Pharmacokinetic study in dogs and monkeys after single intravenous and oral administrations of [14C]-ITF-296

• Published in: European journal of drug metabolism and pharmacokinetics Vol. 23; no. 2; pp. 239 - 250
• Main Authors: GIACHETTI, C, BERTOLINO, M, CANALI, S, LOMBARDINI, E, MONZANI, M. V, SALA, A, ZANOLO, G
• Format: Conference Proceeding Journal Article
• Language: English
• Published: Genève Médecine et hygiène 01.04.1998
• Subjects: Absorption; Administration, Oral; Animals; Antianginal agents. Coronary vasodilator agents; Benzoxazines; Biological and medical sciences; Carbon Radioisotopes; Cardiovascular system; Dogs; Injections, Intravenous; Ischemia - prevention & control; Macaca fascicularis; Male; Medical sciences; Nitrates - blood; Nitrates - pharmacokinetics; Oxazines - blood; Oxazines - pharmacokinetics; Pharmacology. Drug treatments; Antianginal agent; Fissipedia; Carnivora; Intravenous administration; Single dose; Monkey; Oral administration; Vertebrata; Mammalia; Animal; Organic nitrate; Primates; Pharmacokinetics; Dog
• ISSN: 0378-7966; 2107-0180
• DOI: 10.1007/BF03189346

Pharmacokinetics of [14C]-ITF-296 and its metabolites, ITF-1124 and ITF-1577, were studied in dogs and monkeys after a single intravenous (2.5 mg/kg) and oral (10 mg/kg) administration. Radioactivity was measured by LSC while unchanged drug and its metabolites in plasma were assayed by an HPLC-UV method. The absorption of [14C]-ITF-296 after oral administration is practically complete both in dogs and in monkeys. The determination of unchanged drug and its metabolites shows quite a similar profile in dogs and monkeys for ITF-296 and ITF-1124 and a different time-course for ITF-1577. Elimination of radioactivity occurs mainly in urine (namely 70-80%) for both species and the recovery of the dose (higher than 90%) takes place up to 96 h after both treatments.