WO2008111919A2 - A novel combination of water-soluble forms of coenzyme q10 and l-carnitine, process of production and use - Google Patents

A novel combination of water-soluble forms of coenzyme q10 and l-carnitine, process of production and use Download PDF

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Publication number
WO2008111919A2
WO2008111919A2 PCT/SI2008/000012 SI2008000012W WO2008111919A2 WO 2008111919 A2 WO2008111919 A2 WO 2008111919A2 SI 2008000012 W SI2008000012 W SI 2008000012W WO 2008111919 A2 WO2008111919 A2 WO 2008111919A2
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coenzyme
carnitine
combination
previous
products
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PCT/SI2008/000012
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French (fr)
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WO2008111919A3 (en
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Mirko Prosek
Marko Prosek
Alenka Golc-Wondra
Janko Zmitek
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Valens Int. D.O.O.
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Publication of WO2008111919A3 publication Critical patent/WO2008111919A3/en

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    • 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
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A23L2/00—Non-alcoholic beverages; Dry compositions or concentrates therefor; Their preparation
    • A23L2/52—Adding ingredients
    • 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
    • A23L33/17—Amino acids, peptides or proteins
    • A23L33/175—Amino 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
    • A61K31/12—Ketones
    • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • 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
    • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/35—Ketones, e.g. benzophenone
    • A61K8/355—Quinones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/06—Preparations for care of the skin for countering cellulitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/08—Anti-ageing preparations
    • 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

  • the object of this invention is a novel combination or mixture of water-soluble forms of coenzyme Q10 and L-camitine, as well as a process of preparing mixtures and products based on this mixture, and the use of mixtures and products based on this mixture.
  • This invention relates to combinations or mixtures of various, water-soluble forms of coenzyme Q10 and L-carnitine. This invention relates also to processes of preparing the said mixtures and to their use in the form of self- contained preparations or as supplements to pharmaceuticals, cosmetics and nutritional products. This invention relates also to pharmaceuticals, cosmetics and nutritional products that comprise at least one water-soluble form of coenzyme Q10, in combination with L-carnitine, and to the use thereof.
  • CoQ 10 and LC are substances that are indispensable for the cell energy generation in living organisms. Hence, they are indispensable for life. Man ensures sufficient amounts of both substances in the organism by synthesis, and from the food. However, it has been becoming more and more evident that the intake of larger amounts of exogenous CoQIO and LC, than available by conventional nutrition, is often necessary. This is important, especially when hard labor, advanced age, certain diseases, unsuitable diet and the like, are involved. For this reason, fortified food and various CoQIO or LC containing preparations are more and more assessing themselves. They contain recommended daily doses of CoQIO from about 10 mg to several hundred mg and from about several hundred mg to 2 g and more, of LC. Both substances are asserting themselves in cosmetics as well.
  • CoQIO and LC exert a synergistic effect on the organism.
  • CoQIO is a key enzyme in several steps of food conversion into cell energy in mitochondria; whereas, L-carnitine enables or enhances the fat transfer into mitochondria, and the elimination of the bumt-up fat residues from the inner parts of mitochondria.
  • CoQIO enables their transformation into energy. In this manner, they ensure together the required energy for the organism. This is especially important for more active organs, such as the heart. Since this favors the utilization of fats in preference to carbon hydrates, the blood fat amount is diminished as well, which exerts another positive effect on human health.
  • CoQIO stabilizes the cell wall, and acts as a potent antioxidant.
  • LC is important also in the elimination of the neurotoxic ammonia from the organism, thus inhibiting its accumulation in the blood during hard labor, when the organism does not succeed in its complete conversion into urea. In smaller amounts, ammonia causes disturbances of orientation and reflexes; in larger amounts it causes coma or even death.
  • each of CoQ10 and LC separately has an outstanding influence on the functioning of the organism, especially of the heart.
  • they invigorate the organism, improve the psychophysical capacity, vitality and resistance; they prevent or alleviate a series of diseases.
  • the synergistic effect of the combined use of the two active substances yields significantly increased or mutually supplementary effects. For this reason, it is desirable to consume both.
