EP2994100A1 - Petroselinsäure oder einer kombination von wirkstoffen mit mindestens petroselinsäure zur förderung von gewichtsverlust und/oder zur bewahrung des gewichts - Google Patents

Petroselinsäure oder einer kombination von wirkstoffen mit mindestens petroselinsäure zur förderung von gewichtsverlust und/oder zur bewahrung des gewichts

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Publication number
EP2994100A1
EP2994100A1 EP14726780.1A EP14726780A EP2994100A1 EP 2994100 A1 EP2994100 A1 EP 2994100A1 EP 14726780 A EP14726780 A EP 14726780A EP 2994100 A1 EP2994100 A1 EP 2994100A1
Authority
EP
European Patent Office
Prior art keywords
petroselinic acid
combination
weight
active ingredients
functional food
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP14726780.1A
Other languages
English (en)
French (fr)
Inventor
Yann Mahe
Carole BRU
Audrey Gueniche
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nestec SA
Original Assignee
Nestec SA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Nestec SA filed Critical Nestec SA
Publication of EP2994100A1 publication Critical patent/EP2994100A1/de
Withdrawn legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/20Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A61K31/201Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having one or two double bonds, e.g. oleic, linoleic acids
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105Plant extracts, their artificial duplicates or their derivatives
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/115Fatty acids or derivatives thereof; Fats or oils
    • A23L33/12Fatty acids or derivatives thereof
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/16Inorganic salts, minerals or trace elements
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/30Dietetic or nutritional methods, e.g. for losing weight
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/01Hydrocarbons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/191Carboxylic acids, e.g. valproic acid having two or more hydroxy groups, e.g. gluconic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/3533,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355Tocopherols, e.g. vitamin E
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/59Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • A61K31/5939,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/30Zinc; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/66Microorganisms or materials therefrom
    • A61K35/74Bacteria
    • A61K35/741Probiotics
    • A61K35/744Lactic acid bacteria, e.g. enterococci, pediococci, lactococci, streptococci or leuconostocs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/06Fungi, e.g. yeasts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/23Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9728Fungi, e.g. yeasts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/06Preparations for care of the skin for countering cellulitis
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23VINDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00Food compositions, function of food ingredients or processes for food or foodstuffs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/92Oral administration

Definitions

  • Petroselinic acid or combination of active ingredients comprising at least petroselinic acid to promote weight loss and / or weight maintenance
  • the present invention relates to the field of compositions for accompanying weight management, promoting weight loss and / or weight maintenance in a human and / or an animal.
  • petroselinic acid or combinations comprising at least petroselinic acid, useful to support weight management, promote weight loss and / or weight maintenance in a human and / or an animal.
  • the petroselinic acid or the combination of active agents considered in the context of the present invention are preferably used as a medicament or in a functional food.
  • Obesity develops when energy intake is greater than energy expenditure, with excess energy stored primarily as fat in adipose tissue. Weight loss of the body and prevention of weight gain can be achieved by reducing energy intake or bioavailability, increasing energy expenditure and / or reducing storage in the form of fat. Obesity poses a serious threat to health because it is associated with a range of chronic diseases, including diabetes, atherosclerosis, degenerative diseases, respiratory diseases and some cancers.
  • adipose tissue can be observed during hypertrophy of adipose tissue.
  • Inflammation of the adipose tissue especially white subcutaneous adipose tissue (ScWAT) has been particularly well described in the case of obesity.
  • ScWAT white subcutaneous adipose tissue
  • subcutaneous adipose tissue spreads and accumulates under the skin.
  • Adipose tissue is indeed considered in its entirety as an important endocrine organ whose physiology can be altered by the hypertrophy of fat cells and the accumulation of peri-adipocyte immune cells, including the macrophage.
  • pre-adipocytes of non-obese women respond to the factors produced by these macrophages and produce molecules and chemokines such as IL-8 and MCP1 which further amplify and maintain the inflammation of adipose tissue. recruiting new inflammatory cells into adipose tissue (D. Lacasa et al., Endocrinology 148 (2): 868-87 (2007), M. Keophiphat et al., Molecular endocinology 23: 11-24 (2009).
