| Summary: | 碩士 === 國立高雄師範大學 === 化學系 === 107 === In this study, continuous antisolvent sonocrystallization process was used to micronize an active pharmaceutical ingredient (API), sulfathia-zole, to manipulate the crystal size characteristics and crystal habit. Water was selected as an appropriate antisolvent since sulfathiazole is a poorly water-soluble API. According to the solubility values of Sulfathiazole, three solvents including dimethylsulfoxide(DMSO), methanol, and acetone were selected and investigated in solvent/antisolvent screening study.
By considering the crystallization yield , DMSO and water were suitable solvent and antisolvent system for further investigation. Including the effects of sonicated intensity, solution flowrate, solution concentration, antisolvent flowrate, and crystallization temperature in continuous sonocrystallization. At the optimizing condition, mean size of sulfathiazole crystals can be reduced from original 27.83 μm to 10.44 μm.
The smaller sulfathiazole particles can be produced at lower temperature and higher solution flowrates. The effects of sonicated intensity and temperature were significant. Furthermore, Through SEM results showed that with applying power ultrasound, crystal habit of sulfathiazole became regular; compared with the unprocessed sample.
Finally, the solid-state properties of unprocessed and sonocrystallized sulfathiazole; Including the polymorphic, residual solvent, spectroscopic and thermal properties; were examined by HS-GC, DSC, XRPD, FT-IR and TGA analysis. The physical properties remain consistently.
Furthermore, compared with original sulfathiazole, recrystallized sulfathiazole provides an enhanced dissolution rate. These results show that continuous antisolvent sonocrystallization process is a novel and efficient tool for controlling the solid-state properties of an active pharmaceutical ingredient, sulfathiazole.
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