WO2020138420A1 - Composition d'émulsion eau dans l'huile contenant du nicotinamide - Google Patents

Composition d'émulsion eau dans l'huile contenant du nicotinamide Download PDF

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WO2020138420A1
WO2020138420A1 PCT/JP2019/051418 JP2019051418W WO2020138420A1 WO 2020138420 A1 WO2020138420 A1 WO 2020138420A1 JP 2019051418 W JP2019051418 W JP 2019051418W WO 2020138420 A1 WO2020138420 A1 WO 2020138420A1
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polyglyceryl
water
acid
emulsion composition
oil
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PCT/JP2019/051418
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Japanese (ja)
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真佐人 岡
閑久 前澤
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ロート製薬株式会社
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Priority to CN201980086108.8A priority Critical patent/CN113226480A/zh
Publication of WO2020138420A1 publication Critical patent/WO2020138420A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/06—Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/25—Silicon; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/27—Zinc; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/29—Titanium; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—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
    • 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
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/86—Polyethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/89—Polysiloxanes
    • A61K8/891—Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
    • A61K8/894—Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone modified by a polyoxyalkylene group, e.g. cetyl dimethicone copolyol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/08—Anti-ageing preparations

Definitions

  • the present invention relates to a water-in-oil emulsion composition containing nicotinic acid amide.
  • Nicotinic acid amide is one of the vitamins, and has been used as a component for promoting blood circulation, anti-inflammation, ceramide synthesis promotion, etc. in the skin care area, and as a whitening, anti-wrinkle and anti-aging agent. It is known that it also has an effect (for example, patent document 1).
  • Patent Document 2 An oil-in-water emulsion composition containing nicotinic acid amide, a specific active agent, and petrolatum has been proposed (Patent Document 2).
  • JP-A-2004-217629 Japanese Patent Laid-Open No. 2018-172304
  • the water-in-oil composition has excellent properties such as high moisture retention and water resistance, but on the other hand, it is difficult to impart sufficient stability due to problems such as easy separation, and the oil-in-water composition There are many formulation issues when compared to the product.
  • An object of the present invention is to provide a water-in-oil type emulsion composition containing a high concentration of nicotinic acid amide, which has good stability and usability.
  • the present invention provides the following water-in-oil emulsion compositions.
  • Item 1. (A) Nicotinic acid amide 3% by mass or more; (B) one or more surfactants selected from the group consisting of silicone-based surfactants, sorbitan ester surfactants, polyglycerin ester surfactants, and glycerin ester surfactants; and (C) A water-in-oil emulsion composition containing an oil-soluble thickener, which is one or more selected from the group consisting of clay-based thickeners, dextrin fatty acid esters, inulin fatty acid esters, and amino acid-based oil gelling agents.
  • Item 2. Item 2.
  • the component (B) is PEG-10 dimethicone, PEG-3 dimethicone, PEG-12 dimethicone, PEG/PPG-19/19 dimethicone, polysilicone 13, PEG-9 polydimethylsiloxyethyl dimethicone, methylpolysiloxane cetylmethyl.
  • Polysiloxane/poly(oxyethylene/oxypropylene)methyl polysiloxane copolymer lauryl PEG-9 polydimethylsiloxyethyl dimethicone, bisbutyl dimethicone polyglyceryl-3, polyglyceryl-3 polydimethylsiloxyethyl dimethicone, polyglyceryl-3 disiloxane dimethicone , Lauryl polyglyceryl-3 polydimethylsiloxyethyl dimethicone, sorbitan oleate, sorbitan sesquioleate, sorbitan trioleate, sorbitan sesquiisostearate, sorbitan isostearate, sorbitan tristearate, sorbitan sesquistearate, tristearin Acid sorbitan, polyglyceryl triisostearate-2, polyglyceryl isostearate-2, polyglyceryl-10 condensed ricinoleate, polyglyceryl-10 pen
  • the water-in-oil emulsion composition according to Item 1 or 2 which is one or more selected from the group consisting of glyceryl isostearate, glyceryl triisostearate, glyceryl stearate, glyceryl sesquistearate, and glyceryl tristearate.
  • the component (C) is dimethyl distearyl ammonium hectorite, benzyl dimethyl stearyl ammonium hectorite, distearyl dimethyl ammonium chloride treated aluminum magnesium silicate, dextrin palmitate, dextrin oleate, dextrin stearate, dextrin myristate, (palmitin.
  • the water-in-oil emulsion composition according to any one of 1.
  • Item 5 The water-in-oil emulsion composition according to any one of Items 1 to 4, further comprising (D) an ultraviolet absorber.
  • Item 6. The water-in-oil emulsion composition according to Item 5, wherein the total content of the component (D) is 20% by mass or less.
  • the component (B) is two or more kinds of surfactants selected from the group consisting of silicone-based surfactants, sorbitan ester surfactants, polyglycerin ester surfactants, and glycerin ester surfactants.
  • the component (B) is one or more kinds of surfactants selected from (B)-1 component silicone surfactant, and (B)-2 component sorbitan stearate, sorbitan isostearate, sorbitan sesquiisostearate, Sorbitan oleate, sorbitan sesquioleate, glyceryl stearate, glyceryl sesquistearate, glyceryl isostearate, glyceryl sesquiisostearate, glyceryl oleate, glyceryl sesquioleate, polyglyceryl-10 pentastearate, polyglyceryl pentaisostearate-10, Item 8.
  • the (D) UV absorber is a salicylic acid-based UV absorber, a cinnamic acid-based UV absorber, a benzoylmethane-based UV absorber, a benzoate derivative UV absorber, a triazine derivative UV absorber, or a benzalmalonate derivative UV absorber.
  • the (D) UV absorber is a salicylic acid-based UV absorber, a cinnamic acid-based UV absorber, a benzoylmethane-based UV absorber, a benzoate derivative UV absorber, a triazine derivative UV absorber, or a benzalmalonate derivative UV absorber.
  • Water-in-oil according to any one of Items 1 to 10, which is one or more selected from the group consisting of an agent, an octocrylene-based ultraviolet absorber, an imidazolesulfonic acid derivative ultraviolet absorber, and a benzophenone derivative ultraviolet absorber.
  • Emulsion composition Emulsion composition. Item 12.
  • the ultraviolet absorber (D) is 2-ethylhexyl paramethoxycinnamate, 4-tert-butyl-4′-methoxydibenzoylmethane, 2-[4-(diethylamino)-2-hydroxybenzoyl]benzoic acid hexyl ester, 2,4-bis-[ ⁇ 4-(2-ethylhexyloxy)-2-hydroxy ⁇ -phenyl]-6-(4-methoxyphenyl)-1,3,5-triazine, 2,4,6-tris[ Item 1 to 11, which is one or more selected from the group consisting of 4-(2-ethylhexyloxycarbonyl)anilino]-1,3,5-triazine and 2-phenylbenzimidazole-5-sulfonic acid.
