摘要
目的优选艳山姜Alpiniae zerumbet挥发油自乳化释药系统(EOFAZ-SEDDS)的处方,并对其药剂学性质进行评价。方法通过伪三元相图的绘制,以乳化区域面积为指标,筛选处方中乳化剂、助乳化剂、乳化剂与助乳化剂比例(Km),确定最佳处方,并对EOFAZ-SEDDS的外观、粒径、自乳化效率以及稳定性进行评价。结果所得艳山姜挥发油自乳化传递系统的处方为艳山姜挥发油(60%)、Kolliphor HS 15(20%)、无水乙醇(20%)。所得EOFAZ-SEDDS外观为淡黄色澄明液体,加水稀释后可形成乳白色并带淡蓝色乳光的乳液,于透射电子显微镜(TEM)下观察呈球形,分布均匀,粒径为(171.67±7.64)nm,Zeta电位为(-11.51±1.22)m V。EOFAZ-SEDDS在盐酸(0.1 mol/L)中自乳化时间最短。随着介质体积的增加,自乳化时间延长。EOFAZ-SEDDS自乳化后24 h内均未见有沉淀产生和分层现象,且离心30 min仍未发生分层。结论研究考察所得最佳处方制备的EOFAZ-SEDDS粒径适宜,稳定性良好。
Objective To optimize the formulation of essential oil of Alpiniae zerumbet self-emulsifying drug delivery system(EOFAZ-SEDDS) and evaluate its pharmacological properties. Methods The emulsifiers, co-emulsifiers and ratio of emulsifier to co-emulsifier(Km) were selected through the pseudo-ternary phase diagram method, using emulsified area as selection index, and determine the optimal prescription. The appearance, particle diameter, self-emulsification efficiency, and stability were evaluated. Results The optimal SEDDS was composed of volatile oil(60%), Kolliphor HS 15(20%), and anhydrous ethanol(20%). The appearance of EOFAZ-SEDDS was translucent diluted-yellow solution. EOFAZ-SEDDS diluted with water to form milky and pale blue emulsion with a particle size of(171.67 ± 7.64) nm and Zeta potential of(-11.51 ± 1.22) m V. The emulsion was observed to be spherical by transmission electron microscopy and distributed evenly. The self-emulsifying time of EOFAZ-SEDDS in hydrochloric acid(0.1 mol/L) was short. With the increase of the volume of medium, the self-emulsifying time was prolonged. The precipitation and delamination of EOFAZ-SEDDS were not observed within 24 h after self-emulsifying, and no stratification was observed after 30 min centrifugation. Conclusion The EOFAZ-SEDDS prepared by optimum formulationthe of this study has a good particle size and good stability.
出处
《中草药》
CAS
CSCD
北大核心
2017年第19期3970-3976,共7页
Chinese Traditional and Herbal Drugs
基金
国家自然科学基金资助项目(81760725,81360650)
筑科合同[20151001]药07号
贵州省留学人员科技活动项目经费(黔人项目资助合同[2013]02号)
贵州省科技合作项目(黔科合LH字[2016]7368)
贵州省高等教育科技创新团队(黔教合人才团队字[2014]31)
贵州省科技创新创新团队(黔科合人才团队[2015]4025号)
贵州省高层次创新型人才百层次人才(贵州科技厅黔科合人才[2015]4029号)
贵州省教育厅拔尖人才计划(黔教合KY2016[073])
关键词
艳山姜挥发油
自乳化药物传递系统
伪三元相图
稳定性
自乳化效率
essential oil of Alpiniae zerumbet (Pers.) Burttet Smith
self-emulsifying drug delivery system
pseudo ternary phase diagram
stability
self-emulsifying efficiency