emulsion

The emulsion with cannabidiol, hydrocarbon oil, silicone oil, and nonionic surfactant addresses the absorption challenge of CBD, providing effective skincare and stability, enhancing fibroblast activation and skin cell turnover.

JP2026111776APending Publication Date: 2026-07-06TOYO SHINYAKU KK
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Patent Information

Application Number
JP2024227193
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Filing Date
2024-12-24
Publication Date
2026-07-06

AI Technical Summary

Technical Problem

Cannabidiol (CBD) is highly lipophilic and difficult to absorb through the skin, limiting its skin care effectiveness, and existing emulsions do not provide excellent skincare effects, usability, and formulation stability.

Method used

An emulsion containing 0.05% by mass or more of cannabidiol, hydrocarbon oil and/or silicone oil, and a nonionic surfactant, with an average particle size of 60 μm or less, and optionally including a thickening agent and polyhydric alcohol, forming an oil-in-water emulsion for topical skin application.

Benefits of technology

The emulsion achieves excellent skincare effects, improved usability, and enhanced formulation stability, promoting fibroblast activation and skin cell turnover, while maintaining a pleasant feel and non-stickiness.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present invention aims to find an emulsion that enhances the skincare effects of cannabidiol, and to provide an emulsion that enhances the skincare effects of cannabidiol by containing (a) 0.05% by mass or more of cannabidiol, (b) hydrocarbon oil and / or silicone oil, and (c) a nonionic surfactant. [Solution] In an emulsion containing (a) cannabidiol, (b) an oil, and (c) a surfactant, the skincare effect of cannabidiol can be enhanced by incorporating the oil at a concentration of 20-30% by mass.
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Description

Technical Field

[0005]

[0001] The present invention relates to an emulsion containing 0.05% by mass or more of cannabidiol, a hydrocarbon oil and / or a silicone oil, and a nonionic surfactant.

Background Art

[0002] Cannabidiol (CBD) has attracted attention as a component expected to have a new pharmacological action. Cannabidiol is one of the cannabinoids contained in hemp, and for example, therapeutic agents for epilepsy, therapeutic compositions for tuberous sclerosis and inflammatory diseases, etc. have been developed (Patent Documents 1 to 3). In addition, its use as an external preparation has also been developed.

[0003] However, since cannabidiol is a highly lipophilic compound and is difficult to be absorbed from the skin or the like, its skin care action has not been fully exerted. For this reason, an emulsion with an improved skin care action of cannabidiol is desired. In addition, there is no product that can obtain excellent skin care effects, excellent usability, formulation stability and usability, and an emulsion with improved these properties is desired.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Patent Document 2

[0006] The present invention provides an emulsion containing 0.05% by mass or more of cannabidiol, a hydrocarbon oil and / or silicone oil, and a nonionic surfactant.

[0007] The outline of the present invention is as follows: [1] An emulsion comprising (a) 0.05% by mass or more of cannabidiol, (b) hydrocarbon oil and / or silicone oil, and (c) a nonionic surfactant. [2] The emulsion according to [1], characterized in that the average emulsion particle size is 60 μm or less. [3] The emulsion according to [1], further characterized by containing (d) a thickening agent. [4] The emulsifier according to [1], further characterized by containing (e) a polyhydric alcohol. [5] The emulsion according to [1], characterized in that it is an oil-in-water emulsion. [6] The emulsion according to [1], characterized in that it is a topical skin preparation. [7] The emulsion according to [1], characterized in that it is for skincare use. [8] The emulsion according to [7], characterized in that the skin care is to improve and / or promote skin cell turnover. [9] The emulsion according to [7], characterized in that skincare is moisturizing the skin.

[10] The emulsion according to [1], characterized by its cell-activating properties. [Effects of the Invention]

[0008] According to the present invention, it is possible to provide an emulsion that has excellent skincare effects, excellent usability, excellent formulation stability, and excellent usability. [Modes for carrying out the invention]

[0009] The present invention is described below in terms of preferred embodiments. In this specification, skincare effects include effects that improve and / or promote skin cell turnover and skin moisturizing effects. The feel of use includes the spreadability of the emulsion, good skin compatibility, moisturizing effect, and non-stickiness. The stability of the formulation includes stability of appearance, such as the absence of separation, stability of average particle size, and viscosity stability.

[0010] The inventors have discovered that by using an emulsion containing cannabidiol, hydrocarbon oil and / or silicone oil, and a nonionic surfactant, and setting the cannabidiol content to a specific value or higher, it is possible to remarkably improve formulation stability, achieve a pleasant feel, and obtain excellent fibroblast activation activity.

