[The role of ciprofloxacine metabolites in its biliary and urinary elimination in man].

The purpose of the present work was the investigation of the urinary and biliary eliminations of M1, M2, M3 and M4, the four metabolites of ciprofloxacin in twelve recently cholecystectomized patients provided with a T-drain. The four metabolites were measured by HPLC under isocratic conditions for M2 and M4, and by gradient elution for M1 and M3. After a single oral dose of 500 mg of ciprofloxacin, the 24th urinary elimination of the parent compound and its metabolites respectively amounted to 130.1 +/- 15.6; 13 +/- 11; 46.6 +/- 8.2; 13 +/- 3.7 and 0 mg, representing 26.02; 0.54; 1.32; 2.60 and 0% of the administered dose (total: 192.4 mg; 38.5%). During the same investigation period, the biliary elimination respectively reached 1,587 +/- 222; 241 +/- 38; 11,042 +/- 2,489; 144 +/- 51 and 19 +/- 13 micrograms (total: 13 mg) corresponding to 0.32; 0.05; 2.21; 0.03 and 0% (total: 2.61%) of the dose. The urinary and biliary elimination of ciprofloxacin as metabolites respectively represents 12.5 and 2.3% of the dose (total: 14.8%). The important amount of M2 recovered in bile (7 times more than ciprofloxacin itself) let suggest a hepatic biotransformation of ciprofloxacin.