  • CoQIO and LC differ in their physical characteristics: CoQIO is a lipophilic, consequently a water-insoluble substance. On the other hand, LC is a hydrophilic substance consequently it is well water-soluble. Therefore the preparation of formulations, comprising both (CoQIO and LC together), is relatively exacting, especially in the case of higher concentrations. Hitherto, formulations have asserted themselves comprising either CoQIO or LC. Very rare do formulations comprise both simultaneously; even these comprise a relatively limited concentration range, to say minor concentrations. This requires a separate consummation or use of either one or the other. Consequently, two types of formulations, or several types of products, have to be used; one of them containing CoQIO, and the other LC.
  • the task and the aim of this invention are a composition or mixture of CoQIO and LC, which would enable the preparation of preparations, which would contain simultaneously CoQI O, as well as LC, in suitable concentrations, or which would enable the addition of Q10 as well as LC to water based nutritional and other products.
  • the task and the aim of this invention are also preparations, containing CoQIO and LC, and water based products with added CoQIO and LC, and processes for the preparation thereof.
  • the task and aim of this invention are also uses of these preparations and products.
  • the task is solved by preparing combinations of LC and CoQIO, in such a manner, that LC is combined with specific CoQI O forms or with forms having improved water- solubility, or with water soluble forms.
  • the task is solved with the aid of such combinations for the preparation of preparations, and the addition of both components into various water based products, as well as the use of the combination and products containing it, as claimed in independent claims.
  • Figure 1 Average weight loss of a volunteer group during the experiment.
  • the problem of combining CoQIO and LC according to this invention is solved by the application of a suitable CoQIO having enhanced water solubility.
  • the gist of the invention is therefore the use of CoQIO in a suitable form endowed with increased water solubility, which enables optional combinations with the well water soluble LC, and with further water soluble substances.
  • Any CoQIO forms endowed with enhanced water solubility may be used, such as for example complexes of CoQIO with unsubstituted or substituted beta- and gamma-cyclodextrins, micro- and nano-encapsulated CoQIO, liposomal forms and the like, as well as forms generating virtual solutions, for example dispersions or emulsions.
  • CoQIO endowed with enhanced water solubility and LC 1 may be added separately in a simple manner to these products, in order to obtain their mixture only in the product itself.
  • this enables the admixture of a sufficient quantity of CoQIO having enhanced water solubility, and LC, into milk, yoghurt, juices and any other water based product, thus enabling an adult human to consume a daily or even multiple daily dose of CoQIO and LC in a single meal.
  • various pharmaceutical and cosmetic formulations and food supplements in the form of capsules, syrups, solutions, drops, pastes, gels, creams, tablets, powders and other formulations or administration systems.
  • these products may contain also other excipients, especially biologically important or active substances, such as vitamins, minerals, antioxidants, stimulants such as caffeine and others.
  • excipients may be used in the preparation of suitable pharmaceutical, cosmetic and other formulations, and as carriers in the preparation of solid or powdery formulations of COQ10 and LC combinations, starting from solutions.
  • suitable pharmaceutical, cosmetic and other formulations and as carriers in the preparation of solid or powdery formulations of COQ10 and LC combinations, starting from solutions.
  • Such an example is the use of maltodextrin for the preparation of a CoQIO and LC combination in powder form, starting from a solution, by means of spray drying.
  • the obtained powder is suitable especially for the preparation of capsules, effervescent tablets, tablets and the like.
  • the combination of the two substances is simpler to administer and to use, since it enables the consummation of an adequate amount of both substances simultaneously.
  • Combinations or products containing a combination of CoQIO and LC yield improved and synergistic effects of both components, which can be further combined with the effects of other substances. Since the CoQIO forms having enhanced water solubility, exhibit as a rule an enhanced bioavailability, their combination with LC is ever more effective as normally.
  • this combination is applicable for the improvement of various systemic and topical effects, inter alia in prevention and therapy of cardiovascular diseases, increased cholesterol, diabetes, cancer, immune disorders, mitochondrial diseases, muscular dystrophy, oral cavity diseases, and for the improvement of psychophysical performance, as well as in slimming, cellulites elimination, and the like. Owing to the application of water soluble forms known for their enhanced bioavailability, these effects are additionally enhanced in comparison with the separate application of the two substances.
