JP2017066080A - External composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an external composition that effectively inhibits melanogenesis to exhibit excellent skin-whitening effect.SOLUTION: Concurrent use of an ascorbic acid and/or a derivative thereof and an extract from plants of Magnoliaceae Magnolia dramatically enhances melanogenesis inhibitory action to show significantly excellent skin-whitening effect.SELECTED DRAWING: None

Description

  The present invention relates to an external composition that suppresses the production of melanin and exhibits an excellent whitening effect.

  Skin pigmentation such as freckles, freckles, dullness, darkening, liver spots, and senile pigment spots are caused by excessive exposure to melanin due to UV exposure, hormonal abnormalities and physical irritation. It has been found to be caused by deposition. Such skin pigmentation is a major cosmetic problem, especially for women.

  Conventionally, ascorbic acid and its derivatives are known to suppress skin pigmentation and have a whitening effect, and are widely used in external compositions for whitening. However, the current whitening effect of ascorbic acid and its derivatives cannot be said to satisfy consumer needs sufficiently.

  In addition, plant extracts that have a cosmetic effect are also known. For example, Patent Document 1 reports that a honoki extract has an action of inhibiting collagenase activity and is effective in preventing skin aging. Moreover, in Patent Document 2, it is reported that the enzymatic degradation product of prune has an action of suppressing phagocytosis and exhibits a whitening effect by suppressing the movement of melanin to the body surface. However, the cosmetic effect exhibited by the plant extract alone is slow, and there is a drawback that it cannot fully satisfy consumer needs.

  Consumer demand for whitening is increasing year by year, and the whitening effect obtained by conventional formulation technology cannot satisfy consumer demand. Therefore, in order to follow the increasing demands of consumers in the future, it is desired to develop a composition for external use that exhibits a more excellent whitening effect.

JP 2003-146876 A JP 2006-347926 A

  The objective of this invention is providing the composition for external use which shows the outstanding whitening effect by suppressing the production | generation of melanin effectively.

  The present inventor has intensively studied to solve the above-mentioned problems, and as a result, by using ascorbic acid and / or a derivative thereof together with an extract of a magnoliaceae magnolia plant, the production inhibitory effect of melanin is dramatically increased. It has been found that the whitening effect can be remarkably improved. Furthermore, it discovered that whitening effect improved further by combining the extract of a Rosaceae cherry tree genus plant with the said 2 component.

  Furthermore, by formulating the above-mentioned components together with a water-soluble thickener, porous powder, and trimethylglycine, in addition to having an excellent whitening effect, while applying, there is a firm feeling of application, It was found that stickiness was suppressed and there was a refreshing feel, and after application, powderiness was suppressed and an excellent moisturizing feeling was obtained.

The present invention has been completed by further studies based on these findings. That is, this invention provides the invention of the aspect hung up below.
Item 1. A composition for external use, comprising (A) ascorbic acid and / or a derivative thereof, and (B) an extract of a magnoliaceae magnolia plant.
Item 2. The composition for external use according to Item 1, further comprising (C) an extract of a Rosaceae genus Sakura plant.
Item 3. Item 3. The external composition according to Item 1 or 2, wherein the component (B) is an extract of honoki.
Item 4. Item 4. The composition for external use according to any one of Items 1 to 3, wherein the component (C) is an extract of prunes.
Item 5. Item 5. The external composition according to any one of Items 1 to 4, wherein the component (A) is ascorbic acid 2-glucoside.
Item 6. Item 6. The composition for external use according to any one of Items 1 to 5, which is for whitening.

  The composition for external use of the present invention has a high inhibitory action on melanin production, and can effectively prevent or improve pigmentation such as skin spots, freckles, dullness, darkening, liver spots, and senile pigment spots. In addition, in one aspect of the composition for external use of the present invention, while having a solid application feeling, stickiness is suppressed and there is a refreshing feel, and after application, powderiness is suppressed and excellent. A moisturizing feeling can be obtained, and a good feeling can be provided.

  The composition for external use of the present invention comprises ascorbic acid and / or a derivative thereof (sometimes referred to as (A) component), and an extract of a magnoliaceae magnolia plant (sometimes referred to as (B) component). It is characterized by containing. Hereinafter, the external composition of the present invention will be described in detail.

(A) Ascorbic acid and / or derivative thereof The composition for external use of the present invention contains ascorbic acid and / or a derivative thereof. Ascorbic acid and / or its derivatives are known components that have an antioxidant action and are known to have a whitening effect.

  The ascorbic acid and derivatives thereof used in the present invention are not particularly limited as long as they are pharmaceutically or cosmetically acceptable, and examples thereof include ascorbic acid; ascorbic acid 2-glucoside; ascorbic acid monostearate Ascorbic acid monopalmitate, ascorbic acid monoalkyl esters such as ascorbic acid monooleate; ascorbic acid monoesters such as ascorbic acid monophosphate and its magnesium salt; ascorbine such as ascorbic acid distearate, ascorbic acid dipalmitate, ascorbic acid dioleate Acid dialkyl esters; ascorbic acid diesters such as ascorbic acid diphosphate and its salts; ascorbic acid tristearate, ascorbic acid tripalmitate, ascorb Trialkyl esters such as acid triolate; Ascorbic acid triesters such as ascorbic acid triphosphate; 3-O-ethyl, 6-acetyl-ascorbic acid, 3-O-ethyl, 6-butylascorbic acid, 3 -O-ethyl, 6-lauroyl ascorbic acid, 3-O-ethyl, 6-palmitoyl ascorbic acid, 3-O-ethyl, 6-oleoyl ascorbic acid, 3-O-ethyl, 6-stearoyl ascorbic acid, 3- O-ethyl, 6-beherminoyl-ascorbic acid, etc. are mentioned. These ascorbic acid and derivatives thereof may be either L-form or D-form, and preferably L-form.

