WO2023032493A1 - Préparation cutanée externe - Google Patents

Préparation cutanée externe Download PDF

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Publication number
WO2023032493A1
WO2023032493A1 PCT/JP2022/028041 JP2022028041W WO2023032493A1 WO 2023032493 A1 WO2023032493 A1 WO 2023032493A1 JP 2022028041 W JP2022028041 W JP 2022028041W WO 2023032493 A1 WO2023032493 A1 WO 2023032493A1
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WIPO (PCT)
Prior art keywords
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composition
mass
skin
component
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PCT/JP2022/028041
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English (en)
Japanese (ja)
Inventor
安弘 岡田
利哉 森川
Original Assignee
花王株式会社
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Priority to CN202280059108.0A priority Critical patent/CN117897150A/zh
Publication of WO2023032493A1 publication Critical patent/WO2023032493A1/fr

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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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4172—Imidazole-alkanecarboxylic acids, e.g. histidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • 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
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings

Definitions

  • the present invention relates to an external preparation for skin.
  • contact infection is often the route of infection for bacteria or viruses in people's daily lives.
  • Contact infection is mainly caused by the hands and fingers coming into contact with objects such as bacteria or virus infected persons, doorknobs, handles, tableware, toys, other daily necessities, and interior goods.
  • Patent Document 1 discloses niacinamide or a derivative thereof; a first quaternary ammonium salt containing didecyldimethylammonium chloride; benzethonium chloride, benzalkonium chloride, polydiallyldimethylammonium chloride a second quaternary ammonium salt such as; and a cosmetically acceptable base.
  • An external skin preparation comprising an external skin preparation composition contained in a metered discharge container,
  • the composition contains one or more acids or salts thereof (A) selected from the group consisting of lactic acid, pyruvic acid and urocanic acid, Among the acids present in the composition, when an acid present in an acid form is defined as the component (A1), the component (A1 ) content is 0.05 mg or more and 80 mg or less.
  • the step of supplying to the site among the acids present in the composition, when the acid existing in the acid form is (A1), it is discharged from the fixed amount discharge container by one discharge operation.
  • the content of the component (A1) in the composition is 0.05 mg or more and 80 mg or less;
  • the bactericidal agent and antibacterial agent used in the technique disclosed in Patent Document 1 are substantially limited in amount to be incorporated into the composition for skin from the viewpoint of safety to the human body. Therefore, the bactericidal or virucidal activity of the skin by the bactericidal agent or antibacterial agent is not sufficient, and further improvement has been desired.
  • An object of the present invention is to provide an external preparation for skin that exhibits excellent bactericidal or virucidal properties and has low skin irritation.
  • the present inventors have solved the above problems by using an external skin preparation containing a composition containing a predetermined organic acid or a salt thereof in a container that can be discharged so as to satisfy predetermined requirements. I found what I can do.
  • component (A1) existing in an acid form refers to one or more acids selected from the group consisting of lactic acid, pyruvic acid and urocanic acid derived from component (A) in the composition. It means the components present as lactic acid, pyruvic acid and urocanic acid.
  • one or more acids selected from the group consisting of lactic acid, pyruvic acid and urocanic acid derived from component (A) are present in the composition as lactate ion, pyruvate ion and urocanate ion.
  • the component that does so is also referred to as "a component that exists in a dissociated form (A2)".
  • bactericidal or virucidal means bactericidal or virucidal of the skin surface to which the external skin composition is applied.
  • bactericidal activity against Serratia can be specifically evaluated by the method described in Examples.
  • the bactericidal and virucidal properties against other bacteria and viruses can be evaluated in consideration of common technical knowledge.
  • the term "exhibiting bactericidal or virucidal properties" means (1) bactericidal/killing activity against bacteria/viruses adhering to the skin surface after the external skin preparation composition is applied to the skin surface.
  • Viral effect (2) Bactericidal and virucidal effect expressed by applying the composition to bacteria and viruses adhering to the skin, (3) Skin conditioning effect that does not mediate bacteria and viruses, (4) ) The effect of protecting the skin from bacteria and viruses and keeping it hygienic, (5) the effect of preventing the spread and contact infection of bacteria and viruses through the skin, and (6) the effect of protecting the skin from infection against bacteria and viruses. It includes the concept of imparting an effect to enhance, and the like.
  • the external skin preparation of the present invention is an external skin preparation comprising an external skin preparation composition (hereinafter also simply referred to as "composition") contained in a metered discharge container, wherein the composition comprises lactic acid, pyruvic acid and When one or more acids selected from the group consisting of urocanic acid or salts thereof (A) are contained, and among the acids present in the composition, those present in an acid form are used as the component (A1) and an external preparation for skin, wherein the content of the component (A1) in the composition discharged from the fixed quantity discharge container by one discharge operation is 0.05 mg or more and 80 mg or less.
  • composition an external skin preparation composition
  • the external preparation for skin of the present invention means a product for external use for skin comprising the above-mentioned external preparation for skin composition and the above-mentioned metered discharge container.
  • the external preparation for skin of the present invention exhibits excellent bactericidal or virucidal properties and has low skin irritation by having the above constitution.
  • the external preparation for skin of the present invention uses component (A) as a bactericidal or virucidal component.
  • Lactic acid, pyruvic acid, and urocanic acid, which are components (A) are originally present on the human skin as supplied from sweat glands, and especially on the fingers, they have bactericidal and virucidal functions against bacteria, viruses, etc.
  • the inventors of the present invention have found that Therefore, it is thought that the composition for external use on the skin containing the component (A) has bactericidal or virucidal properties, is less irritating to the skin, and is highly safe for the human body.
  • compositions containing component (A) also have higher bactericidal or virucidal properties when the pH is lower.
  • lactic acid which is component (A)
  • the present inventors paid attention to the content of the component (A1) present in the acid form among the acids in the external skin preparation composition applied to the skin. Then, the external skin preparation composition containing the component (A) is accommodated in a metered discharge container, and the component (A1) in the composition discharged from the container by one discharge operation is within a predetermined range. , It has been found that it can exhibit excellent bactericidal or virucidal properties and can reduce skin irritation.
  • the external skin preparation of the present invention comprises the external skin preparation composition contained in the quantitative discharge container, and the components ( The content of A1) is 0.05 mg or more and 80 mg or less.
  • the content of A1) in the discharged composition is within the above range, the external preparation for skin exhibits excellent bactericidal or virucidal properties and is less irritating to the skin.
  • the external preparation for skin of the present invention is excellent because "the content of the component (A1) contained in the composition to be discharged" is controlled to be within the above range by one discharging operation. It is possible to easily and stably supply the component (A1) to the skin in an amount that achieves low irritation to the skin while exhibiting bactericidal or virucidal properties.
  • the content of the component (A1) in the composition discharged from the metered discharge container by one discharge operation is preferably 0.1 mg or more, more preferably 0.2 mg or more, from the viewpoint of improving sterilization or virucidal properties. , more preferably 0.4 mg or more, still more preferably 0.5 mg or more, still more preferably 1.0 mg or more, still more preferably 2.0 mg or more, even if the composition is continuously applied to the skin From the viewpoint of easily suppressing skin irritation, it is preferably 60 mg or less, more preferably 50 mg or less, and even more preferably 45 mg or less.
  • the content of component (A1) in the composition discharged from the metered discharge container by one discharge operation is 0.05 mg or more and 80 mg or less, preferably 0.1 mg or more and 60 mg or less, more preferably 0 mg. 2 mg or more and 60 mg or less, more preferably 0.4 mg or more and 50 mg or less, even more preferably 0.5 mg or more and 50 mg or less, even more preferably 1.0 mg or more and 45 mg or less, still more preferably 2.0 mg or more and 45 mg or less .
  • the content of the component (A1) in the composition ejected by one ejection operation can be calculated by the method described in Examples.
