JP3170040B2 - Whitening cosmetics - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention has a high whitening effect, inhibits the activity of hyaluronidase, and is effective for rough skin, etc.
About the whitening cosmetic composition of the skin except for the scalp.

[0002]

2. Description of the Related Art Scratched stones are the dicotyledonous plant net, the leaf-flowering sub-net, the iridaceae, the hoeaceae, and the genus Harrigwa, which have the scientific names of Cudrania cochinchinensis L.
It is a dried plant whose roots are commonly referred to as Senhaseki. As a conventional use, it has an antibacterial (tuberculosis) action, and can be reduced by pulmonary tuberculosis together with iron wrapping, etc.
It has been used for pale skin, cough, sputum, hemoptysis, chest pain, slight fever, night sweats and other symptoms.

[0003] Nishikawayanagi has given the scientific names of dicotyledonous plant nets, leafy flower subassets, camellia eyes, goryidaceae, and gourd genus to Tamarix chinensis Lour.
This is a dried plant that has a leaf with a leaf, which is generally called gyoryu. Although this plant is native to China, it is a deciduous small tree that has been introduced to Japan for appreciation and is planted in gardens and the like. Conventional uses include sweating, fever relief, diuresis, antitussive, antibacterial (pneumococci, α-streptococci, white staphylococci, influenza) and the like.

On the other hand, various substances having a whitening effect that can be used as raw materials for cosmetics are known, but synthetic products have no guarantee of safety when applied to human skin for a long time. , Use is being restricted. On the other hand, many natural products have a weak whitening effect. However, from the aspect of safety for human skin, many people eat it with natural products,
It is guaranteed in terms of safety, and has a strong whitening effect,
There is a need for a substance that also has other effects on the skin.

[0005]

An object of the present invention is to provide a scalp.
As well as a safe when applied to the skin (hereinafter simply referred to as skin) excluding and large whitening effect to inhibit the activity of hyaluronidase, beauty containing active ingredients such as further rough
The purpose is to provide white cosmetics.

[0006]

Means for Solving the Problems In order to solve the above-mentioned problems, the present inventors have screened and examined plants which have been used for food for many years and whose safety to the human body has been confirmed, and used them as cosmetics. We considered something worthwhile. As a result, they have found that Nishikawayanagi and crushed stone have very similar effectiveness as raw materials for cosmetics or as quasi-drugs, and completed the present invention. The confirmed effects include whitening, inhibition of hyaluronidase activity,
Active oxygen suppression and antioxidant properties were confirmed.

[0007] That is, the present invention is a skin-whitening cosmetic excluding scalp, which contains a crushed stone and / or a solvent extract of Nishikawayanagi.

As a method of using Nishikawayanagi and crushed stone, extraction is performed with water or a hydrophilic organic solvent such as ethanol, methanol or acetone. However, since it is an extract of cosmetic raw materials, it is natural that extraction with water, ethanol, or a mixed solvent thereof is preferable. In some cases, glycerin, 1,3-butylene glycol,
Polyhydric alcohols such as propylene glycol or a mixture of polyhydric alcohol and water can also be used for extraction. Moreover,
Lyophilization and use as a powder are also effective depending on the method of use.

This substance is used as a raw material for other cosmetics such as liquid oils such as squalane and jojoba oil, solid oils such as beeswax and cetyl alcohol, various activators, humectants such as glycerin and 1,3-butylene glycol and various chemicals. In addition, cosmetics of various dosage forms can be prepared. For example, a use form may be considered depending on the purpose, such as a lotion, a cream, an emulsion, a pack, and the like.

