SYNTHESIS AND CHARACTERIZATION OF FLUBENDAZOLE COCRYSTALS

SYNTHESIS AND CHARACTERIZATION OF FLUBENDAZOLE COCRYSTALS

dos Santos, C. R. M.; Carvalho, F. M. S.; Antonio, S. G.; Paiva-Santos, C. O.; Bou-Chacra, N. A.; Ferreira, F. F.; Flores, R. L. R.; de Araujo, G. L. B.

Abstract:

Background/problem statement: Flubendazole (FBZ) has a great potential for the treatment of lymphatic filariasis in humans, but is poorly absorbed in the current formulations available due its low solubility in water. Objective: The present work describes the synthesis and characterization of FBZ cocrystals in combination with carboxilics acids.Methods: Mechanochemical liquid-assisted grinding method was used to obtain mixtures corresponding to 1:1 stoichiometric ratios of flublendazole and the cocrystal former. The mixtures were evaluated by X-ray powder diffraction (Bruker D8 Advance). Results: The XRPD patterns (Fig.1) show a potential cocrystal formation with maleic acid and no evidence of cocrystal with aspirin as former.Conclusions: The combination of flubendazole with maleic acid with application of mechanosynthesis has great potential to obtain cocrystals and can represent a new way for the development of a new oral solid dosage form containing flubendazole.

Background/problem statement: Flubendazole (FBZ) has a great potential for the treatment of lymphatic filariasis in humans, but is poorly absorbed in the current formulations available due its low solubility in water. Objective: The present work describes the synthesis and characterization of FBZ cocrystals in combination with carboxilics acids.Methods: Mechanochemical liquid-assisted grinding method was used to obtain mixtures corresponding to 1:1 stoichiometric ratios of flublendazole and the cocrystal former. The mixtures were evaluated by X-ray powder diffraction (Bruker D8 Advance). Results: The XRPD patterns (Fig.1) show a potential cocrystal formation with maleic acid and no evidence of cocrystal with aspirin as former.Conclusions: The combination of flubendazole with maleic acid with application of mechanosynthesis has great potential to obtain cocrystals and can represent a new way for the development of a new oral solid dosage form containing flubendazole.

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DOI: 10.5151/phypro-sic100-016

Como citar:

dos Santos, C. R. M.; Carvalho, F. M. S.; Antonio, S. G.; Paiva-Santos, C. O.; Bou-Chacra, N. A.; Ferreira, F. F.; Flores, R. L. R.; de Araujo, G. L. B.; "SYNTHESIS AND CHARACTERIZATION OF FLUBENDAZOLE COCRYSTALS", p-16-16. In: Proceedings of the International Symposium on Crystallography [Blucher Physics Proceedings, v.1, n.3]. São Paulo: Blucher, 2015.
ISSN 23582359, DOI 10.5151/phypro-sic100-016