  • the water-in-oil emulsion composition according to any one of claims 1 to 5.
  • the present invention can provide a water-in-oil emulsion composition having excellent stability.
  • the unit "mass%" of the content is synonymous with “g/100g”.
  • Formulations containing a high concentration of nicotinamide having various effects are very useful for producing multifunctional formulations, but water-in-oil emulsion compositions contain a high concentration of nicotinamide. If they are used, the formulation may become unstable, sticky, and sticky, which may affect the feeling of use. According to the present inventors, it is extremely difficult to obtain a water-in-oil emulsion composition that has both good stability and usability while containing a high concentration of nicotinic acid amide. Was found.
  • the conventional water-in-oil composition system cannot stably emulsify a high concentration of nicotinic acid amide, and contains a high concentration of nicotinic acid amide that achieves both good usability and sufficient stability.
  • a water-in-oil emulsion composition For example, in a water-in-oil emulsion composition having a characteristic feeling of use by containing an emulsifying silicone elastomer, a surfactant, an ultraviolet absorber, etc., in addition to not having sufficient stability, It lacks general versatility because it has a characteristic feeling of use that is different from the general emulsified composition in that the aqueous phase is released when a shear stress is applied.
  • water-in-oil type emulsion composition having improved stability at a relatively high temperature by combining an emulsifying silicone elastomer and a solidifying agent, but it cannot be said that the composition has sufficient stability and is solid. It contains a large amount of wax, giving it a squeaky feel.
  • the water-in-oil type emulsion composition of the present invention (A) Nicotinic acid amide 3% by mass or more; (B) a surfactant, which is one or more selected from the group consisting of a silicone-based surfactant, a sorbitan ester surfactant, a polyglycerin ester surfactant, and a glycerin ester surfactant; and (C) clay.
  • the nicotinic acid amide contained in the water-in-oil emulsion composition of the present invention is an amide compound of nicotinic acid (vitamin B 3 /niacin) and is a water-soluble vitamin.
  • Nicotinic acid amide may be an extract from a natural product or a product synthesized by a known method. Specifically, those listed in the 17th revised Japanese Pharmacopoeia can be used. It is known to have a blood circulation promoting action and a rough skin improving action, as well as a melanin production inhibiting action and a whitening effect.
  • the content of the component (A) with respect to the total amount of the water-in-oil type emulsion composition is appropriately set depending on the balance with other components.
  • the content of the component (A) is preferably 20% by mass or less, and more preferably from the viewpoint of alleviating the dryness, stickiness and irritation that may occur with nicotinic acid amide. It is 10 mass% or less, more preferably 8 mass% or less.
  • the content necessary for sufficiently imparting the effects of whitening, anti-aging and the like is such that the total content of the component (A) is 3% by mass or more based on the total amount of the water-in-oil emulsion composition.
  • the component (A) can be preferably 4% by mass or more, more preferably 5% by mass or more.
  • the total content of the component (A) is preferably 3% by mass to 20% by mass, more preferably 3% by mass to 15% by mass, further preferably It is 3% by mass to 10% by mass, and even more preferably 3% by mass to 8% by mass.
  • surfactants selected from the group consisting of silicone-based surfactants, sorbitan ester surfactants, polyglycerin ester surfactants, and glycerin ester surfactants
  • the surfactant contained in the water-in-oil emulsion composition of the present invention is selected from the group consisting of silicone-based surfactants, sorbitan ester surfactants, polyglycerin ester surfactants, and glycerin ester surfactants. One or more of them are listed.
  • the HLB value of such a surfactant is preferably 15 or less, more preferably 10 or less, even more preferably 9 or less, even more preferably 8 or less, most preferably 2- 6 surfactants.
  • the HLB Hydrophilic-lipophilic Balance
  • HLB is an index showing the hydrophilic-lipophilic balance and is calculated by the following (Formula 1) by Oda and Teramura et al.
  • HLB ( ⁇ inorganic value/ ⁇ organic) ⁇ 10 (Equation 1)
  • IOB Inorganic-Organic balance
  • IOB Inorganic-Organic balance
  • silicone surfactant contained in the water-in-oil type emulsion composition of 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 medicines, quasi drugs or cosmetics.
  • the silicone-based surfactant is preferably a polyether-modified silicone-based surfactant, a polyether/alkyl co-modified silicone-based surfactant, a polyglycerin-modified silicone-based surfactant, or a polyglycerin-alkyl-co-modified silicone-based surfactant.
  • An activator is exemplified. More specifically, PEG-10 dimethicone, PEG-3 dimethicone, PEG-12 dimethicone, PEG/PPG-19/19 dimethicone, polysilicone 13, which is a polyoxyethylene/methylpolysiloxane copolymer, and PEG-9.
  • Polyether-modified silicone surfactants such as polydimethylsiloxyethyldimethicone; methylpolysiloxane/cetylmethylpolysiloxane/poly(oxyethylene/oxypropylene)methylpolysiloxane copolymer, lauryl PEG-9 polydimethylsiloxyethyldimethicone Polyether/alkyl co-modified silicone surfactants; bisbutyldimethicone polyglyceryl-3, polyglyceryl-3 polydimethylsiloxyethyl dimethicone, polyglyceryl-3 disiloxane dimethicone and other polyglycerin-modified silicone surfactants; lauryl polyglyceryl-3 Examples thereof include polyglycerin/alkyl co-modified silicone surfactants such as polydimethylsiloxyethyl dimethicone.
  • PEG-10 dimethicone PEG-3 dimethicone
  • PEG-12 dimethicone PEG/PPG-19/19 dimethicone
  • polysilicone 13 PEG-9 polydimethylsiloxyethyl dimethicone, methyl polysiloxane.
  • dimethylsiloxyethyl dimethicone especially PEG-9 polydimethylsiloxyethyl dimethicone, PEG-10 dimethicone, PEG-9 polydimethylsiloxyethyl dimethicone, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, lauryl polyglyceryl-3 polydimethylsiloxy.
  • Ethyl dimethicone is particularly preferred.
  • silicone-based surfactant a commercially available product can be used or a synthetic product can be used.
  • KF-6017 (HLB4.5, Shin-Etsu Chemical Co., Ltd.), KF-6019 (HLB4.5, Shin-Etsu Chemical Co., Ltd.), KF-6015 (HLB4.5, HLB4.5, Shin-Etsu Chemical Co., Ltd., SH3772M (HLB6, Toray Dow Corning) SH3775M (HLB5, Toray Dow Corning) BY-11-030 (HLB6, Toray Dow Corning), KF-6004 (HLB9) Shin-Etsu Chemical Co., Ltd.), KF-6011 (HLB14.5, Shin-Etsu Chemical Co., Ltd.), FZ-2222, FZ-2233, KF-6028, (HLB4, Shin-Etsu Chemical Co., Ltd.), ABIL EM90 (Made by Goldschmidt) ), KF-6048 (HLB3.5, Shin-Etsu Chemical Co., Ltd.), KF-6038 (HLB4.5, Shin-Et
  • the silicone surfactant may be used alone or in combination of two or more.
