中心复合设计法优化盐酸左氧氟沙星缓释片处方

目的:采用中心复合设计法预测盐酸左氧氟沙星缓释片的最优处方。方法:选用羟丙基甲基纤维素和乙基纤维素为骨架材料制备盐酸左氧氟沙星缓释片。采用中心复合设计法,选择体外累积释放百分率为考察指标,对羟丙基甲基纤维素和乙基纤维素用量2个考察因素自变量进行多元线性回归和二项式拟合,对缓释片的最优处方进行预测,并分析缓释片的释药机制。结果:经预测分析,获得最优处方。通过相似因子法比较显示,由此优化处方所制缓释片释放度实测值与预测值基本相符。缓释片体外释药符合一级动力学特征,释药机制为非Fick-ian扩散。结论:中心复合设计法预测性良好,可用于优化处方。

Optimization of Levofloxacin Hydrochloride Sustained-release Tablets by Central Composite Design

Objective: To predict the optimal formulation of levofloxacin hydrochloride sustained-release tablets by Central Composite Design.Methods: HPMC and EC were used to prepare levofloxacin hydrochloride sustained-release tablets as matrix materials.Using the in vitro accumulative dissolution at different sampling time as the evaluation index and the amounts of HPMC and EC as the independent variables,the optimal formulation of the sustained-release tablets was predicted via multiple linear regression and binomial fitting by Central Composite Design.And their dissolution mechanism was analyzed.Results: The measured dissolution of the optimal formulation appeared to essentially agree with the predicted dissolution seen by f2 test.The in vitro dissolution of the sustainedrelease tablets followed first order kinetics,of which the mechanism was non-Fickian diffusion.Conclusion: Central Composite Design has a good predictability and could be used to optimize the formulation.