JP2007126367A - Bleaching ingredient, bleaching method and method for producing bleaching skin care preparation - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To a bleaching ingredient that has an excellent melanogenesis inhibitory action and excellent hypochromic and bleaching effect on pigmentation/stain/freckle/liver spot, etc., after sunburn. <P>SOLUTION: The bleaching ingredient comprises an extract of one or more kinds of plants selected from the group consisting of Pleomele angustifolia (Roxb.) N. E. Br. of a plant of the family Liliaceae, Oxalis corymbosa DC. of a plant of the family Oxalidaceae and Sonchus oleraceus L. of a plant of the family Compositae. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to a whitening agent that suppresses the production of melanin and is effective in preventing and improving pigmentation such as spots and freckles.

  It is thought that pigmentation such as skin spots and freckles causes excessive melanin formation due to hormonal abnormalities, ultraviolet rays, and local inflammation of the skin, which deposits in the skin. This melanin, which causes skin pigmentation, is produced in organelles called melanosomes in pigment cells (melanocytes) in the basal layer of the epidermis, and the produced melanin is taken up by surrounding keratinocytes (keratinocytes). Melanin in the melanocytes is produced by converting tyrosine into black melanin through an enzymatic or non-enzymatic oxidation reaction via dopaquinone by the action of the enzyme tyrosinase. Therefore, it is important to suppress the activity of tyrosinase, which is the first stage reaction, in order to suppress the production of melanin.

  Conventionally, a substance having a whitening action, that is, a substance that suppresses melanin production has been mainly used for the purpose of preventing or improving the above-mentioned pigment abnormality, for example, a method of orally administering vitamin C in a large amount, A method for injecting glutathione or the like, or a method for locally applying kojic acid, vitamin C and its derivatives, cysteine, etc. in the form of an ointment, cream, lotion or the like is known.

  On the other hand, with regard to compounds that suppress the activity of tyrosinase, the effect of skin pigmentation is not sufficiently improved because the effect of the compound is very slow except for hydroquinone. On the other hand, hydroquinone has an effect, but its general use is limited because of its sensitization. In order to improve the safety, attempts have been made to use higher fatty acid monoesters and alkyl monoethers (see Patent Document 1).

JP 58-154507 A

  However, such monoesters of higher fatty acids are not necessarily safe because they are degraded by hydrolyzing enzymes in the body, and ethers are not sufficiently satisfactory in terms of safety. .

  Therefore, as a result of examining the activity inhibitory effect of tyrosinase on various plant extracts, the present inventors have a tyrosinase inhibitory action on a specific plant extract that has not been known to have such an effect so far. As a result, the present invention has been completed.

  The present invention is selected from the group consisting of Pleomele angustifolia (Roxb.) NE Br., A Liliumceae plant, Oxalis corymbosa DC., An Oxalidaceae plant, Sonchus oleraceus L., a Compositae plant It is a whitening agent characterized by including the extract of 1 type, or 2 or more types of plants.

  The present invention is a whitening method characterized in that skin whitening is performed using the whitening agent.

  The present invention is a method for producing a whitening skin external preparation, wherein the whitening agent is added to an aqueous phase or an oil phase to produce a whitening skin external preparation.

The whitening agent of the present invention has an excellent tyrosinase activity inhibitory action, has lightening effects such as pigmentation / stain / freckle / liver spots after sunburn, and has excellent effects on whitening, and also has excellent safety. Is.
Further, according to the present invention, there is provided a whitening method having effects excellent in lightening and whitening of pigmentation / stain / freckle / liver spots after sunburn, and also in safety.
Furthermore, according to the method for producing a skin whitening external preparation according to the present invention, it has a tyrosinase activity inhibitory effect, and has excellent effects on lightening whitening, such as pigmentation / stains / freckle / liver spots after sunburn. It is possible to produce a skin whitening preparation for skin whitening that is excellent in safety.

The best mode of the present invention will be described below.
Pleomele angustifolia (Roxb.) NE Br. Of the Liliaceae plant used in the present invention, Oxalis corymbosa DC. Of the Oxalidaceae plant, and Sonchus oleraceus L. of the Compositae plant are all used in China. It is a plant that grows in Japan and Southeast Asia.

