Emulsion composition

Abstract

Provided is a stable emulsion composition.　Prepared is an emulsion composition comprising: (A) an oily component; (B) 40% by mass or more of one or more selected from the group consisting of polyhydric alcohols having 3 to 5 carbon atoms and polyethylene glycol; (C) one or more selected from the group consisting of polyacrylamide compounds and polyvinylpyrrolidone; (D) 0%-15% by mass of water; and (E) at least one selected from PEG -20 phytosterol, polyoxyethylene arachyl ether, glyceryl behenate, and polyglyceryl-6 octastearate.

Description

emulsifying composition

[0001] The present invention relates to an emulsion composition.

[0002] As external compositions to be applied to the skin, emulsion compositions such as body milk and body cream for application to the hands, feet, and body, and emulsions and face cream for application to the face are widely used. Emulsion compositions can be excellent formulations because they are easy to use and can retain moisturizing properties.

[0003] By incorporating a water-soluble active ingredient into a topical composition, it may be possible to create a formulation that exhibits various effects, such as anti-inflammatory effects, acne-reducing effects, whitening effects, anti-aging effects, antioxidant effects, cell activation effects by promoting the synthesis of biological components such as collagen, and effects of suppressing cell damage and DNA damage caused by ultraviolet rays in epidermal keratinocytes.

[0004] For example, an emulsion composition containing ascorbic acid glucoside has been proposed (Patent Document 1: JP-A-2005-132808).

[0005] Japanese Patent Application Laid-Open No. 2005-132808

[0006] An object of the present invention is to provide a stable emulsion composition.

[0007] When incorporating an active ingredient into a formulation, it may be necessary to use a polyhydric alcohol or polyethylene glycol to dissolve the active ingredient and maintain its stability in the formulation. However, in compositions containing a large amount of such bases, it is very difficult to form a good interface with the oil phase, making it difficult to prepare an emulsion composition.

[0008] As a result of extensive research aimed at solving these problems, the present inventors have found that a stable emulsion composition having a favorable interface between the oil phase and the aqueous phase can be prepared by incorporating (A) an oily component; (B) 40% by mass or more of one or more species selected from the group consisting of polyhydric alcohols having 3 to 5 carbon atoms and polyethylene glycols; (C) one or more species selected from the group consisting of polyacrylamide compounds and polyvinylpyrrolidones; (D) 0 to 15% by mass of water; and (E) at least one surfactant selected from the group consisting of PEG-20 phytosterol, polyoxyethylene arachyl ether, glyceryl behenate, and polyglyceryl-6 octastearate, thereby completing the present invention.

[0009] That is, the present invention provides the following emulsion compositions: Item 1. (A) an oily component; (B) 40% by mass or more of one or more selected from the group consisting of polyhydric alcohols having 3 to 5 carbon atoms and polyethylene glycols; (C) one or more selected from the group consisting of polyacrylamide compounds and polyvinylpyrrolidones; (D) 0 to 15% by mass of water; and (E) at least one surfactant selected from the group consisting of PEG-20 phytosterol, polyoxyethylene arachyl ether, glyceryl behenate, and polyglyceryl-6 octastearate.

[0010] According to the present invention, a stable emulsion composition can be provided.

[0011] In this specification, the unit of content "% by mass" is synonymous with "g / 100 g".

[0012] [Emulsion composition] The emulsion composition of the present invention is an emulsion composition containing: (A) an oily component; (B) 40% by mass or more of one or more selected from the group consisting of polyhydric alcohols having 3 to 5 carbon atoms and polyethylene glycols; (C) one or more selected from the group consisting of polyacrylamide compounds and polyvinylpyrrolidones; (D) 0 to 15% by mass of water; and (E) at least one surfactant selected from the group consisting of PEG-20 phytosterol, polyoxyethylene arachyl ether, glyceryl behenate, and polyglyceryl-6 octastearate.

[0013] (Oil Component (A)) Component (A) can be any oil component that is typically used in topical compositions or cosmetics, without any particular limitations. Specific examples include hydrocarbon oils, ester oils, silicone oils, higher alcohols, higher fatty acids, natural animal and vegetable oils and fats, and oil-soluble UV absorbers. These can be used alone or in combination of two or more. Oil components that are solid at room temperature may be used by dissolving them in liquid oil.

[0014] Examples of hydrocarbon oils that can be used include paraffinic hydrocarbons and olefinic hydrocarbons, such as squalane, squalene, ceresin, paraffin, olefin oligomer, microcrystalline wax, liquid paraffin, petrolatum, hydrogenated polyisobutene, light liquid paraffin, etc. Here, squalane includes animal-derived squalane (e.g., squalane from shark liver oil) and plant-derived squalane (e.g., sugar squalane from sugarcane, or vegetable squalane from olives, etc.).

