Pharmacokinetics and Biotransformation of Beraprost Sodium V : Plasma Level Profile of Beraprost Sodium in Dog

The plasma levels of beraprost sodium and its major metabolites were determined in dogs after oral administration of 3H-labeled beraprost sodium. The major metabolites in the dog plasma were found to be 13, 14-dihydrol-15-oxo-beraprost, 2, 3-dinor-beraprost and 13, 14-dihydro-2, 3-dinor-15-oxo-beraprost as determined by co-chromatography with synthetic reference standards on high-performance liquid chromatography. The plasma concentration of unchanged beraprost sodium increased rapidly, reaching a maximum concentration 20 to 25min (mean value) in males and 10 to 24min (mean value) in females after dosing of 0.008, 0.04 and 0.2mg/kg, and then declined thereafter with a biphasic pattern. The metabolites appeared in the plasma rapidly after dosing and the major metabolite was 13, 14-dihydro-15-oxo-beraprost in both males and females.