WO2022050295A1 - Composition for external use on skin - Google Patents

Composition for external use on skin Download PDF

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Publication number
WO2022050295A1
WO2022050295A1 PCT/JP2021/032069 JP2021032069W WO2022050295A1 WO 2022050295 A1 WO2022050295 A1 WO 2022050295A1 JP 2021032069 W JP2021032069 W JP 2021032069W WO 2022050295 A1 WO2022050295 A1 WO 2022050295A1
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WO
WIPO (PCT)
Prior art keywords
skin
composition
mass
component
external
Prior art date
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PCT/JP2021/032069
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French (fr)
Japanese (ja)
Inventor
愛里 西元
Original Assignee
ロート製薬株式会社
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Application filed by ロート製薬株式会社 filed Critical ロート製薬株式会社
Priority to CN202180053109.XA priority Critical patent/CN115989062A/en
Priority to JP2022546938A priority patent/JPWO2022050295A1/ja
Publication of WO2022050295A1 publication Critical patent/WO2022050295A1/en

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Classifications

    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
    • 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
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K8/34—Alcohols
    • 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
    • A61K8/67—Vitamins
    • 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
    • A61K9/08—Solutions
    • 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P17/18—Antioxidants, e.g. antiradicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

Definitions

  • the present invention relates to a composition for external use on the skin. More specifically, it relates to a composition for external skin containing ascorbic acid and / or a salt thereof and a lower alcohol and contained in a specific container.
  • Ascorbic acid has anti-inflammatory effect, acne improving effect, whitening effect, anti-aging effect, antioxidant effect, cell activation effect by promoting synthesis of biological components such as collagen, and suppresses cell damage and DNA damage caused by ultraviolet rays of epidermal keratinocytes. It is known to exert various effects such as the effect of collagen, and it is used as an external preparation for skin in anticipation of these effects.
  • Such ascorbic acid is provided in a form containing a solvent (for example, Patent Document 1).
  • An object of the present invention is to provide a composition for external use on the skin, which is easy to pack in a container during production and easily discharges an appropriate amount when applied to the skin.
  • the external composition for skin when the external composition for skin is housed in a container containing a polyolefin resin, if the wettability of the external composition for skin to the container is inferior, it may be applied to the upper wall surface of the tube during filling during manufacturing. It has been found that fine water droplets tend to remain, which may interfere with the sealing of the container, and it may be difficult to discharge an appropriate amount when using.
  • the present inventor contains at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol. Therefore, they have found that the composition can have an effect of improving wettability with respect to a resin containing polyolefin, an effect of suppressing pH fluctuation by storage, and an effect of promoting defoaming, and have completed the present invention.
  • the present invention provides the composition for external use on the skin listed below.
  • Item 1 A composition for external use on the skin containing (A) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol.
  • a composition for external skin wherein a part or all of the surface in contact with the external composition for skin is housed in a container containing a resin containing polyolefin.
  • Item 2. The composition for external use on the skin according to Item 1, wherein the total content of the component (B) is 1 to 7% by mass.
  • Item 3. any one of Items 1 or 2 containing at least one selected from the group consisting of the following (C-1), (C-2), (C-3), and (C-4).
  • composition for external use of the skin according to the section: (C-1) Pyridoxine and / or a salt thereof; (C-2) At least one selected from the group consisting of salicylic acid, salicylic acid derivatives, and salts thereof; (C-3) Isopropylmethylphenol; (C-4) Ascorbic acid derivative.
  • Item 4. Item 6. The composition for external use on the skin according to any one of Items 1 to 3, wherein the component (B) contains at least ethanol.
  • Item 6. Item 6.
  • the present invention provides the following methods. Item 7. By allowing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid and (B) a lower alcohol to coexist in the composition, the resin containing the polyolefin in the composition is allowed to coexist. A method of imparting a wettability improving effect.
  • the external composition for skin of the present invention is A composition for external use on the skin containing (A) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol.
  • the external composition for skin is a composition in which a part or all of the surface in contact with the external composition for skin is contained in a container containing a resin containing polyolefin.
  • ascorbic acid used in the present invention At least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid
  • ascorbic acid used in the present invention ascorbic acid used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics can be used, and these are usually L-form, although not limited. Point to.
  • Ascorbic acid salt can also be used.
  • the salt of ascorbic acid is a pharmaceutically acceptable salt.
  • a salt with an organic base for example, a salt with a tertiary amine such as a trimethylamine salt, a triethylamine salt, a monoethanolamine salt, a triethanolamine salt, a pyridine salt, a basic ammonium salt such as arginine).
  • Etc. salts with inorganic bases (eg, alkali metal salts such as ammonium salt, sodium salt, potassium salt, alkaline earth metal salt such as calcium salt, magnesium salt, aluminum salt, etc.) and the like are exemplified.
  • Preferred ascorbic acid salts are sodium salts and potassium salts.
  • ascorbic acid or a salt thereof can be used alone or in combination of two or more. Ascorbic acid is preferable from the viewpoint of remarkably exerting the effect of the present invention.
  • Ascorbic acid or a salt thereof may be synthesized and used, or a commercially available product may be used.
  • the total content of the component (A) with respect to the total amount of the external composition for skin is appropriately set by the balance with other components.
  • the total content of the component (A) is preferably 30% by mass or less, more preferably 10% by mass or less, still more preferably 9% by mass or less, still more preferably 5% by mass or less.
  • the total content of the component (A) with respect to the total amount of the external composition for skin is preferably 0.5% by mass or more, more preferably 1% by mass or more, still more preferably 2% by mass or more. , Even more preferably 3% by mass or more.
  • the total content of the component (A) with respect to the total amount of the external composition for skin is preferably 0.5 to 30% by mass, more preferably 1 to 10% by mass, still more preferably 2 to 9% by mass, and even more. It is preferably 3 to 5% by mass, and may be 1 to 5% by mass, 1 to 3% by mass, 3 to 5% by mass, or 3% by mass.
  • the lower alcohol used in the present invention is not limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics.
  • the term "lower alcohol” refers to alcohols of C1 - C6 , of which alcohols of C1 - C3 can be preferably used. Examples of such examples include methanol, ethanol, n-propanol, isopropanol and the like.
  • the lower alcohol used in the present invention particularly preferably contains or is at least ethanol.
  • the total content of the component (B) with respect to the total amount of the external composition for skin is preferably 0.1 to 20% by mass, more preferably 0.5 to 10% by mass, still more preferably. Is 0.5 to 7% by mass, more preferably 1 to 7% by mass, and particularly preferably 1 to 5% by mass. Further, it may be 0.5 to 5% by mass, 0.5 to 3% by mass, 2 to 5% by mass, 2 to 3% by mass, or the like.
  • the amount of ethanol with respect to the total amount of the external composition for skin is preferably 0.1 to 20% by mass, more preferably 0.5. It is -10% by mass, more preferably 1 to 7% by mass.
  • the ratio of the blending amount of the component (B) to the component (A) is (A) With respect to 1 part by mass of the total content of the component, 0.003 to 40 parts by mass is preferable, 0.05 to 10 parts by mass is more preferable, and 0.2 to 2.5 parts by mass is further preferable.
  • the external composition for skin of the present invention further comprises the following (C-1), (C-2), (C-3), and (C-4).
  • ) May contain at least one selected from the group consisting of.
  • (C-2) At least one selected from the group consisting of salicylic acid, salicylic acid derivatives, and salts thereof;
  • (C-3) Isopropylmethylphenol; (C-4) Ascorbic acid derivative.
  • the pyridoxine and / or a salt thereof used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics.
  • Pyridoxine salt is a pharmaceutically acceptable salt.
  • pyridoxine hydrochloride is exemplified.
  • pyridoxine or a salt thereof can be used alone or in combination of two or more.
  • Pyridoxine hydrochloride is preferable from the viewpoint of remarkably exerting the effect of the present invention.
  • Pyridoxine or a salt thereof may be used synthetically, or a commercially available product may be used.
  • the total content of the component (C-1) with respect to the total amount of the external composition for skin is not limited, but is preferably 0.001% by mass or more, more preferably 0. It is 005% by mass or more, more preferably 0.01% by mass or more.
  • the total content of the component (C-1) with respect to the total amount of the external composition for skin is not limited, but is preferably 1% by mass or less, more preferably 0.5% by mass or less, still more preferably 0. .1% by mass or less.
  • the total content of the component (C-1) with respect to the total amount of the external composition for skin is preferably 0.001 to 1% by mass, preferably 0.005 to 0.5% by mass, and more preferably 0.01 to 0.01. It is 0.1% by mass.
  • the ratio of the blending amount of the component (C-1) to the component (A) is not particularly limited, but is 0.00003 to 1 part by mass of the total content of the component (A). 2 parts by mass is preferable, 0.0005 to 0.5 parts by mass is more preferable, and 0.002 to 0.04 parts by mass is further preferable.
  • (C-2) At least one selected from the group consisting of salicylic acid, salicylic acid derivatives, and salts thereof
  • the salicylic acid, the derivative of salicylic acid, and the salt thereof used in the present invention are not particularly limited as long as they are used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs, and cosmetics.
  • Derivatives of salicylic acid include, but are not limited to, ethylene glycol salicylate, phenyl salicylate, methyl salicylate, 2-ethylhexyl salicylate, dipropylene glycol salicylate, Ti salicylate and the like.
  • the salt of salicylic acid or a derivative of salicylic acid is a pharmaceutically acceptable salt.
  • examples thereof include, but are not limited to, alkali metal salts, alkaline earth metal salts, salts with organic bases, and the like.
  • examples of the salicylate include at least one selected from the group consisting of sodium salicylate, calcium salicylate, magnesium salicylate and potassium salicylate.
  • salicylic acid, salicylic acid derivatives, and salts thereof can be used alone or in combination of two or more. From the viewpoint of remarkably exerting the effect of the present invention, at least one selected from the group consisting of salicylic acid, sodium salicylate, calcium salicylate, magnesium salicylate and potassium salicylate is preferable, and salicylic acid and / or sodium salicylate is more preferable.
  • Salicylic acid, derivatives of salicylic acid, and salts thereof may be used synthetically or commercially available products.
  • the total content of the component (C-2) with respect to the total amount of the external composition for skin is not limited, but is preferably 0.00002% by mass or more, more preferably 0. It is 0005% by mass or more, more preferably 0.05% by mass or more.
  • the total content of the component (C-2) with respect to the total amount of the external composition for skin is not limited, but is preferably 5% by mass or less, more preferably 1% by mass or less, still more preferably 0.5. It is 0% by mass or less, and more preferably 0.2% by mass or less.
  • the total content of the component (C-2) with respect to the total amount of the external composition for skin is preferably 0.00002 to 5% by mass, preferably 0.0005 to 1% by mass, and more preferably 0.05 to 0. It is 5% by mass.
  • the ratio of the blending amount of the component (C-2) to the component (A) is not particularly limited, but is 0.0000006 to 1 part by mass of the total content of the component (A). 10 parts by mass is preferable, 0.00005 to 1 part by mass is more preferable, and 0.01 to 0.2 parts by mass is further preferable.
  • the isopropylmethylphenol used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics. Isopropylmethylphenol has a bactericidal action.
  • Isopropylmethylphenol may be synthesized and used, or a commercially available product may be used.
  • the content of the component (C-3) with respect to the total amount of the external composition for skin is not limited, but is preferably 0.001% by mass or more, more preferably 0.005. It is by mass or more, more preferably 0.01% by mass or more.
  • the content of the component (C-3) with respect to the total amount of the external composition for skin is not limited, but is preferably 5% by mass or less, more preferably 1% by mass or less, still more preferably 0.1% by mass. % Or less.
  • the content of the component (C-3) with respect to the total amount of the external composition for skin is preferably 0.001 to 5% by mass, preferably 0.005 to 1% by mass, and more preferably 0.01 to 0.1. It is mass%.
  • the ratio of the blending amount of the component (C-3) to the component (A) is not particularly limited, but is 0.000003 to 1 part by mass of the total content of the component (A). 10 parts by mass is preferable, 0.0005 to 1 part by mass is more preferable, and 0.002 to 0.04 parts by mass is further preferable.
  • the ascorbic acid derivative used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics.
  • the salt is a pharmaceutically acceptable salt.
  • a salt with an organic base for example, a salt with a tertiary amine such as a trimethylamine salt, a triethylamine salt, a monoethanolamine salt, a triethanolamine salt, a pyridine salt, a basic ammonium salt such as arginine).
  • salts with inorganic bases eg, alkali metal salts such as ammonium salt, sodium salt, potassium salt, alkaline earth metal salt such as calcium salt, magnesium salt, aluminum salt, etc.
  • Particularly preferred salts of 3-O-ethylascorbic acid are sodium salts and potassium salts.
  • the ascorbic acid derivative can be used alone or in combination of two or more. From the viewpoint of remarkably exerting the effect of the present invention, 3-O-ethylascorbic acid or L-ascorbic acid 2-glucoside is preferable.
  • the ascorbic acid derivative may be synthesized and used, or a commercially available product may be used.
  • the total content of the component (C-4) with respect to the total amount of the external composition for skin is preferably 0.0001 to 10% by mass, more preferably 0.0005 to 5% by mass. More preferably, it is 0.001 to 2% by mass. It may be 0.0001 to 2% by mass.
  • the ratio of the blending amount of the component (C-4) to the component (A) is not particularly limited, but is 0.00005 to 1 part by mass of the total content of the component (A). 5 parts by mass is preferable, and 0.0002 to 0.7 parts by mass is more preferable.
  • composition for external use on the skin of the present invention may contain a polyhydric alcohol in addition to the above-mentioned components (A) and (B) as long as the effects of the present invention are not impaired.
  • the polyhydric alcohol used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics.
  • Polyhydric alcohols may be added, but not limited to, for moisturizing or as a solubilizer.
  • a preferred polyhydric alcohol is a diol having 3 carbon atoms, but is not limited.
  • glycerin, diglycerin, dipropylene glycol, 1,3-butylene glycol, 3-methyl-1,3-butanediol and the like are exemplified.
  • the polyhydric alcohol can be used alone or in combination of two or more.
  • the total content of the polyhydric alcohol with respect to the total amount of the external composition for skin of the present invention is preferably 0.1 to 60% by mass, more preferably 1 to 50% by mass, still more preferably 10 to 10 to It is about 45% by mass.
