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在体单向肠灌流模型研究绞股蓝皂苷的肠吸收特性

Intestinal absorption of gypenosides in rats by single pass perfusion in situ
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摘要 目的:对绞股蓝皂苷在大鼠小肠各肠段的吸收情况进行研究。方法:采用大鼠在体肠灌流法,应用HPLC-ELSD法测定肠吸收循环液中绞股蓝皂苷A、人参皂苷Rb1和人参皂苷Rd的浓度。结果:3种绞股蓝皂苷的吸收系数(Ka)和渗透系数(Peff)在小肠各肠段的吸收具有较大差异,渗透系数(Peff)表明3种绞股蓝皂苷在不同肠段的吸收为空肠〉十二指肠〉回肠〉结肠;在0.05~1.0g·L-1内,随着浓度的上升,绞股蓝皂苷会出现过饱和现象;加入地高辛后,人参皂苷Rb1的渗透系数显著下降(P〈0.05),而加入维拉帕米后,人参皂苷Rd的渗透系数增加极显著性(P〈0.01)。结论:绞股蓝皂苷受吸收部位影响较大,空肠是该类皂苷的主要吸收部位,其不完全依赖浓度梯度而进行转运,小肠吸收机制不完全为被动转运,载体蛋白有可能参与了转运,绞股蓝皂苷可能是P-糖蛋白的底物。 OBJECYIVE To determine intestinal absorption of gypenosides in rats. METttOIIS HPLC-ELSD was used to determine the absorption mechanism of gypenoside A, ginsenoside Rbl and ginsenoside Rd. RESULTS The experimental re- sults showed that the absorption rate constant (Ka) value and permeability coefficient (Pelf) displayed difference in various in- testinal segments. The Pelf values of three main gypenosides were different, the main absorption site was jejunum (jejunum〉 duodenum〉ileum〉colon). The gypenosides had excessive satuation phenomenon as the concentration increased from 0. 05 to 1.0μL-1. The values of Ka and Poff were reduced when the gypenosides was perfused with digoxin, especially ginsenoside Rbl decreased significantly (P〈0. 05). On the other hand, Ka and P~lf incleased when perfused with verapamil, especially Pal value of ginsenoside Rd increased very significantly (P〈0. 01). CONCLUSION Gypenosides are greatly influenced by absorption sites, and jejunum is the main absorption site. Gypenosides are not transported by a concentration dependent way entirely, the intestinal absorption of gypenosides is not realized entirely by passive diffusion method and the transporter protein may be in- volved in the process of transportation, and gypenosides might be the substrates of P-glycoprotein.
作者 喻樊 汤新慧 周姝婷 YU Fan1'2'3'4, TANG Xin-hui1 , ZHOU Shu-ting2 (1. Jiangsu Provincial Key Laboratory of Coastal Wetland Biore- sources, Jiangsu Yancheng 224002, China~ 2. College of Pharmacy, Yancheng Teachers University, Jiangsu Yancheng 224051, China; 3. Jiangsu Key Laboratory of Biochemistry and Biotechnology of Marine Wetland, Yancheng Institute of Tech- nology, Jiangsu Yancheng 224051, China~ 4. Key Laboratory of Biorheological Science and Technology, Chongqing University, Ministry of Education, Chongqing 400044, China)
出处 《中国医院药学杂志》 北大核心 2017年第12期1129-1133,共5页 Chinese Journal of Hospital Pharmacy
基金 国家自然科学基金项目(编号:81102817) 国家星火计划项目(编号:2015GA690276) “生物流变科学与技术”教育部重点实验室访问学者基金资助项目(编号:CQKLBST-2016-008) 盐城市农业科技创新专项引导资金项目(编号:YKN2016011) 江苏省青蓝工程项目 江苏省大学生创新重点项目(编号:201410324011Z) 江苏省盐土生物资源研究重点实验室项目(JKLBS2015008) 江苏省海洋滩涂生物化学与生物技术重点建设实验室项目(K2016-12) 盐城师范学院拔尖人才计划项目 大学生创新创业训练计划项目(编号:201710324015X) 2017江苏省高校中青年教师境外研修(访问学者)项目
关键词 绞股蓝皂苷 肠吸收 吸收速率常数 渗透系数 gypenosides intestinal absorption absorption rate constant permeability coefficient
作者简介 喻樊,男,博士,副教授,研究方向:药学,电话:0515—88258773,E-mail:pharmyufan@163.com
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