[0011] (a) Cannabidiol The emulsion of the present invention is characterized by containing cannabidiol. Cannabidiol is a type of cannabinoid and is known to be found in hemp. Cannabidiol is known to have different pharmacological effects from tetrahydrocannabinol, which is also a type of cannabinoid. In the present invention, cannabidiol can be extracted and purified from plants such as hemp or citrus peels, or synthesized, but it is preferable to use cannabidiol that has been purified from natural products or synthesized from natural products in order to enhance safety and the skincare effects of cannabidiol.

[0012] In particular, the present invention, which is an emulsion containing 0.05% or more cannabidiol, hydrocarbon oil and / or silicone oil and a nonionic surfactant, has a fibroblast-activating effect, as described in the examples below. The reason for this is not clear, but it is presumed that by applying an emulsion of cannabidiol, which has anti-inflammatory and moisturizing effects, and hydrocarbon and / or silicone oil, which is known to have moisturizing effects, to the skin, fibroblast activation can be effectively promoted, resulting in excellent skincare effects. Furthermore, even though the present invention contains cannabidiol, an oily substance that tends to be sticky and difficult to emulsify, by incorporating it into an emulsion together with hydrocarbon oil and / or silicone oil and a nonionic surfactant, the emulsion containing cannabidiol becomes more stable. As a result, spreadability, skin compatibility, and stickyness are improved, resulting in a superior feel and improved formulation stability.

[0013] The cannabidiol content in the emulsion of the present invention is not particularly limited, but is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, and particularly preferably 0.5% by mass or more from the viewpoint of obtaining a high skincare effect. Furthermore, it is preferably 10% by mass or less, more preferably 5% by mass or less, and particularly preferably 3% by mass or less from the viewpoint of obtaining an excellent skincare effect.

[0014] (b) Oils In the present invention, the emulsion contains hydrocarbon oil and / or silicone oil, and by maintaining a constant amount of hydrocarbon oil and / or silicone oil in the emulsion, the formulation stability of the emulsion can be improved, the feel of the emulsion can be enhanced, and excellent skincare effects can be achieved.

[0015] <Hydrogen oils> (b) When the oil is a hydrocarbon oil, specific examples include isododecane, isohexadecane, liquid wax, hydrogenated polyisobutene (volatile isoparaffin, light liquid isoparaffin), hydrogenated polydecene, squalane, ceresin, tetradecene, paraffin, polybutene, microcrystalline wax, mineral oil (liquid paraffin), petrolatum, etc. Among these, isohexadecane, hydrogenated polyisobutene, squalane, and mineral oil (liquid paraffin) are preferred, and isohexadecane, squalane, and mineral oil (liquid paraffin) are particularly preferred in that they fully exhibit the formulation stability, feel, and cell activation effect of the emulsion. (b) When hydrocarbon oil is included as an oiling agent, the amount of hydrocarbon oil is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, even more preferably 0.1% by mass or more, and particularly preferably 1% by mass or more, in the emulsion, from the viewpoint of improving the formulation stability, feel, and skincare effect of the emulsion. Furthermore, the amount of hydrocarbon oil is preferably 80% by mass or less, more preferably 70% by mass or less, even more preferably 60% by mass or less, and particularly preferably 50% by mass or less, in the emulsion, from the viewpoint of improving the formulation stability, feel, and skincare effect of the emulsion. If hydrocarbon oils are included, one type of hydrocarbon oil may be used alone, or two or more types may be used in combination. This is also permissible. When two or more hydrocarbon oils are used in combination, the amount of hydrocarbon oil in the emulsion is the total amount of the multiple hydrocarbon oils.

