JPS61176510A - Skin-beautifying cosmetic - Google Patents

Abstract

PURPOSE:To provide a skin-beautifying cosmetic having excellent beautifying effect and high stability, and giving agreeable feeling to the skin, by compounding a specific amount of 10-hydroxy-DELTA<2>-decenoic acid and/or its salt to a cosmetic base. CONSTITUTION:The 10-hydroxy-DELTA<2>-decenoic acid of formula and/or its salt separable from royal jelly and known to have antibacterial activity and antitumor activity is added to a cosmetic in an amount of 0.3-15wt% based on the whole cosmetic. The compound of formula has strong effect to inhibit tyrosinase activity, and exhibits excellent skin-beautifying effect when added to a cosmetic at the above concentration. The compound is white odorless crystal having good handleability and excellent miscibility or solubility with other cosmetic components and applicable to any kind of cosmetic forms.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a skin whitening cosmetic that contains a skin whitening ingredient and has good usability and stability.

More specifically, the present invention provides cosmetic bases with 10-hydroxy-Δ-decenoic acid and (
or) the salt in proportion to the total amount of cosmetics,
The object of the present invention is to provide a whitening cosmetic characterized in that it is blended in an amount of 0.3 to 15% by weight.

It is generally believed that when the skin is irradiated with ultraviolet rays from sunlight, melanin is significantly produced due to the activation of tyrosinase in the skin, causing the skin to darken. Therefore,
In order to prevent and improve dark skin, it is necessary to inhibit tyrosinase activity during the melanin production process and bleach the existing melanin.
Based on this, various whitening ingredients have been proposed.

Conventionally, these whitening ingredients have been proposed, such as sulfur compounds represented by glutathione for inhibiting tyrosinase activity, and hydrogen peroxide and vitamin C for lightening color bleaching. there were.

However, these conventional whitening ingredients have poor stability in the formulation system, resulting in discoloration and unpleasant odors due to decomposition.
The effect/efficacy was insufficient in terms of transdermal absorption.
Moreover, it contains substances that pose safety problems, and as a result, it has not yet been possible to obtain a fully satisfactory product.

Therefore, the present inventors investigated many inorganic compounds and specific compounds from the viewpoint of their tyrosinase activity inhibiting effect.
As a result of intensive exploration and evaluation, 10-hydroxy-△2-
It has been found that decenoic acid and/or its salts have a strong tyrosinase activity inhibiting effect, and when it is contained in a cosmetic base at a certain concentration or more, an excellent whitening effect is exhibited. I found out. The present invention has been made based on this knowledge.

The present invention relates to a whitening cosmetic composition characterized by incorporating 10-hydroxy-Δ2-decenoic acid and/or its salt as an active ingredient into a cosmetic base material.

10-Hydroxy-Δ2-decenoic acid is a substance represented by the following formula, and is also called royal jelly acid. As its name suggests, this substance is naturally contained in royal jelly, is isolated from royal jelly by various isolation methods, and is known to have antibacterial and antitumor activities. It is also known that it can be produced using synthetic means (see JP-A-48-8723 and JP-A-54-88216), but there are no examples of practical use of this substance in cosmetics. Furthermore, it was still completely unknown that this substance had a whitening effect based on its tyrosinase inhibitory activity.

It has been known for a long time that royal jelly raw material is blended into cosmetics, but the content of 10-hydroxy-△2-decenoic acid in raw royal jelly is at most 2% of the total weight of royal jelly. ~3% by weight,
Therefore, even in cosmetics containing raw royal jelly, the content thereof is extremely small, and no practical effect of inhibiting melanin production can be obtained, and a sufficient whitening effect cannot be obtained.

In addition, royal jelly generally contains large amounts of protein and sugar as well as lipids such as fatty acids, and if it were to be incorporated into cosmetics at high concentrations, the amount and dosage form would be severely restricted. This is a fatal drawback as a compounding agent. In other words, in general, in order to obtain a stable and uniform emulsion, it is essential that the ingredients be sufficiently dissolved in the aqueous phase or oil phase during emulsification. Another problem is that it has extremely low solubility in oil, and that protein components undergo thermal denaturation at emulsification temperatures, and that good emulsions cannot be obtained when blended at high concentrations.

