WO2009153200A1 - Préparation contenant de la glucosamine et/ou de la chondroïtine pour la prophylaxie et la thérapie de l'arthrose et pour le renforcement du système immunitaire - Google Patents

Préparation contenant de la glucosamine et/ou de la chondroïtine pour la prophylaxie et la thérapie de l'arthrose et pour le renforcement du système immunitaire Download PDF

Info

Publication number
WO2009153200A1
WO2009153200A1 PCT/EP2009/057171 EP2009057171W WO2009153200A1 WO 2009153200 A1 WO2009153200 A1 WO 2009153200A1 EP 2009057171 W EP2009057171 W EP 2009057171W WO 2009153200 A1 WO2009153200 A1 WO 2009153200A1
Authority
WO
WIPO (PCT)
Prior art keywords
formulation
physiologically acceptable
acid
formulation according
weight
Prior art date
Application number
PCT/EP2009/057171
Other languages
German (de)
English (en)
Inventor
Gertrud Langhoff
Original Assignee
Gertrud Langhoff
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 Gertrud Langhoff filed Critical Gertrud Langhoff
Priority to EP09765780A priority Critical patent/EP2303231A1/fr
Publication of WO2009153200A1 publication Critical patent/WO2009153200A1/fr

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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/737—Sulfated polysaccharides, e.g. chondroitin sulfate, dermatan sulfate
    • 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
    • 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
    • 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
    • A23L33/15—Vitamins
    • 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
    • A23L33/16—Inorganic salts, minerals or trace elements
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7008—Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis

Definitions

  • the invention relates to a liquid, aqueous formulation, a solid which is obtainable from the liquid formulation by drying and a pharmaceutical preparation comprising the formulation or the solid, in particular for the prophylaxis and / or treatment of osteoarthritis in humans and animals. Moreover, the invention relates to the use of the liquid formulation or of the solid as a dietary supplement, dietetic food or cosmetics.
  • both bones of the joint are separated by a joint gap, b) the two bone ends are covered with a cartilage layer, c) in the joint space is the synovial fluid.
  • each articular bone is covered with articular cartilage.
  • the elastic articular cartilage allows in conjunction with the synovial fluid a balanced and low-friction movement.
  • the articular cartilage is also referred to as hyaline cartilage and is unique in its construction.
  • Articular cartilage is characterized by its viscoelastic properties and is ideally adapted to the various biomechanical requirements placed on it. Due to these properties, it is able to provide sufficient support for the differentiated load patterns and weight distributions, while at the same time minimizing the frictional forces involved.
  • the main component of hyaline cartilage is the extracellular matrix, which consists of a network of different collagen fibrils, most notably collagen type II, and proteoglycans. While the collagen fibrils are largely responsible for the structural architecture and biomechanical elasticity of the cartilage and thus provide protection against shear forces, the proteoglycans are responsible for controlling water uptake and release due to their high water binding capacity. Functionally, they can thus adjust the cartilage to different static loads. With the constant intake and release of water, the diet of the chondrocytes in the non-perfused cartilage tissue is ensured at the same time.
  • the cartilage and the synovial fluid form a functional unit. Synovial fluid is a substance that guarantees the metabolism of cartilage. Essential nutrients are supplied to him and degradation products removed. These metabolic processes mediated by the synovial fluid are stimulated by movement. Sufficient movement is thus of crucial importance for the health of the cartilage.
  • the synovial fluid has the special ability to adapt to the different requirements of the movements and thereby protect cartilage and bone.
  • slow movements walking, turning, bending
  • the fluid behaves viscously, spreading evenly throughout the joint space, preventing the cartilaginous layers from rubbing against each other.
  • fast, jerky movements such as running and jumping
  • the synovial fluid behaves like an elastic mass, which absorbs the enormous force effects similar to a shock absorber.
  • the cartilage is not perfused. Nevertheless, like any living tissue, it needs enough nutrients. These are supplied by the synovial fluid. In turn, the synovial fluid receives the nutrients from the peripherally perfused tissue. The better the perfusion of the peripheral tissue, the more efficiently nutrients can be delivered to the synovial fluid and thus to the cartilage.
  • chondroitin that is derived from glucosamine in the body.
  • Glucosamine is much smaller than chondroitin. Because of this, glucosamine is usually better absorbed by the body than chondroitin.
  • the absorption rates for glucosamine sulfate, for example, are above 90%, for chondroitin sulfate at about 5%. Studies have shown that orally ingested glucosamine sulfate is incorporated into the damaged cartilage matrix and the damaged cartilage can be restored.
  • the object of the patent was to provide a nutrient formulation which rapidly supplies the nutrients glucosamine and chondroitin or their physiologically acceptable derivatives to the body and also improves the absorption.
  • Another object of the invention is to enable the absorption of the substances mentioned after administration already through the skin and oral mucosa.
  • therapy should be based on orthomolecular medicine, i. that only substances that the body produces itself or is known to it as natural components come into play.
  • the nutrient formulations can be subjected to spray or freeze-drying, wherein powders are contained in which the vesicular structure is retained and thus rapid absorption is still ensured. That is, when dissolving the powder in water forms the original Emulsion off again. These powders can also be used directly or made into tablets without sacrificing the benefit of rapid resorption.
  • the present invention in a first embodiment is a liquid, aqueous formulation comprising:
  • a component (a) consisting of glucosamine and / or a physiologically acceptable derivative of glucosamine and / or chondroitin and / or a physiologically acceptable derivative of chondroitin,
  • component (b) which consists of phospholipid and / or a physiologically acceptable derivative of a phospholipid
  • a component (c) consisting of a micelle stabilizer selected from the group consisting of
  • polyol (s) selected from the group consisting of: aldoses, ketoses, reduced aldoses and / or ketoses, physiologically acceptable glycosides of aldoses and / or ketoses, C 3 -C 6 -triols, C 3 -C 6 -tetraols, C 3 -C 6 -pentaols and C 3 -C 6 -hexao
  • Component (a) consists of glucosamine and / or a physiologically acceptable derivative of glucosamine and / or chondroitin and / or a physiologically acceptable derivative of chondroitin.
  • Glucosamine (2-amino-2-deoxy-D-glucopyranose) is a derivative of D-glucose.
  • Physiologically acceptable derivatives are, for example, glucosamine sulfate and / or glucosamine hydrochloride.
  • Chondroitin is a mucopolysaccharide consisting of a chain of alternating sugar derivatives (N-acetyl-D-galactosamine and D-glucuronic acid). It is usually used as its sulfuric acid derivative chondroitin sulfate.
