JP2006265141A - Skin-whitening agent - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a skin-whitening agent that has excellent skin-whitening action and develops excellent effects on the sedimentation of the pigment after the sunburn and brightening freckles, liver spots or the like and whitening skin. <P>SOLUTION: The skin-whitening agent comprises solvent-extracted products selected from Eryngium plant, Sterculia villosa Roxb. ex. Smith, Litsea plant and Pterocarpus plants. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to a whitening agent, and more particularly to a whitening agent that is effective in preventing and improving pigmentation, blotches, freckles, and liver spots after sunburn and has an excellent effect on skin whitening.

  Although there are some unclear points about the mechanism of skin blemishes, etc., in general, melanin pigments are formed due to hormonal abnormalities or stimulation of ultraviolet rays from sunlight, which abnormally deposits in the skin. It is considered a thing. This melanin pigment, which causes skin coloration, is produced in melanogenic granules (melanosomes) in melanocytes (melanocytes) between the epidermis and dermis, and the generated melanin diffuses to neighboring cells by osmotic action .

The biochemical reaction in this melanocyte is estimated as follows. That is, a process in which tyrosine, which is an essential amino acid, becomes dopaquinone by the action of the enzyme tyrosinase, which is converted into black melanin through a red pigment and a colorless pigment by enzymatic or non-enzymatic oxidation is a melanin pigment formation process.
As for the above-mentioned whitening agent that suppresses the production of melanin pigment, various plant-derived extracts have been developed in the hope of safety and mildness of irritation to the skin (for example, Patent Documents 1 to 4). reference).
JP-A-8-3109939 JP-A-7-89843 Japanese Patent Laid-Open No. 9-30954 JP 2003-73224 A

  As described above, for plant-derived whitening agents, it is required to find a new plant that exhibits a new whitening effect. Accordingly, the present inventors have aimed to provide a new plant-derived whitening agent in response to such a conventional situation.

  As a result of intensive studies in view of the present situation, the present inventors have found that a specific plant extract has an excellent whitening effect, and have completed the present invention.

  The present invention is selected from the Eryngium plant, the Sterculia Sterculia villosa Roxb.ex.Smith, the Litsea plant, and the Pterocarpus plant It is a whitening agent characterized by comprising one or two or more solvent extracts.

  Moreover, according to this invention, the external preparation for skin characterized by mix | blending the solvent extract of the Aceraceae Eryngium plant (Eryngium) plant is provided.

  Furthermore, according to the present invention, a whitening method characterized by whitening the skin using the whitening agent, and producing a whitening skin cosmetic by adding the whitening agent to an aqueous phase or an oil phase. A method for producing a whitening skin cosmetic is provided.

  Here, Eryngium foetidum L. is suitable as the genus Eryngium plant, and Litsea monopelata Roxb. Pterocarpus sp. Is preferred as the plant.

  The whitening agent of the present invention has an excellent whitening action, and has an excellent effect on lightening and whitening of pigmentation, stains, freckles, and liver spots after sunburn.

Hereinafter, the present invention will be described in detail.
In the present invention, the Apiaceae genus Pleuro is a dicotyledonous plant, and is a hairless annual plant to a perennial plant. More than 200 types are distributed widely from temperate regions to temperate zones around the Mediterranean coast. In the present invention, Eryngium foetidum L. which is suitably used as a plant belonging to the genus Ceramaceae is native to tropical America and has been widely naturalized in temperate and subtropical regions. Young leaves have fragrance, and are used as seasoning vegetables in the American tropics and Malaysia. In Indonesia, the whole plant is called Walang Jeni and is used as a stomachic medicine. It is also used for sputum, high blood pressure, fever and chills.

  Sterculia villosa Roxb.ex.Smith belonging to the genus Pingoponoki used in the present invention is also called as “Bottle Tree” or “Trumpet flower”. A dicotyledonous plant, a deciduous or evergreen tree or shrub. Distributed mainly in the tropics, bark decoction is used to treat psychosis.

