荭草花提取物中5种成分在大鼠体内的肠吸收动力学  

Intestine absorption kinetics for five constituents in Polygonum orientale flower extract in rats

作　　者：谢玉敏[1] 杨武[1] 陆苑[1,2] 郑林[1,2] 陈思颖[1,2] 黄勇[1,2] 

机构地区：[1]贵州医科大学,贵州省药物制剂重点实验室,贵州贵阳550004 [2]贵州医科大学药学院,贵州贵阳550004

出　　处：《中成药》2016年第4期770-776,共7页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金项目(81360664);国家科技支撑计划课题(2013BAI11B01);贵州省中药现代化科技产业专项基金项目(黔科合重G字[2013]4001)

摘　　要：目的研究荭草花Polygonum orientale L.提取物中原儿茶酸、花旗松素、山柰素-葡萄糖苷、槲皮苷、山柰素-鼠李糖苷在大鼠体内的肠吸收动力学特征。方法采用在体肠灌流模型,超高效液相色谱-电喷雾-串联质谱(UPLCESI-MS/MS)法测定这5种成分质量浓度。结果这些成分对p H值均不敏感,可能不是药物转运蛋白P-gp的底物;原儿茶酸、山柰素-葡萄糖苷、槲皮苷和山柰素-鼠李糖苷在高质量浓度下存在饱和现象;胆汁对原儿茶酸的吸收具有抑制作用,而对山柰素-葡萄糖苷的吸收具有促进作用。结论荭草花提取物中这5种成分在整个肠段都有吸收,而且小肠优于结肠,符合一级动力学特征。AIM To study the intestinal absorption kinetic characteristics of protocatechuic acid,taxifolin,kaempferol-3-O-β-D-glucosid,quercitrin and kaempferol-3-O-α-L-rhamnosid in Polygonum orientale flower extract in rats. METHODS Based on the in situ intestinal perfusion model,the concentrations of these five constituents were determined by ultra-performance liquid chromatography electrospray ionization-tandem mass（ UPLC-MS/MS）. RESULTS Being insensitive to p H,these constituents might not be the P-gp substrates. Saturation phenomenon occurred in protocatechuic acid,kaempferol-3-O-β-D-glucosid,quercitrin and kaempferol-3-O-α-L-rhamnosid at high concentration. The bile inhibited the absorption of protocatechuic acid and promoted that of kaempferol-3-O-β-D-glucosid. CONCLUSION These five constituents in Polygonum orientale flower extract can be absorbed in the whole intestinal segments and they are absorbed more in small intestine than those in the colon,which accords with first-order absorption kinetics.

关 键 词：荭草花提取物 原儿茶酸 花旗松素 山柰素-葡萄糖苷 槲皮苷 山柰素-鼠李糖苷 肠吸收动力学 UP-LC-MS/MS 

分 类 号：R969.1[医药卫生—药理学]