RT Journal Article SR Electronic T1 SPIRONOLACTONE METABOLISM IN MAN STUDIED BY GAS CHROMATOGRAPHY-MASS SPECTROMETRY JF Drug Metabolism and Disposition JO Drug Metab Dispos FD American Society for Pharmacology and Experimental Therapeutics SP 467 OP 478 VO 3 IS 6 A1 A. KARIM A1 J. HRIBAR A1 W. AKSAMIT A1 M. DOHERTY A1 L. J. CHINN YR 1975 UL http://dmd.aspetjournals.org/content/3/6/467.abstract AB Gas chromatography-mass spectrometry was used to identify metabolites of spironolactone in human blood and urine. In three healthy men about 20% of the radioactivity was excreted in the urine within 24 hr after an oral dose of [20-3H]spironolactone (200 mg + 200 µCi). About half of this radioactivity was extracted with chloroform at pH 3 and from this extract four stable metabolites were isolated by use of column and thin-layer chromatography. Two of these were the previously identified metabolites, canrenone (VII; 2.9% of dose) and the 6β-hydroxy-sulfoxide (X; 1.8% of the dose). The remaining were the new metabolites, 15α-hydroxycanrenone (XI; 0.8% of dose) and the 6β-hydroxy-thiomethyl derivative (VI; 0.5% of dose). The principal water-soluble urinary metabolite was canrenoate ester glucuronide (XII; 4.5% of dose). In the 24- to 32-hr pooled serum, canrenone (VII) was the principal metabolite in the organic-extractable fraction: VI was present in appreciable amounts but X and Xl were present at extremely low levels. Copyright © 1975 by The American Society for Pharmacology and Experimental Therapeutics