姜黄素-羧甲基壳聚糖偶联物对环孢素A肠吸收的影响  

Effects of curcumin-carboxymethyl chitosan conjugates on intestinal absorption of cyclosporin A

作　　者：耿燕娜[1] 张文鑫[2] 娄婷婷[1] 武毅君[3] 

机构地区：[1]河南大学淮河医院药剂科,河南开封475000 [2]河南中医学院第一附属医院,河南郑州450000 [3]河南大学药学院,河南开封475000

出　　处：《中国医院药学杂志》2015年第3期223-227,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:探讨姜黄素-羧甲基壳聚糖偶联物对环孢素肠吸收的影响,为其临床应用提供理论基础。方法:采用大鼠在体单向肠灌流实验,用HPLC测定灌流液中环孢素的含量,计算不同浓度的姜黄素(Cur)、羧甲基壳聚糖(CMCS)、CMCS-Cur(CC)、CMCS-EDA-Cur(CEC)对环孢素在十二指肠和空肠的表观吸收速率常数(Ka)和肠壁有效通透性系数(Peff)的影响。结果:在十二指肠和空肠部位,加入Cur、CMCS、CC、CEC的实验组环孢素的Ka和Peff值高于单纯环孢素组(P<0.05);0.1%CsA&CMCS组高于0.1%CsA&Cur组(P<0.05);0.1%CEC&CsA组Ka、Peff值高于0.01%和1%CEC&CsA(P<0.05)。结论:Cur、CMCS、CC、CEC均能促进CsA在十二指肠和空肠部位的吸收,相同浓度下CMCS的促环孢素吸收作用优于Cur。OBJECTIVE To study the effects of curcumin-carboxymethyl chitosan conjugates on intestinal absorption of cyclosporin A,provide a theoretical foundation for their clinical applications.METHODS Single pass intestinal perfusion in situ was used to study the effects of curcumin-carboxymethyl chitosan conjugates on intestinal absorption of cyclosporin A.High performance liquid chromatography was used to determine cyclosporin A content,and the effects of different concentrations of Cur,CMCS,CMCS-Cur（CC）and CMCS-EDA-Cur（CEC）on the absorption rate constant（Ka）and intestinal effective permeability coefficient（Peff）of cyclosporin A in duodenum and jejunum.RESULTS The Ka and Peffvalues of experimental groups administering cyclosporine A containing Cur,CMCS,CC or CEC in duodenum and jejunum were higher than those of pure cyclosporin A group（P〈0.05）.The Kaand Peffvalues of 0.1% CsACMCS group were higher than those in 0.1%CsACur group（P〈0.05）,and Ka and Peffvalues of 0.1% CECCsA group were higher than those in 0.01% and 1%CECCsA groups（P〈0.05）.CONCLUSION Cur,CMCS,CC and CEC can promote absorption of cylosporin A in duodenum and jejunum.At the same concentration,the promoting effects of CMCS are superior to those of Cur on absorption of cylosporin A.

关 键 词：姜黄素-羧甲基壳聚糖偶联物 环孢素 肠吸收 在体单向小肠灌注 

分 类 号：R969[医药卫生—药理学]