响应曲面法优化NSC/APT凝胶小球的制备工艺及其释药特性考察  

Optimization of the preparation of N-Succinyl chitosan / attapulgite com- posite hydrogel beads with response surface methodology and their drug release property

作　　者：杨会霞[1,2] 郑易安[1] 张俊平[1] 王爱勤[1] 

机构地区：[1]中国科学院兰州化学物理研究所,兰州730000 [2]清华大学第二附属医院,北京100049

出　　处：《海峡药学》2013年第12期37-41,共5页Strait Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(51003112)

摘　　要：目的探索N-琥珀酰壳聚糖/凹凸棒黏土(NSC/APT)释药凝胶小球的制备工艺,考察其释药特性。方法利用响应曲面法优化了制备工艺,采用安全无毒的氯化钙进行交联。结果与结论通过响应曲面法优化的最佳工艺与模型拟合很好;所得凝胶小球的溶胀率和累积药物释放实验结果表明复合凝胶小球具有pH敏感性,在pH为1.2时基本不溶胀,3h药物仅释放0.66%;pH为5.8时溶胀率增加,3h药物累积释放达到62.55%;pH为6.8时溶胀率最大,药物释放速度最快,3h达到94.51%;但当pH增加至8.0时,溶胀率减小,3h释放了76.05%。琥珀酰壳聚糖的羧基在药物释放中起着关键作用。OBJECTIVE To explore the preparation method of N-succinyl-chitosan/attapulgite （NSC/APT） hydrogel composite beads and investigate their drug release properties. METHODS The hydrogel composite beads were prepared using CaCl2 as the crosslinker according to the response surface methodology （RSM）, RESULTS ＆ CONCLUSION The best preparation method optimized by RSM is fitted with the model very well. The swelling of the NSC/APT beads and the drug release are pH dependent. At pH 1.2 ,no swelling was observed and only 0. 66% of the model drug was released in 3h. Increasing pH to 5.8, an obvious swelling of the beads was observed and 62. 55% of the drug was released in 3h. Further increasing pH to 6. 8 ,the beads have the highest swelling ratio and drug release rate （94. 51% in 3h）. However,the swelling ratio and drug release rate （76. 05% in 3h） were decreased in pH 8.0 solution. -COOH of NSC plays an important role in turning the drug release behaviors.

关 键 词：响应曲面法 N-琥珀酰壳聚糖 凹凸棒黏土 凝胶小球 PH敏感性 药物释放 

分 类 号：TQ460.4[化学工程—制药化工]