氟比洛芬酯脂质体滴眼液处方的优化与评价

Optimization of formulation of flurbiprofen axetil liposome eye drops and evaluation of its ocular safety

目的优化氟比洛芬酯脂质体滴眼液处方并评价其局部应用的安全性。方法采用三因素三水平的Box-Behnken设计,对影响氟比洛芬酯脂质体包封率和平均粒径的三个主要因素进行研究;并采用Buehler和Draize试验评价优化得到的处方。结果最优处方F-68、Lipoid E80和CHOL用量质量分数分别为15. 9%、72. 4%和0. 8%,实测包封率为90. 5%,平均粒径为103. 1 nm;优化后的处方未引起过敏反应且无刺激性。结论 Box-Behnken设计优化的氟比洛芬酯脂质体滴眼液处方可行。

Objective To optimize the formulation parameters of flurbiprofen axetil( FBA) liposome eye drops and evaluate the ocular safety of this formulation. Methods A three-factor,three-level Box-Behnken experimental design was employed,with the molar rate of F-68( X1),lipoid E80( X2) and CHOL( X3) as the independent variables. The optimized formulation was evaluated using Buehler and Draize test. Results The optimization formulation was as follows: under X1,X2 and X3 levels of 15. 9%,72. 4% and 0. 8%,the encapsulation efficiency was 90. 5%,and the average particle size was 103. 1 nm respectively. The formulation had no allergy and non-irritant. Conclusion The observed responses are in close agreement with the predicted values of the mathematic models,and the Box-Behnken design is suitable for optimizing the formulation of flurbiprofen axetil liposome eye drops.