  • pro-fibrotic phenotype can then develop in inflammatory adipose tissue.
  • petroselinic acid or a combination of active agents according to the invention is capable of synergistically increasing the amount of lipoxin A4.
  • Lipoxin A4 belongs to the family of resolvines. This family of compounds naturally produced by the body acts in a complementary manner to conventional anti-inflammatory agents by raising the trigger threshold of a so-called dermatological classic inflammatory response, and more particularly to raise the threshold of appearance of the signals of this inflammation. classic, namely redness, pain and heat.
  • lipoxin A4 appears as a potential target for acting on adipose tissue.
  • the present invention is more particularly concerned with identifying active agents or combinations of active agents having a significant action on lipoxin A4.
  • petroselinic acid or a combination of active agents comprising at least petroselinic acid and at least one compound chosen from zinc, taurine, one of their salts and lycopene. and mixtures thereof, exerts an activity on lipoxin A4.
  • the invention thus firstly relates to petroselinic acid or a combination of active agents comprising at least petroselinic acid and at least one compound chosen from zinc, taurine, one of their salts, lycopene and their salts. mixtures, preferably at least taurine or zinc gluconate and even more preferably at least taurine and zinc gluconate, as a medicament for oral administration or as a functional food for promoting weight loss and / or or maintaining weight in a human and / or animal.
  • the subject of the invention is also petroselinic acid or a combination of active agents comprising at least petroselinic acid and at least one compound chosen from zinc, taurine, one of their salts, lycopene and their mixtures. , preferably at least taurine or zinc gluconate, as a medicament for oral administration or as a functional food intended to reduce the weight of fat of a human and / or an animal.
  • fat mass is intended to mean the mass of adipose tissue, or fat, in a human and / or an animal, as opposed to muscle mass.
  • the subject of the invention is also petroselinic acid or a combination of active agents comprising at least petroselinic acid and at least one compound chosen from zinc, taurine, one of their salts, lycopene and their mixtures. , preferably at least taurine or zinc gluconate, as a medicament for oral administration or as a functional food intended to reduce the total weight of a human and / or animal.
  • the invention also relates to petroselinic acid or a combination of active agents comprising at least petroselinic acid and at least one compound selected from the group consisting of zinc, taurine, one of their salts, lycopene and mixtures thereof, preferably at least taurine or zinc gluconate and even more preferably at least taurine and zinc gluconate, as a medicament for the administration orally or as a functional food for combating obesity.
  • Weight change and weight loss may be due to a slimming diet or pregnancy.
  • “Functional food” or “food product” means a food similar in appearance to a conventional food or a conventional food that is part of the normal diet and has been shown to provide, beyond the nutritional functions of the food. physiological benefits specified by the scientific literature and that it reduces the risk of chronic diseases.
  • the functional food as defined above also includes beverages.
  • BMI Body Mass Index
  • weight is meant for a human adult with a BMI between 25 and 30.
  • Obsity means a state in which the natural energy stored in the adipose tissue of animals, particularly humans and other mammals, is increased in such a way that it associates with a certain state of health or increased mortality.
  • An adult adult with a BMI greater than 30 is considered obese.
  • weight loss refers to a reduction in the body weight of a human and / or an animal. Weight loss can be part of a concern for improving health, shape and / or appearance.
  • weight management or “weight maintenance” is meant the maintenance of total body mass. For example, weight management can be related to keeping the BMI between 18.5 and 25, this range being considered normal.
  • food grade bacterium is meant a bacterium compatible with an administration in a food.
  • probiotic preparations of microbial cells or components of microbial cells having a beneficial effect on the health or well-being of the host.
  • prebiotic food substances that promote the growth of probiotics in the gut. They are not broken down in the stomach and / or upper intestine or absorbed into the digestive tract of the person who eats them, but are fermented by the gastrointestinal microflora and / or probiotics. Prebiotics are for example defined by Glenn R. Gibson and Marcel B. Roberfroid, "Dietary Modulation of the Human Colony Microbiota: Introducing the Concept of Prebiotics", J. Nutr. 1995 125: 1401-1412. ASSET ASSOCIATION a) Petroselinic acid
  • the petroselinic acid or monounsaturated fatty acid (C18: 1 n-12 or cis delta 6) or C18 delta-6-cis-octadecenoic acid can be used in an isolated form. .