[0015] As the ester oil, synthetic esters and esters of higher alcohols and higher fatty acids are used, and examples thereof include diisobutyl adipate, di-2-hexyldecyl adipate, di-2-heptylundecyl adipate, isostearyl isostearate, trimethylolpropane triisostearate, cetyl 2-ethylhexanoate (cetyl ethylhexanoate), neopentyl glycol di-2-ethylhexanoate, trimethylolpropane tri-2-ethylhexanoate, glyceryl tri-2-ethylhexanoate, and pentaerythritol tetra-2-ethylhexanoate. Pentaerythritol tetra-2-ethylhexanoate, octyldodecyl neopentanoate, cetyl octanoate, caprylic / caprylic triglyceride, neopentyl glycol dicaprate, 2-ethylhexyl succinate, isocetyl stearate, butyl stearate, diisopropyl sebacate, cetyl lactate, tetradecyl lactate, octyldodecyl lactate, isopropyl myristate, octyldodecyl myristate, cetyl myristate, myristyl myristate, octyl palmitate, 2-ethylhexyl palmitate, 2-hexyl palmitate Xyldecyl, 2-heptylundecyl palmitate, cholesteryl 12-hydroxystearate, isononyl isononanoate, triethylhexyl trimellitate, diisostearyl malate, pentaerythrityl tetrarosinate, phytosteryl oleate, phytosteryl macadamia nut fatty acid, dimer dilinoleyl diisostearate, di(isostearyl / phytosteryl) dimer dilinoleate, dimer dilinoleyl dimer dilinoleate, dimer dilinoleyl hydrogenated rosin condensate, phytosteryl / isostearyl dimer dilinoleate Dimer Dilinoleyl Dimer Dilinoleate, Bis(Phytosteryl / Behenyl / Isostearyl), Dimer Dilinoleyl Dimer Dilinoleate, Polyglyceryl-10 Dimer Dilinoleate / Stearic Acid / Hydroxystearic Acid, Polyglyceryl-2 Isostearate / Dimer Dilinoleate Copolymer, Bis-Diglyceryl Polyacyladipate-2, Di(Phytosteryl / Octyldodecyl) Lauroyl Glutamate, Dipentaerythrityl Tri-Polyhydroxystearate, Di(Octyldodecyl / Phytosteryl) Lauroyl GlutamateExamples include phytosteryl isostearate and diglyceryl triisostearate.

[0016] Examples of silicone oils include siloxanes such as dimethylpolysiloxane, methylphenylpolysiloxane, methylcyclopentasiloxane, highly polymerized methylpolysiloxane, decamethylcyclopentasiloxane, octamethylcyclotetrasiloxane, methylhydrogenpolysiloxane, methyltrimethicone, dimethiconol, and dimethiconol crosspolymer, alkyl-modified silicones such as caprylyl methicone, amino-modified silicones such as aminopropyl dimethicone and amodimethicone, crosslinked methylpolysiloxane, crosslinked alkyl-modified silicone, amino-modified silicone, polyether-modified silicone, polyglycerin-modified silicone, crosslinked polyether-modified silicone, crosslinked alkylpolyether-modified silicone, silicone / alkyl chain co-modified polyether-modified silicone, silicone / alkyl chain co-modified polyglycerin-modified silicone, polyether-modified branched silicone, polyglycerin-modified branched silicone, acrylic silicone, phenyl-modified silicone, and silicone resin.

[0017] Examples of higher alcohols include cetanol, cetostearyl alcohol, stearyl alcohol, behenyl alcohol, octyldodecanol, isostearyl alcohol, lauryl alcohol, myristyl alcohol, palmityl alcohol, hexadecyl alcohol, oleyl alcohol, hexyldodecanol, batyl alcohol, phytosterol, and cholesterol.

[0018] Examples of higher fatty acids that can be used include saturated or unsaturated, straight-chain or branched-chain fatty acids having 8 or more carbon atoms. Specific examples include lauric acid, myristic acid, palmitic acid, stearic acid, isostearic acid, isopalmitic acid, caprylic acid, capric acid, heptanoic acid, pelargonic acid, behenic acid, undecylenic acid, 2-palmitoleic acid, oleic acid, elaidic acid, ricinoleic acid, linoleic acid, linolenic acid, linoelaidic acid, arachidonic acid, petroselinic acid, ricinoleic acid, and polyhydroxystearic acid.

[0019] Examples of natural animal and vegetable oils and fats include avocado oil, linseed oil, almond oil, olive oil, cacao oil, beef tallow, tung oil, wheat germ oil, sesame oil, rice germ oil, rice bran oil, safflower oil, shea butter, soybean oil, evening primrose oil, camellia oil, corn oil, rapeseed oil, horse fat, persic oil, palm oil, palm kernel oil, castor oil, sunflower oil, sunflower seed wax, lard, grape oil, jojoba oil, macadamia nut oil, mink oil, cottonseed oil, Japan wax, coconut oil, hardened coconut oil, peanut oil, lanolin, egg yolk oil, and rosehip oil.