In addition, if the mixture is forced to a high concentration, it may cause a sticky or rough feeling or a royal jelly odor.
The sensual or tactile functions required for cosmetics are significantly reduced. In particular, this tendency becomes more and more obvious as the amount of addition increases, so conventionally only a very small amount was added as a practical amount.

In addition, the present situation is that it cannot be blended into lotions at all.

The 10-hydroxy-△2-decenoic acid used in the whitening cosmetic composition of the present invention is a white, odorless crystal that is easy to handle and has good miscibility with other cosmetic ingredients.
It also has excellent solubility and can be applied to all dosage forms. Also, unlike royal jelly, it does not contain proteins or other unknown ingredients, so it has excellent preservability.

In the whitening cosmetic of the present invention, 10-hydroxy-Δ
2-decenoic acid may be used as its salt. When used as a salt, the solubility in water is also increased, making it particularly suitable for use in lotions and the like. When 10-hydroxy-Δ2-decenoic acid is used as a salt,
Basic substances for the salt formation include lithium hydroxide, sodium hydroxide, potassium hydroxide, magnesium hydroxide,
Inorganic bases such as calcium hydroxide and ammonium hydroxide, basic amino acids such as arginine, lysine, histidine and ornithine, and organic bases such as monoethanolamine, jetanolamine and triethanolamine are used. The above salt may be prepared in advance and used by adding it, or the salt-forming components may be added separately and reacted in the formulation system to form the salt.

In the whitening cosmetic composition of the present invention, one or more of the above-mentioned 10-hydroxy-Δ-decenoic acid and its salts can be selected and used. The blending ratio thereof is selected to be 0.3 weight percent or more, particularly preferably 1 weight percent or more, based on the total amount of the cosmetic. Even if the amount exceeds 15 parts by weight, there is almost no change in the effect, so there is no need to exceed 15 parts by weight as a blending ratio.

The cosmetic base used in the whitening cosmetic of the present invention is not particularly limited and may be any base commonly used for whitening cosmetics.

Specific dosage forms include creams, ointments, milky lotions, lotions, and creams. For example, cream bases include beeswax, stearyl alcohol, stearic acid, glycerin, propylene glycol, propylene glycol monostearate, phoroxyethylene cetyl ether, squalane, etc.; cream bases include hinyl acetate resin emulsion, j51J vinyl Alcohol, ethanol, etc. and lotion bases include oleyl alcohol, ethanol, phlopylene gelicol, glycerin, lauryl ether, fulvitan monolaurate, and the like.

The cosmetic of the present invention uses these raw materials as appropriate and prepares cream 1. by a conventional method. It is prepared as a cosmetic in an appropriate form, such as Q-tsuku or lotion.

Next, in order to explain in more detail the usefulness of the whitening cosmetics of the present invention, the melanin-suppressing effect of 10-hydroxy-Δ2-decenoic acid, its mechanism of inhibiting tyrosinase activity, and ultraviolet light. Inhibitory effect on melanin production by 10-hydroxy-△2
- The results of experimental examples conducted on the whitening effect of cosmetics containing decenoic acid in actual usage conditions are shown below.

Experimental Example 1 Tyrosinase activity inhibition effect Regarding the tyrosinase activity inhibition effect of 10-hydroxy-Δ-decenoic acid and raw royal jelly, Harding,
-Passay? This was investigated using the enzyme tyrosinase extracted from mouse melanoma. Enzyme activity is determined by Dono Q-
Absorbs the amount of Donoq-chrome produced using the substrate as the maximum 4
A photometric method was followed, measuring absorbance at 75 nm. The strength of the inhibitory effect was determined from the concentration of the test substance that inhibited the tyrosinase activity by 50 times in the absence of the test substance. The results are shown in Table 1.

Table 1 Note) This shows the electric current concentration in the reaction solution.10-Hydroxy-Δ2-decenoic acid has a remarkable tyrosinase activity inhibiting effect, and is moreover at an extremely low concentration compared to raw royal jelly. The superiority of 10-hydroxy-Δ-decenoic acid was demonstrated by showing effective inhibition.

