淀粉支载阿司匹林前药的合成及其体外释放

Synthesis and in vitro drug release of starch aspirin as macromolecular prodrug

以淀粉和乙酰水杨酰氯为原料,合成了淀粉支载的阿司匹林高分子前药,用核磁共振谱对其进行结构表征,用紫外分光光度计测定阿司匹林的接入率,并在人工胃液和人工肠液中进行体外释放研究.结果表明,阿司匹林成功接入到淀粉分子上,该复合物在不同介质的体外释放中均呈现零级缓慢释药且释药的开始阶段无爆释现象出现,与阿司匹林相比较,其作用时间明显增长,有望显著减轻药物对胃粘膜和肠的刺激作用.

In order to obtain a sustained-release aspirin derivative, starch-aspirin conjugation was synthesized by coupling between starch and aeetoxybenzoyl chloride. Its structure was characterized with 1H-NMR. The drug-loading ratio of product was measured by ultraviolet spectrophotometer. And in vitro drug release investigation was carried out in artificial gastric juice and artificial intesti- nal juice. The results clearly showed that aspirin was coupled with the starch molecule successfully and the drug release rate of the conjugatation wss nearly zero order without abrupt release. Compared with aspirin, the effective therapeutic time of the polymer pro- drug was prolonged. So it may lead to less side-effect and relieving stimulation on gastrointestinal tract.