DE202008008059U1 - Composition for the prophylaxis and therapy of osteoarthritis - Google Patents

Abstract

Liquid, aqueous formulation comprising:
an active substance (a) selected from
(a1) glucosamine and / or its physiologically acceptable derivatives or
(a2) chondroitin and / or its physiologically acceptable derivatives; and additionally at least
(b) phospholipid and / or its physiologically acceptable derivatives,
characterized in that the components are present in the following amounts:
(a) 1 to 60% by weight, and
(b) 0.1 to 30% by weight,
wherein the weights in each case relate to the entire formulation.

Description

The The invention relates to an aqueous Formulation and a solid obtained therefrom as the nutrient preparation can be used. About that In addition, the invention relates to a pharmaceutical, in particular a Medicines for the prophylaxis and treatment of osteoarthritis of humans and animal.

• – beide Knochen des Gelenkes sind durch einen Gelenkspalt voneinander getrennt;
• – die beiden Konochenenden sind mit einer Knorpelschicht überzogen;
• – im Gelekspalt befindet sich die Synovialflüssigkeit.

The structure of the joints of the human body is principally characterized by three features:

• - Both bones of the joint are separated by a joint space;
• - the two ends of the batter are covered with a layer of cartilage;
• - in the gel slit is the synovial fluid.

The Ends of each articular bone are covered with articular cartilage. The elastic articular cartilage allows in conjunction with the synovial fluid a balanced and low-friction movement.

physiological the articular cartilage is also called hyaline cartilage and is unique in its construction. Articular cartilage stands out its viscoelastic property and is the different biomechanical demands placed on him are ideal customized. These properties make it capable of differentiated load patterns and weight distributions, the involved joints to provide sufficient support and at the same time the resulting frictional forces to minimize.

Of the The main component of hyaline cartilage is the extracellular matrix, those from a network of different collagen fibrils, especially collagen type II, and proteoglycans. While the Collagen fibrils largely for the structural architecture and the biomechanical elasticity of the cartilage responsible and thus also provide protection against shear forces, are the proteoglycans because of their high water binding capacity for the Control of water absorption and delivery responsible. Functionally they can So set the cartilage to different static loads. With the permanent The intake and release of water will be the nutrition of the same time Chondrocytes in the non-perfused cartilage ensured.

Of the Cartilage and synovial fluid form a functional unit. Synovial fluid is a substance which guarantees the metabolism of the cartilage.

essential nutrient be fed to him and degradation products removed. These metabolic processes conveyed through the synovial fluid are stimulated by exercise. Sufficient movement is thus crucial for the health of the cartilage.

The synovial fluid has the special ability to adapt to the different requirements of the movements and thereby protecting cartilage and bones. For slow movements (walking, Turning, bending) behaves the liquid viscous, by getting even in the joint space distributed and so prevents the rubbing together of the cartilage layers. In fast, jerky Movements, such as running and jumping, on the other hand, behave the synovial fluid like an elastic mass that is similar a shock absorber the cushioning tremendous power effects.

Of the Cartilage is not perfused. Nevertheless, like every living tissue, he needs it enough nutrients. These are supplied to him by the synovial fluid. turn receives the synovial fluid the nutrients from the peripherally perfused tissue. The better the blood circulation Of the peripheral tissue, the more efficient nutrients can be to the synovial fluid and thus be delivered to the cartilage.

from that It can be seen that, in addition to a balanced diet, too sufficient movement for the Preservation of healthy cartilage and joints imperative requirement is. If there is no movement the synovial fluid loses in viscosity and elasticity. The, cartilage is cracked in a row and may possibly disappear completely, so that the bone ends are exposed. This process is like this painful, that even simple movements are painful, it comes to joint arthrosis. This creates a circus vituosis, a self-reinforcing one Circulation. Due to the pain, the joint becomes less Moving and through the lower movement will increase the metabolism Joint sustainably damaged.

