论文部分内容阅读
利用大鼠在体循环灌流模型,采用UPLC-ESI-MS/MS测定灌流液中头花蓼提取物主要活性指标成分没食子酸、原儿茶酸、杨梅苷、金丝桃苷和槲皮苷的含量,并计算出吸收速率常数和累积吸收百分率。分别考察不同药物浓度、不同肠段、胆汁及P-糖蛋白抑制剂对头花蓼提取物中没食子酸等成分在大鼠体内的吸收机制的影响。实验结果表明,头花蓼提取物中没食子酸、原儿茶酸、杨梅苷、槲皮苷在高浓度下存在饱和现象(P<0.05);胆汁对原儿茶酸的吸收具有显著的抑制作用(P<0.05),对杨梅苷和金丝桃苷的吸收具有促进作用(P<0.05);P-糖蛋白抑制剂维拉帕米能显著增加原儿茶酸的吸收(P<0.05);各成分的吸收总体趋势为小肠优于结肠。表明头花蓼提取物在大鼠肠道的吸收符合一级动力学特征。几种成分在整个肠段都有吸收,主要吸收部位在小肠,原儿茶酸可能是转运蛋白P-gp的底物。
The content of gallic acid, protocatechuic acid, myricitrin, hyperoside and quercitrin in the perfusate was determined by UPLC-ESI-MS / MS in rat systemic circulation perfusion model. , And calculated absorption rate constant and cumulative absorption percentage. The effects of different concentrations of drugs, different bowel segments, bile and P-glycoprotein inhibitors on the absorption mechanism of gallic acid and other constituents in Polygonum capitatum extract in rats were investigated. The results showed that there was saturation of gallic acid, protocatechuic acid, myricitrin and quercitrin at the high concentration in Polygonum capitatum extract (P <0.05); bile had a significant inhibitory effect on the absorption of protocatechuic acid (P <0.05), and had a positive effect on the absorption of myricetin and hyperoside (P <0.05). P-glycoprotein inhibitor verapamil significantly increased the absorption of protocatechuic acid (P <0.05). The overall trend for the absorption of each component is that the small intestine is superior to the colon. The results showed that the absorption of Polygonum capitatum extract in rat intestine conformed to the first-order kinetic characteristics. Several components are absorbed throughout the bowel segment, the main absorption site in the small intestine, protocatechuic acid may be the transporter P-gp substrate.