JP2001335458A - Skin care preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a skin care preparation for controlling melanin formation, effective for not only preventing pigmentation after sunburn, spot, freckle, liver spot, etc., but also ameliorating contact dermatitis, psoriasis, other chapped skin, skin disease such as rough skin, etc., having both bleaching action and ameliorating action on chapped skin. SOLUTION: This skin care preparation is obtained by formulating Akebia quinata Decne or its extract with a solvent with one or more kinds selected from the group consisting of xylitol, mannitol and erythritol as active ingredients.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an external preparation for whitening skin and an external preparation for improving skin roughness.
Suppresses the production of melanin and prevents pigmentation, spots,
The present invention relates to an external preparation for skin having both a whitening effect and a skin roughening effect that is effective in preventing freckles and liver spots, and is also effective in improving skin diseases such as contact dermatitis, psoriasis, and other rough and rough skin.

[0002]

2. Description of the Related Art There are some unclear points about the mechanism of the occurrence of skin spots and the like. Is produced, which is believed to be abnormally deposited in the skin. This melanin pigment, which causes the coloring of the skin, is produced in melanin-producing granules (melanosomes) in melanocytes (melanocytes) between the epidermis and the dermis, and the produced melanin diffuses into neighboring cells by osmosis. The biochemical reaction in this melanocyte is estimated as follows. That is, tyrosine, which is an essential amino acid, is converted into dopaquinone by the action of the enzyme tyrosinase, and the process in which it is converted to black melanin via a red pigment and a colorless pigment by an enzymatic or non-enzymatic oxidative action is a melanin pigment production process. Therefore, suppressing the action of tyrosinase, which is the first step of the reaction, is important for suppressing melanin.

[0003] However, compounds that suppress the tyrosinase action, except for hydroquinone, have very slow onset of their effects, so that the effect of improving skin pigmentation is not sufficient. On the other hand, although hydroquinone is recognized as having an effect, its use is generally restricted because of its sensitizing properties. Therefore, in order to improve its safety, attempts have been made to use monoesters or alkyl monoethers of higher fatty acids, but the esters are not always safe because they are decomposed by hydrolyzing enzymes in the body. As for the kind, the thing which fully satisfies in terms of safety has not been obtained.

On the other hand, recently, the mechanism of the occurrence of rough skin has been elucidated biochemically. It has been pointed out that changes in the activities of proteases, particularly serine proteases such as plasmin and plasminogen activator (PA), are deeply involved in the formation of various skin diseases accompanied by rough skin and abnormal keratinization. For example, in psoriasis, which is a representative of inflammatory dyskeratosis, the presence of strong PA activity in the parakeratotic site of the affected epidermis (Haustein: Arch. Klin. Exp. Dermatol;
34, 1969) and psoriasis scales using a high-concentration salt solution
Report that A was extracted (Fraki, Hopsu-Havu: Arch. Der
matol.Res; 256,1976). PA works specifically on plasminogen, the precursor of plasmin,
It is a protease that converts it to active plasmin. There are also reports showing that a compound known as a serine protease inhibitor suppressed skin roughness (Kenj
i kitamura: J. Soc. Cosmet. Chem. Jpn; 29 (2), 1995).

[0005] In view of the above situation, the present inventors have:
As a result of examining the melanin production inhibitory effect, whitening effect and skin roughening effect in a wide variety of combinations of substances, Akebii or its solvent extract, xylitol, mannitol, one or more selected from the group consisting of erythritol It has been found that the combination has a melanin production-suppressing effect, a whitening effect and a skin roughness-improving effect, and the present invention has been completed.

[0006]

That is, the present invention is characterized in that it contains, as an active ingredient, Akebi or its solvent extract and one or more selected from the group consisting of xylitol, mannitol and erythritol. It is a skin external preparation for whitening and / or improving skin roughness.

It is known that akebi or the solvent extract thereof used in the present invention has a beautiful skin effect, an anti-stain effect, and an anti-inflammatory effect (Japanese Patent Publication No. 01-42411). Further, xylitol used in the present invention, mannitol,
It is known that erythritol is effective for improving rough skin (JP-A-4-124118). However, by combining the extract of akebi, which is a feature of the present application, with one or more selected from the group consisting of xylitol, mannitol, and erythritol, it is possible to achieve particularly excellent whitening effect and skin roughness improving effect. Was not known.