[0020] Examples of oil-soluble ultraviolet absorbers include ethylhexyl paramethoxycinnamate, octocrylene, ethylhexyl salicylate, homosalate, diethylamidohydroxybenzoylhexylbenzoate, bisethylhexyloxyphenol methoxyphenyl triazine, t-butylmethoxybenzoylmethane, ethylhexyl triazone, dimethicodiethylbenzalmalonate, and polysilicone-15.

[0021] In the emulsion composition of the present invention, it is particularly preferable that the component (A) is one or more selected from the group consisting of squalane, shea butter, and sunflower seed wax.

[0022] In the emulsion composition of the present invention, the total content of component (A) relative to the total amount of the emulsion composition is preferably 2% by mass or more, more preferably 3% by mass or more, even more preferably 4% by mass or more, still more preferably 7% by mass or more, and particularly preferably 10% by mass or more. The total content of component (A) relative to the total amount of the emulsion composition is preferably 40% by mass or less, more preferably 30% by mass or less, and even more preferably 25% by mass or less.

[0023] (B) At least one selected from the group consisting of polyhydric alcohols having 3 to 5 carbon atoms and polyethylene glycols) The polyhydric alcohols having 3 to 5 carbon atoms or polyethylene glycols used in the present invention are not particularly limited as long as they are used as components of topical skin preparations in the fields of pharmaceuticals, quasi-drugs, or cosmetics. Commercially available products can also be used as they are.

[0024] Examples of polyhydric alcohols having 3 to 5 carbon atoms include propanediol (1,3-propanediol), propylene glycol, isoprene glycol, 1,2-butylene glycol, 1,3-butylene glycol, 2,3-butylene glycol, 2-methyl-1,3-propanediol, tetramethylene glycol, 1,2-pentanediol (pentylene glycol), trimethylolpropane, and glycerin. One or a combination of two or more of these may be used. Of these, propanediol, propylene glycol, isoprene glycol, 1,2-butylene glycol, 1,3-butylene glycol, and 2,3-butylene glycol are preferably used.

[0025] The polyethylene glycol is not particularly limited as long as it is used as a component of topical skin preparations in the fields of pharmaceuticals, quasi-drugs, or cosmetics. In the present invention, polyethylene glycols with a degree of polymerization of 4 or more, a relatively low degree of polymerization, and a low molecular weight are preferably used. While not limited thereto, polyethylene glycols with an average molecular weight of approximately 190 to 700 are preferred, and polyethylene glycols with an average molecular weight of approximately 190 to 420 are even more preferred. Specific examples of such polyethylene glycols include polyethylene glycol 200, polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 500, polyethylene glycol 600, and polyethylene glycol 700. These are commercially available products, and these commercially available products can be obtained and used. Specific examples of commercially available products include polyethylene glycol 200, polyethylene glycol 300, polyethylene glycol 400, and polyethylene glycol 600 sold by NOF Corporation, and polyethylene glycol 200, polyethylene glycol 300, polyethylene glycol 400, and polyethylene glycol 600 sold by Sanyo Chemical Industries, Ltd.

[0026] Here, the average molecular weight can be determined, for example, in accordance with the average molecular weight test described in the section on polyethylene glycol in the Quasi-drug Raw Materials Standards 2006.

[0027] [Method for measuring the average molecular weight of polyethylene glycol with an average molecular weight of 190-210] Accurately weigh approximately 0.8 g of polyethylene glycol and place it in a 200 mL pressure-resistant glass-stoppered bottle. Add approximately 25 mL of pyridine, heat to dissolve, and allow to cool. Separately, take 42 g of phthalic anhydride and add it to a 1 L light-shielded glass-stoppered bottle containing 300 mL of freshly distilled pyridine. Shake vigorously to dissolve, then allow to stand for at least 16 hours. Accurately weigh 25 mL of this solution, add it to the same pressure-resistant glass-stoppered bottle, seal it, wrap it in a sturdy cloth, and place it in a water bath preheated to 98°C ± 2°C. Ensure that the solution in the bottle is submerged in the water. Heat at 98°C ± 2°C for 30 minutes and allow to cool to room temperature. Next, accurately add 50 mL of 0.5 mol / L sodium hydroxide solution, and titrate this solution with 0.5 mol / L sodium hydroxide solution. The indicator used in this test is five drops of phenolphthalein-pyridine solution (1 → 100). The end point of the titration is when the solution turns pale red and lasts for 15 seconds. A blank test is carried out in the same way. The obtained value is applied to the following formula to calculate the average molecular weight. Average molecular weight = [amount of sample (g) x 4000] / (a ​​- b) a: Amount (mL) of 0.5 mol / L sodium hydroxide solution consumed in the blank test b: Amount (mL) of 0.5 mol / L sodium hydroxide solution consumed in the sample test

[0028] In the case of polyethylene glycol having an average molecular weight other than 190 to 210, the test method is similar to that for polyethylene glycol having an average molecular weight of 190 to 210, except that the weighed amount will be different.

[0029] These polyethylene glycols can be used alone or in combination of two or more.

[0030] The use of polyethylene glycol makes it possible to make the topical composition of the present invention a composition with excellent stability.

