Carbonate aerosol topical skin preparation

Abstract

To provide a carbonated aerosol topical skin application comprising a heparinoid, having less irritation and tight feeling to the skin, easy to spread, and capable to maintain weak acidity after ejection.SOLUTION: Provided is a carbonated aerosol topical skin application consisting of an aerosol stock solution comprising the following components (A) to (C) and a propellant comprising component (D), and having a pH immediately after discharge of 4.0 or more and 7.0 or less. (A) A heparinoid. (B) A water-soluble polymer. (C) Water. (D) Carbon dioxide gas.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to a carbonated aerosol skin preparation for external use. [Background technology]

[0002] Heparinoids have many hydrophilic groups in their structure, such as sulfate, carboxyl, and hydroxyl groups, and possess pharmacological effects such as moisturizing and anti-inflammatory effects. The efficacy of topical skin preparations containing heparinoids is said to be for the treatment and prevention of thrombophlebitis (including hemorrhoids), pain and inflammatory diseases caused by circulatory disorders (induration and pain after injection), chilblains, hypertrophic scars and keloids, keratoderma tylodes palmaris progressiva, asteatosis, swelling, hematoma, tenosynovitis, muscle pain, and arthritis after trauma (bruises, sprains, and contusions), and muscular torticollis (in infancy).

[0003] Heparinoid-containing topical skin preparations are commercially available in the form of creams, soft ointments, lotions, and foam sprays. Among these formulations, foam sprays are expected to prevent dripping from the affected area compared to lotions and are easier to spread on the affected area compared to creams and ointments. For example, Patent Document 1 describes a screen former composition containing a heparinoid, a nonionic surfactant, and a specific polyol, which can be used to form a foam using a screen former without using a foaming gas, in consideration of the skin irritation caused by liquefied natural gas. Patent Document 2 also describes a foamable composition containing a heparinoid and a specific nonionic surfactant, a concentrate containing no lower alcohol, and a propellant.

[0004] On the other hand, carbon dioxide gas is known to have blood circulation promoting and warming effects, and aerosol-type cosmetics using carbon dioxide gas as a propellant are in use (for example, Patent Document 3). [Prior art documents] [Patent documents]

[0005] [Patent Document 1] Japanese Patent Application Publication No. 2019-172703 [Patent Document 2] Japanese Patent Application Laid-Open No. 2016-180012 [Patent Document 3] Japanese Patent Application Laid-Open No. 2018-43932 Summary of the Invention [Problem to be solved by the invention]

[0006] The screen former composition described in Patent Document 1 is difficult to produce fine foam and tends to cause friction when applied. In addition, the foaming composition described in Patent Document 2 uses LPG as a propellant, which causes skin irritation.

[0007] The surface of human skin is maintained at a weakly acidic level as part of homeostasis. However, it is known that the pH of dry, inflamed skin, which is the target of topical skin preparations containing heparinoids, increases. While the application of a weakly acidic formulation is important for maintaining healthy skin, the pH of the ejected foam of the compositions described in Patent Documents 1 and 2 is in the neutral range, which is higher than the pH of the skin, which is weakly acidic. However, adding a large amount of pH adjuster to make the formulation weakly acidic and increase its buffering capacity can cause skin irritation and a tight feeling. In contrast, using carbon dioxide as a propellant, as in the cosmetic described in Patent Document 3, can adjust the pH to a weakly acidic level while suppressing skin irritation and a tight feeling. However, it has been found that such formulations increase the pH, becoming closer to neutral, due to the release of carbon dioxide gas from the formulation after ejection. It is also desirable to reduce friction when spreading the formulation on the skin to reduce physical irritation to the skin.

[0008] Therefore, the present invention relates to a heparinoid-containing carbonate aerosol skin preparation for external use that causes little irritation or tightness to the skin, is easy to spread, and maintains weak acidity even after being dispensed. [Means for solving the problem]

[0009] The present inventors have found that the above-mentioned problems can be solved by using carbon dioxide gas as a propellant and including a water-soluble polymer in the concentrate together with a heparinoid.