  • a natural source of glucosamine and chondroitin or their physiologically acceptable derivatives are mussel extracts, for example extracts of the green-lipped mussel (Perna canaliculus). The extracts are extracted from the mussel meat and then freeze-dried. Mussel extracts are particularly preferred because they are rich in glucosaminoglycans. In a preferred embodiment of the present invention, therefore, a mussel extract is used as component (a).
  • the formulations according to the invention contain mussel extract in amounts of up to 40% by weight, preferably 2-30% by weight, particularly preferably 3-10% by weight.
  • the formulations according to the invention contain glucosamine sulfate and / or chondroitin sulfate.
  • the formulations according to the invention particularly preferably contain glucosamine sulfate and chondroitin sulfate, preferably in a weight ratio of glucosamine sulfate: chondroitin sulfate of 100: 1 to 1: 1, more preferably 50: 1 to 2: 1, particularly preferably 20: 1 to 5: 1.
  • Component (a) is present in an amount of 1 to 60% by weight, preferably 3 to 50% by weight, more preferably 5 to 40% by weight, based in each case on the entire formulation.
  • Component (b) consists of a phospholipid and / or a physiologically acceptable derivative of the phospholipid.
  • phosphatidylcholine obtained from soy, rapeseed, milk, fish or egg lecithin.
  • mixtures of several phospholipids are phosphatidylcholine, phosphatidylethanolamine and phosphatidic acid containing at least 50 to 95% by weight of phosphatidylcholine.
  • Particularly preferred is the use of phospholipids obtained from soybean or egg lecithin.
  • the lecithins may be either unsaturated, hydrogenated, hydrolyzed or hydroxylated.
  • phosphatidylcholines characterized by a chain length of the fatty acid of C 6 to C 2 o. In particular, those phospholipids are preferred which carry a Cs-fatty acid radical.
  • Component (b) is present in an amount of from 0.1 to 30% by weight, preferably from 1 to 15% by weight, particularly preferably from 3 to 8% by weight, based in each case on the entire formulation.
  • Component (c) consists of a micelle stabilizer selected from the group consisting of
  • polyol (s) selected from the group consisting of: aldoses, ketoses, reduced aldoses and / or ketoses, physiologically acceptable glycosides of aldoses and / or ketoses, C 3 -C 6 -triols, C 3 -C 6 tetraols, C 3 -C 6 pentaols and C 3 -C 6 hexaols.
  • Component (c) is preferably selected from L-carnitine and / or physiologically acceptable derivatives such as carnitine tartrate and / or acyl-L-carnitine and from the group consisting of glycerol, pentitols, preferably glucose, fructose, maltodextrin, XyNt or hexitol, in particular sorbitol, mannitol, GuNt or inositol, as well as its physiologically acceptable derivatives such as inositol triphosphate and / or disodium inositol.
  • L-carnitine and / or physiologically acceptable derivatives such as carnitine tartrate and / or acyl-L-carnitine and from the group consisting of glycerol, pentitols, preferably glucose, fructose, maltodextrin, XyNt or hexitol, in particular sorbitol, mannitol, Gu
  • Particularly suitable micelle stabilizers are selected from the group consisting of L-ascorbic acid, sodium ascorbate, sucrose, glycerol and fructose.
  • Component (c) is present in an amount of 5-90% by weight, preferably 15-80% by weight, particularly preferably 25-70% by weight, based in each case on the entire formulation.
  • the formulations according to the invention additionally contain hyaluronic acid or the physiologically acceptable derivatives, such as, for example, Sodium hyaluronate.
  • Hyaluronic acid is a glucosaminoglycan and one of the major components of synovial fluid in the joints.
  • Hyaluronic acid and / or its physiologically acceptable derivatives may be present in an amount of 0.1-5% by weight, preferably 0.2-3% by weight, more preferably 0.3-2% by weight, based in each case on entire formulation.
  • the formulations according to the invention may additionally contain dermatan sulfate, and / or keratan sulfate and / or heparan sulfate.
  • the substituents are preferably present in an amount of up to 10% by weight, preferably 1-8% by weight, more preferably 2-5% by weight, based in each case on the entire formulation.
  • the formulations according to the invention contain L-ascorbic acid and / or physiologically acceptable derivatives thereof.
  • the physiologically acceptable derivatives include the alkali and / or alkaline earth metal salts, such as Na, - K, - Mg, - or calcium ascorbate.
  • the physiologically acceptable derivatives include L-ascorbyl-6-palmitate.
  • the formulations according to the invention additionally contain methylsulfonylmethane in amounts of up to 40% by weight, preferably 2 to 30% by weight, more preferably 3 to 20% by weight.
  • the formulations additionally contain triglycerides containing saturated and / or monounsaturated fatty acids and / or polyunsaturated fatty acids and / or their ethyl esters.
  • oils or fats comprising at least one fatty acid selected from linoleic acid, alpha-linolenic acid, di-homo-gamma-linolenic acid, gamma-linolenic acid, conjugated linoleic acid, eicosapentaenoic acid, docosahexaenoic acid.
  • Particularly preferred is fish oil, krill oil or omega-3 fatty acid ethyl ester.
  • oils or fats are characterized in that they contain the above fatty acids in an amount of 3 to 90 wt .-%, based on the oil or fat.
  • the formulations according to the invention preferably contain medium-chain triglycerides.
  • Medium chain triglycerides (MCT for Medium-Chain Triglycerides) are an ester compound of medium chain fatty acids and glycerol.
  • the medium-chain fatty acids consist of a carbon chain with 6 to 12 carbon atoms.
  • the medium chain fatty acids are preferably saturated.
  • Fish oil and krill oil are distinguished by the fact that they contain 10 to 35% by weight of eicosapentaenoic acid and docosahexaenoic acid in the form of their triglycerides, based on the fish oil.
  • Omega-3-Fettklareethylester characterized by the fact that they contain 10 to 90 wt .-% omega-3 fatty acids.