  The camphoraceae genus plant used in the present invention is a dicotyledonous plant, which is a deciduous or evergreen tree. It is widely distributed in the tropics and temperate zones, and about 400 species are known all over the world except Africa and Europe. In the present invention, the decoction juice of the stem and bark of Litsea monopelata Roxb.Pers, which is preferably used as a plant of the genus Camelliaaceae, is used as a wind stimulant and an appetite enhancer.

  The legume Pterocarpus plant used in the present invention is a dicotyledonous plant, which is a deciduous or evergreen tree or a vine. More than 100 species are distributed in the tropics and temperate areas, and high-quality materials are used as furniture and utensils as karin. In the present invention, Pterocarpus sp. Which is suitably used as a leguminous genus Spiraea is useful for fractures, bruises, psoriasis and the like. Bark and xylem are used as dyes.

  The plant extract used in the present invention is obtained by immersing or heating and refluxing the above-mentioned plant leaves, stems, flowers, bark, seeds or fruits, whole plants, etc. together with an extraction solvent, followed by filtration and concentration. Among them, Eryngium foetidum L. is preferably an extract from whole grass, Sterculia villosa Roxb.ex.Smith is preferably an extract from bark, Litsea monopelata Roxb.Pers is preferably an extract from stem or bark, Pterocarpus sp. is preferably an extract from roots.

  The extraction solvent used in the present invention may be any solvent as long as it is usually used for extraction, and in particular, alcohols such as methanol, ethanol and 1,3-butylene glycol, hydrous alcohols, organic solvents such as acetone and ethyl acetate. Can be used alone or in combination, but alcohols such as methanol, ethanol and 1,3-butylene glycol are particularly preferred. An extraction solvent containing a large amount of water is not preferable because extraction of the active ingredient is suppressed.

  In the present invention, there are provided a skin external preparation and a whitening skin external preparation characterized by containing a solvent extract of an Eryngium plant. Here, it is preferable that the Apiaceae genus Phyllophyllum is Eryngium foetidum L.

  Moreover, in this invention, the skin external preparation for whitening can be mix | blended by mix | blending the 1 or 2 or more types of solvent extract chosen from the said plant.

  The compounding quantity of the plant extract in this skin external preparation for whitening is 0.0005-1.0 mass% as a dry substance in the external preparation whole quantity, Preferably it is 0.001-0.5 mass%. If it is less than 0.0005% by mass, the effect referred to in the present invention is not sufficiently exhibited, and if it exceeds 10.0% by mass, it is difficult to make a preparation, which is not preferable. Moreover, even if it mixes 5.0 mass% or more, the improvement of the big effect is not seen.

  In addition to the essential components described above, the skin external preparation and skin whitening external preparation of the present invention include components that are usually used in skin external preparations such as cosmetics and pharmaceuticals, such as humectants, antioxidants, oily components, ultraviolet rays. Absorbers, surfactants, thickeners, alcohols, powder components, colorants, aqueous components, water, various skin nutrients, and the like can be appropriately blended as necessary.

  Others, disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, sequestering agents such as gluconic acid, caffeine, tannin, verapamil, tranexamic acid and its derivatives, licorice extract, grabrizine , Hot water extract of fire thorn fruit, various herbal medicines, drugs such as tocopherol acetate, glycyrrhizic acid and its derivatives or salts thereof, vitamin C, magnesium ascorbate phosphate, glucoside ascorbate, arbutin, kojic acid, etc. Whitening agents, sugars such as glucose, fructose, mannose, sucrose, trehalose and the like can be appropriately blended.

  The skin external preparation and whitening skin external preparation of the present invention may be any one as long as they are used in conventional skin external preparations such as ointments, creams, emulsions, lotions, packs, bath preparations, etc., and the dosage form is not particularly limited.

The present invention will be described in more detail with reference to the following examples, but the present invention is not limited thereto. Unless otherwise specified, the amount is shown in mass%.
Prior to the examples, the test method and the results regarding the melanin production inhibitory effect of the plant extract of the present invention will be described.