  • the ratio of the compounding amount of the polyhydric alcohol to the component (A) is not particularly limited, but 0.003 to 120 parts by mass with respect to 1 part by mass of the total content of the component (A). Is preferable, 0.1 to 50 parts by mass is more preferable, and 2 to 15 parts by mass is further preferable.
  • the diol having 3 carbon atoms used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics. Further, as such a diol having 3 carbon atoms, a commercially available product can be used as it is.
  • the diol having 3 carbon atoms is not limited, but is, for example, 1,3-propanediol (CAS number: 504-63-2, English name: 1,3-Dihydroxypropane or TrimethyleneGlycol) or propylene glycol (CAS number: 57).
  • the total content of the diol having 3 carbon atoms with respect to the total amount of the external composition for skin is 1% by mass or more, preferably 5% by mass or more, and more preferably 10% by mass. That is all.
  • the total content of the diol having 3 carbon atoms with respect to the total amount of the external composition for skin is 50% by mass or less, preferably 40% by mass or less, and more preferably 30% by mass or less.
  • the total content of the diol having 3 carbon atoms with respect to the total amount of the external composition for skin is 1 to 50% by mass, preferably 5 to 40% by mass, and more preferably 10 to 30% by mass.
  • the ratio of the blending amount of the diol having 3 carbon atoms to the component (A) is not particularly limited, but is 0.003 to 0.003 with respect to 1 part by mass of the total content of the component (A). 120 parts by mass is preferable, 0.1 to 50 parts by mass is more preferable, and 2 to 15 parts by mass is further preferable.
  • the blending amount of propylene glycol is preferably 1% by mass or more, more preferably 5% by mass or more, still more preferably 10% by mass, based on the total amount of the external composition for skin. That is all.
  • the blending amount of propylene glycol is preferably 40% by mass or less, more preferably 30% by mass or less, still more preferably 20% by mass or less, still more preferably 10% by mass or less.
  • the total content of propylene glycol with respect to the total amount of the external composition for skin is 1 to 40% by mass, preferably 5 to 30% by mass, and more preferably 10 to 20% by mass.
  • the ratio of the blending amount of propylene glycol to the component (A) is not particularly limited, but 0.03 to 80 parts by mass is based on 1 part by mass of the total content of the component (A).
  • 0.5 to 30 parts by mass is more preferable, 1 to 10 parts by mass is further preferable, and 2 to 7 parts by mass is even more preferable.
  • the blending amount of 1,3-propanediol is preferably 1% by mass or more, more preferably 5% by mass or more, still more preferably, based on the total amount of the external composition for skin. It is 10% by mass or more.
  • the blending amount of 1,3-propanediol is 30% by mass or less, more preferably 25% by mass or less, still more preferably 20% by mass or less, still more preferably 15% by mass or less.
  • the total content of 1,3-propanediol with respect to the total amount of the external composition for skin is 1 to 30% by mass, preferably 5 to 20% by mass, and more preferably 10 to 15% by mass.
  • the ratio of the blending amount of 1,3-propanediol to the component (A) is not particularly limited, but 0.03 to 0.03 to 1 part by mass of the total content of the component (A). 60 parts by mass is preferable, 0.5 to 20 parts by mass is more preferable, 1 to 7.5 parts by mass is further preferable, and 2 to 5 parts by mass is even more preferable.
  • the composition for external use on the skin of the present invention may contain water in addition to the above-mentioned components (A) and (B) as long as the effects of the present invention are not impaired.
  • the content of water with respect to the total amount of the external composition for skin is preferably 0.1 to 30% by mass, more preferably 1 to 20% by mass, still more preferably 2 to 15% by mass. It may be 0.1 to 90% by mass, 0.5 to 80% by mass, 1 to 70% by mass, 2 to 60% by mass, or the like.
  • composition for external use on the skin of the present invention contains vitamin Es such as tocopherol, a salt of tocopherol, and a derivative of tocopherol in addition to the above components (A) and (B) as long as the effects of the present invention are not impaired. You may be.
  • the tocopherol, the salt of tocopherol, the derivative of tocopherol and the like used in the present invention a compound usually used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics can be used. It may be either a body or a dl body, and may have any of ⁇ , ⁇ , ⁇ , and ⁇ structures.
  • tocopherols include d- ⁇ -tocopherol, d- ⁇ -tocopherol, d- ⁇ -tocopherol and d- ⁇ -tocopherol, l- ⁇ -tocopherol, l- ⁇ -tocopherol, l- ⁇ -tocopherol, l-.
  • examples thereof include ⁇ -tocopherol, dl- ⁇ -tocopherol, dl- ⁇ -tocopherol, dl- ⁇ -tocopherol, dl- ⁇ -tocopherol, dl- ⁇ -tocopherol and the like, which are mixtures thereof.
  • the derivative of tocopherol is not limited, but an ester of tocopherol is preferable.
  • tocopherol Derivatives of tocopherol include tocopherol acetate, tocopherol nicotinic acid ester or a salt thereof, tocopherol succinic acid ester or a salt thereof, tocopherol linolenic acid ester, tocopherol phosphate or a salt thereof, tocopherol (linoleic acid / oleic acid), and tocotoerinol.
  • An example is one selected from the group consisting of.
  • the total content of vitamin E with respect to the total amount of the external composition for skin is not particularly limited, but is preferably 0.00001 to 10% by mass, more preferably 0.0001 to 5% by mass. %, More preferably 0.001 to 1% by mass, still more preferably 0.01 to 0.5% by mass.
  • the composition for external use on the skin of the present invention may contain a surfactant in addition to the above-mentioned components (A) and (B) as long as the effects of the present invention are not impaired.
  • a surfactant is contained, a nonionic surfactant is preferable, and for example, polyoxyethylene hydrogenated castor oil 40, polyoxyethylene hydrogenated castor oil 60, polyoxyethylene hydrogenated castor oil 80, and polyoxy Ethylene polyoxypropylene decyltetradecyl ether, polyoxyethylene (20) polyoxypropylene (4) cetyl ether, PEG-8 glyceryl isostearate, polyoxyethylene sorbitan monolaurate (20EO), polyoxyethylene sorbitan isostearate (20EO), Polyoxyethylene sorbitan stearate (20EO), palm oil fatty acid polyglyceryl-10, palm oil fatty acid polyglyceryl-3, palm oil fatty acid PEG-7 glyceryl, polyglyceryl diole
  • Polyglyceryl-10, PEG-40 glyceryl triisostearate, PEG-40 glyceryl isostearate, polyglyceryl-10 trilaurate, hexaglyceryl tricaprylate, polyglyceryl laurate, polyglyceryl myristate, polyoxyethylene lauryl ether and the like can be used.
  • Polyoxyethylene sorbitan acid (20EO) and polyglyceryl laurate are preferred.
  • the total content of the surfactant with respect to the total amount of the external composition for skin is appropriately set depending on the balance with other components.
  • the total content of the surfactant with respect to the total amount of the external composition for skin is preferably 0.001 to 10% by mass, more preferably 0.005 to 7% by mass, still more preferably 0.01 to 5% by mass. Is.
  • the external composition for skin of the present invention includes a whitening component, an anti-inflammatory component, an antibacterial component, a cell activating component, an astringent component, an antioxidant component, and an acne improving component.
  • a whitening component an anti-inflammatory component
  • an antibacterial component such as collagen
  • a cell activating component such as collagen
  • an astringent component such as collagen
  • a moisturizing component such as collagen
  • an anti-aging component such as collagen
  • a blood circulation promoting component such as collagen
  • a moisturizing component such as collagen
  • an anti-aging component such as collagen, a blood circulation promoting component, a moisturizing component, and an anti-aging component can be blended in one or a combination of two or more. It is preferably one or more components of a whitening component, an anti-inflammatory component, an antibacterial component, a cell activating component, an astringent component, an antioxidant component, an anti-aging component or a moisturizing component.
  • Particularly preferable combinations of these components are a combination with a whitening component, a combination of a whitening component and an antioxidant component, each combination with an antioxidant component, a combination with an anti-aging component, and a whitening component and an anti-aging component.
  • Each combination of can be mentioned.
  • Each of these components is not particularly limited as long as it is conventionally used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs, or cosmetics, and will be used in the future, and any component may be appropriately selected.
  • dipotassium glycyrrhizinate which is an anti-inflammatory component, is preferably used.
  • These components may be used alone or in combination of two or more.
  • composition for external use on the skin of the present invention may further contain a solubilizing component, oils and fats, saccharides, or a transdermal absorption promoting component in addition to each of the above components.
  • a solubilizing component or oils and fats by blending a solubilizing component or oils and fats, the stability, effectiveness and usability of ascorbic acid in an aqueous solvent can be further improved.
  • composition for external use on the skin of the present invention is, if necessary, a pharmaceutical product, a quasi-drug, or a pharmaceutical product, within a quantitative and qualitative range that does not impair the quality such as appearance stability and viscosity, and does not impair the effect of the present invention.
  • Various components commonly used as components of external agents in the cosmetic field such as amino acids, irritation reducing agents, thickeners, preservatives, UV protection agents, coloring agents, dispersants, additional pH regulators, fragrances, etc. Can be blended. These components may be used alone or in combination of two or more.
  • the external composition for skin of the present invention is contained in a container containing a resin containing a polyolefin, in part or in whole of the surface in contact with the external composition for skin.
  • the polyolefin includes polyethylene (PE) (including high-density polyethylene (HDPE), low-density polyethylene (LDPE), ultra-low-density polyethylene, linear low-density polyethylene (LLDPE), ultra-high-molecular-weight polyethylene, etc.).
  • PE polyethylene
  • HDPE high-density polyethylene
  • LDPE low-density polyethylene
  • LLDPE linear low-density polyethylene
  • ultra-high-molecular-weight polyethylene etc.
  • Polyethylene (PP) including homopolymers, random copolymers, block copolymers, etc.
  • ethylene-propylene copolymers, cyclic olefin copolymers, polymethylpentene, polybutene-1,1,2-polybutadiene are preferred, polyethylene resin or polypropylene resin is more preferred. preferable. Of these, a resin containing at least polyethylene is particularly preferable.
  • the shape of the container to be used can be appropriately selected according to the purpose, and examples include tube type, jar type, dropper type, dispenser-type, pouch pack, spray type, bottle type, and cheer pack. Of these, a container that has undergone a heat sealing step is preferable, and a tube type, a pouch pack, a cheer pack, and the like are particularly preferable.
  • the container include, for example, an aluminum tube in which the innermost surface in contact with the external composition for skin is laminated with a resin containing polyolefin, an aluminum bag in which the innermost surface in contact with the external composition for skin is laminated with a resin containing polyolefin, and the like.
  • a storage container a stand pouch with a chuck whose innermost surface in contact with the external composition for skin is laminated with a resin containing polyolefin, and a container in which the lid is heat-sealed with an aluminum film whose innermost surface in contact with the external composition for skin is laminated with a resin containing polyolefin. And so on.
  • the external composition for skin of the present invention is contained in a tube, for example, it can be expected to have an effect that one to several drops are particularly easy to drop. Therefore, although not limited, it is preferable that a part or all of the dropping portion is composed of the polyolefin resin.
  • composition In the external composition for skin of the present invention, one or more of the above-mentioned optional components in addition to the component (A) and the component (B) and, if necessary, the component (C) are blended and mixed, and further, if necessary, others.
  • Liquid, milky liquid, cream, paste, mousse, gel, sheet (base material supported), aerosol, spray, etc. Can be prepared in various desired forms. Although not limited, it is preferable to make it liquid from the viewpoint of remarkably exerting the effect of the present application. These can be manufactured by conventional methods in the art.
  • the external composition for skin of the present invention can be prepared as a composition having an appropriate viscosity desired especially when using the external composition for skin used for application to the skin.
  • the composition for external use on the skin of the present invention may usually have a liquid property of pH 1 to 8, but is preferable from the viewpoints of stability of ascorbic acid, hypoallergenicity to the skin and mucous membranes, and good skin usability.
  • the pH is 2 to 7, more preferably pH 2 to 6, still more preferably pH 2 to 5.0, and most preferably pH 2 to 4.5. It is desirable that it is in an acidic region.
  • the external composition for skin of the present invention is particularly effective as a whitening agent, an anti-inflammatory agent, and an anti-aging agent, and has, for example, acne prevention, treatment, and antioxidative effects. Further, when applied to the skin, the transparency of the skin is enhanced, the moisture is maintained, the texture is smoothed, and the effect of suppressing roughness may be exhibited. In addition, it may have effects such as moisturizing the skin where acne scars and pores are anxious, making the pores inconspicuous, leading to smooth skin, moisturizing the skin, and for preventing and treating spots. It can also be used.
  • the external composition for skin of the present invention is, for example, basic cosmetics such as beauty liquids, lotions, sunscreen creams, milky lotions, creams, lotions, oils and packs; foundations, lipsticks, lip creams, mascara, eye shadows and eye liners. , Makeup cosmetics such as eyebrows and beautiful nails; Cleaning agents such as facial cleansers, cleansers, and body cleaning agents; It can be used as various external skin compositions belonging to the fields of cosmetics, external medicines or external pharmaceutical products such as acne therapeutic agents, hemorrhagic agents, sterilizing and disinfecting agents, whitening agents, ultraviolet protective agents and the like. From the viewpoint of the effect on the skin, the present invention is preferably used for products applied to the outer skin such as external skin preparations (formulations for the outer skin).
  • the composition of the present invention can be used once or several times a day according to the intended use and the like, in a known or commonly used dosage and administration.
  • the present invention also comprises coexistence of (A) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol so that the composition contains a resin or a resin containing a polyolefin. It also includes a method of imparting a wettability improving effect to a container molded from such a resin.
  • the contents described in the above-mentioned external composition for skin shall be applied.
  • the present invention also comprises coexistence of (A) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol so that the composition contains a resin or a resin containing a polyolefin. It also includes a method of suppressing pH fluctuation when stored in a container molded from such a resin. Since pH fluctuations are related to quality fluctuations of the composition, suppression of fluctuations leads to quality maintenance.
  • the present invention also comprises coexistence of (A) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol, so that the composition contains a resin or a resin containing a polyolefin. It also includes methods of promoting defoaming when housed in such resin-molded containers. Ingredients, especially ascorbic acid and the like, may affect stability such as coloring due to contact with air. Especially in a liquid composition, when the rate at which bubbles generated by vibration or impact disappear (defoaming rate) is slow, the chance of contact between the compounding component and air can be increased or extended. Therefore, promotion of defoaming leads to maintenance of quality of the composition.
