加味佛手散主要成分同步缓释滴丸的处方筛选与性质表征  

Prescription and characteristics of the synchronized and sustained dropping pills of the multiple components from Jiawei Foshou San

作　　者：彭春梅[1] 张宇[1] 唐勤[1] 徐晓玉[1,2] 张继芬[1] 

机构地区：[1]西南大学药学院,重庆400716 [2]重庆市药效评价工程技术中心,重庆400716

出　　处：《中国新药杂志》2013年第14期1632-1637,1683,共7页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2010ZX09401-306-3-16);西南大学"国家大学生创新性实验计划"项目(1010635);西南大学基本科研业务费专项基金(XDJK 2009 C084)

摘　　要：目的:研究实现加味佛手散3种主要成分同步缓释的滴丸处方,探索药物性质和辅料对同步释药的影响和滴丸的缓释机制。方法:采用熔融法制备滴丸,比较不同类型的基质对阿魏酸、川芎嗪、延胡索乙素3种组分体外释放的影响,探讨同步释药机制。结果:不同基质对体外释放的影响与药物溶解度、酸碱性有明显关系。优化的滴丸在模拟胃肠道环境下,阿魏酸与川芎嗪、阿魏酸与延胡索乙素、川芎嗪与延胡索乙素的f2值分别为53.37,56.17和57.85。药物以非晶型态分散在载体中,载体与药物组分间无化学作用,释药机制为骨架孔道形成-药物溶解-药物扩散。结论:基于固体分散技术的缓释滴丸可实现加味佛手散3种主要成分的体外同步缓释,药物溶解性对缓释辅料选择有重要影响。Objective： To establish synchronized and sustained release dropping pills of the multiple components from Jiawei Foshou San,and explore the effects of both drug properties and excipients on release and the mechanism.Methods： The dropping pills with different kinds of excipients were respectively prepared through a melt fusion method.The release profiles of the components（ferulic acid,ligustrazine and tetrahydropulmatine） were compared.The structure and characterization of dropping pills were investigated by DSC,SEM and IR.Results： The effects of different excipients on the in vitro release were significantly related to drug solubility and acidbase properties.Under the simulated gastrointestinal pH conditions,the value of similarity factor（f2） of ferulic acid and ligustrazine,ferulic acid and tetrahydropulmatine,ligustrazine and tetrahydropulmatine was 53.37,56.17 and 57.85,respectively.The compounds were distributed in matrix in amorphous form.Moreover,there were no chemical action between compounds and matrix.The mechanism of drug release was the formation of porous channel in skeleton-drug dissolvation-drug diffusion.Conclusion： The sustained-release dropping pills based on solid dispersion technology can achieve synchronized and sustained release of the multiple components from Jawei Foshou San.The solution of components has a great effect on the selection of sustained excipients.

关 键 词：同步缓释 滴丸 加味佛手散 阿魏酸 川芎嗪 延胡索乙素 子宫内膜异位症 

分 类 号：R943.41[医药卫生—药剂学]