posted on 2024-01-17, 20:35authored byIvana Kundisová, Helena Colom, M. Emília Juan, Joana M. Planas
The pharmacokinetics (PK) of hydroxytyrosol and its metabolites
were characterized following oral administration to Sprague-Dawley
rats of 3.85 and 7.70 g of destoned Arbequina table olives/kg. Plasma
samples were analyzed using a fully validated method consisting of
liquid extraction followed by liquid chromatography-tandem mass spectrometry
(LC-MS/MS). Noncompartmental PK analysis of hydroxytyrosol demonstrated
linear PK between doses of 2.95 and 5.85 mg hydroxytyrosol/kg. Half-life
was approximately 2.5 h, while mean residence time was around 4 h.
Clearance occurred by conversion to two sulfate and two glucuronide
conjugates. The area under the plasma concentration–time curve
(AUC) ratios of metabolites versus parent hydroxytyrosol was approximately
7–9-fold for the sulfate and below 0.25 for the glucuronide,
indicating sulfation as the predominant metabolic pathway. Despite
extensive metabolism, hydroxytyrosol remained in plasma for up to
8 h with AUCs of 4293 and 8919 min·nmol/L for the doses of 3.85
and 7.70 g/kg, respectively. Therefore, table olives provide a more
sustained plasma profile than other foods containing hydroxytyrosol,
which may enhance its health-protecting activities.