Metabolic disposition of prostaglandin E1 in man.

Metabolism of [17, 18-3H]prostaglandin E1 was investigated in three healthy male volunteers during intravenous infusion. The infusion rate was 5.0 ng/kg per min. Blood samples were obtained before the end of the infusion as well as 5, 10, 20, 40, 90 and 180 min afterwards; urine and feces were collected until 96 and 72 h, respectively, after the experiment. All samples were analyzed for radioactivity. Urine was further chromatographed, including by high-pressure liquid chromatography, and subsequently analyzed by gas chromatography-mass spectrometry. Radioactivity in plasma rapidly declined during the first 10 min after termination of the infusion, and then was eliminated exponentially with a mean half-life of 181 min, probably reflecting slow excretion of one or more metabolite. 12% of the administered radioactivity could be recovered from feces and 88% from urine. From the radioactive material obtained from urine the following metabolites could be identified (each number represents data of one volunteer): 7 alpha-hydroxy-5,11-diketotetranor-prostane-1,16-dioic acid (10.4, 20.4 and 30.1%), 7 alpha-hydroxy-5,11-diketotetranor-prostanoic acid (8.2, 6.9 and 9.3%), 5 alpha, 7 alpha-dihydroxy-11-ketotetranor-prostane-1,16-dioic acid and its delta-lactone (together accounting for 4.1, 2.1 and 3.8%).