The Pharmacokinetic Profile of a New Gastroresistant Capsule Preparation of Eicosapentaenoic Acid as the Free Fatty Acid.

Eleonora Scaioli,Mark A Hull,Andrea Belluzzi,Carla Cardamone,Alessandra Munarini,Elisa Liverani

doi:10.1155/2015/360825

Eleonora Scaioli, Mark A Hull + Show 4 more

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https://doi.org/10.1155/2015/360825

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Abstract

Supplementation with n-3 polyunsaturated fatty acids (n-3 PUFAs) may be beneficial for patients with inflammatory bowel diseases (IBD). In this study we analyzed the pharmacokinetic profile of eicosapentaenoic acid (EPA), as the free fatty acid (FFA), in an enteric-coated preparation, in 10 ulcerative colitis (UC) and 10 Crohn's disease (CD) patients and 15 healthy volunteers (HV). Subjects received 2 g daily of EPA-FFA for 8 weeks. Plasma phospholipid and red blood cell (RBC) membrane fatty acid content were measured by gas chromatography-mass spectrometry. There was a rapid incorporation of EPA into plasma phospholipids by 2 weeks and a slower, but highly consistent, incorporation into RBC membranes (4% total fatty acid content; coefficient of variation 10–16%). There was a concomitant reduction in relative n-6 PUFA content. Elongation and desaturation of EPA into docosahexaenoic acid (DHA) via docosapentaenoic acid (DPA) were apparent and DHA content also increased in membranes. EPA-FFA is well tolerated and no difference in the pharmacokinetic profile of n-3 PUFA incorporation was detected between IBD patients and HV. Our data support the concept that EPA can be considered the “universal donor” with respect to key n-3 PUFAs and that this enteric-coated formulation allows long term treatment with a high level of compliance.

Highlights

The major natural dietary source of long-chain n-3 polyunsaturated fatty acids (n-3 Polyunsaturated fatty acids linoleic acid (LA) (PUFAs)) is cold-water, oily fish, which can be consumed safely in large quantities
Written, informed consent was obtained from 20 inflammatory bowel diseases (IBD) patients (10 Crohn’s disease (CD) and 10 ulcerative colitis (UC)), who were in stable clinical remission according to routine clinical scores (Crohn’s Disease Activity Index—CDAI < 150 and Simple Clinical Colitis Activity Index—SCCAI = 0) [18, 19] for at least 3 months, attending the outpatient clinic, and 15 healthy volunteers (HV) recruited among medical students
Baseline plasma and red blood cell (RBC) Polyunsaturated fatty acids LA (PUFAs) profiles in IBD patients and HV are noted in Tables 2 and 3

Summary

Introduction

The major natural dietary source of long-chain n-3 polyunsaturated fatty acids (n-3 PUFAs) is cold-water, oily fish, which can be consumed safely in large quantities. Oral administration of fish oil containing the two main bioactive components C20:5n3 eicosapentaenoic acid (EPA) and C22:6n3 docosahexaenoic acid (DHA) can replace C18:2n6 linoleic acid (LA) and C20:4n6 arachidonic acid (AA) in a time- and dose-dependent manner in plasma and cellular phospholipid membranes [2]. Plasma n-3 PUFA level is the easiest marker of EPA and DHA intake for measuring compliance in taking supplements as various fish oil preparations. The relatively long half-life of the RBC (120 days) provides a more stable measure of the incorporation of fatty acids into cellular phospholipid membranes [9]. The Omega-3 index (the combined percentage EPA, docosapentaenoic acid-DPA, and DHA content in RBC phospholipid membranes) can reach ≥8% with achievable n-3 PUFA intake [10]

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