KR100415278B1 - Skin whitening compositions using the Fragrance - Google Patents

Abstract

The present invention relates to a cosmetic composition having no skin irritation and excellent whitening effect by containing a perfume substance having an excellent melanin production inhibitory effect, and more specifically, geraniol (alpha-Santalol) And a mixture thereof, the present invention relates to a whitening cosmetic composition for enhancing the whitening effect without skin irritation.

Description

Skin whitening compositions using the Fragrance}

The present invention relates to a cosmetic composition having no skin irritation and excellent whitening effect by containing a perfume substance having an excellent melanin production inhibitory effect, and more specifically, geraniol (alpha-Santalol) And a mixture thereof, the present invention relates to a whitening cosmetic composition for enhancing the whitening effect without skin irritation.

Since ancient times in Korea, people with white and soft skin like white jade have been included in the condition of beauty to emphasize the importance of white skin. However, in modern times, our skin is irritated by air pollution, ultraviolet rays, and drugs, and the skin color is black. The color of the skin is black because the amino acid Tyrosine in our body reacts with an enzyme called Tyrosinase and then, through oxidation, black cells called melanin are produced.

In particular, when melanin production in pigment cells is abnormally activated due to abnormal secretion of ultraviolet rays or hormones, excessive melanin production and deposition results in skin pigmentation disorders such as blemishes and freckles. May interfere with normal social activities. In order to suppress melanin production, cosmetics and pharmaceutical products using tyrosinase inhibitors such as kojic acid, arbutin, hydroquinone, etc. have been developed and marketed, but there are insufficient skin whitening effects when combined with cosmetics and pharmaceuticals. There was a limit to its use due to problems such as.

In addition, in addition to the above-described whitening materials, research has been conducted to find whitening active ingredients in natural products, among which is Sangbaekpi (Japanese Patent Publication No. 55-4437 5, Small 64-26507, Small 64-83009, Pyeong 1) -25687, Korean Patent No. 5-139950, Korean Patent Nos. 92-002109, 97-021273), Licorice (Japanese Patent Publication No. 60-214721, 60-214728, Small 63-23809, Small 64-63506, Hei 1-149706, Korean Patent Nos. 92-002109, 97-025601), Peony (Japanese Patent Laid-Open No. 61-246109 and Korean Patent No. 92-002111), Cinnamon ( Japanese Laid-Open Patent Publication No. 63-30403, Hei 5-139954), Gosam (Japanese Laid-Open Patent Publication No. 64-26507 and Korean Laid-Open Patent Publication No. 92-002110), Brown root (Japanese Laid-Open Patent Publication No. 60-214727, Small 64 -16709), Angelica (Japanese Patent Laid-Open No. 56-92211, Hei 4-26 610), Bark Skin (Japanese Laid-Open Patent No. 60-214721, No. 61-50915, No. 61-246109), Banha ( Japanese Patent Laid-Open No. 2-207028, Korean Patent Publication No. 96-03 3442), aloe (Japanese Patent Laid-Open No. 52-44375, Hei 2-207030, Hei 5-139950) and many plant extracts and herbal extracts have been found to act on tyrosinase to inhibit melanin production. However, they also have many problems in using them beyond the effective concentrations in cosmetics and pharmaceuticals in terms of safety and discoloration potential, and did not reach the expected level in terms of whitening effects.

Accordingly, the present inventors searched for perfumes to find a new whitening substance that can overcome the problems of known whitening efficacy substances, and melanin having excellent geraniol and alpha-santalol. It has been found that the skin cosmetic composition having the effect of inhibiting production and containing the above substances can exhibit an excellent whitening effect without skin irritation, thereby completing the present invention.

In addition, it has been found that the geraniol and alpha-santarol further increase the whitening effect when used in combination with a known whitening fragrance ingredient (Santalum album) essential oil (Japanese Patent Publication No. 60-48931).

Accordingly, it is an object of the present invention to provide a whitening cosmetic composition exhibiting excellent whitening effect without skin irritation.

In order to achieve the above object, the skin whitening cosmetic composition according to the present invention is Geraniol (Geraniol), alpha-Santalol (alpha-Santalol) and mixtures thereof in a ratio of 0.001 to 5% by weight relative to the total weight of the composition It is characterized by containing. In addition, the composition is characterized by further containing essential oil (Santalum album).