  • this invention relates to combinations of water-soluble forms of coenzyme Q10 or CoQIO forms having enhanced water solubility, with LC, to the preparation and use of these combination as product supplement, or to the preparation and use of nutritional products, pharmaceuticals, and cosmetics with the self-contained combination or mixture according to this invention, or with added excipients or other active substances.
  • the invention relates also to the use of the combination and products thereof, relating to the functions of the human organism associated with co-enzyme Q10 and LC.
  • CoQIO having improved water solubility QiOVital® (Valens Int., Slovenia), AlI-Q ( S ) (DSM, Netherlands), ProQsan® (Germany), NanoQ® (China), Novasol® (Italy), anhydrous caffeine (Fluka), currant antocyans (Kemijski institut, Ljubljana, Slovenia), fruit syrups and juices Fructal® (Slovenia), Alpsko mleko® (Ljubljanske mlekarne, Slovenia), probiotic yoghurts Ego® (Celjske mlekame, Slovenia) and Actimel® (Danone, France).
  • the obtained mixtures were used in the preparation of diluted aqueous solutions, for supplementing various products, and in the preparation of various products.
  • LC (20 g), caffeine (2 g) and CoQ10 having improved water solubility (560 mg) were admixed to 500 mL of raspberry syrup (33 %, supplemented with citric acid). Subsequently, 500 mL of the syrup were added under stirring to the obtained mixture, and stirred to yield a homogenous product. Obtained was syrup comprising about 20 mg of LC/mL, 2 mg of caffeine/mL, and 0.56 mg of CoQ10/mL. The syrup was kept in a dark bottle in a refrigerator. It was used alone or diluted with water in a ratio of about 1 : 10.
  • Randomly chosen volunteers (5 men and 15 women, 29-61 years) consumed each 40-50 mL of the beverage of Example 3, during 5 weeks twice daily. Monitored were their body weight, blood pressure and fat/water ratio of the body. Their general vitality and revitalization were evaluated. The volunteers observed in 81 % an improvement of the general vitality, and in 74 % a revitalization during several hours after consumption. The remaining results are represented on Figs 1-3.
  • Example 1 CoQ10:LC ratio 1 :20
  • the effects of the mixture of Example 1 (CoQ10:LC ratio 1 :20) on cellulites diminishment were compared with the effects of the aqueous solution of sole LC in equal concentration, applied by massage rubbing to the thigh skin, twice daily during 4 weeks. Monitored were the appearance and the circumference of the thighs.
  • the comparison of the starting values with final results showed in both cases a visual improvement, which was however significantly better in the case, when the mixture had been applied.
  • the thickness of the thigh skin wrinkle was decreased in the case of applying LC from 32 mm to 31 mm, and in the case of applying the mixture from 32 mm to 28 mm.
  • the novel combination of coenzyme Q10 and L-camitine according to the invention is characterized in that coenzyme Q10, in a suitable form having enhanced water solubility, forms a mixture with L-carnitine.
  • the coenzyme Q10 and L-carnitine are in optional ratio, preferably in a weight ratio within the range of 1 :200 to 10:1 , more preferably within the range of 1 :1 to 1 :100.
  • the combination of coenzyme Q10 and L-camitine is solid or in the form of a solution or suspension, in water or in an aqueous medium; it is pure or it comprises added excipients and/or bioactive substances.
  • coenzyme Q10 and L-carnitine are used in the preparation of pharmaceuticals, nutritional products, and cosmetics, by addition, either in a premix or separately.
  • the preparation of products containing coenzyme Q10 and L-carnitine is characterized in that coenzyme Q10 and L-carnitine according to previous claims, are added, either combined or separately, during a convenient manufacturing step.
  • Products according to this invention comprise a combination of coenzyme Q10 and L-carnitine according to the invention.
  • the products may comprise in addition to coenzyme Q10 and L-carnitine other bioactive substances and excipients, such as vitamins, antioxidants, stimulants and the like.
