WO2004080454A1 - Composition contenant du 5-hydroxytryptophane destinee a diminuer ou soulager les effets du sevrage nicotinique et son utilisation - Google Patents

Composition contenant du 5-hydroxytryptophane destinee a diminuer ou soulager les effets du sevrage nicotinique et son utilisation Download PDF

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Publication number
WO2004080454A1
WO2004080454A1 PCT/IB2004/000726 IB2004000726W WO2004080454A1 WO 2004080454 A1 WO2004080454 A1 WO 2004080454A1 IB 2004000726 W IB2004000726 W IB 2004000726W WO 2004080454 A1 WO2004080454 A1 WO 2004080454A1
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WO
WIPO (PCT)
Prior art keywords
composition according
smoking
composition
cessation
vitamin
Prior art date
Application number
PCT/IB2004/000726
Other languages
English (en)
Inventor
Andries Petrus Burger
Original Assignee
Andries Petrus Burger
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 Andries Petrus Burger filed Critical Andries Petrus Burger
Publication of WO2004080454A1 publication Critical patent/WO2004080454A1/fr

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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
    • A61K31/33—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
    • A61K31/4415—Pyridoxine, i.e. Vitamin B6
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355—Tocopherols, e.g. vitamin E
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A61K31/51—Thiamines, e.g. vitamin B1
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse

Definitions

  • the invention relates to a composition, particularly for use in alleviating and reducing the effects of the cessation of smoking, and more particularly during voluntary cessation attempts, forced temporary abstinence and/or as an aid to smoking reduction.
  • Nicotine also depletes serotonin (5-HT) in the brain. Smoking is becoming increasingly a social problem.
  • Environmental tobacco smoke also known as “passive smoking”, “involuntary smoking” or “second-hand smoke”
  • Smokers seem to be well aware of the problem of weight gain following smoking cessation. Greater appetite and hunger as well as increased preference for carbohydrates are common withdrawal symptoms. Smokers compensate for non-smoking by an increase in eating and nibbling. The fear of weight gain after smoking cessation may be an important factor in the persistence of smoking, particularly for women who use cigarettes as a method of appetite suppression and weight control.
  • NRT nicotine replacement therapies
  • non-nicotine based medications which are mostly prescription drugs.
  • the applicant has thus identified a need for a non-nicotine based, freely available over-the-counter (OTC) and cost-effective pharmacological aid which addresses both the physiological and psychological aspects of dependence on cigarette smoking.
  • the composition may be used to alleviate and reduce withdrawal symptoms as an aid to smoking cessation, smoking reduction or during temporary abstinence
  • 5-hydroxytryptophan for use in alleviating and reducing one or more of the effects of the cessation of nicotine withdrawal.
  • the nicotine withdrawal is typically as a result of the cessation of tobacco smoking, in particular during voluntary cessation attempts, temporary abstinence and/or as an aid to smoking reduction.
  • the temporary abstinence may be for a period of from a few hours to a few days, as a result of a smoker being temporarily restricted to a no-smoking area, such as an aircraft, airport building or hospital. Typically, the period is for less than 48 hours.
  • the effects of nicotine withdrawal which are reduced may include nicotine craving, increased appetite, dysphoria or depressed mood, sleeplessness, irritability, frustration, anger, anxiety, difficulty in concentrating and restlessness.
  • nicotine craving and/or increase in appetite are reduced.
  • 5-HTP in the manufacture of a composition for use in alleviating and reducing the effects of the cessation of smoking during voluntary cessation attempts and temporary abstinence and as an aid to smoking reduction.
  • compositions particularly for use in alleviating and reducing the effects of cessation of smoking, including 5-HTP, together with one or more of a potentiator, an anti- stress agent and an antioxidant, in particular during voluntary cessation attempts, temporary abstinence and/or as an aid to smoking reduction.
  • the 5-HTP is used, in the manner described above, in combination with a glycine compound selected from N- monomethyl glycine, N,N-dimethyl glycine, trimethyl glycine, and salts thereof.
  • a glycine compound selected from N- monomethyl glycine, N,N-dimethyl glycine, trimethyl glycine, and salts thereof.
  • the invention provides the use of 5-hydroxytryptophan (5-HTP) for use in alleviating and reducing the effects of the cessation of smoking, in particular during voluntary cessation attempts, temporary abstinence and/or as an aid to smoking reduction.
  • 5-hydroxytryptophan 5-HTP
  • Serotonin or 5-Hydroxytriptamine (5-HT) is a downstream metabolite in the two-step metabolic pathway that begins with the precursor amino acid L- tryptophan. Once in the body, L-tryptophan is converted to 5-HTP and from there, serotonin (5-HT) is produced.
  • 5-HTP is the immediate precursor in the biosynthesis of serotonin (5-HT). 5- HTP readily crosses the blood-brain barrier and becomes available for serotonin (5-HT) synthesis. In the brain, serotonin (5-HT) fulfils the function of a neurotransmitter in the central nervous system.
  • Serotonin (5-HT) is involved in a large number of physiological events and a multitude of brain functions are influenced by serotonin (5-HT). These include sleep, appetite, the perception of pain, mood, anxiety, aggression, stress and nervousness.
  • the oral administration of 5-HTP may help to restore or increase serotonin (5-HT) levels in the brain.
  • 5-HTP is obtained from a natural plant extract from the seeds of the African tree, Griffonia Simplicifolia.
  • the 5-HTP will be administered in the form of a composition.
  • the composition may be divided into a number of easily administered units such that when all the units are taken over a day, this provides the required daily dose of the 5-HTP for the patient.
  • the daily dose of 5-HTP will typically be in the range of from 25 mg to 400 mg, in: i. divided doses of 5 mg to 100 mg, or ii. a single, controlled-release dosage form.
  • the composition will typically be a solid, for example a tablet or capsule, a semi-solid, such as a soft gelatine capsule, or in liquid form, for example a solution or flowable dispersion.
  • the method of administering the composition is sub-lingual, where absorption from the oral mucosa enhances the bio-availability of 5-HTP in the central nervous system.
  • sub-lingual administration prevents the peripheral conversion of 5-HTP to serotonin (5-HT) outside the central nervous system.
  • the composition may also contain a glycine compound, a potentiator such as folic acid, an anti-stress agent such as vitamin B1 thiamine hydrochloride and/or vitamin B6 pyridoxine hydrochloride or an anti-oxidant such as vitamin C or vitamin E.
  • a glycine compound such as folic acid
  • an anti-stress agent such as vitamin B1 thiamine hydrochloride and/or vitamin B6 pyridoxine hydrochloride or an anti-oxidant such as vitamin C or vitamin E.
  • the composition will also contain usual excipients known in the art.
  • composition contained the following ingredients:
  • composition contained the following ingredients:
  • Vitamin C (Sodium Ascorbate) 3 mg
  • a controlled release tablet contained the following ingredients:

