EP2723326A1 - Topische filmbildende zusammensetzung und ihre verwendung zur behandlung von mykosen - Google Patents

Topische filmbildende zusammensetzung und ihre verwendung zur behandlung von mykosen

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Publication number
EP2723326A1
EP2723326A1 EP12731594.3A EP12731594A EP2723326A1 EP 2723326 A1 EP2723326 A1 EP 2723326A1 EP 12731594 A EP12731594 A EP 12731594A EP 2723326 A1 EP2723326 A1 EP 2723326A1
Authority
EP
European Patent Office
Prior art keywords
acid
composition according
weight
composition
agents
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.)
Withdrawn
Application number
EP12731594.3A
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English (en)
French (fr)
Inventor
Claire BOUVIER
Nathalie DERAIN
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.)
Laboratoires Urgo SAS
Original Assignee
Laboratoires Urgo SAS
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Filing date
Publication date
Application filed by Laboratoires Urgo SAS filed Critical Laboratoires Urgo SAS
Publication of EP2723326A1 publication Critical patent/EP2723326A1/de
Withdrawn legal-status Critical Current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
    • 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
    • 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
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/20—Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • 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
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7015—Drug-containing film-forming compositions, e.g. spray-on
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics

Definitions

  • the subject of the present invention is a topical film-forming composition comprising at least one hydroxamic acid and at least one alpha hydroxylated acid, as well as its use for the treatment of dermatophytoses, more specifically fungal infections of the feet, and in particular for the treatment of symptoms related to dermatophytoses. , specifically athlete's foot symptoms.
  • Dermatophytosis are infections of the skin or integuments due to filamentous microscopic fungi: dermatophytes. They belong to 3 genera, Trichophyton, Microsporum and Epidermophyton. These fungi are keratinophilic, they have a predilection for the keratin of the stratum corneum of skin, hair, hair and nails in humans, skin, hair and claws in animals. They are responsible for superficial cutaneous infections of the skin and integuments but always respect the mucous membranes. Dermatophytes are always pathogenic, absent from the permanent or transient flora of the skin.
  • dermatophytoses Among the known dermatophytoses, mention may be made, for example, of ringworms (which more particularly reach the hair or the hair), the epidermophyties (they are attacks of the glabrous skin), the onyxis and dermatophyties.
  • Athlete's foot (Latin name tinea pedis) is a dermatophytosis, that is to say a chronic infection of the feet by microscopic fungi.
  • Athlete's foot is one of the most common skin diseases in the United States after acne, and can affect up to 15% of the population.
  • Trichophyton especially Trichophyton rubrum or Trichophyton mentagrophytes
  • Epidermophyton Epidermophyton
  • Microsporum yeast Candida albicans.
  • the infection can spread to all inter-toe spaces. It can also reach the top and bottom of the foot where we can see the development of red areas that itch heavily. An attack of the nails of the feet (thickened nails, brittle) and / or the sole of the foot (appearing thick, with skins which are detached) can also be observed.
  • an infection with bacteria can also occur secondarily.
  • athlete's foot is treated locally with compositions in the form of creams, sprays, liquids or powders comprising imidazole antifungal compounds such as clotrimazole or miconazole, zinc undecenoate, allylamines, such as terbinafme or tolnaflate.
  • imidazole antifungal compounds such as clotrimazole or miconazole, zinc undecenoate, allylamines, such as terbinafme or tolnaflate.
  • oral antifungals may be prescribed for systemic treatment alone or in addition to topical antifungal compositions. These oral treatments can treat inflammation without helping to heal areas of injured feet, affected by the infection.
  • the subject of the present invention is a topical, fungogenic composition making it possible to treat the dermatophytosis-related symptoms, more specifically the symptoms related to athlete's foot, and in particular the crevices, and to promote the cicatrization of the cutaneous lesions generated by this inflammation.
  • the present composition also makes it possible to prevent bacterial or fungal proliferation in the injured skin.
  • the subject of the invention is, according to a first aspect, a topical, film-forming composition comprising, in a pharmaceutically acceptable medium, at least one hydroxamic acid, its salts and / or complexes, and at least one alpha hydroxylated acid.
