The bioavailability of chlorogenic acid, a major polyphenol of the human diet that is particularly abundant in coffee and various fruits, was explored in rats. To identify the form under which it is absorbed through the gut mucosa and the site of absorption along the gastrointestinal tract, rats were fed a diet supplemented with chlorogenic acid (0.25%, wt:wt). Chlorogenic acid and its metabolites were estimated in the stomach, small intestine and cecal contents as well as in bladder urine and plasma by HPLC with coulometric detection at several time points (1.5, 3, 4.5, and 7 h) after the beginning of the meal. Minor hydrolysis of chlorogenic acid (<1%) occurred in the stomach and small intestine contents, whereas 15-32% of ingested chlorogenic acid was hydrolyzed into caffeic acid in the cecum. Chlorogenic acid and caffeic acid appeared early (at 1.5 h) in plasma and urine, suggesting an absorption of chlorogenic acid into the upper part of the gastrointestinal tract. Gastric absorption of chlorogenic acid was further examined by infusing chlorogenic acid in the ligated stomach of food-deprived rats. After 30 min of infusion, intact chlorogenic acid was found in the gastric vein and aorta. No other metabolites could be detected by HPLC-electrospray ionization-MS-MS. These results show for the first time that chlorogenic acid is quickly absorbed in the rat stomach in its intact form.