emulsion
The emulsion with 20-30% oil and polyglycerol fatty acid ester addresses CBD's absorption issues, offering superior skincare and stability, enhancing CBD's anti-inflammatory and moisturizing effects.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- TOYO SHINYAKU KK
- Filing Date
- 2024-12-19
- Publication Date
- 2026-07-01
AI Technical Summary
Cannabidiol (CBD) is highly lipophilic and difficult to absorb through the skin, limiting its skin care effects, and existing emulsions fail to provide excellent skincare, usability, and formulation stability simultaneously.
An emulsion containing 20-30% by mass of oil and a surfactant, specifically polyglycerol fatty acid ester, enhances CBD's skincare effects, providing improved absorption and stability.
The emulsion achieves excellent skincare effects, including anti-inflammatory and moisturizing benefits, with enhanced usability and formulation stability, as demonstrated by reduced IL-1β gene expression and stable emulsification.
Smart Images

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Abstract
Description
Technical Field
[0001] The present invention relates to an emulsion containing cannabidiol, a specific amount of an oil agent, and a surfactant. Specifically, it relates to an emulsion characterized by enhancing the skin care effect of cannabidiol. More specifically, in an emulsion containing cannabidiol, 20 to 30% by mass of an oil agent, and a surfactant, the emulsion is characterized by blending polyglycerol fatty acid ester as a surfactant for the purpose of enhancing the skin care effect of cannabidiol.
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 etc., its skin care effect has not been fully exerted. Therefore, an emulsion with an improved skin care effect of cannabidiol is desired. In addition, there is no product that can obtain excellent skin care effects, excellent usability, formulation stability, and usability at the same time, and an emulsion with improved these properties is desired.
Prior Art Documents
Patent Documents
[0004]
Patent Document 1
Patent Document 2
Patent Document 3
Summary of the Invention
Problems to be Solved by the Invention
[0005] According to the present invention, it is possible to provide a topical skin preparation that has excellent skincare effects, a pleasant feel to use, and excellent formulation stability. [Means for solving the problem]
[0006] The inventors of this invention investigated the skincare effects of cannabidiol with various substances in order to find an emulsion containing cannabidiol that enhances the skincare effects of cannabidiol. As a result, they found that a specific combination of oil and surfactant enhances the skincare effects of cannabidiol, leading to the completion of the present invention. Specifically, the present invention relates to an emulsion characterized by containing cannabidiol, 20-30% by mass of oil and a surfactant, and the emulsion having an excellent effect of improving the skincare effects of cannabidiol. Furthermore, the present invention relates to an emulsion characterized by containing cannabidiol, 20-30% by mass of oil and a surfactant, which not only provides an excellent effect of improving the skincare effects of cannabidiol, but also to an emulsion with excellent usability, formulation stability and ease of use.
[0007] The outline of the present invention is as follows: [1] An emulsion containing (a) cannabidiol, (b) an oil, 20-30% by mass, and (c) a surfactant. [2] The emulsion according to [1], characterized in that component (c) is a polyglycerol fatty acid ester. [3] The emulsion according to [1], further characterized by containing (d) a polyhydric alcohol. [4] The emulsifier according to [1], further characterized by containing (e) a fragrance. [5](a) The emulsion according to [1], characterized by containing 0.2% or more of component [5](a). [6] The emulsion according to [1], characterized in that component (c) is at least one selected from polyglyceryl diisostearate and polyglyceryl laurate. [7] The emulsion according to [1], characterized in that it is an oil-in-water emulsion. [8] The emulsion according to [1], characterized in that it is a topical skin preparation. [9] The emulsion according to [1], characterized in that it is a bath additive.
[10] The emulsion according to [1], characterized in that it is for skincare use.
[11] The emulsion according to [8], characterized in that the skincare is for preventing and / or improving rough skin.
[12] The emulsion according to [8], characterized in that skincare is moisturizing the skin.
