尼非韦罗微乳热敏原位凝胶的稳定性和流变性考察  

Stability and rheological characteristics of nifeviroc-loaded microemulsion thermosensitive in situ gel

作　　者：田芳[1] 温成丽[1,2] 王玉柱[1] 夏敏杰[1] 杨凯 李卫华[1] 丁训诚[1] 

机构地区：[1]上海市计划生育科学研究所国家计划生育药具重点实验室,上海200032 [2]复旦大学公共卫生学院,上海200032 [3]英国马尔文仪器有限公司,上海200233

出　　处：《中国新药杂志》2014年第9期1019-1023,共5页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2012ZX10001007-009-003;2013ZX10001006-003-002);十二五国家科技支撑计划(2012BAI31B04);国家自然科学基金青年基金(81100459);上海市科委项目(11PJ1408400;11140902900);上海市人口和计划生育委员会(2012JG03)

摘　　要：目的：研究Nifeviroc微乳热敏原位凝胶（NFVR／ME-TISG）的稳定性和流变性。方法：通过稳定性试验，考察凝胶在d5和d10的外观性状、pH值、粒径和Zeta电位有无变化；高级流变仪检测在10～45℃内，凝胶的弹性模量G′,黏性模量G″和相位角δ的变化及变化特征。结果：稳定性试验显示，在d5和d10的凝胶外观性状、pH值、粒径和Zeta电位无明显变化；流变仪测其相转变温度为30℃；在低温（〈25℃）时为牛顿流体，黏度很小；随着温度升高（30和35℃）时，黏弹性模量升高，相角较低，不随频率增加而改变，表现出典型的假塑性流体特征。结论：NFVR／ME-TISG稳定性较好，具有随温度改变黏弹性流变力学特点。Objectives：To characterize the stability and rheological properties of nifeviroc-loaded microe- mulsion thermosensitive in situ gel （ NFVR/ME-TISG）. Methods ： To detect the changes of gel＇s appearance, pH value,partical size and Zata potentials in the fifth days and the tenth days, stability experiment were conducted. Rheological parameters of NFVR/ME-TISG were measured during phase transition at different temperature to evalu- ate rheological characteristics. Results：Stability experiment shows that there is no difference in the fifth days and the tenth days in the gel＇s appearance, pH value,partical size and Zata potentials. The sol-gel transition temperature （Ts-g） is 30 ℃ detected by rotational rheometer. The poloxamer solution below Ts-g（ 〈 25 ℃ ）shows Newtonian fluid characteristics with comparatively low viscosity;with the increase of temperature, viscoelastic modulus rose, phase angle drooped, but there is no obvious change when the frequency increased, it shows characteristics of the pseudoplastic fluid. Conclusion：NFVR/ME-TISG has a desirable stability and will change its viscoelastic modulus as the tempetature changes.

关 键 词：尼非韦罗 微乳 热敏原位凝胶 稳定性 流变特性 

分 类 号：R943[医药卫生—药剂学] R978.7[医药卫生—药学]