[0010] The present invention provides a carbonated aerosol skin preparation for topical use, which comprises an aerosol concentrate containing the following components (A) to (C) and a propellant containing component (D), and which has a pH of 4.0 or higher and 7.0 or lower immediately after ejection. (A) Heparinoids (B) Water-soluble polymer (C) Water (D) Carbon dioxide [Effects of the Invention]

[0011] The carbonated aerosol skin preparation of the present invention is less irritating to the skin and causes less tightness, is easy to spread, and maintains its weak acidity even after being dispensed. DETAILED DESCRIPTION OF THE INVENTION

[0012] Aerosol concentrate The aerosol concentrate of the carbonated aerosol skin preparation for external use of the present invention contains the following components (A) to (C).

[0013] [Component (A): Heparinoid] The heparinoid of component (A) is also known as a mucopolysaccharide polysulfate ester or heparinoid, and is a polysulfated mucopolysaccharide having a repeating unit of a disaccharide consisting of D-glucuronic acid and N-acetyl-D-galactosamine. As the heparinoid, a heparinoid listed in the Japanese Pharmacopoeia Non-Drug Standards 2002 is preferred.

[0014] The average molecular weight of the heparinoid is not particularly limited, but from the viewpoint of medicinal efficacy such as moisturizing effect, it is preferably 1,000 to 1,000,000 Mw, and more preferably 5,000 to 100,000 Mw. The amount (%) of organic sulfate groups in the heparinoid is not particularly limited, but from the viewpoint of medicinal efficacy such as moisturizing effect, it is preferably 20 to 40%, and more preferably 25 to 38%. The amount of organic sulfate groups is measured by the method described in the section on "Heparinoids" in the Japanese Pharmacopoeia 2002.

[0015] The content of component (A) in the aerosol concentrate is preferably 0.05% by mass or more, more preferably 0.07% by mass or more, even more preferably 0.1% by mass or more, and is preferably 0.6% by mass or less, more preferably 0.5% by mass or less, even more preferably 0.4% by mass or less, from the viewpoints of medicinal effects such as moisturizing action, feeling when used, etc. The specific range of the content of component (A) in the aerosol concentrate is preferably 0.05 to 0.6% by mass, more preferably 0.07 to 0.5% by mass, even more preferably 0.1 to 0.4% by mass.

[0016] [Component (B): Water-soluble polymer] The water-soluble polymer of component (B) is not limited as long as it is one commonly used in topical skin preparations, and examples thereof include plant-derived polymers, microbial polymers, mucopolysaccharides, cellulose-based polymers, starch-based polymers, vinyl-based polymers, acrylic polymers, and polyoxyethylene-based polymers. The weight-average molecular weight of the water-soluble polymer of component (B) is preferably 10,000 or more. The weight-average molecular weight is measured using a gel permeation chromatography (GPC)-multiangle laser light scattering (MALLS) system with polyethylene oxide as the standard substance.

[0017] The viscosity of a 2% by mass aqueous solution of component (B) at 20°C is preferably 5 mPa·s or more, more preferably 10 mPa·s or more, and even more preferably 20 mPa·s or more, from the viewpoint of maintaining the agent in a weakly acidic state after ejection, and is preferably 100,000 mPa·s or less, more preferably 8,000 mPa·s or less, and even more preferably 5,000 mPa·s or less, from the viewpoint of improving ejection properties. The viscosity was measured at 20°C using a Brookfield viscometer (e.g., VISCOMETER TVB-10, manufactured by Toki Sangyo Co., Ltd.).

