Pharmacokinetics and bioavailability of the flavonol quercetin in humans

Abstract

Flavonoids are plant polyphenolic compounds present in the daily diet. Latest epidemiological studies point to a crucial role of the flavonol quercetin in the prevention of cardiovascular diseases. It is assumed that this protective effect derives from the antioxidative capacity which quercetin shows in in vitro experiments. The antiproliferative and antimutagenic activities in vitro have made it a candidate for clinical trials in cancer therapy. Quercetin is also regarded as a putative active compound in various phytopharmaceuticals. However, in vivo data on the disposition, absorption, bioavailability, and metabolism of quercetin after intravenous and oral administration in humans are scarce and contradictory. The pharmacokinetic parameters following intravenous injection were determined in two studies. The elimination half-life was reported to be 2.4 h and 0.7 h, the volume of distribution at steady-state was 92.6 l and 6.2 l, and total body clearance was 34.6 lxh(-1) and 28.1 lxh(-1), respectively. Absorption after oral administration ranged from 0 to over 50% of the dose. These inconsistencies can partly be attributed to a lack of highly sensitive and specific assay methodology. The data available so far are insufficient to clarify whether or not quercetin can be held responsible for any protective or curative effect observed after oral intake.