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WO1992013540A1 - Antalgic ointment - Google Patents

Antalgic ointment Download PDF

Info

Publication number
WO1992013540A1
WO1992013540A1 PCT/EP1992/000244 EP9200244W WO9213540A1 WO 1992013540 A1 WO1992013540 A1 WO 1992013540A1 EP 9200244 W EP9200244 W EP 9200244W WO 9213540 A1 WO9213540 A1 WO 9213540A1
Authority
WO
WIPO (PCT)
Prior art keywords
ointment
cocaine
menthol
analgesic
salicylic ester
Prior art date
Application number
PCT/EP1992/000244
Other languages
French (fr)
Inventor
Guy Parent
Marc Parent
Original Assignee
Guy Parent
Marc Parent
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 Guy Parent, Marc Parent filed Critical Guy Parent
Publication of WO1992013540A1 publication Critical patent/WO1992013540A1/en

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
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A61K31/618—Salicylic acid; Derivatives thereof having the carboxyl group in position 1 esterified, e.g. salsalate
    • A61K31/621—Salicylic acid; Derivatives thereof having the carboxyl group in position 1 esterified, e.g. salsalate having the hydroxy group in position 2 esterified, e.g. benorylate
    • 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
    • A61K31/60—Salicylic acid; Derivatives thereof

Definitions

  • the present invention relates to an analgesic ointment which acts very quickly, effectively and harmlessly through the skin against any muscular pain such as tendinitis, elongation, muscle fatigue, cramping, breakdown, joint pain, torticollis, lumbago, rheumatism.
  • the resulting relaxation allows better restoration of function and readjustment.
  • 'ointments containing plant extracts such as for example arnica, or containing medicinal products such as aluminum acetate, salicylic acid or its esters, butazolidine, coritsone and its derivatives, etc.
  • the object of the present invention was to develop a preparation capable of quickly relieving muscle or joint pain, generally requiring only one application or a small number of applications and causing neither irritation nor any other harmful effect.
  • the active constituents of the ointment according to the invention either cocaine (or one of the compounds mentioned below), menthol and an ester of salicylated acid are all well known in medicine.
  • the desired analgesic effect is however only obtained by using these constituents in the proportions specified in the claims. Any other proportion by far does not give the same good results.
  • the cocaine is preferably used in the form of its hydrochloride which represents the preferred antal ⁇ gic constituent.
  • the preferred salicylate is ethyl or ethyl salicylate, more preferably methyl salicylate.
  • any pharmaceutically acceptable base can be used, that is to say a base which does not irritate the skin and which easily penetrates the skin barrier, such as petrolatum, lanolin is the base of choice.
  • a cocaine derivative can be used and / or optionally add one or more of the following constituents:
  • the proportions are preferably the same as using cocaine.
  • a preferred composition is obtained by mixing:

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

Abstract

An excellent antalgic ointment contains an antalgic compound, preferably cocaine or novocaine, as well as menthol and a salicylic ester. The ointment may be administered through the skin to treat any muscular pain.

