摘要
目的合成吡硫醇聚乙二醇前体药物,对目标化合物进行初步体外释放及刺激性试验研究。方法以单甲氧基聚乙二醇4000为原料,与丁二酸酐反应后再与N-羟基丁二酰亚胺缩合得到活泼酯,最后与吡硫醇反应得到目标化合物;用薄层色谱、紫外、红外、核磁共振氢谱对其结构进行表征。结果与结论合成产物的结构表征结果表明单甲氧基聚乙二醇4000成功地连接到了吡硫醇上;初步的体外降解及刺激性试验表明该前药具有一定缓释作用,且能显著减小对注射部位及血管的刺激作用。
Objective To synthesize and characterize pyritinol-PEG prodrug, and assess its in vitro release and irritation. Methods mPEG4K was first reacted with succinic anhydride, and then treated with Nhydroxyl succinic anhydride, finally, reacted with pyritinol to give the target pyritinol-PEG which is the prodrug of pyritinol. Results The chemical structure of pyritinol-PEG was characterized by TLC, UV, FFIR and 1H-NMR. Conclusion The structural characterization of the target compound showed that mPEG4K was bonded to pyritinol. This prodrug has slow-release profile during in vitro release test, and significantly low vascular irritation.
出处
《广东药学院学报》
CAS
2009年第5期493-495,共3页
Academic Journal of Guangdong College of Pharmacy
基金
湖北省自然科学基金资助课题(2007ABA213)
