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Artículo

Very fast dissolving acid carboxymethylcellulose-rifampicin matrix: development and solid-state characterization

Luciani Giacobbe, Laura CarolinaIcon ; Ramírez Rigo, María VeronicaIcon ; Garro Linck, YamilaIcon ; Monti, Gustavo AlbertoIcon ; Manzo, Ruben HilarioIcon ; Olivera, Maria EugeniaIcon
Fecha de publicación: 10/2016
Editorial: Elsevier Science
Revista: European Journal Of Pharmaceutical Sciences
ISSN: 0928-0987
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:
Ética Médica; Otras Ciencias Químicas

Resumen

One of the main obstacles to the successful treatment of tuberculosis is the poor and variable oral bioavailability of rifampicin (RIF), which is mainly due to its low hydrophilicity and dissolution rate. The aim of this work was to obtain a hydrophilic new material that allows a very fast dissolution rate of RIF and therefore is potentially useful in the development of oral solid dosage forms. The acid form of carboxymethylcellulose (CMC) was co-processed with RIF by solvent impregnation to obtain CMC-RIF powder, which was characterized by polarized optical microscopy, powder x-ray diffraction, DSC-TGA, hot stage microscopy, 13C and 15N solid-state NMR and FT-IR spectroscopy. In addition, the CMC-RIF matrices were subjected to water uptake and dissolution studies to assess hydrophilicity and release kinetics. CMC-RIF is a crystalline solid dispersion. Solid-state characterization indicated that no ionic interaction occurred between the components, but RIF crystallized as a zwitterion over the surface of CMC, which drastically increased the hydrophilicity of the solid. The CMC-RIF matrices significantly improved the water uptake of RIF and disintegrated in a very short period immediately releasing RIF. As CMC improves the hydrophilicity and delivery properties of RIF, CMC-RIF is very useful in the design of oral solid dosage forms with very fast dissolution of RIF, either alone or in combination with other antitubercular drugs.
Palabras clave: Crystalline Solid Dispersion , Dissolution Rate , Drug Delivery , Rifampicin , Solid-State Properties , Wetting , Zwitterion
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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Atribución-NoComercial-SinDerivadas 2.5 Argentina (CC BY-NC-ND 2.5 AR)
Identificadores
URI: http://hdl.handle.net/11336/27091
DOI: http://dx.doi.org/10.1016/j.ejps.2016.10.013
URL: http://www.sciencedirect.com/science/article/pii/S0928098716304365
Colecciones
Articulos(IFEG)
Articulos de INST.DE FISICA ENRIQUE GAVIOLA
Articulos(PLAPIQUI)
Articulos de PLANTA PILOTO DE INGENIERIA QUIMICA (I)
Articulos(UNITEFA)
Articulos de UNIDAD DE INVESTIGACION Y DESARROLLO EN TECNOLOGIA FARMACEUTICA
Citación
Luciani Giacobbe, Laura Carolina; Ramírez Rigo, María Veronica; Garro Linck, Yamila; Monti, Gustavo Alberto; Manzo, Ruben Hilario; et al.; Very fast dissolving acid carboxymethylcellulose-rifampicin matrix: development and solid-state characterization; Elsevier Science; European Journal Of Pharmaceutical Sciences; 96; 10-2016; 398-410
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