Kinetics of kavain and its metabolites after oral application

Abstract Kavain metabolism in humans was the target of this current investigation. In the present study a high-performance liquid chromatographic (HPLC–DAD) assay method for the simultaneous determination of kavain and its main metabolites ( p -hydroxykavain, p -hydroxy-5,6-dehydrokavain and p -hydroxy-7,8-dihydrokavain) in serum and urine was developed and validated. The metabolites were mainly excreted in the form of their conjugates. All kavain metabolites were detectable in serum and urine, except for p -hydroxy-7,8-dihydrokavain, which was found in urine only. Confirmation of the results and identification of the metabolites were performed by LC–MS or LC–MS–MS. Kinetics of kavain and its metabolites in serum were investigated after administration of a single oral dose (800 mg kavain). Within 1 and 4 h after uptake, the serum concentrations ranged between 40 and 10 ng/ml for kavain, 300 and 125 ng/ml for p -hydroxykavain, 90 and 40 ng/ml for o -desmethyl-hydroxy-5,6-dehydrokavain, and 50 and 30 ng/ml for 5,6-dehydrokavain.