  These ascorbic acid and its derivative may be used individually by 1 type, and may be used in combination of 2 or more type. Among these ascorbic acids and derivatives thereof, from the viewpoints of stability, whitening effect and the like, preferably derivatives of ascorbic acid, and more preferably ascorbic acid 2-glucoside.

  The content of the component (A) in the external composition of the present invention may be appropriately set according to the formulation form of the external composition, for example, 0.1 to 10% by weight, preferably 0.3. -8 wt%, more preferably 0.5-7 wt%.

(B) Extract of magnoliaceae magnolia plant The composition for external use of the present invention contains an extract of magnolia magnolia plant together with ascorbic acid and / or a derivative thereof. Thus, by using ascorbic acid and / or a derivative thereof and an extract of the magnoliaceae magnolia plant, the melanin production inhibitory action is dramatically increased, and it is possible to achieve a remarkably excellent whitening effect. Become.

  An extract of a magnoliaceae magnolia plant can be obtained by performing a solvent extraction treatment using the magnolia magnolia plant as an extraction raw material.

  The magnoliaceae magnolia plant used as the raw material for extraction includes those listed in the “Primary Color World Plant Encyclopedia” (published on April 20, 1986, Hokuryukan Co., Ltd.). In particular, magnolia biloba, bow shunka, white magnolia, kobushi (Yamaararagi, kobushihajikami, imouebana), magnolia (mokurenge, shimokure), calahoo (Shinahonoki), magnolia sprengeri, hoonoshiwa, hoogoshino, hogoshinono, oga shiwa . Among these extraction raw material plants, one kind of plant may be used alone, or two or more kinds of plants may be used in combination. Among these extraction raw materials, honoki is preferred from the viewpoint of achieving a more excellent whitening effect.

  The magnoliaceae magnolia plant extract may be extracted from the bark of the plant, but the extraction target may be, in addition to the bark, flowers, ears, pericarps, fruits, stems as necessary. , Leaves, branches, branches and leaves, trunks, rhizomes, roots, seeds, and the like, and may be whole trees.

  Examples of the extraction solvent used in the solvent extraction treatment of magnoliaceae magnolia plants include, for example, water; lower alcohols having 1 to 5 carbon atoms such as methanol, ethanol, propanol, isopropyl alcohol, butanol, and isobutanol; propylene glycol And polyhydric alcohols such as 1,3-butylene glycol and glycerin; and mixtures thereof. Among these extraction solvents, preferably, water, a mixed solution of a lower alcohol having 1 to 5 carbon atoms and water, a mixed solution of polyhydric alcohol and water, more preferably a mixed solution of water, ethanol and water, 1, 3 -A mixed liquid of butylene glycol and water, and a mixed liquid of propylene glycol and water.

  When using a mixed solution of lower alcohol having 1 to 5 carbon atoms and / or polyhydric alcohol and water as an extraction solvent, the concentration of lower alcohol and / or polyhydric alcohol having 1 to 5 carbon atoms is not particularly limited. Is, for example, 20 to 90% by weight, preferably 30 to 85% by weight in total of the lower alcohol and / or polyhydric alcohol having 1 to 5 carbon atoms.

  The magnoliaceae magnolia plant extract is obtained by extracting the plant part to be extracted as it is or after drying, chopping, crushing, pressing, enzyme treatment, boiling or fermentation treatment with the extraction solvent. Can be obtained. As the solvent extraction treatment, a commonly used extraction method of plant extracts can be employed. Specifically, immersion methods such as cold immersion and digestion; a method of stirring under heating; or a percolation method Etc.

  The extract obtained by the solvent extraction treatment may be used in a liquid state, but may be used as a concentrate or a dried product by being subjected to a treatment such as concentration and drying, if necessary. Good. Further, after concentration or drying, the obtained concentrate or dried product may be purified by washing with a non-soluble solvent, or may be used by further dissolving or suspending it in a suitable solvent.

  Moreover, what can be obtained commercially easily can also be used as an extract of a magnoliaceae magnolia plant. Examples of the extract of honoki bark include “Falcolex Honoki B” and “Falcolex Honoki E” manufactured by Ichimaru Falcos Co., Ltd.

  The content of the component (B) in the external composition of the present invention may be appropriately set according to the formulation form of the external composition, for example, 0.00001 in terms of the dry weight of the component (B) More specifically, it is 0.00001 to 0.1% by weight. From the viewpoint of producing a more excellent whitening effect, the content of the component (B) in the external composition of the present invention is preferably 0.00005 to 0.05% by weight in terms of the dry weight of the component (B). More preferably, 0.0001 to 0.01% by weight is mentioned.

  Further, in the composition for external use of the present invention, the ratio of the component (A) and the component (B) is determined according to each content described above, but from the viewpoint of achieving a more excellent whitening effect, the component (A) 0.001 part by weight or more, preferably 0.001 to 1 part by weight, more preferably 0.005 to 0.5 part by weight, and still more preferably 0.001 part by weight or more in terms of dry weight of component (B) per 100 parts by weight. 01-0.1 weight part is mentioned.

(C) Extract of Rosaceae genus Sakura plant In the composition for external use of the present invention, in addition to (A) component and (B) component, extract of Rosaceae genus Sakura plant (denoted as (C) component) May also be included. When the extract of the Rosaceae genus Sakura plant is included together with the component (A) and the component (B), the whitening effect can be further improved.

  The extract of the Rosaceae genus Sakura can be obtained by performing a solvent extraction process using the Rosaceae genus Sakura as an extraction raw material.