[0031] In the emulsion composition of the present invention, the total content of component (B) relative to the total amount of the emulsion composition is preferably 40% by mass or more, more preferably 45% by mass or more, and even more preferably 50% by mass or more. The total content of component (B) relative to the total amount of the emulsion composition is preferably 90% by mass or less, more preferably 85% by mass or less, and even more preferably 75% by mass or less.

[0032] In the emulsion composition of the present invention, the ratio of the blending amount of component (B) to component (A) is not particularly limited, but is preferably 1 to 15 parts by mass, more preferably 2 to 10 parts by mass, and even more preferably 2.5 to 8 parts by mass per part by mass of the total content of component (A).From another perspective, it is preferably 3 to 35 parts by mass, more preferably 5 to 25 parts by mass, and even more preferably 10 to 20 parts by mass.

[0033] (C) Polymer Selected from the Group Consisting of Polyacrylamide Compounds and Polyvinylpyrrolidone) The polyacrylamide compound or polyvinylpyrrolidone used in the present invention is not particularly limited as long as it is used as a component of a topical skin preparation in the fields of pharmaceuticals, quasi-drugs, or cosmetics. Commercially available products can also be used as they are.

[0034] Polyacrylamide compounds include homopolymers of acrylamide and its derivatives, or copolymers containing them. Examples of polyacrylamide compounds include polyacrylamide, copolymers of ammonium acryloyldimethyltaurate and vinylpyrrolidone, (dimethylacrylamide / sodium acryloyldimethyltaurate) crosspolymers, copolymers of acrylamide and acrylic acid, copolymers of acrylic acid and acryloyldimethyltaurate, and copolymers of hydroxyalkyl acrylate and acryloyldimethyltaurate. One or more of these can be used in combination. Of these, acrylamide homopolymers are preferred.

[0035] As the component (C), one or more polyacrylamide compounds, polyvinylpyrrolidone alone, or a combination of polyvinylpyrrolidone and a polyacrylamide compound can be used.

[0036] In the emulsion composition of the present invention, the total content of component (C) relative to the total amount of the emulsion composition is preferably 0.4% by mass or more, more preferably 0.6% by mass or more, and even more preferably 0.8% by mass or more, and is preferably 5% by mass or less, more preferably 4.5% by mass or less, and even more preferably 4% by mass or less.

[0037] In the emulsion composition of the present invention, the ratio of the blending amount of component (C) to component (B) is not particularly limited, but is preferably 0.003 to 40 parts by mass, more preferably 0.005 to 35 parts by mass, and even more preferably 0.006 to 30 parts by mass, per part by mass of the total content of component (B).

[0038] (D) Water) The emulsion composition of the present invention may further contain water. The water content is 0 to 15% by mass, preferably 0 to 12% by mass, and more preferably 0 to 5% by mass, relative to the total amount of the emulsion composition. For example, it can be 0.1% by mass or more, 1% by mass or more, or 3% by mass or more. The water content (D) relative to the total amount of the emulsion composition is 15% by mass or less, more preferably 13% by mass or less, even more preferably 12% by mass or less, even more preferably 11% by mass or less, and particularly preferably 5% by mass or less.

[0039] (E) Surfactant The emulsion composition of the present invention further contains a specific surfactant. The surfactant used in the present invention is not particularly limited as long as it is used as a component of topical skin preparations in the fields of pharmaceuticals, quasi-drugs, or cosmetics. Commercially available products can also be used as they are. The specific surfactant is at least one surfactant selected from the group consisting of PEG-20 phytosterol, polyoxyethylene arachyl ether, glyceryl behenate, and polyglyceryl-6 octastearate. One or a combination of two or more of these components can also be used.

[0040] In the emulsion composition of the present invention, the total content of component (E) relative to the total amount of the emulsion composition is preferably 1% by mass or more, more preferably 2% by mass or more, and even more preferably 5% by mass or more, and is preferably 20% by mass or less, more preferably 15% by mass or less, and even more preferably 13% by mass or less, relative to the total amount of the emulsion composition.

[0041] In the emulsion composition of the present invention, the ratio of the blending amount of component (E) to component (A) is not particularly limited, but is preferably 0.02 to 1 part by mass, more preferably 0.03 to 0.6 parts by mass, and even more preferably 0.04 to 0.4 parts by mass, per 1 part by mass of the total content of component (A). From another perspective, it is preferably 0.1 to 3 parts by mass, more preferably 0.2 to 2.5 parts by mass, and even more preferably 0.3 to 2 parts by mass.

[0042] The emulsion composition of the present invention may optionally contain (F) an organic acid or a salt thereof in addition to the above-mentioned components (A), (B), (C), (D), and (E), as long as the effects of the present invention are not impaired. The creamy composition of the present invention contains a small amount of water and a large amount of polyhydric alcohol or polyethylene glycol, so that it can contain ingredients that are unstable in water or ingredients that are easily soluble in polyhydric alcohol. Typical examples of such ingredients include organic acids and salts thereof.

