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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 study the prescription of dripping pills for simultaneous release of three main components of flavored bergamot powder, to explore the influence of drug properties and excipients on synchronous drug release and the slow release mechanism of drip pills. Methods: Droplets were prepared by melt method. The effects of different types of matrix on the in vitro release of three components of ferulic acid, ligustrazine and tetrahydropalmatine were compared. The mechanism of simultaneous drug release was discussed. Results: The influence of different matrix on drug release and acidity and alkalinity were obviously related. In the simulated gastrointestinal tract, f2 values of ferulic acid and ligustrazine, ferulic acid and tetrahydropalmatine, ligustrazine and tetrahydropalmatine were 53.37, 56.17 and 57.85, respectively. The drug is dispersed in the carrier in an amorphous form, and there is no chemical interaction between the carrier and the drug components. The drug release mechanism is the formation of framework pores - drug dissolution - drug diffusion. CONCLUSION: The sustained-release drip pills based on solid dispersion technology can achieve simultaneous in vitro release of three main components of flavored bergamot. The drug solubility has an important influence on the selection of sustained-release excipients.