  Examples of Rosaceae, which are used as raw materials for extraction, include those listed in “Primary Color World Plant Encyclopedia” (published on April 20, 1986, first edition published by Hokuryukan Co., Ltd.). Prunes (Prunus apricots), Apricots (Karamomo), Prunus Conradinae, Kasumi cherry (Keyama cherry), Choza cherry, Inu cherry, Uwamizu cherry, Yamazakura, Bean cherry (Fuji cherry), Weeping cherry (Itozakura), Niwaume (Plum) , Kanzan (Sekiyama), Oshima cherry, Miyazakura, Ume, Minesakukura, Bungouume, Chishimazakura, Peach, Edhigan (Ubahigan), Plum (Hatankyo), Oyamazakura, Limbo (Holly), Shiorizakura, Miyusakura Class (co cherry tree which flowers early), Someiyoshino, Bakuchinoki (erosion, Biranju) and the like. Among these extraction raw material plants, one kind of plant may be used alone, or two or more kinds of plants may be used in combination. Among these extraction raw materials, prunes are preferable from the viewpoint of further enhancing the effect of improving the whitening effect.

  The extract of the Rosaceae cherry genus plant only needs to be extracted from the flesh of the plant, but the plant part to be extracted includes fruit skin, seeds, etc., if necessary, in addition to the flesh. Also good.

  Moreover, as an extraction solvent used for the solvent extraction process of the Rosaceae cherry genus plant, for example, water; lower alcohols having 1 to 5 carbon atoms such as methanol, ethanol, propanol, isopropyl alcohol, butanol, isobutanol; propylene glycol 1,3-butylene glycol, 1,2-butylene glycol, 1,4-butylene glycol, 1,5-pentanediol, 1,2-pentanediol, 1,3-pentanediol, 1,4-pentanediol, And polyhydric alcohols such as 1,3,5-pentanetriol; phenoxyethanol, paraben, ethylparaben, methylparaben, propylparaben; and mixtures thereof. Among these extraction solvents, preferably, water, a mixed solution of polyhydric alcohol and water, a mixed solution of a lower alcohol having 1 to 5 carbon atoms and water, more preferably a mixture of water, 1,3-butylene glycol and water. Liquid.

  When using a mixed solution of lower alcohol having 1 to 5 carbon atoms and / or polyhydric alcohol and water as an extraction solvent, the concentration of lower alcohol and / or polyhydric alcohol having 1 to 5 carbon atoms is not particularly limited. Is, for example, 20 to 90% by weight, preferably 30 to 85% by weight in total of the lower alcohol and / or polyhydric alcohol having 1 to 5 carbon atoms.

  The extract of the Rosaceae cherry genus plant is the above extraction target plant part as it is or, if necessary, dried, shredded, crushed, pressed, enzymatically treated, boiled or fermented with the above extraction solvent. It is obtained by doing. In particular, in the present invention, it is desirable that the Rosaceae genus plant to be subjected to the extraction treatment is subjected to an enzyme treatment in advance. By using an enzyme-treated Rosaceae genus Sakura as an extraction raw material, it is possible to obtain an extract with an extremely high effect of improving the whitening effect.

  The enzyme used for the enzyme treatment of the Rosaceae genus plants may be any fibrinolytic enzyme capable of degrading fibrin in the pulp, and specifically includes cellulase, hemicellulase, pectinase and the like. These enzymes may be used individually by 1 type, and may be used in combination of 2 or more type.

  The enzyme treatment conditions are not particularly limited, and may be set within the range of the working temperature and working pH of the enzyme to be used, and may be performed until the enzymatic reaction proceeds so as to obtain a desired effect. The conditions which make it react for 3 to 24 hours at 20-45 degreeC are mentioned. After carrying out the enzyme treatment to the Rosaceae cherry genus plant, the enzyme may be deactivated by heating or the like, if necessary, and subjected to the solvent extraction treatment.

  As the solvent extraction treatment, a commonly used extraction method of plant extracts can be employed. Specifically, immersion methods such as cold immersion and digestion; a method of stirring under heating; or a percolation method Etc.

  The extract obtained by the solvent extraction treatment may be used in a liquid state, but may be used as a concentrate or a dried product by being subjected to a treatment such as concentration and drying, if necessary. Good. Further, after concentration or drying, the obtained concentrate or dried product may be purified by washing with a non-soluble solvent, or may be used by further dissolving or suspending it in a suitable solvent.

  In addition, as an extract of a Rosaceae genus Sakura plant or an enzyme-treated extract of a Rosaceae genus Sakura, a commercially available product can be used. For example, as an extract of prunes that have been enzymatically decomposed, “Cleaage” manufactured by Ichimaru Falcos Co., Ltd. can be mentioned.

  The content of the component (C) in the external composition of the present invention may be appropriately set according to the formulation form of the external composition, for example, 0.00001 in terms of the dry weight of the component (C) The weight percent or more, specifically low, may be 0.00001 to 0.1 wt%. From the viewpoint of further enhancing the effect of improving the whitening effect, the content of the component (C) in the composition for external use of the present invention is preferably 0.00005 to 0.01 weight in terms of the dry weight of the component (C). %, More preferably 0.0001 to 0.001% by weight.

  Further, in the composition for external use of the present invention, the ratio of the component (B) and the component (C) is determined according to each content described above, but from the viewpoint of achieving a more excellent whitening effect, (B) It is 1 part by weight or more, preferably 1 to 5000 parts by weight, more preferably 5 to 500 parts by weight, and still more preferably 5 to 5 parts by weight per 100 parts by weight (in terms of dry weight) of the component. 100 parts by weight, particularly preferably 10 to 100 parts by weight.

