Intestinal absorption of p-coumaric and gallic acids in rats after oral administration.
Ferulic acid (FA) and p-coumaric acid (CA) are absorbed by the monocarboxylic acid transporter (MCT) in Caco-2 cells, although gallic acid (GA) is not. Therefore, the MCT is selective for certain phenolic acids. Absorption of orally administered CA and GA in rats was studied to obtain serum pharmacokinetic profiles and to investigate their intestinal absorption characteristics in vivo. Rats were administered 100 micromol/kg body weight of CA and GA, and blood was collected from the portal vein and abdominal artery after administration. CA, GA, and their metabolites were quantified with a highly selective and sensitive coulometric detection method using high-performance liquid chromatography-electrochemical detection. Ingested CA was rapidly absorbed in the gastrointestinal tract in an intact form. The serum concentration of intact CA in the portal vein peaked 10 min after dosing (C(max) was 165.7 micromol/L). In contrast, GA was slowly absorbed, with a t(max) for intact GA of 60 min and a C(max) of 0.71 micromol/L. The area under the curve for intact CA and GA was calculated from the serum concentration profile in the portal vein to be 2991.3 and 42.6 micromol min L(-)(1), respectively. The relative bioavailability of CA against GA was about 70. This is the first demonstration that absorption efficiency of CA is much higher than that of GA in vivo. The absorption characteristics of CA are clearly different from those of GA. These findings are in good agreement with the results obtained in vitro using a Caco-2 cell system.
Konishi
Yutaka
Y
Applied Bioresearch Center, Research & Development Department, Kirin Brewery Co., Ltd., 3 Miyaharacho, Takasaki-shi, Gunma 370-1295, Japan. konishiy@kirin.co.jp
Hitomi
Yoshitaka
Y
Yoshioka
Eiji
E
D000005:Abdomen / Q000098:blood supply; D000818:Animals; D001158:Arteries; D002851:Chromatography, High Pressure Liquid; D003373:Coumaric Acids / Q000097:blood / Q000493:pharmacokinetics*; D005707:Gallic Acid / Q000097:blood / Q000493:pharmacokinetics*; D007408:Intestinal Absorption; D008297:Male; D011169:Portal Vein; D011422:Propionates; D051381:Rats; D017207:Rats, Sprague-Dawley
D003373:Coumaric Acids; D011422:Propionates; D005707:Gallic Acid; C495469:p-coumaric acid