Description

Onguent antalgique Analgesic ointment
La présente invention se réfère a un onguent antal gique agissant très rapidement, effectivement et inoffen- sivement par voie cutanée contre toute douleur musculaire tel que tendinite, elongation, fatique musculaire, crampe, claquage, douleurs articulaires, torticolis, lumbagos, rheumatisme. La décontraction qui en résulte permet mieux la restauration de la fonction et la réadaption.The present invention relates to an analgesic ointment which acts very quickly, effectively and harmlessly through the skin against any muscular pain such as tendinitis, elongation, muscle fatigue, cramping, breakdown, joint pain, torticollis, lumbago, rheumatism. The resulting relaxation allows better restoration of function and readjustment.
On a tenté depuis très longtemps de traiter des douleurs musculaires qui peuvent être extrêmement des¬ agréables et peuvent inactiver le patient pendant des t t jours et des semaines, par application de lotions etWe have tried for a very long time to treat muscular pains which can be extremely pleasant and can inactivate the patient for t t days and weeks, by applying lotions and
' d'onguents contenant des extraits de plantes, tel que par exemple d'arnica, ou contenant des médicaments tel que l'acétate d'aluminium, l'acide salicylique ou ses esters, la butazolidine, la coritsone et ses dérivés, etc.'ointments containing plant extracts, such as for example arnica, or containing medicinal products such as aluminum acetate, salicylic acid or its esters, butazolidine, coritsone and its derivatives, etc.
Les produits connus jusqu'à présent, tout en donnant des résultats acceptables, demandent une applica¬ tion prolongée, généralement d'une semaine au moins avec plusieurs applications par jour. Un tel traitement n'amoin¬ dris les douleurs que lentement et risque par sa durée de provoquer des irritations de la peau.The products known up to now, while giving acceptable results, require a prolonged application, generally one week at least with several applications per day. Such treatment reduces pain only slowly and risks, over time, causing skin irritation.
Le but de la présente invention était de déve¬ lopper une préparation capable de soulager rapidement la douleur musculaire ou articulaire, ne nécessitant en géné¬ ral qu'une application ou un petit nombre d'applications et ne provoquant ni irritation ni autre effet nocif.The object of the present invention was to develop a preparation capable of quickly relieving muscle or joint pain, generally requiring only one application or a small number of applications and causing neither irritation nor any other harmful effect.
Ce but a été atteint d'une manière étonnante par l'onguent antalgique tel que défini dans les revendica¬ tions 1 et 4.This object was surprisingly achieved by the analgesic ointment as defined in claims 1 and 4.
Les constituants actifs de l'onguent selon l'in¬ vention, soit la cocaine (ou un des composés sous-men- tionnés) , le menthol et un ester d'acide salicylé sont tous bien connus en médicine. L'effet analgésique désiré n'est cependant obtenu qu'en utilisant ces constituant dans les proportions spécifiées dans les revendications. Toute autre proportion ne donne de loin pas les mêmes bons résultats.The active constituents of the ointment according to the invention, either cocaine (or one of the compounds mentioned below), menthol and an ester of salicylated acid are all well known in medicine. The desired analgesic effect is however only obtained by using these constituents in the proportions specified in the claims. Any other proportion by far does not give the same good results.
La cocaine est de préférence employée sous forme de son hydrochloride qui représente le constituant antal¬ gique préféré. Le salicylate préféré est le salicylate de éthyle ou d'éthyle, mieux le salicylate de méthyle.The cocaine is preferably used in the form of its hydrochloride which represents the preferred antal¬ gic constituent. The preferred salicylate is ethyl or ethyl salicylate, more preferably methyl salicylate.
Comme base d'onguent on peut employer toute base pharmaceutiquement acceptable, c'est-à-dire une base n'irritant pas la peau et pénétrant facilement la barrière cutanée, telle que la vaseline, la lanoline est la base de choix.As an ointment base, any pharmaceutically acceptable base can be used, that is to say a base which does not irritate the skin and which easily penetrates the skin barrier, such as petrolatum, lanolin is the base of choice.
Pour préparer l'onguent selon l'invention il suffit de mélanger selon les règles de l'art les consti¬ tuants à température ambiante jusqu'à homogénité complète et dissolution complète des constituants actifs dans la base. L'emploi de solvant est inutile.To prepare the ointment according to the invention, it suffices to mix according to the rules of the art the constituents at room temperature until complete homogeneity and complete dissolution of the active constituents in the base. The use of solvent is unnecessary.
Au lieu de la cocaïne on peut employer un dérivé de la cocaïne et/ou éventuellement ajouter un ou plusieurs des constituents suivants :Instead of cocaine, a cocaine derivative can be used and / or optionally add one or more of the following constituents:
lidocaîne fentanyl méthadone epinéphrine tetracaîne cimétidine hydroxyzine prilocaine vérapamil lithium carbonate de lithium imidazoles diacêtylmorphine oxymétazoline procaîne propanolamine solution TEC éthylsergide ergotamine ainsi que tout composé similaire. Les proportions sont de préférence les mêmes qu'en em¬ ployant la cocaïne.lidocaine fentanyl methadone epinephrine tetracaine cimetidine hydroxyzine prilocaine verapamil lithium lithium carbonate imidazoles diacetylmorphine oxymetazoline procain propanolamine TEC solution ethylsergide ergotamine as well as any similar compound. The proportions are preferably the same as using cocaine.
Une composition préférée est obtenue en mélan¬ geant :A preferred composition is obtained by mixing:
1 % en poids de cocaïne . HC1 3 % en poids de menthol1% by weight of cocaine. HC1 3% by weight of menthol
16 % en poids de 'salïcylat de méthyle16% by weight of methyl salicylate
80 % en poids de vaseline à température ambiante pendant 30 minutes. Ce mélange est en suite formulé en crème, pommade, gel ou onguent selon des méthodes connues. 80% by weight of petrolatum at room temperature for 30 minutes. This mixture is then formulated as a cream, ointment, gel or ointment according to known methods.

