WO2003026606A1 - Compositions ameliorant la fonction barriere de la peau - Google Patents

Compositions ameliorant la fonction barriere de la peau Download PDF

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Publication number
WO2003026606A1
WO2003026606A1 PCT/JP2002/009895 JP0209895W WO03026606A1 WO 2003026606 A1 WO2003026606 A1 WO 2003026606A1 JP 0209895 W JP0209895 W JP 0209895W WO 03026606 A1 WO03026606 A1 WO 03026606A1
Authority
WO
WIPO (PCT)
Prior art keywords
barrier function
composition
skin barrier
skin
improving
Prior art date
Application number
PCT/JP2002/009895
Other languages
English (en)
Japanese (ja)
Inventor
Tatsuo Shimizu
Kiyoshi Kuriyama
Original Assignee
Sekisui Chemical Co., Ltd.
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 Sekisui Chemical Co., Ltd. filed Critical Sekisui Chemical Co., Ltd.
Publication of WO2003026606A1 publication Critical patent/WO2003026606A1/fr

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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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • A61K8/736—Chitin; Chitosan; 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • 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
    • 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
    • A61Q19/007—Preparations for dry skin

Definitions

  • composition for improving skin barrier function Composition for improving skin barrier function
  • the present invention relates to a skin barrier function improving composition having an excellent skin barrier function improving effect and an antipruritic effect, and exhibiting good sustained retention and feeling of use.
  • Skin is subject to various physical, chemical and biological stimuli.
  • the skin barrier function protects the living body from these external stimuli. If this function deteriorates, external irritation causes rough skin, skin contamination and various dermatitis such as contact dermatitis. In addition, reduced skin barrier function increases the amount of water transpired from the skin, causing dry skin and itching.
  • the skin barrier function is measured by the amount of water transpiration from the skin (transepidermal water transpiration; TEWL).
  • humectants such as urea and heparin-like substances, barrier function improving agents such as serine and the like, which prevent moisture from evaporating from the skin, and polymer-coated films have been used to prevent drying of the skin.
  • humectants such as urea and heparin-like substances, barrier function improving agents such as serine and the like, which prevent moisture from evaporating from the skin, and polymer-coated films have been used to prevent drying of the skin.
  • they were not effective enough and had an unpleasant feeling of use such as stickiness, discomfort or irritation. Also, it was not possible to improve itching due to drying.
  • Japanese Patent Application Laid-Open No. H10-182323 / Japanese Patent Application Laid-Open No. 2000-212203 describes chitosan and derivatives thereof as raw materials for cosmetics. I have. However, neither of these documents describes a skin barrier function improving effect or an antipruritic effect.
  • emulsified formulations such as emulsions and creams are being developed.
  • these emulsified formulations use surfactants and emulsifiers, which are known to show cytotoxicity due to cell membrane rupture and protein denaturation, etc.
  • surfactants and emulsifiers which are known to show cytotoxicity due to cell membrane rupture and protein denaturation, etc.
  • the function may be deteriorated, and the skin may be dried more.
  • An object of the present invention is to provide a skin barrier function improving composition having an excellent skin barrier function improving effect and an antipruritic effect and exhibiting good sustained retention and a feeling of use.
  • the present invention is a skin barrier function-improving composition containing 0.2 to 20% by weight of mucopolysaccharide or a derivative thereof.
  • the mucopolysaccharide is preferably at least one selected from the group consisting of hyaluronic acid, chondroitin sulfate, dermatan sulfate, keratan sulfate, heparin, chitin and chitosan.
