摘要
目的:研究北五味子提取物的吸收调控机制。方法:通过建立Caco-2细胞体外模型研究北五味子提取物在不同浓度下以及在P-糖蛋白抑制药维拉帕米共同作用下的吸收差异。结果:随着浓度的提高,低、中浓度的五味子醇甲和五味子酯甲两种有效成分在聚碳酯膜上转运的吸收速率常数(Ka)和表观渗透系数(Papp)差异均有统计学意义(P<0.05),而高、中浓度间差异无统计学意义(P>0.05)。加入维拉帕米后,在AP侧到BL侧(AP-BL)转运中,五味子醇甲和五味子酯甲的Ka和Papp均显著升高(P<0.05),而在BL侧到AP侧(BL-AP)方向的转运中,两种有效成分的Ka和Papp均显著降低(P<0.05)。结论:五味子提取物中五味子醇甲、酯甲两种有效成分在小肠的吸收转运方式为载体媒介转运,而且皆为P-gp的底物。通过加入P-gp抑制药能抑制P-gp的外排作用从而促进药物在小肠的吸收转运。为今后五味子相关制剂研究开发提供理论依据。
Objective：To investigate the absorption mechanism of Schisandra extraction.Methods：Caco-2 cells model in vitro was established and the absorption differences between schisantherin A and schisandrin A with different concentrations combined with a Pgp inhibitor verapamil （VP） were detected.Results：With the increase of Schisandrae extracts concentration,Ka and Papp for the transportation on polycarbonate membrane of Schisandrol A and Schisantherin A in the low dose group were significant higher than those in the medium dose group （P 〈0.05）,and the high dose group showed no significant difference compared with the medium dose group（P 〉 0.05）.Under the interaction of VP,Ka and Papp of Schisandrol A and Schisantherin A were significantly increased in the AP-BL transportation （P 〈 0.05）,while those in the BL-AP transportation were both decreased significantly （P 〈 0.05）.Conclusion：The absorption and transportation of Schisandrol A and Schisantherin A are in the carrier-mediated ways in intestine,and they are both the substrate of P-gp.By adding the P-gp inhibitor VP can inhibits efflux function of P-gp to promote absorption of drugs.The experiment can provide a theoretical basis for Schisandra relevant preparations
出处
《中国药师》
CAS
2014年第6期908-911,共4页
China Pharmacist
基金
国家自然科学基金项目(编号:81102548)
