Classifications

• • C—CHEMISTRY; METALLURGY
  • C11—ANIMAL OR VEGETABLE OILS, FATS, FATTY SUBSTANCES OR WAXES; FATTY ACIDS THEREFROM; DETERGENTS; CANDLES
  • C11C—FATTY ACIDS FROM FATS, OILS OR WAXES; CANDLES; FATS, OILS OR FATTY ACIDS BY CHEMICAL MODIFICATION OF FATS, OILS, OR FATTY ACIDS OBTAINED THEREFROM
  • C11C3/00—Fats, oils, or fatty acids by chemical modification of fats, oils, or fatty acids obtained therefrom
  • C11C3/04—Fats, oils, or fatty acids by chemical modification of fats, oils, or fatty acids obtained therefrom by esterification of fats or fatty oils
  • C11C3/10—Ester interchange
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23D—EDIBLE OILS OR FATS, e.g. MARGARINES, SHORTENINGS, COOKING OILS
  • A23D7/00—Edible oil or fat compositions containing an aqueous phase, e.g. margarines
  • A23D7/003—Compositions other than spreads
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23D—EDIBLE OILS OR FATS, e.g. MARGARINES, SHORTENINGS, COOKING OILS
  • A23D9/00—Other edible oils or fats, e.g. shortenings, cooking oils
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23K—FODDER
  • A23K20/00—Accessory food factors for animal feeding-stuffs
  • A23K20/10—Organic substances
  • A23K20/158—Fatty acids; Fats; Products containing oils or fats
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23K—FODDER
  • A23K40/00—Shaping or working-up of animal feeding-stuffs
  • A23K40/30—Shaping or working-up of animal feeding-stuffs by encapsulating; by coating
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
  • A23L33/115—Fatty acids or derivatives thereof; Fats or oils
  • A23L33/12—Fatty acids or derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
  • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
  • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
  • A61K31/23—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
  • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
  • C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
  • C07C69/22—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety
  • C07C69/30—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with trihydroxylic compounds
• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
  • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
  • C07C69/52—Esters of acyclic unsaturated carboxylic acids having the esterified carboxyl group bound to an acyclic carbon atom
  • C07C69/587—Monocarboxylic acid esters having at least two carbon-to-carbon double bonds
• • C—CHEMISTRY; METALLURGY
  • C11—ANIMAL OR VEGETABLE OILS, FATS, FATTY SUBSTANCES OR WAXES; FATTY ACIDS THEREFROM; DETERGENTS; CANDLES
  • C11C—FATTY ACIDS FROM FATS, OILS OR WAXES; CANDLES; FATS, OILS OR FATTY ACIDS BY CHEMICAL MODIFICATION OF FATS, OILS, OR FATTY ACIDS OBTAINED THEREFROM
  • C11C1/00—Preparation of fatty acids from fats, fatty oils, or waxes; Refining the fatty acids
  • C11C1/002—Sources of fatty acids, e.g. natural glycerides, characterised by the nature, the quantities or the distribution of said acids
• • C—CHEMISTRY; METALLURGY
  • C11—ANIMAL OR VEGETABLE OILS, FATS, FATTY SUBSTANCES OR WAXES; FATTY ACIDS THEREFROM; DETERGENTS; CANDLES
  • C11C—FATTY ACIDS FROM FATS, OILS OR WAXES; CANDLES; FATS, OILS OR FATTY ACIDS BY CHEMICAL MODIFICATION OF FATS, OILS, OR FATTY ACIDS OBTAINED THEREFROM
  • C11C3/00—Fats, oils, or fatty acids by chemical modification of fats, oils, or fatty acids obtained therefrom
  • C11C3/04—Fats, oils, or fatty acids by chemical modification of fats, oils, or fatty acids obtained therefrom by esterification of fats or fatty oils
  • C11C3/08—Fats, oils, or fatty acids by chemical modification of fats, oils, or fatty acids obtained therefrom by esterification of fats or fatty oils with fatty acids