  • ester-based surfactant The ester-based surfactant that can be contained in the water-in-oil type emulsion composition of the present invention is not particularly limited as long as it is used as a component of, for example, a skin external preparation in the fields of medicine, quasi drugs or cosmetics.
  • the ester-based surfactant is preferably exemplified by a sorbitan ester surfactant, a polyglycerin ester surfactant, and a glycerin ester surfactant.
  • a sorbitan ester surfactant e.g., sorbitan oleate, sorbitan sesquioleate, sorbitan trioleate, sorbitan sesquiisostearate, sorbitan isostearate, sorbitan triisostearate, sorbitan stearate, sorbitan tristearate, sorbitan sesquistearate.
  • Polyglyceryl ester surfactants such as polyglyceryl-10 hydroxystearate, polyglyceryl-6 condensed ricinoleate, polyglyceryl-6 pentaisostearate, polyglyceryl-6 pentaoleate, polyglyceryl-6 pentahydroxystearate; glyceryl oleate, sesquiolein Examples thereof include glyceryl ester surfactants such as glyceryl acid salt, glyceryl trioleate, glyceryl sesquiisostearate, glyceryl isostearate, glyceryl triisostearate,
  • sorbitan oleate sorbitan sesquioleate, sorbitan trioleate, sorbitan sesquiisostearate, sorbitan isostearate, sorbitan triisostearate, sorbitan sesquistearate, tristearic acid.
  • condensed ricinoleic acid polyglyceryl-10, pentaisostearate polyglyceryl-10, pentaoleic acid polyglyceryl-10, pentastearic acid polyglyceryl-10, or pentahydroxystearic acid polyglyceryl-10 is even more preferable. ..
  • ester-based surfactant a commercially available product can be used or a synthetic product can be used.
  • NIKKOL SO-10V manufactured by Nikko Chemicals
  • NIKKOL SO-15V manufactured by Nikko Chemicals
  • NIKKOL SO-30V manufactured by Nikko Chemicals
  • NIKKOL SI-15RV NIKKOL SI-15RV
  • Such a component (B) can contribute to both the stability of the formulation and the feeling of use even when the nicotinic acid amide of the component (A) is contained in a high concentration.
  • the total content of the component (B) with respect to the total amount of the water-in-oil emulsion composition is preferably 0.5% by mass or more, more preferably 1% by mass. % Or more, more preferably 1.5% by mass or more, even more preferably 2% by mass or more, and most preferably 3% by mass or more.
  • the total content of the component (B) with respect to the total amount of the water-in-oil emulsion composition is preferably 20% by mass or less, more preferably 10% by mass or less, and further preferably 8% by mass or less. Yes, even more preferably 6% by mass or less, and most preferably 4% by mass or less.
  • the total content of the component (B) with respect to the total amount of the water-in-oil emulsion composition is preferably 0.5 to 8% by mass, more preferably 0.5 to 5% by mass, and further preferably 1 to 5% by mass. , Even more preferably 2 to 5% by mass, most preferably 2 to 4% by mass.
  • the ratio of the total content of the component (B) to the component (A) is not particularly limited, but is preferably 1 part by mass of the total content of the component (A).
  • the amount is 0.2 to 1 part by mass, more preferably 0.4 to 1.0 part by mass, still more preferably 0.4 to 0.8 part by mass.
  • the component (B) used in the water-in-oil emulsion composition of the present invention is at least one selected from silicone-based surfactants, sorbitan ester surfactants, polyglycerin ester surfactants, and glycerin ester surfactants.
  • the surfactant is preferably PEG-9 polydimethylsiloxyethyl dimethicone, PEG-10 dimethicone, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, lauryl polyglyceryl-3 polydimethylsiloxyethyl dimethicone, sorbitan stearate, isostearic acid.
  • PEG-9 polydimethylsiloxyethyl dimethicone PEG-10 dimethicone, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, lauryl polyglyceryl-3 polydimethylsiloxyethyl dimethicone, polyglyceryl-10 pentastearate, polyglyceryl pentaisostearate, polyglyceryl-10 pentahydroxystearate, pentaolein
  • the component (B) used in the water-in-oil emulsion composition of the present invention is at least two selected from silicone-based surfactants, sorbitan ester surfactants, polyglycerin ester surfactants, and glycerin ester surfactants.
  • the surfactant is preferably at least one of PEG-9 polydimethylsiloxyethyl dimethicone, PEG-10 dimethicone, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, lauryl polyglyceryl-3 polydimethylsiloxyethyl dimethicone and stearin.
  • a silicone-based surfactant As one specific embodiment of the combination of two or more kinds of the component (B) used in the water-in-oil type emulsion composition of the present invention, and the component (B) as a constituent element, at least a silicone-based surfactant.
  • a combination of two or more kinds of surfactants selected from is preferable.
  • PEG-9 polydimethylsiloxyethyl dimethicone PEG-10 dimethicone
  • lauryl PEG-9 polydimethylsiloxyethyl dimethicone and lauryl polyglyceryl-3 polydimethylsiloxyethyl dimethi
  • component (B) used in the water-in-oil type emulsion composition of the present invention (B)-1 component One or more surfactants selected from silicone-based surfactants, and (B)-2 component sorbitan stearate, sorbitan isostearate, sorbitan sesquiisostearate, sorbitan oleate, sesquioleic acid.
  • (B)-1 component selected from the group consisting of PEG-9 polydimethylsiloxyethyl dimethicone, PEG-10 dimethicone, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, and lauryl polyglyceryl-3 polydimethylsiloxyethyl dimethicone
  • PEG-9 polydimethylsiloxyethyl dimethicone PEG-9 polydimethylsiloxyethyl dimethicone
  • lauryl PEG-9 polydimethylsiloxyethyl dimethicone lauryl polyglyceryl-3 polydimethylsiloxyethyl dimethicone
  • B)-2 component selected from polyglyceryl pentastearate-10, polyglyceryl pentaisostearate-10, polyglyceryl pentahydroxystearate-10, and polyglyceryl pentaoleate-10 It is even more preferable to contain the above surfactants.
  • the B-1 component is selected from the group consisting of PEG-9 polydimethylsiloxyethyl dimethicone, PEG-10 dimethicone, lauryl PEG-9 polydimethylsiloxyethyl dimethicone, and lauryl polyglyceryl-3 polydimethylsiloxyethyl dimethicone 1
  • a combination of two or more kinds of surfactants can be exemplified.