[13] The emulsion according to [1], characterized in that it is for anti-inflammatory purposes. [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 will now be described in terms of preferred embodiments. The present invention relates to an emulsion characterized by containing cannabidiol, 20-30% by mass of an oil, and a surfactant. In this specification, skin care effects include the effect of preventing and / or improving rough skin, and the moisturizing and anti-inflammatory effects on the skin. Furthermore, the feeling of use includes the feeling of moisture on the skin after use. Moreover, the feeling of moisture on the skin after use includes a fast-responding improvement effect, such as 5 minutes after adding it to bath water and bathing. And the feeling of use includes the ease of use as a bath additive, such as spreading uniformly when the emulsion is added to bath water and stirred. The inventors have found that by combining (a) cannabidiol, (b) 20-30% by mass of an oil, and (c) a surfactant with components such as (d) polyhydric alcohol and (e) fragrance, it is possible to obtain excellent skin care effects, enhance the feeling of use with great effectiveness, and improve the stability and usability of the formulation.
[0010] (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.
[0011] In particular, in the present invention, which uses an emulsion containing cannabidiol, an oil, and a surfactant, and in which the content is 20-30% by mass or higher, it has an IL-1β gene expression promoting effect, as described in the examples below. The reason for this is not clear, but it is presumed that by applying cannabidiol, which has anti-inflammatory and moisturizing effects, and an oil known to have moisturizing effects, to the skin as an emulsion, the IL-1β gene expression promoting effect can be effectively achieved, and excellent anti-inflammatory effects can be obtained. Furthermore, in the present invention, even if cannabidiol, an oily substance that is prone to stickiness and difficult to emulsify, is included in the emulsion together with the oil and surfactant, and the oil content is above a specific amount, the emulsion containing cannabidiol becomes more stable. As a result, improved penetration and stickyness suppression effects are obtained, resulting in a superior feel and improved formulation stability.
[0012] The cannabidiol content in the emulsion of the present invention is not particularly limited, but is preferably 0.0001% by mass or more, more preferably 0.001% by mass or more, and particularly preferably 0.01% 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 a high skincare effect.
[0013] (b) Oils The emulsion of the present invention is characterized by containing cannabidiol along with 20-30% by mass of an oil and a surfactant. The oil used in the present invention may be any oil that can be applied to the skin, and can be either polar or nonpolar. Furthermore, it may be either a liquid or a solid at room temperature (20°C), and is not particularly limited, but a liquid oil at room temperature is preferred from the viewpoint of enhancing the skincare effect of cannabidiol, providing excellent usability, stability, and ease of use. Specifically, for example, hydrocarbon oils such as liquid paraffin, squalane, squalene, and mineral oil; fatty acids such as isostearic acid, oleic acid, and polyhydroxystearic acid; higher alcohols such as octyldodecanol and tetradecyldecanol; isopropyl palmitate, isopropyl myristate, isopropyl stearate, isobutyl stearate, 2-ethylhexyl stearate, isopropyl isostearate, butyl isostearate, decyl isostearate, lauryl isostearate, isodecyl isodecanoate, isodecyl isononanoate, isotridecyl isononanoate, isononyl isononanoate, diisostearyl malate, neopentyl glycoside dioctanoate, propylene glycoside dicaprate, propylene glycoside dicaprylate, glyceryl tri-2-ethylhexanoate, monoisosulfate Examples include ester oils such as polyglyceryl thearate, polyglyceryl diisostearate, diglyceryl triisostearate, diglyceryl tetraisostearate, diethyl sebacate, cetyl 2-ethylhexanoate, ethylhexyl palmitate, octyldodecyl myristate, oleyl oleate, ethyl oleate, triethylhexanoin, ester oils such as N-lauroyl glutamate di(phytosteryl / 2-octyldodecyl), N-lauroyl glutamate di(phytosteryl / behenyl / 2-octyldodecyl), N-lauroyl glutamate di(cholesteryl / 2-octyldodecyl), and N-lauroyl sarcosinate isopropyl; silicone oils such as dimethylpolysiloxane, cyclopentasiloxane, and alkoxy-modified polysiloxane; and one or more of these can be used.