Therefore, of prime importance are mechanisms that support the occurrence or healing of joint arthrosis by prophylactic and therapeutic measures. To date, there is no causal pharmacological osteoarthritis therapy. However, there are substances that stop cartilage loss and the general joint function sustainably improved. These substances are glucosamine and chondroitin.

glucosamine gets from the healthy youthful body even made from ingredients of the food. It is as a ground substance for cartilage, synovial fluid, Tendons, bones, but also for the connective tissue of the arterial walls irreplaceable.

analog applies to Chondroitin that is derived from glucosamine in the body. glucosamine is much smaller than chondroitin. That's why glucosamine is used usually better from the body taken as chondroitin. The absorption rates for glucosamine sulfate for example, are above 90%, for chondroitin sulfate at about 5%. Studies have shown that ingested glucosamine sulfate in the injured Cartilage matrix is stored and the damaged cartilage restored can be.

With As you age, the body loses more and more the ability To absorb chondroitin sulfate and glucosamine sulfate from the diet. Negative effects also have the changing food habits. Cartilage and connective tissue are present in most people today not on the menu anymore. As a result of a lack of these Both substances in the diet, the synovial fluid is reduced. In the further course erosions occur.

task the present invention was now to provide a nutrient formulation which the nutrients Glucosamine and chondroitin supplies very quickly to the body and also the chondroitin absorption improved. Another object of the invention was to absorb the substances mentioned after oral administration already on the To allow skin and oral mucosa. At the same time should be exclusive Substances that the body makes itself or as natural ingredients are known.

Surprised has now been found that with a formulation of phospholipids, Glucosamine and / or chondroitin, a very rapid onset of action Arthrosis prophylaxis and therapy already achieved via mucous membranes can be at the same time in an experimental studies, positive subjective rating of the people evoked. On the use Synthetic Coemulgatoren can also be dispensed with.

It also became surprising found that the liquid Formulations of a spray or freeze-drying supplied can be containing powders in which the micellar structure is obtained remains and thus ensures rapid absorption continues is. That is, at resolution of the powder in water, the original emulsion forms again. These powders can also used directly or processed into tablets, without losing the benefit of rapid absorption.

• (a1) Glucosamin und/oder dessen physiologisch akzeptablen Derivate oder
• (a2) Chondroitin und/oder dessen physiologisch akzeptablen Derivate; und
• (b) Phospholipid und/oder dessen physiologisch akzeptablen Derivate

dadurch gekennzeichnet, dass die Komponenten in den folgenden Mengen vorliegen:

• (a) 1 bis 60 Gew.-%, und
• (b) 0,1 bis 30 Gew.-%,

wobei sich die Gewichtsangaben jeweils auf die gesamte Formulierung beziehen.The present invention in a first embodiment is a liquid, aqueous formulation comprising:
an active substance (a) selected from

• (a1) glucosamine and / or its physiologically acceptable derivatives or
• (a2) chondroitin and / or its physiologically acceptable derivatives; and
• (b) phospholipid and / or its physiologically acceptable derivatives

characterized in that the components are present in the following amounts:

• (a) 1 to 60% by weight, and
• (b) 0.1 to 30% by weight,

wherein the weights in each case relate to the entire formulation.

active substance (a) is preferably glucosamine and / or chondroitin.

glucosamine (2-amino-2-deoxy-D-glucopyranose) is a derivative of D-glucose. Physiologically acceptable derivatives are, for example, the physiological acceptable Salts, such as glucosamine sulfate and / or glucosamine hydrochloride. Chondroitin sulfate is a sulfated mucopolysaccharide which from a chain of alternating sugar derivatives (N-acetyl-D-galactosamine and D-glucuronic acid) consists. It is usually considered to be its derivative of chondroitin sulfate used.

Component (a) is particularly preferred in an amount of 1-60% by weight, preferably 3-50% by weight At least 5-40 wt .-%, in each case based on the entire formulation before.

Component (b) is a phospholipid, preferably lecithin. Particularly preferred is the use of phosphatidylcholine obtained from soybean or egg lecithin. Also particularly preferred are phosphatidylcholines characterized by a chain length of the fatty acid of C ₆ to C ₂₀ , in particular octanoates.

