Pharmacokinetics and excretion of dalbavancin in the rat

Autor: Luigi Colombo, Simona Riva, Marco Cavaleri, James A. Dowell, Martin Stogniew, Marco Guanci, Anna Valagussa
Rok vydání: 2005
Předmět:
Zdroj: Journal of Antimicrobial Chemotherapy. 55:ii31-ii35
ISSN: 1460-2091
0305-7453
Popis: Objectives: The pharmacokinetics, tissue distribution and excretion routes of dalbavancin, a semi-synthetic glycopeptide, were investigated in rats. Methods: A 20 mg/kg intravenous dose of dalbavancin or [ 3 H]dalbavancin was administered to rats in three studies. Concentrations of dalbavancin or drug-derived radioactivity were assessed in blood, plasma, tissues, bile, urine and faeces by HPLC-MS/MS, scintillation counting or microbiological methods. Results: Dalbavancin decayed tri-exponentially in plasma with an apparent terminal t 1/2 of 187h (approximately 8 days). Dalbavancin has dual routes of elimination, with around two-thirds of the excreted drug-derived radioactivity being found in the urine and around one-third in the faeces. After 70 days, 44.2% and 22.3% of the drug-derived radioactivity had been recovered in the urine and faeces, respectively. Biliary excretion of drug-derived radioactivity accounted for over half of the radioactivity excreted faecally. At 70 days post-dose
Databáze: OpenAIRE