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星点设计-效应面法优化芷芎散温敏凝胶的处方及其鼻黏膜渗透特性研究
引用本文:卢浩扬,林媛媛,车俊秀,曾维东,陈宝,吴传斌,徐月红. 星点设计-效应面法优化芷芎散温敏凝胶的处方及其鼻黏膜渗透特性研究[J]. 中草药, 2014, 45(13): 1845-1849
作者姓名:卢浩扬  林媛媛  车俊秀  曾维东  陈宝  吴传斌  徐月红
作者单位:中山大学药学院, 广东 广州 510006;中山大学药学院, 广东 广州 510006;中山大学药学院, 广东 广州 510006;中山大学药学院, 广东 广州 510006;中山大学药学院, 广东 广州 510006;中山大学药学院, 广东 广州 510006;中山大学药学院, 广东 广州 510006
基金项目:广东省科技计划项目(2010B030700009024)
摘    要: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。

关 键 词:白芷  川芎  泊洛沙姆  温敏凝胶  体外释放  鼻黏膜渗透性
收稿时间:2014-01-19

Optimization for formulation of Zhi Xiong San thermo-sensitive gel by central composite design-response surface method and study on characterization of its nasal mucosal permeability
LU Hao-yang,LIN Yuan-yuan,CHE Jun-xiu,ZENG Wei-dong,CHEN Bao,WU Chuan-bin and XU Yue-hong. Optimization for formulation of Zhi Xiong San thermo-sensitive gel by central composite design-response surface method and study on characterization of its nasal mucosal permeability[J]. Chinese Traditional and Herbal Drugs, 2014, 45(13): 1845-1849
Authors:LU Hao-yang  LIN Yuan-yuan  CHE Jun-xiu  ZENG Wei-dong  CHEN Bao  WU Chuan-bin  XU Yue-hong
Affiliation:School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China;School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China;School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China;School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China;School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China;School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China;School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China
Abstract: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.
Keywords:Angelicae Dahuricae Radix  Chuanxiong Rhizoma  Poloxamer  thermo-sensitive gel  in vitro release  nasal mucosal permeability
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