  • the above-mentioned mucopolysaccharide or its derivative preferably has an average degree of polymerization of 5 or more and less than 100.
  • the mucopolysaccharide has an average degree of polymerization of 5 or more and less than 100 parts by weight of chitosan 100 parts by weight, and an average degree of polymerization of 1000 or more and less than 500 parts of chitosan 30 to 3 parts by weight. It is preferably a mixture with 100 parts by weight.
  • composition for improving skin barrier function of the present invention preferably further contains a liquid oil, and the liquid oil is more preferably squalane. Further, the composition for improving skin barrier function of the present invention preferably further contains urea and does not contain a compound having a sulfur atom as a Maillard reaction preventing component.
  • the composition for improving skin barrier function of the present invention contains a mucopolysaccharide or a derivative thereof.
  • the mucopolysaccharide means a polysaccharide containing hexosamine as a component.
  • the mucopolysaccharide is not particularly limited, but is preferably, for example, at least one selected from the group consisting of hyaluronic acid, chondroitin sulfate, dermatan sulfate, keratan sulfate, heparin, chitin, and chitosan.
  • the derivative of the mucopolysaccharide means a compound produced by a change in a small part of the molecule in the mucopolysaccharide, and examples thereof include hyaluronate and chondroitin sulfate.
  • the mucopolysaccharide chitosan or a derivative thereof is more preferably used.
  • chitosan is obtained by heating chitin with a concentrated alkaline solution or the like to obtain 40 mo 1 / mo Poly-N-acetyl-D-darcosamine obtained by deacetylation of 1% or more.
  • a concentrated alkaline solution or the like there is no particular limitation on the type of raw material chitin used and the method for producing chitosan.
  • chitosan derivatives include, for example, alkylation, succinylation, hydroxyanolekinorei, alkylcarboxylation, and alkylation of an amino group, an OH group or an CH 2 OH group of a dalcosamine residue of chitosan.
  • Roxyalkylcarbonylated compounds and the like can be mentioned.
  • those in which a deacetylated amino group of chitin forms a salt with an organic acid or an inorganic acid are also exemplified.
  • the mucopolysaccharide or a derivative thereof preferably has an average degree of polymerization of 5 or more and less than 1000. If it is less than 5, the effect of improving the skin barrier function may not be sufficiently obtained, and if it exceeds 100, the physical properties may be changed, and the effect of improving the skin barrier function may not be obtained sufficiently. .
  • the average degree of polymerization is more preferably 50 or more and less than 800.
  • chitosan When chitosan is used as the mucopolysaccharide or a derivative thereof, chitosan having an average degree of polymerization of 5 or more and less than 1000 and chitosan having an average degree of polymerization of 10000 or more and less than 500 Is preferred.
  • Chitosan with an average degree of polymerization of 5 or more and less than 1000 which has a high skin barrier function improving effect, and an average degree of polymerization that provides good spreadability and light feeling of use (freshness) and permeability (easiness of adaptation)
  • a composition for improving skin barrier function having both characteristics can be obtained.
  • the mixing ratio between the chitosan having an average degree of polymerization of 5 or more and less than 1000 and the chitosan having an average degree of polymerization of 1000 or more and less than 500 is as follows.
  • the lower limit of the content of the mucopolysaccharide or a derivative thereof is preferably 0.2% by weight.
  • a new upper limit is 20% by weight. If the amount is less than 0.2% by weight, a sufficient effect of improving the skin barrier function may not be obtained. If the amount exceeds 20% by weight, no further effect can be expected, and in addition, it is difficult to dissolve, and the viscosity is low. And the ability to follow the skin may be impaired.
