JPH0812566A - Inhibitor of tyrosinase activity - Google Patents

Abstract

PURPOSE:To obtain the subject inhibitor having inhibiting actions on tyrosinase activities, excellent in lightening of the color, beautifying and whitening of pigmentation, dermal stains, ephelides, chloasmata, etc., after sunburn, excellent in safety and useful as an ointment, a cream, etc., by blending an extract of a specific plant therein. CONSTITUTION:This inhibitor is obtained by blending one or more selected from extracts of plants of Chanca-piedra (botanical name: Phyllanthus niruri L.), Matico (botanical name: Piper elongatum Vahl. & Piper ungustifolium) and Ortiga (botanical name: Urtica urens) therein. The amount of the blended extracts is 0.005-20.0wt.%, preferably 0.01-10.0wt.%. For example, an extract prepared by immersing the whole herb of the plants in an extracting solvent or refluxing the solvent together with the whole herb therein under heating, filtering the resultant extract solution, concentrating the prpared filtrate, etc., is preferably used as the extract.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention contains a tyrosinase activity having an inhibitory effect on tyrosinase activity, which is effective for preventing and improving pigmentation, spots, freckles, chloasma, etc. after sunburn by incorporating an extract of a specific plant. Regarding inhibitors.

[0002]

BACKGROUND OF THE INVENTION Although there are some unclear points about the mechanism of skin spots and the like, in general, melanin pigments are formed due to hormonal abnormalities and irritation of ultraviolet rays from the sun, and this is the skin. It is thought to be abnormally deposited inside. This melanin pigment, which causes skin coloring, is produced in melanin-producing granules (melanosomes) in melanocytes (melanocytes) between the epidermis and dermis,
The generated melanin diffuses into adjacent cells by the osmotic effect. The biochemical reaction in this melanocyte is presumed to be as follows.

That is, the process in which tyrosine, which is an essential amino acid, becomes dopaquinone by the action of the enzyme tyrosinase and is converted to black melanin through the red pigment and the colorless pigment by the enzymatic or non-enzymatic oxidation action is the process of producing melanin pigment. is there. Therefore, suppressing the action of tyrosinase, which is the first step of the reaction, is important for suppressing melanin production.

[0004]

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 higher fatty acid monoesters or alkyl monoethers (JP-A-58-154507), but the esters are decomposed by a hydrolase in the body. Therefore, it is not always safe, and ethers have not been sufficiently satisfactory in terms of safety.

[0005]

As a result of investigating the tyrosinase activity inhibitory effect of various substances as a solution to these problems, the inventors of the present invention have found that a specific plant extract has a tyrosinase activity inhibitory effect. The present invention has been completed and the present invention has been completed. There has been no report on the tyrosinase activity inhibitory action of the extracts of these plants described later, and its application to a whitening agent has never been known. The present inventors have completed the present invention based on the above findings.

[0006] That is, the present invention is a tyrosinase activity inhibitor characterized by containing one or more selected from the following plant extracts.

(1) Chanka-Piedra
piedra, scientific name: Phyllanthus niruri L.) (2) Matico, scientific name: Piper elongatum Va
hl. & Piper ungustifolium) (3) Ortiga (scientific name: Urtica urens)

The structure of the present invention will be described in detail below. The plants used in the present invention are plants that grow in South America, especially dry grasslands such as the Andes, grasses and the like. The extract used in the present invention, such as leaves and stems or fruits of the above-mentioned plants, after soaking or heating under reflux with the whole plant with an extraction solvent,
Obtained by filtration and concentration. The extraction solvent used in the present invention may be any solvent used in ordinary extraction,
In particular, alcohols such as methanol and ethanol, hydroalcohols, organic solvents such as acetone and ethyl acetate can be used alone or in combination.

The blending amount of the plant extract in the present invention is 0.005 to 20.0% by weight, preferably 0.01 to 10.0% by weight, as a dried product, in the total amount of the external preparation. 0.
If it is less than 005% by weight, the effect of the present invention is not sufficiently exhibited, and if it exceeds 20.0% by weight, formulation is difficult, which is not preferable. Further, even if it is blended in an amount of 10.0% by weight or more, the effect is not so much improved.

The tyrosinase activity inhibitor of the present invention contains, in addition to the above-mentioned essential components, components usually used in external preparations for skin such as cosmetics and pharmaceuticals, for example, other whitening agents, moisturizers, antioxidants, and oiliness agents. Ingredients, ultraviolet absorbers, surfactants, thickeners, alcohols, powder components, colorants, aqueous components, water, various skin nutrients and the like can be appropriately blended as necessary.

