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化学学报
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化学学报 ›› 2011, Vol. 69 ›› Issue (07): 843-847. 上一篇    下一篇

研究论文

非甾体类药物含糖乙烯醇酯共聚物制备及药物释放研究

吴承尧1，谢建刚1,2，权静*,1朱利民*,1   

  1. (1东华大学化学化工与生物工程学院 上海 201620)
    (2郑州师范学院化学系 郑州 450016)
  • 投稿日期:2009-09-11 修回日期:2010-10-10 发布日期:2010-12-10
  • 通讯作者: 朱利民 E-mail:lzhu@dhu.edu.cn，jquan@dhu.edu.cn

Preparation and Sustained-release of Polymeric Drug-glucose Conjugates with NSAIDs Pendants

Wu Chengyao1 Xie Jiangang1,2 Quan Jing*,1 Zhu Limin*,1   

  1. (1 Donghua University, Chemical Engineering and Biotechnology, Shanghai 201620)
    (2 Department of Chemistry, Zhengzhou Normal University, Zhengzhou 450016)
  • Received:2009-09-11 Revised:2010-10-10 Published:2010-12-10

PDF

1047

被引次数

10

分别利用化学法和酶促法合成了三种药物(萘普生、酮洛芬、布洛芬)乙烯酯和葡萄糖丁二酸乙烯酯(6-O-乙烯丁二酰-D-葡萄糖)两种聚合单体, 通过两种单体的自由基聚合反应制备了具有较高分子量的含糖聚合物前药. 通过IR、NMR对聚合物的结构进行了表征, 用GPC测定共聚物分子量. 含糖聚合物前药的体外释放研究表明, 将小分子原药制备成含糖聚合物前药后, 药物的释放时间大大延长, 达到了缓释的目的. 三种含糖聚合物的药物释放研究表明, 酮洛芬含糖高分子前药的药物释放速率较快, 萘普生含糖高分子前药的药物释放速率较慢. 不同的pH条件下的含糖聚合物的药物释放研究表明, 碱性环境下的药物释放较快, 酸性环境下的药物释放较慢.

关键词: 高分子前药, 酮洛芬, 布洛芬, 萘普生, 含糖药物, 共聚物

An enzymatic synthesis and chemical polymerization strategy has been used to synthesize drug vinyl ester and 6-O-vinylsuccinoyl-D-glucose. Then, polymeric drug-glucose conjugates with NSAIDs (nonsteroidal anti-inflammatory drugs) pendants were prepared by the two kinds of monomers through free radical reaction using AIBN as initiator. The structures of products were characterized by IR, NMR, and GPC. In vitro release behavior of these copolymers was investigated in PBS solution (pH＝7.4) at 37 ℃. Contrast to the parent drug, the outcome demonstrated that the polymeric prodrugs effectively prolonged the drug release rate, and the drug release rate was higher from naproxen prodrug than that of ibuprofen prodrug. The drug release behavior at various pH suggested that the drug release at alkaline medium was higher than that of acidic condition.

Key words: polymeric prodrug, ketoprofen, ibuprofen, naproxen, drug-saccharide conjugate, copolymer