大鼠外翻肠囊法研究马钱子中马钱子碱、士的宁的肠吸收特性  

Rat intestine absorption characteristics of brucine and strychnine with everted intestion model

作　　者：吕丹[1] 蒋且英[2] 梁新丽[1] 廖正根[1] 张婧[1] 曾荣贵 汤涛[1] 孔小强 

机构地区：[1]江西中医药大学现代中药制剂教育部重点实验室,南昌330004 [2]江西中医药大学继续教育学院,南昌330004

出　　处：《中药药理与临床》2016年第4期31-35,共5页Pharmacology and Clinics of Chinese Materia Medica

基　　金："赣鄱英才555"工程领导人才培养计划(赣财教指[2013]296号);江西省青年科学家培养对象(20153BCB23019)

摘　　要：目的:研究马钱子中马钱子碱、士的宁在大鼠肠道的吸收特性。方法:以表观渗透系数(Papp)为指标,运用大鼠外翻肠囊模型,研究不同肠段、浓度、p H、P-gp抑制剂、MRP抑制剂、细胞间紧密连接开放剂对马钱子中马钱子碱和士的宁在大鼠肠吸收的影响。结果:不同肠段中,马钱子中马钱子碱和士的宁的Papp为回肠≈结肠>空肠>十二指肠;不同浓度下,两者Papp无显著性差异;不同p H条件下,两者吸收有较大差异,其中p H=7.4条件下,两者吸收最好;在分别加入P-gp和MRP抑制剂后,两者的肠吸收均显著性增加;加入细胞间紧密连接开放剂,两者的肠吸收有一定的增加,但不显著。结论:马钱子中马钱子碱、士的宁肠吸收机制可能是以被动转运为主,且均受P-gp和MRP的影响。Objective： To study intestinal absorption characteristics of Brucine and Strychnine from the seed of Strychnos nux-vomica on rat. Methods： Taking Papp as the index, using rat everted gut sac model, to research the influence of the factors including different segments of intestine, concentration, pH, inhibitor of P-gp, inhibitor of MRP, inhibitor of cell tight junction on the rat intestinal absorption of Brucine and Strychnine. Results：The result showed that Brucine and Strychnine could be absorbed at all of the four intestinal segments with increasing ab- sorption amount per unit as follows： ileum ≈colon 〉 jejunal 〉 duodenal; The Papp of Brucine and Strychnine had no significant difference in the different drug concentration; The Papp of Brucine and strychnine had significant difference in the different pH, and the absorption was best under the pH 7.4 ; The intestinal absorption of Brucine or Strychnine had significantly increased after the addition of the inhibitor of P-gp or inhibitor of MRP; The intestinal absorption of Brucine and Strychnine had slightly rather significantly increased after the addition of the in- hibitor cell tight junction. Conclusion： Brucine and Strychnine absorption in intestine was mainly passive diffusion, and their intestinal ab- sorption also effected by P-gp and MRP.

关 键 词：马钱子碱 士的宁 外翻肠囊模型 P-GP MRP 细胞间紧密连接 

分 类 号：R285.5[医药卫生—中药学]