SIMULTANEOUS COCRYSTALLIZATION AND MICRONIZATION OF PARACETAMOL-DIPICOLINIC ACID COCRYSTAL BY SUPERCRITICAL ANTISOLVENT (SAS)
Keywords:
Paracetamol, Dipicolinic acid, Cocrystal, Supercritical antisolvent, Tabletability, MicronizationAbstract
Objective: This present study aims to produce cocrystal of paracetamol (PCA)-dipicolinic acid (DPA) using supercritical antisolvent (SAS) cocrystallization process in order to improve tabletability profile of PCA.
Methods: The PCA-DPA cocrystal prepared by SAS cocrystallization were compared to those produced using a traditional solvent evaporation. The cocrystals produced were characterized using Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), Polarized Light Microscopy (PLM), Fourier Transform Infrared (FTIR) spectroscopy, particle size analysis, Scanning Electron Microscopy (SEM) and High Performance Liquid Chromatography (HPLC). Analysis of flowability, drug content, solubility, dissolution, stability and powder compaction were performed to evaluate the cocrystals.
Results: Cocrystal particles with mean diameter of 4.18 µm were produced from SAS process, smaller than those produced by traditional solvent evaporation method (mean diameter of 64.93 μm). The PCA-DPA cocrystal from SAS process showed an enhanced dissolution rate by 2.45 times compared to PCA, higher than cocrystal from traditional solvent evaporation (enhanced dissolution rate by 1.72 times compared to PCA). Tabletability study revealed superior tableting performance of both cocrystals compared to PCA.
Conclusion: This study showed the utility of PCA-DPA cocrystal to improve mechanical properties of PCA while also demonstrating that simultaneous micronization and cocrystallization process can be obtained using SAS process.
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