Topical preparation for skin
A topical skin preparation combining niacinamide, D-pantothenyl alcohol, and plant/yeast-derived components with specific ratios and pH adjustments effectively addresses skin issues by enhancing epidermal cell activation and stability, improving skin texture and transparency.
Patent Information
- Application Number
- JP2024059832
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2024-04-02
- Publication Date
- 2025-10-15
AI Technical Summary
Existing topical skin preparations containing multiple active ingredients face issues with efficacy, stability, and usability in addressing skin aging, dryness, rough skin, age spots, and freckles.
A combination of niacinamide and D-pantothenyl alcohol, along with plant- and yeast-derived components, is formulated into a topical skin preparation with specific mass ratios and pH adjustments to enhance epidermal cell activation and stability, incorporating additional active ingredients like tranexamic acid and organic acids.
The formulation activates epidermal cell energy metabolism, improving skin texture and transparency while maintaining stability against discoloration and crystallization.
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Figure 2025157011000003
Abstract
Description
[Technical Field]
[0001] The present invention relates to an external skin preparation containing multiple active ingredients. [Background technology]
[0002] It has been known that skin aging, dryness, rough skin, age spots, and freckles are phenomena that arise from a complex interplay of internal factors, such as the inactivation of cell proliferation and differentiation, decreased hormone secretion, and a quantitative decrease in extracellular matrix components, with external factors, such as cell and tissue damage caused by active oxygen induced by sunlight (ultraviolet rays), or inflammation.There is a demand for active ingredients that can prevent and improve these conditions, such as aging, dryness, rough skin, age spots, and freckles.
[0003] Conventionally, as shown in Patent Documents 1 to 3, for example, topical skin preparations containing multiple active ingredients (tranexamic acid, niacinamide, D-pantothenyl alcohol, ascorbic acid or a derivative thereof, and glycyrrhizinic acid or a derivative thereof, etc.) that prevent or improve skin aging, dryness, rough skin, blemishes, freckles, or wrinkles have been proposed, but there have been problems with efficacy, stability, usability, and effectiveness.
[0004] [Patent Document 1] Patent Publication No. 2012-041302 [Patent Document 2] Patent Publication No. 2020-180103 [Patent Document 3] Patent Publication No. 2021-063076 DISCLOSURE OF THE INVENTION [Problem to be solved by the invention]
[0005] The present invention was made based on the discovery that a combination of niacinamide and D-pantothenyl alcohol has an epidermal cell activation effect, and that plant- and yeast-derived components that, when combined with niacinamide and D-pantothenyl alcohol, have a synergistic effect in terms of epidermal cell activation. The present invention also provides a highly stable topical skin preparation that contains the combination of niacinamide and D-pantothenyl alcohol and other active ingredients (tranexamic acid, glycyrrhizin, or a derivative thereof). [Means for solving the problem]
[0006] The present invention is an epidermal cell activator containing (a) niacinamide and (b) D-pantothenyl alcohol as active ingredients. The present invention also relates to an external skin preparation containing (a) niacinamide, (b) D-pantothenyl alcohol, and (C) tranexamic acid or a derivative thereof, wherein the mass ratio of (a) / (b) is preferably in the range of 50:1-3, the mass ratio of (a) / (c) is preferably in the range of 5:1-2, and the mass ratio of (b) / (c) is preferably in the range of 1-3:10-20. The present invention also relates to an external skin preparation further comprising (d) one or more components derived from grasses, cucurbits, rosaceae, legumes, and yeast. The present invention also provides an external skin preparation characterized by further comprising (e) an organic acid and a salt thereof and having a pH of 5.0 to 7.0. [Effects of the Invention]
[0007] According to the present invention, it is possible to provide an external skin preparation that activates the energy metabolism of epidermal cells through an epidermal cell activation effect and contains a plurality of highly stable active ingredients. DETAILED DESCRIPTION OF THE INVENTION
[0008] In the present invention, niacinamide is a type of water-soluble vitamin B group, and is also called nicotinic acid amide.
[0009] D-pantothenyl alcohol is an alcohol derivative of pantothenic acid and is also known as panthenol.
[0010] In the present invention, examples of derivatives of tranexamic acid include tranexamic acid esters (for example, tranexamic acid lauryl ester, tranexamic acid hexadecyl ester, tranexamic acid cetyl ester, or salts thereof), and amides of tranexamic acid (for example, tranexamic acid methylamide).
[0011] In the present invention, when niacinamide and D-pantothenyl alcohol are combined and incorporated into an external skin preparation, the mass ratio of niacinamide:D-pantothenyl alcohol is preferably in the range of 50:1-3 from the viewpoint of stability (coloration, crystallization, feel).
[0012] Furthermore, when niacinamide and D-pantothenyl alcohol are combined with tranexamic acid or a derivative thereof to be formulated into an external skin preparation, from the viewpoint of stability (coloration, crystallization, feel), it is preferable that the mass ratio of niacinamide to tranexamic acid is in the range of 5:1-5, and it is also preferable that the mass ratio of D-pantothenyl alcohol to tranexamic acid is in the range of 1-3:10-20.
[0013] In the present invention, niacinamide, D-pantothenyl alcohol, and tranexamic acid or a derivative thereof may be further combined with one or more of glycyrrhizinic acid or a salt thereof or a derivative of glycyrrhizinic acid, and glycyrrhetinic acid or a salt thereof or a derivative of glycyrrhetinic acid. Examples of salts or derivatives of glycyrrhizinic acid include trisodium glycyrrhizinate, dipotassium glycyrrhizinate, and monoammonium glycyrrhizinate. Examples of glycyrrhetinic acid or a derivative thereof include stearyl glycyrrhetinate. In the present invention, a licorice extract containing a salt or derivative of glycyrrhizinic acid, or glycyrrhetinic acid or a derivative thereof may also be used.
