Purpose: Licorice and honey-treated licorice are widely used in clinical Chinese medicine. Our previous study indicated that honey significantly altered the presystemic metabolism and pharmacokinetics of glycyrrhizin (GZ) in rabbits. This study aimed to investigate the causative component in honey. Methods: Rabbits were given GZ with and without glucose, fructose or 5-hydroxymethyl-furaldehyde (HMF), respectively, in crossover designs. HPLC method was used for the determination of concentrations of GZ and glycyrrhetic acid (GA) in serum as well as GA and 3-dehydroGA in feces suspension. Noncompartment model was used for the calculation of pharmacokinetic parameters and ANOVA was used for statistical comparison. Results: The pharmacokinetics of GZ and GA were not significantly altered when glucose or fructose was coadministered, whereas the AUC of GA was significantly increased by 29 % when HMF was coadministered. In vitro study using feces to incubate GZ or GA indicated that the oxidation of GA to 3-dehydroGA was significantly inhibited in the presence of HMF and it might result in more GA available for absorption. Conclusions: HMF was the causative component in honey that affected the presystemic metabolism and pharmacokinetics of GZ and might increase the toxicity of GZ.
關聯:
2nd World congress of the board of Pharmaceutical sciences of FIP