Experimental Example 2 Suppressive effect on melanin production by ultraviolet rays C57B
A group of 6 L mice was given test cream on the right auricle.
That is, to the basic cream formulation shown in Example 1, a cream containing a predetermined amount of 10-hydroxyΔ2-decenoic acid or fresh royal jelly was applied by adjusting the proportion of water at 0.05F each. The same amount of a control cream in which the test substance was replaced with water was applied to the left ear of the same mouse.

Then, using an FL20/5F30 lamp as a light source, the auricle was placed directly under the light source and irradiated with ultraviolet rays of 33 μw/5 ec-H2 for accelerated seconds (0.1 Joule). Sample application to the mouse ear pinna was performed once a day, and ultraviolet irradiation was performed three times a week, every other day. The same treatment was continued for 4 weeks. After the experiment was completed, the left and right auricles were collected, followed by NaBr treatment to separate the epidermis. The epidermis was treated with protease to digest auricular tissue proteins and obtain melanin granules. The melanin granules were oxidatively decomposed with H2O2, and the amount of melanin was measured using a fluorescence method. The results are shown in Table-2.

Table 2 From this table, 10-hydroxy-
△-decenoic acid clearly inhibits melanin production caused by ultraviolet rays at 0.3 parts by weight or more, but the inhibitory effect is slight in raw royal jelly even at the upper limit concentration that can be incorporated as a practical cosmetic, that is, in a cream containing 5%. It turns out that it is not satisfactory as a whitening cosmetic.

Experimental Example 3 Practical use test for whitening effect The cream of the present invention shown in Example 1 described later and the base cream that does not contain 10-hydroxy-Δ-decenoic acid were applied continuously for three months to a group of women with statistically equivalent age groups. When we investigated the whitening effect, as shown in Table 3, 10-hydroxy-△2
- The cream of the present invention containing decenoic acid was proven to be clearly more effective in improving dark skin, age spots, and freckles than the base cream. In addition, no unfavorable reactions were observed on the skin at the site where the cream of the present invention was applied.

In addition to the above, skin whitening effects can be achieved by using the whitening cosmetic composition according to the present invention and a base for each cosmetic composition according to the dosage form.
Tests were conducted to remove age spots and freckles, as well as skin beautification effects, and the results showed that the cosmetics of the present invention were extremely effective, demonstrating the whitening effect of 10-hydroxy-△2-decenoic acid. Ta.

Examples (prescription examples) of the whitening cosmetic of the present invention are shown below. Note that the blending ratio is in parts by weight.

Example 1 (whitening cream) Oil phase Whale wax
3.0 cetanol
2.0 stearic acid
1.0 Vaseline
5.0olive oil
4.0 squalane
5.0 Glycerin Monostearate 1.
0 polyoxyethylene (20) sorbitan monostearate 3.010-hydroxy-perdecenoic acid
2.0 Aqueous phase glycerin
-3,0 polyethylene glycol
3.0 Fragrances/Preservatives
Suitable girl
co
^Example 2 (whitening emulsion) Oil phase Vaseline
1.0 whale wax
1.0 squalane
5.0 jojoba oil
1.010-hydroxymedecenoic acid
2.0 Sorbitan Monostearate
1.0 polyoxyethylene (25)
Monostearate 2.0 aqueous phase carboxyvinyl polymer 0.2 triethanolamine
0.5 Propylene glycol 5.0 Fragrance/preservative
Appropriate amount of water
81.3 Example 3 (whitening lotion) Glycerin 2.
0 Malpitsuto
1.0 polyethylene glycol
4. Sodium 2-decenoate to 10-hydroxy-□ 1.0 Polyoxyethylene 0υ Hydrogenated castor oil 1.0 Ethanol
5.0PCA-Na

O,5 fragrance/preservative
Suitable for citric acid/sodium citrate buffer
0.11 water
85.39 Example 4 (Whitening/Q-Tsuction agent)

Claims (1)

[Claims] 1. 10-hydroxy-△^2-decenoic acid and (or) its salt as an active ingredient in a cosmetic base, the proportion of which is 0.3 to 15% of the total amount of the cosmetic. A whitening cosmetic characterized by being formulated in an amount of % by weight.