  • combinations and products according to the invention is characterized in that they are used to ensure synergistic effects of coenzyme Q10 and L-carnitine, especially to improve the psychophysical capacity, to diminish the contents of cholesterol and fats in the blood, to diminish the body weight, to enhance the resistance, to retard ageing processes, to alleviate the symptoms of mitochondrial diseases, to alleviate fatigue symptoms, and for other positive prophylactic and therapeutic effects caused by the combined effects of coenzyme Q10 and L-carnitine.
  • the use of the combination according to the invention relates to slimming, cellulites elimination, skin tonification and rejuvenation, and to other effects associated with the appearance.
  • Products according to the invention are used as energy beverages for invigoration, fatigue alleviation, vitality enhancement and the like.

Abstract

The object of this invention is a novel combination or mixture of water-soluble forms of coenzyme Q10 and L-carnitine, as well as a process of preparing mixtures and products based on this mixture, and the use of mixtures and products based on this mixture. In the novel combination of coenzyme Q10 and L-carnitine according to the invention, the coenzyme Q10, in a suitable form having enhanced water solubility, forms a mixture with L-carnitine. The coenzyme Q10 and L-carnitine are in optional ratios, preferably in a weight ratio within the range of 1 :200 to 10:1, more preferably within the range of 1 :1 to 1 :100. The combination of coenzyme Q10 and L-carnitine is solid or in the form of a solution or suspension in water or an aqueous medium; it can be pure or it comprises added excipients and/or bioactive substances. The combination of coenzyme Q10 and L-carnitine according to the invention is used in the preparation of pharmaceuticals, nutritional products, and cosmetics, as additive, either to the premix or separately.

Description

A NOVEL COMBINATION OF WATER-SOLUBLE FORMS OF COENZYME Q10 AND L-CARNltlNE, PROCESS OF PRODUCTION AND USE
The object of this invention is a novel combination or mixture of water-soluble forms of coenzyme Q10 and L-camitine, as well as a process of preparing mixtures and products based on this mixture, and the use of mixtures and products based on this mixture.
This invention relates to combinations or mixtures of various, water-soluble forms of coenzyme Q10 and L-carnitine. This invention relates also to processes of preparing the said mixtures and to their use in the form of self- contained preparations or as supplements to pharmaceuticals, cosmetics and nutritional products. This invention relates also to pharmaceuticals, cosmetics and nutritional products that comprise at least one water-soluble form of coenzyme Q10, in combination with L-carnitine, and to the use thereof.
In the following text the following synonyms are used:
- for coenzyme Q10: CoQ10
- for L-carnitine: LC.
CoQ 10 and LC are substances that are indispensable for the cell energy generation in living organisms. Hence, they are indispensable for life. Man ensures sufficient amounts of both substances in the organism by synthesis, and from the food. However, it has been becoming more and more evident that the intake of larger amounts of exogenous CoQIO and LC, than available by conventional nutrition, is often necessary. This is important, especially when hard labor, advanced age, certain diseases, unsuitable diet and the like, are involved. For this reason, fortified food and various CoQIO or LC containing preparations are more and more assessing themselves. They contain recommended daily doses of CoQIO from about 10 mg to several hundred mg and from about several hundred mg to 2 g and more, of LC. Both substances are asserting themselves in cosmetics as well.
CoQIO and LC exert a synergistic effect on the organism. Namely, CoQIO is a key enzyme in several steps of food conversion into cell energy in mitochondria; whereas, L-carnitine enables or enhances the fat transfer into mitochondria, and the elimination of the bumt-up fat residues from the inner parts of mitochondria. CoQIO enables their transformation into energy. In this manner, they ensure together the required energy for the organism. This is especially important for more active organs, such as the heart. Since this favors the utilization of fats in preference to carbon hydrates, the blood fat amount is diminished as well, which exerts another positive effect on human health. In addition, CoQIO stabilizes the cell wall, and acts as a potent antioxidant. This is of the utmost importance, as its reduced form, acting as an antioxidant, is generated just on the site of formation of free radicals in the organism. LC is important also in the elimination of the neurotoxic ammonia from the organism, thus inhibiting its accumulation in the blood during hard labor, when the organism does not succeed in its complete conversion into urea. In smaller amounts, ammonia causes disturbances of orientation and reflexes; in larger amounts it causes coma or even death.
