甲氧基聚乙二醇吡硫醇制备条件的优化研究  

Preparation optimization of mPEG pyritinol

作　　者：万芬[1] 王红[1] 吴红菱[2] 蔡波涛[1] 马俊[1] 

机构地区：[1]湖北中医药大学药学院药物化学教研室,武汉430065 [2]湖北医药学院药检系,湖北十堰442000

出　　处：《中南药学》2011年第8期573-576,共4页Central South Pharmacy

基　　金：湖北省自然科学基金资助课题(编号:2007ABA213)

摘　　要：目的优化甲氧基聚乙二醇吡硫醇的制备条件。方法采用N-羟基丁二酰亚胺活性酯法合成甲氧基聚乙二醇吡硫醇,并以紫外分光光度法测定的甲氧基聚乙二醇吡硫醇中吡硫醇的载药量为考察指标,通过正交试验对合成工艺进行优化。结果甲氧基聚乙二醇吡硫醇较优工艺条件为:单甲氧基聚乙二醇4000琥珀酸单酯(mPEG4K-S)与N-羟基丁二酰亚胺(NHS)物质的量比为1∶1.5,在5℃反应2.5 h后再在5℃下加入吡硫醇和4-二甲氨基吡啶(DMAP)反应20 h。结论该合成工艺操作简便,稳定可行,产物中吡硫醇的载药量高。Objective To optimize the preparation of methoxy polyethylene glycol（mPEG） pyritinol.Methods mPEG pyritinol was synthesized by N-hydroxy succinimide active ester.Drug-loading rate of the prodrugs as the index was measured by the UV and the synthetic process was optimized by the orthogonal test.Results The optimal conditions are as follows：methoxy polyethylene glylol succiate（mPEG4K-S） and N-hydroxysuccinimide（NHS）（1∶1.5,n/n）reacted for 2.5 h at 5 ℃,and pyritinol and 4-dimethylamio pryidine（DMAP） were added and reacted for 20 h at 5 ℃.Conclusion The method is simple,stable and acceptable.It shows a high drug-loading rate of pyritinol in the product.

关 键 词：甲氧基聚乙二醇吡硫醇 单甲氧基聚乙二醇4000琥珀酸单酯 合成工艺 正交试验 

分 类 号：R914[医药卫生—药物化学] TQ460.31[医药卫生—药学]