Pharmacokinetics and Biotransformation of Beraprost Sodium III：Metabolites in Tissues and Enterohepatic Circulation of Beraprost Sodium in Rat

• Published in: Xenobiotic metabolism and disposition Vol. 4; no. 6; pp. 743 - 753
• Main Authors: YUGE, Takuro, HAMASAKI, Tadashi, TANJI, Shoji, HORIBA, Masahiro, MATSUMOTO, Kazuhisa, TAJIMA, Atsuko, OHNO, Kiyotaka
• Format: Journal Article
• Language: English; Japanese
• Published: Japanese Society for the Study of Xenobiotics 1989
• ISSN: 0916-1139
• DOI: 10.2133/dmpk.4.743

The metabolites of beraprost sodium in plasma and tissues, and its biliary excretion and enterohepatic circulation were investigated in male and female rats using 3H-labelled substance. The most predominant metabolite, 2, 3-dinor-beraprost was shown to be distributed mainly in the liver. However, this a-oxidation metabolite was found to be produced in male rats at an apparently higher level than in female rats. On the other hand, as the oxidation of C-15 alcohol is concerned, the females possess higher capacity for this biotransformation process. he study on biliary excretion showed that male rats could excrete more drug, principally as 2, 3-dinor-beraprost, into the bile compared to the female rats. This sex difference in biliary excretion was facilitated by the following enterohepatic circulation. As a result, urinary excretion of beraprost sodium in female rats attained nearly four times of that in male rats. All these results seem to be basically related to the difference in n-oxidation capacity in the liver of both sexes.