主 办:北 京 中 医 药 大 学
ISSN 1006-2157 CN 11-3574/R

北京中医药大学学报 ›› 2015, Vol. 38 ›› Issue (9): 624-628.doi: 10.3969/j.issn.1006-2157.2015.09.010

• 药代动力学 • 上一篇    下一篇

在体单向肠灌流模型研究千金子甾醇在大鼠肠吸收特性*

张秀婷1 王英姿1# 李韶菁2 段飞鹏1 王晴1 张春泥1 李凤英1 李文华1 骆声秀1   

  1. 1 北京中医药大学中药学院 北京 100102; 2 中国中医科学院中药研究所
  • 收稿日期:2015-03-18 出版日期:2015-09-30 发布日期:2015-09-30
  • 通讯作者: 王英姿,女,博士,教授,博士生导师,研究方向:中药制剂新技术研究,E-mail: wangyzi@sina.com
  • 作者简介:张秀婷,女,在读硕士生
  • 基金资助:
    *国家自然科学基金资助项目(No.81274082),北京中医药大学协同创新建设计划(No.2013-XTCX-03)

Characteristic of intestinal absorption of euphorbia factor L1 by rats single pass intestinal perfusion moder in situ*

ZHANG Xiuting1, WANG Yingzi1#, LI Shaojing2,DUAN Feipeng1, WANG Qing1, ZHANG Chunni1, LI Fengying1,LI Wenhua1, LUO Shengxiu1   

  1. 1 School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102; 2 Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences
  • Received:2015-03-18 Online:2015-09-30 Published:2015-09-30

摘要: 目的 研究千金子甾醇在大鼠肠道内的吸收情况以及 P-糖蛋白(P-gp)和多药耐药相关蛋白(MRP2)对千金子甾醇肠吸收的影响。方法 采用大鼠在体单向肠灌流模型,运用高效液相色谱法测定十二指肠、空肠、回肠、结肠灌流液中千金子甾醇的含量,计算吸收速率常数(Ka)和表观渗透系数(Papp)。结果 千金子甾醇在大鼠结肠的Ka及Papp最高(P<0.05)。加入P-gp抑制剂盐酸维拉帕米后,千金子甾醇在结肠段的Ka及Papp显著增加;而加入MRP2抑制剂吲哚美辛后,千金子甾醇在大鼠结肠段的Ka及Papp普遍降低。结论 千金子甾醇在肠道中的主要吸收部位为结肠,推测千金子甾醇可能为P-gp的底物,而非MRP2的底物。

关键词: 单向肠灌流, 千金子甾醇, P-糖蛋白, 多药耐药相关蛋白, 大鼠

Abstract: Objective To study the characteristic of absorption of euphorbia factor L1 in intestine of rats, and to observe the effects of P-glycoprotein(P-gp)and multidrug resistance-associated protein(MRP2)on intestinal absorption of euphorbia factor L1. Methods The contents of euphorbia factor L1 of intestinal perfusion fluid of duodenum, jejunum, ileum and colon in the rats in situ single-pass intestinal perfusion model were determined by using HPLC. The drug absorption rate constant(Ka) and the apparent absorption coefficient(Papp) in four intestinal regions were calculated. Results Ka and Papp of euphorbia factor L1 at colon were the highest of the whole rat intestine. Significant increase of Ka and Papp showed at rat colon when co-perfused with verapamil hydrochloride, by contrast, decrease of Ka and Papp found when co-perfused with indomethacin. Conclusion We inferred that verapamil hydrochloride be the substrate of P-gp and that indomethacin be not the substrate of MRP2.

Key words: single-pass intestinal perfusion, euphorbia factor L1, P-glycoprotein, multidrug resistance-associated protein, rats

中图分类号: 

  • R969.1