JP6807636B2 - Topical composition - Google Patents

Description

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

Pigmentation of skin stains, freckles, dullness, darkening, chloasma, senile pigmented spots, etc. causes excessive formation of melanin due to exposure to ultraviolet rays, hormonal abnormalities, physical irritation, etc. It is known to be caused by deposition in. Such skin pigmentation is a major cosmetic problem, especially for women.

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

In addition, some plant extracts have a cosmetic effect. For example, in Patent Document 1, it is reported that Magnolia obovata extract has an action of inhibiting collagenase activity and is effective in preventing skin aging. Further, in Patent Document 2, it is reported that an enzymatically decomposed product of prunes has an action of suppressing phagocytosis and suppresses the movement of melanin pigment to the body surface to exert a whitening effect. However, the cosmetic effect exerted by the plant extract alone is slow, and there is a drawback that the consumer needs cannot be fully satisfied.

Consumers' demands for whitening are increasing year by year, and the whitening effect obtained by conventional formulation technology cannot satisfy consumers' demands. Therefore, in order to meet the ever-increasing demands of consumers in the future, it is desired to develop an external composition having a more excellent whitening effect.

Japanese Unexamined Patent Publication No. 2003-146876 Japanese Unexamined Patent Publication No. 2006-347926

An object of the present invention is to provide an external composition having an excellent whitening effect by effectively suppressing the production of melanin.

As a result of diligent studies to solve the above-mentioned problems, the present inventor has found that ascorbic acid and / or a derivative thereof can be used in combination with an extract of a plant belonging to the genus Magnolia of the Magnolia family to dramatically suppress the production of melanin. It was found that it can produce a remarkably excellent whitening effect. Furthermore, it has been found that the whitening effect is further improved by combining the above two components with an extract of a plant belonging to the genus Plum of the Rosaceae family.

Furthermore, by formulating the above-mentioned components together with a water-soluble thickener, a porous powder, and trimethylglycine, an excellent whitening effect can be obtained, and at the time of application, there is a firm application feeling. It has been found that stickiness is suppressed and a refreshing feel is obtained, powderiness is suppressed after application, and an excellent moisturizing feeling can be obtained.

The present invention has been completed by further studies based on these findings. That is, the present invention provides the inventions of the following aspects.
Item 1. A composition for external use, which comprises (A) ascorbic acid and / or a derivative thereof, and (B) an extract of a plant belonging to the genus Magnolia of the Magnolia family.
Item 2. Item 2. The external composition according to Item 1, further comprising (C) an extract of a plant belonging to the genus Plum of the Rosaceae family.
Item 3. Item 2. The external composition according to Item 1 or 2, wherein the component (B) is an extract of Magnolia obovata.
Item 4. Item 2. The external composition according to any one of Items 1 to 3, wherein the component (C) is an extract of prunes.
Item 5. Item 2. The external composition according to any one of Items 1 to 4, wherein the component (A) is ascorbic acid 2-glucoside.
Item 6. Item 8. The external composition according to any one of Items 1 to 5, which is used for whitening.

The external composition of the present invention has a high effect of suppressing the production of melanin, and can effectively prevent or improve pigmentation such as skin spots, freckles, dullness, darkening, chloasma, and senile pigmented spots. Further, in one aspect of the external composition of the present invention, while having a firm coating feeling, stickiness is suppressed and there is a refreshing feel, and after coating, powderiness is suppressed and excellent. A moisturizing feeling can be obtained, and a good feeling of use can be provided.

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

(A) Ascorbic acid and / or its derivative The external composition of the present invention contains ascorbic acid and / or its derivative. Ascorbic acid and / or its derivative is a known component having an antioxidant effect and a known whitening effect.

The ascorbic acid and its derivatives used in the present invention are not particularly limited as long as they are pharmaceutically or cosmetically acceptable, and for example, ascorbic acid; ascorbic acid 2-glucoside; ascorbic acid monostearate. , Ascorbic acid monoalkyl esters such as ascorbic acid monopalmitate and ascorbic acid monooleate; ascorbic acid monoesters such as ascorbic acid monophosphate ester and its magnesium salt; ascorbic acid distearate, ascorbic acid dipalmitate, ascorbic acid diolate and the like Acid dialkyl esters; ascorbic acid diesters such as ascorbic acid diphosphate ester and salts thereof; trialkyl esters such as ascorbic acid tristearate, ascorbic acid tripalmitate, ascorbic acid triolate; ascorbic acid triphosphates and the like Ascorbic acid triesters; 3-O-ethyl, 6-acetyl-ascorbic acid, 3-O-ethyl, 6-butylascorbic acid, 3-O-ethyl, 6-lauroyl ascorbic acid, 3-O-ethyl, 6 Examples thereof include -palmitoyl ascorbic acid, 3-O-ethyl, 6-oleyl ascorbic acid, 3-O-ethyl, 6-stearoyl ascorbic acid, 3-O-ethyl, 6-beherminoyl-ascorbic acid and the like. These ascorbic acid and its derivatives may be either L-form or D-form, but L-form is preferable.