  • the petroselinic acid is used in the form of a plant extract containing it, such as an oil.
  • This form is particularly adapted to the oral route of administration.
  • the oils rich in petroselinic acid are more particularly chosen from umbelliferous oils.
  • Oil rich in petroselinic acid is understood to mean an oil comprising at least 40% petroselinic acid.
  • Umbelliferae are plants whose flowers are arranged in umbels, the species particularly rich in petroselinic acid being Umbellifarea-Apiacea and Araliaceae. Plants of the genus Thapsia are also sources of petroselinic acid (Avato et al, Lipids, 2001, 36, 845). The preferred species used in the invention are coriander, chervil, carrot, celery, caraway, caraway, parsley and dill, or mixtures thereof. Umbellifer oil source of petroselinic acid particularly suitable for the invention can be extracted from the seed of these umbellifers, for example by grinding or pressing, then refining.
  • Umbellifer oil has a petroselinic acid content that varies according to the umbelliferous seed from which it is extracted.
  • the petroselinic acid content also varies according to the country of origin of the umbellifer and according to the extraction which can be more or less complete.
  • Petroselinic acid is also an abundant compound (approximately 48%) of Geranium sanguineum seed oil.
  • petroselinic acid can be used in the form of an umbelliferous oil or Geranium sanguineum.
  • the umbelliferous oil more particularly considered in the invention can be chosen from coriander, chervil, carrot, celery, caraway, caraway and parsley seed oils. dill, and mixtures thereof.
  • the petroselinic acid is used in the form of a coriander seed oil.
  • coriander seed oils are covered by the term "coriander oil”.
  • the contents are variable depending on whether the combination of active agents according to the invention is used in a medicament for oral administration or a functional food.
  • the content of petroselinic acid in a drug intended for oral administration in accordance with the invention may be between 0.01 and 70% by weight, especially between 0.1 and 70% by weight, particularly between 1 and 70% by weight, based on the total weight of the drug.
  • the content of petroselinic acid in a functional food according to the invention may be between 0.05 and 2% by weight, especially between 0.1 and 1% by weight, particularly between 0.3 and 0.6%. by weight, based on the total weight of the functional food.
  • the petroselinic acid content in a medicament intended for oral administration or in a functional food according to the invention may such that the daily dose of said petroselinic acid is between 0.5 and 2000 mg / day, particularly between 1 and 1000 mg / day, and especially between 5 and 700 mg / day.
  • An association of assets according to the invention may comprise taurine, or hypotaurine. It can also implement one of their salts.
  • the salts that can be used are obviously chosen for their total safety.
  • Alkaline or alkaline earth salts, in particular salts of magnesium, manganese, iron II or zinc, are suitable for this purpose.
  • the content of taurine, hypotaurine or a salt thereof in a medicament intended for oral administration according to the invention or in a functional food according to the invention may be such that the daily dose of said taurine, hypotaurine or one of its salts is between 1 and 700 mg / day, particularly between 10 and 500 mg / day and in particular between 50 and 300 mg / day.
  • Zinc Zinc
  • Zinc is understood to mean zinc or one of its salts (acetate, chloride, citrate, lactate, gluconate, lactate, oxide, carbonate or zinc sulphate), in particular the salts of Zn (II) and preferably complexed with one or more (poly) hydroxy acids such as gluconate.
  • (Poly) hydroxy acid means any carboxylic acid which comprises a linear or branched, saturated or unsaturated hydrocarbon-based chain, preferably saturated and / or linear, comprising from 1 to 10 carbon atoms and from 1 to 9 hydroxyl groups, and comprising from 1 to 4 carboxylic groups -C (O) -OH, at least one of said -C (O) -OH functions is in the form of carboxylate -C (O) -O- complexed with the Zn atom, preferably Zn (II).
  • the zinc salt is complex with two carboxylate groups such as that of formula (I)
  • R and R ' which may be identical or different, represent a (C 1 -C 6) (poly) hydroxyalkyl group
  • the compound of formula (I) is zinc gluconate.
