摘要
目的：为了改善阿司匹林药效，降低其毒副作用，探索出一条操作简便、成本低廉的糖基化方法，研制出一种副作用低的缓释药物葡萄糖-阿司匹林偶联物．方法：本文采用吡啶、浓NaOH溶液和浓硫酸作催化剂，在常压、不同温度、不同n（乙酰水杨酰氯）：n（葡萄糖）条件下，合成葡萄糖-阿司匹林共价偶联物，通过FT-IR、^1HNMR对其结构进行了表征。研究催化剂、反应温度以及反应物料比对酯化反应的影响，同时利用紫外分光光度法测定偶联物的接枝率。结果：在常压，50℃，n（乙酰水杨酰氯）：n（葡萄糖）=5：1，吡啶为催化剂条件下，偶联物的接枝率可达到54．9％。结论：在此反应中，吡啶是一种良好的催化剂；50℃是该反应的最佳反应温度；n（乙酰水杨酰氯）：n（葡萄糖）=5：1时，偶联物的接枝率和乙酰水杨酰氯的转化率都比较高。
Objective： To improve the drug effect of aspirin, reduce its side effect, find out a good glucosidation method and synthesize a glucose-aspirin conjugate which is of low side effect. Methods： ha this paper, Glucose-aspirin conjugate was synthesized via a reaction of o-acetoxybenzoyl chloride and glucose in normal pressure, at different temperature. Pyridine, NaOH and H2SO4 were used as catalyst ha the reaction. The products were characterized by FT-IR and ^1HNMR. Factors like catalysts, reaction temperature and molar ratio of reactants were investigated. The drug-loading ratio was measured by UV spectrophotometry. Results： The experiment confirmed that the drug-loading ratio reached up to 54.9% in normal pressure, at 50℃. O-acetoxybenzoyl chloride （Smol） and glucose （lmol） and pyridine were used as catalyst. Conclusions： In the experiment, pyridine was a good catalyst; the optimum temperature was 50℃; when o-acetoxybenzoyl chloride： glucose=5：1, both the drug-loading ratio and converting efficiency of o-acetoxybenzoyl chloride were very high.
出处
《现代生物医学进展》
CAS
2007年第7期1086-1088,共3页
Progress in Modern Biomedicine
基金
江西省科技厅资助项目
