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WO2008145149A1 - Antiphlogistic and analgesic composition for topical use in a region of an animal locomotive system - Google Patents

Antiphlogistic and analgesic composition for topical use in a region of an animal locomotive system Download PDF

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Publication number
WO2008145149A1
WO2008145149A1 PCT/EP2007/004713 EP2007004713W WO2008145149A1 WO 2008145149 A1 WO2008145149 A1 WO 2008145149A1 EP 2007004713 W EP2007004713 W EP 2007004713W WO 2008145149 A1 WO2008145149 A1 WO 2008145149A1
Authority
WO
WIPO (PCT)
Prior art keywords
hydrogel
composition
antiphlogistic
arnica
active ingredients
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/EP2007/004713
Other languages
French (fr)
Inventor
Vincenzo Massimo Lombardo
Alberto Antonio Molinari
Ruggero Ferraiolo
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
Priority to BRPI0721696-3A priority Critical patent/BRPI0721696A2/en
Priority to EA200970667A priority patent/EA015702B1/en
Priority to PCT/EP2007/004713 priority patent/WO2008145149A1/en
Priority to JP2010509684A priority patent/JP2010528065A/en
Publication of WO2008145149A1 publication Critical patent/WO2008145149A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/728—Hyaluronic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • 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
    • A61K9/0017—Non-human animal skin, e.g. pour-on, spot-on
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • the present invention refers to an antiphlogistic and analgesic composition for use on the epidermis site where pains are felt from muscles, articulations, tendons and ligaments caused by pathologies, contusions and trauma.
  • the prior art comprises a number of compositions in the form of ointment, cream, spray or foam which are able to assuage the above specified pains and treat their cause in a notable or little extent.
  • the commercial products are cited that are sold under the names of Voltaren ®, Algesal ®, Lasonil ®, Artrosilene ® wherein the active ingredients are, respectively, diclofenac diethyl ammonium, diethyl amine salicylate , ketoprofene, lysine salt ketoprofene whereas there is a number of other products used to the same purposes that employ other active ingredients comprised in the pharmacopeia relevant to said purposes.
  • JP 11 279065 discloses an anti-inflammatory product in the form of topical solution composed by two water soluble anti-inflammatory agents, one of the steroidal type and the other of non-steroidal type, and by hyaluronic acid.
  • the efficacy of the analgesic and anti-inflammatory effect of the known compositions is affected by the fact that such compositions comprise in most cases an active ingredient only which is not well vehiculated into the suffering body region. Consequently, the efficacy of said compositions may be of short time and not so extended in the concerned region.
  • the known compositions may cause undesired effects due to light or notable hyperaesthesia against one or more components and to allergic reactions .
  • the invented compositions obviates the above mentioned limitations and drawbacks and offers advantages that will be described fartheron.
  • the invented composition comprises as active ingredients a salt of hyaluronic acid, an arnica extract and a non steroidal anti-inflammatory agent (FANS - as for instance methyl salicylate, diclofenac, lysine salt ketoprofene) soluble in a gel and, as vehicle of the active ingredients, hydrogel of the type used in medicine for applying ultrasounds and electric transmissions, type of gel which proved to give the compositions the best physical properties and that will be referred to as - hydrogel - in the following.
  • FANS - non steroidal anti-inflammatory agent
  • the hyaluronic acid as anti-inflammatory and chemotactic agent is known for a long time and is generally and successfully used into injectable solutions for treating osteoarthrosis, gonarthrosis, wounds and burns, in the beauty surgery and culture and also as a component for ophthalmic use.
  • the hyarulonic acid is preferably used as sodium hyaluronate, dissolved in just necessary purified water before preparing the composition.
  • Such an efficacy is substantially due to the anti-inflammatory and chemotactic properties as well as to the notable hydrophilia of the hyaluronic acid.
  • the latter makes pores of the basal membrane dilate and, supported by the high vehiculation favoured by the hydrogel, causes itself and the other two antiphlogistic and analgesic components to rapidly penetrate into the suffering region.
  • undesirable effects and allergic reactions of this composition have not been recorded in case of long-term use.
  • any hydrogel-soluble non steroidal anti-inflammatory agent from 2% to 10%, - hydrogel from 70% to 95%,
  • non steroidal anti-inflammatory agents As it is known, there is a number of non steroidal anti-inflammatory agents and the inventors proved that each of them, provided is soluble in hydrogel, may be used in this compositions in a proportion from 2% to 10% in order to provide the composition with the desired efficacy. It has been proved that the most afficacious anti-inflammatory agent in the invented composition is methyl salicylate.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Dermatology (AREA)
  • Microbiology (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Medical Informatics (AREA)
  • Biochemistry (AREA)
  • Mycology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The antiphlogistic and analgesic composition for topical use consists by weight of 0,01% - 3 % hyaluronic acid, 0.5 % - 7% arnica glycolic extract, 2% - 10% of any hydrogel-soluble non steroidal anti-inflammatory agent and 70% - 95% hydrogel.