Definitions

• the invention relates to an emulsion and a use of the emulsion as a parenteral preparation.
• triglyceride is important as a nutrient, especially " for diseased humans, there is a need for an emulsion of 2-eicosapentaenoyl-l,3-dioctanoyl glycerol, which can be used for parenteral nutrition, and which exhibits a better bioavailability than hitherto known parenteral emulsions used as a source for EPA.
• a very important clinical aspect in regard to the bioavailability is the slower metabolism in comparison to emulsions containing MCT, which are known to cause metabolic acidosis when infused intravenously.
• the emulsion according to the invention with an aqueous continuous phase and containing as the discontinous phase the triglyceride 2-eicosapentaenoyl-l,3-dioctanoyl glycerol, is characterized by the fact that it is formulated for parenteral use. Any worker skilled in the art will know in principle how to compose such formulation. Surprisingly it has been found that the emulsion according to the invention exhibits a better bioavailability than hitherto known parenteral emulsions used as a source for EPA.
• the above-mentioned triglycerides turn out, surprisingly, to be very efficient sources of energy in when applied in parenteral nutrition - the EPA acid moiety of the triglycerides being in an optimal position in the molecule in respect to their cleavage by lipoprotein lipase.
• the above triglycerides appear to exhibit physical properties which allow facile formulation of the compounds in liquid products as well as in powdered products exhibiting excellent wetability properties.
• the products of the invention possess excellent stabilities making sterilization of e.g. parenteral products containing the above-mentioned triglycerides reliable, easy and safe.
• the above-mentioned triglycerides are advantageously applied in such emulsions due to their fast conversion by lipoprotein lipase and endothelial lipase and the consequential avoidance of the discomfort and side effects of lipolipaedemia.
• Arachidonic acid applied in above triglycerides is thus cleared quickly and efficiently thereby providing the essential fatty acid concomitantly with short chain acids useful as energy substrates.
• triglycerides in parenteral nutritional products is further particularly advantageous since the relatively high polarity of the triglycerides favour the stability of their emulsions which are subjected to severe heat treatments during their manufacturing. Use of such emulsion is particularly advantageous for nutrition of severely ill patients e.g. post-operatively.
• Another advantage of the products of the invention has to do with the stability of the EPA towards oxidation and thus the avoidance of problems associated with oxidation of polyunsaturated fatty acids. It thus turns out that products according to the invention allows preparation of EPA containing lipids with an improved quality of EPA as compared to other sources of the essential fatty acid. Detrimental processes of polyunsaturated fats and oils leading to negative nutritional forms are thus commonly associated with gastric and intestinal problems due to oxidation and polymerisation products of the polyunsaturated fatty acid. Such oxidized forms of EPA can interfere with nitrogen uptake by interacting with sensitive amino acids. These highly undesired effects are diminished or even avoided by applying triglycerides according to the invention.
• a preferred embodiment of the emulsion according to the invention is characterized by the fact that the average diameter of the triglyceride globules is between 5 and 1000 nm, and that less than 5% of the triglyceride globules exhibits a diameter above 5000 nm.
• This emulsion is well suited as a parenteral emulsion and shows a good bioavailability.
• a preferred embodiment of the emulsion according to the invention is characterized by the fact that the average diameter of the triglyceride globules is between 5 and 1000 nm, that less than 5% of the triglyceride globules exhibits a diameter above 5000 nm, that the amount of the triglyceride in relation to the amount of the entire emulsion is between 2 and 30% by weight, and that the emulsion contains glycerol to isotonicity and 0.2 - 10% by weight of an emulsifier.
• This emulsion is very well suited as a parenteral emulsion and shows a superior absorption ability.
• a preferred emulsifier is a phospholipid.
• a preferred embodiment of the emulsion according to the invention is characterized by the fact that the triglyceride has a purity of at least 10%, preferably at least 30%, more preferably at least 50%, even more preferably at least 75%, and most preferably at least 90%.
• the invention comprises a use of the emulsion according to the invention as a parenteral preparation.
• a parenteral feeding product was prepared according to the following formula:
• the product was filled in a suitable package and sterilized in an autoclave at 120°C for 20 minutes.

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• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Organic Chemistry (AREA)
• Engineering & Computer Science (AREA)
• Health & Medical Sciences (AREA)
• Polymers & Plastics (AREA)
• Oil, Petroleum & Natural Gas (AREA)
• Food Science & Technology (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Wood Science & Technology (AREA)
• Public Health (AREA)
• Zoology (AREA)
• Pharmacology & Pharmacy (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
• Emergency Medicine (AREA)
• Nutrition Science (AREA)
• Diabetes (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Obesity (AREA)
• Mycology (AREA)
• Hematology (AREA)
• Animal Husbandry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Epidemiology (AREA)
• Microbiology (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicinal Preparation (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Coloring Foods And Improving Nutritive Qualities (AREA)
• Fats And Perfumes (AREA)