[0018] Examples of plant-based polymers include gum arabic, locust bean gum, guar gum, karaya gum, carrageenan, pectin, agar, and starch (rice, corn, potato, wheat), while examples of microbial polymers include xanthan gum and gellan gum. Examples of mucopolysaccharides include hyaluronic acid, tuberose polysaccharide, and tremella fuciformis polysaccharide. Examples of cellulose-based polymers include methylcellulose, ethylcellulose, carboxymethylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxypropylmethylcellulose stearoxy ether, nitrocellulose, sodium cellulose sulfate, sodium carboxymethylcellulose, crystalline cellulose, cellulose powder, hydroxyethylcellulose hydroxypropylstearylether, sodium hydroxypropylsulfonate, and the like. Examples of starch-based polymers include carboxymethylstarch and methylhydroxypropylstarch. Examples of vinyl-based polymers include polyvinylmethylether, polyvinylpyrrolidone, and carboxyvinyl polymer. Examples of acrylic polymers include sodium polyacrylate, polyethyl acrylate, polyacrylic acid amide, acrylic acid / (meth)acrylate alkyl copolymer, (sodium acrylate / sodium acryloyldimethyltaurate) copolymer, polyacrylate crosspolymer-6, 2-methacryloyloxyethyl phosphorylcholine / butyl methacrylate copolymer, etc. Examples of polyoxyethylene polymers include polyethylene oxide, etc.

[0019] Of these, from the viewpoint of maintaining the agent at a weakly acidic state after ejection and reducing friction during application, water-soluble polymers having a sugar skeleton such as plant-based polymers, microbial-based polymers, mucopolysaccharides, cellulose-based polymers, and starch-based polymers are desirable, with cellulose-based polymers being more preferred, and hydroxypropyl methylcellulose, hydroxypropyl methylcellulose stearoxy ether, and hydroxyethyl cellulose being even more preferred.

[0020] From the viewpoint of maintaining the agent weakly acidic after ejection and reducing friction during application, the content of component (B) in the aerosol concentrate is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, even more preferably 0.10% by mass or more, even more preferably 0.20% by mass or more, and is preferably 5.0% by mass or less, more preferably 2.0% by mass or less, even more preferably 1.0% by mass or less, even more preferably 0.80% by mass or less. The specific range of the content of component (B) in the aerosol concentrate is preferably 0.01 to 5.0% by mass, more preferably 0.05 to 2.0% by mass, even more preferably 0.10 to 1.0% by mass, even more preferably 0.20 to 0.80% by mass.

[0021] From the viewpoints of increasing the uniformity of the drug and improving the feel when spread, the mass ratio (A) / (B) of component (A) to component (B) in the aerosol concentrate is preferably 0.01 or more, more preferably 0.03 or more, even more preferably 0.1 or more, and is preferably 60 or less, more preferably 10 or less, even more preferably 4 or less. The specific range of the mass ratio (A) / (B) of component (A) to component (B) in the aerosol concentrate is preferably 0.01 to 60, more preferably 0.03 to 10, even more preferably 0.1 to 4.

[0022] [Component (C): Water] The content of water as component (C) in the aerosol concentrate is preferably 10% by mass or more, more preferably 20% by mass or more, and even more preferably 40% by mass or more, from the viewpoints of the penetration feel of the ejected agent into the skin and the solubility of the heparinoid and other components, and is preferably 90% by mass or less, more preferably 85% by mass or less, and even more preferably 80% by mass or less. The specific range of the content of component (C) in the aerosol concentrate is preferably 10 to 90% by mass, more preferably 20 to 85% by mass, and even more preferably 40 to 80% by mass.

[0023] [Component (E): Specific pH adjuster] The aerosol concentrate may further contain one or more pH adjusters selected from the group consisting of organic acids, organic acid salts, amino acids, amino acid salts, amines, inorganic acids, inorganic acid salts, and inorganic bases. Examples of organic acids include glycolic acid, citric acid, malic acid, succinic acid, tartaric acid, and lactic acid, and examples of their salts include potassium salts and sodium salts. Examples of amino acids include glutamic acid, aspartic acid, arginine, and lysine, and examples of their salts include sodium salts, hydrochlorides, and succinates. Examples of amines include aliphatic amines such as monoethanolamine, triethanolamine, methylamine, ethylamine, trimethylamine, triethylamine, ethylenediamine, and tetramethylethylenediamine. Examples of inorganic acids include phosphoric acid, and examples of inorganic acid salts include potassium dihydrogen phosphate and disodium hydrogen phosphate. Examples of inorganic bases include alkali metal hydroxides such as lithium hydroxide, sodium hydroxide, and potassium hydroxide. Of these, organic acids, organic acid salts, amino acids, amino acid salts, amines, and inorganic bases are preferred from the viewpoint of enhancing the stability of the heparinoid.

