JP4684269B2 - Skin composition containing ascorbic acid - Google Patents

Description

  The present invention relates to an aqueous skin composition containing ascorbic acid, an ester derivative thereof, an ether derivative thereof or a salt thereof (hereinafter collectively referred to as “ascorbic acids” in the present specification). More specifically, the present invention relates to an outer skin composition that holds ascorbic acids stably in an aqueous medium.

  Conventionally, ascorbic acids have been widely used in medicines, quasi drugs, cosmetics, foods, and the like as skin improvers, nutritional supplements, or antioxidants. In particular, ascorbic acid has an anti-inflammatory effect, an acne improving effect, a whitening effect, an anti-aging effect, an antioxidant effect, a cell activation effect by promoting the synthesis of biological components such as collagen, and an ultraviolet ray of epidermal keratinocytes. It is known to exhibit various effects, such as an effect of suppressing damage and DNA damage, and is widely used as an ingredient for externally used pharmaceuticals, quasi-drugs, cosmetics and the like in anticipation of these effects.

  However, ascorbic acid is a water-soluble component that is hardly soluble in organic solvents, water is preferably used for dissolution, but it is very unstable in water and easily irreversibly hydrolyzes, thus losing the above effect. Have the disadvantage of For this reason, in order to effectively exhibit the effects of ascorbic acids in an aqueous skin composition, methods for stably holding ascorbic acids in an aqueous medium have been studied.

  For example, US Pat. No. 5,140,043 discloses a mixed solvent of water and an alkylene glycol or a mixture of an alkylene glycol and a hydroxyalkyl cellulose derivative (1: 1, preferably 2: 1 to 10: 1) (pH 3.5 or less). It has been shown that ascorbic acid is stabilized and the permeability to the skin is improved by dissolving ascorbic acid. However, since such a mixed solvent contains a large amount of polyhydric alcohol, the skin becomes sticky, and is unsuitable as a base for external use from the viewpoint of use feeling.

  In US Pat. No. 4,983,382, ascorbic acid is dissolved in a mixed solvent of 12% or less of water, water miscible polyhydric alcohols such as propylene glycol, glycerin, dipropylene glycol and polypropylene glycol, and ethanol. It has been shown that ascorbic acid can be stabilized. However, since the mixed amount of water in this mixed solvent is 12% or less, ascorbic acid cannot be added in an amount of more than 10%, and the skin is sticky because it contains a large amount of polyhydric alcohol as described above. It is not preferable as a skin external base because it is irritating to the skin due to the effect of ethanol added for the purpose of improvement.

  Further, in JP-A-8-245336, as a method for stably maintaining ascorbic acid, a first compartment comprising ascorbic acid in an anhydrous composition composed of glycerin, polyethylene glycol or the like, and an alkaline aqueous composition are disclosed. A method is described in which the two compartments are separately housed in a multi-compartment dispenser and both are mixed during use. However, this publication does not disclose a direct method for stably holding ascorbic acid in an aqueous medium.

  WO98 / 23152 discloses a composition in which an ascorbic acid derivative is stably held in an aqueous medium containing propylene glycol and glycerin. However, the invention described in the publication is directed to an ascorbic acid fatty acid ester particularly rich in fat solubility as an ascorbic acid derivative, and stably dissolves water-soluble ascorbic acid or a highly water-soluble ascorbic acid derivative in an aqueous medium. It does not disclose a direct method of holding.

  The present invention has been made in view of such circumstances. That is, an object of the present invention is to provide an aqueous skin composition in which ascorbic acids are stably held in an aqueous medium.

  As a result of intensive studies to solve the above-mentioned problems, the present inventors have found that ascorbic acids compounded by using a mixed aqueous solvent of water and glycol ether as an aqueous medium for compounding ascorbic acids. It was found that it can be stably maintained over a long period of time. Furthermore, the present inventors can add a desired amount of water-soluble ascorbic acid to the mixed aqueous solvent so that the desired effect can be obtained, and as a base for an external preparation for skin containing ascorbic acid as an active ingredient. It was confirmed that it was extremely suitable. The present invention has been developed based on such knowledge.

That is, this invention is the composition for outer skin hung up to the following (1)-(5):
(1) i) at least one selected from the group consisting of ascorbic acid, ester derivatives thereof, ether derivatives thereof and salts thereof;
ii) water,
iii) glycol ethers, and
iv) ethanol, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, diethylene glycol, dipropylene glycol, hydrogenated soybean phospholipid, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene lanolin alcohol, polyoxyethylene castor oil, At least one solubilizing component selected from the group consisting of polyoxyethylene hydrogenated castor oil and polyoxyethylene alkyl ether (provided that only one propylene glycol is not selected)
A composition for an outer skin, comprising:
(2) The skin composition according to (1), wherein the glycol ether is at least one selected from the group consisting of diethylene glycol ether, monoethylene glycol ether, dipropylene glycol ether, and monopropylene glycol ether.
(3) Glycol ether is ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, ethylene glycol monopropyl ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, diethylene glycol monopropyl ether, propylene glycol monoethyl ether, propylene glycol monopropyl ether, The composition for external use according to the above (2), which is at least one selected from the group consisting of dipropylene glycol monoethyl ether and dipropylene glycol monopropyl ether.
(4) The solubilizing component is at least one selected from the group consisting of ethanol, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, diethylene glycol, dipropylene glycol, and hydrogenated soybean phospholipid (provided that The outer skin composition according to any one of the above (1) to (3), wherein only one type of propylene glycol is not selected.
(5) The skin composition according to any one of (1) to (4), wherein the solubilizing component is contained in the skin composition at a ratio of 0.01 to 80% by weight.

  The outer skin composition of the present invention containing ascorbic acid as an active ingredient generally keeps unstable ascorbic acid in a stable state in the presence of water by using a mixed solvent of water and glycol ether as an aqueous medium. be able to. Therefore, according to the outer skin composition of the present invention, the action of ascorbic acids can be blended and prepared so that the maximum effect can be exhibited with the minimum effective amount.