It It has been shown that the use of phospholipids is an important Function for the stabilization and emulsification of the aqueous formulation takes over.

component (b) is in an amount of 0.1-30% by weight, preferably 1-15% by weight, particularly preferred 3-8 Wt .-%, each based on the total formulation before.

In addition, the formulations according to the invention a micelle stabilizer (c) included.

• (c1) Carnitin und/oder einem physiologisch verträglichen Carnitin-Derivat und/oder
• (c2) einem oder mehrere Polyol(e), ausgewählt aus der Gruppe umfassend: Aldosen, Ketosen, reduzierte Aldosen und/oder Ketosen, physiologisch akzeptable Glycoside von Aldosen und/oder Ketosen, C₃-C₆-Tri, -Tetra- -Penta- oder -Hexaole.

Component (c) is preferably selected from

• (c1) carnitine and / or a physiologically acceptable carnitine derivative and / or
• (c2) one or more polyol (s) selected from the group comprising: aldoses, ketoses, reduced aldoses and / or ketoses, physiologically acceptable glycosides of aldoses and / or ketoses, C ₃ -C ₆ -Tri, -Tetra- Penta or hexaole.

Prefers are glucose, fructose, glycerol, pentite, more preferably xylitol or hexites, especially sorbitol, mannitol, gulite or inositol, as well as its physiologically acceptable derivatives, such as. B. inositol triphosphate and / or disodium inositol.

component (c) is preferably present in an amount of 5-90% by weight, preferably 15-80% by weight, particularly preferred 25-70 Wt .-%, each based on the total formulation before.

In a further preferred embodiment contain the formulations according to the invention additionally hyaluronic acid or its physiologically acceptable derivatives such. For example, sodium hyaluronate. hyaluronic acid is a glycosaminoglycan 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 Wt .-%, particularly preferably 0.3-2 Wt .-%, each based on the total formulation, are present.

Furthermore can the formulations according to the invention additionally Dermatan sulfate, and / or keratan sulfate and / or heparan sulfate. The substances are preferably in an amount up to 10 wt .-%, preferably 1-8% by weight, more preferably 2-5 Wt .-%, each based on the total formulation included.

In a further embodiment contain the nutrient according to the invention Preparations in addition L-ascorbic acid and / or their physiologically acceptable derivatives. To the physiological include acceptable derivatives the alkali and / or alkaline earth metal salts, such as Na, - K, - Mg, - or Calcium ascorbate. Continues to count to the physiologically acceptable derivatives L-ascorbyl-6-palmitate. L-ascorbic acid and / or its physiologically acceptable derivatives can be used in from 0.1 to 30% by weight, preferably from 0.5 to 15% by weight, particularly preferably 0.8 to 10 wt .-%, each based on the total Formulation, present.

In a further embodiment contain the formulations according to the invention additionally MSM in amounts up to 40 wt .-%, preferably 2-30 wt .-%, particularly preferably 3-20% by weight, in each case based on the entire formulation.

In a further embodiment In the present invention, the nutrient preparations additionally contain triglycerides comprising polyunsaturated fatty acids and / or polyunsaturated fatty acids and / or their ethyl esters. Preferably used are oils or Fats that are selected from at least one fatty acid linoleic acid, alpha-linolenic acid, di-homo-gamma-linolenic acid, gamma-linolenic acid, conjugated linoleic acid. Particularly preferred is fish oil, krill oil or omega-3 fatty acid ethyl ester.

The oils or Fats are characterized by the fact that they contain the fatty acids mentioned above an amount of from 3 to 90% by weight, based on the oil or fat, contain.

Draw fish oil and krill oil characterized in that they 10 to 35 wt .-% eicosapentaenoic acid and docosahexaenoic acid in the form of their triglycerides, based on the fish oil.

Omega-3 fatty acid ethyl esters are characterized by the fact that they contain 10 to 90 wt .-% omega-3 fatty acids.

