WO2007080511A2 - Dermocosmetic composition comprising at least one antimycotic substance combined with a reepithelizing substance - Google Patents

Dermocosmetic composition comprising at least one antimycotic substance combined with a reepithelizing substance Download PDF

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Publication number
WO2007080511A2
WO2007080511A2 PCT/IB2007/000089 IB2007000089W WO2007080511A2 WO 2007080511 A2 WO2007080511 A2 WO 2007080511A2 IB 2007000089 W IB2007000089 W IB 2007000089W WO 2007080511 A2 WO2007080511 A2 WO 2007080511A2
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WO
WIPO (PCT)
Prior art keywords
substance
composition
approximately
skin
foregoing
Prior art date
Application number
PCT/IB2007/000089
Other languages
French (fr)
Other versions
WO2007080511A3 (en
Inventor
Carlo Felice Fornara
Arie Ciuntu
Adele Sparavigna
Michele Setaro
Alessandro Mazzetti
Original Assignee
Dermogyn S.R.L.
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 Dermogyn S.R.L. filed Critical Dermogyn S.R.L.
Publication of WO2007080511A2 publication Critical patent/WO2007080511A2/en
Publication of WO2007080511A3 publication Critical patent/WO2007080511A3/en

Links

Classifications

    • 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
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4946—Imidazoles or their condensed derivatives, e.g. benzimidazoles
    • 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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • A61K8/732—Starch; Amylose; Amylopectin; Derivatives 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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • A61K8/735—Mucopolysaccharides, e.g. hyaluronic acid; Derivatives thereof
    • 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
    • A61Q17/005—Antimicrobial preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/74—Biological properties of particular ingredients
    • A61K2800/75—Anti-irritant

Definitions

  • the present invention relates to a dermocosmetic composition for dermatological and cosmetic use, and in particular for the treatment of skin irritation with or without associated superinfections caused by specific alterations of the skin, and specifically of the stratum corneum.
  • antimycotic substances Pharmaceutical use of antimycotic substances is known, and is governed by law. In particular, antimycotic activity with various concentrations of climbazole is known .
  • antimycotic substances in general, and climbazole in particular are used, for example, in certain shampoos.
  • a dermocosmetic composition in particular for the treatment of skin irritation, possibly associated with superinfections caused by specific alterations of the skin, and specifically of the stratum corneum, characterized by comprising at least one antimycotic substance combined with a reepithelizing substance.
  • the composition according to the invention also comprises, in combination with the antimycotic substance and the reepithelizing substance, a skin-protecting substance, such as corn starch.
  • a skin-protecting substance such as corn starch.
  • the antimycotic substance is climbazole; the reepithelizing substance is hyaluronic acid or a hyaluronic acid salt (hyaluronate) ; and the skin- protecting substance, if any, is corn starch.
  • the antimycotic substance if climbazole, is used in concentrations ranging from approximately 0.05% to approximately 1%, and preferably from approximately 0.2% to approximately 0.6%;
  • the reepithelizing substance, if hyaluronic acid is used in concentrations ranging from approximately 0.05% to approximately 1%, and preferably from approximately 0.05% to approximately 0.5%;
  • the skin-protecting substance, if corn starch is used in concentrations ranging from approximately 1% to approximately 6%, and preferably from approximately 2% to approximately 5%.
  • the dermocosmetic composition according to the invention not only prevents the onset of irritation, with or without infection complications, but is also highly effective in soothing irritation, even in the presence of superinfections, once these arise, and with none of the aforementioned drawbacks typically associated with currently used products.
  • composition according to the invention is also effective at such low antimycotic substance concentrations as to be suitable for dermocosmetic use.
  • the composition according to the invention has also proved effective in treating irritation, possibly associated with superinfections caused by specific alterations of the skin, and in particular of the stratum corneum, by maintaining, restoring, and/or improving the barrier function of the stratum corneum.
  • the invention therefore relates, in general, to the use of a combination of an antimycotic substance, a reepithelizing substance, and possibly a skin-protecting substance, with a buffered acid pH, as a dermocosmetic composition for the treatment of irritation, possibly associated with superinfections caused by specific alterations of the skin, and in particular of the stratum corneum, i.e. the outermost layer of the epidermis.
  • composition according to the invention in fact, has been found to have a positive effect on the biochemistry of the stratum corneum, which, though predominantly formed of flaking cells with no nuclei, still has a metabolic and enzymatic activity of its own; and, if this activity is compromised, the stratum corneum is no longer able to guarantee the functions for which it is designed, and in particular, correct desquamation and effective protection of the underlying tissues (barrier effect) .
  • the composition according to the invention aims more at treating the outermost stratum corneum, thus reversing the principle so far adopted of treating skin irritation by exclusively targeting the deep layers, in that, very often, skin irritation derives mainly from primitive alterations of the stratum corneum.
  • the composition is preferably, though not exclusively, in the form of an aqueous emulsion, but may be prepared in other forms.
  • the composition in addition to emulsion (W/0, water in oil, and O/W, oil in water) , the composition may be prepared in the form of gel, powder, lotion, foam, liquid patch, gauze, etc.; and the various forms may be produced using normal technology, or innovative technology such as nanotechnology .
  • the composition has an acid pH. More specifically, the composition has a pH ranging from approximately 5.5 to approximately 7.0, and preferably ranging from approximately 6.5 to approximately 6.8.
  • the composition comprises a buffer system, e.g. a phosphate buffer system.
  • composition also comprises one or more optional substances chosen from the group comprising: lipid restructuring substances, natural emulsifiers, water- resistant filmogens, soothing substances.
  • a first composition in accordance with the invention was prepared containing, in aqueous emulsion:
  • a second composition was prepared containing, also in aqueous emulsion:
  • compositions similar to those described above, were prepared, both in aqueous emulsion and other forms, by varying the concentration of climbazole (from approximately 0.05% to approximately 1%) and/or of hyaluronic acid salt (from approximately 0.05% to approximately 1%) and/or of corn starch (to approximately 6%), as well as that of the other components.
  • the buffer systems were also varied to obtain compositions with pH values ranging from approximately 5.5 to approximately 7.0.
  • compositions proved effective in both preventive and protective treatment of irritation, possibly associated with superinfections, caused by specific alterations of the skin, and in particular of the stratum corneum.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cosmetics (AREA)

