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WO2003011340A1 - Formulation medicamenteuse destinee a une utilisation topique aux fins de therapie et de prophylaxie d'hyperhydrose - Google Patents

Formulation medicamenteuse destinee a une utilisation topique aux fins de therapie et de prophylaxie d'hyperhydrose Download PDF

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Publication number
WO2003011340A1
WO2003011340A1 PCT/EP2002/008101 EP0208101W WO03011340A1 WO 2003011340 A1 WO2003011340 A1 WO 2003011340A1 EP 0208101 W EP0208101 W EP 0208101W WO 03011340 A1 WO03011340 A1 WO 03011340A1
Authority
WO
WIPO (PCT)
Prior art keywords
hyperhidrosis
glycopyrrolate
salts
derivatives
enantiomers
Prior art date
Application number
PCT/EP2002/008101
Other languages
German (de)
English (en)
Inventor
Johannes Wohlrab
Original Assignee
Johannes Wohlrab
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 Johannes Wohlrab filed Critical Johannes Wohlrab
Publication of WO2003011340A1 publication Critical patent/WO2003011340A1/fr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels

Definitions

  • the invention relates to a pharmaceutical formulation for topical use for the therapy and prophylaxis of hyperhidrosis axillary, palmaris et plantaris and other forms of hyperhidrosis.
  • This pharmaceutical formulation is based on the use of glycopyrrolate, its salts and / or its derivatives.
  • glycopyrronium bromide with the chemical formula 3- (cyclopentylhydroxyphenyl-acetoxy) -1, 1-dimethylpyrronium bromide is a spasmolytic, anticholinergic (parasympatholytic)
  • GPB has an effect.
  • the mechanism of action is due to a blockade of the muscarinic receptors.
  • the strong hydrophilicity of GPB prevents passage through the blood-brain barrier and thus central effects.
  • the molar mass of the glycopyrronium bromide is 398.36 g / mol and the melting point of the compound is 193-198 ° C.
  • GPB is a white powder.
  • the stability of this compound is pH-dependent, the stability decreasing at a pH> 6.
  • GPB is a slightly water-soluble compound.
  • GPB has so far been used primarily as a secretion-inhibiting and spasmolytic substance in adjuvant therapy with special anesthetic or surgical procedures.
  • BTX botulinum toxin
  • a pharmaceutical formulation for topical use for the therapy and prophylaxis of hyperhidrosis axillary, palamaris et plantaris and / or other forms of hyperhidrosis is provided.
  • This pharmaceutical formulation contains a glycopyrrolate, its salts and / or its derivatives and / or its enantiomers in an amount between 0.05 and 20% by weight.
  • a gel and / or colloid-containing carrier system is used as the vehicle system.
  • the application is not locally restricted here; rather, these vehicle systems enable the pharmaceutical formulation according to the invention to can be easily applied in the armpit area, for example, and even with increased sweat secretion, the penetration of the active ingredient can be ensured over a longer period of time compared to aqueous solutions.
  • glycopyrrolate, its salts and / or its derivatives are preferably used in a concentration of between 0.5 and 5% by weight.
  • Glycopyrronium bromide is preferably used as the salt of the glycopyrrolate.
  • hydroxyethyl cellulose gel is preferably used.
  • glycopyrrolate, its salts and / or its derivatives and / or its enantiomers for the manufacture of a medicament for topical use for the therapy and prophylaxis of hyperhidrosis axillaris, palmaris et plantaris and / or other forms of hyperhidrosis is also used according to the invention taught.
  • the compound is used in a concentration between 0.05 to 20% by weight, preferably between 0.5 and 5% by weight.
  • Three concentrations were placebo-controlled with GPB (0.5; 2.0; 4.0%) in hydroxyethyl cellulose gel (hydroxyethyl cellulose 10000 2.5 parts; glycerol 85% 10.0 parts; water (cons.) 87, 5 parts) examined for their effectiveness.
  • the hyperhidrosis was objectified using quantitative hidroiuetry.
  • Group 1 1 week 3 times a day + 3 weeks 1 time a day
  • Group 2 2 weeks 2 times a day + 2 weeks 1 time a day
  • Group 3 1 week 3 times a day + 1 week 2 times a day + 2 weeks 1 time a day
  • Group 4 4 weeks 3 times a day
  • the hyperhidrosis was objectified using quantitative hydrometry.
  • the analysis of variance was used to analyze three and more samples (treatment groups) from normally distributed populations with the same variance. Since only one factor, the influence of the investigational medicinal product, was to be examined in the various mean value groups, the one-way analysis of variance (one-way ANOVA) was used. Here random samples with unknown common variance are examined. In addition, the differences between the individual groups will be examined using the Scheffe assessment of linear contrasts. For comparison of three or more independent groups, the Kruskal-Wallis-Test (H-Test) was offered, which tests the analog hypotheses of the one-way analysis of variance as a non-parametric test. The unpaired t-test was used to compare two samples with the same variance. Differences with an error probability of p ⁇ 0.05 were rated as statistically significant.
  • H-Test Kruskal-Wallis-Test
  • test preparations were stored in 75 ml glass jars with a ball attachment.
  • hydroxyethyl cellulose gel as a vehicle system is only suitable for the therapy of hyperhidrosis axillaris, but not for hyperhidrosis palmaris (FIG. 2).