  The outer skin composition of the present invention contains i) at least one selected from the group consisting of ascorbic acid, an ester derivative thereof, an ether derivative thereof and a salt thereof, ii) water, and iii) a glycol ether. And

i) Ascorbic acid Ascorbic acid used in the present invention is not particularly limited as long as it is used as a component of an external preparation in the pharmaceutical, quasi-drug or cosmetic field. Usually, L-ascorbic acid known by the common name of vitamin C can be mentioned.

  The derivative of ascorbic acid used in the present invention is not particularly limited as long as it is used as a component of an external preparation in the pharmaceutical, quasi-drug or cosmetic field, as in ascorbic acid, and any ester derivative or ether Derivatives can be mentioned. Preferred are water-soluble or highly water-soluble ester derivatives or ether derivatives. Specific examples of the ester derivatives of ascorbic acid include L-ascorbic acid phosphate such as L-ascorbic acid monophosphate, L-ascorbic acid diphosphate and L-ascorbyl triphosphate, and L-ascorbic acid. -2- means sulfate. The ether derivative of ascorbic acid specifically means L-ascorbic acid-2-glucoside.

  Examples of the salt of ascorbic acid, its ester derivative or its ether derivative (ascorbic acid) used in the present invention include alkali metal salts such as sodium and potassium, alkaline earth metal salts such as magnesium, calcium and barium, and aluminum. Metal salts such as polyvalent metal salts of: ammonium salts such as ammonium and tricyclohexylammonium, and various alkanolamine salts such as monoethanolamine, diethanolamine, triethanolamine, monoisopropanolamine, diisopropanolamine and triisopropanolamine Can be mentioned.

  The ascorbic acid is preferably L-ascorbic acid, L-ascorbic acid phosphate, L-ascorbic acid-2-sulfate, L-ascorbic acid-2-glucoside, and salts thereof, and particularly preferably skin. And L-ascorbic acid, L-ascorbic acid monophosphate ester, L-ascorbic acid-2-glucoside or a salt thereof because of their high safety and effectiveness for mucous membranes.

  In addition, even if it uses said ascorbic acid, its ester derivative, its ether derivative, and those salts individually as an ascorbic acid, the outer skin composition of this invention is used in combination of 2 or more types arbitrarily. It can also be used.

  The proportion of the ascorbic acid compounded in the skin composition of the present invention is not particularly limited as long as the skin composition of the present invention has an action caused by the ascorbic acid. The action can be selected as appropriate according to the action (for example, anti-inflammatory action, acne improving action, whitening action, anti-aging action, action of promoting synthesis of biological components such as collagen, cell damage and DNA damage suppressing action by ultraviolet rays, etc.). Usually in the range of 0.001 to 30% by weight, preferably 0.01 to 30% by weight, more preferably 0.1 to 25% by weight, still more preferably 1 to 20% by weight, particularly preferably 5 to 20% by weight. Can be mentioned.

ii) the ratio of water to be blended in the dermatological composition of the water present invention is not particularly limited that the dermatological compositions of the present invention to hold the ascorbic acids in a stable state a limit, usually 0.01 It can be used by appropriately selecting from a range of ˜90 wt%. Preferably, it is desirable to appropriately select and adjust in consideration of the feeling of skin use and / or the stability of ascorbic acids. From this viewpoint, the range is preferably 5 to 90% by weight, more preferably 5 to 80% by weight, still more preferably 10 to 70% by weight, and particularly preferably 10 to 55% by weight.

iii) Glycol ether glycol ether is monoethylene glycol ether, diethylene glycol ether, propylene glycol ether, dipropylene glycol ether, specifically ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, ethylene glycol monopropyl ether; diethylene glycol monomethyl Ether, diethylene glycol monoethyl ether, diethylene glycol monopropyl ether; propylene glycol monoethyl ether, propylene glycol monopropyl ether; dipropylene glycol monoethyl ether, dipropylene glycol monopropyl ether.

  The blending ratio of the glycol ether blended in the outer skin composition of the present invention is not particularly limited as long as the ascorbic acids can be kept in a stable state in an aqueous medium, and usually 0.001 to 99 weights. % Can be appropriately selected from the range of%. From the viewpoint of the stability of ascorbic acids in the outer skin composition, preferably 1 to 90% by weight, more preferably 10 to 80% by weight, still more preferably 20 to 70% by weight, particularly preferably 30 to 60% by weight. Can be mentioned.

  Further, the blending weight ratio of glycol ether and water in the outer skin composition is not particularly limited as long as the ascorbic acids are stably maintained in the outer skin composition, and usually 1 part by weight of glycol ether. The water can be appropriately selected and adjusted in such a range that the water content is 0.0001 to 10,000 parts by weight. From the viewpoint of the stability of ascorbic acids, the range of water is preferably 0.01 to 500, more preferably 0.1 to 50, based on 1 part by weight of glycol ether. From the viewpoint of usability, the range of 0.1 to 3 parts by weight of water, and particularly preferably 0.2 to 2 parts by weight of water based on 1 part by weight of glycol ether can be mentioned.

  Furthermore, the blending weight ratio of the glycol ether and the ascorbic acid in the outer skin composition is not particularly limited as long as the ascorbic acid is kept in a stable state in the outer skin composition. Ascorbic acids can be appropriately selected and adjusted from a range in which the ratio of ascorbic acids is 0.0001 to 10,000 with respect to the parts. From the viewpoint of the stability of ascorbic acids, it is preferably 0.01 to 100 parts by weight, more preferably 0.01 to 50 parts by weight, and still more preferably 0.1 to 10 parts by weight with respect to 1 part by weight of glycol ether. The most preferable range is 0.2 to 0.8 parts by weight.

  The outer skin composition of the present invention may further contain a solubilizing component in addition to the above components, and by adding the solubilizing component, the stability of ascorbic acids in an aqueous solvent is further improved. be able to.

  Here, the solubilizing component is not particularly limited as long as it is used as a component of an external preparation in the pharmaceutical, quasi-drug or cosmetic field. For example, lower alcohols such as ethanol; polyhydric alcohols such as glycerin, ethylene glycol, and propylene glycol; other hydrogenated soybean phospholipids, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene lanolin alcohol, polyoxyethylene castor oil, poly Examples thereof include oxyethylene hydrogenated castor oil, polyoxyethylene sterol, polyoxyethylene alkyl ether, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene alkylphenyl ether, and the like. Preferably, ethanol, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, diethylene glycol, dipropylene glycol, hydrogenated soybean phospholipid, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene lanolin alcohol, polyoxyethylene castor oil , Polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, more preferably ethanol, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, diethylene glycol, dipropylene glycol, hydrogenated soybean phospholipid . These solubilizing components may be used alone or in any combination of two or more.

