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WO2012136204A2 - Préparation ou complément alimentaire - Google Patents

Préparation ou complément alimentaire Download PDF

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Publication number
WO2012136204A2
WO2012136204A2 PCT/DE2012/100090 DE2012100090W WO2012136204A2 WO 2012136204 A2 WO2012136204 A2 WO 2012136204A2 DE 2012100090 W DE2012100090 W DE 2012100090W WO 2012136204 A2 WO2012136204 A2 WO 2012136204A2
Authority
WO
WIPO (PCT)
Prior art keywords
preparation
dietary supplement
cysteine
glycine
acetaldehyde
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/DE2012/100090
Other languages
German (de)
English (en)
Other versions
WO2012136204A3 (fr
Inventor
Gunnar Frank
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
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Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of WO2012136204A2 publication Critical patent/WO2012136204A2/fr
Publication of WO2012136204A3 publication Critical patent/WO2012136204A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/30—Zinc; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A61K38/063—Glutathione
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • the invention relates to a pharmaceutical preparation or dietary supplement for improving the metabolism of alcohol, in particular ethanol.
  • Such a preparation or dietary supplement is suitable to increase the alcohol metabolism, so as to avoid or reduce the adverse effects of alcohol consumption.
  • NAD + and ADH form an enzyme-coenzyme complex (ADH-NAD + complex), while NAD + is simultaneously reduced to NADH.
  • the NADH is then released and the ADH is ready to repeat the reaction by incorporating a new NAD + molecule.
  • the cell has a limited capacity to oxidize NADH back to NAD +, which determines the maximum rate of the reaction.
  • ADH enzymes for the reaction.
  • the alcohol-reacted acetaldehyde molecules migrate into cytoplasmic organelles, known as mitochondria, where they are oxidized to acetic acid in a reaction catalyzed by the enzyme aldehyde dehydrogenase (ALDH) (Figure 2)
  • Fig. 2 In this reaction, too, one molecule of the coenzyme NAD + is reduced to NADH. Both the latter and the previously cytoplasmic NADH are reoxidized in the mitochondrial respiratory chain with the maximum capacity of the system to NAD +. The maximum capacity of the mitochondrial respiratory chain depends on the overall level of metabolism of the body.
  • the metabolic harmless acetic acid derived from alcohol by acetaldehyde is oxidized to carbon dioxide and water mainly in extrahepatic tissues.
  • the organism NAD + As an oxidizing agent, the organism NAD +, as a reducing agent is mainly reduced nicotinamide adenine dinucleotide phosphate (NADPH) is used.
  • NADPH nicotinamide adenine dinucleotide phosphate
  • the ratio NADH / NAD + is small ( ⁇ 1), whereas in order to obtain a negative redox potential, the ratio
  • NAD (P) + transhydrogenase To maintain the balance between the two coenzyme systems u.a. the enzyme NAD (P) + transhydrogenase. From reduced NADH and oxidized NADP +, it catalyzes oxidized NAD + and reduced NADPH. This reaction can be according to the formula
  • Acetaldehyde is a cytotoxin that binds to various proteins of the liver and also to DNA and damages the mitochondria as well as the microtubular system.
  • Acetaldehyde is the first degradation product of ethanol, which is degraded in a further step to acetic acid. Acetaldehyde is held responsible for a number of alcohol-related organ damage.
  • acetaldehyde An accumulation of acetaldehyde by inhibiting the acetaldehyde degradation leads to headache, accelerated pulse rate, palpitations, nausea and vomiting and occurs in genetically induced alcohol intolerance after alcohol consumption on a regular basis. Much of the cat symptoms are attributed to the toxic effects of acetaldehyde.
