Generation and physicochemical characterization of posaconazole cocrystals using Gas Antisolvent (GAS) and Supercritical Solvent (CSS) methods

Posaconazole (PSZ) is a BCS (biopharmaceutical classification system) Class II anti-fungal drug used to treat infections in immunocompromised patients. The work presented herein describes the generation of cocrystals PSZ with 4-aminobenzoic acid (4AMB) using supercritical CO2 as an antisolvent GAS (Gas Antisolvent) acetonitrile, and solvent CSS (Cocrystallization Supercritical Solvent) methods. Cocrystals PSZ-4AMB were obtained 2:3 stoichiometric ratio for first time by methods, producing higher-purity samples compared method. investigates influence critical processing variables crystallization methods respect formation PSZ-4AMB. A Design Experiments (DoE) approach was performed assess outcome formation, impacted such pressure, temperature, stirring rate resulting cocrystalline phase identified differential scanning calorimetry (DSC) powder X-ray diffraction (PXRD). particle morphologies size distributions determined electron microscopy automated static imaging, respectively.