These Substances can up to 40% by weight, preferably 2 to 30% by weight, more preferably 3 to 20 wt .-%, each based on the formulation be.

Furthermore can the wording additionally herbal ingredients or herbal extracts of red wine, cistus fruits, blueberries, Acerola, elderberry, frankincense or red clover, preferably, flavonoids / anthocyanidins such as OPC (oligomeric procyanidins), quercetin, naringin, Rutin, chrysin, or others such as resveratrol. Preferably, the plant ingredients are in an amount to to 80 wt .-%, particularly preferably 1 to 60 wt .-%, in particular 5-30% by weight, each based on the entire formulation.

Secondary plant substances such as OPC (oligomeric procyanidins), resveratrol or rutin, their absorption usually is very poor, can be with the formulations of the invention absorb well. These substances are characterized by excellent radically catching properties and are therefore an ideal complement. Especially in the nanoemulsions according to the invention are used according to the invention Plant extracts are absorbed much better by the body, and so too without the use of alcohol. Due to the greatly improved absorption have to lower amounts of these substances are used to make a positive Effect effect.

Furthermore can the formulations in addition one or more ingredients selected from taurine, beta-carotene, Vitamin A, Lycopene, Zeaxanthin, Astaxanthin, Vitamin K, Vitamin E, tocotrienols, vitamin K, biologically active selenium derivatives, or one or more water-soluble Contain vitamins. Furthermore you can the formulations have one or more elements in their physiological acceptable form selected the group consisting of boron, iron, copper, manganese, zinc, molybdenum and chromium include.

• – 0,1 bis 10 Gew. Teil, vorzugsweise 1–5 Gew Teile Taurin;
• – 0,1 bis 1 Gew. Teil, vorzugsweise 0,3–0,6 Gew Teile Beta-Carotin;
• – 0,03 bis 0,3 Gew. Teile, vorzugsweise, 0,07 bis 0,2 Gew. Teile Vitamin A;
• – 0,1 bis 1 Gew. Teil, vorzugsweise 0,3–0,6 Gew Teile Lycopin;
• – 0,1 bis 1 Gew. Teil, vorzugsweise 0,3–0,6 Gew Teile Zeaxanthin;
• – 0,1 bis 1 Gew. Teil, vorzugsweise 0,3–0,6 Gew Teile Astaxanthin;
• – 0,1 bis 5 Gew. Teile, vorzugsweise 0,3 bis 2 Gew. Teile Vitamin E;
• – 0,1 bis 5 Gew. Teile, vorzugsweise 0,3 bis 2 Gew. Teile Tocotrienole;
• – 0,1 bis 1 Gew. Teil, vorzugsweise 0,3–0,6 Gew Teile Vitamin K;
• – 10^–5 bis 3 × 10^–5 Gew. Teile, vorzugsweise 1,3 × 10^–4 bis 2,7 × 10^–4 Gew. Teile biologisch wirksames Selen;
• – ein oder mehrere der wasserlöslichen Vitamine und/oder seine physiologisch akzeptablen Derivate, Thiamin, Riboflavin, Niacin, NADH, NADPH, Pyridoxin, Panthotensäure, Biotin, Folsäure und Cobalamin in den nachfolgenden Gewichtsanteilen:

Vitamin Von Bis Bevorzugt von Bevorzugt bis Thiamin 10^–3 0,01 3 × 10^–3 8 × 10^–3 Riboflavin 10^–3 0,01 3 × 10^–3 8 × 10^–3 Niacin 2 × 10^–3 0,03 6 × 10^–3 2 × 10^–2 NADH 2 × 10^–3 0,03 6 × 10^–3 2 × 10^–2 Pyridoxin 10^–3 0,01 3 × 10^–3 8 × 10^–3 Panthotensäure 0,01 0,1 0,03 0,08 Biotin 10^–4 10^–3 3 × 10^–4 8 × 10^–4 Folsäure 10^–4 10^–3 3 × 10^–4 8 × 10^–4 Cobalamin 10^–5 10^–4 3 × 10^–5 8 × 10^–4 By way of example only, it should be noted that the formulation according to the invention, based on 100 parts by weight of the formulation according to the invention, may furthermore contain independently of one another:

• 0.1 to 10 parts by weight, preferably 1 to 5 parts by weight of taurine;
• 0.1 to 1 part by weight, preferably 0.3 to 0.6 parts by weight of beta-carotene;
• - 0.03 to 0.3 parts by weight, preferably, 0.07 to 0.2 parts by weight of vitamin A;
• 0.1 to 1 part by weight, preferably 0.3 to 0.6 parts by weight of lycopene;
• From 0.1 to 1 part by weight, preferably from 0.3 to 0.6 parts by weight of zeaxanthin;
• 0.1 to 1 part by weight, preferably 0.3 to 0.6 parts by weight of astaxanthin;
• - 0.1 to 5 parts by weight, preferably 0.3 to 2 parts by weight of vitamin E;
• From 0.1 to 5 parts by weight, preferably from 0.3 to 2 parts by weight of tocotrienols;
• From 0.1 to 1 part by weight, preferably from 0.3 to 0.6 parts by weight of vitamin K;
• Parts from 10 ^-5 to 3 × 10 ^-5 parts by weight, preferably from 1.3 × 10 ^-4 to 2.7 × 10 ^-4 parts by weight of biologically active selenium;
• One or more of the water-soluble vitamins and / or its physiologically acceptable derivatives, thiamine, riboflavin, niacin, NADH, NADPH, pyridoxine, pantothenic acid, biotin, folic acid and cobalamin in the following proportions by weight:

vitamin From To Preferred from Preferably until thiamine 10 ^-3 0.01 3 × 10 ^-3 8 × 10 ^-3 riboflavin 10 ^-3 0.01 3 × 10 ^-3 8 × 10 ^-3 niacin 2 × 10 ^-3 0.03 6 × 10 ^-3 2 × 10 ^-2 NADH 2 × 10 ^-3 0.03 6 × 10 ^-3 2 × 10 ^-2 pyridoxine 10 ^-3 0.01 3 × 10 ^-3 8 × 10 ^-3 pantothenic acid 0.01 0.1 0.03 0.08 biotin 10 ^-4 10 ^-3 3 × 10 ^-4 8 × 10 ^-4 folic acid 10 ^-4 10 ^-3 3 × 10 ^-4 8 × 10 ^-4 cobalamin 10 ^-5 10 ^-4 3 × 10 ^-5 8 × 10 ^-4

One or more elements in their physiologically acceptable form selected from the group be made of boron, iron, copper, iodine, manganese, zinc, molybdenum and chromium. element From To Preferred from Preferably until boron 10 ⁴ 0.01 3 × 10 ^-4 8 × 10 ^-4 iron 0.01 0.05 0.02 0.03 phosphorus 0.01 0.05 0.02 0.03 copper 10 ^-3 5 × 10 ^-3 2 × 10 ^-3 3 × 10 ^-3 iodine 10 ^-4 5 × 10 ^-4 2 × 10 ^-4 3 × 10 ^-4 manganese 10 ^-3 5 × 10 ^-3 2 × 10 ^-3 3 × 10 ^-3 molybdenum 2 × 10 ^-5 5 × 10 ^-4 2 × 10 ^-4 3 × 10 ^-4 chrome 2 × 10 ^-5 5 × 10 ^-4 2 × 10 ^-4 3 × 10 ^-4

In a further embodiment In the present invention, the formulations contain extracts Stevia rebaudiana containing about 10-25% by weight steviol glycosides, based on the dry extract, which have about 300 times greater sweetening power as sugar. The formulations preferably contain 0.1-20% by weight, more preferably 0.2-10 Wt .-%, in particular 0.3-2 Wt .-%, each based on the total formulation.

In a further preferred embodiment of the present inventive formulation the formulation is essentially free of primary volatiles Alcohols (VOC) and / or ethoxylated or other synthetic Surfactants.