Abstract

A dermocosmetic composition for dermatological and cosmetic use, in particular for treating skin irritation with or without associated superinfections caused by- specific alterations of the skin, and specifically of the stratum corneum, includes at least one antimycotic substance combined with a reepithelizing substance and a skin-protecting substance. The antimycotic substance is, for example, climbazole; the reepithelizing substance is, for example, hyaluronic acid or a hyaluronic acid salt; the skin-protecting substance is, for example, corn starch; and the composition also has a buffer system, e.g. a phosphate buffer system, to maintain the pH of the composition at predetermined values ranging from approximately 5.5 to approximately 7.0.

Description

DERMOCOSMETIC COMPOSITION, IN PARTICULAR FOR THE TREATMENT OF SKIN IRRITATION, POSSIBLY ASSOCIATED WITH SUPERINFECTIONS CAUSED BY SPECIFIC ALTERATIONS OF THE SKIN, AND SPECIFICALLY OF THE STRATUM CORNEUM
TECHNICAL FIELD
The present invention relates to a dermocosmetic composition for dermatological and cosmetic use, and in particular for the treatment of skin irritation with or without associated superinfections caused by specific alterations of the skin, and specifically of the stratum corneum.
BACKGROUND ART
Pharmaceutical use of antimycotic substances is known, and is governed by law. In particular, antimycotic activity with various concentrations of climbazole is known .
In dermatology and cosmetics, antimycotic substances in general, and climbazole in particular, are used, for example, in certain shampoos.
In cosmetics, on the other hand, i.e. a field not subject to legislation governing pharmaceutical formulations, no dermocosmetic compositions are yet available for the treatment of skin irritation associated with skin and mucous superinfections and/or deepithelization, as for example in the case (relatively common) of candidiasis.
Cases of this sort call for the use of products in the form of ointment or at any rate containing adsorbent powders combined with various topical antimycotic drugs. At present, such product combinations are unsatisfactory, not only in terms of effectiveness, but also as regards practical use and aesthetic considerations, in that application is clearly visible and stains clothing. DISCLOSURE OF INVENTION
It is an object of the present invention to eliminate the aforementioned drawbacks of currently used procedures; more specifically, it is an object of the invention to provide a soothing dermocosmetic composition, which may also be used effectively in the case of superinfections.
According to the present invention, there is provided a dermocosmetic composition, in particular for the treatment of skin irritation, possibly associated with superinfections caused by specific alterations of the skin, and specifically of the stratum corneum, characterized by comprising at least one antimycotic substance combined with a reepithelizing substance.
In a preferred embodiment, the composition according to the invention also comprises, in combination with the antimycotic substance and the reepithelizing substance, a skin-protecting substance, such as corn starch. Preferably, the antimycotic substance is climbazole; the reepithelizing substance is hyaluronic acid or a hyaluronic acid salt (hyaluronate) ; and the skin- protecting substance, if any, is corn starch. More specifically, the antimycotic substance, if climbazole, is used in concentrations ranging from approximately 0.05% to approximately 1%, and preferably from approximately 0.2% to approximately 0.6%; the reepithelizing substance, if hyaluronic acid, is used in concentrations ranging from approximately 0.05% to approximately 1%, and preferably from approximately 0.05% to approximately 0.5%; and the skin-protecting substance, if corn starch, is used in concentrations ranging from approximately 1% to approximately 6%, and preferably from approximately 2% to approximately 5%.
The dermocosmetic composition according to the invention not only prevents the onset of irritation, with or without infection complications, but is also highly effective in soothing irritation, even in the presence of superinfections, once these arise, and with none of the aforementioned drawbacks typically associated with currently used products.