Other metal sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, gluconic acid, caffeine, tannin, verapamil, tranexamic acid and its derivatives, licorice extraction Substance, glabridin, hot water extract of fruits of fire thorns, various crude drugs, tocopherol acetate,
Drugs such as glycyrrhizic acid and its derivatives or salts thereof, vitamin C, magnesium ascorbate phosphate,
Other whitening agents such as ascorbic acid glucoside, arbutin, kojic acid, glucose, fructose, mannose,
Sugars such as sucrose and trehalose can also be appropriately added.

The tyrosinase activity inhibitor of the present invention may be any ointment, cream, milky lotion, lotion, pack, bath agent or the like, as long as it is used in the conventional external preparation for skin, and its dosage form is not particularly limited.

[0013]

Next, the present invention will be described in more detail by way of examples. The present invention is not limited to this. The blending amount is% by weight. Prior to the examples, the test method and the result of the tyrosinase activity inhibitory effect of the plant extract of the present invention will be described.

Test Method and Results 1. Sample Preparation (1) Chanca-piedr
a) Extract solution 50 g of the stem and branch portion of Chanca-piedra was immersed in ethanol at room temperature for 1 week, and the extract solution was concentrated to obtain 2.7 g of an ethanol extract. This extract was dissolved in DMSO at a concentration of 1%, the solution was diluted to adjust the concentration, and the following experiment was conducted using this.

(2) Matico Extract Liquid Matico stem and branch portions (50 g) were immersed in ethanol at room temperature for one week, and the extract liquid was concentrated to obtain 6.8 g of an ethanol extract. This extract was dissolved in DMSO at a concentration of 1%, the solution was diluted to adjust the concentration, and the following experiment was conducted using this.

(3) Ortiga Extract 50 g of stems and branches of Ortiga
Was immersed in ethanol for 1 week at room temperature, and the extract was concentrated to obtain 3.0 g of an ethanol extract. This extract is D
The solution was dissolved in MSO at 1%, the solution was diluted to adjust the concentration, and the following experiment was carried out using this.

2. Cell Culture Method B16 melanoma cultured cells derived from mouse were used. 1
0% FBS and theophylline (0.09 mg / ml)
The cells were cultured in an Eagle MEM medium containing C. in a CO ₂ incubator (95% air, 5% carbon dioxide) at 37 ° C. After 24 hours of culturing, the sample solution was added so as to have a final concentration (concentration of extracted dry matter) of 10 ^-2 to 10 ^-5 % by weight, culturing was continued for 3 days, and the tyrosinase activity inhibitory effect was measured by the following method. did.

3. Measurement of tyrosinase activity Before the measurement, the medium in the wells is removed, and the wells are washed twice with 100 μl of PBS. 45 μl of 1% Triton-X in each well
(Rohm and Haas product name, surfactant) containing PBS is added. Shake the plate for 1 minute, break the cell membrane well, and use a microplate reader for 475n.
The absorbance at m was measured, and this was taken as the absorbance at 0 minutes. Then, 5 μl of 10 mM L-DOPA solution was quickly added, and the mixture was transferred to an incubator at 37 ° C. and reacted for 60 minutes. The plate was shaken for 1 minute, and the absorbance (475 nm) at 60 minutes was measured. The tyrosinase activity inhibition rate (%) was defined as the decrease in the absorbance difference of the plant extract-added sample with respect to the absorbance difference at 0 minutes and 60 minutes in the case of the sample to which the plant extract was not added (control). Table 1 shows the results. In addition, as a reference example, the same test as described above was performed on an ethanol extract of mussel, which has already been known to have a tyrosinase activity-inhibiting action. The results are also shown in Table 1.
Shown in In the table, "toxic" means that cytotoxicity was observed, and "-" means that no significant difference was observed within a risk rate of 5% as compared with the control.

