The bioavailability and pharmacodynamics of different concentrations of omega-3 acid ethyl esters.
Omega-3 fatty acids have a long history of use as dietary supplements and more recently for therapeutic applications as prescription pharmaceuticals. Achieving a high concentration is critical for developing convenient, practical therapeutic formulations. The objective of the study was to explore the uptake and effects of different concentrations of omega-3 acid ethyl esters. Three different omega-3 concentrations were investigated in a clinical study with 101 subjects. All participants were dosed for 14 days with 5.1g per day of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) ethyl esters provided in three concentrations: 62.5%, 80% and 85% of total fatty acids. Key endpoints of the study were serum phospholipids and standard fasting lipid panels at day 14. Although administered the same quantity of omega-3 fatty acids, the patients taking the more concentrated formulations had higher levels of EPA/DHA in serum phospholipids and greater reductions in serum triglyceride and VLDL cholesterol levels. Total and non-HDL cholesterol were significantly reduced from baseline with all three formulations. In conclusion the concentration of omega-3 fatty acids of the formulations studied had independent effects on the uptake and effect outcomes during short-term administration. Very high concentrations of omega-3 acid ethyl esters (80%) appear to have higher uptake and are more potent for reducing triglycerides (TGs) and VLDL-cholesterol than formulations with lower concentrations.
Bryhn
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M
Pronova Biocare, R&D, Vollsveien 6, N-1327 Lysaker, Norway. morten.bryhn@pronova.com
Hansteen
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H
Schanche
T
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Aakre
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SE
D000293:Adolescent; D000328:Adult; D001682:Biological Availability; D019587:Dietary Supplements; D004281:Docosahexaenoic Acids / Q000008:administration & dosage / Q000493:pharmacokinetics; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D015118:Eicosapentaenoic Acid / Q000008:administration & dosage / Q000493:pharmacokinetics; D004952:Esters / Q000008:administration & dosage / Q000493:pharmacokinetics; D015525:Fatty Acids, Omega-3 / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D008055:Lipids / Q000032:analysis / Q000097:blood; D008297:Male; D008875:Middle Aged; D010599:Pharmacokinetics; D010743:Phospholipids / Q000032:analysis / Q000097:blood
D004952:Esters; D015525:Fatty Acids, Omega-3; D008055:Lipids; D010743:Phospholipids; D004281:Docosahexaenoic Acids; D015118:Eicosapentaenoic Acid