# US 2019/0167802 A1 · Self-emulsifying composition of omega3 fatty acid > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2019/0167802 A1 - Document ID: US20190167802A1 - Status: Published application - Kind: A1 - Application number: 16/272,713 - Filed: 2019-02-11 - Published: 2019-06-06 - Earliest claimed: 2015-01-21 - Assignees: Mochida Pharmaceutical Co., Ltd. - Applicants: Mochida Pharmaceutical Co., Ltd. - Inventors: Hiromitsu ITO; Hirosato FUJII; Motoo YAMAGATA; Daichi TANAKA - Web page: https://patentgrep.com/patent/US20190167802A1 ## CPC - A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14) - A23L 33/12: Fatty acids or derivatives thereof - A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration} - A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)} - A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)} - A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)} - A61K 9/4858: {Organic compounds} - A61K 9/4866: {Organic macromolecular compounds} - A61K 9/4875: {Compounds of unknown constitution, e.g. material from plants or animals (oils, fats, waxes, shellac A61K9/4858)} - A61K 31/202: having three or more double bonds, e.g. linolenic (eicosanoids, e.g. leukotrienes A61K31/557) - A61K 31/232: having three or more double bonds, e.g. etretinate - A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids - A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin - A61P 3/06: Antihyperlipidemics - A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors - A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis - A61P 25/00: Drugs for disorders of the nervous system - A61P 25/04: Centrally acting analgesics, e.g. opioids - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - A61P 35/00: Antineoplastic agents - A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION ## 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. ## Claims ### Claim 1 A method for reducing the side effects of ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters, comprising: administering a self-emulsifying composition, wherein, when the total amount of the self-emulsifying composition is 100% by weight, the composition comprises: (1) a) 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, b) 0.5 to 6% by weight of water, c) 1 to 29% by weight of an emulsifier (not including lecithin), which is preferably polyoxyethylene sorbitan fatty acid ester, d) lecithin at an amount of 3 to 40 parts by weight, or 1 to 25 parts by weight in relation to 100 parts by weight of the at least one compound, and e) a content of ethanol and/or polyhydric alcohol is up to 4% by weight of the total composition; or (2) f) 70 to 90% 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, g) 0.5 to 6% by weight of water, h) 1 to 29% by weight of an emulsifier, i) lecithin at an amount of 3 to 40 parts by weight, or 1 to 25 parts by weight in relation to 100 parts by weight of at least one compound selected from the group consisting of ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters, j) a content of ethanol is up to 4% by weight of the total composition, and k) a content of polyhydric alcohol is up to 4% by weight of the total composition. ### Claim 2 (depends on 1) The method for reducing the side effects according to claim 1, wherein the at least one compound is administered at an individual daily dose of 100 mg to 4000 mg. ### Claim 3 (depends on 1) The method for reducing the side effects according to claim 1, wherein the at least one compound is administered at an individual daily dose of 2000 mg or 4000 mg. ### Claim 4 (depends on 1) The method for reducing the side effects according to claim 1, wherein the at least one compound is administered at an individual daily dose of at least 4000 mg. ### Claim 5 (depends on 1) The method for reducing the side effects according to claim 1, further comprising administering polyoxyethylene castor oil. ### Claim 6 (depends on 1) The method for reducing the side effects according to claim 1, further comprising administering polyoxyethylene castor oil, wherein the polyoxyethylene castor oil is up to 120 parts by weight to 100 parts by weight of an emulsifier. ### Claim 7 (depends on 1) The method for reducing the side effects according to claim 1, wherein the at least one compound is administered once a day. ### Claim 8 (depends on 1) The method for reducing the side effects according to claim 1, wherein the at least one compound is administered under fasting, before the meal, immediately after the meal, or after the meal. ### Claim 9 (depends on 1) The method for reducing the side effects according to claim 1, wherein, when the at least one compound is administered at an individual dose of 500 to 10000 mg once a day under fasting, before the meal, immediately after the meal or after the meal, at least one member selected from the maximum plasma ω3 polyunsaturated fatty acids concentration calculated by correcting the value by subtracting the plasma ω3 polyunsaturated fatty acids concentration before the administration, the plasma ω3 polyunsaturated fatty acids concentration 2 hours after the administration, the time required to reach the maximum plasma ω3 polyunsaturated fatty acids concentration and the area under the curve of the plasma ω3 polyunsaturated fatty acids concentration at 0 to 72 hours after the administration is substantially the same as the corresponding value obtained by administering 1800 mg/day of the ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters immediately after the meal. ### Claim 10 (depends