Edema ameliorating agent and cosmetic

Abstract

One form of the edema-improving agent disclosed herein contains 1-(2-hydroxyethyl)-2-imidazolinone or a derivative thereof as an active ingredient.

Description

Technical Field

[0001] This invention relates to edema-improving agents and cosmetics. Background Technology

[0002] The vascular system of the skin, located in the dermis, consists of blood vessels and lymphatic vessels. To maintain homeostasis, tissue fluid that has left the blood vessels must return to the veins. Veins in the skin effectively transport blood to the central nervous system. However, veins themselves have a poor capacity to absorb tissue fluid. Therefore, it is understandable that lymphatic vessels, which absorb tissue fluid, are also essential structures in the skin.

[0003] Lymphatic vessels play a vital role in maintaining a homeostatic microenvironment around cells by recycling waste products present in the skin, as well as water and proteins that continuously leak from blood vessels. The condition where water and other substances that have leaked out of blood vessels cannot be effectively recycled back into veins or lymph, and instead accumulate excessively between cells, is commonly known as "edema."

[0004] For example, facial swelling upon waking and leg swelling when fatigued are not only detrimental to health but also a major enemy of beauty. Furthermore, if this swelling is left untreated, surrounding blood vessels can be compressed, causing the swelling to progress and sometimes leading to pathological edema.

[0005] Previously, methods to eliminate edema included improving blood and lymph circulation through massage, which helped to drain excess water. In addition, pharmaceuticals and plant extracts are considered effective in improving edema. For example, the following have been disclosed: an edema improver with α-glucosylrutin as the active ingredient (see Patent Document 1); an edema improver with α-glucosylhesperidin as the active ingredient (see Patent Document 2); an edema improver with Poria cocos as the active ingredient (see Patent Document 3); a skin edema improver containing one or more of the following: extracts selected from Bupleurum plants, Coix plants, Zea plants, and whey extracts (see Patent Document 4); and a blend containing Acorus scabra (Acorus Scalamus L., Acorus gramineus Soland, etc.), Hamamelis virginiana L., etc., Citrus aurantium citrus (Citrus aurantium var. citrus), etc. The technology comprises one or more extracts of plants from the genera Zanthoxylum (Zanthoxylum piperitum mL. DC., etc.), Carica (Carica papaya L., etc.), Vitis (Vitis vinifera L., etc.), Thymus (Thymus serpyllum L., etc.), Pinus (Pinus sylvestris L., etc.), and Salvia (Salviasplendens Sellow, etc.) as edema-improving agents (see Patent Document 5), etc.

[0006] However, despite many such attempts, the effect on improving edema is not very satisfactory, and there is an urgent need to provide edema-improving agents that can more effectively improve edema.

[0007] <Prior art documents> <Patent Documents> Patent Document 1: Japanese Patent Application Publication No. 10-182468 Patent Document 2: Japanese Patent Application Publication No. 10-218777 Patent Document 3: Japanese Patent Application Publication No. 2000-239138 Patent Document 4: Japanese Patent Application Publication No. 2003-14739 Patent Document 5: Japanese Patent Application Publication No. 2004-35425 Summary of the Invention <Problem to be solved by this invention> In view of the above, one objective of the present invention is to provide an edema-improving agent with excellent edema-improving effects.

[0008] <Methods for solving problems> To address the aforementioned issues, one aspect of the edema-improving agent according to the present invention is characterized by containing 1-(2-hydroxyethyl)-2-imidazolinone or a derivative thereof as an active ingredient.

[0009] <The Effects of the Invention> According to one aspect of the present invention, an edema-improving agent with excellent edema-improving effects can be provided. Attached Figure Description

[0010] Figure 1 This is a graph illustrating gravitational expansion when evaluating the edema-improving effect of an edema-improving agent according to one embodiment.

[0011] Figure 2 This is a diagram illustrating the gravity indentation used to evaluate the edema-improving effect of an edema-improving agent according to one embodiment.

[0012] Figure 3A This is a schematic diagram illustrating a pair of left and right face photographs from Experiment Example 1.

[0013] Figure 3B This is a graph showing the results of the visual sensory assessment in Experiment Example 1. The vertical axis represents the results of the visual sensory assessment, and the horizontal axis represents the period in which the visual sensory assessment was conducted.

[0014] Figure 4 This is a graph showing the change in facial edema (Sc) from week 0 to week 6 of the experiment in Example 1. The vertical axis represents the improvement in edema (Sc) (cc), and the horizontal axis represents the experiment period (weeks). Detailed Implementation

[0015] The embodiments of the present invention are described in detail below. It should be noted that the embodiments are not limited to the following description and can be appropriately modified without departing from the spirit of the invention. Furthermore, in this specification, unless otherwise stated, the "~" indicating a numerical range means that the values ​​before and after it are included as the lower and upper limits.

[0016] (Edema-reducing agent) One embodiment of the edema-improving agent contains 1-(2-hydroxyethyl)-2-imidazolinone or a derivative thereof as an active ingredient, and may also contain other ingredients as needed.

[0017] Edema refers to a condition in which water leaks from the blood vessels and accumulates abnormally in the skin or subcutaneous tissues due to various reasons. Edema is also known as swelling.

[0018] There are no particular limitations on the method for confirming the edema-improving effect of the edema-improving agent involved in one embodiment, and it can be appropriately selected according to the purpose. For example, by sensory evaluation, when edema can be clearly felt to be improved after using the edema-improving agent compared with before or without using the edema-improving agent, it can be determined that the edema-improving agent has an edema-improving effect.

