JP4950390B2 - Topical skin preparation - Google Patents

Description

【００２７】
【効果】
パラオ共和国のウルクタープル島のミルキーウェイにある白色の海泥、或いは白色の海泥の溶媒抽出物は抗チロシナーゼや肌荒れ防止効果がありこれらを配合した皮膚外用剤は美白、肌荒れ防止、クスミの予防等の有効性があり安全性も非常に高い。[0001]
[Industrial application fields]
The present invention relates to a skin external preparation that is extremely effective for whitening the skin, smoothes the skin, and has high safety.
[0002]
[Prior art]
Skin is the only organ that touches the outside world in various human organs. For this reason, it is directly affected by the outside world. The cause is affected by light, temperature, moisture, foreign matter, etc., but scratches and some inflammations will be resolved over time, but the effect will not be resolved or accumulated. There are also things to go. For example, there are inflammation, darkening of the skin, wrinkles, etc. due to sunburn. Among them, skin darkening, blotches and freckles are those in which the balance between production and excretion of melanin is lost and melanin is excessively accumulated in epidermal cells. These causes also have a genetic component, but are promoted by ultraviolet light, that is, sunlight. In order to suppress this action, various whitening agents are already known. For example, ascorbic acid or its derivatives, placenta extract, hydroquinone, or hydroquinone derivatives (arbutin), kojic acid, cysteine, colloidal sulfur, various plant extracts, etc. are known, and whitening cosmetics containing these are known. Proposed. Further, coral powder has been shown to be applied to cosmetics by Patent Registration No. 2890027 and Japanese Patent Application Laid-Open No. 2000-355515, but it is used for applications such as moisturizing action or anti-inflammatory action, suppression of skin roughness. It has been.
[0003]
[Problems to be solved by the invention]
However, the whitening agent that is not always satisfactory because the stability in the preparation is insufficient, there are problems in terms of skin safety such as allergies and skin irritation, and the effect is insufficient. There is a need for more effective whitening agents. In addition, ingredients that have effects other than whitening are expected, and the ingredients of cosmetics that have a strong whitening effect on the skin and have other effective effects on the skin are also considered to be safe and stable. It was.
[0004]
[Means for Solving the Problems]
As a result of intensive studies, the present inventors have found that white sea mud in a certain region of the Republic of Palau is the most suitable for the purpose of the present invention. More specifically, it was found that the white sea mud of Milky Way on Urkutapur Island in the Republic of Palau is effective for skin whitening, sunburned skin, and rough skin. This white sea mud seems to have been deposited by fossilization of dredging etc., but similar white mud and coral powder in other areas have little effect, only white sea mud in this area Very effective. Although various chemical analyzes were conducted, no effective substance could be identified, but it was found that a tyrosinase activity inhibitory component was present in the portion extracted with hot water. That is, in the present invention, “white sea mud” refers to white sea mud on Milky Way on Urkutapur Island in the Republic of Palau.
[0005]
One method is to collect this white sea mud, wash it with water if necessary, remove unnecessary materials, perform heat sterilization, etc. if necessary, or add a step of further finer particles depending on the application. It is. This is used for cosmetics. Although it is not limited to a dosage form in particular, when it is used in a lotion or the like, it becomes cloudy and does not become a transparent dosage form. Also, depending on the viscosity of the product, stirring or the like is required before use, and caution is required for lotions and the like. Furthermore, it is also possible to use what extracted this white sea mud. It has been found that extraction may be performed with water or a combination of water and a hydrophilic organic solvent. Examples of the hydrophilic organic solvent include ethanol, methanol, butanol, ethylene glycol, diethylene glycol, triethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol, 1,4-butylene glycol, glycerin, diglycerin and the like. Is done. Extraction is more efficient when stirring or heating is applied. In particular, when extracting with water only, heating is required. The extracted product is used after removing the solvent if necessary. In this case, unlike the case where white mud is used as it is, the use restriction is reduced.
[0006]
The white sea mud treated as described above or the white sea mud extract can be blended into various dosage forms. For example, it can be selected from arbitrary dosage forms such as lotions, emulsions, gels, creams, cosmetic liquids, ointments, packs, bathing agents and the like.