  • topical composition in the sense of the present application, a form of administration of a composition on a specific region of the body.
  • the topical composition may be a solution, a cream, an ointment, an ointment, a gel, a lotion or a varnish.
  • the film-forming composition according to the invention is preferably resistant to water, that is to say that the film that it forms when it is applied to the skin or integuments does not decompose in the presence of water. .
  • the invention also relates to the use of such a composition for the treatment of fungal infections of the feet and in particular for the treatment of symptoms related to athlete's foot.
  • the film-forming composition according to the invention not only makes it possible to treat the fungi responsible for fungal infections of the feet, but also effectively inhibits the bacterial overgrowth. level of the damaged skin, in particular by filling the crevices generated by these skin infections.
  • composition according to the invention comprises at least one hydroxamic acid, its salts and / or its complexes. These compounds are described in detail in document WO 2009/070736.
  • the hydroxamic acid is preferably an alkyl hydroxamic acid.
  • hydroxamic acid in particular the alkyl hydroxamic acid
  • the hydroxamic acid may be used in the compositions of the invention in a free (non-neutralized) form or in the form of a salt (neutralized).
  • the terms "hydroxamic acid” and “alkyl hydroxamic acid” therefore include, within the meaning of the present invention, the free forms, the salts or complexes of said acids, as well as their precursors, and the salts and complexes of these precursors.
  • the alkyl hydroxamic acids are compounds of formula (I):
  • R is a linear or branched, substituted or unsubstituted carbon chain comprising from two to twenty-two carbon atoms, which may be interrupted by one or more oxygen atoms, and may include saturated or unsaturated carbon bonds.
  • R groups may include, for example, alkyl, alkenyl, alkynyl, alkoxy, alkenoxy, alkynoxy and similar linear or branched groups which may be functionalized with substitution groups including hydroxy groups or other pharmaceutically functional groups. or cosmetically acceptable.
  • RI may be hydrogen or the R radical previously described.
  • the alkyl hydroxamic acid may therefore in particular comprise a linear or branched, saturated or unsaturated, substituted or unsubstituted carbon chain comprising from two to twenty-two carbon atoms, and preferably from 6 to 12 carbon atoms.
  • the carbon chains can comprise ethylenic unsaturations, and / or carry particular chemical groups, chosen according to the final properties desired for the alkyl hydroxamic acid.
  • the presence of hydroxy groups on the chain may allow a better compatibility of the compound with water.
  • the carbon chains may also include other pharmaceutically or cosmetically acceptable functional groups.
  • the alkyl hydroxamic acids can be synthesized from natural oils using lipase catalysis as well as other hydroxamic synthesis techniques known to those skilled in the art.
  • the alkyl hydroxamic acid corresponds to formula (I) in which R is a linear or branched, saturated or unsaturated, substituted or unsubstituted carbon chain comprising from two to twenty-two carbon atoms, and preferably from 6 to at 12 carbon atoms, and RI is hydrogen.
  • the alkyl hydroxamic acid is preferably selected from the group consisting, in a non-limiting manner, of hexanohydroxamic acid, caprylohydroxamic acid, caprohydroxamic acid, laurohydroxamic acid and mixtures thereof.
  • the alkyl hydroxamic acid is chosen from caprylohydroxamic acid (ie having a linear hydrocarbon chain comprising eight carbon atoms) and caprohydroxamic acid (ie having a linear hydrocarbon chain comprising ten atoms. of carbon).
  • the alkyl hydroxamic acid is caprylohydroxamic acid.
  • the precursors of the alkyl hydroxamic acid such as hydroxy acids in combination with, for example, hydroxylamine hydrochloride or similar compounds, which can react within the composition of the invention to form the alkyl hydroxamic acid, or salts and / or complexes thereof may be introduced into the composition according to the invention in place of the alkyl hydroxamic acid.
  • the hydroxamic acid is present in a content ranging from 0.01 to 10% by weight, preferably from 0.1 to 8%, and more preferably from 0.1 to 5% by weight. , relative to the total weight of the composition.
  • the hydroxamic acid is introduced into the composition according to the invention in the form of a premix with at least one alcohol.
  • Particularly preferred alcohols for forming a premix with hydroxamic acid are vicinal diols.
