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Artículo

Diloxanide furoate binary complexes with β-, methyl-β-, and hydroxypropyl-β-cyclodextrins: inclusion mode, characterization in solution and in solid state and in vitro dissolution studies

Aloisio, CarolinaIcon ; Longhi, Marcela RaquelIcon
Fecha de publicación: 08/2018
Editorial: Taylor
Revista: Pharmaceutical Development and Technology
ISSN: 1083-7450
e-ISSN: 1097-9867
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:
Otras Ciencias Químicas

Resumen

The purpose of this study was to investigate the effect on solubility and dissolution rate of binary complexes of b -( b CD), methyl-(M b CD) and hydroxypropyl- b -cyclodextrin (HP b CD) with diloxanide furoate (DF).The complexation in solution was evaluated by phase solubility studies and1H nuclear magnetic resonance (NMR). Enhanced water solubility of DF was obtained with the DF:M b CD system (61-fold). The mode of inclusion was supported by NMR experiments, which indicated that real inclusion complexes wereformed between DF and M b CD or HP b CD. Solid state analysis was performed using infrared and thermal methods, which suggested the formation of true inclusion complexes of DF with two derivatized cyclodex-trins, M b CD and HP b CD, and an exclusion complex with b CD when the systems were prepared by freeze-dried technique. Dissolution studies conducted in simulated gastric fluid (2 h) and subsequent simulated intestinal fluid (next 4 h) showed increased dissolution rate of DF from the freeze-dried systems with b CD, M b CD, and HP b CD (85; 77 and 75% of dissolved drug at 5 min, respectively) and 100% of the drug dissolved at 150 min for the three systems. The enhancement of the solubility and the dissolution of DF observed make these complexes promising candidates for the preparation of oral pharmaceuticalformulations.
Palabras clave: Complexation , Cyclodextrin , Diloxanide Furoate , In Vitro Dissolution , Mode of Interaction , Solid State Characterization
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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)
Identificadores
URI: http://hdl.handle.net/11336/62930
DOI: http://dx.doi.org/10.1080/10837450.2017.1362435
URL: https://www.tandfonline.com/doi/abs/10.1080/10837450.2017.1362435
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Articulos(UNITEFA)
Articulos de UNIDAD DE INVESTIGACION Y DESARROLLO EN TECNOLOGIA FARMACEUTICA
Citación
Aloisio, Carolina; Longhi, Marcela Raquel; Diloxanide furoate binary complexes with β-, methyl-β-, and hydroxypropyl-β-cyclodextrins: inclusion mode, characterization in solution and in solid state and in vitro dissolution studies; Taylor; Pharmaceutical Development and Technology; 23; 7; 8-2018; 723-731
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