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目的合成具有p H敏感特性的聚N-(2-羟丙基)甲基丙烯酰胺(HPMA)负载地塞米松(Dex)的前药。方法以双甘氨肽(Gly-Gly-OH)为连接臂,将Dex与HPMA共价连接,再经聚合反应形成高分子地塞米松前药(P-Dex)。考察其水溶性,通过核磁共振表征其结构,酸水解后HPLC法测定Dex的含量。考察P-Dex在p H5、p H7.4的释药特性。结果合成的P-Dex改善了Dex的水溶性,P-Dex中Dex的含量为4.59%。P-Dex在p H7.4缓冲体系中几乎不释放Dex,在p H5的缓冲体系中,每天约释放0.86%Dex。结论合成的P-Dex增强了Dex的水溶性,具有p H敏感释放的特点。
OBJECTIVE To synthesize poly-N- (2-hydroxypropyl) methacrylamide (HPMA) loaded dexamethasone (Dex) prodrug with p H-sensitive properties. Methods Dex was covalently linked to HPMA with Gly-Gly-OH as the linker and then polymerized to form the dexamethasone prodrug (P-Dex). The water solubility was investigated. The structure was characterized by 1H NMR. The content of Dex was determined by HPLC after acid hydrolysis. The release characteristics of P-Dex at p H5 and p H7.4 were investigated. Results The synthetic P-Dex improved the water-solubility of Dex, with a Dex content of 4.59% in P-Dex. P-Dex almost does not release Dex in the p H7.4 buffer system, and about 0.86% Dex is released per day in the p H5 buffer system. Conclusion The synthesized P-Dex enhanced the water-solubility of Dex and possessed the characteristics of sensitive release of p H.