外翻肠囊法研究藏族药翼首草肠吸收成分及其吸收特征

Investigation on intestinal absorption ingredients and their absorption characteristics in Pterocephali Herba by everted intestinal sac method

通过大鼠肠外翻模型评价翼首草中环烯醚萜苷和酚酸类10个化学成分的体外肠吸收特征。收集高、中、低浓度翼首草提取物给药后不同时间的肠囊液,采用UPLC-PDA检测肠吸收液样品中10个化学成分的含量,计算各成分在各肠段的累计吸收量和吸收速率常数,比较翼首草提取物与肠吸收液中指标成分的比例变化情况。结果发现:在不同给药浓度下,10个化学成分的肠吸收均为线性吸收(R2>0. 9),符合零级吸收速率;吸收速率常数与给药浓度、肠道部位有关,提示各成分的体外肠吸收有被动运输和主动转运;不同浓度翼首草肠吸收液的成分间比例与原提取物中各成分间比例存在差异。因此,肠道对翼首草中10个化学成分均有吸收,外翻肠囊法可有效地评价各成分的吸收特征。

The intestinal absorption characteristics of ten iridoid glycosides and phenolic acids in the Pterocephali Herba were evaluated via rat intestinal valgus model.The intestinal sac fluids at different time after administration of high,medium and low concentrations of Pterocephali Herba extract were collected and ten chemical components in fluid samples were detected by UPLC-PDA.Accumulative absorbed doses(Q)and absorption rate constants(Ka)of ten chemical constituents were calculated,while proportions between Pterocephali Herba extract and intestinal absorption liquid were compared.The results showed that the intestinal absorption of 10 chemical components was linear absorption(R2>0.9)at different concentrations,which accorded with the zero-order absorption rate.The absorption rate constant was related to the concentration of the drug and the intestinal site,which indicated that intestinal adsorption mechanism of the components were passive diffusion and active transport.Proportions of chemical constituents in intestinal sac fluid were different from those in Pterocephali Herba extract.Therefore,those ten chemical components in Pterocephali Herba extract can be absorbed in whole intestine.Everted intestinal sac model can be used to evaluate intestinal absorption characteristics of ingredients in Pterocephali Herba extract effectively.