US 2020/0345852 A1Published application

Self-emulsifying composition of omega-3 fatty acid

AssigneeMochida Pharmaceutical Co., Ltd.

InventorsHiromitsu ITO, Hirosato FUJII, Motoo YAMAGATA

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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.

Claims14

Dependent claims

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 ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters,
(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 ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters,
which upon administration to human satisfies at least one selected from among following (g) to (k) calculated by conducting correction by subtracting plasma ω3 polyunsaturated fatty acid concentration before the administration:
(g) maximum plasma ω3 polyunsaturated fatty acid concentration is at least 50 μg/mL;
(h) plasma ω3 polyunsaturated fatty acid concentration 2 hours after the administration is at least 20 μg/mL;
(i) time required to reach the maximum plasma ω3 polyunsaturated fatty acid concentration (Tmax) is up to 6 hours;
(j) 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
(k) blood ω3 polyunsaturated fatty acid concentration 24 hours after the administration is 5 to 100 μg/mL.

10 more elements

A self-emulsifying composition comprising, when the total composition is 100% by weight,

a) 50 to 95% by weight of at least one compound selected from the group consisting of ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters,
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 ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters,
which upon administration to human satisfies at least one selected from among following (g) to (k) calculated by conducting correction by subtracting plasma ω3 polyunsaturated fatty acid concentration before the administration:
(g) maximum plasma ω3 polyunsaturated fatty acid concentration is at least 50 μg/mL;
(h) plasma ω3 polyunsaturated fatty acid concentration 2 hours after the administration is at least 20 μg/mL;
(i) time required to reach the maximum plasma ω3 polyunsaturated fatty acid concentration (Tmax) is up to 6 hours;
(j) 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
(k) blood ω3 polyunsaturated fatty acid concentration 24 hours after the administration is 5 to 100 μg/mL.

10 more elements

Dependencies are inferred from the claim text.

Facts

Application: 16/931,592Filed 17 Jul 2020
Priority: 20 Jul 2017
Published: 5 Nov 2020
Term ends: Not estimatedThe source records don’t support an estimate.

Classification25 codes

A61K 47/44
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents…: oils,…
A23L 33/12
Fatty acids or derivatives thereof; Fats or oils: fatty acids or derivatives thereof
A61K 9/0053
Galenical forms characterised by the site of application: mouth and digestive tract, i.e. intraoral and peroral administration
A61K 9/107
Dispersions; Emulsions: emulsions ; Emulsion preconcentrates; Micelles

Family

Application15/545,197Continuation · filed 20 Jul 2017
Application16/931,592Continuation
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US 11,911,480 B2Related patent
US 2017/0368184 A1Published application
US 2020/0345852 A1This patent

From the US filing history. Foreign family members aren’t listed.