WO2024253632A1 - Agent en composition - eugéroïque - Google Patents

Agent en composition - eugéroïque Download PDF

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Publication number
WO2024253632A1
WO2024253632A1 PCT/UA2024/000033 UA2024000033W WO2024253632A1 WO 2024253632 A1 WO2024253632 A1 WO 2024253632A1 UA 2024000033 W UA2024000033 W UA 2024000033W WO 2024253632 A1 WO2024253632 A1 WO 2024253632A1
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WO
WIPO (PCT)
Prior art keywords
eugeroic
dextrorotatory
levorotatory
caffeine
racemic
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/UA2024/000033
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English (en)
Russian (ru)
Inventor
Вадим Алексеевич Козловский
Роман Васильевич ЕФИМЕНКО
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Individual
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Individual
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Publication of WO2024253632A1 publication Critical patent/WO2024253632A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • A61K31/205—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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/221—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4172—Imidazole-alkanecarboxylic acids, e.g. histidine
    • 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 medicine, in particular to nutritional science and pharmaceuticals, namely, to the composition of a composition for relieving fatigue and tiredness.
  • Fatigue is defined as a state of the body in which the physiological processes of the body cannot be maintained at a level sufficient for normal functioning due to excessive load for a given process or, in other words, the organs cannot maintain a given intensity of physical or mental load [Lebedev M.A., Palatov S.Yu., Kovrov G.V. RMZh. Medical Review. Vol. 22, No. 4, 2014, pp. 4-7].
  • Fatigue is a symptom complex accompanying tiredness, its, figuratively speaking, "business card”, manifested by a feeling of weakness, lethargy, impotence, drowsiness, combined with a feeling of physical and mental discomfort, decreased physical and mental performance, changes in mood and quality of life. Fatigue syndrome can occur as a result of overexertion, and also develop and last chronically. In the latter case, this condition requires long-term complex treatment. In contrast, fatigue due to overexertion is a physiological process and disappears after proper and sufficient rest.
  • Fatigue is a complex physiological process that includes many physiological and biochemical factors, and this normal physiological phenomenon inevitably occurs at a certain stage of mental activity or physical activity of the body. This means a temporary decrease in the initial performance of the body and is a sign that the body needs rest [Lebedev M. A., Palatov S. Yu., Kovrov G. V. RMZh. Medical Review. Vol. 22, No. 4, 2014, pp. 4-7].
  • a typical representative is phenamine (amphetamine) [Heal, David J; Smith, Sharon L; Gosden, Jane; Nutt, David J. Amphetamine, past and present - a pharmacological and clinical perspective bnrnnZ of Psychopharmacology. 27 (6): 479-496. doi: 10.1177/0269881113482532].
  • Another class of drugs are eugeroics, i.e. drugs against drowsiness as an extreme manifestation of fatigue.
  • a representative of this group is modafinil. Its use leads to an improvement in concentration, determination, memory and other mental abilities; a decrease in drowsiness; an increase in performance; as well as a decrease in appetite and a decrease in food consumption [Y. In, K. Tomoo, T. Ishida, Y. Sakamoto: Crystal and Molecular Structure of an (S)-(+)- Enantiomer of Modafinil, a Novel Wake-Promoting Agent. In: Chem. Pharm. Bull. 52, 2004, S. [1186-1189].
  • modafinil is accompanied by a number of common side effects.
  • the most common side effects are insomnia, headache, loss of appetite.
  • Simultaneous use of modafinil with alcohol and other psychoactive drugs can lead to death. With prolonged use of the drug and its sudden cancellation, modafinil withdrawal syndrome develops.
  • Caffeine is a natural substance that exhibits its effect precisely when nervous system fatigue develops and is widely used to temporarily increase performance. Its action is associated with competitive antagonism with a neurotransmitter substance in the brain that accumulates during fatigue - adenosine. Caffeine, by blocking the brain's receptors to adenosine, delays the development of the sensation of the brain "falling asleep".
  • the present invention provides methods for mixing a chewing gum composition with caffeine, which also reduce bitterness by selecting caffeine, wherein the caffeine has a particle size distribution of about 0.0% by 40 mesh, about 1-20% by 60 mesh, about 5-30% by 80 mesh and at least about 50% by 80 mesh. processing time and sequence for mixing the various ingredients.
  • a chewing gum composition comprising a water-insoluble base portion, a water-soluble portion and caffeine, wherein the caffeine has a particle size distribution of about 0.0% by 40 mesh, about 1-20% by 60 mesh, about 5-30% by 80 mesh and at least about 50% by 80 mesh.
  • the small particle size of caffeine in combination with the sweeteners acesulfame and gluconolactone makes this gum palatable and ensures the release of caffeine into the oral cavity [US 6024988 A, A23G 4/06, A23G 4/068, A23V 2002/00, published 15.02.2000].
  • a nutraceutical composition of caffeine with theanine is also known.
  • the embodiment of this invention provides compositions or mechanisms for oral administration of caffeine using a functional nutraceutical confectionery composition.
  • the nutraceutical confectionery composition is provided with a ratio of caffeine to L-theanine in the range of from about 1:1 to about 1:2.
  • the nutraceutical confectionery composition can contain caffeine in the range of from about 5 mg to about 100 mg per serving.
  • L-theanine can be provided in the range of from about 5 mg to about 200 mg per serving.