[0008]

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in detail.
The external preparation for skin of the present invention contains, as active ingredients, Akebii or a solvent extract thereof and one or more selected from the group consisting of xylitol, mannitol, and erythritol. Akebia (Akebia quinata D) used in the present invention
ecne) is a plant classified in the genus Akebi in the genus Akebiaceae, and whole plants such as stems, roots, leaves, and seeds thereof are suitable for the present invention. Incidentally, in the present invention, Akebia (Akebia quinata D
ecne, a congener of Akebia quinata
Decne) and Akebia akebi (akebiapentaphylla Makino)
Stalks, leaves, seeds and the like of closely related species and subspecies can also be suitably used.

These plants can be used either raw or dried, but are preferably used as a dry powder or a solvent extract from the viewpoints of usability, formulation and the like.

The above plant extract can be obtained by a conventional method. For example, the plant extract can be obtained by immersing or heating and refluxing the plant with an extraction solvent, followed by filtration and concentration. As the extraction solvent, any solvent can be used as long as it is a solvent usually used for extraction. For example, organic solvents such as alcohols such as methanol and ethanol, aqueous alcohols, acetone, ethyl acetate, and 1,3-butylene glycol are used. And water can be used alone or in combination. The extract may be obtained by using the above-mentioned solvent and subjecting it to a treatment such as partitioning or purification such as chromatography.

The amount of Akebei or the solvent extract thereof in the present invention is 0.000 as a dry matter in the total amount of the external preparation.
01 to 20.0% by weight, preferably 0.0001 to 1
0.0% by weight. If the amount is less than 0.00001% by weight, the effects of the present invention cannot be sufficiently exhibited, and if it exceeds 20.0% by weight, it is difficult to formulate the composition, which is not preferable. Further, even if the content is 10.0% by weight or more, the effect is not so much improved.

The xylitol, mannitol and erythritol of the present invention are sugar alcohols. The carbon number is 5 for xylitol, 6 for mannitol, and 4 for erythritol.

In the present invention, the amount of the xylitol compound is 0.001 to 20.0% as a dry matter in the total amount of the external preparation.
% By weight, preferably 0.01 to 10.0% by weight.
If the amount is less than 0.001% by weight, the effect of the present invention is not sufficiently exhibited, and if the amount is more than 20.0% by weight, it is not preferable because formulation is difficult.

The external preparation for skin of the present invention includes, in addition to the above essential components, components usually used in external preparations for skin such as cosmetics and pharmaceuticals, for example, as long as the effects of the present invention are not impaired.
Moisturizing agents, antioxidants, oily components, ultraviolet absorbers, emulsifiers, surfactants, thickeners, alcohols, powder components, coloring materials, aqueous components, water, various skin nutrients, etc. as needed can do.

For example, imparting a moisturizing effect is useful for the purpose of preventing aging due to drying of the skin. In this case, for example, polyethylene glycol, propylene glycol, glycerin, 1,3-butylene glycol, hexylene glycol, sorbitol, maltitol, chondroitin sulfate, hyaluronic acid, acetylhyaluronic acid, mucoitin sulfate, caronic acid, atelocollagen,
Cholesteryl-12-hydroxystearate, sodium lactate, bile salts, dl-pyrrolidone carboxylate,
Moisturizing agents such as short-chain soluble collagen, diglycerin (EO) PO adduct, lycopodium extract, yarrow extract, and melilot extract can be added to the skin external preparation of the present invention.

In order to further provide a whitening effect, placenta extract, glutathione, Saxifraga extract, arbutin,
Skin lightening agents such as kojic acid, ellagic acid, lucinol, extract of Cola de Caballo, extract of ginger plant Lumpuyan, and the like can be blended in the skin external preparation of the present invention.

In order to impart an anti-inflammatory effect, an anti-inflammatory agent such as a glycyrrhizic acid derivative, a glycyrrhetinic acid derivative, a salicylic acid derivative, hinokitiol, zinc oxide, or allantoin can be added to the external preparation for skin of the present invention.

In addition, activators such as royal jelly, photosensitizers, cholesterol derivatives, calf blood extract, etc., nonylate valenylamide, nicotine, etc., for the purpose of alleviating the adverse effects of ultraviolet rays on the skin and suppressing the aging of the skin. Acid benzyl ester, nicotinic acid β-butoxyethyl ester, capsaicin, gingerone, canthari tincture, itctamol, caffeine, tannic acid, α-borneol, nicotinic acid tocophenol, inositol hexanicotinate, cyclandate, cinnarizine, tolazoline, Acetylcholine, verapamil, cepharanthin,
A flow-promoting agent such as γ-oryzanol, an antiseborrheic agent such as sulfur and thianthol, and the like can be added to the skin external preparation of the present invention.