  When these solubilizing components are used, the blending ratio in the outer skin composition is not particularly limited as long as it does not affect the skin and mucous membranes and does not interfere with the effects of the present invention. It can be appropriately selected and used within a range such that it is contained in the product at a ratio of 0.01 to 80% by weight. From the viewpoint of the stability of ascorbic acids in the skin composition and the feeling on use of the skin, the range is preferably 0.1 to 70% by weight, more preferably 0.1 to 60% by weight. The blending ratio of the solubilizing component to 100 parts by weight of the glycol ether in the outer skin composition is 0.01 to 1000 parts by weight, preferably 0.01 to 500 parts by weight, from the viewpoint of improving the stability of ascorbic acids. Preferably the range of 0.01-250 weight part can be illustrated. Furthermore, the blending ratio of the solubilizing component to 100 parts by weight of ascorbic acids in the outer skin composition is 0.1 to 1000 parts by weight, preferably 1 to 1000 parts by weight, more preferably from the viewpoint of improving the stability of ascorbic acids. Can exemplify a range of 1 to 100 parts by weight.

  Since the composition for the outer skin of the present invention having the above configuration is an aqueous composition, it can be blended with water-soluble or highly water-soluble ascorbic acids in an effective amount or more in a ratio higher than the desired effect, And although it is an aqueous composition, ascorbic acids can be kept in a stable state. For this reason, the composition for the outer skin of the present invention has various actions of ascorbic acids to be incorporated (for example, an anti-inflammatory action, an acne improving action, a whitening action, an anti-aging action, an antioxidant action, an action for promoting the synthesis of biological components such as collagen, And the like can effectively exhibit cell damage and DNA damage-inhibiting effects caused by ultraviolet rays.

  The skin composition of the present invention has other whitening ingredients and anti-inflammatory ingredients for the purpose of enhancing or supplementing the various actions of ascorbic acids or for adding other useful actions to the skin composition. 1 type or 2 or more types of anti-wrinkle component, antibacterial component, cell activation component, astringent component, antioxidant component, acne improving component, anti-aging component, biological component synthesis promoting component such as collagen, blood circulation promoting component, moisturizing component It can mix | blend in combination. Each of these components is not particularly limited as long as it is conventionally used as a component of an external preparation in the pharmaceutical, quasi-drug, or cosmetic field, and is used in the future. Can do.

  For example, whitening ingredients include: placenta; arbutin; kojic acid; ellagic acid; phytic acid; chamomile ET; Lucille; vitamin A or a derivative thereof, vitamin E or a derivative thereof, vitamins such as pantothenic acid or a derivative thereof; ), Clove, turmeric, capsicum, pickaxe, aloe, aloe vera, tea, licorice, eel, camomile, soakakuhi, kakon, salamander, buttonpi, ginkgo, ages, auren, hypericum, gardenia, kujin, rice, rice bran , Cucumbers, sedgefish, tea, touki, kingweed, hamamelis, safflower, amethyst, azalea, enoki, oysters (Diospyros kaki), sage, radish, azalea, parsley, hops, and yokoinin Plant extracts and essential oils). Preferred are plant extracts and essential oils derived from aloe, iris (iris), aloe vera, tea, or chamomile, pantothenic acid or derivatives thereof, vitamin A or derivatives thereof, vitamin E or derivatives thereof, phytic acid or ellagic acid. These whitening components may be used alone or in combination of two or more.

  When using the said whitening component, the ratio to mix | blend with the composition for outer_layer | skins becomes like this. Preferably it is 0.0003 to 10 weight%, More preferably, it is 0.01 to 5 weight%. Further, the whitening component is 0.001 to 1000 parts by weight, preferably 0.005 to 500 parts by weight, more preferably 0.01 to 100 parts by weight with respect to 100 parts by weight of ascorbic acids contained in the outer skin composition. It is desirable to mix them so that they are included in proportions.

  Anti-inflammatory ingredients include ogon, arnica, licorice, buckwheat, eucalyptus, mint, achacha, aloe, enamel, barley, hypericum, hypericum perforatum, orange, chamomile, roman chamomile, sagebrush, gardenia, confetti, radish , Peonies, mint, senkyu, assembly, sage, peony, taiso, thyme, pearl millet, tonin, carrot, parsley, nettle, sandalwood, loquat, butcher bloom, grape, safflower, button, maroonier, peach, cornflower, mugwort, Anti-inflammatory plant components such as lavender, carrot and rosemary (eg plant extracts and essential oils); biotin, allantoin, calamine, glycyrrhizic acid and derivatives thereof; Acid and derivatives thereof; other, zinc oxide, guaiazulene, tocopherol acetate, pyridoxine hydrochloride, menthol, camphor, turpentine oil, indomethacin, and the like salicylic acid and derivatives thereof. Preferable are plant extracts and essential oils derived from dragonfly, licorice or buckwheat, allantoin, glycyrrhizic acid and derivatives thereof, glycyrrhetinic acid and derivatives thereof, guaiazulene and menthol.

  When using the said anti-inflammatory component, the ratio mix | blended with the composition for outer_layer | skins becomes like this. Preferably it is 0.0003 to 10 weight%, More preferably, it is 0.01 to 5 weight%. In addition, the anti-inflammatory component is a ratio of 0.001 to 1000 parts by weight, preferably 0.005 to 500 parts by weight, more preferably 0.01 to 100 parts by weight with respect to 100 parts by weight of ascorbic acids in the outer skin composition. It is desirable to blend so that

  Examples of the anti-wrinkle component include retinoids (retinol, retinoic acid, retinal, etc.), pangamic acid, kinetin, ursolic acid, turmeric extract, sphingosine derivatives, silicon, silicic acid, N-methyl-L-serine, mevalonolactone, and the like. Preferred are retinoid (retinol, retinoic acid, retinal, etc.) and kinetin.