[0019]

[Table 1] ───────────────────────────── Test tyrosinase activity inhibition rate (%) ────────── ─────────────── Concentration (wt%) 10 ^-5 10 ^-4 10 ^-3 10 ^-2 ────────────────── ─────────── Chanka-Piedra extract 36 22 38 Toxic Machiko extract -17 44 Toxic Ortiga extract --- 16 48 Kaigai extract --- --55 ───────── ────────────────────

Example 1 Cream (Formulation) Stearic acid 5.0% by weight Stearyl alcohol 4.0 Isopropyl myristate 18.0 Glycerin monostearate 3.0 Propylene glycol 10.0 Chunker-Piedra methanol extract 0.01 Caustic potash 0.2 Sodium bisulfite 0.01 Preservative proper amount Perfume proper amount Ion-exchanged water Residue (production method) Dissolve propylene glycol, Chanca-Piedra methanol extract and caustic potash in ion-exchanged water and heat to maintain at 70 ° C ( Water phase). The other ingredients are mixed, heated and melted and maintained at 70 ° 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 the reaction. Then, it is uniformly emulsified with a homomixer and cooled to 30 ° C. with thorough stirring.

Example 2 Cream (Formulation) Stearic acid 2.0% by weight 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 2.0 Propylene glycol 5.0 Chunker-Piedra ethanol extract 0.05 Sodium hydrogen sulfite 0.03 Ethylparaben 0.3 Perfume suitable amount Ion-exchanged water Residual (production method) Propylene in ion-exchanged water Add glycol,
Heat to maintain 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase to carry out preliminary emulsification, and the mixture is uniformly emulsified with a homomixer and then cooled to 30 ° C. with thorough stirring.

Example 3 Cream (Formulation) Solid paraffin 5.0% by weight Beeswax 10.0 Vaseline 15.0 Liquid paraffin 41.0 Glycerin monostearate 2.0 Polyoxyethylene (20 mol) sorbitan monolaurate 2 .0 soap powder 0.1 borax 0.2 Chanka-Piedraacetone extract 0.05 Chanka-Piedra ethanol extract 0.05 Sodium bisulfite 0.03 Ethylparaben 0.3 Perfume proper amount Ion-exchanged water Residue (production method) Ion Soap powder and borax are added to exchanged water, and the mixture is heated and melted and kept at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is stirred into the water phase and gradually added to carry out the reaction. After the reaction is completed, the mixture is uniformly emulsified with a homomixer, and after emulsification, the mixture is cooled to 30 ° C. with thorough stirring.

Example 4 Emulsion (formulation) Stearic acid 2.5 wt% 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 (trade name: Carbopol 941, BFGoodrich Chemical company) Chanka-Piedra acetic acid ethyl ester extract 0.01 sodium bisulfite 0.01 ethylparaben 0.3 perfume proper amount ion Exchanged water Residue (production method) A carboxyvinyl polymer is dissolved in a small amount of ion exchanged water (phase A). Polyethylene glycol 1500 and triethanolamine were added to the remaining ion-exchanged water, and the mixture was heated and dissolved and maintained at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase for preliminary emulsification, the phase A is added and the mixture is homogenized with a homomixer, and after emulsification, the mixture is cooled to 30 ° C. while being well stirred.

Example 5 Emulsion (Formulation) Microcrystalline wax 1.0% by weight Beeswax 2.0 Lanolin 20.0 Liquid paraffin 10.0 Squalane 5.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 moles) ) Sorbitan monooleate 1.0 Propylene glycol 7.0 Chanka-Piedraacetone extract 10.0 Sodium bisulfite 0.01 Ethylparaben 0.3 Perfume proper amount Ion-exchanged water Residue (production method) Propylene glycol is added to ion-exchanged water In addition,
Heat to maintain 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 to this and the mixture is uniformly emulsified with a homomixer. After emulsification, cool to 30 ° C while stirring well.

Example 6 Jelly (formulation) 95% ethyl alcohol 10.0 wt% dipropylene glycol 15.0 polyoxyethylene (50 mol) oleyl alcohol ether 2.0 carboxyvinyl polymer 1.0 (trade name: Carbopol 940, BFGoodrich Chemical company) Caustic soda 0.15 L-Arginine 0.1 Chanka-Piedra 50% ethanol aqueous solution extract 7.0 2-Hydroxy-4-methoxybenzophenone sodium sulfonate 0.05 Ethylenediaminetetraacetate-3 sodium-2 Water 0.05 Methylparaben 0.2 Perfume Suitable amount Ion-exchanged water Residue (production method) Carbopol 940 is uniformly dissolved in ion-exchanged water, while Chanka-Piedra 5 is added to 95% ethanol.
0% aqueous ethanol extract, polyoxyethylene (5
0 mol) oleyl alcohol ether is dissolved 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.

