PEG-HA-MEL的合成及其工艺优化  

Synthesis and Process Optimization of PEG-HA-MEL

作　　者：徐海星[1] 姜晓晔 许沛虎[1] 黄志军[1] 李冉[1] 陈伟平[1] 

机构地区：[1]武汉理工大学化学工程学院,武汉430070

出　　处：《武汉理工大学学报》2012年第6期119-123,共5页Journal of Wuhan University of Technology

基　　金：湖北省自然科学基金(2010CDB01006;2011CDA056);武汉市科技局国际合作与交流项目(201171034316)

摘　　要：将PEG2000进行活化后用来修饰透明质酸,得到PEG-HA,与美法仑键合得到前药PEG-HA-MEL。采用单因素实验考察相关因素对产率的影响,主要包括投料比、时间、催化剂和pH等,最终得到了各步骤的最优反应条件。用红外光谱、动态光散射和透射电镜对合成产物进行表征。结果表明:最优条件下,PEG活化的产率达到86.8%;PGE活性酯的产率达到84.2%;PEG-HA的产率为78.8%;PEG-HA-MEL的产率最高为62.3%。PEG-HA-MEL能在水溶液中形成胶束且其粒径在分布在120nm左右。Using activated PEG to modify HA, PEG-HA was then connected with melphalan （MEL） to prepare PEC-HA-MEL pro-drug. The factors affecting the yield were studied through the single factor method, which include feed rati o, reaction time, catalyst and pH. Finally optimal reaction conditions were got for each step. The products were characterized by infrared spectrum,DLS and TEM. It was showed that, with the optimal conditions , the yield of the activation of PEG was proved to be 86.8%,the PEG-active ester was 84. 2% ,PEG-HA was 78. 8% and PEG-HA-MEL was up to 62.3%. PEG-HA-MEL can form miceHes in aqueous solution, which particle size distribution of 120 nm.

关 键 词：卵巢癌 聚乙二醇 透明质酸 美法仑 合成 单因素实验 

分 类 号：O636.9[理学—高分子化学]