In a further preferred embodiment of the formulation according to the invention contains the formulation coenzyme Q10 also called ubiquinone or its physiologically acceptable Derivatives. Among the physiologically acceptable derivatives include coenzyme Q3, coenzyme Q4, coenzyme Q5, coenzyme Q6, coenzyme Q7, coenzyme Q8 or Coenzyme Q9.

The Component is preferably in an amount of 0.1-20% by weight, preferably 0.2-8 Wt .-% particularly preferably 0.3 to 4 wt .-% based on the total Formulation before.

Furthermore contain the formulations, preferably taurine and / or physiologically acceptable derivatives such. As taurine-chloramine and / or taurine-bromamine. The component is preferably in an amount of 0.1-50% by weight, preferably 0.5-30 Wt .-%, more preferably 1-10 Wt .-%, based on the total formulation, before.

Farther can usual ingredients, like flavors, dyes, thickeners and common physiological acceptable release agents in the formulations according to the invention be.

The liquid aqueous according to the invention Formulations form micelles, in which especially lipophilic Substances can be solubilized. The formation of micelles also makes it possible to concentrate liquid formulations produce, for example, a water content below 40 wt .-%, based on the total formulation. In a preferred embodiment are the liquid ones aqueous Formulations as an emulsion in the form of a micellar concentrate in front. The micelles in the liquid, aqueous formulations according to the invention have preferably has a mean diameter of less than 300 nm, preferably from 10 to 250 nm, more preferably from 50 to 230 nm and especially from 130 to 210 nm. In a preferred embodiment, the liquid aqueous Formulations according to the present Invention transparent before.

Of the average diameter of the micelles can be familiar to those skilled in the process be determined, for example, a Coulter Counter N24. The production The nano-emulsions according to the invention can be prepared by means of commercial high-pressure homogenizers carried out with which the formulations according to the invention homogenized become. In particular, when the present formulations according to the invention as nano-emulsion (mean diameter of micelles from 10 to 250 nm) can exist the formulations fast from the body be recorded. It's surprising have shown that the formulations according to the invention, especially the micellar concentrates to a much faster and increased Absorption of both hydrophilic and lipophilic components leads. Especially when the present aqueous liquid formulations As nano-emulsions, it is also possible without synthetic emulsifiers or Co-emulsifiers and alcohols (ethanol) work.

The formulations according to the invention can also be dried.

One Another object of the present invention is therefore a solid, available from a formulation according to the invention by drying, preferably spray-drying or freeze-drying. It has become more surprising Way proved that in the dried solids the micellar Structure is retained, so that when dissolving the solid in water the original recovered micellar emulsion can be. This has considerable advantages, since so the formulation of the invention simply as a nutrient Formulate solid preparations.

In a preferred embodiment are the solids of the invention so before that, in addition 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, especially Na, Mg, or Ca gluconates.

One Another object of the present invention is a nutrient Preparation comprising a formulation according to the invention or a solid according to the invention.

The Composition according to the invention is generally dosed so that the total amount of body-supplied amounts to component (a), preferably glucosamine sulfate, between 200 and 2000 mg / day, preferably 250 to 1500 mg / day, more preferably 350 to 1000 mg / day (and individual with a body weight of 75 kg).

The quantitative shares the components (b) and optionally (c) can be calculated on the basis of the amount of Component (a) based on its abovementioned percentage Shares are calculated.

One Another object of the present invention is a nutrient A preparation comprising a formulation according to the invention or a solid according to the invention for the therapy and prophylaxis of arthrosis in humans and animals.

In a particular embodiment The present invention serves the nutrient of the invention Preparation of therapy and prophylaxis of osteoarthritis.

The Composition according to the invention can be administered in several single doses throughout the day become. About that It is also possible the components (a) and (b) and optionally (c) to be administered individually.