[0016] <Silicone oil> (b) When the oil agent is silicone oil, specifically, for example, volatile and non-volatile linear dimethylpolysiloxanes such as dimethylpolysiloxane (1 cs), dimethylpolysiloxane (1.5 cs), dimethylpolysiloxane (2 cs), dimethylpolysiloxane (6 cs), dimethylpolysiloxane (20 cs), dimethylpolysiloxane (100 cs); branched siloxanes such as methyltrimethicone, tris(trimethylsilyl)methylsilane, tetrakis(trimethylsilyl)silane; cyclic dimethylsiloxanes such as cyclopentasiloxane, octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, dodecamethylcyclohexasiloxane; methylphenylpolysiloxanes such as crosslinked methylpolysiloxane, networked methylpolysiloxane, methyltrimethicone, diphenylsiloxyphenyltrimethicone, and higher alcohol-modified organopolysiloxane. Among these, volatile and non-volatile linear dimethylpolysiloxanes and cyclic dimethylsiloxanes are preferred, volatile linear dimethylpolysiloxanes and cyclic dimethylsiloxanes are more preferred, and dimethylpolysiloxane and cyclopentasiloxane are particularly preferred in terms of further enhancing the formulation stability, usability, and skin care effect of the emulsion. (b) When containing silicone oil as the oil agent, from the viewpoint of enhancing the formulation stability, usability, and skin care effect of the emulsion, the amount of silicone oil is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, still more preferably 0.1% by mass or more, and particularly preferably 1% by mass or more in the emulsion. Also, from the viewpoint of enhancing the formulation stability, usability, and skin care effect of the emulsion, the amount of silicone oil is preferably 80% by mass or less, more preferably 70% by mass or less, still more preferably 60% by mass or less, and particularly preferably 50% by mass or less in the emulsion. When containing silicone oil, one kind of silicone oil may be used alone or two or more kinds may be used in combination. When two or more kinds of silicone oil are used in combination, the amount of silicone oil in the above emulsion is the total amount of the plurality of hydrocarbon oils.

[0017] The content of the oil agent (b) in the emulsion of the present invention is not particularly limited, but from the viewpoints of enhancing the formulation stability, usability, and skin care effect of the emulsion, it is preferably 0.01% by mass or more, more preferably 0.1% by mass or more, and particularly preferably 1% by mass or more. Also, from the viewpoints of enhancing the formulation stability, usability, and skin care effect of the emulsion, it is preferably 50% by mass or less, more preferably 40% by mass or less, and particularly preferably 30% by mass or less. The oil agent may be used alone as one kind of hydrocarbon oil or silicone oil, or a hydrocarbon oil and a silicone oil may be used in combination. When two or more kinds of hydrocarbon oils and silicone oils are used in combination, the amount of the oil agent in the above emulsion is the total amount of the plurality of hydrocarbon oils and silicone oils.

[0018] The content of the oil agent with respect to cannabidiol in the emulsion of the present invention is not particularly limited. From the viewpoints of enhancing the formulation stability, usability, and skin care effect of the emulsion, when the content of cannabidiol is taken as 1, 1:0.005 to 1,000,000 is preferable, more preferably 1:0.01 to 500,000, and particularly preferably 1:0.02 to 100,000. When two or more kinds of oil agents are used, the content of the oil agent with respect to cannabidiol is the total amount thereof.

[0019] (c) Nonionic surfactant In the present invention, when the emulsion contains a nonionic surfactant and the amount of the nonionic surfactant in the emulsion is made constant, the formulation stability of the emulsion can be improved, the usability of the emulsion can be improved, and the skin care effect can be achieved. The nonionic surfactant used in the present invention may be any nonionic surfactant that can be used by applying it to the skin. It may be liquid, or may be a solid such as powder, fine granule, granule, flake, solid form, etc., and is not particularly limited. From the viewpoints of storage stability, ease of handling, and the effect of enhancing the skin care effect of cannabidiol, those that can be uniformly dissolved in water at room temperature (20°C) are preferable.

[0020] The nonionic surfactant of the present invention may be any nonionic surfactant that can be applied to the skin and is not particularly limited as long as it is water-soluble and can be dispersed or dissolved in water. Examples of nonionic surfactants include glycerin fatty acid esters, sorbitan fatty acid esters, sucrose fatty acid esters, polyoxyalkylene alkyl ethers, polyoxyalkylene alkylphenyl ethers, fatty acid alkanolamides, lecithin, and saponins.

[0021] The HLB value of the nonionic surfactant used in the present invention is not particularly limited, but from the viewpoint of achieving formulation stability of the emulsion, feel, cell activation effect, and ease of handling, it is preferably 8 or higher, more preferably 9 or higher, particularly preferably 10 or higher, preferably 12 or lower, preferably 11 or lower, and particularly preferably 10 or lower. The HLB value is an index that shows the hydrophilic-lipophilic balance, and represents the molecular weight of the hydrophilic group portion in the total molecular weight of the surfactant, and can be determined, for example, by Griffin's formula.