[0043] (F) Organic Acid or Salt Thereof) The emulsion composition of the present invention may further contain an organic acid or a salt thereof in addition to the above components (A), (B), (C), (D), and (E). The organic acid or salt thereof used in the present invention is not limited, but is preferably ascorbic acid or a salt thereof, or a derivative of ascorbic acid or a salt thereof, or azelaic acid or a salt thereof, more preferably ascorbic acid or a salt thereof, or azelaic acid, and particularly preferably ascorbic acid or a salt thereof. As the organic acid or a salt thereof, components commercially available as components of topical skin preparations in the fields of pharmaceuticals, quasi-drugs, or cosmetics can be used.

[0044] Here, the salt refers to a pharmaceutically acceptable salt. Examples include, but are not limited to, salts with organic bases (e.g., salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, and pyridine salt, basic ammonium salts such as arginine, etc.), salts with inorganic bases (e.g., alkali metal salts such as ammonium salt, sodium salt, and potassium salt, alkaline earth metal salts such as calcium salt and magnesium salt, aluminum salt, etc.), etc. Among these, sodium salts and magnesium salts are preferred.

[0045] Ascorbic acid is usually more preferably in the L-form.

[0046] Examples of ascorbic acid derivatives include, but are not limited to, 3-O-ethyl ascorbic acid, ascorbyl tetra-2-hexyldecanoate, 3-glyceryl ascorbic acid, 3-laurylglyceryl ascorbic acid, and L-ascorbic acid 2-glucoside. Salts of ascorbic acid derivatives can also be used. Specific examples include sodium ascorbic acid monophosphate, sodium ascorbic acid diphosphate, sodium ascorbic acid triphosphate, sodium ascorbic acid 2-sulfate, and magnesium ascorbic acid monophosphate.

[0047] In the present invention, one or more organic acids or salts thereof may be used in combination.

[0048] In the emulsion composition of the present invention, the total content of the component (F) relative to the total amount of the emulsion composition is preferably 1% by mass or more, more preferably 3% by mass or more, and preferably 30% by mass or less, more preferably 20% by mass or less, even more preferably 15% by mass or less, still more preferably 10% by mass or less, and most preferably 8% by mass or less.

[0049] (G) Inorganic Acid or Salt Thereof The emulsion composition of the present invention may further contain an inorganic acid or a salt thereof in addition to the above components (A), (B), (C), (D), and (E). The inorganic acid or a salt thereof used in the present invention is not limited, but is preferably pyrosulfite or a salt thereof, or phosphoric acid or a salt thereof, and particularly preferably pyrosulfite or a salt thereof.

[0050] Here, the salt refers to a pharmaceutically acceptable salt. Examples of the salt include, but are not limited to, salts with organic bases (e.g., salts with tertiary amines such as trimethylamine salt, triethylamine salt, monoethanolamine salt, triethanolamine salt, and pyridine salt, basic ammonium salts such as arginine, etc.), salts with inorganic bases (e.g., alkali metal salts such as ammonium salt, sodium salt, and potassium salt, alkaline earth metal salts such as calcium salt and magnesium salt, aluminum salt, etc.), etc. Among these, sodium salts of inorganic acids or potassium salts of inorganic acids are preferred.

[0051] (Other Components) In addition to the components (A), (B), (C), (D), and (E), the emulsion composition of the present invention may further contain one or more of various components, such as a whitening component, an anti-inflammatory component, an antibacterial component, a cell activating component, an astringent component, an antioxidant component, an acne-reducing component, an anti-aging component, a component promoting biocomponent synthesis such as collagen, a blood circulation promoting component, a moisturizing component, or an anti-aging component, in combination. Preferably, one or more of the whitening component, anti-inflammatory component, antibacterial component, cell activating component, astringent component, antioxidant component, anti-aging component, or moisturizing component is used. Particularly preferred combinations of these components include a combination with a whitening component, a combination of a whitening component and an antioxidant component, combinations with an antioxidant component, combinations with an anti-aging component, and combinations of a whitening component and an anti-aging component. These components are not particularly limited as long as they have been used or will be used in the future as components of topical skin preparations in the fields of pharmaceuticals, quasi-drugs, or cosmetics, and any component may be appropriately selected and used.

[0052] (Additives) The emulsion composition of the present invention may contain, as needed, various components commonly used as components of topical skin preparations in the fields of pharmaceuticals, quasi-drugs, or cosmetics, within quantitative and qualitative ranges that do not impair the qualities such as appearance stability and viscosity, or that do not impair the effects of the present invention, such as amino acids, surfactants other than component (E), irritation reducers, thickeners, preservatives, UV absorbers, UV protection agents, colorants, dispersants, additional pH adjusters, fragrances, etc. These components may be used alone, or two or more may be used in any combination.

[0053] (Properties) The emulsion composition of the present invention is a composition that has no fluidity and is not translucent.

