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Pharmacokinetics of drugs in blood I. Unusual distribution of gentamicin
Author(s) -
Lee Myung G.,
Chen MeiLing,
Huang ShiewMei,
Chiou Win L.
Publication year - 1981
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510020110
Subject(s) - gentamicin , pharmacokinetics , chemistry , kinetics , distribution (mathematics) , blood plasma , aminoglycoside , centrifugation , antibiotics , pharmacology , chromatography , biochemistry , medicine , mathematical analysis , physics , mathematics , quantum mechanics
Distribution kinetics of gentamicin in whole blood were studied. After spiking human blood to an initial concentration of 20 μg 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.