These ascorbic acid and its derivatives may be used alone or in combination of two or more. Among these ascorbic acid and its derivatives, a derivative of ascorbic acid is preferable, and ascorbic acid 2-glucoside is more preferable, from the viewpoint of stability and whitening effect.

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, etc., and is, for example, 0.1 to 10% by weight, preferably 0.3. -8% by weight, more preferably 0.5-7% by weight.

(B) Extract of Magnolia family Magnolia plant The external composition of the present invention contains an extract of Magnolia family Magnolia plant together with ascorbic acid and / or a derivative thereof. In this way, by using ascorbic acid and / or a derivative thereof in combination with an extract of a plant belonging to the genus Magnolia of the Magnolia family, the effect of suppressing the production of melanin is dramatically enhanced, and it is possible to achieve a remarkably excellent whitening effect. Become.

An extract of a Magnolia family Magnolia plant can be obtained by performing a solvent extraction treatment using a Magnolia family Magnolia plant as an extraction raw material.

Examples of Magnolia magnolia plants used as extraction raw materials include those listed in the "Primary Color World Botanical Encyclopedia" (first edition published on April 20, 1986, Kitatakakan Co., Ltd.). Magnolia magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia, magnolia .. From 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, Magnolia obovata is preferably mentioned from the viewpoint of exerting an even more excellent whitening effect.

The extract of the Magnolia family Magnolia genus plant may be extracted from the bark of the plant, but the site to be extracted is not only the bark but also flowers, spikes, fruit bark, fruits and stems as needed. , Leaves, branches, branches and leaves, trunks, bark, roots, seeds and the like may be included, and may be a whole tree.

Examples of the extraction solvent used for the solvent extraction treatment of plants of the genus Mokuren of the family Mokuren include water; lower alcohols having 1 to 5 carbon atoms such as methanol, ethanol, propanol, isopropyl alcohol, butanol, and isobutanol; and propylene glycol. Polyhydric alcohols such as 1,3-butylene glycol and glycerin; and mixtures thereof and the like can be mentioned. Among these extraction solvents, preferably water, a mixed solution of lower alcohol and water having 1 to 5 carbon atoms, a mixed solution of polyhydric alcohol and water, and more preferably water, a mixed solution of ethanol and water, 1, 3 -A mixture of butylene glycol and water, and a mixture of propylene glycol and water can be mentioned.

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

The extract of the Magnolia family Magnolia genus plant is obtained by extracting the plant part to be extracted as it is or, if necessary, dried, shredded, crushed, squeezed, enzyme-treated, boiled or fermented with the above-mentioned extraction solvent. Obtained by As the solvent extraction treatment, a commonly used method for extracting a plant extract can be adopted. Specifically, a dipping method such as cold immersion or warm immersion; a method of stirring under warming; or a percolation method. And so on.

The extract obtained by the solvent extraction treatment may be used in a liquid state, or may be used as a concentrate or a dried product by subjecting it to treatments such as concentration and drying, if necessary. Good. Further, after concentration or drying, the obtained concentrate or dried product may be washed with an insoluble solvent to be purified and used, or this may be further dissolved or suspended in a suitable solvent for use.

In addition, as an extract of a plant belonging to the genus Magnolia of the Magnolia family, a commercially available extract can be conveniently used. For example, examples of the bark extract of Magnolia obovata include "Falcolex Magnolia B" and "Falcolex Magnolia 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, etc., but for example, 0.00001 in terms of dry weight of the component (B). It is by weight% or more, and specific examples thereof include 0.00001 to 0.1% by weight. From the viewpoint of producing an even 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.

Further, in the external composition of the present invention, the ratio of the component (A) to the component (B) is determined according to each of the above-mentioned contents, but the component (A) is obtained from the viewpoint of producing an even more excellent whitening effect. In terms of dry weight of the component (B) per 100 parts by weight, 0.001 parts by weight or more, preferably 0.001 to 1 part by weight, more preferably 0.005 to 0.5 parts by weight, still more preferably 0. 01 to 0.1 parts by weight can be mentioned.

(C) Extract of Rosaceae Plums In addition to the components (A) and (B), the external composition of the present invention shall be referred to as the extract of Rosaceae Plums ((C) component). Also) may be included. When an extract of a plant belonging to the genus Plum of the Rosaceae family is contained together with the components (A) and (B), the whitening effect can be further improved.

An extract of a Rosaceae Plum can be obtained by subjecting a solvent extraction treatment using a Rosaceae Plum as an extraction raw material.

