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

Acta Chimica Sinica ›› 2011, Vol. 69 ›› Issue (07): 843-847. Previous Articles Next Articles

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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

(¹Donghua University, Chemical Engineering and Biotechnology, Shanghai 201620)
(²Department of Chemistry, Zhengzhou Normal University, Zhengzhou 450016)

Received:2009-09-11 Revised:2010-10-10 Published:2010-12-10

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

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WU Cheng-Yao, XIE Jian-Gang, QUAN Jing, ZHU Li-Min. Preparation and Sustained-release of Polymeric Drug-glucose Conjugates with NSAIDs Pendants[J]. Acta Chimica Sinica, 2011, 69(07): 843-847.

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非甾体类药物含糖乙烯醇酯共聚物制备及药物释放研究

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

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