The solubility of solid active pharmaceutical ingredients in supercritical fluids is a major thermodynamic criterion for selection and screening of microparticle generation processes. To develop an efficient method for solubility prediction, a solution model was adopted to establish the correlations of the solid solubilities of six sulfonamides in supercritical CO₂. The model was capable of determining solubility correlations. Accordingly, it was attempted to simplify and generalize the model, yielding a predictive solution model, which provided order‐consistent solubility predictions. A case study for model extrapolation was conducted. After understanding the mechanisms underlying the solubility of sulfonamides, the rapid expansion of supercritical solutions (RESS) process was applied to produce microparticles of p‐toluenesulfonamide, an anticancer drug. The effects of RESS process parameters were investigated.

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磺酰胺的固体溶解性和超临界溶液的快速膨胀在制备微粒中的应用

固体活性药物成分在超临界流体中的溶解度是选择和筛选微粒生成过程的主要热力学标准。为了开发一种有效的溶解度预测方法，采用了溶液模型来建立六种磺酰胺在超临界CO ₂中的固体溶解度的相关性。。该模型能够确定溶解度相关性。因此，尝试对模型进行简化和泛化，以产生预测解决方案模型，该模型提供了顺序一致的溶解度预测。进行了模型外推的案例研究。在了解了磺酰胺溶解性的基本机理后，超临界溶液（RESS）工艺的快速膨胀被用于生产抗癌药物对甲苯磺酰胺的微粒。研究了RESS工艺参数的影响。