  • the zinc is not a zinc oxide but a zinc salt.
  • Zn (II) is meant a zinc atom of oxidation state Zn 2+ .
  • the content of zinc gluconate in a drug intended for oral administration in accordance with the invention or in a functional food according to the invention may be such that the daily dose of said zinc gluconate is between 0.01 and 300. mg / d, in particular between 0.1 and 200 mg / day, particularly between 1 and 100 mg / day. d) Lycopene
  • An active combination according to the invention may also comprise lycopene.
  • Lycopene is a natural pigment found in ripe fruit, particularly in tomatoes, but it also exists in synthetic form, especially synthesized from a fungus, Blakeslea trispora.
  • Lyc-O-Mato ® It may in particular be sold by Lycored under the name Lyc-O-Mato ®.
  • lycopene is used in a combination of active agents according to the invention.
  • the combination of assets comprises or consists of petroselinic acid and lycopene.
  • the content of lycopene in a medicament intended for oral administration in accordance with the invention or in a functional food according to the invention may be such that the daily dose of lycopene is between 0.01 and 20 mg / day. particularly between 0.1 and 15 mg / day, and especially between 0.5 and 10 mg / day.
  • the asset or combination of assets according to the present invention may further be implemented with additional assets adapted to the mode of administration considered as described below.
  • the drug or functional food may further comprise vitamin D3 and / or tocopherol acetate.
  • the petroselinic acid or the combination of active agents according to the present invention is used in a medicament for oral administration or in a functional food, said medicament or functional food. comprising petroselinic acid, taurine, zinc, preferably zinc gluconate, vitamin D3 and tocopherol acetate.
  • the drugs intended for oral administration in accordance with the present invention may be in any of the galenical forms normally used for the oral route.
  • a medicinal product intended for oral administration in accordance with the invention comprises:
  • petroselinic acid in a content of between 1 and 70% by weight, especially between 10 and 70% by weight, particularly between 20 and 70% by weight, relative to the total weight of the combination of assets;
  • taurine in a content of between 1 and 50% by weight, especially between 5 and 40% by weight, particularly between 10 and 30% by weight, relative to the total weight of the combination of active ingredients;
  • At least one zinc (poly) hydroxyacid preferably zinc gluconate, in a content of between 0.001 and 40% by weight, in particular between 0.01 and 25% by weight, particularly between 0.1% and 20% by weight; by weight, relative to the total weight of the combination of assets;
  • vitamin D3 in a content of between 0.0001 and 1.0% by weight, especially between 0.0001 and 0.5% by weight, particularly between 0.0001 and 0.1% by weight , in relation to the total weight of the asset combination;
  • tocopherol acetate in a content of between 0.01 and 10% by weight, especially between 0.1 and 10% by weight, particularly between 0.2 and 5% by weight, relative to total weight of the asset combination.
  • a medicament intended for oral administration comprises the ingredients i) to v), as taken together or independently: - (i) petroselinic acid in a content of between 1 and 70% by weight, especially between 10 and 70% by weight, particularly between 15 and 70% by weight, relative to the total weight of the drug;
  • At least one zinc (poly) hydroxyacid preferably zinc gluconate, in a content of between 0.001 and 30% by weight, especially between 0.01 and 25% by weight, particularly between 0.1% and 20% by weight; by weight, based on the total weight of the drug;
  • vitamin D3 in a content of between 0.0001 and 1.0% by weight, especially between 0.0001 and 0.5% by weight, particularly between 0.0001 and 0.1% by weight , based on the total weight of the drug;
  • the medicament intended for oral administration comprises all of the above-mentioned ingredients (i) to (iii).
  • the medicinal product intended for oral administration comprises all of the above-mentioned ingredients (i) to (v).
  • the formulation of the drug according to the invention can be carried out by the usual methods for producing dragees, capsules, gels, emulsions, tablets, tablets or capsules.
  • the medicaments according to the invention intended for oral administration may in particular comprise all or only part of the daily dose.
  • one to three drugs can be administered per day.