[0019] Alternatively, the method of using finger pressure to confirm the presence of edema, particularly in the feet, can be used as previously employed. Specifically, before or without applying an edema-improving agent, press the skin of the target area with your fingertips for 5 seconds and measure the time it takes for the skin to return to its original state after releasing your fingers (hereinafter, "T0"). Then, after applying the edema-improving agent, press the same target area with your fingertips for 5 seconds and measure the time it takes for the skin to return to its original state after releasing your fingers (hereinafter, "T1"). When T1 is shorter than T0, i.e., (T1-T0) is a positive value, it can be determined that the edema-improving agent has an effect on reducing edema.

[0020] Furthermore, when confirming facial edema, the improvement effect can also be confirmed through the following quantitative method. Specifically, before or without using the edema-improving agent, data representing the three-dimensional shape of the subject's face (hereinafter, sometimes referred to as "three-dimensional shape facial images") are captured using a known three-dimensional imaging device. Three-dimensional shape facial images are obtained when the subject's face is in a horizontal position (specifically, when the midline of the face is perpendicular to the direction of gravity and at rest) and in a vertical position (specifically, when the midline of the face is parallel to the direction of gravity and at rest). Then, using a computer, based on the change in three-dimensional shape between the three-dimensional shape images of the subject's face in the horizontal and vertical positions, the following gravitational expansion (VCswelling) and gravitational depression (VCshrinking) are calculated. Next, based on the gravitational expansion (VCswelling) and gravitational depression (VCshrinking), the following facial edema amount (Sc) is calculated. Similarly, after applying the edema-improving agent to the test subjects, the gravitational expansion (VCswelling), gravitational depression (VCshrinking), and facial edema (Sc) were calculated from data representing the three-dimensional shape of the test subjects' faces. Then, by comparing the facial edema (Sc) before or without using the edema-improving agent with the facial edema (Sc) after using the edema-improving agent, it can be determined that the edema-improving agent has an edema-improving effect.

[0021] -Calculation of gravitational expansion (VCswelling)- Figure 1 This is a diagram illustrating gravitational expansion according to an embodiment of the present invention. When acquiring three-dimensional images of the subject's face in a horizontal position and three-dimensional images of the subject's face in a vertical position, and comparing the three-dimensional shapes in the horizontal and vertical positions, then... Figure 1 The area within the dotted line has a larger volume in the vertical position. Therefore, by comparing the three-dimensional shape of the test subject in the horizontal position with that in the vertical position, the difference in volume between the two (i.e., horizontal and vertical positions) of the area with the larger volume in the vertical position is taken as the gravitational expansion (VCswelling).

[0022] -Calculation of gravity-induced indentation (VCshrinking)- Figure 2 This is a diagram illustrating a gravity depression according to an embodiment of the present invention. When a three-dimensional image of the subject's face in a horizontal position and a three-dimensional image of the subject's face in a vertical position are acquired, and the three-dimensional shape in the horizontal position is compared with the three-dimensional shape in the vertical position, then... Figure 2 The area within the dotted line has a smaller volume in the vertical position. Therefore, the difference in volume between the smaller area in the vertical position and the horizontal position is taken as the gravitational indentation (VCshrinking).

[0023] -Calculation of facial edema (Sc)- The amount of facial edema (Sc) can be calculated using the following formula (1).

[0024] [Number 1] (In Equation (1), “Sc” represents the amount of facial edema, “VCswelling” represents the amount of gravitational expansion, and “VCshrinking” represents the amount of gravitational depression.) When the amount of facial edema before or without using the edema improver is set as "Sc0", and the amount of facial edema after using the edema improver is set as "Sc1", the improvement in facial edema (Sc) can be calculated according to the following formula (2). When the improvement in facial edema (Sc) is positive, it can be confirmed that the edema improver has an edema-improving effect. In addition, the larger the value of the improvement in edema (Sc), the better the edema-improving effect brought about by the edema improver. In addition, the edema-improving effect of the edema improver on edema can also be confirmed by using the method described in the test examples described later.

[0025] Improvement in facial edema (Sc) = Sc0 - Sc1 ... Equation (2) <1-(2-hydroxyethyl)-2-imidazolinone or its derivatives> As for 1-(2-hydroxyethyl)-2-imidazolinone (hereinafter, sometimes referred to as "HEI") or its derivatives, there are no particular restrictions as long as they have the effect of improving edema, and they can be appropriately selected according to the purpose. The cyclic carboxamide derivatives or their salts shown in the following general formula (1) are preferred.

[0026] [Chemistry 1] (wherein, in the above general formula (1), n ​​represents an integer from 1 to 3, R) 1 X represents a hydrogen atom or a hydrocarbon group having 1 to 6 carbon atoms, optionally substituted with a hydroxyl group; X represents -CH2- or a hydrocarbon group consisting of -N(R) 2 )- represents the group, R 2 (This represents a hydrogen atom or a hydrocarbon group having 1 to 6 carbon atoms, optionally replaced by a hydroxyl group.) In general formula (1), n ​​is an integer from 1 to 3, preferably an integer from 1 to 2, and more preferably an integer of 1.

[0027] In general formula (1), when R1 When the hydrocarbon group is optionally substituted with a hydroxyl group and has 1 to 6 carbon atoms, the number of carbon atoms in the hydrocarbon group is preferably 1 to 4, more preferably 1 to 3, and even more preferably 2.

[0028] In the above general formula (1), when X is derived from -N(R) 2 When R represents a group, )- 2 It is a hydrogen atom or a hydrocarbon group having 1 to 6 carbon atoms, optionally substituted with a hydroxyl group, preferably a hydrogen atom.

[0029] Among the cyclic carboxamide derivatives shown in the above general formula (1), the compound shown in the following structural formula (1) is 1-(2-hydroxyethyl)-2-imidazolinone.

