PMID: 7236873Jan 1, 1981Paper

Pharmacokinetics of drugs in blood. I. Unusual distribution of gentamicin

Biopharmaceutics & Drug Disposition
M G LeeW L Chiou

Abstract

Distribution kinetics of gentamicin in whole blood were studied. After spiking human blood to an initial concentration of 20 microgram ml-1, plasma gentamicin concentrations dropped to minima at about 5 min then increased to maxima at about 15 min and remained constant afterwards. A difference of up to 36 per cent between the maximum and minimum was found. The equilibration was faster with lower initial concentrations. These unusual distribution phenomena might be attributed to the Schiff base formation between nonprotonated amino groups of gentamicin and free fatty aldehyde groups on blood cell membrane. The mean equilibrium blood cells/plasma partition ratio was about 0.1. Similar equilibration kinetics were observed with blood of rabbits after being intravenously dosed with gentamicin. Therefore, the time elapsed between the collection and centrifugation of blood samples, especially shortly after dosing, may have a significant effect on the 'measured' plasma gentamicin concentration. Distribution between plasma and blood cells may also occur in a similar manner with other drugs which have primary amino groups. It is recommended that distribution kinetics of drugs and metabolites in blood be included in pharmacokinetic studies.

References

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Citations

Nov 1, 1994·Journal of Pharmacological and Toxicological Methods·P M BungayP Krindel
Sep 11, 2012·Journal of Pharmaceutical Sciences·Trudy RodgersMalcolm Rowland
Jul 30, 2009·Biopharmaceutics & Drug Disposition·Young H ChoiM G Lee
Aug 1, 1988·Journal of Clinical Pharmacology·R D ColucciR J Greenstein
Apr 19, 2016·Expert Opinion on Drug Metabolism & Toxicology·Suzanne L ParkerJason A Roberts
Mar 1, 1991·Journal of Veterinary Pharmacology and Therapeutics·S A Brown, J E Riviere
Dec 1, 1982·Journal of Pharmaceutical Sciences·M L ChenW L Chiou
Oct 1, 1995·Biopharmaceutics & Drug Disposition·S H Lee, M G Lee
Jul 1, 1988·Biopharmaceutics & Drug Disposition·P A Cossum
Jun 4, 2010·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Y H ChoiM G Lee
Apr 1, 1985·Journal of Pharmacokinetics and Biopharmaceutics·C Y LuiW L Chiou

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