  When using the said anti-wrinkle component, the ratio mix | blended with the composition for outer skins becomes like this. Preferably it is 0.0003 to 10 weight%, More preferably, it is 0.01 to 5 weight%. The anti-wrinkle component is 0.001 to 1000 parts by weight, preferably 0.005 to 500 parts by weight, more preferably 0.01 to 100 parts by weight, based on 100 parts by weight of ascorbic acids contained in the outer skin composition. It is desirable to mix | blend so that it may become a ratio.

  Antibacterial components include chlorhexidine, salicylic acid, benzalkonium chloride, acrinol, ethanol, benzethonium chloride, cresol, gluconic acid and derivatives thereof, popidone iodine, potassium iodide, iodine, isopropylmethylphenol, triclocarban, triclosan, photosensitizer 101 Photosensitive element 201, paraben, phenoxyethanol, 1,2-pentanediol, alkyldiaminoglycine hydrochloride and the like. In addition, mugwort, asparagus, aloe, ginkgo, turmeric, pear, enema, ogon, auren, hypericum, Hypericum perforatum, orange, pearwood, gardenia, kumazasa, clara, grapefruit, gentian, salamander, shiso Antibacterial effects such as honeysuckle, achillea millefolium, mint mint, cucumber, sage, sedgefish, thyme, clove, eucalyptus, buttons, hops, mint, peaches, eucalyptus, lavender, rosehip, rosemary, mugwort, peonies, ginger, sorghum Some plant components (such as plant extracts and essential oils) can also be used. Preferably, benzalkonium chloride, benzethonium chloride, gluconic acid and derivatives thereof, isopropylmethylphenol, triclocarban, triclosan, photosensitizer 101, photosensitizer 201, paraben, phenoxyethanol, 1,2-pentanediol, alkyldiamino hydrochloride Examples include glycine. More preferred are benzalkonium chloride, gluconic acid and its derivatives, benzethonium chloride, and isopropylmethylphenol.

  When using the said antibacterial component, the ratio mix | blended with the composition for outer skins becomes like this. Preferably it is 0.0003 to 10 weight%, More preferably, it is 0.01 to 5 weight%. Further, the antibacterial component is 0.001 to 1000 parts by weight, preferably 0.005 to 500 parts by weight, more preferably 0.01 to 100 parts by weight with respect to 100 parts by weight of ascorbic acids contained in the outer skin composition. It is desirable to mix them in proportions.

  Cell activation components include amino acids such as γ-aminobutyric acid and ε-aminoproic acid: vitamins such as retinol, thiamine, riboflavin, pyridoxine hydrochloride and pantothenic acids: α-hydroxy acids such as glycolic acid and lactic acid: tannin, flavonoids , Saponin, allantoin, photosensitizer No. 301: plant components (plant extracts, essential oils, etc.) such as kagome kombu, hibamata, wakame mekabu, lessonik, mozuku, and pebbles. Preferred are amino acids such as γ-aminobutyric acid and ε-aminoproic acid: vitamins such as retinol, thiamine, riboflavin, pyridoxine hydrochloride, tocopherol acetate and pantothenic acids.

  When the cell activation component is used, the proportion to be added to the outer skin composition is preferably 0.0003 to 10% by weight, more preferably 0.01 to 5% by weight. In addition, the cell activation component is 0.001 to 1000 parts by weight, preferably 0.005 to 500 parts by weight, more preferably 0.01 to 100 parts by weight with respect to 100 parts by weight of ascorbic acids contained in the outer skin composition. It is desirable to mix | blend so that it may become a ratio.

  Examples of the astringent component include metal salts such as alum, chlorohydroxyaluminum, aluminum chloride, allantoin aluminum salt, zinc sulfate, and aluminum potassium sulfate; organic acids such as tannic acid, citric acid, lactic acid, and succinic acid. Achacha, Aloe, Fennel, Ages, Hypericum perforatum, Odrianthus, Orange, Common wormwood, Raspberry, Kiwi, Gentian, Birch, Sage, Thyme, Tea, Grape, Hops, Maronier, Melissa, Cornflower, Artemisia, Apple, Lemon, Lenge It is also possible to use an astringent plant component (plant extract, essential oil, etc.) such as rosehip, honeysuckle, peony, and horsetail. Alum, chlorohydroxyaluminum, aluminum chloride, allantoin aluminum salt, aluminum potassium sulfate, and tannic acid are preferred.

  When the astringent component is used, the proportion to be added to the skin composition is usually 0.0003 to 10% by weight, preferably 0.01 to 5% by weight, more preferably 0.01 to 5% by weight. The astringent component is 0.001 to 1000 parts by weight, preferably 0.005 to 500 parts by weight, more preferably 0.01 to 100 parts by weight, based on 100 parts by weight of ascorbic acids contained in the outer skin composition. It is desirable to mix them in proportions.

  Antioxidant components include tocopherol and its derivatives, butylhydroxyanisole, dibutylhydroxytoluene, sodium bisulfite, erythorbic acid and its salts, flavonoids, glutathione, glutathione peroxidase, glutathione-S-transferase, catalase, superoxide dismutase, thioredoxin, Examples include taurine, thiotaurine, and hypotaurine. Achacha, Turmeric, Ages, Echinashi, Ogon, Hypericum, Gobaishi, Genposhi, Rice, Rice bran, Comfrey, Salamander, Perilla, Peonies, Soybean, Natto, Tea, Clove, Loquat, Button, Maronie, Yukinoshita, Rooibos Moreover, plant components (for example, plant extracts and essential oils) having an antioxidative effect such as rosemary, spirulina, chlorella and donariella can also be used. Preferred are tocopherol and its derivatives, thiotaurine, hypotaurine, thioredoxin, tea extract, and flavonoid.

  When the antioxidant component is used, the proportion to be added to the outer skin composition is usually 0.0001 to 10% by weight, preferably 0.0001 to 5% by weight, more preferably 0.001 to 5% by weight. The antioxidant component is 0.001 to 1000 parts by weight, preferably 0.005 to 500 parts by weight, more preferably 0.01 to 100 parts by weight, based on 100 parts by weight of ascorbic acids contained in the outer skin composition. It is desirable to mix | blend so that it may become a ratio.