In conformance with the above, each of CoQ10 and LC separately has an outstanding influence on the functioning of the organism, especially of the heart. In addition, they invigorate the organism, improve the psychophysical capacity, vitality and resistance; they prevent or alleviate a series of diseases. The synergistic effect of the combined use of the two active substances yields significantly increased or mutually supplementary effects. For this reason, it is desirable to consume both.
CoQIO and LC, however, differ in their physical characteristics: CoQIO is a lipophilic, consequently a water-insoluble substance. On the other hand, LC is a hydrophilic substance consequently it is well water-soluble. Therefore the preparation of formulations, comprising both (CoQIO and LC together), is relatively exacting, especially in the case of higher concentrations. Hitherto, formulations have asserted themselves comprising either CoQIO or LC. Very rare do formulations comprise both simultaneously; even these comprise a relatively limited concentration range, to say minor concentrations. This requires a separate consummation or use of either one or the other. Consequently, two types of formulations, or several types of products, have to be used; one of them containing CoQIO, and the other LC. This is a burden for the consumers, and causes the intake of large amounts of various unnecessary substances, which are contained in such products. In addition, the use of separate formulations or products, based on different active substances, diminishes the synergistic effects of CoQIO and LC.
A specific problem, hitherto not adequately solved, presents the preparation of such water based preparations, which would contain simultaneously CQ10 and LC in suitable concentrations; also the addition of both to water based products has not been solved. There is a continuously felt need for solving the preparation and use of the composition of CoQIO and LC, which would enable a simple preparation of products containing them, or the addition of both to water based nutritional, pharmaceutical and cosmetic products.
The task and the aim of this invention are a composition or mixture of CoQIO and LC, which would enable the preparation of preparations, which would contain simultaneously CoQI O, as well as LC, in suitable concentrations, or which would enable the addition of Q10 as well as LC to water based nutritional and other products. The task and the aim of this invention are also preparations, containing CoQIO and LC, and water based products with added CoQIO and LC, and processes for the preparation thereof. The task and aim of this invention are also uses of these preparations and products.
According to this invention the task is solved by preparing combinations of LC and CoQIO, in such a manner, that LC is combined with specific CoQI O forms or with forms having improved water- solubility, or with water soluble forms.
According to this invention, the task is solved with the aid of such combinations for the preparation of preparations, and the addition of both components into various water based products, as well as the use of the combination and products containing it, as claimed in independent claims.
The invention is illustrated with the aid of working Examples, and Figures, representing:
Figure 1. Average weight loss of a volunteer group during the experiment.
Figure 2. Fat content reduction (%) and the increase of body water percentage during the performance of the experiment. Represented is the medium value of all measurements.
Figure 3. Variation of individual parameters during the performance of the experiment.
The problem of combining CoQIO and LC according to this invention is solved by the application of a suitable CoQIO having enhanced water solubility. The gist of the invention is therefore the use of CoQIO in a suitable form endowed with increased water solubility, which enables optional combinations with the well water soluble LC, and with further water soluble substances. Any CoQIO forms endowed with enhanced water solubility may be used, such as for example complexes of CoQIO with unsubstituted or substituted beta- and gamma-cyclodextrins, micro- and nano-encapsulated CoQIO, liposomal forms and the like, as well as forms generating virtual solutions, for example dispersions or emulsions. In such a manner are obtained stable solid mixtures of CoQ10 and LC in desired ratios, or mixtures in the form of aqueous solutions or suspensions, which may be added in a simple way to various nutritional, water based products, such as milk, yoghurts, cottage cheese, cheese and other dairy products, marmalade, jams, chutneys, fruit and vegetable juices, nectars or syrups, and various beverages, compotes (stewed fruit), gruel, porridge, cereal products, chocolate products, honey products, meat products and the like. In an analogous manner, they may be added to water based pharmaceutical and cosmetic products. In the same manner, CoQIO endowed with enhanced water solubility and LC1 may be added separately in a simple manner to these products, in order to obtain their mixture only in the product itself. For example, this enables the admixture of a sufficient quantity of CoQIO having enhanced water solubility, and LC, into milk, yoghurt, juices and any other water based product, thus enabling an adult human to consume a daily or even multiple daily dose of CoQIO and LC in a single meal. In an analogous manner are obtainable various pharmaceutical and cosmetic formulations and food supplements in the form of capsules, syrups, solutions, drops, pastes, gels, creams, tablets, powders and other formulations or administration systems. In addition to the combination of CoQIO and LC these products may contain also other excipients, especially biologically important or active substances, such as vitamins, minerals, antioxidants, stimulants such as caffeine and others. Optionally, excipients may be used in the preparation of suitable pharmaceutical, cosmetic and other formulations, and as carriers in the preparation of solid or powdery formulations of COQ10 and LC combinations, starting from solutions. Such an example is the use of maltodextrin for the preparation of a CoQIO and LC combination in powder form, starting from a solution, by means of spray drying. The obtained powder is suitable especially for the preparation of capsules, effervescent tablets, tablets and the like.