Examples of plants belonging to the genus Prunus speciosa used as raw materials for extraction include those listed in the "Primary Color World Plant Encyclopedia" (first edition published on April 20, 1986, Kitatakakan Co., Ltd.). Prunus (Yoshino cherry), Anzu (Rosaceae), Prunus conradinae, Prunus verecunda (Keyama cherry), Prunus verecunda, Inuzakura, Uwamizuzakura, Yamazakura, Mamezakura (Fujizakura), Shidarezakura (Itozakura), Niwaume (Koume) , Kanzan (Sekiyama), Oshimazakura, Miyamazakura, Ume, Minezakura, Bungoume, Chishimazakura, Momo, Edohigan (Ubahigan), Sumomo (Hatankyo), Oyamazakura, Rinboku (Hiragigashi), Shiurizakura (Miyamaizakura) Higanzakura), Somei Yoshino, Bakuchinoki (Vilan, Vilange) and the like. From 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 preferably mentioned from the viewpoint of further enhancing the whitening effect improving effect.

The extract of a plant belonging to the genus Plum of the Rosaceae family may be extracted from the flesh of the plant, but the plant part to be extracted includes not only the flesh but also the peel, seeds and the like, if necessary. May be good.

Examples of the extraction solvent used for solvent extraction treatment of plants belonging to the genus Sakura of the family Rose are water; lower alcohols having 1 to 5 carbon atoms such as methanol, ethanol, propanol, isopropyl alcohol, butanol, and 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, Polyhydric alcohols such as 1,3,5-pentantriol; phenoxyethanol, paraben, ethylparaben, methylparaben, propylparaben; and mixtures thereof and the like can be mentioned. Among these extraction solvents, water, a mixture of polyhydric alcohol and water, a mixture of lower alcohol having 1 to 5 carbon atoms and water, and more preferably water, a mixture of 1,3-butylene glycol and water are preferable. Liquid is mentioned.

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

The extract of the Rosaceae Plum genus is obtained by extracting the plant part to be extracted as it is, or, if necessary, drying, shredding, crushing, squeezing, enzyme-treating, boiling or fermenting the plant with the above-mentioned extraction solvent. Obtained by doing. In particular, in the present invention, it is desirable that the Rosaceae Plum genus plant to be subjected to the extraction treatment is subjected to the enzyme treatment in advance. By using an enzyme-treated plant belonging to the genus Plum of the Rosaceae family as an extraction raw material, it becomes possible to obtain an extract having a significantly higher effect of improving the whitening effect.

The enzyme used for the enzyme treatment of plants of the genus Plum of the Rosaceae family may be any fibrinolytic enzyme capable of decomposing fibrinoide in fruit flesh, and specific examples thereof include cellulase, hemicellulase, and pectinase. These enzymes may be used alone or in combination of two or more.

The enzyme treatment conditions are not particularly limited, and may be set within the range of the action temperature and the action pH of the enzyme to be used, and may be carried out until the enzyme reaction proceeds so that the desired effect can be obtained. Conditions include a condition of reacting at 20 to 45 ° C. for 3 to 24 hours. After the plant of the genus Plum of the Rosaceae is treated with the enzyme, the enzyme may be inactivated by heating or the like, if necessary, and subjected to the solvent extraction treatment.

As the solvent extraction treatment, a commonly used method for extracting a plant extract can be adopted. Specifically, a dipping method such as cold immersion or warm immersion; a method of stirring under warming; or a percolation method. And so on.

The extract obtained by the solvent extraction treatment may be used in a liquid state, or may be used as a concentrate or a dried product by subjecting it to treatments such as concentration and drying, if necessary. Good. Further, after concentration or drying, the obtained concentrate or dried product may be washed with an insoluble solvent to be purified and used, or this may be further dissolved or suspended in a suitable solvent for use.

In addition, as an extract of a plant belonging to the genus Plum of the Rosaceae family or an extract of a plant of the genus Plumaceae of the Rosaceae that has been treated with an enzyme, a commercially available extract can be conveniently used. For example, examples of the enzyme-decomposed prunes extract include "Creage" manufactured by Ichimaru Falcos Co., Ltd.

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, etc., but for example, 0.00001 in terms of dry weight of the component (C). Specific lows of% by weight or more include 0.00001 to 0.1% by weight. From the viewpoint of further enhancing the action of improving the whitening effect, the content of the component (C) in the external composition 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 external composition of the present invention, the ratio of the component (B) to the component (C) is determined according to each of the above-mentioned contents, but from the viewpoint of producing an even more excellent whitening effect, (B) In terms of dry weight of component (C), it is 1 part by weight or more, preferably 1 to 5000 parts by weight, more preferably 5 to 500 parts by weight, and further preferably 5 to 5 parts by weight per 100 parts by weight of the component (converted to dry weight). 100 parts by weight, particularly preferably 10 to 100 parts by weight.