[0030] [Chemistry 2] The derivatives of 1-(2-hydroxyethyl)-2-imidazolinone are compounds other than those shown in the above-described structural formula (1) among the cyclic carboxamide derivatives of the above general formula (1). As a derivative of 1-(2-hydroxyethyl)-2-imidazolinone, there are no particular limitations as long as it has the effect of improving edema, and it can be appropriately selected according to the purpose. Preferably, it is the compound 2-imidazolinone shown in the following structural formula (2) or the compound 1-(2-hydroxyethyl)-2-pyrrolidone shown in the following structural formula (3).

[0031] [Chemistry 3] [Chemistry 4] There are no particular restrictions on the salts of the cyclic carboxamide derivatives shown in the above general formula (1), which can be either inorganic or organic salts.

[0032] As inorganic salts, there are no particular restrictions, and they can be selected appropriately according to the purpose. Examples include hydrochloride, sulfate, phosphate, hydrobromide, sodium salt, potassium salt, magnesium salt, calcium salt, and ammonium salt.

[0033] As organic salts, there are no particular restrictions, and appropriate selection can be made according to the purpose. Examples include acetates, lactates, maleates, fumarates, tartrates, citrates, methanesulfonates, p-toluenesulfonates, triethanolamine salts, diethanolamine salts, and amino acid salts.

[0034] In one embodiment of the edema-improving agent, 1-(2-hydroxyethyl)-2-imidazolinone or a derivative thereof may be used alone or in combination with one of the cyclic carboxamide derivatives or salts thereof shown in general formula (1).

[0035] 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives may be products that are suitably synthesized by known methods or commercially available products.

[0036] The content of 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives in the edema-improving agent according to one embodiment is not particularly limited as long as it is sufficient to effectively improve edema, and can be appropriately selected according to the purpose. Relative to the total mass of the edema-improving agent, it is preferably 0.0001% by mass or more, more preferably 0.001% by mass or more, further preferably 0.01% by mass or more, even more preferably 0.1% by mass or more, and particularly preferably 1% by mass or more. The upper limit of the content of 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives in the edema-improving agent according to one embodiment is not particularly limited as long as it is sufficient to effectively improve edema, and can be appropriately selected according to the purpose. Relative to the total mass of the edema-improving agent, it is preferably 5% by mass or less, more preferably 4% by mass or less, further preferably 3% by mass or less, even more preferably 2% by mass or less, and particularly preferably 1.5% by mass or less. The lower and upper limits of the content of 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives in the edema-improving agent according to one embodiment can be appropriately combined. Relative to the total mass of the edema-improving agent, it is preferably 0.0001% to 5% by mass, more preferably 0.001% to 4% by mass, further preferably 0.01% to 3% by mass, even more preferably 0.1% to 2% by mass, and particularly preferably 1% to 1.5% by mass. It should be noted that when the edema-improving agent according to one embodiment contains two or more selected from 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives, the content of 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives refers to the total content of the two or more 1-(2-hydroxyethyl)-2-imidazolinone or their derivatives.

[0037] <Other Ingredients> For an edema-improving agent according to one embodiment, it may contain other ingredients besides 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives, as long as the edema-improving effect is not impaired. Examples of other ingredients include pharmaceutically acceptable carriers or excipients such as diluents, binders, disintegrants, thickeners, dispersants, reabsorption promoters, flavoring agents, buffers, surfactants, solubilizers, preservatives, emulsifiers, isotonic agents, stabilizers, and pH adjusters. These may be used alone or in combination of two or more.

[0038] The content of other components in the edema-improving agent involved in one embodiment is not particularly limited, as long as it does not impair the edema-improving effect, and can be appropriately selected according to the purpose. It should be noted that the edema-improving agent involved in one embodiment may consist only of 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives.

[0039] [Administration method and dosage] As one embodiment, the usage and dosage of the edema-improving agent are not particularly limited as long as they can improve edema, and can be appropriately selected according to the purpose. As for the method of administration, examples include local administration, oral administration, and non-oral administration (e.g., intravenous administration, intraperitoneal administration, etc.), etc., with local administration being preferred, and application to the skin being more preferred.

[0040] One embodiment of the edema-improving agent preferably improves edema by applying it to the skin. There are no particular limitations on the method and dosage when applying it to the skin; appropriate choices can be made based on the dosage form, the age, weight, and state of edema of the target individual. As for the method of application, it is preferred to apply it several times a day, more preferably once to five times. It can be applied directly to the skin or soaked in a substrate such as gauze before being applied to the skin. As for the dosage, it is preferred to apply it per 1 cm... 2 0.001 mL to 1 mL for skin.

[0041] [Dosage Form] The dosage form of the edema-improving agent involved in one embodiment is not particularly limited and can be appropriately selected according to the purpose. When used as a topical skin agent for local administration, examples include solutions, soluble forms, emulsions, powder dispersions, water-oil two-layer forms, water-oil-powder three-layer forms, ointments, creams, lotions, lotions, gels, and aerosols. Additionally, patches can be made by impregnating these dosage forms in a substrate. Furthermore, when used orally, examples include solid dosage forms such as tablets, coated tablets, sugar-coated tablets, granules, powders, and capsules (e.g., hard and soft gelatin capsules); and liquid dosage forms (solutions, suspensions) such as oral liquids and syrups. When used non-oral, examples include injections.

[0042] [Manufacturing Method] There are no particular limitations on the method for manufacturing the edema-improving agent involved in one embodiment. It can be manufactured by a method appropriately selected from known methods, depending on the dosage form.

[0043] It should be noted that the use of 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives for the improvement of edema, and the use of 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives in the manufacture of edema improvers are also included within the scope of this disclosure.

[0044] (cosmetic) One embodiment of the cosmetic contains the edema-improving agent of one embodiment, and may also contain other ingredients as needed.

[0045] <Edema Relief Agent> One embodiment of the cosmetic contains an edema-improving agent as described in the above-mentioned (edema-improving agent) item.