  • oil-soluble thickeners selected from the group consisting of clay-based thickeners, dextrin fatty acid esters, inulin fatty acid esters, and amino acid oil gelling agents.
  • the oil-soluble thickener contained in the water-in-oil type emulsion composition of the present invention is not particularly limited as long as it is used as a component of an external preparation for skin in the fields of medicines, quasi drugs or cosmetics.
  • the oil-soluble thickener contained in the water-in-oil emulsion composition of the present invention is selected from the group consisting of clay-based thickeners, dextrin fatty acid esters, inulin fatty acid esters, and amino acid-based oil gelling agents 1. There are more than one species. At least one selected from the group consisting of clay-based thickeners, dextrin fatty acid esters, and inulin fatty acid esters is preferable.
  • the “clay thickener” means an organic modified clay mineral, and examples thereof include quaternary ammonium salt type cation modified clay mineral. Specific examples include dimethyl distearyl ammonium hectorite, dimethyl alkyl ammonium hectorite, dimethyl distearyl ammonium bentonite, benzyl dimethyl stearyl ammonium hectorite, distearyl dimethyl ammonium chloride treated aluminum magnesium silicate, and the like.
  • such organically modified clay mineral is preferably dimethyl distearyl ammonium hectorite, dimethyl alkyl ammonium hectorite, dimethyl distearyl ammonium bentonite, or benzyl dimethyl stearyl ammonium hectorite, among which, Dimethyl distearyl ammonium hectorite or benzyl dimethyl stearyl ammonium hectorite is more preferred, and dimethyl distearyl ammonium hectorite is even more preferred.
  • the clay-based thickener a commercially available product can be used or a synthetic product can be used.
  • Benton 38V Benton 38VG (manufactured by Elementis Japan KK)
  • Benton 38VCG manufactured by Elementis Japan KK
  • Benton 27 manufactured by Elementis Japan KK
  • dextrin fatty acid ester examples include dextrin derivatives such as dextrin palmitate, dextrin oleate, dextrin stearate, dextrin myristate, (palmitic acid/ethylhexanoic acid) dextrin, and (palmitic acid/hexyldecanoic acid) dextrin. It is illustrated.
  • such dextrin fatty acid ester is preferably a dextrin derivative such as dextrin palmitate, dextrin myristic acid, dextrin (palmitic acid/ethylhexanoic acid), and dextrin (palmitic acid/hexyldecanoic acid), More preferable are dextrin palmitate, dextrin myristate, and (palmitic acid/hexyldecanoic acid) dextrin.
  • dextrin fatty acid ester a commercially available product can be used or a synthetic product can be used.
  • the inulin fatty acid ester includes, but is not limited to, inulin stearate, inulin palmitate, and inulin myristate, and inulin stearate is particularly preferable.
  • the fatty acid inulin can be a commercially available product or can be synthesized and used.
  • amino acid oil gelling agent is not limited, and examples thereof include dibutyl lauroyl glutamide and dibutyl ethyl hexanoyl glutamide.
  • amino acid oil gelling agent a commercially available product can be used or a synthetic product can be used.
  • the commercially available products include, but are not limited to, GB-21 (manufactured by Ajinomoto Co.) and EB-21 (manufactured by Ajinomoto Co.).
  • Such a component (C) can contribute to both the stability of the preparation and the feeling of use even when the nicotinic acid amide of the component (A) is contained in a high concentration.
  • the oil-soluble thickener of the present invention is an oil-soluble thickener that is at least one selected from the group consisting of clay-based thickeners, dextrin fatty acid esters, inulin fatty acid esters, and amino acid-based oil gelling agents.
  • clay-based thickeners dextrin fatty acid esters, inulin fatty acid esters, and amino acid-based oil gelling agents.
  • benzyl dimethyl stearyl ammonium hectorite dimethyl distearyl ammonium hectorite, inulin stearate, (palmitic acid/ethyl hexanoic acid) dextrin, palmitic acid dextrin, myristic acid dextrin, dibutyl lauroyl glutamide, and dibutyl ethyl hexanoyl glutamide.
  • oil-soluble thickeners selected from the group consisting of the following: dimethyl distearyl ammonium hectorite, inulin stearate, (palmitic acid/ethylhexanoic acid) dextrin, dextrin palmitate, and It is more preferable to contain one or more oil-soluble thickeners selected from the group consisting of dextrin myristate, dimethyl distearyl ammonium hectorite, inulin stearate, (palmitic acid/ethylhexanoic acid) dextrin, and palmitin.
  • oil-soluble thickeners selected from the group consisting of acid dextrins, and one or more oil-soluble selected from the group consisting of dimethyl distearyl ammonium hectorite and inulin stearate. It is particularly preferred to include a thickening agent.
  • the total content of the component (C) with respect to the total amount of the water-in-oil type emulsion composition may be appropriately adjusted depending on the type and combination of the component (C) to be used. From the viewpoint of being suppressed, it is preferably 5% by mass or less, more preferably 3% by mass or less, and even more preferably 2% by mass or less.
  • the total content of the component (C) with respect to the total amount of the water-in-oil type emulsion composition is preferably 0.1% by mass or more, and more preferably 0.2, from the viewpoint of providing better stability.
  • the content is at least mass%, more preferably at least 0.5 mass%, and even more preferably at least 1 mass%.
  • the total content of the component (C) with respect to the total amount of the water-in-oil type emulsion composition is preferably 0.5 to 5% by mass, more preferably 0.5 to 5% by mass from the viewpoint of providing better thermal stability. It is 3% by mass, more preferably 0.5 to 2% by mass.
  • the ratio of the content of the component (C) to the component (A) is not particularly limited, but is preferably 0 with respect to the total content of the component (A) of 1 part by mass.
  • UV absorber The water-in-oil type emulsion composition of the present invention, from the viewpoint of improving the feeling of use, stability, etc., unless the effects of the present invention are impaired, the above-mentioned (A) component, (B) component, and (C) component, Besides, (D) an ultraviolet absorber may be contained.
  • the ultraviolet absorber used in the present invention is not particularly limited as long as it is used as a component of, for example, a skin external preparation in the fields of medicines, quasi drugs or cosmetics.
  • the UV absorber is not limited, but preferably salicylic acid UV absorbers, cinnamic acid UV absorbers, benzoylmethane UV absorbers, benzoic acid ester derivative UV absorbers, triazine derivative UV absorbers, benzal It may be a malonate derivative UV absorber, an octocrylene-based UV absorber, an imidazolesulfonic acid derivative UV absorber, a benzophenone derivative UV absorber, or the like.
  • salicylic acid-based UV absorbers such as 2-ethylhexyl salicylate, homomenthyl salicylate, or ethylene glycol salicylate; diparamethoxycinnamic acid mono-2-ethylhexanoate glyceryl, paradihydroxypropylbenzoic acid.
