WO2003061707A1 - Dermatological water-resistant compositions with sun screens and method for production and use of such compositions - Google Patents

Dermatological water-resistant compositions with sun screens and method for production and use of such compositions Download PDF

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Publication number
WO2003061707A1
WO2003061707A1 PCT/FR2003/000158 FR0300158W WO03061707A1 WO 2003061707 A1 WO2003061707 A1 WO 2003061707A1 FR 0300158 W FR0300158 W FR 0300158W WO 03061707 A1 WO03061707 A1 WO 03061707A1
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Prior art keywords
composition according
dermatological composition
water
skin
derivative
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PCT/FR2003/000158
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French (fr)
Inventor
Catherine Lacaze
Sylvie Cuart
Laurent Terrassin
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Ellipse Pharmaceuticals
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Priority to EP03709889A priority Critical patent/EP1467766A1/en
Publication of WO2003061707A1 publication Critical patent/WO2003061707A1/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/06—Emulsions
    • 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
    • A61K47/02—Inorganic compounds
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/27—Zinc; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/29—Titanium; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations

Definitions

  • the present invention relates to water-resistant dermatological compositions comprising sun filters.
  • the invention also covers the manufacturing process and the uses of these compositions. Dermatological conditions are treated in particular by means of two families of active principles which are: antifungals, such as the imidazole family, for the treatment of skin mycosis, and antiviral drugs, such as aciclovir, for the treatment of 'labial and cutaneous herpes.
  • antifungals such as the imidazole family
  • antiviral drugs such as aciclovir
  • compositions are known, in particular that called “Pevaryl” which have antifungal activities on various strains such as dermatophytes, candidas and certain yeasts, Pityrosporum orbiculare and ovale, molds and certain other fungi.
  • Pevaryl which have antifungal activities on various strains such as dermatophytes, candidas and certain yeasts, Pityrosporum orbiculare and ovale, molds and certain other fungi.
  • Such a product includes econazole nitrate, generally at 1%, which is an imidazole derivative endowed with fungicidal activity.
  • a dosage form containing this active ingredient is a cream which allows application to the skin.
  • compositions are also commercially available for treating herpes, such as the cream sold under the name Zovirax, based on aciclovir.
  • Aciclovir is a guanine analogue which, to be active, must be phosphorylated to aciclovir tri-phosphate by an enzyme, thymidine kinase, found in herpes viruses. The dosage is generally 5%.
  • This cream is also an oil-in-water emulsion, that is to say that the formulation has no resistance to water.
  • sunscreens which would prevent the appearance of the skin lesions mentioned above.
  • the object of the invention is to provide a composition which overcomes the drawbacks of the products known from the prior art.
  • the composition by presenting an increased resistance to water, avoids dilution in perspiration or in the water within which the patients evolve and guarantees a better effectiveness by maintaining the active principle at its place of application.
  • compositions according to the invention contain an antifungal or an antiviral, in particular econazole nitrate or aciclovir, and sun filters. They have excellent water resistance and strong sun protection.
  • formulations are emulsions of the water in oil type, that is to say, a predominant oily phase.
  • compositions are numerous and in particular that of allowing the production of an occlusive film favorable to the penetration of the active ingredients through the skin, which reinforces its activity.
  • the filters used can be chemical and / or physical.
  • the compositions are now described in detail by the example through specific formulations.
  • Each composition is an emulsion of water in oil in order to present a so-called waterproof character.
  • the water / oil ratio must remain in a range between 37.5 and 60%.
  • the filters used for the following description are of different types.
  • the sun filters are included in the present invention chemical filters and physical filters.
  • Chemical filters are generally aromatic compounds rich in double bonds and which have absorption maxima at wavelengths of UV radiation, between 300 nm (UVB) up to 350 nm (UVA).
  • UVB 300 nm
  • UVA 350 nm
  • chemical sunscreens which can be used alone or in combination, mention may be made of aminobenzoic acid, cinoxate, diethanolamine methoxy cinnamate, dioxybenzone, oxybenzone, octyl methoxycinnamate.
  • Physical filters are powders dispersed in creams which create a screen between ultraviolet radiation and the skin. In general we consider that the protection indices are better with physical filters
  • Antifungal composition :
  • the active principle is present in an amount of 1.00% to 10.00% by weight of the entire composition.
  • the other associated compounds are: - active ingredient: 1.00% to 10.00%
  • UV filter chemical, 1.00 to 10.00% of octyl ethoxycinnamate (commercial product known under the name Escalol 557, or: physical, 10.00 to 40.00% of zinc oxide sold under the denomination of Z dimension HP1.
  • an absorption promoter 1.00 to 6.00% of a mixture of polyethylene glycol and glycerol esters, in particular that marketed under the name Labraf il M1944, - an emulsifier suitable for water in oil mixtures : 2.00 to 10.00% of sorbitan monooleate, in particular that sold under the name Span 80.
  • a fatty agent 15.00 to 30.00% of white petrolatum, an antioxidant: 0.002 to 0.010% of buthylhydroxyanisole, - a microbial preservative: 0.10 to 1.00% benzoic acid or an agent from the class of para-amino benzoic acid esters, a thickener: 1.00 to 6.00% silicon dioxide , marketed under the name Aerosil 200. Distilled water qs.
  • Example 2 antifungal composition - 1.00% of econazole nitrate
  • Example 4 Composition ⁇ ntivir ⁇ l
  • the process for manufacturing these compositions comprises the following stages: the constituents of the oily phase are melted at a temperature between 60 and 65 ° C, the active principle is added progressively to the oily phase simultaneously, thus as the thickener and the chemical or physical sunscreens, - the constituents of the hydrophilic phase are heated to a temperature between 60 and 65 ° C, after having optionally added preservatives and surfactants, and the phase is slowly added aqueous with stirring.
  • a cream is thus obtained by emulsion of water in oil, with an antifungal or antiviral effect, water resistant with sun protection.
  • the results of the tests carried out make it possible to determine the resistance to water and the radiation protection U V.
  • the tests are conducted on albino guinea pigs. Is applied to the right flank of 12 of these guinea pigs, 0.5 ml of the cream obtained according to Example 1, this
  • the doses are 160, 20 and 50 mJ / cm 2 on the control flank and 1400, 1800 and 2250 mL / cm 2 on the treated flank.
  • a regular rinsing is carried out by means of a shower inducing a regular trickle of water.