  • the content of component (A1) in the composition ejected by one ejection operation is the content of component (A) in the composition used for the external skin preparation of the present invention, the pH of the composition, and the It can be controlled by the viscosity, the type of the metered discharge container, the discharge amount by one discharge operation, or a combination thereof.
  • the amount of the composition discharged from the metered discharge container in one discharge operation is preferable from the viewpoint of improving the bactericidal or virucidal properties and improving the applicability to the skin.
  • the amount of the composition discharged from the fixed quantity discharge container in one discharge operation is preferably 0.05 g or more and 3.0 g or less, more preferably 0.1 g or more and 2.5 g or less, and still more preferably 0 g. .2 g or more and 2.0 g or less.
  • the external preparation for skin of the present invention comprises an external preparation for skin composition containing one or more acids or salts thereof (A) selected from the group consisting of lactic acid, pyruvic acid and urocanic acid, contained in a metered discharge container.
  • A one or more acids or salts thereof
  • concentration discharge container refers to a container capable of containing an external skin preparation composition. A container that can dispense a large amount of liquid.
  • Examples of fixed-quantity discharge containers include press-type containers such as stroke-type and squeeze-type containers; electric dispenser-type containers; and the like.
  • a single-use, individually-wrapped container is also included in the metered-discharge container of the present invention.
  • Examples of press-type containers examples of stroke-type press-type containers include pump-type and spray-type containers.
  • the squeeze-type push-type container the squeeze-type push-type container described in Japanese Patent Application Laid-Open No. 2001-151283 can be exemplified.
  • Examples of the electric dispenser type container include a container equipped with a mechanism that automatically discharges a certain amount of the content when a hand is held over a sensor portion.
  • one discharge operation of the fixed quantity discharge container is defined as follows.
  • the fixed quantity dispensing container is a stroke-type pressing container
  • one discharging operation is an operation of pressing the container once with a full stroke.
  • the full stroke here means a state in which a load of 7 kg is applied for 3 seconds by stroke.
  • one discharge operation is an operation of pressing the pressing portion of the container once to squeeze and deform the container.
  • the squeeze deformation as used herein means a state in which a load of 7 kg is applied for 3 seconds by pressing.
  • the pressing portion of the container means, for example, the side peripheral portion of the container, although it varies depending on the shape of the container.
  • the fixed quantity dispensing container is an electric dispenser
  • one dispensing operation is, for example, an operation of holding a hand once over a sensor unit that controls the dispensing of the contents of the container.
  • the volume of the fixed-quantity discharge container assuming multiple discharges is not particularly limited, it is usually in the range of 5 mL or more and 2,000 mL or less from the viewpoint of containing the external skin preparation composition.
  • the external skin preparation composition used in the external skin preparation of the present invention (hereinafter also referred to as the external skin preparation composition of the present invention or the composition of the present invention) is one selected from the group consisting of lactic acid, pyruvic acid and urocanic acid.
  • a composition containing the above acid or salt thereof (A). The composition is housed in the fixed quantity discharge container and discharged from the fixed quantity discharge container for use.
  • Component (A) is one or more acids or salts thereof selected from the group consisting of lactic acid, pyruvic acid and urocanic acid.
  • Component (A) acts as a bactericidal or virucidal component.
  • Examples of salts of lactic acid, pyruvic acid and urocanic acid include alkali metal salts such as potassium salts and sodium salts of lactic acid or pyruvic acid; alkaline earth metal salts such as calcium salts and magnesium salts; amine salts; and ammonium salts. be done.
  • component (A) is preferably lactic acid or a salt thereof, more preferably one or more selected from the group consisting of lactic acid, potassium lactate, sodium lactate, and calcium lactate, and contains lactic acid. is more preferred.
  • component (A) contains lactic acid
  • the content of lactic acid or a salt thereof in the total amount of component (A) is preferably 80% by mass or more, more preferably 90% by mass, from the viewpoint of improving bactericidal or virucidal properties. % or more, and most preferably 100% by mass.
  • the content of component (A) in the composition of the present invention is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, and still more preferably 0.1% by mass or more, from the viewpoint of improving bactericidal or virucidal properties. It is 2% by mass or more, more preferably 0.3% by mass or more, and even more preferably 0.5% by mass or more. In addition, from the viewpoint of suppressing skin irritation, it is preferably 15% by mass or less, more preferably 10% by mass or less, even more preferably 5.0% by mass or less, even more preferably 4.0% by mass or less, and even more preferably is 3.0% by mass or less, more preferably 2.5% by mass or less, and even more preferably 2.0% by mass or less.
  • the content of component (A) in the composition is preferably 0.05% by mass or more and 15% by mass or less, more preferably 0.05% by mass or more and 10% by mass or less, and still more preferably 0.1% by mass. 10% by mass or less, more preferably 0.2% by mass or more and 5.0% by mass or less, even more preferably 0.3% by mass or more and 4.0% by mass or less, still more preferably 0.5% by mass or more and 3 0 mass % or less, more preferably 0.5 mass % or more and 2.5 mass % or less, and even more preferably 0.5 mass % or more and 2.0 mass % or less.
  • the “content of the component (A)” refers to the acid ("the component present in the acid form (A1)” and “the component present in the dissociated form (A2)”) and the amount obtained by converting the amount of the salt into the dissociated form.
  • the content of component (A1) in the composition of the present invention is preferably 0.02% by mass or more, more preferably 0.04% by mass or more, and still more preferably 0.04% by mass or more, from the viewpoint of improving bactericidal or virucidal properties. 05% by mass or more, more preferably 0.1% by mass or more, still more preferably 0.2% by mass or more, and even more preferably 0.3% by mass or more. In addition, from the viewpoint of suppressing skin irritation, the It is more preferably 2.5% by mass or less, even more preferably 2.0% by mass or less, and even more preferably 1.0% by mass or less.
  • the content of component (A1) in the composition of the present invention is preferably 0.02% by mass or more and 10% by mass or less, more preferably 0.04% by mass or more and 5.0% by mass or less, and still more preferably 0.05% by mass or more and 4.0% by mass or less, more preferably 0.1% by mass or more and 3.0% by mass or less, still more preferably 0.2% by mass or more and 2.5% by mass or less, still more preferably is 0.3% by mass or more and 2.0% by mass or less, more preferably 0.3% by mass or more and 1.0% by mass or less.
  • the content of the component (A1) in the composition of the present invention is such that among the acids derived from the component (A) present in the composition of the present invention, those present in the acid form are the components (A1), dissociated When the component (A2) is present in the form, it can be calculated from the following formula.
  • Content (% by mass) of component (A1) in the composition content (% by mass) of component (A) in the composition x molar ratio in the composition [(A1) / ⁇ (A1) + (A2 ) ⁇ ]
  • the "molar ratio [(A1) / ⁇ (A1) + (A2) ⁇ ] in the composition” refers to the total of component (A1) and component (A2) present in the composition (A1 ), which can be specifically calculated by the method described in Examples in the present invention.
  • the molar ratio [(A1)/ ⁇ (A1)+(A2) ⁇ ] in the composition is preferably 0.2 or more, more preferably 0.3 or more, and still more preferably from the viewpoint of improving bactericidal or virucidal properties.
  • the composition is 0.4 or more. From the viewpoint of suppressing skin irritation, it is preferably 0.6 or less, more preferably 0.55 or less, and even more preferably 0.5 or less. Then, among the acids derived from the component (A) present in the composition, when the acid present in the acid form is the component (A1) and the acid present in the dissociated form is the component (A2), the composition
  • the molar ratio [(A1) / ⁇ (A1) + (A2) ⁇ ] is preferably 0.2 to 0.6, more preferably 0.3 to 0.55, and still more preferably 0.4 0.5 or less.
  • the skin external preparation composition can further contain a nonionic thickener as component (B) from the viewpoint of improving the feeling of use.
  • a nonionic thickener as component (B) from the viewpoint of improving the feeling of use.
  • the term "good feeling in use” means that the composition for external use for skin is applied to the skin, dried, and then moistened with water with little squeaky feeling and good feel.