(D) Water-soluble thickener, (E) Porous powder, and (F) Trimethylglycine The external composition of the present invention is referred to as a water-soluble thickener ((D) component) in addition to the above-mentioned components. It may also contain porous powder (sometimes referred to as component (E)), and trimethylglycine (sometimes referred to as component (F)). When these (D) to (F) components are contained together with the above-mentioned components, in addition to an excellent whitening effect, stickiness is suppressed and refreshing while having a firm application feeling at the time of application. It has a smooth feel, and after application, it is possible to suppress powderiness and impart an excellent moisturizing feeling.

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

The force-ruboxyvinyl polymer is a water-soluble vinyl polymer having a carboxyl group, and specifically, it has a crosslinked structure with acrylic acid and / or metaglylic acid as a main chain and allyl sucrose, pentaerythritol, or the like. It is a polymer.

Further, the alkyl-modified carboxyvinyl polymer is a polymer in which at least a part of the carboxyl groups of the carboxyvinyl polymer is esterified with an alkyl group. In the alkyl-modified carboxyvinyl polymer, the alkyl group bonded by the ester bond may be in the form of a straight or branched form. The number of carbon atoms of the alkyl group is not particularly limited, and examples thereof include 8 to 35, preferably 8 to 30.

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

These water-soluble thickeners may be used alone or in combination of two or more. From the viewpoint of further improving the above-mentioned usability, it is preferable to use a carboxyvinyl polymer and an alkyl-modified carboxyvinyl polymer in combination as the water-soluble thickener. When the carboxyvinyl polymer and the alkyl-modified carboxyvinyl polymer are used in combination, the ratio thereof is not particularly limited, but for example, the alkyl-modified carboxyvinyl polymer is preferably 1 to 10000 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.

Commercially available water-soluble thickeners can also be used. For example, as commercially available products of carboxyvinyl polymer, "AQPEC HV-501E" and "AQUP EC HV-505E" manufactured by Sumitomo Seika Chemical Industries, Ltd .; "Carbopol 940" and "Carbopole 941" manufactured by Lubrizol Advanced Materials. , "Carbopole 980"; "Hybrid Wako I 103", "Hybis Wako I 104", "Hybis Wako I 105" manufactured by Wako Pure Chemical Industries, Ltd .; "Syntaren K", "Syntaren L" manufactured by 3V Sigma, etc. Be done. As commercial products of alkyl-modified carboxyvinyl polymer, "AQUAPEC HV-501ER" manufactured by Sumitomo Seika Chemical Co., Ltd .; "Carpopole ultraz20", "Carbopole ultraz21", "Carbopole 1342" manufactured by Lubrizol Advanced Materials. , "Carbopole ETD2020", "Pemren TR-1", "Pemren 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, etc., and is, for example, 0.1 to 3% by weight, preferably 0.3. It is about 2% by weight, more preferably 0.3 to 1.5% by weight. By satisfying such a content, it becomes possible to more effectively enhance a firm coating feeling and a moisturizing feeling after coating by 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, and for example, silica, talc, titanium oxide, myrity, zinc oxide, kaolin, barium sulfate, bismuth oxychloride. , Aluminum hydroxide, aluminum silicate, silicic anhydride, hydrous silicic acid, inorganic powders such as montmorillonite; polyester, polyethylene, polystyrene, methyl methacrylate resin, cellulose, nylon, styrene and acrylic acid copolymer, polypropylene, Examples thereof include polymer powders such as vinyl chloride. These porous powder rests 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 not sticky feeling during coating and more effectively improving 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. The amount of oil absorbed by 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 can be mentioned. Here, the average particle size of the porous powder is the “arithmetic mean value of the particle diameter” defined in JIS Z 8901: 2006 “Test powder and test particles”. The oil absorption of the porous powder is a value measured in accordance with JIS K5101-13-1. The specific surface area of the porous powder is the BET specific surface area measured in accordance with JIS K6430 Annex 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, etc., and is, for example, 0.05 to 5% by weight, preferably 0.5. ~ 3% by weight, more preferably 1 to 3% by weight.

Trimethylglycine is present in plants of the family Chenopodiaceae, seaweeds, fish, crustaceans, etc., and is a widely used component as an amino acid-based moisturizer.

Commercially available trimethylglycine can also be used. Specific examples of commercially available trimethylglycine products include "Aqua Dew AN-100" manufactured by Ajinomoto Co., Inc. and "Amino Coat" manufactured by Asahi Kasei Chemicals Co., Ltd.

When the components (D) to (F) are contained in the external composition of the present invention, the ratio of the component (D) to the component (F) is 0 per part by weight of the component (D). .1 to 6 parts by weight is desirable. By satisfying such a ratio, it is possible to effectively impart the feeling of use during and after the above-mentioned coating. From the viewpoint of more effectively imparting the feeling of use during and after application, the ratio of component (D) to component (F) is such that component (F) per part by weight of component (D). It is preferably 1 to 4 parts by weight, more preferably 1.5 to 4 parts by weight.

