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  • Title: Solid Forms of The New Antitrypanosomal 1-(4-Acetamide-Benzenesulfonyl)-Benzimidazole: Preparation and Physicochemical Characterization.
    Author: Marcos Valdez MM, Fandiño OE, Faudone SN, Ayala AP, Caira MR, Sperandeo NR.
    Journal: J Pharm Sci; 2023 Dec; 112(12):3233-3239. PubMed ID: 37716530.
    Abstract:
    This study aimed to investigate the polymorphism of 1-(4-acetamide-benzenesulfonyl)-benzimidazole (PABZI), a newly developed compound with significant activity against Trypanosoma cruzi, the parasite which causes American trypanosomiasis (Chagas disease). Three different crystalline forms of PABZI [a solvent-free form (form I), three isostructural solvates (from isopropanol; acetonitrile-dichloromethane, and methanol-benzene) and a non-isostructural solvate from methanol] were isolated and characterized. The crystal structure of form I was resolved at 173 K and 300 K by single crystal X-ray diffraction. Physicochemical properties, including solubility, dissolution rate, wettability, and solid-state stability were assessed for the two most viable solid forms of PABZI, viz. form I and the isopropanol solvate (PABZI-isoOH). Form I exhibited a higher solubility and dissolution rate, and superior stability towards moisture (40 °C/75 % relative humidity) and UV-Visible light than PABZI-isoOH. Based on the solid-state stability results, form I was selected over PABZI-isoOH for further preclinical studies.
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