  • the duration of this treatment intended for oral administration may be greater than 4 weeks, in particular from 4 to 15 weeks, with, if necessary, one or more periods of interruption ranging from a few days to several months.
  • any additional additives and / or their quantity in such a way that the advantageous properties of the combination according to the invention or of the medicinal product comprising the combination according to the invention are not or substantially not affected by the addition envisaged.
  • the drug or functional food according to the present invention may further contain protective hydrocolloids (such as gums, proteins, etc.). modified starches), binders, film-forming agents, encapsulating agents / materials, core / shell materials, matrix compounds, coating agents, emulsifiers, surfactants, solubilizing agents (oils, greases, waxes, lecithins, etc.), adsorbents, "carriers", fillers, co-compounds, dispersing agents, wetting agents, "processing aids” agents for the process (solvents ), flow agents, taste masking agents, weighting agents, gelling agents, gelling agents, antioxidants and antimicrobial agents.
  • protective hydrocolloids such as gums, proteins, etc.
  • binders such as gums, proteins, etc.
  • film-forming agents such as gums, proteins, etc.
  • encapsulating agents / materials such as gums, proteins, etc.
  • core / shell materials such as binders, film-forming agents
  • composition may also contain conventional pharmaceutical additives and adjuvants, excipients and diluents, including but not limited to water, gelatin of any origin, vegetable gums, ligninsulfonate, talc, sugars, starch, gum arabic, vegetable oils, polyalkylene glycols, flavoring agents, preservatives, stabilizers, emulsifiers, buffers, lubricants, colorants, wetting agents, charges and the like. In all cases, these other components are chosen according to their destination.
  • conventional pharmaceutical additives and adjuvants, excipients and diluents including but not limited to water, gelatin of any origin, vegetable gums, ligninsulfonate, talc, sugars, starch, gum arabic, vegetable oils, polyalkylene glycols, flavoring agents, preservatives, stabilizers, emulsifiers, buffers, lubricants, colorants, wetting agents, charges and the like. In all cases, these other components are chosen according to
  • composition can be a complete nutritional formula.
  • the composition according to the invention may comprise a source of proteins.
  • Any suitable dietary protein may be used, for example animal proteins (such as milk proteins, meat proteins and egg proteins); vegetable proteins (such as soy protein, wheat protein, rice protein and pea protein), free amino acid mixtures; or their combinations. Milk proteins such as casein and whey, and soy protein are particularly preferred.
  • the proteins may be intact or hydrolyzed or take the form of a mixture of intact and hydrolysed proteins. It may be desirable to provide partially hydrolysed proteins (degree of hydrolysis of between 2 and 20%), for example for animals suspected of being at risk of developing cow's milk allergy. If the hydrolysed proteins are required, the hydrolysis process can be carried out according to techniques known to those skilled in the art.
  • a whey protein hydrolyzate can be prepared by enzymatic hydrolysis of the whey fraction in one or more steps. If the whey fraction used as a starting material is substantially free of lactose, it has been found that the protein undergoes a smaller number of blockages of its lysines during the hydrolysis process. This makes it possible to pass from about 15% by weight of lysines blocked to less than 10% by weight of blocked lysines, relative to the total weight of lysines of the protein, for example about 7% by weight of lysines, which significantly improves the nutritional quality of the protein source.
  • the composition may also contain a source of sugars and a source of fat.
  • the lipid source preferably provides from 5% to 40% of the energy of the composition, for example from 20% to 30% of the energy.
  • a suitable fat profile can be obtained by using a blend of canola oil, corn oil and high oleic sunflower oil.
  • a carbohydrate source may be added to the composition.
  • the sugar source preferably provides from 40% to 80% of the energy of the composition.
  • Any type of suitable sugar or carbohydrate may be used, for example sucrose, lactose, glucose, fructose, dehydrated glucose syrup, maltodextrins and mixtures thereof.
  • Dietary fiber can also be added. Dietary fiber passes through the small intestine and is not digested by enzymes and functions as a natural swelling agent and laxative. Dietary fiber may be soluble or insoluble, and in general a mixture of both types is preferred.
