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WO2016018178A1 - Produit anti-nicotinique universel - Google Patents

Produit anti-nicotinique universel Download PDF

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Publication number
WO2016018178A1
WO2016018178A1 PCT/RU2015/000438 RU2015000438W WO2016018178A1 WO 2016018178 A1 WO2016018178 A1 WO 2016018178A1 RU 2015000438 W RU2015000438 W RU 2015000438W WO 2016018178 A1 WO2016018178 A1 WO 2016018178A1
Authority
WO
WIPO (PCT)
Prior art keywords
nicotine
smoking
theanine
tryptophan
rule
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/RU2015/000438
Other languages
English (en)
Russian (ru)
Other versions
WO2016018178A4 (fr
Inventor
Дмитрий Евгеньевич ДЕНИСОВ
Людмила Борисовна ТИМИРОВА
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
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of WO2016018178A1 publication Critical patent/WO2016018178A1/fr
Publication of WO2016018178A4 publication Critical patent/WO2016018178A4/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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • A61K31/465—Nicotine; Derivatives thereof

Definitions

  • the invention relates to pharmaceuticals and parapharmaceuticals, and in particular to means for smoking cessation.
  • the difficulty of weaning from cigarettes lies in the nature of the mechanism of dependence on smoking, which affects all systems of the human body. Physical nicotine dependence is due to the participation of nicotine in the biochemical processes of the body. Psychological is based on the fact that smoking tones and improves mood.
  • Nicotine and alkaloids based on nicotine and alkaloids with the nicotine-like action of Tabex, Lobesil, Gamibazin, Nicoretto, Nicotinell and others, produced in various forms (tablets, chewing gums, cigarettes, transdermal systems, etc.) are widely known. These drugs facilitate smoking cessation, but are substitution therapy, reduce the physical symptoms of withdrawal symptoms and do not affect the psychological component of nicotine addiction. The disadvantage of these funds is the toxic effect of nicotine and alkoloids with a nicotine-like effect.
  • Antagonists of nicotinic acetylcholine receptors Varenicline (Champex) and the antidepressant Bupropion are more effective.
  • a medicament containing nicotinic acid, Vinibis, pyroxan and nootropil is proposed. (RU 2132203). Pyroxan - eliminates the craving for nicotine. Nootropil and nicotinic acid restore and strengthen the walls of blood vessels, improve brain nutrition. The main disadvantage of this solution is its low effectiveness in relation to the physical symptoms of withdrawal.
  • compositions containing the amino acids theanine and / or tryptophan with the ability to reduce craving for smoking (US7094787, EP2338360, CA2385415).
  • the proposed funds do not contain components of replacement therapy.
  • the technical result of the proposed solution is the creation of a means to quit smoking or reduce craving for smoking during periods of forced abstinence, with a reduced content of nicotine and alkaloids with a nicotine-like effect, in order to reduce the toxicity of these compounds and additionally has a faster and more effective action compared to analogues.
  • the claimed result is achieved by creating a composition comprising nicotine or a nicotine-like alkaloid, and the amino acids theanine and tryptophan.
  • nicotine means the nicotine alkaloid and its derivatives (base, salts, etc.), for example nicotine hydrochloride, nicotine sulfate, nicotine salicylate, nicotine ditartrate dihydrate and others.
  • SUBSTITUTE SHEET (RULE 26)
  • the concept of “alkaloids with a nicotine-like effect” encompasses nicotine-type compounds — cytisine, lobelia hydrochloride, anabazine, anatabine, nornikotin, beta-nicotirine, beta-nornototirin and n-nicotine oxide, and others.
  • the term “theanine” (L-theanine, 1-thianine, 1-Theanine, 1-teanin) of the present invention is an amino acid derived from glutamic acid ( ⁇ -glutamyl ethylamide), obtained mainly from tea leaves, as well as synthetic and microbiological . Any form of the amino acid L-theanine, D-theanine and DL-theanine can be used, but it is preferable to use the L-form.
  • Theanine of the present invention can be used both as an amino acid and as an extract of green tea.
  • the tryptophan of the present invention may be 1-tryptophan, 5-hydroxytryptophan and other biologically active forms of tryptophan and its derivatives obtained by various methods.
  • Nicotine and its substitutes in the composition help reduce the severity of physiological withdrawal symptoms.
  • Theanine increases the level of dopamine, has a calming and relaxing, but at the same time activating mental activity.
  • L-tryptophan - enhances the production of the neurotransmitter serotonin and melatonin, which are responsible for mood and quality of sleep.
  • tryptophan stimulates the release of endorphin, the level of which decreases sharply after quitting smoking (US 20081031 11).
  • Group 1 Four men aged 35-42 years, smoking experience 10-14 years, the number of cigarettes smoked from 10 to 15 per day.
  • Group 2 Two men aged 35-44 years and Two women aged 32-37 years, smoking experience 10-15 years, the number of cigarettes smoked from 10 to 20 per day.
  • Cytisine - 1 mg, tryptophan -50 mg and excipients The group was asked to take pills every time they had another desire to smoke, while completely abstaining from smoking for 3 days.
  • Group 3 Three men aged 32-45 years, two women 29 and 45 years old smoking 10–25 years, the number of cigarettes smoked from 10 to 25 per day.
  • Pills were taken every time a regular desire to smoke arose with complete abstinence from smoking for 3 days.
  • Nicotine and nicotine-like alkaloids may be contained in the proposed anti-nicotine agent in the following dosages of nicotine from 1.5 mg to 1 mg, lobelin hydrochloride from 1.5 mg to 1
  • SUBSTITUTE SHEET (RULE 26) mg, anabazine hydrochloride 2 mg - 1 mg, cytisine from 1 mg to 0.5 mg in 1 dose.
  • the concentration of theanine can vary from 50 to 200 mg per dose, but more preferably 100-150 mg; tryptophan - from 8 to 50 mg per dose, more preferably from 20 to 40 mg.
  • the frequency of use of the proposed tool is selected individually, depending on the number of cigarettes smoked per day and smoking experience, type and condition of the nervous system, etc., and can vary from 4 to 6 times a day, with a gradual decrease in the frequency of intake.
  • the use of the drug can be started either after the complete cessation of smoking, or after reducing the number of cigarettes smoked.
  • the duration of the course is also selected individually and is at least 5 days and can be continued up to 4-6 weeks. In relapses (resuming smoking), the course of treatment can be repeated.
  • the anticotinic agent of the present invention can be used in the form of sweets (chewing, caramel, lozenges, lozenges, etc.), chewing gum, tablets (chewing, sublingual, etc.), as well as drops, syrups and transdermal systems with controlled release as explained by the examples below.
  • the active substances are introduced into the tablet mass at the granulation stage.
  • Example 2 Tablets for oral administration.
  • microcrystalline, talc, calcium stearate microcrystalline, talc, calcium stearate.
  • microcrystalline, talc, calcium stearate microcrystalline, talc, calcium stearate.
  • Excipients sorbitol, anhydrous sodium carbonate, sodium bicarbonate, flavor, glycerol, semisynt.
  • Nicotine, theanine and tryptophan are directly introduced with stirring into the mass of chewing gum at a temperature not exceeding 5 ° C.
  • SUBSTITUTE SHEET (RULE 26) citric acid, flavor, color.
  • the current composition is introduced in powder form at the stage of preparation and processing of the mass of chewing candy at a temperature of from 50 ° C to 35-40 ° C.
  • Example 5 Syrup for oral administration - 20 doses.
  • thermopsis extract with a cytisine content of 0.15% - 12 ml

