半乳糖酰化壳聚糖衍生物包复的5-氟尿嘧啶白蛋白微球的制备  

Preparation of 5-Fluorouracil Albumin Microsphere Coated by N-Galactosylated Chitosan Derivative

作　　者：程耀[1] 张灿[2] 平其能[1] 熊净[1] 

机构地区：[1]中国药科大学药剂学教研室 [2]中国药科大学新药研究中心,南京210009

出　　处：《中国药科大学学报》2004年第6期517-520,共4页Journal of China Pharmaceutical University

摘　　要：目的制备肝靶向的半乳糖酰化壳聚糖衍生物包复的5氟尿嘧啶白蛋白微球。方法采用乳化交联固化法制备了5氟尿嘧啶白蛋白微球,分别以均匀设计和单因素处方分析优化了该制备工艺,然后在其表面通过静电作用力包裹壳聚糖衍生物,采用正交实验设计确定最佳包裹条件,得到壳聚糖衍生物包复的5氟尿嘧啶白蛋白微球。结果优化后的制备条件为5氟尿嘧啶浓度10μg/ml,w/o体积比1/20,戊二醛加入量10ml/100mg牛血清白蛋白,固化时间4h,衍生物包复时包裹时间10min,衍生物浓度2%,冰醋酸浓度2%。结论本法简便、易操作,实验设计方案经济有效。AIM:To prepare 5-fluorouracil albumin microspheres coated by N-galactosylated chitosan derivative for liver targeting. METHOD:First,fluorouracil bovine serum albumin microspheres were prepared by emulsion-crosslinking stabilization technique,and were optimized by the uniform design and single factor optimization,then the microspheres were coated chitosan derivative,orthogonal experiment design was used to get the optimum coated condition. RESULT:The preparation procedure after optimization is:5-Fu 10.0 mg/ml,w/o=1/20,glutaraldehyde 1.0 ml,cross-linking time 4 h,the concentrations of derivative and acetic acid both are 2% and coating time is 10 min. CONCLUSION:The preparation procedure is good and simple;the experiment design is economical and effective.

关 键 词：5-氟尿嘧啶 微球 白蛋白 半乳糖酰化壳聚糖衍生物 包裹 

分 类 号：R943[医药卫生—药剂学]