The effects of combining an antimycotic substance, a reepithelizing substance, and possibly also a skin- protecting substance in accordance with the invention, in fact, go far beyond a simple sum of the effects one would expect from the individual components, in that, besides involving none of the practical and aesthetic problems mentioned of known products, the composition according to the invention is also effective at such low antimycotic substance concentrations as to be suitable for dermocosmetic use. The composition according to the invention has also proved effective in treating irritation, possibly associated with superinfections caused by specific alterations of the skin, and in particular of the stratum corneum, by maintaining, restoring, and/or improving the barrier function of the stratum corneum.
The invention therefore relates, in general, to the use of a combination of an antimycotic substance, a reepithelizing substance, and possibly a skin-protecting substance, with a buffered acid pH, as a dermocosmetic composition for the treatment of irritation, possibly associated with superinfections caused by specific alterations of the skin, and in particular of the stratum corneum, i.e. the outermost layer of the epidermis. The composition according to the invention, in fact, has been found to have a positive effect on the biochemistry of the stratum corneum, which, though predominantly formed of flaking cells with no nuclei, still has a metabolic and enzymatic activity of its own; and, if this activity is compromised, the stratum corneum is no longer able to guarantee the functions for which it is designed, and in particular, correct desquamation and effective protection of the underlying tissues (barrier effect) . Unlike the traditional approach, which aims at treating the deep layers of the epidermis and especially the dermis, the composition according to the invention therefore aims more at treating the outermost stratum corneum, thus reversing the principle so far adopted of treating skin irritation by exclusively targeting the deep layers, in that, very often, skin irritation derives mainly from primitive alterations of the stratum corneum. The composition is preferably, though not exclusively, in the form of an aqueous emulsion, but may be prepared in other forms. For example, in addition to emulsion (W/0, water in oil, and O/W, oil in water) , the composition may be prepared in the form of gel, powder, lotion, foam, liquid patch, gauze, etc.; and the various forms may be produced using normal technology, or innovative technology such as nanotechnology .
According to a particularly important aspect of the invention, the composition has an acid pH. More specifically, the composition has a pH ranging from approximately 5.5 to approximately 7.0, and preferably ranging from approximately 6.5 to approximately 6.8.
To maintain the predetermined pH values, the composition comprises a buffer system, e.g. a phosphate buffer system.
The composition also comprises one or more optional substances chosen from the group comprising: lipid restructuring substances, natural emulsifiers, water- resistant filmogens, soothing substances.
BEST MODE FOR CARRYING OUT THE INVENTION
The invention is further described in the following non-limiting embodiments. A first composition in accordance with the invention was prepared containing, in aqueous emulsion:
- climbazole 0.2%
- hyaluronic acid salt 0.1% - lipophilic corn starch 2.0% and also containing:
- a phosphate buffer system (pH 6.5-6.8)
- 18β-glycirretic and alpha-bisabolol acid as soothing substances; - red algae and hydrolyzed jojoba ester as water- resistant filmogens;
- barley extract and almond wax as lipid restructuring substances .
A second composition was prepared containing, also in aqueous emulsion:
- climbazole 0.5%
- hyaluronic acid salt 0.1%
- lipophilic corn starch 5.0% and also containing: - a phosphate buffer system (pH 6.5-6.8)
- 18β-glycirretic and alpha-bisabolol acid;
- tocopheryl acetate;
- linoleic acid;
- almond wax. Further compositions, similar to those described above, were prepared, both in aqueous emulsion and other forms, by varying the concentration of climbazole (from approximately 0.05% to approximately 1%) and/or of hyaluronic acid salt (from approximately 0.05% to approximately 1%) and/or of corn starch (to approximately 6%), as well as that of the other components.
The buffer systems were also varied to obtain compositions with pH values ranging from approximately 5.5 to approximately 7.0.
All the compositions proved effective in both preventive and protective treatment of irritation, possibly associated with superinfections, caused by specific alterations of the skin, and in particular of the stratum corneum.

