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

GUZMAN, MARIA LAURA; ROMAÑUK, CAROLINA; LUCIANI GIACOBBE, CAROLINA; SANCHEZ, MARÍA FLORENCIA; MARIA E OLIVERA ME

Congreso; 76th World Congress of Pharmacy & Pharmaceutical Sciences; 2016

Backgrounds: New extended release tablets composed by a carbomer-ciprofloxacin ionic complex (CCIC) weredeveloped 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 releaseprofiles.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 ofCCIC or the reference. Urine was collected during 36 h and quantified by HPLC-fluorescence. Rate of urinary excretion ateach 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 doseand 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. Nosignificant differences were observed in the parameters calculated for CCIC and the reference (p<0.05 ANOVA) exceptfor Tmax. E(t) and E(∞) are related to the absorbed dose of ciprofloxacin suggesting they would not affect the amount ofdrug absorption.Conclusions: CCIC is an original alternative for the treatment of urinary infections. It represents an advantage since itcan be obtained by the current technologies used in tablet formulations making it affordable for developing countries.