  • vicinal diol is used when the two hydroxyl groups are in the vicinal position, that is to say attached to adjacent carbon atoms.
  • a vicinal diol which can be used in the context of the present application, mention may be made, without limitation, of ethylene glycol (ethane-1,2-diol), propylene glycol (propane-1,2- diol), 1,2-pentanediol, 1,2-hexanediol, caprylyl glycol, 1,2-decanediol as well as glycerin derivatives such as glyceryl monoethers, for example ethylhexylglycerin, monolaurate, glyceryl, mono caproate, or glyceryl monocaprylate.
  • glyceryl monoethers for example ethylhexylglycerin, monolaurate, glyceryl, mono caproate, or glyceryl monocaprylate.
  • compositions according to the invention preferably comprise vicinal diols in a content ranging from 0.1 to 45% by weight, preferably from 0.5 to 20% by weight, relative to the total weight of the composition.
  • the hydroxamic acid is introduced into the composition according to the invention in the form of a premix with caprylyl glycol and glycerine.
  • Pre-mixtures of hydroxamic acid with caprylyl glycol and glycerin that may be suitable in the context of the present application are in particular the products sold by the company Inolex under the name Spectrastat.
  • the composition according to the invention also comprises at least one alpha hydroxylated acid.
  • ⁇ -Hydroxy acids or AHAs are carboxylic acids derived from fruit sugars or milk.
  • the most used ⁇ -hydroxy acids are glycolic acid and lactic acid because they have a particular ability to penetrate the skin and to allow the retention of hydration, as well as the initiation of collagen formation.
  • the hydroxylated acid alpha according to the invention may in particular be selected from the group consisting of lactic acid, glycolic acid, malic acid, citric acid, tartaric acid, and mixtures thereof.
  • the alpha hydroxylated acid introduced into the composition according to the invention is glycolic acid.
  • the hydroxylated alpha acid may be present in the composition in a content ranging from 0.01 to 10% by weight, preferably from 0.1 to 5% by weight, relative to the total weight of the composition.
  • composition according to the invention comprises a pharmaceutically acceptable medium comprising at least one organic solvent.
  • pharmaceutically acceptable medium is meant, within the meaning of the present application, a medium compatible with the skin.
  • the organic solvent may especially be chosen from:
  • liquid ketones such as methyl ethyl ketone, methyl isobutyl ketone, diisobutyl ketone, isophorone, cyclohexanone, acetone; alcohols, other than the vicinal diols described above, which are liquid at room temperature, such as ethanol, isopropanol, diacetone alcohol, 2-butoxyethanol or cyclohexanol;
  • propylene glycol ethers which are liquid at ambient temperature, such as propylene glycol monomethyl ether, propylene glycol monomethyl ether acetate or dipropylene glycol mono-butyl ether;
  • cyclic ethers such as ⁇ -butyrolactone
  • short chain esters such as ethyl acetate, butyl acetate, methyl acetate, propyl acetate, isopropyl acetate, isopentyl acetate, methoxypropyl acetate, butyl lactate; ethers such as diethyl ether, dimethyl ether or dichlorodiethyl ether;
  • alkanes that are liquid at room temperature such as decane, heptane, dodecane or cyclohexane;
  • alkyl sulfoxides such as dimethylsulfoxide
  • aldehydes that are liquid at room temperature, such as benzaldehyde or acetaldehyde; ethyl 3-ethoxypropionate;
  • carbonates such as propylene carbonate, dimethyl carbonate, acetals such as methylal;
  • the organic solvent is chosen from:
  • alcohols other than the vicinal diols described above, which are liquid at room temperature, such as ethanol, isopropanol, diacetone alcohol, 2-butoxyethanol, cyclohexanol and, preferably, ethanol,
  • short-chain esters having from 3 to 8 carbon atoms in total
  • short-chain esters such as ethyl acetate, butyl acetate, methyl acetate, propyl acetate, isopropyl acetate isopentyl acetate, methoxypropyl acetate, butyl lactate, and preferably ethyl acetate
  • the organic solvent used in the compositions according to the invention consists of a mixture of ethanol and ethyl acetate.
  • the organic solvent may represent from 40 to 98% by weight, preferably from 60 to 95% by weight, and more preferably from 70 to 90% by weight, relative to the total weight of the composition.
