固体分散体相图的理论预测。
Theoretical prediction of a phase diagram for solid dispersions.
作者信息
Tian Bin, Wang Xiaoyan, Zhang Yuanyuan, Zhang Keru, Zhang Yu, Tang Xing
机构信息
Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang, 110016, Liaoning Province, People's Republic of China.
出版信息
Pharm Res. 2015 Mar;32(3):840-51. doi: 10.1007/s11095-014-1500-6. Epub 2014 Aug 28.
PURPOSE
To predict the temperature-composition phase diagram of solid dispersions (SDs) through theoretical approaches using cinnarizine-Soluplus(®) SD as a model system and evaluate the predicted results.
METHODS
A complete phase diagram of cinnarizine-Soluplus(®) SD, including the solubility curve, miscibility curve and glass transition temperature curve, was constructed on the basis of the solid-liquid equilibrium (SLE) equation, Florry-Huggins (F-H) theory and Fox equation. Cinnarizine-Soluplus(®) SDs with different drug loadings were prepared by hot melt extrusion. The extrudates and corresponding physical mixtures were analyzed to check the predicted results.
RESULTS
The experimental data revealed a solubility of 7.9 wt% at 110°C and a miscibility level of 65 wt% at room temperature, which were both consistent with predicted values.
CONCLUSIONS
The predicted phase diagram agrees well with the experimental results for the non-polar components which mainly interact through dispersion forces, thus facilitating the formulation design of SDs.
目的
以桂利嗪 - 固体分散体（Soluplus®）作为模型系统，通过理论方法预测固体分散体（SDs）的温度 - 组成相图，并评估预测结果。
方法
基于固液平衡（SLE）方程、弗洛里 - 哈金斯（F - H）理论和福克斯方程构建了桂利嗪 - 固体分散体（Soluplus®）的完整相图，包括溶解度曲线、混溶曲线和玻璃化转变温度曲线。通过热熔挤出法制备了不同载药量的桂利嗪 - 固体分散体（Soluplus®）。对挤出物和相应的物理混合物进行分析以检验预测结果。
结果
实验数据显示在110°C时溶解度为7.9 wt%，在室温下混溶水平为65 wt%，这两者均与预测值一致。
结论
预测的相图与主要通过色散力相互作用的非极性组分的实验结果吻合良好，从而有助于固体分散体的制剂设计。
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