[0024] The content of component (E) in the aerosol concentrate is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, and even more preferably 0.1% by mass or more, from the viewpoint of the stability of the heparinoid, and is preferably 0.7% by mass or less, more preferably 0.5% by mass or less, and even more preferably 0.4% by mass or less, from the viewpoint of reducing skin irritation and a feeling of tightness. The specific range of the content of component (E) in the aerosol concentrate is preferably 0.01 to 0.7% by mass, more preferably 0.05 to 0.5% by mass, and even more preferably 0.1 to 0.4% by mass.

[0025] From the viewpoint of reducing skin irritation and a feeling of tightness, the mass ratio (A) / (E) of component (A) to component (E) in the aerosol concentrate is preferably 0.05 or more, more preferably 0.1 or more, even more preferably 0.2 or more, and is preferably 60 or less, more preferably 10 or less, even more preferably 4 or less. The specific range of the mass ratio (A) / (E) of component (A) to component (E) in the aerosol concentrate is preferably 0.05 to 60, more preferably 0.1 to 10, even more preferably 0.2 to 4.

[0026] From the viewpoint of maintaining the agent in a weakly acidic state after ejection, the mass ratio (B) / (E) of component (B) to component (E) in the aerosol concentrate is preferably 0.01 or more, more preferably 0.1 or more, even more preferably 0.2 or more, and is preferably 500 or less, more preferably 40 or less, even more preferably 2.5 or less. The specific range of the mass ratio (B) / (E) of component (B) to component (E) in the aerosol concentrate is preferably 0.01 to 500, more preferably 0.1 to 40, even more preferably 0.2 to 2.5.

[0027] From the viewpoint of reducing skin irritation and a feeling of tightness, the mass ratio (D) / (E) of component (D) to component (E) in the aerosol concentrate is preferably 0.01 or more, more preferably 0.2 or more, even more preferably 2.5 or more, even more preferably 3.0 or more, and even more preferably 3.5 or more, and from the viewpoint of the stability of the heparinoid, it is preferably 500 or less, more preferably 60 or less, even more preferably 30 or less, even more preferably 15 or less, and even more preferably 10 or less. The specific range of the mass ratio (D) / (E) of component (D) to component (E) in the aerosol concentrate is preferably 0.01 to 500, more preferably 0.2 to 60, even more preferably 2.5 to 30, even more preferably 3.0 to 15, and even more preferably 3.5 to 10.

[0028] [Other optional ingredients] The aerosol concentrate may contain other ingredients commonly used in topical skin preparations in addition to the above-mentioned ingredients. Examples of such ingredients include oils that are liquid at 25°C, polyhydric alcohols, thickeners, preservatives, powders, ethanol, antioxidants, colorants, fragrances, moisturizers, blood circulation promoters, cooling agents, antiperspirants, disinfectants, whitening agents, anti-inflammatory agents, and skin activators. These ingredients are not limited to their intended use, but can also be diverted to other uses or used in combination with other uses depending on the intended purpose. For example, an antiperspirant may be used as a fragrance, or a combination of an antiperspirant and a fragrance may be used.

