大鼠在体肠灌注研究五味子有效成分肠吸收

Study on Intestinal Absorptive Mechanism of Effective Components of Schisandra by Rats Intestinal Perfusion in Situ

目的:考察五味子醇提取物中五味子醇甲、五味子酯甲、五味子甲素和五味子乙素四种有效成分在大鼠体内肠吸收机制。方法:通过建立大鼠在体循环肠灌注模型并运用HPLC法检测四种有效成分在不同浓度下以及在P-gp抑制剂共同作用下的吸收差异。结果:五味子四种有效成分,在考察的浓度范围以内浓度增加一倍,吸收速率常数Ka和表观渗透系数却没有显著性差异(P>0.05)。加入P-gp抑制剂维拉帕米(VP)与正常组相比,五味子酯甲、甲素和乙素的吸收速率常数(Ka)和表观渗透系数(Papp)都显著增加(P<0.05)。结论:五味子四种有效成分的吸收并非简单的被动扩散,而是载体媒介转运,其中五味子酯甲、五味子甲素和五味子乙素为P-gp的底物,通过加入P-gp抑制剂可促进这三种成分的吸收。

Objective：To investigate rat intestinal absorption mechanism of four active components,schisandrol A,schisantherin A,schisandrin A and schisandrin B.Methods：Established intestinal perfusion model in suit and used HPLC to determinate absorption differences of the four active components in different concentration and interaction with P-gp inhibitor.Results：The result of in situ intestinal perfusion display that four active components of Schisandrol A、Schisantherin A、Schisandrin A and Schisandrin B,while the concentration doubled,the absorption rate constant（Ka）and apparent permeability coefficient（Papp）was not significantly different Within the concentration range in the study（P0.05）.Adding P-gp inhibitors verapamil（VP）compared with normal group,four active ingredients of Schisandra on the absorption rate constant（Ka） and apparent permeability coefficient of schisantherin A,schisandrin A and schisandrin B are significant increase（P0.05）.Conclusion：It suggested that the transport mechanisms of four active components were not passive diffusion but active transport.Schisantherin A、Schisandrin A and Schisandrin B are the substrate of P-gp.There can promote the absorption of these three components.by joining the P-gp inhibitors.