混料设计法优化单硝酸异山梨酯缓释片处方

Formulation Optimization of Isosorbide Mononitrate Sustained-release Tablets by Mixture Design

目的:评价混料设计法在处方设计中的应用。方法:以单硝酸异山梨酯(ISMN)为模型药物,运用混料设计法优化ISMN缓释片的处方,并与市售ISMN缓释片进行体外释放度的比较。结果:采用混料设计法优化后处方制备的样品其验证值与目标值比较,相似度因子f2达到86.56。且样品体外释放度与市售片比较无差异。结论:混料设计法适合用于处方的优化,并能预测药物的体外释放。

OBJECTIVE： To evaluate the application of mixture design in the design of formulation. METHODS： Isosorbide mononitrate （ISMN） was used as model drug, and the formulation of ISMN sustained- release tablet was optimized by the mixture design. The optimized ISMN sustained - release tablets were compared with the ISMN sustained - release tablets in market in respect of the release rate in vitro. RESULTS： The comparison between the validating value and the target value of the optimized sample showed a similarity factor（f2） of 86.56, and there were no differences between the optimized sample and that in market in respect of the drug release in vitro. CONCLUSION： The mixture design is applicable for the optimization of formulation and it can be used to predict the drug release in vitro.