  • a more preferred lower limit is 0.5% by weight, a more preferred upper limit is 10% by weight, a still more preferred lower limit is 1% by weight, and a still more preferred upper limit is 5% by weight.
  • the composition for improving skin barrier function of the present invention preferably contains an acid to make the chitosan or derivative thereof water-soluble.
  • an inorganic acid or an organic acid can be used as the acid.
  • the inorganic acid include hydrochloric acid, phosphoric acid, sulfuric acid, nitric acid and the like.
  • the organic acid include acetic acid, succinic acid, malic acid, lactic acid, butyric acid, fumaric acid, malonic acid, itaconic acid, dalconic acid, glycolic acid, tartaric acid, and citric acid.
  • a hydroxy acid which is a fatty acid having a chemical structure having a hydroxy group in a carboxylic acid is preferable. These acids may be used alone or in combination of two or more.
  • a preferable lower limit of the content of the acid is 0. 1% by weight, the upper limit is preferably 1 0 weight 0/0. If the amount is less than 0.1% by weight, chitosan or a derivative thereof may not be sufficiently soluble in water. If the amount exceeds 10% by weight, skin irritation may occur depending on the application site.
  • a more preferred lower limit is 0.5 weight. / 0 , a more preferred upper limit is 5% by weight.
  • the composition for improving skin barrier function of the present invention preferably further contains a liquid oil.
  • the liquid oils are not particularly limited, and include, for example, hydrocarbons such as squalane, ester oils such as tocopher acetate, and glyceride oils such as triglyceride. Of these, squalane is particularly preferred.
  • the preferred lower limit of the content of the liquid oils is 2% by weight, the preferred upper limit is 20% by weight, the more preferred lower limit is 5% by weight, and the more preferred upper limit is 15% by weight.
  • the composition for improving skin barrier function of the present invention preferably further contains urea. Mucopolysaccharides, especially chitosan, in an aqueous solution tend to cause a Maillard reaction due to heat and may turn brown, but the present inventors have found that adding urea It has been found that chitosan and the like can be stabilized to prevent browning.
  • the preferred lower limit of the urea content is 0.1% by weight / 0
  • the preferred upper limit is 3% by weight. 0.1 weight. / Sufficient effect is less than zero may not be obtained, and when it exceeds 3 wt%, the effect is not only not increased more, mucopolysaccharide is deposited, it may be difficult formulate .
  • a more preferred upper limit is 1.5% by weight.
  • composition for improving skin barrier function of the present invention it is preferable that a compound having a sulfur atom as a Maillard reaction-inhibiting component, for example, a sulfite, is not contained because the effect of the present invention may be lost.
  • a compound having a sulfur atom as a Maillard reaction-inhibiting component for example, a sulfite
  • composition for improving skin barrier function of the present invention includes powders, oils, surfactants, thickeners, organic solvents, plasticizers, dyes, pigments, fragrances, antiseptics, An oxidizing agent or the like may be contained.
  • the composition for improving skin barrier function of the present invention has an excellent effect of suppressing moisture evaporation from the skin, and has an effect of keeping dry skin healthy by having a good feeling of use. That is, it is possible to improve dry skin due to various causes such as drying of the skin, for example, decrease in environmental humidity, malnutrition, aging, and skin diseases.
  • the skin barrier function-improved product of the present invention can be used for atopic skin (dry skin), senile xeroderma, skin dryness after renal dialysis, cracks, irritations, progressive palmar keratoderma, etc. It is also effective on dry skin and can also suppress itching of the skin due to dryness of the skin. In addition, it can reduce skin roughness, skin contamination and various dermatitis caused by physical, chemical and biological stimuli.
  • composition for improving skin barrier function of the present invention is disclosed in Japanese Unexamined Patent Publication No.