Abstract

The invention relates to a dermatological composition comprising an active principle which is an anti-fungal or an anti-viral derivative, characterised in that the above comprises an emulsion of the water-in-oil type with a minor water phase and a major oil phase. The invention further relates to a method for production and uses.

Description

COMPOSITIONS ÙERMATOLOGIQUES, RESISTANTES A L'EAU, AVEC FILTRES SOLAIRES, PROCEÙE OE FABRICATION ET UTILISATIONS ÙE WATER RESISTANT ÙERMATOLOGICAL COMPOSITIONS WITH SOLAR FILTERS, MANUFACTURING PROCEEDS AND USES THEREOF
CES COMPOSITIONSTHESE COMPOSITIONS
La présente invention concerne des compositions dermatologiques résistantes à l'eau et comprenant des filtres solaires.The present invention relates to water-resistant dermatological compositions comprising sun filters.
L'invention couvre aussi le procédé de fabrication et les utilisations de ces compositions. Les affections dermatologiques sont traitées en particulier au moyen de deux familles de principes actifs que sont : les antifongiques, comme la famille des imidazolés, pour le traitement des mycoses cutanées, et les anti-viraux, comme l'aciclovir, pour le traitement de l'herpès labial et cutané,.The invention also covers the manufacturing process and the uses of these compositions. Dermatological conditions are treated in particular by means of two families of active principles which are: antifungals, such as the imidazole family, for the treatment of skin mycosis, and antiviral drugs, such as aciclovir, for the treatment of 'labial and cutaneous herpes.
On connaît des compositions du commerce notamment celle dénommée "Pévaryl" qui ont des activités antifongiques sur différentes souches comme les dermatophytes, les candidas et certaines levures, le Pityrosporum orbiculare et ovale, les moisissures et certains autres champignons. Un tel produit inclut du nitrate d'éconazole, généralement à 1%, qui est un dérivé imidazolé doué d'activité fongicide. Une forme galénique contenant ce principe actif est une crème qui permet une application sur la peau.Commercial compositions are known, in particular that called "Pevaryl" which have antifungal activities on various strains such as dermatophytes, candidas and certain yeasts, Pityrosporum orbiculare and ovale, molds and certain other fungi. Such a product includes econazole nitrate, generally at 1%, which is an imidazole derivative endowed with fungicidal activity. A dosage form containing this active ingredient is a cream which allows application to the skin.
Ce type de formulation est une emulsion du type huile dans l'eau, ce qui induit une phase huileuse minoritaire dispersée dans une phase aqueuse majoritaire. D'autres compositions sont également disponibles dans le commerce pour traiter l'herpès, comme la crème vendue sous la dénomination Zovirax, à base d'aciclovir. L'aciclovir est un analogue de la guanine qui, pour être actif, doit être phosphorylé en aciclovir tri-phosphate par une enzyme , la thymidine kinase, présente au sein des virus de l'herpès. Le dosage est généralement à 5%.This type of formulation is an oil-in-water type emulsion, which induces a minority oily phase dispersed in a majority aqueous phase. Other compositions are also commercially available for treating herpes, such as the cream sold under the name Zovirax, based on aciclovir. Aciclovir is a guanine analogue which, to be active, must be phosphorylated to aciclovir tri-phosphate by an enzyme, thymidine kinase, found in herpes viruses. The dosage is generally 5%.
Cette crème est également une emulsion huile dans l'eau c'est-à-dire que la formulation ne présente aucune résistance à l'eau.This cream is also an oil-in-water emulsion, that is to say that the formulation has no resistance to water.
La faible résistance à l'eau de ces formulations est un inconvénient important, ce qui explique qu'il faille appliquer plusieurs fois par jour la crème quand les patients sont au contact de l'eau ou produisent une transpiration abondante.The low water resistance of these formulations is a major drawback, which explains why it is necessary to apply the cream several times a day when the patients are in contact with water or produce profuse sweating.
