Effects of glucose, fructose and 5-hydroxymethyl-2-furaldehyde on the presystemic metabolism and absorption of glycyrrhizin in rabbits

Authors: Y.C. Hou1; H. Ching2; P.D.L. Chao3; S.Y. Tsai3; K.C. Wen4; P.H. Hsieh2; S.L. Hsiu3

Source: Journal of Pharmacy and Pharmacology, Volume 57, Number 2, February 2005 , pp. 247-251(5)

Publisher: Pharmaceutical Press

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Abstract:

Our previous study reported that co-administration of honey significantly increased the serum levels of glycyrrhetic acid (GA) after oral administration of glycyrrhizin (GZ) in rabbits. The components of honey are sucrose, glucose, fructose and 5-hydroxymethyl-furaldehyde (HMF). To clarify the causative component(s) in honey that altered the metabolic pharmacokinetics of GZ, rabbits were given GZ (150 mg kg–1) with and without glucose (5 g/rabbit), fructose (5 g/rabbit) and HMF (1 mg kg–1), respectively, in crossover designs. An HPLC method was used to determine concentrations of GZ and GA in serum as well as GA and 3-dehydroglycyrrhetic acid (3-dehydroGA) in faeces suspension. A noncompartment model was used to calculate the pharmacokinetic parameters and analysis of variance was used for statistical comparison. Our results indicated that the area under curve (AUC) of GA was significantly increased by 29% when HMF was coadministered, whereas the pharmacokinetics of GZ and GA were not significantly altered by coadministration of glucose or fructose. An in-vitro study, using faeces to incubate GZ and GA individually, indicated that HMF significantly inhibited the oxidation of GA to 3-dehydroGA and this may explain the enhanced GA absorption in-vivo. It was concluded that HMF is the causative component in honey that affects the presystemic metabolism and pharmacokinetics of GZ in-vivo.

Document Type: Short communication

DOI: 10.1211/0022357055281

Affiliations: 1: School of Chinese Medicine, China Medical University, Taichung, Taiwan, 404, R.O.C. 2: Institute of Chinese Pharmaceutical Sciences, China Medical University, Taichung, Taiwan, 404, R.O.C. 3: School of Pharmacy, China Medical University, Taichung, Taiwan, 404, R.O.C. 4: School of Cosmeceutics, China Medical University, Taichung, Taiwan, 404, R.O.C.

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