(D) Water-soluble thickener, (E) Porous powder, and (F) Trimethylglycine The composition for external use of the present invention includes a water-soluble thickener (denoted as component (D) in addition to the components described above. May be included), porous powder (sometimes referred to as (E) component), and trimethylglycine (sometimes referred to as (F) component). When these components (D) to (F) are included together with the above-mentioned components, in addition to the excellent whitening effect, the stickiness is suppressed while being firmly applied at the time of application, and refreshed. After application, it is possible to suppress the powderiness and to give an excellent moisturizing feeling.

  The water-soluble thickener is not particularly limited as long as it is pharmaceutically or cosmetically acceptable. For example, carboxyvinyl polymer, alkyl-modified carboxyvinyl polymer, cellulose gum, xanthan gum, hydroxypropyl methylcellulose, hydroxy Examples include ethyl cellulose, carboxymethyl cellulose, (acryloyldimethyltaurine ammonium / VP) copolymer, sodium polyacrylate, carrageenan, xanthan gum, sclerotium gum, polystyrene sulfonate, karaya gum, and pectin. Among these, carboxyvinyl polymer and alkyl-modified carboxyvinyl polymer are preferable from the viewpoint of more effectively improving a firm coating feeling and a moisturizing feeling.

  The strong ruruboxy vinyl polymer is a water-soluble vinyl polymer having a carboxyl group, and specifically has a cross-linked structure with allyl sucrose, allyl ether of pentaerythritol, etc. with acrylic acid and / or metaglylic acid as the main chain. It is a polymer.

  The alkyl-modified carboxyvinyl polymer is a polymer in which at least a part of the carboxyl group of the carboxyvinyl polymer is esterified with an alkyl group. In the alkyl-modified carboxyvinyl polymer, the alkyl group bonded by an ester bond may be either straight or branched. Moreover, although it does not restrict | limit especially about carbon number of the said alkyl group, For example, 8-35, Preferably 8-30 is mentioned.

  The molecular weight of the carboxyvinyl polymer and the alkyl-modified carboxyvinyl polymer is not particularly limited. For example, the viscosity at 20 ° C. of an aqueous solution (pH 6.5) dissolved so as to be 5% by weight is preferably 500 mPa · s or more. May be 500 to 100,000 mPa · s. Here, for the viscosity, in a B-type viscometer “TOKI SANGYO VISCOMETER TVB-10” (manufactured by Toki Sangyo Co., Ltd.), rotor: M3 (rotation speed: 20 rpm, time: 1 minute, unit: mPa · s) It is a value measured using.

  These water-soluble thickeners may be used individually by 1 type, and may be used in combination of 2 or more type. From the viewpoint of further improving the feeling of use described above, it is preferable to use a carboxyvinyl polymer and an alkyl-modified carboxyvinyl polymer in combination as a water-soluble thickener. When the carboxyvinyl polymer and the alkyl-modified carboxyvinyl polymer are used in combination, these ratios are not particularly limited. For example, the alkyl-modified carboxyvinyl polymer is preferably 1 to 10,000 parts by weight per 100 parts by weight of the carboxyvinyl polymer. Is 50 to 5000 parts by weight, more preferably 10 to 1000 parts by weight.

  A commercially available water-soluble thickener can also be used. For example, commercially available products of carboxyvinyl polymer include “AQPEC HV-501E” and “AQUP EC HV-505E” manufactured by Sumitomo Seika Co., Ltd .; “Carbopol 940” and “Carbopol 941” manufactured by Lubrizol Advanced Materials. “Carbopol 980”; “Hibiswaco 1103”, “Hibiswaco 1104”, “Hibiswaco 1105” manufactured by Wako Pure Chemical Industries, Ltd .; “Sintalen K”, “Sintalen L” manufactured by 3V Sigma, etc. It is done. Commercially available alkyl-modified carboxyvinyl polymers include “AQUPEC HV-501ER” manufactured by Sumitomo Seika Co., Ltd .; “Carpopol ultrez20”, “Carbopol ultrez21”, and “Carbopol 1342” manufactured by Lubrizol Advanced Materials. , “Carbopol ETD2020”, “Pemlen TR-1”, “Pemlen TR-2”, and the like.

  The content of the component (D) in the external composition of the present invention may be appropriately set according to the formulation form of the external composition, for example, 0.1 to 3% by weight, preferably 0.3. -2% by weight, more preferably 0.3-1.5% by weight. By satisfying such a content, it is possible to more effectively enhance the firm feeling of application and the moisturizing feeling after application due to the interaction with the components (E) and (F) described later.

  The porous powder is not particularly limited as long as it is pharmaceutically or cosmetically acceptable. For example, silica, talc, titanium oxide, my strength, zinc oxide, kaolin, barium sulfate, bismuth oxychloride. , Inorganic powders such as aluminum hydroxide, aluminum silicate, silicic anhydride, hydrous silicic acid, montmorillonite; polyester, polyethylene, polystyrene, methyl methacrylate resin, cellulose, nylon, copolymer of styrene and acrylic acid, polypropylene, Examples thereof include polymer powders such as vinyl chloride. These porous powders may be used alone or in combination of two or more.

  Among these porous powders, silica, mica, talc, nylon, and more preferably silica are preferable from the viewpoint of more effectively improving the feeling of stickiness during application and the refreshing feeling. .

The average particle size of the porous powder is not particularly limited, and examples thereof include 1 to 25 μm, preferably 3 to 20 μm, and more preferably 3 to 15 μm. Further, the oil absorption amount of the porous powder is not particularly limited, and examples thereof include 50 to 500 ml / 100 g, preferably 50 to 300 ml / 100 g, and more preferably 50 to 200 ml / 100 g. The specific surface area of the porous powder is not particularly limited, but is, for example, 30 to 1000 m ² / g, preferably 100 to 950 m ² / g, more preferably 200 to 800 m ² / g, and more preferably 200 to 600 m. ² / g. Here, the average particle diameter of the porous powder is an “arithmetic average value of particle diameters” defined in JIS Z 8901: 2006 “Test Powder and Test Particles”. The oil absorption of the porous powder is a value measured according to JIS K5101-13-1. The specific surface area of the porous powder is a BET specific surface area measured in accordance with JIS K6430 Appendix E.