  • Etc., and other components and their contents are the same as those described in the above-mentioned external composition for skin.
  • the unit of each component amount in the table is mass% unless otherwise specified in the table.
  • the external composition for skin having the compositions shown in Tables 1 to 13 was prepared according to a conventional method.
  • Test Example 1 Wetting property test
  • the wettability of the polyethylene resin (AS ONE: PEN-50503) and the polypropylene resin (AS ONE: PPN-05503) was evaluated by contact angle measurement.
  • a resin having a thickness of 3 mm was cut into 2 cm ⁇ 6 cm and used.
  • 0.5 ⁇ L of the test solution was dropped on the plate surface, and the contact angle was measured.
  • Each composition was measured 10 times in succession under the same temperature conditions (at room temperature) using the same container material, and evaluated by the average value. The results are shown in the table.
  • the measurement conditions for the contact angle are as follows.
  • the contact angle was increased by adding ethanol, but it was found that the composition of the example had a smaller contact angle with respect to the polyethylene resin and the wettability was improved.
  • composition of the example had a smaller contact angle with respect to the polypropylene resin and the wettability was improved as compared with the composition of the comparative example.
  • Test Example 2 A polyethylene container (AS ONE PE Spitch 10 mL (model number 2-467-02)) is filled with 9 mL of a composition containing ethanol and a polyol (propylene glycol, 1,3-propanediol or glycerin) shown in Comparative Example in the table. Then, it was subjected to aging. Specifically, it was allowed to stand at 60 ° C. for 7 days with the lid upright.
  • AS ONE PE Spitch 10 mL model number 2-467-02
  • Table 14 below shows a prescription example.
  • the prescription examples were all beauty essences, and each prescription was filled in a polyethylene resin or polypropylene resin container.
  • the content in each of the formulation examples is mass%.

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Abstract

Provided is a composition for external use on skin, which can be packed in a container easily in the production thereof and is configured such that a proper amount can be discharged upon the application onto the skin.　A composition for external use on skin is produced, which has good wettability on a polyolefin resin. The composition for external use on skin is prepared, the composition for external use on skin comprising (A) at least one component selected from the group consisting of ascorbic acid and an ascorbic acid salt and (B) a lower alcohol, and the composition for external use on skin being packed in a container in which a portion or the whole of a face that comes into contact with the composition for external use on skin comprises a resin containing a polyolefin.

Description

皮膚外用組成物External composition for skin
　本発明は、皮膚外用組成物に関する。より詳細には、アスコルビン酸及び／又はその塩及び低級アルコールを含有し、特定の容器に収容されてなる皮膚外用組成物に関する。 The present invention relates to a composition for external use on the skin. More specifically, it relates to a composition for external skin containing ascorbic acid and / or a salt thereof and a lower alcohol and contained in a specific container.
　アスコルビン酸は、抗炎症効果、ニキビ改善効果、美白効果、老化防止効果、抗酸化効果、コラーゲン等の生体成分の合成促進による細胞賦活効果、表皮角化細胞の紫外線による細胞障害やＤＮＡ損傷を抑制する効果といった各種の効果を発揮することが知られており、これらの効果を期待して皮膚外用剤として用いられている。このようなアスコルビン酸は、溶媒を含む形態で提供されている（例えば、特許文献１）。 Ascorbic acid has anti-inflammatory effect, acne improving effect, whitening effect, anti-aging effect, antioxidant effect, cell activation effect by promoting synthesis of biological components such as collagen, and suppresses cell damage and DNA damage caused by ultraviolet rays of epidermal keratinocytes. It is known to exert various effects such as the effect of collagen, and it is used as an external preparation for skin in anticipation of these effects. Such ascorbic acid is provided in a form containing a solvent (for example, Patent Document 1).
特開２００５－２２５８６５号公報Japanese Unexamined Patent Publication No. 2005-225856
　本発明は、製造の際に容器に詰めやすく、皮膚に適用する際には、適量を排出しやすい、皮膚外用組成物を提供することを目的とする。 An object of the present invention is to provide a composition for external use on the skin, which is easy to pack in a container during production and easily discharges an appropriate amount when applied to the skin.
　本発明者の検討によると、皮膚外用組成物をポリオレフィン樹脂を含む容器に収容する場合、皮膚外用組成物の容器に対する濡れ性が劣れば、製造時の充填の際に、チューブの上部壁面に細かな水滴が残りやすく、容器のシールに支障をきたすことがあり、また、使用する際に適量を排出しづらい場合があることが判明した。 According to the study of the present inventor, when the external composition for skin is housed in a container containing a polyolefin resin, if the wettability of the external composition for skin to the container is inferior, it may be applied to the upper wall surface of the tube during filling during manufacturing. It has been found that fine water droplets tend to remain, which may interfere with the sealing of the container, and it may be difficult to discharge an appropriate amount when using.
　本発明者は、本課題を解決すべく鋭意検討を重ねた結果、（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種、及び（Ｂ）低級アルコールを含有させることで、該組成物に、ポリオレフィンを含有する樹脂に対する濡れ性向上作用、保存によるｐＨ変動抑制作用、及び消泡促進作用が得られることを見出し、本発明を完成するに至った。 As a result of diligent studies to solve this problem, the present inventor contains at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol. Therefore, they have found that the composition can have an effect of improving wettability with respect to a resin containing polyolefin, an effect of suppressing pH fluctuation by storage, and an effect of promoting defoaming, and have completed the present invention.
　すなわち、本発明は、下記に掲げる皮膚外用組成物を提供する。
　項１．
　（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種、及び（Ｂ）低級アルコールを含有する皮膚外用組成物であって、
　該皮膚外用組成物と接触する面の一部又は全部が、ポリオレフィンを含有する樹脂を含む容器に収容してなる皮膚外用組成物。
　項２．
　前記（Ｂ）成分の総含有量が、１～７質量％である、項１に記載の皮膚外用組成物。
　項３．
　さらに、以下の（Ｃ－１）、（Ｃ－２）、（Ｃ－３）、及び（Ｃ－４）からなる群より選択される少なくとも１種を含有する、項１又は２のいずれか１項に記載の皮膚外用組成物：
（Ｃ－１）ピリドキシン及び／又はその塩；
（Ｃ－２）サリチル酸、サリチル酸の誘導体、及びそれらの塩からなる群より選択される少なくとも１種；
（Ｃ－３）イソプロピルメチルフェノール；
（Ｃ－４）アスコルビン酸誘導体。
　項４．
　前記（Ｂ）成分が、少なくともエタノールを含む、項１～３のいずれか１項に記載の皮膚外用組成物。
　項５．
　前記（Ａ）成分の総含有量が、０．５～３０質量％である、項１～４のいずれか１項に記載の皮膚外用組成物。
　項６．
　前記容器がチューブタイプ、パウチパック、又はチアパックである、項１～５のいずれか１項に記載の皮膚外用組成物。 That is, the present invention provides the composition for external use on the skin listed below.
Item 1.
A composition for external use on the skin containing (A) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol.
A composition for external skin, wherein a part or all of the surface in contact with the external composition for skin is housed in a container containing a resin containing polyolefin.
Item 2.
Item 2. The composition for external use on the skin according to Item 1, wherein the total content of the component (B) is 1 to 7% by mass.
Item 3.
Further, any one of Items 1 or 2 containing at least one selected from the group consisting of the following (C-1), (C-2), (C-3), and (C-4). The composition for external use of the skin according to the section:
(C-1) Pyridoxine and / or a salt thereof;
(C-2) At least one selected from the group consisting of salicylic acid, salicylic acid derivatives, and salts thereof;
(C-3) Isopropylmethylphenol;
(C-4) Ascorbic acid derivative.
Item 4.
Item 6. The composition for external use on the skin according to any one of Items 1 to 3, wherein the component (B) contains at least ethanol.
Item 5.
Item 6. The composition for external use on the skin according to any one of Items 1 to 4, wherein the total content of the component (A) is 0.5 to 30% by mass.
Item 6.
Item 6. The composition for external use on the skin according to any one of Items 1 to 5, wherein the container is a tube type, a pouch pack, or a cheer pack.
　さらに、本発明は、以下の方法を提供する。
　項７．
　組成物中に、（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種、及び（Ｂ）低級アルコールを共存させることで、該組成物に、ポリオレフィンを含有する樹脂に対する濡れ性向上作用を付与する方法。 Furthermore, the present invention provides the following methods.
Item 7.
By allowing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid and (B) a lower alcohol to coexist in the composition, the resin containing the polyolefin in the composition is allowed to coexist. A method of imparting a wettability improving effect.
　本発明により、ポリオレフィンを含有する樹脂に対する濡れ性が良好で、安定な皮膚外用組成物を提供することができる。 INDUSTRIAL APPLICABILITY According to the present invention, it is possible to provide a stable composition for external use on the skin, which has good wettability to a resin containing a polyolefin.
　本明細書において、含有量の単位「質量％」は、「ｇ／１００ｇ」と同義である。 In the present specification, the unit of content "mass%" is synonymous with "g / 100g".
[皮膚外用組成物]
　本発明の皮膚外用組成物は、
　（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種、及び（Ｂ）低級アルコールを含有する皮膚外用組成物であって、
　該皮膚外用組成物と接触する面の一部又は全部が、ポリオレフィンを含有する樹脂を含む容器に収容してなる皮膚外用組成物である。 [External skin composition]
The external composition for skin of the present invention is
A composition for external use on the skin containing (A) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol.
The external composition for skin is a composition in which a part or all of the surface in contact with the external composition for skin is contained in a container containing a resin containing polyolefin.
(（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種)
　本発明に用いられるアスコルビン酸としては、医薬品、医薬部外品又は化粧品分野において皮膚外用剤の成分として用いられるアスコルビン酸を使用することができ、これらは、限定はされないが、通常Ｌ体のものを指す。 (At least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid)
As the ascorbic acid used in the present invention, ascorbic acid used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics can be used, and these are usually L-form, although not limited. Point to.
　アスコルビン酸の塩も使用できる。ここで、アスコルビン酸の塩とは、薬学上許容される塩である。限定はされないが、例えば、有機塩基との塩（例えば、トリメチルアミン塩、トリエチルアミン塩、モノエタノールアミン塩、トリエタノールアミン塩、ピリジン塩等の第３級アミンとの塩、アルギニン等の塩基性アンモニウム塩等）、無機塩基との塩（例えば、アンモニウム塩、ナトリウム塩、カリウム塩等のアルカリ金属塩、カルシウム塩、マグネシウム塩等のアルカリ土類金属塩、アルミニウム塩等）等が例示される。好ましいアスコルビン酸の塩は、ナトリウム塩、カリウム塩である。 Ascorbic acid salt can also be used. Here, the salt of ascorbic acid is a pharmaceutically acceptable salt. Although not limited, for example, a salt with an organic base (for example, a salt with a tertiary amine such as a trimethylamine salt, a triethylamine salt, a monoethanolamine salt, a triethanolamine salt, a pyridine salt, a basic ammonium salt such as arginine). Etc.), salts with inorganic bases (eg, alkali metal salts such as ammonium salt, sodium salt, potassium salt, alkaline earth metal salt such as calcium salt, magnesium salt, aluminum salt, etc.) and the like are exemplified. Preferred ascorbic acid salts are sodium salts and potassium salts.
　本発明において、アスコルビン酸又はその塩は、１種類又は２種類以上を組み合わせて使用できる。本発明の効果を顕著に奏する観点から、アスコルビン酸が好ましい。（Ａ）アスコルビン酸又はその塩は合成して用いてもよく、市販品を用いてもよい。 In the present invention, ascorbic acid or a salt thereof can be used alone or in combination of two or more. Ascorbic acid is preferable from the viewpoint of remarkably exerting the effect of the present invention. (A) Ascorbic acid or a salt thereof may be synthesized and used, or a commercially available product may be used.
　本発明の皮膚外用組成物において、皮膚外用組成物の全量に対する（Ａ）成分の総含有量は、他の成分とのバランスによって適宜設定される。皮膚外用組成物の全量に対する、
（Ａ）成分の総含有量は、好ましくは、３０質量％以下であり、より好ましくは１０質量％以下、さらに好ましくは９質量％以下、さらにより好ましくは５質量％以下である。皮膚外用組成物の全量に対する、（Ａ）成分の総含有量は、好ましくは、０．５質量％以上であり、より好ましくは、１質量％以上であり、さらに好ましくは２質量％以上であり、さらにより好ましくは３質量％以上である。皮膚外用組成物の全量に対する、（Ａ）成分の総含有量は、好ましくは、０．５～３０質量％、より好ましくは１～１０質量％、さらに好ましくは、２～９質量％、さらにより好ましくは３～５質量％であり、１～５質量％、１～３質量％、３～５質量％、３質量％であってもよい。 In the external composition for skin of the present invention, the total content of the component (A) with respect to the total amount of the external composition for skin is appropriately set by the balance with other components. For the total amount of external skin composition
The total content of the component (A) is preferably 30% by mass or less, more preferably 10% by mass or less, still more preferably 9% by mass or less, still more preferably 5% by mass or less. The total content of the component (A) with respect to the total amount of the external composition for skin is preferably 0.5% by mass or more, more preferably 1% by mass or more, still more preferably 2% by mass or more. , Even more preferably 3% by mass or more. The total content of the component (A) with respect to the total amount of the external composition for skin is preferably 0.5 to 30% by mass, more preferably 1 to 10% by mass, still more preferably 2 to 9% by mass, and even more. It is preferably 3 to 5% by mass, and may be 1 to 5% by mass, 1 to 3% by mass, 3 to 5% by mass, or 3% by mass.
（（Ｂ）低級アルコール）
　本発明に用いられる低級アルコールとしては、医薬品、医薬部外品又は化粧品分野において皮膚外用剤の成分として用いられるものであれば限定されない。本明細書において、「低級アルコール」というときは、Ｃ１－Ｃ６のアルコールを指し、そのうち、Ｃ１－Ｃ３のアルコールを好ましく用いることができる。このような例として、メタノール、エタノール、ｎ－プロパノール、イソプロパノール等が挙げられる。さらに、本発明に用いられる低級アルコールは、特に好ましくは、少なくともエタノールを含むかエタノールである。 ((B) Lower alcohol)
The lower alcohol used in the present invention is not limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics. In the present specification, the term "lower alcohol" refers to alcohols of C1 - C6 , of which alcohols of C1 - C3 can be preferably used. Examples of such examples include methanol, ethanol, n-propanol, isopropanol and the like. Furthermore, the lower alcohol used in the present invention particularly preferably contains or is at least ethanol.
