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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.
Three drugs (naproxen, ketoprofen, ibuprofen) and vinyl gluconate succinate (6-O-vinyl succinyl-D-glucose) were synthesized by chemical and enzymatic methods respectively A kind of polymer monomer was prepared by free radical polymerization of two monomers to prepare the polymer precursor with high molecular weight.The structure of the polymer was characterized by IR and NMR.The molecular weight of the copolymer was determined by GPC Studies on in vitro release of sugar polymer prodrugs showed that the drug release time was greatly prolonged after the small molecule prodrugs were prepared as the prodrugs of sugar-containing polymers, and the sustained release was achieved. The drug release studies of three sugar-containing polymers The results showed that the rate of drug release from ketoprofen-containing glycopolymer prodrug was higher than that of drug-release from naproxen-containing glycopolymer prodrug.Studies on the drug release of sugar-containing polymers at different pH showed that, Drug release in alkaline environment is faster, and drug release in acidic environment is slower.