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高分子前药可以有效控制药物的释放速率,在药物后期性能改善方面发挥重要作用。本研究以酮洛芬为药物模型,利用化学法合成酮洛芬乙烯酯单体,再通过自由基聚合制备具有较高分子量的聚合物前药。为改善酮洛芬高分子前药的缓释行为,在酮洛芬高分子前药中加入亲水性聚乙烯吡咯烷酮进行高压静电喷雾,制备酮洛芬高分子前药的聚合物微球。用FT-IR、NMR、SEM、XRD对前药聚合物的结构和形貌进行表征。结果表明,酮洛芬前药以无定形态形式分布于聚乙烯吡咯烷酮中。电喷法制得的前药聚合物微球的平均粒径约200~400nm。酮洛芬聚合物纳米微球载药量(w/w)为20%,2h内释放的药物总量占总体的48.1%,具有良好的缓释性能。
Polymer prodrugs can effectively control the release rate of drugs and play an important role in the improvement of drug performance later. In this study, ketoprofen as a drug model, the chemical synthesis of ketoprofen vinyl ester monomer, and then prepared by free radical polymerization of higher molecular weight polymer prodrugs. In order to improve the sustained-release behavior of ketoprofen prodrugs, a hydrophilic polyvinylpyrrolidone was added to the ketoprofen prodrugs for electrostatic spraying at high pressure to prepare polymer microspheres of ketoprofen prodrugs. The structure and morphology of the prodrugs were characterized by FT-IR, NMR, SEM and XRD. The results showed that ketoprofen prodrugs were distributed in amorphous form in polyvinylpyrrolidone. The average particle size of the prodrug polymer microspheres prepared by electrospray method is about 200-400 nm. The drug loading of ketoprofen polymer microspheres (w / w) was 20%, and the total amount of drug released in 2h accounted for 48.1% of the total, with good sustained-release properties.