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DOI: 10.1055/s-0030-1271120
© Georg Thieme Verlag KG Stuttgart · New York
Absolute/Relative Bioavailability and Metabolism of Dodeca-2E,4E,8Z,10E/Z-Tetraenoic Acid Isobutylamides (Tetraenes) after Intravenous and Oral Single Doses to Rats
Publikationsverlauf
received February 12, 2011
revised April 17, 2011
accepted April 26, 2011
Publikationsdatum:
20. Mai 2011 (online)
![](https://www.thieme-connect.de/media/plantamedica/201116/lookinside/thumbnails/10.1055-s-0030-1271120-1.jpg)
Abstract
The present study assessed the absolute and relative bioavailabilities of dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides (tetraenes), the main bioactive constituents in Echinacea, administered as pure compounds or in the form of an Echinacea purpurea root extract preparation. Tetraenes were administered orally by gavage or intravenously in a dose of 0.75 mg/kg. The extract was administered orally in a dose of 158.6 mg/kg which corresponds to the same amount of tetraenes. Pharmacokinetic parameters of tetraenes were calculated by non-compartmental analysis using WinNonlin® 5.2 software. Mean dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamide dose-normalized plasma area under the concentration-time curve (AUC0–∞/dose) was 3.24 ± 0.32 min · ng/mL/µg and 0.95 ± 0.16 min · ng/mL/µg after iv and oral administrations, respectively, and 1.53 ± 0.18 min · ng/mL/µg after oral administration of the Echinacea root extract. The absolute oral bioavailability of dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides was 29.2 ± 2.3 %, which was increased to 47.1 ± 7.2 % (1.6-fold) by administration of the Echinacea extract. Administration of an Echinacea extract increased blood exposure with no impact on Cmax, but prolonged the elimination half-life to 123.3 ± 15.7 min in comparison to 35.8 ± 6.5 min after administration of the pure dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides.
Key words
Echinacea - Asteraceae - dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides - absolute bioavailability - relative bioavailability - LC-MS
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Dr. Veronika Butterweck, Associate Professor of Pharmaceutics
Department of Pharmaceutics, College of Pharmacy
University of Florida
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Gainesville, Florida 32610
USA
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