The combination of the two substances is simpler to administer and to use, since it enables the consummation of an adequate amount of both substances simultaneously. Combinations or products containing a combination of CoQIO and LC yield improved and synergistic effects of both components, which can be further combined with the effects of other substances. Since the CoQIO forms having enhanced water solubility, exhibit as a rule an enhanced bioavailability, their combination with LC is ever more effective as normally.
Therefore this combination is applicable for the improvement of various systemic and topical effects, inter alia in prevention and therapy of cardiovascular diseases, increased cholesterol, diabetes, cancer, immune disorders, mitochondrial diseases, muscular dystrophy, oral cavity diseases, and for the improvement of psychophysical performance, as well as in slimming, cellulites elimination, and the like. Owing to the application of water soluble forms known for their enhanced bioavailability, these effects are additionally enhanced in comparison with the separate application of the two substances.
Therefore this invention relates to combinations of water-soluble forms of coenzyme Q10 or CoQIO forms having enhanced water solubility, with LC, to the preparation and use of these combination as product supplement, or to the preparation and use of nutritional products, pharmaceuticals, and cosmetics with the self-contained combination or mixture according to this invention, or with added excipients or other active substances.
The invention relates also to the use of the combination and products thereof, relating to the functions of the human organism associated with co-enzyme Q10 and LC.
The invention is illustrated, but in no way limited by the following Examples.
Used was CoQIO having improved water solubility QiOVital® (Valens Int., Slovenia), AlI-Q(S) (DSM, Netherlands), ProQsan® (Germany), NanoQ® (China), Novasol® (Italy), anhydrous caffeine (Fluka), currant antocyans (Kemijski institut, Ljubljana, Slovenia), fruit syrups and juices Fructal® (Slovenia), Alpsko mleko® (Ljubljanske mlekarne, Slovenia), probiotic yoghurts Ego® (Celjske mlekame, Slovenia) and Actimel® (Danone, France).
EXAMPLE 1 - Preparation of a liquid mixture of CoQIO and LC
To an aqueous solution of CoQIO having enhanced water solubility (QiOVital®, 7.3%, and 100 g) were added successively under stirring at room temperature 73 g, 146 g and 365 g LC. Obtained were stable aqueous mixtures of CoQIO and LC in weight ratios of 1 :10, 1 :20 and 1 :50. If required, pasteurization was performed for 15 minutes at a temperature of 80-85 0C. The mixtures were kept in a refrigerator. HPLC analysis showed that the concentrations remained virtually unaltered during 4 moths. In an analogous manner were prepared mixtures with different ratios. Water was added, if necessary.
The obtained mixtures were used in the preparation of diluted aqueous solutions, for supplementing various products, and in the preparation of various products.
EXAMPLE 2 - Preparation of an aqueous solution of CoQIO and LC
In water (100 mL) was under stirring dissolved at first LC (201 mg), followed by CoQ10 (All-Q®, 10 %, 20.6 mg), to obtain a stable solution of CoQIO and LC in a ratio approximately 1 :100. The solution was kept in a refrigerator.
