星点设计-效应面法优化及制备安妥沙星眼用温度敏感原位凝胶  

The preparation of thermosensitive in situ gel system containing antofloxacin for ocular use by the optimization of central composite design-response surface methodology

作　　者：孙思雨[1] 马涛[1] 王清清[1] 

机构地区：[1]蚌埠医学院药学系,安徽蚌埠233030

出　　处：《蚌埠医学院学报》2013年第7期869-872,共4页Journal of Bengbu Medical College

基　　金：安徽省高等学校省级自然科学研究资助项目(KJ2011Z250)

摘　　要：目的:探讨星点设计-效应面法优化安妥沙星眼用温度敏感原位凝胶处方。方法:以泊洛沙姆407与泊洛沙姆188为材料,以模拟泪液稀释前后的溶液-凝胶相转变温度为考察指标,采用二项式模型描述各因素与指标间的数学关系,根据二项式模型绘制效应面图及等高线图,通过重叠等高线图确定优化处方并进行验证。结果:安妥沙星眼用温度敏感原位凝胶优化后的处方为22.5%泊洛沙姆407与1.0%泊洛沙姆188;优化处方在室温下是自由流动的液体,经泪液稀释后能发生相转变形成凝胶。结论:安妥沙星眼用温度敏感原位凝胶符合眼部用药要求,具有实际的临床意义和应用价值。Objective： To optimize the thermosensitive in situ gel system containing antofloxacin for ocular use by the central composite design-response surface methodology. Methods：The in situ thermosensitive gel system containing antofloxacin was prepared with Poloxamer 407 and Poloxamer 188. The phase transition temperature of the solution-gel before and after the STF dilution was used as index. The mathematic relation of the factors and indicators, effective surface figure and contour map were described using binomial model. The formulation was optimized and validated by superimposed contour plot. Results： Optimized formulation of in situ thermosensitive gel system containing antofloxacin for ocular use consisted of 22.5% of Poloxamer 407 and 1.0% of Poloxamer 188, which was a flee-flowing liquid at room temperature and converted to firm gel after STF dilution. Conclusions：The thermosensitive in situ gel system containing antofloxacin hydrochloride satisfied the requirement of ophthalmic application, which has clinical significance and application value.

关 键 词：盐酸安妥沙星 星点设计-效应面法 泊洛沙姆 原位凝胶 

分 类 号：R944.1[医药卫生—药剂学]