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丙磺舒药物键合两亲共聚物的制备
Synthesis of Amphiphilic Macromolecular Prodrugs Anchored with Probenecid
【摘要】 将非甾体抗炎药丙磺舒 (4 (二丙基氨磺酰基 )苯甲酸 )的羧基以酯键连接到甲基丙烯酸 2 羟基乙酯上得含丙磺舒单体 1 甲基丙烯酸 2 (4 (二丙基氨磺酰基 )苯甲酸 )乙二醇酯 (HP) ,HP在偶氮二异丁腈 (AIBN)引发下与聚环氧乙烷大单体 (PEO MA)共聚 ,合成了含丙磺舒药物基团的两亲共聚物 ,聚合产物运用1HNMR、FT IR和GPC进行了表征 ,讨论了引发剂、单体配比对共聚物分子量和丙磺舒含量的影响。结果表明 ,共聚物的分子量随AIBN用量增大逐渐变小 ,共聚物中的丙磺舒含量随单体投料中HP含量的增大逐渐变大
【Abstract】 A nonsteroidal antiinflammatory drug, probenecid, was covalently linked with 2-hydroxyethyl methacrylate(HEMA) through esterification reaction. The drug-linked HEMA(abbreviated as HP) was copolymerized with polyoxyethylene macromers(PEO-MA) to obtain macromolecular prodrugs using azobisisobutyronitrile(AIBN) as an initiator. The polymer was characterized with IR, 1H NMR and GPC. The effect of initiator amount and the ratio of drug to monomer were discussed. Increasing the amount of AIBN decreased the molecular weight of the copolymer. Increasing HP content in monomers increased probenecid content in the copolymer.
- 【文献出处】 应用化学 ,Chinese Journal of Applied Chemistry , 编辑部邮箱 ,2004年12期
- 【分类号】TQ463
- 【下载频次】118