Artículo
Solid-state properties of Nifurtimox. Preparation, analytical characterization, and stability of an amorphous phase
Moroni, Aldana Beatriz
; Perez Mayoral, Elena; Lionello, Diego Fernando
; Vega, Daniel Roberto; Kaufman, Teodoro Saul
; Calvo, Natalia Lorena
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Fecha de publicación:
01/2023
Editorial:
Elsevier Science
Revista:
European Journal of Pharmaceutics and Biopharmaceutics
ISSN:
0939-6411
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
Nifurtimox (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 nearinfrared), 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.
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Articulos(IQUIR)
Articulos de INST.DE QUIMICA ROSARIO
Articulos de INST.DE QUIMICA ROSARIO
Citación
Moroni, Aldana Beatriz; Perez Mayoral, Elena; Lionello, Diego Fernando; Vega, Daniel Roberto; Kaufman, Teodoro Saul; et al.; Solid-state properties of Nifurtimox. Preparation, analytical characterization, and stability of an amorphous phase; Elsevier Science; European Journal of Pharmaceutics and Biopharmaceutics; 184; 1-2023; 25-35
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