US 11,911,480 B2
Self-emulsifying composition of ω-3 fatty acid
Hiromitsu Ito, Tokyo (JP); Hirosato Fujii, Tokyo (JP); and Motoo Yamagata, Tokyo (JP)
Assigned to MOCHIDA PHARMACEUTICAL CO., LTD., Tokyo (JP)
Filed by MOCHIDA PHARMACEUTICAL CO., LTD., Tokyo (JP)
Filed on Jul. 17, 2020, as Appl. No. 16/931,592.
Application 16/931,592 is a continuation of application No. 15/545,197, granted, now 10,758,622, previously published as PCT/JP2015/051558, filed on Jan. 21, 2015.
Prior Publication US 2020/0345852 A1, Nov. 5, 2020
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 47/44 (2017.01); A23L 33/12 (2016.01); A61K 9/00 (2006.01); A61K 9/107 (2006.01); A61K 9/48 (2006.01); A61K 31/202 (2006.01); A61K 31/232 (2006.01); A61K 47/24 (2006.01); A61K 47/26 (2006.01)
CPC A61K 47/44 (2013.01) [A23L 33/12 (2016.08); A61K 9/0053 (2013.01); A61K 9/107 (2013.01); A61K 9/1075 (2013.01); A61K 9/48 (2013.01); A61K 9/4858 (2013.01); A61K 9/4866 (2013.01); A61K 9/4875 (2013.01); A61K 31/202 (2013.01); A61K 31/232 (2013.01); A61K 47/24 (2013.01); A61K 47/26 (2013.01); A23V 2002/00 (2013.01)] 12 Claims
 
1. A self-emulsifying preparation containing a self-emulsifying composition encapsulated in a capsule, the self-emulsifying composition comprising, when total amount of the self-emulsifying composition is 100% by weight,
(a) 50 to 95% by weight of at least one compound selected from the group consisting of eicosapentaenoic acid (EPA) and pharmaceutically acceptable salts and esters thereof,
(b) 0.5 to 6% by weight of water,
(c) 1 to 29% by weight of an emulsifier which is a nonionic surfactant,
(d) a content of polyhydric alcohol is up to 4% by weight of total amount of the composition,
(e) a content of ethanol is up to 4% by weight of total amount of the composition, and
(f) 3 to 40 parts by weight of lecithin in relation to 100 parts by weight of the at least one compound selected from the group consisting of EPA and pharmaceutically acceptable salts and esters thereof,
which upon administration to human satisfies at least one selected from among following (g) to (k) calculated by conducting a correction by subtracting plasma EPA concentration before the administration:
(g) maximum plasma EPA concentration is at least 50 μg/mL;
(h) plasma EPA concentration 2 hours after the administration is at least 20 μg/mL;
(i) time required to reach the maximum plasma EPA concentration (Tmax) is up to 6 hours;
(j) area under the curve of the plasma EPA concentration at 0 to 72 hours after the administration is at least 500 μg·hr/mL; and
(k) blood EPA concentration 24 hours after the administration is 5 to 100 μg/mL.