EXAMPLE 3 - Preparation of a fruit beverage containing CoQIO, LC and caffeine
LC (20 g), caffeine (2 g) and CoQ10 having improved water solubility (560 mg) were admixed to 500 mL of raspberry syrup (33 %, supplemented with citric acid). Subsequently, 500 mL of the syrup were added under stirring to the obtained mixture, and stirred to yield a homogenous product. Obtained was syrup comprising about 20 mg of LC/mL, 2 mg of caffeine/mL, and 0.56 mg of CoQ10/mL. The syrup was kept in a dark bottle in a refrigerator. It was used alone or diluted with water in a ratio of about 1 : 10.
EXAMPLE 4 - Testing of a beverage containing CoQ10, LC and caffeine
Randomly chosen volunteers (5 men and 15 women, 29-61 years) consumed each 40-50 mL of the beverage of Example 3, during 5 weeks twice daily. Monitored were their body weight, blood pressure and fat/water ratio of the body. Their general vitality and revitalization were evaluated. The volunteers observed in 81 % an improvement of the general vitality, and in 74 % a revitalization during several hours after consumption. The remaining results are represented on Figs 1-3.
EXAMPLE 5 - Testing cellulites diminishment efficiency
The effects of the mixture of Example 1 (CoQ10:LC ratio 1 :20) on cellulites diminishment were compared with the effects of the aqueous solution of sole LC in equal concentration, applied by massage rubbing to the thigh skin, twice daily during 4 weeks. Monitored were the appearance and the circumference of the thighs. The comparison of the starting values with final results showed in both cases a visual improvement, which was however significantly better in the case, when the mixture had been applied. The thickness of the thigh skin wrinkle was decreased in the case of applying LC from 32 mm to 31 mm, and in the case of applying the mixture from 32 mm to 28 mm.
EXAMPLE 6 - Preparation of syrup containing CoQIO and LC
A liquid mixture of 750 g CoQIO and 3.75 kg LC in water, prepared in an analogous manner as in Example 1 , was added under vigorous stirring at a temperature of 30-40 0C to 33 L of natural syrup made of wild berries. The stirring was continued for about 0.5 hours, to yield homogenous syrup. Then the stirring was slowed down, and stirred for further 0.5 hours. Obtained was about 50 L of syrup having a concentration of about 15 mg of CoQ10/mL and about 75 mg of LC/mL. The obtained syrup is especially suitable for higher dosage of the two components.
The novel combination of coenzyme Q10 and L-camitine according to the invention is characterized in that coenzyme Q10, in a suitable form having enhanced water solubility, forms a mixture with L-carnitine. The coenzyme Q10 and L-carnitine are in optional ratio, preferably in a weight ratio within the range of 1 :200 to 10:1 , more preferably within the range of 1 :1 to 1 :100. The combination of coenzyme Q10 and L-camitine is solid or in the form of a solution or suspension, in water or in an aqueous medium; it is pure or it comprises added excipients and/or bioactive substances.
The combination of coenzyme Q10 and L-carnitine according to the invention is used in the preparation of pharmaceuticals, nutritional products, and cosmetics, by addition, either in a premix or separately.
The preparation of products containing coenzyme Q10 and L-carnitine is characterized in that coenzyme Q10 and L-carnitine according to previous claims, are added, either combined or separately, during a convenient manufacturing step.
Products according to this invention comprise a combination of coenzyme Q10 and L-carnitine according to the invention. The products may comprise in addition to coenzyme Q10 and L-carnitine other bioactive substances and excipients, such as vitamins, antioxidants, stimulants and the like.
The use of combinations and products according to the invention is characterized in that they are used to ensure synergistic effects of coenzyme Q10 and L-carnitine, especially to improve the psychophysical capacity, to diminish the contents of cholesterol and fats in the blood, to diminish the body weight, to enhance the resistance, to retard ageing processes, to alleviate the symptoms of mitochondrial diseases, to alleviate fatigue symptoms, and for other positive prophylactic and therapeutic effects caused by the combined effects of coenzyme Q10 and L-carnitine. The use of the combination according to the invention relates to slimming, cellulites elimination, skin tonification and rejuvenation, and to other effects associated with the appearance. Products according to the invention are used as energy beverages for invigoration, fatigue alleviation, vitality enhancement and the like.

Claims

What is claimed is:
1. A novel combination of coenzyme Q10 and L-camitine, wherein coenzyme Q10, in a suitable form having enhanced water solubility, forms a mixture with L- carnitine.