  • acetaldehyde In a normal liver, 99% of the alcohol introduced by the blood circulation is degraded to acetic acid. The remaining percent is released as acetaldehyde in the cycle. Therefore, the capacity of the alcohol-degrading tissue is not sufficient to oxidize all the acetaldehyde (Fig. 1) in acetic acid as shown in Fig. 2. Acetaldehyde enters the bloodstream at a rate of approximately 1 mg / min (60 mg / h).
  • acetaldehyde binding compounds have been developed to reduce the amount of acetaldehyde released into the large blood circulation and to reduce the consequences of such release.
  • These compounds include the sulfur-containing amino acids cysteine and methionine. Oral administration of methionine to subjects while drinking alcohol has resulted in a 20% reduction in blood acetaldehyde concentrations.
  • methionine-bound acetaldehyde can later liberate and thus extinguish the small advantage achieved.
  • methionine and other similar substances do not affect the rate of alcohol metabolism or the
  • D-glyceraldehyde a metabolite of fructose
  • D-GA D-glyceraldehyde
  • No. 4,450,153 A proposes a solution to the problem in which the blood alcohol concentration can be lowered rapidly when an alcohol oxidase enzyme isolated from certain types of yeast is used. The said enzyme breaks down alcohol in the extracellular space to acetaldehyde. As a result, large amounts of acetaldehyde enter the bloodstream and consequently pose the risk of acetaldehyde poisoning.
  • EP 1 562 576 B1 describes the use of D-glyceric acid, its salts or its ester for the preparation of a pharmaceutical preparation for the improvement of alcohol metabolism.
  • D-glyceric acid d. H. the dextrorotatory optical isomer of glyceric acid.
  • D-glyceric acid is administered in greater than physiological amounts, it undergoes a conversion to D-GA.
  • This reaction uses the coenzyme NADH, which is oxidized to NAD +.
  • NADH coenzyme NADH
  • glutathione Due to its antioxidant effect glutathione is sold as a dietary supplement.
  • the therapeutic benefit of dietary glutathione is highly questionable because the orally taken tripeptide can neither be resorbed nor absorbed into the cells due to its size. It is decomposed into its amino acid constituents before absorption and resynthesized in the cell interior.
  • every body cell has the ability to produce glutathione.
  • WO 2006/103316 A1 and WO 2007/135241 A2 propose a combination of cysteine with various other substances, which is intended to achieve a uniform release of the cysteine in the gastrointestinal tract and a prevention of absorption.
  • the cysteine should enter into a chemical bond with the acetaldehyde. This is intended to reduce or eliminate the acetaldehyde from the cysteine in the gastrointestinal tract.
  • Another reaction such as a glutathione synthesis, can not occur in the intestine due to lack of enzymes.
  • the low efficiency of the cysteine which may be due to a reaction of the cysteine with other reactants, has proven to be disadvantageous.
  • the release of the cysteine in the gastrointestinal tract the amount of substance available for binding the acetaldehyde is comparatively low.
  • EP 0 397 646 A1 relates to a pharmaceutical preparation for the treatment of liver diseases.
  • the liver protection preparation can be used for the treatment of metabolic and toxic liver diseases in human and veterinary medicine.
  • Glutamic acid and cysteine play an important role in the formation of glutathione, which is important in the detoxification processes of the liver.
  • WO 2007/017139 A1 describes a composition for controlling the metabolism of alcohol and for reducing the risk of alcohol-related diseases, wherein the composition may, inter alia, also contain glutamine.
  • US 2003/021 1 172 A1 proposes a composition containing glycine and glutathione.