Il serait très utile de disposer d'une formulation qui permette des applications moins nombreuses afin de limiter les contraintes, plus particulièrement pour les personnes amenées à se baigner ou en contact avec l'eau et les personnes ayant une sudation abondante et/ou sportive, tout en ayant une action efficace.It would be very useful to have a formulation which allows fewer applications in order to limit the constraints, more particularly for people brought to bathe or in contact with water and people with profuse sweating and / or sports, while having an effective action.
De plus de tels produits ne contiennent aucun filtre solaire. Or, ces types d'affections dermatologiques nécessitent pour les patients de se protéger du soleil qui peut être un facteur favorisant. C'est notamment le cas de l'herpès labial et cutané et des dermatoses fongiques cutanées comme le Pityriasis versicolor.In addition, such products do not contain any sunscreen. However, these types of dermatological conditions require for patients to protect themselves from the sun which can be a favorable factor. This is particularly the case of lip and skin herpes and skin fungal dermatoses such as Pityriasis versicolor.
Dans le cas de l'herpès labial et cutané, il a été démontré qu'une exposition au soleil favorise les risques d'apparition du bouton de fièvre (Prévention of ultraviolet-light-induced herpès labialis by sunscreen, ooney James <& al , The Lancet, v 338, n° 8780, pp 1419-1422).In the case of labial and cutaneous herpes, it has been shown that exposure to the sun promotes the risk of the appearance of cold sores (Prévention of ultraviolet-light-induced herpes labialis by sunscreen, ooney James <& al, The Lancet, v 338, n ° 8780, pp 1419-1422).
Pour les dermatoses fongiques, il est démontré que l'apparition des tâches caractéristiques blanches ou brunes qui se développent sur la peau est favorisée par l'exposition au soleil comme c'est le cas pour le Pityriasis versicolor. Un dénominateur commun à ces deux pathologies est qu'elles se développent souvent l'été et touchent particulièrement les sportifs ou les gens ayant des activités en plein air.For fungal dermatoses, it is shown that the appearance of the characteristic white or brown spots that develop on the skin is favored by exposure to the sun as is the case for Pityriasis versicolor. A common denominator for these two pathologies is that they often develop in summer and particularly affect sportspeople or people engaged in outdoor activities.
Pour prévenir l'apparition de ces dermatoses il serait particulièrement judicieux d'y inclure des filtres solaires qui préviendraient l'apparition des lésions cutanées mentionnées ci-dessus.To prevent the appearance of these dermatoses it would be particularly advisable to include sunscreens which would prevent the appearance of the skin lesions mentioned above.
L'objet de l'invention est de proposer une composition qui pallie les inconvénients des produits connus de l'art antérieur. La composition , en présentant une résistance accrue à l'eau, évite la dilution dans la transpiration ou dans l'eau au sein de laquelle évoluent les patients et garantit une meilleure efficacité en maintenant le principe actif sur son lieu d'application.The object of the invention is to provide a composition which overcomes the drawbacks of the products known from the prior art. The composition, by presenting an increased resistance to water, avoids dilution in perspiration or in the water within which the patients evolve and guarantees a better effectiveness by maintaining the active principle at its place of application.
