Omega-3 Fatty Acid Ester Compositions

摘要

Described herein are compositions including at least one Omega-3 fatty acid ester and at least one surface active agent; wherein the compositions form micelles when in contact with an aqueous medium. Also provided is a method of administering to a subject a composition comprising at least one Omega-3 fatty acid ester and at least one surface active agent, wherein the at least one Omega-3 fatty acid ester forms micelles when in contact with an aqueous medium, and the bioavailability of the at least one Omega-3 fatty acid ester is substantially independent of a food effect. Said compositions are useful for treating cardiovascular conditions or disorders in a subject and for reducing side effects associated with the ingestion of Omega-3 fatty acid esters. Described are also various dosage forms for administering said compositions and use of said compositions in functional foods. Provided herein are also kits with instructions on how to administer said compositions.

主权项

1. A pharmaceutical composition comprising a mixture of EPA and DHA ethyl esters and at least one surface active agent; wherein the ratio of EPA:DHA is from more than 2:1 to not more than 3.4:1 and wherein said EPA and DHA ethyl esters combined comprise from about 60% (wt/wt) to about 70% (wt/wt) of said composition; wherein said at least one surface active agent comprises from about 15% to about 31% polysorbate 80 and from about 0.5% (wt/wt) to about 5% (wt/wt) of a block copolymer of polyethylene glycol and polypropylene glycol polyoxamer having a chemical formula HO(C2H4O)64(C3H6O)37(C2H6O)37(C2H4O)64H (Pluronic F87); wherein said composition is free of active ingredients other than omega-3 fatty acid esters; and wherein said composition when administered after a single 6 g dose (2,172 mg of EPA+996 mg of DHA) to a human under fed and fasted conditions at equal dosage strengths provides for:
a. a baseline adjusted AUC0-t arithmetic mean under fed conditions for EPA total lipids and DHA total lipids is from about 1495 nmol·hr/ml to about 3569 nmol·hr/m and from about 530 nmol·hr/ml to about 1486 nmol·hr respectively; and b. a baseline adjusted AUC0-t arithmetic mean under fasting conditions for EPA total lipids and DHA total lipids is from about 1169 nmol·hr/mL to about 3239 nmol·hr/ml and from about 647 nmol·hr/ml to about 1615.7 nmol·hr/ml respectively.