Table 5

Radiometabolite patterns in the excreta and bile of bile duct-cannulated rats following oral and intravenous administration of [14C]gemifloxacin mesylate

CompoundPercentage of Administered Dose
Oral (168 mg fb/kg)Intravenous (10 mg fb/kg)
UrineBileFecesTotalUrineBileFecesTotal
Gemifloxacin6.2N.S.61.868.033.4N.S.15.849.2
Gemifloxacin acyl glucuronide0.11.6N.D.1.7N.D.4.0N.D.4.0
E-Isomer of gemifloxacin0.60.12.83.54.30.21.45.9
N-Acetyl gemifloxacin0.30.31.62.21.60.92.44.9
Hydroxymethyl gemifloxacinN.D.0.1N.D.0.1N.D.0.30.81.1
Gemifloxacin glutamate0.10.2N.D.0.30.50.5N.D.1.0

Radiometabolite patterns were determined in pooled 0- to 24-h urine and bile samples and in extracts of 0- to 48-h fecal extracts. Data are mean values (n = 3).

  • N.D., not detected; N.S., gemifloxacin did not separate from its carboxylic acid derivative under the analytical conditions used; together the two compounds accounted for 0.6 and 2.0% of the dose in the bile after oral and intravenous administration, respectively.