One Another object of the present invention is a kit of parts, comprising components (a) and (b) and optionally (c), wherein at least one of the components spatially separate from the others. The kit of parts can do this container in which there are two or more compartments in which the Components (a) and (b) and optionally (c) are included. In the kit according to the invention can the individual components independently from each other in the form of a micellar concentrate, a spray-dried powder or tablets, dragees, capsules obtained therefrom. In a preferred embodiment has the kit according to the invention at least a compartment on and an additional container, wherein in at least one of the compartments and / or in the container two the components selected from the components (a) and (b) and optionally (c) are included.

One Another object of the present invention is a method for the preparation of a composition, characterized in that a liquid aqueous Formulation of the emulsion-type, water-soluble, concentrate of one Spray drying or freeze-drying supplied is such that micelles are obtained in the obtained dried good stay.

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, in particular calcium and / or Magnesium citrate or gluconic acid and / or gluconic acid, in particular Na, or Ca-gluconates, the spray or freeze-drying supplied is such that micelles are retained in the dried material.

One Another object of the present invention is therefore the use the formulation according to the invention or the nutrient of the invention Preparation for the prophylaxis and therapy of osteoarthritis. Furthermore can the nutrient preparation according to the invention or the formulation of the invention in a process for the preparation of nutritional preparations, preferably in a process for preparing a nutrient preparation for prophylaxis and therapy of osteoarthritis can be used.

One Another object of the present invention is also the use the formulation according to the invention or the solid according to the invention as a dietary supplement, dietetic Food or as a medicine.

One additional The subject of the present invention is a pharmaceutical, preferably a means of therapy and prophylaxis of osteoarthritis in humans and Animal comprising a liquid formulation according to the invention or a solid according to the invention.

The Medicines for prophylaxis and therapy is used to treat Human and animal, preferably on the skin around the joints applied. The medicines can However, they are also administered orally, and they preferably already have the Oral mucosa are absorbed.

at Application to the skin, it is beneficial if the drug a higher one viscosity have to form an adhesive depot on the skin surface to be able to. Another object of the invention is therefore a gel or a Lotion or cream comprising the formulation of the invention.

EXAMPLES

example 1 raw material Quantity in weight percent soya phospholipid 3 glucosamine 25 sodium ascorbate 9 water ad 100

• Homogenisator: Panda 2 K, NS 10012 von der Fa. Niro Soavi.; Temp: 25°C; bei 400 bar.
• Durchschnittliche Teilchengröße der Micellen des micellaren Konzentrats: 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 400 bar.
• Average particle size of the micelles of the micellar concentrate: 50 nm

Example 2 raw material Quantity in weight percent soya phospholipid 3 glucosamine 20 chondroitin sulfate 2 sodium ascorbate 9 water ad 100

• Homogenisator: Panda 2 K, NS 10012 von der Fa. Niro Soavi.; Temp: 25°C; bei 400 bar.
• Durchschnittliche Teilchengröße der Micellen des micellaren Konzentrats: 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 400 bar.
• Average particle size of the micelles of the micellar concentrate: 50 nm

Claims (20)