Description

ANTIPHLOGISTIC AND ANALGESIC COMPOSITION FOR TOPICAL USE ESf A REGION OF AN ANIMAL LOCOMOTIVE SYSTEM.
BACKGROUND OF THE INVENTION The present invention refers to an antiphlogistic and analgesic composition for use on the epidermis site where pains are felt from muscles, articulations, tendons and ligaments caused by pathologies, contusions and trauma.
DESCRIPTION OF THE RELATED ART The prior art comprises a number of compositions in the form of ointment, cream, spray or foam which are able to assuage the above specified pains and treat their cause in a notable or little extent. As examples, the commercial products are cited that are sold under the names of Voltaren ®, Algesal ®, Lasonil ®, Artrosilene ® wherein the active ingredients are, respectively, diclofenac diethyl ammonium, diethyl amine salicylate , ketoprofene, lysine salt ketoprofene whereas there is a number of other products used to the same purposes that employ other active ingredients comprised in the pharmacopeia relevant to said purposes. Also document JP 11 279065 is known that discloses an anti-inflammatory product in the form of topical solution composed by two water soluble anti-inflammatory agents, one of the steroidal type and the other of non-steroidal type, and by hyaluronic acid. The efficacy of the analgesic and anti-inflammatory effect of the known compositions is affected by the fact that such compositions comprise in most cases an active ingredient only which is not well vehiculated into the suffering body region. Consequently, the efficacy of said compositions may be of short time and not so extended in the concerned region. Moreover, the known compositions may cause undesired effects due to light or notable hyperaesthesia against one or more components and to allergic reactions .
SUMMARY OF THE INVENTION
The invented compositions obviates the above mentioned limitations and drawbacks and offers advantages that will be described fartheron. The invented composition comprises as active ingredients a salt of hyaluronic acid, an arnica extract and a non steroidal anti-inflammatory agent (FANS - as for instance methyl salicylate, diclofenac, lysine salt ketoprofene) soluble in a gel and, as vehicle of the active ingredients, hydrogel of the type used in medicine for applying ultrasounds and electric transmissions, type of gel which proved to give the compositions the best physical properties and that will be referred to as - hydrogel - in the following.
The hyaluronic acid as anti-inflammatory and chemotactic agent is known for a long time and is generally and successfully used into injectable solutions for treating osteoarthrosis, gonarthrosis, wounds and burns, in the beauty surgery and culture and also as a component for ophthalmic use. In the invented composition the hyarulonic acid is preferably used as sodium hyaluronate, dissolved in just necessary purified water before preparing the composition.
The efficacy is known for a long time of : arnica in the treatment of consequences of trauma and of symptoms similar with "post-trauma"; FANS in the treatment of pains and as antiphlogistic agent ; hydrogel as vehicle of medicaments applied to the epidermis.
The combination in the invented composition of said three active ingredients and the presence of a hydrogel, all the four in the proposed proportions, leads to a fluid and rubbable product which is absorbed rapidly by the epidermis and is of high efficacy in assuaging pains of articular and osteomuscular origin, in the reduction of possible inflammation and in the absorption of possible serous or blood extravasation caused by trauma or contusion.
Such an efficacy is substantially due to the anti-inflammatory and chemotactic properties as well as to the notable hydrophilia of the hyaluronic acid. The latter makes pores of the basal membrane dilate and, supported by the high vehiculation favoured by the hydrogel, causes itself and the other two antiphlogistic and analgesic components to rapidly penetrate into the suffering region. Moreover, undesirable effects and allergic reactions of this composition have not been recorded in case of long-term use.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
According to first formulae of this composition that proved to be of considerable efficacy through tests carried out on many persons, a hundred grams of the composition comprise by weight :
- sodium hyaluronate from 0.01% to 3.00 %,
- arnica glycolic extract from 0.5% to 7.0%,
- any hydrogel-soluble non steroidal anti-inflammatory agent from 2% to 10%, - hydrogel from 70% to 95%,
- purified water 0.2 %,
As it is known, there is a number of non steroidal anti-inflammatory agents and the inventors proved that each of them, provided is soluble in hydrogel, may be used in this compositions in a proportion from 2% to 10% in order to provide the composition with the desired efficacy. It has been proved that the most afficacious anti-inflammatory agent in the invented composition is methyl salicylate.
According to a formula of this composition that proved to be the most efficacious through tests carried out on a great number of persons and in a number of percentage alternatives for the four components, the following formula in weight reaches the desired purposes : - sodium hyaluronate about 0.2 %,
- purified water about 0.2 %,
- arnica glycolic extract about 2 %,
- methyl salicylate about 5%, - hydrogel about 92.6 %.
It is realized that the percentages shown in the above formula may be varies slightly without departing from the claimed composition.