Example 7 Beauty Serum (Formulation) (Phase A) Ethyl Alcohol (95%) 10.0% by Weight Polyoxyethylene (20 mol) Octyldodecanol 1.0 Pantotenyl Ethyl Ether 0.1 Chanka-Piedra Methanol 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 (trade name: Carbo Pole 940, BFGoodrich Chemical company) Purified water Residue (production method) Phases A and C are uniformly dissolved, and A is added to phase C
Add phase and solubilize. Next, phase B is added and then filling is performed.

Example 8 Pack (Formulation) (Phase A) 5.0% by weight dipropylene glycol Polyoxyethylene (60 mol) hydrogenated castor oil 5.0 (Phase B) Chanka-Piedra methanol extract 0.01 Olive oil 5 0.0 Tocopherol acetate 0.2 Ethylparaben 0.2 Perfume 0.2 (Phase C) Sodium hydrogen sulfite 0.03 Polyvinyl alcohol 13.0 (Saponification degree 90, degree of polymerization 2,000) Ethanol 7.0 Purified water Residue (Manufacturing method) Phase A, phase B, and phase C are uniformly dissolved,
Phase B is added to the phase to solubilize it. Next, this is added to phase C and then filled.

Example 9 Solid Foundation (Formulation) Talc 43.1% by weight Kaolin 15.0 Sericite 10.0 Zinc white 7.0 Titanium dioxide 3.8 Yellow iron oxide 2.9 Black iron oxide 0.2 Squalane 8 0.0 Isostearic acid 4.0 POE sorbitan monooleate 3.0 Isocetyl octoate 2.0 Chunker-Piedra ethanol extract 1.0 Preservative proper amount Fragrance appropriate amount (manufacturing method) A powdery component of talc to black iron oxide is sufficient with a blender. After mixing, an oily component of squalane to isocetyl octoate, a Chanka-Piedra ethanol extract, an antiseptic and a fragrance are added and kneaded well, then filled into a container and molded.

Example 10 Emulsion type foundation (cream type) (Formulation) (Powder part) Titanium dioxide 10.3 wt% 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 (Aqueous phase) Purified water 50.0 1,3-Butylene glycol 4.5 Chunker -Piedra ethanol extract 1.5 sorbitan sesquioleate 3.0 preservative proper amount perfume proper amount (manufacturing method) After heating and stirring the aqueous phase, a powder portion thoroughly mixed and pulverized is added and treated with a homomixer. Further, the heated and mixed oil phase is added and subjected to a homomixer treatment, and then a fragrance is added with stirring and cooled to room temperature.

Example 11 Cream (Formulation) Stearic acid 5.0% by weight Stearyl alcohol 4.0 Isopropyl myristate 18.0 Glycerin monostearate 3.0 Propylene glycol 10.0 Machicomethanol extract 0.01 Caustic potash 0 .2 Sodium bisulfite 0.01 Preservative Suitable amount Perfume Suitable amount Ion-exchanged water Residual (production method) Dissolve propylene glycol, Machiko methanol extract and caustic potash in ion-exchanged water and heat to 7
Keep at 0 ° C (aqueous phase). Mix other ingredients and heat to 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 the reaction. Then, it is uniformly emulsified with a homomixer and cooled to 30 ° C. with thorough stirring.

Example 12 Cream (formulation) Stearic acid 2.0% by weight 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 2.0 Propylene glycol 5.0 Macycoethanol extract 0.05 Sodium bisulfite 0.03 Ethylparaben 0.3 Perfume Suitable amount Ion-exchanged water Residual (production method) Propylene glycol is added to ion-exchanged water In addition,
Heat to maintain 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase to carry out preliminary emulsification, and the mixture is uniformly emulsified with a homomixer and then cooled to 30 ° C. with thorough stirring.

Example 13 Cream (Formulation) Solid paraffin 5.0% by weight Beeswax 10.0 Vaseline 15.0 Liquid paraffin 41.0 Glycerin monostearate 2.0 Polyoxyethylene (20 mol) sorbitan monolaurate 2 0.0 Soap powder 0.1 Borax 0.2 Machicoacetone extract 0.05 Machicoethanol extract 0.05 Sodium bisulfite 0.03 Ethylparaben 0.3 Perfume suitable amount Ion-exchanged water Residual (production method) Soap to ion-exchanged water The powder and borax are added, melted by heating and kept at 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is stirred into the water phase and gradually added to carry out the reaction. After the reaction is completed, the mixture is uniformly emulsified with a homomixer, and after emulsification, the mixture is cooled to 30 ° C. with thorough stirring.