  • the dosage form of the composition for improving skin barrier function of the present invention is not particularly limited.
  • the method for producing the composition for improving skin barrier function of the present invention is not particularly limited, and the composition can be produced by a conventionally known method.
  • the application amount of the composition for improving skin barrier function of the present invention is not particularly limited by the type and concentration of the active ingredient and the condition of the site to be applied, but is usually one to several times a day, 0.01 to 10 g. It is preferable to apply about Zl times.
  • the method for applying the composition for improving skin barrier function of the present invention is not particularly limited. In addition to the usual method of applying a skin external preparation using fingers or a tool (spatula, etc.), a pump-type, spray-type, or tube-type container can be used. Direct coating, compressing, etc. are mentioned. BEST MODE FOR CARRYING OUT THE INVENTION
  • Lactic acid was dissolved in distilled water by stirring using a magnetic stirrer in distilled water to obtain a composition of Comparative Example 1 to obtain 2% by weight.
  • Comparative Example 2 white petrolatum (Japanese Pharmacopoeia, manufactured by Maruishi Pharmaceutical Co., Ltd.) was used.
  • Comparative Example 3 urea (manufactured by Wako Pure Chemical Industries, Ltd.), which is often used as a humectant, was used as a macrogol ointment base (this pharmacy)
  • a urea ointment was prepared by mixing 20% by weight of a urea ointment with the product (Maruishi Pharmaceutical).
  • X 50% or more of the area in which the dye has protruded greatly from the application site, and has spread, peeled off, or dropped off
  • Table 2 shows chitosan (manufactured by Wako Pure Chemical Industries), lactic acid (manufactured by Evis Pharmaceuticals), squalane (manufactured by Maruha), and urea (manufactured by Kosakai Pharmaceutical Co., Ltd.) having an average degree of polymerization of 300 and 300,000.
  • the composition of Examples 15 to 25 was obtained by stirring and suspending in water for injection (manufactured by Otsuka Pharmaceutical Co., Ltd.) so as to have the indicated concentration (% by weight).
  • Comparative Examples 4, 5 Comparative Examples 4, 5
  • Vaseline (made by Maruishi Pharmaceutical Co., Ltd.) was used as Comparative Example 4, and heparinoid ointment (made by Maruho Pharmaceutical Co., Ltd.) was used as Comparative Example 5.
  • composition of each example was dispensed into a 5 OmL glass sample bottle with a screw cap and stored at 40 ° C. After 24 hours, the presence or absence of separation was visually checked. The separated product was evaluated as “X”.
  • composition of each example was dispensed into a 5 OmL glass sample bottle with a screw cap and stored at 40 ° C. After two weeks, the change in color tone was visually observed. Those that turned brown were evaluated as “X”.
  • TEWL transepidermal water loss
  • Example 5 Heparinoid ointment 2 26.5 27.0 Healthy skin 5.6.7.7 Damaged skin 27.3
  • the mucopolysaccharide was added to water for injection (manufactured by Otsuka Pharmaceutical Co., Ltd.) so as to have the content (% by weight) shown in Table 3, followed by stirring and dissolving to obtain the compositions of Examples 26 to 31.
  • Comparative Example 9 was an antihistamine ointment (Kowasha Co., Ltd., “Restamine Co ⁇ ”) used as an external preparation for antipruritus, Comparative Example 10 was Vaseline (Maruishi Pharmaceutical Co., Ltd.), and Comparative Example 11 was urea ointment ( Kowasha) was used.
  • a 40-year-old male atopy patient with itchy back was used as a test subject. Each composition was applied to the affected area, and the itch of the affected area was evaluated from immediately after application to 6 hours after application. "Excellent” was evaluated as ⁇ , "Effective” as “ ⁇ ”, “Slightly effective” as “ ⁇ ”, and "Invalid” as X.
  • TEWL transepidermal water loss
  • a skin barrier function improving composition having an excellent skin barrier function improving effect and an antipruritic effect and exhibiting a good sustained staying property and a feeling of use:

