基于在体循环肠灌流模型分析羊耳菊提取物的肠吸收特性  

Analysis of Intestinal Absorption Characteristics of Inula cappa Extract by in situ Intestinal Circulating Perfusion Model

作　　者：伍萍[1] 李梅[1] 巩仔鹏[1] 侯靖宇[1] 吴林霖 陈亭亭 李月婷[1] 陈思颖[1] 王爱民[1] 李勇军[1] 王永林[1] 兰燕宇[1] 

机构地区：[1]贵州医科大学贵州省药物制剂重点实验室民族药与中药开发应用教育部工程研究中心药学院国家苗药工程技术研究中心

出　　处：《中国实验方剂学杂志》2018年第2期1-8,共8页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(81360680);贵州省优秀青年科技人才培养项目(黔科合人字[2015]11号);贵州省民族药药效物质基础研究科技创新人才团队项目(黔科合平台人才[2016]5613);贵州省高层次创新型人才培养项目(百层次黔科合平台人才[2016]5677);贵州省科技合作计划项目(黔科合LH字[2015]7362)

摘　　要：目的：考察羊耳菊提取物在大鼠肠内的吸收特征。方法：采用大鼠在体循环肠灌流模型，选择羊耳菊提取物中东莨菪苷等9种代表性成分为考察对象，建立其UPLC-MS／MS并测量各成分的累计吸收量，探究药物质量浓度，胆汁，P-糖蛋白（P-gP）抑制剂及不同肠段对羊耳菊提取物中东莨菪苷等成分肠吸收的影响，阐明各成分在不同肠段的吸收特征。结果：东莨菪苷在高质量浓度条件下存在饱和现象，提示可能的吸收方式为主动转运，而1，3-二咖啡酰基奎宁酸等其余8种成分则无明显高浓度饱和现象，提示这8种成分可能的吸收方式均为被动扩散。木犀草苷，1，3-0-二咖啡酰基奎宁酸，3，4．0-二咖啡酰基奎宁酸和4，5-0-二咖啡酰基奎宁酸的主要吸收部位在空肠，东莨菪苷和3，5-0-二咖啡酰基奎宁酸的主要吸收部位在回肠，绿原酸、新绿原酸和隐绿原酸的主要吸收部位在十二指肠。羊耳菊提取物中东莨菪苷等9种成分的肠吸收均受到pH和胆汁的影响。结论：羊耳菊提取物中9种成分在小肠均有吸收，但各成分的吸收速率、最佳吸收部位及吸收机制不尽相同。Objective： To study on the absorptive characteristics oflnula cappa extract in rats by in situ intestinal circulating perfusion model. Method： Nine representative ingredients in I. cappa extract were selected as objects of this study. An UPLC-MS/MS was established to determine their cumulative absorption amount and investigate the absorptive amount of the nine components at different intestinal segments, influence of extract concentration, pH value, P-glycoprotein inhibitor, bile and different intestinal segments on intestinal absorption of the nine components for expounding the absorptive characteristics of ingredients in different intestinal sections. Result： Scopolin in high concentration existed saturation phenomenon, it indicated the transport mechanism of scopolin was active transport in the intestine and the other 8 compounds were passive diffusion. The best absorption sites of luteolin-7-glucoside, 1, 3-O-dicaffeoylquinic acid, 4, 5-O-dicaffeoylquinic acid and 3, 4-0- dicaffeoylquinic acid were jejunum. The best absorption sites of scopolin and 3, 5-O-dicaffeoylquinic acid were ileum. The best absorption sites of chlorogenic acid, cryptochlorogenic acid and neochlorogenic acid were duodenum. The absorption of all the compounds were affected by pH and bile. Conclusion： All of the nine ingredients in I. cappa extract can be absorbed in small intestine, but their absorption rate, the best absorptive site and mechanism are not the same.

关 键 词：羊耳菊 提取物 咖啡酰基奎宁酸 肠吸收 木犀草苷 在体循环肠灌流模型 绿原酸 

分 类 号：R283.6[医药卫生—中药学] R945[医药卫生—中医学]