穿心莲内酯自微乳在Caco-2细胞模型中的转运机制研究  

Study on Transport Mechanism of Andrographolide Self-microemulsion in Caco-2 Cell Model

作　　者：李韶清 张焕滨 刘丹霞[1] 廖华卫[1] 崔升淼[1] 

机构地区：[1]广东药学院中药学院,广东广州510006

出　　处：《亚太传统医药》2016年第1期12-15,共4页Asia-Pacific Traditional Medicine

基　　金：2014年国家级大学生创新创业训练计划项目(201410573008)

摘　　要：目的:研究穿心莲内酯自微乳在Caco-2细胞模型中的跨膜转运机制,预测其提高药物生物利用度的能力。方法:采用Caco-2细胞模型进行穿心莲内酯及穿心莲内酯自微乳的转运研究,考察药物浓度、温度及P-gp抑制剂对药物转运的影响。结果:穿心莲内酯自微乳的P_(app)(AP-BL)值较穿心莲内酯增加了约5倍;穿心莲内酯P_(app)值随浓度和温度的增加变化不大;加入P-gp抑制剂后,穿心莲内酯外排率(ER)由1.57降为1.2,降低了23.6%。结论:穿心莲内酯自微乳能促进药物的跨膜转运,药物在Caco-2细胞模型中的转运机制主要是被动扩散,同时存在P-gp蛋白介导的外排作用。Objective：To study the transport mechanism of andrographolide self-microemulsion（AP-SME）by using Caco-2cell model and predict the ability of improving bioavailability.Methods：The effects of concentration,temperature and verapamil（P-gp inhibitor）on the transport of AP and AP-SME in Caco-2cell monolayer model were studied.Results：Compared with AP,the Papp（AP-BL）of AP-SME increased about 5times,and Papp varied little while concentration of AP or temperature increased.When coupled with P-gp inhibitor（Verapamil）,the efflux rate（ER）of AP decreased from 1.57 to 1.2.Conclusion：AP-SME promoted the permeation of AP,and the absorption of AP-SME in Caco-2cell model was mainly through a passive transcellular transport with active efflux possibly mediated by the P-glycoprotein.

关 键 词：穿心莲内酯 自微乳 CACO-2细胞模型 跨膜转运 

分 类 号：R283.6[医药卫生—中药学]