1. Sample preparation
(1) Sterculia villosa Roxb.ex.Smith methanol extract
100 mL of methanol was added to 10.0 g of bark of Sterculia villosa Roxb.ex.Smith, and it was immersed for 7 days at room temperature and then filtered. The methanol in the filtrate was distilled off to obtain 1.313 g (solid content concentration) of the extract.
(2) Litsea monopelata Roxb.Pers methanol extract
100 mL of methanol was added to 10.0 g of stem and bark of Litsea monopelata Roxb.Pers, and after immersion for 7 days at room temperature, filtration was performed. The methanol in the filtrate was distilled off to obtain 0.224 g (solid content concentration) of the extract.
(3) Eryngium foetidum L. Methanol extract
200 mL of methanol was added to 10.0 g of whole plant of Eryngium foetidum L., and immersed for 7 days at room temperature, followed by filtration. The methanol in the filtrate was distilled off to obtain 0.695 g (solid content concentration) of the extract.
(4) Pterocarpus sp. Methanol extract
100 mL of methanol was added to 10.0 g of roots of Pterocarpus sp., Immersed for 7 days at room temperature, and then filtered. The methanol in the filtrate was distilled off to obtain 1.169 g (solid content concentration) of the extract.

2. Melanin production inhibitory effect test method and the results The resulting plant methanol extract was used as a test sample, and the melanin production inhibitory effect was measured and evaluated by the following method.

(1) Cell culture method Mouse-derived B16 melanoma culture cells were used. The cells were cultured in an Eagle's MEM medium containing 10% FBS and theophylline (0.09 mg / ml) in a CO ₂ incubator (95% air, 5% carbon dioxide) at 37 ° C. After 24 hours of culturing, the sample solution was added so that the final concentration (concentration in terms of dried extract) was 10 ^{−4 to} 5 × 10 ⁻³ mass%, and the culture was further continued for 3 days. Visibility determination was performed.
Further, arbutin, which has been known to have a melanin production inhibitory effect, was also tested in the same manner as described above.

(2) Visibility measurement of melanin amount Place the diffusion plate on the lid of the well plate, observe the amount of melanin in the cell with an inverted microscope, and the sample (reference) to which no plant extract is added Compared. The results are shown in Table 1.

(Score: Criteria)
In the case of the sample (reference) to which no plant extract is added, “0” is set, “−2” is set to “−2”, which is judged to be sufficiently white compared to the reference and the amount of melanin is small. Judgment was made.

  Table 1 shows that Eryngium foetidum L., Sterculia villosa Roxb.ex.Smith, Litsea monopelata Roxb.Pers, and Pterocarpus sp. Have an excellent melanin inhibitory effect and are useful as a whitening agent.

  Below, the formulation example of the skin external preparation by this invention of various dosage forms is demonstrated as an Example.

Example 1 Cream (Prescription)
Stearic acid 5.0% by mass
Stearyl alcohol 4.0
Isopropyl myristate 18.0
Glycerol monostearate 3.0
Propylene glycol 10.0
Eryngium foetidum L. Methanol extract 0.01
Caustic potash 0.2
Sodium bisulfite 0.01
Preservative Appropriate amount Perfume Appropriate amount Ion-exchanged water Residue (Process)
Propylene glycol, Eryngium foetidum L. methanol extract and caustic potash are added to ion-exchanged water, dissolved, heated and maintained at 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted, and kept at 70 ° C. (oil phase). The oil phase is gradually added to the aqueous phase, and after the addition is complete, the temperature is maintained for a while to cause the reaction. Thereafter, the mixture is uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well.

Example 2 Cream (Prescription)
Stearic acid 2.0% by mass
Stearyl alcohol 7.0
Hydrogenated Lanolin 2.0
Squalane 5.0
2-Octyldodecyl alcohol 6.0
Polyoxyethylene (25 mol) cetyl alcohol ether 3.0
Glycerin monostearate ester 2.0
Propylene glycol 5.0
Sterculia villosa Roxb.ex.Smith ethanol extract 0.05
Sodium bisulfite 0.03
Ethylparaben 0.3
Perfume Appropriate amount Ion exchange water Residue (Production method)
Propylene glycol is added to ion-exchanged water and heated to 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted, and kept at 70 ° C. (oil phase). The oil phase is added to the aqueous phase, pre-emulsified, and uniformly emulsified with a homomixer, and then cooled to 30 ° C. while stirring well.