[0022] Examples of nonionic surfactants with an HLB value of 8 to 12 include polyglycerin fatty acid esters [e.g., polyglyceryl-10 diisostearate (HLB 10.0), hexaglyceryl monomyristate (HLB 11.0), hexaglyceryl monostearate (HLB 9.0), hexaglyceryl monooleate (HLB 9.0), decaglyceryl monostearate (HLB 12.0), decaglyceryl monoisostearate (HLB 12.0), decaglyceryl monooleate (HLB 12.0), decaglyceryl distearate (HLB 9.5) and decaglyceryl diisostearate (HLB 10.0)]; polyoxyethylene glycerol fatty acid esters (e.g., polyoxyethylene ("POE")(5) glyceryl monostearate (HLB 9.5) and POE(5) glycerol monooleate (HLB 9.5)); polyoxyethylene sorbitan fatty acid esters [e.g., POE(6) sorbitan monostearate (HLB 9.5), POE(20) sorbitan tristearate (HLB 10.5), POE(6) sorbitan monooleate (HLB 10.0) and POE(20) Sorbitan trioleate (HLB 11.0); polyoxyethylene sorbitol fatty acid ester [e.g., POE(30) sorbitol tetraoleate (HLB 11.5)]; polyoxyethylene lanolin / lanolin alcohol / beeswax derivatives [e.g., POE(10) lanolin (HLB 12.0) and POE(20) sorbitol beeswax (HLB 9.5)]; polyoxyethylene castor oil / hydrogenated castor oil [e.g., POE(20) castor oil (HLB 10.5), POE(20) hydrogenated castor oil (HLB 10.5), and POE(30) hydrogenated castor oil (H LB11.0)]; Polyoxyethylene sterols / hydrogenated sterols [e.g., POE(5) phytosterol (HLB9.5)]; Polyoxyethylene alkyl ethers [e.g., POE(2) lauryl ether (HLB9.5), POE(4.2) lauryl ether (HLB11.5), POE(5.5) cetyl ether (HLB10.5), POE(7) cetyl ether (HLB11.5), POE(4) stearyl ether (HLB9.0), POE(7) oleyl ether (HLB10.5), POE(10) behenyl ether (HLB10.0), POE(2)(C12-15) alkyl ether (HLB 9.0), POE(4)(C12-15) alkyl ether (HLB 10.5), POE(5) secondary alkyl ether (HLB 10.5), and POE(7) secondary alkyl ether (HLB 12.0)]; polyoxyethylene polyoxypropylene alkyl ethers [e.g., POE(1) polyoxypropylene ("POP")(4) cetyl ether (HLB 9.5), POE(10) POP(4) cetyl ether (HLB 10.5), POE(20) POP(6) decyltetradecyl ether (HLB 11.0), and Examples include POE(30)POP(6) decyltetradecyl ether (HLB 12.0); polyethylene glycol fatty acid esters [e.g., PEG(10) monostearate (HLB 11.0), PEG(10) monooleate (HLB 11.0), and PEG diisostearate (HLB 9.5)]; and (tri)polyoxyethylene glyceryl isostearates [e.g., PEG(8) glyceryl isostearate (HLB 10.0), PEG(10) glyceryl isostearate (HLB 10.0), and PEG(15) glyceryl isostearate (HLB 12.0)].

[0023] In the present invention, when two or more nonionic surfactants are used, the HLB value is the arithmetic mean of the HLB values ​​of each nonionic surfactant based on their blending ratio. Therefore, even if the HLB value of each individual nonionic surfactant is less than 8 or greater than 12, if the mixed HLB value is between 8 and 12, it is considered a nonionic surfactant with an HLB value between 8 and 12 in the present invention.

[0024] In this invention, only one of these nonionic surfactants may be used, or two or more may be used.

[0025] The content of nonionic surfactant in the emulsion of the present invention is not particularly limited, but from the viewpoint of enhancing the formulation stability, feel, and skincare effect of the emulsion, it is preferably 0.000005% by mass or more, more preferably 0.00005% by mass or more, and particularly preferably 0.0001% by mass or more. Furthermore, it is preferably 50% by mass or less, more preferably 40% by mass or less, and particularly preferably 30% by mass or less. When two or more surfactants are used, the surfactant content is the total amount.

[0026] The amount of surfactant relative to cannabidiol in the emulsion of the present invention is not particularly limited. However, from the viewpoint of enhancing the formulation stability, feel, and skincare effect of the emulsion, a ratio of 1:0.005 to 1,000,000 is preferred, more preferably 1:0.01 to 500,000, and particularly preferred 1:0.02 to 1,000,000, when the cannabidiol content is set to 1. When two or more nonionic surfactants are used, the amount of surfactant relative to cannabidiol is the total amount.

