JP2021091643A - Topical skin preparation - Google Patents

Abstract

To provide a topical skin preparation that uses specific components in combination to produce the effects of reducing the transepidermal water loss and improving the epidermal state.SOLUTION: A topical skin preparation contains pullulan and tranexamic acid or a salt thereof.SELECTED DRAWING: None

Description

The present invention relates to an external preparation for skin containing pullulan and tranexamic acid or a salt thereof.

The evaluation of the barrier function of the stratum corneum is performed using the amount of water evaporated from the skin (transepidermal water loss: TEWL) as an index (Non-Patent Document 1).
Tranexamic acid has been used as an active ingredient in cosmetics because it has moisturizing and whitening effects (Patent Document 1).

However, there is a problem that the effect of tranexamic acid on improving the barrier function of the stratum corneum is low.

JP-A-2017-109972

New Cosmetics Handbook, published October 30, 2006, 505p New Cosmetics Handbook, published October 30, 2006, 118p

It is an object of the present invention to provide a skin external preparation in which TEWL is improved by adding pullulan to a skin external preparation containing tranexamic acid or a salt thereof.

The present invention provides a skin external preparation containing tranexamic acid or a salt thereof and pullulan.

The external preparation for skin of the present invention exerts a TEWL improving effect.

Hereinafter, embodiments for carrying out the present invention will be described.

The external preparation for skin of the present invention can be used for any of cosmetics, quasi-drugs, pharmaceuticals and the like.

Tranexamic acid or a salt thereof may be any as long as it is generally used for cosmetics and the like. The content is preferably 0.01 to 5% by mass, more preferably 1 to 2.5% by mass, and most preferably 2% by mass with respect to the total amount of the external preparation for skin.

The pullulan used in the present invention is not particularly limited as long as it can be blended with an external preparation for skin, but it is preferable to use pullulan having a molecular weight of 100,000 to 100,000. Examples of commercially available pullulan products include "Cosmetic pullulan" and "Food additive pullulan" (all manufactured by Hayashibara Biochemical Research Institute).

The content of pullulan in 100% by mass of the external preparation for skin of the present invention is preferably 0.01% by mass or more, more preferably 0.03% by mass or more, from the viewpoint of moisturizing effect and non-sticky feeling. Yes, preferably 1.0% by mass or less, more preferably 0.5% by mass or less, still more preferably 0.2% by mass or less.

Next, an optional component that can be blended in the external preparation for skin of the present invention will be described.

The external preparation for skin of the present invention can contain one or more anti-inflammatory agents selected from glycyrrhizic acid, glycyrrhetinic acid, azulene, salicylic acid, allantoin, derivatives thereof and salts thereof.

The glycyrrhizic acid, its derivative, and a salt thereof are not particularly limited as long as they can be blended with an external preparation for skin, and specific examples thereof include glycyrrhizic acid, dipotassium glycyrrhizinate, and monoammonium glycyrrhizinate. Of these, it is preferable to use dipotassium glycyrrhizinate. Commercially available products include glycyrrhizic acid, dipotassium glycyrrhizinate, monoammonium glycyrrhizinate (manufactured by Alps Pharmaceutical Co., Ltd.), dipotassium glycyrrhizinate, monoammonium glycyrrhizinate (manufactured by Maruzen Pharmaceuticals Co., Ltd.), dipotassium glycyrrhizinate "Kouki", Examples thereof include monoammonium glycyrrhizinate "Kouki" (all manufactured by Kouki Co., Ltd.).

When glycyrrhizic acid, a derivative thereof, and a salt thereof are blended, the blending amount is preferably 0.0001% by mass or more with respect to the total amount of the external preparation for skin. Further, it is preferably 2% by mass or less, more preferably 0.8% by mass or less for those that are washed away, and more preferably 0.5% by mass or less for those that are not washed away.

