ISOLATION AND IDENTIFICATION OF BETA-HYDROXYETHYLAPROPHEN - A URINARY METABOLITE OF APROPHEN IN RATS

The metabolism of the anticholinergic drug aprophen was studied in rats after oral administration via stomach intubation. Beta-Hydroxyethylaprophen, a major urinary metabolite of aprophen, was isolated and identified by normal-phase high-performance liquid chromatography and electron ionization mass spectrometry. More than 22% of the parent drug was recovered and quantified over a 72-h collection period. Results show that 2,2-diphenylpropionic acid, another major metabolite of aprophen which lacks anti-cholinergic properties, was also isolated and identified in this study. Experiments are currently underway to synthesize and test the anticholinergic properties of beta-hydroxyethylaprophen in mammals.