[0007]
To formulating these dosage forms, mink oil, castor oil, olive oil, evening primrose oil, coconut oil, natural animal and vegetable oils and fats Ma Kademianattsu oil; jojoba oil, beeswax, lanolin, carnauba wax, such as candelilla wax wax; Higher alcohols such as stearyl alcohol, cetyl alcohol, and oleyl alcohol; higher fatty acids such as palmitic acid, stearic acid, oleic acid, behenic acid, and lanolin fatty acid; higher aliphatics such as liquid paraffin, solid paraffin, squalane, ceresin, and microcrystalline wax hydrocarbons; butyl stearate, hexyl laurate, diisopropyl adipate, diisopropyl sebacate, octyl dodecyl myristate, isopropyl myristate, isopropyl palmitate, isopropyl myristate, Sechirui Octanoate, synthetic ester oils such as neopentyl glycol dicaprate; methyl silicone, silicone derivatives such as silicone oil and methyl phenyl silicone;
[0008]
Surfactants include anionic surfactants such as alkyl sulfates, fatty acid salts, alkyl phosphates, phosphates and sulfates of polyoxyethylene alkyl ethers; glycerin fatty acid esters, polyoxyethylene sorbitan fatty acid esters, poly Nonionic surfactants such as oxyethylene alkyl ether, sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, polyglycerin fatty acid ester; alkyl betaine, phosphobetaine, phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylglycerol, phosphatidylinositol and In addition to these lyso forms, double-sided active agents such as phosphophatidic acid and its salts ;
[0009]
Sugar alcohols such as ethylene glycol, diethylene glycol, triethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol, 1,4-butylene glycol, glycerin, diglycerin, polyglycerin, sorbitol, mannitol, xylitol, maltitol , Ethylene oxide of glycerol (hereinafter abbreviated as EO), propylene oxide (hereinafter abbreviated as PO) adduct, EO of sugar alcohols, PO adduct, monosaccharides such as galactose, glucose, fructose and its EO, PO Moisturizers such as adducts, polysaccharides such as maltose and lactose and their EO and PO adducts ;
[0010]
Examples include tocopherol, tocopherol acetate, vitamin C, allantoin, placental extract, elastin, arbutin, collagen, triclosan, trichlorocarban, dipotassium glycyrrhizinate, methylparaben, and butylparaben.
[0011]
【Example】
Hereinafter, the present invention will be described more specifically with reference to production examples and examples. However, it is needless to say that the present invention is not limited to these production examples and examples.
[0012]
[Production Example 1]
The white sea mud collected in Urukutapuru island Milky Way of the Republic of Palau washed with water, was pulverized in a mixer.
[0013]
[Production Example 2]
10 g of Production Example 1 was taken, 30 ml of distilled water was added, and extracted twice at 100 ° C. for 2 hours to obtain an extract. The solid content of this extract was 0.97%.
[0014]
Example-1 Clay Pack A
Production Example 1 30.0 parts by weight Titanium oxide 2.0 parts by weight Polyoxyethylene (20E.0) cetyl ether 1.0 part by weight 1,3 butylene glycol 10.0 parts by weight Glycerin 10.0 parts by weight Methyl paraoxybenzoate 0.1 parts by weight B
Polyvinyl alcohol 1.0 part by weight Purified water 50.0 part by weight <Preparation method>
A is heated at 50 ° C. and mixed uniformly. B dissolves uniformly at room temperature. While stirring A, gradually add B and mix uniformly. Cool with stirring and stop stirring at 35 ° C.
[0015]
Example-2 Cream A
Squalane 25.0 parts by weight Jojoba oil 5.0 parts by weight Beeswax 5.0 parts by weight Cetanol 3.0 parts by weight Monoglyceryl stearate 2.0 parts by weight B
Polyoxyethylene (20 mol) sorbitan monostearate 3.0 parts by weight Production Example 2 10.0 parts by weight Glycerin 7.0 parts by weight 1,3 butylene glycol 7.0 parts by weight Methyl paraoxybenzoate 0.3 parts by weight Part Purified water 41.7 parts by weight In the production method, A and B were heated and stirred, while B was gradually added to A and cooled.
[0016]
Example-3 Latex A
Decaglyceryl monomyristate 2.1 parts by weight Hydrogenated soybean phospholipid 0.6 part by weight Stearic acid 0.5 part by weight Behenyl alcohol 1.6 part by weight Cetyl palmitate 0.6 part by weight α-olefin oligomer 6.0 part by weight Cetyl 2-ethylhexanoate 6.0 parts by weight Glyceryl tri-2-ethylhexanoate 6.0 parts by weight Production Example 2 2.0 parts by weight Glycerin 5.0 parts by weight Paraoxybenzoic acid 0.3 parts by weight B
Purified water 54.2 parts by weight C
Carboxyvinyl polymer 0.1 parts by weight Purified water 10.0 parts by weight D
Sodium hydroxide 0.04 parts by weight Purified water 4.96 parts by weight In the preparation method, both A and B are heated and dissolved at 80 ° C., and B is gradually added to A while stirring with a homomixer and emulsified at 5,000 rpm for 5 minutes. To do. Add C and D with paddle stirring, cool, stop stirring at 40-35 ° C., and let stand.
[0017]
Example-4 Lotion A
Dipotassium glycyrrhizinate 0.2 parts by weight Citric acid 0.1 parts by weight Sodium citrate 0.3 parts by weight Purified water 82.9 parts by weight B
Tetraoleate P0E (60) sorbitol 0.9 parts by weight Sorbitan monooleate 0.1 parts by weight olive oil 0.1 part by weight of dipropylene glycol 5.0 parts by weight Preparation Example 2 0.1 parts by weight Ethanol 10. 0 part by weight p-hydroxybenzoic acid 0.3 part by weight In the preparation method, both A and B are heated and dissolved at 50 ° C., and B is gradually added to A while stirring and solubilized. Cool with stirring, stop stirring at 30 ° C. and let stand.
[0018]
Example-5 Face Wash A
Lauric acid 2.0 parts by weight Myristic acid 17.0 parts by weight Palmitic acid 4.0 parts by weight Stearic acid 4.0 parts by weight Palm oil fatty acid potassium 8.0 parts by weight Palm oil fatty acid diethanolamide 3.0 parts by weight N-cocoyl Methyl taurine sodium 10.0 parts by weight Concentrated glycerin 5.0 parts by weight 1,3-butylene glycol 5.0 parts by weight Production Example 1 5.0 parts by weight p-hydroxybenzoic acid 0.3 parts by weight B
Potassium hydroxide 5.5 parts by weight Tedesodium edetate 0.2 parts by weight Purified water 28.3 parts by weight In the preparation method, A is heated and dissolved at 80 ° C. B dissolves at room temperature. Slowly add B to A while stirring and dissolve uniformly. Cool with stirring, stop stirring at 35 ° C. and let stand.
[0019]
Use evaluation 1
48-year-old woman from the 23-year-old, used in cosmetic process and the same way up to the 5 dishes of Example 5 from Example 1 in 12 people chosen at random out of 24 people three months were asked to use (now I was asked to).
As a result, 10 people answered that the skin became white, 7 people said that the skin was no longer rough, 8 people answered that the skin was fine, and 6 people said that the skin was gone As a result, 11 people answered that they wanted to use Examples 1 to 5 rather than the cosmetics used so far. No one complained of irritation or discomfort in the skin.
[0020]
For the remaining 12 people, Production Example 1 was replaced with coral powder and Production Example 2 was replaced with extracts obtained by treating coral powder in the same manner as in Production Example 2. Examples 1 to 5 (that is, Comparative Examples 1 to 5) were replaced for 3 months. We had you use.
As a result, one person replied that the skin became white, two persons replied that the rough skin disappeared, one person replied that the skin texture became fine, and two persons replied that Kusumi disappeared As a result, there was one person who answered that Comparative Examples 1 to 5 would like to use the cosmetics used so far. No one complained of irritation or discomfort in the skin.
[0021]
Use evaluation 2
After tanning 5 women aged 21 to 33 years old, the skin lotion of Example 4 was used 3 times a day. The state returned to normal soon.
[0022]
Usage evaluation 3
38-year-old woman from 23 years old, eight to Example 1 of the clay pack as in Production Example 1 Example 1 is replaced with coral powder (i.e. Comparative Example 1) The once daily One not a Katakao, 2 months use I was asked to.
As a result, 7 people answered that the skin of the example was whiter, 6 people answered that the skin of the example was less rough, and 5 people answered that the example had less skin. No one answered that the comparative example was better for any of the items.
[0023]
Although the effectiveness of the preparation has been confirmed, we have experimented with a part of how it works, so the experimental method and results are described below.
Anti-tyrosinase experiment method [Experiment method]
And 0.5ml of the test liquid in a test tube, a substrate L-dopa solution (0.03%, 1 / 15M phosphate buffer solution, dissolved in pH 6.8) to e 0.5 m l pressurized, 25 ° C., 10 minutes Warmed up.
Next, 0.5 ml of tyrosinase solution (dissolved in phosphate buffer) was added, and the mixture was heated at 25 ° C. for 5 minutes.
After the reaction, the absorbance at 475 nm was measured (D1).
Separately, the same operation was performed without adding the substrate, the absorbance (D2) and the amount of dopachrome produced (D3) with no test solution added were measured, and the inhibition rate was determined by the following formula.
Inhibition rate = (D3-D1) / (D3-D2) × 100
Incidentally, the test those test liquid which is collected white mud taken at Urukutapuru island Milky Way Palau from three, the liquid was extracted same Production Example 2 of water was added 10ml to 15ml Liquids 1 to 3 were prepared (test liquid 1 was prepared by adding 10 ml of water to 15 ml of Production Example 2).
Moreover, what prepared 3 types of coral powders and processed it by the same method as the above was made into the test liquids 4-6.
The results are shown below.
Test solution 1 inhibition rate 67.9%
Test solution 2 inhibition rate 57.3%
Test solution 3 inhibition rate 68.1%
Test solution 4 inhibition rate 15.5%
Test solution 5 inhibition rate 4.6%
Test solution 6 inhibition rate 12.4%
Thus, white extract of mud collected in Urukutapuru island Milky Way Palau is coral powder was observed antityrosinase ability strongly is was observed antityrosinase ability be treated similarly.
[0024]
Rough skin test [Experimental method]
Hartley guinea pigs were depilated back of (female, 6 weeks old, 5 mice per group), 3% sodium lauryl sulfate - white Waseri down 0. 2 g was applied continuously for 3 days to create rough skin. Apply the water, production example 2, coral powder hot water extract (extraction method is the same as in production example 2) 1 ml, 3 times / day (1 place is not applied) 3 The degree of skin roughness was evaluated according to the criteria determined by observation after the day.
Judgment criteria are described below.
There is almost no erythema or desquamation = 0
Mild desquamation without erythema = 1
Moderate desquamation without erythema = 2
Desquamation with weak erythema = 3
Desquamation with moderate erythema = 4
Desquamation with marked erythema = 5
When the experimental results are expressed in total evaluation points, purified water was 23 points, production example 2 was 5 points, and coral powder was 16 points (by the way, 24 points for the uncoated portion).
As a result, Production Example 2 was confirmed to be effective in improving rough skin.
[0025]
Since the effectiveness was confirmed as described above, an experiment was conducted as follows for safety, which is one of the qualities required as an external preparation for skin.
Skin primary irritation test 0.2 ml of Hartley guinea pig (5 mice per group, body weight around 340 g) with hair removed from the back (Production Example 1 was 0.2 g of white petrolatum dispersed in 20%) was applied. . Judgment was performed 24 hours after application using the primary irritation scoring method with erythema and edema as indices.
As a result, in both Production Example 1 and Production Example 2, in all animals, no erythema and edema were observed, and it was judged negative.
Cumulative skin irritation test Hartley guinea pig (female, 5 mice per group, body weight around 340 g) with hair removed on the flank, once a day, 0.2 ml (Production Example 1 is white) 0.2 g) of 20% dispersed in petrolatum was applied. Application was performed over 4 weeks, and hair removal was performed on the last application day of each week. Judgment was performed on the day after the last day of each week by using the primary irritation scoring method with erythema and edema as indices.
As a result, in both Production Example 1 and Production Example 2, in all animals, no erythema and edema were observed for 1 to 4 weeks after application, and the result was determined to be negative.
[0026]
Although the effectiveness and safety were confirmed as described above, it was found that the effective components are components extracted from hot water, but it was not possible to identify the substances. Since elemental analysis was performed for reference, it is shown in the following Table 1 (unit: μg / mg).
[Table 1]

[0027]
【effect】
White mud in Urukutapuru Island Milky Way Palau, or solvent extract of white mud skin external preparation containing a combination of these may antityrosinase or rough skin prevention effect whitening, skin roughness prevention of dullness prevention, etc. It is effective and very safe.

Claims (4)

A skin whitening preparation for whitening comprising white sea mud in Milky Way on Urkutapur Island in the Republic of Palau . A skin external preparation for whitening comprising a solvent extract obtained by extracting white sea mud in Milky Way of Urkutapur Island in the Republic of Palau with water and / or a hydrophilic organic solvent. Cosmetics for whitening, characterized by blending white sea mud from Milky Way on Urkutapur Island in the Republic of Palau . A whitening cosmetic product comprising a solvent extract obtained by extracting white sea mud in Milky Way on the island of Urkutapur in Palau with water and / or a hydrophilic organic solvent.