The biliary and urinary metabolites of [3H]17 alpha-ethynylestradiol in women.
The metabolism of 17 alpha-ethynyl[6,7-3H]estradiol (3H-EE2) (50 micrograms) given orally was studied in two groups of women: (a) six subjects from whom duodenal bile samples were obtained after 4 h by endoscopic aspiration; (b) two subjects with bile-duct (T-tube) drainage. The first group eliminated 16.6 +/- 7.8% (mean +/- S.D.) of the dose in urine over 72 h, the second group 28.6% and 27.5%. Biliary excretion by the latter was 41.9% and 28.3% of the dose, respectively, during the first 24 h after dosing. The metabolites excreted in bile and urine were largely polar conjugates: 1-12% of the 3H was ether extractable. Approx. 70-90% of urinary and biliary 3H was extractable following beta-glucuronidase-arylsulphohydrolase hydrolysis. Both beta-glucuronides and arylsulphates were excreted. Unchanged 3H-EE2 was the principal 3H-labelled component of the glucuronide and arylsulphate fractions of bile, and it was a major component of urinary fractions. 2-Hydroxy-EE2 and 2-methoxy-EE2 were identified as conjugated biliary metabolites.
D000368:Aged; D001192:Arylsulfatases; D001646:Bile / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D004997:Ethinyl Estradiol / Q000378:metabolism* / Q000652:urine; D005260:Female; D005965:Glucuronates / Q000378:metabolism; D005966:Glucuronidase; D006801:Humans; D006868:Hydrolysis; D007700:Kinetics; D008875:Middle Aged; D013463:Sulfuric Acid Esters / Q000378:metabolism; D014316:Tritium
D005965:Glucuronates; D013463:Sulfuric Acid Esters; D014316:Tritium; D004997:Ethinyl Estradiol; D001192:Arylsulfatases; D005966:Glucuronidase