The effect of the extract of the present invention is, as described above, firstly a skin whitening effect. The second is the action of suppressing the activity of hyaluronidase. Hyaluronidase is an enzyme that is widely distributed in living organisms and also present in the skin. As its name implies, it degrades hyaluronic acid. Hyaluronic acid is β-DN
-Acetylglucosamine and β-D-glucuronic acid are linear high molecular polysaccharides alternately bonded together and are a kind of glucosaminoglucan widely present in connective tissues of mammals together with chondroitin sulfate. The function of hyaluronic acid in connective tissue is to hold water in the intercellular space, form a jelly-like matrix in the tissue to hold the cells, maintain the lubricity and flexibility of the skin, Disorder)
And prevent bacterial infection. Hyaluronic acid in the skin decreases with age and, as a result,
It is said to cause aging such as wrinkles and rust. Therefore, suppressing the activity of hyaluronidase, which degrades this, can improve the stability of hyaluronic acid used in the preparation, the stability of hyaluronic acid in the preparation after application to the skin, and the hyaluronic acid existing in the skin. It is thought to contribute.

The third is an active oxygen suppressing action. Without oxygen, organisms (except anaerobic ones) cannot exist. However, oxygen becomes active oxygen under the influence of ultraviolet rays and enzymes. Active oxygen oxidizes fatty acids and produces peroxide. Phospholipids in biological membranes of living organisms also oxidize and cause damage. In addition, it is said that the generated peroxide and active oxygen damage DNA and promote aging. This active oxygen also affects the mechanism of producing melanin from tyrosine, and is also involved in skin darkening. Suppressing this active oxygen is important for the skin, in other words, an important factor required for cosmetics. The crushed stone and Nishikawayanagi of the present invention also have this active oxygen suppressing action and antioxidant property.

[0012]

EXAMPLES The following is an example of an actual method of use, but the present invention is not limited to this example. The following is an example of the production of the crushed stone and Nishikawayanagi used in the present invention.

(Production Example 1) 300 ml of ethanol was added to 10 g of crushed stone (dry product), and the mixture was left for 5 days with occasional stirring. This was lyophilized after filtration.

(Production Example 2) 5 g per 10 g of crushed stone (dry product)
300 ml of 0% methanol aqueous solution was added, and the mixture was left for 5 days with occasional stirring. This was lyophilized after filtration.

(Production Example 3) 300 ml of purified water is added to 10 g of crushed stone (dry product) and heated for 3 hours. After allowing to cool, it was filtered and freeze-dried.

(Production Example 4) 300 ml of ethanol was added to 10 g of Nishikawayanagi (dried product), and the mixture was left for 5 days with occasional stirring. This was lyophilized after filtration.

(Production Example 5) 5 to 10 g of Nishikawayanagi (dried product)
300 ml of 0% methanol aqueous solution was added, and the mixture was left for 5 days with occasional stirring. This was lyophilized after filtration.

(Production Example 6) 300 ml of purified water is added to 10 g of Nishikawayanagi (dried product) and heated for 3 hours. After allowing to cool, it was filtered and freeze-dried.

(Example 1) Lotion olive oil 0.5 Ethanol extract of crushed stone from Production Example 1 0.5 polyoxyethylene (20E.O.) sorbitan monostearate 2.0 polyoxyethylene (60E.O. .) Hydrogenated castor oil 2.0 ethanol 10.0 1.0% aqueous sodium hyaluronate solution 5.0 purified water 80.0

Example 2 Cream A Squalane 20.0 Olive Oil 2.0 Mink Oil 1.0 Jojoba Oil 5.0 Beeswax 5.0 Cetostearyl Alcohol 2.0 Glycerin Monostearate 1.0 Sorbitan Monostearate 2 2.0 50% methanol extract of the crushed stone of Production Example 2 1.0 B Purified water 47.9 Polyoxyethylene (20E.O.) sorbitan monostearate 2.0 Polyoxyethylene (60E.O.) curing Castor oil 1.0 Glycerin 5.0 1.0% aqueous sodium hyaluronate solution 5.0 Methyl parahydroxybenzoate 0.1 A and B are each weighed, heated to 70 ° C., and gradually stirred into B while A is stirred. And then slowly stirring for 30 minutes.
Cooled to ° C.

