WO2007125074A1 - Utilisation de l'alverine pour la prevention et/ou le traitement des troubles de la sexualite chez les hommes et les femmes - Google Patents

Utilisation de l'alverine pour la prevention et/ou le traitement des troubles de la sexualite chez les hommes et les femmes Download PDF

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Publication number
WO2007125074A1
WO2007125074A1 PCT/EP2007/054094 EP2007054094W WO2007125074A1 WO 2007125074 A1 WO2007125074 A1 WO 2007125074A1 EP 2007054094 W EP2007054094 W EP 2007054094W WO 2007125074 A1 WO2007125074 A1 WO 2007125074A1
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WO
WIPO (PCT)
Prior art keywords
sexual
alverine
increase
pharmaceutical composition
metabolites
Prior art date
Application number
PCT/EP2007/054094
Other languages
English (en)
Inventor
Mark Crawford
Frédéric Revah
Original Assignee
Cerep
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 Cerep filed Critical Cerep
Publication of WO2007125074A1 publication Critical patent/WO2007125074A1/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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives

Definitions

  • Alverine for the prevention and/or treatment of male and female sexual dysfunctions
  • the present invention relates to the utilization of a drug for the prevention and/or treatment of sexual dysfunctions in men and women, and particularly hypoactive sexual desire disorder (or hypoactive sexual desire disease).
  • This invention relates in particular to the use of a drug designed to improve the syndrome known as Hypoactive Sexual Desire
  • HSDD Homeopathic Disease
  • Such a drug contains the active ingredient Alverine, or its metabolites, salts or esters.
  • Hypoactive Sexual Desire Disease or Hypoactive Sexual Desire Disorder
  • HSDD Hypoactive Sexual Desire Disorder
  • HSDD can be at the origin of a feeling of malaise, concern or frustration and have negative consequences on the relationship between a woman and her partner.
  • it is estimated that one woman out of three following surgical menopause, suffers from a decrease in sexual desire and almost half of these women develop the related feeling of personal distress (Leiblum S, Koochaki P, Rodenberg C, Rosen R. Prevalence of low sexual desire and sexual activity levels amongst populations of menopausal women, NAMS Oral presentation 2002).
  • This disorder despite presenting several clinical signs similar to depression, is distinct and unrelated to underlying causes of depression.
  • the preferred route of administration for a medication designed to treat sexual dysfunctions is the oral route, and the drug itself must be as well tolerated as possible and have as few contraindications as possible.
  • Alverine to reduce the signs of sexual dysfunctions and in particular of HSDD.
  • the advantage of Alverine is that it is a drug which has been on the market for more than 50 years and which shows a very low level of toxicity and side effects compared to most drugs.
  • the present invention relates to the new therapeutic use of Alverine or its metabolites, esters and salts for the preparation of pharmaceutical compositions for the prevention and/or treatment of male and female sexual dysfunctions.
  • the present invention relates to a method for the prevention and/or treatment of male and female sexual dysfunctions in humans, particularly HSDD, comprising administering Alverine or its metabolites, esters and salts.
  • the invention also concerns a method to increase sexual desire and/or to increase sexual activity and/or to increase sexual performances and/or to increase the intensity of sexual pleasure and/or to increase sexual satisfaction, by administration of a pharmaceutical composition containing Alverine or its metabolites, salts and esters, in humans not suffering from sexual dysfunctions.
  • Alverine means N-Ethyl-3,3'-diphenyldipropylamine:
  • Alverine metabolites include in particular, but not only, the mono or poly- hydroxylated derivatives on the phenyl rings and the mono or poly-carboxylation of the aliphatic chains.
  • Metabolite 1 Three of the main metabolites following incubation of Alverine with human liver microsomes are: Metabolite 1:
  • Pharmaceutically acceptable salts are defined as salts combined with Alverine which can be obtained by chemical reaction of Alverine with a mineral or organic acid, using a known chemical method.
  • acids which can be used for this purpose, one can list the sulphuric, chlorhydric, bromhydric; phosphoric, 4-toluene-sulfonic, methane- sulfonic, cyclohexyl sulfamic, axalic, succinic, formic, fumaric, maleic, citric, aspartic, cinnamic, lactic, glutamic, N-acetyl aspartic, N-acetyl glutamic, ascorbic, malic, benzoic, nicotinic and acetic acids.
