薬理と治療

Abstract

Objectives　The objective of the present study was to compare the pharmacokinetics of compound comprising Isoquercitrin included by γ-Cyclodextrin（C-IQC-CD）, and the physically mixed quercetin and dextrin（C-QD）in healthy adult male subjects. Methods　Healthy male volunteers（8 subjects）aged between 22 to 51 years were performed in a non-randomized, double-blind, crossover controlled study, and ingested 1.1 g of C-IQC-CD（i. e. 220 mg Isoquercitrin）or 1.1 g of C-QD（i. e. 143 mg quercetin）with 100 mL water. Blood samples were collected at 0, 0.5,1 , 2, 3, 6, 8, and 24 h after the supplementations. Results　In this crossover study, the overall kinetic behavior of total quercetin metabolites differed remarkably after the ingestion of either C-IQC-CD or C-QD. The area under the curve （AUC）of plasma concentration from 0 to 3 h of C-IQC-CD（15.92±2.15μM・h）was more than 48 times higher compared to C-QD（0.33±0.11μM・h）. and AUC0-24 of C-IQC-CD （36.81±4.3μM・h）was more than 10 times higher compared to C-QD（3.47±1.12μM・h）. Also, the Cmax of C-IQC-CD（10.19±1.52μM）was found about 29 times higher than C-QD （0.35±0.07μM）.Conclusion　Compound comprising Isoquercitrin included by γ-Cyclodextrin（C-IQC-CD） with improved solubility of Isoquercitrin showed a dramatically higher bioavailability than physically mixed quercetin and dextrin（C-QD）. It implies that C-IQC-CD could have the ability to show various biological effects on human health. Their results could be applied to functional foods health supplements, and complementary and alternative medicines after further investigations（. UMIN ID: UMIN000038580）