title: A ciprofloxacin extended release tablet based on swellable drug polyelectrolyte matrices.
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)(50)Na( 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)(50)Na( 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)(50)Na(10) to (CB-Cip)(50)Na(14). 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.
authors.affiliation: Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA, Córdoba, Argentina.
authors.forename: José M
authors.initials: JM
authors.lastname: Bermúdez
authors.forename: Alvaro F
authors.initials: AF
authors.lastname: Jimenez-Kairuz
authors.forename: Maria E
authors.initials: ME
authors.lastname: Olivera
authors.forename: Daniel A
authors.initials: DA
authors.lastname: Allemandi
authors.forename: Ruben H
authors.initials: RH
authors.lastname: Manzo
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry* / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical; D002939:Ciprofloxacin / Q000737:chemistry* / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics; D004573:Electrolytes / Q000737:chemistry* / Q000493:pharmacokinetics*; D005750:Gastric Juice / Q000737:chemistry / Q000378:metabolism; D011108:Polymers / Q000737:chemistry / Q000493:pharmacokinetics; D017550:Spectroscopy, Fourier Transform Infrared; D013607:Tablets
chemical_list: D000180:Acrylic Resins; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004573:Electrolytes; D011108:Polymers; D013607:Tablets; C006903:carbopol 940; D002939:Ciprofloxacin