[0054] (Viscosity) Here, the viscosity is preferably 15 to 1700 Pa s, more preferably 50 to 1200 Pa s, and even more preferably 100 to 750 Pa s. The viscosity (Pa s) is measured using a Brookfield viscometer (manufactured by Toki Sangyo Co., Ltd.) with Range H Rotor No. 7 at 2.5 rpm for 60 seconds at 25°C.

[0055] (Light-blocking property) Here, "not translucent" means that, for example, 4 ml of gel is added to a 6-well plate, the absorbance (A') at a wavelength of 660 nm is measured using a microplate reader, and the light transmittance (%) calculated using formula I is 10% or less. The microplate used in measuring the absorbance (A') was "CORNING Costar, 3513, 12-well transparent TC-Treated microplates, individually wrapped, sterile," and the plate reader used was "MICROPLATE READER SH-9000Lab: manufactured by Corona Electric Co., Ltd." Light transmittance (%) = 100 / (10^(A')) (I)

[0056] (pH) When the pH of the emulsion composition is measured immediately after preparation using a pH meter (manufactured by HORIBA), it is preferably 2.5 to 7.5, more preferably 2.6 to 6.5, and even more preferably 2.7 to 4.0 at 25°C.

[0057] [Production Method] The method for producing the emulsion composition of the present invention is not particularly limited, and the stirring method, the order and speed of adding the ingredients, etc. can be set appropriately.

[0058] Specifically, for example, a polyhydric alcohol, a thickener, and, if included, water or a water-soluble active ingredient, etc., are mixed to prepare a gel composition, and a surfactant and an oily component are mixed separately from this, and the mixture is added to the gel composition to prepare an emulsion composition.

[0059] [Formulation] The emulsion composition of the present invention can be mixed with a base or carrier used in the fields of pharmaceuticals, quasi-drugs, or cosmetics, and, if necessary, additives, to form a topical composition for pharmaceuticals, quasi-drugs, or cosmetics.

[0060] The emulsion composition of the present invention can typically be used as an emulsion or cream formulation (creamy composition). The emulsion composition may be either an oil-in-water type or a water-in-oil type. The oil-in-water type is preferred.

[0061] Specific uses of the emulsion composition for pharmaceuticals, quasi-drugs, or cosmetics include, in the form of an emulsion or cream preparation, basic cosmetics such as face cream, eye cream, beauty serum, sunscreen cosmetics, hand cream, and body cream, face makeup cosmetics such as foundation and makeup base, and lip cosmetics such as lipstick, lip cream, lip gloss, and lip liner.

[0062] [Stabilization Method] The present invention also encompasses a method for stabilizing an emulsion composition obtained by adding (E) at least one surfactant selected from the group consisting of PEG-20 phytosterol, polyoxyethylene arachidonic ether, glyceryl behenate, and polyglyceryl-6 octastearate to a composition containing: (A) an oily component; (B) 40% by mass or more of one or more selected from the group consisting of polyhydric alcohols having 3 to 5 carbon atoms and polyethylene glycols; (C) one or more selected from the group consisting of polyacrylamide compounds and polyvinylpyrrolidones; and (D) 0 to 15% by mass of water. The conditions for the stabilization method, such as the content and ratio of each component and other components, are the same as those described in [Emulsion Composition].

[0063] [Uses] The emulsion composition of the present invention can be used for a wide range of applications as a milky lotion or cream formulation. Although not particularly limited, ingredients such as ascorbic acid or its salts can be added, and depending on the ingredient, the composition can be effective as a whitening agent, anti-inflammatory agent, or anti-aging agent. Such emulsion compositions have, for example, acne prevention and treatment and antioxidant effects. Furthermore, they can be used in products for whitening, anti-wrinkle, and anti-aging purposes. Application to the skin may enhance skin transparency, maintain moisture, improve skin texture, and reduce roughness. Furthermore, they may have effects such as reducing the appearance of pores and moisturizing the skin, and can also be used to prevent and treat age spots.

[0064] Due to its effect on the skin, the emulsion composition of the present invention is used in products to be applied as external preparations for the skin (preparations for the skin). The emulsion composition of the present invention can be used in products to be used in known or commonly used dosages and administration methods, from once to several times a day depending on the intended use.

[0065] The present invention includes the following aspects. [1] An emulsion composition comprising: (A) an oily component; (B) 40% by mass or more of one or more selected from the group consisting of polyhydric alcohols having 3 to 5 carbon atoms and polyethylene glycols; (C) one or more selected from the group consisting of polyacrylamide compounds and polyvinylpyrrolidone; (D) 0 to 15% by mass of water; and (E) at least one surfactant selected from the group consisting of PEG-20 phytosterol, polyoxyethylene arachidyl ether, glyceryl behenate, and polyglyceryl-6 octastearate. [2] The emulsion composition according to [1], wherein the component (C) is polyacrylamide and / or polyvinylpyrrolidone. [3] The emulsion composition according to [1] or [2], wherein the content of the component (C) is 0.4 to 5.0% by mass. [4] The emulsion composition according to any one of [1] to [3], wherein the component (A) is one or more selected from the group consisting of shea butter, squalane, and sunflower seed wax. [5] The emulsified topical composition according to [4], wherein the squalane is one or more selected from the group consisting of shark liver oil squalane, sugar cane-derived sugar squalane, and olive-derived vegetable squalane. [6] The emulsified composition according to any one of [1] to [5], further comprising (F) an organic acid or a salt thereof. [7] The emulsified topical composition according to [6], wherein the organic acid is ascorbic acid or azelaic acid. [8] The emulsified composition according to any one of [1] to [7], wherein the content of the component (A) is 3 to 40% by mass. [9] The emulsified composition according to any one of [1] to [8], further comprising (G) an inorganic acid or a salt thereof.