  • Cinnamic acid UV absorbers such as ethyl or 2-ethylhexyl paramethoxycinnamate; Benzoylmethane UV absorbers such as 4-tert-butyl-4'-methoxydibenzoylmethane; 2-[4-(diethylamino )-2-Hydroxybenzoyl]benzoic acid hexyl ester and other benzoic acid ester derivative UV absorbers; 2-methoxyhexyl dimethoxybenzylidenedioxoimidazolidinepropionate; 2,2′-methylenebis[6-(2H-benzotriazol-2) Iyl)-4-(1,1,3,3-tetramethylbutyl)phenol]; 2,4-bis-[ ⁇ 4-(2-ethylhexyloxy)-2-hydroxy ⁇ -phenyl]-6-(4 Triazines such as -methoxyphenyl)-1,3,5-triazine, diethy
  • examples of such an ultraviolet absorber include 2-ethylhexyl paramethoxycinnamate, 4-tert-butyl-4′-methoxydibenzoylmethane, 2-[4-(diethylamino)- 2-Hydroxybenzoyl]benzoic acid hexyl ester, dimethoxybenzylidene dioxoimidazolidine propionate 2-ethylhexyl, 2,2′-methylenebis[6-(2H-benzotriazol-2yl)-4-(1,1,3) ,3-Tetramethylbutyl)phenol], 2,4-bis-[ ⁇ 4-(2-ethylhexyloxy)-2-hydroxy ⁇ -phenyl]-6-(4-methoxyphenyl)-1,3,5- Triazine, 2,4,6-tris[4-(2-ethylhexyloxycarbonyl)anilino]-1,3,5-triazine, 2,4,6-
  • the ultraviolet absorber can be a commercially available product or can be synthesized and used.
  • the total content of the ultraviolet absorber relative to the total amount of the water-in-oil type emulsion composition is preferably 20% by mass or less, more preferably 15% by mass or less, and further preferably Is 10% by mass or less.
  • the total content of the ultraviolet absorber with respect to the total amount of the water-in-oil emulsion composition is preferably 1% by mass or more, more preferably 3% by mass or more, even more preferably 6% by mass or more, even more preferably Is 7% by mass or more.
  • the total content of the ultraviolet absorber with respect to the total amount of the water-in-oil emulsion composition is preferably 1 to 20% by mass, more preferably 3 to 20% by mass, still more preferably 5 to 20% by mass, and particularly preferably It is 6 to 20% by mass, most preferably 7 to 15% by mass.
  • the ratio of the content of the ultraviolet absorber to the component (A) is not particularly limited, but it is preferably 0. 0 with respect to the total content of the component (A) of 1 part by mass.
  • the amount is 6 to 2 parts by mass, more preferably 1 to 2 parts by mass, still more preferably 1.4 to 2 parts by mass.
  • the water-in-oil type emulsion composition of the present invention from the viewpoint of improving the feeling of use, stability, etc., unless the effects of the present invention are impaired, the above-mentioned (A) component, (B) component, and (C) component, In addition to the above, it may further contain (E) an ultraviolet protective agent. Specific examples thereof include fine particle titanium oxide, fine particle zinc oxide, iron oxide, and cerium oxide, but are not limited thereto. In the present invention, the ultraviolet protective agent (E) is preferably, but not limited to, fine particle titanium oxide or fine particle zinc oxide. These (E) UV protection agents may be surface-treated.
  • Examples of the type of surface treatment agent used for the surface treatment include amphipathic components, silicone components, silane compounds, fatty acid components, alkyl titanates, and the like, but are not particularly limited thereto, and these surface treatment agents include 1 You may use 1 type, or 2 or more types.
  • Examples of the amphipathic component of the surface treatment agent include metal soap, perfluoroalkylethyl phosphate diethanolamine salt, fluoroalkyl acrylate/polyalkylene glycol acrylate polymer, perfluoropolyether phosphoric acid, perfluoropolyether chain.
  • anionic or cationic polymers polyurethane-27 or polyurethane-26
  • hydrogenated lecithin acylated amino acids
  • ⁇ -tocopherol phosphate ester salt etc.
  • It may be a monomer type or a polymer type as long as it exhibits a sorption property.
  • silicone component of the surface treatment agent examples include dimethylpolysiloxane, methylhydrogenpolysiloxane, ⁇ -monoalkoxypolydimethylsiloxane, ⁇ -dialkoxypolydimethylsiloxane, ⁇ -trialkoxypolydimethylsiloxane, and triethoxysilylethyl.
  • silicone component of the surface treatment agent examples include dimethylpolysiloxane, methylhydrogenpolysiloxane, ⁇ -monoalkoxypolydimethylsiloxane, ⁇ -dialkoxypolydimethylsiloxane, ⁇ -trialkoxypolydimethylsiloxane, and triethoxysilylethyl.
  • Examples of the silane compound of the surface treatment agent include triethoxycaprylylsilane, aminopropyltriethoxysilane, perfluorooctylethyltriethoxysilane, and perfluorooctyltriethoxysilane.
  • Examples of the fatty acid component of the surface treatment agent include stearic acid, isostearic acid, oleic acid, hydroxystearic acid, myristic acid and the like.
  • Examples of the alkyl titanate as the surface treatment agent include pyrophosphoric acid type alkyl titanate, phosphorous acid type alkyl titanate, amino acid type alkyl titanate, and long chain carboxylic acid type alkyl titanate. Specific examples of the alkyl titanate include isopropyl triisostearoyl titanate.
  • the total content of the ultraviolet protective agent with respect to the total amount of the water-in-oil emulsion composition is preferably 3 to 10% by mass. By blending in this range, it is possible to improve the ultraviolet protection effect while achieving both the feeling of use and the stability.
  • the (D) ultraviolet absorber and the (E) ultraviolet protector may be compounded, supported or encapsulated in another component, and the combination thereof is not particularly limited. ..
  • the water-in-oil type emulsion composition of the present invention from the viewpoint of improving the feeling of use, stability, etc., unless the effects of the present invention are impaired, the above-mentioned (A) component, (B) component, and (C) component,
  • a base or carrier may be included.
  • the base or carrier include, but are not limited to, cellulose derivatives; polyvinylpyrrolidone; carrageenan; polyvinyl butyrate; polyethylene glycol; glycol ethers; lower alcohols such as ethanol and isopropanol; Known components to be added to the external skin preparations such as cosmetics and pharmaceuticals can be used.
  • an oil component functioning as a base or carrier can be used.
  • a base or carrier include hydrocarbons such as paraffin and petrolatum; ester oils such as isopropyl myristate; oils and fats derived from animals and plants such as evening primrose oil; waxes such as beeswax; methyl polysiloxane.
  • Siloxanes, alkyl-modified silicones such as caprylyl methicone, cross-linked methyl polysiloxanes, cross-linked alkyl-modified silicones, acrylic silicones, and silicones such as silicone resins, but are not limited thereto.