  • the formulation may additionally contain vegetable ingredients or plant extracts of red wine, Cistrus fruits, blueberry, acerola, elderberry, frankincense, red clover, ginseng or turmeric, for example flavonoids / anthocyanidins such as OPC (oligomeric procyanidins), quercetin, naringin, rutin, chrysin, ginsenoids or others, such as the trans-stilbene derivative resveratrol.
  • the plant constituents are preferably present in an amount of up to 80% by weight, more preferably 1 to 60% by weight, in particular 5 to 30% by weight, based in each case on the entire formulation.
  • Secondary plant substances such as OPC (oligomeric procyanidins), resveratrol or rutin, whose absorption is usually very poor, can be well absorbed with the formulations according to the invention. These substances are characterized by excellent radical scavenging properties and are therefore an ideal complement.
  • OPC oligomeric procyanidins
  • resveratrol or rutin whose absorption is usually very poor
  • these substances are characterized by excellent radical scavenging properties and are therefore an ideal complement.
  • the plant extracts to be used according to the invention are absorbed much better by the body, and this also without the use of alcohol. Due to the greatly improved absorption of smaller amounts of these substances must be used to achieve a positive effect effect.
  • the formulations may additionally contain one or more ingredients selected from taurine, beta carotene, vitamin A, lycopene, zeaxanthin, astaxanthin, vitamin K, vitamin E, tocotrienols, vitamin K, biologically active selenide derivatives, or one or more water soluble vitamins ,
  • the formulations may comprise one or more elements in their physiologically acceptable form selected from the group consisting of boron, iron, copper, manganese, zinc, molybdenum and chromium.
  • the formulation according to the invention may furthermore contain independently of one another:
  • vitamin E 0.1 to 5 parts by weight, preferably 0.3 to 2 parts by weight of vitamin E.
  • water-soluble vitamins and / or its physiologically acceptable derivatives include thiamine, riboflavin, niacin, NADH, NADPH, pyridoxine,
  • Pantothenic acid, biotin, folic acid and cobalamin in the following proportions by weight: Vitamin From To Preferred From Preferred To
  • Pantothenic acid 0.01 0.1 0.03 0.08
  • One or more elements in their physiologically compatible form selected from the group consisting of boron, iron, copper, iodine, manganese, zinc, molybdenum and chromium.
  • the formulations according to the invention may be present as a nutrient preparation and may additionally contain extracts of Stevia rebandiana.
  • the formulations contain extracts of Stevia rebaudiana containing about 10-25% by weight of steviol glycosides, based on the dry extract, which have about 300 times more sweetening power than sugar.
  • the formulations preferably contain 0.1 to 20% by weight, more preferably 0.2 to 10% by weight, in particular 0.3 to 2% by weight, based in each case on the entire formulation.
  • the formulation is substantially free of primary volatile alcohols (VOC) and / or ethoxylated or other synthetic surfactants, in particular substantially free of ethanol.
  • the formulation coenzyme Q10 also contains ubiquinone or its physiologically acceptable derivatives.
  • physiologically acceptable derivatives are coenzyme Q3, coenzyme Q4, coenzyme Q5, coenzyme Q6, coenzyme Q7, coenzyme Q8 or coenzyme Q9.
  • the formulation preferably contains coenzyme Q 10 and / or its physiologically acceptable derivatives in an amount of 0.1-20% by weight, preferably 0.2-8% by weight, particularly preferably 0.3-4% by weight, in each case based on the entire formulation.
  • the formulations preferably taurine and / or their physiologically acceptable derivatives such as e.g. Taurine chloramine and / or taurine bromine.
  • the component is preferably present in an amount of 0.1-50% by weight, preferably 0.5-30% by weight, more preferably 1-10% by weight, based on the total formulation.
  • the formulations may comprise silicic acids, for example ortho or meta-silicic acids, in particular water-soluble silicic acids.
  • the silicas may preferably be used in amounts of from 0.1 to 8% by weight, based on the formulation.
  • customary constituents such as flavorings, dyes, thickeners and customary physiologically acceptable release agents may be present in the formulations according to the invention.
  • the liquid aqueous formulations according to the invention form vesicular structures.
  • the formation of the vesicular structures also makes it possible to produce concentrated liquid formulations which, for example, have a water content of less than 40% by weight, based on the total formulation.
  • the liquid aqueous formulations are present as an emulsion in the form of a micellar concentrate.
  • the micelles in the liquid, aqueous formulations according to the invention preferably have an average diameter of less than 300 nm, preferably from 10 to 250 nm, more preferably from 50 to 230 nm and in particular from 130 to 210 nm or 50 to 130 nm.
  • the liquid aqueous formulations according to the present invention are transparent to translucent.
  • the mean diameter of the vesicular structures can be determined by methods known to those skilled in the art, for example a Coulter Counter N24. For this purpose are at Room temperature (25 ° C) diluted a few drops of a sample with distilled water and placed in a cuvette. Subsequently, the average particle size is determined by means of light scattering.
  • the preparation of the formulation according to the invention can be carried out by means of commercial high-pressure homogenizers with which the formulations according to the invention are homogenized.
  • the present formulations according to the invention are present as a nano-emulsion (average diameter of the micelles from 10 to 250 nm), the formulations can be rapidly absorbed by the body.
  • the formulations according to the invention in particular the micellar concentrates, lead to a significantly faster and increased absorption of both hydrophilic and lipophilic constituents.