In addition, for various purposes, the following components can be used: muk roe extract component, psyllium extract component, oak extract component, sicon extract component, peony extract component, assembly extract component, birch extract component, sage extract component, loquat extract component, carrot extract component, Aloe extract, mallow extract, iris extract, grape extract, yokuinin extract, loofah extract, lily extract, saffron extract, senkyu extract, ginger extract, hypericum extract, ononis extract, rose Marie extract ingredients,
Garlic extract, pepper extract, licorice extract,
Chimney extract, corn extract, marjoram extract, yakisou extract, karin extract, psycho extract, edible maize extract, emicaceae extract, whey extract and the like can be blended in the skin external preparation of the present invention. .

Further, in order to impart unique effects possessed by each vitamin, vitamin A such as vitamin A, β-carotene, retinol, retinol acetate, retinol propionate, retinol palmitate, riboflavin,
Vitamin B2 such as riboflavin butyrate, flavin adenine nucleotide, vitamin B6 such as pyridoxine hydrochloride and pyridoxine dioctanoate, ascorbic acid,
Vitamin Cs such as magnesium ascorbate, ascorbic acid glucoside, ascorbic acid dipalmitate, ascorbic acid-2-sodium sulfate, ascorbic acid phosphate, DL-α-tocophenol-ascorbic acid diester dipotassium phosphate;
Pantothenic acids such as calcium pantothenate, pantoenyl alcohol, pantoenyl ether ether, and acetyl pantothenyl ethyl ether; vitamin Ds such as ergocalciphenol and cholecalciphenol; nicotinic acids such as nicotinic acid, nicotinamide, and benzyl nicotinate , Α-tocopherol acetate, tocopherol acetate, nicotinic acid-α-tocopherol, succinic acid-α-tocopherol and other vitamins E, vitamin P, biotin and other vitamins can be incorporated into the skin external preparation of the present invention.

Further, disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, gluconic acid, malic acid,
Sequestering agents such as trisodium hydroxyethyl triacetate,
Tranexamic acid and its derivatives, arginine, lysine, ornithine, glutamine, alanine, histidine,
Leukine, isoleucine, methionine, threonine, phenylalanine, tryptophan, cysteine, cystine, tyrosine, proline, aspartic acid, glutamic acid, amino acids such as serine and derivatives thereof, trimethylglycine, polypeptides such as polyaspartic acid, etc. Agent.

Further, the external preparation for skin of the present invention can be widely applied to cosmetics, pharmaceuticals and quasi-drugs applied to the outer skin, particularly preferably cosmetics. Any solution can be used as long as it can be applied to a solution system, a solubilizing system, an emulsifying system, a powder dispersion system, a water-oil two-layer system, and a water-oil-
An arbitrary dosage form such as a three-layer powder system, an ointment, a gel, and an aerosol is applied.

The form of use is arbitrary, for example, lotion, cream, milky lotion, lotion, pack, ointment,
In addition to mousse and soap, any cosmetics such as foundations and lipsticks, bath preparations and the like may be used as long as they are conventionally used for external preparations for the skin, and the dosage form is not particularly limited.

[0024]

EXAMPLES Next, the present invention will be described in more detail with reference to examples, but the technical scope of the present invention is not limited to these examples. In addition, all compounding amounts are weight%. Prior to the examples, test methods and results of a melanin-suppressing effect, a whitening effect, and a skin roughness-improving effect of the external preparation for skin according to the present invention will be described.

Test Methods for Melanin Suppressing Effect and Whitening Effect and Their Results Preparation of Sample 50 g of a stem portion of Akebia (Akebia quinata Decne) was immersed in ethanol at room temperature for 1 week, and the extract was concentrated to obtain 2.28 g of an ethanol extract. These extracts are combined with DM
Dissolve 1% in SO, dilute this solution to adjust the concentration,
The following experiment was performed using this.

2. Cell culture method B16 melanoma cultured cells derived from mice were used. 1
0% FBS and theophylline (0.09 mg / ml)
Was cultured in a CO ₂ incubator (95% air, 5% carbon dioxide) at 37 ° C. in an Eagle MEM medium containing After 24 hours of culture, the plant extract solution was adjusted to a final concentration of 1
0 ^-2 to 10 ^-5 % by weight was added. Sugar alcohol was added at a concentration of 0.1%. After the addition, the culture was further continued for 3 days, and the visual evaluation of the amount of melanin production was determined by the following method.