  • the composition advantageously comprises at least one film-forming polymer.
  • film-forming polymer means a polymer capable of forming on its own or in the presence of an auxiliary film-forming agent, a continuous and adherent film on a support, in particular on the skin.
  • the film-forming polymers used in the composition according to the invention are not soluble in water.
  • the film-forming polymer may be chosen in particular from cellulose polymers such as nitrocellulose, cellulose acetate, cellulose acetate butyrate, cellulose acetate propionate, ethyl cellulose, or even polyurethanes, acrylic polymers, vinyl polymers, polyvinyl butyrals, alkyd resins, resins derived from aldehyde condensation products such as arylsulfonamide formaldehyde resins such as toluene sulfonamide formaldehyde resin, epoxy aryl-sulfonamide resins or ethyl tosylamide resins, the copolymer of PolyVinyl Methyl Ether and Maleic Anhydride (PVM / MA).
  • cellulose polymers such as nitrocellulose, cellulose acetate, cellulose acetate butyrate, cellulose acetate propionate, ethyl cellulose, or even polyurethanes
  • acrylic polymers vinyl polymers, polyvinyl
  • RS 1/8 nitrocellulose can be used in particular; RS [1/4] sec. ; [1/2] sec. ; RS 5 sec. ; RS 15 sec. ; RS 35 sec. ; RS 75 sec; RS 150 sec; AS [1/4] sec. ; AS [1/2] sec. ; SS [1/4] sec. ; SS [1/2] sec.
  • the film-forming polymer used in the composition is nitrocellulose, in particular sold by NOBEL under the name DHL 120/170 IPA.
  • the film-forming polymer may be present in the composition according to the invention in a dry matter content ranging from 0.1% to 20% by weight, preferably ranging from 1% to 15% by weight, relative to the total weight of the composition.
  • Auxiliary filming agent is a dry matter content ranging from 0.1% to 20% by weight, preferably ranging from 1% to 15% by weight, relative to the total weight of the composition.
  • an auxiliary film-forming agent may advantageously be added.
  • the auxiliary film-forming agent is, of course, different from the organic solvent present in the pharmaceutically acceptable medium.
  • auxiliary film-forming agent may be chosen from all the compounds known to those skilled in the art, as being capable of fulfilling the desired function, and in particular be chosen from plasticizers and coalescers of the polymer (s). film (s).
  • composition may further comprise at least one plasticizer and / or a coalescing agent.
  • plasticizers and coalescence agents such as:
  • fatty alcohols such as octyldodecanol, 2-butyloctanol, 2-hexyl decanol, 2-undecylpentadecanol and oleyl alcohol;
  • glycols and their derivatives such as glycerol, diethylene glycol ethyl ether, diethylene glycol methyl ether, diethylene glycol butyl ether or else diethylene glycol hexyl ether, ethylene glycol ethyl ether, ethylene glycol butyl ether, ethylene glycol hexyl ether;
  • fatty acids such as oleic acid, linoleic acid, linolenic acid;
  • glycol esters such as triacetin (or glyceryl triacetate);
  • propylene glycol derivatives and in particular propylene glycol phenyl ether, propylene glycol diacetate, dipropylene glycol ethyl ether, tripropylene glycol methyl ether, propylene glycol butyl ether;
  • esters of acids especially carboxylic acids, such as citrates, phthalates, adipates, carbonates, tartrates, phosphates, sebacates and in particular the monocarboxylic acid esters such as isononyl isononanoate, oleyl erucate or octyl-2-dodecyl neopentanoate;
  • oxyethylenated derivatives such as oxyethylenated oils, especially vegetable oils, such as sesame oil, castor oil, almond oil, canola oil, hazelnut oil, Pistachio oil, linseed oil, borage oil, hemp oil, jojoba oil, sunflower oil, wheat germ oil, corn oil and / or corn germ, peanut oil, avocado oil, safflower oil, rapeseed oil, olive oil, argan oil, sunflower oil , grape seed oil, soybean oil, walnut oil, pumpkin seed oil, palm oil, coconut oil, and mixtures thereof.
