Cocrystal engineering of Tizoxanide: Design, synthesis and characterization

Congreso; I Reunión Latinoam. Cristalogr. y IX Reunión Anual Asoc. Arg Cristalogr,; 2013

Cocrystal technology has shown great promise in rectifying the undesirable properties of a drug substance [1, 2]. Tizoxanide (TIZ), a new potent anti-infective agent which may enhance current therapies for Leishmaniasis, Chagas disease and Viral Hepatitis, was chosen as a model system, due to its low aqueous solubility, and submitted to a cocrystal screening. Since empirical information on complementary functional groups and their likely supramolecular synthons is a prerequisite for the design of pharmaceutical cocrystals, searches of existing structures stored in the Cambridge Structural Database (CSD) were conducted to identify known synthons and to facilitate the selection of possible coformers for TIZ, with the following criteria: R factor < 0.05, 3D coordinates present, ordered structures and organic compounds only. The experimental screenings were performed byliquid-assisted sonication (LAS). The resulting samples were characterized by Powder X-ray diffraction (PXRD), Raman spectroscopy (FT Raman), Diffuse Reflectance Infrared Fourier Transform (DRIFT) and Thermomicroscopy (TM).