Hereinafter, the present invention will be described in more detail.

The present invention has a melanin formation inhibitory effect in order to provide an excellent whitening effect, and also in the proportion of 0.001 to 5% by weight based on the total weight of the composition by mixing or alone with geraniol and alpha-santarol without skin irritation It contains.

Geraniol (Geraniol, 2-trans-3,7-dimethyl-2,6-octadien-8-ol) used in the present invention has a rose scent and is a synthetic fragrance that is often used when making various floral scents. , Molecular weight 154.26, specific gravity 0.89, boiling point 230 ° C.

Alpha-Santalol, 2-Methyl 5- (2,3-dimethyltricyclo [2.2.1.0 (2.6)] hept-3-yl-2-penten-1-ol) gives a lot of sandalwood sensation , Synthetic fragrance mainly used to make soft wood fragrance. Molecular weight 220.36, specific gravity 0.98, boiling point 302 ℃.

On the other hand, the sandalwood essential oil further contained in the present invention was obtained by slicing the sandalwood finely to supply water vapor, vaporize it, and then liquefy.

In the present invention, it was found that the above fragrances can inhibit melanin production, the effect was confirmed by performing a whitening effect test and skin irritation test in animals and humans.

In order to obtain the desired whitening effect in the present invention, it is preferable to contain the geraniol, alpha-santarol and mixtures thereof in an amount ranging from 0.001 to 5% by weight based on the total weight of the composition. If the content is less than the above range, the whitening effect does not appear, and if it exceeds the above range, it is not preferable because of stability of the formulation. However, in some cases, the content of the active ingredient may be an amount outside the above range.

The whitening cosmetic of the present invention is not particularly limited in the formulation, for example, supple cosmetics, astringent cosmetics, nourishing cosmetics, nutrition cream, massage cream, essence, eye cream, eye essence, cleansing cream, cleansing foam, cleansing It may have a formulation such as water, pack, powder, body lotion, body cream, body oil, body essence.

In addition, in the whitening cosmetic composition of each formulation, other components in addition to the above fragrances may be arbitrarily selected by the present inventors according to the formulation or use purpose of other cosmetics.

Hereinafter, although an Example and a test example are given and this invention is demonstrated in detail, this invention is not limited only to these examples.

Test Example 1 Measurement of Melanin Inhibition Effect Using Pigment Cells

Mel-Ab cells from C57BL / 6 mice, 10% fetal calf serum, 10 nM 12-O-tetradecanoylphorbol-13-acetate in Dulbecco's modified Eagle's media (DMEM) , 1 nM cholera toxin was added to the culture medium at 37 ℃, 5% CO ₂ conditions. After incubating the cells at a concentration of 10 ⁵ cells / well in a 24-well plate and confirming the cell attachment, the cells were cultured for 3 days by adding a constant concentration of test substances to the cell culture. Here, the test substances were dissolved in the mixed solvent in which the ratio of propylene glycol: ethanol: purified water is 5: 3: 2, which is known as a flavoring agent and a whitening agent, as shown in Table 1 below. The culture solution was removed, washed with PBS, and the cells were dissolved with 1 N sodium hydroxide to measure absorbance at 400 nm. The melanin production inhibition rate was calculated according to Equation 1 below and the results are shown in Table 1.

Test substance Treatment concentration (%) Melanin production inhibition rate (%) Eucalyptus essential oil 0.001 20.5 Tea-Tree Refinery 0.001 25.4 Geraniol 0.001 59.7 Eugenol 0.001 18.2 Geranyl acetate 0.001 20.2 Alpha-Santarol 0.001 52.5 Rinnarul 0.001 15.8 Sandalwood essential oil + geraniol 0.001 60.4 Sandalwood Essential Oil + Alpha-Santarol 0.001 59.1 Geraniol + Alpha-Santarol 0.001 61.2 Sandalwood Essential Oil + Geraniol + Alpha-Santarol 0.001 62.1 Kojisan 0.001 30.4

From the above results, geraniol and alpha-santarol in natural and synthetic fragrances have high melanin production inhibitory effect even at a low concentration of about 0.001%, and show excellent melanin production inhibitory effect even compared to kojic acid, which is already known as an excellent whitening agent. It was confirmed. In addition, when two or more of these fragrances are mixed and treated, the melanin production inhibitory effect is higher than when treated alone, and the sandalwood oil, which is already known as a whitening substance, is further mixed with the single fragrance or a mixture of spices. In this case, it was found that the more excellent melanin production inhibitory effect.