3. Visual measurement of the amount of melanin Place the diffusion plate on the lid of the plate of the well, observe the amount of melanin in the cells with an inverted microscope, and compare the case of the sample without the extract of plant and sugar alcohol (reference). Compared. Table 1 shows the results.

<Judgment Criteria> ：: White (melanin content) Δ: Slightly white (melanin content) ×: Standard (melanin content)

[0029]

[Table 1] ─────────────────────────────────── Test Melanin production visual evaluation ─────濃度 Concentration (% by weight) 10 ^-5 10 ^-4 10 ^-3 10 ^-2 10 ^-1 ─────────────────── ──────────────── Akebi extract × × × ○ − Xylitol − − − − − × Mannitol − − − − − × Erythritol − − − − × Xylitol 0.1% + Akebi extract × × ○ ○ − 0.1% mannitol + Akebi extract × × △ ○ − Erythritol 0.1% + Akebi extract × × ○ ○ − ────────────────────── ─────────────

4. Skin whitening effect test [Test method] Each subject was exposed to sunlight in summer for 4 hours (2 hours a day for 2 days). It was applied once every morning and evening for four weeks. The panel was divided into 8 groups and divided into 4 groups, and the test was performed according to the following prescription. <Production method> An aqueous phase and an alcohol phase are respectively prepared, and then both are mixed and solubilized.

[Evaluation Method] The lightening effect after use was determined based on the following criteria. <Judgment criteria> ：: When the ratio showing significant effect and effectiveness among the subjects is 80% or more 割 合: The ratio showing significant effect and effectiveness among the subjects is 50% or more
Less than 80% △: The proportion of the test subjects showing excellent and effective is 30% or more
Less than 50% ×: The proportion of subjects showing excellent and effective is less than 30%

[0032]

[Table 2] 薬 剤 Drug (Blending amount, wt%) Effect ──────── ───────────────────── No addition × Akebi extract (0.1%) △ Xylitol (1.0%) × Akebi extract (0.1% ) + Xylitol (1.0%) ○ ─────────────────────────────

As is clear from Table 2, the effect of the combination of the Akebae extract and xylitol prevents the deposition of excessive melanin pigment and prevents the color from becoming dark after exposure to sunlight. It was recognized that.

Test Method for Improving Roughness of Skin and Results Thereof As a sample, 50 g of stem portion of akebia (Akebia quinata Decne) was immersed in hot water and filtered to obtain an extract.
The effect of improving skin roughness was evaluated on a human body panel using a lotion having the formulation shown in FIG. That is, a replica of the skin (face cheek) of a healthy female was collected using a replica agent, and the skin surface morphology was observed with a microscope (17 ×). Based on the skin crest state and the peeling state of the stratum corneum, 30 persons who were judged to have a rough skin rating of 1 or 2 based on the following criterion were set as rough skin panels, divided into three groups of ten persons, and each sample lotion for each group. Was assigned. A sample lotion was applied to the face twice a day for 4 weeks, and after 4 weeks, the skin condition was observed again according to the replica method described above and evaluated according to the criteria. Table 4 shows the results.

[0035]

[Table 3] 料 Sample of the present invention Comparative product 1 Comparative product 2 品───────────────────────── Akebi extract 2.0 2.0-xylitol 1.0-1.0 glycerin 1.0 1.0 1.0 1,3-butylene glycol 4.0 4.0 4.0 ethanol 7.0 7.0 7.0 Polyoxyethylene (20 mol) Oleyl alcohol 0.5 0.5 0.5 Purified water Residue Residue Residue ──────────────────────────────

<Replica Judgment Criteria> 1: Elimination of skin sulcus and skin ridges, and turning-up of a wide range of stratum corneum are recognized. 2: The crevices and crevices are unclear and the horny layer is turned up. 3: Skin sulcus and skin ridge are recognized, but flat. 4: Skin sulcus and skin hills are clear. 5: The skin groove and skin hills are clear and well-ordered.

[0037]

[Table 4]

As can be seen from Table 4, the lotion of the present invention exhibited an excellent effect of improving rough skin as compared with the lotion of the comparative product.