  • Well-known ingredients to be added to external preparations for skin such as pharmaceuticals can be used.
  • the base or carrier may be used alone or in combination of two or more.
  • additives to be added to pharmaceuticals, quasi drugs, or cosmetics for example, antioxidants and thickeners.
  • Preservatives, pH adjusters, stabilizers, irritation reducing agents, preservatives, coloring agents, fragrances, powders and/or pearlescent agents can be added.
  • antioxidants examples include dibutylhydroxytoluene, butylhydroxyanisole, sorbic acid, sodium sulfite, ascorbic acid, ascorbic acid derivative, tocopherol, tocopherol derivative, erythorbic acid, and L-cysteine hydrochloride.
  • thickener for example, guar gum, locust bean gum, carrageenan, xanthan gum, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl polymer, alkyl methacrylate acrylate copolymer, (hydroxyethyl acrylate/acryloyldimethyltaurine Na) copolymer, (Na acrylate/acryloyl dimethyl taurine Na) copolymer, polyacrylic acid amide, polyethylene glycol, alginic acid, macrogol, sodium chondroitin sulfate, and a cellulosic thickener such as hydroxyethyl cellulose.
  • preservatives and preservatives examples include benzoic acid, sodium benzoate, dehydroacetic acid, sodium dehydroacetate, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, butyl paraoxybenzoate, ethyl paraoxybenzoate, propyl paraoxybenzoate, and paraoxybenzoate.
  • Benzyl benzoate methyl paraoxybenzoate, phenoxyethanol, benzyl alcohol, chlorobutanol, sorbic acid and its salts, chlorhexidine gluconate, caprylhydroxysamic acid, propynyl butylcarbamate and 1,2-pentanediol, 2,4- Hexanediol, 1,2-hexanediol, 1,2-octanediol and the like can be mentioned.
  • pH adjusters examples include inorganic acids, organic acids, and organic bases.
  • Examples of the stabilizer include sodium polyacrylate, dibutylhydroxytoluene, butylhydroxyanisole and the like.
  • Examples of the irritation reducing agent include licorice extract and sodium alginate.
  • colorant examples include pigment grade titanium oxide, zinc oxide, iron oxide, organic pigments, talc, sericite, mica, synthetic mica, chromium oxide, and Gunjou.
  • powder may be blended for the purpose of improving the feel and imparting a makeup effect, and specifically, boron nitride, silica, alumina, aluminum hydroxide, metal soap, silicone powder, amino acid, polymethylmethacryl Methyl acid etc. are mentioned.
  • the additives can be used alone or in combination of two or more.
  • the present invention is not limited to these, and known components that are blended in external preparations for skin such as cosmetics and pharmaceuticals can be appropriately used.
  • the water-in-oil type emulsion composition of the present invention may contain other active ingredients within a range that does not impair the effects of the present invention.
  • specific examples of the active ingredient include, for example, a cooling component, a moisturizing component, an anti-inflammatory component, an antibacterial or bactericidal component, a vitamin, an amino acid or a derivative thereof, a cell activating component, an antiaging component, a blood circulation promoting component, a keratin softening component, Examples include whitening ingredients and astringent ingredients.
  • cooling component examples include camphor, menthol, borneol, eugenol, cineol, thymol, bisabolol, ⁇ -pinene, sesquiterpene such as monoterpene such as limonene, diterpene, eucalyptus oil, peppermint oil, clove oil, cinnamon barley.
  • Essential oils such as oil, peppermint oil, mint oil, tea tree oil, chamomile oil, rosemary oil, lemon oil, orange oil, thyme oil, sage oil, clove oil and the like can be mentioned.
  • moisturizing ingredients include high molecular compounds such as sodium hyaluronate, heparin analogs, sodium chondroitin sulfate, collagen, elastin, keratin, chitin, and chitosan or hydrolysates thereof; glycine, aspartic acid, arginine, etc.
  • Amino acids such as sodium lactate, urea, and sodium pyrrolidonecarboxylate; lipids such as ceramides and phospholipids; macromolecules with phospholipid polar groups such as MPC polymers; polyoxypropylene methyl glucoside; PPG- 10 methyl glucose, PEG/PPG/polybutylene glycol 8/5/3 glycerin; trimethylglycine (betaine); hydroxyethyl urea; acrylic acid/acrylamide/dimethyldiallylammonium chloride copolymer; and coix seed extract, mugwort leaf Extracts, chamomile extract, hamamelis extract, birch sap, hamcho extract, lilac extract, tea extract, lavender oil, and plant extract extracts such as perilla extract; animal extracts such as placenta extract.
  • anti-inflammatory component for example, a component derived from a plant (for example, conflict-), allantoin, glycyrrhizic acid or its derivative, glycyrrhetinic acid or its derivative, zinc oxide, pyridoxine hydrochloride, tocopherol acetate, salicylic acid or its derivative, Examples include azulene, steroids and ⁇ -aminocaproic acid.
  • antibacterial or bactericidal component examples include chlorhexidine, salicylic acid, benzalkonium chloride, acrinol, sulfur, resorcin, ethanol, benzethonium chloride, adapalene, benzoyl peroxide, clindamycin, cresol, gluconic acid and its derivatives, and povidone-yo.
  • paraben phenoxyethanol, 1,2-pentanediol, alkyldiaminoglycine hydrochloride, chlorhexidine gluconate, and Examples include zinc paraphenol sulfonate, picrotone olamine, and miconazole.
  • vitamins include retinol derivatives (retinol, retinol acetate, retinol palmitate, etc.) retinoic acid, tocopheryl retinoate, and other vitamin A; tocopherol, tocopherol acetate, and other vitamin Es; riboflavin
  • vitamin B2 retinol derivatives (retinol, retinol acetate, retinol palmitate, etc.) retinoic acid, tocopheryl retinoate, and other vitamin A; tocopherol, tocopherol acetate, and other vitamin Es; riboflavin
  • vitamin B2 nicotinic acids other than nicotinamide
  • vitamin Cs such as ascorbic acid, ascorbate, ascorbic acid derivative
  • vitamin Ds vitamin Ks, ⁇ -oryzanol, vitamin B1s
  • pyridoxine hydrochloride etc.
  • amino acid or its derivative examples include betaine (trimethylglycine), proline, hydroxyproline, arginine, lysine, serine, glycine, alanine, phenylalanine, ⁇ -alanine, threonine, glutamic acid, glutamine, asparagine, aspartic acid, cysteine, cystine. , Methionine, leucine, isoleucine, valine, histidine, taurine, ⁇ -aminobutyric acid, ⁇ -amino- ⁇ -hydroxybutyric acid, carnitine, carnosine, and creatine.