[0014] When formulating (b) an oil agent in the emulsion of the present invention, its content is not particularly limited, but it is preferably 20% by mass or more, more preferably 21% by mass or more. From the viewpoint of having a high skin care effect and obtaining an emulsion with excellent usability, stability and handling properties, it is particularly preferably 22% by mass or more. Also, it is preferably 30% by mass or less, more preferably 27.5% by mass or less. From the viewpoint of obtaining an emulsion with a high skin care effect, excellent usability, stability and handling properties, it is particularly preferably 25% by mass or less.
[0015] The content of the oil agent relative to cannabidiol in the emulsion of the present invention is not particularly limited. When the content of cannabidiol is taken as 1, it is preferably 1:0.005 to 1,000,000, more preferably 1:0.01 to 500,000. From the viewpoint of improving the skin care effect of cannabidiol, excellent usability, stability and handling properties, it is particularly preferably 1:0.02 to 100,000. When two or more oil agents are used, the content of the oil agent relative to cannabidiol is the total amount thereof.
[0016] (b) Surfactant The emulsifier of the present invention is characterized by containing 20 to 30% by mass of an oil agent together with cannabidiol and a surfactant. The surfactant used in the present invention may be any surfactant that can be applied to the skin and used, and 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 improving the skin care action of cannabidiol, those that can be uniformly dissolved in water at room temperature (20°C) are preferred.
[0017] The emulsifier of the present invention is not particularly limited as long as it is a surfactant that can be applied to the skin, and as long as it is water-soluble and can be dispersed or dissolved in water. For example, emulsifiers with an HLB of 5 to 20 can be mentioned. From the perspective of facilitating phase inversion emulsification and obtaining a stable oil-in-water emulsion, an emulsifier with an HLB of 6 to 19 is preferred, and more preferably an anionic surfactant, cationic surfactant, amphoteric surfactant, and nonionic surfactant with an HLB of 7 to 18, and even more preferably a nonionic surfactant with an HLB of 8 to 18.
[0018] The HLB value of the nonionic surfactant used in the present invention is not particularly limited. From the perspectives of improving the skin care effect of cannabidiol, excellent usability, stability, usability, and ease of handling, it is preferably greater than 5, more preferably greater than 6, even more preferably 7 or more, preferably 8 or more, preferably less than 20, preferably less than 19, and particularly preferably less than 18. The HLB value is an index indicating the hydrophilic-lipophilic balance (Hydrophilic-Lypophilic Balance), and indicates the molecular weight of the hydrophilic group portion in the total molecular weight of the surfactant, and can be obtained, for example, by Griffin's formula.
[0019] Examples of nonionic surfactants with an HLB value greater than 5 include polyether-modified silicone, polyoxyethylene hydrogenated castor oil, polyoxyethylene sterol, polyoxyethylene-polyoxyalkylene copolymer, polyglycerol fatty acid ester, and sorbitan fatty acid ester. Among these, polyglycerol fatty acid ester is preferred from the perspectives of improving the skin care effect of cannabidiol, excellent usability, stability, usability, and ease of handling, and polyglycerol fatty acid ester with an HLB value of 8.0 to less than 18 is particularly preferred.
