A Ciprofloxacin Extended Release Tablet Based on Swellable Drug Polyelectrolyte Matrices |
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Authors: | José M. Bermúdez Alvaro F. Jimenez-Kairuz Maria E. Olivera Daniel A. Allemandi Ruben H. Manzo |
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Affiliation: | (1) Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA Córdoba, Argentina |
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Abstract: | The aim of this work was the development of extended release tablets of 500 mg of ciprofloxacin based on swellable drug polyelectrolyte matrices (SDPM). A set of complexes of carbomer, ciprofloxacin and sodium, (CB–Cip)50Na x , having a molar ratio Cip/CB acid groups of 0.5 and variable proportions of Na+ was used to prepare SDPM. Characterization of complexes by FT-IR, powder X-ray diffraction and thermal analysis revealed that Cip, in its protonated form, is ionically bonded to the functional groups of CB. Rates of fluid uptake of (CB–Cip)50Na x matrices as well as Cip release in simulated gastric fluid were modulated by changes in the proportion of Na+ incorporated in the complexes. A direct correlation between fluid uptake and delivery rate was observed along the series of matrices. Release rates were modulated from 1.4 mg/min to 25 mg/min in going from (CB–Cip)50Na10 to (CB–Cip)50Na14. The analysis of kinetic data suggest that rates of swelling, ionic pair dissociation and drug diffusion play a role in the kinetic control of delivery. Complexes were satisfactorily prepared and processed together with small amounts of antiadherent and lubricant excipients to obtain a series of extended release SDPM tablets through the current tableting technology processes. Cip release from matrices was widely modulated by the composition of the complexes yielding a flexible system that allows selecting a composition that releases in 120 min 90% of the dose in simulated gastric fluid. |
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Keywords: | ciprofloxacin extended release swellable drug– polyelectrolyte matrices |
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