Interaction of sulfadiazine with cyclodextrins in aqueous solution and solid state

The main objective of this work was to increase the solubility of sulfadiazine by formation of inclusion complexes with β-cyclodextrin, and methyl-β-cyclodextrin. The apparent stability constants have been determined by phase solubility studies in water and buffer solutions of pH values of 2 and 8....

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Detalles Bibliográficos
Autores: Delrivo, Alicia, Zoppi, Ariana, Longhi, Marcela Raquel
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2012
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/190106
Acceso en línea:http://hdl.handle.net/11336/190106
Access Level:acceso abierto
Palabra clave:COMPLEXATION
CYCLODEXTRINS
NUCLEAR MAGNETIC RESONANCE
SCANNING ELECTRON MICROSCOPY
SULFADIAZINE
X-RAY DIFFRACTOMETRY
https://purl.org/becyt/ford/2.11
https://purl.org/becyt/ford/2
Descripción
Sumario:The main objective of this work was to increase the solubility of sulfadiazine by formation of inclusion complexes with β-cyclodextrin, and methyl-β-cyclodextrin. The apparent stability constants have been determined by phase solubility studies in water and buffer solutions of pH values of 2 and 8. The stoichiometry of all complexes was found to be 1:1 but different relative affinities were found for each cyclodextrin. It was possible to obtain a greater overall solubility by using a combined approach of pH adjustment and complexation with cyclodextrins. Guest-host interactions have been investigated using nuclear magnetic resonance. Complexes were prepared in solid state by different methods and were characterized using differential scanning calorimetry, thermogravimetric analysis, Fourier-transform infrared spectroscopy, X-ray diffractometry and scanning electron microscopy. The dissolution rate of the drug from the inclusion complex made by freeze-dried was much faster than this of the pure drug.