Example 14 Emulsion (formulation) Stearic acid 2.5% by weight 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 (Brand name: Carbopol 941, BFGoodrich Chemical company) Machico acetic acid ethyl ester extract 0.01 Sodium bisulfite 0.01 Ethylparaben 0.3 Perfume proper amount Ion-exchanged water Residual (manufacturing method) The carboxyvinyl polymer is dissolved in a small amount of ion-exchanged water (phase A). Polyethylene glycol 1500 and triethanolamine were added to the remaining ion-exchanged water, and the mixture was heated and dissolved and maintained at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase for preliminary emulsification, the phase A is added and the mixture is homogenized with a homomixer, and after emulsification, the mixture is cooled to 30 ° C. while being well stirred.

Example 15 Emulsion (Formulation) Microcrystalline wax 1.0% by weight Beeswax 2.0 Lanolin 20.0 Liquid paraffin 10.0 Squalane 5.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 moles) ) Sorbitan monooleate 1.0 Propylene glycol 7.0 Macicoacetone extract 10.0 Sodium hydrogen sulfite 0.01 Ethylparaben 0.3 Perfume suitable amount Ion-exchanged water Residue (production method) Propylene glycol is added to ion-exchanged water,
Heat to maintain 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 to this and the mixture is uniformly emulsified with a homomixer. After emulsification, cool to 30 ° C while stirring well.

Example 16 Jelly (formulation) 95% ethyl alcohol 10.0 wt% dipropylene glycol 15.0 polyoxyethylene (50 mol) oleyl alcohol ether 2.0 carboxyvinyl polymer 1.0 (trade name: Carbopol 940, BFGoodrich Chemical company) Caustic soda 0.15 L-Arginine 0.1 Machico 50% ethanol aqueous solution extract 7.0 2-Hydroxy-4-methoxybenzophenone sodium sulfonate 0.05 Ethylenediaminetetraacetate ・ 3 sodium ・ 2 water 0 .05 Methylparaben 0.2 Fragrance Appropriate amount Ion-exchanged water Residual (production method) Carbopol 940 was uniformly dissolved in ion-exchanged water, while 95% ethanol was mixed with 50% aqueous solution of Machiko and polyoxyethylene (50 mol) oleyl. alcohol Was dissolved ether, is added to the aqueous phase. Next, after adding other components, the mixture is neutralized with caustic soda and L-arginine to increase the viscosity.

Example 17 Beauty Serum (Formulation) (Phase A) Ethyl Alcohol (95%) 10.0% by Weight Polyoxyethylene (20 mol) Octyldodecanol 1.0 Pantotenyl Ethyl Ether 0.1 Macychomethanol 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 (trade name: Carbopol 940 , BFGoodrich Chemical company) Purified water Residual (manufacturing method) A phase and C phase are uniformly dissolved, and A is added to C phase.
Add phase and solubilize. Next, phase B is added and then filling is performed.

Example 18 Pack (Formulation) (Phase A) Dipropylene glycol 5.0 wt% Polyoxyethylene (60 mol) hydrogenated castor oil 5.0 (Phase B) Machikomethanol extract 0.01 Olive oil 5.0 Tocopherol acetate 0.2 Ethylparaben 0.2 Perfume 0.2 (Phase C) Sodium hydrogen sulfite 0.03 Polyvinyl alcohol 13.0 (Saponification degree 90, degree of polymerization 2,000) Ethanol 7.0 Purified water Residual (manufacturing method ) A phase, B phase, and C phase are uniformly dissolved,
Phase B is added to the phase to solubilize it. Next, this is added to phase C and then filled.

Example 19 Solid Foundation (Formulation) Talc 43.1% by weight Kaolin 15.0 Sericite 10.0 Zinc white 7.0 Titanium dioxide 3.8 Yellow iron oxide 2.9 Black iron oxide 0.2 Squalane 8 0.0 isostearic acid 4.0 POE sorbitan monooleate 3.0 isocetyl octoate 2.0 Macicoethanol extract 1.0 preservative appropriate amount perfume appropriate amount (manufacturing process) Talc-black iron oxide powder components are thoroughly mixed with a blender. Then, an oily component of squalane to isocetyl octoate, a macycoethanol extract, an antiseptic and a fragrance are added and kneaded well, then filled into a container and molded.