[Test Example 2] Evaluation of the whitening effect at the animal level

Brown guinea pigs (Tortoiseshell guinea pigs) are animals that cause pigmentation due to ultraviolet rays, UV rays, and allergic reactions, such as humans. If you choose, you can use a wide range of areas after hair growth. Pigmentation is produced by the method enumerated below, and the improvement effect of pigmentation can be screened by the method of apply | coating a whitening agent to the pigmentation site | part. In addition, the substance whose effects have been recognized by this method can be usefully used as a primary in vivo screening method because of the high probability that the effect also appears in human evaluation in ultraviolet pigmented plaques.

① Preparation of UV Pigment

Preparation of pigmentation by ultraviolet (UVB) is performed by attaching SE light (wavelength 290 to 320nm, Toshiba) was irradiated with ultraviolet (UVB) (total amount of irradiation energy 1350 mJ / ㎠). After irradiation, the aluminum foil was peeled off and the whitening effect of the test substance was evaluated by the following coating method. Pigmentation after UV irradiation appears after two or three days, reaching a peak after about two weeks. It is important that the resulting color tone of the ultraviolet pigmentation spot is the same and that spots do not form. An individual with poor formation of the ultraviolet pigmentation spot should not be used for good results.

② Coating method of whitening agent

The time point of application of the whitening agent after the ultraviolet roughening began about 14 days after the pigmentation became the highest, that is, the pigmentation was established. The number of coatings was once or twice a day, and the coating was continued for 50 days. The coating material is obtained by dissolving the test substances in Table 1 in a concentration that does not show cumulative stimulation in an excipient (propylene solvent: ethanol: purified water = 5: 3: 2 mixed solvent), and is applied with a cotton swab and the solvent must be applied to other parts. The control site was placed as a control.

③ judgment of effect

The whitening effect was determined by measuring the black-and-white degree of skin using a color difference meter (Minolta CR2002). L ^* a ^* b ^* colorimetric system was used to display the color, and in the present invention, the L ^* value (brightness) is mainly used as an index. The L ^* value is calibrated with a defined whiteboard, and the measurement is carried out by measuring the pigmentation portion evenly by repeating the measurement five times or more at one site. Difference (ΔL ^* ) of the skin color at the start and completion of the application was calculated according to Equation 2 shown in Table 2. The whitening effect is determined by comparing ΔL ^* between the sample application site and the control site. When the value of ΔL ^* is about 2, the whitening effect of the deposited pigment is clear. .

Test substance Treatment concentration (%) Whitening effect (△ L ^* ) Geraniol 1.0 1.76 Alpha-Santarol 1.0 1.85 Sandalwood essential oil + geraniol 1.0 2.02 Sandalwood Essential Oil + Alpha-Santarol 1.0 2.04 Geraniol + Alpha-Santarol 1.0 1.92 Sandalwood Essential Oil + Geraniol + Alpha-Santarol 1.0 2.11 Kojisan 1.0 1.54 Excipients (Vihicle) 0.82

From the results of Table 2, it was confirmed that the fragrances of geraniol and alpha-santarol, as well as the whitening effect superior to kojic acid even when mixed with each other, and also sandalwood alone or in a mixture of these components. It can be seen that the effect is more excellent when the essential oil is further mixed.

Test Example 3 Whitening Effect Test on Human Skin

Twelve healthy men were attached with an opaque tape with 6 holes of 1.5 cm in diameter on the upper forearm of the subject, and each subject was irradiated with UVB (1.5-2 times the minimum erythema). Induced blackening. Containing each of the test substances in Table 2, the lotion formulated in the Examples and Comparative Examples of Table 3 was applied twice a day (morning, evening) every day, and after two months of skin using a color difference meter Contrast was measured.