  • the oil can also be a derivative of one of the vegetable oils mentioned above. It may be hydrogenated oil or not, peroxidized or not.
  • the auxiliary film-forming agent is chosen from oxyethylenated derivatives, such as oxyethylenated oils, especially vegetable oils, such as castor oil.
  • the auxiliary filming agent is castor oil.
  • auxiliary film-forming agent may range from 0.01% to 20% and in particular from 0.5% to 15% by weight relative to the total weight of the composition. additives
  • composition according to the invention may comprise one or more pharmaceutically acceptable additives, for example perfumes, flavors, dyes, pigments, matifying agents, rheological agents, preservatives, vitamins, essential oils and agents.
  • active agents chosen in particular from anti-bacterial agents, antiseptics, anti-virals, antifungal agents, anti-pain agents, anti-inflammatory agents, agents promoting healing, moisturizing agents, depigmenting agents, keratolytic agents, restructuring actives, anesthetics and sunscreens.
  • active agents that can be introduced into the composition according to the invention can be chosen from:
  • anti-bacterials such as Polymyxin B, penicillins (Amoxycillin), clavulanic acid, tetracyclines, Minocycline, chlorotetracycline, aminoglycosides, Amikacin, Gentamicin, Neomycin, silver and its salts ( Sulfadiazine argentic), probiotics;
  • antiseptics such as sodium mercurothiolate, eosin, chlorhexidine, phenylmercury borate, hydrogen peroxide, Dakin liquor, triclosan, biguanide, hexamidine, thymol, Lugol, Povidone iodine , Merbromine, Benzalkonium and Benzethonium Chloride, ethanol, isopropanol;
  • anti-virals such as Aciclovir, Famciclovir, Ritonavir;
  • antifungals such as polyenes, Nystatin, Amphotericin B, Natamycin, imidazoles (Miconazole, Ketoconazole, Clotrimazole, Econazole, Bifonazole, Butoconazole, Fenticonazole, Isoconazole, Oxiconazole, Sertaconazole, Sulconazole, Thiabendazole, Tioconazole), triazoles (Fluconazole, Itraconazole, Ravuconazole, Posaconazole, Voriconazole), allylamines, Terbinafine, Amorolfme, Naftifme, Butenafine;
  • Flucytosine antioxidants
  • Griseofulvin Caspofungin
  • Micafungin anti-pain agents
  • anti-pain agents such as Paracetamol, Codeine, Dextropropoxyphene, Tramadol, Morphine and its derivatives, Corticosteroids and derivatives
  • anti-inflammatories such as Glucocorticoids, Nonsteroidal Anti-inflammatories, Aspirin, Ibuprofen, Ketoprofen, Flurbiprofen, Diclofenac, Aceclofenac, Ketorolac, Meloxicam, Piroxicam, Tenoxicam, Naproxen , Indomethacin, Naproxcinod, Nimesulide, Celecoxib, Etoricoxib, Parecoxib, Rofecoxib, Valdecoxib, Phenylbutazone, Niflumic acid, Mefenamic acid;
  • healing promoting agents such as retinol, vitamin A, vitamin E, N-acetyl-hydroxyproline, extracts of Centella Asiatica, papain, silicones, essential oils of thyme, niaouli, rosemary and sage, hyaluronic acid, synthetic polysulfated oligosaccharides having 1 to 4 units such as the potassium salt of octasulfated sucrose, the silver salt of octasulfated sucrose or sucralfate, Allantoin; moisturizing agents such as hyaluronic acid, urea, glycerol, fatty acids, modulators of aquaporins, vegetable oils, chitosan, certain sugars including sorbitol, butters and waxes;
  • depigmenting agents such as kojic acid (Kojic Acid SL® - Quimasso (Sino Lion)), Arbutin (Olevatin® - Quimasso (Sino Lion)), the mixture of palmitoylpropyl of sodium and white water lily extract ( Sepicalm® - Seppic), undecylenoyl phenylalanine (Sepiwhite® - Seppic), licorice extract obtained by fermentation of Aspergillus and ethoxydiglycol (Gatuline Whitening® - Gattefossé), octadecenedioic acid (ODA White® - Sederma), alpha-arbutin (Alpha-arbutin®, SACI-CFPA (Pentapharm)), the aqueous extract of Arctophylos Uva leaves