[0046] As one implementation method, the content of the edema-improving agent in the cosmetic is not particularly limited as long as it can improve edema, and can be appropriately selected according to the purpose.

[0047] <Other Ingredients> One embodiment of the cosmetic may contain ingredients other than edema-reducing agents. There are no particular limitations on these other ingredients; they can be appropriately selected from commonly compounded ingredients in cosmetics, depending on the cosmetic's form, etc. Examples include glycols, glycerin derivatives, sugar alcohols, sugars, oils, polymers, surfactants, powders, coloring materials, solvents, silicones, fragrances, pharmaceuticals or active ingredients other than edema-reducing agents, pH adjusters, metal ion blocking agents, etc. They can be used individually or in combination of two or more.

[0048] Diols Examples of glycols include propylene glycol, dipropylene glycol, 1,3-butanediol, 1,4-butanediol, diethylene glycol, triethylene glycol, and polyethylene glycol.

[0049] <<glycerin>> Examples of glycerol derivatives include glycerol, diglycerol, and polyglycerol.

[0050] <<Sugar alcohols>> Examples of sugar alcohols include sorbitol, mannitol, maltitol, xylitol, and erythritol.

[0051] <<Carbohydrates>> Examples of sugars include fructose, glucose, galactose, maltose, lactose, and trehalose.

[0052] <<Oil content>> Examples of oils include fats and greases, waxes, hydrocarbon oils, higher fatty acids, higher alcohols, ester oils, silicone oils, and oil-soluble pharmaceuticals. They can be used individually or in combination of two or more.

[0053] -Fats- Examples of oils and fats include avocado oil, camellia seed oil, turtle oil, macadamia nut oil, corn oil, mink oil, olive oil, rapeseed oil, sesame oil, almond oil, wheat germ oil, camellia oil, castor oil, flaxseed oil, safflower oil, cottonseed oil, perilla oil, soybean oil, peanut oil, tea seed oil, torreya seed oil, rice bran oil, Chinese tung oil, Japanese tung oil, jojoba seed oil, wheat germ oil, cocoa butter, coconut oil, hydrogenated coconut oil, palm oil, palm kernel oil, and wild lacquer fruit wax kernel oil, among other plant-based oils; and egg yolk oil, horse oil, beef tallow, mutton tallow, hydrogenated beef tallow, lard, beef bone oil, and beef foot oil, among other animal-based oils.

[0054] -Waxes- Examples of waxes include lacquer wax, beeswax, candelilla wax, cotton wax, carnauba wax, laurel wax, white wax, whale wax, lignite wax, rice bran wax, lanolin, kapok wax, lanolin acetate, liquid lanolin, sugarcane wax, isopropyl lanolinate, hexyl laurate, reduced lanolin, jojoba wax, hard lanolin, and shellac wax.

[0055] -hydrocarbon oil- Examples of hydrocarbon oils include linear, branched, or volatile hydrocarbon oils. Specific examples of hydrocarbon oils include liquid paraffin, squalane, isoalkanes, α-olefin oligomers, polybutene, microcrystalline wax, and hydrogenated polydecene.

[0056] -Higher fatty acids- Examples of high-grade fatty acids include lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, 12-hydroxystearic acid, undecenoic acid, lanolin fatty acids, isostearic acid, linoleic acid, linolenic acid, and eicosapentaenoic acid.

[0057] -Higher alcohols- Examples of higher alcohols include alcohols with 6 or more carbon atoms. Specific examples of higher alcohols include lauryl alcohol, cetyl alcohol, stearyl alcohol, behenyl alcohol, myristyl alcohol, oleyl alcohol, cetearyl alcohol, monostearate glyceryl ether (squalyl alcohol), 2-decyltetradecyl alcohol, 2-octyldodecyl alcohol, lanolin alcohol, cholesterol, phytosterol, hexyldodecyl alcohol, isostearyl alcohol, octyldodecyl alcohol, and other straight-chain or branched higher alcohols.

[0058] -Ester oil- Examples of ester oils include triisooctanoic acid glyceride, triisopalmitoic acid glyceride, octyl isopalmitate, isostearate isostearate, isostearyl isostearate, isocetyl isostearate, hexyl isostearate, myristyl isostearate, isocetyl octanoate, isocetyl isooctanoate, isostearyl octanoate, isodecanyl isononanoate, octyldodecyl dimethyl octanoate, oleyl myristate, isostearyl erucate, isocetyl stearate, octyl stearate, isostearyl palmitate, isocetyl palmitate, palmitate, etc. Octyl myristate, isostearyl myristate, isocetyl myristate, octyl dodecyl myristate, decyl myristate, isopropyl palmitate, isopropyl myristate, trimethylolpropane triisostearate, neopentyl glycol didecanoate, dioctyl sebacate, octyl lauryl 12-stearoyloxystearate, dioctyl dodecyl stearoyl glutamate, dioctyl adipate, diisostearyl malate, octyl methoxycinnamate, octyl dodecyl lactate, isostearyl lactate, octyl p-dimethylaminobenzoate, etc.

[0059] -Silicone oil- Examples of silicone oils include volatile cyclic silicones, volatile dimethyl polysiloxanes, and methylphenyl silicones.

[0060] Oil-soluble drugs- Examples of fat-soluble pharmaceutical agents include vitamin A, retinol, retinyl acetate, retinyl palmitate, benzyl nicotinate, dl-α-tocopherol nicotinate, vitamin D2, and tocopherol.

[0061] <<Polymers>> Examples of polymers include plant-based polymers, animal-based polymers, microbial polymers, starch-based polymers, cellulose-based polymers, alginate-based polymers, ethylene-based polymers, acrylic acid-based polymers, and inorganic water-soluble polymers. These polymers can be used as thickeners.

