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含葡糖基酮洛芬乙烯醇酯共聚物的合成及其药物释放性能 被引量:1

Preparation and Sustained-release of Ketoprofen Polymeric Prodrug with Glucose Pendant
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摘要 分别利用化学法和酶促法合成了酮洛芬乙烯酯和葡萄糖丁二酸乙烯酯(6-O-乙烯丁二酰-D-葡萄糖)2种聚合单体,通过2种单体的自由基聚合反应制备了具有较高分子量的酮洛芬葡萄糖共聚物前药,通过IR、NMR对聚合物的结构进行了表征,用GPC方法测定共聚物分子量。研究了聚合单体投料比例对共聚物分子量和载药量的影响。结果表明,随着药物乙烯酯在投料中比例的增加,聚合物前药的分子量逐渐下降,聚合物中酮洛芬的载药量逐渐增加。酮洛芬含糖聚合物前药的体外释放研究表明,酮洛芬的释放时间大大延长,达到了缓释的目的,释药速率随着聚合物前药中葡萄糖含量增加而加快。聚合物前药的释放动力学模拟结果显示,共聚物释药更符合一级动力学释放模型。 An enzymatic synthesis and chemical polymerization strategy has been used to prepare ketoprofen polymeric prodrug with glucose pendant.Polymerizable ketoprofen vinyl ester(KVE) and glucose derivative(6-O-vinylsuccinoyl-D-glucose)(VSUG) were obtained.Then,polymeric prodrugs of ketoprofen were synthesized by the two kinds of monomers with different molar ratios(n(KVE) :n(VSUG) :1:1,1:2,2:1,4:1) through free radical reaction using AIBN as the initiator.The structures of products were confirmed by IR,NMR,and GPC.The results suggested that the molecular weight decreased and drug loading capacity increased as the ratio of KVE in the feed raised.In vitro release behavior of these copolymers was investigated in PBS(pH = 7.4) at 37 ℃.Contrast to the parent drug,the outcome demonstrated that the polymeric prodrug could effectively prolong the drug release rate.And the release rate of ketoprofen from polymeric prodrugs increased with the raising of glucose in the polymeric prodrug.Furthermore,investigations of the drug release profiles and kinetics suggested that the drug release gave a good fit to first-order kinetic model.
出处 《应用化学》 CAS CSCD 北大核心 2010年第12期1386-1391,共6页 Chinese Journal of Applied Chemistry
基金 国家自然科学基金(50773009) 上海市科委基金(08JC1400600) 中央高校基本科研业务费专项资金资助项目
关键词 共聚物 酮洛芬 含糖药物 酶促合成 释放动力学 载药系统 copolymer ketoprofen saccharide enzyme-catalyzed synthesis dynamic release drug delivery
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  • 1Natu MV, HCde Sousa, MH Gil, Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fi-bers[J]. Int J Pharm, 2010,397 (1-2) : 50-58.
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  • 7吴承尧,权静,李树白,朱利民.高分子药物载体的应用及研究趋势[J].化学世界,2009,50(9):561-563. 被引量:11
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  • 9吴承尧,谢建刚,权静,朱利民.非甾体类药物含糖乙烯醇酯共聚物制备及药物释放研究[J].化学学报,2011,69(7):843-847. 被引量:4
  • 10朱全刚,胡晋红,范国荣,孙华君,刘成,李凤前.酮洛芬异丙酯在皮肤细胞中的代谢[J].中国医院药学杂志,2002,22(4):195-197. 被引量:15

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