The glycyrrhetinic acid, its derivative, and a salt thereof are not particularly limited as long as they can be blended with an external preparation for skin, and specific examples thereof include glycyrrhetinic acid, stearyl glycyrrhetinate, and glycerin glycyrrhetinate. Of these, it is preferable to use glycyrrhetinic acid and stearyl glycyrrhetinate. Commercially available products include β-glycyrrhetinic acid, stearyl glycyrrhetinate (above, manufactured by Alps Pharmaceutical Co., Ltd.), glycyrrhetinic acid, sea-augretinol (registered trademark) (above, manufactured by Maruzen Pharmaceuticals Co., Ltd.), agritinone, aglycinone stearyl (above, manufactured by Maruzen Pharmaceuticals Co., Ltd.). Examples include Tokiwa Phytochemical Research Institute), glycyrrhetinic acid "Kouki", and stearyl glycyrrhetinate "Kouki" (manufactured by Kouki Co., Ltd.).

When glycyrrhetinic acid, a derivative thereof, and a salt thereof are blended, the blending amount is preferably 0.0001% by mass or more with respect to the total amount of the external preparation for skin. Further, it is preferably 2% by mass or less, more preferably 0.8% by mass or less for those that are washed away, and more preferably 0.5% by mass or less for those that are not washed away.

The azulene, its derivative and a salt thereof are not particularly limited as long as they can be blended in an external preparation for skin, and specific examples thereof include azulene, guaiazlene, ethyl guaiazlene sulfonate, sodium guaiazlene sulfonate, chamazulene and the like. Be done. Of these, it is preferable to use sodium guaiazulene sulfonate. Examples of commercially available products include Guaiazulene and water-soluble azulene (all manufactured by Konan Kako Co., Ltd.).

When azulene, a derivative thereof, and a salt thereof are blended, the blending amount is preferably 0.0001% by mass or more with respect to the total amount of the external preparation for skin. Further, 1% by mass or less is preferable, and 0.1% by mass or less is more preferable.

The salicylic acid, its derivative and a salt thereof are not particularly limited as long as they can be blended in an external preparation for skin, and specific examples thereof include salicylic acid, methyl salicylate, glycol salicylate, sodium salicylate, ethylhexyl salicylate and the like. Be done. Among these, ethylhexyl salicylate and sodium salicylate are preferably used. Commercially available products include SALICYLIC ACID (manufactured by Solvay), methyl salicylate (manufactured by IP Corporation), sodium salicylsanate (manufactured by Yoshitomi Fine Chemicals), escalol 587 (manufactured by Ashland Japan), and pulsor EHS (DSM). (Manufactured by the company) and the like.

When salicylic acid, a derivative thereof, and a salt thereof are blended, the blending amount is preferably 0.0001% by mass or more with respect to the total amount of the external preparation for skin. Further, 1% by mass or less is preferable, and 0.2% by mass or less is more preferable.

The allantoin, its derivative, and a salt thereof are not particularly limited as long as they can be blended with an external preparation for skin, and specific examples thereof include allantoin, allantoin chlorohydroxyaluminum, and allantoindihydroxyaluminum. Of these, it is preferable to use allantoin. Examples of commercially available products include allantoin (manufactured by Ashland Japan Co., Ltd.), allantoin, ALCA (manufactured by Kawaken Fine Chemical Co., Ltd.), RonaCare (registered trademark) Allantoin (manufactured by Meeck), and the like.

When allantoin, a derivative thereof, and a salt thereof are blended, the blending amount is preferably 0.0001% by mass or more with respect to the total amount of the external preparation for skin. Further, it is preferably 1% by mass or less, more preferably 0.5% by mass or less for those that are washed away, and more preferably 0.3% by mass or less for those that are not washed away.

The external preparation for skin of the present invention comprises one or more whitening agents selected from ascorbic acid, its derivatives and their salts, hydroquinone, its derivatives and their salts, nicotinic acid, its derivatives and their salts. Can be contained.