Example 20 Emulsion type foundation (cream type) (Prescription) (Powder part) Titanium dioxide 10.3 wt% 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 (Aqueous phase) Purified water 50.0 1,3-Butylene glycol 4.5 Machico Ethanol extract 1.5 Sorbitan sesquioleate ester 3.0 Preservative proper amount Perfume proper amount (Production method) After heating and stirring the aqueous phase, the powder portion thoroughly mixed and pulverized is added and subjected to a homomixer treatment. Further, the heated and mixed oil phase is added and subjected to a homomixer treatment, and then a fragrance is added with stirring and cooled to room temperature.

Example 21 Cream (Formulation) Stearic acid 5.0% by weight Stearyl alcohol 4.0 Isopropyl myristate 18.0 Glycerin monostearate 3.0 Propylene glycol 10.0 Ortigamethanol extract 0.01 Caustic potash 0 .2 Sodium bisulfite 0.01 Preservative proper amount Fragrance proper amount Ion-exchanged water Residual (production method) Dissolve propylene glycol, ortigamethanol extract and caustic potash in ion-exchanged water, dissolve and heat to maintain at 70 ° C (water phase). The other ingredients are mixed, heated and melted and maintained at 70 ° 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 the reaction. Then, it is uniformly emulsified with a homomixer and cooled to 30 ° C. with thorough stirring.

Example 22 Cream (formulation) Stearic acid 2.0% by weight 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 2.0 Propylene glycol 5.0 Ortiga ethanol extract 0.05 Sodium hydrogen sulfite 0.03 Ethylparaben 0.3 Perfume proper amount Ion-exchanged water Residue (production method) Propylene glycol is added to ion-exchanged water In addition,
Heat to maintain 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase to carry out preliminary emulsification, and the mixture is uniformly emulsified with a homomixer and then cooled to 30 ° C. with thorough stirring.

Example 23 Cream (Formulation) Solid paraffin 5.0% by weight Beeswax 10.0 Vaseline 15.0 Liquid paraffin 41.0 Glycerin monostearate 2.0 Polyoxyethylene (20 mol) sorbitan monolaurate 2 0.0 Soap powder 0.1 Borax 0.2 Ortiga acetone extract 0.05 Ortiga ethanol extract 0.05 Sodium hydrogen sulfite 0.03 Ethylparaben 0.3 Perfume suitable amount Ion-exchanged water Residual (production method) Soap to ion-exchanged water The powder and borax are added, melted by heating and kept at 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is stirred into the water phase and gradually added to carry out the reaction. After the reaction is completed, the mixture is uniformly emulsified with a homomixer, and after emulsification, the mixture is cooled to 30 ° C. with thorough stirring.

Example 24 Emulsion (formulation) Stearic acid 2.5% by weight 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 (Brand name: Carbopol 941, BFGoodrich Chemical company) Ortiga acetic acid ethyl ester extract 0.01 Sodium hydrogen sulfite 0.01 Ethylparaben 0.3 Perfume proper amount Ion-exchanged water Residual (manufacturing method) The carboxyvinyl polymer is dissolved in a small amount of ion-exchanged water (phase A). Polyethylene glycol 1500 and triethanolamine were added to the remaining ion-exchanged water, and the mixture was heated and dissolved and maintained at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase for preliminary emulsification, the phase A is added and the mixture is homogenized with a homomixer, and after emulsification, the mixture is cooled to 30 ° C. while being well stirred.

Example 25 Emulsion (Formulation) Microcrystalline wax 1.0% by weight Beeswax 2.0 Lanolin 20.0 Liquid paraffin 10.0 Squalane 5.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 moles) ) Sorbitan monooleate 1.0 Propylene glycol 7.0 Ortigaacetone extract 10.0 Sodium hydrogen sulfite 0.01 Ethylparaben 0.3 Perfume suitable amount Ion-exchanged water Residue (production method) Propylene glycol is added to ion-exchanged water,
Heat to maintain 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 to this and the mixture is uniformly emulsified with a homomixer. After emulsification, cool to 30 ° C while stirring well.