  • DE 10 201 1 008 478 A1 shows a holistic dietary supplement which consists of mixtures of various dried vegetable and fruit powders. Due to the large number of active substances contained therein, the new dietary supplements are generally used for the prevention of malnutrition and diseases, which also glutathione, coenzyme Q10 and / or L-carnitine may be added.
  • EP 1 982 604 A1 relates to a food supplement which comprises a vegetable constituent, a grass constituent, a fruit constituent, a vitamin and preferably an amino acid which may also contain L-glutamine or L-cysteine.
  • the object of the present invention is to propose a preparation or food supplement for improving the metabolism of alcohol, in particular ethanol, which ensures efficient degradation of the acetaldehyde.
  • the object is achieved by a preparation or dietary supplement for improving the metabolism of alcohol, which contains as an essential component glutathione and / or substances from which the body synthesizes the glutathione.
  • the invention is based on the finding that in glutathione reductase from a GSSG dimer with consumption of NADPH, the production of the required for the degradation of acetaldehyde by acetaldehyde dehydrogenase to acetate coenzyme NAD + can be increased, the essential idea of the invention is that not as in the prior art teaching, the acetaldehyde is removed from the gastrointestinal tract by a chemical bond, but rather is formed by the glutathione NAD + which, as a limiting ingredient, accelerates ADH and ALDH.
  • the enzymatic conversion is substantially accelerated or catalyzed without a direct chemical reaction of the glutathione with the acetaldehyde. It has been shown that the rate of degradation of acetaldehyde can be significantly increased in this way, so that after a short time, the undesirable side effects are significantly reduced or disappear.
  • the substances used comprise at least cysteine and also glycine and / or glutamic acid.
  • the supply of cysteine as well as glycine and / or glutamic acid increases the production of glutathione in the body.
  • the glutathione transfers electrons free radicals to neutralize them, whereby the glutathione is oxidized.
  • This is converted by glutathione disulfide reductase into doubly reduced glutathione.
  • This NADPH is oxidized to NADP +, which is subsequently converted to NAD +.
  • the NAD + is thus directly available for the degradation of alcohol as well as the acetaldehyde degradation.
  • cysteine is not consumed by further reactions, but remains available for the production of glutathione.
  • cysteine leads to the formation of glutathione, but due to the lack of stimulation by another building block and by the reaction with other reactants, the rate of synthesis will be lower.
  • a substrate amount of 10% to 20% of the cysteine used suffices.
  • a particularly effective modification is achieved by administration as a powder, granules, capsule, tablet or in a solution. This achieves a simple dosage for the user and at the same time creates the conditions for a release of the constituents in the desired proportions.
  • the release of the cysteine and of the glycine and / or the glutamic acid is delayed in time by a corresponding galenics.
  • the ratio between glutamic acid, cysteine and glycine is 1: 2: 1 or, for cysteine, glutamine and glycine, between
  • a one-sided excess which in practice leads to an undesirable shift in the reaction equilibrium, can be avoided.
  • the preparation or dietary supplement contains essentially only two of the components cysteine, glutamine and glycine, these being present in an amount ratio of 1-20: 1-20. In practice, this corresponds to a daily dose in an amount between 100 mg and 13.4 g of the respective component cysteine, glutamine or glycine.
  • the preparation or dietary supplement containing pantothenic acid and zinc. Furthermore, it has already proven to be particularly practical if the preparation or dietary supplement additionally contains vitamins and minerals, which improve the effectiveness.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)