Determination of the effect was determined by obtaining the L ^* value representing the lightness of the skin as in animal testing (skin color of unburned Koreans generally ranges between 50 and 70). Was represented by - (L ^* value immediately before the test the final L ^* value), if the effective use of each of Examples and Comparative Examples lotion is the L ^* value is gradually increased comparison between test substance is ΔL ^* The results are shown in Table 4 below.

ingredient weight% Example 1 Example 2 Example 3 Example 4 Example 5 Example 6 Comparative Example 1 Beeswax 4.0 4.0 4.0 4.0 4.0 4.0 4.0 Polysorbate 60 1.5 1.5 1.5 1.5 1.5 1.5 1.5 Solbitan Sesquiolade 0.5 0.5 0.5 0.5 0.5 0.5 0.5 Liquid paraffin 5.0 5.0 5.0 5.0 5.0 5.0 5.0 Squalane 5.0 5.0 5.0 5.0 5.0 5.0 5.0 Caprylic / Capric Triglycerides 5.0 5.0 5.0 5.0 5.0 5.0 5.0 glycerin 3.0 3.0 3.0 3.0 3.0 3.0 3.0 Butylene glycol 3.0 3.0 3.0 3.0 3.0 3.0 3.0 Propylene glycol 3.0 3.0 3.0 3.0 3.0 3.0 3.0 Carboxy Vinyl Polymer 0.1 0.1 0.1 0.1 0.1 0.1 0.1 Triethanolamine 0.2 0.2 0.2 0.2 0.2 0.2 0.2 antiseptic a very small amount a very small amount a very small amount a very small amount a very small amount a very small amount a very small amount Purified water to 100 to 100 to 100 to 100 to 100 to 100 to 100 Geraniol 1.0 - 0.5 - 0.5 0.3 - Alpha-Santarol - 1.0 - 0.5 0.5 0.3 - Sandalwood essential oil - - 0.5 0.5 - 0.4 - Kojisan - - - - - - 1.0 Pigment a very small amount a very small amount a very small amount a very small amount a very small amount a very small amount a very small amount

Whitening effect (△ L ^* ) Example 1 1.76 Example 2 1.65 Example 3 1.81 Example 4 1.92 Example 5 1.87 Example 6 1.98 Comparative Example 1 1.63

[Test Example 4] Skin irritation effect test

For the lotion formulations of the Examples and Comparative Examples of Table 3, to which the respective test substances were added, skin safety was examined.

Conventional patch tests (CTFA Safety Testing Guideline: The Cosmetic, Toiletry, and Fragrance Association, Inc., Washington D.C. 1981: p1-4) were conducted for skin safety testing. A pinn chamber containing a sample was placed under the arm of 20 people, and after 24 hours and 48 hours, the patch was removed and the skin condition was observed. Gave. Then, the average value of 20 subjects was calculated, and the results are shown in Table 5 below.

<Score>

4: very irritating (skin damage)

3: severe irritation (bubble, etc.)

2: slight irritation (redness)

1: Almost no irritation.

0: No irritation at all, good for sensitive skin.

Judgment 24 hours later 48 hours later Example 1 1.8 0.9 Example 2 1.3 0.7 Example 3 1.9 0.8 Example 4 1.6 0.7 Example 5 1.9 0.9 Example 6 0.9 1.1 Comparative Example 1 1.5 1.1

From the results of Table 5, it can be seen that each embodiment containing the fragrance of the present invention is a safe substance having little skin irritation, and is suitable for use as a whitening cosmetic.

As described above, in the present invention, these perfumes inhibit melanin production by containing geraniol and alpha-santarol, which are fragrance substances having a whitening effect alone or in combination, or further containing sandalwood essential oil. It is possible to provide a whitening cosmetic composition exhibiting an excellent whitening effect, and also solved the problem of skin safety.

Claims (2)

The geraniol, alpha-Santa roll or whitening cosmetic composition characterized in that it contains an amount of between 0.001 and 5 wt% with respect to the total composition weight of a mixture thereof as a whitening active ingredient. According to claim 1, wherein the composition is a whitening cosmetic composition, characterized in that it further contains a sandalum (Santalum album) essential oil.