KR100821482B1 - External skin application composition for skin whitening - Google Patents

Abstract

The present invention relates to a whitening skin external composition for improving or preventing skin pigment abnormalities and skin pigment overdeposition. More specifically, by containing kojic acid, ascorbic acid and derivatives thereof, tocopherol and derivatives thereof, ubiquinone and the like as active ingredients, the production of melanin as a skin pigment is suppressed with an excellent tyrosinase inhibitory effect, The present invention relates to a whitening skin external composition having an excellent skin whitening effect such as preventing skin pigmentation such as blemishes, freckles, skin blemishes, and sunburn.

The whitening effect of the skin external preparation composition for whitening according to the present invention, ascorbic acid, tocopherol and ubiquinone, which have excellent antioxidant ability, complementarily act to prevent browning and reduction of titer of kojic acid, This is because it effectively inhibited sinease activity. Therefore, the whitening skin external preparation composition according to the present invention can reduce the blending content of kojic acid used to achieve the same degree of whitening effect. In addition, the topical skin preparation composition for whitening according to the present invention has no skin side effects and is excellent in stability in terms of formulation.

Whitening, kojic acid, ascorbic acid, tocopherol, ubiquinone, melanin

Description

External skin application composition for skin whitening}

The present invention relates to a whitening skin external composition for improving or preventing skin pigment abnormalities and skin pigment overdeposition. More specifically, by containing kojic acid, ascorbic acid and derivatives thereof, tocopherol and derivatives thereof, ubiquinone and the like as active ingredients, the production of melanin as a skin pigment is suppressed with an excellent tyrosinase inhibitory effect, The present invention relates to a whitening skin external composition having an excellent skin whitening effect such as preventing skin pigmentation such as blemishes, freckles, skin blemishes, and sunburn.

In general, the pigmentation phenomenon on the skin is a combination of a number of external factors such as ultraviolet rays, medications, pollutants, external irritant skin, and internal factors such as hormonal imbalance, inflammatory response factors, cytokines, etc. What is important is exposure to ultraviolet light. When the skin is exposed to ultraviolet rays, the activity of an enzyme called tyrosinase in the melanocytes in the basement layer increases, and this enzyme acts on tyrosine, a type of amino acid present in skin tissue. It acts to produce DOPA, which in turn turns into Dopaquinone, which automatically triggers a complex, multi-step reaction that forms melanin, which causes skin pigmentation. Meanwhile, the melanin pigment thus produced is widely distributed to the surrounding keratinocytes through dendrite of melanocytes, thereby changing the color of the skin. In normal skin, keratinocytes containing melanin pigment are differentiated into keratinocytes without nuclei through the keratinization process for about 4 weeks and naturally fall off from the skin. However, skin pigment abnormalities such as blemishes, freckles, and senile plaques are caused by abnormally excessive melanogenesis in melanocytes, but do not fall off normally.

Such hyperpigmentation often acts as a serious mental burden from the point of view of skin cosmetology and may adversely affect normal social activities. Therefore, while the main causes and mechanisms of skin hyperpigmentation as described above are revealed to some extent, substances that can inhibit the activity of tyrosinase in dermatological science, in addition to the method of blocking ultraviolet rays to prevent pigmentation. By incorporating them into cosmetics, many studies have been actively conducted to improve or prevent pigmentation such as blemishes and freckles. In particular, Asians, such as Korea, Japan, and China, who consider having white skin as a measure of beauty, are very interested in skin whitening cosmetics, and the desire to expect a substantial skin improvement effect from such whitening cosmetics is very high. strong.                         

Conventionally, it was intended to provide cosmetics having a whitening effect by combining tyrosinase activity inhibitors such as kojic acid, ascorbic acid, arbutin, hydroquinone, glutathione, and derivatives thereof, but the safety of these active materials for skin There is much room for improvement as a result of sufficient whitening effects due to the stability of the substance itself, the constraints on the amount of formulation required to achieve substantial efficacy, and the lack of an effective skin delivery system of the active substance.

Koji liquid seed, a representative substance that has the ability to inhibit the activity of tyrosinase, is a component obtained from fermentation broth of yeast fungi, and is one of the most widely used ingredients in the world since Japan's Goce Cosmetics was used for whitening cosmetics. The whitening effect of kojic acid is known not only to directly inhibit tyrosinase activity but also to inhibit melanin polymerization in melanocytes. In other words, cozixide forms coordination bonds with copper ions, which are indispensable to the action of tyrosinase, and thus the activity of tyrosinase, which is involved in the reaction from tyrosine to dopa and dopaquinone in the initial stage of melanogenesis. Incapacitate and inhibit melanin production by blocking the polymerization of 5,6-dihydroxyindole produced in dopachrome.

