A ciprofloxacin extended release tablet based on swellable drug polyelectrolyte matrices.
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.
Bermúdez
José M
JM
Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA, Córdoba, Argentina.
Jimenez-Kairuz
Alvaro F
AF
Olivera
Maria E
ME
Allemandi
Daniel A
DA
Manzo
Ruben H
RH
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
D000180:Acrylic Resins; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004573:Electrolytes; D011108:Polymers; D013607:Tablets; C006903:carbopol 940; D002939:Ciprofloxacin