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目的研制适合眼部用药的辅酶Q10微乳制剂。方法以溶解度、乳化效率及伪三元相图法筛选最佳油相、乳化剂及助乳化剂;以星点设计-效应面法及制备工艺的单因素考察,优化处方和工艺;并进行了辅酶Q10微乳制剂在角膜的滞留时间,辅酶Q10眼用微乳的稳定性初步评价以及家兔眼部刺激性实验的考察。结果经处方筛选和星点效应面法优化得出最佳处方为:MCT,Cremophor EL,Capmul MCM C8 EP分别为油相,乳化剂和助乳化剂,比例为3∶5∶2,药用浓度为10 mg·mL 1;乳化温度和时间对粒径没有明显影响;高温、强光考察10 d,粒径、pH值和含量均有明显变化,低温保存各指标没有变化明显;辅酶Q10微乳在家兔角膜滞留可达2 h;刺激性实验显示该制剂对家兔眼部无刺激性。结论该处方及工艺筛选、优化法简便可行,容易控制,制备的眼用微乳可延长在角膜的滞留时间,安全无刺激,低温避光保存稳定,适合眼部用药。
Objective To develop a coenzyme Q10 microemulsion suitable for ophthalmic administration. Methods The optimal oil phase, emulsifier and co-emulsifier were screened by solubility, emulsification efficiency and pseudo-ternary phase diagram method. The formulation and process were optimized by single point factor-design-response surface method and preparation process. Coenzyme Q10 microemulsion in the cornea residence time, the stability of coenzyme Q10 ophthalmic microemulsion initial evaluation and eye irritation experiments in rabbits. Results The optimal prescriptions were obtained through prescription screening and star-spot effect surface method. The optimum prescriptions were as follows: MCT, Cremophor EL, Capmul MCM C8 EP respectively oil phase, emulsifier and co-emulsifier in the ratio of 3: 5: 10 mg · mL -1. The temperature and time of emulsification had no significant effect on the particle size. At 10 days after high temperature and light exposure, the particle size, pH value and content all changed obviously, In rabbit cornea retention up to 2 h; irritation experiments showed that the preparation of rabbits eye irritation. Conclusion The prescription and process screening, optimization method is simple and feasible, easy to control, the preparation of ophthalmic microemulsion can extend the residence time in the cornea, safe and non-stimulated, low temperature and light preservation and stability, suitable for eye medication.