EP1890689A2 - Zusammensetzung zur verlangsamung der entwicklung von morbus alzheimer - Google Patents

Zusammensetzung zur verlangsamung der entwicklung von morbus alzheimer

Info

Publication number
EP1890689A2
EP1890689A2 EP06755300A EP06755300A EP1890689A2 EP 1890689 A2 EP1890689 A2 EP 1890689A2 EP 06755300 A EP06755300 A EP 06755300A EP 06755300 A EP06755300 A EP 06755300A EP 1890689 A2 EP1890689 A2 EP 1890689A2
Authority
EP
European Patent Office
Prior art keywords
composition
vitamin
disease
composition according
alzheimer
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Withdrawn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
EP06755300A
Other languages
English (en)
French (fr)
Inventor
Dominique Bourgeade
Jean-Christophe Anton
François MICELI
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.)
Cothera
Original Assignee
Cothera
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 Cothera filed Critical Cothera
Publication of EP1890689A2 publication Critical patent/EP1890689A2/de
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • 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
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • 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
    • A23L33/15—Vitamins
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic 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
    • A61K31/201—Carboxylic 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
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic 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
    • A61K31/202—Carboxylic 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 three or more double bonds, e.g. linolenic
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic 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
    • A61K31/352—Heterocyclic 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 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355—Tocopherols, e.g. vitamin E
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs

