【摘要】 以壳聚糖为载体 ,戊二醛为交联剂 ,以span 80和硬脂酸镁为复合乳化剂 ,真空泵油和石蜡油相混合为油相 ,通过乳液 化学交联法制备了 5 氟尿嘧啶壳聚糖微球 ,所得微球的药物包封率可达 43 6%～ 84 8% ,比文献报道的 (约 1 5 1 % )高 2～ 4倍。在Na2 HPO4 KH2 PO4缓冲溶液 (pH =7 4)和柠檬酸钠 盐酸缓冲溶液 (pH=3 9)中进行的药物释放实验表明 ,5 氟尿嘧啶与壳聚糖的质量投料比 ,戊二醛用量及释药介质的pH值均对微球的释药速率产生影响 :随着m( 5 Fu) /m(CS)比的减小 ,微球的释药速率减慢 ;随着n(CHO) /n(NH2 )比的增大 ,微球的释药速率减慢 ;在酸性条件下的缓释效果更好。IR和SEM对微球进行的结构表征和形态观察表明 ,壳聚糖与 5 氟尿嘧啶之间有比较强的分子间作用力 ,微球球形规整 ,分散性好 ,粒径分布在 1～ 5 μm之间。更多还原

【Abstract】 Fluorouracil(5-Fu) chitosan(CS) microspheres were prepared in emulsion by using glutaradelhyde as cross-linking agent, span-80 and magnesium stearate mixture as emulsifer and vacuum-pump oil-paraffin oil mixture as oil phase. 5-Fu encapsulated capacity was of 43.6%～84.8%, one to several times higher than that reported in literatures(about 15.1%). Drug releasing property of 5-Fu/CS capsules was studied in the phosphate buffer(pH=7.4) and citrate buffer(pH=3.9) solutions. The results showed that m(5-Fu)/ m(CS), amount of cross-linking agent and the pH value of media all affected the releasing of 5-Fu from microspheres. The drug releasing rate was found decreased with m(5-Fu)/m(CS) and increased with n(CHO)/n(NH 2). The drug releasing performance was better in the acid media than in the alkali one. The IR results indicated there was a strong molecular interaction between 5-Fu and chitosan. SEM images show the 5-Fu-CS microspheres are spherical shape with diameters ranged from 1～5 μm.更多还原