Example 3 Example 3 is a lotion prepared by changing the extract of Production Example 1 of Example 1 to the extract of Production Example 3.

Example 4 Example 4 is a cream prepared by replacing the extract of Production Example 2 of Example 2 with the extract of Production Example 4.

(Example 5) Example 5 is a lotion prepared by changing the extract of Production Example 1 of Example 1 to the extract of Production Example 5.

(Example 6) Example 6 is a cream prepared as the B component by changing the extract of Production Example 2 of Example 2 to the extract of Production Example 6.

(Tyrosinase activity inhibition: whitening action test) (Test method) Mcllvaln buffer 0.9
ml, 1.66 mM Tyrosine solution 1.0 ml, 0.1 wt / v% aqueous solution of the above preparation example (lyophilized product) (If it is difficult to dissolve, add ethanol and then dissolve, then add purified water, and evaporate. After removing ethanol,
1.0 ml was adjusted to 0.1 wt / v%) in a screw vial, and heated in a 37 ° C constant temperature water bath for 5 minutes or more. Tyrosinase solution (Sigma, from mushrooms,
(914 units / ml) 0.1 ml was added, the temperature was kept in a constant temperature water bath at 37 ° C., and the absorbance was measured at 475 nm after 10 minutes. As a control, pure water was added instead of the sample solution, and the measurement was performed in the same manner. In this test, the final concentration of the sample is 0.033%. (Calculation formula) Tyrosinase activity inhibition rate (%) = {B- (AP)} /
B × 100 where A: Absorbance of sample specimen B: Absorbance of control P: Absorbance due to coloring of sample specimen (3-fold dilution) Table 1 shows the results of measurements on the samples of Production Examples 1 to 6 described above.
Shown in

[0026]

[Table 1]

(Test for inhibiting hyaluronidase activity) (Test method) 0.4% sodium hyaluronate 0.1M
(PH 6.0) Weigh 6 g of phosphate buffer solution,
After standing in a constant temperature water bath at 5 ° C. for 5 minutes, a 0.1 wt / v% aqueous solution of the above production example (freeze-dried product) (if it is difficult to dissolve, add ethanol and dissolve, then add purified water, evaporate, and evaporate the ethanol. After removal, 1.0 ml of the mixture was adjusted to 0.1 wt / v%), stirred, and added with 0.01% hyaluronidase (Sigma-made bovine testes, type IS).
1 ml of a 0.1 M (pH 6.0) phosphate buffer solution was added, and the mixture was immediately stirred, and 6 ml of the solution was placed in an Ostwald viscometer placed in a thermostat bath at 37 ° C. After 1 minute, 5 minutes, 10 minutes, 20 minutes, and 40 minutes, the viscosity was measured. As a control, pure water was added instead of the sample solution, and the measurement was performed in the same manner.
In this test, the final concentration of the sample is 0.0125%. 1
The results are shown in Tables 2 to 5 as an index, with the viscosity after one minute being 100.

[0028]

[Table 2]

[Table 3]

[Table 4]

[Table 5]

(Test for Suppressing Effect of Active Oxygen) There are various methods for measuring the effect of suppressing active oxygen. The following method was used in this study. pH 7.8 50 mM potassium phosphate buffer (containing 1.3 mM DETAPAC) 133 ml 40 unit / ml catalase above potassium phosphate buffer 5 ml 2 mM nitro blue tetrazolium above potassium phosphate buffer 5 ml 1.8 mM xanthine above Potassium phosphate buffer solution 17 ml 160 ml 2.4 ml of the mixture of reagents and 0.3 ml of a sample are added,
Xanthine oxynase (water is used as a sample in advance, and when the experiment is carried out, adjust the solution with the above potassium phosphate buffer so that the absorbance increases by about 0.02 per minute).
Immediately after adding ml, the absorbance (560 nm) is measured. (Measurement is divided into two to confirm linearity.) (Calculation formula) Inhibition rate = ((AB) / A) × 100 A: Change in absorbance per minute when water is used as a sample B: Change in Absorbance per Minute of Sample The concentration step was performed several times, and a 50% active oxygen production inhibiting concentration was searched for. The method of preparing the sample is as follows. The above-mentioned production example (lyophilized product) is dissolved in an aqueous solution of an appropriate concentration (if it is difficult to dissolve, ethanol is added thereto, and then purified water is added thereto, followed by evaporation.
After removing the ethanol, the concentration was adjusted to an appropriate concentration%). About the sample of the said manufacture examples 1-6,
Table 6 shows the results of the measured 50% active oxygen production inhibition concentration (final concentration%).