[0014] Furthermore, the present invention may further comprise one or more components derived from grasses, cucurbits, roses, legumes, and yeast.
[0015] Furthermore, particularly preferred ingredients derived from grass plants include rice leaf hydrolysate, rice extract hydrolysate, rice bran extract hydrolysate, germinated brown rice hydrolysate, rice fermentation liquid (lactic acid bacteria fermentation liquid, fermentation liquid of lactic acid bacteria and yeast) and matured products thereof, sake lees extract derived from sake, bamboo shoot skin extract of Madake or Moso bamboo, and Job's tears seed extract or fermented products thereof.
[0016] As the component derived from a plant of the Cucurbitaceae family, loofah extract is particularly preferred.
[0017] As the component derived from a plant of the Rosaceae family, preferred are extracts of damask rose flowers, extracts of peach flowers, leaves or immature fruit, extracts of apricot fruits or seeds, extracts of strawberry flowers, and extracts of cherry blossom flowers or leaves. Also, a mixture of sake lees extract and cherry blossom extract, which are components derived from plants of the Poaceae family, may be used.
[0018] Furthermore, as legume-derived components, particularly preferred are extracts of white soybeans or black soybeans or hydrolysates thereof, fermented soy milk broth, adzuki bean extract, red clover extract, kudzu root extract, sophora flavescens extract, and rooibos extract.
[0019] Examples of yeast include yeasts of the genus Saccharomyces such as Saccharomyces cerevisiae, Saccharomyces awamori, Saccharomyces chevalieri, Saccharomyces carlsbergensis, and Saccharomyces bayonus; yeasts of the genus Torulaspora such as Torulaspora delbruekii, Torulaspora fermentati, and Torulaspora rosei; yeasts of the genus Torulaspora such as Zygosaccharomyces rouxii and Zygosaccharomyces sojae; Yeasts of the genus Zygosaccharomyces, such as Zygosaccharomyces soybean, Zygosaccharomyces sake, Zygosaccharomyces miso, and Zygosaccharomyces lactis; yeasts of the genus Candida, such as Candida versatilis, Candida etchellsii, Candida kefyr, Candida sake, and Candida scottii; yeasts of the genus Candida, such as Aureobasidium pullulans, Aureobasidium mansonii, and Aureobasidium microstictum. Examples include yeasts of the genus Aureobasidium such as Aureobasidium microstictum.Of the above-mentioned yeasts, yeasts of the genus Saccharomyces (e.g., Saccharomyces cerevisiae) are preferred from the standpoint of safety and effectiveness, but yeasts of the genus Saccharomyces can be of any origin, such as those derived from sake or beer, those derived from plants such as roses, lilies, cherry blossoms, or camellia flowers, or those of marine origin. Examples of yeast-derived components include yeast extracts and yeast extracts, which can be obtained by, for example, culturing yeast in a culture medium, hydrolysis methods in which the cultured yeast is solubilized with an acid or alkali to solubilize the cell components, autolysis methods in which the cultured yeast utilizes protease or the like present in the yeast cells, or enzymatic methods in which the cultured yeast utilizes an enzyme such as a protease.
[0020] The carbon source used in culturing yeast is not particularly limited, and examples thereof include glucose, fructose, lactose, raffinose, etc. In addition to the carbon source, a nitrogen source may also be added, and examples thereof include amino acids and peptones.
[0021] The temperature for culturing the yeast is in the range of 25° C. to 40° C., preferably in the range of 28° C. to 35° C. The pH is in the range of 3.0 to 8.5, preferably in the range of 3.5 to 7.5.
[0022] Furthermore, in topical skin preparations containing niacinamide and D-pantothenyl alcohol, it is preferable to adjust the pH to a range of 5.0 to 7.0. Here, when adjusting the pH, it is preferable to use an organic acid or a salt thereof. Examples of organic acids or salts thereof include citric acid, acetic acid, gluconic acid, malic acid, lactic acid, succinic acid, tartaric acid, lactic acid, and salts thereof (sodium salt, potassium salt, etc.). Furthermore, in topical skin preparations containing niacinamide, D-pantothenyl alcohol, and tranexamic acid, it is preferable to use sodium metabisulfite in combination.
[0023] When the active ingredient according to the present invention is incorporated into a topical skin preparation, in addition to the essential ingredients, ingredients typically used in topical skin preparations, such as oily ingredients, surfactants (synthetic or natural), moisturizers, anti-inflammatory agents, thickeners, preservatives / bactericides, anti-acne agents, sebum secretion inhibitors, cell activators, powder ingredients, ultraviolet absorbers, antioxidants, stabilizers, pigmentation prevention agents, anti-wrinkle agents, pigments, fragrances, etc., may be incorporated as needed.
[0024] Examples of oily ingredients include olive oil, jojoba oil, castor oil, soybean oil, rice oil, rice germ oil, coconut oil, palm oil, cocoa oil, meadowfoam oil, shea butter, tea tree oil, avocado oil, macadamia nut oil, bergamot oil, lavender oil, rose oil, mandarin orange oil, chamomile oil, and other plant-derived oils and fats such as squalane; vitamin A oil; animal-derived oils and fats such as mink oil and turtle oil; waxes such as beeswax, carnauba wax, rice wax, and lanolin; liquid paraffin, petrolatum, and paraffin wax. Examples of suitable glycerides include hydrocarbons such as cocos and squalane; fatty acids such as myristic acid, palmitic acid, stearic acid, oleic acid, isostearic acid, and cis-11-eicosenoic acid; higher alcohols such as lauryl alcohol, cetanol, pantothenyl alcohol, and stearyl alcohol; and synthetic esters and synthetic triglycerides such as isopropyl myristate, isopropyl palmitate, butyl oleate, 2-ethylhexyl glyceride, and higher fatty acid octyldodecyl (e.g., octyldodecyl stearate).