However, although kojic acid is superior to other whitening ingredients such as ascorbic acid and arbutin, the effect of inhibiting the activity of tyrosinase is known to cause skin abnormalities when a high content is used. In addition, the cosmetics containing kojic acid has a problem of easily oxidized at a high temperature (45 ℃) over time, the color is severely changed, the whitening activity is sharply dropped. In order to overcome these problems in formulation, the derivatives of kojic acid are synthesized, the contact with oxygen as much as possible by using a multi-emulsification technique, or the kojic acid is separated into a powder state and mixed before use Various types of products are being developed, such as the use of the product, but have not yet reached a satisfactory level.

The skin is covered with a natural protective layer of sebum and sweat at the outermost skin, and keratinocytes are also connected to each other by keratinocytes, so the skin is essentially more affinity for lipophilic components than hydrophilic components. Larger, and as a result, the absorption into the skin is also higher than that of the hydrophilic component. However, most of the active ingredients to help whitening are easily soluble in water, and the activity is easily lost by the surrounding environment. Therefore, the problem of how to effectively deliver the whitening ingredients into the skin is closely related to the determination of the necessary content to anticipate the whitening effect and the occurrence of skin abnormalities. As a result, it is impossible to develop a cosmetic that is safe on the skin and can exhibit a whitening effect in a short time without considering effective skin absorption enhancement methods.

The present invention is to solve the problems of the prior art as described above, an object of the present invention, in the whitening cosmetics containing kojic acid, ascorbic acid and its derivatives, tocopherol and derivatives thereof By using a combination of ubiquinone, etc., there is no skin side effect, it prevents browning phenomenon and reduced titer, and it inhibits tyrosinase activity, so it is excellent in whitening effect and excellent in stability in terms of formulation. It is to provide an external composition for skin.

Whitening skin external composition of the present invention is a Kojic acid 0.01 to 5.0% by weight, preferably 0.1 to 2.0% by weight relative to the total weight of the composition, ascorbic acid and its derivatives 0.01 to 5.0% by weight, Preferably 0.1 to 3.0% by weight, tocopherol and its derivatives 0.01 to 5.0% by weight, preferably 0.1 to 3.0% by weight, ubiquinone to 0.01 to 1.0% by weight, preferably 0.05 It is contained in an amount of -0.5% by weight, wherein the active ingredients to help the whitening are contained in an amount of 0.1 to 10% by weight based on the total weight of the composition as a whole.

In the whitening skin external composition of the present invention, the ascorbic acid and its derivatives are ascorbic acid, magnesium ascorbyl phosphate, sodium ascorbyl phosphate, ascorbyl glucoside, aminopropyl ascorbyl phosphate or a mixture of two or more thereof. It features. In the whitening skin external composition of the present invention, the tocopherol and its derivatives are tocopherol, tocopheryl acetate, tocopheryl linoleate, tocopheryl nicotinate, tocopheryl glucoside, tocopheryl succinate or mixtures of two or more thereof. It is characterized by that.

In the skin whitening composition for skin whitening of the present invention, the skin whitening composition for whitening has a softening lotion, nourishing longevity, massage cream, nutrition cream, essence, pack, gel, ampoule or skin adhesive type cosmetic formulation, lotion, It is characterized by having a transdermal dosage form such as an ointment, gel, cream, patch or spray.

In the formulation of the whitening skin external preparation composition of the present invention, the ampoules are separated from each other and packaged in powder and liquid, and immediately before use, the powder and the milk are mixed with each other to take an appropriate amount by means of a pump, an eyedropper or another method. As applied to the powder, the powder is kojic acid, ascorbic acid and its derivatives, excipients or mixtures of one or more thereof, and the liquid is a transparent or opaque cosmetic having flowability such as softening water, nutrient cosmetic water, essence, etc. It is characterized by. On the other hand, the excipient is hyaluronic acid, locust bean gum, cellulose gum, xanthan gum, carrageenan, karaya gum, tragacanth gum, tamarindus indica seed gum, guar gum, queen's seed gum, D-mannitol, betaine, trehalose , Dextrin, cyclodextrin or mixtures of one or more thereof.

