基于热塑弹性体的辣椒素贴剂的制备及评价  

Preparation and evaluation of capsaicin patch based on thermoplastic elastomer

作　　者：张定[1] 王承潇[1] 韩伟[2] 

机构地区：[1]昆明理工大学生命科学与技术学院,云南昆明650500 [2]华东理工大学药学院,上海200237

出　　处：《中国医院药学杂志》2015年第23期2102-2107,共6页Chinese Journal of Hospital Pharmacy

基　　金：国家自然科学基金(编号:81001651;81303230);江苏省大学生实践创新省级重点项目(编号:201310315029Z)

摘　　要：目的:以热塑弹性体为骨架材料,采用熔融共混法制备贴剂基质,制备辣椒素热熔压敏胶贴剂。方法:用红外光谱和偏振光显微镜考察药物在贴剂基质中的存在状态,同时以国外上市贴剂为对照,采用Franz扩散池考察贴剂中辣椒素的释放和体外透皮特性。以SD大鼠为模型动物,考察贴剂的体内透皮吸收行为。结果:辣椒素药物与热熔压敏胶基质相容性好,但贴剂的稳定性有待进一步提高。药物在两者种贴剂中的释放遵循Higuchi方程。实验室自制热熔胶贴剂的体内外透皮行为与国外市售贴剂相比无显著性差异。结论:热熔胶贴剂基质与皮肤和药物的相容性较好,具有良好的体外-体内透皮相关性。OBJECTIVE Capsaicin patch based on hot-melt pressure sensitive adhesive were prepared by hot-melt methods.METHODS Fourier transform infrared spectroscopy and polarization light microscope were applied to investigate the interactions between drug and matrix.Patch adhesion profile,drug release,in vitro and in vivo penetration profiles were performed by comparing the lab-prepared patch with a commercial product as reference sample.HPLC was applied to performin vivo drug absorption using SD rat as model animals.RESULTS Capsaicin showed a great interaction with the prepared patch matrix,but the stability of the patch could be improved.Drug release profiles from patches followed Higuchi equation.Compared with Commercial patch,Lab-prepared patch possessed the same percutaneous permeability in vitro and in vivo.CONCLUSIONHot-melt pressure sensitive adhesive is suitable for preparation capsaicin patch for its good adhesion properties and good compatibility with drug and skin.It showed a well skin permeation ability without significant differences when comparing with commercial products.

关 键 词：热塑弹性体 辣椒素 药物释放 透皮吸收 药动学 

分 类 号：R966[医药卫生—药理学]