Claims

R e v e n d i c a t i o n s Claims
1. Onguent antalgique, caractérisé en ce qu'il contient1. Analgesic ointment, characterized in that it contains
0,8 à 1,5 % de cocaïne sous forme de sel, ou de la novacaîne,0.8 to 1.5% cocaine in the form of salt, or novacaine,
2 à 5 % de menthol,2 to 5% menthol,
12 à 20 % d'un ester salicylique dans une base d'onguent pharmaceutiquement acceptable, les pourcentages indiqués se référant au poids total de la composition.12 to 20% of a salicylic ester in a pharmaceutically acceptable ointment base, the percentages indicated referring to the total weight of the composition.
2. Onguent selon la revendication 1, caractéri¬ sé en ce qu'il contient 0,8 à 1,2 % de cocaïne.HC1 et de préférence 1 .2. Ointment according to claim 1, characterized in that it contains 0.8 to 1.2% cocaine.HC1 and preferably 1.
3. Onguent selon la revendication 2, caractérisé par la composition suivante : cocaïne.HC1 1 % menthol 3 % salicylate de méthyle 16 % vaseline 80 % .3. Ointment according to claim 2, characterized by the following composition: cocaine.HC1 1% menthol 3% methyl salicylate 16% vaseline 80%.
4. Onguent antalgique, caractérisé en ce qu'il contient un ou plusieurs des composés suivants : lidocaîne diactéylmorphine fentanyl méthadone epinéphrine tetracaîne cïmétïdine hydroxyzine prilocaîne vérapamil lithium carbonate de lithium imidazoles oxy étazline procaîme propanolamine solution TEC méthvlsergide ergotamine ge avec du menthol et un ester salicylique, 4. Analgesic ointment, characterized in that it contains one or more of the following compounds: lidocaine diactéylmorphine fentanyl méthadone epinephrine tetracaine cimetimine hydroxyzine prilocaine verapamil lithium lithium carbonate imidazoles oxy etazline procaine propanolamine solution TEC methvlsergide ergotamine ge with menthol and a salicylic ester,
PCT/EP1992/000244 1991-02-06 1992-01-31 Antalgic ointment WO1992013540A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH37191 1991-02-06
CH371/91-5 1991-02-06

Publications (1)

Publication Number Publication Date
WO1992013540A1 true WO1992013540A1 (en) 1992-08-20

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1992/000244 WO1992013540A1 (en) 1991-02-06 1992-01-31 Antalgic ointment

Country Status (2)