The content of the component (E) in the external composition of the present invention may be appropriately set so as to satisfy the ratio of the component (D) and the component (F) described above. For example, the content of the component (D) is contained. When the amount is 0.1 to 3% by weight, the content of the component (E) is 0.01 to 18% by weight, preferably 0.1 to 12% by weight, and more preferably 0.15 to 12%. Weight% is mentioned.

Polyhydric alcohol The external composition of the present invention may contain a polyhydric alcohol, if necessary, for the purpose of enhancing the moisturizing effect.

The polyhydric alcohol is not particularly limited as long as it is pharmaceutically or cosmetically acceptable, and for example, propylene glycol, ethylene glycol, 1,3-butylene glycol, isoprene glycol, diethylene glycol, dipropylene glycol, etc. Glycerin and the like can be mentioned. These polyhydric alcohols may be used alone or in combination of two or more. Among these polyhydric alcohols, 1,3-butylene glycol and glycerin are preferable.

When the external composition of the present invention contains a polyhydric alcohol, the content thereof may be appropriately set according to the type of the polyhydric alcohol used, the formulation form of the external composition, and the like. 0.01 to 30% by weight, preferably 0.1 to 20% by weight, 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 above-mentioned components (D) and (F) are contained, it is desirable to include water as a base for dissolving those components.

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

Other Ingredients The external composition of the present invention may contain other pharmacological ingredients in addition to the above-mentioned ingredients, if necessary. Examples of such pharmacological components include antihistamines (diphenhydramine, diphenhydramine hydrochloride, chlorhexidine maleate, etc.) and local anesthetics (lydocaine, dibucaine, methyl aminobenzoate, procaine, tetracaine, bupipacaine, mepipacaine, chloroprocine). , Proparacaine, meprilkine or salts thereof, orthokine, oxesazein, oxypolyentoxydecane, funnel extract, percaminpase, tesitdecitin, etc.), anti-inflammatory agents (alantin, glycyrrhizinic acid, methyl glycyrrhizinate, stearyl glycyrrhizinate, dipotassium glycyrrhizinate, glycyrrhizinate) Monoammonium, glycyrrhetinic acid, pyridoxin glycyrrhetinate, stearyl glycyrrhetinate, glyceryl glycyrrhetinate, monoglucuronide glycyrrhetinate, salicylic acid, methyl salicylate, glycol salicylate, indomethacin, fervinac, diclofenac sodium, loxoprofen sodium, ufenamate, ibuprofenol Zack, sprofene, bufexamac, etc.), bactericides (benzalconium chloride, decalinium chloride, benzethonium chloride, cetylpyridinium chloride, chlorhexidine chloride, chlorhexidine gluconate, isopropylmethylphenol, aqueous ammonia, sulfaziazine, lactic acid, phenol Etc.), skin protectants (colodione, castor oil, etc.), blood circulation promoters (nonyl acid vanillylamide, nicotinic acid benzyl ester, capsaicin, capsicum extract, etc.), refreshing agents (menthol, camphor, etc.), vitamins (vitamin A, B, D, etc.), mucopolysaccharides (sodium chondroitin sulfate, glucosamine, hyaluronic acid, etc.) and the like.

In addition, the external composition of the present invention may contain a base or an additive, if necessary, in order to obtain a desired formulation form. Such bases and additives are not particularly limited as long as they are pharmaceutically acceptable, but are, for example, aqueous bases such as lower alcohols (ethanol, isopropanol, etc.); oils (olive oil, saflower oil, etc.). , 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, vaseline, etc.), waxes and waxes. (Mitsurou, carnauba wax, candelilla wax, selecin, rice wax, microcrystalin wax, etc.), ester oil (isopropyl myristate, isopropyl adipate, diethyl sebacate, isopropyl sebacate, isopropyl palmitate, cetyl palmitate, ethyl oleate, etc.) , Tri2-ethylhexarate glyceryl, etc.), fatty acid alkyl esters, fatty acids (stearic acid, oleic acid, palmitic acid, bechenic acid, linoleic acid, lanolin, etc.), fatty acid esters (cetyl palmitate, isopropyl palmitate, ethyl linoleate, etc.) 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, linoleil alcohol, octyl Oil-based bases such as dodecanol, hexyldecanol, isostearyl alcohol, etc.), cetyl 2-ethylhexanoate, silicone oil (dimethylpolysiloxane, cyclic silicone, etc.); POE (10 to 50 mol) phytosterol ether, POE (10 to 50 mol) 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 (5-30 mol) 2-decyltetradecyl ether, POE (10-50 mol) polyoxypropylene (2-30 mol) Polyoxyethylene alkyl ethers such as cetyl ethers, their phosphates and phosphates (POE cetyl ether sodium phosphate, etc.), POE (20-60 mol) Solbitan monoolate, 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, monolaurate polyethylene glycol, monopalmitate polyethylene glycol, monostearate polyethylene glycol, dilaurate polyethylene glycol, dipalmitate polyethylene glycol, distearate polyethylene glycol, dioleate polyethylene glycol, Surface activity of polyethylene glycol diricinoleate, polyoxyethylene hydrogenated castor oil (5-100), polysorbate (20-85), glycerin fatty acid ester (glycerin monostearate, etc.), hydrogenated soybean phospholipid, hydrogenated lanolin alcohol, etc. Agents: Cooling agents (mentol, camphor, borneol, peppermint water, peppermint oil, etc.), preservatives (methylparaben, propylparaben, benzoic acid, sodium benzoate, sorbic acid, etc.), flavoring agents (citral, 1,8- Cionel, citronellal, farnesol, etc.), colorants (tar pigments (brown 201, blue 201, yellow 4, yellow 403, etc.), cocoa pigments, chlorofil, aluminum oxide, etc.), pH adjusters (phosphate, hydrochloric acid, etc.) , Citric acid, sodium citrate, succinic acid, tartaric acid, sodium hydroxide, potassium hydroxide, triethanolamine, triisopropanolamine, etc.), wetting agents (dol-sodium pyrrolidone carboxylate solution, D-sorbitol solution, macrogol, etc.) ), Stabilizers (dibutylhydroxytoluene, butylhydroxyanisole, sodium edetate, sodium metaphosphate, L-arginine, L-aspartic acid, DL-alanine, glycine, sodium erythorbinate, propyl gallate, sodium sulfite, sulfur dioxide , Chlorogenic acid, catechin, rosemary extract, etc.), antioxidants, UV absorbers, chelating agents, adhesives, buffers, solubilizers, solubilizers, preservatives and other additives.