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention se rapporte à une composition destinée en particulier à diminuer et à soulager au moins l'un des effets du sevrage nicotinique, et contenant du 5-hydroxytryptophane (5-HTP). Le sevrage nicotinique intervient généralement lorsqu'on cesse de fumer du tabac, en particulier lors de tentatives délibérées pour cesser de fumer, d'une interruption momentanée et/ou d'une diminution du niveau de consommation. Les effets de ce sevrage qui sont diminués ou soulagés comprennent le manque de nicotine, la dysphorie ou un état dépressif, l'insomnie, l'irritabilité, la frustration, la colère, l'anxiété, le manque de concentration et l'agitation, ainsi que, en particulier, une augmentation de l'appétit. Cette composition peut contenir un composé de glycine.
PCT/IB2004/000726 2003-03-14 2004-03-15 Composition contenant du 5-hydroxytryptophane destinee a diminuer ou soulager les effets du sevrage nicotinique et son utilisation WO2004080454A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ZA200302082 2003-03-14
ZA2003/2082 2003-03-14

Publications (1)

Publication Number Publication Date
WO2004080454A1 true WO2004080454A1 (fr) 2004-09-23

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Application Number Title Priority Date Filing Date
PCT/IB2004/000726 WO2004080454A1 (fr) 2003-03-14 2004-03-15 Composition contenant du 5-hydroxytryptophane destinee a diminuer ou soulager les effets du sevrage nicotinique et son utilisation

Country Status (1)

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WO (1) WO2004080454A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006075011A3 (fr) * 2005-01-14 2006-11-23 Organon Nv Inhibiteurs du recaptage de la glycine pour le traitement de la dependance a une drogue

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA914078B (en) * 1990-03-07 1992-03-25 Rautenbach Ignatius A composition containing an active ingredient
BE1005200A3 (fr) * 1991-08-27 1993-05-25 Vandendael Kathleen Mariette Utilisation de tryptophane et composition nutritionnelle comprenant du tryptophane.
ZA99925B (en) * 1998-02-11 1999-08-05 Andries Petrus Burger Composition.
US6132724A (en) * 1998-04-29 2000-10-17 City Of Hope National Medical Center Allelic polygene diagnosis of reward deficiency syndrome and treatment
US20010036486A1 (en) * 2000-05-08 2001-11-01 Rosenthal Norman E. Method for treating nicotine addiction and deterring tobacco use with hypericum perforatum
US20020078969A1 (en) * 2000-12-21 2002-06-27 David Wastchak Method for reducing the effect of nicotine addiction and dependancy

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA914078B (en) * 1990-03-07 1992-03-25 Rautenbach Ignatius A composition containing an active ingredient
BE1005200A3 (fr) * 1991-08-27 1993-05-25 Vandendael Kathleen Mariette Utilisation de tryptophane et composition nutritionnelle comprenant du tryptophane.
ZA99925B (en) * 1998-02-11 1999-08-05 Andries Petrus Burger Composition.
US6132724A (en) * 1998-04-29 2000-10-17 City Of Hope National Medical Center Allelic polygene diagnosis of reward deficiency syndrome and treatment
US20010036486A1 (en) * 2000-05-08 2001-11-01 Rosenthal Norman E. Method for treating nicotine addiction and deterring tobacco use with hypericum perforatum
US20020078969A1 (en) * 2000-12-21 2002-06-27 David Wastchak Method for reducing the effect of nicotine addiction and dependancy

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DATABASE CHEMABS [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 4 October 1992 (1992-10-04), RAUTENBACH, IGNATIUS ET AL: "A composition containing tryptophan for alleviating side effects of cessation of smoking", XP002287643, retrieved from STN Database accession no. 1992:537703 *
DATABASE WPI Section Ch Week 200003, Derwent World Patents Index; Class B05, AN 2000-039503, XP002287655 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006075011A3 (fr) * 2005-01-14 2006-11-23 Organon Nv Inhibiteurs du recaptage de la glycine pour le traitement de la dependance a une drogue
AU2006205796B2 (en) * 2005-01-14 2010-09-02 Merck Sharp & Dohme B.V. Glycine reuptake inhibitors for treating drug and alcohol dependence

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