[0025] Examples of surfactants include nonionic surfactants such as polyoxyethylene alkyl ethers, polyoxyethylene alkylene glycerol ethers, polyoxypropylene diglyceryl ethers, polyoxyethylene polyoxypropylene ethers, polyoxyethylene polyoxypropylene butyl ethers, polyoxyethylene fatty acid esters, polyoxyethylene sorbitan fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, polyoxyethylene hydrogenated castor oil, and polyoxyethylene sorbitol fatty acid esters; fatty acid salts, alkyl sulfates, alkylbenzene sulfonates, polyoxyethylene alkyl ether sulfates, polyoxyethylene fatty amine sulfates, polyoxyethylene alkylphenyl ether sulfates, polyoxyethylene alkyl ... Examples of surfactants that can be used include anionic surfactants such as polyoxyethylene alkyl ether phosphates, α-sulfonated fatty acid alkyl ester salts, and polyoxyethylene alkylphenyl ether phosphates; cationic surfactants such as quaternary ammonium salts, primary to tertiary fatty amine salts, trialkylbenzylammonium salts, alkylpyridinium salts, 2-alkyl-1-alkyl-1-hydroxyethylimidazolinium salts, N,N-dialkylmorpholinium salts, and polyethylenepolyamine fatty acid amide salts; and amphoteric surfactants such as N,N-dimethyl-N-alkyl-N-carboxymethylammoniobetaine, N,N,N-trialkyl-N-alkyleneammoniocarboxybetaine, N-acylamidopropyl-N', N'-dimethyl-N'-β-hydroxypropylammoniosulfobetaine.
[0026] Examples of emulsifiers and / or emulsifying aids that can be blended include stevia derivatives such as enzyme-treated stevia, saponin or derivatives thereof, casein or its salts (sodium, etc.), sugar and protein complexes, sucrose or esters thereof, lactose, soybean-derived water-soluble polysaccharides, soybean-derived protein and polysaccharide complexes, lanolin or derivatives thereof, cholesterol, stevia derivatives (enzyme-treated stevia, etc.), silicates (aluminum, magnesium, etc.), carbonates (calcium, sodium, etc.), saponin and derivatives thereof, lecithin and derivatives thereof (hydrogenated lecithin, etc.), lactic acid bacteria-fermented rice, lactic acid bacteria-fermented germinated rice, lactic acid bacteria-fermented grains (wheat, beans, millet, etc.), etc.
[0027] Examples of moisturizing agents include glycerin, concentrated glycerin, propylene glycol, dipropylene glycol, 1,3-butylene glycol, polyethylene glycol, sorbitol, xylitol, sodium pyrrolidone carboxylate, and the like, as well as sugars such as trehalose and raffinose, elastin and its derivatives, NMF-related substances, lactic acid, urea, octyldodecyl higher fatty acids, seaweed extracts, estradiol, various amino acids and their derivatives, phosphorylcholine-containing polymers (2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer liquid, polymethacryloyloxyethyl phosphorylcholine, 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer, etc.), hyaluronic acid or its salts, hyaluronic acid hydrolysates, hyaluronic acid fermentation products, collagen or its derivatives, collagen hydrolysates or fermentation products, and ceramides.
[0028] Examples of thickeners include components derived from brown algae, green algae, or red algae, such as alginic acid, agar, carrageenan, and fucoidan; polysaccharides such as pectin and aloe polysaccharide; gums such as tragacanth gum, locust bean gum, xanthan gum, gellan gum, and guar gum; cellulose derivatives such as carboxymethyl cellulose, hydroxyethyl cellulose, and hydroxypropyl cellulose; synthetic polymers such as carboxyvinyl polymers, alkyl-modified carboxyvinyl polymers, polyvinyl alcohol, polyvinylpyrrolidone, and acrylic acid-methacrylic acid copolymers; hyaluronic acid and its derivatives; polyglutamic acid and its derivatives, and polyacrylic acid.
[0029] Examples of anti-inflammatory or anti-inflammatory agents include allantoin, ε-aminocaproic acid, d-camphor, dl-camphor, zinc oxide, pyridoxine or its hydrochloride, and riboflavin or its derivatives.
[0030] Examples of antiseptics and disinfectants include urea; benzoic acid or its salts, parahydroxybenzoic acid esters such as methyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, and butyl parahydroxybenzoate; phenoxyethanol, dichlorophene, hexachlorophene, chlorhexidine hydrochloride, benzalkonium chloride, salicylic acid, sodium salicylate, zinc pyrithione, benzalkonium chloride, ethanol, undecylenic acid, phenols, alkylisoquinolinium bromide, resorcinol, jamal (imidazoline), nirurea), isopropyl methylphenol, triclosan, trichlorocarbanide, trichlorohydroxydiphenol ether, hinokitiol, polyhydric alcohols (1,3-butylene glycol, 1,2-pentanediol, propanediol, 1,2-hexanediol, glycerin, diglycerin, concentrated glycerin), concentrated benzalkonium chloride solution 50, essential oils such as peppermint oil and eucalyptus oil, bark dry distillate, radish fermented liquid, hydroxyalkyl urea, and alcohols derived from plants such as sugar cane and corn.
[0031] Examples of cell activators include menthol, dl-menthol, and γ-oryzanol.
[0032] Anti-acne agents include sulfur, salicylic acid or its salts, photosensitizer No. 201, pyridoxine dicaprylate, isopropylmethylphenol, and the like.
[0033] Examples of powder components include sericite, titanium oxide, talc, kaolin, bentonite, zinc oxide, magnesium carbonate, magnesium oxide, zirconium oxide, barium sulfate, silicic anhydride, mica, nylon powder, polyethylene powder, silk powder, cellulose-based powder, powder of grains (rice, wheat, corn, millet, etc.), powder of beans (soybean, adzuki bean, etc.), and the like.