Abstract

Préparation pharmaceutique ou complément alimentaire destinés à l'amélioration du métabolisme de l'alcool. Pour obtenir une dégradation particulièrement efficace de l'acétaldéhyde, ladite préparation contient, en tant que constituant essentiel, du glutathion et/ou des substances à partir desquelles le corps synthétise le glutathion. La conversion enzymatique est ainsi considérablement accélérée ou catalysée, sans qu'il se produise une réaction chimique directe du glutathion avec l'acétaldéhyde. Il est apparu que la vitesse de dégradation de l'acétaldéhyde peut être considérablement augmentée de cette manière, si bien que les effets secondaires indésirables sont notablement diminués ou disparaissent au bout d'un court laps de temps.
PCT/DE2012/100090 2011-04-04 2012-04-03 Préparation ou complément alimentaire Ceased WO2012136204A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102011001768.2 2011-04-04
DE102011001768A DE102011001768A1 (de) 2011-04-04 2011-04-04 Präparat oder Nahrungsergänzungsmittel

Publications (2)

Publication Number Publication Date
WO2012136204A2 true WO2012136204A2 (fr) 2012-10-11
WO2012136204A3 WO2012136204A3 (fr) 2012-12-27

Family

ID=46201055

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DE2012/100090 Ceased WO2012136204A2 (fr) 2011-04-04 2012-04-03 Préparation ou complément alimentaire

Country Status (2)

Country Link
DE (1) DE102011001768A1 (fr)
WO (1) WO2012136204A2 (fr)

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4450153A (en) 1982-09-30 1984-05-22 Phillips Petroleum Company Alcohol removal from blood with alcohol oxidase
EP0397646A1 (fr) 1989-05-11 1990-11-14 Homosan Ag Préparation pharmaceutique pour le traîtement de maladies hépatiques
US20030211172A1 (en) 2002-05-10 2003-11-13 Jones Jeremy Park Composition and method for substantially reducing the deleterious effects of alcohol on the body
EP1562576B1 (fr) 2002-10-14 2006-06-21 Remedal Ltd. Amelioration du metabolisme de l'alcool
WO2006103316A1 (fr) 2005-04-01 2006-10-05 Biohit Oyj Préparation alimentaire se liant à l'acétaldéhyde présent dans la bouche et dans l'appareil digestif, et méthode d'élaboration de ladite préparation
WO2007017139A1 (fr) 2005-07-29 2007-02-15 Tima Foundation Composition destinée à modérer le métabolisme de l’alcool et à réduire le risque de maladies induites par l’alcool
WO2007135241A2 (fr) 2006-05-22 2007-11-29 Biohit Oyj Composition et méthode de liaison de l'acétaldéhyde dans l'estomac
EP1982604A1 (fr) 2007-04-20 2008-10-22 Naturheilzentrum Allgäu Complément alimentaire destiné à équilibrer les carences alimentaires
DE102011008478A1 (de) 2010-01-29 2011-08-04 Müller-Schulte, Detlef, Dr., 52066 Ganzheitliches Nahrungsergänzungsmittel

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090104313A1 (en) * 2007-10-18 2009-04-23 Brian Lottig Nutrient-enhanced alcoholic beverage formulations and methods of making the same

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4450153A (en) 1982-09-30 1984-05-22 Phillips Petroleum Company Alcohol removal from blood with alcohol oxidase
EP0397646A1 (fr) 1989-05-11 1990-11-14 Homosan Ag Préparation pharmaceutique pour le traîtement de maladies hépatiques
US20030211172A1 (en) 2002-05-10 2003-11-13 Jones Jeremy Park Composition and method for substantially reducing the deleterious effects of alcohol on the body
EP1562576B1 (fr) 2002-10-14 2006-06-21 Remedal Ltd. Amelioration du metabolisme de l'alcool
DE60306410T2 (de) 2002-10-14 2007-06-14 Remedal Ltd. Verbesserung des alkoholstoffwechsels
WO2006103316A1 (fr) 2005-04-01 2006-10-05 Biohit Oyj Préparation alimentaire se liant à l'acétaldéhyde présent dans la bouche et dans l'appareil digestif, et méthode d'élaboration de ladite préparation
WO2007017139A1 (fr) 2005-07-29 2007-02-15 Tima Foundation Composition destinée à modérer le métabolisme de l’alcool et à réduire le risque de maladies induites par l’alcool
WO2007135241A2 (fr) 2006-05-22 2007-11-29 Biohit Oyj Composition et méthode de liaison de l'acétaldéhyde dans l'estomac
EP1982604A1 (fr) 2007-04-20 2008-10-22 Naturheilzentrum Allgäu Complément alimentaire destiné à équilibrer les carences alimentaires
DE102011008478A1 (de) 2010-01-29 2011-08-04 Müller-Schulte, Detlef, Dr., 52066 Ganzheitliches Nahrungsergänzungsmittel

Also Published As

Publication number Publication date
WO2012136204A3 (fr) 2012-12-27
DE102011001768A1 (de) 2012-10-04

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