Abstract
The metabolism of 14C labeled Q-35 [(±)-1-cyclopropyl-6-fluoro-1, 4-dihydro-8-methoxy-7 (3-methylaminopiperidin-1-yl)-4-oxoquinoline-3-carboxylic acid], a new fluoroquinolone antimicrobial agent, was studied in rats and dogs.
1. Two metabolites were identified in the urine and the bile (or the feces) after a sigle oral administration of 14C-Q-35 to rats and dogs: glucuronic acid conjugate of Q-35 as the main metabolite and aminopiperidinyl N-desmethylated derivative (N-desmetyl Q-35) as a minor metabolite.
2. Q-35 glucuronide was excreted mainly in the bile or feces. Most of the radioactivity in the urine and the plasma was unchanged Q-35.
3. The bioautographic study revealed that the antibacterial activity present in the urine and the bile was related to unchanged Q-35 but not to its metabolites. These results indicate that the transformation of Q-35 hardly occurs and that most of the drug administerd remains unchanged Q-35 in rats and dogs.
