高效液相色谱-质谱联用法研究芍药苷的大鼠小肠吸收

 目的研究芍药苷的大鼠小肠吸收,探讨芍药苷的吸收机制及其影响因素。方法使用高效液相色谱-质谱联用技术,采用肠外翻模型,测定不同质量浓度芍药苷溶液在大鼠空肠和回肠的吸收,同时观察加入聚山梨醇酯-80和P-糖蛋白抑制剂维拉帕米对芍药苷吸收的影响。结果在20～120mg·L^-1内,芍药苷吸收未饱和,呈线性吸收,在低质量浓度下空肠与回肠吸收速率无明显差异,中、高质量浓度时回肠吸收速率要高于空肠,2g·L^-1的聚山梨醇-80对空肠吸收有促进作用,维拉帕米对芍药苷吸收有显著促进作用。结论芍药苷在小肠外翻模型中吸收遵循一级动力学,芍药苷在不同肠段的吸收有差异,芍药苷是P-糖蛋白的底物,聚山梨醇-80有利于提高芍药苷的吸收。

Studies on Absorption of Paeoniflorin in Rat Small Intestines by HPLC-MS

OBJECTIVE To study the absorption of paeoniflorin in the small intestines of rat,and discuss the metabolism and the influence factors of absorption. METHODS The rat jejunum and ileum were incubated with different concentrations of paeoniflorin solution respectively,and the absorption of paeoniflorin in different models was determined by high performance liquid chromatography with mass detector (HPLC-MS). The influence on the absorption of paeoniflorin was investigated after adding Tween-80 and Verapamil,a p-glycoprotein inhibitor.RESULTS When the concentration was from 20 to 120 mg·L^-1,the uptake of paeoniflorin increased linearly and did not appear to be saturated. There wasn′t significant difference in the permeability coefficient between the jejunum and ileum at low concentration,but the latter was higher than the former at middle and high concentration. Tween -80 enhanced the absorption of paeoniflorin in jejunum,and Verapamil showed effect on increasing the absorption of paeoniflorin remarkably. CONCLUSION The absorption of paeoniflorin is different in the diverse intestinal segments,and is accorded with first-order kinetics. Paeoniflorin is the substrate of p-glycoprotein. Tween-80 can enhance the absorption of paeoniflorin.