  Blood circulation promoting ingredients include: Ashitaba, Arnica, Ginkgo, fennel, Enmeiso, Dutch oak, Chamomile, Roman chamomile, Carrot, Gentian, Burdock, Rice, Hawthorn, Shiitake, Hawthorn, Prunus, Senkyu, Assembly, Thyme, Clove, Chimpi , Spruce, Spruce, Spruce, Carrot, Garlic, Butcher Bloom, Grape, Button, Maronie, Melissa, Yuzu, Yokuinin, Rosemary, Rosehip, Chimpi, Spruce, Spruce, Peach, Apricot, Walnut, Corn, etc. Plant components (for example, plant extracts and essential oils) having

  When these blood circulation promoting components are used, the proportion to be blended in the outer skin composition is usually 0.00001 to 10% by weight, preferably 0.00001 to 5% by weight, more preferably 0.001 in terms of dry matter. 0001 to 4% by weight. In addition, the blood circulation promoting component is in a ratio of 0.0001 to 100 parts by weight, preferably 0.001 to 50 parts by weight, based on 100 parts by weight of ascorbic acids contained in the outer skin composition, in terms of dry matter. It is desirable to blend.

  As moisturizing ingredients, carrots, ginseng, aloe, nettle, fennel, witch hazel (hamamelis), turmeric, scallop (Ogon), yellowfin (weed), hypericum, rice (rice), chamomile, kawara mugi , Clara (Kujin), Grape, Gardenia, Comfrey (Herusiumus), Savonsou, Giant, Perilla, Peonies, Birch, Horsetail, Bodaige, Salvia (Sage), Assembly, Cyprus, Mulberry, Soybean, Ginger ), Toki, Tokinsenka, Parsley, Barley (Yokuinin), Butchiya's Bloom, Loofah, Hop, Maronie, Melissa, Peach, Yukinoshita, Raspberry, Lavender, Astragalus, Rose, Neubara (Ages), Rose Lee (Mannenrou), Licorice, Cha (Ryokucha, Kocha, Oolongcha), Lily, Barley (Mort Root), Wheat, Apricot (Noodle), Oats, Murasaki (Sicon), Lemon, Quince, Orange, Strawberry, Safflower, Gentian (Ryutan), peppermint, green pepper (spearmint), mint mint (peppermint), mugwort, eucalyptus, mandarin duck, pine, cornflower, walnut mushroom (jiyu), avocado, seaweed, grapefruit, prunes, lime, yuzu (kijitsu), auren, hinoki , Buttons (button pi), olives, sunflower (safflower), jojoba, macadamia nuts, medhome, camellia, almonds, cacao, sesame, and other moisturizing plant components (for example, plant extracts and essential oils) . In addition, the inside of () shows the kind of plant, an alias, or a herbal medicine name.

  When these moisturizing components are used, the proportion to be blended in the outer skin composition is usually 0.00001 to 10% by weight, preferably 0.00001 to 5% by weight, more preferably 0.0001 in terms of dry matter. ~ 4% by weight. Further, the moisturizing component is blended so as to be a ratio of 0.0001 to 100 parts by weight, preferably 0.001 to 50 parts by weight with respect to 100 parts by weight of ascorbic acids contained in the composition for the skin, in terms of dry matter. It is desirable to do.

  As described above, various effects (whitening action, anti-inflammatory action, anti-wrinkle action, antibacterial action, cell activation action, astringent action, antioxidant action, acne improving action, aging as optional active ingredients are included in the skin composition. Plant components (including plant extracts and essential oils) having an inhibitory action, an action of promoting the synthesis of biological components such as collagen, an action of promoting blood circulation, an action of moisturizing, and the like can be blended. When a plant component is used as an active ingredient, it is usually 0.00001 to 10% by weight, preferably 0.00001 to 5% by weight, more preferably 0.0001 to 4% by weight in terms of dry matter. It is desirable to blend in the skin composition. In addition, it is desirable that the plant component is blended at a ratio (in terms of dry matter) of 0.0001 to 100 parts by weight, preferably 0.001 to 50 parts by weight, with respect to 100 parts by weight of ascorbic acids contained in the outer skin composition. .

  In addition to the above-mentioned components, the skin composition of the present invention may further contain a surfactant, fats and oils, or a transdermal absorption promoting component.

  Examples of the surfactant used herein include POE-branched alkyl ethers such as polyoxyethylene (hereinafter referred to as POE) -octyldodecyl alcohol and POE-2-decyltetradecyl alcohol; POE-oleyl alcohol ether and POE-cetyl alcohol. POE-alkyl ethers such as ethers; sorbitan esters such as sorbitan monooleate, sorbitan monoisostearate and sorbitan monolaurate; POE-sorbitan monooleate, POE-sorbitan monoisostearate, and POE-sorbitan monolaurate POE-sorbitan esters such as glycerol; glycerol fatty acid esters such as glycerol monooleate, glycerol monostearate, and glycerol monomyristate; POE-glycerol monoo POE-cured fatty acid esters such as reate, POE-glycerin monostearate, and POE-glycerin monomyristate; POE-cured such as POE-dihydrocholesterol ester, POE-cured castor oil, and POE-cured castor oil isostearate Castor oil fatty acid ester; POE-alkyl aryl ether such as POE-octylphenyl ether; Glycerin alkyl ether such as monoisostearyl glyceryl ether and monomyristyl glyceryl ether; POE such as POE-monostearyl glyceryl ether and POE-monomyristyl glyceryl ether -Glycerin alkyl ethers; diglyceryl monostearate, decaglyceryl decastearate, decaglyceryl decaisostearate, and diglyceride Polyglycerol fatty acid esters such as Lil diisostearate, various nonionic surfactants and the like can be exemplified. These surfactants may be used alone or in any combination of two or more.