  The content of the component (E) in the external composition of the present invention may be appropriately set according to the formulation form of the external composition, for example, 0.05 to 5% by weight, preferably 0.5 -3% by weight, more preferably 1-3% by weight.

  Trimethylglycine is a component that is widely used as an amino acid-based moisturizing agent in plants of sea urchins, seaweeds, fish, crustaceans and the like.

  Commercially available trimethylglycine can also be used. Specific examples of commercially available trimethylglycine include “AQUADUO AN-100” manufactured by Ajinomoto Co., Inc., “Aminocoat” manufactured by Asahi Kasei Chemicals Corporation, and the like.

  In the composition for external use of the present invention, when the components (D) to (F) are contained, the ratio of the component (D) to the component (F) is 0 (F) component per 1 part by weight of the component (D). .1-6 parts by weight is desirable. By satisfying such a ratio, it is possible to effectively impart a feeling of use at the time of application and after application. From the viewpoint of more effectively imparting a feeling of use after coating and after coating, the ratio of the component (D) to the component (F) is as follows. Preferably it is 1-4 weight part, More preferably, 1.5-4 weight part is mentioned.

  The content of the component (E) in the composition for external use of the present invention may be appropriately set so that the ratio of the component (D) and the component (F) described above can be satisfied.For example, the content of the component (D) If the amount is 0.1 to 3% by weight, the content of component (E) is 0.01 to 18% by weight, preferably 0.1 to 12% by weight, more preferably 0.15 to 12%. % By weight.

Polyhydric alcohol The composition for external use of the present invention may contain a polyhydric alcohol as necessary for the purpose of enhancing the moisturizing action.

  The polyhydric alcohol is not particularly limited as long as it is pharmaceutically or cosmetically acceptable. For example, propylene glycol, ethylene glycol, 1,3-butylene glycol, isoprene glycol, diethylene glycol, dipropylene glycol, Examples include glycerin. These polyhydric alcohols may be used individually by 1 type, and may be used in combination of 2 or more type. Among these polyhydric alcohols, 1,3-butylene glycol and glycerin are preferable.

  In the composition for external use of the present invention, when polyhydric alcohol is contained, the content may be appropriately set according to the type of polyhydric alcohol used, the formulation form of the composition for external use, etc. 0.01 to 30% by weight, preferably 0.1 to 20% by weight, and more preferably 1 to 20% by weight.

Composition for external use of the water present invention, to achieve the desired formulation, if necessary, may contain water as a base. In particular, when the components (D) and (F) described above are included, it is desirable to include water as a base for dissolving these components.

  In the composition for external use of the present invention, the content of water is not particularly limited, and for example, 10 to 99.5% by weight, preferably 10 to 98% by weight, more specifically, (D) and If the component (F) is contained, the water content is 25 to 95% by weight, preferably 35 to 95% by weight, and more preferably 45 to 95% by weight.

Other Components The composition for external use of the present invention may contain other pharmacological components as necessary in addition to the components described above. Examples of such pharmacological components include antihistamines (diphenhydramine, diphenhydramine hydrochloride, chlorpheniramine maleate, etc.), local anesthetics (lidocaine, dibucaine, methyl aminobenzoate, procaine, tetracaine, bupipacaine, mepipacaine, chloroprocaine). , Proparacaine, Meprilucaine or salts thereof, Orthocaine, Oxesasein, Oxypolyentoxydecane, Rohto extract, Percamine ase, Tesitdecitine Monoammonium, glycyrrhetinic acid, pyridoxine glycyrrhetinate, stearyl glycyrrhetinate, glycyrrhetin Glyceryl, glycyrrhetinic acid monoglucuronide, salicylic acid, methyl salicylate, glycol salicylate, indomethacin, ferbinac, diclofenac sodium, loxoprofen sodium, ufenamate, ibuprofen piconol, suprofen, bendazac, suprofen, bufexamac, etc., bactericides (benzarconium chloride) , Decalinium chloride, Benzethonium chloride, Cetylpyridinium chloride, Chlorhexidine chloride, Chlorhexidine gluconate, Isopropylmethylphenol, Ammonia water, Sulphadiazine, Lactic acid, Phenol, etc.), Skin protectants (Colodion, castor oil, etc.), Blood circulation promotion Agents (nonyl acid vanillyl amide, nicotinic acid benzyl ester, capsaicin, red pepper extract, etc.), refreshing Agent (menthol, camphor), vitamins (vitamin A, B, D, etc.), mucopolysaccharides (sodium chondroitin sulfate, glucosamine, hyaluronic acid, etc.) and the like.

