摘要
目的:研究辣椒碱亚微乳注射剂的处方以及制备工艺,并对其质量进行评价。方法:以静脉注射用中链脂肪酸三甘油酯为油相,大豆磷脂和泊洛沙姆F68为复合乳化剂,采用高压均质法制备辣椒碱亚微乳。以粒径为指标,在单因素试验基础上采用正交设计法优化处方。结果:筛选辣椒碱亚微乳处方为辣椒碱∶中链脂肪酸三甘油酯∶豆磷脂∶泊洛沙姆F68∶无水乙醇∶油酸钠(0.02∶0.5∶1.5∶0.2∶0.75∶0.1)。所制得亚微乳平均粒径128.2 nm,多分散系数0.219,粒度分布均匀,表面电位-69.94 mV;包封率84.38%,加速试验结果表明,稳定性良好。结论:本实验获得辣椒碱亚微乳符合亚微乳注射剂主要指标要求,为进一步开发其应用奠定基础。
Objective: To investigate the prescription and preparation of capsaicin submicron emulsion, and evaluate its quality. Methods: The prescription composition and the ratio of capsaicin submicron emulsion in- cluding medium-chain triglyceride (MCT), soybean phospholipid and poloxamer F68 were selected. Capsaicin submicron emulsion was prepared according to high pressure homogenization, and the prescription was optimized with the orthogonal test on basis of single factor experiment using particle size as selection index. Results: The se- lected prescription was capsaicin: MCT: soybean phospholipid: poloxamer F68: absolute alcohol: sodium oleate =- 0.02: 0.5: 1.5: 0.2: 0.75: 0.1. The submicron emulsion was well-distributed with the mean particle size of 128.2 nm, the polydispersity index of 0. 219 and the zeta potential of -69.94 mV. The mean entrapment efficiency was up to 84.38%. The result of accelerated test indicated that the stability of capsaicin submicron emulsion was well. Conclusion: The preparation obtained in this study is consistent with the main index of submicron emulsion injec- tion, offering the basis for further research of capsaicin.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2013年第16期1956-1961,共6页
Chinese Journal of New Drugs
关键词
辣椒碱
亚微乳
正交试验
粒径
包封率
capsaicin
submicron emulsion
orthogonal test
particle size
entrapment efficiency