  • the component (B) used in the composition of the present invention is a water-soluble nonion from the viewpoint of improving the feeling of use, improving or maintaining the bactericidal or virucidal properties, and improving the solubility in the composition. It is preferably a viscous thickener.
  • the component (B) include cellulose ethers such as hydroxybutylmethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, and hydroxyethylcellulose; propylene glycol alginate, polyvinyl alcohol, polyvinylpyrrolidone, hydroxypropyl guar gum, locust bean gum, and amylose. , hydroxyethyl amylose, starch or derivatives thereof, and the like, and one or more of these can be used.
  • the component (B) is preferably one or more selected from the group consisting of cellulose ethers and polyvinyl alcohol from the viewpoint of maintaining the bactericidal or virucidal properties and improving the feeling of use of the composition.
  • hydroxybutylmethylcellulose more preferably one or more selected from the group consisting of hydroxybutylmethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxyethylcellulose, and polyvinyl alcohol, more preferably one or more selected from the group consisting of hydroxyethylcellulose and polyvinyl alcohol , and more preferably hydroxyethyl cellulose.
  • the polymerization degree of the polyvinyl alcohol used as the component (B) is preferably 500 or more, more preferably 700 or more, still more preferably 1,000 or more, and still more preferably 1,000 or more, from the viewpoint of improving the feeling of use of the composition. It is 500 or more, more preferably 2,000 or more, preferably 8,000 or less, more preferably 6,000 or less, and still more preferably 5,000 or less from the viewpoint of the ejection property of the composition.
  • the degree of polymerization of polyvinyl alcohol is preferably 500 or more and 8,000 or less, more preferably 700 or more and 8,000 or less, still more preferably 1,000 or more and 6,000 or less, and even more preferably 1,500 or more and 6,000 or less.
  • the saponification degree of polyvinyl alcohol is not particularly limited, it is preferably 80 mol% or more, more preferably 85 mol% or more, still more preferably 90 mol% or more, still more preferably from the viewpoint of improving the feeling of use of the composition. It is 95 mol % or more and 100 mol % or less.
  • a commercially available nonionic thickener can also be used as component (B).
  • hydroxyethyl cellulose examples include "Natrosol HEC 250HHX” manufactured by Ashland and "HEC Daicel 850SE” manufactured by Daicel. be done.
  • the content of component (B) in the composition in the present invention is preferably 0.01% by mass or more, more preferably 0.02% by mass, from the viewpoint of improving the feeling of use of the composition. % or more, more preferably 0.05% by mass or more, still more preferably 0.1% by mass or more, and even more preferably 0.2% by mass or more, and the ejection property of the composition in the present invention, and the sterilization or From the viewpoint of improving or maintaining virucidal properties, the content is preferably 20% by mass or less, more preferably 15% by mass or less, even more preferably 10% by mass or less, even more preferably 5% by mass or less, and even more preferably 3% by mass.
  • component (B) in the composition of the present invention is preferably 0.01% by mass or more and 20% by mass or less, more preferably 0.02% by mass or more and 15% by mass or less, and still more preferably 0.02% by mass or more and 15% by mass or less.
  • the external skin preparation composition of the present invention preferably further contains water.
  • the content of water in the composition is preferably 40% by mass or more, more preferably 70% by mass or more, and still more preferably 80% by mass or more, from the viewpoint of dissolving the component (A) and improving the dischargeability. , more preferably 85% by mass or more, still more preferably 90% by mass or more, still more preferably 95% by mass or more, and preferably 99.95% by mass or less.
  • the total content of component (A) and water in the external skin preparation composition of the present invention is preferably 70.05% by mass or more, more preferably 75% by mass or more, still more preferably 80% by mass or more, even more preferably 85% by mass or more, still more preferably 90% by mass or more, and even more preferably 95% by mass or more There is, and it is 100 mass % or less.
  • the external composition for skin of the present invention has a polarity close to that of the skin surface, is easily spreadable on the skin, and exhibits a bactericidal or virucidal component evenly on the intended application surface, and further contains a polyol. can contain.
  • the polyol those satisfying a logPow value of -2.0 or more, which is the octanol/water partition coefficient, can be preferably used.
  • a higher logPow value indicates higher hydrophobicity, and by including a predetermined amount of such a polyol in the composition, it can be expected that the composition will be made hydrophobic and will be more compatible with the skin than pure water.
  • the logPow values of polyols are calculated according to Renxiao Wang et al. , J. Chem. Inf. Model. 2007, Vol. 47, pp. 2140 can be used to determine the calculated value.
  • polyols include propylene glycol (1,2-propanediol), 1,3-propanediol, dipropylene glycol, 1,2-butylene glycol, 1,3-butylene glycol, 1,4-butylene glycol, 2,3-butanediol, 1,2-pentanediol, 1,5-pentanediol, 1,2-hexanediol, 2,5-hexanediol, 1,6-hexanediol, 1,2-heptanediol, 1 ,7-heptanediol, 1,2-octanediol, 1,8-octanediol, 1,2-nonanediol, 1,9-nonanediol, 1,2-decanediol, 1,10-decanediol, 1, Linear diols such as 2-dodecanediol, 1,12-dol,
  • the content of the polyol in the topical skin preparation composition is such that it can be easily spread over the skin and the bactericidal or virucidal component can be exhibited evenly on the intended application surface. Therefore, it is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, still more preferably 0.5% by mass or more, still more preferably 1.0% by mass or more, and still more preferably 1.0% by mass or more. 5% by mass or more, more preferably 2.0% by mass or more, and from the viewpoint of reducing stickiness during application, preferably 50% by mass or less, more preferably 30% by mass or less, and further preferably 20% by mass. % or less.
  • the polyol content in the external skin preparation composition is preferably 0.05% by mass or more and 50% by mass or less, more preferably 0.1% by mass or more and 50% by mass or less, and still more preferably 0.5% by mass. % by mass or more and 30% by mass or less, more preferably 1.0% by mass or more and 30% by mass or less, even more preferably 1.5% by mass or more and 20% by mass or less, still more preferably 2.0% by mass or more and 20% by mass % or less.
  • the skin external preparation composition of the present invention preferably contains a pH adjuster from the viewpoint of adjusting the pH to a suitable range.
  • the pH adjuster may be any component as long as it can adjust the pH of the composition to a desired range, and examples thereof include acid components, alkali components, buffer components, and the like. Among these, it is preferable to use at least an alkaline component as a pH adjuster from the viewpoint of adjusting the pH of the composition containing component (A) at 25° C. to the range described below (preferably 3.5 or higher).
  • the alkali component either an organic alkali agent or an inorganic alkali agent can be used, but the inorganic alkali agent is preferable from the viewpoints of solubility in water, availability and economy.
  • inorganic alkaline agents include metal hydroxides such as sodium hydroxide, potassium hydroxide and calcium hydroxide, metal carbonates such as sodium carbonate and sodium hydrogen carbonate, and the like. can be used. Among these, from the viewpoint of availability and economy, it is preferably one or more selected from the group consisting of alkali metal hydroxides and alkaline earth metal hydroxides, more preferably alkali metal metals It is a hydroxide, more preferably one or more selected from the group consisting of sodium hydroxide and potassium hydroxide, and still more preferably sodium hydroxide.
  • the content of the pH adjuster in the composition may be an amount that can adjust the pH of the composition to a desired range.
  • the external skin preparation composition contains an alkali metal hydroxide and an alkali One or more selected from the group consisting of hydroxides of earth metals is preferably used. Alkali metal hydroxides and alkaline earth metal hydroxides are as described above.
  • the metal ion concentration in the external skin preparation composition is preferably 0.002 mol/L or more, More preferably 0.005 mol/L or more, still more preferably 0.01 mol/L or more, still more preferably 0.02 mol/L or more.
  • the metal ion concentration in the skin external preparation composition is preferably 0.80 mol/L or less, more preferably 0.50 mol/L or less, still more preferably 0.30 mol/L, from the viewpoint of maintaining the mineral balance of the skin. L or less, more preferably 0.20 mol/L or less.
