季铵盐改性蒙脱石对五氟尿嘧啶的吸附和释药性能  

Adsorption and Release Performance of Quaternary Ammonium Modified Montmorillonite for 5-Fluorouracil

作　　者：彭琪[1] 葛莹莹 王帆帆 PENG Qi;GE Yingying;WANG Fanfan(College of Chemisty and Chemical Engineering,Xinyang Normal University,Xinyang 464000,China;Department of Pharmacy,Xinyang Central Hospital,Xinyang 464000,China)

机构地区：[1]信阳师范学院化学化工学院,河南信阳464000 [2]信阳市中心医院药剂科,河南信阳464000

出　　处：《信阳师范学院学报（自然科学版）》2018年第4期636-640,共5页Journal of Xinyang Normal University(Natural Science Edition)

基　　金：河南省科技计划项目(162102210403);河南省教育厅自然科学研究项目(12B150026)

摘　　要：以钠基蒙脱石为原料,用十六烷基三甲基氯化铵(CTAC)进行有机改性制备季铵盐改性蒙脱石(CMMT),之后吸附五氟尿嘧啶(5-FU),再用海藻酸钠(SA)进行包衣,最后测定该载药凝胶球的释药性能.考察p H值和释放时间等因素对载药凝胶球体外释放5-FU的影响规律,通过三种体外释放模型对其释药数据进行拟合,探讨了凝胶球中5-FU的释放机理,说明了季铵盐改性蒙脱石作为5-FU治疗结肠癌控释载体材料的可行性.结果表明:CMMT/SA对5-FU的载药量远大于MMT/SA,其载药量可达到0.6827 g/g;而载药凝胶球中5-FU的体外释放能力主要受释放介质p H值的影响,当p H 7.4时,5-FU/CMMT/SA中5-FU的累积释放率最大,可达到77.10%,在p H 1.5时的结果最小;一级动力学模型能比Korsmeyer-Peppas模型和Higuchi模型更好地拟合5-FU在不同p H下的体外释放情况.Cetyl trimethyl ammonium chloride(CTAC)was used to modify montmorillonite(MMT)to prepare organic montmorillonite(CMMT).Then the complexes were used to absorb the 5-fluorouracil(5-FU)and coated with sodium alginate(SA).The performance of the release of the drug-loaded gels was measured,and the effects of pH and time on 5-FU release from the complexes were explored.Three models of in vitro drug release were used to simulate the release performance of 5-FU-loaded gels.The release mechanism of 5-FU from the gels and the feasibility of MMT as the sustained-release drug carrier were discussed.The results showed that CMMT/SA had the larger drug loading rate than MMT/SA,and the drug loading reached 0.6827 g/g.The release performance of 5-FU-loaded gels was mainly influenced by the pH value of media.The in vitro cumulative amount of 5-FU released from 5-FU/CMMT/SA at pH 7.4 reached 77.10%,and the lowest was at a pH value of 1.5.The first order kinetics model was better used to describe the variation of in vitro release rate of 5-FU with time at different pH values,compared to the Korsmeyer-Peppas and Higuchi models.

关 键 词：蒙脱石 五氟尿嘧啶 季铵 吸附 释放 

分 类 号：O647.32[理学—物理化学]