Une application toute particulière est la prévention dans des milieux propices à la propagation des infections comme les piscines, les saunas ou les centres de thalassothérapie. A cet effet, les compositions dermatologiques selon l'invention contiennent un antifongique ou un antiviral, notamment le nitrate d'éconazole ou l'aciclovir, et des filtres solaires. Elles présentent une excellente résistance à l'eau et une forte protection solaire.One very specific application is prevention in environments conducive to the spread of infections such as swimming pools, saunas or thalassotherapy centers. To this end, the dermatological compositions according to the invention contain an antifungal or an antiviral, in particular econazole nitrate or aciclovir, and sun filters. They have excellent water resistance and strong sun protection.
Ces formulations sont des émulsions du type eau dans l'huile, c'est-à-dire, une phase huileuse majoritaire.These formulations are emulsions of the water in oil type, that is to say, a predominant oily phase.
Les avantages de telles compositions sont nombreux et notamment celui de permettre la réalisation d'un film occlusif favorable à la pénétration des principes actifs au travers de la peau, ce qui renforce son activité.The advantages of such compositions are numerous and in particular that of allowing the production of an occlusive film favorable to the penetration of the active ingredients through the skin, which reinforces its activity.
Les filtres utilisés peuvent être de type chimique et/ou physique. Les compositions sont décrites maintenant en détail par l'exemple à travers des formulations particulières.The filters used can be chemical and / or physical. The compositions are now described in detail by the example through specific formulations.
Chaque composition est une emulsion d'eau dans l'huile afin de présenter un caractère dit waterproof . Le rapport eau / huile doit rester dans une plage comprise entre 37,5 et 60 %.Each composition is an emulsion of water in oil in order to present a so-called waterproof character. The water / oil ratio must remain in a range between 37.5 and 60%.
Quant aux filtres utilisés pour la suite de la description, ils sont de différentes natures. Parmi les filtres solaires on inclut dans la présente invention les filtres chimiques et les filtres physiques.As for the filters used for the following description, they are of different types. Among the sun filters are included in the present invention chemical filters and physical filters.
Les filtres chimiques sont en général des composés aromatiques riches en doubles liaisons et qui présentent des maxima d'absorption aux longueurs d'onde des rayonnements UV, entre 300 nm (UVB) jusqu'à 350 nm (UVA). Parmi les filtres solaires chimiques que l'on peut utiliser seul ou en combinaison, on peut citer l'acide aminobenzoïque, le cinoxate, le diéthano lamine methoxy cinnamate, la dioxybenzone, l'oxybenzone, l'octyl methoxycinnamate.Chemical filters are generally aromatic compounds rich in double bonds and which have absorption maxima at wavelengths of UV radiation, between 300 nm (UVB) up to 350 nm (UVA). Among the chemical sunscreens which can be used alone or in combination, mention may be made of aminobenzoic acid, cinoxate, diethanolamine methoxy cinnamate, dioxybenzone, oxybenzone, octyl methoxycinnamate.
Les filtres physiques sont des poudres dispersées dans les crèmes qui réalisent un écran entre les radiations ultraviolettes et la peau. En général on considère que les indices de protection sont meilleurs avec les filtres physiquesPhysical filters are powders dispersed in creams which create a screen between ultraviolet radiation and the skin. In general we consider that the protection indices are better with physical filters
Parmi les filtres physiques particulièrement bien adaptés pour cette indication on peut citer le dioxyde de titane et l'oxyde de zinc, ou une combinaison de ceux-ci. Les exemples qui vont suivre sont précis pour la formulation mais non limitatifs.Among the physical filters which are particularly well suited for this indication, mention may be made of titanium dioxide and zinc oxide, or a combination of these. The examples which follow are precise for the formulation but not limiting.
Composition antifongique :Antifungal composition:
