甲氨蝶呤/蒙脱土纳米插层化合物的制备及缓释作用研究  

Preparation and sustained-release action of Methotrexate/Montmor-illonite Intercalation system

作　　者：全先高[1] 王慧云[1] 丁林[1] 孙珊珊[1] 宋雪艳[1] 徐娜[1] 

机构地区：[1]济宁医学院药学院,山东日照276826

出　　处：《济宁医学院学报》2014年第4期251-255,259,共6页Journal of Jining Medical University

基　　金：济宁医学院立项项目(编号:JY2013KJ022)

摘　　要：目的制备甲氨蝶呤(MTX)/蒙脱土(MMT)插层体系,研究插层化合物的体外释放性能,为新型药物载体材料及新剂型的开发提供依据和指导。方法以MTX为插层客体,MMT为插层主体,采用溶液插层技术制备了MTX/MMT插层体系,采用傅立叶红外变换光谱仪,X射线衍射分析仪,差示扫描量热仪等手段进行了表征;考察了初始药物浓度、反应时间,反应温度等因素对MMT载药量的影响,并通过在模拟胃肠液的体外释放实验来考察插层体系的释放规律和内在机理。结果在初始浓度为0.8800mmol/g,反应温度为323K,反应时间为4h时插层体系载药量最大,体外释放试验表明在模拟胃液和模拟肠液中均具有明显的缓释效果,且在模拟胃液中释放速率明显低于模拟肠液。结论 MTX/MMT插层体系具有明显的缓释作用,且其释放行为受到释放介质pH的影响。Objective In order to provide basis and guidance for the development of the new materials for the drug delivery system and new drug forms,the Methotrexate（MTX）/Montmorillonite（MMT） intercalation system was prepared and its Release Properties in vitro were investigated. Methods The MTX/MMT system was prepared with MTX as intercalating object and MMT as intercalating subject by solution intercalation technique,and the product was characterized by infrared spectra（FTIR）, the X-ray diffraction（XRD）,and the Thermogravimetric Analyzer（TG）. Moreover, the factors such as the initial drug concentration,reaction time and temperature which influence the drug loading of the Methotrexate/Montmorillonite composite were investigated. Furthermore, the rules and the internal mechanism of the slow release in vitro of the MTX/MMT intercalation system was studied through the simulation fluid of gastric and intestinal. Results The results showed that the drug loading was the largest under the optimal conditions of the initial concentration of drug 0. 8800mmol/g, reaction temperature 323 K,reaction time 4h. The release results in vitro indicated that the sustained release behavior of Methotrexate/ Montmorillonite composite was obviously observed in simulated gastric fluid and simulated intestinal fluid. Moreover, the release rate in simulated gastric juice was significantly lower than that of in the simulated intestinal juice. Conclusion MTX/MMT intercalation composite was the sustained release system,and release behavior was affected by the pH values of the release medium. And Montmorillonite as a kind of inorganic drug carrier material has a broad application prospects in developing new dosage forms of drug.

关 键 词：蒙脱土 甲氨蝶呤 插层化合物 缓释 

分 类 号：TB332[一般工业技术—材料科学与工程]