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)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une formulation médicamenteuse destinée à une utilisation topique aux fins de thérapie et de prophylaxie d'hyperhydrose axillaire, palmaire et plantaire et d'autres formes d'hyperhydrose. Cette formulation médicamenteuse est basée sur l'utilisation de glycopyrrolate, de ses sels et/ou de ses dérivés.
PCT/EP2002/008101 2001-07-26 2002-07-19 Formulation medicamenteuse destinee a une utilisation topique aux fins de therapie et de prophylaxie d'hyperhydrose WO2003011340A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2001136404 DE10136404A1 (de) 2001-07-26 2001-07-26 Arzneiformulierung zur topischen Anwendung für die Therapie und Prophylaxe von Hyperhidrosis
DE10136404.0 2001-07-26

Publications (1)

Publication Number Publication Date
WO2003011340A1 true WO2003011340A1 (fr) 2003-02-13

Family

ID=7693160

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/008101 WO2003011340A1 (fr) 2001-07-26 2002-07-19 Formulation medicamenteuse destinee a une utilisation topique aux fins de therapie et de prophylaxie d'hyperhydrose

Country Status (2)

Country Link
DE (1) DE10136404A1 (fr)
WO (1) WO2003011340A1 (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004084905A3 (fr) * 2003-03-24 2005-04-28 Univ Florida Methodes de traitement de l'hyperhidrose idiopathique et de pathologies associees
WO2006069998A2 (fr) 2004-12-27 2006-07-06 Beiersdorf Ag Le compose glycopyrrolate dans des preparations cosmetiques
US8558008B2 (en) 2013-02-28 2013-10-15 Dermira, Inc. Crystalline glycopyrrolate tosylate
WO2014134510A1 (fr) * 2013-02-28 2014-09-04 Dermira, Inc. Sels de glycopyrrolate
US9006462B2 (en) 2013-02-28 2015-04-14 Dermira, Inc. Glycopyrrolate salts
MD4369C1 (ro) * 2011-03-04 2016-04-30 Sosei R&D Ltd Utilizarea glicopirolatului pentru tratarea tahicardiei, doză unică, dispozitiv de administrare, metodă de tratament şi profilaxie a tahicardiei
KR20180091361A (ko) 2017-02-06 2018-08-16 주식회사 퍼슨 발한억제 기능을 가지는 자외선 차단 화장료 조성물 및 이를 사용한 자외선 차단제의 제조방법

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102005029388B4 (de) * 2005-06-23 2018-12-27 Beiersdorf Ag Wirkstoffkombinationen aus Glycopyrroniumbromid und einem oder mehreren partiell neutralisierten Ester von Monoglyceriden und/oder Diglyceriden gesättigter Fettsäuren mit Zitronensäure
DE102004063726A1 (de) * 2004-12-27 2006-07-06 Beiersdorf Ag Emulsionen enthaltend Glycopyrroniumbromid, Polyethylenglykol(2) stearylether und Polyethylenglykol(21) stearylether
DE102005029389A1 (de) * 2005-06-23 2007-01-04 Beiersdorf Ag Wirkstoffkombinationen aus Glycopyrroniumbromid und dialkylsubstituierten Essigsäuren
DE102005029387B4 (de) 2005-06-23 2018-12-27 Beiersdorf Ag Wirkstoffkombinationen aus Glycopyrroniumbromid und Polyglyceryl(3)-Methylglucosedistearat
DE102005029386A1 (de) * 2005-06-23 2007-01-11 Beiersdorf Ag Wirkstoffkombinationen aus Glycopyrroniumbromid und einem oder mehreren Hydrokolloiden
DE102005029390A1 (de) * 2005-06-23 2007-01-04 Beiersdorf Ag Wirkstoffkombinationen aus Glycopyrroniumbromid und Polyolen

