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Relative bioavailability of coumarin from cinnamon and cinnamon-containing foods compared to isolated coumarin: A crossover study in human volunteers

Purpose: Cassia cinnamon contains high levels (up to 1%) of coumarin. Heavy consumption of this spice may result in a dose exceeding the tolerable daily intake (TDI) which is derived from toxicological data on isolated coumarin (animal experiments and medicinal drug in humans). In this context, the question was raised whether coumarin in the plant matrix of cinnamon has the same bioavailability as isolated coumarin. Methods: A crossover study was performed, in which the same dose of 12mg coumarin was administered to 24 healthy volunteers. They received four different formulations: isolated coumarin in a capsule (reference), cinnamonin capsules, cinnamon tea prepared from the same cinnamon, and cinnamon in rice pudding as a typical meal. The relative extent of absorption was measured as urinary excretion of the main metabolite 7-hydroxycoumarin (7OHC) within 8 h after application. In order to monitor the velocity of absorption, 7OHC plasma levels were measured for 105 min after administration. Results: Plasma levels of 7OHC revealed a fast absorption of coumarin especially from cinnamon tea leading to the highest peak concentrations. Mean urinary excretion of 7OHC was found to be 62.8% for isolated coumarin in a capsule, 56.0% for cinnamon in capsules, 66.1% for cinnamon tea, and 54.7% for cinnamon in rice pudding. Therefore,the relative extent of absorption of coumarin from powder of cassia cinnamon was only slightly lower than that of isolated coumarin,and the TDI of 0.1 mg/kg bw can be used for risk assessment of coumarin exposure from cinnamon-containing meals.

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