  • the metal ion concentration in the external skin composition is preferably 0.002 mol/L or more and 0.80 mol/L or less, more preferably 0.002 mol/L or more and 0.50 mol/L or less, and still more preferably 0.002 mol/L or more and 0.50 mol/L or less.
  • 005 mol/L or more and 0.50 mol/L or less more preferably 0.01 mol/L or more and 0.30 mol/L or less, still more preferably 0.02 mol/L or more and 0.20 mol/L or less.
  • the term "metal ion concentration in an external skin preparation composition” means the concentration of all metal ions present in the composition. In the composition used in the present invention, it is mainly the total concentration of the metal ions derived from the predetermined organic acid salt contained in the component (A) and the metal ions derived from the pH adjuster. In general, the presence of metal ions in the composition tends to inhibit the bactericidal efficacy of bactericidal agents such as benzalkonium chloride. However, in the skin external preparation composition used in the present invention, the bactericidal or virucidal properties of the component (A) are not inhibited by metal ions, and thus excellent bactericidal or virucidal properties can be exhibited. The metal ion concentration in the composition can be measured by an ion selective electrode method.
  • the external skin preparation composition of the present invention may optionally contain other ingredients such as surfactants, ultraviolet absorbers, antioxidants, preservatives, antiperspirants, fragrances, moisturizers, and feel agents. Modulators, anti-inflammatory agents and the like can also be included.
  • the external skin preparation composition of the present invention does not contain a monoalcohol having 4 or less carbon atoms such as ethanol and isopropanol. It is capable of expressing virucidal properties. Furthermore, from the viewpoint of suppressing skin irritation, the content of monoalcohol having 4 or less carbon atoms in the composition is preferably 60% by mass or less, more preferably 50% by mass or less, and still more preferably 40% by mass or less.
  • Component (C) Organic acid or salt thereof other than component (A)
  • the external skin preparation composition contains an organic acid other than component (A) or a salt thereof (hereinafter also referred to as "component (C)").
  • Bactericidal or virucidal properties can be expressed without blending.
  • the content of the organic acid or its salt (C) other than the component (A) in the composition is preferably 15% by mass or less, more preferably 10% by mass or less.
  • component (C) is an organic acid salt
  • content of the component (C) refers to the amount in terms of the organic acid.
  • the mass ratio [(C)/(A)] of an organic acid other than component (A) or a salt thereof (C) to component (A) in the external skin preparation composition has bactericidal or virucidal properties. From the viewpoint of maintenance and the viewpoint of suppressing skin irritation, it is preferably less than 1, more preferably 0.8 or less, still more preferably 0.6 or less, even more preferably 0.5 or less, and still more preferably 0.3 or less, more preferably 0.2 or less, still more preferably 0.1 or less, still more preferably 0.05 or less, still more preferably 0.01 or less, and even more preferably substantially zero be.
  • Examples of organic acids other than component (A) or salts thereof corresponding to component (C) include carboxylic acid compounds other than component (A), sulfonic acid compounds, and salts thereof.
  • Examples of the carboxylic acid compounds or salts thereof include aliphatic monocarboxylic acids having 4 or less carbon atoms such as acetic acid, propionic acid and butanoic acid; aromatic monocarboxylic acids such as benzoic acid; malonic acid, succinic acid, Aliphatic dicarboxylic acids such as glutaric acid, adipic acid, maleic acid, fumaric acid; Aromatic dicarboxylic acids such as phthalic acid and isophthalic acid; Polycarboxylic acids such as polyglutamic acid; Malic acid, glycolic acid, hydroxyacrylic acid, glyceric acid hydroxycarboxylic acids such as , tartaric acid and citric acid; acidic amino acids such as glutamic acid and aspartic acid; pyrrolidonecarboxylic acid;
  • Examples of the sulfonic acid compounds or salts thereof include aliphatic sulfonic acids such as methanesulfonic acid and ethanesulfonic acid; aromatic sulfonic acids such as p-toluenesulfonic acid and naphthalenesulfonic acid; and salts thereof.
  • Examples of the salt of the organic acid include alkali metal salts such as potassium salts and sodium salts; alkaline earth metal salts such as calcium salts and magnesium salts; amine salts; and ammonium salts.
  • the external skin preparation composition includes quaternary ammonium salts such as benzalkonium chloride and benzethonium chloride; alkyldiaminoethylglycine chlorides and alkylpolyamino chlorides; amphoteric surfactants such as ethylglycine; biguanides such as chlorhexidine gluconic acid; sodium hypochlorite; aldehydes such as glutaral, phthalal and formalin; It exhibits bactericidal or virucidal properties without adding any agents.
  • quaternary ammonium salts such as benzalkonium chloride and benzethonium chloride
  • alkyldiaminoethylglycine chlorides and alkylpolyamino chlorides amphoteric surfactants such as ethylglycine
  • biguanides such as chlorhexidine gluconic acid
  • sodium hypochlorite aldehydes
  • the content of the disinfectant in the composition is preferably 15% by mass or less, more preferably 10% by mass or less, even more preferably 5% by mass or less, and even more preferably is 3% by mass or less, more preferably 1% by mass or less, even more preferably 0.07% by mass or less, still more preferably 0.05% by mass or less, and even more preferably 0.03 % by mass or less, more preferably less than 0.01% by mass, and most preferably substantially 0% by mass.
  • the content of the fungicide in the composition is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, from the viewpoint of improving bactericidal or virucidal properties.
  • the mass ratio of the disinfectant to component (A) (sterilant/component (A)) is preferably 0.5 or less, more preferably 0.2 or less, and still more preferably, from the viewpoint of suppressing skin irritation. is 0.1 or less, more preferably 0.05 or less, still more preferably 0.03 or less, still more preferably 0.01 or less, and is most preferably substantially 0.
  • the mass ratio of the fungicide to component (A) is preferably 0.01 or more, and more Preferably it is 0.05 or more.
  • the above-mentioned agent that is a bactericide and also acts as a surfactant is defined as a bactericide.
  • the viscosity of the external preparation composition for skin at 25° C. is preferably 1.0 mPa ⁇ s or more from the viewpoint of uniforming the discharge amount per discharge operation of the metered discharge container and from the viewpoint of improving the applicability to the skin.
  • the viscosity of the external skin preparation composition the more difficult it is to control the amount supplied to the skin. It is advantageous in that it can be supplied.
  • the metered discharge container containing the composition is a stroke-type and pump-type pressing container, the viscosity of the composition at 25° C. is further increased from the viewpoint of enhancing dischargeability and spreadability during application.
  • the viscosity may be 5.0 mPa ⁇ s or more, further 100 mPa ⁇ s or more.
  • the viscosity may be 5.0 mPa ⁇ s or more, further 10.0 mPa ⁇ s or more.
  • the viscosity of the composition at 25° C. is more preferably 25,000 mPa ⁇ s or less, still more preferably 25,000 mPa ⁇ s or less, from the viewpoint of metered discharge performance. is 10,000 mPa s or less, more preferably 8,000 mPa s or less, even more preferably 6,500 mPa s or less, and even more preferably 2,000 mPa s or less. It is preferably 100 mPa ⁇ s or more, and more preferably 500 mPa ⁇ s or more.
  • the fixed-quantity discharge container containing the composition is an electric dispenser container, the viscosity of the composition at 25° C.
  • the viscosity may be 5.0 mPa ⁇ s or more, further 10.0 mPa ⁇ s or more. Specifically, the viscosity of the composition at 25° C. can be measured by the method described in Examples.
  • the skin external preparation composition preferably has a pH at 25°C of 3.5 or more, from the viewpoint of adjusting the content ratio of the component (A1) in the composition of the present invention and from the viewpoint of suppressing skin irritation. More preferably, it is 3.7 or more. From the viewpoint of improving bactericidal or virucidal properties, it is preferably 5.0 or less, more preferably 4.5 or less.