[0020] Examples of polyglycerin fatty acid esters include polyglyceryl-10 isostearate (HLB value: 14), polyglyceryl-2 isostearate (HLB value: 5), polyglyceryl-4 isostearate (HLB value: 8), polyglyceryl-6 isostearate (HLB value: 11), polyglyceryl-10 oleate (HLB value: 13), polyglyceryl-2 oleate (HLB value: 6), polyglyceryl-4 oleate (HLB value: 9), polyglyceryl-6 oleate (HLB value: 12), polyglyceryl-2 caprylate (HLB value: 8), polyglyceryl-6 caprylate (HLB value: 10), polyglyceryl-10 diisostearate (HLB value: 11), and dioleic acid Examples include polyglyceryl-10 (HLB value: 12), polyglyceryl-6 dicaprate (HLB value: 10), polyglyceryl-10 distearate (HLB value: 12), polyglyceryl-10 stearate (HLB value: 14), polyglyceryl-2 stearate (HLB value: 5), polyglyceryl-4 stearate (HLB value: 6), polyglyceryl-2 sesquicaprylate (HLB value: 8), polyglyceryl-10 tristearate (HLB value: 8), polyglyceryl-10 myristate (HLB value: 15), polyglyceryl-4 laurate (HLB value: 10), polyglyceryl-6 laurate (HLB value: 14), and polyglyceryl-10 laurate (HLB value: 14.8).Of these, from the perspective of improving the skincare effect of cannabidiol, providing excellent usability, stability, and usability, polyglyceryl-6 isostearate, polyglyceryl-10 oleate, polyglyceryl-6 oleate, polyglyceryl-6 caprylate, polyglyceryl-10 diisostearate, polyglyceryl-10 dioleate, polyglyceryl-6 dicaprate, polyglyceryl-10 distearate, polyglyceryl-10 stearate, polyglyceryl-10 myristate, polyglyceryl-4 laurate, and laurate are selected. It is more preferable to use polyglyceryl-6 phosphate and polyglyceryl-10 laurate, and particularly preferable to use polyglyceryl-10 isostearate, polyglyceryl-6 isostearate, polyglyceryl-10 oleate, polyglyceryl-6 oleate, polyglyceryl-10 diisostearate, polyglyceryl-10 dioleate, polyglyceryl-10 distearate, polyglyceryl-10 stearate, polyglyceryl-10 myristate, polyglyceryl-6 laurate, and polyglyceryl-10 laurate.
[0021] 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 5 or less, or greater than 20, if the mixed HLB value is greater than 5 and 20 or less, it is considered a nonionic surfactant with an HLB value greater than 5 and 20 or less in the present invention.
[0022] In this invention, only one of these nonionic surfactants may be used, or two or more may be used.
[0023] The surfactant content in the emulsion of the present invention is not particularly limited, but is preferably 0.000005% by mass or more, more preferably 0.0001% by mass or more, and particularly preferably 0.00005% by mass or more from the viewpoint of improving the skincare effect of cannabidiol, providing excellent usability, stability and usability. Furthermore, it is preferably 50% by mass or less, more preferably 40% by mass or less, and particularly preferably 30% by mass or less from the viewpoint of improving the skincare effect of cannabidiol, providing excellent usability, stability and usability. When two or more surfactants are used, the surfactant content is the total amount of those surfactants.
[0024] The surfactant content relative to cannabidiol in the emulsion of the present invention is not particularly limited. When the cannabidiol content is set to 1, a ratio of 1:0.005 to 1,000,000 is preferred, more preferably 1:0.01 to 500,000, and particularly preferred from the viewpoint of improving the skincare effect of cannabidiol, providing excellent usability, stability, and usability, 1:0.02 to 1,000,000. When two or more nonionic surfactants are used, the surfactant content relative to cannabidiol is the total amount of those surfactants.
[0025] (d) Polyhydric alcohols The emulsion of the present invention is characterized by containing a polyhydric alcohol. 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 from the viewpoint of improving the skincare effect of cannabidiol, providing excellent usability, stability, and usability.
[0026] The polyhydric alcohol used in this invention may be one of these types only, or two or more types may be used. Combining a trihydric alcohol with one or more dihydric or tetrahydric alcohols is particularly preferable from the viewpoint of improving the skincare effect of cannabidiol, providing excellent usability, stability, and ease of use.
[0027] The polyhydric alcohol content in the emulsion of the present invention is not particularly limited, but 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 from the viewpoint of improving the skincare effect of cannabidiol, providing excellent usability, stability and usability. Furthermore, it is preferably 60% by mass or less, more preferably 50% by mass or less, and particularly preferably 40% by mass or less from the viewpoint of improving the skincare effect of cannabidiol, providing excellent usability, stability and usability. When two or more polyhydric alcohols are used, the polyhydric alcohol content is the total amount.
[0028] The polyhydric alcohol content relative to cannabidiol in the emulsion of the present invention is not particularly limited. When the cannabidiol content is set to 1, a ratio of 1:0.001 to 10,000,000 is preferred, more preferably 1:0.01 to 100,000, and particularly preferred from the viewpoint of improving the skincare effect of cannabidiol, providing excellent usability, stability, and usability, a ratio of 1:0.05 to 10,000 is preferred.