  • betaine trimethylglycine
  • proline hydroxyproline
  • arginine proline
  • hydroxyproline arginine
  • lysine serine
  • glycine alanine
  • phenylalanine phenylalanine
  • ⁇ -alanine threonine
  • glutamic acid glutamine
  • cysteine cystine
  • the cell activating component examples include amino acids; vitamins; ⁇ -hydroxy acids such as glycolic acid and lactic acid; tannin; flavonoids; saponin; allantoin; and Photosensitizer No. 301.
  • the antiaging component for example, hydrolyzed soybean protein, retinoid (retinol and its derivatives, retinoic acid, retinal, etc.), pangaminic acid, kinetin, ursolic acid, turmeric extract, sphingosine derivative, silicon, silicic acid, Examples thereof include N-methyl-L-serine and mevalonolactone.
  • Examples of the blood circulation promoting component include plants (for example, Panax ginseng, ashitaba, arnica, ginkgo, fennel, ginkgo, Dutch oak, chamomile, roma-chamomile, carrot, gentian, burdock, rice, hawthorn, shiitake mushroom, hawthorn, hazelnut , Senkyu, senburi, thyme, clove, chimp, touki, tounin, spruce, carrot, garlic, butcher-bloom, grape, button, horse chestnut, melissa, yuzu, yokuinin, rosemary, rosehip, chimp, Components derived from spruce, spruce, peach, apricot, walnut, and corn); and glucosyl hesperidin.
  • plants for example, Panax ginseng, ashitaba, arnica, ginkgo, fennel, ginkgo, Dutch oak, chamomile,
  • Examples of the keratin softening component include lanolin, urea, ⁇ -hydroxy acid and sulfur.
  • the whitening component include ascorbic acid and its derivative, arbutin, and tocopherol, tranexamic acid, hydroquinone, kojic acid, salicylic acid derivative, placenta extract, linoleic acid and a plant component having a whitening effect (for example, Yukinoshita, aloe). Etc.) and the like.
  • Examples of the astringent component include zinc paraphenol sulfonate, zinc oxide, menthol, and ethanol.
  • compositions for skin may be used alone or in combination of two or more.
  • present invention is not limited to these, and known components that are blended in external preparations for skin such as cosmetics and pharmaceuticals can be appropriately used.
  • the method for producing the water-in-oil type emulsion composition of the present invention is not particularly limited, and the stirring method at the time of emulsification, the emulsification temperature, the feeding order of the oil phase and the aqueous phase, the feeding speed and the like may be appropriately set.
  • a method of preparing an oil phase and a water phase, respectively, which are mixed after heating and melting if necessary, gradually adding water to the oil phase at room temperature, and emulsifying by mechanical stirring force such as a homogenizer, and the like can be mentioned.
  • mechanical stirring force such as a homogenizer, and the like
  • a step of swelling the oil-soluble thickener may be included in the manufacturing process, and examples thereof include, but are not limited to, heat dispersion, mechanical disintegration, preliminary stirring in the oil phase, and the like.
  • the water-in-oil emulsion composition of the present invention is a drug, a quasi drug, or a base or carrier usually used for cosmetics, and, if necessary, mixed with an additive, a drug, a quasi drug, Alternatively, it can be a water-in-oil type emulsion composition for cosmetics.
  • the form of the water-in-oil type emulsion composition for pharmaceuticals is not particularly limited, and examples thereof include solutions, suspensions, emulsions, creams, ointments, gels, liniments, lotions, patches and aerosols. And so on. These preparations can be produced according to the method described in the 17th revised Japanese Pharmacopoeia general rules. Among them, solutions, suspensions, emulsions, creams, ointments, gels, lotions and patches are preferable, and creams, emulsions, ointments, lotions and gels are more preferable.
  • a water-in-oil type emulsion composition for quasi-drugs or cosmetics
  • the same forms as the above-mentioned drugs can be used.
  • a stick agent, a sheet agent obtained by impregnating a non-woven fabric with a chemical solution, and the like can be given.
  • solutions, suspensions, emulsions, creams, ointments, gels, lotions, sticks and sheets are preferable, and creams, emulsions, ointments, gels or lotions are more preferable.
  • the water-in-oil type emulsion composition of the present invention contains an oily base and an aqueous base, and typically can be in the form of a cream or emulsion.
  • water-in-oil emulsion composition for quasi-drugs or cosmetics include, for example, lotion, emulsion, gel, cream, beauty essence, sunscreen cosmetic, pack, and mask.
  • Basic creams such as hand creams, all-in-one gels and body creams; and face makeup cosmetics such as BB creams, foundations and makeup bases, lip cosmetics such as lipsticks, lip balms, lip glosses and lip liners.
  • Cosmetics for hair such as styling agents and the like.
  • the water-in-oil type emulsion composition for skin is particularly preferable.
  • the water-in-oil type emulsion composition of the present invention can be used as a skin-water-in-oil type emulsion composition for pharmaceuticals, quasi drugs, or cosmetics.
  • the formulation form of the water-in-oil emulsion composition is the same as that of the water-in-oil emulsion composition of the present invention.
  • usable bases or carriers, additives, active ingredients, and preferable ones thereof are the same as in the case of the water-in-oil type emulsion composition of the present invention.
  • the water-in-oil type emulsion composition of the present invention can be used by being housed in a container having a shape and a material selected appropriately according to the purpose of use and application.
  • Specific containers include, for example, spray type, bottle type, tube type, jar type, drop type, dispenser type, stick type, pouch bags, and cheer packs. Since the water-in-oil type emulsion composition of the present invention can be used in a preferable state from the viewpoint of easy ejection from a container, it is possible to increase the degree of freedom in designing a formulation containing a high concentration of nicotinic acid amide. ..
  • a high-concentration nicotinic acid amide-containing preparation can be easily used in a wide variety of containers such as sprays, bottles, tubes, and dispensers, as well as jars and sticks, thus providing flexibility in product design. It is possible to secure the above, and it is very usefully applicable particularly to tube type, dispenser type and bottle type containers.
  • examples of the material of the container include polyethylene terephthalate, polypropylene, polyethylene (HDPE, LDPE, LLDPE, etc.), ABS resin, ethylene vinyl alcohol resin, polystyrene, glass, and metal (aluminum, etc.). Further, these materials may be subjected to various coating treatments in consideration of strength, flexibility, weather resistance, stability of components, etc., or these materials may be combined, for example, by mixing, or laminated. It can be used as a container material. Of these, polypropylene, polyethylene (HDPE, LDPE, LLDPE, etc.), ethylene vinyl alcohol resin, and metal (aluminum, etc.) are preferably used.
  • the water-in-oil type emulsion composition of the present invention can be suitably used for the purpose of promoting blood circulation, anti-inflammation, and ceramide synthesis in expectation of physiological activity of nicotinic acid amide.