Example 26 Jelly (formulation) 95% ethyl alcohol 10.0 wt% dipropylene glycol 15.0 polyoxyethylene (50 mol) oleyl alcohol ether 2.0 carboxyvinyl polymer 1.0 (trade name: Carbopol 940, BFGoodrich Chemical company) Caustic soda 0.15 L-Arginine 0.1 Ortiga 50% ethanol aqueous solution extract 7.0 2-Hydroxy-4-methoxybenzophenone sulfonic acid sodium salt 0.05 Ethylenediaminetetraacetate.3 sodium.2 water 0 .05 Methylparaben 0.2 Fragrance Suitable amount Ion-exchanged water Residual (manufacturing method) Carbopol 940 is uniformly dissolved in ion-exchanged water, while 95% ethanol is Ortiga 50% ethanol aqueous solution extract, polyoxyethylene (50 mol)
Dissolve the oleyl alcohol ether and add to the aqueous phase. Next, after adding other ingredients, caustic soda, L
-Neutralize with arginine to thicken.

Example 27 Beauty Serum (Formulation) (Phase A) Ethyl Alcohol (95%) 10.0% by Weight Polyoxyethylene (20 mol) Octyldodecanol 1.0 Pantotenyl Ethyl Ether 0.1 Ortigamethanol 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 (trade name: Carbopol 940 , BFGoodrich Chemical company) Purified water Residual (manufacturing method) A phase and C phase are uniformly dissolved, and A is added to C phase.
Add phase and solubilize. Next, phase B is added and then filling is performed.

Example 28 Pack (formulation) (Phase A) Dipropylene glycol 5.0% by weight Polyoxyethylene (60 mol) hydrogenated castor oil 5.0 (Phase B) Ortigamethanol extract 0.01 Olive oil 5.0 Tocopherol acetate 0.2 Ethylparaben 0.2 Perfume 0.2 (Phase C) Sodium hydrogen sulfite 0.03 Polyvinyl alcohol 13.0 (Saponification degree 90, degree of polymerization 2,000) Ethanol 7.0 Purified water Residual (manufacturing method ) A phase, B phase, and C phase are uniformly dissolved,
Phase B is added to the phase to solubilize it. Next, this is added to phase C and then filled.

Example 29 Solid Foundation (Formulation) Talc 43.1% by weight Kaolin 15.0 Sericite 10.0 Zinc white 7.0 Titanium dioxide 3.8 Yellow iron oxide 2.9 Black iron oxide 0.2 Squalane 8 0.0 isostearic acid 4.0 POE sorbitan monooleate 3.0 isocetyl octanoate 2.0 ortiga ethanol extract 1.0 preservative appropriate amount perfume appropriate amount (production method) Talc-black iron oxide powder components are thoroughly mixed with a blender. Then, an oily component of squalane to isocetyl octoate, an ortiga ethanol extract, a preservative and a fragrance are added, and the mixture is well kneaded and then filled into a container and molded.

Example 30 Emulsion type foundation (cream type) (Prescription) (Powder part) Titanium dioxide 10.3% by weight 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 (Aqueous phase) Purified water 50.0 1,3-Butylene glycol 4.5 Ortiga Ethanol extract 1.5 Sorbitan sesquioleate ester 3.0 Preservative proper amount Perfume proper amount (Production method) After heating and stirring the aqueous phase, the powder portion thoroughly mixed and pulverized is added and subjected to a homomixer treatment. Further, the heated and mixed oil phase is added and subjected to a homomixer treatment, and then a fragrance is added with stirring and cooled to room temperature.

[0050]

Industrial Applicability As described above, the tyrosinase activity inhibitor of the present invention has an excellent tyrosinase activity inhibitory effect, and is effective for reducing pigmentation, stains, freckles, melasma, and whitening after sunburn. In addition to having an excellent effect, it is also excellent in safety.

Front page continuation (72) Masako Naganuma, Masako Naganuma, 1050 Shinba-cho, Kohoku-ku, Yokohama, Kanagawa, Shiseido Daiichi Research Center, Inc. Shiseido Daiichi Research Center

Claims (2)

[Claims] 1. A tyrosinase activity inhibitor comprising one or more selected from the following plant extracts. (1) Chanca-piedra
a, Scientific name: Phyllanthus niruri L.) (2) Matico, Scientific name: Piper elongatum Va
hl. & Piper ungustifolium) (3) Ortiga (scientific name: Urtica urens) 2. The blending amount of the plant extract is 0.005 to 2
The tyrosinase activity inhibitor according to claim 1, which is 0.0% by weight.