　本発明の皮膚外用組成物において、皮膚外用組成物の全量に対する（Ｂ）成分の総含有量は、好ましくは、０．１～２０質量％、より好ましくは０．５～１０質量％、さらに好ましくは０．５～７質量％、さらにより好ましくは１～７質量％、特に好ましく１～５質量％である。また、０．５～５質量％、０．５～３質量％、２～５質量％、２～３質量％などであってもよい。 In the external composition for skin of the present invention, the total content of the component (B) with respect to the total amount of the external composition for skin is preferably 0.1 to 20% by mass, more preferably 0.5 to 10% by mass, still more preferably. Is 0.5 to 7% by mass, more preferably 1 to 7% by mass, and particularly preferably 1 to 5% by mass. Further, it may be 0.5 to 5% by mass, 0.5 to 3% by mass, 2 to 5% by mass, 2 to 3% by mass, or the like.
　また、限定はされないが、典型的には、本発明の皮膚外用組成物において、皮膚外用組成物の全量に対するエタノールの量は、好ましくは、０．１～２０質量％、より好ましくは０．５～１０質量％、さらに好ましくは、１～７質量％である。 In addition, although not limited, typically, in the external composition for skin of the present invention, the amount of ethanol with respect to the total amount of the external composition for skin is preferably 0.1 to 20% by mass, more preferably 0.5. It is -10% by mass, more preferably 1 to 7% by mass.
　本発明の皮膚外用組成物において、（Ａ）成分に対する（Ｂ）成分の配合量の比率は、
（Ａ）成分の総含有量１質量部に対して、０．００３～４０質量部が好ましく、０．０５～１０質量部がより好ましく、０．２～２．５質量部がさらに好ましい。 In the external composition for skin of the present invention, the ratio of the blending amount of the component (B) to the component (A) is
(A) With respect to 1 part by mass of the total content of the component, 0.003 to 40 parts by mass is preferable, 0.05 to 10 parts by mass is more preferable, and 0.2 to 2.5 parts by mass is further preferable.
　本発明の皮膚外用組成物は、上記（Ａ）成分及び（Ｂ）成分の他に、さらに、以下の（Ｃ－１）、（Ｃ－２）、（Ｃ－３）、及び（Ｃ－４）からなる群より選択される少なくとも１種を含有していても良い。
（Ｃ－１）ピリドキシン及び／又はその塩；
（Ｃ－２）サリチル酸、サリチル酸の誘導体、及びそれらの塩からなる群より選択される少なくとも１種；
（Ｃ－３）イソプロピルメチルフェノール；
（Ｃ－４）アスコルビン酸誘導体。 In addition to the above components (A) and (B), the external composition for skin of the present invention further comprises the following (C-1), (C-2), (C-3), and (C-4). ) May contain at least one selected from the group consisting of.
(C-1) Pyridoxine and / or a salt thereof;
(C-2) At least one selected from the group consisting of salicylic acid, salicylic acid derivatives, and salts thereof;
(C-3) Isopropylmethylphenol;
(C-4) Ascorbic acid derivative.
（（Ｃ－１）ピリドキシン及び／又はその塩）
　本発明に用いられるピリドキシン及び／又はその塩としては、医薬品、医薬部外品又は化粧品分野において皮膚外用剤の成分として用いられるものであれば特に限定されない。 ((C-1) Pyridoxine and / or a salt thereof)
The pyridoxine and / or a salt thereof used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics.
　ピリドキシンの塩とは、薬学上許容される塩である。限定はされないが、例えば、ピリドキシン塩酸塩が例示される。 Pyridoxine salt is a pharmaceutically acceptable salt. For example, but not limited to, pyridoxine hydrochloride is exemplified.
　本発明において、ピリドキシン又はその塩は、１種類又は２種類以上を組み合わせて使用できる。本発明の効果を顕著に奏する観点から、ピリドキシン塩酸塩が好ましい。ピリドキシン又はその塩は合成して用いてもよく、市販品を用いてもよい。 In the present invention, pyridoxine or a salt thereof can be used alone or in combination of two or more. Pyridoxine hydrochloride is preferable from the viewpoint of remarkably exerting the effect of the present invention. Pyridoxine or a salt thereof may be used synthetically, or a commercially available product may be used.
　本発明の皮膚外用組成物において、皮膚外用組成物の全量に対する（Ｃ－１）成分の総含有量は、限定はされないが、好ましくは、０．００１質量％以上であり、より好ましくは０．００５質量％以上、さらに好ましくは０．０１質量％以上である。
　皮膚外用組成物の全量に対する（Ｃ－１）成分の総含有量は、限定はされないが、好ましくは、１質量％以下であり、より好ましくは、０．５質量％以下、さらに好ましくは、０．１質量％以下である。 In the external composition for skin of the present invention, the total content of the component (C-1) with respect to the total amount of the external composition for skin is not limited, but is preferably 0.001% by mass or more, more preferably 0. It is 005% by mass or more, more preferably 0.01% by mass or more.
The total content of the component (C-1) with respect to the total amount of the external composition for skin is not limited, but is preferably 1% by mass or less, more preferably 0.5% by mass or less, still more preferably 0. .1% by mass or less.
　皮膚外用組成物の全量に対する（Ｃ－１）成分の総含有量は、好ましくは０．００１～１質量％、好ましくは、０．００５～０．５質量％、さらに好ましくは、０．０１～０．１質量％である。 The total content of the component (C-1) with respect to the total amount of the external composition for skin is preferably 0.001 to 1% by mass, preferably 0.005 to 0.5% by mass, and more preferably 0.01 to 0.01. It is 0.1% by mass.
　本発明の皮膚外用組成物において、（Ａ）成分に対する（Ｃ－１）成分の配合量の比率は特に限定されないが、（Ａ）成分の総含有量１質量部に対して、０．００００３～２質量部が好ましく、０．０００５～０．５質量部がより好ましく、０．００２～０．０４質量部がさらに好ましい。 In the composition for external use on the skin of the present invention, the ratio of the blending amount of the component (C-1) to the component (A) is not particularly limited, but is 0.00003 to 1 part by mass of the total content of the component (A). 2 parts by mass is preferable, 0.0005 to 0.5 parts by mass is more preferable, and 0.002 to 0.04 parts by mass is further preferable.
（（Ｃ－２）サリチル酸、サリチル酸の誘導体、及びそれらの塩からなる群より選択される少なくとも１種）
　本発明に用いられるサリチル酸、サリチル酸の誘導体、及びそれらの塩としては、医薬品、医薬部外品又は化粧品分野において皮膚外用剤の成分として用いられるものであれば特に限定されない。 ((C-2) At least one selected from the group consisting of salicylic acid, salicylic acid derivatives, and salts thereof)
The salicylic acid, the derivative of salicylic acid, and the salt thereof used in the present invention are not particularly limited as long as they are used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs, and cosmetics.
　サリチル酸の誘導体としては、限定はされないが、例えば、サリチル酸エチレングリコール、サリチル酸フェニル、サリチル酸メチル、サリチル酸２－エチルヘキシル、サリチル酸ジプロピレングリコール、サリチル酸Ｔｉ等が含まれる。 Derivatives of salicylic acid include, but are not limited to, ethylene glycol salicylate, phenyl salicylate, methyl salicylate, 2-ethylhexyl salicylate, dipropylene glycol salicylate, Ti salicylate and the like.
　ここで、サリチル酸或いはサリチル酸の誘導体の塩とは、薬学上許容される塩である。限定はされないが、例えば、アルカリ金属塩、アルカリ土類金属塩、有機塩基等との塩等が例示される。サリチル酸塩は、例えば、サリチル酸ナトリウム、サリチル酸カルシウム、サリチル酸マグネシウム及びサリチル酸カリウムからなる群より選択される少なくとも１種が挙げられる。 Here, the salt of salicylic acid or a derivative of salicylic acid is a pharmaceutically acceptable salt. Examples thereof include, but are not limited to, alkali metal salts, alkaline earth metal salts, salts with organic bases, and the like. Examples of the salicylate include at least one selected from the group consisting of sodium salicylate, calcium salicylate, magnesium salicylate and potassium salicylate.
　本発明において、サリチル酸、サリチル酸の誘導体、及びそれらの塩は、１種類又は２種類以上を組み合わせて使用できる。本発明の効果を顕著に奏する観点から、サリチル酸、サリチル酸ナトリウム、サリチル酸カルシウム、サリチル酸マグネシウム及びサリチル酸カリウムからなる群より選択される少なくとも１種が好ましく、サリチル酸及び／又はサリチル酸ナトリウムがより好ましい。サリチル酸、サリチル酸の誘導体、及びそれらの塩は、合成して用いてもよく、市販品を用いてもよい。 In the present invention, salicylic acid, salicylic acid derivatives, and salts thereof can be used alone or in combination of two or more. From the viewpoint of remarkably exerting the effect of the present invention, at least one selected from the group consisting of salicylic acid, sodium salicylate, calcium salicylate, magnesium salicylate and potassium salicylate is preferable, and salicylic acid and / or sodium salicylate is more preferable. Salicylic acid, derivatives of salicylic acid, and salts thereof may be used synthetically or commercially available products.
　本発明の皮膚外用組成物において、皮膚外用組成物の全量に対する（Ｃ－２）成分の総含有量は、限定はされないが、好ましくは、０．００００２質量％以上であり、より好ましくは０．０００５質量％以上、さらに好ましくは０．０５質量％以上である。
　皮膚外用組成物の全量に対する（Ｃ－２）成分の総含有量は、限定はされないが、好ましくは、５質量％以下であり、より好ましくは、１質量％以下、さらに好ましくは、０．５質量％以下、さらにより好ましくは０．２質量％以下である。 In the external composition for skin of the present invention, the total content of the component (C-2) with respect to the total amount of the external composition for skin is not limited, but is preferably 0.00002% by mass or more, more preferably 0. It is 0005% by mass or more, more preferably 0.05% by mass or more.
The total content of the component (C-2) with respect to the total amount of the external composition for skin is not limited, but is preferably 5% by mass or less, more preferably 1% by mass or less, still more preferably 0.5. It is 0% by mass or less, and more preferably 0.2% by mass or less.
　皮膚外用組成物の全量に対する（Ｃ－２）成分の総含有量は、好ましくは０．００００２～５質量％、好ましくは、０．０００５～１質量％、さらに好ましくは、０．０５～０．５質量％である。 The total content of the component (C-2) with respect to the total amount of the external composition for skin is preferably 0.00002 to 5% by mass, preferably 0.0005 to 1% by mass, and more preferably 0.05 to 0. It is 5% by mass.
　本発明の皮膚外用組成物において、（Ａ）成分に対する（Ｃ－２）成分の配合量の比率は特に限定されないが、（Ａ）成分の総含有量１質量部に対して、０．００００００６～１０質量部が好ましく、０．００００５～１質量部がより好ましく、０．０１～０．２質量部がさらに好ましい。 In the composition for external use on the skin of the present invention, the ratio of the blending amount of the component (C-2) to the component (A) is not particularly limited, but is 0.0000006 to 1 part by mass of the total content of the component (A). 10 parts by mass is preferable, 0.00005 to 1 part by mass is more preferable, and 0.01 to 0.2 parts by mass is further preferable.
（（Ｃ－３）イソプロピルメチルフェノール）
　本発明に用いられるイソプロピルメチルフェノールとしては、医薬品、医薬部外品又は化粧品分野において皮膚外用剤の成分として用いられるものであれば特に限定されない。イソプロピルメチルフェノールは殺菌作用を有する。 ((C-3) Isopropylmethylphenol)
The isopropylmethylphenol used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics. Isopropylmethylphenol has a bactericidal action.
　イソプロピルメチルフェノールは、合成して用いてもよく、市販品を用いてもよい。 Isopropylmethylphenol may be synthesized and used, or a commercially available product may be used.
　本発明の皮膚外用組成物において、皮膚外用組成物の全量に対する（Ｃ－３）成分の含有量は、限定はされないが、好ましくは、０．００１質量％以上であり、より好ましくは０．００５質量％以上、さらに好ましくは０．０１質量％以上である。
　皮膚外用組成物の全量に対する（Ｃ－３）成分の含有量は、限定はされないが、好ましくは、５質量％以下であり、より好ましくは、１質量％以下、さらに好ましくは、０．１質量％以下である。 In the external composition for skin of the present invention, the content of the component (C-3) with respect to the total amount of the external composition for skin is not limited, but is preferably 0.001% by mass or more, more preferably 0.005. It is by mass or more, more preferably 0.01% by mass or more.
The content of the component (C-3) with respect to the total amount of the external composition for skin is not limited, but is preferably 5% by mass or less, more preferably 1% by mass or less, still more preferably 0.1% by mass. % Or less.
　皮膚外用組成物の全量に対する（Ｃ－３）成分の含有量は、好ましくは０．００１～５質量％、好ましくは、０．００５～１質量％、さらに好ましくは、０．０１～０．１質量％である。 The content of the component (C-3) with respect to the total amount of the external composition for skin is preferably 0.001 to 5% by mass, preferably 0.005 to 1% by mass, and more preferably 0.01 to 0.1. It is mass%.
　本発明の皮膚外用組成物において、（Ａ）成分に対する（Ｃ－３）成分の配合量の比率は特に限定されないが、（Ａ）成分の総含有量１質量部に対して、０.００００３～１０質量部が好ましく、０．０００５～１質量部がより好ましく、０．００２～０．０４質量部がさらに好ましい。 In the composition for external use on the skin of the present invention, the ratio of the blending amount of the component (C-3) to the component (A) is not particularly limited, but is 0.000003 to 1 part by mass of the total content of the component (A). 10 parts by mass is preferable, 0.0005 to 1 part by mass is more preferable, and 0.002 to 0.04 parts by mass is further preferable.