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Dermatology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Birds (AREA)
  • Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne des compositions qui sont destinées à améliorer la fonction barrière de la peau. Ces compositions présentent d'excellents effets d'amélioration de la fonction barrière de la peau et de soulagement des démangeaisons, offrent une bonne texture lors de l'utilisation et font preuve d'une tenue prolongée favorable. Les compositions destinées à améliorer la fonction barrière de la peau renferment de 0,2 à 20 % en poids de mucopolysaccharides ou de dérivés de ces derniers.
PCT/JP2002/009895 2001-09-25 2002-09-25 Compositions ameliorant la fonction barriere de la peau WO2003026606A1 (fr)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
JP2001291916 2001-09-25
JP2001291915 2001-09-25
JP2001-291916 2001-09-25
JP2001-291915 2001-09-25
JP2002092392 2002-03-28
JP2002-92392 2002-03-28
JP2002-186446 2002-06-26
JP2002186446 2002-06-26

Publications (1)

Publication Number Publication Date
WO2003026606A1 true WO2003026606A1 (fr) 2003-04-03

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111246888A (zh) * 2017-10-20 2020-06-05 日本乐敦制药株式会社 皮肤障碍改善用组合物

Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0622070A1 (fr) * 1993-04-29 1994-11-02 MERCK PATENT GmbH Mélange pulvérulent pour la coloration de la peau
EP0715852A1 (fr) * 1994-12-05 1996-06-12 Denki Kagaku Kogyo Kabushiki Kaisha Utilisation de l'acide hyaluronique ou son sel pour le traitement des désordres de la peau
JPH0952848A (ja) * 1995-08-07 1997-02-25 Pola Chem Ind Inc 皮膚外用剤
JPH10158304A (ja) * 1996-12-04 1998-06-16 Akuseenu Kk キトサン誘導体と、そのキトサン誘導体を含有する化粧料
JPH10298092A (ja) * 1997-04-30 1998-11-10 Noevir Co Ltd 抗掻痒ローション
JPH11124324A (ja) * 1997-10-17 1999-05-11 Tosco Co Ltd アトピー性皮膚炎症用化粧料
JP2000169327A (ja) * 1998-12-03 2000-06-20 Pias Arise Kk 低刺激性皮膚外用剤及び浴用剤
JP2000290153A (ja) * 1999-04-09 2000-10-17 Kao Corp 皮膚外用剤
JP2000302660A (ja) * 1999-04-20 2000-10-31 Pola Chem Ind Inc 冬季用の皮膚外用剤
JP2001106623A (ja) * 1999-08-03 2001-04-17 Noevir Co Ltd 皮膚保護剤及び皮膚外用剤
JP2001181180A (ja) * 1999-12-24 2001-07-03 Lion Corp 油中水型乳化組成物
JP2001240529A (ja) * 2000-03-01 2001-09-04 Pola Chem Ind Inc 美肌用の化粧料
JP2002145753A (ja) * 2000-11-06 2002-05-22 Orbis Inc 保湿用組成物及び該組成物を含有する化粧料

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0622070A1 (fr) * 1993-04-29 1994-11-02 MERCK PATENT GmbH Mélange pulvérulent pour la coloration de la peau
EP0715852A1 (fr) * 1994-12-05 1996-06-12 Denki Kagaku Kogyo Kabushiki Kaisha Utilisation de l'acide hyaluronique ou son sel pour le traitement des désordres de la peau
JPH0952848A (ja) * 1995-08-07 1997-02-25 Pola Chem Ind Inc 皮膚外用剤
JPH10158304A (ja) * 1996-12-04 1998-06-16 Akuseenu Kk キトサン誘導体と、そのキトサン誘導体を含有する化粧料
JPH10298092A (ja) * 1997-04-30 1998-11-10 Noevir Co Ltd 抗掻痒ローション
JPH11124324A (ja) * 1997-10-17 1999-05-11 Tosco Co Ltd アトピー性皮膚炎症用化粧料
JP2000169327A (ja) * 1998-12-03 2000-06-20 Pias Arise Kk 低刺激性皮膚外用剤及び浴用剤
JP2000290153A (ja) * 1999-04-09 2000-10-17 Kao Corp 皮膚外用剤
JP2000302660A (ja) * 1999-04-20 2000-10-31 Pola Chem Ind Inc 冬季用の皮膚外用剤
JP2001106623A (ja) * 1999-08-03 2001-04-17 Noevir Co Ltd 皮膚保護剤及び皮膚外用剤
JP2001181180A (ja) * 1999-12-24 2001-07-03 Lion Corp 油中水型乳化組成物
JP2001240529A (ja) * 2000-03-01 2001-09-04 Pola Chem Ind Inc 美肌用の化粧料
JP2002145753A (ja) * 2000-11-06 2002-05-22 Orbis Inc 保湿用組成物及び該組成物を含有する化粧料

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111246888A (zh) * 2017-10-20 2020-06-05 日本乐敦制药株式会社 皮肤障碍改善用组合物

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