[0029] (e)Fragrance The emulsion of the present invention is characterized by containing a fragrance. The fragrance used in the present invention is not particularly limited as long as it is an ingredient that can be applied to the skin, but specifically, for example, essential oils extracted from the flowers, leaves, peels, seeds, roots, resins, and woods of natural plants (for example, citrus oils such as orange oil, grapefruit oil, bergamot oil, lemon oil, yuzu oil, lavender oil, ylang-ylang oil, geranium oil, peppermint oil, lemongrass oil, Litsea cubeba fruit oil, spearmint oil, tea tree leaf oil, and basil). Examples of fragrances (scenting agents) include yam oil, geranium oil, bitter orange flower oil, cinnamon leaf oil, cardamom seed oil, clary sage oil, juniper oil, wild rose oil, Roman chamomile flower oil, rosemary leaf oil, etc., and chemically synthesized fragrances (fragrance oils, for example, referring to compounds that have an aromatic scent due to their chemical structure, such as hydrocarbons, alcohols, aldehydes, ketones, esters, lactones, phenols, acetals, etc.).
[0030] The fragrance content in the emulsion of the present invention is not particularly limited, but is preferably 0.00001% by mass or more, more preferably 0.0001% by mass or more, and especially preferably 0.001% by mass or more. It is also preferably 10% by mass or less, more preferably 5% by mass or less, and especially preferably 2% by mass or less. If two or more fragrances are blended, the total amount refers to the total amount of those fragrances.
[0031] The amount of fragrance relative to cannabidiol in the emulsion of the present invention is not particularly limited. When the cannabidiol content is set to 1, a ratio of 1:0.05 to 100,000,000 is preferred, more preferably 1:0.07 to 1000,000, and particularly preferred from the viewpoint of improving the skincare effect of cannabidiol, providing excellent usability, stability, and ease of use.
[0032] The dosage form of the emulsion of the present invention is not particularly limited, but from the viewpoint of enhancing the skincare effect of cannabidiol, excellent usability, stability and usability, and formulation properties, it can take any of the following forms: oil-in-water, water-in-oil, water-in-oil-in-water, or oil-in-water in oil. However, from the viewpoint of enhancing the skincare effect of cannabidiol, excellent usability, stability and usability, it is preferably an oil-in-water emulsion.
[0033] The emulsion particle size of the emulsion of the present invention is preferably 0.5 μm or larger, preferably 1.5 μm or smaller, more preferably 1.1 μm or smaller, and even more preferably 1.0 μm or smaller, from the viewpoint of exhibiting the skincare effect of cannabidiol, excellent usability, stability, and usability. The average emulsion particle size of the bath additive used in 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).
[0034] The pH of the emulsion of the present invention at 25°C is 3 or more and 7 or less. This allows for low irritation and a good skin feel, while also providing a good feel to the bathwater when the emulsion is used as a bath additive. Furthermore, it is possible to effectively reduce the particle size of the emulsion, enabling 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 7 or less, preferably 6 or less.
[0035] 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, for example, it can be used 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 cannabidiol's skincare effect-enhancing properties, excellent feel, stability, and usability, it is preferably 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 a bath additive.
[0036] In addition to the cannabidiol, 20-30% by mass of oil, surfactant, polyhydric alcohol, and fragrance 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.
[0037] The following describes some typical components contained in the emulsion according to the present invention, other than cannabidiol, oils (20-30% by mass), surfactants, polyhydric alcohols, and fragrances.
[0038] 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.
[0039] The emulsion according to the present invention exhibits excellent skincare effects of cannabidiol, and by allowing cannabidiol to act on the skin, it can be used as a cosmetic, pharmaceutical, or quasi-drug for purposes such as skincare, prevention and / or improvement of rough skin, moisturizing the skin, and anti-inflammatory effects. When using the emulsion of the present invention 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]
[0040] 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.