[0029] The polyhydric alcohol may be any one that is commonly used in cosmetics, and examples thereof include dihydric polyhydric alcohols such as ethylene glycol, propylene glycol, propanediol, 1,3-butylene glycol, 1,3-propanediol, dipropylene glycol, polyethylene glycol, and polypropylene glycol; and trihydric or higher polyhydric alcohols such as glycerin and sorbitol. Of these, from the viewpoint of improving the penetration feel and uniform application of the ejected agent into the skin, glycerin and dihydric polyols are preferred, with glycerin, propylene glycol, propanediol, 1,3-butylene glycol, 1,3-propanediol, and dipropylene glycol being more preferred, glycerin, 1,3-propanediol, and dipropylene glycol being even more preferred, and a composition containing glycerin and dipropylene glycol being even more preferred.

[0030] From the viewpoint of improving the penetration feeling of the ejected agent into the skin and improving uniform application, the content of the polyhydric alcohol in the aerosol concentrate is preferably 1% by mass or more, more preferably 2% by mass or more, even more preferably 5% by mass or more, even more preferably 10% by mass or more, and is preferably 50% by mass or less, more preferably 40% by mass or less, even more preferably 30% by mass or less, even more preferably 20% by mass or less. The specific range of the content of the polyhydric alcohol in the aerosol concentrate is preferably 1 to 50% by mass, more preferably 2 to 40% by mass, even more preferably 5 to 30% by mass, even more preferably 10 to 20% by mass.

[0031] Propellant [Component (D): Carbon dioxide] In the present invention, carbon dioxide gas (component (D)) is used as a propellant. Other propellants can be used in combination with carbon dioxide gas. Examples of propellants other than carbon dioxide gas include liquefied petroleum gas (ethane, propane, ethylene, isobutane, normal butane, propylene, and mixtures thereof (e.g., mixtures of isobutane and propane, or propane and butane)), ether-based propellants (dimethyl ether, etc.), fluorocarbons (fluorocarbons, chlorofluorocarbons, bromochlorofluorocarbons, etc.), compressed gases (nitrogen, air, mixtures thereof, etc.), and chlorofluorocarbons (monochlorodifluoroethane, tetrafluoroethane, etc.). Of these, nitrogen, dimethyl ether, and liquefied petroleum gas are preferred. When other propellants are used in combination with carbon dioxide gas (component (D)), any of these can be used alone or in combinations of two or more.

[0032] When a propellant other than carbon dioxide gas of component (D) is used in combination as a propellant, in order not to impair the effect of carbon dioxide gas, the proportion of carbon dioxide gas of component (D) in the total propellant is preferably 20% or more, more preferably 40% or more, even more preferably 60% or more, and even more preferably 80% or more, based on the volume of the gaseous state (1013.25 hPa, 25°C).

[0033] Carbonated aerosol skin topical agent The carbonated aerosol skin preparation of the present invention can be produced by preparing an aerosol concentrate containing components (A) to (C) and filling it into a pressure-resistant container together with a propellant containing component (D). The spray form is preferably a foam type, in which the aerosol is discharged in the form of a foam.

[0034] The ratio of (D) carbon dioxide gas to 100 parts by mass of the aerosol concentrate is, from the viewpoint of improving the solubility of carbon dioxide gas in the aerosol concentrate, foam viscosity, and sprayability, preferably 0.01 parts by mass or more, more preferably 0.10 parts by mass or more, even more preferably 0.125 parts by mass or more, even more preferably 0.25 parts by mass or more, even more preferably 0.5 parts by mass or more, and even more preferably 1.0 part by mass or more, and is preferably 5.0 parts by mass or less, more preferably 3.0 parts by mass or less.

[0035] The pH of the aerosol topical skin preparation of the present invention immediately after ejection is 4.0 to 7.0, and the pH adjuster of component (E) can be used to adjust the pH within this range. The pH immediately after ejection is preferably 4.5 or higher, more preferably 5.0 or higher, and preferably 6.5 or lower, more preferably 6.0 or lower. In the present invention, the pH immediately after ejection refers to the pH measured 1 minute after ejection from the aerosol container in a 25°C environment.