[0062] Examples of plant-based polymers include gum arabic, astragalus gum, galactomannan, guar gum, carob gum, erythrina gum, gellan gum, carrageenan, pectin, and agar.

[0063] Examples of animal-based macromolecules include collagen, casein, albumin, and gelatin.

[0064] Examples of microbial macromolecules include xanthan gum, dextran, succinyl dextran, and pullulan.

[0065] Examples of starch-based macromolecules include plant-based starches such as corn, wheat, potato, and rice; carboxymethyl starch; and methyl hydroxypropyl starch.

[0066] Examples of cellulose-based polymers include methylcellulose, nitrocellulose, ethylcellulose, methyl hydroxypropylcellulose, hydroxyethylcellulose, sodium cellulose sulfate, hydroxypropylcellulose, sodium carboxymethyl cellulose, and crystalline cellulose.

[0067] Examples of alginate polymers include sodium alginate and propylene glycol alginate.

[0068] Examples of ethylene-based polymers include polyvinyl alcohol, polyvinyl acetate, polyvinyl methyl ether, polyvinylpyrrolidone, copolymers of vinylpyrrolidone and vinyl acetate, and polycarboxyethylene.

[0069] Examples of acrylic polymers include sodium polyacrylate, ethyl polyacrylate, alkanolamine polyacrylate, copolymers of alkyl methacrylate and dimethylaminoethyl methacrylate, poly(2-acrylamido-2-methylpropanesulfonic acid), and poly(methacryloyloxytrimethylammonium).

[0070] Examples of inorganic water-soluble polymers include polyethyleneimine, cationic polymers, bentonite, magnesium aluminum silicate, lithium saponite, hydropyrite, and silicic anhydride.

[0071] <<Surfactants>> Examples of surfactants include anionic surfactants, cationic surfactants, nonionic surfactants, and amphoteric surfactants.

[0072] Examples of anionic surfactants include: fatty acid soaps such as soap base, sodium lauryl sulfate, and sodium palmitate; higher alkyl sulfate salts such as sodium lauryl sulfate and potassium lauryl sulfate; alkyl ether sulfate salts such as polyoxyethylene (hereinafter, sometimes simply "POE") lauryl sulfate triethanolamine and POE lauryl sulfate sodium; N-acyl sarcosine salts such as lauroyl sarcosine sodium; higher fatty acid amide sulfonates such as N-myristoyl-N-methyl taurate sodium and coconut oil fatty acid methyl taurate sodium; phosphate salts such as POE stearyl ether phosphate sodium; and monolauroyl monoethanolamide POE sulfosuccinate. Sulfosuccinates such as sodium lauryl polypropylene glycol sulfosuccinate; alkylbenzene sulfonates such as sodium linear dodecylbenzene sulfonate and triethanolamine linear dodecylbenzene sulfonate; N-acylglutamate salts such as disodium N-stearoylglutamate and monosodium N-stearoylglutamate; higher fatty acid ester sulfates such as sodium hydrogenated coconut oil fatty acid glycerol sulfate; sulfated oils such as Turkish red oil; POE alkyl ether carboxylates and POE alkyl allyl ether carboxylates; higher fatty acid ester sulfonates; secondary alcohol sulfates; higher fatty acid alkanolamide sulfates; sodium lauroyl monoethanolamide succinate; sodium casein, etc.

[0073] Examples of cationic surfactants include alkyl trimethylammonium salts such as stearyltrimethylammonium chloride and lauryltrimethylammonium chloride; dialkyl dimethylammonium salts such as distearate dimethylammonium chloride; alkyl pyridinium salts such as cetylpyridinium chloride; alkyl quaternary ammonium salts; alkyl dimethyl benzyl ammonium salts; alkyl isoquinoline onion salts; dialkyl morpholine onion salts; POE alkylamines; alkylamine salts; polyamine fatty acid derivatives; pentanol fatty acid derivatives; benzalkonium chloride, etc.

[0074] Examples of nonionic surfactants include lipophilic and hydrophilic nonionic surfactants. Examples of lipophilic nonionic surfactants include sorbitan fatty acid esters such as sorbitan monooleate, sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, and sorbitan trioleate; glycerol polyglycerol fatty acids such as cottonseed oil fatty acid glycerides, glycerol monostearate, sesquioleic acid glycerides, and glycerol monostearate malate; propylene glycol fatty acid esters such as propylene glycol monostearate; glyceryl alkyl ethers; and POE-methylpolysiloxane copolymers. Examples of hydrophilic nonionic surfactants include POE sorbitan monooleate, POE sorbitan monostearate, and other POE sorbitan fatty acid esters; POE sorbitan monolaurate, POE sorbitan monooleate, POE sorbitan monostearate, and other POE sorbitan fatty acid esters; POE monooleate, POE distearate, POE monodioleate, and other POE fatty acid esters; POE lauryl ether, POE oleyl ether, POE cholesterol ester, and other POE octyl ether. POE alkylphenyl ethers such as POE nonylphenyl ether; POE·polyoxypropylene (hereinafter sometimes referred to as "POP") monobutyl ether, POE·POP cetyl ether, POE·POP glyceryl ether and other POE·POP alkyl ethers; POE beeswax·lanolin derivatives such as POE sorbitan beeswax; alkylolamides such as coconut oil fatty acid diethanolamide and fatty acid isopropanolamide; POE propylene glycol fatty acid esters; POE fatty acid amides and POE alkylamines; sucrose fatty acid esters and alkylethoxydimethylamine oxides, etc.

[0075] Examples of amphoteric surfactants include imidazoline-based amphoteric surfactants such as 2-cocoyl-2-imidazolineonium hydroxide-1-carboxyethoxy disodium salt; and betaine surfactants such as amide betaine and sulfobetaine.