The ascorbic acid, its derivative and a salt thereof are not particularly limited as long as they can be blended in an external preparation for skin. Specifically, ascorbic acid is L-ascorbic acid, and ascorbic acid derivative is L. -Ascorbic acid glucoside, L-ascorbic acid-2-phosphate ester, L-ascorbic acid-3-phosphate ester, L-ascorbic acid-6-phosphate ester, L-ascorbic acid-2-polyphosphate ester, L L-ascorbic acid monoesters such as −ascorbic acid-2-sulfate ester, L-ascorbic acid-2-palmitic acid ester, L-ascorbic acid-6-palmitic acid ester, L-ascorbic acid-2-stearic acid ester , L-ascorbic acid monoalkyl esters such as L-ascorbic acid-6-stearic acid ester, L-ascorbic acid-2,6-dibutyl ester, L-ascorbic acid-2,6-dipalmitic acid ester and the like. L-ascorbic acid dialkyl esters, L-ascorbic acid tristearate, L-ascorbic acid trioleate, L-ascorbic acid tripalmitate and other L-ascorbic acid trialkyl esters, L-ascorbic acid triphosphate and the like L -Ascorbic acid triesters, L-ascorbic acid tetraalkyl esters such as L-ascorbic acid tetraisopalmitate, ascorbic acid and ascorbic acid derivatives salt include sodium salt, potassium salt, magnesium salt, calcium salt, barium salt. , Ammonium salt, monoethanolamine salt, diethanolamine salt, triethanolamine salt, monoisopropanolamine salt, triisopropanolamine salt and the like. Of these, 2-glucoside ascorbic acid and magnesium ascorbyl phosphate are preferably used. Examples of commercially available products include AA2G (manufactured by Hayashibara Biochemical Research Institute), Seamate (manufactured by BASF Japan), NIKKOL VC-PMG (manufactured by Nikko Chemicals Co., Ltd.) and the like.

Hydroquinone, a derivative thereof, and a salt thereof are not particularly limited as long as they can be blended with an external preparation for skin, but hydroquinone glycosides are preferably exemplified. The sugar chain portion of the hydroquinone glycoside includes pentasaccharides such as L-arabinose, D-xylose, D-ribose, D-xylulose, D-lyxose, and D-ribbulose, D-glucose, D-galactose, and D-. Examples thereof include hexamonosaccharides such as mannose, D-tagalose, D-fructose, and L-sorbose, and amino acid sugars such as D-glucosamine, D-galactosamine, sialic acid, and muramic acid. Examples of hydroquinone derivatives and salts thereof include uronic acids such as D-glucuronic acid, D-galacturonic acid, D-mannuronic acid, and L-iduronic acid, or methyl compounds and acetyl compounds thereof. Examples of these salts include sodium salt, potassium salt, magnesium salt, calcium salt, barium salt, ammonium salt, monoethanolamine salt, diethanolamine salt, triethanolamine salt, monoisopropanolamine salt, and triisopropanolamine salt. Can be mentioned. Among the hydroquinone derivatives, it is preferable to use arbutin and / or a salt thereof having a chemical structure in which hydroquinone and glucose are bonded. Examples of commercially available products include arbutin (manufactured by Nippon Fine Chemical Co., Ltd.) and ARUBTIN (manufactured by SK bioland).

The nicotinic acid, its derivative and a salt thereof are not particularly limited as long as they can be blended in an external preparation for skin, and specific examples of the nicotinic acid derivative include nicotinic acid amide and nicotinic acid ester. Examples of the ester include tocopherol nicotinate, benzyl nicotinate, methyl nicotinate, ethyl nicotinate and the like. Among these, it is preferable to use nicotinamide. Examples of commercially available products include niacinamide USP PC (manufactured by Lonza Japan) and nicotinamide (manufactured by DSM Nutrition Japan).

