Urinary excretion of ciprofloxacin after administration of extended release tablet in healthy volunteers. Hydrophilic carbomer-ciprofloxacin matrix versus bilayer tablets

ROMAÑUK CAROLINA BEATRIZ; GUZMAN MARIA LAURA; LUCIANI GIACOBBE LAURA CAROLINA; SANCHEZ MARIA FLORENCIA; MANZO RUBEN HILARIO; OLIVERA MARIA EUGENIA

Buenos Aires

Congreso; 76th World Congress of Pharmacy & Pharmaceutical Sciences, International Pharmaceutical Federation (FIP); 2016

International Pharmaceutical Federation (FIP)

Backgrounds: New extended release tablets composed by a carbomer-ciprofloxacin ionic complex (CCIC) were developed by wet granulation for the treatment of urinary infections, as an alternative to a bilayer patented formulation.CCIC showed dissolution efficiency similar to the bilayer reference tablets in spite of their different early times reléase profiles.Purpose: To compare in vivo ciprofloxacin urinary excretion after a single dose of both formulations.Methods: A phase 4, double-blind, randomized, crossover clinical trial was performed. Volunteers received a dose of CCIC or the reference. Urine was collected during 36 h and quantified by HPLC-fluorescence. Rate of urinary excretion at each time, corresponding to the half interval of samples collection were obtained (dE/dt vs time), from which (dE/dt)max, Tmax and E(∞) (area under the curve dE/dt versus t from 0 to ∞) were calculated. E%(t) and E(t) (percentage of the dose and the amount (mg) excreted in urine without change) were also determined.Results: Urinary excretion parameters for CCIC and the reference were, respectively: (dE/dt)max: 37±4 and 31±4 mg/h; Tmax: 2±0 and 2±1 h; E%:33±2 and 31±3 %; E(t):164±9 and (16±2)x101 mg; E(∞):(19±2)x101 y (18±2)x101mg. No significant differences were observed in the parameters calculated for CCIC and the reference (p<0.05 ANOVA) except for Tmax. E(t) and E (∞) are related to the absorbed dose of ciprofloxacin suggesting they would not affect the amount of drug absorption.Conclusions: CCIC is an original alternative for the treatment of urinary infections. It represents an advantage since it can be obtained by the current technologies used in tablet formulations making it affordable for developing countries.