  When these surfactants are used, the blending ratio in the outer skin composition is not particularly limited as long as it does not affect the skin and mucous membranes and does not hinder the effects of the present invention. It can be appropriately selected and used within a range such that it is contained in a proportion of 0.01 to 70% by weight. From the viewpoints of the stability of ascorbic acids in the skin composition and the feeling of use on the skin, it is preferably 0.1 to 50% by weight, more preferably 0.5 to 20% by weight. The blending ratio of the surfactant to 100 parts by weight of the glycol ether contained in the outer skin composition is 0.01 to 1000 parts by weight, preferably 0.01 to 500 parts by weight, more preferably 0.1 to 250 parts by weight. The range of the part can be illustrated. Furthermore, as a compounding ratio of the surfactant with respect to 100 parts by weight of ascorbic acids contained in the outer skin composition, 0.1 to 1000 parts by weight, preferably 0.1 to 500 parts by weight, more preferably 0.1 to 0.1 parts by weight. A range of 100 parts by weight can be exemplified.

  The fats and oils are not particularly limited as long as they are used as components of external preparations in the field of pharmaceuticals, quasi drugs and cosmetics. For example, synthetic fats and oils such as medium chain fatty acid triglycerides; soybean oil, rice oil, rapeseed oil, cottonseed oil, sesame oil, safflower oil, castor oil, olive oil, cacao oil, coconut oil, sunflower oil, palm oil, flax oil, perilla oil, shea Vegetable oils such as oil, monkey oil, palm oil, tree wax, jojoba oil, grape seed oil, and avocado oil; animal oils such as mink oil, egg yolk oil, beef tallow, milk fat, and pork fat; beeswax, whale wax, lanolin Waxes such as carnauba wax and candelilla wax; hydrocarbons such as liquid paraffin, squalene, squalane, microcrystalline wax, ceresin wax, paraffin wax, petrolatum; lauric acid, myristic acid, stearic acid, oleic acid, isostearic acid, Natural and synthetic fatty acids such as behenic acid; cetanol, stearyl alcohol, hexylde Nord, octyldecanol, natural and synthetic higher alcohols such as lauryl alcohol; isopropyl myristate, isopropyl palmitate, octyldodecyl myristate, octyldodecyl oleate, esters and ethers such as cholesterol oleate; silicone oil, and the like. Preferably, soybean oil, rice oil, rapeseed oil, cottonseed oil, sesame oil, safflower oil, castor oil, olive oil, cacao oil, coconut oil, sunflower oil, palm oil, flax oil, perilla oil, coconut oil, jojoba oil, grape seed oil And vegetable liquid oils such as avocado oil. These fats and oils may be used alone or in any combination of two or more.

  When these oils and fats are used, the blending ratio in the outer skin composition is not particularly limited as long as it does not affect the skin and mucous membranes and does not interfere with the effects of the present invention. Can be appropriately selected and used within the range of 0.01 to 80% by weight. From the viewpoint of the stability of ascorbic acids in the skin composition and the feeling of skin use, the content is preferably 0.1 to 80% by weight, more preferably 0.1 to 60% by weight. Moreover, as a mixture ratio of fats and oils with respect to 100 parts by weight of glycol ether contained in the outer skin composition, 0.01 to 1000 parts by weight, preferably 0.1 to 800 parts by weight, more preferably 0.5 to 500 parts by weight. The range of the part can be illustrated. Furthermore, 0.1 to 1000 parts by weight, preferably 0.1 to 500 parts by weight, more preferably 0.1 to 100 parts by weight, as a blending ratio of fats and oils with respect to 100 parts by weight of ascorbic acids contained in the outer skin composition. The range of can be illustrated.

  The transdermal absorption promoting component is not particularly limited as long as it is used as a component of an external preparation in the pharmaceutical, quasi-drug, or cosmetic field. For example, urea; α-hydroxy acid such as lactic acid, fruit acid, glycolic acid; sulfur; β-hydroxy acid such as salicylic acid; oleic acid, undecanoic acid, octanol, nonanol, menthol, thymol, limonene, dimethyl sulfoxide (DMSO), Dodecylmethyl sulfoxide, dimethyl lacetamide, N, N-dimethylformamide, sodium lauryl sulfate, N, N-bis (2 hydroxy ethy) oleylamine, polyoxyethylene (20) sorbitan monooleate, Dodecyl dimethyl ammoniopropane sulfate, propylene glycol, polyethylene glycol , N, n-dimethyl-m-toluamide, DEET (diethyl-m-toluamide), Laurocapram, cyclodextrin, 1-dodecylazacycloheptan-2-one, isopropyl myristate, isopropyl palmitate, N-mono or disubstituted -P-menthan-3-ca Bokishiamido, 2- (2-methoxy-1-methylethyl) -5-methyl cyclohexanol - le, and azacycloalkane derivatives. Of these, urea, lactic acid, fruit acid, glycolic acid, salicylic acid, oleic acid, menthol, polyoxyethylene (20) sorbitan monooleate, and cyclodextrin are preferable. These percutaneous absorption enhancing components may be used alone or in any combination of two or more.

  When these percutaneous absorption enhancing components are used, they are contained in the outer skin composition in an amount of 0.0003 to 20% by weight, preferably 0.01 to 10% by weight, as a proportion of the outer skin composition. Such a range can be mentioned. Moreover, as a mixture ratio with respect to 100 weight part of ascorbic acids contained in the composition for outer skin, 0.001-1000 weight part, Preferably it is 0.001-300 weight part, More preferably, it is the range of 0.01-200 weight part. It can be illustrated.

  Furthermore, the composition for the outer skin of the present invention does not impair quality such as appearance stability and viscosity, and does not impair the effects of the present invention. Or various ingredients commonly used as components of external preparations in the cosmetics field, such as amino acids, irritation reducers, thickeners, preservatives, UV protection agents, colorants, dispersants, pH adjusters, fragrances, etc. can do. In addition, these components can be mix | blended individually by 1 type or in combination of 2 or more types.

  The outer skin composition of the present invention comprises the above ascorbic acids, water and glycol ether, and the above-mentioned optional components as necessary. Further, if necessary, other solvents and bases for commonly used external preparations. Etc. to prepare various desired forms such as paste, mousse, gel, liquid, emulsion, cream, sheet (for example, supported on a substrate), aerosol, spray, etc. Can do. These can be produced by conventional methods in the art.