[0076] <<Powder>> The powder can be inorganic or organic.

[0077] Examples of inorganic powder components include mica, talc, kaolin, sericite, muscovite, phlogopite, synthetic mica, red mica, biotite, lepidolite, synthetic mica, silicic anhydride (silicon dioxide), aluminum silicate, barium silicate, calcium silicate, magnesium silicate, strontium silicate, aluminum oxide, barium sulfate, zeolite, titanium oxide, zinc oxide, and boron nitride.

[0078] Examples of organic powders include polyamide resin powder (nylon powder), polyethylene powder, polymethyl methacrylate powder, polystyrene powder, calcium carbonate powder, magnesium carbonate powder, copolymer resin powder of styrene and acrylic acid, cellulose powder, etc.

[0079] <<Coloring Materials>> Examples of coloring materials include pigments and dyes.

[0080] -pigment- Examples of pigments include inorganic pigments, organic pigments, pearl pigments, and metallic powder pigments.

[0081] Examples of inorganic pigments include titanium dioxide, zinc oxide and other inorganic white pigments; iron oxide (iron red) and other inorganic red pigments; yellow iron oxide, yellow ochre and other inorganic yellow pigments; black iron oxide, carbon black and other black pigments; chromium oxide, chromium hydroxide, cobalt titanate and other inorganic green pigments; and ultramarine blue, iron blue and other inorganic blue pigments.

[0082] Examples of organic pigments include Red No. 3, Red No. 104, Red No. 106, Red No. 201, Red No. 202, Red No. 204, Red No. 205, Red No. 220, Red No. 226, Red No. 227, Red No. 228, Red No. 230, Red No. 401, Red No. 405, Red No. 505, Orange No. 203, Orange No. 204, Orange No. 205, Yellow No. 4, Yellow No. 5, Yellow No. 202, Yellow No. 203, Yellow No. 205, Yellow No. 401, Blue No. 1, Blue No. 404, Green No. 3, and their zirconium lakes, barium lakes, or aluminum lakes.

[0083] Examples of pearl pigments include titanium dioxide-coated mica, colored titanium dioxide-coated mica, bismuth oxychloride, and fish scale foil.

[0084] Examples of metallic powder pigments include aluminum powder and copper powder.

[0085] -pigment- Examples of pigments include natural pigments such as chlorophyll and beta-carotene.

[0086] <<Solvent>> Examples of solvents include water and lower alcohols. Examples of lower alcohols include alcohols with 5 or fewer carbon atoms. Specific examples of lower alcohols include methanol, ethanol, propanol, isopropanol, 2-amino-2-methyl-1-propanol, and 2-amino-2-methyl-1,3-propanediol.

[0087] Silicones As silicones, there are no particular restrictions, and appropriate choices can be made according to the purpose. Examples include chain silicones, cyclic silicones, and modified silicones.

[0088] Examples of chain-like silicones include polydimethylsiloxane (dimethyl silicone oil), polymethylphenylsiloxane (phenylmethyl silicone oil), and polymethylhydrosiloxane.

[0089] Examples of cyclic silicones include octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, and dodecylcyclohexasiloxane.

[0090] Examples of modified silicones include amino-modified silicone oils, polyether-modified silicone oils, carboxyl-modified silicone oils, alkyl-modified silicone oils, ammonium salt-modified silicone oils, and fluorine-modified silicone oils.

[0091] These silicones can be used alone or in combination of two or more.

[0092] <<Drugs or active ingredients>> As a pharmaceutical agent, there are no particular restrictions on any agent or active ingredient other than edema-reducing agents. Examples include vitamins, ultraviolet absorbers, chelating agents, preservatives, plant extracts, moisturizers, anti-inflammatory agents, whitening agents, cooling agents, amino acids, antioxidants, bactericides, and various skin nutrients.

[0093] -Vitamins- Examples of vitamins include water-soluble vitamins such as vitamin B6 hydrochloride, panthenol ether, pyridoxine hydrochloride, nicotinamide, pantothenic acid, and biotin.

[0094] -UV absorber- Examples of UV absorbers include benzoic acid UV absorbers such as p-aminobenzoic acid; anthranilic acid UV absorbers such as methyl anthranilate; salicylic acid UV absorbers such as octyl salicylate; cinnamic acid UV absorbers such as isopropyl p-methoxycinnamate and octyl p-methoxycinnamate; UV absorbers such as urocanthioneic acid and ethyl urocanthione; benzophenone UV absorbers such as 2-hydroxy-4-methoxybenzophenone and dihydroxybenzophenone; benzotriazole UV absorbers; and 2-phenylbenzimidazole-5-sulfonic acid.

[0095] -chelating agent- As chelating agents, for example, citramalic acid, agaric acid, glyceric acid, shikimic acid, hinokitiol, gallic acid, tannic acid, caffeic acid, disodium ethylenediamine-N,N,N′,N′-tetraacetate dihydrate (EDTA-2Na-2H2O), ethylene glycol bis(2-aminoethylether)-N,N,N′,N′-tetraacetic acid, diethylenetriaminepentaacetic acid, phytic acid, polyphosphoric acid, metaphosphoric acid, their analogs, their alkali metal salts, their carboxylic acid esters, etc. can be cited.

[0096] - Preservative - As preservatives, for example, benzoic acid, salicylic acid, p-hydroxybenzoates (methyl p-hydroxybenzoate, ethyl p-hydroxybenzoate, butyl p-hydroxybenzoate, etc.), sorbic acid, parachlorometacresol, hexachlorophene, benzalkonium chloride, chlorhexidine hydrochloride, triclocarban, photosensitizers, phenoxyethanol, chlorphenesin, etc. can be cited.

