Self-emulsifying composition of omega3 fatty acid

Abstract

A self-emulsifying composition contains: 70 to 90% by weight of at least one compound selected from the group consisting of ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters; 0.5 to 6% by weight of water; 1 to 29% by weight of a polyoxyethylene sorbitan fatty acid ester as an emulsifier (optionally including a polyoxyl castor oil, and not including lecithin); and lecithin in an amount of 3 to 40 parts by weight in relation to 100 parts by weight of ω3 polyunsaturated fatty acids and the like. The self-emulsifying composition is excellent in self-emulsifying property, composition dispersibility, emulsion stability, and absorbability, is free from ethanol and polyhydric alcohols or only has such an alcohol added thereto at a reduced concentration, and is useful for foods and pharmaceuticals.

1 . A self-emulsifying composition comprising at least one compound selected from the group consisting of ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters as well as lecithin and/or a polyoxyethylene sorbitan fatty acid ester as an emulsifier, which upon administration to human satisfies at least one selected from among following (a) to (e) calculated by conducting correction by subtracting plasma ω3 polyunsaturated fatty acid concentration before the administration:
 (a) maximum plasma ω3 polyunsaturated fatty acid concentration is at least 50 μg/mL; 
 (b) plasma ω3 polyunsaturated fatty acid concentration 2 hours after the administration is at least 20 μg/mL; 
 (c) time required to reach the maximum plasma ω3 polyunsaturated fatty acid concentration (Tmax) is up to 6 hours; 
 (d) area under the curve of the plasma ω3 polyunsaturated fatty acid concentration at 0 to 72 hours after the administration is at least 500 μg·hr/mL; and 
 (e) blood ω3 polyunsaturated fatty acid concentration 24 hours after the administration is 5 to 100 μg/mL. 
 
     
     
         2 . A self-emulsifying composition according to  claim 1  wherein the at least one compound selected from the group consisting of ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters in the composition to be administered to human is 1000 mg to 10000 mg. 
     
     
         3 . A self-emulsifying composition according to  claim 1  wherein the ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters in the composition to be administered to human are at least one member selected from the group consisting of EPA and their pharmaceutically acceptable salts and esters. 
     
     
         4 . A self-emulsifying composition according to  claim 3  wherein the EPA and their pharmaceutically acceptable salts and esters are an ethyl ester of EPA. 
     
     
         5 . A self-emulsifying composition according to  claim 1  wherein when the composition is administered, the maximum plasma ω3 polyunsaturated fatty acid concentration calculated by conducting the correction by subtracting the plasma ω3 polyunsaturated fatty acid concentration before the administration is at least 50 μg/mL, and the area under the curve of the plasma ω3 polyunsaturated fatty acid concentration at 0 to 72 hours after the administration is at least 500 μg·hr/mL. 
     
     
         6 . A self-emulsifying composition according to  claim 1  wherein, when the composition is administered under fasting, the maximum plasma ω3 polyunsaturated fatty acid concentration calculated by conducting the correction by subtracting the plasma ω3 polyunsaturated fatty acid concentration before the administration is at least three times as high as the maximum plasma ω3 polyunsaturated fatty acid concentration immediately after the meal, or the area under the curve of the plasma ω3 polyunsaturated fatty acid concentration at 0 to 72 hours after the administration is at least twice as large as the area under the curve of the plasma ω3 polyunsaturated fatty acid concentration immediately after the meal. 
     
     
         7 . A self-emulsifying composition according to  claim 1  wherein the composition contains lecithin and a polyoxyethylene sorbitan fatty acid ester as an emulsifier. 
     
     
         8 . A self-emulsifying composition according to  claim 1  wherein the composition further contains polyoxyethylene castor oil as an emulsifier. 
     
     
         9 . A self-emulsifying composition according to  claim 1  wherein the composition containing 1000 mg to 10000 mg of the at least one compound selected from the group consisting of ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters is administered once a day. 
     
     
         10 . A self-emulsifying composition according to  claim 1  wherein the composition contains water.