Pharmacokinetics of metformin after intravenous and oral administration to man.

Abstract:

:The kinetics of 14C-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 (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.

journal_name

Eur J Clin Pharmacol

authors

Pentikäinen PJ,Neuvonen PJ,Penttilä A

doi

10.1007/BF00562061

subject

Has Abstract

pub_date

1979-09-01 00:00:00

pages

195-202

issue

3

eissn

0031-6970

issn

1432-1041

journal_volume

16

pub_type

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