Dans le cas d'une composition antifongique, les plages des différentes composés sont indiquées ci-après:In the case of an antifungal composition, the ranges of the various compounds are indicated below:
Le principe actif est présent à raison de 1,00 % à 10,00% en poids de la totalité de la composition.The active principle is present in an amount of 1.00% to 10.00% by weight of the entire composition.
Les autres composés associés sont : - principe actif : 1,00% à 10,00%The other associated compounds are: - active ingredient: 1.00% to 10.00%
- un filtre UV : chimique, 1,00 à 10,00% d'octyl éthoxycinnamate ( produit du commerce connu sous la dénomination Escalol 557, ou : physique, 10,00 à 40,00% d'oxyde de zinc commercialisé sous la dénomination de Z cote HP1.- a UV filter: chemical, 1.00 to 10.00% of octyl ethoxycinnamate (commercial product known under the name Escalol 557, or: physical, 10.00 to 40.00% of zinc oxide sold under the denomination of Z dimension HP1.
- un promoteur d'absorption : 1,00 à 6,00% d'un mélange d'esters de polyéthylène glycol et de glycérol, notamment celui commercialisé sous la dénomination Labraf il M1944, - un émulsifiant adapté aux mélanges eau dans l'huile : 2,00 à 10,00% de sorbitan monooléate, notamment celui commercialisé sous la dénomination Span 80. un agent gras : 15,00 à 30,00 % de vaseline blanche, un antioxydant : 0,002 à 0,010% de buthylhydroxyanisole, - un conservateur microbien : 0,10 à 1,00% d'acide benzoïque ou d'un agent de la classe des esters de l'acide para-amino-benzoïque, un épaississant : 1,00 à 6,00% de dioxyde de silicium, commercialisé sous la dénomination Aérosil 200. Eau distillée qsp.- an absorption promoter: 1.00 to 6.00% of a mixture of polyethylene glycol and glycerol esters, in particular that marketed under the name Labraf il M1944, - an emulsifier suitable for water in oil mixtures : 2.00 to 10.00% of sorbitan monooleate, in particular that sold under the name Span 80. a fatty agent: 15.00 to 30.00% of white petrolatum, an antioxidant: 0.002 to 0.010% of buthylhydroxyanisole, - a microbial preservative: 0.10 to 1.00% benzoic acid or an agent from the class of para-amino benzoic acid esters, a thickener: 1.00 to 6.00% silicon dioxide , marketed under the name Aerosil 200. Distilled water qs.
Exemple 1 : composition antifongiqueExample 1: antifungal composition
1,00% de nitrate d'éconazole, 5,00% d'octyl méthoxycinnamate (Escalol 557), 2,607o de promoteur d'absorption (Labraf il M1944CS), - 6,30% de sorbitan monooléate, (Span 80),1.00% of econazole nitrate, 5.00% of octyl methoxycinnamate (Escalol 557), 2.607o of absorption promoter (Labraf il M1944CS), - 6.30% of sorbitan monooleate, (Span 80),
22,60% de vaseline blanche, 0,075% de buthylhydroxyanisole, 0,20% d'acide benzoïque, 4,44% de dioxyde de silicium (Aérosil 200), et eau distillée, qsp.22.60% white petrolatum, 0.075% buthylhydroxyanisole, 0.20% benzoic acid, 4.44% silicon dioxide (Aerosil 200), and distilled water, qs.
Exemple 2 : composition antifongique - 1,00% de nitrate d'éconazole,Example 2: antifungal composition - 1.00% of econazole nitrate,
15,00% d'oxyde de zinc (Z cote HP1),15.00% zinc oxide (Z dimension HP1),
2,60% de promoteur d'absorption (Labraf il M1944CS),2.60% absorption promoter (Labraf il M1944CS),
6,30% de sorbitan monooléate, (Span 80),6.30% sorbitan monooleate, (Span 80),
27,825% de vaseline blanche, - 3,00% de béhénate de glyceryl (Compritol ATO)27.825% white petrolatum, - 3.00% glyceryl behenate (Compritol ATO)
0,075% de buthylhydroxyanisole,0.075% buthylhydroxyanisole,
0,10% de POBM,0.10% POBM,
0,05% de POBP, et eau distillée, qsp.0.05% POBP, and distilled water, qs.
Exemple 3 : Composition antiviralExample 3 Antiviral composition
5,00% d'aciclovir,5.00% aciclovir,
5,00% d'un filtre chimique octyl méthoxycinnamate (Escalol 557) - 2,60% de promoteur d'absorption (Labraf il M1944CS),5.00% of an octyl methoxycinnamate chemical filter (Escalol 557) - 2.60% of absorption promoter (Labraf il M1944CS),
6,30%> de sorbitan monooléate, (Span 80),6.30%> of sorbitan monooleate, (Span 80),
27,825% de vaseline blanche,27.825% white petrolatum,