  Moreover, in order to make the external composition of this invention into a desired formulation form, the base and the additive may be contained as needed. Such bases and additives are not particularly limited as long as they are pharmaceutically acceptable, but for example, aqueous bases such as lower alcohols (ethanol, isopropanol, etc.); oils (olive oil, safflower oil) , Soybean oil, camellia oil, corn oil, rapeseed oil, sunflower oil, cottonseed oil, peanut oil, lard, squalane, fish oil, etc.), mineral oil (liquid paraffin, paraffin, gelled hydrocarbon, petroleum jelly, etc.), waxes and waxes (Beeswax, carnauba wax, candelilla wax, ceresin, rice wax, microcrystalline wax, etc.), ester oil (isopropyl myristate, isopropyl adipate, diethyl sebacate, isopropyl sebacate, isopropyl palmitate, cetyl palmitate, ethyl oleate) , Tri 2-Echi Glyceryl hexanoate), fatty acid alkyl ester, fatty acid (stearic acid, oleic acid, palmitic acid, behenic acid, linoleic acid, lanolin, etc.), fatty acid ester (cetyl palmitate, isopropyl palmitate, ethyl linoleate, etc.), medium chain Fatty acid triglycerides, higher alcohols (stearyl alcohol, cetanol, behenyl alcohol, myristyl alcohol, oleyl alcohol, hexadecyl alcohol, lanolin alcohol, cholesterol, dihydrocholesterol, phytosterol, lauryl alcohol, cetostearyl alcohol, linoleyl alcohol, octyldodecanol, hexyldecanol, Isostearyl alcohol, etc.), cetyl 2-ethylhexanoate, silicone oil (dimethylpolysiloxa) Oily bases such as POE (10-50 mol) phytosterol ether, POE (10-50 mol) dihydrocholesterol ether, POE (10-50 mol) 2-octyldodecyl ether, POE (10-50) Mol) decyltetradecyl ether, POE (10-50 mol) oleyl ether, POE (2-50 mol) cetyl ether, POE (5-50 mol) behenyl ether, POE (5-30 mol) polyoxypropylene (5-5 mol) 30 mol) polyoxyethylene alkyl ethers such as 2-decyltetradecyl ether, POE (10 to 50 mol) polyoxypropylene (2 to 30 mol) cetyl ether, phosphoric acid / phosphate (POE cetyl ether phosphoric acid) Sodium), POE (20-60 mol) Sorbitan monooleate, POE (10-60 mol) sorbitan monoisostearate, POE (10-80 mol) glyceryl monoisostearate, POE (10-30 mol) glyceryl monostearate, POE (20-100 mol) Polyoxypropylene modified silicone, POE / alkyl modified silicone, polyethylene glycol monolaurate, polyethylene glycol monopalmitate, polyethylene glycol monostearate, polyethylene glycol dilaurate, polyethylene glycol dipalmitate, polyethylene glycol distearate, polyethylene glycol dioleate, Polyethylene glycol diricinoleate, polyoxyethylene hydrogenated castor oil (5-100), polysorbate (20-85), Surfactants such as lysine fatty acid esters (glyceryl monostearate), hydrogenated soybean phospholipid, hydrogenated lanolin alcohol, etc .; refreshing agents (menthol, camphor, borneol, mint water, mint oil, etc.), preservatives (methylparaben, Propylparaben, benzoic acid, sodium benzoate, sorbic acid, etc.), flavoring agents (citral, 1,8-shioner, citronellal, farnesol, etc.), coloring agents (tar pigments (brown 201, blue 201, yellow 4) , Yellow 403, etc.), cacao pigment, chlorophyll, aluminum oxide, etc.), pH adjuster (phosphoric acid, hydrochloric acid, citric acid, sodium citrate, succinic acid, tartaric acid, sodium hydroxide, potassium hydroxide, triethanolamine, Triisopropanolamine, etc.), wetting agent (dl-pyrrolidone) Sodium rubonate solution, D-sorbitol solution, macrogol, etc.), stabilizer (dibutylhydroxytoluene, butylhydroxyanisole, sodium edetate, sodium metaphosphate, L-arginine, L-aspartic acid, DL-alanine, glycine, Sodium erythorbate, propyl gallate, sodium sulfite, sulfur dioxide, chlorogenic acid, catechin, rosemary extract, etc.), antioxidant, UV absorber, chelating agent, adhesive, buffer, solubilizer, solubilizer And additives such as preservatives.

Formulation Form As long as the composition for external use is a preparation form that can be applied transdermally, the formulation form is not particularly limited, and is liquid, solid, semi-solid (cream, gel, ointment, paste) Any of these may be used. Further, the composition for external use of the present invention may be a non-emulsifying preparation such as an aqueous preparation or an oily preparation, or an emulsion preparation such as an oil-in-water emulsion preparation or a water-in-oil emulsion preparation.

  As a preparation form of the composition for external use, a liquid form or a cream form is preferably used from the viewpoint of more effective whitening effect.

  The external composition may be in any form of pharmaceutical preparation for skin external use, cosmetics, skin cleansing agents and the like as long as it is applied to the skin.

  Specific preparation forms of the external composition include liquids (including lotions, sprays, aerosols, and emulsions), water-soluble ointments, oily ointments, creams, foams, and gels. And skin external preparations such as patches; cosmetics such as ointments, creams, emulsions, lotions, lotions, packs and gels; and skin cleansing agents such as body shampoos, hair shampoos and rinses. Among these preparation forms, preferably a skin external medicine, more preferably a liquid or cream. These preparation forms can be prepared by formulating with additives according to the preparation form according to a known method described in the 16th revised Japanese Pharmacopoeia General Rules for Preparations.

Use The composition for external use of the present invention can suppress the production of melanin, and can prevent or improve skin spots, freckles, dullness, liver spots, senile pigment spots, darkening due to physical irritation, etc. It is suitably used as an external composition for whitening.

  EXAMPLES The present invention will be described more specifically with reference to the following examples, but the present invention is not limited to these examples.