Example 3 Cream (Prescription)
Solid paraffin 5.0% by mass
Beeswax 10.0
Vaseline 15.0
Liquid paraffin 41.0
Glycerin monostearate ester 2.0
Polyoxyethylene (20 mol) sorbitan monolaurate 2.0
Soap powder 0.1
Borax 0.2
Litsea monopelata Roxb.Pers acetone extract 0.05
Pterocarpus sp. Ethanol extract 0.05
Sodium bisulfite 0.03
Ethylparaben 0.3
Perfume Appropriate amount Ion exchange water Residue (Production method)
Add soap powder and borax to ion-exchanged water, dissolve by heating and maintain at 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted, and kept at 70 ° C. (oil phase). The reaction is gradually added while stirring the oil phase in the aqueous phase. After completion of the reaction, the mixture is uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well after emulsification.

Example 4 Latex (Prescription)
Stearic acid 2.5% by mass
Cetyl alcohol 1.5
Vaseline 5.0
Liquid paraffin 10.0
Polyoxyethylene (10 mol) monooleate 2.0
Polyethylene glycol 1500 3.0
Triethanolamine 1.0
Carboxyvinyl polymer 0.05
(Product name: Carbopol 941, BFGoodrich Chemical company)
Eryngium foetidum L. Acetic acid ethyl ester extract 0.01
Sodium bisulfite 0.01
Ethylparaben 0.3
Perfume Appropriate amount Ion exchange water Residue (Production method)
Dissolve the carboxyvinyl polymer in a small amount of ion-exchanged water (A phase). Polyethylene glycol 1500 and triethanolamine are added to the remaining ion-exchanged water, dissolved by heating and maintained at 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted, and kept at 70 ° C. (oil phase). Add the oil phase to the water phase, preliminarily emulsify, add the A phase and uniformly emulsify with a homomixer.

Example 5 Latex (Prescription)
Microcrystalline wax 1.0% by mass
Beeswax 2.0
Lanolin 20.0
Liquid paraffin 10.0
Squalane 5.0
Sorbitan sesquioleate ester 4.0
Polyoxyethylene (20 mol) sorbitan monooleate 1.0
Propylene glycol 7.0
Sterculia villosa Roxb.ex.Smith acetone extract 10.0
Sodium bisulfite 0.01
Ethylparaben 0.3
Perfume Appropriate amount Ion exchange water Residue (Production method)
Propylene glycol is added to ion-exchanged water and heated to 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted and kept at 70 ° C. (oil phase). While stirring the oil phase, the aqueous phase is gradually added thereto and emulsified uniformly with a homomixer. Cool to 30 ° C. while stirring well after emulsification.

Example 6 Jelly (Prescription)
95% ethyl alcohol 10.0% by mass
Dipropylene glycol 15.0
Polyoxyethylene (50 mol) oleyl alcohol ether 2.0
Carboxyvinyl polymer 1.0
(Product name: Carbopol 940, BFGoodrich Chemical company)
Caustic soda 0.15
L-Arginine 0.1
Litsea monopelata Roxb.Pers ethanol extract 7.0
Sodium 2-hydroxy-4-methoxybenzophenone sulfonate 0.05
Ethylenediaminetetraacetate, 3 sodium, 2 water 0.05
Methylparaben 0.2
Perfume Appropriate amount Ion exchange water Residue (Production method)
Carbopol 940 is uniformly dissolved in ion-exchanged water, while Litsea monopelata Roxb.Pers ethanol extract, polyoxyethylene (50 mol) oleyl alcohol ether is dissolved in 95% ethanol and added to the aqueous phase. Next, after adding other components, the mixture is neutralized and thickened with caustic soda and L-arginine.