[0027] (d) Thickening agent In the present invention, the emulsion contains a thickening agent, and by maintaining a constant amount of the thickening agent in the emulsion, the formulation stability, feel, and skincare effect of the emulsion can be further enhanced. Examples of thickening agents used in the present invention include various types that can be used in the cosmetics and pharmaceutical fields. For example, natural polysaccharides, cellulosic polymers, synthetic polymers, and clay minerals can be used. The thickening agent used in the present invention is not particularly limited as long as it is a polyhydric alcohol that can be applied to the skin, but specifically, examples include guar gum, locust bean gum, carrageenan, xanthan gum, carboxymethylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl polymer, alkyl acrylate methacrylate copolymer, polyethylene glycol, bentonite, (hydroxyethyl acrylate / sodium acryloyldimethyltaurate) copolymer, (ammonium acryloyldimethyltaurate / vinylpyrrolidone) copolymer, etc. Of these, xanthan gum, alkyl acrylate methacrylate copolymer, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyethylene glycol, carboxyvinyl polymer, (hydroxyethyl acrylate / sodium acryloyldimethyltaurate) copolymer, and (ammonium acryloyldimethyltaurate / vinylpyrrolidone) copolymer are preferred, with carboxyvinyl polymer being particularly preferred, from the viewpoint of further enhancing the formulation stability, feel, and skincare effect of the emulsion. In the present invention, only one of these thickeners may be used, or two or more may be used.

[0028] The content of the thickener in the emulsion of the present invention is not particularly limited, but from the viewpoint of improving the formulation stability, feel, and skincare effect of the emulsion, it is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, and particularly preferably 0.01% by mass or more. Furthermore, from the viewpoint of improving the formulation stability, feel, and skincare effect of the emulsion, it is preferably 10% by mass or less, more preferably 5% by mass or less, and particularly preferably 1% by mass or less. When two or more thickeners are used, the content of the thickeners is the total amount.

[0029] The amount of thickener relative to cannabidiol in the emulsion of the present invention is not particularly limited. However, from the viewpoint of improving the formulation stability, feel, and skincare effect of the emulsion, a ratio of 1:0.001 to 10,000,000 is preferred, more preferably 1:0.01 to 100,000, and most preferably 1:0.05 to 10,000, when the cannabidiol content is set to 1.

[0030] (e) Polyhydric alcohols The emulsion of the present invention contains a polyhydric alcohol, and by maintaining a constant amount of polyhydric alcohol in the emulsion, the formulation stability of the emulsion can be improved, the feel of the emulsion can be enhanced, and skincare effects can be achieved. The polyhydric alcohol used in the present invention is an organic compound having two or more hydroxyl groups in one molecule. The polyhydric alcohol used in the present invention is not particularly limited as long as it is a polyhydric alcohol that can be applied to the skin, but examples include glycerin; polyglycerins such as diglycerin, triglycerin, and tetraglycerin; dihydric or higher alcohols such as ethylene glycol, 1,3-butylene glycol, 1,4-butylene glycol, propylene glycol, polyethylene glycol, and 1,3-propanediol; sugar alcohols such as erythritol, maltitol, mannitol, sorbitol, and xylitol; and sugars such as sucrose and trehalose. Of these, glycerin, diglycerin, ethylene glycol, 1,3-butylene glycol, 1,4-butylene glycol, propylene glycol, polyethylene glycol, and 1,3-propanediol are particularly preferred in terms of further enhancing the formulation stability, feel, and skincare effects of the emulsion.

[0031] The polyhydric alcohols used in this invention may be one type only, or two or more types may be used. Combining one or more alcohols selected from dihydric or tetrahydric alcohols is particularly preferable in that it further enhances the formulation stability, feel, and skincare effects of the emulsion.

[0032] The polyhydric alcohol content in the emulsion of the present invention is not particularly limited, but from the viewpoint of enhancing the formulation stability, feel, and skincare effect of the emulsion, it is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, and particularly preferably 0.05% by mass or more. Furthermore, from the viewpoint of enhancing the formulation stability, feel, and skincare effect of the emulsion, it is preferably 60% by mass or less, more preferably 50% by mass or less, and particularly preferably 40% by mass or less. When two or more polyhydric alcohols are used, the polyhydric alcohol content is the total amount of those alcohols.

[0033] The polyhydric alcohol content relative to cannabidiol in the emulsion of the present invention is not particularly limited. However, in order to further enhance the formulation stability, feel, and skincare effects of the emulsion, a ratio of 1:0.001 to 10,000,000 is preferred, more preferably 1:0.01 to 100,000, and most preferably 1:0.05 to 10,000, when the cannabidiol content is set to 1.