[0041] <Preparation of Emulsified Products> According to the composition shown in Table 1, components (a), (b), and (c) were placed in a container and mixed while being heated to 80°C. Components other than (a), (b), and (c) were then added and mixed. The mixture was then stirred for 5 minutes at a rotation speed of 500 rpm using a stirrer (Three One Motor High Power BLh1200, manufactured by SHINTO Scientific Co., Ltd.) to obtain 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 the ester oil, ethylhexyl palmitate, which is liquid at room temperature (20°C) and has an SP value of 19.0, was used. As hydrocarbon oils, squalane with an SP value of 16.2 and mineral oil with an SP value of 22.5 were used. As surfactants, we used polyglyceryl-10 diisostearate with an HLB value of 11.1 and polyglyceryl-10 laurate with an HLB value of 17.1, both of which are polyglycerin fatty acid esters. For comparative examples, PPG-15 stearyl (polypropylene glycol ether of stearyl alcohol) with an HLB value of 7.5 and glyceryl stearate with an HLB value of 7.0 were used as surfactants. As polyhydric alcohols, 1,3-butylene glycol, propylene glycol, 1,3-propanediol, diglycerin, and glycerin were used. Synthetic fragrances were used as the flavoring agent.
[0042] [Table 1]
[0043] <Confirmation test of skincare effects> IL-1β, an inflammatory cytokine, is known to increase in response to UV radiation exposure to the skin. By evaluating the suppression of IL-1β gene expression using UV-irradiated human cells, it is possible to assess its anti-inflammatory effects in actual skin. Furthermore, by confirming its anti-inflammatory effects, it is possible to confirm that it also provides skincare benefits such as preventing and / or improving rough skin and moisturizing the skin. (1) In a 37°C, 5V %CO2 incubator, 75 cm 2 Normal human epidermal keratinocytes (NHEKs) were cultured in flasks using Keratinocyte Growth Medium 2 Kit (KGM-2). (2) Cells suspended by trypsin treatment were seeded at a cell density of 1.0 × 10^4 cells / well in each well of a collagen-coated 96-well plate and pre-cultured for 48 hours in a 37°C, 5V %CO2 incubator. (3) UVB (20 mJ / cm²) into the cells 2 After irradiation with ), the culture medium was removed from each well, and 100 μL / well of culture medium containing the test substance was added. The cultures were then incubated at 37°C in a 5V %CO2 incubator for 6 hours. (4) KGM-2 was used as the culture medium for preparing the test substance, and the total concentration of the test substance in the culture medium was set to 0.01%. (5) After 6 hours of incubation, the culture medium was removed, RNA was recovered using the Rneasy Mini Kit (QIAGEN), and cDNA was synthesized using ReverTra Ace® qPCR RT Master Mix (TOYOBO). (6) The obtained cDNA was used as a template for quantitative real-time PCR using the Rotor-Gene SYBR Green PCR Kit (QIAGEN). (7) The gene expression level of IL-1β was measured using an IL-1β primer (Eurofins Genomics). In addition, as an endogenous control, the gene expression level of ACTB was measured using an ACTB primer (QIAGEN). (8) The relative expression level of IL-1β was calculated with the value of Comparative Example 1 set to 1.
[0044] <Test to confirm user experience> To evaluate the usability of the resulting emulsions, three subjects aged 20-30 were randomly selected. 30 mL of each emulsion was added to 150 L of bath water set at 40°C. Immediately after stirring the bath water, subjects bathed up to their shoulders for 5 or 20 minutes. The usability (moisture after bathing, and usability depending on bathing time) was evaluated comprehensively using a 10-point scale, and a questionnaire was administered. The average value for each item on the questionnaire was calculated and used for evaluation.
[0045] Evaluation Criteria for User Experience 10: Very good (Leaves skin very moisturized after bathing) 9: Very good (Leaves skin very moisturized after bathing) 8: Good (Leaves skin feeling moisturized after bathing) 7: Fairly good (Leaves skin slightly moisturized after bathing) 6: Slightly good (Leaves skin slightly moisturized after bathing) 5: Neither (I feel a slight moisturizing effect after bathing) 4: Slightly bad (I hardly feel any moisturizing effect after bathing) 3: Poor (Doesn't feel moisturized after bathing) 2: Very bad (I don't feel any moisturizing effect after bathing) 1: Very bad (I didn't feel any moisturizing effect after bathing, making it unsuitable for use.)