  • Ursi (Melfade-J® - SACI-CFPA (Pentapharm)), Gigawhite® complex plant mix (SACI-CFPA (Alpaflor)), diacetyl boldine (Lumiskin® - Sederma), mandarin extract from Japan (Melaslow) ® - Sederma), the lemon extract mixture enriched with citric acid and cucumber extract (Uninontan®U-34 - Unipex), the mixture of Rumex occidentalis extract and vitamin C (Tyrostat® 11 - Unipex ), oligopeptides (Melanostatin 5® - Unipex), kojic dipalmitate (KAD-15® - Quimasso (Sino Lion)), LCW's Vegewhite® natural origin complex, wheat germ extracts (Clariskin® II - Silab), ethyldiamine triacetate (EDTA); keratolytic agents such as salicylic acid, zinc salicylate, ascorbic acid, alpha
  • restructuring assets for example rescutants of integuments
  • integuments such as silica derivatives, vitamin E, chamomile, calcium, horsetail extract, silk lipester
  • anesthetics such as benzocaine, lidocaine, dibucaine, pramoxine hydrochloride, bupivacaine, mepivacaine, prilocaine, etidocaine;
  • sunscreens such as chemical filters (Oxybenzone, Sulisobenzone, Dioxybenzone, Tinosorb S®, Avobenzone, 2-ethoxyethyl p-methoxycinnamate,
  • the subject of the invention is the composition as defined above for its use in a method for treating dermatophytoses, more specifically foot fungi, and in particular for the treatment of symptoms related to dermatophytosis, more specifically athlete's foot-related symptoms.
  • the subject of the invention is also, according to another embodiment, the composition as defined above for its use in a wound healing method generated by dermatophytoses, and in particular by the athlete's foot.
  • the composition according to the invention also makes it possible to avoid bacterial and fungal proliferations in the skin condition.
  • a topical film-forming composition according to the invention was prepared having the following composition:
  • the nitrocellulose is then dispersed in the mixture with stirring.
  • a placebo topical film-forming composition having the following composition was prepared:
  • Nitrocellulose DHL 120/170 IPA marketed by the manufacturer
  • Castor Oil (RicinusCommunis (Castor) Seed Oil),
  • the nitrocellulose is then dispersed in the mixture with stirring.
  • the film-forming composition according to the invention was contacted with a known inoculum of dermatophyte Trichophyton mentagrophytes ATCC9533 and the fungal activity of the composition according to the invention was quantitatively evaluated after 7 days of contact according to standard NF EN 1275:
  • Antiseptics and chemical disinfectants quantitative suspension test for the evaluation of the fungicidal and basic yeasticidal activity of antiseptics and chemical disinfectants - Test Method and Prescription (Phase 1) - April 2006. i.
  • the culture media and the diluent used are as follows:
  • a red vial containing Sabouraud agar medium is inoculated with the Trichophyton mentagrophytes microorganism and incubated at 30 ° C ⁇ 1 ° C until spores (9 to 11 days) are obtained.
  • the fungal suspension is prepared in Sabouraud broth and adjusted to approximately 10 7 CFU (Colony Forming Units) / ml. This inoculum is noted N. The exact titre of the inoculum is determined by counting on agar plate by depositing 2 ⁇ 1 ml of dilutions 10 "5 and 10 " 6 made in tryptone salt solution and adding 15 to 20 ml of agar Sabouraud supercooled and then incubating for 48 to 72 hours at 30 ° C. iii. The tests were carried out according to the following method:
  • composition according to the invention 0
  • the filmogenic topical composition thus obtained thus makes it possible to avoid fungal growth.
  • the composition according to the invention allows the treatment of mycosis of the feet and in particular for the treatment of symptoms related to athlete's foot.
  • a topical formulation having the following composition was prepared:
  • composition according to the invention was artificially contaminated by means of inoculum of microorganisms at the origin of mycosis of the feet and in particular of the symptoms related to athlete's foot.
  • the inoculated preparations were then held at 22.5 ⁇ 2.5 ° C and protected from light, and samples of the medium were taken at given time intervals. The organisms were counted in the samples collected.