Example 7 Essence (Prescription)
(Phase A)
Ethyl alcohol (95%) 10.0% by mass
Polyoxyethylene (20 mol) octyldodecanol 1.0
Pantotenyl ethyl ether 0.1
Pterocarpus sp. 1,3-butylene glycol extract 1.5
(Solid content concentration 0.16%)
Methylparaben 0.15
(Phase B)
Potassium hydroxide 0.1
(Phase C)
Glycerin 5.0
Dipropylene glycol 10.0
Sodium bisulfite 0.03
Carboxyvinyl polymer 0.2
(Product name: Carbopol 940, BFGoodrich Chemical company)
Purified water residue (production method)
A phase and C phase are uniformly dissolved, and A phase is added to C phase to solubilize. Next, filling is performed after adding phase B.

Example 8 Pack (Prescription)
(Phase A)
Dipropylene glycol 5.0% by mass
Polyoxyethylene (60 mol) hydrogenated castor oil 5.0
(Phase B)
Eryngium foetidum L. Methanol extract 0.01
Olive oil 5.0
Tocopherol acetate 0.2
Ethylparaben 0.2
Fragrance 0.2
(Phase C)
Sodium bisulfite 0.03
Polyvinyl alcohol 13.0
(Saponification degree 90, polymerization degree 2,000)
Ethanol 7.0
Purified water residue (production method)
A phase, B phase, and C phase are uniformly dissolved, and B phase is added to A phase to solubilize. Next, this is added to phase C and then filled.

Example 9 Solid Foundation (Prescription)
Talc 43.1% by mass
Kaolin 15.0
Sericite 10.0
Zinc flower 7.0
Titanium dioxide 3.8
Yellow iron oxide 2.9
Black iron oxide 0.2
Squalane 8.0
Isostearic acid 4.0
Monooleic acid POE sorbitan 3.0
Isocetyl octoate 2.0
Sterculia villosa Roxb.ex.Smith ethanol extract 1.0
Preservative appropriate amount perfume appropriate amount (production method)
Thoroughly mix the powder components of talc to black iron oxide with a blender. Fill and mold.

Example 10 Emulsification Foundation (Cream Type)
(Prescription)
(Powder part)
Titanium dioxide 10.3% by mass
Sericite 5.4
Kaolin 3.0
Yellow iron oxide 0.8
Bengala 0.3
Black iron oxide 0.2
(Oil phase)
Decamethylcyclopentasiloxane 11.5
Liquid paraffin 4.5
Polyoxyethylene-modified dimethylpolysiloxane 4.0
(Water phase)
Purified water 50.0
1,3-butylene glycol 4.5
Litsea monopelata Roxb.Pers ethanol extract 1.5
Sorbitan sesquioleate 3.0
Preservative appropriate amount perfume appropriate amount (production method)
After the aqueous phase is heated and stirred, the powder part sufficiently mixed and pulverized is added and homomixed. Furthermore, after adding the heat-mixed oil phase and carrying out a homomixer process, a fragrance | flavor is added with stirring and it cools to room temperature.

Claims (10)

  One or two selected from the genus Eryngium, Sterculia villosa Roxb.ex.Smith from the genus Pteropaceae (Sterculia), the Litsea plant, and the Pterocarpus plant A whitening agent comprising a solvent extract of at least seeds.   The whitening agent according to claim 1, wherein the plant belonging to the genus Ceratoceae is an Eryngium foetidum L.   The whitening agent according to claim 1, wherein the camphoraceae plant is Litsea monopelata Roxb.Pers.   The whitening agent according to claim 1, wherein the leguminous genus Spiraea is Pterocarpus sp.   An external preparation for skin comprising a solvent extract of Eryngium plant.   The external preparation for skin according to claim 4, wherein the plant of the genus Ceratoceae is an Eryngium foetidum L.   A skin whitening preparation for skin whitening comprising a solvent extract of an Eryngium plant.   The skin external preparation for skin whitening according to claim 4, wherein the genus Ceratoceae is an Eryngium foetidum L.   A whitening method comprising whitening the skin using the whitening agent according to claim 1. A method for producing a whitening skin cosmetic, wherein the whitening agent according to claim 1 is added to an aqueous phase or an oil phase to produce a whitening skin cosmetic.