  • Suitable sources include soy, pea, oat fiber, pectin, guar gum, gum arabic, fructo-oligosaccharide, galacto-oligosaccharide, sialyl-lactose and oligosaccharide derivatives of original milk animal.
  • a preferred fiber blend is a mixture of inulin and short chain fructooligosaccharides.
  • the fiber content is between 2 and 40 g / l of the ready-to-eat composition, preferably between 4 and 10 g / l.
  • the composition may also contain minerals and trace elements such as micronutrients and vitamins, as recommended by government agencies such as the United States Recommended Daily Allowances (USRDA).
  • the composition may contain, per daily dose, one or more of the following micronutrients in the ranges indicated: 300 to 500 mg of calcium, 50 to 100 mg of magnesium, 150 to 250 mg of phosphorus, 5 to 20 mg of iron, 1 to 7 mg of zinc, 0.1 to 0.3 mg of copper, 50 to 200 mg of iodine, 5 to 15 ⁇ g of selenium, 1000 to 3000 ⁇ g of beta-carotene, 10 to 80 mg of vitamin C, 1 to 2 mg of vitamin B1, 0.5 to 1.5 mg of vitamin B6, 0.5 to 2 mg of vitamin B2, 5 to 18 mg of niacin, 0, 5 to 2.0 ⁇ g of vitamin B12, 100 to 800 ⁇ g of folic acid, 30 to 70 ⁇ g of biotin, 1 to 5 ⁇ g of vitamin D, 3 to 10 ⁇ g of vitamin E.
  • One or more food grade emulsifiers may be included in the composition.
  • diacetyltartaric acid esters of mono- and diglycerides, lecithin and mono-and di-glycerides may be included.
  • suitable salts and stabilizers may be included.
  • composition can be administered in the form of a powder for reconstitution with milk or water.
  • the composition is in the form of a powder, for example a long-life powder.
  • the long preservation can be obtained, for example by providing the composition with an activity in water of less than 0.2, for example of the order of 0.19 to 0.05, preferably less than 0.15.
  • Water activity or "a w " is a measure of the energy status of water in a system. It is defined as the vapor pressure of water divided by that of pure water at the same temperature. Therefore, pure distilled water has a water activity of exactly one.
  • the composition described above may be prepared by any suitable method. For example, it can be prepared by mixing the proteins, the carbohydrate source and the fat source together in appropriate proportions. If they emulsifiers can be incorporated at this stage. Vitamins and minerals can be added at this stage, but are usually added later to prevent thermal degradation. All lipophilic vitamins, emulsifiers and the like can be dissolved in the fat source before mixing. Water, preferably water which has been subjected to reverse osmosis, may then be mixed to form a liquid mixture. The temperature of the water is preferably between about 50 ° C and about 80 ° C to facilitate dispersion of the ingredients. Commercially available liquefying agents can be used to form the liquid mixture. The liquid mixture is then homogenized, for example in two stages.
  • the liquid mixture may then be heat-treated to reduce the bacterial load, by rapidly heating the liquid mixture to a temperature in the range of about 80 ° C to about 150 ° C for about 5 seconds to about 5 minutes, for example .
  • This can be done by steam injection, autoclave or by heat exchanger, for example a plate heat exchanger.
  • the liquid mixture can be cooled to about 60 ° C to about 85 ° C, for example by flash cooling.
  • the liquid mixture can then be homogenized again, for example in two steps from about 10 MPa to about 30 MPa in the first step and from about 2 MPa to about 10 MPa in the second step.
  • the homogenized mixture can then be cooled so that heat-sensitive components such as vitamins and minerals can be added.
  • the pH and dry matter content of the homogenized mixture is conventionally adjusted at this stage.
  • the homogenized mixture is transferred to a suitable drying apparatus, such as a spray dryer or lyophilizer and converted to powder.
  • a suitable drying apparatus such as a spray dryer or lyophilizer and converted to powder.
  • the powder should have a moisture content of less than about 5% by weight.
  • the animals treated with the composition according to the present invention are at least two years old. This age limit applies in particular to the man. If the animals treated with the composition according to the present invention are dogs or cats, for example, the latter are advantageously at least 4 months old.