Claims

1. Antiphlogistic and analgesic composition for use in a region of an animal locomotive system comprising as active ingredients a non steroidal anti-inflammatory agent and hyaluronic acid and arnica mixed in a product adapted to vehiculate the active ingredients characterized in that the composition is a mixture of a salt of hyaluronic acid, an arnica glycolic extract and a hydrogel-soluble non steroidal antiinflammatory agent and hydrogel as vehicle of the active ingredients.
2. Composition according to claim 1 characterized in that it comprises by weight
- sodium hyaluronate from 0.01 % to 3.0 %, - arnica glycolic extract from 0.5 % to 7.0 %,
- any hydrogel-soluble non steroidal anti-inflammatory agent from 2% to 10%, - hydrogel from 70% to 95%,
- purified water 0.2%.
3. Composition according to claims 1 and 2 characterized in that the hydrogel-soluble non steroidal anti- inflammatory agent is methyl salicylate.
4. Antiphlogistic and analgesic composition for use in a region of an animal locomotive system comprising as active ingredients a non steroidal anti-inflammatory agent and hyaluronic acid and arnica mixed in a product adapted to vehiculate the active ingredients characterized in that the composition consists by weight of - sodium hyaluronate 0.2%,
- purified water 0.2%,
- arnica glycolic extract 2%,
- methyl salicylate 5%, - hydrogel 92,6%. * * *
PCT/EP2007/004713 2007-05-28 2007-05-28 Antiphlogistic and analgesic composition for topical use in a region of an animal locomotive system Ceased WO2008145149A1 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
BRPI0721696-3A BRPI0721696A2 (en) 2007-05-28 2007-05-28 antiflogistic and analgesic composition for topical use in a region of an animal locomotor system
EA200970667A EA015702B1 (en) 2007-05-28 2007-05-28 Antiphlogistic and analgesic composition for topical use in a region of an animal locomotive system
PCT/EP2007/004713 WO2008145149A1 (en) 2007-05-28 2007-05-28 Antiphlogistic and analgesic composition for topical use in a region of an animal locomotive system
JP2010509684A JP2010528065A (en) 2007-05-28 2007-05-28 Anti-inflammatory and analgesic compositions for topical use in the field of animal motor systems

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP2007/004713 WO2008145149A1 (en) 2007-05-28 2007-05-28 Antiphlogistic and analgesic composition for topical use in a region of an animal locomotive system

Publications (1)

Publication Number Publication Date
WO2008145149A1 true WO2008145149A1 (en) 2008-12-04

