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含丙磺舒高分子药物的合成与表征
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摘要
非甾体抗炎药丙磺舒以酯键连接到甲基丙烯酸2-羟基乙酯上得含丙磺舒单体(简称为HP),此单体在THF中经偶氮二异丁腈引发进行了均聚、与甲基丙烯酸甲酯进行了共聚,合成了含丙磺舒侧基的高分子药物,在水中与甲基丙烯酸甲酯进行了乳液聚合,合成了含丙磺舒的纳米高分子微球。为了增加高分子药物的亲水性,HP和乙氧基聚氧乙烯(PEO)大单体进行共聚,合成了两亲的高分子药物;含丙磺舒端基PEO大单体和甲基丙烯酸甲酯进行共聚,也达到了同样的目的。合成产物运用~1H-NMR、IR、GPC、DSC和,TEM进行了表征,并考察了反应条件对产物的影响。
Nonsteroidal antiinflammatory drug, probenecid, was linked with 2-hydroxyethyl methacrylate ( HEMA ) through covalent linkage. Initiated by azobisisobutyronitrile (AIBN), the drug-linked HEMA (abbreviated as HP) was homopolymerized and copolymerized with methy methyacrylate (MMA) to obtain polymeric drug in THE. HP polymeric nano-particles were prepared by emulsion copolymerization in water. To enhance polymer's hydrophilicity , amphiphilic graft copolymer containing probenecid was synthesized from radical copolymerization of HP with poly(ethylene oxide) (PEG) macromonomer. It was also synthesized from radical copolymerization of MMA with poly (ethylene oxide) macromonomer containing HP. Synthetic products were characterized with IR, 1H-NMR, GPC, DSC and TEM. Various experiment parameters controlling the copolymerization were studied in detail.
引文
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