[0046] <Stability confirmation test> To evaluate the stability of the obtained emulsions, 30 mL of each emulsion was filled into a sealed transparent container and stored in a 40°C constant temperature bath for 28 days. The appearance was then visually observed and comprehensively evaluated according to the following criteria.
[0047] Stability evaluation criteria 5: No creaming or separation whatsoever. 4: Very slight creaming is observed. 3: Creaming is observed. 2: Very slight separation is observed. 1: Separation is observed.
[0048] <Test to confirm usability> 30 mL of each emulsion was added to 150 L of bath water set at 40°C, and the appearance of the bath water after stirring was visually observed and evaluated according to the following criteria.
[0049] Evaluation Criteria for Usability 5. Emulsify uniformly until milky white. 4: Emulsifies uniformly to a slightly cloudy to milky white color. 3: Slightly cloudy to whitish, with a slight oily residue on the surface of the bathwater. 2: Slightly cloudy to milky white, with oil floating on the surface of the bathwater. 1: It is colorless and transparent without emulsification, and there is an oily residue on the surface of the bath water.
[0050] <Measurement of emulsion particle size> The emulsions of each sample immediately after emulsification (initial stage) were observed using a microscope (KEYENCE digital microscope VHX-8000; lenses used: RZ lens; dual-light high-magnification zoom lens: VH-Z250R / VH-Z250T), and the average particle size of the emulsion particles was measured three times. Here, particle size is the particle size observed by 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] <pH measurement> The pH of the emulsions of each example immediately after emulsification (initial stage) was measured with a pH meter.
[0052] The results of each test are shown in Tables 2 and 3. From the results of Tables 2 and 3, when containing cannabidiol, 20 to 30% by mass of an oil agent, and a surfactant, compared with the case of containing cannabidiol and 19% by mass of an oil agent, the gene expression level of IL-1β was high, and it was excellent in the feeling of use when used as a bath agent, the stability of the emulsion, and the ease of use as a bath agent. Further, when the surfactant was polyglycerol fatty acid ester, compared with the case where the surfactant was not polyglycerol fatty acid ester (Comparative Example 2), the inhibitory effect on the gene expression level of IL-1β was high, and it was excellent in the feeling of use when used as a bath agent, the stability of the emulsion, and the ease of use as a bath agent. In Comparative Example 2, the oil phase and the aqueous phase were separated and no emulsion was obtained, and the average emulsified particle diameter and pH could not be measured. Therefore, the emulsion according to the present invention is excellent in the gene expression inhibitory effect of cannabidiol on IL-1β, and thus is excellent not only in the anti-inflammatory effect, the preventive and / or improving effect of rough skin, the moisturizing effect of the skin, and the skin care effect, but also in the feeling of use when used as a bath agent, the stability of the emulsion, and the ease of use as a bath agent.
[0053] [Table 2]
[0054] [Table 3]
[0055] As is clear from the above test results, according to the present invention, there is an excellent skin care effect, and an emulsion with an excellent feeling of use, stability, and usability can be provided.
[0056] <Formulation Examples 1 to 8> A bath additive, which is an oil-in-water emulsion, was manufactured according to the composition shown in Table 4 below. Specifically, the aqueous phase component and the oil phase component were prepared and emulsified at a predetermined temperature. The bath additive obtained using the following formulation example has high skincare effects, as well as excellent usability, stability, and ease of use.
[0057] [Table 4]
Claims
1. (a) Cannabidiol, (b) an emulsion containing 20-30% by mass of an oil, and (c) a surfactant.
2. (c) The emulsion according to claim 1, characterized in that component is a polyglycerol fatty acid ester.
3. Furthermore, the emulsion according to claim 1, characterized in that it contains (d) a polyhydric alcohol.
4. Furthermore, the emulsion according to claim 1, characterized in that it contains (e) a fragrance.
5. (c) The emulsion according to claim 1, characterized in that the component is at least one selected from polyglyceryl diisostearate and polyglyceryl laurate.
6. The emulsion according to claim 1, characterized in that it is a topical skin preparation.
7. The emulsion according to claim 1, characterized in that it is an oil-in-water emulsion.