Definitions

  • composition for delaying the development of Alzheimer's disease Composition for delaying the development of Alzheimer's disease
  • the present invention relates to a composition for delaying the development of Alzheimer's disease and improving the quality of life of patients.
  • This composition is intended to be incorporated into a vector that can be assimilated by the human body, preferably by the dietary route.
  • composition according to the invention may also be used in the veterinary field as a supplement to the feeding of animals, in particular carnivorous domestic animals, more particularly dogs or cats.
  • Alzheimer's disease is a type of dementia that usually affects the elderly, and against which there is currently no decisive treatment. It is characterized by the progressive and irreversible alteration of cognitive functions and by particular neuro-histological lesions. There is currently a small number of drugs that can improve, and only very transiently, the condition of some patients with this disease.
  • This neurodegenerative disease of the central nervous system first causes a severe amnesic syndrome, which results mainly lesions of neurons of the hippocampus, region of convergence of stored information and first site of localization of the disease. Subsequently, the extension of the lesions is towards the neo-cortex and, more precisely, towards the associative areas, thus causing the disruption of so-called instrumental functions.
  • the lesions that appear with the disease are cortical atrophy, senile plaques (deposition of an amyloid substance) and neurofibrillary tangles.
  • the first cognitive signs are usually memory and executive functions disorders. In addition, however, there are sometimes viso-spatial disorders or language.
  • the memory disorders characteristic of Alzheimer's disease first of all relate to so-called episodic memory, which allows the fixation of new information, leading in particular to temporal disorientation. Disorientation in space is usually later.
  • the patient has more and more difficulty organizing and performing a more or less complex cognitive task.
  • Alzheimer's disease also causes non-cognitive dysfunction, such as depression, anxiety, apathy, some form of verbal and physical aggression, as well as sleep disorders, and hyperphagia.
  • the present invention therefore relates to a novel composition for delaying the development of Alzheimer's disease and improving the quality of life of patients.
  • dietary supplement compositions comprising mixtures of fatty acids, vitamin cocktails and optionally mineral salts, sources of proteins and sugars are known from the state of the art. However, depending on the nature of the associated ingredients, the use of these dietary supplements varies from body building to depression to help with breastfeeding.
  • patent application US 2003/0580341 discloses a combination of vitamins with DHA for the treatment of a multitude of disorders in adults or children, in connection with a supposedly beneficial effect of DHA.
  • US patent application 2004/0071825 describes vitamin cocktails, minerals and plant extracts in the form of granules, especially for "bodybuilding” or the increase in intellectual activity.
  • Patent application EP 815 735 for its part describes dairy products for everyday consumption comprising various fatty acids, optionally enriched with vitamins.
  • the patent application EP 920 813 describes a process for accelerating the digestion rate of a protein, in particular for producing infant food compositions.
  • the patent application EP 126 666 describes food compositions comprising carbohydrates, vitamins, mineral salts, a lipid fraction and a protein fraction comprising 3 types of minipeptides, as a protein and energy supply, particularly in the treatment of gastrointestinal pathologies.
  • the patent application FR 2 860 976 describes synergistic compositions for improving the bioavailability of polyunsaturated fatty acids, in particular for the treatment of disorders of brain function (memory impairment, depression or psychological disorders).
  • the patent application FR 2,520,232 describes a diet for liver diseases comprising carbohydrates, fats, vitamins, trace elements and a particular mixture of amino acids.
  • the application FR 2 292 437 describes a food for shellfish and fish based on fish waste with vegetable oils and vitamin cocktails.
  • the patent application FR 2 497 068 describes a nutritional composition adapted for enteral feeding, comprising sources of carbohydrates, fat proteins, vitamins, etc., to promote a diet by direct injection of food into the gastrointestinal tract. -intestinal by means of a tube.
  • the patent application FR 2,691,616 describes micronutrient-rich nutritional bio vectors, including in particular fatty acids and vitamin mixtures so as to form pentagonal structures.
  • the patent application FR 2 706 255 polyamine poor food compositions, used in particular as anticancer, analgesic or to stimulate the immune system or to reduce appetite.
  • US 6,403,142 discloses a hypoallergenic food composition for animals comprising hydrolysed proteins.
  • Feed compositions are well known, including carbohydrates, lipids and vitamins.
  • US Patent 5,455,235 discloses a food composition comprising lactosucrose to inhibit the formation of putrefactive products in the intestines. These food compositions include conventional blends of fats, proteins and vitamins.
  • compositions comprising the usual ingredients of this type of compositions. This involves, in particular, associating essential fatty acids with iron as a dietary supplement for pregnant women.
  • the compositions may comprise in particular linoleic and linoleic acids, in a weight ratio of 1/1, vitamin E and vitamin B9.
  • GB patent 806 714 describes an improvement in the stability of pharmaceutical compositions comprising vitamin B 12, optionally with other vitamins and mixtures of fatty acids.
  • the patent application EP 1 302 115 describes a nutritional composition comprising cystathionine to promote cysteine intakes.
  • Patent application EP 689 834 describes a dietary supplement comprising vitamins and minerals with sustained release.
  • US patent application 2002/0032234 describes a dietary supplement for women before and during breastfeeding.
  • This supplement comprises linoleic acid and / or linolenic acid.
  • Compositions comprising in particular linoleic and linoleic acids in a weight ratio of 1/1, vitamin E and vitamin B9 are described.
  • Mixtures of oils and vitamins are also well known in other areas of the state of the art, especially for cosmetic applications.
  • patent application EP 330 583 describes a method for improving the aesthetic appearance of the skin using vitamin cocktails, optionally combined with oils to form topically applicable emulsions.
  • compositions are known from the state of the art, including mixtures of fatty acids, including linoleic and / or linolenic acids, vegetable oils and vitamin cocktails.
  • compositions are not identified for a particular use vis-à-vis the evolution of Alzheimer's disease. This lack of indication with respect to this disease also comes from the choice of fatty acids and oils used in these compositions.
  • the family of polyunsaturated fatty acids includes many subfamilies (omega 3, 6 and 9) and for each of them many compounds. These different compounds according to their chemical structures have different physiological and pharmacological functions.
  • DHA is involved in the synthesis chain of leukotrienes and prostaglandins, reducing their synthesis which leads to an anti-inflammatory effect.
  • linolenic and linoleic acids are inserted in the cell membranes thus making it possible to promote cellular communication and the synthesis of certain neuromediators. It is clear that the type of fatty acid chosen depends on the observed action.
  • the object of the invention is a specific combination of fatty acids and vitamins which, in use, improves the process of slowing the development of the disease by preserving or improving the quality of life of patients.
  • composition according to the invention comprises: a vegetable oil containing at least one linoleic acid and at least one linolenic acid;
  • the weight ratio linoleic acid / linolenic acid being between 3 and 5, preferably about 4.
  • the vegetable oil comprising at least one linoleic acid and at least one linolenic acid is walnut oil.
  • composition according to the invention can be in different forms depending on how it will be administered. It may be a concentrate consisting essentially of the three components defined above.
  • It may be a pharmaceutical-type or nutraceutical composition, where the three components are associated with an acceptable vehicle, more particularly for a oral administration, in forms such as tablets, capsules, powders, granules and oral solutions or suspensions.
  • the combination of the three components according to the invention is mixed with a vehicle such as gelatin, starch, lactose, magnesium stearate, talc, gum Arabic or the like.
  • a vehicle such as gelatin, starch, lactose, magnesium stearate, talc, gum Arabic or the like.
  • the tablets can be coated with sucrose or other suitable materials or they can be treated in such a way that they have prolonged or delayed activity and continuously release a predetermined amount of the combination.
  • a preparation in capsules is obtained by mixing the combination of the three components according to the invention with a diluent and pouring the resulting mixture into soft or hard gelatin capsules.
  • a syrup or elixir preparation may contain the combination of the three components of the invention together with a sweetener, an antiseptic, as well as a flavoring agent and a suitable colorant.
  • the water-dispersible powders or granules may contain the combination of the three components according to the invention mixed with dispersants or wetting agents, or suspending agents, as well as with correcting agents. taste or sweeteners.
  • a usual food composition such as for example cereal bars, drinks, food dishes, products salting and any type of food preparation usually consumed.
  • the amount of each of the three constituents of the composition according to the invention will depend on the mode of administration (1, 2 or more doses) and the daily amount.
  • the daily amount administered to patients of linoleic acid is between 100 and 500 mg, while the daily amount of linolenic acid is between 50 and 200 mg.
  • the daily amount of linoleic acid is 360 mg, while that of linolenic acid is equal to 90 mg.
  • the daily quantity in the composition of the invention is between 5 and 2000 mg.
  • the daily amount of vitamin E chosen is equal to 10 mg.
  • the daily amount of vitamin B9 must be between 100 and 500 ⁇ g, and preferably equal to 200 ⁇ g.
  • the vitamins employed in the composition according to the invention may be vitamins derived from natural extracts or chemical synthesis products.
  • the invention also relates to a use of the above composition for the manufacture of a medicament for delaying the development of Alzheimer's disease or preventing its occurrence.
  • the use of a vegetable oil containing at least one linoleic acid and at least one linolenic acid has been shown to be effective in animal experiments and in human clinical trials in Alzheimer's disease.
  • the acid ratio was optimized by determining the fatty acid profile and cholesterol content of the cortex and nerve endings of these structures. This ratio optimizes the enzymatic kinetics of fatty acid utilization, allowing in particular optimal and maximum conversion to polyunsaturated fatty acids with a very long chain.
  • the main criterion is the improvement, statistically significant, of the following main clinical signs: orientation in space, cooperation (with family, relatives, etc.), mood, organization, memory to short and long term, sleep disorders, wakefulness and attention during the day, hallucinations, expression (can the patient express himself clearly and convey his ideas).
  • the combination of these acids is used in the composition of the invention to improve the quality of life of patients.
  • Vitamin E helps to neutralize free radicals that can accumulate in the body's fatty tissue, and plays a vital role in protecting the cell membrane.
  • vitamin E deficiency in the brain.
  • the use of this substance is therefore indicated to slow the development of the disease.
  • the absorption of vitamin-rich foods, in particular E is strongly correlated with a decrease in the risk of occurrence of the disease, especially in smokers.
  • the antioxidant properties of vitamin E would be responsible for this protective effect for neurons.
  • Vitamin B9 or folates are involved in the metabolism of homocysteine.
  • a first food supplement composition according to the invention is carried out with the following components: - Linoleic acid 360 mg
  • Capsules prepared according to the standard techniques of the pharmaceutical industry may include the following constituents: Modified starch, glycerol, hydrogenated soybean oil, carrageenan, titanium dioxide, soy lecithin, disodium phosphate.
  • Recommendation of use Take one or two capsules per day, at the time of the meals, with a glass of water, during at least 3 months, to renew as much as necessary.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Mycology (AREA)
  • Nutrition Science (AREA)
  • Polymers & Plastics (AREA)
  • Food Science & Technology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Hospice & Palliative Care (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Psychiatry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP06755300A 2005-05-27 2006-05-24 Zusammensetzung zur verlangsamung der entwicklung von morbus alzheimer Withdrawn EP1890689A2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0505365A FR2886154B1 (fr) 2005-05-27 2005-05-27 Composition pour retarder le developpement de la maladie d'alzheimer
PCT/EP2006/062608 WO2006125810A2 (fr) 2005-05-27 2006-05-24 Composition pour retarder le développement de la maladie d'alzheimer