[0034] Examples of ultraviolet absorbers include ethyl para-aminobenzoate, ethylhexyl para-dimethylaminobenzoate, amyl salicylate and its derivatives, 2-ethylhexyl para-methoxycinnamate, octyl cinnamate, oxybenzone, 2,4-dihydroxybenzophenone, 2-hydroxy-4-methoxybenzophenone-5-sulfonate, 4-tert-butyl-4-methoxybenzoylmethane, 2-(2-hydroxy-5-methylphenyl)benzotriazole, urocanic acid, ethyl urocanate, and aloe extract.
[0035] Examples of antioxidants include butylhydroxyanisole, butylhydroxytoluene, propyl gallate, coenzyme Q10, carotenoids such as astaxanthin, vitamin A or a derivative thereof (retinol palmitate, etc.).
[0036] In the present invention, the stabilizer refers to an organic acid, an inorganic acid, or the like that suppresses coloration, precipitation, crystallization, odor, etc. Examples include citric acid, sodium citrate, sodium pyrosulfite, disodium edetate, trisodium edetate, tetrasodium edetate, etidronic acid, and phytic acid.
[0037] Examples of anti-pigmentation agents include one or more selected from kojic acid or its derivatives, ascorbic acid or its derivatives, arbutin, placenta (placenta extract), 4-methoxysalicylic acid potassium salt, magnolignan (5,5'-dipropyl-biphenyl-2,2'-diol), linoleic acid, hydroxybenzoic acid and its derivatives (e.g., 2,5-diacetoxybenzoic acid, 2-acetoxy-5-hydroxybenzoic acid, 2-hydroxy-5-propionyloxybenzoic acid, etc.), α-hydroxy acids (e.g., lactic acid, malic acid, succinic acid, citric acid, α-hydroxyoctanoic acid, etc.), AMP (adenosine monophosphate, adenosine monophosphate), t-cycloamino acid derivatives, Morus alba extract, chamomile extract, hydrolyzed rice bran extract, saxifrage extract, and white mustard extract or hydrolyzates thereof.
[0038] In the present invention, examples of kojic acid derivatives include kojic acid esters such as kojic acid monobutyrate, kojic acid monocaprate, kojic acid monopalmitate, and kojic acid dibutyrate, kojic acid ethers, and kojic acid sugar derivatives such as kojic acid glucoside. Examples of ascorbic acid derivatives include ascorbic acid ester salts such as sodium L-ascorbic acid 2-phosphate, magnesium L-ascorbic acid 2-phosphate, sodium L-ascorbic acid 2-sulfate, and magnesium L-ascorbic acid 2-sulfate, L-ascorbic acid 2-glucoside (2-O-α-D-glucopyranosyl-L-ascorbic acid), and L-ascorbic acid 5-glucoside (5-O-α-D-glucuronidyl-L-ascorbic acid). ascorbic acid sugar derivatives such as L-ascorbic acid tetraisopalmitate and L-ascorbic acid tetralaurate; L-ascorbic acid tetra-fatty acid esters such as L-ascorbic acid tetraisopalmitate and L-ascorbic acid tetralaurate; 3-O-ethyl ascorbic acid; and sodium L-ascorbic acid-2-phosphate-6-O-palmitate.
[0039] As physiologically active substances, lactic acid bacteria culture, Brassicaceae plants, Theaceae plants, Paeoniaceae plants, Rutaceae plants, Amaranthaceae plants, Zosteraea plants, Asteraceae plants, Malvaceae plants, Gentianaceae plants, Lamiaceae plants, Nelumbaceae plants, Araliaceae plants, Solanaceae plants, Bignoniaceae plants, Actinidiaceae plants, Mulberry plants, Iridaceae plants, Campanulaceae plants, Oleaceae plants, Actinidiaceae plants, Mulberry plants, Rhamnaceae plants, Orchidaceae plants, Anacardiaceae plants, Garciniaceae plants, Valenciaceae plants, Rutaceae plants, Myrtaceae plants, Yuzu It is preferred to combine it with one or more of the following: extracts of one or more plants selected from the Lithuaceae family, Crassulaceae family, Cupressaceae family, Convolvulaceae family, and Asparagaceae family, or hydrolysates or fermented products thereof; extracts of one or more seaweeds selected from the Laminariaceae family, Mirrataceae family, and Ulvaceae family, or hydrolysates or fermented products thereof; jellyfish (autolyzed products of moon jellyfish, Nomura's jellyfish, etc.); hydrolysates or fermented products of hyaluronic acid; and extracts of royal jelly, or hydrolysates or fermented products thereof.