[10] The emulsified topical composition according to [9], wherein the inorganic acid is pyrosulfite or phosphoric acid.

[11] The emulsified composition according to any one of [1] to

[10] , wherein the content of the component (D) is 0 to 5% by mass.

[12] A method for stabilizing an emulsion composition obtained by adding (E) at least one surfactant selected from the group consisting of PEG-20 phytosterol, polyoxyethylene arachidone, glyceryl behenate, and polyglyceryl-6 octastearate to a composition containing (A) an oily component; (B) 40% by mass or more of one or more selected from the group consisting of polyhydric alcohols having 3 to 5 carbon atoms and polyethylene glycols; (C) one or more selected from the group consisting of polyacrylamide compounds and polyvinylpyrrolidone; and (D) 0 to 15% by mass of water.

[13] The method according to

[12] , wherein the component (C) is polyacrylamide and / or polyvinylpyrrolidone.

[14] The method according to

[12] or

[13] , wherein the content of the component (C) is 0.4 to 5.0% by mass.

[15] The method according to any one of

[12] to

[14] , wherein the component (A) is one or more selected from the group consisting of shea butter, squalane, and sunflower seed wax.

[16] The method according to

[15] , wherein the squalane is one or more selected from the group consisting of squalane from shark liver oil, sugar squalane derived from sugarcane, and vegetable squalane derived from olives.

[17] The method according to any one of

[12] to

[16] , wherein the composition further contains (F) an organic acid or a salt thereof.

[18] The method according to

[17] , wherein the organic acid is ascorbic acid or azelaic acid.

[19] The method according to any one of

[12] to

[18] , wherein the composition further contains (G) an inorganic acid or a salt thereof.

[20] The method according to

[19] , wherein the organic acid is pyrosulfite or phosphoric acid.

[21] The method according to any one of

[12] to

[20] , wherein the content of the component (A) in the composition is 3 to 40% by mass.

[22] The method according to any one of

[12] to

[21] , wherein the content of the component (D) in the composition is 0 to 5 mass%.

[0066] EXAMPLES Next, the present invention will be described in detail with reference to Examples, but the present invention is not limited to the following Examples. The unit of the amount of each component in the tables is % by mass unless otherwise specified in the tables.

[0067] Compositions were prepared according to the formulations shown in Tables 1 to 4. First, ascorbic acid, polyhydric alcohol, thickener, and, if included, water were mixed to prepare a gel composition. Separately, a surfactant and an oily component were mixed and added to the gel composition to prepare an emulsion composition.

[0068] The main raw materials used in the examples are as follows: Polyvinylpyrrolidone (product name: FlexiThix, manufacturer: Ashland Japan Co., Ltd.) Mixture of polyacrylic acid amide, light liquid isoparaffin, polyoxyethylene lauryl ether (7E.O.), and purified water (product name: Sepigel 305, manufacturer: SEPPIC S.A.) (breakdown: polyacrylic acid amide 40% by mass, light liquid isoparaffin 24% by mass, polyoxyethylene lauryl ether (7E.O.) 6% by mass, and purified water 30% by mass) Sugar squalane (product name: NIKKOL Sugar Squalane, manufacturer: Nikko Chemicals Co., Ltd.) Sunflower seed wax (product name: TOWAX-6F2, manufacturer: Toa Kasei Co., Ltd.) Shea butter (product name: CROPURE SHEA BUTTER-SO-(JP), manufacturer: Croda Japan Co., Ltd.) Polyoxyethylene arachyl ether and stearyl alcohol mixture (product name: NIKKOL WAX-230, manufacturer: Nikko Chemicals Co., Ltd.) (breakdown: 25% by mass of polyoxyethylene arachyl ether, 75% by mass of stearyl alcohol), glyceryl behenate, polyglyceryl-6 octastearate (product name: TAISET 50C, Taiyo Kagaku Co., Ltd.) (breakdown: 50% by mass of glyceryl behenate, 50% by mass of polyglyceryl-6 octastearate), steareth-3 (product name: EMALEX 603, manufacturer: Nippon Emulsion Co., Ltd.), Beheneth-30 (product name: NIKKOL BB-30, manufacturer: Nikko Chemicals Co., Ltd.), pentaglyceryl tristearate (product name: NIKKOL Decaglyn3-SV, manufacturer: Nikko Chemicals Co., Ltd.). Disteareth-5 lauroyl glutamate (product name: AMITER LGS-5(H), manufacturer: Nippon Emulsion Co., Ltd.) Mixture of behenyl alcohol, decaglyceryl pentastearate, and sodium stearoyl lactylate (product name: Nikomulus 41, manufacturer: Nikko Chemicals Co., Ltd.) Polyglyceryl-2 stearate, glyceryl stearate, stearyl alcohol (product name: PolyAquol 2W, manufacturer: Innovacos) Glycerin monostearate (product name: NIKKOL MGS-BMV, manufacturer: Nikko Chemicals Co., Ltd.)PEG-20 phytosterol (product name: NIKKOL BPS-20, manufacturer: Nikko Chemicals Co., Ltd.) Sucrose laurate (product name: RYOTO (registered trademark) Sugar Ether L-1695, manufacturer: Mitsubishi Chemical Foods Corporation)