Among them, Pleomele angustifolia (Roxb.) NE Br. Is a lily family plant called Chinese dragon blood tree, and it is known that it heats the lungs by producing heat, produces saliva, and cools the blood.
Oxalis corymbosa DC. Is a plant of the family Oxalis, which is called safflower sausage in China and is used for colds, coughs, burns and trauma.
Sonchus oleraceus L. is a chrysanthemum plant (harnogeshi), which is called bitter dish in China and is known to be used for dysentery and stomatitis.

  The plant extract used in the present invention is obtained by immersing or heating and refluxing the above-mentioned plant leaves, stems including root stems, roots, fruits, whole plant plants and the like together with an extraction solvent, followed by filtration and concentration. The extraction solvent used in the present invention is not particularly limited as long as it is a solvent that is usually used for extraction, particularly alcohols such as methanol, ethanol, 1,3-butylene glycol, hydrous alcohols, water, acetone, ethyl acetate, etc. Organic solvents can be used alone or in combination. The whitening agent of the present invention contains the above plant extract, but the above plant may be a plant extract used alone or a plant extract used by mixing.

  Pleomele angustifolia (Roxb.) N. E. Br. Used in the present invention preferably uses bark, but other sites can also be used.

  Oxalis corymbosa DC. Used in the present invention is preferably whole plant, but other parts can also be used.

  As Sonchus oleraceus L. used in the present invention, it is preferable to use whole plants, but other sites can also be used.

  In the present invention, each plant can be used either naturally grown or cultivated, and the above plant extract may be used in combination of two or more.

  The whitening agent of the present invention comprises the group consisting of Pleomele angustifolia (Roxb.) NE Br. Of the Liliaceae plant, Oxalis corymbosa DC. Of the Oxalidaceae plant, and Sonchus oleraceus L. of the Compositae plant. Although it contains the extract of the 1 type or 2 or more types of plant selected more, Preferably it consists only of the said plant extract substantially.

  The amount of the above-mentioned plant extract in the external preparation for skin containing the whitening agent of the present invention is 0.001 to 20.0 mass%, preferably 0.01 to 10.0 mass% as a dry product in the total amount of external preparation. It is. If it is less than 0.001% by mass, the effect of the present invention tends to be poor, and if it exceeds 20.0% by mass, it is difficult to make a preparation. Moreover, even if it mixes exceeding 10.0 mass%, the improvement of the big effect is not seen.

  In addition to the above essential components, the external preparation for skin containing the whitening agent of the present invention is usually used for external preparations for skin such as cosmetics and pharmaceuticals, for example, other whitening agents, moisturizers, antioxidants, oily ingredients. UV absorbers, surfactants, thickeners, alcohols, powder components, coloring materials, 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 spine 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, lucinol, ellag Other whitening agents such as acid and chamomile, and sugars such as glucose, fructose, mannose, sucrose, and trehalose can be appropriately blended.

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

  Next, the present invention will be described in more detail with reference to examples. In addition, this invention is not limited by this. A compounding quantity is the mass%. Prior to the examples, a test method and results regarding the tyrosinase activity inhibitory effect and whitening effect of the plant extract of the present invention will be described.

Test method and results Sample preparation (1) Pleomele angustifolia (Roxb.) NE Br. Extract
Pleomele angustifolia (Roxb.) NE Br. Bark 55.85 g was immersed in methanol at room temperature for 1 week, the extract was filtered and the solvent was distilled off to obtain 6.35 g of methanol extract. This extract was dissolved in 1% by mass in DMSO, and this solution was diluted to adjust the concentration. Using this, the following experiment was conducted.
(2) Oxalis corymbosa DC. Extract
30.45 g of whole plant of Oxalis corymbosa DC. Was immersed in methanol at room temperature for 1 week, the extract was filtered and the solvent was distilled off to obtain 4.09 g of methanol extract. This extract was dissolved in 1% by mass in DMSO, and this solution was diluted to adjust the concentration. Using this, the following experiment was conducted.
(3) Sonchus oleraceus L. extract
35.87 g of whole plant portion of Sonchus oleraceus L. was immersed in methanol at room temperature for 1 week, the extract was filtered and the solvent was distilled off to obtain 2.59 g of methanol extract. This extract was dissolved in 1% by mass in DMSO, and this solution was diluted to adjust the concentration. Using this, the following experiment was conducted.