（（Ｃ－４）アスコルビン酸誘導体）
　本発明に用いられるアスコルビン酸誘導体としては、医薬品、医薬部外品又は化粧品分野において皮膚外用剤の成分として用いられるものであれば特に限定されない。３－Ｏ－エチルアスコルビン酸、Ｌ－アスコルビン酸２－グルコシド、テトラ２－ヘキシルデカン酸アスコルビル、デヒドロアスコルビン酸、アスコルビン酸リン酸エステルナトリウム、アスコルビン酸リン酸エステルマグネシウム、アスコルビン酸モノリン酸エステルナトリウム、アスコルビン酸ジリン酸エステルナトリウム、アスコルビン酸トリリン酸エステルナトリウム、アスコルビン酸－２－硫酸エステルナトリウム、又はそれらの塩等が例示される。 ((C-4) Ascorbic acid derivative)
The ascorbic acid derivative used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics. 3-O-ethylascorbic acid, L-ascorbic acid 2-glucoside, tetra2-hexyldecanoic acid ascorbyl, dehydroascorbic acid, ascorbic acid phosphate sodium, ascorbic acid phosphate ester magnesium, ascorbic acid monophosphate ester sodium, ascorbic acid Examples thereof include sodium diphosphate ester, sodium ascorbic acid triphosphate ester, sodium ascorbic acid-2-sulfate ester, and salts thereof.
　ここで、塩とは、薬学上許容される塩である。限定はされないが、例えば、有機塩基との塩（例えば、トリメチルアミン塩、トリエチルアミン塩、モノエタノールアミン塩、トリエタノールアミン塩、ピリジン塩等の第３級アミンとの塩、アルギニン等の塩基性アンモニウム塩等）、無機塩基との塩（例えば、アンモニウム塩、ナトリウム塩、カリウム塩等のアルカリ金属塩、カルシウム塩、マグネシウム塩等のアルカリ土類金属塩、アルミニウム塩等）等が例示される。特に好ましい３－Ｏ－エチルアスコルビン酸の塩は、ナトリウム塩、カリウム塩である。 Here, the salt is a pharmaceutically acceptable salt. Although not limited, for example, a salt with an organic base (for example, a salt with a tertiary amine such as a trimethylamine salt, a triethylamine salt, a monoethanolamine salt, a triethanolamine salt, a pyridine salt, a basic ammonium salt such as arginine). Etc.), salts with inorganic bases (eg, alkali metal salts such as ammonium salt, sodium salt, potassium salt, alkaline earth metal salt such as calcium salt, magnesium salt, aluminum salt, etc.) and the like are exemplified. Particularly preferred salts of 3-O-ethylascorbic acid are sodium salts and potassium salts.
　本発明において、アスコルビン酸誘導体は、１種類又は２種類以上を組み合わせて使用できる。本発明の効果を顕著に奏する観点から、３－Ｏ－エチルアスコルビン酸又はＬ－アスコルビン酸２－グルコシドが好ましい。アスコルビン酸誘導体は、合成して用いてもよく、市販品を用いてもよい。 In the present invention, the ascorbic acid derivative can be used alone or in combination of two or more. From the viewpoint of remarkably exerting the effect of the present invention, 3-O-ethylascorbic acid or L-ascorbic acid 2-glucoside is preferable. The ascorbic acid derivative may be synthesized and used, or a commercially available product may be used.
　本発明の皮膚外用組成物において、皮膚外用組成物の全量に対する（Ｃ－４）成分の総含有量は、好ましくは０．０００１～１０質量％、より好ましくは、０．０００５～５質量％、さらに好ましくは、０．００１～２質量％である。０．０００１～２質量％であってもよい。 In the external composition for skin of the present invention, the total content of the component (C-4) with respect to the total amount of the external composition for skin is preferably 0.0001 to 10% by mass, more preferably 0.0005 to 5% by mass. More preferably, it is 0.001 to 2% by mass. It may be 0.0001 to 2% by mass.
　本発明の皮膚外用組成物において、（Ａ）成分に対する（Ｃ－４）成分の配合量の比率は特に限定されないが、（Ａ）成分の総含有量１質量部に対して、０．００００５～５質量部が好ましく、０．０００２～０．７質量部がより好ましい。 In the composition for external use on the skin of the present invention, the ratio of the blending amount of the component (C-4) to the component (A) is not particularly limited, but is 0.00005 to 1 part by mass of the total content of the component (A). 5 parts by mass is preferable, and 0.0002 to 0.7 parts by mass is more preferable.
（多価アルコール）
　本発明の皮膚外用組成物は、本発明の効果を妨げない限り、上記（Ａ）成分及び（Ｂ）成分の他に、多価アルコールを含んでいてもよい。 (Multivalent alcohol)
The composition for external use on the skin of the present invention may contain a polyhydric alcohol in addition to the above-mentioned components (A) and (B) as long as the effects of the present invention are not impaired.
　本発明に用いられる多価アルコールとしては、医薬品、医薬部外品又は化粧品分野において皮膚外用剤の成分として用いられるものであれば特に限定されない。多価アルコールは、限定はされないが、保湿のため又は可溶化剤として加える場合もある。好ましい多価アルコールは、炭素数３個のジオールであるが、限定はされない。この他に、グリセリン、ジグリセリン、ジプロピレングリコール、１、３－ブチレングリコール、３-メチル-１,３-ブタンジオール等が例示される。本発明において、多価アルコールは、１種類又は２種類以上を組み合わせて使用できる。 The polyhydric alcohol used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics. Polyhydric alcohols may be added, but not limited to, for moisturizing or as a solubilizer. A preferred polyhydric alcohol is a diol having 3 carbon atoms, but is not limited. In addition, glycerin, diglycerin, dipropylene glycol, 1,3-butylene glycol, 3-methyl-1,3-butanediol and the like are exemplified. In the present invention, the polyhydric alcohol can be used alone or in combination of two or more.
　本発明の皮膚外用組成物の全量に対する多価アルコールの総含有量は、含まれる場合は、好ましくは０．１～６０質量％、より好ましくは、１～５０質量％、さらに好ましくは、１０～４５質量％程度である。 When contained, the total content of the polyhydric alcohol with respect to the total amount of the external composition for skin of the present invention is preferably 0.1 to 60% by mass, more preferably 1 to 50% by mass, still more preferably 10 to 10 to It is about 45% by mass.
　本発明の皮膚外用組成物において、（Ａ）成分に対する多価アルコールの配合量の比率は特に限定されないが、（Ａ）成分の総含有量１質量部に対して、０．００３～１２０質量部が好ましく、０．１～５０質量部がより好ましく、２～１５質量部がさらに好ましい。 In the composition for external use on the skin of the present invention, the ratio of the compounding amount of the polyhydric alcohol to the component (A) is not particularly limited, but 0.003 to 120 parts by mass with respect to 1 part by mass of the total content of the component (A). Is preferable, 0.1 to 50 parts by mass is more preferable, and 2 to 15 parts by mass is further preferable.
(炭素数３個のジオール)
　本発明に用いられる炭素数３個のジオールとしては、医薬品、医薬部外品又は化粧品分野において皮膚外用剤の成分として用いられるものであれば特に限定されない。また、このような炭素数３個のジオールは、市販品をそのまま用いることもできる。炭素数３個のジオールとしては、限定はされないが、例えば、１、３-プロパンジオール（ＣＡＳ番号：５０４－６３－２、英名：１，３-Ｄｉｈｙｄｒｏｘｙｐｒｏｐａｎｅ又はＴｒｉｍｅｔｈｙｌｅｎｅＧｌｙｃｏｌ）又はプロピレングリコール（ＣＡＳ番号：５７－５５－６、英名：１，２－Ｄｉｈｙｄｒｏｘｙｐｒｏｐａｎｅ、和名別名：１，２-プロパンジオール）が例示でき、１種類を使用しても、適宜組み合わせて使用してもよい。１、３-プロパンジオール及びプロピレングリコールを組み合わせることも好ましい態様の一つであり、炭素数３個のジオールとして、少なくとも１、３-プロパンジオールを含むことがより好ましい。 (Glycol with 3 carbon atoms)
The diol having 3 carbon atoms used in the present invention is not particularly limited as long as it is used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics. Further, as such a diol having 3 carbon atoms, a commercially available product can be used as it is. The diol having 3 carbon atoms is not limited, but is, for example, 1,3-propanediol (CAS number: 504-63-2, English name: 1,3-Dihydroxypropane or TrimethyleneGlycol) or propylene glycol (CAS number: 57). -55-6, English name: 1,2-Dihydroxypropane, Japanese name alias: 1,2-propanediol) can be exemplified, and one type may be used or may be used in combination as appropriate. A combination of 1,3-propanediol and propylene glycol is also one of the preferred embodiments, and it is more preferable to include at least 1,3-propanediol as the diol having 3 carbon atoms.
　本発明の皮膚外用組成物において、皮膚外用組成物の全量に対する炭素数３個のジオールの総含有量は、１質量％以上であり、好ましくは、５質量％以上、より好ましくは、１０質量％以上である。
　皮膚外用組成物の全量に対する炭素数３個のジオールの総含有量は、５０質量％以下であり、好ましくは、４０質量％以下、さらに好ましくは、３０質量％以下である。 In the external composition for skin of the present invention, the total content of the diol having 3 carbon atoms with respect to the total amount of the external composition for skin is 1% by mass or more, preferably 5% by mass or more, and more preferably 10% by mass. That is all.
The total content of the diol having 3 carbon atoms with respect to the total amount of the external composition for skin is 50% by mass or less, preferably 40% by mass or less, and more preferably 30% by mass or less.
　皮膚外用組成物の全量に対する炭素数３個のジオールの総含有量は、１～５０質量％、好ましくは、５～４０質量％、さらに好ましくは、１０～３０質量％である。 The total content of the diol having 3 carbon atoms with respect to the total amount of the external composition for skin is 1 to 50% by mass, preferably 5 to 40% by mass, and more preferably 10 to 30% by mass.
　本発明の皮膚外用組成物において、（Ａ）成分に対する炭素数３個のジオールの配合量の比率は特に限定されないが、（Ａ）成分の総含有量１質量部に対して、０．００３～１２０質量部が好ましく、０．１～５０質量部がより好ましく、２～１５質量部がさらに好ましい。 In the external composition for skin of the present invention, the ratio of the blending amount of the diol having 3 carbon atoms to the component (A) is not particularly limited, but is 0.003 to 0.003 with respect to 1 part by mass of the total content of the component (A). 120 parts by mass is preferable, 0.1 to 50 parts by mass is more preferable, and 2 to 15 parts by mass is further preferable.
　炭素数３個のジオールのうち、プロピレングリコールの配合量は、皮膚外用組成物の全量に対して、好ましくは、１質量％以上、より好ましくは、５質量％以上、さらに好ましくは、１０質量％以上である。プロピレングリコールの配合量は、好ましくは、４０質量％以下、より好ましくは、３０質量％以下、さらに好ましくは、２０質量％以下、さらにより好ましくは、１０質量％以下である。 Of the diols having 3 carbon atoms, the blending amount of propylene glycol is preferably 1% by mass or more, more preferably 5% by mass or more, still more preferably 10% by mass, based on the total amount of the external composition for skin. That is all. The blending amount of propylene glycol is preferably 40% by mass or less, more preferably 30% by mass or less, still more preferably 20% by mass or less, still more preferably 10% by mass or less.
　皮膚外用組成物の全量に対するプロピレングリコールの総含有量は、１～４０質量％、好ましくは、５～３０質量％、さらに好ましくは、１０～２０質量％である。 The total content of propylene glycol with respect to the total amount of the external composition for skin is 1 to 40% by mass, preferably 5 to 30% by mass, and more preferably 10 to 20% by mass.
　本発明の皮膚外用組成物において、（Ａ）成分に対するプロピレングリコールの配合量の比率は特に限定されないが、（Ａ）成分の総含有量１質量部に対して、０．０３～８０質量部が好ましく、０．５～３０質量部がより好ましく、１～１０質量部がさらに好ましく、２～７質量部がさらにより好ましい。 In the composition for external use on the skin of the present invention, the ratio of the blending amount of propylene glycol to the component (A) is not particularly limited, but 0.03 to 80 parts by mass is based on 1 part by mass of the total content of the component (A). Preferably, 0.5 to 30 parts by mass is more preferable, 1 to 10 parts by mass is further preferable, and 2 to 7 parts by mass is even more preferable.
　炭素数３個のジオールのうち、１、３-プロパンジオールの配合量は、皮膚外用組成物の全量に対して、好ましくは、１質量％以上、より好ましくは、５質量％以上、さらに好ましくは、１０質量％以上である。１、３-プロパンジオールの配合量は３０質量％以下、より好ましくは２５質量％以下、さらに好ましくは２０質量％以下、さらにより好ましくは１５質量％以下である。 Of the diols having 3 carbon atoms, the blending amount of 1,3-propanediol is preferably 1% by mass or more, more preferably 5% by mass or more, still more preferably, based on the total amount of the external composition for skin. It is 10% by mass or more. The blending amount of 1,3-propanediol is 30% by mass or less, more preferably 25% by mass or less, still more preferably 20% by mass or less, still more preferably 15% by mass or less.
　皮膚外用組成物の全量に対する１、３-プロパンジオールの総含有量は、１～３０質量％、好ましくは、５～２０質量％、さらに好ましくは、１０～１５質量％である。 The total content of 1,3-propanediol with respect to the total amount of the external composition for skin is 1 to 30% by mass, preferably 5 to 20% by mass, and more preferably 10 to 15% by mass.
　本発明の皮膚外用組成物において、（Ａ）成分に対する１、３-プロパンジオールの配合量の比率は特に限定されないが、（Ａ）成分の総含有量１質量部に対して、０．０３～６０質量部が好ましく、０．５～２０質量部がより好ましく、１～７．５質量部がさらに好ましく、２～５質量部がさらにより好ましい。 In the composition for external use on the skin of the present invention, the ratio of the blending amount of 1,3-propanediol to the component (A) is not particularly limited, but 0.03 to 0.03 to 1 part by mass of the total content of the component (A). 60 parts by mass is preferable, 0.5 to 20 parts by mass is more preferable, 1 to 7.5 parts by mass is further preferable, and 2 to 5 parts by mass is even more preferable.
