Solid forms of the new antitrypanosomal 1-(4-acetamide-benzenesulfonyl)-benzimidazole: preparation and physicochemical characterization.

NR SPRANDEO

J Pharm Sci

Elsevier

Año: 2023 vol. 112 p. 3233 - 3233

his 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. Three different crystalline forms of PABZI (a solvent-free form (form I), three isostructural solvates (from isopropanol; acetonitrile-dichloromethane and from 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, powder 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