2. Tyrosinase activity inhibitory effect test The enzyme inhibitory action of the plant extract of the present invention was examined using tyrosinase derived from mouse melanoma cell B16 as an enzyme source. That is, the test plant extract and the enzyme of the density | concentration in a table | surface were added to 2 mM L-Tyrosine and 0.1 mM dopa, and it incubated at 37 degreeC. After the reaction, the absorbance of the resulting reddish purple reaction solution was measured at 475 nm. The result was calculated | required by the suppression rate (%) with respect to a test plant extract no addition group.

  The results in Table 1 show that the extracts of Pleomele angustifolia (Roxb.) NE Br., Oxalis corymbosa DC., And Sonchus oleraceus L. inhibit tyrosinase activity without affecting cell growth. It was found to have a whitening effect.

3. Whitening effect test (1) Preparation of whitening agent-containing external preparation for skin The whitening agent was prepared as follows for each sample. The preparation method was carried out by preparing an alcohol phase and an aqueous phase according to a conventional method.
(Alcohol phase)
99% ethanol 70.0 mass%
Whitening agent described in “Table 2” Amount described in “Table 2” (aqueous phase)
Glycerin 5.0
Ion exchange water

(2) Test method For the skin of the panel (n = 5) exposed to ultraviolet rays, each prescription solution was applied once a day for 8 weeks starting 14 days after the exposure to ultraviolet rays. After the application was completed, whether or not there was an inhibitory effect on the pigmentation induced by ultraviolet irradiation was examined at the end of the test using four evaluation criteria. The results are shown in Table 2.
(Evaluation criteria)
4: Excellent effect 3: Effective 2: Slightly effective 1: No effect

  As is clear from Table 2, the prescription solution containing Pleomele angustifolia (Roxb.) NE Br., Oxalis corymbosa DC., And Sonchus oleraceus L. on the panel exposed to ultraviolet rays prevents the deposition of melanin pigments and makes the color black. Prevention / improvement was observed.

  Below, the Example of the skin external preparation which mix | blended the whitening agent of this invention is given. The whitening agent used was the one prepared above. A compounding quantity represents the mass%. The skin external preparations obtained in Examples 1 to 10 were all effective in the whitening effect test.

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
Pleomele angustifolia (Roxb.) NE Br. Ethanol extract 0.01
Caustic potash 0.2
Sodium bisulfite 0.01
Preservative Appropriate amount Perfume Appropriate amount Ion-exchange water Residue
Propylene glycol, Pleomele angustifolia (Roxb.) NE Br. Ethanol 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
Pleomele angustifolia (Roxb.) NE Br.Hexane 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). Preliminarily emulsify by adding an oil phase to the aqueous phase, uniformly emulsify with a homomixer, and then cool 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
Oxalis corymbosa DC. Acetone 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
Sonchus oleraceus 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
Pleomele angustifolia (Roxb.) NE Br. Water 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 uniformly emulsified 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
Caustic soda 0.15
L-Arginine 0.1
Oxalis corymbosa DC. 50% aqueous 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 Oxalis corymbosa DC. 50% aqueous 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 Cosmetic liquid (prescription)
(Phase A)
Ethyl alcohol (95%) 10.0% by mass
Polyoxyethylene (20 mol) octyldodecanol 1.0
Pantotenyl ethyl ether 0.1
Oxalis corymbosa DC. Ethanol extract 1.5
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
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)
Sonchus oleraceus L. Ethanol 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
Pleomele angustifolia (Roxb.) NE Br. Ethanol extract 1.0
Preservative appropriate amount perfume appropriate amount (production method)
After thoroughly mixing the powder component of talc to black iron oxide with a blender, add the oily component of squalane to isocetyl octoate, Pleomele angustifolia (Roxb.) NE Br. Ethanol extract, preservative, flavor, Fill and mold the container.

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
Sonchus oleraceus L. 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, stirring, and it cools to room temperature.

Claims (3)

  Liliaceae plant Pleomele angustifolia (Roxb.) NE Br., Oxalidaceae plant Oxalis corymbosa DC., Compositae plant Sonchus oleraceus L., one species selected from the group consisting of Or the whitening agent characterized by including the extract of 2 or more types of plants.   A whitening method comprising whitening the skin using the whitening agent according to claim 1. A method for producing a whitening skin external preparation, which comprises adding the whitening agent according to claim 1 to an aqueous phase or an oil phase to produce a whitening skin external preparation.