  • the pH of the external skin preparation composition at 25°C is preferably 3.5 or more and 5.0 or less, more preferably 3.5 or more and 4.5 or less, and still more preferably 3.7 or more and 4.5 or less. .
  • the pH of the composition at 25°C can be measured by the method described in Examples.
  • the external skin preparation composition used in the present invention may have fluidity at 25°C.
  • the form is not particularly limited, and may be, for example, liquid, gel, cream, or foam. It is preferably in a liquid form, from the viewpoint of being easy to spread on the skin and exhibiting the bactericidal or virucidal component evenly on the intended application surface.
  • it is preferably gel-like, cream-like, or foam-like.
  • the composition may be in the form of an emulsion composition, and the emulsion composition may be either an oil-in-water emulsion composition or a water-in-oil emulsion composition.
  • An oil-in-water emulsified composition is preferred from the viewpoint of easy application to the skin and the ability to exhibit the bactericidal or virucidal component evenly on the intended application surface.
  • it is preferably a water-in-oil emulsion composition.
  • the external preparation for skin of the present invention is more preferably in the following (I) or (II) mode.
  • An external skin preparation comprising an external skin preparation composition contained in a metered discharge container,
  • the composition contains one or more acids or salts thereof (A) selected from the group consisting of lactic acid, pyruvic acid and urocanic acid, Among the acids present in the composition, when an acid present in an acid form is defined as the component (A1), the component (A1 ) content of 0.05 mg or more and 80 mg or less,
  • the component (A) is lactic acid or a salt thereof,
  • the mass ratio [(C)/(A)] of the organic acid other than the component (A) or a salt thereof (C) to the component (A) in the composition is less than 1;
  • An external preparation for skin, wherein has a pH of 3.5 or more and 5.0 or less at 25°C.
  • An external skin preparation comprising an external skin preparation composition contained in a metered discharge container,
  • the composition contains one or more acids or salts thereof (A) selected from the group consisting of lactic acid, pyruvic acid and urocanic acid, Among the acids present in the composition, when an acid present in an acid form is defined as the component (A1), the component (A1 ) content of 0.05 mg or more and 80 mg or less,
  • the composition further contains a nonionic thickener (B), An external preparation for skin, wherein the composition has a viscosity of 100 mPa ⁇ s or more and 10,000 mPa ⁇ s or less at 25°C.
  • the external preparation for skin according to the aspect (I) exhibits a remarkable effect of improving bactericidal or virucidal properties by having the above constitution.
  • the mass ratio of the organic acid or its salt (C) other than the component (A) to the component (A) in the external skin preparation composition used for the external skin preparation of the aspect (I) [(C)/(A )] is less than 1, preferably 0.8 or less, more preferably 0.6 or less, even more preferably 0.5 or less, even more preferably 0.3 or less, even more preferably 0.2 or less, It is even more preferably 0.1 or less, still more preferably 0.05 or less, still more preferably 0.01 or less, and even more preferably substantially zero.
  • the external skin preparation composition used in the external skin preparation of the aspect (I) is 3.5 or more and 5.0 or less, preferably 3.5 or more and 4.5 or less, more preferably 3. .7 or more and 4.5 or less.
  • Other requirements and preferred ranges are the same as above.
  • the external preparation for skin according to the aspect (II) can achieve both bactericidal or virucidal properties and a better feel during use by having the above constitution.
  • the viscosity at 25° C. of the external skin preparation composition used in the external skin preparation of the aspect (II) is 100 mPa ⁇ s or more and 10,000 mPa from the viewpoint of maintaining the bactericidal or virucidal properties and improving the feeling of use.
  • s or less preferably 100 mPa s or more and 5,000 mPa s or less, more preferably 100 mPa s or more and 8,000 mPa s or less, still more preferably 100 mPa s or more and 2,000 mPa s or less more preferably 100 mPa ⁇ s or more and 1,000 mPa ⁇ s or less, still more preferably 100 mPa ⁇ s or more and 800 mPa ⁇ s or less, still more preferably 100 mPa ⁇ s or more and 700 mPa ⁇ s or less.
  • Other requirements and preferred ranges are the same as above.
  • the external preparation for skin of the present invention exhibits bactericidal or virucidal properties on the skin surface by leaving component (A), which is a bactericidal or virucidal component, contained in the discharged composition on the skin surface.
  • the external skin preparation of the present invention is preferably a leave-on skin preparation. That is, when the external skin preparation of the present invention is used, the composition discharged from a metered discharge container is applied to the skin by coating or the like, and then the composition is not removed by washing with water or the like, but left on the skin surface before use. .
  • the external skin preparation of the present invention is more preferably a leave-on skin preparation for fingers.
  • Bacteria or viruses for which the external preparation for skin of the present invention exhibits bactericidal or virucidal properties are not particularly limited as long as they are inactivated or killed by contact with acid. It is thought that the microorganisms described in the guidelines for infectious disease control in Japan can be applied.
  • the bacteria include Gram-positive bacteria such as Bacillus anthracis, Mycobacterium tuberculosis, Streptococcus hemolyticus, Staphylococcus aureus, and Streptococcus pneumoniae, or Gram-negative bacteria such as Tularemia, Yersinia pestis, Brucella, and Bacillus mallei.
  • Viruses include envelope viruses such as arenavirus, ebola virus, smallpox virus, nairovirus, marburg virus, coronavirus, monkeypox virus, beta coronavirus, influenza virus, respiratory syncytial virus, herpes virus, mumps virus, and varicella virus. ⁇ Herpes zoster virus, rubella virus, measles virus, etc., and non-enveloped viruses such as enterovirus, adenovirus, coxsackievirus, norovirus, rotavirus, etc.
  • bactericidal and virucidal properties were evaluated using Serratia as an example, but the target bacteria or viruses of the present invention are not limited thereto.
  • the present invention also provides a method for supplying one or more acids or salts thereof (A) selected from the group consisting of lactic acid, pyruvic acid and urocanic acid to an application site on the skin surface, comprising the following steps (I) and A method having (II) in order (hereinafter also simply referred to as "the method of the present invention") is provided.
  • Step (II) The composition containing the component (A) is discharged from a metered discharge container containing the composition by one discharge operation, and the application is performed.
  • step of supplying to the site when the acid existing in the acid form is (A1), it is discharged from the fixed amount discharge container by one discharge operation.
  • a step in which the content of component (A1) in the composition is 0.05 mg or more and 80 mg or less
  • the component (A), the composition containing the component (A), the metered discharge container, and preferred embodiments thereof are the same as described above.
  • step (I) water, soap, body soap, hand soap, etc. are used in advance to wash the application site on the skin surface. After washing, the skin is in a state where naturally occurring components such as lactic acid are washed away, and the defense against external bacteria and viruses is reduced. Therefore, step (II) is performed after step (I). It is preferred to apply the composition and carry out the method of the invention in.
  • step (I) After washing in step (I), the application site on the skin surface can be dried by air drying or the like before step (II) can be performed.
  • step (II) the composition containing component (A) is discharged onto the application site on the skin surface that has been washed in step (I).
  • the content of the component (A1) in the composition discharged from the metered discharge container by one discharge operation is 0.05 mg or more, preferably 0.1 mg or more, from the viewpoint of improving sterilization or virucidal properties.
  • the content of component (A1) in the composition discharged from the metered discharge container by one discharge operation is 0.05 mg or more and 80 mg or less, preferably 0.1 mg or more and 60 mg or less, more preferably 0 mg.
  • component (A1) in the composition ejected by one ejection operation can be obtained by the same method as described above.
  • the composition After supplying the composition to the skin in step (II), it is preferable to leave the composition on the skin surface without removing it by washing with water or the like. This is because the composition can be used as a leave-on preparation to leave the component (A), which is a bactericidal or virucidal component, on the skin surface, thereby imparting bactericidal or virucidal properties to the skin surface.