3,00% de béhénate de glyceryl (Compritol ATO)3.00% glyceryl behenate (Compritol ATO)
0,075% de buthylhydroxyanisole, - 0,10% de POBM,0.075% buthylhydroxyanisole, - 0.10% POBM,
0,05% de POBP, et eau distillée, qsp. Exemple 4 : Composition αntivirαl0.05% POBP, and distilled water, qs. Example 4: Composition αntivirαl
5,00% d'aciclovir,5.00% aciclovir,
15,00% d'oxyde de zinc (Z cote HP1),15.00% zinc oxide (Z dimension HP1),
2,60% de promoteur d'absorption (Labraf il M1944CS), - 6,30% de sorbitan monooléate, (Span 80),2.60% absorption promoter (Labraf il M1944CS), - 6.30% sorbitan monooleate, (Span 80),
27,825% de vaseline blanche,27.825% white petrolatum,
3,00% de béhénate de glyceryl (Compritol ATO)3.00% glyceryl behenate (Compritol ATO)
0,075% de buthylhydroxyanisole,0.075% buthylhydroxyanisole,
0,10% de POBM, - 0,05% de POBP, et eau distillée, qsp.0.10% POBM, - 0.05% POBP, and distilled water, qs.
Le procédé de fabrication de ces compositions comprend la succession des étapes suivantes : on fond les constituants de la phase huileuse à une température comprise entre 60 et 65°C, on ajoute le principe actif au fur et à mesure dans la phase huileuse simultanément , ainsi que l'épaississant et les filtres solaires chimiques ou physiques, - on chauffe les constituants de la phase hydrophile à une température comprise entre 60 et 65°C, après y avoir éventuellement ajouté les conservateurs et les tensioactif s, et on ajoute lentement la phase aqueuse sous agitation.The process for manufacturing these compositions comprises the following stages: the constituents of the oily phase are melted at a temperature between 60 and 65 ° C, the active principle is added progressively to the oily phase simultaneously, thus as the thickener and the chemical or physical sunscreens, - the constituents of the hydrophilic phase are heated to a temperature between 60 and 65 ° C, after having optionally added preservatives and surfactants, and the phase is slowly added aqueous with stirring.
On obtient ainsi une crème par emulsion d'eau dans l'huile, avec un effet antifongique ou antiviral, résistante à l'eau avec une protection solaire.A cream is thus obtained by emulsion of water in oil, with an antifungal or antiviral effect, water resistant with sun protection.
Les résultats des tests effectués permettent de déterminer la résistance à I ' eau et la protection aux rayonnements U V. Les tests sont conduits sur des cobayes albinos. On applique sur le flanc droit de 12 de ces cobayes, 0,5 ml de la crème obtenue suivant l'exemple 1, ceciThe results of the tests carried out make it possible to determine the resistance to water and the radiation protection U V. The tests are conducted on albino guinea pigs. Is applied to the right flank of 12 of these guinea pigs, 0.5 ml of the cream obtained according to Example 1, this
20 minutes avant l'irradiation par des UVB.20 minutes before irradiation with UVB.
Les doses sont de 160, 20 et 50 mJ/cm2 sur le flanc témoin et de 1400, 1800 et 2250 mL/cm2 sur le flanc traité.The doses are 160, 20 and 50 mJ / cm 2 on the control flank and 1400, 1800 and 2250 mL / cm 2 on the treated flank.
On constate que la moyenne des coefficients de protection individuelle est de 8,1 ± 1,1 ce qui est synonyme d'une très haute protection.It can be seen that the average of the individual protection coefficients is 8.1 ± 1.1, which is synonymous with very high protection.
On réalise des tests complémentaires pour la résistance à l'eau. A cet effet, on procède à un rinçage régulier au moyen d'une douchette induisant un filet d'eau régulier.Additional tests are carried out for water resistance. For this purpose, a regular rinsing is carried out by means of a shower inducing a regular trickle of water.
On procède à une irradiation dans les mêmes conditions que précédemment.An irradiation is carried out under the same conditions as above.
On constate un coefficient de protection solaire de 8,3 ± 1,1, ce qui prouve le caractère résistant à l'eau de ces formulations. There is a sun protection coefficient of 8.3 ± 1.1, which proves the water-resistant nature of these formulations.