  • the present aqueous liquid formulations are present as nano-emulsions, it is also possible to work without synthetic emulsifiers or co-emulsifiers and alcohols (ethanol).
  • the formulations according to the invention are preferably homogenized formulations, in particular homogenized emulsions.
  • aqueous formulations according to the invention offer the following advantages over conventional crystalline or conventional administration forms of glucosamine, and / or chondroitin sulfate:
  • the active ingredient ie the glucosamine, and / or chondroitin sulfate is present in vesicles.
  • the vesicles have a very large surface, resulting in a large interaction area.
  • the vesicles are stabilized by a phospholipid layer.
  • the active substance vesicles have a modified particle surface which is hydrophilic and therefore allows the free mobility of the vesicles in an aqueous environment.
  • the nanoscale vesicles have an increased solution pressure, which significantly improves the absorption capacity.
  • nano-emulsions are particularly effective for the therapy and prophylaxis of osteoarthritis in humans and animals.
  • the formulations according to the invention can moreover be fed directly, ie unchanged and without further auxiliaries, to a suitable drying process, it being possible to obtain nanoscale vesicularly structured powders.
  • the formulations according to the invention can also be dried.
  • Another object of the present invention is therefore a solid, obtainable from a formulation according to the invention by drying, preferably spray-drying or freeze-drying. It has surprisingly been found that the micellar structure is retained in the dried solids, so that the dissolution of the solid in water, the original micellar / vesicular emulsion structured can be recovered. This has considerable advantages since it allows the formulation according to the invention to be formulated simply as solid preparations.
  • the solids according to the invention are such that they additionally contain a polycarboxylic acid, preferably citric acid and / or polycarboxylic acid salt, preferably citric acid salt, in particular calcium and / or magnesium citrate or gluconic acid and / or gluconic acid salt, in particular Na, Mg or Ca.
  • Gluconates have.
  • the solids according to the invention are present in such a way that they additionally have bicarbonate, preferably sodium bicarbonate.
  • Another object is a granule, a chewable tablet, a tablet, dragee or capsule containing the solid according to the invention.
  • Another object of the present invention is a pharmaceutical preparation comprising a formulation according to the invention or a solid according to the invention.
  • Another object is a pharmaceutical preparation comprising a formulation according to the invention or a solid according to the invention for the therapy or prophylaxis of joint diseases, in particular arthritis in humans and animals.
  • the pharmaceutical preparation according to the invention is generally metered so that the amount of the amounts of component (a), preferably glucosamine sulphate, administered to the body is between 20 and 2000 mg / day, preferably 450 to 1500 mg / day, more preferably 200 to 1000 mg / Day (and individual with a body weight of 75 kg).
  • component (a) preferably glucosamine sulphate
  • the quantitative proportions of components (b) and (c) may be calculated based on the amount of component (c) based on their percentages mentioned above.
  • the preparation according to the invention can be administered in several single doses throughout the day. In addition, it is also possible to administer the components (a) to (c) individually.
  • kits of parts comprising the components (a) to (c), wherein at least one of the components is spatially separated from the other.
  • the kit of parts can be a container in which there are two or more compartments containing components (a) to (c).
  • the individual components can be present independently of one another in the form of a micellar concentrate, a spray-dried or freeze-dried powder or tablets, dragees, capsules obtained therefrom.
  • the kit according to the invention comprises at least one compartment and an additional container, two of the components selected from components (a) to (c) being contained in at least one of the compartments and / or in the container.
  • Another object of the present invention is a process for the preparation of a composition, characterized in that a liquid aqueous formulation of the emulsion-type, water-soluble, concentrate is spray-dried or freeze-dried such that micelles are retained in the resulting dried product.
  • the drying is preferably carried out at temperatures below 100 0 C.
  • the drying can also be such that partial components of the formulation according to the invention are converted into a solid and the remaining components are then applied to the already formed solids, preferably sprayed.
  • the emulsion-type, water-soluble concentrate may be used together with another aqueous formulation A containing a polycarboxylic acid, preferably citric acid and / or polycarboxylic acid salt, preferably citric acid salt, especially calcium and / or magnesium citrate or gluconic acid and / or gluconic acid salt, especially Na, Mg or Ca Gluconate, the spray or freeze-drying is fed, preferably such that micelles are retained in the dried material.
  • Another object of the present invention is a gel comprising the liquid formulation of the invention or the solid according to the invention.
  • the gels according to the invention are preferably obtainable in which a gelling agent, for example xanthan gum, is added to the aqueous formulation according to the invention.
  • the gel is particularly suitable for topical applications.
  • formulations or gels according to the invention can be topically applied to the bodies of the human and animal body which are affected by osteoarthritis.
  • the formulations or gels according to the invention also act transdermally. This applies in particular to the formulations with a mean vesicle size in the range from 10 to 250 nm.