  • the composition When the composition is a drug, the doses in active ingredients can be adjusted by a physician. When the composition is a functional food. Access to this functional food is available to everyone. As a result, the treatment of obesity could be initiated at a much earlier stage.
  • the composition according to the present invention is a food product or functional food intended for humans, pets or livestock.
  • the composition is intended for animals selected from the group consisting of dogs, cats, pigs, cattle, horses, goats, sheep, poultry and humans, and in a preferred embodiment the food product is intended for humans, especially human adults.
  • the composition of the present invention may also comprise at least quality or food grade bacteria or yeast.
  • the food grade bacteria may be probiotic bacteria and are preferably selected from the group consisting of lactic acid bacteria, bifidobacteria, propionic bacteria or mixtures thereof.
  • Probiotic bacteria can be lactic acid bacteria or bifidobacteria with established probiotic characteristics. For example, they may also be able to promote the development of a bifidogenic intestinal flora.
  • Suitable probiotic bifidobacterium strains include Bifidobacterium lactis CNCM 1-3446 sold in particular by Christian Hansen of Denmark under the trademark Bbl2, Bifidobacterium longum ATCC BAA-999 sold by Morinaga Milk Industry Co. Ltd.
  • yeast quality or food grade include Saccharomyces cerevisiae and / or Saccharomyces boulardii.
  • the composition may further contain at least one prebiotic.
  • Prebiotics can promote the growth of certain food grade bacteria, particularly probiotic bacteria, when present in the composition.
  • prebiotics are selected from oligosaccharides and optionally contain fructose, galactose, mannose, soy and / or inulin, dietary fiber or mixtures thereof.
  • Example 1 Composition for the oral route in the form of a soft capsule
  • Vitamin D3 0, 115
  • Blood mononuclear cells are cultured at 5% CO 2 and at 37 ° C. in macrophage-free serum medium (SFM Macrophage, Invitrogen 12065074) for 24 hours.
  • SFM Macrophage macrophage-free serum medium
  • the medium is replaced by the same fresh test medium containing in addition the active agents at different doses for 30 minutes in the presence of the different products to be evaluated, as indicated in the table of results below.
  • the inflammatory response was then triggered in the presence of phorbol myristate (0.05 ⁇ ) and calcium ionophore (1 ⁇ ) and a mixture of lipid substrate composed of docosahexaenoic acid (DHA - 1 ⁇ g / mL) and eicosapentaenoic acid (EPA - 1 ⁇ g / mL).
  • SPE SPE
  • the analytical method used consists in separating the different analytes by high pressure liquid chromatography as a function of their retention time and quantifying them by mass spectrometry.
  • a combination of active ingredients according to the invention comprising coriander oil, rich in petroselinic acid, and Lycomato, rich in lycopene, as well as these same compounds individually, have been tested in accordance with what is indicated herein. -above.
  • petroselinic 0.25mg / ml It is observed that coriander oil containing petroselinic acid stimulates the production of lipoxin A4.
  • Lycomato alone does not cause any variation in the level of lipoxin A4 production.
  • Example 4 Demonstration of the activating effect of petroselinic acid and the combination of petroselinic acid with taurine according to the invention on the synthesis / basal release of lipoxin A4 by keratinocytes.
  • lipoxin A4 94% was observed compared to the basal level of production of this anti-inflammatory component when the lymphocyte cells tested were brought into contact with the combination of active.
  • Example 3 A protocol similar to that described in Example 3 was carried out, however replacing the lycomato with zinc gluconate.
  • actives according to the invention comprising coriander oil, rich in petroselinic acid, and zinc gluconate, as well as these same compounds individually, have been tested in accordance with what is indicated herein. -after.
  • lipoxin A4 94% was observed compared to the basal level of production of this anti-inflammatory component when the lymphocyte cells tested were brought into contact with the combination of active.
  • Dairy products milk, milk powder and cream
  • a low-temperature container (8-15 ° C) and mixed to moisturize dairy ingredients.
  • the mixture is then heated to a temperature of up to 68-75 ° C and the other ingredients: sugar, starch, inulin, carrageenan are incorporated.