  • a method of treatment for increasing energy and alertness while maintaining relaxation and concentration is provided.
  • the method includes orally administering to an individual a nutraceutical confectionery composition containing caffeine and L-theanine in combination with a nutraceutically acceptable carrier such that caffeine and L-theanine are absorbed through the oral mucosa of the individual.
  • a variant of the confectionery composition is chewing gum, which allows for the release of ingredients into the oral cavity. This allows for enhancing and accelerating the effects of caffeine [US 10441535 B2, IPC: A61K 9/68, A23K 31/198, A23K 31/522, A23G 4/06, A61G 4/12, A61G 4/14, A23L 33/105, A23L 33/175, A61K 9/20, publ. [15.10.2019].
  • the invention provides a healthy alternative in beverages that provide energy and focus and that feature increased availability of beneficial nutrients.
  • a source of choline is used (citicoline is particularly useful) and is surprisingly effective even at low levels (or even in the absence) of caffeine in increasing energy levels in subjects who drink these compositions.
  • the energy composition of this embodiment comprises a relatively low concentration of methylated xanthine, a choline derivative, and at least one flavoring agent in an amount sufficient to make the energy composition palatable.
  • the energy composition further comprises one or more amino acids or amino acid derivatives.
  • amino acids or derivatives thereof include, but are not limited to, N-acetyl L-tyrosine, L-phenylalanine, taurine, and combinations thereof.
  • the amino acids or derivatives thereof are present in an amount of from about 0.005 to about 0.05 g/mL.
  • the amino acids or derivatives thereof are present in an amount of from about 0.01 to about 0.03 g/mL.
  • the amino acids or derivatives thereof are present in an amount of from about 0.0125 to about 0.025 g/mL.
  • N-acetyl L-tyrosine is present in an amount of from about 0.001 to about 0.01 g/mL. In a particular case, N-acetyl L-tyrosine is present in an amount of from about 0.002 to about 0.009 g/mL. In another particular case, N-acetyl L-tyrosine is present in an amount of from about 0.003 to about 0.007 g/mL.
  • L-phenylalanine is present in an amount of about 0.001 to about 0.008 g/ml. In a particular case, L-phenylalanine is present in an amount of about 0.002 to about 0.007 g/ml. In another particular case, L-phenylalanine is present in an amount of about 0.003 to about 0.007 g/ml [RU 2487645 C2, IPC: A23L 2/38, published 20.07.2013, Bulletin No. 20].
  • the invention was based on the task of creating a composite eugeroic agent by selecting components, which would have a significant eugeroic effect and contribute to increased vigor and performance, would have a rapid effect, and would also expand the range of effective means for the prevention of fatigue and tiredness.
  • the composite eugeroic agent based on amino acids contains amino acids or their derivatives, selected from the group: dextrorotatory, levorotatory or racemic tyrosine, dextrorotatory, levorotatory or racemic histidine, dextrorotatory, levorotatory or racemic acetyltyrosine, dextrorotatory, levorotatory or racemic acetylhistidine, 2-methylguanidine aminoacetic acid (creatine) in the form of pharmaceutically acceptable salts.
  • the second additional difference is that for every 1 mass fraction of tyrosine there is additionally from 0.2 to 1 mass fraction of a psychostimulant.
  • a third additional difference is that the psychostimulant is caffeine in the form of a pharmaceutically acceptable salt or its plant equivalent.
  • the fourth additional difference is that the psychostimulant is modafinil or its derivative in the form of a pharmaceutically acceptable salt.
  • One of the options for producing the composition is to make it in the form of an effervescent tablet.
  • compositions are its use in the form of lozenges, with a different composition of excipients, where in one embodiment of the invention the tablet is a lollipop.
  • composition is to use it in the form of a solution or drink.
  • Such a composition exhibits a significant eugeric effect and helps to increase vigor and performance in general, and the use of the lozenge form accelerates its action, since the composition, when used in this way, releases substances into the oral cavity, from where they are absorbed very quickly.
  • the manufacturing stages include calculating the required quantities of components, mixing them until a homogeneous mass is obtained, for example using a "drunk barrel” mixer, adding substances to the mixture that ensure the mass is tableted, mixing them, feeding them to the tableting device, followed by the pressing stage, preliminarily, if necessary, moistening and granulating the mass for tableting.
  • the resulting tablets are packed in primary packaging.
  • Flavoring agent The effectiveness of the proposed composition was also tested in a study on the authors themselves in the Ratatype typing test.
  • the essence of the test is typing text on a computer for 1 minute in the browser of the www.ratatype.com website (https://www.ratatype.ua/typing-test/).
  • the typing speed is automatically measured in characters/min - how many characters per minute are typed without errors. Any symbol, including spaces, is considered a "character”. Only correctly typed words are taken into account. As a result, the speed (in characters/min) and the accuracy of the typed text (in %) are determined.
  • the authors performed the test typing for 2 days in a row, in the morning and in the evening. Day 1 is a control day, day 2 is an experimental day, when the composition according to the invention was taken in the best version 15 minutes before the test.
  • the eugeroic compound reduced the subjective feeling of evening lethargy and drowsiness after use in each of the researchers.
  • Industrial acceptability All substances are available on the market. A person skilled in the art will have no difficulty in producing a form of the composition according to the invention using generally accepted methods and means.