The external preparation for skin of the present invention may contain one or more selected from the above whitening agents.
When the whitening agent is blended, the blending amount is preferably 0.0001% by mass or more, more preferably 0.001% by mass or more, still more preferably 0.1% by mass or more, based on the total amount of the external preparation for skin. Thereby, a whitening effect can be obtained. The blending amount of the whitening agent is preferably 5% by mass or less, more preferably 3% by mass or less, and further preferably 1% by mass or less, based on the total amount of the external preparation for skin.
For example, when the whitening agent is blended, the blending amount is preferably 0.0001% by mass to 5% by mass, more preferably 0.001% by mass to 3% by mass, and 0.1 to 1 with respect to the total amount of the external preparation for skin. Mass% is more preferred.

The external preparation for skin of the present invention can be used as a sunscreen cosmetic by blending metal oxide fine particles and an organic ultraviolet absorber.

The metal oxide fine particles are not particularly limited, but it is common to use one or two kinds selected from fine particle titanium oxide and fine particle zinc oxide. The metal oxide fine particles can be blended as they are in the external preparation for skin of the present invention, but it is also possible to use those previously dispersed in a silicone oil, an ester oil, or an aqueous component. Further, a powder obtained by coating the surface of a plate-shaped powder with metal oxide fine particles and a powder obtained by modifying the powder with a surface modifier can also be used.

The type of the organic ultraviolet absorber is not particularly limited, and a known organic ultraviolet absorber can be used without limitation. Examples of such known organic ultraviolet absorbers include silicic acid derivatives such as 2-ethylhexyl paramethoxycinerate, isopropyl methoxycinnamate, and isoamyl methoxycinnamate; paraaminobenzoic acid (hereinafter abbreviated as "PABA"). PABA derivatives such as ethyl PABA, ethyl-dihydroxypropyl PABA, ethylhexyl-dimethyl PABA, glyceryl PABA; salicylic acid derivatives such as homosalate, ethylhexyl salicylate, dipropylene glycol salicylate, TEA salicylate; benzophenone-1, Benzophenone derivatives such as benzophenone-2, benzophenone-3 or oxybenzone, benzophenone-4, benzophenone-5, benzophenone-6, benzophenone-8, benzophenone-9, benzophenone-12; Benzophenone succino derivatives such as sulphonic acid, methosulfate benzophenone sulconium, terephthalilidene sulphonic acid, polyacrylamide methylbenzylene sulphonate; anisotriazine, diethylhexylbutamidotriazone, 2,4,6-tris (diisobutyl- 4'-aminobenzalmaronate) -s-triazine, 2,4-bis- [{4- (2-ethylhexyloxy) -2-hydroxy} -phenyl] -6- (4-methoxyphenyl) -1, Triazine derivatives such as 3,5-triazine, 2,4,6-tris [4- (2-ethylhexyloxycarbonyl) anilino] -1,3,5-triazine; phenylbenzo such as phenyldibenzoimidazole tetrasulfonate disodium Imidazole derivatives; phenylbenzotriazole derivatives such as drometrizoletrisiloxane and methylenebis (benzotriazolyltetramethylbutylphenol); anthranil derivatives such as menthyl anthranylate; imidazoline derivatives such as dimethoxybenzidyleneoxoimidazolidinepropionate 2-ethylhexyl; ben Benzophenone derivatives such as polyorganosiloxane having a zarmaronate functional group; 4,4-diarylbutadiene derivatives such as 1,1-dicarboxy (2,2'-dimethylpropyl) -4,4-diphenylbutadiene; Octocrine, 2- [4- (diethylamino) -2-hydroxybenzophenone] hexyl benzoate, 4-te Examples thereof include rt-butyl-4'-methoxydibenzoylmethane. The organic ultraviolet absorber may be used alone or in combination of two or more.

