目的 制备并优化芷芎散鼻用温敏凝胶的处方，并考察其体外释放机制和鼻黏膜渗透特性。方法 利用星点设计-效应面法优化泊洛沙姆温敏凝胶基质处方，然后经Franz扩散池法考察欧前胡素、阿魏酸的体外释放机制及其离体家兔鼻黏膜渗透特性。结果 最优处方为泊洛沙姆407（P407）20%、泊洛沙姆188（P188）6.5%，欧前胡素接近零级释放模型，阿魏酸接近Higuchi模型，处方对欧前胡素和阿魏酸的透过鼻黏膜均具有促进作用。结论 优化所得的处方为芷芎散新给药途径制剂的开发提供基础。

Objective To prepare and optimize the formulation of intranasal thermo-sensitive gel of Zhi Xiong San and to evaluate its in vitro release mechanism and nasal mucosa permeability. Methods The formulations of poloxamer thermo-sensitive gel were optimized by a central composite design-response surface method and its in vitro release mechanism and nasal mucosa permeability were evaluated by Franz diffusion chambers. Results The optimal formulation was Poloxamer 407 (P407) 20% and Poloxamer 188 (P188) 6.5%. Imperatorin was released from the thermo-sensitive gels approximately with a zero-order mechanism, while ferulic acid with a Higuchi model. The formulation demonstrated the enhancement of nasal mucosa permeability. Conclusion The optimal formulation provides a basis for the development of new administration routes and dosage forms of Zhi Xiong San.

广东省科技计划项目（2010B030700009024）