  • the pharmaceutical preparations can therefore also be used for the topical therapy and prophylaxis of joint diseases, in particular arthrosis in humans and animals.
  • Another object of the present invention is therefore the use of the formulation according to the invention for the prophylaxis and therapy of osteoarthritis.
  • the nutrient preparation or the formulation according to the invention in a process for the preparation of nutrient preparations, preferably in a process for the preparation of a nutrient preparation for the prophylaxis and therapy of joint diseases, in particular arthritis in humans and animals.
  • Another object of the present invention is also the use of the formulation of the invention or the solid or gel according to the invention as a dietary supplement, dietetic food, pharmaceutical or cosmetic in humans and animals.
  • the raw materials are dispersed in water and homogenized with soy phospholipid.
  • Homogenizer Panda 2K, NS 10012 from Niro Soavi .; Temp: 25 ° C; at 400bar.
  • Average particle size of the micelles of the micellar concentrate 50 nm
  • the raw materials are dispersed in water and homogenized with soy phospholipid.
  • Homogenizer Panda 2K, NS 10012 from Niro Soavi .; Temp: 25 ° C; at 400bar.
  • the raw materials are dispersed in water and homogenized with soy phospholipid.
  • Homogenizer Panda 2K, NS 10012 from Niro Soavi .; Temp: 25 ° C; at 400bar.
  • Average particle size of the micelles of the micellar concentrate 150 nm
  • the emulsion of example 3 can be made into a gel with a content of 2% xanthan, based on the entire formulation. This gel can also be used for skin care or topical treatment of osteoarthritis on the affected joint.
  • the raw materials are dispersed in water and homogenized together with soy phospholipid.
  • Homogenizer Panda 2K, NS 10012 from Niro Soavi .; Temp: 25 ° C; at 400bar.
  • Average particle size of the micelles of the micellar concentrate 190 nm
  • the emulsion thus obtained is subsequently freeze-dried.
  • the Soluthin MD ® is sprayed at 70 0 C in the dry space with a 5% aqueous solution of glucosamine sulphate.
  • Example 3 On the basis of the emulsion of Example 3, a human observational study was performed, the duration of which extended over 6 weeks. The two comparison groups each consisted of 5 subjects (all aged between 53 and 75 years). The subjects equally suffered from hip arthrosis. All patients took a non-steroidal anti-inflammatory drug at the beginning of the study, which had to be taken daily.
  • capsules were administered orally in the comparison group with 5 subjects daily, in which the components glucosamine sulfate, chondroitin sulfate and coenzyme Q10 in powder form in appropriate amounts, as in Example 3, were present.
  • composition used Capsules with powdery constituents (not according to the invention)
  • Example 3 The success of the emulsion from Example 3 is already clearly noticeable after 6 weeks (in some cases a success was observed already after 10 days). In particular, the subjects were also able to significantly reduce the frequency of taking painkillers.
  • Example 4 On the basis of the freeze-dried emulsion of Example 4, an observational study was carried out on dogs. On average, the dogs had a weight of 25 kg. The two comparison groups each consisted of 5 dogs. All dogs suffered equally from hip arthrosis and were treated daily with a nonsteroidal anti-inflammatory drug.
  • the amount of mussel extract supplied was identical in both experimental groups.
  • the dogs were subjectively rated.
  • a “1” means that the mobility of the dogs in the morning is comparable to that of non-diseased dogs, i.e. that the agent used has a very good effect.
  • the rating "5" means that for the dog the mobility in the morning did not change over the experimental period, i.e. that the agent has no effect.
  • the dogs were also rated subjectively.
  • a “1” means that the mobility of the dogs is comparable to that of non-affected dogs.
  • the rating “5" means that the dog's enjoyment of exercise has not changed over the experimental period, that is, the agent has no effect.
  • the solid according to the invention shows a significant improvement in the mobility in the morning, as well as in the joy of movement. It is noteworthy that an improvement was observed in part already after 1 week.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Polymers & Plastics (AREA)
  • Food Science & Technology (AREA)
  • Nutrition Science (AREA)
  • Mycology (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Biophysics (AREA)
  • Inorganic Chemistry (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dispersion Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne une formulation aqueuse liquide, qui comprend : 1 à 60 % en poids d'un composant (a), qui est constitué de glucosamine et/ou d'un dérivé physiologiquement acceptable de glucosamine et/ou de chondroïtine et/ou d'un dérivé physiologiquement acceptable de chondroïtine, 0,1 à 30 % en poids d'un composant (b), qui est constitué d'un phospholipide et/ou d'un dérivé physiologiquement acceptable d'un phospholipide, et 5 à 90 % en poids d'un composant (c), qui est constitué d'un stabilisateur de micelles, choisi dans le groupe constitué de (c1) la carnitine et/ou un dérivé physiologiquement compatible de carnitine et (c2) un ou plusieurs polyols, choisis dans le groupe constitué des : aldoses, cétoses, aldoses et/ou cétoses réduits, glycosides physiologiquement acceptables d’aldoses et/ou de cétoses, triols en C3-C6, tétraols en C3-C6, pentaols en C3-C6 et hexaols en C3-C6, les quantités en poids se rapportant à chaque fois à la totalité de la formulation.
PCT/EP2009/057171 2008-06-18 2009-06-10 Préparation contenant de la glucosamine et/ou de la chondroïtine pour la prophylaxie et la thérapie de l'arthrose et pour le renforcement du système immunitaire WO2009153200A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP09765780A EP2303231A1 (fr) 2008-06-18 2009-06-10 Préparation contenant de la glucosamine et/ou de la chondroïtine pour la prophylaxie et la thérapie de l'arthrose et pour le renforcement du système immunitaire