When the organic ultraviolet absorber is blended, the blending amount is preferably 1 to 20% by mass. If it is less than 1% by mass, a sufficient sunscreen effect cannot be obtained, and if it exceeds 20% by mass, it has an adverse effect on usability, such as stickiness and increased primary irritation to the skin.

The external preparation for skin of the present invention can contain solid spherical borosilicate particles.
The average particle size of the solid spherical borosilicate particles is preferably 0.1 μm or more, more preferably 1 μm or more, further preferably 5 μm or more, and even more preferably 7 μm or more. The average particle size of the solid spherical borosilicate particles is preferably 20 μm or less, more preferably 15 μm or less, and even more preferably 13 μm or less. For example, the average particle size of the solid spherical borosilicate particles is preferably 1 to 20 μm, more preferably 5 to 15 μm, and further preferably 7 to 13 μm from the viewpoint of the stickiness reducing effect. The average particle size of the solid spherical borosilicate particles can be measured as the average particle size of the number average according to the principle of microscopy according to the shape of the powder particles.

In the solid spherical borosilicate particles, the borosilicate may be an alkali metal salt such as Na or K, an alkaline earth metal salt such as Mg or Ca, an Al salt, or a combination thereof. It is preferably Na borosilicate, Ca borosilicate, Al borosilicate, borosilicate (Ca / Na), borosilicate (Ca / Al), and more preferably borosilicate (Ca / Na).
The solid spherical borosilicate particles are displayed as borosilicate (Ca / Na) (CALCIUM SODIUM BOROSILICATE), borosilicate (Ca / Al) (CALCIUM ALUMINUM BOROSILICATE), etc. as cosmetic labeling names (INCI name). In the present invention, solid spherical borosilicate particles having any display name may be used, and it is more preferable to use borosilicate (Ca / Na).

When the solid spherical borosilicate particles are blended, the blending amount of the solid spherical borosilicate particles is not particularly limited, but is preferably 0.01% by mass or more, preferably 0.1% by mass or more, based on the total amount of the external preparation for skin. Is more preferable, and 1% by mass or more is further preferable. The blending amount of the solid spherical borosilicate particles is not particularly limited, but is preferably 30% by mass or less, more preferably 20% by mass or less, still more preferably 10% by mass or less, based on the total amount of the external preparation for skin.
For example, the blending amount of the solid spherical borosilicate particles is preferably 0.01 to 30% by mass, more preferably 0.1 to 20% by mass, and further preferably 1 to 10 with respect to the total amount of the external preparation for skin. It is mass%. For example, in an aqueous or oil-based dosage form for external skin preparation, the solid spherical borosilicate particles are more preferably 0.01 to 10% by mass based on the total amount of the external preparation for skin. Further, in the powdery or solid dosage form of the external preparation for skin, the solid spherical borosilicate particles are more preferably 0.1 to 20% by mass based on the total amount of the external preparation for skin.

The solid spherical borosilicate particles may be untreated, or may be hydrophilized or hydrophobized.

A zinc oxide-coated spherical powder can be blended in the external preparation for skin of the present invention. The zinc oxide-coated spherical powder has a sebum solidifying ability and can be expected to have an effect of improving makeup retention.

The spherical powder used for the zinc oxide-coated spherical powder is not particularly limited as long as it can be blended with an external preparation for skin, but is (Acrylate / ethylhexyl acrylate) cross polymer, alkenyl succinate starch ester metal salt, spherical borokei. It is preferable to use one or more selected from the acid salt powders from the viewpoint of the effect of improving the long-lasting makeup.

The zinc oxide used in the zinc oxide-coated spherical powder is not particularly limited as long as it can be blended in the solid powder cosmetics. The shape of zinc oxide is not particularly limited. The average powder diameter of zinc oxide is preferably 10 to 200 nm, more preferably 15 to 100 nm, and even more preferably 15 to 50 nm from the viewpoint of sebum solidifying ability.