The manufacturers of the main components used in the following test examples and formulation examples are as follows.
L-ascorbic acid 2-glucoside : trade name “AA2G” (manufactured by Hayashibara Co., Ltd.)
Honoki extract : Trade name “Falco Rex Honoki B” (Ichimaru Falcos Co., Ltd.), liquid, dry solid concentration 0.175% by weight, Honoki (Magnolia obovatta Thunberg (Magnoliaceae)) bark , 3-Butylene glycol aqueous solution obtained by solvent extraction treatment
Prune extract : trade name “Creage” (manufactured by Ichimaru Falcos), liquid, dry solid concentration of 7.78% by weight, prune (Prunus domestica Lindl. (Rosaceae)) pulp with fibrinolytic enzyme Extract obtained by adding water and 1,3-butylene glycol to those obtained by decomposition in
Artichoke leaf extract : trade name “Biobenefiti” (manufactured by Ichimaru Falcos), liquid, dry solid concentration 0.08% by weight, leaves of Cynara sclymus L. (Compositae) in ethanol solution Extract obtained by concentrating and drying the extract obtained by extraction and adding 1,3-butylene glycol solution
Himefuuro extract : Trade name “Princess Care” (manufactured by Ichimaru Falcos), liquid, dry solid concentration of 1% by weight, 1,3-butylene glycol solution from whole plant of Geranium robotium L. (Geraniaceae) Extract obtained by extraction
Alpinia katsuma seed extract : Trade name “Alpinia White” (Ichimaru Falcos Co., Ltd.), liquid, dry solid concentration 0.2 wt%, Alpinia katsumadai Hayata (Zingiberaceae) seeds in ethanol solution Extract obtained by concentrating extract obtained by extraction and adding 1,3-butylene glycol solution
Chimp extract : Trade name “Mandarin” (manufactured by Ichimaru Falcos), liquid, dry solid concentration 3% by weight, mandarin orange (Citrus reticulate Blanco (Rutaceae)), 1,3-butylene glycol solution Extract obtained by extraction with
Bilberry leaf extract : Trade name “Cure Berry” (manufactured by Ichimaru Falcos), liquid, dry solid concentration of 0.2% by weight, 1,3-butylene glycol from the leaves of bilberry (Vaccinium myrtillus L. (Ericaceae)) Extract obtained by extraction with solution
Carboxyvinyl polymer : Trade name “Carbopol 980” (manufactured by Lubrizol Advanced Materials)
Alkyl-modified carboxyvinyl polymer : trade name “Carbopol ultraz20” (manufactured by Lubrizol Advanced Materials, carbon number of alkyl group: 10-30)
Silica : Trade name “God Ball D-25C” (manufactured by Suzuki Yushi Kogyo Co., Ltd.), average particle size 7 to 10 μm, specific surface area 300 to 500 m ² / g, oil absorption 70 to 110 ml / 100 g

Test Example 1: Evaluation of melanin production inhibitory effect The melanin production inhibitory effect was evaluated using a three-dimensional cultured skin model (MEL-300-A, manufactured by MatTek). The specific test method is as follows.

A MEL-300 skin model cup was set in each well of a 6-well plate containing 0.9 ml of maintenance medium (EPI-100LLMM) warmed to 37 ° C., and placed in an incubator (37 ° C., 5% CO ₂ ) for 1 hour. Left to stand. Next, 50 μl of each sample solution (pH 6.5) having the composition shown in Tables 1 and 2 was added to the inside of the skin model cup and cultured in an incubator (37 ° C., 5% CO ₂ ) for 24 hours. Thereafter, ultraviolet (UV-B) irradiation was performed under the condition of 0.5 mW × 12 seconds per time, and further cultured for 24 hours. In addition, ultraviolet irradiation was performed using a UVB lamp (Toshiba Lighting & Technology Corp., Toshiba Health Line fluorescent lamp) and a UV detector (TOPCON, UV-1). Thereafter, the medium was changed and further cultured for 24 hours. Each time the medium was changed, 50 μl of a predetermined sample solution was added to the skin model cup. Furthermore, ultraviolet irradiation and medium exchange were repeated four times under the same conditions, so that ultraviolet irradiation was performed five times in total (total ultraviolet irradiation amount 30 mJ / cm ² ), and medium replacement was performed five times in total. Thereafter, cell viability and melanin production were measured by the methods described below. Further, as a control, an aqueous solution containing 0.5% by weight of 1,3-butylene glycol was used as a sample solution, and the test was performed under the same conditions as described above.

<Measurement of cell activity>
Cell viability was measured by MTT test. Specifically, 0.75 ml of MTT test drug and 8.25 ml of maintenance medium (EPI-100LLMM) were mixed and added to 300 μl per well. The skin model cup was transferred to the medium containing MTT prepared above and cultured in an incubator for exactly 3 hours. Thereafter, the bottom surface of the tissue was gently washed with PBS washing solution and transferred to a new plate. 0.04N HCl acidic isopropanol was added to the inside of the skin model cup in an amount of 1 ml, and blue formazan was extracted in an incubator overnight with a cover seal attached to the plate to prevent evaporation. After extraction, the isopropanol was mixed well and 200 μl was transferred to a 96-well plate. The optical densities at 570 nm and 620 nm were measured with a microplate reader, and the difference between them was taken as the cell activity.

<Measurement of melanin production>
After washing the MEL-300 skin model cup with PBS, the cell tissue was peeled off with a scalpel and collected. The obtained cell tissue was immersed in PBS, and crushed and centrifuged (2,000 rpm, 10 minutes). Thereafter, the supernatant was removed, and a mixed solution of ethanol and dimethyl ether (ethanol: dimethyl ether = 3: 1 (volume ratio)) was added, followed by stirring and centrifugation (2,000 rpm, 10 minutes). The supernatant was then removed and dried. A 1N aqueous sodium hydroxide solution (containing 10% by weight DMSO) was added to the dried product, treated in a water bath at 90 ° C. for 20 minutes, and heated to melt. Thereafter, the heated and melted solution was gently stirred by vortexing and cooled to room temperature, and then the absorbance at 405 nm was measured to determine the amount of melanin produced.