[0036] When the carbonated aerosol topical skin preparation of the present invention is a foam type, the viscosity of the discharged foam is preferably 0.1 Pa·s or more, more preferably 0.5 Pa·s or more, even more preferably 1.0 Pa·s or more, from the viewpoint of maintaining weak acidity, and is preferably 50 Pa·s or less, more preferably 40 Pa·s or less, even more preferably 30 Pa·s or less. Here, the viscosity of the discharged foam is measured using a B-type viscometer (e.g., VISCOMETER TVB-10, manufactured by Toki Sangyo Co., Ltd.) under the conditions of rotor No. 3, 12 rpm, 25°C, and 10 seconds.

[0037] [How to use] The carbonic acid aerosol skin preparation of the present invention is applied in an appropriate amount to the skin, particularly to the skin of the entire body excluding the scalp, preferably to the face, body, limbs, etc., more preferably to the skin of the hands and feet. It may be taken in the hands and spread over the target area, or it may be ejected directly onto the target area. In the case of a foam type, it is preferable to take it in the hands and apply it without crushing the foam. It is particularly preferable to apply it to areas with thick stratum corneum that are prone to dryness, such as the hands, feet, their fingers, heels, elbows, and knees. The amount to be applied is preferably about 1 g for both hands.

[0038] With respect to the above-described embodiment, further preferred aspects of the present invention will be disclosed below.

[0039] <1> A carbonated aerosol skin topical preparation comprising an aerosol concentrate containing the following components (A) to (C) and a propellant containing component (D), the pH of which immediately after ejection is 4.0 or more and 7.0 or less. (A) Heparinoids (B) Water-soluble polymer (C) Water (D) Carbon dioxide

[0040] <2> The content of component (A) in the aerosol concentrate is preferably 0.05% by mass or more, more preferably 0.07% by mass or more, even more preferably 0.1% by mass or more, and is preferably 0.6% by mass or less, more preferably 0.5% by mass or less, even more preferably 0.4% by mass or less. <1> 2. The carbonate aerosol skin topical preparation according to claim 1.

[0041] <3> Component (B) is preferably one or more selected from plant-based polymers, microbial-based polymers, mucopolysaccharides, cellulose-based polymers, starch-based polymers, vinyl-based polymers, acrylic-based polymers, and polyoxyethylene-based polymers, more preferably one or more selected from water-soluble polymers having a sugar skeleton, even more preferably one or more cellulose-based polymers, and even more preferably one or more selected from hydroxypropyl methylcellulose, hydroxypropyl methylcellulose stearoxy ether, and hydroxyethyl cellulose. <1> or <2> 2. The carbonate aerosol skin topical preparation according to claim 1.

[0042] <4> The viscosity of a 2% by mass aqueous solution of component (B) at 20°C is preferably 5 mPa·s or more, more preferably 10 mPa·s or more, even more preferably 20 mPa·s or more, and is preferably 100,000 mPa·s or less, more preferably 8,000 mPa·s or less, even more preferably 5,000 mPa·s or less. <1> ~ <3> 10. The carbonated aerosol topical skin preparation according to claim 1, wherein the

[0043] <5> The content of component (B) in the aerosol concentrate is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, even more preferably 0.10% by mass or more, and even more preferably 0.20% by mass or more, and is preferably 5.0% by mass or less, more preferably 2.0% by mass or less, even more preferably 1.0% by mass or less, and even more preferably 0.80% by mass or less. <1> ~ <4> 10. The carbonated aerosol topical skin preparation according to claim 1, wherein the

[0044] <6> The mass ratio (A) / (B) of component (A) to component (B) in the aerosol concentrate is preferably 0.01 or more, more preferably 0.03 or more, even more preferably 0.1 or more, and is preferably 60 or less, more preferably 10 or less, even more preferably 4 or less. <1> ~ <5> 10. The carbonated aerosol topical skin preparation according to claim 1, wherein the

[0045] <7> The content of component (C) in the aerosol concentrate is preferably 10% by mass or more, more preferably 20% by mass or more, even more preferably 40% by mass or more, and is preferably 90% by mass or less, more preferably 85% by mass or less, even more preferably 80% by mass or less. <1> ~ <6> 10. The carbonated aerosol topical skin preparation according to claim 1, wherein the

