Solid Solubilities of Sulfonamides and Use of Rapid Expansion of Supercritical Solutions for Microparticle Production. Issue 6 (6th May 2020)

• Record Type: Journal Article
• Authors: Yang, Tsung-Mao; Li, Jin-Shuh; Yeh, Tsao-Fa; Su, Chie-Shaan
• Other Names: Flood Adrian guestEditor.
• Is Part Of: Chemical engineering & technology. Volume 43:Issue 6(2020)
• Page Start: 1115
• Page End: 1123
• Publication Date: 2020-05-06
• Subjects: Microparticle production -- Sulfonamide -- Supercritical CO2 -- Rapid expansion of supercritical solutions -- p‐Toluenesulfonamide; Chemical engineering -- Periodicals; Chemical processes -- Periodicals; 660.05
• DOI: 10.1002/ceat.201900646
• Languages: English
• ISSNs: 0930-7516

Abstract

Abstract: 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. Abstract : A predictive solution model was developed to predict the solid solubility of sulfonamides in supercritical CO2 . Microparticles of p ‐toluenesulfonamide, an anticancer drug, with a mean size of 1.09 μm were successfully produced through an organic solvent‐free rapid expansion of supercritical solutions process. The effects of rapid expansion of supercritical solutions process parameters were evaluated.