  • the whole is then mixed for about half an hour until complete dissolution of the various ingredients.
  • a homogenization step using an APV Gaulin GmbH Homogenisator (type: 132MC4 5TBSX) is carried out by applying a pressure of 50-120 bar by using a supply pressure of 4bar. The product is then sterilized at 130 ° C for 20-30 s. The product is then cooled to 5-10 ° C and then dosed.
  • Example 8 Example of Formulation of a Functional Food Drink

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EP14726780.1A 2013-05-07 2014-05-06 Petroselinsäure oder einer kombination von wirkstoffen mit mindestens petroselinsäure zur förderung von gewichtsverlust und/oder zur bewahrung des gewichts Withdrawn EP2994100A1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR1354185A FR3005418B1 (fr) 2013-05-07 2013-05-07 Acide petroselinique ou association d'actifs comprenant au moins l'acide petroselinique pour favoriser la perte de poids et/ou le maintien du poids
PCT/IB2014/061235 WO2014181249A1 (fr) 2013-05-07 2014-05-06 Acide pétrosélinique ou association d'actifs comprenant au moins l'acide pétrosélinique pour favoriser la perte de poids et/ou le maintien du poids

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EP2994100A1 true EP2994100A1 (de) 2016-03-16

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EP14726780.1A Withdrawn EP2994100A1 (de) 2013-05-07 2014-05-06 Petroselinsäure oder einer kombination von wirkstoffen mit mindestens petroselinsäure zur förderung von gewichtsverlust und/oder zur bewahrung des gewichts

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US (1) US20160106695A1 (de)
EP (1) EP2994100A1 (de)
CN (1) CN105358127A (de)
BR (1) BR112015027991A2 (de)
FR (1) FR3005418B1 (de)
WO (1) WO2014181249A1 (de)

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US10881125B1 (en) * 2016-04-28 2021-01-05 Stephen C. Perry Taurine-containing composition for improving assimilation of compounds contained in ingestible items
CN107157982A (zh) * 2017-06-07 2017-09-15 南京晶云化工有限公司 一种用于治疗骨折的中药组合物及其制备方法和应用
FR3080769B1 (fr) * 2018-05-04 2020-10-16 Soc Dexploitation De Produits Pour Les Industries Chimiques Seppic Utilisation orale d'huile de graines d'au moins une plante ombellifere pour un effet apaisant des peaux reactives
WO2020052742A1 (en) * 2018-09-11 2020-03-19 Parapharm Development Limited Capsule, tablet or pill
CN115105492B (zh) * 2021-03-17 2023-08-25 南方医科大学南方医院 岩芹酸的新用途

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FR2725370B1 (fr) * 1994-10-07 1997-06-06 Oreal Composition cosmetique ou dermatologique contenant une huile riche en acide petroselinique
EP0888773A1 (de) * 1997-07-05 1999-01-07 Societe Des Produits Nestle S.A. Verwendung von Petroselinsäure zur Behandlung von Entzündungen der oberflächlichen Gewebe
ES2248962T5 (es) * 1998-12-22 2010-01-04 Unilever N.V. Uso cosmetico del acido petroselenico.
US20030054015A1 (en) * 2000-12-25 2003-03-20 Shinichiro Haze Sympathetic-activating perfume composition
WO2003075941A1 (en) * 2002-03-11 2003-09-18 General Nutrition Investment Company Methods for the treatment and prevention of overweight in mammals
JP2005126405A (ja) * 2003-10-25 2005-05-19 Sadami Ishibashi 肥満防止剤
EP1932509A1 (de) * 2006-12-14 2008-06-18 L'oreal Génération d'eau à partir d'air en utilisant l'énergie solaire et une unité de réfrigération d'adsorption
CN101265177A (zh) * 2007-03-16 2008-09-17 中国医学科学院药物研究所 洋芫荽子酸类化合物

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See also references of WO2014181249A1 *

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WO2014181249A1 (fr) 2014-11-13
CN105358127A (zh) 2016-02-24
FR3005418B1 (fr) 2015-05-22
FR3005418A1 (fr) 2014-11-14
US20160106695A1 (en) 2016-04-21

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