[0034] The dosage form of the emulsion of the present invention is not particularly limited, but in order to improve the formulation stability, feel, and skincare effect of the emulsion, it may take any of the following forms: oil-in-water, water-in-oil, water-in-water, or oil-in-water. However, an oil-in-water emulsion is preferred in order to further enhance the formulation stability, feel, and skincare effect of the emulsion.

[0035] The emulsion of the present invention preferably has an average particle size of 60 μm or less, as this improves the penetration of the emulsion into the skin and other surfaces, thereby further enhancing the effects of the present invention. From these points of view, the average particle size of the emulsion is preferably 55 μm or less, and more preferably 50 μm or less. On the other hand, the average particle size of the emulsion is, for example 100It is preferable that the size be 1 nm or larger in terms of material availability and ease of manufacturing. 1000 A value of nm or greater is more preferable. The average particle size of the emulsion of the present invention was measured using a microscope (KEYENCE digital microscope VHX-8000; lens used: RZ lens; dual-light high-magnification zoom lens: VH-Z250R / VH-Z250T).

[0036] The viscosity of the emulsion of the present invention is 2,000 to 100,000 mPa·s at 25°C, preferably 2,500 to 90,000 mPa·s, more preferably 3,000 to 80,000 mPa·s, even more preferably 3,500 to 70,000 mPa·s, and particularly preferably 400 to 65,000 mPa·s, from the viewpoint of further enhancing the formulation stability, feel, and skincare effect of the emulsion.

[0037] The pH of the emulsion of the present invention at 25°C is 3 or more and 7 or less. This allows for effective reduction of the emulsion particle size while maintaining low irritation and a good skin feel, and enables excellent formulation stability. From the viewpoint of effectively enhancing the stability of the formulation in combination with the above components, the pH of the emulsion of the present invention at 25°C is 3 or more, preferably 3.4 or more, and more preferably 3.8 or more. From the viewpoint of approximating the pH environment of the skin and ensuring low irritation, the pH of the emulsion of the present invention is 8 or less, preferably 7 or less.

[0038] The emulsion of the present invention may be a topical skin preparation, a composition used by applying it to the skin, and is not particularly limited as long as it is a topical preparation used by applying it to the skin, and can be used, for example, as a cosmetic, pharmaceutical, or quasi-drug. When the topical skin preparation of the present invention is a cosmetic or quasi-drug, examples include lotions, serums, creams, emulsions, all-in-one gels, packs, cleansers, soaps, ointments, and bath additives. However, from the viewpoint of further enhancing the formulation stability, feel, and skincare effect of the emulsion, it is preferable to be a lotion, serum, cream, all-in-one gel, emulsion, bath additive, cleanser, or soap, more preferably a lotion, serum, cream, emulsion, or bath additive, and particularly preferably an emulsion or cream.

[0039] In addition to the cannabidiol, hydrocarbon oil and / or silicone oil, nonionic surfactant, thickener, and polyhydric alcohol mentioned above, the emulsion of the present invention may contain various active ingredients, pH adjusters, thickeners, fragrances, colorants, antioxidants, antibacterial and antifungal agents, alcohols (excluding polyhydric alcohols), inorganic salts, lubricants, solvents, and other components commonly used in emulsions, as long as they do not impair the effects of the present invention, depending on the application and purpose.

[0040] The following describes some representative components contained in the emulsion according to the present invention, other than cannabidiol, hydrocarbon oils and / or silicone oils, nonionic surfactants, thickeners, and polyhydric alcohols.

[0041] The active ingredients used in this invention are not particularly limited, and any drugs or plant extracts used in cosmetics, pharmaceuticals, quasi-drugs, etc., can be used as needed. Typical examples include glycyrrhizic acid or its derivatives, whitening agents such as placental extract, and plant components such as licorice. As for plant components, the whole plant, leaves (leaf blade, petiole, etc.), fruits (mature, immature, etc.), seeds, flowers (petals, ovary, etc.), stems, rhizomes, roots, tubers, etc., can be used after being dried or powdered, but it is common to use extracts obtained by conventional methods using solvents such as water, ethanol, or polyhydric alcohols.

[0042] The emulsion according to the present invention has excellent skincare effects and can be used as a cosmetic, pharmaceutical, or quasi-drug for the purpose of skincare, improving and / or promoting skin overturning, and moisturizing the skin by allowing cannabidiol to act on the skin. When the emulsion of the present invention is used as a cosmetic, pharmaceutical, or quasi-drug, it can be used in a container suitable for storage and use. Examples of containers include plastic, glass, and metal, and are not particularly limited, but a light-shielding container is preferred from the viewpoint of maintaining the stability and shelf life of cannabidiol, and maintaining and improving the action and effects of cannabidiol. [Examples]

[0043] The present invention will be described in more detail below with reference to examples, but the scope of the present invention is not limited to these examples.

