Metabolism of ¹⁴C-Miloxacin in Rats

—Metabolites in Urine, Bile and Feces—

Abstract

Isolation and characterization of metabolites of miloxacin, a new antimicrobial agent, were undertaken with rats. ¹⁴C-Miloxacin was orally administered to Sprague-Dawley rats at a dose of 50 mg/kg, and urine, bile and feces were collected. The metabolites extracted from the biological samples were isolated by column and thin-layer chromatographies. Characterization of the isolated metabolites was carried out by comparison with the authentic materials in various physicochemical analyses. Eight metabolites together with intact miloxacin were iden-tified; containing the metabolites of N-demethoxy (M-1), catechol (M-3) and 6-met hoxy (M-2 and M-4) types and their conjugates with glucuronic acid.