2. The combination of coenzyme Q10 and L-camitine according to claim 1 , wherein coenzyme Q10 and L-camitine are in optional ratio, preferably in a weight ratio within the range of 1 :200 to 10:1 , more preferably within the range of 1 :1 to 1 :100.
3. The combination of coenzyme Q10 and L-carnitine according to previous claims, wherein the combination is solid or in the form of a solution or suspension, in water or in an aqueous medium.
4. The combination of coenzyme Q10 and L-carnitine according to previous claims, wherein the combination is pure or it comprises added excipients and/or bioactive substances.
5. A use of the combination of coenzyme Q10 and L-camitine according to previous claims, in the preparation of pharmaceuticals, nutritional products, and cosmetics, wherein they are added either in a premix or separately.
6. The use of the combination of coenzyme Q10 and L-carnitine according to previous claims, for supplementing water based nutritional products, pharmaceuticals, and cosmetics, wherein they are added either in a premix or separately.
7. A process for preparing products containing coenzyme Q10 and L- carnitine, wherein coenzyme Q10 and L-carnitine according to previous claims are added, either combined or separately, during a convenient manufacturing step.
8. Products comprising a combination of coenzyme Q10 and L-camitine according to previous claims.
9. Products according to previous claims, comprising in addition to coenzyme Q10 and L-carnitine other bioactive substances and excipients, such as vitamins, antioxidants, stimulants and the like.
10. The use of combinations and products according to previous claims, to ensure synergistic effects of coenzyme Q10 and L-carnitine.
11. The use of combinations and products according to previous claims, wherein they are used to improve the psychophysical capacity, to diminish the contents of cholesterol and fats in the blood, to diminish the body weight, to enhance the resistance, to retard ageing processes, to act against the symptoms of mitochondrial diseases, to alleviate fatigue symptoms, and for other positive prophylactic and therapeutic effects derived from the combined effects of coenzyme Q10 and L-carnitine.
12. The use of a combination according to previous claims, characterized in that it relates to slimming, cellulites elimination, skin tonification and rejuvenation, and to other effects associated with the appearance.
13. Products according to previous claims, characterized in that they are used as energy beverages for invigoration, fatigue alleviation, vitality enhancement and the like.
PCT/SI2008/000012 2007-03-15 2008-02-27 A novel combination of water-soluble forms of coenzyme q10 and l-carnitine, process of production and use WO2008111919A2 (en)

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Citations (6)

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US20030129177A1 (en) * 2000-04-04 2003-07-10 Sigma-Tau Healthscience S.P.A. Dietary supplement energy-providing to skeletal muscles and protecting the cardiovascular tract
EP1681053A1 (en) * 2003-10-31 2006-07-19 Kaneka Corporation Composition containing reduced coenzyme q
WO2006110924A2 (en) * 2005-04-14 2006-10-19 Jarrow Formulas, Inc. Dietary supplement formulations for improved delivery of coenzyme q10 and methods of administration
US20060269535A1 (en) * 2005-05-31 2006-11-30 Naidu A S Metallo-lactoferrin-coenzyme compositions for trigger and release of bioenergy
US20060292134A1 (en) * 2005-06-22 2006-12-28 Sidney Stohs Composition for enhancing cellular energy
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Publication number Priority date Publication date Assignee Title
US20030129177A1 (en) * 2000-04-04 2003-07-10 Sigma-Tau Healthscience S.P.A. Dietary supplement energy-providing to skeletal muscles and protecting the cardiovascular tract
EP1681053A1 (en) * 2003-10-31 2006-07-19 Kaneka Corporation Composition containing reduced coenzyme q
US20070085059A1 (en) * 2004-02-23 2007-04-19 Texas A&M University System Bioactive Complexes Compositions and Methods of Use Thereof
WO2006110924A2 (en) * 2005-04-14 2006-10-19 Jarrow Formulas, Inc. Dietary supplement formulations for improved delivery of coenzyme q10 and methods of administration
US20060269535A1 (en) * 2005-05-31 2006-11-30 Naidu A S Metallo-lactoferrin-coenzyme compositions for trigger and release of bioenergy
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