The disposition of clavulanic acid in man
| Autor: | D J Jeffery, G D Allen, B E Davies, G C Bolton, C W Filer |
|---|---|
| Rok vydání: | 1986 |
| Předmět: |
Male
Health Toxicology and Mutagenesis Urine Absorption (skin) Pharmacology Toxicology Biochemistry Clavulanic Acids Excretion Feces Oral administration Clavulanic acid medicine Humans Tissue Distribution Dosing Clavulanic Acid Volume of distribution Chemistry Feces analysis General Medicine Middle Aged Kinetics Injections Intravenous Chromatography Thin Layer medicine.drug |
| Zdroj: | Xenobiotica. 16:853-863 |
| ISSN: | 1366-5928 0049-8254 |
| DOI: | 10.3109/00498258609038967 |
| Popis: | Following oral administration of potassium 14C-clavulanate to four human subjects, at least 73% of the radioactive dose was absorbed. The mean absolute bioavailability was 64%. Absorption was rapid with peak plasma concentrations of radioactivity and clavulanic acid (2-6 micrograms/ml) occurring between 45 min and three hours after dosing. Values for the volume of distribution at steady-state and terminal half-life of clavulanic acid in the plasma were 12.01 and 0.8 h respectively. Following intravenous administration of clavulanic acid to the same subjects, the clearance, and volume of distribution at steady-state were 0.21 l/min, and 12.01, respectively. Clavulanic acid was the major radioactive component present in 0-24 h urine following oral dosing (23% of the dose). The two major metabolites were 2,5-dihydro-4-(2-hydroxyethyl)-5-oxo-1H-pyrrole-3-carboxylic acid (15% of the dose) and 1-amino-4-hydroxybutan-2-one (8.8% of the dose). Clavulanic acid and 1-amino-4-hydroxybutan-2-one were the major components in plasma following oral administration (52 and 21% of plasma radioactivity respectively at two hours after dosing). The major route of excretion of radioactivity following oral administration was via the urine (73% of the dose). Most of this radioactivity was excreted in the first 24 h after dosing (68% of the dose). The renal clearance of clavulanic acid was 0.1 l/min. Elimination of radioactivity also occurred via the expired air (17% of the dose) and the faeces (8% of the dose). |
| Databáze: | OpenAIRE |
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