Claims

1) A dermocosmetic composition, in particular for the treatment of skin irritation, possibly associated with superinfections caused by specific alterations of the skin, and specifically of the stratum corneum, characterized by comprising at least one antimycotic substance combined with a reepithelizing substance.
2) A composition as claimed in Claim 1, characterized in that the antimycotic substance is climbazole.
3) A composition as claimed in Claim 1 or 2, characterized in that the reepithelizing substance is hyaluronic acid or a hyaluronic acid salt. 4) A composition as claimed in one of the foregoing Claims, characterized by also comprising a skin- protecting substance in combination with the antimycotic substance and the reepithelizing substance.
5) A composition as claimed in Claim 4, characterized in that the skin-protecting substance is corn starch.
6) A composition as claimed in one of the foregoing Claims, characterized by being in the form of aqueous emulsion, in particular W/0 or 0/W emulsion, or in the form of gel, powder, lotion, foam, liquid patch, gauze.
7) A composition as claimed in one of the foregoing Claims, characterized by having an acid pH.
8) A composition as claimed in one of the foregoing Claims, characterized by having an acid pH ranging from approximately 5.5 to approximately 7.0.
9) A composition as claimed in one of the foregoing Claims, characterized by having an acid pH ranging from approximately 6.5 to approximately 6.8.
10) A composition as claimed in one of the foregoing Claims, characterized by comprising a buffer system for maintaining the predetermined pH values of the composition. 11) A composition as claimed in Claim 10, characterized in that the buffer system is a phosphate buffer system.
12) A composition as claimed in one of the foregoing Claims, characterized by comprising one or more substances chosen from the group comprising: lipid restructuring substances, natural emulsifiers, water- resistance filmogens, soothing substances.
13) A composition as claimed in one of the foregoing Claims, characterized in that the antimycotic substance is present in concentrations ranging from approximately 0.05% to approximately 1%, and preferably from approximately 0.2% to approximately 0.6%.
14) A composition as claimed in one of the foregoing Claims, characterized in that the reepithelizing substance is used in concentrations ranging from approximately 0.05% to approximately 1%, and preferably from approximately 0.05% to approximately 0.5%.
15) A composition as claimed in one of the foregoing Claims, characterized in that the skin-protecting substance is used in concentrations ranging from approximately 1% to approximately 6%, and preferably from approximately 2% to approximately 5%.
16) Use of a combination of an antimycotic substance, a reepithelizing substance, and an optional skin-protecting substance, as a dermocosmetic composition for treatment of the stratum corneum.
PCT/IB2007/000089 2006-01-13 2007-01-12 Dermocosmetic composition comprising at least one antimycotic substance combined with a reepithelizing substance WO2007080511A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITMI20060050 ITMI20060050A1 (en) 2006-01-13 2006-01-13 DERMOCOSMETIC COMPOSITION IN PARTICULAR FOR THE TREATMENT OF CUTANEOUS IRRITATION STATES THAT MAY BE ASSOCIATED WITH STATES OF OVER-INFECTION DERIVED FROM DSA SPECIFIC SKIN ALTERATIONS AND SPECIFICALLY OF THE CORNEO STATE
ITMI2006A000050 2006-01-13

Publications (2)

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WO2007080511A2 true WO2007080511A2 (en) 2007-07-19
WO2007080511A3 WO2007080511A3 (en) 2007-12-13

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PCT/IB2007/000089 WO2007080511A2 (en) 2006-01-13 2007-01-12 Dermocosmetic composition comprising at least one antimycotic substance combined with a reepithelizing substance

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2628479A1 (en) * 2011-11-29 2013-08-21 Henkel AG&Co. KGAA Cosmetic use of climbazol

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004017903A2 (en) * 2002-08-20 2004-03-04 Pinnell Doren M Methods for treating fungal infections

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004017903A2 (en) * 2002-08-20 2004-03-04 Pinnell Doren M Methods for treating fungal infections

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2628479A1 (en) * 2011-11-29 2013-08-21 Henkel AG&Co. KGAA Cosmetic use of climbazol

Also Published As

Publication number Publication date
WO2007080511A3 (en) 2007-12-13
ITMI20060050A1 (en) 2007-07-14

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