ABSORPTION, DISTRIBUTION AND EXCRETION OF PIPEMIDIC ACID

Abstract

Pipemidic acid (PPA) was well absorbed by the oral route. When administered to mice, rats, dogs, monkeys and men at a single oral dose of about 50 mg/kg, average plasma levels reached peaks ranging between 4.7 and 11.9 μg/ml. About 20% of PPA was bound to proteins in dog plasma and about 30% in human serum. PPA was widely distributed to various organs and tissues at concentrations comparable to or higher than the plasma level. Peak urine levels of PPA were around 1, 000 μg/ml in animals and men, and 24 to 88% of administered doses was recovered from urine for 24 hours. An average recovery from feces was about 25% in men receiving a single oral dose of 1 g. A main active principle in plasma and urine was unchanged PPA itself.