[0046] <8> Preferably, the aerosol concentrate further contains, as component (E), one or more pH adjusters selected from the group consisting of organic acids, organic acid salts, amino acids, amino acid salts, amines, and inorganic bases. <1> ~ <7> 10. The carbonated aerosol topical skin preparation according to claim 1, wherein the

[0047] <9> The content of component (E) in the aerosol concentrate is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, even more preferably 0.1% by mass or more, and is preferably 0.7% by mass or less, more preferably 0.5% by mass or less, even more preferably 0.4% by mass or less. <1> ~ <8> 10. The carbonated aerosol topical skin preparation according to claim 1, wherein the

[0048] <10> The mass ratio (A) / (E) of component (A) to component (E) in the aerosol concentrate is preferably 0.05 or more, more preferably 0.1 or more, even more preferably 0.2 or more, and is preferably 60 or less, more preferably 10 or less, even more preferably 4 or less. <8> or <9> 2. The carbonate aerosol skin topical preparation according to claim 1.

[0049] <11> The mass ratio (B) / (E) of component (B) to component (E) in the aerosol concentrate is preferably 0.01 or more, more preferably 0.1 or more, even more preferably 0.2 or more, and is preferably 500 or less, more preferably 40 or less, even more preferably 2.5 or less. <8> ~ <10> 10. The carbonated aerosol topical skin preparation according to claim 1, wherein the

[0050] <12> Preferably, the aerosol concentrate further contains a polyhydric alcohol. <1> ~ <11> 10. The carbonated aerosol topical skin preparation according to claim 1, wherein the

[0051] <13> The polyhydric alcohol is preferably one or more selected from glycerin and dihydric polyols, more preferably one or more selected from glycerin, propylene glycol, propanediol, 1,3-butylene glycol, 1,3-propanediol, and dipropylene glycol, even more preferably one or more selected from glycerin, 1,3-propanediol, and dipropylene glycol, and even more preferably glycerin and dipropylene glycol. <12> 2. The carbonate aerosol skin topical preparation according to claim 1.

[0052] <14> The content of polyhydric alcohol in the aerosol concentrate is preferably 1% by mass or more, more preferably 2% by mass or more, even more preferably 5% by mass or more, even more preferably 10% by mass or more, and is preferably 50% by mass or less, more preferably 40% by mass or less, even more preferably 30% by mass or less, even more preferably 20% by mass or less. <12> or <13> 2. The carbonate aerosol skin topical preparation according to claim 1.

[0053] <15> The ratio of component (D) to 100 parts by mass of the aerosol stock solution is preferably 0.01 part by mass or more, more preferably 0.10 part by mass or more, still more preferably 0.125 part by mass or more, still more preferably 0.25 part by mass or more, still more preferably 0.5 part by mass or more, still more preferably 1.0 part by mass or more, and is preferably 5.0 parts by mass or less, more preferably 3.0 parts by mass or less. The carbonated aerosol topical skin preparation according to any one of <1> to <14>.

[0054] <16> The pH immediately after ejection is preferably 4.5 or more, more preferably 5.0 or more, and is preferably 6.5 or less. The carbonated aerosol topical skin preparation according to any one of <1> to <15>.

[0055] <17> Preferably, it is ejected in a foamy state. The carbonated aerosol topical skin preparation according to any one of <1> to <16>.

Examples

[0056] Examples 1 to 19, Comparative Examples 1 to 4 Aerosol stock solutions were prepared according to the formulations shown in Tables 1 to 2, filled into an aluminum pressure-resistant container together with an ejectant (carbon dioxide gas or LPG), and aerosol skin cosmetics were manufactured. Regarding these aerosol skin cosmetics, the persistence of pH, foam quality, and usability during application after ejection were evaluated according to the following methods and criteria.