  The amount of melanin produced per cell was determined by dividing the amount of melanin produced by the cell viability. Furthermore, assuming that the amount of melanin produced per cell of control was 100, the ratio of the amount of melanin produced per cell (melanin production ratio) when each sample solution was added was calculated.

  The obtained results are shown in Tables 1 and 2. As a result, the honoki extract alone (Comparative Example 2) did not show the melanin production inhibitory effect, and the ascorbic acid 2-glucoside alone (Comparative Example 1) had an insufficient melanin production inhibitory effect. In addition, ascorbic acid 2-glucoside and plant extracts with known melanin production inhibitory effects (prunes extract, chimpi extract, artichoke leaf extract, bilberry leaf extract, alpinia katsumadai seed extract, himefuuro extract ) Were combined (Comparative Examples 3 to 8), almost no enhancement of the melanin production inhibitory effect was observed.

  On the other hand, when ascorbic acid 2-glucoside and a honoki extract were combined (Examples 1-11), the melanin production inhibitory effect was increasing markedly. Furthermore, when the prune extract was combined with the ascorbic acid 2-glucoside and the honoki extract (Examples 4 to 8), a dramatic improvement in the melanin production inhibitory effect was observed. On the other hand, prunes can be obtained by combining scorbic acid 2-glucoside and honoki extract with other plant extracts (artichoke leaf extract, himefuuro extract, alpinia katsudai seed extract) that are known to suppress melanin production. The improvement of the melanin production inhibitory effect was not recognized as in the case of the extract.

Test Example 2: Evaluation of use feeling Skin cosmetics (solutions) having the compositions shown in Tables 3 and 4 were prepared. Specifically, the manufacturing procedure is as follows. A carboxyvinyl polymer and an alkyl-modified carboxyvinyl polymer were stirred and dissolved in purified water, and then glycerin was added and dissolved by stirring to obtain Preparation A. Separately, trimethylglycine and / or silica was added to 1,3-butylene glycol, and the mixture was stirred and homogenized to obtain Preparation B. Then, while stirring the preparation A, the preparation B was added, and the mixture was stirred with a homomixer and homogenized. Further, after adjusting the pH to 6.5 by adding potassium hydroxide, L-ascorbic acid 2-glucoside, honoki extract, and prune extract are added and stirred to homogenize the skin cosmetic. Prepared.

  About each obtained skin cosmetics, the firm application feeling at the time of application | coating, the non-stickiness feeling and the refreshing feeling, the non-powder-like feeling after application | coating, and the heat retention feeling were evaluated with the following method.

Ten evaluation monitors apply about 0.5g of each skin cosmetic to the arm, and a firm application feeling at the time of application, no stickiness and refreshing feeling, and no powderiness after application and moisturizing The feeling was evaluated. Specifically, the evaluation was scored by conducting a questionnaire based on Visual Analogue Scale (hereinafter sometimes referred to as VAS) with “1” and “10” as follows. The questionnaire results were averaged, and the evaluation results were summarized by rounding off the first decimal place.
<During application>
・ A feeling of application that feels tangled / No feeling of application that crushes the gel “1”
"10" with a feeling of application that entangles / apply that crushes the gel
・ "1" that there is no refreshing feeling
"10" has a refreshing feeling
・ "1" that feels sticky
"10" which does not feel sticky
<30 seconds after application>
・ "1" to feel the powderiness
"10" which does not feel powdery
・ "1" without moisturizing feeling (moist feeling)
"10" with moisturizing feeling (moist feeling)

  The results obtained are shown in Tables 3 and 4. In addition to ascorbic acid 2-glucoside, honoki extract and prune extract, water-soluble thickener (carboxyvinyl polymer, alkyl-modified carboxyvinyl polymer), silica, and trimethylglycine provide a firm feel The results were satisfactory in terms of lack of stickiness, refreshment, lack of powderiness and moisturizing feeling. In particular, when trimethylglycine satisfies 0.1 to 6 parts by weight with respect to 1 part by weight of the water-soluble thickener, a solid coating feeling, no stickiness, a refreshing feeling, no powderiness and The moisturizing feeling was a very good result.

Formulation Examples 1-9
According to the formulation described in Table 5, skin cosmetics were prepared by a conventional method (Prescription Examples 1 to 6 were pH 6.5, and Formulation Examples 7 to 9 were pH 4.5).

Formulation Examples 10-15
According to the formulation described in Table 6, skin cosmetics were prepared by the following procedure.
Step (1): L-ascorbic acid 2-glucoside or L-ascorbyl magnesium phosphate was dissolved in purified water, and then the pH was adjusted to 6 with a solution of potassium hydroxide dissolved in purified water (preparation (A -1)).
Step (2): (B) and (C) were dissolved under heating and stirring (Preparation (B) and Preparation (C)).
Step (3): The preparation (C) was added while stirring the preparation (B), and the mixture was stirred and homogenized with a homomixer.
Step (4): After that, the mixture was gradually cooled to 40 ° C. or lower while stirring, and the remainder of the preparations (A-1) and (A) were added to homogenize and prepare a skin cosmetic.

Claims (6)

  A composition for external use, comprising (A) ascorbic acid and / or a derivative thereof, and (B) an extract of a magnoliaceae magnolia plant.   Furthermore, the composition for external use of Claim 1 containing the extract of the (C) Rosaceae cherry genus plant.   The composition for external use according to claim 1 or 2, wherein the component (B) is an extract of honoki.   The external composition according to any one of claims 1 to 3, wherein the component (C) is an extract of prunes.   The external composition in any one of Claims 1-4 whose said (A) component is ascorbic acid 2-glucoside.   The composition for external use in any one of Claims 1-5 which is an object for whitening.