星点设计优化丙酸氟替卡松鼻用温敏凝胶处方并对其体外释放及滞留性进行考察  

Optimization of the formulation of fluticasone propionate thermosensitive in-situ Gel nasal drops by central composite design-response surface methodology and investigation of vitro release retention

作　　者：邓小丽[1] 秦冬梅[1] 陈文[1] 

机构地区：[1]石河子大学药学院,新疆石河子832000

出　　处：《石河子大学学报（自然科学版）》2017年第1期119-123,共5页Journal of Shihezi University(Natural Science)

基　　金：国家自然科学基金项目(81560699)

摘　　要：为优化丙酸氟替卡松温敏型原位凝胶滴鼻剂处方,对其体外释放及滞留性进行考察。以丙酸氟替卡松为主药,泊洛沙姆407(P407)、泊洛沙姆188(P188)为基质,采用冷法制备丙酸氟替卡松鼻用温敏凝胶;以影响制剂胶凝温度的泊洛沙姆P407、P188用量为考察因素,胶凝温度为考察指标进行星点设计优选处方。用Franz扩散池法对体外释放进行考查。结果显示,凝胶基质中以P407为19%、P188为2%时为最优处方,此时胶凝温度为32℃。体外释放符合Higuchi方程。由此可知,丙酸氟替卡松温敏凝胶制备工艺切实可行,且适宜经鼻给药,释放性能良好,作为鼻腔给药剂型有很好的应用前景。To optimize the formulation of thermo-sensitive in situ nasal gel of fluticasone propionate（FP）,and to invsestigate its release and retention behavior in vitro.FP was used as main drug,poloxamer P407 and poloxamer P188 as gel materials.FP thermosensitive gel was prepared by cold solution method.The formulation was optimized by central composite design-response surface methodology.the different amount of P407 and P188,which influenced the gel temperature was used as factors and phase-transition temperature as the index.The release in vitro was examined by Franz diffusion pool method.Results showed the content of poloxamer407 and poloxamer188 was 19% and 4% separately,and gelation temperature was 32℃.The drug release was controlled by gel erosion.The conclusion is that the formula and preparation process of FP nasal thermo-sensitive gel are reasonable and feasible with control quality,which indicate a good slow release effect and retention,and can become a new drug delivery system for treatment of diseases of nasal.It will have a good application prospect.

关 键 词：丙酸氟替卡松 鼻用温敏凝胶 星点设计-响应面法 胶凝温度 

分 类 号：R284.1[医药卫生—中药学]