IDENTIFICATION AND DETERMINATION OF THE 2 PRINCIPAL METABOLITES OF MINOCYCLINE IN HUMANS

A chromatographic method has been developed for the quantification of minocycline in human serum and urine. The chromatographically determined concentration of minocycline correlated well with the microbiologically active concentration in serum. Two metabolites, 9-hydroxyminocycline and N-demethylated minocycline, could be isolated and identified as the principal metabolites of this tetracycline antibiotic. The structure of the 9-hydroxy compund was proved by nuclear magnetic resonance analysis for the first time. About 15% of the drug was actively converted in the body into a substance less microbiologically active than the parent compound and excreted in the urine within 96 h after the application.