[0044] <Preparation of Emulsified Products> According to the compositions shown in Tables 1-3, components (a), (b), and (c) were placed in a container and mixed while heating to 80°C. In Examples 1-8 and 10-13, component (e), which had been mixed in a separate container while heating to 80°C, and water were added in small portions. In Example 9, only water was added in small portions. The mixture was stirred at 5000 rpm for 5 minutes using a stirrer (tabletop quick homomixer LR type, manufactured by MIZUHO Corporation), then cooled to room temperature. Component (d), which had been mixed in a separate container, and phenoxyethanol were added in small portions while stirring at 500 rpm using a stirrer (Three One Motor High Power BLh1200), resulting in a milky white liquid emulsion (oil-in-water emulsion). For cannabidiol, we used CBD powder refined from natural sources (CBD content of 99% or more). As hydrocarbon oils, squalane with an SP value of 16.2 and mineral oil with an SP value of 22.5 were used. As silicone oils, dimethicone with an SP value of 19.0 and liquid at room temperature (20°C) and cyclopentasiloxane with an SP value of 19.0 and liquid at room temperature (20°C) were used. As comparative examples of oils, we used beeswax, which is solid at room temperature (20°C); macadamia nut fatty acid phytosteryl, which is liquid at room temperature (20°C); behenyl alcohol, which is solid at room temperature (20°C); cetanol, which is solid at room temperature (20°C); triethylhexanoin, which is liquid at room temperature (20°C) with an SP value of 18.1; and diisostearyl malate, which is liquid at room temperature (20°C) with an SP value of 18.5. As surfactants, we used polyglyceryl-10 diisostearate with an HLB value of 11.1 (a polyglycerin fatty acid ester), polysorbate 65 (polyoxyethylene sorbitan tristearate (Tween 65)) with an HLB value of 10.5, laureth-2 (polyoxyethylene lauryl ether) with an HLB value of 9.5, and glyceryl stearate with an HLB value of 7.0. For the comparative example, PEG-20 glyceryl isostearate with an HLB value of 15.4 was used as the surfactant. Diglycerin and 1,3-propanediol were used as polyhydric alcohols.

[0045] [Table 1]

[0046] [Table 2]

[0047] [Table 3]

[0048] <Confirmation test of fibroblast activation effect> By confirming the activation of fibroblasts, which are cells that produce collagen and hyaluronic acid in the dermis of the skin, it is possible to confirm the promotion of collagen and hyaluronic acid production in the skin. This can be seen as promoting skin cell turnover, providing moisture, and potentially improving skin problems such as sagging, dryness, roughness, and wrinkles. (1) Normal human dermal fibroblasts (NHDF) were cultured in a 75 cm² flask in a 37°C, 5 vol. %CO₂ incubator using DMEM medium containing 10% fetal bovine serum (FBS). (2) Cells suspended by trypsin treatment were seeded in each well of a 96-well plate (collagen coated) at a cell density of 1.5 × 10^3 cells / well and pre-cultured for 24 hours in a 37°C, 5V %CO2 incubator. (3) After removing the culture medium from each well, 100 μL / well of culture medium containing the test substance, prepared to the specified concentration, was added and incubated for 24 hours at 37°C in a 5V %CO2 incubator. DMEM medium containing 10% FBS was used as the culture medium, and the total concentration of the test substance in the medium was set to 0.05% (w / v). (4) After 24 hours of incubation, the culture medium was removed, each well was washed once with PBS, and 150 μL of Cell Counting Kit-8 (manufactured by Dojin Chemical Co., Ltd.), diluted 30 times by volume with serum-free DMEM, was added to each well. (5) The samples were left standing in a 37°C, 5-volume %CO2 incubator to allow them to develop color appropriately, and then the absorbance at 450 nm was measured. (6) Based on the obtained data, the percentage of control was calculated. % of control = (Data sample - Data blank) / (Data control - Data blank) × 100 (7) The relative values ​​are shown below, with the Control (culture medium only) value set to 100. The denominator (baseline) of the above formula, "Data control - Data blank," is the value obtained by subtracting the absorbance of the "blank" sample at 450 nm from the absorbance of the sample without the test substance (control) at 450 nm. On the other hand, the numerator, "Data sample - Data blank," is the value obtained by subtracting the absorbance of the "blank" sample at 450 nm from the absorbance of the sample with the test substance added at 450 nm. It is known that the value obtained by subtracting the absorbance of the "blank" sample at 450 nm from the absorbance of the sample at 450 nm is proportional to the number of viable cells, and "% of control" represents the relative value of the number of viable cells in the culture medium with the test substance added, with the number of viable cells in the culture medium without the test substance being set to 100.

