caa a22 4500 475818822 CHVBK 20180406123816.0 cr unu---uuuuu 170329e20001101xx s 000 0 eng 10.1007/s002280000197 doi (NATIONALLICENCE)springer-10.1007/s002280000197 Pharmacokinetics of quercetin from quercetin aglycone and rutin in healthy volunteers [Elektronische Daten] [I. Erlund, T. Kosonen, G. Alfthan, J. Mäenpää, K. Perttunen, J. Kenraali, J. Parantainen, A. Aro] Abstract.: Background: Quercetin is a flavonoid with a wide range of biological activities. It mainly occurs in plants as glycosides, such as rutin (quercetin rutinoside) in tea. Quercetin and rutin are used in many countries as vasoprotectants and are ingredients of numerous multivitamin preparations and herbal remedies. Objectives: The primary objective was to characterise and compare the absorption and the pharmacokinetics of quercetin from quercetin aglycone and rutin. A secondary objective was to investigate which forms of quercetin are present in plasma. Methods: In this double blind, diet-controlled, two-period cross-over study, 16 healthy volunteers received three different doses of quercetin and rutin orally. The doses corresponded to 8mg, 20mg and 50mg quercetin aglycone. Blood samples were obtained between 0h and 32h post-dose. Results: The overall kinetic behaviour of quercetin differed remarkably after ingestion of quercetin aglycone or rutin. The mean area under the plasma concentration-time curve from 0h to 32h [AUC(0-32)] and maximum plasma concentration (Cmax) values of the two treatments were similar. However, time to reach Cmax (tmax) was significantly shorter after the quercetin aglycone treatment than after the rutin treatment (1.9, 2.7 and 4.8 versus 6.5, 7.4 and 7.5h, for doses 1, 2 and 3, respectively). Also, the absorption of quercetin from quercetin aglycone was predictable and inter-individual variation was small. In contrast, after ingestion of rutin, inter-individual variations in AUC(0-32) and Cmax values were considerable and seemed to be associated with gender and use of oral contraceptives. Quercetin and rutin were found in plasma as glucuronides and/or sulfates of quercetin and as unconjugated quercetin aglycone, but no rutin was detected. Conclusions: In clinical trials, studying the effects of quercetin from rutin, bioavailability must be taken into consideration and plasma quercetin concentrations monitored. Whether our results apply to other glycosidic drugs as well, especially other rutosides, should be investigated. Springer-Verlag, 2000 Quercetin Rutin Flavonoids nationallicence Erlund I. Department of Nutrition, National Public Health Institute (KTL), Mannerheimintie 166, FIN-00300, Helsinki, Finland aut Kosonen T. Clinical Research, Leiras Oy, Pasilanraitio 9, PO Box 325, FIN-00101, Helsinki, Finland aut Alfthan G. Department of Nutrition, National Public Health Institute (KTL), Mannerheimintie 166, FIN-00300, Helsinki, Finland aut Mäenpää J. Clinical Research, Leiras Oy, Pasilanraitio 9, PO Box 325, FIN-00101, Helsinki, Finland aut Perttunen K. Clinical Research, Leiras Oy, Pasilanraitio 9, PO Box 325, FIN-00101, Helsinki, Finland aut Kenraali J. Clinical Research, Leiras Oy, Pasilanraitio 9, PO Box 325, FIN-00101, Helsinki, Finland aut Parantainen J. Clinical Research, Leiras Oy, Pasilanraitio 9, PO Box 325, FIN-00101, Helsinki, Finland aut Aro A. Department of Nutrition, National Public Health Institute (KTL), Mannerheimintie 166, FIN-00300, Helsinki, Finland aut European Journal of Clinical Pharmacology Springer-Verlag 56/8(2000-11-01), 545-553 0031-6970 56:8<545 2000 56 228 https://doi.org/10.1007/s002280000197 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s002280000197 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Erlund I. Department of Nutrition, National Public Health Institute (KTL), Mannerheimintie 166, FIN-00300, Helsinki, Finland aut NATIONALLICENCE 700 1- Kosonen T. Clinical Research, Leiras Oy, Pasilanraitio 9, PO Box 325, FIN-00101, Helsinki, Finland aut NATIONALLICENCE 700 1- Alfthan G. Department of Nutrition, National Public Health Institute (KTL), Mannerheimintie 166, FIN-00300, Helsinki, Finland aut NATIONALLICENCE 700 1- Mäenpää J. Clinical Research, Leiras Oy, Pasilanraitio 9, PO Box 325, FIN-00101, Helsinki, Finland aut NATIONALLICENCE 700 1- Perttunen K. Clinical Research, Leiras Oy, Pasilanraitio 9, PO Box 325, FIN-00101, Helsinki, Finland aut NATIONALLICENCE 700 1- Kenraali J. Clinical Research, Leiras Oy, Pasilanraitio 9, PO Box 325, FIN-00101, Helsinki, Finland aut NATIONALLICENCE 700 1- Parantainen J. Clinical Research, Leiras Oy, Pasilanraitio 9, PO Box 325, FIN-00101, Helsinki, Finland aut NATIONALLICENCE 700 1- Aro A. Department of Nutrition, National Public Health Institute (KTL), Mannerheimintie 166, FIN-00300, Helsinki, Finland aut NATIONALLICENCE 773 0- European Journal of Clinical Pharmacology Springer-Verlag 56/8(2000-11-01), 545-553 0031-6970 56:8<545 2000 56 228 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer