JP3270219B2 - External preparation for skin - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION The present invention relates to an antithylli
s) It relates to an external preparation for skin which has an excellent effect on pigmentation, spots, freckles, liver spots, etc. after sunburn by incorporating an extract of a genus plant.

[0002]

2. Description of the Related Art Although there are some unclear points about the mechanism of the occurrence of skin spots and the like, melanin pigments are generally formed due to hormonal abnormalities and stimulation of ultraviolet rays from sunlight. It is believed to be abnormally deposited within. Treatment of such spots and bruises includes substances that suppress the production of melanin, such as a method of administering a large amount of vitamin C, a method of injecting glutathione, etc., or kojic acid,
A method of applying L-ascorbic acid, cysteine, or the like in the form of an ointment, a cream, a lotion, or the like, and topically applying the composition is employed. Generally, hydroquinone preparations are used as pharmaceuticals in Europe and the United States.

[0003]

However, these compounds, except for hydroquinone, exhibit very slow effects, and do not have a sufficient whitening effect. On the other hand, although hydroquinone has been recognized as having an effect, its use is generally restricted due to its sensitizing properties. Attempts have been made to improve the safety of monoesters and alkyl monoethers of higher fatty acids, but esters are not always safe because they are degraded by hydrolyzing enzymes in the body. No such products have been obtained that are sufficiently satisfactory in terms of safety.

[0004]

As a solution to these problems, the present inventors have investigated the whitening effect of a wide variety of substances. If the extract of a plant belonging to the genus Antithyllis (Anthyllis), which has been used for pickling tinctures or powders for astringent, hemostatic, laxative, coughing, swollen, detoxifying, etc., is added to cosmetics, the pigment after sunburn The present inventors have found that the present invention has an excellent effect on lightening and whitening of deposits, spots, freckles, liver spots and the like, and has completed the present invention. That is, the present invention relates to an external preparation for skin, characterized by containing an extract of a plant belonging to the genus Antilis of the genus Legumes as an active ingredient.

[0005]

DETAILED DESCRIPTION OF THE STRUCTURE The structure of the present invention is described in detail below. The antilith used in the present invention is a bean family Antilith that grows on dry grasslands and pastures in Europe and the like.
It is a plant of the genus (Anthyllis). The extract used in the present invention is obtained by immersing or heating and refluxing the above-mentioned leaves and stems or whole Antilis with an extraction solvent, followed by filtration and concentration. The extraction solvent used in the present invention may be any solvent that is usually used for extraction, and in particular, alcohols such as methanol and ethanol, and organic solvents such as acetone can be used alone or in combination.

The amount of the antilith extract in the present invention is 0.005 to 20% by weight as a dry matter in the total amount of the cosmetic,
Preferably it is 0.01 to 10% by weight. If the amount is less than 0.005% by weight, the effect of the present invention is not sufficiently exhibited, and if it exceeds 20% by weight, the preparation is difficult, which is not preferable. Also, 10
Even if it is blended in an amount of not less than% by weight, the effect is not so greatly improved.

[0007] In addition to the above-mentioned essential components, the external preparation for skin of the present invention may contain various components generally used in cosmetics, pharmaceuticals and the like, ie, aqueous components and powder components, if necessary, as long as the effects of the present invention are not impaired. , An oil, a surfactant, a humectant, a thickener, a preservative, an antioxidant, a fragrance, a coloring agent, a drug, and the like. Further, the dosage form of the external preparation for skin of the present invention is arbitrary, for example, a solubilizing system such as a lotion, an emulsion, an emulsifying system such as a cream or a foundation, a dispersion,
Various dosage forms such as a two-layer lotion can be used.

[0008]

Next, the present invention will be described in more detail by way of examples. Note that the present invention is not limited by this. The compounding amount is% by weight. Prior to the examples, the effect test method and the evaluation method of the present invention will be described.

Test Example 1 (Whitening Effect) [Test Method] Forty subjects exposed to sunlight in the summer for 4 hours (2 hours a day for 2 days) were exposed to the sunlight on the inner skin of the upper arm. Five days after the day, each sample was applied once in the morning and evening for four weeks. The panel was divided into 10 groups and divided into 4 groups, and the test was performed according to the following formulation. (Alcohol phase) 95% Ethyl alcohol 55.0 Polyoxyethylene (25 mol) Hardened castor oil ether 2.0 Antioxidant / preservatives Appropriate amount Fragrance Appropriate amount Chemical (Table 1) 0.1 to 10.0 (Aqueous phase) Glycerin 5.0 Sodium hexametaphosphate Appropriate amount Ion Exchange water residue <Production method> Adjust the aqueous phase and the alcohol phase, and then mix and solubilize both.

[Evaluation method] The lightening effect after use was determined based on the following criteria. <Judgment criteria > ：: When the proportion of the subjects showing the significant and effective is 80% or more ○: The proportion of the subjects showing the great and effective is 50 to 8
0%: △: The proportion of the test subjects showing excellent and effective was 50 to 3
0%: ×: The proportion of subjects who show excellent and effective is 30% or less

Examples 1-2 and Comparative Examples 1-2 Samples having the composition described in the above test method were prepared.
The whitening effects were compared using the indicated agents. The results are shown in Table 1.

[0012]

[Table 1] 量 Formulation amount (% by weight) Effect ─ ────────────────────────────────── Comparative Example 1 No additive-× Comparative Example 2 Hydroquinone 1.0 △ Example 1 Antilith 0.1 ○ Example 2 Antilith 1.0 ○ Example 3 Antilith 10.0 ◎ ──────────────────────────────── ───

The antiliths in Table 1 were obtained by heating and refluxing whole plants of Antithyllis Sericea in ethanol, followed by filtration, concentration and drying.

As is clear from Table 1, the effect of the embodiment after exposure to sunlight can be prevented from being excessively melanin pigment deposition and preventing blackening, as compared with the comparative example. Admitted.

Example 4 Cream (Formulation) Stearic acid 5.0 Stearyl alcohol 4.0 Isopropyl myristate 18.0 Glycerin monostearate ester 3.0 Propylene glycol 10.0 Antilith methanol extract 0.01 Caustic potash 0.2 Sodium bisulfite 0.01 Preservatives Appropriate perfume Appropriate amount Ion-exchanged water residue (Production method) Propylene glycol, antilith extract and caustic potash are added to ion-exchanged water, dissolved and heated to 70 ° C. (aqueous phase). Mix with other ingredients, heat and maintain at 70 ° C
(Oil phase). The oil phase is gradually added to the aqueous phase, and after the addition is completed, the temperature is maintained for a while to cause a reaction. After that, emulsify uniformly with a homomixer and stir well at 30 ° C.
Cool down to

Example 5 Cream (Formulation) Stearyl alcohol 7.0 Stearic acid 2.0 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 Antilith Ethanol extract 0.05 Perfume Appropriate amount Sodium bisulfite 0.03 Ethyl paraben 0.3 Ion-exchanged water Residue (Preparation method) Add propylene glycol to ion-exchanged water and heat to 70 ° C (aqueous phase). Mix the other ingredients, heat and melt, and keep at 70 ° C (oil phase). Add the oil phase to the water phase, pre-emulsify, homogenize with a homomixer, and cool to 30 ° C with good stirring.

Example 6 Cream (Formulation) Solid Paraffin 5.0 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 Antilith Acetone Extract 0.05 Anne Tiris Ethanol extract 0.05 Ion-exchanged water Residual fragrance Appropriate amount Sodium bisulfite 0.03 Ethylparaben 0.3 (Preparation method) Add soap powder and borax to ion-exchanged water, heat and maintain at 70 ° C (aqueous phase). Mix and melt other ingredients
Keep at 70 ° C (oil phase). The oil phase is gradually added to the aqueous phase while stirring to carry out the reaction. After the completion of the reaction, the mixture is uniformly emulsified with a homomixer, and cooled to 30 ° C. while stirring well after emulsification.

Example 7 Emulsion (Prescription) 2.5 Cetyl alcohol stearic acid 1.5 Vaseline 5.0 Liquid paraffin 10.0 Polyoxyethylene (10 mol) monooleate 2.0 Polyethylene glycol 1500 3.0 Triethanolamine 1.0 Antilith Methanol extract 0.01 Sodium bisulfite 0.01 Ethylparaben 0.3 Carboxyvinyl polymer (trade name: Carbopol 941) 0.05 BF Goodrich Chemical company Perfume Appropriate amount Ion-exchange water Residue (Preparation method) Dissolve the carboxyvinyl polymer in a small amount of ion-exchange water (A phase). Polyethylene glycol 1500 and triethanolamine are added to the remaining ion-exchanged water, dissolved by heating, and kept at 70 ° C. (aqueous phase). Mix the other ingredients, heat and melt to keep at 70 ° C (oil phase). The oil phase is added to the water phase, preliminarily emulsified, the phase A is added, homogenized with a homomixer, and after emulsification, cooled to 30 ° C with good stirring.

Example 8 Emulsion (Formulation) Microcrystalline wax 1.0 Beeswax 2.0 Lanolin 20.0 Liquid paraffin 10.0 Squalane 5.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 mol) Sorbitan monooleate 1.0 Propylene glycol 7.0 Antilith Acetone extraction Product 10.0 Ethylparaben 0.3 Sodium bisulfite 0.01 Perfume Appropriate amount Ion-exchange water residue (Production method) Add propylene glycol to ion-exchange water,
Heat and maintain at 70 ° C. (aqueous phase). The other components are mixed, dissolved by heating and kept at 70 ° C. (oil phase). While stirring the oil phase, the aqueous phase is gradually added thereto, and the mixture is uniformly emulsified with a homomixer. After emulsification, cool to 30 ° C while stirring well.

Example 9 Jelly (formulation) 95% ethyl alcohol 10.0 dipropylene glycol 15.0 polyoxyethylene (50 mol) oleyl alcohol ether 2.0 carboxyvinyl polymer (trade name: Carbopol 940) 1.0 BF Goodrich Chemical company Caustic soda 0.15 L- Arginine 0.1 Antilis Ethanol extract 7.0 2-Hydroxy-4-methoxybenzophenophenone Sodium sulfonate 0.05 Methyl paraben 0.2 Ethylenediaminetetraacetate 3 Sodium 2 Water 0.05 Perfume Appropriate amount Ion exchange water Residue (Production method) Carbopol 940 in ion exchange water While the Antilith acetone extract, polyoxyethylene (50 mol) oleyl alcohol ether is dissolved in 95% ethanol and added to the aqueous phase. Then, after adding other components, the mixture is neutralized with caustic soda and L-arginine to increase the viscosity.

Example 10 Essence (Formulation) (A phase) Ethanol (95%) 10.0 Polyoxyethylene (20) Octyldodecanol 1.0 Methyl paraben 0.15 Pantothenyl ethyl ether 0.1 Antilith Methanol extract 1.5 (B phase) Hydroxidation Potassium 0.1 (Phase C) Glycerin 5.0 Dipropylene glycol 10.0 Sodium bisulfite 0.03 Carboxyvinyl polymer 0.2 (trade name: Carbopol 940) BF Goodrich Chemical company Purified water Residue (Production method) Dissolve the phases A and C uniformly, A for C phase
Add phases and solubilize. Then, after adding the phase B, filling is performed.

Example 11 Pack (Formulation) (Phase A) Dipropylene glycol 5.0 Polyoxyethylene (60 mol) Hardened castor oil 5.0 (Phase B) Antilith methanol extract 0.01 Olive oil 5.0 Tocopherol acetate 0.2 Ethyl paraben 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 (Preparation method) A phase, B phase, and C phase are uniformly dissolved, and B phase is added to A phase. Solubilize. Then, after adding this to the phase C, filling is performed.

Example 12 Solid Foundation (Formulation) Talc 43.1 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 POE Sorbitan Monooleate 3.0 Isocetyl Octanoate 2.0 Antilith Ethanol Extract 1.0 Preservatives Appropriate amount Fragrance Appropriate amount (Preparation method) Thoroughly mix the powder component of talc to black iron oxide with a blender, and add the oil component of squalane to isocetyl octanoate, Antilith ethanol extract, preservative,
After adding fragrance and kneading well, the mixture is filled into a container and molded.

Example 13 Emulsion type foundation (cream type) (Formulation) (Powder part) Titanium dioxide 10.3 Sericite 5.4 Kaolin 3.0 Yellow iron oxide 0.8 Bengala 0.3 Black iron oxide 0.2 (Oil phase) Decamethylcyclopentasiloxane 11.5 Flow Paraffin 4.5 Polyoxyethylene-modified dimethylpolysiloxane 4.0 (aqueous phase) Purified water 50.0 1,3-butylene glycol 4.5 Antilith ethanol extract 1.5 Sorbitan sesquioleate 3.0 Preservatives Appropriate amount (perfume) Appropriate amount (production method) Heat the aqueous phase After the stirring, a powder portion sufficiently mixed and pulverized is added and subjected to a homomixer treatment. Further, the oil phase mixed by heating is added, and the mixture is treated with a homomixer. Then, a fragrance is added with stirring, and the mixture is cooled to room temperature.

[0025]

The external preparation for skin of the present invention is an external preparation for skin which has excellent effects on lightening of pigmentation, spots, freckles, liver spots and the like after sunburn, whitening, and excellent safety. .

──────────────────────────────────────────────────の Continued on the front page (72) Inventor Yoshihiro Yokokawa 1050 Nippa-cho, Kohoku-ku, Yokohama, Kanagawa Prefecture Inside Shiseido Daiichi Research Center (72) Inventor Rumiko Kaku 1050 Nippacho, Kohoku-ku, Yokohama, Kanagawa (56) Reference European Patent Application Publication 461085 (EP, A1) (58) Fields investigated (Int. Cl. ⁷ , DB name) A61K ^7/ 00-7/50 CA ( STN)

Claims (1)

(57) [Claims] Have a [claim 1] of legume Anne Tirith a plant belonging to the genus extract
An external preparation for skin whitening characterized by containing as an active ingredient .