[0057] <pH immediately after ejection> Under a 25°C environment, the aerosol topical skin preparation was ejected from the pressure-resistant container and about 5 g was weighed into a 20 mL plastic cup. After 1 minute of ejection, it was measured using a pH meter (LAQUA F-74).

[0058] <Persistence of pH> In a 25°C environment, approximately 5 g of the aerosol skin preparation was dispensed from a pressure-resistant container into a 20 mL plastic cup, stirred at 200 rpm for 5 minutes, and then measured using a pH meter (LAQUA F-74). The difference between this measured value and the pH immediately after dispensing was defined as ΔpH and was determined as follows: A: ΔpH≦0.5 B: 0.5<ΔpH≦1.0 C: 1.0<ΔpH≦1.5 D: 1.5<ΔpH X: High pH immediately after discharge

[0059] <Foam quality> Approximately 1 g of the aerosol skin preparation was dispensed from a pressure-resistant container onto the palm of the hand, and the appearance of the foam after 10 seconds was evaluated by five expert panelists on the following scale: fine (2 points), coarse foam (1 point), or no foam (0 point). The total evaluation scores are shown in the table.

[0060] <Feel when applying> 0.5 g of the aerosol skin topical preparation dispensed from a pressure-resistant container was applied to the forearm, and the feel when spreading it with the palm of the hand on the side not being treated was evaluated by five expert panelists on the following scale: able to spread smoothly on the skin with no friction (2 points); able to spread somewhat smoothly on the skin with some friction (1 point); difficult to spread on the skin with some friction (0 point). The total evaluation scores are shown in the table.

[0061] <Tight feeling> 0.5g of the aerosol skin topical agent dispensed from a pressure-resistant container was applied to the forearm, and the skin sensation 5 minutes after spreading was evaluated by five expert panelists on a scale of no tightness at all (2 points), almost no tightness (1 point), or some tightness (0 point). The total evaluation scores are shown in the table.

[0062] [Table 1]

[0063] [Table 2]

[0064] *1:Metolose 90SH-15000 (Shin-Etsu Chemical Co., Ltd.) *2:Metolose 60SH-4000 (Shin-Etsu Chemical Co., Ltd.) *3: Sangelose 90L (manufactured by Daido Chemical Industry Co., Ltd.) *4:Natrosol 250HX PHARM (manufactured by Ashland) *5: Alcox E-100 (manufactured by Meisei Chemical Industry Co., Ltd.) *6: CMC Daicel 1150 (manufactured by Daicel Miraize) *7: Carbopol 980 (manufactured by Lubrizol Advanced Materials) *8: Pemulen TR-1 (manufactured by Lubrizol Advanced Materials) *9: Echo Gum T (manufactured by DSP Gokyo Food & Chemical Co., Ltd.) *10: Lipidure PMB (NOF Corporation)

Claims

1. A carbonated aerosol skin preparation for external use, comprising an aerosol concentrate containing the following components (A) to (C) and a propellant containing component (D): The proportion of component (D) in the total propellant is 40% or more by volume in a gaseous state (1013.25 hPa, 25°C), The pH immediately after discharge is 4.0 or more and 7.0 or less. Carbonated aerosol skin topical agent. (A) Heparinoids (B) Water-soluble polymer (C) Water (D) Carbon dioxide

2. 2. The carbonated aerosol skin preparation according to claim 1, which is discharged in the form of foam.

3. 3. The carbonated aerosol skin preparation according to claim 1, wherein the content of component (B) in the aerosol concentrate is 0.01% by mass or more and 5.0% by mass or less.

4. 4. The carbonic acid aerosol skin preparation according to claim 1, wherein component (B) is a water-soluble polymer having a sugar skeleton.

5. 5. The carbonic acid aerosol skin preparation according to claim 4, wherein component (B) is a cellulose-based polymer.

6. The carbonated aerosol skin topical preparation according to any one of claims 1 to 5, further comprising, as component (E), one or more pH adjusters selected from the group consisting of organic acids, organic acid salts, amino acids, amino acid salts, amines, and inorganic bases in the aerosol concentrate.

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