  • the tests are carried out in simulation of use, either after reinoculations at times T2 days, T7 days and T10 days.
  • the culture media used are as follows:
  • the surface of an agar is seeded with the recently obtained parent culture of each of the specified microorganisms.
  • the bacterial cultures are incubated at a temperature of 32.5 ° C ⁇ 2.5 ° C for 18/24 h, the culture of Candida albicans at a temperature of 22.5 ° C ⁇ 2.5 ° C for 48 h.
  • Microbial suspensions are prepared and adjusted to titrate 10 8 CFU (Colony Fromant Unit) per milliliter.
  • the exact titre of the inoculum is determined by agar plate count.
  • the agar plate count method at the dilution of product 10-2 was validated for the microorganisms tested: Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans and Trichophyton rubrum. iii. The tests were carried out according to the following method:
  • a series of containers containing the composition according to the invention was inoculated with a suspension of one of the test microorganisms in order to obtain an inoculum of 10 5 to 10 6 microorganisms per gram of preparation.
  • the containers are mixed by manual and mechanical agitation (vortex type).
  • the seeded product is then kept at a temperature of 22.5 ° C ⁇ 2.5 ° C protected from light.
  • the number of viable microorganisms is determined for each time by counting on agar plates according to the previously validated method.
  • test microorganism After each enumeration, the test microorganism is reinoculated into the product at times 2j, 7j and 10d. • At the end of the tests, for each microorganism, the logarithmic reduction in the number of viable microorganisms relative to the value obtained for the inoculum is calculated. iv. Results:
  • compositions according to the invention thus make it possible not only to treat the fungi causing foot fungus, but also to effectively inhibit the bacterial proliferation associated with these diseases.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Communicable Diseases (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Oncology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP12731594.3A 2011-06-22 2012-06-21 Topische filmbildende zusammensetzung und ihre verwendung zur behandlung von mykosen Withdrawn EP2723326A1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR1155492A FR2976806B1 (fr) 2011-06-22 2011-06-22 Composition topique filmogene et son utilisation pour le traitement des mycoses
PCT/FR2012/051420 WO2012175881A1 (fr) 2011-06-22 2012-06-21 Composition topique filmogène et son utilisation pour le traitement des mycoses

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Publication Number Publication Date
EP2723326A1 true EP2723326A1 (de) 2014-04-30

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Country Link
US (1) US20140128468A1 (de)
EP (1) EP2723326A1 (de)
FR (1) FR2976806B1 (de)
WO (1) WO2012175881A1 (de)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR3019552B1 (fr) * 2014-04-03 2016-04-01 Urgo Lab Composition filmogene
EP3478234A4 (de) * 2016-06-29 2020-02-26 IVIEW Therapeutics, Inc. Neuartige zusammensetzungen zur formung von dünnschichten mit schneller abscheidung als wirksame wundpflegebehandlung

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5861142A (en) * 1996-03-25 1999-01-19 Schick; Mary Pichler Method for promoting hair, nail, and skin keratinization
US6231875B1 (en) * 1998-03-31 2001-05-15 Johnson & Johnson Consumer Companies, Inc. Acidified composition for topical treatment of nail and skin conditions
SG166105A1 (en) * 2005-09-29 2010-11-29 Novartis Ag Antifungal composition
PL2224973T3 (pl) * 2007-11-29 2016-11-30 Środki konserwujące do kosmetyków, środków do pielęgnacji ciała i kompozycji farmaceutycznych

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ANONYMOUS: "Face Masks | Types | Homemade Recipes", 15 May 2015 (2015-05-15), XP055189478, Retrieved from the Internet <URL:http://www.natural-skin-care-info.com/face_masks.html> [retrieved on 20150515] *
ANONYMOUS: "Xanthan - Datenbank Zusatzstoffe", 15 May 2015 (2015-05-15), XP055189480, Retrieved from the Internet <URL:http://www.zusatzstoffe-online.de/zusatzstoffe/153.e415_xanthan.html> [retrieved on 20150515] *

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Publication number Publication date
US20140128468A1 (en) 2014-05-08
WO2012175881A1 (fr) 2012-12-27
FR2976806B1 (fr) 2013-06-28
FR2976806A1 (fr) 2012-12-28

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