[0097] - Plant extract - As plant extracts, for example, houttuynia cordata extract, phellodendron bark extract, licorice extract, peony extract, tree peony extract, towel gourd extract, saxifrage extract, eucalyptus globulus leaf extract, clove extract, aesculus hippocastanum extract, cornflower extract, seaweed extract, thyme extract, etc. can be cited. These plant extracts may contain caffeine, tannic acid, etc.

[0098] - Humectant - As humectants, for example, polyethylene glycol (hereinafter sometimes simply referred to as "PEG"), sodium chondroitin sulfate, sodium hyaluronate, sodium lactate, glucosamine, cyclodextrin, etc. can be cited. In addition, the above-mentioned glycols, the above-mentioned glycerols, the above-mentioned sugar alcohols, and the above-mentioned saccharides can also be used as humectants.

[0099] - Anti-inflammatory agent - As anti-inflammatory agents, for example, sodium glycyrrhetinic acid, liquiritigenin, lysozyme hydrochloride, pyridoxine hydrochloride, sulfur, etc. can be cited.

[0100] - Whitening agent - As whitening agents, for example, arbutin, 4-methoxysalicylic acid, tranexamic acid, vitamin C, ethyl vitamin C, magnesium ascorbyl phosphate, glucosyl ascorbate, kojic acid, etc. can be cited.

[0101] - Cooling agent - As cooling agents, for example, L-menthol, camphor, etc. can be cited.

[0102] - Antioxidant - As antioxidants, for example, ascorbic acid, α-tocopherol, carotenoids, etc. can be cited.

[0103] <<pH regulator>> Examples of pH adjusters include potassium hydroxide, sodium hydroxide, triethanolamine, sodium carbonate, lactic acid, citric acid, sodium citrate, glycolic acid, succinic acid, tartaric acid, malic acid, sodium bicarbonate, and ammonium bicarbonate.

[0104] <<Metal Ion Blocking Agents>> Examples of metal ion blocking agents include disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, and gluconic acid.

[0105] In a cosmetic product according to one embodiment, the content of other ingredients is not particularly limited, as long as it does not impair the effect of the cosmetic product according to one embodiment, and can be appropriately selected according to the purpose.

[0106] [use] The use of cosmetics involved in one implementation method is not particularly limited, and can be appropriately selected according to the purpose. Examples include toners, lotions, creams, serums, gels, ointments, face masks, foundations, etc.

[0107] Example The following examples, comparative examples, and test examples are provided to illustrate the implementation in more detail, but the implementation is not limited to these examples, comparative examples, and test examples. It should be noted that in the examples and comparative examples shown in Table 1 below, the mixing amount represents "mass%" relative to the total mass of the lotion.

[0108] (Example 1) The toners with the compositions and mixing amounts shown in Table 1 below were prepared using conventional methods.

[0109] (Comparative Example 1) The toners with the compositions and mixing amounts shown in Table 1 below were prepared using conventional methods.

[0110] [Table 1] (Experimental Example 1) Thirty-nine healthy Japanese women aged 20 to 60 years were instructed to apply 0.3 mL of the lotion from Example 1 to one side of their face twice a day, once in the morning and once in the evening. It should be noted that the allocation of the left and right sides of the face was randomized; 19 subjects applied the lotion from Example 1 to the right side of their facial midline, and 20 subjects applied it to the left side of their facial midline. The side of the face with the lotion from Example 1 applied was designated "Q side". Next, on the opposite side of the same subject's face (the side opposite to the side with the lotion from Example 1 applied), 0.3 mL of the lotion from Comparative Example 1 was applied twice a day, once in the morning and once in the evening. The opposite side of the same subject's face (the side opposite to the side with the lotion from Example 1 applied) means, for example, that for a subject who applied the lotion from Example 1 to the left side of their facial midline, the lotion from Comparative Example 1 was applied to the right side of their facial midline. The side of the face with the lotion from Comparative Example 1 applied was designated "P side". The toners of Example 1 and Comparative Example 1 were applied for 6 weeks. It should be noted that this was conducted without disclosing the composition of the toners of Example 1 and Comparative Example 1 to the subjects. Next, the following visual sensory assessments and quantitative evaluations were performed.

[0111] <Visual Sensory Judgment> For the half of the face that was coated with the toner of Example 1 (Q half of the face) and the half of the face that was coated with the toner of Comparative Example 1 (P half of the face), when the midline of the face was set as the front view, photos of the left and right sides of the face were taken using a digital camera at a 45-degree angle from the opposite front view. The left and right face photos were used as a group, and four professional evaluators performed visual sensory judgment on "which side of the face was swollen". Figure 3A This is a schematic diagram illustrating a set of left and right face photographs. It should be noted that the specific side of the face to which the toners of Example 1 and Comparative Example 1 were applied was not disclosed to professional evaluators, but a visual sensory judgment was performed under these conditions.

[0112] Judgments were performed before the first application of the toners of Example 1 and Comparative Example 1 (hereinafter referred to as "week 0"), and 3 weeks and 6 weeks after the application of the toners of Example 1 and Comparative Example 1. In each week's judgment, four professional evaluators performed five judgments. Judgments were based on the following evaluation criteria. The scores from each professional evaluator were assigned to the Q side of the face and the P side of the face, respectively. For each subject in each week's judgment, the average score 'a' of the five judgments by each professional evaluator was calculated. Then, the average score 'b' of the average score 'a' for each of the 39 subjects at week 0, week 3, and week 6 was calculated. Next, the average score 'c' of the average score 'b' from the four professional evaluators was calculated. Furthermore, the standard error of the average score 'b' was calculated.