  • whitening, anti-wrinkle and anti-aging effects can be expected, and it is useful as a multi-functional preparation including a whitening agent and a sunscreen.
  • the container for containing the composition and the method of using the composition are the same as those of the water-in-oil emulsion composition of the present invention.
  • the present invention also includes a method for improving the usability of a water-in-oil emulsion composition containing (A) nicotinic acid amide.
  • a water-in-oil emulsion composition containing (A) nicotinic acid amide.
  • the water-in-oil type emulsion composition containing the oil-soluble thickener it is possible to improve the usability of the water-in-oil type emulsion composition.
  • improving the feeling of use means, for example, in the case of a cream or the like, when applied to the skin, it spreads well and has good familiarity, non-greasiness, moisturizing, maintaining appropriate softness, etc. Point to.
  • the water-in-oil type emulsion composition of the present invention is also excellent in stability.
  • excellent in stability means that stability is assured, for example, at high temperature or at low temperature, although not limited thereto. Specifically, it means that separation or the like is suppressed even when at least the water-in-oil emulsion composition is stored.
  • the conditions and the like of the above; and (C) the water-in-oil type emulsion composition containing the oil-soluble thickener are the same as those used in the above-mentioned water-in-oil type emulsion composition.
  • the product obtained by this method can be used once or several times a day in accordance with the intended use, according to the known or commonly used usage and dose.
  • compositions of Examples and Comparative Examples described in the table were prepared, and the state of the preparation for 1 hour after the production and the state after storage were observed.
  • the compositions of Examples and Comparative Examples were prepared by heating and dissolving the oil phase and the water phase, respectively, and bringing both phases to room temperature, and then using a homomixer while gradually containing the water phase in the oil phase. It was carried out by sufficiently stirring the resulting mixture to obtain the desired water-in-oil type emulsion composition.
  • Heat load test thermo stability
  • the compositions of Examples and Comparative Examples were filled in 30 mL glass bottles and stored in a constant temperature bath at 50°C. After 3 days and 2 weeks, the test preparation was taken out of the constant temperature bath, returned to room temperature, and visually evaluated for appearance to determine whether the compositions of Examples and Comparative Examples had long-term stability. did.
  • Examples 1 to 3 even when the nicotinic acid amide (A) was contained at a high concentration, by combining the components (B) and (C), the state immediately after the production and the stability were improved, and the water-in-oil type emulsion compositions were obtained.
  • Comparative Examples 1 to 3 in which the oil-soluble thickener was not contained, separation occurred immediately after the production.
  • Comparative Example 4 containing the ether-based surfactant polyethylene glycol dipolyhydroxystearate, separation occurred immediately after the production. Further, the water-in-oil type emulsion compositions of Examples 1 to 3 and Comparative Examples 1 to 3 were used on the skin and the feeling of use was evaluated.
  • the water-in-oil type emulsion compositions of Examples are the oils of Comparative Examples. It was confirmed that, as compared with the water-in-water emulsion composition, no precipitation was observed, the formulation spread well, and the composition was not sticky. Hereinafter, also in the examples, the feeling of use was evaluated in the same manner.
  • Example 4 a water-in-oil type emulsion composition having good stability and heat stability immediately after production and a good feeling in use was obtained. Particularly, by using a silicone-based surfactant and a polyglycerin ester surfactant having an HLB of 2 to 6, it was confirmed that the thermal stability was good.
  • compositions of Examples 5, 11-13 which contained the oil-soluble thickener, had high stability and thermal stability. Separation was confirmed immediately after production in the composition of Comparative Example 5 containing a water-soluble thickener instead of the oil-soluble thickener. Regarding the thermal stability, the compositions of Examples 5 and 11 maintained good stability even under considerably severe conditions of 50° C. for 2 weeks, and therefore, inulin stearate or dimethyl distearyl ammonium hectorite. It has been confirmed that it is particularly preferable to contain one or more oil-soluble thickeners selected more.

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  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne une composition d'émulsion eau dans l'huile offrant une excellente sensation lors de l'utilisation. Une composition d'émulsion eau dans l'huile est préparée, laquelle contient (A) 3 % en masse ou plus de nicotinamide ; (B) un ou plusieurs tensioactifs choisis dans le groupe constitué par des tensioactifs à base de silicone, des tensioactifs d'ester de sorbitan, des tensioactifs d'ester de polyglycérine et des tensioactifs d'ester de glycérine ; et (C) un ou plusieurs épaississants solubles dans l'huile choisis dans le groupe constitué d'épaississants à base d'argile, d'esters d'acide gras de dextrine, d'esters d'acide gras d'inuline et d'agents gélifiants d'huile à base d'acides aminés.
PCT/JP2019/051418 2018-12-28 2019-12-27 Composition d'émulsion eau dans l'huile contenant du nicotinamide WO2020138420A1 (fr)

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JP7471092B2 (ja) 2020-01-24 2024-04-19 株式会社ノエビア 油中水型乳化化粧料
WO2023054168A1 (fr) * 2021-09-30 2023-04-06 ロート製薬株式会社 Composition d'eau dans l'huile à usage externe contenant de l'acide ascorbique et/ou un sel de celui-ci
CN115998626A (zh) * 2022-11-15 2023-04-25 华熙生物科技股份有限公司 用于化妆品的微珠及其应用

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KR20150011887A (ko) * 2013-07-23 2015-02-03 주식회사 서울화장품 스폰지 폼에 함침시켜 제조하는 자외선 차단용 화장품
JP2019014709A (ja) * 2017-07-07 2019-01-31 ポーラ化成工業株式会社 皮膚外用組成物
JP2019131538A (ja) * 2018-01-29 2019-08-08 株式会社コーセー 油性皮膚外用剤または油性化粧料
JP2019131550A (ja) * 2018-02-01 2019-08-08 株式会社コーセー カロテノイドの安定化方法

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US20070128137A1 (en) * 2005-12-02 2007-06-07 Naohisa Yoshimi Water in oil emulsion compositions containing siloxane elastomers
JP2010163379A (ja) * 2009-01-14 2010-07-29 Shiseido Co Ltd 油中水型乳化組成物
JP5777162B2 (ja) * 2011-11-22 2015-09-09 アサヌマ コーポレーション株式会社 油中水型乳化化粧料

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KR20150011887A (ko) * 2013-07-23 2015-02-03 주식회사 서울화장품 스폰지 폼에 함침시켜 제조하는 자외선 차단용 화장품
JP2019014709A (ja) * 2017-07-07 2019-01-31 ポーラ化成工業株式会社 皮膚外用組成物
JP2019131538A (ja) * 2018-01-29 2019-08-08 株式会社コーセー 油性皮膚外用剤または油性化粧料
JP2019131550A (ja) * 2018-02-01 2019-08-08 株式会社コーセー カロテノイドの安定化方法

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