  • component (A) which is a bactericidal or virucidal component
  • An external skin preparation comprising an external skin preparation composition contained in a fixed-quantity discharge container,
  • the composition contains one or more acids or salts thereof (A) selected from the group consisting of lactic acid, pyruvic acid and urocanic acid, Among the acids present in the composition, when an acid present in an acid form is used as the component (A1), the component (A1) in the composition discharged from the metered discharge container by one discharge operation content of 0.05 mg or more and 80 mg or less.
  • the content of the component (A1) in the composition discharged from the fixed quantity discharge container by one discharge operation is preferably 0.1 mg or more and 60 mg or less, more preferably 0.2 mg or more and 60 mg or less, still more preferably 0.4 mg or more and 50 mg or less, still more preferably 0.5 mg or more and 50 mg or less, still more preferably 1.0 mg or more and 45 mg or less, still more preferably 2.0 mg or more and 45 mg or less, for external use on the skin according to ⁇ 1> agent.
  • the amount of the composition discharged from the fixed quantity discharge container in one discharge operation is preferably 0.05 g or more and 3.0 g or less, more preferably 0.1 g or more and 2.5 g or less, and still more preferably 0.2 g.
  • the external preparation for skin according to ⁇ 1> or ⁇ 2> which is 2.0 g or less.
  • ⁇ 4> Any of ⁇ 1> to ⁇ 3>, wherein the component (A) contains lactic acid or a salt thereof, preferably one or more selected from the group consisting of lactic acid, potassium lactate, sodium lactate, and calcium lactate, more preferably lactic acid. 1.
  • the skin external preparation according to 1. ⁇ 5> The component (A) contains lactic acid, and the content of lactic acid or a salt thereof in the total amount of component (A) is preferably 80% by mass or more, more preferably 90% by mass or more, and most preferably 100% by mass. %, the skin external preparation according to any one of ⁇ 1> to ⁇ 4>.
  • the content of component (A) in the composition is preferably 0.05% by mass or more and 15% by mass or less, more preferably 0.05% by mass or more and 10% by mass or less, and still more preferably 0.1% by mass or more. 10 mass % or less, more preferably 0.2 mass % or more and 5.0 mass % or less, even more preferably 0.3 mass % or more and 4.0 mass % or less, still more preferably 0.5 mass % or more3.
  • the skin external preparation according to 1.
  • the content of component (A1) in the composition is preferably 0.02% by mass or more and 10% by mass or less, more preferably 0.04% by mass or more and 5.0% by mass or less, and still more preferably 0.05% by mass. % or more and 4.0 mass % or less, more preferably 0.1 mass % or more and 3.0 mass % or less, still more preferably 0.2 mass % or more and 2.5 mass % or less, still more preferably 0.3 mass %
  • the external preparation for skin according to any one of ⁇ 1> to ⁇ 6>, which is 0.3% to 1.0% by mass, more preferably 0.3% to 1.0% by mass.
  • the composition when the component (A1) exists in an acid form and the component (A2) exists in a dissociated form, the composition is preferably 0.2 or more and 0.6 or less, more preferably 0.3 or more and 0.55 or less, still more preferably 0.4
  • the composition further contains a nonionic thickener as component (B).
  • the component (B) is a water-soluble nonionic thickener, preferably cellulose ethers, propylene glycol alginate, polyvinyl alcohol, polyvinylpyrrolidone, hydroxypropyl guar gum, locust bean gum, amylose, hydroxyethyl amylose, starch or derivatives thereof.
  • the degree of polymerization of the polyvinyl alcohol is preferably 500 or more and 8,000 or less, more preferably 700 or more and 8,000 or less, still more preferably 1,000 or more and 6,000 or less, still more preferably 1,500 or more and 6,000.
  • the saponification degree of the polyvinyl alcohol is preferably 80 mol% or more, more preferably 85 mol% or more, still more preferably 90 mol% or more, still more preferably 95 mol% or more, and 100 mol% or less.
  • the content of component (B) in the composition is preferably 0.01% by mass or more and 20% by mass or less, more preferably 0.02% by mass or more and 15% by mass or less, and still more preferably 0.05% by mass or more. 15% by mass or less, more preferably 0.1% by mass or more and 10% by mass or less, even more preferably 0.2% by mass or more and 5% by mass or less, still more preferably 0.2% by mass or more and 3% by mass or less,
  • the composition further contains water, and the water content in the composition is preferably 40% by mass or more, more preferably 70% by mass or more, still more preferably 80% by mass or more, and even more preferably 85% by mass. % or more, more preferably 90% by mass or more, still more preferably 95% by mass or more, and preferably 99.95% by mass or less, any one of ⁇ 1> to ⁇ 13> Skin external agent.
  • the total content of component (A) and water in the composition is preferably 70.05% by mass or more, more preferably 75% by mass or more, still more preferably 80% by mass or more, and even more preferably 85% by mass or more. , Still more preferably 90% by mass or more, still more preferably 95% by mass or more, and 100% by mass or less, any one of ⁇ 1> to ⁇ 14>.
  • ⁇ 16> The external preparation for skin according to any one of ⁇ 1> to ⁇ 15>, wherein the composition further contains a polyol.
  • ⁇ 17> The external preparation for skin according to ⁇ 16>, wherein the polyol satisfies a logPow value of -2.0 or more, which is an octanol/water partition coefficient.
  • the polyol is propylene glycol (1,2-propanediol), 1,3-propanediol, dipropylene glycol, 1,2-butylene glycol, 1,3-butylene glycol, 1,4-butylene glycol, 2,3 -butanediol, 1,2-pentanediol, 1,5-pentanediol, 1,2-hexanediol, 2,5-hexanediol, 1,6-hexanediol, 1,2-heptanediol, 1,7- Heptanediol, 1,2-octanediol, 1,8-octanediol, 1,2-nonanediol, 1,9-nonanediol, 1,2-decanediol, 1,10-decanediol, 1,2-dodecane Diol, 1,12-dodecanediol, 1,
  • the content of the polyol in the composition is preferably 0.05% by mass or more and 50% by mass or less, more preferably 0.1% by mass or more and 50% by mass or less, and still more preferably 0.5% by mass or more and 30% by mass. % by mass or less, more preferably 1.0% by mass or more and 30% by mass or less, even more preferably 1.5% by mass or more and 20% by mass or less, still more preferably 2.0% by mass or more and 20% by mass or less ,
  • the skin external preparation according to any one of ⁇ 16> to ⁇ 18>.
  • the composition is a pH adjuster, preferably an inorganic alkali agent, more preferably one or more selected from the group consisting of alkali metal hydroxides and alkaline earth metal hydroxides, and more preferably alkali metal metal water.
  • the skin according to any one of ⁇ 1> to ⁇ 19>, which contains an oxide, more preferably one or more selected from the group consisting of sodium hydroxide and potassium hydroxide, and still more preferably sodium hydroxide. External agents.
  • the metal ion concentration in the composition is preferably 0.002 mol/L or more and 0.80 mol/L or less, more preferably 0.002 mol/L or more and 0.50 mol/L or less, and still more preferably 0.005 mol/L or more.
  • 0.50 mol/L or less more preferably 0.01 mol/L or more and 0.30 mol/L or less, still more preferably 0.02 mol/L or more and 0.20 mol/L or less, ⁇ 1> to ⁇ 20>
  • the skin external preparation according to any one of 1.
  • the content of monoalcohols having 4 or less carbon atoms in the composition is preferably 60% by mass or less, more preferably 50% by mass or less, even more preferably 40% by mass or less, still more preferably 30% by mass or less, and more More preferably 10% by mass or less, still more preferably 5.0% by mass or less, still more preferably 1.0% by mass or less, still more preferably 0.05% by mass or less, and more
  • the external preparation for skin according to any one of ⁇ 1> to ⁇ 21>, which is more preferably less than 0.01% by mass, and most preferably substantially 0% by mass.
