外翻肠囊法研究Pluronic/SWCNTs对P-糖蛋白底物罗丹明123小肠吸收的影响  

Effect of Pluronic/SWCNTs on intestinal absorption of rhodamine 123,a P-gp substrate via everted intestinal sacs

作　　者：关延彬[1,2] 韩冰 周树瑶 田雨冬 贾永艳[1,2] GUAN Yan-bin;HAN Bing;ZHOU Shu-yao;TIAN Yu-dong;JIA Yong-yan(School of Pharmacy,Henan University of TCM,Henan Zhengzhou 450040,China;Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment ＆ Chinese Medicine Development of Henan Province,Henan Zhengzhou 450040,China;Department of Urology Surgery,First Affiliated Hospital of Zhengzhou University,Henan Zhengzhou 450052,China)

机构地区：[1]河南中医药大学药学院,河南郑州450040 [2]呼吸疾病诊疗技术与新药研发河南省协同创新中心,河南郑州450040 [3]郑州大学第一附属医院泌尿外科,河南郑州450052

出　　处：《中国医院药学杂志》2018年第16期1681-1685,共5页Chinese Journal of Hospital Pharmacy

基　　金：河南省科技攻关项目(编号:182102310096);河南省教育厅科学技术研究重点项目(编号:13A350554);河南中医学院省属科研业务专项基金(编号:2014KYYWF-QN12)

摘　　要：目的:考察3种Pluronic/SWCNTs载体材料对小肠P-糖蛋白(P-gp)药泵的抑制作用。方法:采用外翻肠囊模型进行肠吸收实验,以P-gp特异性底物罗丹明123(R-123)大鼠肠吸收参数为考察指标,研究Pluronic/SWCNTs对R-123肠吸收的影响。结果:Pluronic/SWCNTs可以显著增加R-123在各肠段的累计吸收量与吸收速率常数,特别是在浓度为5μg·mL-1与10μg·mL-1时作用最明显(P<0.05)。结论:Pluronic/SWCNTs可以通过抑制P-gp药泵作用改善P-gp底物药物的小肠吸收,在口服载药系统的应用中具备很大的潜力。OBJECTIVE To investigate the effect of three types of functionalized Pluronic/SWCNTs on intestinal P-glycoprotein（P-gp）.METHODS The in vitro everted gut sacs models were adopted for intestinal absorption test and rhodamine 123（R-123）was used as the specific substrate of P-gp.The intestinal absorption parameters of R-123 were the indices for the evaluation of the effects of Pluronic/SWCNTs on intestinal absorption of R-123.RESULTS The three Pluronic/SWCNTs significantly increased the accumulative absorption and absorption rate constants of R-123 in excised ileum of rats,especially at the concentrations of 5 and 10μg·mL-1.CONCLUSION Pluronic/SWCNTs are capable of modulating the intestinal absorption of P-gp substrate by inhibiting intestinal P-gp activity.Pluronic/SWCNTs exhibit strong potential for the oral drug delivery applications.

关 键 词：P-糖蛋白 外翻肠囊法 Pluronic/SWCNTs 肠吸收 

分 类 号：R96[医药卫生—药理学]