A liquid, aqueous formulation comprising: an active ingredient (a) selected from (a1) glucosamine and / or its physiologically acceptable derivatives or (a2) chondroitin and / or its physiologically acceptable derivatives; and additionally at least (b) phospholipid and / or its physiologically acceptable derivatives, characterized in that the components are present in the following amounts: (a) from 1 to 60% by weight, and (B) 0.1 to 30 wt .-%, wherein the weights are in each case based on the entire formulation. A formulation according to claim 1, characterized in that the component (b) lecithin, preferably soy and / or egg lecithin, particularly preferably phosphatidylcholines carrying a C ₆ - to C ₂₀ fatty acid residue, in particular C ₈ fatty acid residue is. A formulation according to any one of claims 1 or 2, characterized in that the formulation is a micelle stabilizer (c) selected from (c1) carnitine and / or a physiologically acceptable carnitine derivative; or (c2) one or more 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 tri-, tetra , Penta- or -hexaols, or (c3) mixtures of (c1) and (c2), wherein the micelle stabilizer (c) is present in an amount of 5 to 90% by weight. Formulation according to claim 3, characterized in that the component (c) is selected from L-carnitine and / or its physiologically acceptable derivatives such as for example, carnitine tartrate and / or acyl-L-carnitine or from the group consisting of glycerol, pentite, preferably glucose, Fructose, xylitol or hexitol, in particular sorbitol, mannitol, gulite or Inositol, and its physiologically acceptable derivatives such as Inositol triphosphate and / or disodium inositol. Formulation according to one of Claims 1 to 4, characterized that the wording additionally hyaluronic acid or its physiologically acceptable derivatives, for example sodium hyaluronate. Formulation according to one the claims 1 to 5, characterized in that the formulation additionally dermatan sulfate and / or keratan sulfate and / or heparan sulfate. Formulation according to one of Claims 1 to 6, characterized that the wording additionally L-ascorbic acid and / or their physiologically acceptable derivatives. Formulation according to one of Claims 1 to 7, characterized that the wording additionally Methylsulfonalmethane (MSM) contains. Formulation according to one of Claims 1 to 8, characterized that the wording additionally Triglycerides comprising polyunsaturated fatty acid residues and / or polyunsaturated fatty acids and / or their ethyl ester contains, prefers oils or fats comprising at least one fatty acid residue selected from linoleic acid, alpha-linolenic acid, Di-homo-gamma-linolenic acid, Gamma-linolenic acid, conjugated linoleic acid, especially prefers fish oil, Krill oil, Omega-3 fatty acid ethyl esters, contains. A formulation according to any one of claims 1 to 9, characterized in that the formulation additionally vegetable Ingredients or plant extracts contain, for example Red wine, cistus fruits, blueberry, Acerola, elderberry, frankincense or red clover, preferably, flavonoids / anthocyanidins, for example, OPC (oligomeric procyanidins), quercetin, naringin, Rutin, chrysin or resveratrol. A formulation according to any one of claims 1 to 10, characterized in that the formulation additionally a or more of the water-soluble Vitamins and / or its physiologically acceptable derivatives selected from the group of B vitamins consisting of pagamic acid, orotic acid, Thiamine, riboflavin, niacin, NADH, pyridoxine, pantothenic acid, biotin, Cobalamin and folic acid contains. A formulation according to any one of claims 1 to 11, characterized in that the formulation additionally a or several ingredients selected from taurine or its physiologically acceptable derivatives, beta-carotene, Vitamin A, Lycopene, Zeaxanthin, Astaxanthin, Vitamin K, Vitamin E, tocotrienols, vitamin K, coenzyme Q10 or its physiological acceptable derivatives, biologically active selenium derivatives, one or more water-soluble Vitamins or one or more elements in their physiologically acceptable Form selected from the group consisting of boron, iron, copper, phosphorus, manganese, Zinc, molybdenum and chromium. Formulation according to one of claims 1 to 12, characterized in that the nutrient preparation additionally contains extracts of Stevia rebaudiana, preferably in a proportion of about 10-25%. Steviol glycosides, based on the dry extract. Formulation according to Claims 1 to 13, characterized that the formulation is essentially free of primary volatile Alcohols (VOC) and / or ethoxylated or other synthetic surfactants. A formulation according to any one of claims 1 to 14, characterized in that the formulation is in the form of an emulsion, the micelles with a mean diameter of less than 300 nm, preferably from 10 to 250 nm, more preferably from 50 nm have up to 130 nm. Solid available from a formulation according to a the claims 1 to 15 by drying, in particular spray drying or freeze drying. Solid according to claim 16, characterized in that it additionally contains 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, in particular Na, Mg or Ca gluconates having. Cream or lotion or gel comprising a formulation according to one the claims 1 to 15. A pharmaceutical composition comprising a formulation according to one the claims 1 to 15 or a solid according to any one of claims 16 or 17th Medicament according to claim 19 for the treatment or prophylaxis of osteoarthritis in humans or animals.