利用Caco-2细胞模拟羟基喜树碱在小肠内吸收的研究  

Absorption of hydroxycamptothecin by simulating epithelial cells of intestine with Caco-2 cells

作　　者：蒲晓辉[1,2] 杨浩[1] 孙进[2] 王永军[2] 何仲贵[2] 

机构地区：[1]河南大学药学院,河南开封475004 [2]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《中成药》2012年第7期1203-1208,共6页Chinese Traditional Patent Medicine

基　　金：国家重点基础研究发展计划(973项目)(2009CB930300);国家自然基金项目(81173008)

摘　　要：目的研究羟基喜树碱在小肠内的可能吸收机制。方法采用Caco-2细胞模型模拟小肠上皮细胞,研究质量浓度、表面活性剂和P-gp抑制剂对羟基喜树碱的跨膜吸收与转运的影响,总结羟基喜树碱的吸收与转运规律,通过数据分析推断出羟基喜树碱在小肠内的可能吸收机制。结果药物摄取量随质量浓度的增加而非线性增加。表面活性剂和P-gp抑制剂的加入都能增加药物的跨膜吸收量与转运速率。结论羟基喜树碱的跨膜吸收可能受到P-gp的外排作用。AIM To study the absorption mechanism of hydroxycamptothecin（HCPT） in small intestines.METHODS Caco-2 cell model was used to simulate small intestinal epithelial cells.The influence of concentration,surfactant and P-gp inhibitors on the absorption across membrane of HCPT was studied.The absorption mechanism of HCPT from the small intestines was concluded by analyzing the data.RESULTS In the cell test of the different HCPT concentrations,the results showed the intake of HCPT increased nonlinearly with the increase of HCPT concentration.The results in the influencing test proved that surfactant and P-gp inhibitors could increase the absorptivity and transport rate of HCPT across cell monolayer.CONCLUSION The experimental results show that the absorption process of HCPT is possibly affected by P-gp.

关 键 词：羟基喜树碱 纳米混悬剂 CACO-2细胞 摄取与转运 

分 类 号：R966[医药卫生—药理学]