QUANTITATION IN PLASMA AND URINE OF ACEBUTOLOL AND A MAJOR METABOLITE WITH PRELIMINARY-OBSERVATIONS ON THEIR DISPOSITION KINETICS IN MAN

  • 1 January 1976
    • journal article
    • research article
    • Vol. 15  (1) , 31-51
Abstract
An acetyl-homologue-metabolite, present in concentrations of up to ten times those of the unchanged drug, in the plasma of patients receiving oral doses of acebutolol, [a.beta. adrenergic receptor antagonist] is reported. Combined gas chromatography-mass spectrometry was utilized to determine the structure of the acetyl-metabolite. This acetyl-metabolite was measured as acebutolol by previously published non-specific methods for the determination of acebutolol in biological fluids. A specific and sensitive gas chromatographic method is described for the separate quantitation of acebutolol and its acetyl-metabolite in plasma and urine. Using this method, preliminary data on the disposition kinetics of acebutolol are presented. The difficulties in interpreting previously published pharmacokinetic data for acebutolol, based on a non-specific method of analysis, are emphasized.

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