Summary
The kinetics of14C-metformin have been studied in five healthy subjects after oral and intravenous administration. The intravenous dose was distributed to a small central compartment of 9.9±1.61 (\(\bar X\)±SE), from which its elimination could be described using three-compartment open model. The elimination half-life from plasma was 1.7±0.1 h. Urinary excretion data revealed a quantitatively minor terminal elimination phase with a half-life of 8.9±0.7 h. After the intravenous dose, metformin was completely excreted unchanged in urine with a renal clearance of 454±47 ml/min. Metformin was not bound to plasma proteins. The concentration of metformin in saliva was considerably lower than in plasma and declined more slowly. The bioavailability of metformin tablets averaged 50–60%. The rate of absorption was slower than that of elimination, which resulted in a plasma concentration profile of “flip-flop” type for oral metformin.
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Pentikäinen, P.J., Neuvonen, P.J. & Penttilä, A. Pharmacokinetics of metformin after intravenous and oral administration to man. Eur J Clin Pharmacol 16, 195–202 (1979). https://doi.org/10.1007/BF00562061
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DOI: https://doi.org/10.1007/BF00562061