（水）
　本発明の皮膚外用組成物は、本発明の効果を妨げない限り、上記（Ａ）成分及び（Ｂ）成分の他に、水を含んでいてもよい。限定はされないが、皮膚外用組成物の全量に対する水の含有量は、好ましくは、０．１～３０質量％、より好ましくは、１～２０質量％、さらに好ましくは２～１５質量％である。０．１～９０質量％、０．５～８０質量％、１～７０質量％、２～６０質量％などであってもよい。 (water)
The composition for external use on the skin of the present invention may contain water in addition to the above-mentioned components (A) and (B) as long as the effects of the present invention are not impaired. Although not limited, the content of water with respect to the total amount of the external composition for skin is preferably 0.1 to 30% by mass, more preferably 1 to 20% by mass, still more preferably 2 to 15% by mass. It may be 0.1 to 90% by mass, 0.5 to 80% by mass, 1 to 70% by mass, 2 to 60% by mass, or the like.
（ビタミンＥ類）
　本発明の皮膚外用組成物は、本発明の効果を妨げない限り、上記（Ａ）成分及び（Ｂ）成分の他に、トコフェロール、トコフェロールの塩、及びトコフェロールの誘導体等のビタミンＥ類を含んでいてもよい。本発明に用いられるトコフェロール、トコフェロールの塩、及びトコフェロールの誘導体等としては、医薬品、医薬部外品又は化粧品分野において皮膚外用剤の成分として通常用いられる化合物を使用することができ、ｄ体、ｌ体、又はｄｌ体のいずれであってもよく、またα、β、γ、δの構造のいずれであってもよい。トコフェロールとしては、例えば、ｄ－α－トコフェロール、ｄ－β－トコフェロール、ｄ－γ－トコフェロール及びｄ－δ－トコフェロール、ｌ－α－トコフェロール、ｌ－β－トコフェロール、ｌ－γ－トコフェロール、ｌ－δ－トコフェロール、それらの混合物であるｄｌ－α－トコフェロール、ｄｌ－β－トコフェロール、ｄｌ－γ－トコフェロール、ｄｌ－δ－トコフェロール等が挙げられる。トコフェロールの誘導体としては、限定はされないが、トコフェロールのエステルが好ましい。トコフェロールの誘導体としては、酢酸トコフェロール、トコフェロールニコチン酸エステル又はその塩、トコフェロールコハク酸エステル又はその塩、トコフェロールリノレン酸エステル、リン酸トコフェロール又はその塩、（リノール酸／オレイン酸）トコフェロール、及びトコトエリノールからなる群より選択される１種等が例示される。 (Vitamin E)
The composition for external use on the skin of the present invention contains vitamin Es such as tocopherol, a salt of tocopherol, and a derivative of tocopherol in addition to the above components (A) and (B) as long as the effects of the present invention are not impaired. You may be. As the tocopherol, the salt of tocopherol, the derivative of tocopherol and the like used in the present invention, a compound usually used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs or cosmetics can be used. It may be either a body or a dl body, and may have any of α, β, γ, and δ structures. Examples of tocopherols include d-α-tocopherol, d-β-tocopherol, d-γ-tocopherol and d-δ-tocopherol, l-α-tocopherol, l-β-tocopherol, l-γ-tocopherol, l-. Examples thereof include δ-tocopherol, dl-α-tocopherol, dl-β-tocopherol, dl-γ-tocopherol, dl-δ-tocopherol and the like, which are mixtures thereof. The derivative of tocopherol is not limited, but an ester of tocopherol is preferable. Derivatives of tocopherol include tocopherol acetate, tocopherol nicotinic acid ester or a salt thereof, tocopherol succinic acid ester or a salt thereof, tocopherol linolenic acid ester, tocopherol phosphate or a salt thereof, tocopherol (linoleic acid / oleic acid), and tocotoerinol. An example is one selected from the group consisting of.
　本発明の皮膚外用組成物において、皮膚外用組成物の全量に対するビタミンＥ類の総含有量は特に限定されないが、好ましくは、０．００００１～１０質量％、より好ましくは、０．０００１～５質量％、さらに好ましくは０．００１～１質量％、さらにより好ましくは０．０１～０．５質量％である。 In the external composition for skin of the present invention, the total content of vitamin E with respect to the total amount of the external composition for skin is not particularly limited, but is preferably 0.00001 to 10% by mass, more preferably 0.0001 to 5% by mass. %, More preferably 0.001 to 1% by mass, still more preferably 0.01 to 0.5% by mass.
　（界面活性剤）
　本発明の皮膚外用組成物は、本発明の効果を妨げない限り、上記（Ａ）成分及び（Ｂ）成分の他に、界面活性剤を含んでいてもよい。界面活性剤を含む場合には、限定はされないが、非イオン性界面活性剤が好ましく、たとえばポリオキシエチレン硬化ヒマシ油４０、ポリオキシエチレン硬化ヒマシ油６０、ポリオキシエチレン硬化ヒマシ油８０、ポリオキシエチレンポリオキシプロピレンデシルテトラデシルエーテル、ポリオキシエチレン（２０）ポリオキシプロピレン（４）セチルエーテル、イソステアリン酸ＰＥＧ－８グリセリル、モノラウリン酸ポリオキシエチレンソルビタン（２０Ｅ．Ｏ．）、イソステアリン酸ポリオキシエチレンソルビタン（２０Ｅ．Ｏ．）、ステアリン酸ポリオキシエチレンソルビタン（２０Ｅ．Ｏ．）、ヤシ油脂肪酸ポリグリセリル－１０、ヤシ油脂肪酸ポリグリセリル－３、ヤシ油脂肪酸ＰＥＧ－７グリセリル、ジオレイン酸ポリグリセリル－１０、ジイソステアリン酸ポリグリセリル－１０、トリイソステアリン酸ＰＥＧ－４０グリセリル、イソステアリン酸ＰＥＧ－４０グリセリル、トリラウリン酸ポリグリセリル－１０、トリカプリル酸ヘキサグリセリル、ラウリン酸ポリグリセリル、ミリスチン酸ポリグリセリル、ポリオキシエチレンラウリルエーテル等を用いる事ができ、特にポリオキシエチレンポリオキシプロピレンデシルテトラデシルエーテル、ポリオキシエチレン硬化ヒマシ油４０、ポリオキシエチレン硬化ヒマシ油６０、ポリオキシエチレン硬化ヒマシ油８０、イソステアリン酸ポリオキシエチレンソルビタン（２０Ｅ．Ｏ．）、モノラウリン酸ポリオキシエチレンソルビタン（２０Ｅ．Ｏ．）、ラウリン酸ポリグリセリルが好ましい。 (Surfactant)
The composition for external use on the skin of the present invention may contain a surfactant in addition to the above-mentioned components (A) and (B) as long as the effects of the present invention are not impaired. When a surfactant is contained, a nonionic surfactant is preferable, and for example, polyoxyethylene hydrogenated castor oil 40, polyoxyethylene hydrogenated castor oil 60, polyoxyethylene hydrogenated castor oil 80, and polyoxy Ethylene polyoxypropylene decyltetradecyl ether, polyoxyethylene (20) polyoxypropylene (4) cetyl ether, PEG-8 glyceryl isostearate, polyoxyethylene sorbitan monolaurate (20EO), polyoxyethylene sorbitan isostearate (20EO), Polyoxyethylene sorbitan stearate (20EO), palm oil fatty acid polyglyceryl-10, palm oil fatty acid polyglyceryl-3, palm oil fatty acid PEG-7 glyceryl, polyglyceryl dioleate-10, diisostearic acid. Polyglyceryl-10, PEG-40 glyceryl triisostearate, PEG-40 glyceryl isostearate, polyglyceryl-10 trilaurate, hexaglyceryl tricaprylate, polyglyceryl laurate, polyglyceryl myristate, polyoxyethylene lauryl ether and the like can be used. In particular, polyoxyethylene polyoxypropylene decyltetradecyl ether, polyoxyethylene hydrogenated castor oil 40, polyoxyethylene hydrogenated castor oil 60, polyoxyethylene hydrogenated castor oil 80, polyoxyethylene sorbitan isostearate (20EO), monolaurin. Polyoxyethylene sorbitan acid (20EO) and polyglyceryl laurate are preferred.
　本発明の皮膚外用組成物において、皮膚外用組成物の全量に対する界面活性剤の総含有量は、他の成分とのバランスによって適宜設定される。皮膚外用組成物の全量に対する、界面活性剤の総含有量は、好ましくは０．００１～１０質量％、より好ましくは、０．００５～７質量％、さらに好ましくは、０．０１～５質量％である。 In the external composition for skin of the present invention, the total content of the surfactant with respect to the total amount of the external composition for skin is appropriately set depending on the balance with other components. The total content of the surfactant with respect to the total amount of the external composition for skin is preferably 0.001 to 10% by mass, more preferably 0.005 to 7% by mass, still more preferably 0.01 to 5% by mass. Is.
　（その他の成分）
　本発明の皮膚外用組成物には、上記（Ａ）成分及び（Ｂ）成分の他に、美白成分、抗炎症成分、抗菌成分、細胞賦活化成分、収斂成分、抗酸化成分、ニキビ改善成分、老化防止成分、コラーゲン等の生体成分合成促進成分、血行促進成分、保湿成分、老化防止成分等の各種成分を１種又は２種以上組み合わせて配合することができる。好ましくは美白成分、抗炎症成分、抗菌成分、細胞賦活化成分、収斂成分、抗酸化成分、老化防止成分又は保湿成分の１種又は２種以上の成分である。これらの成分の組み合わせとして特に好ましいものとしては、美白成分との組み合わせ、美白成分と抗酸化成分との組み合わせ、抗酸化成分との各組み合わせ、老化防止成分との組み合わせ、美白成分と老化防止成分との各組み合わせを挙げることができる。これらの各成分としては、医薬品、医薬部外品、又は化粧品分野において皮膚外用剤の成分として従来から使用され、また将来使用されるものであれば特に制限されず、任意のものを適宜選択し使用することができる。これらのうち、例えば、抗炎症成分であるグリチルリチン酸ジカリウムは好ましく用いられる。これらの成分は、１種類又は２種類以上を組み合わせて使用できる。 (Other ingredients)
In addition to the above-mentioned components (A) and (B), the external composition for skin of the present invention includes a whitening component, an anti-inflammatory component, an antibacterial component, a cell activating component, an astringent component, an antioxidant component, and an acne improving component. Various components such as an anti-aging component, a biological component synthesis promoting component such as collagen, a blood circulation promoting component, a moisturizing component, and an anti-aging component can be blended in one or a combination of two or more. It is preferably one or more components of a whitening component, an anti-inflammatory component, an antibacterial component, a cell activating component, an astringent component, an antioxidant component, an anti-aging component or a moisturizing component. Particularly preferable combinations of these components are a combination with a whitening component, a combination of a whitening component and an antioxidant component, each combination with an antioxidant component, a combination with an anti-aging component, and a whitening component and an anti-aging component. Each combination of can be mentioned. Each of these components is not particularly limited as long as it is conventionally used as a component of a skin external preparation in the fields of pharmaceuticals, quasi-drugs, or cosmetics, and will be used in the future, and any component may be appropriately selected. Can be used. Of these, for example, dipotassium glycyrrhizinate, which is an anti-inflammatory component, is preferably used. These components may be used alone or in combination of two or more.
　本発明の皮膚外用組成物は、上記各成分に加えて、さらに可溶化成分、油脂類、糖類又は経皮吸収促進成分を配合することもできる。特に可溶化成分又は油脂類を配合することによって、水性溶媒中におけるアスコルビン酸の安定性、有効性、使用感をより向上させることができる。 The composition for external use on the skin of the present invention may further contain a solubilizing component, oils and fats, saccharides, or a transdermal absorption promoting component in addition to each of the above components. In particular, by blending a solubilizing component or oils and fats, the stability, effectiveness and usability of ascorbic acid in an aqueous solvent can be further improved.
　本発明の皮膚外用組成物には、外観安定性や粘度等の品質を損なわず、また本発明の効果を損なわない量的及び質的範囲内で、必要に応じて医薬品、医薬部外品又は化粧品分野において外用剤の成分として一般的に用いられる各種の成分、例えば、アミノ酸、刺激軽減剤、増粘剤、防腐剤、紫外線防御剤、着色剤、分散剤、追加のｐＨ調整剤、香料等を配合することができる。これらの成分は１種類又は２種類以上を組み合わせて使用できる。 The composition for external use on the skin of the present invention is, if necessary, a pharmaceutical product, a quasi-drug, or a pharmaceutical product, within a quantitative and qualitative range that does not impair the quality such as appearance stability and viscosity, and does not impair the effect of the present invention. Various components commonly used as components of external agents in the cosmetic field, such as amino acids, irritation reducing agents, thickeners, preservatives, UV protection agents, coloring agents, dispersants, additional pH regulators, fragrances, etc. Can be blended. These components may be used alone or in combination of two or more.
（容器）
　本発明の皮膚外用組成物は、該皮膚外用組成物と接触する面の一部又は全部が、ポリオレフィンを含有する樹脂を含む容器に収容してなる。
　ここで、ポリオレフィンとしては、ポリエチレン(ＰＥ)（高密度ポリエチレン(ＨＤＰＥ)、低密度ポリエチレン(ＬＤＰＥ)、超低密度ポリエチレン、直鎖状低密度ポリエチレン(ＬＬＤＰＥ)、超高分子量ポリエチレンなどを含む）、ポリプロピレン(ＰＰ)（ホモポリマー、ランダムコポリマー、ブロックコポリマーなどを含む）、及びエチレン・プロピレンコポリマー、環状オレフィンコポリマー、ポリメチルペンテン、ポリブテンー１、１，２-ポリブタジエンが好ましく、ポリエチレン樹脂又はポリプロピレン樹脂がより好ましい。このうち、少なくともポリエチレンを含む樹脂であることが特に好ましい。 (container)
The external composition for skin of the present invention is contained in a container containing a resin containing a polyolefin, in part or in whole of the surface in contact with the external composition for skin.
Here, the polyolefin includes polyethylene (PE) (including high-density polyethylene (HDPE), low-density polyethylene (LDPE), ultra-low-density polyethylene, linear low-density polyethylene (LLDPE), ultra-high-molecular-weight polyethylene, etc.). Polyethylene (PP) (including homopolymers, random copolymers, block copolymers, etc.), and ethylene-propylene copolymers, cyclic olefin copolymers, polymethylpentene, polybutene-1,1,2-polybutadiene are preferred, polyethylene resin or polypropylene resin is more preferred. preferable. Of these, a resin containing at least polyethylene is particularly preferable.