Hereinafter, the configuration and operation of the present invention will be described in more detail with reference to Examples and Test Examples of the present invention. However, the present invention is not limited to these examples.

<Test Example 1: Determination of melanin production inhibitory effect using pigment cells of rats>

The pigment cells of the rats were treated with the composition of Table 1 below to determine the melanin production inhibitory effect.

Active ingredient Content (% by weight) Kojic acid ¹⁾ 30 Ascorbic Acid ²⁾ 30 Tocopherol ³⁾ 20 Ubiquinone ⁴⁾ 20 1) Alps Pharmaceutical Co., Ltd., Japan 2) Roche, France 3) Eisai, Japan 4) Nisin Flower Milling Company, Japan

Mel-Ab cells from C57BL / 6 mice were derived from Dulbecco's modified Eagle's media (DMEM) with 10% fetal bovine serum, 10 nM 12-O-tetradeca. It was incubated at 37 ° C. and 5% CO ₂ with medium containing noyl forbolol (tetradecanoylphorbol) -13-acetate and 1 nM cholera toxin. Cells were cultured at a concentration of 105 cells / well in a 24-well plate, and cell adhesion was confirmed. Then, a constant concentration of test substance was added to the cell culture, followed by incubation for 3 days. At this time, the test substance was dissolved in each of the composition components of Table 1 in a specific solvent, and then dissolved in a mixed solution in which the ratio of propylene glycol: ethanol: purified water is 5: 3: 2, diluted to the test concentration, and in the same ratio. It is a mixture.

After removing the culture solution, washed with PBS, and dissolved the cells with 1N sodium hydroxide to measure the absorbance at 400nm, to calculate the melanin production inhibition rate according to the following equation 1, the results are shown in Table 2 below ( Dooley Act).

Test substance (treatment concentration) Melanin production inhibition rate (%) Whitening composition 0.02% 85 Whitening Composition 0.01% 60 Whitening Composition 0.005% 25 Kojic acid 0.02% 55 Control 0

As shown in Table 2, the whitening skin external preparation composition according to the present invention shows a very high melanin production inhibitory effect even at a low concentration of about 0.01%, showing that it shows a better effect than when using only kojic acid alone Could.

<Test Example 2: Evaluation of the whitening effect at the animal level>

Brown tortoiseshell guinea pig (Tortoiseshell guinea pig) is pigmented by ultraviolet rays, ultraviolet A (PUVA), allergic reactions, etc., like humans. If you choose brown, you can remove the hair and use a wider skin area. The effect of improving pigmentation can be verified by causing pigmentation on the brown malt by the methods listed below and applying a whitening composition to the pigmentation site. In addition, the substance whose pigmentation improvement effect is recognized by this method is very useful as a primary in vivo retrieval method because it is very likely to have an effect even in the evaluation in human ultraviolet pigmented plaque.

① Preparation of UV Pigment

Pigmentation induced by ultraviolet light (UVB) was performed by bonding a light shielding aluminum foil having six open windows of 3 × 3 cm to the skin from which the hairs behind the brown malmot were removed, followed by an SE lamp (wavelength 290 to 320 nm, Toshiba) was irradiated with ultraviolet light (UVB) so that the total irradiation energy amount was 1,350 mJ / cm 2. After UV 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 2-3 days, peaking after about 2 weeks. It is important that the color tone of the resulting ultraviolet pigment plate is the same and that stains do not occur. It is preferable that an individual having poor formation of the ultraviolet pigment plate is not used for good results.

② Application method of composition

After irradiation with ultraviolet rays, the pigmentation became the best, that is, about 14 days after the pigmentation was formed, the application of the composition of Test Example 1 (see Table 1) was started. The number of applications was continued once a day or twice for 60 days. The composition was dissolved and diluted in a mixed solution of propylene glycol: ethanol: water = 5: 3: 2 and applied to the pigmentation site by a predetermined amount with a soft cotton swab. A control site was prepared to apply only the mixed solution to other sites. The effect by the mixed solution of the experiment was excluded. In addition, the effects of cumulative irritation were also observed.