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE202008008059.2 2008-06-18
DE202008008059U DE202008008059U1 (de) 2008-06-18 2008-06-18 Zusammensetzung zur Prophylaxe und Therapie der Arthrose

Publications (1)

Publication Number Publication Date
WO2009153200A1 true WO2009153200A1 (fr) 2009-12-23

Family

ID=40934147

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2009/057171 WO2009153200A1 (fr) 2008-06-18 2009-06-10 Préparation contenant de la glucosamine et/ou de la chondroïtine pour la prophylaxie et la thérapie de l'arthrose et pour le renforcement du système immunitaire

Country Status (3)

Country Link
EP (1) EP2303231A1 (fr)
DE (1) DE202008008059U1 (fr)
WO (1) WO2009153200A1 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102010003550A1 (de) * 2010-03-31 2011-10-06 Medivatis Gmbh Futtermittel zur Vorbeugung und Linderung von Gelenkbeschwerden
CN103463624A (zh) * 2013-09-22 2013-12-25 徐波 一种骨关节复合营养强化剂及其制备方法
EP2944312A1 (fr) * 2014-05-16 2015-11-18 TP Tumapharma Ltd Préparation de combinaison, comprenant de la glucosamine et du sulfate de chondroïtine
CN105769885A (zh) * 2016-03-23 2016-07-20 北京康力基生物科技有限公司 改善骨关节疾病的药物组合物、崩解片及其制备方法
CN115737910A (zh) * 2021-09-03 2023-03-07 青岛农业大学 一种促进软骨高效分泌粘多糖的硫酸软骨素/甘油二酯纳米乳液制备方法

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102011105703A1 (de) * 2011-06-22 2012-12-27 Wolfgang Langhoff Diätetikum zur Behandlung mitochondrialer Dysfunktionen
FR3009963B1 (fr) * 2013-09-03 2017-03-03 Biolis Composition de lutte contre les troubles de la locomotion
EA025549B1 (ru) * 2014-09-09 2017-01-30 Замертон Холдингс Лимитед Композиция и средства для профилактики и лечения заболеваний суставов и позвоночника и способы их применения

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050142194A1 (en) * 2003-12-30 2005-06-30 Altergon S.A. Composition comprising CS
US20050181047A1 (en) * 2004-02-18 2005-08-18 Jaime Romero Compositions and methods for timed release of water-soluble nutritional supplements
WO2008000534A1 (fr) * 2006-06-30 2008-01-03 Gertrud Langhoff Formulations de solubilisât

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050142194A1 (en) * 2003-12-30 2005-06-30 Altergon S.A. Composition comprising CS
US20050181047A1 (en) * 2004-02-18 2005-08-18 Jaime Romero Compositions and methods for timed release of water-soluble nutritional supplements
WO2008000534A1 (fr) * 2006-06-30 2008-01-03 Gertrud Langhoff Formulations de solubilisât

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ROTE LISTE SERVICE GMBH: "Rote Liste 2002", 2002, ECV EDITION CANTOR VERLAG AULENDORF, AULENDORF, XP002541038 *