Formulation form The external composition is not particularly limited as long as it is a formulation form that can be applied transdermally, and is liquid, solid, semi-solid (cream, gel, ointment, paste). Etc. may be used. Further, the external composition of the present invention may be a non-emulsified preparation such as an aqueous preparation or an oil-based preparation, or may be an emulsified preparation such as an oil-in-water emulsified preparation or a water-in-oil emulsified preparation.

The formulation form of the external composition is preferably liquid or creamy from the viewpoint of exerting a whitening effect even more effectively.

In addition, the external composition may be in any form of preparation such as an external medicine for skin, a cosmetic, and a skin cleansing agent as long as it is applied to the skin.

Specific examples of the formulation form of the external composition include liquid preparations (including lotions, sprays, aerosols, and emulsions), water-soluble ointments, oily ointments, creams, foams, and gels. , Topical skin preparations such as patches; cosmetics such as ointments, creams, milky lotions, lotions, lotions, packs and gels; skin cleaning agents such as body shampoos, hair shampoos and rinses. Among these formulation forms, a skin external preparation is preferable, and a liquid preparation and a cream preparation are more preferable. These formulations can be prepared by formulating them with additives according to the formulation according to the known method described in the 16th revised Japanese Pharmacopoeia General Regulations for Formulation.

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

The present invention will be described in more detail with reference to Examples below, but the present invention is not limited thereto.

