Solid-state properties of Nifurtimox. Preparation, analytical characterization, and stability of an amorphous phase

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dc.citation.titleEuropean Journal of Pharmaceutics and Biopharmaceutics
dc.citation.volume184
dc.creatorMoroni, Aldana Beatriz
dc.creatorPérez Mayoral, Elena
dc.creatorLionello, Diego Fernando
dc.creatorVega, Daniel Roberto
dc.creatorKaufman, Teodoro Saúl
dc.creatorCalvo, Natalia Lorena
dc.date.accessioned2024-09-24T13:49:54Z
dc.date.available2024-09-24T13:49:54Z
dc.date.issued2023-01-13
dc.description.abstractNifurtimox (NFX) is a nitrofuran derivative used to treat Chagas disease, a neglected disease caused by the protozoan Trypanosoma cruzi. The drug is very sparingly soluble in aqueous media and no other solid phases of NFX have been reported to date. The preparation of the amorphous mode of NFX is reported, as well as its characterization by hot stage microscopy, thermal (differential scanning calorimetry and thermogravimetric analysis), spectroscopic (solid state nuclear magnetic resonance, mid-infrared, and near-infrared), diffractometric and functional (powder dissolution rate) means. The stability of the new phase was investigated. This was characterized using thermal, spectroscopic, and diffractometric methods, finding out its spontaneous reversion to the crystalline state, as sign of instability. In addition, the amorphous material proved to be sensitive to temperature, pressure, and mechanical stress, all of which accelerated phase conversion. However, it was able to remain stable in a model polymeric amorphous solid dispersion with PEG 4000 for more than one month. An approach for monitoring the conversion of the amorphous phase to its crystalline counterpart under thermal stress by chemometric analysis of mid-infrared spectra at different temperatures is also disclosed.
dc.description.filFil: Moroni, Aldana Beatriz. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario (IQUIR-CONICET). Área de Análisis de Medicamentos; Argentina.
dc.description.filFil: Pérez Mayoral, Elena. Universidad Nacional de Educación a Distancia. Departamento de Química Inorgánica y Química Técnica; España.
dc.description.filFil: Lionello, Diego Fernando. Universidad Nacional General San Martín. Instituto de Tecnología Sabato (CNEA); Argentina.
dc.description.filFil: Lionello, Diego Fernando. Comisión Nacional de Energía Atómica. Centro Atómico Constituyentes. Departamento de Física de la Materia Condensada (CONICET/UNSaM); Argentina.
dc.description.filFil: Vega, Daniel Roberto. Universidad Nacional General San Martín. Escuela de Ciencia y Tecnologia (CNEA); Argentina.
dc.description.filFil: Vega, Daniel Roberto. Comisión Nacional de Energía Atómica. Centro Atómico Constituyentes. Departamento de Física de la Materia Condensada (CONICET/UNSaM); Argentina.
dc.description.filFil: Kaufman, Teodoro Saúl. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario (IQUIR-CONICET). Área de Análisis de Medicamentos; Argentina.
dc.description.filFil: Calvo, Natalia Lorena. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario (IQUIR-CONICET). Área de Análisis de Medicamentos; Argentina.
dc.description.sponsorshipConsejo Nacional de Investigaciones Científicas y Técnicas (CONICET): PUE IQUIR 2016
dc.description.sponsorshipAgencia Nacional de Promoción de la Investigación, el Desarrollo Tecnológico y la Innovación (Agencia I+D+i): ICT 2019- 1155
dc.description.sponsorshipAgencia Santafesina de Ciencia Tecnología e Innovación (ASaCTeI): IO-2019-302
dc.description.sponsorshipFundación Carolina
dc.description.sponsorshipMinisterio de Educación de la República Argentina. Mobility Program for Argentine Teachers
dc.description.versionpeerreviewed
dc.format.extent1-11
dc.identifier.citationMoroni, A. B., Pérez Mayoral, E., Lionello, D. F., Vega, D. R., Calvo, N. L. and Kaufman, T. S. (2023). Solid-state properties of Nifurtimox. Preparation, analytical characterization, and stability of an amorphous phase. European Journal of Pharmaceutics and Biopharmaceutics, 184, 25-35. https://doi.org/10.1016/j.ejpb.2023.01.008
dc.identifier.e-issn1873-3441
dc.identifier.issn0939-6411
dc.identifier.urihttps://hdl.handle.net/2133/27844
dc.language.isoen
dc.publisherElsevier
dc.relation.publisherversionhttps://doi.org/10.1016/j.ejpb.2023.01.008
dc.relation.publisherversionhttps://www.sciencedirect.com/science/article/abs/pii/S0939641123000085?via%3Dihub
dc.rightsembargoedAccess
dc.rights.holderMoroni, Aldana Beatriz
dc.rights.holderPérez Mayoral, Elena
dc.rights.holderLionello, Diego Fernando
dc.rights.holderVega, Daniel Roberto
dc.rights.holderKaufman, Teodoro Saúl
dc.rights.holderCalvo, Natalia Lorena
dc.rights.holderUniversidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas
dc.rights.holderElsevier
dc.rights.textAttribution-NonCommercial-NoDerivatives 4.0 Internationalen
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subjectAmorphous phase
dc.subjectChemometrics method
dc.subjectNifurtimox physical phase stability
dc.subjectSolid-state characterization
dc.subjectSpectroscopy and diffractometry
dc.subjectThermal methods
dc.titleSolid-state properties of Nifurtimox. Preparation, analytical characterization, and stability of an amorphous phase
dc.typearticulo
dc.type.versionacceptedVersion

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