1989 Volume 4 Issue 6 Pages 779-792
The excretion and metabolism of beraprost sodium were investigated in dogs after oral administration of 3H-labeled beraprost sodium.
In males, the orally administered radioactivity was excreted into urine and feces in 14.7% and 73.8% of administered dose, respectively, within 72hrs after dosing. In females, 17.6% and 69.6% of the dose were excreted into urine and feces, respectively.
Beraprost sodium was metabolized by various reactions involving β-oxidation of α-side chain, reduction of C-13 double bond, oxidation of C-15 hydroxy group, ω-oxidation of ω-side chain and taurine conjugation. The major metabolites in urine and feces were 2, 3-dinor-beraprost and 13, 14-dihydro-2, 3-dinor-15-oxo-beraprost, accounting for 25.77% and 9.31% of the total dose in males, and 26.80% and 9.80% in females, respectively, as determined by HPLC. Identified metabolites accounted for 67.23% of the dose in males and 68.84% in females, respectively.
No difference was observed in excretion as well as metabolism between male and female dog.