  • the content of the organic acid or its salt (C) other than the component (A) in the composition is preferably 15% by mass or less, more preferably 10% by mass or less, even more preferably 5% by mass or less, and even more preferably is 3% by mass or less, even more preferably 1% by mass or less, even more preferably 0.5% by mass or less, even more preferably less than 0.5% by mass, and even more preferably less than 0.1% by mass;
  • the external preparation for skin according to any one of ⁇ 1> to ⁇ 22>, which is most preferably substantially 0% by mass.
  • the mass ratio [(C)/(A)] of an organic acid other than component (A) or a salt thereof (C) to component (A) in the composition is preferably less than 1, more preferably 0.8 or less, more preferably 0.6 or less, even more preferably 0.5 or less, still more preferably 0.3 or less, still more preferably 0.2 or less, still more preferably 0.1 or less, more
  • the topical skin preparation according to ⁇ 23> which is more preferably 0.05 or less, still more preferably 0.01 or less, and even more preferably substantially 0.
  • the content of the fungicide in the composition is preferably 15% by mass or less, more preferably 10% by mass or less, even more preferably 5% by mass or less, even more preferably 3% by mass or less, and even more preferably 1% by mass. % or less, more preferably 0.07 mass % or less, still more preferably 0.05 mass % or less, still more preferably 0.03 mass % or less, and even more preferably 0.05 mass % or less.
  • the external preparation for skin according to any one of ⁇ 1> to ⁇ 24>, which is less than 01% by mass, most preferably substantially 0% by mass.
  • composition contains a disinfectant, and the content of the disinfectant in the composition is preferably 0.01% by mass or more, more preferably 0.05% by mass or more.
  • the skin external preparation according to any one of 1.
  • the viscosity of the composition at 25° C. is preferably 1.0 mPa ⁇ s or more, more preferably 2.0 mPa ⁇ s or more, still more preferably 3.0 mPa ⁇ s or more, and preferably 30,000 mPa ⁇ s or less.
  • the metered discharge container for containing the composition is a stroke type and pump type pressure container, and the viscosity of the composition at 25° C.
  • the metered discharge container containing the composition is a stroke-type and spray-type push-type container, and the viscosity of the composition at 25° C. is more preferably 800 mPa ⁇ s or less, still more preferably 500 mPa ⁇ s or less.
  • the constant-dispensing container containing the composition is a squeeze-type press container, and the viscosity of the composition at 25° C. is more preferably 25,000 mPa ⁇ s or less, still more preferably 10,000 mPa ⁇ s or less.
  • the external preparation for skin according to ⁇ 27> which is s or more.
  • the metered discharge container for containing the composition is an electric dispenser type container, and the viscosity of the composition at 25° C. is more preferably 800 mPa ⁇ s or less, still more preferably 500 mPa ⁇ s or less, and still more preferably 300 mPa.
  • the pH of the composition at 25°C is preferably 3.5 to 5.0, more preferably 3.5 to 4.5, even more preferably 3.7 to 4.5.
  • ⁇ 33> The external preparation for skin according to any one of ⁇ 1> to ⁇ 32>, which is an embodiment of (I) or (II) below.
  • An external skin preparation comprising an external skin preparation composition contained in a metered discharge container,
  • the composition contains one or more acids or salts thereof (A) selected from the group consisting of lactic acid, pyruvic acid and urocanic acid, Among the acids present in the composition, when an acid present in an acid form is defined as the component (A1), the component (A1 ) content of 0.05 mg or more and 80 mg or less,
  • the component (A) is lactic acid or a salt thereof,
  • the mass ratio [(C)/(A)] of the organic acid other than the component (A) or a salt thereof (C) to the component (A) in the composition is less than 1;
  • An external preparation for skin wherein the composition has a pH of 3.5 or more and 5.0 or less at 25°C.
  • An external skin preparation comprising an external skin preparation composition contained in a metered discharge container,
  • the composition contains one or more acids or salts thereof (A) selected from the group consisting of lactic acid, pyruvic acid and urocanic acid, Among the acids present in the composition, when an acid present in an acid form is defined as the component (A1), the component (A1 ) content of 0.05 mg or more and 80 mg or less,
  • the composition further contains a nonionic thickener (B),
  • An external preparation for skin wherein the composition has a viscosity of 100 mPa ⁇ s or more and 10,000 mPa ⁇ s or less at 25°C. ⁇ 34> The viscosity at 25° C.
  • the external skin preparation composition used in the external skin preparation of the aspect (II) is preferably 100 mPa ⁇ s or more and 5,000 mPa ⁇ s or less, more preferably 100 mPa ⁇ s or more and 8,000 mPa ⁇ s. s or less, more preferably 100 mPa s or more and 2,000 mPa s or less, even more preferably 100 mPa s or more and 1,000 mPa s or less, still more preferably 100 mPa s or more and 800 mPa s or less. , and more preferably 100 mPa ⁇ s or more and 700 mPa ⁇ s or less, the external preparation for skin according to ⁇ 33>.
  • ⁇ 35> The external preparation for skin according to any one of ⁇ 1> to ⁇ 34>, wherein the composition is liquid, gel, cream, or foam.
  • ⁇ 36> The external skin preparation according to any one of ⁇ 1> to ⁇ 35>, wherein the external skin preparation is a leave-on skin preparation, preferably a leave-on skin preparation for fingers.
  • An external skin product comprising an external skin preparation composition contained in a metered discharge container,
  • the composition contains one or more acids or salts thereof (A) selected from the group consisting of lactic acid, pyruvic acid and urocanic acid, Among the acids present in the composition, when an acid present in an acid form is used as the component (A1), the component (A1 ) content is 0.05 mg or more and 80 mg or less.
  • the step of supplying to the site among the acids present in the composition, when the acid present in the acid form is (A1), it is discharged from the fixed amount discharge container by one discharge operation.
  • a step in which the content of component (A1) in the composition is 0.05 mg or more and 80 mg or less
  • the sodium ion concentration of the external skin preparation composition was obtained by calculation from the blended amount of the pH adjuster (sodium hydroxide aqueous solution with a concentration of 1 mol/L).
  • the metal ions contained in the compositions of Examples and Comparative Examples are considered to be only sodium ions.
  • viscosity The viscosity of the external skin preparation composition was measured three times at 25° C. using a vibrating viscometer ("VM-10AL" manufactured by Sekonic Co., Ltd.), and the average value was obtained.
  • the measurement conditions according to the target viscosity are as follows: ⁇ Viscosity: 1 to 100mPa ⁇ s Jig M1, rotation speed 60 rpm ⁇ Viscosity over 100 mPa ⁇ s and 1,000 mPa ⁇ s or less Jig M2, rotation speed 30 rpm ⁇ Viscosity over 1,000 mPa s and 10,000 mPa s or less Jig M3, rotation speed 12 rpm ⁇ Viscosity over 10,000 mPa s and 100,000 mPa s or less Jig M4, rotation speed 6 rpm
  • pH The pH of the external skin preparation composition was measured at 25° C. using an electrode 6367-10D (manufactured by Horiba, Ltd.).
  • the content (% by mass) of the component (A1) in the external skin preparation composition is defined as, among acids derived from the component (A) present in the composition, the component (A1), which exists in an acid form, is dissociated.
  • the component (A2) is present in the form, it is obtained from the following formula.
  • Content (% by mass) of component (A1) in external skin preparation composition content (% by mass) of component (A) in composition ⁇ ⁇ molar ratio in composition [(A1)/ ⁇ (A1 ) + (A2)] ⁇
  • the content (mg) of the component (A1) in the ejected composition is determined by the following formula.
  • the "molar ratio [(A1)/ ⁇ (A1)+(A2)] in the composition” is obtained by the following calculation.
  • the molar amount of component (A1) is denoted as "HA”
  • the molar amount of component (A2) is denoted as " A- ".
  • the component (A) consists of a plurality of components
  • the following calculation method is defined in the present invention.
  • the molar ratio of each component [(A1) / ⁇ (A1) + (A2)] demand.