The manufacturers of the main components used in the following test examples and prescription examples are as follows.
L-ascorbic acid 2-glucoside : Product name "AA2G" (manufactured by Hayashibara Co., Ltd.)
Magnolia obovata extract : Trade name "Falcolex Magnolia B" (manufactured by Ichimaru Falcos Co., Ltd.), liquid, dry solid content concentration 0.175% by weight, Magnolia obovata Tumberg (Magnoliaceae) bark (Wakopaku) 1 , An extract obtained by solvent extraction treatment using an aqueous solution of 3-butylene glycol
Prunes extract : Trade name "Cleage" (manufactured by Ichimaru Falcos Co., Ltd.), liquid, dry solid content concentration 7.78% by weight, prunes (Prunus domestica Lindl. (Rosaceae)) flesh is a fibrinolytic enzyme Extract obtained by adding water and 1,3-butylene glycol to the one obtained by decomposition in
Artichoke leaf extract : Trade name "Biobenefity" (manufactured by Ichimaru Falcos Co., Ltd.), liquid, dry solid content concentration 0.08% by weight, leaves of Cynara scorymus L. (Composite) in ethanol solution Extract obtained by concentrating and drying the extract obtained by extraction and adding a 1,3-butylene glycol solution.
Herb robert extract : Brand name "Princess Care" (manufactured by Ichimaru Falcos Co., Ltd.), liquid, dry solid content concentration 1% by weight, from whole herb robert (Geraniium L. (Geraniaceae)) in 1,3-butylene glycol solution Extract obtained by extraction
Alpinia katsumadai seed extract : Brand name "Alpinia White" (manufactured by Ichimaru Falcos Co., Ltd.), liquid, dry solid content concentration 0.2% by weight, Alpinia katsumadai Hayata (Zingiberaceae) seeds in ethanol solution Extract obtained by concentrating the extract obtained by extraction and adding a 1,3-butylene glycol solution.
Chimpi extract : Trade name "Mandarinkria" (manufactured by Ichimaru Falcos Co., Ltd.), liquid, dry solid content concentration 3% by weight, mature peel of mandarin orange (Citrus reticulate Blanco (Rutaceae)) in 1,3-butylene glycol solution Extract obtained by extraction in
Bilberry leaf extract : trade name "Cure Berry" (manufactured by Ichimaru Falcos Co., Ltd.), liquid, dry solid content concentration 0.2% by weight, 1,3-butylene glycol from bilberry (Vaccinium myrtillus L. (Ericaceae)) leaves Extract obtained by extracting with a solution
Carboxyvinyl polymer : Product 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 to 30)
Silica : Product name "Godball D-25C" (manufactured by Suzuki Yushi Kogyo Co., Ltd.), average particle diameter 7-10 μm, specific surface area 300-500 m ² / g, oil absorption 70-110 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. It was left still. 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 the cells were cultured in an incubator (37 ° C., 5% CO ₂ ) for 24 hours. Then, it was irradiated with ultraviolet rays (UV-B) under the condition of 0.5 mW × 12 seconds each time, and cultured for another 24 hours. The ultraviolet irradiation was carried out using a UVB lamp (manufactured by Toshiba Lighting & Technology Corporation, a fluorescent lamp for Toshiba Health Line) and a UV detector (manufactured by TOPCON, UV-1). Then, the medium was exchanged, and the cells were further cultured for 24 hours. In addition, 50 μl of a predetermined sample solution was added to the skin model cup each time the medium was changed. Further, by repeating the ultraviolet irradiation and the medium exchange four times under the same conditions, the ultraviolet irradiation was carried out a total of five times (total ultraviolet irradiation amount 30 mJ / cm ² ), and the medium exchange was carried out a total of five times. Then, the cell viability and the amount of melanin produced were measured by the methods shown below. 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 conducted under the same conditions as described above.

<Measurement of cell activity>
Cell viability was measured by MTT test. Specifically, 0.75 ml of the MTT assay drug and 8.25 ml of the maintenance medium (EPI-100LLMM) were mixed and added so as to be 300 μl per well. The skin model cup was transferred to the medium containing the MTT prepared above and cultured in the incubator for exactly 3 hours. The bottom of the tissue was then lightly washed with PBS wash and transferred to a new plate. 1 ml of 0.04N HCl acidic isopropanol was added to the inside of the skin model cup, a cover seal was attached to the plate to prevent evaporation, and the blue formazan was extracted in an incubator overnight. After extraction, isopropanol was mixed well and 200 μl of it was transferred to a 96-well plate. The optical densities of 570 nm and 620 nm were measured with a microplate reader, and the difference between them was used 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). Then, the supernatant was removed, a mixed solution of ethanol and dimethyl ether (ethanol: dimethyl ether = 3: 1 (volume ratio)) was further added, and the mixture was stirred and centrifuged (2,000 rpm, 10 minutes). The supernatant was then removed and dried. A 1N aqueous sodium hydroxide solution (containing 10 wt% DMSO) was added to the dried product, treated in a water bath at 90 ° C. for 20 minutes, and heated and melted. Then, the heat-melted solution was lightly stirred with a vortex, 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. Further, the ratio of the amount of melanin produced per cell (melanin production ratio) when each sample solution was added was calculated with the amount of melanin produced per cell of the control being 100.

The results obtained are shown in Tables 1 and 2. As a result, no melanin production inhibitory effect was observed with the magnolia obovata extract alone (Comparative Example 2), and the melanin production inhibitory effect was insufficient even with ascorbic acid 2-glucoside alone (Comparative Example 1). In addition, ascorbic acid 2-glucoside and plant extracts known to suppress melanin production (prune extract, chimpi extract, artichoke leaf extract, bilberry leaf extract, alpinia katsumadai seed extract, Himefuuro extract) ) Was combined (Comparative Examples 3 to 8), but almost no enhancement of the melanin production inhibitory effect was observed.

On the other hand, when the ascorbic acid 2-glucoside and the magnolia obovata extract were combined (Examples 1 to 11), the effect of suppressing melanin production was remarkably enhanced. Furthermore, when the prune extract was combined with the ascorbic acid 2-glucoside and the magnolia obovata extract (Examples 4 to 8), a dramatic improvement in the effect of suppressing melanin production was observed. On the other hand, when scorbic acid 2-glucoside and honoki extract are combined with other plant extracts known to have an inhibitory effect on melanin production (artichoke leaf extract, Himefuuro extract, Alpinia katsumadai seed extract), prune No improvement in the effect of suppressing melanin production was observed as in the case of the extract.

