ABSORPTION, METABOLISM AND EXCRETION OF IBUPROFEN IN BEAGLE DOGS AND RABBITS

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Absorption, metabolism and excretion of ibuprofen were examined in rabbits and beagle dogs. Two metabolism of ibuprofen were prepared by preparative thin layer chromatography from rabbit urine. They were characterized as 2, 4'-(2-hydroxy-2-methylpropyl) phenylpropionic acid (IPH-A) and 2, 4'-(2-carboxypropyl) phenylpropionic acid (IPC) by NMR and IR. Beagle dogs were administered a single oral dose of 50 mg/kg of ibuprofen tablets. Ibprofen and IPH-A were detected in blood and urine. A peak level of ibuprofen (65.78±26.06 μg/ml) in plasma was observed at 4 hours after drug administration. The drug was detected in plasma up to 24 hours. A peak level of IPII-A (5.69±5.30 μg/ml) in plasma was observed at 6 hours after drug administration. The IPH-A peak was attained 2 hours after that of ibuprofen, and IPH-A detected was only one-21st of the ibuprofen peak level. In the urine, ibuprofen and IPH-A were detected on day 1 and 2, and 90.4% of them were excreted on day 1. Of the administered dose, 2.03±2.57% of the ibuprofen and 7.06±4.00% of the IPH-A were excreted. IPC could not be detected in this procedure. For determination of ibuprofen and metabolites, UV absorption was detected directly on thin layer chromatogram spots by densitometer.
名古屋市立大学の論文
1977-11-28