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5962505A (en) * 1998-08-31 1999-10-05 Bobrove; Arthur M. Method for treating hot flashes in humans
WO2000012087A1 (fr) * 1998-08-31 2000-03-09 Bobrove Arthur M Traitement des bouffees de chaleur chez des sujets humains
WO2001008681A1 (fr) * 1999-08-02 2001-02-08 First Horizon Pharmaceutical Corporation Methodes d'administration de compositions de glycopyrrolates

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5962505A (en) * 1998-08-31 1999-10-05 Bobrove; Arthur M. Method for treating hot flashes in humans
WO2000012087A1 (fr) * 1998-08-31 2000-03-09 Bobrove Arthur M Traitement des bouffees de chaleur chez des sujets humains
WO2001008681A1 (fr) * 1999-08-02 2001-02-08 First Horizon Pharmaceutical Corporation Methodes d'administration de compositions de glycopyrrolates

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
MAY J S ET AL: "Frey's syndrome: treatment with topical glycopyrrolate.", HEAD & NECK. UNITED STATES 1989 JAN-FEB, vol. 11, no. 1, January 1989 (1989-01-01), pages 85 - 89, XP008009263, ISSN: 1043-3074 *
SEUKERAN D C ET AL: "The use of topical glycopyrrolate in the treatment of hyperhidrosis.", 1998, CLINICAL AND EXPERIMENTAL DERMATOLOGY, VOL. 23, NR. 5, PAGE(S) 204-205, ISSN: 0307-6938, XP001122802 *

Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004084905A3 (fr) * 2003-03-24 2005-04-28 Univ Florida Methodes de traitement de l'hyperhidrose idiopathique et de pathologies associees
WO2006069998A2 (fr) 2004-12-27 2006-07-06 Beiersdorf Ag Le compose glycopyrrolate dans des preparations cosmetiques
MD4369C1 (ro) * 2011-03-04 2016-04-30 Sosei R&D Ltd Utilizarea glicopirolatului pentru tratarea tahicardiei, doză unică, dispozitiv de administrare, metodă de tratament şi profilaxie a tahicardiei
US8859610B2 (en) 2013-02-28 2014-10-14 Dermira, Inc. Crystalline glycopyrrolate tosylate
US10004717B2 (en) 2013-02-28 2018-06-26 Dermira, Inc. Glycopyrrolate salts
US9006462B2 (en) 2013-02-28 2015-04-14 Dermira, Inc. Glycopyrrolate salts
US9006461B2 (en) 2013-02-28 2015-04-14 Dermira, Inc. Crystalline glycopyrrolate tosylate
US9259414B2 (en) 2013-02-28 2016-02-16 Dermira, Inc. Glycopyrrolate salts
US8558008B2 (en) 2013-02-28 2013-10-15 Dermira, Inc. Crystalline glycopyrrolate tosylate
US9610278B2 (en) 2013-02-28 2017-04-04 Dermira, Inc. Glycopyrrolate salts
WO2014134510A1 (fr) * 2013-02-28 2014-09-04 Dermira, Inc. Sels de glycopyrrolate
US11291651B2 (en) 2013-02-28 2022-04-05 Journey Medical Corporation Glycopyrrolate salts
EP3473615A1 (fr) * 2013-02-28 2019-04-24 Dermira, Inc. Sels de glycopyrrolate
US10543192B2 (en) 2013-02-28 2020-01-28 Dermira, Inc. Glycopyrrolate salts
US10548875B2 (en) 2013-02-28 2020-02-04 Dermira, Inc. Glycopyrrolate salts
US11291652B2 (en) 2013-02-28 2022-04-05 Journey Medical Corporation Glycopyrrolate salts
KR20180091361A (ko) 2017-02-06 2018-08-16 주식회사 퍼슨 발한억제 기능을 가지는 자외선 차단 화장료 조성물 및 이를 사용한 자외선 차단제의 제조방법

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Publication number Publication date
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