Claims

R E V E N D I C A T I O N S
1. Composition dermatologique comprenant un principe actif du type dérivé antifongique ou dérivé antiviral, caractérisée en ce qu'elle comprend une emulsion de type eau dans l'huile comprenant une phase aqueuse minoritaire et une phase huileuse majoritaire. 1. Dermatological composition comprising an active principle of the antifungal derivative or antiviral derivative type, characterized in that it comprises a water-in-oil emulsion comprising a minority aqueous phase and a majority oily phase.
2. Composition dermatologique selon la revendication 1, caractérisée en ce que le dérivé antifongique est de la famille des imidazolés.2. Dermatological composition according to claim 1, characterized in that the antifungal derivative is from the family of imidazoles.
3. Composition dermatologique selon la revendication 2, caractérisée en ce que le dérivé antifongique est le nitrate d'éconazole.3. Dermatological composition according to claim 2, characterized in that the antifungal derivative is econazole nitrate.
4. Composition dermatologique selon la revendication 1, caractérisée en ce que le dérivé antiviral est l'aciclovir.4. Dermatological composition according to claim 1, characterized in that the antiviral derivative is aciclovir.
5. Composition dermatologique selon l'une quelconque des revendications précédentes, caractérisée en ce qu'elle inclut des filtres solaires physiques et/ou chimiques.5. Dermatological composition according to any one of the preceding claims, characterized in that it includes physical and / or chemical sun filters.
6. Composition dermatologique selon la revendication 5, caractérisée en ce que le filtre solaire chimique est choisi parmi l'acide ami obenzoïque, le cinoxate, le diéthanolamine methoxy cinnamate, la dioxybenzone, l'oxybenzone, l'octyl méthoxycinnamate.6. Dermatological composition according to claim 5, characterized in that the chemical sunscreen is chosen from obenzoic acid friend, cinoxate, diethanolamine methoxy cinnamate, dioxybenzone, oxybenzone, octyl methoxycinnamate.
7. Composition dermatologique selon la revendication 5, caractérisée en ce que le filtre solaire physique est choisi comprend du dioxyde de titane et/ou de l'oxyde de zinc.7. Dermatological composition according to claim 5, characterized in that the physical sun filter is chosen comprises titanium dioxide and / or zinc oxide.
8. Composition dermatologique selon l'une quelconque des revendications précédentes, caractérisée en ce qu'elle comprend des agents conservateurs et/ou des agents oxydants.8. Dermatological composition according to any one of the preceding claims, characterized in that it comprises preserving agents and / or oxidizing agents.
9. Procédé de fabrication d'une composition dermatologique selon l'une quelconque des revendications précédentes, caractérisé en ce qu'il consiste en la succession des étapes suivantes : - on fond les constituants de la phase huileuse à une température comprise entre 60 et 65°C,9. Method for manufacturing a dermatological composition according to any one of the preceding claims, characterized in that it consists of the succession of the following steps: the constituents of the oily phase are melted at a temperature between 60 and 65 ° C,
- on ajoute le principe actif au fur et à mesure dans la phase huileuse simultanément , ainsi que l'épaississant et les filtres solaires chimiques ou physiques,- the active principle is added progressively in the oily phase simultaneously, as well as the thickener and the chemical or physical sun filters,
- on chauffe les constituants de la phase hydrophile à une température comprise entre 60 et 65°C, après y avoir éventuellement ajouté les conservateurs et les tensioactifs, etthe constituents of the hydrophilic phase are heated to a temperature between 60 and 65 ° C, after having optionally added preservatives and surfactants, and
- on ajoute lentement la phase aqueuse sous agitation. - The aqueous phase is added slowly with stirring.
10. Utilisation de la composition selon l'une quelconque des revendications10. Use of the composition according to any one of the claims
1 à 3 et 5 à 8, pour son activité antifongique et pour sa résistance à l'eau, par application sur la peau, en permettant la réalisation d'un film occlusif favorable à la pénétration du principe actif au travers de ladite peau.1 to 3 and 5 to 8, for its antifungal activity and for its resistance to water, by application to the skin, allowing the production of an occlusive film favorable to the penetration of the active principle through said skin.
11. Utilisation de la composition selon l'une quelconque des revendications 1, 4 et 5 à 8, pour lutter contre l'herpès et pour sa résistance à l'eau, par application sur la peau, en permettant la réalisation d'un film occlusif favorable à la pénétration du principe actif au travers de ladite peau. 11. Use of the composition according to any one of claims 1, 4 and 5 to 8, for combating herpes and for its resistance to water, by application to the skin, by allowing the production of a film occlusive favorable for the penetration of the active principle through said skin.
PCT/FR2003/000158 2002-01-22 2003-01-20 Dermatological water-resistant compositions with sun screens and method for production and use of such compositions WO2003061707A1 (en)