  • Alverine citrate and tartrate have been widely used for pharmaceutical preparations in other indications.
  • Alverine is marketed as an antispasmodic agent specifically for symptomatic relief of pain due to irritable bowl and dysmenorrhoea.
  • There are several publications demonstrating antispasmodic action in animal models for example, see Bouvier, M; Grimaud, JC; Abysique, A; Chiarelli, P; Effects of alverine on the spontaneous electrical activity and nervous control of the proximal colon of the rabbit; Gastroenterol Clin Biol. 1992;16(4):334-8).
  • Castroenterol Clin Biol. 1992;16(4):334-8 there are published clinical trials suggesting that Alverine is no more effective than placebo in relieving pain associated with irritable bowel syndrome.
  • Alverine The mode of action of Alverine remains unknown.
  • the activity of Alverine as an agent useful to prevent of treat sexual dysfunctions has never been described, reported or suggested
  • Alverine, its metabolites, salts and esters can be administered in acceptable pharmaceutical compositions by several routes well known for this type of product.
  • this invention relates to the utilization of Alverine and/or of its metabolites in a pharmaceutically acceptable composition to be administered by oral, sublingual, buccal, sub-cutaneous, transdermal, local, rectal, intranasal or injectable (in particular intra-peritoneal, intra-venous or intra-muscular) routes.
  • this invention relates to the utilization of Alverine and/or its metabolites, salts and esters for the preparation of a pharmaceutical composition which can be administered orally, particularly as tablets or capsules.
  • the active ingredients of the pharmaceutical compositions included in this invention may be in any form suitable for oral administration, including tablets, capsules and liquid preparations such as elixirs and syrups including various additional substances designed to modify the color, taste or stability of the preparation.
  • the active ingredient can be mixed with various common substances such a starch, calcium carbonate, lactose, sucrose, dicalcium-phosphate to facilitate the encapsulation process.
  • various common substances such as starch, calcium carbonate, lactose, sucrose, dicalcium-phosphate to facilitate the encapsulation process.
  • Magnesium stearate may be used in addition for its lubricating properties if necessary.
  • the present invention also relates to the utilization of Alverine and/or its metabolites, salts and esters, for the preparation of a pharmaceutical composition which can be administered via an injection.
  • the active ingredients of the injectable pharmaceutical preparations in this invention may be dissolved or mixed in a suspension in a pharmaceutically acceptable sterile liquid, such as sterile water, sterile organic solvent or a mixture of both for an intravenous preparation.
  • a pharmaceutically acceptable sterile liquid such as sterile water, sterile organic solvent or a mixture of both for an intravenous preparation.
  • routes of administration include, but are not limited to, subcutaneous implants and other preparations to be administered by the buccal, sublingual, transdermal, topical, intranasal or rectal routes.
  • Biodegradable and non-biodegradable systems may also be used.
  • this invention relates to the utilization of Alverine, its metabolites, salts and esters for the preparation of a pharmaceutical composition to be administered through one of the above-mentioned routes at doses of 1 to 1000 mg of the active ingredient formulated as capsules or tablets or at doses of 0.1 to 500 mg of the active ingredient formulated as suppositories, ointments, creams, gels, aerosols, to be administered in human therapeutics in one or several daily doses for an adult of 60-70 kg of average weight.
  • this invention relates to the utilization of Alverine, its metabolites, salts and esters for the preparation of a pharmaceutical composition designed to be administered to prevent or treat hypoactive sexual desire disorders.
  • this invention relates to the non- therapeutic utilization of Alverine, its metabolites, salts and esters for the preparation of a pharmaceutical composition to be used to increase sexual desire and/or increase sexual activity and/or increase sexual performance and/or increase the intensity of sexual pleasure and/or increase the sexual intercourse satisfaction in humans not suffering from sexual dysfunctions.

