新型负载5-氨基水杨酸微胶囊的制备及其载药效果

采用锐孔/聚合法制备了平均粒径为1.89 mm、负载5-氨基水杨酸(5-ASA)的纤维素硫酸钠(NaCS)-壳聚糖微胶囊，采用Box-Behnken响应面法进行实验设计和分析，考察了内、外水相pH值和NaCS浓度、多聚磷酸钠(PPS)浓度对微胶囊载药量和包封率的影响. 结果表明，内水相pH值对负载5-ASA微胶囊的载药量和包封率起关键作用. 最佳制备条件为内水相pH 4.25，外水相pH 6.0，NaCS浓度14 g/L, PPS浓度5 g/L，该条件下所制微胶囊最大载药量为59.02%，最大包封率为89.96%..

Preparation of Novel Microcapsules Loading 5-Aminosalicylic Acid and Their Loading and Encapsulation Efficiency

The microcapsules loading 5-aminosalicylic acid (5-ASA) were prepared with sodium cellulose sulfate (NaCS) and chitosan via orifice-polymerization method, and their average diameter was 1.89 mm. The effects of pH values of inner water and outer water phases, concentrations of NaCS and sodium polyphosphate (PPS) on the drug loading rate and encapsulation rate of microcapsules were mainly investigated. Box-Behnken method was used to design the experiments. The results showed that the pH value of inner water phase played a key role to the drug loading and encapsulation rates of microcapsules. The optimal conditions were pH values of inner and outer phases 4.25 and 6.0, concentrations of NaCS and PPS 14 and 5 g/L, the drug loading and encapsulation rates of microcapsules were 59.02% and 89.96%, respectively.