  The outer skin composition of the present invention may usually have a liquidity of pH 2 to 8, but preferably has a pH of 2 from the viewpoints of stability of ascorbic acids, mild irritation to skin and mucous membranes, and good skin feeling. It is desirable that the acidity be ˜7, more preferably weakly acidic at pH 2.5-6.

  The skin composition of the present invention includes, for example, makeup cosmetics such as foundation, lipstick, mascara, eye shadow, eyeliner, eyebrow, and nail care; basic cosmetics such as emulsion, cream, lotion, oil and pack; Cleaning agents such as skin care, cleansing and body cleaning agents; anti-odorants, athlete's foot treatments, antipruritic agents, wound healing agents, cleaning agents, anti-inflammatory agents, anti-acne agents, anti-acne agents, anti-inflammatory agents, antiseptics, whitening Various external compositions belonging to the field of cosmetics, external medicines or external quasi-drugs, such as skin external preparations such as agents and UV protection agents. It is preferably used for basic cosmetics and external preparations for skin (preparation for skin) because of its action effect on the skin.

The present invention includes the following embodiments.
(1) An aqueous composition comprising at least one selected from the group consisting of i) ascorbic acid, an ester derivative thereof, an ether derivative thereof and a salt thereof, ii) water, and iii) a glycol ether.
(2) The aqueous composition according to (1), wherein the ester derivative of ascorbic acid is L-ascorbic acid monophosphate.
(3) The aqueous composition according to (3) or (2), wherein the glycol ether is at least one selected from the group consisting of diethylene glycol ether, monoethylene glycol ether, dipropylene glycol ether, and monopropylene glycol ether. .
(4) The glycol ether is at least one selected from the group consisting of diethylene glycol monoethyl ether, monoethylene glycol monoethyl ether, dipropylene glycol monoethyl ether, and monopropylene glycol monoethyl ether (1) to ( The aqueous composition according to any one of 3).
(5) The aqueous composition according to any one of (1) to (4), further containing a solubilizing component.
(6) Whitening component, anti-inflammatory component, anti-wrinkle component, antibacterial component, cell activation component, astringent component, antioxidant component, blood circulation promoting component, moisturizing component, anti-aging component, collagen synthesis promoting component, or acne improving component The aqueous composition according to any one of (1) to (5).
(7) As the above-mentioned whitening component, anti-inflammatory component, anti-wrinkle component, antibacterial component, cell activation component, astringent component, antioxidant component, blood circulation promoting component, moisturizing component, anti-aging component, collagen synthesis promoting component, or acne improving component The aqueous composition as described in (6) containing a plant component.
(8) The aqueous composition according to any one of (1) to (7), wherein the aqueous composition is at least one selected from the group consisting of foods, cosmetics, pharmaceuticals, and quasi drugs.
(9) The aqueous composition according to any one of (1) to (7), wherein the aqueous composition is an external preparation for skin.

(10) Ascorbic acid, an ester derivative thereof, an ether derivative thereof, or a salt thereof in an aqueous medium mixed with water and glycol ether, ascorbic acid, an ester derivative thereof, or a salt thereof, Method for stabilizing derivatives or their salts.
(11) The stabilization method according to (10), wherein the ester derivative of ascorbic acid is L-ascorbic acid monophosphate.
(12) The stabilization method according to (10) or (11), wherein the glycol ether is at least one selected from the group consisting of diethylene glycol ether, monoethylene glycol ether, dipropylene glycol ether, and monopropylene glycol ether. .
(13) The glycol ether is at least one selected from the group consisting of diethylene glycol monoethyl ether, monoethylene glycol monoethyl ether, dipropylene glycol monoethyl ether, and monopropylene glycol monoethyl ether (10) or ( The stabilization method as described in 11).
(14) The mixed aqueous solvent of water and glycol ether is such that the ratio of water to 1 part by weight of glycol ether is 0.1 to 3 parts by weight, particularly preferably 0.2 to 2 parts by weight. The stabilization method according to any one of (1).
(15) 0.01 to 100 parts by weight, preferably 0.01 to 50 parts by weight of ascorbic acid, an ester derivative thereof, an ether derivative thereof or a salt thereof with respect to 1 part by weight of glycol ether in the mixed aqueous solvent; The stabilization method according to any one of (10) to (14), more preferably 0.1 to 10 parts by weight, and still more preferably 0.2 to 0.8 parts by weight.

  In the skin composition of the present invention, ascorbic acids, water and glycol ether are in a coexisting state in the same system, so long as the ascorbic acids are not present. The ascorbic acid may be dissolved, dispersed or suspended in the skin composition, but at least a part, more preferably all ascorbic acid is dissolved in the skin composition. It is desirable that

  Hereinafter, the present invention will be described in more detail based on examples and test examples, but the present invention is not limited to these examples. In the following formulations,% means weight (W / W)% unless otherwise specified.

Example 1 Whitening lotion L-sodium ascorbate 20.0 (%)
Diethylene glycol monoethyl ether 30.0
Propylene glycol 20.0
Glycerin 5.0
Lactic acid 1.5
Iris Root Extract 0.01
Fragrance 0.1
Purified water 23.39
Total 100.00%.

Example 2 lotion L-ascorbic acid 10.0 (%)
Polyoxyethylene hydrogenated castor oil 1.0
Dipropylene glycol monoethyl ether 30.0
1,3-butylene glycol 5.0
Squalane 1.0
Rosemary oil 0.2
Fragrance 0.2
Purified water 52.6
Total 100.0%.

Example 3 Latex L-ascorbic acid diphosphate sodium salt 20.0 (%)
Stearic acid polyglyceride 1.0
Ethylene glycol monoethyl ether 40.0
Sodium lactate 0.1
Cetanol 2.0
Paraffin 0.5
Lavender oil 1.0
Chamomile extract 0.5
Purified water 34.9
Total 100.0%.

Example 4 Cream L-ascorbic acid-2-sulfonic acid ester 15.0 (%)
Propylene glycol monoethyl ether 30.0
Polyoxyethylene cetostearyl ether 1.5
Cetostearyl alcohol 2.0
Allantoin 0.1
Propylene glycol 5.0
Xanthan gum 0.1
Vaseline 10.0
Oat extract 0.1
Purified water 36.2
Total 100.0%.

