A Ciprofloxacin Extended Release Tablet Based on Swellable Drug Polyelectrolyte Matrices

Abstract

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.

Swellable drug-polyelectrolyte matrices of drug-carboxymethylcellulose complexes. Characterization and delivery properties

“…The body of information provided by FT-infrared spectroscopy, power X-ray diffraction, DSC, and TG supports the conclusion about the ionic nature of the interaction between the carboxylic groups of HCMC and the basic group of D (Jimenez-Kairuz et al, 2005;Ramírez Rigo et al, 2006;Bermudez et al, 2008;Takka, 2003;Esteban, 2007;Quinteros, 2008). Figures 1-3 show representative results.…”

“…Such SDPM were developed using complexes of carbomer or alginic acid-sodium alginate as acid PE and a set of model drugs having basic groups. Development of extended release tablets based on SDPM was also reported (Bermudez et al, 2008).…”

Development of a prolonged-release gastroretentive tablet formulation of ciprofloxacin hydrochloride: Pharmacokinetic characterization in healthy human volunteers

“…Therefore, there has been significant interest in the development of a convenient once-daily formulation of ciprofloxacin. In this respect, two attempts have so far been made to deliver ciprofloxacin in a prolonged manner in order to extend its therapeutic effect for longer period of time (Arza et al, 2009;Bermúdez et al, 2008). However, these studies lack in vivo pharmacokinetic assessments.…”

Swelling/Floating Capability and Drug Release Characterizations of Gastroretentive Drug Delivery System Based on a Combination of Hydroxyethyl Cellulose and Sodium Carboxymethyl Cellulose

“…As shown in Table 3 , release rates ( k value) of ciprofloxacin from CF1–4 and CF1–1 in media with increasing concentrations of NaCl were 0.46, 0.73, 0.54, 0.66, and 0.83, 0.96, 0.89, and 0.94, respectively, which indicates that overall release rates were faster in CF1–1 compared to those in CF1–4. This might have been caused by the acid-base interactions between the carboxyl groups of NaCMC and the aliphatic piperazine nitrogen of ciprofloxacin, which also was shown by Bermúdez et al [ 38 ]. The extent of acid-base interactions was unapparent with a lower amount of NaCMC, so the release rate increased when ciprofloxacin was incorporated in CF1–1, whereas such an interaction was hindered by the increased ionic strength, resulting in a faster release rate in the higher NaCl medium.…”