[0049] <Test to confirm user experience> The feel of the resulting emulsion was evaluated. Samples used were those prepared at the time of preparation (day 0). Three subjects, all in their 20s and 30s and with experience in evaluating topical skin preparations, were randomly selected. The emulsion was applied to the subjects' faces, and a questionnaire was administered regarding the feel of the emulsion, using a 10-point scale to evaluate spreadability, skin absorption, and moisturizing effect. The average value for each item on the questionnaire was calculated and used for evaluation. The results are shown in Table 4. 10: Very good 9: Very good 8: Good 7: Fairly good • 6: Slightly better 5: Neither (The stretch is not noticeable during use) 4: Slightly bad 3: Bad 2: Very bad 1: Very bad

[0050] <Measurement of emulsion particle size> For each emulsion sample immediately after preparation (Day 0), the average particle size of the emulsion particles was measured three times by observing it with a microscope (KEYENCE VHX-8000 digital microscope; lenses used: RZ lens; dual-light high-magnification zoom lens: VH-Z250R / VH-Z250T). Here, particle size is the particle size observed with the microscope, and the average particle size is expressed as the equivalent diameter of a circle, and is shown as the range of the three measurement results.

[0051] <Evaluation of formulation stability> The viscosity and pH of the prepared emulsion were evaluated immediately after preparation (day 0). After storage at 40°C for 28 days, changes in viscosity, separation, and pH were evaluated. Viscosity changes were assessed using a viscometer (Brookfield DV1 VISCOMETER), separation was assessed by determining whether oil and water separation due to creaming was observed in the emulsion, and pH was evaluated using a pH meter. In each case, the formulation stability was comprehensively evaluated by assigning a score of 5 to the least significant change among Comparative Examples 1-6 and Examples 1-13, assigning a score of 1 to the most significant change, and evaluating the others on a graded scale.

[0052] The results of each test are shown in Tables 4-6. From the results in Tables 4-6, when the formulation contained 0.05% by mass or more of cannabidiol, hydrocarbon oil and / or silicone oil, and a nonionic surfactant, the fibroblast activation rate was higher, the average emulsion particle size was smaller, resulting in superior formulation stability and a better feel compared to when it contained 0.04% by mass of cannabidiol, hydrocarbon oil and / or silicone oil, and an ionic surfactant (Comparative Example 6). Furthermore, when the oil was hydrocarbon oil and / or silicone oil, the fibroblast activation rate was higher, the viscosity, pH, and appearance changed less even after storage under high-temperature conditions, demonstrating superior stability and a better feel compared to when the oil was not hydrocarbon oil and / or silicone oil (Comparative Examples 2-5). In Comparative Example 1, because it did not contain cannabidiol, no fibroblast activation effect was confirmed, and formulation stability was not achieved. Therefore, it was confirmed that the emulsion according to the present invention has excellent fibroblast activation effects, and due to its excellent fibroblast activation effects, it can provide effects such as improving and / or promoting skin turnover, moisturizing effects, and improving skin problems such as sagging, dryness, rough skin, and wrinkles. Furthermore, it was found that not only are these skin care effects excellent, but the formulation is also stable and easy to use as a topical skin preparation.

[0053] [Table 4]

[0054] [Table 5]

[0055] [Table 6]

[0056] As is clear from the above test results, the present invention provides an emulsion with excellent skincare effects, as well as excellent usability and stability.

[0057] <Prescription Examples 1-8> A skin preparation (lotion, cream) that is an oil-in-water emulsion was manufactured according to the composition shown in Table 7 below. Specifically, the aqueous phase component and the oil phase component were prepared and emulsified at a predetermined temperature. The lotion and cream obtained in the following formulation example have high skincare efficacy, as well as excellent usability and stability.

[0058] [Table 7]

Claims

1. (a) Cannabidiol 0.05% by mass or more, (b) Hydrocarbon oil and / or silicone oil and (c) Emulsion containing a nonionic surfactant.

2. The emulsion according to claim 1, characterized in that the average emulsion particle size is 60 μm or less.

Citation Information

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