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention se rapporte au domaine de la médecine, notamment au domaine de la nutrition et de la pharmacie, et concerne notamment la formule d'une composition pour éliminer la fatigue et l'épuisement. Cet agent en composition - eugéroïque comprend des acides aminés ou leurs dérivés choisis dans le groupe: tyrosine dextrogyre ou sinistrogyre ou racémique, histidine dextrogyre ou sinistrogyre ou racémique, acétyltyrosine dextrogyre ou sinistrogyre ou racémique, acétylhistidine dextrogyre ou sinistrogyre ou racémique, acide 2-méthyl-guanidinoacétique (créatine) ou ses dérivés phosphorés sous forme de sels pharmaceutiquement acceptables. Cet agent assure un effet eugéroïque important, une augmentation de la vigueur et de la capacité de travail, une action rapide ainsi qu'un élargissement du nombre de moyens efficaces pour prévenir la fatigue et l'épuisement.
PCT/UA2024/000033 2023-06-06 2024-06-06 Agent en composition - eugéroïque Ceased WO2024253632A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
UAA202302737 2023-06-06
UAA202302737 2023-06-06

Publications (1)

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WO2024253632A1 true WO2024253632A1 (fr) 2024-12-12

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Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
PLISZKA ANDREW G.: "Modafinil: A Review and Its Potential Use in the Treatment of Long CO VID Fatigue and Neurocognitive Deficits", THE AMERICAN JOURNAL OF PSYCHIATRY RESIDENTS JOURNAL, vol. 17, no. 4, pages 5 - 7, XP093250618, DOI: 10.1176/appi.ajp-rj.2022.170402 *
SASAHARA IKUKO, FUJIMURA NAOKO, NOZAWA YOSHIZU, FURUHATA YASUFUMI, SATO HITOSHI: "The effect of histidine on mental fatigue and cognitive performance in subjects with high fatigue and sleep disruption scores", PHYSIOLOGY AND BEHAVIOR, ELSEVIER SCIENCE LTD., OXFORD, GB, vol. 147, 1 August 2015 (2015-08-01), GB , pages 238 - 244, XP093250612, ISSN: 0031-9384, DOI: 10.1016/j.physbeh.2015.04.042 *
STULIKOVA E.L., KHRISTULENKO A.L., GNILITSKAYA V.B., KRIVUSHCHEV V.B.: "Kofe: pol'za ili vred dlya serdechno-sosudistoy sistemy? [Coffee: Benefit or Harm for the Cardiovascular System?]", AKTUALNYE VOPROSY KARDIOLOGII [CURRENT ISSUES IN CARDIOLOGY]; DONETSK, DECEMBER 23, 2022, DONETSK, 23 December 2022 (2022-12-23) - 23 December 2022 (2022-12-23), Donetsk, pages 1 - 18, XP009561042 *
TKACHEVA NATALIA, ELISEEVA TATYANA: "Tyrosine - description, benefits, effects on the body and the best sources", JOURNAL OF HEALTHY NUTRITION AND DIETETICS, vol. 7, no. 1, 1 January 2019 (2019-01-01), XP093250611 *
WATANABE AIRI, KATO NOBUMASA, KATO TADAFUMI: "Effects of creatine on mental fatigue and cerebral hemoglobin oxygenation", NEUROSCIENCE RESEARCH., ELSEVIER, SHANNON., IR, vol. 42, no. 4, 1 April 2002 (2002-04-01), IR , pages 279 - 285, XP093250613, ISSN: 0168-0102, DOI: 10.1016/S0168-0102(02)00007-X *
WIEGMANN D.L., D. F. NERI, R. R. STANNY, S. A. SHAPPELL, A. H. MCCARDIE, D. L. MCKAY: "Behavioral Effects of Tyrosine During Sustained Wakefulness", NAVAL AEROSPACE MEDIC-AL RESEARCH LABORATORY, 20 December 1993 (1993-12-20), XP093250607, Retrieved from the Internet <URL:https://apps.dtic.mil/sti/tr/pdf/ADA279789.pdf> *

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