　使用される容器の形状は、目的に応じて適宜選択でき、チューブタイプ、ジャータイプ、スポイドタイプ、ディスペンサ-タイプ、パウチパック、スプレータイプ、ボトルタイプ、及びチアパックなどを例示できる。このうち、ヒートシール工程を経る容器であることが好ましく、チューブタイプ、パウチパック、及びチアパックなどが特に好ましい。 The shape of the container to be used can be appropriately selected according to the purpose, and examples include tube type, jar type, dropper type, dispenser-type, pouch pack, spray type, bottle type, and cheer pack. Of these, a container that has undergone a heat sealing step is preferable, and a tube type, a pouch pack, a cheer pack, and the like are particularly preferable.
　容器の詳細な具体例としては、例えば、皮膚外用組成物が接する最内面をポリオレフィンを含む樹脂でラミネートしたアルミチューブ、皮膚外用組成物が接する最内面をポリオレフィンを含む樹脂でラミネートしたアルミバッグ等の保存容器、皮膚外用組成物が接する最内面をポリオレフィンを含む樹脂でラミネートしたチャック付きスタンドパウチ、皮膚外用組成物が接する最内面をポリオレフィンを含む樹脂でラミネートしたアルミフィルム等で蓋をヒートシールした容器等が挙げられる。 Specific examples of the container include, for example, an aluminum tube in which the innermost surface in contact with the external composition for skin is laminated with a resin containing polyolefin, an aluminum bag in which the innermost surface in contact with the external composition for skin is laminated with a resin containing polyolefin, and the like. A storage container, a stand pouch with a chuck whose innermost surface in contact with the external composition for skin is laminated with a resin containing polyolefin, and a container in which the lid is heat-sealed with an aluminum film whose innermost surface in contact with the external composition for skin is laminated with a resin containing polyolefin. And so on.
　本発明の皮膚外用組成物が例えばチューブに収容される形態の場合には、特に１滴～数滴の滴下がしやすいなどの効果を期待することもできる。このため、限定はされないが、滴下部分の一部又は全部がポリオレフィン樹脂で構成されることが好ましい。 When the external composition for skin of the present invention is contained in a tube, for example, it can be expected to have an effect that one to several drops are particularly easy to drop. Therefore, although not limited, it is preferable that a part or all of the dropping portion is composed of the polyolefin resin.
　（形態）
　本発明の皮膚外用組成物は、（Ａ）成分及び（Ｂ）成分、及び必要に応じて（Ｃ）成分の他上記各任意成分のいずれか又は複数を配合混合し、さらに必要に応じてその他の溶媒や通常使用される外用剤の基剤等を配合することによって、液状、乳液状、クリーム状、ペースト状、ムース状、ジェル状、シート状（基材担持）、エアゾール状、スプレー状等の各種所望の形態に調製することができる。限定はされないが、本願の効果を顕著に奏する観点から液状にすることが好ましい。これらは当業界の通常の方法にて製造することができる。 (form)
In the external composition for skin of the present invention, one or more of the above-mentioned optional components in addition to the component (A) and the component (B) and, if necessary, the component (C) are blended and mixed, and further, if necessary, others. Liquid, milky liquid, cream, paste, mousse, gel, sheet (base material supported), aerosol, spray, etc. Can be prepared in various desired forms. Although not limited, it is preferable to make it liquid from the viewpoint of remarkably exerting the effect of the present application. These can be manufactured by conventional methods in the art.
　（粘度）
　本発明の皮膚外用組成物は、特に皮膚に適用するために用いられる皮膚外用組成物の使用の際に望まれる適度な粘性を備えた組成物として調製することができる。本発明の皮膚外用組成物の粘度は、特に限定はされないが、例えば、Ｅ型粘度計を用いて２５℃で測定した場合の粘度が通常１～３００ｍＰａ・ｓ程度、好ましくは１～２００ｍＰａ・ｓ程度、より好ましくは１～１００ｍＰａ・ｓ程度、最も好ましくは、１～５０ｍＰａ・ｓ程度である。粘度測定方法は、より詳細には、第１６改正日本薬局方[Ｂ]一般試験法　２．物理的試験法　その他の物理的試験法　２．５３　粘度測定法　２．第２法　回転粘度計法　２．１．３　円すい‐平板形回転粘度計（コーンプレート型粘度計）に記載の方法に準ずる。 (viscosity)
The external composition for skin of the present invention can be prepared as a composition having an appropriate viscosity desired especially when using the external composition for skin used for application to the skin. The viscosity of the external composition for skin of the present invention is not particularly limited, but for example, the viscosity when measured at 25 ° C. using an E-type viscometer is usually about 1 to 300 mPa · s, preferably 1 to 200 mPa · s. The degree, more preferably about 1 to 100 mPa · s, and most preferably about 1 to 50 mPa · s. More specifically, the viscosity measurement method is the 16th revised Japanese Pharmacopoeia [B] general test method. Physical test method Other physical test methods 2.53 Viscosity measurement method 2. Second method Rotational viscometer method 2.1.3 Follow the method described in the cone-plate type rotational viscometer (cone plate type viscometer).
　（ｐＨ）
　本発明の皮膚外用組成物は、通常ｐＨ１～８の液性を備えていればよいが、アスコルビン酸の安定性、皮膚や粘膜に対する低刺激性、及び皮膚使用感の良さという観点から、好ましくはｐＨ２～７、より好ましくはｐＨ２～６、さらに好ましくは、ｐＨ２～５．０、最も好ましくは、ｐＨ２～４．５である。酸性領域であることが望ましい。 (PH)
The composition for external use on the skin of the present invention may usually have a liquid property of pH 1 to 8, but is preferable from the viewpoints of stability of ascorbic acid, hypoallergenicity to the skin and mucous membranes, and good skin usability. The pH is 2 to 7, more preferably pH 2 to 6, still more preferably pH 2 to 5.0, and most preferably pH 2 to 4.5. It is desirable that it is in an acidic region.
　（用途）
　本発明の皮膚外用組成物は、特には、美白剤、抗炎症剤、抗老化剤として有効であり、例えば、にきび予防や治療、抗酸化の作用を有する。さらに、皮膚への適用により、皮膚の透明感が高まり、潤いが保持され、キメが整い、ざらつきを抑える効果が発揮される場合がある。さらには、にきび痕や毛穴が気になる肌にうるおいを与える、毛穴を目立たなくさせる、なめらかな肌に導く、整肌保湿等の効果が発揮される場合がある他、しみの予防や治療に用いることもできる。 (Use)
The external composition for skin of the present invention is particularly effective as a whitening agent, an anti-inflammatory agent, and an anti-aging agent, and has, for example, acne prevention, treatment, and antioxidative effects. Further, when applied to the skin, the transparency of the skin is enhanced, the moisture is maintained, the texture is smoothed, and the effect of suppressing roughness may be exhibited. In addition, it may have effects such as moisturizing the skin where acne scars and pores are anxious, making the pores inconspicuous, leading to smooth skin, moisturizing the skin, and for preventing and treating spots. It can also be used.
　本発明の皮膚外用組成物は、例えば、美容液、化粧水、日焼け止めクリーム、乳液、クリーム、ローション、オイル及びパック等の基礎化粧料；ファンデーション、口紅、リップクリーム、マスカラ、アイシャドウ、アイライナー、眉墨及び美爪料等のメーキャップ化粧料；洗顔料やクレンジング、ボディ洗浄料等の洗浄料；腋臭防止剤、水虫治療剤、鎮痒剤、創傷治癒剤、清拭剤、清浄剤、消炎鎮痛剤、にきび治療剤、痔疾用剤、殺菌消毒剤、美白剤、紫外線防御剤等の、化粧品、外用医薬品又は外用医薬部外品の分野に属する各種の皮膚外用組成物とすることができる。皮膚への作用効果から、本発明は皮膚外用剤（外皮用の製剤）等の外皮に適用される製品に使用されることが好ましい。本発明の組成物は、用途等に応じて１日あたり１回から数回に分けて、公知あるいは慣用されている用法・用量にて使用することができる。 The external composition for skin of the present invention is, for example, basic cosmetics such as beauty liquids, lotions, sunscreen creams, milky lotions, creams, lotions, oils and packs; foundations, lipsticks, lip creams, mascara, eye shadows and eye liners. , Makeup cosmetics such as eyebrows and beautiful nails; Cleaning agents such as facial cleansers, cleansers, and body cleaning agents; It can be used as various external skin compositions belonging to the fields of cosmetics, external medicines or external pharmaceutical products such as acne therapeutic agents, hemorrhagic agents, sterilizing and disinfecting agents, whitening agents, ultraviolet protective agents and the like. From the viewpoint of the effect on the skin, the present invention is preferably used for products applied to the outer skin such as external skin preparations (formulations for the outer skin). The composition of the present invention can be used once or several times a day according to the intended use and the like, in a known or commonly used dosage and administration.
　[濡れ性向上方法]
　本発明はまた、（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種、及び（Ｂ）低級アルコールを共存させることで、該組成物に、ポリオレフィンを含有する樹脂又はそのような樹脂で成型された容器に対する濡れ性向上作用を付与する方法をも包含する。本発明の濡れ性向上方法において、（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種；及び（Ｂ）低級アルコールを含有する皮膚外用組成物とすることやそれらの含有量等、その他の成分とそれらの含有量については、前記皮膚外用組成物で記載した内容に準じる。 [How to improve wettability]
The present invention also comprises coexistence of (A) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol so that the composition contains a resin or a resin containing a polyolefin. It also includes a method of imparting a wettability improving effect to a container molded from such a resin. In the method for improving wettability of the present invention, at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid; and (B) a composition for external skin containing lower alcohol and their components. Regarding other components such as the content and their content, the contents described in the above-mentioned external composition for skin shall be applied.
　[ｐＨ変動抑制方法]
　本発明はまた、（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種、及び（Ｂ）低級アルコールを共存させることで、該組成物に、ポリオレフィンを含有する樹脂又はそのような樹脂で成型された容器に収容されて保存された場合のｐＨ変動を抑制する方法をも包含する。ｐＨ変動は組成物の品質変動に関連することから、変動抑制は品質保持に繋がる。本発明の当該方法において、（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種；及び（Ｂ）低級アルコールを含有する皮膚外用組成物とすることやそれらの含有量等、その他の成分とそれらの含有量については、前記皮膚外用組成物で記載した内容に準じる。 [Method for suppressing pH fluctuation]
The present invention also comprises coexistence of (A) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol so that the composition contains a resin or a resin containing a polyolefin. It also includes a method of suppressing pH fluctuation when stored in a container molded from such a resin. Since pH fluctuations are related to quality fluctuations of the composition, suppression of fluctuations leads to quality maintenance. In the method of the present invention, at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid; and (B) a composition for external use on the skin containing a lower alcohol and its content. Etc., and other components and their contents are the same as those described in the above-mentioned external composition for skin.
　[消泡促進方法]
　本発明はまた、（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種、及び（Ｂ）低級アルコールを共存させることで、該組成物に、ポリオレフィンを含有する樹脂又はそのような樹脂で成型された容器に収容された場合の消泡を促進する方法をも包含する。配合成分、特にアスコルビン酸等は、空気との接触によって着色等、安定性に影響を及ぼすことがある。特に液状の組成物において、振動又は衝撃により発生した泡の消える速度（消泡速度）が遅い場合、配合成分と空気との接触機会が増加、延長し得る。従って、消泡促進は、組成物の品質保持に繋がる。本発明の当該方法において、（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種；及び（Ｂ）低級アルコールを含有する皮膚外用組成物とすることやそれらの含有量等、その他の成分とそれらの含有量については、前記皮膚外用組成物で記載した内容に準じる。 [Defoaming promotion method]
The present invention also comprises coexistence of (A) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol, so that the composition contains a resin or a resin containing a polyolefin. It also includes methods of promoting defoaming when housed in such resin-molded containers. Ingredients, especially ascorbic acid and the like, may affect stability such as coloring due to contact with air. Especially in a liquid composition, when the rate at which bubbles generated by vibration or impact disappear (defoaming rate) is slow, the chance of contact between the compounding component and air can be increased or extended. Therefore, promotion of defoaming leads to maintenance of quality of the composition. In the method of the present invention, at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid; and (B) a composition for external use on the skin containing a lower alcohol and its content. Etc., and other components and their contents are the same as those described in the above-mentioned external composition for skin.
　次に、実施例により本発明を具体的に説明するが、本発明は以下の実施例に限定されるものではない。なお、表における各成分量の単位は、表中特に断りがない限り、質量％である。 Next, the present invention will be specifically described with reference to Examples, but the present invention is not limited to the following Examples. The unit of each component amount in the table is mass% unless otherwise specified in the table.
　表１～表１３に示す組成の皮膚外用組成物を常法に従って調製した。 The external composition for skin having the compositions shown in Tables 1 to 13 was prepared according to a conventional method.
　［試験例１：濡れ性試験］
　実施例及び比較例の組成物について、ポリエチレン樹脂（アズワン社製：ＰＥＮ－０５０５０３）及び、ポリプロピレン樹脂（アズワン社製：ＰＰＮ－０５０５０３）に対する濡れ性の評価を接触角測定にて行った。それぞれ、厚さ３ｍｍの樹脂を２ｃｍ×６ｃｍにカットして使用した。接触角計の付属シリンジを用いて、被験液０．５μＬをプレート表面に着滴させ、接触角を測定した。各組成物について、同一の容器材質を使用して同一の温度条件下（室温下）で１０回続けて測定し、その平均値で評価した。その結果を表に示す。接触角の測定条件は以下の通りである。
　使用機器： 接触角計 Drop Master 500 （協和界面科学）
　液滴量：　0.5μL
　接触角計算方法：　θ/2法
　接触面の材質：ポリエチレン樹脂、ポリプロピレン樹脂
　表中の略語は以下の意味である。
ＶＢ６：ピリドキシン塩酸塩
ＶＣエチル：３－Ｏ－エチルアスコルビン酸
ＶＣグルコシド：Ｌ－アスコルビン酸２－グルコシド
ＩＰＭＰ：イソプロピルメチルフェノール
ＰＧ：プロピレングリコール
ＰＤ：１，３－プロパンジオール
ＢＧ：ブチレングリコール [Test Example 1: Wetting property test]
For the compositions of Examples and Comparative Examples, the wettability of the polyethylene resin (AS ONE: PEN-50503) and the polypropylene resin (AS ONE: PPN-05503) was evaluated by contact angle measurement. A resin having a thickness of 3 mm was cut into 2 cm × 6 cm and used. Using the syringe attached to the contact angle meter, 0.5 μL of the test solution was dropped on the plate surface, and the contact angle was measured. Each composition was measured 10 times in succession under the same temperature conditions (at room temperature) using the same container material, and evaluated by the average value. The results are shown in the table. The measurement conditions for the contact angle are as follows.