[0040] As Brassicaceae plants, particularly preferred are extracts of seeds of holly, burdock, or porcini, or hydrolysates or fermented products thereof. Furthermore, as components derived from Theaceae plants, particularly green tea (Yabukita, Samidori, Asahi, Goko, Ujimidori, Kyomidori, Ujihikari, Samidori, Benifuki, etc.) and black tea (Darjeeling, Assam, Ceylon, Earl Grey, honey-scented black tea, etc.) are preferred. Furthermore, as components derived from Paeoniaceae plants, particularly extracts of peony root or flower and peony flower or root are preferred. Furthermore, as components derived from Amaranthaceae plants, particularly Salicornia extract is preferred. Furthermore, as components derived from Zosteraeae plants, particularly extracts of Zostera marina or Zostera serrata are preferred. Furthermore, as components derived from Asteraceae plants, particularly burdock root extract, sunflower sprout extract, Arctium gracilis extract, arnica extract, or chamomile flower extract are preferred. As a component derived from a plant of the Malvaceae family, fermented products of hibiscus, rose of sharon, or hibiscus are preferred. As a component derived from a plant of the Gentianaceae family, gentian extract is preferred. As a plant of the Lamiaceae family, perilla extract and Veronica purpurea fruit extract are preferred. As a component derived from a plant of the Nelumboceae family, particularly lotus flower or lotus seed extract or fermented lotus seed product is preferred. As a component derived from a plant of the Araliaceae family, an extract or fermented product of ginseng is preferred. As a component derived from a plant of the Solanaceae family, an extract of eggplant (long eggplant, water eggplant, rice eggplant, Kamo eggplant, etc.) is preferred. As a component derived from a plant of the Bignoniaceae family, pau d'arco bark extract is preferred. As a component derived from a plant of the Actinidiaceae family, immature kiwi extract is preferred. As a component derived from a plant of the Moraceae family, Morus alba extract, mulberry fruit extract, and fig fruit or bark extract are preferred. As a component derived from a plant of the Rhamnaceae family, jujube fruit extract is preferred. Furthermore, as an ingredient derived from an Iridaceae plant, saffron is preferred. As an ingredient derived from a Campanulaceae plant, an extract or hydrolysate of Codonopsis arvensis root is preferred. As an ingredient derived from an Anacardiaceae plant, mango fruit extract is particularly preferred. As an ingredient derived from a Garciniaceae plant, mangosteen fruit extract is particularly preferred. As an ingredient derived from a Valenciaceae plant, cherimoya fruit extract is preferred.Preferred components derived from Rutaceae plants are Satsuma mandarin, bergamot fruit extract, grapefruit or late peiyu fruit (including immature fruits), or Japanese pepper seed extract. Preferred components derived from Liliaceae plants are extracts of daylilies, daylilies, Casablanca lilies, Madonna lilies, or Japanese lilies. Preferred components derived from Crassulaceae plants are extracts or fermented products of Rhodiola rosea (Rhodiola rosea). Preferred components derived from Oleaceae plants are jasmine flower extract. Preferred components derived from Cupressaceae plants are Juniperus communis fruit extract. Preferred components derived from Myrtaceae plants are guava leaf extract. Preferred components derived from Orchidaceae plants are Bleached lily root (white part). Preferred components derived from Convolvulaceae plants are sweet potato extract or fermented product thereof, or sweet potato shochu lees extract or fermented product thereof. Asparagus (green asparagus and white asparagus) is preferred as a plant of the Asparagaceae family. As a component derived from seaweed of the Laminaria family, kelp extract is particularly preferred, as a component derived from seaweed of the Mirinaceae family, katamen kyrinsai extract is preferred, and as a component derived from seaweed of the Ulva family, Ulva pertusa extract is particularly preferred. As a component derived from seaweed of the Funoriaceae family, funori extract is particularly preferred.
[0041] Test Example 1: Evaluation test of epidermal cell activation effect [Sample preparation] Three compositions containing niacinamide (ingredient 1) and D-pantothenyl alcohol (ingredient 2) (Compositions 1 to 3 of the present invention) were prepared as shown in Table 1. A hydrolyzate of rice extract, a component derived from a grass family plant, was prepared as ingredient 3 (for example, this can be prepared with reference to the description in JP 05-221844 A). A loofah extract, a component derived from a Cucurbitaceae plant, was prepared as ingredient 4 (for example, this can be prepared with reference to the description in JP 2016-222622 A). A mixture of sake lees extract, a component derived from a grass family plant, and cherry blossom extract, a component derived from a Rosaceae family, was prepared as ingredient 5 (for example, this can be prepared with reference to the description in JP 2022-182173 A). An example of a yeast-derived component as ingredient 6 is a yeast extract (yeast hydrolysate solution) obtained by culturing yeast (Saccharomyces cerevisiae) in a medium and hydrolyzing the culture solution with an acid. [Evaluation test] Human epidermal keratinocytes (NHEK) were cultured at 8 × 10 cells / well in a 96-well microplate containing HuMedia KG2 medium (Kurabo). 3Cells were seeded at 1000 cells / well and pre-cultured at 37°C and 5.0% CO2 for 1 day. The medium was then replaced with HuMedia KB2. PBS(-) containing Compositions 1 to 15 of the present invention, as shown in Tables 1 to 3, was added as sample solutions, and the cells were cultured under the same conditions for another 2 days. The concentrations of Components 3 to 6 shown in Tables 2 and 3 represent the final concentrations in the total volume of the sample solution. After removing the medium, Hoechst 33342 was added to stain DNA. Measurements were performed at Ex = 355 nm and Em = 460 nm using a fluorescent plate reader (Fluoroscan Ascent, Thermo Fisher Scientific). After the measurements, 0.03% MTT was added and incubated at 37°C for 1 hour. The resulting formazan was extracted with isopropanol, and the MTT value was measured at wavelengths of 570-630 nm using a microplate reader (Model 680, Bio-Rad). The same procedure was repeated for a control (control) in which the same concentration of PBS(-) was added instead of the sample solution, and the MTT activity per epidermal cell was calculated by dividing the obtained MTT value by the amount of DNA. The obtained MTT activity per epidermal cell was expressed as a relative value, with the control value set at 100.
[0042] The results of Test Example 1 are shown in Tables 1 to 3. [Table 1] JPEG2025157011000001.jpg4699
[0043] [Table 2] JPEG2025157011000002.jpg116100
[0044] [Table 3] JPEG2025157011000003.jpg123102
[0045] As shown in Tables 1 to 3, it was confirmed that Compositions 1 to 3, which combine niacinamide and D-pantothenyl alcohol according to the present invention, have a significant epidermal cell activation effect. Furthermore, it was also confirmed that the effect of epidermal cell activation is enhanced by combining them with plant-derived or yeast-derived components (Components 3 to 6). This suggests that the energy metabolism of epidermal cells may be enhanced, for example, to promote normalization of skin turnover, or to improve skin texture and transparency.