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  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (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)

Abstract

La présente invention concerne la préparation d'une composition pharmaceutique comprenant de l'alvérine, ses métabolites, ses sels ou ses esters, destinée à prévenir ou à traiter les troubles de la sexualité chez les hommes et les femmes, en particulier les troubles liés à l'hypoactivité du désir sexuel. La présente invention concerne en particulier la préparation d'une composition pharmaceutique destinée à prévenir ou à traiter les troubles des réponses physiologiques et/ou anatomiques à la stimulation sexuelle chez les humains.
PCT/EP2007/054094 2006-04-28 2007-04-26 Utilisation de l'alverine pour la prevention et/ou le traitement des troubles de la sexualite chez les hommes et les femmes WO2007125074A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0603849A FR2900337A1 (fr) 2006-04-28 2006-04-28 Utilisation de l'alverine pour le traitement des dysfonctions sexuelles
FR0603849 2006-04-28

Publications (1)

Publication Number Publication Date
WO2007125074A1 true WO2007125074A1 (fr) 2007-11-08

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2007/054094 WO2007125074A1 (fr) 2006-04-28 2007-04-26 Utilisation de l'alverine pour la prevention et/ou le traitement des troubles de la sexualite chez les hommes et les femmes

Country Status (2)

Country Link
FR (1) FR2900337A1 (fr)
WO (1) WO2007125074A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2165704A1 (fr) 2008-09-23 2010-03-24 François Fauran Utilisation de l'alvérine dans le traitement des affections cutanées

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992002488A1 (fr) * 1990-08-08 1992-02-20 Norgine Limited Derives de propylamine
GB2272155A (en) * 1992-11-05 1994-05-11 Wyeth John & Brother Ltd Piperazine derivatives for treatment of cognitive disorders
FR2798590A1 (fr) * 1999-09-21 2001-03-23 Oreal Utilisation de l'alverine pour diminuer les rides
US6239126B1 (en) * 1998-12-17 2001-05-29 American Home Products Corporation Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives
FR2869538A1 (fr) * 2004-04-30 2005-11-04 Cerep Sa Utilisation de l'alverine, seul ou en combinaison avec un antidepresseur tricyclique ou un antidepresseur inhibiteur specifique de la recapture de la serotonine pour le traitement de la depression

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992002488A1 (fr) * 1990-08-08 1992-02-20 Norgine Limited Derives de propylamine
GB2272155A (en) * 1992-11-05 1994-05-11 Wyeth John & Brother Ltd Piperazine derivatives for treatment of cognitive disorders
US6239126B1 (en) * 1998-12-17 2001-05-29 American Home Products Corporation Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives
FR2798590A1 (fr) * 1999-09-21 2001-03-23 Oreal Utilisation de l'alverine pour diminuer les rides
FR2869538A1 (fr) * 2004-04-30 2005-11-04 Cerep Sa Utilisation de l'alverine, seul ou en combinaison avec un antidepresseur tricyclique ou un antidepresseur inhibiteur specifique de la recapture de la serotonine pour le traitement de la depression

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
COELHO A-M ET AL: "RECTAL ANTINOCICEPTIVE PROPERTIES OF ALVERINE CITRATE ARE LINKED TO ANTAGONISM AT EH 5-HT1A RECEPTOR SUBTYPE", JOURNAL OF PHARMACY AND PHARMACOLOGY, LONDON, GB, vol. 53, no. 10, 2001, pages 1419 - 1426, XP009025660, ISSN: 0022-3573 *
FAVA MAURIZIO ET AL: "SEXUAL FUNCTIONING AND SSRIS", JOURNAL OF CLINICAL PSYCHIATRY, XX, XX, vol. 63, no. SUPPL 5, 2002, pages 13 - 16,23, XP009076331, ISSN: 0160-6689 *
GUTHRIE E ET AL: "Severe sexual dysfunction in women with the irritable bowel syndrome: comparison with inflammatory bowel disease and duodenal ulceration.", BRITISH MEDICAL JOURNAL (CLINICAL RESEARCH ED.) 5 SEP 1987, vol. 295, no. 6598, 5 September 1987 (1987-09-05), pages 577 - 578, XP002411916, ISSN: 0267-0623 *
SMITH GRAEME D: "Effect of nurse-led gut-directed hypnotherapy upon health-related quality of life in patients with irritable bowel syndrome.", JOURNAL OF CLINICAL NURSING. JUN 2006, vol. 15, no. 6, June 2006 (2006-06-01), pages 678 - 684, XP002411917, ISSN: 0962-1067 *
WARNOCK JULIA JILL K: "Female hypoactive sexual desire disorder: epidemiology, diagnosis and treatment.", CNS DRUGS. 2002, vol. 16, no. 11, 2002, pages 745 - 753, XP009076278, ISSN: 1172-7047 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2165704A1 (fr) 2008-09-23 2010-03-24 François Fauran Utilisation de l'alvérine dans le traitement des affections cutanées

Also Published As

Publication number Publication date
FR2900337A1 (fr) 2007-11-02

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