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FR0200727A FR2834895B1 (en) 2002-01-22 2002-01-22 WATER-RESISTANT, DERMATOLOGICAL COMPOSITIONS WITH SOLAR FILTERS, METHOD FOR MANUFACTURING THE SAME, AND USES THEREOF
FR02/00727 2002-01-22

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EP1541136A1 (en) * 2003-12-10 2005-06-15 Schering AG UV light-stable semi-solid transdermal systems comprising a photosensitive active agent and an UV-absorbing component
WO2008003632A1 (en) * 2006-07-07 2008-01-10 Henkel Ag & Co. Kgaa Disinfectant skin care product

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EP0586106A1 (en) * 1992-08-06 1994-03-09 JOHNSON &amp; JOHNSON CONSUMER PRODUCTS, INC. Skin care compositions containing imidazoles and retinoids
EP0747042A1 (en) * 1995-06-06 1996-12-11 Unilever Plc Compositions containing azole derivatives for topical application to skin
WO1996040144A1 (en) * 1995-06-07 1996-12-19 Pharmavene, Inc. Oral acyclovir delivery
US5660839A (en) * 1994-07-11 1997-08-26 L'oreal Nongreasy/nonsticky fatty cosmetic/dermatological compositions

Patent Citations (4)

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Publication number Priority date Publication date Assignee Title
EP0586106A1 (en) * 1992-08-06 1994-03-09 JOHNSON &amp; JOHNSON CONSUMER PRODUCTS, INC. Skin care compositions containing imidazoles and retinoids
US5660839A (en) * 1994-07-11 1997-08-26 L'oreal Nongreasy/nonsticky fatty cosmetic/dermatological compositions
EP0747042A1 (en) * 1995-06-06 1996-12-11 Unilever Plc Compositions containing azole derivatives for topical application to skin
WO1996040144A1 (en) * 1995-06-07 1996-12-19 Pharmavene, Inc. Oral acyclovir delivery

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1541136A1 (en) * 2003-12-10 2005-06-15 Schering AG UV light-stable semi-solid transdermal systems comprising a photosensitive active agent and an UV-absorbing component
WO2005055975A2 (en) * 2003-12-10 2005-06-23 Schering Ag Uv-stable semi-solid transdermal systems comprising a photosensitive active ingredient and a uv absorber
JP2007534643A (en) * 2003-12-10 2007-11-29 シェーリング アーゲー UV-stable, liquid or semi-solid transdermal dosage form containing photosensitive active ingredient
EA010239B1 (en) * 2003-12-10 2008-06-30 Шеринг Акциенгезельшафт Uv-stable, liquid or semi-liquid transdermal administration form comprising a photosensitive active ingredient
AU2004296539B2 (en) * 2003-12-10 2008-10-09 Bayer Schering Pharma Aktiengesellschaft UV-stable, liquid or semi-solid transdermal administration form comprising a photosensitive active ingredient
WO2005055975A3 (en) * 2003-12-10 2009-03-12 Schering Ag Uv-stable semi-solid transdermal systems comprising a photosensitive active ingredient and a uv absorber
WO2008003632A1 (en) * 2006-07-07 2008-01-10 Henkel Ag & Co. Kgaa Disinfectant skin care product

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FR2834895B1 (en) 2006-06-23
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