[0046] Formulation examples containing niacinamide and D-pantothenyl alcohol according to the present invention are shown below, but the present invention is not limited thereto. To improve stability (inhibiting discoloration, inhibiting precipitation of crystals and sediments, and improving texture), the mass ratio of niacinamide to D-pantothenyl alcohol is preferably in the range of 50:1-3, as shown in the formulation examples below. Furthermore, when niacinamide and D-pantothenyl alcohol are combined with tranexamic acid or a derivative thereof to be incorporated into a topical skin preparation, from the viewpoint of stability (discoloration, crystallization, and texture), the mass ratio of niacinamide to tranexamic acid is preferably in the range of 5:1-2, and the mass ratio of D-pantothenyl alcohol to tranexamic acid is preferably in the range of 1-3:10-20. Furthermore, it has been confirmed that adjusting the pH to 5.0-7.0 in the formulation examples below can inhibit discoloration, crystallization, and sedimentation while maintaining a good texture.
[0047] Prescription example 1. Lotion [Ingredients] Part Niacinamide 6.0 D-Pantothenyl alcohol 0.2 1,3-butylene glycol 5.0 1,2-Pentanediol 1.0 Carboxyvinyl polymer 0.01 pH adjuster (sodium citrate) appropriate amount Purified water (enough to make the total volume 100 parts)
[0048] Prescription example 2: Lotion [Ingredients] Part Niacinamide 5.5 D-Pantothenyl alcohol 0.15 1,3-butylene glycol 5.0 1,2-Pentanediol 1.0 Sodium citrate 0.2 Rice extract hydrolyzate 1.0 Sodium hyaluronate 0.001 Water-soluble collagen 0.001 pH adjuster (sodium citrate) appropriate amount Purified water (enough to make the total volume 100 parts)
[0049] Prescription example 3: Lotion A lotion was obtained with the same composition as in Formulation Example 2, except that 1.0 part of loofah extract was used instead of the rice extract hydrolysate.
[0050] Prescription example 4: Lotion A lotion was obtained with the same composition as in Formulation Example 2, except that the rice extract hydrolyzate in the lotion was replaced with a mixture of 0.5 parts of cherry blossom extract and 0.5 parts of sake lees extract.
[0051] Prescription example 5. Lotion A lotion was obtained with the same composition as in Formulation Example 2, except that 1.0 part of yeast extract was used instead of the rice extract hydrolysate.
[0052] Prescription example 6. Lotion A lotion was obtained with the same composition as in Formulation Example 2, except that 1.0 part of soybean extract hydrolysate was used in place of the rice extract hydrolysate in Formulation Example 2.
[0053] Prescription example 7. Lotion [Ingredients] Part Niacinamide 5.0 D-Pantothenyl alcohol 0.3 Tranexamic acid 2.0 1,3-butylene glycol 5.0 Propanediol 1.0 Carboxyvinyl polymer 0.01 Sodium pyrosulfite 0.05 Rice extract hydrolyzate 1.0 Sodium hyaluronate 0.001 Water-soluble collagen 0.001 pH adjuster (sodium citrate) appropriate amount Purified water (enough to make the total volume 100 parts)
[0054] Prescription example 8. Lotion A lotion was obtained with the same composition as in Formulation Example 7, except that 1.0 part of loofah extract was used instead of the rice extract hydrolysate.
[0055] Prescription example 9. Lotion A lotion was obtained with the same composition as in Formulation Example 7, except that the rice extract hydrolysate in Formulation Example 7 was replaced with a mixture of 0.5 parts of cherry blossom extract and 0.5 parts of sake lees extract.
[0056] Prescription example 10. Lotion A lotion was obtained with the same composition as in Formulation Example 7, except that 1.0 part of yeast extract was used instead of the rice extract hydrolysate.
[0057] Prescription example 11. Lotion A lotion was obtained with the same composition as in Formulation Example 7, except that 1.0 part of soybean extract hydrolysate was used instead of the rice extract hydrolysate in Formulation Example 7.
[0058] Prescription example 12. Lotion [Ingredients] Part Niacinamide 3.0 Tranexamic acid 1.0 D-Pantothenyl alcohol 0.1 Dipotassium glycyrrhizinate 0.08 1,3-butylene glycol 1.0 1,2-Pentanediol 2.0 Sodium pyrosulfite 0.1 Sodium citrate 0.2 Carboxymethyl cellulose 0.01 pH adjuster (potassium hydroxide) appropriate amount Purified water (enough to make the total volume 100 parts)
[0059] Prescription example 13. Lotion [Ingredients] Part Niacinamide 3.5 Ascorbic acid derivative (L-ascorbic acid 2-glucoside) 2.0 D-Pantothenyl alcohol 0.1 1,3-butylene glycol 5.0 Hexanediol 1.0 Phenoxyethanol 0.3 Sodium citrate 0.2 Sodium pyrosulfite 0.2 Acrylic acid / alkyl methacrylate copolymer 0.01 pH adjuster (appropriate amount) Purified water (enough to make the total volume 100 parts)
[0060] Prescription example 14. Lotion [Ingredients] Part Niacinamide 4.0 D-Pantothenyl alcohol 0.15 Tranexamic acid 1.0 Sodium hyaluronate 0.01 Propanediol 1.0 1,2-Pentanediol 1.0 1,3-butylene glycol 1.0 Sodium citrate 0.2 Sodium pyrosulfite 0.2 Xanthan gum 0.01 pH adjuster (potassium hydroxide) appropriate amount Purified water (enough to make the total volume 100 parts)
[0061] Prescription example 15. Lotion A lotion was obtained with the same composition as in Formulation Example 14, except that 0.01 parts of hydrolyzed hyaluronic acid was used instead of sodium hyaluronate.
[0062] Prescription example 15. Lotion A lotion was obtained with the same composition as in Formulation Example 14, except that 0.01 parts of acetylated hyaluronic acid was used instead of sodium hyaluronate.
[0063] Prescription example 16. Lotion A lotion was obtained with the same composition as in Formulation Example 14, except that 0.01 parts of lactic acid fermented hyaluronic acid was used instead of sodium hyaluronate.
[0064] Prescription example 17. Lotion A lotion was obtained with the same composition as in Formulation Example 14, except that ceramide 1 (0.1 part) was used instead of sodium hyaluronate.