[0030]

[Table 6]

(Antioxidant test) The following test solutions were prepared in 50 ml test tubes with screw caps. Specimen 5 mg 2% linoleic acid ethanol solution 10 ml 0.1 M, pH 7.0 phosphate buffer 10 ml purified water 5 ml Before putting it in a thermostat, the following measurements were made after 3, 6 and 8 days. Test solution 0.125 ml, 75% ethanol 12.1
25ml, 30% ammonium thiocyanate 0.125ml
After stirring for 3 minutes, 0.125 ml of a 0.02N ferrous chloride 3.5% HCl aqueous solution was added, and the mixture was stirred and left for 3 minutes. Then, the absorbance was measured at a wavelength of 500 nm. Cell length 10
mm, control cell is water with test liquid replaced. (The same sample was measured three times and averaged.) However, for the test liquids of the samples of Production Examples 4 to 6, 2
The experiment was performed by changing the ethanol solution of 1% linoleic acid to the ethanol solution of 1% linoleic acid in a constant temperature bath at 50 ° C., while leaving the solution in a constant temperature bath at 40 ° C. with the light shielding. As the above Production Examples 1 to 6 and Comparative Examples, vitamin E (Liken E oil 700) and dibutylhydroxytoluene (BH
Table 7 and Table 8 show the test results for T).

[0032]

[Table 7]

[Table 8]

(Usage test) The face of each of five women was divided into left and right, one of which was used as an example and the other as a comparative example.
A questionnaire was given three months later after having used it at least once.
In the comparative examples, various extracts of the production examples were replaced with water from the examples. (Comparative Examples 1 and 2) In addition, 15
We divided into groups and conducted experiments using the following samples.

Experiment No. Samples used 1 Examples 1 and 2, Comparative examples 1 and 2 2 Examples 3 and 4 Comparative examples 1 and 3 Examples 5 and 6 Comparative examples 1 and 2 The following table summarizes the results of the questionnaire. Example is very good 3 Example is considerably better 2 Example is slightly better 1 No difference 0 Comparative example is slightly better -1 Comparative example is much better -2 Comparative example Table 9 shows the total value of the determination results.

[0035]

[Table 9]

[0036]

The whitening cosmetic containing the plant extract of the present invention is applied to the skin of the skin except the scalp, has a large whitening effect, inhibits the activity of hyaluronidase, Keeps skin lubricious and soft and prevents bacterial infection. Furthermore, since it has active oxygen suppression and antioxidant properties, it suppresses the production of peroxide and active oxygen, suppresses aging of the skin, and also prevents darkening of the skin. Therefore, it prevents rough skin and maintains the luster of the skin, so that it is extremely effective as a whitening cosmetic. Moreover, since it has been used as an internal medicine for many years, its safety to the human body is guaranteed.

Continuation of the front page (51) Int.Cl. ⁷ identification code FI A61K 35/78 A61K 35/78 W A61P 17/00 A61P 17/00 (58) Field surveyed (Int.Cl. ⁷ , DB name) A61K 7 / 00-7/50 A61K 35/78 CA (STN)

Claims (1)

(57) [Claims] 1. A skin-whitening cosmetic excluding scalp containing a crushed stone and / or a solvent extract of Nishikawayanagi.