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102010003550A1 (de) * 2010-03-31 2011-10-06 Medivatis Gmbh Futtermittel zur Vorbeugung und Linderung von Gelenkbeschwerden
DE102010003550B4 (de) * 2010-03-31 2015-04-16 Vievital Gmbh Futtermittel zur Vorbeugung und Linderung von Gelenkbeschwerden
CN103463624A (zh) * 2013-09-22 2013-12-25 徐波 一种骨关节复合营养强化剂及其制备方法
EP2944312A1 (fr) * 2014-05-16 2015-11-18 TP Tumapharma Ltd Préparation de combinaison, comprenant de la glucosamine et du sulfate de chondroïtine
CN105769885A (zh) * 2016-03-23 2016-07-20 北京康力基生物科技有限公司 改善骨关节疾病的药物组合物、崩解片及其制备方法
CN115737910A (zh) * 2021-09-03 2023-03-07 青岛农业大学 一种促进软骨高效分泌粘多糖的硫酸软骨素/甘油二酯纳米乳液制备方法
CN115737910B (zh) * 2021-09-03 2024-04-05 青岛农业大学 一种促进软骨高效分泌粘多糖的硫酸软骨素/甘油二酯纳米乳液制备方法

Also Published As

Publication number Publication date
EP2303231A1 (fr) 2011-04-06
DE202008008059U1 (de) 2009-10-29

Similar Documents

Publication Publication Date Title
WO2009153200A1 (fr) Préparation contenant de la glucosamine et/ou de la chondroïtine pour la prophylaxie et la thérapie de l'arthrose et pour le renforcement du système immunitaire
DE60032778T2 (de) Zusammensetzungen für stabile Karotin-Xanthophyl enthaltende Kapseln und Methoden zum Gebrauch
DE69822832T2 (de) Therapeutische und lebensmittel-zusammensetzungen, welche essentielle fettsäuren und bioaktive disulfide enthalten
DE102008034944B4 (de) Mikroemulsion
DE60221367T2 (de) ZUSAMMENSETZUNG ZUR PRÄVENTION VON OSTEOPOROSE bestehend aus EINER KOMBINATION AUS ISOFLAVONEN UND POLYUNGESÄTTIGTEN FETTSÄUREN
DE2648551A1 (de) Gemisch aus fettsaeure-polyol-polyestern und vitaminen fuer ernaehrungs- und pharmazeutische zwecke
EP1377273B1 (fr) Procede de production d'un concentre d'isoflavone
DE202011050351U1 (de) Diätetische Erzeugnisse bzw. Formulierungen
WO2006040324A1 (fr) Compositions contenant des acides gras omega-3 et omega-6
EP1135146A1 (fr) Composition pharmaceutique contenant de l'huile de poisson, de la vitamine e et c et de l'acide acetylsalicylique contre l'arteriosclerose
WO2010057804A1 (fr) Émulsion grasse pour l'alimentation artificielle de patients gravement malades en soins intensifs
DE10326822A1 (de) Mittel zur Nahrungsergänzung, dieses Mittel enthaltende pharmazeutische Präparate und Verwendungen des Mittels
EP1660097B1 (fr) Composition physiologiquement active a base de phosphatidylserine
DE102009012465A1 (de) Pharmazeutische Zusammensetzung zur Prophylaxe und Behandlung der Arteriosklerose, sowie zur Schmerzbekämpfung und zur Entzündungshemmung
DE19733892C2 (de) Bestrahlungsschutz-Verfahren
DE4405545A1 (de) Fettlösliche Vitamine enthaltende Zubereitung zur oralen Applikation
DE60124516T3 (de) Kombination des lezithins mit ascorbinsäure
DE202013002498U1 (de) Futtermittelzusatz für Nutz- und Haustiere
DE202004013660U1 (de) Vitamin-enthaltendes Produkt
DE102007056424A1 (de) Pharmazeutische Zusammensetzung, enthaltend eine Öl/Wasser-Emulsion
EP1529524B1 (fr) Gélule comprenant des vitamines liposolubles et des acides gras essentiels
DE60319131T2 (de) Dicolfenac-haltige liposomale schmerzstillende formulierung und ihre verwendung zur behandlung von pferden
DE102009011742A1 (de) Nährstoffzubereitung und pharmazeutische Zusammensetzung zur Behandlung und Prophylaxe der Migräne
DE102016002090A1 (de) Komposition für die Nahrungsergänzung menschlicher Ernährung und deren Verwendung
DE10317922B4 (de) Verwendung eines Kombinationspräparates aus oralem Kontrazeptivum und Calcium/Vitamin D

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 09765780

Country of ref document: EP

Kind code of ref document: A1

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 2009765780

Country of ref document: EP