Example 5 Spray cosmetic L-ascorbic acid 8.0 (%)
Ethylene glycol monopropyl ether 50.0
Ethanol 10.0
Aloe extract 0.01
Purified water 31.99
Total 100.00%.

Example 6 Skin L-Ascorbic acid-2-sulfate 5.0 (%)
Polyoxyethylene sorbitan fatty acid ester 1.0
Dipropylene glycol monopropyl ether 40.0
Jojoba oil 5.0
Hamamelis extract 0.01
Isopropyl methylphenol 0.05
Carboxyvinyl polymer 0.5
Triethanolamine 0.3
Purified water 48.14
Total 100.00%.

Example 7 Acne Lotion L-ascorbic acid triphosphate magnesium 15.0 (%)
1,3-butylene glycol 3.0
Diethylene glycol monoethyl ether 20.0
Benzalkonium chloride 0.5
Hamelis extract 0.1
Mukuroji extract 0.1
Ethanol 5.0
Fragrance 0.1
Menthol 0.01
Purified water 56.29
Total 100.0%.

Example 8 Cosmetic liquid L-ascorbic acid 15.0 (%)
Diethylene glycol monobutyl ether 60.0
Glycerin 5.0
Carrot extract 0.5
Purified water 19.5
Total 100.0%.

Example 9 Cosmetic liquid L-ascorbic acid 10.0 (%)
L-ascorbic acid monophosphate sodium salt 2.0
Diethylene glycol monoethyl ether 51.0
Propylene glycol 23.0
Aloe extract 2.0
Purified water 12.0
Total 100.0%.

Test Example 1 Effect of Glycol Ether on Ascorbic Acid Stability in Aqueous Medium 80 g of diethylene glycol monoethyl ether (DEGME) and 10 g of distilled water were mixed, and 10 g of L-ascorbic acid was added to this while stirring to add 10% ascorbine. An acid-containing DEGME (80%) + water (10%) mixed solution (referred to as “DEGME (80%) + water (10%) solution”) was prepared. Similarly, a 10% ascorbic acid-containing DEGME (45%) + water (45%) mixed solution (referred to as “DEGME (45%) + water (45%) solution”) was prepared. Further, as a comparative example, 10 g of L-ascorbic acid was added to 90 g of distilled water while stirring to prepare a 10% ascorbic acid-containing aqueous solution (referred to as “aqueous solution”).

  Ten ml of these solution samples were dispensed and sealed in brown ampule tubes and stored at 60 ° C. The content of ascorbic acid in each solution sample was measured before storage and 1, 5, and 9 days after storage, and the residual rate (%) of ascorbic acid was calculated. The content of ascorbic acid in the solution sample is 0.25 g from the solution sample, which is diluted with a mixture of methanol and mercaptoethanol (1000: 1), and this is used as a measurement sample for a reverse phase column (CAPCELL PAK Ph UG120, manufactured by Shiseido Co., Ltd.) (mobile phase: acetonitrile / 0.02 M phosphoric acid solution (pH 3.0) (1: 9), absorbance detection wavelength: 270 nm) in the solution. It was performed by measuring the amount of L-ascorbic acid contained in.

  The solution sample was diluted with a mixed solution of methanol and mercaptoethanol (1000: 1) to obtain a measurement sample for the following reason. That is, L-ascorbic acid quickly loses a hydrogen atom from the 2- and 3-position enol groups in the presence of water to form a keto isomer, dehydroascorbic acid, where dehydroascorbic acid and L-ascorbic acid Is in a reversible equilibrium state, and the dehydroascorbic acid has almost the same physiological activity as L-ascorbic acid. Therefore, in the measurement, dehydroascorbic acid was converted to L-ascorbic acid by placing the sample solution in the presence of mercaptoethanol as a reducing agent, and the total amount of both was measured as the amount of L-ascorbic acid.

  The results are shown in Table 1. In addition, ascorbic acid residual rate (%) is shown as a ratio of the ascorbic acid content in the solution sample after the storage when the ascorbic acid content in the solution sample before the storage is 100.

  As can be seen from the results in Table 1, the ascorbic acid aqueous solution in which ascorbic acid was mixed with a mixed solvent of diethylene glycol monoethyl ether (DEGME) and water did not decompose L-ascorbic acid even when stored under high temperature conditions. Excellent stability over a long period of time. This shows that ascorbic acid is stably held in an aqueous medium containing glycol ether (DEGME).

Claims (6)

i) at least one selected from the group consisting of ascorbic acid and salts thereof,
ii) water,
iii) glycol ethers, and
iv) ethanol, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, diethylene glycol, dipropylene glycol, hydrogenated soybean phospholipid, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene lanolin alcohol, polyoxyethylene castor oil, At least one solubilizing component selected from the group consisting of polyoxyethylene hydrogenated castor oil and polyoxyethylene alkyl ether (provided that only one propylene glycol is not selected)
A skin composition comprising:
A skin composition comprising the component i) in a proportion of 5 to 30% by weight in the skin composition. The skin composition according to claim 1, wherein the glycol ether is at least one selected from the group consisting of diethylene glycol ether, monoethylene glycol ether, dipropylene glycol ether, and monopropylene glycol ether. Glycol ether is ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, ethylene glycol monopropyl ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, diethylene glycol monopropyl ether, propylene glycol monoethyl ether, propylene glycol monopropyl ether, dipropylene glycol The composition for external use according to claim 2, which is at least one selected from the group consisting of monoethyl ether and dipropylene glycol monopropyl ether. The solubilizing component is at least one selected from the group consisting of ethanol, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, diethylene glycol, dipropylene glycol, and hydrogenated soybean phospholipid (provided that propylene glycol 1 The composition for an outer skin according to any one of claims 1 to 3, wherein only the seed is selected. The skin composition according to any one of claims 1 to 4, wherein the solubilizing component is contained in the skin composition at a ratio of 0.01 to 80% by weight. Furthermore, 1 or more types chosen from a whitening component, an anti-inflammatory component, an anti-wrinkle component, an antibacterial component, a cell activation component, an astringent component, an antioxidant component, fats and oils, and a percutaneous absorption promotion component are contained. The composition for outer skin in any one.