[0069] [Evaluation of Emulsion Composition Formation] Each composition was prepared, and emulsified by visually confirming that the composition had a viscosity of 15 Pa·s or more and was creamy and opaque.

[0070] [Evaluation of emulsion stability] After preparing each composition, the sample was left to stand at room temperature and at 50° C., and the state of the preparation was evaluated after 3 days and 1 month. If the smooth creamy consistency was maintained after storage, as seen by visual inspection, as it was immediately after preparation, it was evaluated as ◯, and if crystal grains or separation were observed, it was evaluated as ×.

[0071] [Evaluation of Ascorbic Acid Residual Rate] After preparing each composition shown in Table 4, the amount of L-ascorbic acid contained in the composition was measured and compared with the amount of L-ascorbic acid after 1 month at 50°C. The residual rate (%) of L-ascorbic acid after 1 month at 50°C was calculated, assuming the value before storage as 100%, and is shown in the table.

[0072] The HPLC conditions for measuring the amount of L-ascorbic acid in the compositions described in Examples 8 to 9 and 12 to 15 were as follows, and the content was calculated from a calibration curve using a standard concentration solution. Reverse-phase column: A stainless steel tube with an inner diameter of 4.6 mm and a length of 15 cm packed with 5 μm octadecylsilylated silica gel for liquid chromatography. Eluent: A water / acetonitrile mixture (9:1) adjusted to pH 3.0 with phosphoric acid. Column temperature: 40°C. Detector UV: 250 nm.

[0073] The evaluation results of the compositions of the examples and comparative examples are shown in Tables 1 to 4.

[0074]

[0075]

[0076] The results in Tables 1 to 4 show that the compositions of the Examples not only had a good emulsified state immediately after production, but also maintained a good emulsified state after storage. On the other hand, the compositions of the Comparative Examples sometimes failed to emulsify, and sometimes, even after emulsification, crystal grains formed after storage.

[0077] When the color of each composition was visually confirmed, it was confirmed that the compositions of the Examples showed a less severe degree of yellowing after storage than the compositions of the Comparative Examples.

[0078] In Examples 8, 9, 12, 13, 14, and 15, it was confirmed that ascorbic acid remained in a good state even after one month at 50°C.

[0079] [Formulation Examples] Formulation examples are shown in Table 5 below.

[0080]

Claims

1. An emulsion composition comprising: (A) an oily component; (B) 40% by mass or more of one or more selected from the group consisting of polyhydric alcohols having 3 to 5 carbon atoms and polyethylene glycols; (C) one or more selected from the group consisting of polyacrylamide compounds and polyvinylpyrrolidones; (D) 0 to 15% by mass of water; and (E) at least one surfactant selected from the group consisting of PEG-20 phytosterol, polyoxyethylene arachyl ether, glyceryl behenate, and polyglyceryl-6 octastearate.

2. The emulsion composition according to claim 1, wherein the component (C) is polyacrylamide and / or polyvinylpyrrolidone.

3. The emulsion composition according to claim 1, wherein the content of component (C) is 0.4 to 5.0 mass %.

4. The emulsion composition according to claim 1, wherein the component (A) is one or more selected from the group consisting of shea butter, squalane, and sunflower seed wax.

5. The emulsion composition according to claim 1, further comprising (F) an organic acid or a salt thereof.

6. The emulsion composition according to claim 1, further comprising (G) an inorganic acid or a salt thereof.

7. The emulsion composition according to claim 5, wherein the content of component (D) is 0 to 5 mass %.

8. A method for stabilizing an emulsion composition obtained by causing a composition comprising: (A) an oily component; (B) 40% by mass or more of one or more selected from the group consisting of polyhydric alcohols having 3 to 5 carbon atoms and polyethylene glycols; (C) one or more selected from the group consisting of polyacrylamide compounds and polyvinylpyrrolidones; and (D) 0 to 15% by mass of water to coexist with (E) at least one surfactant selected from the group consisting of PEG-20 phytosterol, polyoxyethylene arachyl ether, glyceryl behenate, and polyglyceryl-6 octastearate.

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