[0065] Prescription example 18. Lotion A lotion was obtained with the same composition as in Formulation Example 14, except that 0.01 parts of atelocollagen was used instead of sodium hyaluronate.
[0066] Prescription example 19. Lotion [Ingredients] Part Niacinamide 5.0 Tranexamic acid 2.0 Pantothenyl alcohol 0.2 Ascorbic acid derivative (L-ascorbic acid 2-glucoside) 2.0 Glyceryl Caprylate 3.0 Polyglyceryl-10 Laurate 3.0 Cetyl alcohol 2.0 Behenyl Alcohol 2.0 Methylparaben 0.1 Diglycerin 1.0 1,3-butylene glycol 1.0 Sodium citrate 0.2 Sodium pyrosulfite 0.02 Carboxyvinyl polymer 0.01 pH adjuster (potassium hydroxide) appropriate amount Purified water (enough to make the total volume 100 parts)
[0067] Prescription example 20. Emulsion [Ingredients] Part Niacinamide 4.0 Tranexamic acid 1.0 D-Pantothenyl alcohol 0.1 Dipotassium glycyrrhizinate 0.03 Squalane 5.0 Cyclopentanesiloxane 1.0 Hexalan 3.0 Hexyldecyl Isostearate 1.0 Caprylic / Capric Triglyceride 1.0 Polyglyceryl-10 Laurate 5.0 Polyglyceryl-10 Isostearate 5.0 Ascorbyl Dipalmitate 5.0 Hydrogenated soy lecithin 1.5 Glycerin 3.0 1,3-butylene glycol 2.0 Carboxymethylcellulose 0.1 Xanthan gum 0.01 Tremella fuciformis polysaccharide 0.01 Isopropylmethylphenol 0.1 Tocopheryl acetate 0.3 Sodium hyaluronate 0.001 Hydrolyzed Sodium Hyaluronate 0.001 Ceramide 0.1 moisturizer ※1) 0.1 Sodium citrate 0.1 Sodium pyrosulfite 0.01 Rice extract hydrolyzate 0.5 Loofah extract 0.5 Cherry blossom extract 0.5 Sake lees extract 0.5 Yeast extract 0.5 Royal jelly fermented product 0.1 Water-soluble collagen 0.001 pH adjuster (potassium hydroxide) appropriate amount Purified water (enough to make the total volume 100 parts) *1) 2-Methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer
[0068] Prescription example 21. Emulsion An emulsion was obtained in the same manner as in Formulation Example 20, except that 0.1 part of stearyl glycyrrhetinate was used in place of 0.1 part of dipotassium glycyrrhizinate.
[0069] Prescription example 22. Cream [Ingredients] Part Niacinamide 5.0 Tranexamic acid 2.0 Dipotassium glycyrrhizinate 0.04 D-Pantothenyl alcohol 0.2 Olive oil 5.0 Jojoba oil 5.0 Squalane 5.0 Hexyldecyl Isostearate 5.0 Dioctyldodecyl / Phytosteryl Lauroyl Glutamate / Behenyl) 5.0 Glyceryl Caprylate 1.0 Glyceryl stearate 1.0 Isostearyl glyceryl 3.0 γ-oryzanol 0.1 Behenyl Alcohol 2.0 Palmitic acid 2.5 Allantoin 0.1 Riboflavin 0.01 Resorcinol 0.1 Benzalkonium chloride 0.05 Urea 3.0 β-Glycyrrhetinic acid 0.1 Lactic acid bacteria fermented rice 2.0 Hydrogenated lecithin 0.5 Hydrogenated lysolecithin 0.5 Fermented rice liquid 1.0 Soy extract hydrolyzate 1.0 Ceramide 1 0.01 Ceramide 2 0.01 Ceramide 3 0.01 Coenzyme Q10 0.3 Xanthan gum 1.0 Zinc oxide 0.5 Diglycerin 1.0 1,3-butylene glycol 1.0 1,2-Pentanediol 1.0 Purified water (enough to make the total volume 100 parts)
[0070] Prescription example 23. Cream [Ingredients] Part Niacinamide 5.5 Tranexamic acid 1.5 Dipotassium glycyrrhizinate 0.08 D-Pantothenyl alcohol 0.1 Olive oil 5.0 Squalane 5.0 Jojoba oil 5.0 Jojoba Wax 1.0 Shea Butter 2.0 Behenyl Alcohol 1.0 Stearyl alcohol 1.5 Candelilla Wax 0.5 Lactic acid bacteria fermented rice 3.0 Carboxyvinyl polymer 0.3 Sodium alginate 0.2 Sodium hyaluronate 0.01 Diglycerin 1.0 1,2-Pentanediol 1.0 Propanediol 1.0 Sodium pyrosulfite 0.05 Sodium citrate 0.2 Carboxyvinyl polymer 0.1 Rice extract hydrolyzate 0.5 Loofah extract 0.5 Cherry blossom extract 0.5 Sake lees extract 0.5 Yeast extract 0.5 pH adjuster (appropriate amount) Purified water (enough to make the total volume 100 parts)
[0071] Prescription example 24. Pack Niacinamide 5.0 D-Pantothenyl alcohol 0.1 Dipotassium glycyrrhizinate 0.1 Polyoxyethylene (60) hydrogenated castor oil 5.0 Cetyl alcohol 3.0 Behenyl Alcohol 3.0 Allantoin 0.1 Salicylic acid 0.1 Tranexamic acid 2.0 Tocopheryl acetate 0.5 Tocopherol nicotinate 0.1 Resorcinol 0.1 Sulfur 2.0 Estradiol 1.0 Rice extract hydrolysis 0.5 Loofah extract 0.5 Cherry blossom extract 0.25 Sake lees extract 0.25 Yeast extract 0.5 Soybean extract hydrolyzate 0.5 Polyglyceryl-6 Myristate 1.0 Potassium cocoyl glutamate 1.0 Polyglyceryl fatty acid ester 1.0 Hydrogenated Lecithin 3.0 Hydroxylated Lecithin 3.0 Hydrolyzed Collagen 0.01 Acetylated hyaluronic acid 0.01 Hyaluronic acid fermentation product 0.01 Dipropylene Glycol 5.0 Propanediol 1.0 1,2-Hexanediol 1.0 Purified water (enough to make the total volume 100 parts)