[0113] -Judgment Criteria- Rating -1 point: Q - Half of the face shows visible swelling. Rating 1 point: P Half of the face shows visible swelling. The results are as follows Figure 3B As shown. In Figure 3B In the diagram, "*" indicates a significant difference (p=0.013) based on a pared-T test (two-tailed t-test) between the two sides of the face before application (week 0) and 6 weeks after application. Before application (week 0), there was no difference between the P and Q sides of the face. However, from 6 weeks after application, the P side appeared significantly more swollen, while the Q side did not appear swollen.

[0114] <Quantitative Evaluation> Before the first application of the lotions of Example 1 and Comparative Example 1 (week 0), and 3 weeks and 6 weeks after the application of the lotions of Example 1 and Comparative Example 1, data (three-dimensional shape facial images) showing the three-dimensional shape of the subjects' faces were captured using a 3D image imaging analysis device (VECTRA Handy H2 (VEC-H2, manufactured by Canfield Scientific)). At this time, three-dimensional shape facial images were obtained when the subjects' faces were in a horizontal position (specifically, when the midline of the face was perpendicular to the direction of gravity and at rest) and in a vertical position (specifically, when the midline of the face was parallel to the direction of gravity and at rest). Then, using a computer, based on the change in three-dimensional shape between the three-dimensional shape facial images when the subjects' faces were in a horizontal position and in a vertical position, the gravitational expansion (VCswelling) and gravitational depression (VCshrinking) were calculated for the half of the face (Q half) with the lotion of Example 1 applied (Q half) and the half of the face (P half) with the lotion of Comparative Example 1 applied (P half). Next, based on the gravitational expansion (VCswelling) and gravitational depression (VCshrinking), the following facial edema (Sc) was calculated.

[0115] -Calculation of facial edema (Sc)- Facial edema (Sc) was calculated using the following formula (1). It should be noted that for the acquisition of three-dimensional facial images, each subject was measured three times at 0 weeks, 3 weeks, and 6 weeks, and the average of these measurements was taken as the subject's facial edema (Sc).

[0116] [Number 2] (In Equation (1), “Sc” represents the amount of facial edema, “VCswelling” represents the amount of gravitational expansion, and “VCshrinking” represents the amount of gravitational depression.) Next, the improvement in facial edema (Sc) is calculated using the following formulas (3) and (4).

[0117] The difference in facial edema (Sc) between the left and right sides = [Q half of the face edema (Sc)] - [P half of the face edema (Sc)] ... Equation (3) Improvement in facial edema (Sc) = [Difference between left and right sides of facial edema (Sc) at week 0] - [Difference between left and right sides of facial edema (Sc) after n weeks] ... Equation (4) (where n = 3 or 6 in equation (4)) Figure 4 The figure shows a graph illustrating the change in the amount of facial edema (Sc) from week 0 to week 6 after the start of the test. Figure 4 In the figure, "*" indicates p<0.05. According to the results, the p values ​​after 0 and 6 weeks were less than 0.05, and the Q side of the face that was treated with the toner of Example 1 showed a significant improvement in edema (Sc) compared to the P side of the face that was treated with the toner of Comparative Example 1.

[0118] The results of Experiment 1 and Experiment 2 show that edema-improving agents containing 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives as active ingredients have excellent edema-improving effects.

[0119] As an example of the present invention, the following can be listed.

[0120] <1> An edema-improving agent, characterized in that it contains 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives as an active ingredient.

[0121] <2> According to the above <1> The edema-improving agent, wherein the 1-(2-hydroxyethyl)-2-imidazolinone or its derivative contains a cyclic carboxamide derivative or its salt as shown in general formula (1) as an active ingredient.

[0122] [Chemistry 5] (wherein, in the above general formula (1), n ​​represents an integer from 1 to 3, R) 1 X represents a hydrogen atom or a hydrocarbon group having 1 to 6 carbon atoms, optionally substituted with a hydroxyl group; X represents -CH2- or a hydrocarbon group consisting of -N(R) 2 )- represents the group, R 2 (This represents a hydrogen atom or a hydrocarbon group having 1 to 6 carbon atoms, optionally replaced by a hydroxyl group.) <3> According to the above <1> or <2> The edema-improving agent is a topical skin agent.

[0123] <4> A cosmetic product, characterized in that it contains the above-mentioned... <1> to <3> The edema-improving agent mentioned in any one of the following.

[0124] <5> 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives are used to improve edema.

[0125] <6> Application of 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives in the preparation of edema-improving agents.

[0126] As described above, the present invention has been illustrated based on specific embodiments and examples. However, these embodiments and examples are provided merely as examples, and the present invention is not limited to the above embodiments and examples. The above embodiments can be implemented in various other forms, and various combinations, omissions, substitutions, additions, modifications, etc., can be made without departing from the spirit of the invention. These embodiments or their variations are included in the scope and spirit of the invention, and are included within the scope equivalent to the invention described in the claims.

[0127] This international application claims priority to Japanese Patent Application No. 2023-220018, filed on December 26, 2023, which is incorporated herein by reference in its entirety.

Claims

1. An edema-improving agent, characterized in that, It contains 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives as active ingredients.

2. The edema-improving agent according to claim 1, wherein, The 1-(2-hydroxyethyl)-2-imidazolinone or its derivatives contain a cyclic carboxamide derivative or its salt as represented by the following general formula (1) as an active ingredient. In the general formula (1), n ​​represents an integer from 1 to 3, and R 1 X represents a hydrogen atom or a hydrocarbon group having 1 to 6 carbon atoms, optionally substituted with a hydroxyl group; X represents -CH2- or a hydrocarbon group consisting of -N(R) 2 )- represents the group, R 2 It represents a hydrogen atom or a hydrocarbon group having 1 to 6 carbon atoms that may be optionally replaced by a hydroxyl group.

3. The edema-improving agent according to claim 1 is a topical skin agent.

4. A cosmetic product, characterized in that, It contains the edema-improving agent as described in claim 1.