Group Title: BMC Pharmacology
Title: Absolute and relative bioavailabilities of dodeca-2E, 4E, 8E, 10E/Z-tetraenoic acid isobutylamides after intravenous and oral single doses in rats
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 Material Information
Title: Absolute and relative bioavailabilities of dodeca-2E, 4E, 8E, 10E/Z-tetraenoic acid isobutylamides after intravenous and oral single doses in rats
Physical Description: Book
Language: English
Creator: Wölkart, Karin
Frye, Reginald
Derendorf, Hartmut
Butterweck, Veronika
Bauer, Rudolf
Publisher: BMC Pharmacology
Publication Date: 2009
 Notes
General Note: Start page A36
General Note: M3: 10.1186/1471-2210-9-S2-A36
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Bibliographic ID: UF00099948
Volume ID: VID00001
Source Institution: University of Florida
Holding Location: University of Florida
Rights Management: Open Access: http://www.biomedcentral.com/info/about/openaccess/
Resource Identifier: issn - 1471-2210
http://www.biomedcentral.com/1471-2210/9/S2/A36

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Meeting abstract


Absolute and relative bioavailabilities of dodeca-2E, 4E, 8E,
I OE/Z-tetraenoic acid isobutylamides after intravenous and oral
single doses in rats
Karin W1olkart', Reginald Frye2, Hartmut Derendorf3, Veronika Butterweck3
and Rudolf Bauer* I

Address: 'Institute of Pharmaceutical Sciences, Department of Pharmacognosy, Karl Franzens University Graz, 8010 Graz, Austria, 2Department
of Pharmacy Practice, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA and 3Department of Pharmaceutics, College of
Pharmacy, University of Florida, Gainesville, FL 32610, USA
Email: Rudolf Bauer* rudolf.bauer@uni-graz.at
* Corresponding author



from 15th Scientific Symposium of the Austrian Pharmacological Society (APHAR) Joint meeting with the Hungarian Society of Experimental and Clinical
Pharmacology (MFT) and the Slovenian Pharmacological Society (SDF)
Graz, Austria. 19-21 November 2009

Published: 12 November 2009
BMC Pharmacology 2009, 9(Suppl 2):A36 doi:10.1186/1471-2210-9-S2-A36


This abstract is available from: http://www.biomedcentral.com/1471-2210/9/S2/A36
2009 Wolkart et al; licensee BioMed Central Ltd.


Background
Dodeca-2E,4E,8E,10E/Z-tetraenoic acid isobutylamides
are the main alkamides in Echinacea preparations, which
have been demonstrated to possess biological activities in
various bio-assays, such as immune-modulating activities
and effects on cannabinoid receptors [1]. Therefore, the
evaluation of systemic availability of these active plant
constituents is a major prerequisite for the interpretation
of in vitro pharmacological testing. This study assessed the
absolute and relative bioavailabilities of dodeca-
2E,4E,8E, 10E/Z-tetraenoic acid isobutylamides
(tetraenes) administered as pure compounds or as an
Echinacea purpurea root extract preparation.

Methods
Ten rats received 0.75 mg/kg dodeca-2E,4E,8E, 0E/Z-
tetraenoic acid isobutylamides orally, pure and within
158.6 mg/kg Echinacea purpurea extract, or intravenously
to compare the absorption and pharmacokinetic proper-
ties. Pharmacokinetic parameters and bioavailability data
of tetraenes were obtained by non-compartmental analy-
sis (NCA) using WinNonlin 5.2 software.


Results
Mean dodeca-2E,4E,8E,10E/Z-tetraenoic acid isobutyla-
mide plasma area under the concentration-time curve
(AUCo-. per dose) was 3.2 + 0.3 min ng/mL/ ig and 1.0 +
0.2 min-ng/mL/lig after i.v. and oral administration,
respectively, and 1.5 0.2 min-ng/mL/lig after oral
administration of the Echinacea root extract. The absolute
bioavailability of dodeca-2E,4E,8E,10E/Z-tetraenoic acid
isobutylamides was 29%, which was increased to 47%
(1.6 fold) by the administration of an Echinacea extract.
The relative bioavailability was over 100%.

Conclusion
Administration of a whole Echinacea extract increases
blood exposure with no impact on Cmax. The high area
under the curve concentration resulted in a longer elimi-
nation half-life with 123 min in comparison to 36 min
after administration of the pure dodeca-2E,4E,8E,10E/Z-
tetraenoic acid isobutylamides. The approximately 2-fold
higher percentage of relative bioavailability achieved with
the Echinacea root extract resulted in a 3.4 and 3.6 times
higher terminal elimination half-life and mean residence
time (MRT), respectively. A rapid absorption followed by
a slower elimination phase was observed.



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http://www.biomedcentral.com/1471-2210/9/S2/A36


Acknowledgements
Supported by the Erwin-Schrodinger scholarship (FWF)J2754-B05.

References
1. Woelkart K, Bauer R: The role ofalkamides as an active princi-
ple of Echinacea. Planta Med 2007, 73:615-623.


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