[0072] Prescription example 25. Hair shampoo [Ingredients] Part Niacinamide 1.0 D-Pantothenyl alcohol 0.05 Dipotassium glycyrrhizinate 0.1 Sodium Laureth Sulfate 10.0 Glyceryl Monostearate 1.0 Coconut oil fatty acid diethanolamide 2.0 Polyoxyethylene (40) hydrogenated castor oil 0.5 Benzalkonium chloride 1.0 Stearyl Alcohol 2.0 Behenyl Alcohol 2.0 Dimethicone 3.0 Allantoin 0.1 Salicylic acid 0.1 Sodium salicylate 0.1 Tocopherol acetate 0.1 Pyrithione Zinc 0.3 Benzoic acid 0.2 Triclosan 0.2 Citric acid 0.1 Propylene glycol 1.0 Propanediol 2.0 Rice extract hydrolysis 0.5 Loofah extract 0.5 Cherry blossom extract 0.25 Sake lees extract 0.25 Yeast extract 0.5 Purified water (enough to make the total volume 100 parts)
[0073] Prescription example 26. Hair conditioner [Ingredients] Part Niacinamide 1.0 D-Pantothenyl alcohol 0.05 Dipotassium glycyrrhizinate 0.05 Polyoxyethylene (10) hydrogenated castor oil 1.0 Distearyldimethylammonium chloride 1.5 Stearyltrimethylammonium chloride 2.0 Glyceryl 2-ethylhexanoate 1.0 Benzalkonium chloride 1.0 Cetyl alcohol 3.0 Stearyl Alcohol 1.0 Rice extract hydrolysis 0.5 Loofah extract 0.5 Cherry blossom extract 0.25 Sake lees extract 0.25 Yeast extract 0.5 Allantoin 0.1 Isopropylmethylphenol 0.1 Salicylic acid 0.1 Sulfur 0.5 Alkylisoquinolinium bromide solution (75%) 0.06 Pyrithione Zinc 0.3 Methylparaben 0.1 Triclosan 0.2 Resorcinol 0.1 Purified water (enough to make the total volume 100 parts)
[0074] Formulation example 27. Cleansing cosmetics [Ingredients] Part Niacinamide 1.0 D-Pantothenyl alcohol 0.05 Dipotassium glycyrrhizinate 0.05 Potassium cocoyl glycinate 5.0 Glycerin 10.0 Glyceryl Caprylate 1.0 Sodium lauroyl aspartate 10.0 Water-soluble collagen 5.0 Cetyl alcohol 3.0 Myristyl Alcohol 3.0 Isopropyl methyl alcohol 0.1 Allantoin 0.1 Sulfur 0.5 Isopropylmethylphenol 0.1 Tocopheryl acetate 0.2 Trichlorohydroxydiphenyl ether 0.2 Concentrated Benzalkonium Chloride Solution 50 0.2 Benzalkonium chloride 0.1 Rice extract hydrolysis 0.5 Loofah extract 0.5 Cherry blossom extract 0.25 Sake lees extract 0.25 Yeast extract 0.5 Purified water (enough to make the total volume 100 parts)
[0075] Prescription example 28. Sheet mask A sheet mask is obtained by impregnating a nonwoven fabric with the following ingredients. [Ingredients] Part Niacinamide 5.0 Tranexamic acid 2.0 D-Pantothenyl alcohol 0.15 Dipotassium glycyrrhizinate 0.05 Isopropylmethylphenol 0.1 Glycerin 1.0 Diglycerin 1.0 1,3-butylene glycol 2.0 Citric acid 0.1 Sodium citrate 0.3 Xanthan gum 1.0 Water-soluble collagen 1.0 Sodium hyaluronate 0.01 Acetylated hyaluronic acid 0.01 Hydrolyzed Sodium Hyaluronate 0.01 Rice extract hydrolysis 0.5 Loofah extract 0.5 Cherry blossom extract 0.25 Sake lees extract 0.25 Yeast extract 0.5 Potassium hydroxide (appropriate amount) Purified water (enough to make the total volume 100 parts)
[0076] Prescription example 29. Beauty serum [Ingredients] Part Niacinamide 5.0 D-Pantothenyl alcohol 0.1 Tranexamic acid 1.5 Hyaluronic acid fermentation product 0.01 Water-soluble collagen 0.01 Rice extract hydrolysis 1.0 Soy extract hydrolyzate 1.0 Phenoxyethanol 0.1 1,3-butylene glycol 2.0 Phenoxyethanol 0.5 Sodium pyrosulfite 0.01 Citric acid 0.3 Sodium citrate 0.6 Purified water (enough to make the total volume 100 parts)
Claims
1. An epidermal cell activator containing (a) niacinamide and (b) D-pantothenyl alcohol as active ingredients.
2. A topical skin preparation comprising (a) niacinamide, (b) D-pantothenyl alcohol, and (c) tranexamic acid or a derivative thereof.
3. The topical skin preparation according to claim 1 or 2, further comprising (d) one or more components derived from grasses, cucurbits, rosaceae, legumes, and yeasts.
4. The external skin preparation according to any one of claims 1 to 3, characterized in that it contains (e) an organic acid and a salt thereof and has a pH of 5.0 to 7.0.
Citation Information
Patent Citations
Method for supporting epidermal stem cell self-renewal
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Autophagy activator
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Topical Compositions
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Aqueous cosmetic preparation
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compositions
WO2023180214A1