为空肠>回肠>结肠。P-糖蛋白抑制剂维拉帕米（100μmol·L-1）可显著增加芍药苷在回肠的吸收（P<0.05）。给予白芍提取物5天后，回肠中罗丹明123的摄取显著增加（P<0.01）。
芍药苷的肠道吸收为零级速率过程且为被动吸收。芍药苷是P-糖蛋白的底物，白芍提取物可诱导P-糖蛋白的表达。