Publications (1)

Publication Number Publication Date
EP1890689A2 true EP1890689A2 (de) 2008-02-27

Family

ID=35466542

Family Applications (1)

Application Number Title Priority Date Filing Date
EP06755300A Withdrawn EP1890689A2 (de) 2005-05-27 2006-05-24 Zusammensetzung zur verlangsamung der entwicklung von morbus alzheimer

Country Status (4)

Country Link
US (1) US20090181974A1 (de)
EP (1) EP1890689A2 (de)
FR (1) FR2886154B1 (de)
WO (1) WO2006125810A2 (de)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2568826A4 (de) 2010-05-13 2014-03-26 Nitromega Corp Nitro-fettsäuren-neuroprotektion und/oder hemmung von kognitiver beeinträchtigung
US10137164B2 (en) * 2015-01-02 2018-11-27 Melaleuca, Inc. Dietary supplement compositions
TWI790189B (zh) 2015-01-02 2023-01-21 美商梅拉洛伊卡公司 細菌組成物
TWI759260B (zh) 2015-01-02 2022-04-01 美商梅拉洛伊卡公司 多元補充品組成物

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JPS57110176A (en) * 1980-12-27 1982-07-08 Snow Brand Milk Prod Co Ltd Nutrious food composition for tube feeding
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Also Published As

Publication number Publication date
WO2006125810A3 (fr) 2007-05-10
WO2006125810A2 (fr) 2006-11-30
US20090181974A1 (en) 2009-07-16
FR2886154A1 (fr) 2006-12-01
FR2886154B1 (fr) 2010-03-26

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