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2007/004713 Ceased WO2008145149A1 (en) 2007-05-28 2007-05-28 Antiphlogistic and analgesic composition for topical use in a region of an animal locomotive system

Country Status (4)

Country Link
JP (1) JP2010528065A (en)
BR (1) BRPI0721696A2 (en)
EA (1) EA015702B1 (en)
WO (1) WO2008145149A1 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119656137A (en) * 2024-12-20 2025-03-21 沈阳药科大学 Compound arnica-diclofenac sodium gel emplastrum and preparation method and application thereof

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0307277A1 (en) * 1987-09-09 1989-03-15 Marie-Christine Seguin Product on a silanol basis for the care of the superficial lymphatic vessels
WO1991000083A1 (en) * 1989-06-23 1991-01-10 Revlon, Inc. Skin care preparation
EP0695187A1 (en) * 1993-04-16 1996-02-07 Hyal Pharmaceutical Corporation Compositions for inhibition, control and regression of angiogenesis, containing hyaluronic acid and nsaid
WO2000045796A1 (en) * 1997-04-22 2000-08-10 Archer Heidi K Analgesic and antiphlogistic compositions and therapeutic wrap for topical delivery
US20050147570A1 (en) * 2004-01-06 2005-07-07 Nordsiek Michael T. Methods of administering diclofenac compositions for treating photodamaged skin, rosacea and/or acne
EP1710257A1 (en) * 2004-01-07 2006-10-11 Seikagaku Corporation Hyaluronic acid derivative and drug containing the same

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0617300B2 (en) * 1986-09-22 1994-03-09 サンスタ−株式会社 Composition for treating periodontal disease
JP2788340B2 (en) * 1989-12-21 1998-08-20 株式会社ニッショー Inflammation treatment
CA2061566C (en) * 1992-02-20 2002-07-09 Rudolf E. Falk Treatment of disease employing hyaluronic acid and nsaids
CA2154103C (en) * 1995-07-18 1998-02-24 Samuel Simon Asculai Treatment of mucous membrane disease, trauma or condition and for the relief of pain
JPH11279065A (en) * 1998-03-25 1999-10-12 Shiseido Co Ltd Inflammation treating agent for local administration
JP2005126341A (en) * 2003-10-22 2005-05-19 Lion Corp Anti-inflammatory analgesic patch for external use
US20050196450A1 (en) * 2004-03-04 2005-09-08 Elka Touitou Method and composition for burned skin
ITMI20061132A1 (en) * 2006-06-13 2007-12-14 Sinclair Pharmaceuticals Ltd TOPIC ANTIMICROBIAL COMPOSITIONS INCLUDING LATTOFERRINA, HYALURONIC ACID OR ITS SALTS AND VEGETABLE EXTRACTS

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0307277A1 (en) * 1987-09-09 1989-03-15 Marie-Christine Seguin Product on a silanol basis for the care of the superficial lymphatic vessels
WO1991000083A1 (en) * 1989-06-23 1991-01-10 Revlon, Inc. Skin care preparation
EP0695187A1 (en) * 1993-04-16 1996-02-07 Hyal Pharmaceutical Corporation Compositions for inhibition, control and regression of angiogenesis, containing hyaluronic acid and nsaid
WO2000045796A1 (en) * 1997-04-22 2000-08-10 Archer Heidi K Analgesic and antiphlogistic compositions and therapeutic wrap for topical delivery
US20050147570A1 (en) * 2004-01-06 2005-07-07 Nordsiek Michael T. Methods of administering diclofenac compositions for treating photodamaged skin, rosacea and/or acne
EP1710257A1 (en) * 2004-01-07 2006-10-11 Seikagaku Corporation Hyaluronic acid derivative and drug containing the same

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119656137A (en) * 2024-12-20 2025-03-21 沈阳药科大学 Compound arnica-diclofenac sodium gel emplastrum and preparation method and application thereof

Also Published As

Publication number Publication date
JP2010528065A (en) 2010-08-19
EA015702B1 (en) 2011-10-31
BRPI0721696A2 (en) 2011-06-21
EA200970667A1 (en) 2010-06-30

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