on 1) The method for reducing the side effects according to claim 1, wherein, when the at least one compound is administered at an individual dose of 500 to 10000 mg under fasting, before the meal, immediately after the meal, or after the meal, at least one value selected front the maximum plasma ω3 polyunsaturated fatty acids concentration calculated by correcting the value by subtracting the plasma ω3 polyunsaturated fatty acids concentration before the administration, the plasma ω3 polyunsaturated fatty acids concentration 2 hours after the administration, the time required to reach the maximum plasma ω3 polyunsaturated fatty acids concentration, and the area under the curve of the plasma ω3 polyunsaturated fatty acids concentration at 0 to 72 hours after the administration is 70 to 130% of the corresponding value obtained by administering 1800 mg/day of the at least one compound immediately after the meal. ### Claim 11 (depends on 1) The method for reducing the side effects according to claim 1, wherein, when the at least one compound is administered at an individual dose of 500 to 10000 mg once a day under fasting, before the meal, immediately after the meal, or after the meal, at least one value selected from the maximum plasma ω3 polyunsaturated fatty acids concentration calculated by correcting the value by subtracting the plasma ω3 polyunsaturated fatty acids concentration before the administration, the plasma ω3 polyunsaturated fatty acids concentration 2 hours after the administration, the time required to reach the maximum plasma ω3 polyunsaturated fatty acids concentration the area under the curve of the plasma ω3 polyunsaturated fatty acids concentration at 0 to 72 hours after the administration, the area under the curve of the plasma ω3 polyunsaturated fatty acids concentration at 0 to 24 hours after the administration, maximum ω3PUFA plasma concentration in steady state, minimum ω3PUFA plasma concentration in steady state, and average ω3PUFA plasma concentration in steady state is substantially the same as the corresponding value obtained by administering 1800 mg/day of the ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters immediately after the meal. ### Claim 12 (depends on 1) The method for reducing the side effects according to claim 1, wherein, when the at least one compound is administered at an individual dose of 500 to 10000 mg under fasting, before the meal, immediately after the meal, or after the meal, at least one value selected from the maximum plasma ω3 polyunsaturated fatty acids concentration calculated by correcting the value by subtracting the plasma ω3 polyunsaturated fatty acids concentration before the administration, the plasma ω3 polyunsaturated fatty acids concentration 2 hours after the administration, the time required to reach the maximum plasma ω3 polyunsaturated fatty acids concentration, the area under the curve of the plasma ω3 polyunsaturated fatty acids concentration at 0 to 72 hours after the administration, the area under the curve of the plasma ω3 polyunsaturated fatty acids concentration at 0 to 24 hours after the administration, maximum ω3PUFA plasma concentration in steady stale, minimum ω3PUFA plasma concentration in steady state, and average ω3PUFA plasma concentration in steady state is 70 to 130% of the corresponding value obtained by administering 1800 mg/day of the ω3 polyunsaturated fatty acids and their pharmaceutically acceptable salts and esters immediately after the meal. ### Claim 13 (depends on 1) The method for reducing the side effects according to claim 1, wherein the maximum plasma ω3 polyunsaturated fatty acids concentration is at least 50 μg/mL. ### Claim 14 (depends on 1) The method for reducing the side effects according to claim 1, wherein the plasma ω3 polyunsaturated fatty acids concentration 2 hours after the administration is at least 20 μg/mL. ### Claim 15 (depends on 1) The method for reducing the side effects according to claim 1, wherein the time required to reach the maximum plasma ω3 polyunsaturated fatty acids concentration is up to 6 hours. ### Claim 16 (depends on 1) The method for reducing the side effects according to claim 1, wherein the area under the curve of the plasma ω3 polyunsaturated fatty acids concentration at 0 to 72 hours after the administration is at least 500 μg·hr/mL. ### Claim 17 (depends on 1) The method for reducing the side effects according to claim 1, wherein the area under the curve of the plasma ω3 polyunsaturated fatty acids concentration at 0 to 24 hours after the administration is at least 100 μg·hr/mL. ### Claim 18 (depends on 1) The method for reducing the side effects according to claim 1, wherein the maximum plasma ω3 polyunsaturated fatty acids concentration in steady state is at least 50 μg·hr/mL. ### Claim 19 (depends on 1) The method for reducing the side effects according to claim 1 wherein the minimum plasma ω3 polyunsaturated fatty acids concentration in steady state is at least 10 μg·hr/mL. ### Claim 20 (depends on 1) The method for reducing the side effects according to claim 1, wherein the average ω3 polyunsaturated fatty acids plasma concentration in steady state is at least 30 μg·hr/mL. ### Claim 21 (depends on 1) The method for reducing the side effects according to claim 1, wherein the self-emulsifying composition is encapsulated by a hard capsule and/or a soft capsule. ### Claim 22 (depends on 21) The method for reducing the side effects according to claim 21, wherein the hard capsule and/or the soft capsule comprises gelatin.