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SHR Neuro Cancer Cardio Lipid Metab Microb
Ardjomand-Woelkart, K; Kollroser, M; Magnes, C; Sinner, F; Frye, RF; Derendorf, H; Bauer, R; Butterweck, V.
Absolute/relative bioavailability and metabolism of dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides (tetraenes) after intravenous and oral single doses to rats.
Planta Med. 2011; 77(16):1794-1799
Doi: 10.1055/s-0030-1271120
Web of Science
PubMed
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- Co-authors Med Uni Graz
- Kollroser Manfred
- Sinner Frank Michael
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- Abstract:
- The present study assessed the absolute and relative bioavailabilities of dodeca-2 E,4 E,8 Z,10 E/ 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-2 E,4 E,8 Z,10 E/ 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-2 E,4 E,8 Z,10 E/ 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 C(max), 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-2 E,4 E,8 Z,10 E/ Z-tetraenoic acid isobutylamides. © Georg Thieme Verlag KG Stuttgart · New York.
- Find related publications in this database (using NLM MeSH Indexing)
- Administration, Oral -
- Animals -
- Biological Availability -
- Chromatography, Liquid -
- Dose-Response Relationship, Drug -
- Echinacea - chemistry
- Fatty Acids, Unsaturated - administration & dosage
- Fatty Acids, Unsaturated - chemistry
- Fatty Acids, Unsaturated - metabolism
- Fatty Acids, Unsaturated - pharmacokinetics
- Half-Life -
- Injections, Intravenous -
- Male -
- Mass Spectrometry -
- Plant Extracts - administration & dosage
- Plant Extracts - chemistry
- Plant Extracts - metabolism
- Plant Extracts - pharmacokinetics
- Plant Roots - chemistry
- Polyunsaturated Alkamides - administration & dosage
- Polyunsaturated Alkamides - chemistry
- Polyunsaturated Alkamides - metabolism
- Polyunsaturated Alkamides - pharmacokinetics
- Rats -
- Rats, Sprague-Dawley -
- Time Factors -
- Tissue Distribution -
- Find related publications in this database (Keywords)
- Echinacea
- Asteraceae
- dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamides
- absolute bioavailability
- relative bioavailability
- LC-MS