The zinc oxide-coated spherical powder can be obtained, for example, by coating the spherical powder with zinc oxide.
As the zinc oxide, untreated zinc oxide can be used as it is, but it is preferable to use zinc oxide that has been hydrophobized. The hydrophobizing agent is not particularly limited, and examples thereof include dimethicone, methylhydrogenpolysiloxane, and metal soap. Among these hydrophobizing agents, it is preferable to use dimethicone. The coating amount of the hydrophobizing agent may be an amount sufficient for hydrophobizing zinc oxide. Specifically, the mass ratio of zinc oxide to the hydrophobizing agent is preferably 85: 15-99: 1, and more preferably 90: 10-98: 2.

In the zinc oxide-coated spherical powder used for the external preparation for skin of the present invention, the coating amount of zinc oxide is preferably 0.01 part by mass or more, more preferably 0.05 part by mass or more, based on 1 part by mass of the spherical powder. .. Further, the coating amount of zinc oxide is preferably 2 parts by mass or less, and more preferably 1.5 parts by mass or less with respect to 1 part by mass of the spherical powder. In this range, the sebum solidifying ability can be further enhanced and sebum collapse can be further prevented.
The coating amount of zinc oxide is preferably 0.01 to 2 parts by mass, more preferably 0.05 to 1.5 parts by mass with respect to 1 part by mass of the spherical powder.

As a method for coating the spherical powder with zinc oxide, various methods known so far can be used. For example, a physicochemical mixed grinding method (dry or wet), a chemical deposition method or the like can be used. Can be done. From the viewpoint of the sebum solidifying ability of the zinc oxide-coated spherical powder, a dry mixed grinding method can be preferably used.

Examples of commercially available zinc oxide-coated spherical powders include Prussia ASOS-20, Prussia OPZ-NV, and Prusair CBZ-NV (all manufactured by Suzuki Yushi Kogyo Co., Ltd.).

In addition to the above-mentioned components, the external preparation for skin of the present invention can contain any components used in ordinary cosmetics and quasi-drugs to the extent that the effects of the present invention are not impaired. Specific examples thereof include oil agents, surfactants, thickeners, preservatives, fragrances, moisturizers, antioxidants, antibacterial agents and the like.

The dosage form of the external preparation for skin of the present invention is not particularly limited, and any dosage form such as water-based, oil-based, emulsified type, and powder type may be used.

The external preparation for skin of the present invention can be prepared by a conventional method.

The external preparation for skin of the present invention can be used in, for example, lotions, emulsions, ointments, and powder-type dosage forms.

Hereinafter, the present invention will be specifically described with reference to Examples, but the scope of the present invention is not limited thereto. The blending amount is mass% unless otherwise specified.

[TEWL test]
・ Wash the inner part of the forearm with a predetermined soap and wipe off the water from the forearm.
・ Rest for 15 minutes in an environment of 21 ± 0.5 ° C. and 50 ± 5% relative humidity to acclimatize.
・ Three areas of 3.0 cm × 3.0 cm were marked on the left forearm, a total of 6.75 mg of the Examples or Comparative Examples shown in Table 1 was applied, and the amount of water evaporation 1 hour after application was measured. The rate of change from before application was calculated. A TEWL measuring instrument (SWL4081) manufactured by Keystone Scientific Co., Ltd. was used for the measurement.
The three subjects conducted the test under the guidance of not using cosmetics on the medial part of the forearm for one week before the test, and the average value measured twice for each measurement area was used as the measured value.

As shown in Table 1, tranexamic acid alone did not show a TEWL improving effect, but the addition of pullulan showed a dramatic improvement in TEWL.

Table 2 shows the anti-rough skin cream, Table 3 shows the whitening emulsion, Table 4 shows the formulation of the water-in-oil emulsified sunscreen cosmetic, and Table 5 shows the formulation of the oil-in-water emulsified sunscreen cosmetic.

Claims (1)

An external preparation for the skin containing pullulan and tranexamic acid or a salt thereof.