Title: Metabolic fate of Sodium 5-(acetylamino)-3,5-dideoxy-D-glycero-D-galacto-2-nonulosonate (KI-111). (I): Absorption, distribution, metabolism and excretion in rats.
Abstract: The absorption, distribution, metabolism and excretion of 14C-labelled Sodium 5-(acetylamino)-3, 5-dideoxy-D-glycero-D-galacto-2-nonulosonate (KI-111) were studied in rats following the intratracheal administration.The half-life of pulmonary absorption of KI-111 was 1.42 hour and the elimination half-life of KI-111 estimated from the urinary excretion data was found to be about 1.44 hour. The plasma levels of radioactivity reached the maximum at 1.5 hour after administration of KI-111. The peak concentration of the compound in the plasma was observed at 1.5 hour after administration, and then decreased with a half-life of 3.7 hours.The compound was excreted mainly in the urine. Within 24 hours, the urinary excretion amounted to 99.8% of the dose. Within 6 hours, a biliary excretion was not observed. Metabolites in the urine were analyzed by HPLC. Ninety eight % of the radioactivity present in the urine was recovered as the unchanged compound and 2 % of as N-acetylmannosamine.After the intravenous administration of KI-111 to rats, the plasma levels of KI-111 decreased biphasically with a corresponding half-lives of 1.5 minutes and 22.4 minutes. And three hours after i.v. administration, the KI-111 was not detected in the plasma.