Equipment used: Contact angle meter Drop Master 500 (Kyowa Interface Science)
Droplet volume: 0.5 μL
Contact angle calculation method: θ / 2 method Contact surface material: Polyethylene resin, polypropylene resin The abbreviations in the table have the following meanings.
VB6: Pyridoxine hydrochloride VC ethyl: 3-O-ethylascorbic acid VC glucoside: L-ascorbic acid 2-glucoside IPMP: isopropylmethylphenol PG: propylene glycol PD: 1,3-propanediol BG: butylene glycol
Figure JPOXMLDOC01-appb-T000001
Figure JPOXMLDOC01-appb-T000001
Figure JPOXMLDOC01-appb-T000002
Figure JPOXMLDOC01-appb-T000002
　比較例の組成物に比べて、エタノールを加えることで接触角が大きくなったが、実施例の組成物は、ポリエチレン樹脂に対する接触角が小さくなり、濡れ性が改善されていることが分かった。
Figure JPOXMLDOC01-appb-T000003
 Compared with the composition of the comparative example, the contact angle was increased by adding ethanol, but it was found that the composition of the example had a smaller contact angle with respect to the polyethylene resin and the wettability was improved.
Figure JPOXMLDOC01-appb-T000003
Figure JPOXMLDOC01-appb-T000004
Figure JPOXMLDOC01-appb-T000004
　比較例の組成物に比べて、実施例の組成物は、ポリプロピレン樹脂に対する接触角が小さくなり、濡れ性が改善されていることが分かった。 It was found that the composition of the example had a smaller contact angle with respect to the polypropylene resin and the wettability was improved as compared with the composition of the comparative example.
　ピリドキシン、サリチル酸、イソプロピルメチルフェノール、３－Ｏ－エチルアスコルビン酸又はＬ－アスコルビン酸２－グルコシドを配合している実施例では、接触角がより小さく、さらに濡れ性が改善していた。 In the examples containing pyridoxine, salicylic acid, isopropylmethylphenol, 3-O-ethylascorbic acid or L-ascorbic acid 2-glucoside, the contact angle was smaller and the wettability was further improved.
　なお、１，３－プロパンジオールをブチレングリコールやグリセリンに変更した試験例においても同様に濡れ性の改善が見られた。
Figure JPOXMLDOC01-appb-T000005
Figure JPOXMLDOC01-appb-T000006
 Similarly, improvement in wettability was observed in the test examples in which 1,3-propanediol was changed to butylene glycol or glycerin.
Figure JPOXMLDOC01-appb-T000005
Figure JPOXMLDOC01-appb-T000006
[試験例２]
　ポリエチレン製の容器（アズワン PEスピッチ １０ｍＬ (型番２－４６７－０２)に、表中の比較例に示すエタノールとポリオール（プロピレングリコール、１，３－プロパンジオール又はグリセリン）を配合した組成物を９ｍＬ充填し、エイジングに供した。具体的には、蓋を上にして立てた状態で６０℃にて７日間静置した。同様に、表に示すように、エタノール、ポリオール、及びアスコルビン酸、さらに、（Ｃ－１）、（Ｃ－２）、（Ｃ－３）又は（Ｃ－４）成分を配合した実施例に示す組成物についても同様にエイジングに供した。その後、エイジング前後のｐＨを測定し、変化を評価した。 [Test Example 2]
A polyethylene container (AS ONE PE Spitch 10 mL (model number 2-467-02)) is filled with 9 mL of a composition containing ethanol and a polyol (propylene glycol, 1,3-propanediol or glycerin) shown in Comparative Example in the table. Then, it was subjected to aging. Specifically, it was allowed to stand at 60 ° C. for 7 days with the lid upright. Similarly, as shown in the table, ethanol, polyol, and ascorbic acid, and further, The composition shown in the example containing the components (C-1), (C-2), (C-3) or (C-4) was also subjected to aging in the same manner, and then the pH before and after aging was measured. And evaluated the changes.
Figure JPOXMLDOC01-appb-T000007
Figure JPOXMLDOC01-appb-T000007
Figure JPOXMLDOC01-appb-T000008
Figure JPOXMLDOC01-appb-T000008
　この結果、エタノールとポリオール（プロピレングリコール、１，３－プロパンジオール又はグリセリン）を配合した対応する比較例の組成物では、エイジングによるｐＨの変動があったが、アスコルビン酸、（Ｃ－１）、（Ｃ－２）、（Ｃ－３）又は（Ｃ－４）成分を配合した実施例の組成物では、変化が生じにくくなった。
　ここで、ｐＨ変化改善率（％）は以下のように求めた。
ｐＨ変化改善率（％）＝（|対応比較例におけるエイジング前後の差|-|各実施例におけるエイジング前後の差|）／|対応比較例におけるエイジング前後の差|×100 As a result, in the composition of the corresponding comparative example containing ethanol and the polyol (propylene glycol, 1,3-propanediol or glycerin), the pH fluctuated due to aging, but ascorbic acid, (C-1),. In the composition of the example containing the components (C-2), (C-3) or (C-4), the change was less likely to occur.
Here, the pH change improvement rate (%) was determined as follows.
pH change improvement rate (%) = (| Difference before and after aging in the corresponding comparative example |-| Difference before and after aging in each example |) / | Difference before and after aging in the corresponding comparative example | × 100
　次に、ポリプロピレン製の容器（アズワン PPスピッチ １０ｍＬ(型番4-812-01)）に、表中の比較例に示すエタノールとポリオール（プロピレングリコール、１，３－プロパンジオール又はグリセリン）を配合し、ポリエチレン製の容器を使用した試験と同様の方法で同様にエイジングに供した。同様に、エタノール、ポリオール、及びアスコルビン酸、さらに、（Ｃ－１）、（Ｃ－２）、（Ｃ－３）又は（Ｃ－４）成分を配合した実施例に示す組成物をエイジングに供した。 Next, in a polypropylene container (AS ONE PP Spitch 10 mL (model number 4-812-01)), the ethanol and polyol (propylene glycol, 1,3-propanediol or glycerin) shown in the comparative example in the table are mixed. It was subjected to aging in the same manner as in the test using a polyethylene container. Similarly, the composition shown in the example containing ethanol, a polyol, and ascorbic acid, and further components (C-1), (C-2), (C-3), or (C-4) is subjected to aging. did.
Figure JPOXMLDOC01-appb-T000009
Figure JPOXMLDOC01-appb-T000009
Figure JPOXMLDOC01-appb-T000010
Figure JPOXMLDOC01-appb-T000010
　この結果、エタノールとポリオール（プロピレングリコール、１，３－プロパンジオール又はグリセリン）を配合した対応する比較例の組成物では、エイジングによるｐＨの変動があったが、アスコルビン酸、（Ｃ－１）、（Ｃ－２）、（Ｃ－３）又は（Ｃ－４）成分を配合した実施例の組成物では、変化が生じにくくなった。 As a result, in the composition of the corresponding comparative example containing ethanol and the polyol (propylene glycol, 1,3-propanediol or glycerin), the pH fluctuated due to aging, but ascorbic acid, (C-1),. In the composition of the example containing the components (C-2), (C-3) or (C-4), the change was less likely to occur.
　なお、ガラス容器ではアスコルビン酸を加えてもそのような効果は生じなかった。
Figure JPOXMLDOC01-appb-T000011
 In addition, in the glass container, even if ascorbic acid was added, such an effect did not occur.
Figure JPOXMLDOC01-appb-T000011
[試験例３]
　ポリエチレン製容器（アズワンＰＥスピッチ １０ｍＬ (型番２－４６７－０２)に調製した組成物を５ｍＬ、容器のふたを下にして振盪器（Ｉｗａｋｉ ＫＭ Ｓｈａｋｅｒ （ＭＯＤＥＬ: ＶＤ－Ｘ）)を使って３５０回（３５０ｓｐｍで１分間）浸透し、３分後の吸光度（波長６６０ｎｍ）を分光光度計（アズワン　ＡＳＶ１１ｄ－Ｈ）にて測定した。 [Test Example 3]
5 mL of the composition prepared in a polyethylene container (AS ONE PE Spitch 10 mL (model number 2-467-02), 350 times using a shaker (Iwaki KM Shaker (MODEL: VD-X)) with the container lid down. The mixture was infiltrated (at 350 spm for 1 minute), and the absorbance (wavelength 660 nm) after 3 minutes was measured with a spectrophotometer (AS ONE ASV11d-H).
Figure JPOXMLDOC01-appb-T000012
Figure JPOXMLDOC01-appb-T000012
Figure JPOXMLDOC01-appb-T000013
Figure JPOXMLDOC01-appb-T000013
　ポリオールとエタノールを配合した組成物の吸光度よりも、アスコルビン酸やその他（Ｃ）成分を配合した組成物の方が吸光度が低く、一旦生じた泡が消えやすくなっているという結果であった。なお、ガラスでは吸光度の変化は見られなかった。ここで、改善率は以下のようにして求めた。
改善率＝（対応比較例における180秒後の吸光度-各実施例における180秒後の吸光度）／対応比較例における180秒後の吸光度）×100 The result was that the absorbance of the composition containing ascorbic acid and other components (C) was lower than that of the composition containing the polyol and ethanol, and the bubbles once formed were more likely to disappear. No change in absorbance was observed in the glass. Here, the improvement rate was calculated as follows.
Improvement rate = (absorbance after 180 seconds in the corresponding comparative example-absorbance after 180 seconds in each example) / absorbance after 180 seconds in the corresponding comparative example) × 100
[処方例]
　下記表１４に処方例を示す。処方例は、いずれも美容液で、各処方について、ポリエチレン樹脂製、ポリプロピレン樹脂製の容器に充填した。処方例中の含有量はいずれも質量％である。 [Prescription example]
Table 14 below shows a prescription example. The prescription examples were all beauty essences, and each prescription was filled in a polyethylene resin or polypropylene resin container. The content in each of the formulation examples is mass%.
Figure JPOXMLDOC01-appb-T000014
Figure JPOXMLDOC01-appb-T000014

Claims (7)

  1. 　（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種、及び（Ｂ）低級アルコールを含有する皮膚外用組成物であって、
    　該皮膚外用組成物と接触する面の一部又は全部が、ポリオレフィンを含有する樹脂を含む容器に収容してなる皮膚外用組成物。     A composition for external use on the skin containing (A) at least one selected from the group consisting of ascorbic acid and a salt of ascorbic acid, and (B) a lower alcohol.
    A composition for external skin, wherein a part or all of the surface in contact with the external composition for skin is housed in a container containing a resin containing polyolefin.
  2. 　前記（Ｂ）成分の総含有量が、１～７質量％である、請求項１に記載の皮膚外用組成物。 The composition for external use on the skin according to claim 1, wherein the total content of the component (B) is 1 to 7% by mass.
  3. 　さらに、以下の（Ｃ－１）、（Ｃ－２）、（Ｃ－３）、及び（Ｃ－４）からなる群より選択される少なくとも１種を含有する、請求項１又は２に記載の皮膚外用組成物：
    （Ｃ－１）ピリドキシン及び／又はその塩；
    （Ｃ－２）サリチル酸、サリチル酸の誘導体、及びそれらの塩からなる群より選択される少なくとも１種；
    （Ｃ－３）イソプロピルメチルフェノール；
    （Ｃ－４）アスコルビン酸誘導体。     The invention according to claim 1 or 2, further comprising at least one selected from the group consisting of the following (C-1), (C-2), (C-3), and (C-4). External composition for skin:
    (C-1) Pyridoxine and / or a salt thereof;
    (C-2) At least one selected from the group consisting of salicylic acid, salicylic acid derivatives, and salts thereof;
    (C-3) Isopropylmethylphenol;
    (C-4) Ascorbic acid derivative.
  4. 　前記（Ｂ）成分が、少なくともエタノールを含む、請求項１～３のいずれか１項に記載の皮膚外用組成物。 The composition for external use on the skin according to any one of claims 1 to 3, wherein the component (B) contains at least ethanol.
  5. 　前記（Ａ）成分の総含有量が、０．５～３０質量％である、請求項１～４のいずれか１項に記載の皮膚外用組成物。 The composition for external use on the skin according to any one of claims 1 to 4, wherein the total content of the component (A) is 0.5 to 30% by mass.
  6. 　前記容器が、チューブタイプ、パウチパック、又はチアパックである、請求項１～５のいずれか１項に記載の皮膚外用組成物。 The external composition for skin according to any one of claims 1 to 5, wherein the container is a tube type, a pouch pack, or a cheer pack.
  7. 　組成物中に、（Ａ）アスコルビン酸、及びアスコルビン酸の塩からなる群より選択される少なくとも１種、及び（Ｂ）低級アルコールを共存させることで、該組成物に、ポリオレフィンを含有する樹脂に対する濡れ性向上作用を付与する方法。
          By allowing at least one selected from the group consisting of (A) ascorbic acid and a salt of ascorbic acid and (B) a lower alcohol to coexist in the composition, the resin containing the polyolefin in the composition is allowed to coexist. A method of imparting a wettability improving effect.
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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007099629A (en) * 2005-09-30 2007-04-19 Mochida Pharmaceut Co Ltd Bleaching composition
JP2009280578A (en) * 2008-05-20 2009-12-03 Evonik Goldschmidt Gmbh Stable high vitamin c content polyol-in-oil emulsified system, and method for preparing the same
KR20160054096A (en) * 2014-11-05 2016-05-16 주식회사 위드엔젤 Cosmetic Compositions to stabilize Ascorbic acid and Pouch

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007099629A (en) * 2005-09-30 2007-04-19 Mochida Pharmaceut Co Ltd Bleaching composition
JP2009280578A (en) * 2008-05-20 2009-12-03 Evonik Goldschmidt Gmbh Stable high vitamin c content polyol-in-oil emulsified system, and method for preparing the same
KR20160054096A (en) * 2014-11-05 2016-05-16 주식회사 위드엔젤 Cosmetic Compositions to stabilize Ascorbic acid and Pouch

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