Test Example 2: Evaluation of usability A skin cosmetic (liquid) having the composition shown in Tables 3 and 4 was prepared. Specifically, the manufacturing procedure is as follows. After stirring and dissolving the carboxyvinyl polymer and the alkyl-modified carboxyvinyl polymer in purified water, glycerin was added and dissolved by stirring to obtain Preparation A. Separately, trimethylglycine and / or silica was added to 1,3-butylene glycol and stirred and mixed to homogenize to obtain Preparation B. Then, while stirring the preparation A, the preparation B was added, and the mixture was stirred with a homomixer to homogenize. Further, potassium hydroxide was added to adjust the pH to 6.5, and then L-ascorbic acid 2-glucoside, magnolia obovata extract, and prune extract were added and stirred to homogenize the skin cosmetics. Prepared.

Each of the obtained skin cosmetics was evaluated by the following methods for a firm application feeling at the time of application, a non-sticky feeling and a refreshing feeling, a non-powderful feeling after application, and a heat retention feeling.

Ten evaluation monitors applied about 0.5 g of each skin cosmetic to their arms, and they gave a firm feeling of application, no stickiness and refreshing feeling, and no powderiness and moisturizing after application. I evaluated the feeling. Specifically, the evaluation was scored by conducting a questionnaire by a Visual Analogue Scale (hereinafter, also referred to as VAS) in which the following were designated as "1" and "10". The evaluation results were summarized by averaging the questionnaire results and rounding off to the first decimal place.
<At the time of application>
・ Application feeling There is no entangled application feeling / application feeling that crushes the gel "1"
"10" with a feeling of entanglement / feeling of application that crushes the gel
・ Refreshing feeling "1" without a refreshing feeling
"10" with a refreshing feeling
・"1" that feels sticky without stickiness
"10" that does not feel sticky
<30 seconds after application>
・ No powderiness "1" that feels powdery
"10" that does not feel powdery
・ Moisturizing feeling "1" without moisturizing feeling (moist feeling)
"L0" with a moisturizing feeling (moist feeling)

The results obtained are shown in Tables 3 and 4. Firm application feeling when containing water-soluble thickeners (carboxyvinyl polymer, alkyl-modified carboxyvinyl polymer), silica, and trimethylglycine in addition to ascorbic acid 2-glucoside, magnolia obovata extract and prune extract The results were satisfactory in terms of non-stickiness, refreshing feeling, non-powderiness and moisturizing feeling. In particular, when trimethylglycine fills 0.1 to 6 parts by weight with respect to 1 part by weight of the water-soluble thickener, it has a firm coating feeling, no stickiness, a refreshing feeling, and no powderiness. The moisturizing feeling was an extremely good result.

Prescription Examples 1-9
Skin cosmetics were prepared by a conventional method according to the formulations shown in Table 5 (pH 6.5 for Formulation Examples 1 to 6 and pH 4.5 for Formulation Examples 7 to 9).

Prescription Examples 10 to 15
According to the formulation shown in Table 6, skin cosmetics were prepared according to the following procedure.
Step (1): L-ascorbic acid 2-glucoside or L-ascorbic magnesium phosphate was dissolved in purified water, and then the pH was adjusted to 6 with a solution in which potassium hydroxide was dissolved in purified water (preparation (A). -1)).
Step (2): (B) and (C) were dissolved by heating and stirring (preparation (B), preparation (C)), respectively.
Step (3): The preparation (C) was added while heating and stirring the preparation (B), and the mixture was made uniform by stirring with a homomixer.
Step (4): Then, the mixture was gradually cooled to 40 ° C. or lower with stirring, the rest of the preparations (A-1) and (A) were added, and the mixture was stirred and homogenized to prepare a skin cosmetic.

Claims (3)

(A) Ascorbic acid , ascorbic acid 2-glucoside, ascorbic acid monostearate, ascorbic acid monopalmitate, ascorbic acid monooleate, ascorbic acid monophosphate ester and its magnesium salt, ascorbic acid distearate, ascorbic acid dipalmitate, ascorbic acid diolate, Ascorbic acid diphosphate ester and its salts, ascorbic acid tristearate, ascorbic acid tripalmitate, ascorbic acid triolate, ascorbic acid triphosphate ester, 3-O-ethyl, 6-acetyl-ascorbic acid, 3-O-ethyl , 6-Butyl ascorbic acid, 3-O-ethyl, 6-lauroyl ascorbic acid, 3-O-ethyl, 6-palmitoyl ascorbic acid, 3-O-ethyl, 6-oleoil ascorbic acid, 3-O-ethyl, Contains 6-stearoyl ascorbic acid and at least one selected from the group consisting of 3-O-ethyl, 6-beherminoyl-ascorbic acid , (B) sardine extract, and (C) prune flesh extract. An external composition, characterized in that it does. The external composition according to claim 1, wherein the component (A) is ascorbic acid 2-glucoside. The external composition according to claim 1 or 2, which is for whitening.