主链含5-氟尿嘧啶聚酯酰胺的合成及体外释药性能研究

采用N-[2-（氯乙酰氧基）乙基]氯乙酰胺、N-[3-（氯乙酰氧基）丙基]氯乙酰胺和N-[5-（氯乙酰氧基）戊基]氯乙酰胺分别与抗肿瘤药物5-氟尿嘧啶缩聚反应得到3种主链含5-氟尿嘧啶的聚酯酰胺高分子药物，用红外光谱、核磁共振谱、紫外光谱等手段对高分子药物的结构进行了表征，探索了最佳合成工艺条件：反应温度为120℃，反应时间12h，产物的最大产率为86．5％。并研究了其体外释药性能，在水溶液中20h最大释药率为72．6％。对聚合物在人工胃液中的释药性能进行了测试，结果表明酶溶液对聚酯酰胺的释药性能有明显的促进作用．

Synthesis, Characterization and in vitro Release Effect of Polyesteramides Containing 5-fluorouracil in the Main Chain

A series of biodegradable polyesteramides containing 5-fluorouracil in the main chain are prepared by the reaction of N - [ 2- （chloroacetyloxy） ethyl ] chloroacetamide, N - [ 3- （chloroacetyloxy） proyi ] chloroacetamide and N-[ 5-（chloroacetyloxy） pentyl ] chloroacetamide with potassium salt of 5- fluorouracil respectively. The copolymers are characterized by means of FT-IR, ^1H-NMR and UV spectroscopy. The optimum condition of the polycondensation is determined： the reaction tempature is 120℃, reaction time is 12h, the maximum yield of the polyesteramide could reach 86.5%. The drug release in vitro of the copolymers is studied and the influence of solution on the drug release in vitro is investigated, the maximum value of release percentage is 72.6% in 20h. The result of enzyme hydrolysis shows that the enzyme solution has significant promotion to drug release of copolymers .