[0039] (Manufacturing method) Propylene glycol, akebi ethanol extract and caustic potash were added to ion-exchanged water, dissolved and heated.
Keep at 0 ° C. (aqueous phase). Mix other ingredients, heat and melt.
Keep at 0 ° C. (oil phase). The oil phase is gradually added to the water phase, and after the addition is completed, the temperature is maintained for a while to cause a reaction. Thereafter, the mixture is uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well.

[0040] (Production method) Add propylene glycol to ion-exchanged water,
Heat and maintain at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is added to the water phase, pre-emulsified, homogenized with a homomixer, and cooled to 30 ° C. with good stirring.

[0041] (Preparation method) Soap powder and borax are added to ion-exchanged water and heated to 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is gradually added to the aqueous phase while stirring to carry out the reaction. Thereafter, the mixture is uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well.

Example 4 Emulsion (Prescription)% by Weight Stearic Acid 2.5 Cetyl Alcohol 1.5 Vaseline 5.0 Liquid Paraffin 10.0 Polyoxyethylene (10 mol) Monooleate 2.0 Polyethylene Glycol 1500 0 Triethanolamine 1.0 Carboxyvinyl polymer 0.05 (trade name: Carbopol 941, BFGoodrich Chemical company) Echiacetate ethyl acetate extract 0.02 Erythritol 1.0 Retinol 0.1 Sodium bisulfite 0.01 Ethyl paraben 0 0.3 Appropriate amount of perfume Residual ion-exchanged water (Preparation method) Dissolve the carboxyvinyl polymer in a small amount of ion-exchanged water (phase A). Polyethylene glycol 1500 and triethanolamine are added to the remaining ion-exchanged water, and the mixture is heated and dissolved and maintained at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is added to the water phase, pre-emulsification is performed, phase A is added, and the mixture is uniformly emulsified with a homomixer. After the emulsification, the mixture is cooled to 30 ° C. while stirring well.

[0043] (Production method) Add propylene glycol to ion-exchanged water,
Heat and maintain at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The aqueous phase is gradually added while stirring the oil phase, and after uniform emulsification with a homomixer,
Cool to 30 ° C with good stirring.

[0044] (Production method) Carbopol 940 is uniformly dissolved in ion-exchanged water, while a plant extract and polyoxyethylene (50 mol) oleyl alcohol ether are dissolved in 95% ethanol and added to the aqueous phase. Next, after adding other components, the mixture is neutralized with caustic soda and L-arginine to increase the viscosity.

[0045] (Production method) Dissolve A phase and B phase uniformly, and add B
Add phases and solubilize. Next, the C phase in which the Akebei dry powder is dispersed is added thereto, followed by filling.

[0046]

As described above, the external preparation for skin of the present invention has an effect of inhibiting melanin production, and is excellent in lightening and whitening of pigmentation, spots, freckles, liver spots, etc. after sunburn. It has an effect, and also has an excellent effect in improving skin roughness and roughness.

Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat II (Reference) A61P 17/00 A61P 17/00 (72) Inventor Taiichi Nakayama 1050 Nippacho, Kohoku-ku, Yokohama-shi, Kanagawa Shiseido Co., Ltd. F-term in the 1st Research Center (reference) 4C083 AA111 AA112 AA122 AB352 AC022 AC072 AC102 AC122 AC131 AC132 AC182 AC242 AC312 AC352 AC422 AC482 AC542 AC582 AD092 AD202 AD512 AD622 AD662 CC02 CC05 CC07 DD27 DD31 EE12 EE16 4C088 AB12 AC04 CA04 CA05 BA08 MA08 MA63 NA14 ZA89 ZC75 4C206 AA01 AA02 CA05 MA02 MA04 MA83 NA14 ZA89 ZC75

Claims (4)

[Claims] 1. An external preparation for whitening skin, comprising, as active ingredients, an akebi or a solvent extract thereof and one or more selected from the group consisting of xylitol, mannitol and erythritol. 2. A skin external preparation for improving rough skin, comprising as active ingredients, Akebii or a solvent extract thereof and one or more selected from the group consisting of xylitol, mannitol and erythritol. 3. An external preparation for both use in improving whitening and rough skin, characterized by containing as active ingredients, akebi or a solvent extract thereof and one or more selected from the group consisting of xylitol, mannitol and erythritol. . 4. The compounding amount of the akebi or the solvent extract thereof is 0.00001 to 20.0% by weight in terms of solid content,
Xylitol, mannitol, one or more selected from the group consisting of erythritol in a compounding amount of 0.00
The external preparation for skin according to any one of claims 1 to 3, which is 1 to 20.0% by weight.