STABLE MICELLES OF FATTY ACID ESTERS

摘要

Described herein are compositions comprising 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 composition which forms stable micelles upon contact with an aqueous medium, said composition comprising:
a. from about 40% (wt/wt)—about 95% (wt/wt) of at least one omega-3 fatty acid ester or a derivative thereof, selected from the group consisting of (all-Z omega-3)-5,8,11,14,17-eicosapentaenoic acids (EPA) ester, (all-Z omega-3)-4,7,10,13,16,19-docosahexaenoic acids (DHA) ester, hexadecatrienoic acid (“HTA” or 16:3 (n-3), or all-Z-7,10,13-hexadecatrienoic acid), α-linolenic acid (“ALA” or 18:3 (n-3), or all-Z-9,12,15-octadecatrienoic acid), stearidonic acid (“SDA” or 18:4 (n-3) or all-Z-6,9,12,15-octadecatetraenoic acid), eicosatrienoic acid (“ETE” or 20:3 (n-3) or all-Z-11,14,17 eicosatrienoic acid), eicosatetraenoic acid (“ETA” or 20:4 (n-3), heneicosapentaenoic acid (“HPA” or 21:5 (n-3) or all-Z-6,9,12,15,18-heneicosapentaenoic acid), docosapentenoic acid (“DPA”, or clupanodonic acid or 22:5 (n-3) or all-Z-7,10,13,16,19-docosapentenoic acid), tetracosapentenoic acid (24:5 (n-3) or all-Z-9,12,15,18,21-tetracosapentenoic acid), and tetracosahexaenoic acid (nisinic acid or 24:6 (n-3) and all-Z-6,9,12,15,18,21-tetracosahexaenoic acid; b. a surface active agent which comprises, in combination, at least one non-ionic polyoxyethylene glycol sorbitan alkyl ester (a polysorbate) selected from the group consisting of polyoxyethylene (20) sorbitan monolaurate (polysorbate 20), polyoxyethylene (20) sorbitan monopalmitate (polysorbate 40), (polyoxyethylene (20) sorbitan monostearate (polysorbate 60) and polyoxyethylene (20) sorbitan monooleate (polysorbate 80); and a block copolymer of polyethylene glycol and polypropylene glycol having the formula [(HO(C2H4O)64 (C3H6O)37 (C2H4O)64H] (Poloxamer 237); wherein said polysorbate is present in an amount within the range of about 15% (wt/wt) to about 99% (wt/wt) of said composition; and said Poloxamer 237 is present in an amount within the range of about 0.05% (wt/wt) to about 50% (wt/wt) of said composition; whereby said combination of surface active agents are effective to form said stable micelles upon contact with said aqueous medium.