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ID=8144235

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• 1988
  • 1988-10-11 DK DK565288A patent/DK565288D0/da unknown
• 1989
  • 1989-10-10 EP EP89911778A patent/EP0437518B1/de not_active Expired - Lifetime
  • 1989-10-10 JP JP1510969A patent/JPH04500974A/ja active Pending
  • 1989-10-10 JP JP1510970A patent/JPH04501113A/ja active Pending
  • 1989-10-10 DE DE89911784T patent/DE68909053T2/de not_active Expired - Fee Related
  • 1989-10-10 CA CA002000395A patent/CA2000395A1/en not_active Abandoned
  • 1989-10-10 WO PCT/DK1989/000232 patent/WO1990004008A1/en not_active Application Discontinuation
  • 1989-10-10 WO PCT/DK1989/000236 patent/WO1990003787A1/en not_active Application Discontinuation
  • 1989-10-10 CA CA002000397A patent/CA2000397A1/en not_active Abandoned
  • 1989-10-10 CA CA002000398A patent/CA2000398A1/en not_active Abandoned
  • 1989-10-10 EP EP89911785A patent/EP0437524B1/de not_active Expired - Lifetime
  • 1989-10-10 JP JP1510967A patent/JPH04500972A/ja active Pending
  • 1989-10-10 AU AU44204/89A patent/AU629866B2/en not_active Ceased
  • 1989-10-10 AU AU44205/89A patent/AU640353B2/en not_active Ceased
  • 1989-10-10 AU AU44219/89A patent/AU631816B2/en not_active Ceased
  • 1989-10-10 JP JP1510973A patent/JPH04501116A/ja active Pending
  • 1989-10-10 EP EP89911783A patent/EP0438483B1/de not_active Expired - Lifetime
  • 1989-10-10 WO PCT/DK1989/000238 patent/WO1990004012A1/en not_active Application Discontinuation
  • 1989-10-10 JP JP1510968A patent/JPH04500973A/ja active Pending
  • 1989-10-10 AU AU44211/89A patent/AU4421189A/en not_active Abandoned
  • 1989-10-10 JP JP1510966A patent/JPH04500971A/ja active Pending
  • 1989-10-10 EP EP89911782A patent/EP0437522A1/de not_active Withdrawn
  • 1989-10-10 CA CA002000394A patent/CA2000394A1/en not_active Abandoned
  • 1989-10-10 CA CA002000393A patent/CA2000393A1/en not_active Abandoned
  • 1989-10-10 WO PCT/DK1989/000239 patent/WO1990004013A1/en not_active Application Discontinuation
  • 1989-10-10 EP EP89911784A patent/EP0437523B1/de not_active Expired - Lifetime
  • 1989-10-10 WO PCT/DK1989/000237 patent/WO1990004011A1/en not_active Application Discontinuation
  • 1989-10-10 CA CA002000391A patent/CA2000391A1/en not_active Abandoned
  • 1989-10-10 EP EP89911779A patent/EP0437519B1/de not_active Expired - Lifetime
  • 1989-10-10 AU AU44220/89A patent/AU630120B2/en not_active Ceased
  • 1989-10-10 WO PCT/DK1989/000233 patent/WO1990004009A1/en active IP Right Grant
  • 1989-10-10 EP EP89911780A patent/EP0437520B1/de not_active Expired - Lifetime
  • 1989-10-10 JP JP1510972A patent/JPH04501115A/ja active Pending
  • 1989-10-10 AU AU44222/89A patent/AU639675B2/en not_active Ceased
  • 1989-10-10 AU AU44224/89A patent/AU636582B2/en not_active Ceased
  • 1989-10-10 EP EP89911781A patent/EP0437521A1/de not_active Withdrawn
  • 1989-10-10 JP JP1510971A patent/JPH04501114A/ja active Pending
  • 1989-10-10 AU AU44210/89A patent/AU4421089A/en not_active Abandoned
  • 1989-10-10 WO PCT/DK1989/000234 patent/WO1990004010A1/en not_active Application Discontinuation
  • 1989-10-10 CA CA002000392A patent/CA2000392A1/en not_active Abandoned
  • 1989-10-10 CA CA002000396A patent/CA2000396A1/en not_active Abandoned
  • 1989-10-10 WO PCT/DK1989/000235 patent/WO1990003786A1/en not_active Application Discontinuation
  • 1989-10-11 ZA ZA897693A patent/ZA897693B/xx unknown
  • 1989-10-11 ZA ZA897692A patent/ZA897692B/xx unknown

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