Country Link
AU (1) AU1183092A (en)
WO (1) WO1992013540A1 (en)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2092449A1 (en) * 1995-05-08 1996-11-16 Nan Kwang Hyeng Lee Processes for obtaining a soothing cream for pains in the muscles, joints, bones, lumbago, anti-inflammatory rheuma and slight burns.
WO1998000168A1 (en) * 1996-07-02 1998-01-08 Novartis Consumer Health S.A. Topical composition comprising a combination of antihistaminic compounds with terpenoid compounds
US5866143A (en) * 1995-03-24 1999-02-02 El Khoury And Stein, Ltd. Topical application of opioid drugs such as morphine for relief of itching and skin disease
US5919473A (en) * 1997-05-12 1999-07-06 Elkhoury; George F. Methods and devices for delivering opioid analgesics to wounds via a subdermal implant
US5994330A (en) * 1998-11-09 1999-11-30 El Khoury; Georges F. Topical application of muscarinic agents such as neostigmine for treatment of acne and other inflammatory conditions
US6011022A (en) * 1998-03-03 2000-01-04 El Khoury; George F. Topical application of muscarinic analgesic drugs such as neostigmine
US6143278A (en) * 1998-02-23 2000-11-07 Elkhoury; George F. Topical application of opioid analgesic drugs such as morphine
WO2000071125A2 (en) * 1999-05-21 2000-11-30 Lts Lohmann Therapie-Systeme Ag Pharmaceutical preparation containing the active substance diamorphine and its utilization in a method for treating opiate addiction
US6299902B1 (en) 1999-05-19 2001-10-09 The University Of Georgia Research Foundation, Inc. Enhanced transdermal anesthesia of local anesthetic agents

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ARCHIVES INTERNATIONALES DE PHYSIOLOGIE ET DE BIOCHIMIE vol. 95, no. 2, Juin 1987, pages 113 - 120; HIJI Y. ET AL.: 'enhancement of local anaesthesia action by organic acid salts' *
Dialog 1981749; Martindale Online; Martindale Id 2667-n9-d; dec 1989; *

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5866143A (en) * 1995-03-24 1999-02-02 El Khoury And Stein, Ltd. Topical application of opioid drugs such as morphine for relief of itching and skin disease
ES2092449A1 (en) * 1995-05-08 1996-11-16 Nan Kwang Hyeng Lee Processes for obtaining a soothing cream for pains in the muscles, joints, bones, lumbago, anti-inflammatory rheuma and slight burns.
WO1998000168A1 (en) * 1996-07-02 1998-01-08 Novartis Consumer Health S.A. Topical composition comprising a combination of antihistaminic compounds with terpenoid compounds
US5919473A (en) * 1997-05-12 1999-07-06 Elkhoury; George F. Methods and devices for delivering opioid analgesics to wounds via a subdermal implant
US6143278A (en) * 1998-02-23 2000-11-07 Elkhoury; George F. Topical application of opioid analgesic drugs such as morphine
US6011022A (en) * 1998-03-03 2000-01-04 El Khoury; George F. Topical application of muscarinic analgesic drugs such as neostigmine
US5994330A (en) * 1998-11-09 1999-11-30 El Khoury; Georges F. Topical application of muscarinic agents such as neostigmine for treatment of acne and other inflammatory conditions
US6299902B1 (en) 1999-05-19 2001-10-09 The University Of Georgia Research Foundation, Inc. Enhanced transdermal anesthesia of local anesthetic agents
WO2000071125A2 (en) * 1999-05-21 2000-11-30 Lts Lohmann Therapie-Systeme Ag Pharmaceutical preparation containing the active substance diamorphine and its utilization in a method for treating opiate addiction
WO2000071125A3 (en) * 1999-05-21 2001-03-15 Lohmann Therapie Syst Lts Pharmaceutical preparation containing the active substance diamorphine and its utilization in a method for treating opiate addiction
CN100457107C (en) * 1999-05-21 2009-02-04 Lts勒曼治疗系统股份公司 Pharmaceutical preparation containing the active substance heroin and its utilization in a method for treating opiate addiction
CZ301230B6 (en) * 1999-05-21 2009-12-16 Lts Lohmann Therapie-Systeme Ag Pharmaceutical composition for continuous and controlled administration, transdermal therapeutic system, process for preparing thereof and use thereof for the preparation of medicaments intended for treating opiate addiction

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Publication number Publication date
AU1183092A (en) 1992-09-07

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