Ciprofloxacin Betaine/Ciprofloxacin Hydrochloride

This paper builds on a previous paper in which new ciprofloxacin extended-release tablets were developed based on a ciprofloxacin-based swellable drug polyelectrolyte matrix (SDPM-CIP). The matrix contains a molecular dispersion of ciprofloxacin ionically bonded to the acidic groups of carbomer, forming the polyelectrolyte-drug complex CB-CIP. This formulation showed that the release profile of the ciprofloxacin bilayer tablets currently commercialised can be achieved with a simpler strategy. Thus, since ciprofloxacin urine concentrations are associated with the clinical cure of urinary tract infections, the goal of this work was to compare the urinary excretion of SDPM-CIP tablets with those of the CIPRO XR® bilayer tablets. A batch of SDPM-CIP tablets was manufactured by the wet granulation method and the CB-CIP ionic complex was obtained in situ. Fasted healthy volunteers received a single oral dose of 500 mg ciprofloxacin of either formulation in a randomised crossover study. Urinary concentrations were assessed by HPLC at intervals up to 36 h. Pharmacokinetic parameters (rate of urinary excretion, maximum urine excretion rate, t_max, area under the curve, amount and percentage of the ciprofloxacin dose excreted in urine) showed no statistical differences between both formulations at any of the time intervals of collection. The processing conditions to obtain SDPM-CIP tablets are easy to scale up since they involve technology currently employed in the pharmaceutical industry and the process is less challenging to implement. In addition, SDPM-CIP tablets met pharmacopoeial quality specifications.

The aim of this trial was to compare the efficacy and safety of extended-release ciprofloxacin (CIPRO XR) versus the immediate-release formulation (CIPRO IR) in the treatment of complicated urinary tract infections (UTIs). 212 patients were randomized to CIPRO XR 1,000 mg tablet once daily or CIPROXIN IR 500 mg tablet twice daily. Treatment efficacy was evaluated by bacteriological outcome. Safety was measured by recording adverse events. The rate of bacteriological eradication was 83% in the CIPRO XR group and 75% in the CIPRO IR. the overall incidence of adverse events reported was higher in the CIPRO IR group. The authors conclude that CIPRO XR is a safe and effective treatment for complicated UTIs. Although the limited data available do not consent to support a statistically superior efficacy or safety compared to CIPRO IR, a trend in favor of CIPRO XR is clearly evident in all efficacy and safety variables. CIPRO XR is associated with reduced frequencies of drug-related adverse events compared to CIPRO IR.