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Solubility and apparent thermodynamic analysis of pomalidomide in (acetone + ethanol/isopropanol) and (ethyl acetate + ethanol/isopropanol) and its correlation with thermodynamic model
The Journal of Chemical Thermodynamics ( IF 2.6 ) Pub Date : 2021-03-01 , DOI: 10.1016/j.jct.2020.106345
Rongrong Li , Bo Zhao , Xianlang Chen , Jieyu Zhang , Zhiying Liu , Xianling Zhu , Deman Han

Abstract Co-solvency has been extensively utilized as a very helpful dissolving technique for the poorly soluble pharmaceutical compounds. The dissolution of pomalidomide racemic mixture in four mixtures including (acetone + ethanol), (acetone + isopropanol), (ethyl acetate + ethanol) and (ethyl acetate + isopropanol) over the temperature from 278.15 K to 318.15 K was studied and correlated using the Jouyban-Acree model. In the acetone mixture, the increases occurred monotonously with the increasing mass fraction of acetone, while it increases to a maximum value with the rising concentration of ethyl acetate, and then decreases in ethyl acetate systems. The correlation result was evaluated by relative average deviation (RAD), which indicates that the Jouyban-Acree model can provide a reasonable correlation. The different types of interaction on the solubility were analysed by a multiple linear regression analysis (MLRA). In addition, apparent thermodynamic analysis indicates that the dissolution process of pomalidomide in four mixtures selected is an endothermic and entropy driven process. More importantly, the co-solvency on the dissolution process for pomalidomide is an important aspect of its purification and recrystallization.

中文翻译:

泊马度胺在(丙酮+乙醇/异丙醇)和(乙酸乙酯+乙醇/异丙醇)中的溶解度和表观热力学分析及其与热力学模型的相关性

摘要 共溶解作为一种非常有用的溶解技术,已被广泛用于难溶性药物化合物。研究了泊马度胺外消旋混合物在包括(丙酮 + 乙醇)、(丙酮 + 异丙醇)、(乙酸乙酯 + 乙醇)和(乙酸乙酯 + 异丙醇)的四种混合物中在 278.15 K 至 318.15 K 的温度下的溶解情况并使用Jouyban-Acree 模型。在丙酮混合物中,随着丙酮质量分数的增加单调增加,而随着乙酸乙酯浓度的增加而增加到最大值,然后在乙酸乙酯体系中减少。相关结果通过相对平均偏差(RAD)进行评估,表明Jouyban-Acree模型可以提供合理的相关性。通过多元线性回归分析(MLRA)分析对溶解度的不同类型的相互作用。此外,表观热力学分析表明泊马度胺在所选四种混合物中的溶解过程是吸热和熵驱动的过程。更重要的是,泊马度胺溶解过程中的共溶性是其纯化和重结晶的一个重要方面。
更新日期:2021-03-01
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