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne la pharmacie et la parapharmacie et notamment des produits pour se déshabituer du tabac. On propose un produit anti-nicotinique complexe contenant de la nicotine ou un alcaloïde de type nicotine et des acides aminés théanine 5-200 mg et tryptophane 8-50 mg dans une dose. Le produit peut être conditionnée sous forme de bonbons, gomme à mâcher, comprimés, gouttes, sirops et systèmes transdermiques.
PCT/RU2015/000438 2014-07-29 2015-07-10 Produit anti-nicotinique universel Ceased WO2016018178A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2014131493/15A RU2572720C1 (ru) 2014-07-29 2014-07-29 Комплексное антиникотиновое средство
RU2014131493 2014-07-29

Publications (2)

Publication Number Publication Date
WO2016018178A1 true WO2016018178A1 (fr) 2016-02-04
WO2016018178A4 WO2016018178A4 (fr) 2016-03-24

Family

ID=55087022

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU2015/000438 Ceased WO2016018178A1 (fr) 2014-07-29 2015-07-10 Produit anti-nicotinique universel

Country Status (2)

Country Link
RU (1) RU2572720C1 (fr)
WO (1) WO2016018178A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020206511A1 (fr) * 2019-04-12 2020-10-15 Sopharma Ad Composition pharmaceutique orale contenant un alcaloïde végétal pour le traitement de dépendances
CN115813011A (zh) * 2022-12-30 2023-03-21 东莞市吉纯生物技术有限公司 一种具有茶氨酸的雾化液的制备方法与应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5316759A (en) * 1986-03-17 1994-05-31 Robert J. Schaap Agonist-antagonist combination to reduce the use of nicotine and other drugs
CA2385415A1 (fr) * 2000-07-21 2002-01-31 Taiyo Kagaku Co., Ltd. Compositions pour reguler le desir de fumer
EP2338360A1 (fr) * 2008-09-17 2011-06-29 Yonglin Liang Matériau de filtre de cigarette alexipharmique et sa préparation

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2499067T3 (es) * 2005-10-13 2014-09-26 Nitto Denko Corporation Preparación transdérmica de nicotina y método de producción de la misma

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5316759A (en) * 1986-03-17 1994-05-31 Robert J. Schaap Agonist-antagonist combination to reduce the use of nicotine and other drugs
CA2385415A1 (fr) * 2000-07-21 2002-01-31 Taiyo Kagaku Co., Ltd. Compositions pour reguler le desir de fumer
EP2338360A1 (fr) * 2008-09-17 2011-06-29 Yonglin Liang Matériau de filtre de cigarette alexipharmique et sa préparation

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020206511A1 (fr) * 2019-04-12 2020-10-15 Sopharma Ad Composition pharmaceutique orale contenant un alcaloïde végétal pour le traitement de dépendances
JP2022528299A (ja) * 2019-04-12 2022-06-10 ソファーマ アクツィオネルノ ドロジェストヴォ 依存症の治療のための植物アルカロイドを有する経口薬学的組成物
US12156944B2 (en) 2019-04-12 2024-12-03 Sopharma Ad Oral pharmaceutical composition with a plant alkaloid for treatment of dependencies
CN115813011A (zh) * 2022-12-30 2023-03-21 东莞市吉纯生物技术有限公司 一种具有茶氨酸的雾化液的制备方法与应用

Also Published As

Publication number Publication date
WO2016018178A4 (fr) 2016-03-24
RU2572720C1 (ru) 2016-01-20

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