  • the molar ratio [(A1) / ⁇ (A1) + (A2)] in each component can be obtained.
  • Examples 1 to 12 Comparative Examples 1 to 8 (Preparation and Evaluation of External Skin Preparation Composition) After blending each component in the amount shown in Tables 1 and 2 and mixing at room temperature, using a hydrochloric acid aqueous solution with a concentration of 1 mol / L and / or a sodium hydroxide aqueous solution with a concentration of 1 mol / L as a pH adjuster A skin external preparation composition was prepared by adjusting the pH as described.
  • the blending amounts shown in Tables 1 and 2 are the active ingredient amounts (% by mass) of each component. After containing this skin external preparation composition in a metered discharge container, the amount shown in Tables 1 and 2 was discharged, and the following model experiment was conducted.
  • compositions shown in Tables 1 and 2 were applied to the skin surface in an amount corresponding to the condition of spreading over the entire palms of both hands by the method described later.
  • amount corresponding to the condition of spreading over the entire palms of both hands refers to the amount obtained by dividing the discharged composition amount (g) by 500 cm 2 , which is the average area of the palms of both hands.
  • the value of the average palm area of 500 cm 2 of both hands is obtained from Hyuk Choi et al., ⁇ Palm surface area database and estimation formula in Korean children using the alginate method'' (Applied Ergonomics, Vol.42 (2011), 873-882). It is a value estimated based on the value of TPSA (total palm surface area mean palm area with fingers) described in Table 2, which is the arithmetic mean value of the surface area of one hand. More specifically, the arithmetic mean of the total TPSA value (cm 2 ) for men and the total TPSA value (cm 2 ) for women shown in Table 2 is calculated, and double this value is measured on the palms of both hands. average area.
  • TPSA total palm surface area mean palm area with fingers
  • Lactic acid Fujifilm Wako Pure Chemical Co., Ltd. “lactic acid (active: 90%)”
  • Citric acid manufactured by FUJIFILM Wako Pure Chemical Industries, Ltd.
  • C2 Pyrrolidone carboxylic acid: manufactured by FUJIFILM Wako Pure Chemical Industries, Ltd.
  • pH adjuster hydrochloric acid aqueous solution with a concentration of 1 mol / L and / or with a concentration of 1 mol / L
  • Sodium hydroxide aqueous solution/hydrochloric acid aqueous solution FUJIFILM Wako Pure Chemical Co., Ltd.
  • Benzalkonium chloride "Benzalkonium chloride (50% aqueous solution)” manufactured by Tokyo Chemical Industry Co., Ltd.
  • the use of the external preparation for skin of this example has high bactericidal activity on the skin surface and can suppress skin irritation.
  • the skin external preparation composition used in this example unlike the benzalkonium chloride aqueous solution (Comparative Example 8), which is an existing disinfectant, was applied to the skin for some time. It can be seen that the bactericidal activity tends to improve rather than decrease as the temperature increases.
  • Examples 13-29 Ejection test of external skin preparation composition
  • a hydrochloric acid aqueous solution with a concentration of 1 mol / L and / or a sodium hydroxide aqueous solution with a concentration of 1 mol / L as a pH adjuster.
  • the pH was adjusted to prepare a skin external preparation composition.
  • the blending amount shown in Table 3 is the active ingredient amount (% by mass) of each component.
  • This external skin preparation composition was filled in a metered discharge container (stroke-type spray container X or pump container Y) shown in Table 3 to obtain a container-packed external skin preparation.
  • the filling amount of the skin external preparation composition was 50 mL in the spray container X and 120 mL in the pump container Y.
  • each ejection operation was performed once, and the amount of the composition ejected by one ejection operation was confirmed.
  • One discharge operation was performed by applying a load of 7 kg to the stroke of the metered discharge container for 3 seconds.
  • Example 16 ⁇ Using Fixed Dispensing Container X> 1: More squeaky than in Example 13 2: Slightly more squeaky than in Example 13 3: Equivalent to Example 13 4: Slightly less squeaky than in Example 13 5: Less squeaky than in Example 13 ⁇ When using the fixed quantity discharge container Y> 1: More squeaky than in Example 16 2: Slightly more squeaky than in Example 16 3: Equivalent to Example 16 4: Slightly less squeaky than in Example 16 5: Less squeaky than in Example 16
  • Lactic acid Fujifilm Wako Pure Chemical Co., Ltd. “lactic acid (active: 90%)”
  • B1 Polyvinyl alcohol: “JC-40” manufactured by Japan Vinyl Acetate & Poval Co., Ltd., polymerization degree 4,000, ken value 99.0 to 99.5 mol%
  • B2 Hydroxyethyl cellulose 1: "Natrosol HEC 250HHX” manufactured by Ashland Co., Ltd.

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Abstract

Préparation cutanée externe comprenant un récipient à éjection de quantité constante et une composition de préparation cutanée externe retenue à l'intérieur, la composition comprenant (A) soit au moins un acide sélectionné dans le groupe constitué de l'acide lactique, de l'acide pyruvique, et de l'acide urocanique ou leurs sels. Lorsque n'importe lequel des composés acides dans la composition qui est présent sous une forme acide est pris comme constituant (A1), alors la quantité du constituant (A1) contenu dans la composition éjectée du récipient à éjection de quantité constante par une opération d'éjection est de 0,05 à 80 mg.
PCT/JP2022/028041 2021-09-06 2022-07-19 Préparation cutanée externe WO2023032493A1 (fr)

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Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1498160A (en) * 1975-01-09 1978-01-18 Dermacia Ab Agent for skin treatment and a wet diaper prepared therewith
EP1050297A2 (fr) * 1999-05-03 2000-11-08 Fort James Corporation Produits tissés imbibés contenant un composé équilibrateur de pH pour la peau
JP2017025062A (ja) * 2015-07-23 2017-02-02 ジョンソン・アンド・ジョンソン・コンシューマー・インコーポレイテッド 低ｐＨを有する皮膚用組成物の局所送達
JP2019026592A (ja) * 2017-07-28 2019-02-21 イーダ株式会社 アルコール系消毒剤
JP2021161102A (ja) * 2020-04-03 2021-10-11 花王株式会社 皮膚を菌又はウイルスから防御する方法
WO2021246352A1 (fr) * 2020-06-05 2021-12-09 花王株式会社 Composition dermatologique externe pour une utilisation germicide et virucide
WO2022034911A1 (fr) * 2020-08-13 2022-02-17 花王株式会社 Composition pour préparation externe cutanée de type sans rinçage

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1498160A (en) * 1975-01-09 1978-01-18 Dermacia Ab Agent for skin treatment and a wet diaper prepared therewith
EP1050297A2 (fr) * 1999-05-03 2000-11-08 Fort James Corporation Produits tissés imbibés contenant un composé équilibrateur de pH pour la peau
JP2017025062A (ja) * 2015-07-23 2017-02-02 ジョンソン・アンド・ジョンソン・コンシューマー・インコーポレイテッド 低ｐＨを有する皮膚用組成物の局所送達
JP2019026592A (ja) * 2017-07-28 2019-02-21 イーダ株式会社 アルコール系消毒剤
JP2021161102A (ja) * 2020-04-03 2021-10-11 花王株式会社 皮膚を菌又はウイルスから防御する方法
WO2021246352A1 (fr) * 2020-06-05 2021-12-09 花王株式会社 Composition dermatologique externe pour une utilisation germicide et virucide
WO2022034911A1 (fr) * 2020-08-13 2022-02-17 花王株式会社 Composition pour préparation externe cutanée de type sans rinçage

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MATSUDA, TOSHIO ET AL.: "Antimicrobial Activities of Organic Acids Determined by Minimum Inhibitory Concentrations at Different pH Ranged from 4.0 to 7.0", NIPPON SHOKUHIN KOGYO GAKKAISHI, vol. 41, no. 10, 1 January 1994 (1994-01-01), pages 687 - 702, XP055624200 *

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