③ judgment of effect

The effect was determined by measuring the degree of black and white of the skin color using a color difference meter (Minolta CR2002, Japan). In general, L * a * b * colorimeter is used to indicate color, and in the present invention, L * value (brightness) is mainly used as an index. L * values were calibrated with a standard whiteboard, and the measurements were evenly measured for pigmentation sites by repeating the measurement at least 5 times for one site. The difference (ΔL *) of the skin color at the start and completion of the application was calculated according to the following equation (2).

ΔL * = L * value 60 days after application—L * value at the start of application

The whitening effect is determined by comparing the ΔL * value of the sample application site and the control site where only the mixed solution is applied. If the ΔL * value is about 2, the whitening effect of the deposited pigment is clear. It can be determined. The measurement results of the whitening effect in the brown molemot are shown in Table 3 below.

Substance (treatment concentration) Whitening Effect (ΔL *) Whitening Composition (1.0%) 2.15 Whitening Composition (0.2%) 1.72 Kojic acid (1.0%) 1.26 Control 0.65

From the results of Table 3, it was found that the composition of the present invention has a clear whitening effect of the pigment deposited at 1.0% concentration and a whitening effect at 0.2% concentration. On the other hand, in the case of kojic acid, a slight whitening effect was observed when visually observed, but a reddish pigment was deposited on the rear part of the material-treated brown malt, which resulted in a decrease in the whitening effect. .

<Example 1 and Comparative Examples 1-5>

Example 1 and Comparative Examples 1 to 5 for testing the whitening effect on human skin are prepared as follows in the composition of Table 4 below. The raw materials 1-9 of Table 4 are mixed, it melt | dissolves completely, and it heats to 70 degreeC, and it is set as a water part. On the other hand, raw materials 10 to 18 are mixed and completely dissolved while heating to 70 ° C. to obtain an oil part. The oil part is added to the water part and stirred with a homogenizer (Tokushu Kika Kogyo Co., Ltd., Japan) for 3 minutes to form an emulsion. Then, raw materials 19 and 20 are added and stirred for 2 minutes. Thereafter, bubbles were removed and cooled to room temperature to prepare Example 1 and Comparative Examples 1 to 5.

number ingredient Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 One Purified water To 100 To 100 To 100 To 100 To 100 To 100 2 glycerin 7.0 7.0 7.0 7.0 7.0 7.0 3 Butylene Glycol 5.0 5.0 5.0 5.0 5.0 5.0 4 Propylene glycol 3.0 3.0 3.0 3.0 3.0 3.0 5 Skirt Mushroom Polysaccharides 6.0 6.0 6.0 6.0 6.0 6.0 6 Hyaluronic Acid Extract 4.0 4.0 4.0 4.0 4.0 4.0 7 Carbomer 0.12 0.12 0.12 0.12 0.12 0.12 8 Kojic acid 0.3 - 1.0 - - - 9 Ascorbic Acid 0.3 - - 1.0 - - 10 Tocopherol 0.2 - - - 1.0 - 11 Ubiquinone 0.2 - - - - 1.0 12 Cetearylglucoside 1.5 1.5 1.5 1.5 1.5 1.5 13 Glyceryl Stearate SE 0.8 0.8 0.8 0.8 0.8 0.8 14 Cetearyl Alcohol 0.6 0.6 0.6 0.6 0.6 0.6 15 Vegetable squalane 6.0 6.0 6.0 6.0 6.0 6.0 16 Caprylic Capric Triglyceride 3.0 3.0 3.0 3.0 3.0 3.0 17 Cyclomethicone 5.0 5.0 5.0 5.0 5.0 5.0 18 antiseptic Quantity Quantity Quantity Quantity Quantity Quantity 19 incense Quantity Quantity Quantity Quantity Quantity Quantity 20 Triethanolamine 0.12 0.12 0.12 0.12 0.12 0.12

Test Example 3: Safety Evaluation of Composition on Human Skin

Before the test for confirming the whitening effect on the human skin by the compositions of Example 1 and Comparative Examples 1 to 5 was carried out a human skin cumulative stimulation test to verify the skin safety of each composition.

A total of nine healthy adults underwent a total of nine 24-hour cumulative patching on the same site of the upper forearm. The patch method uses a Fin chamber or a similar kind of chamber, in which 15 μl of a composition is added dropwise per chamber, and the reactivity of the skin is calculated according to Equation 3 below. Table 5 shows. At this time, ± 1 point, + 2 points +, + 4 points (the highest score) in the reactivity, and when the average reactivity is less than 3 was determined as a safe composition for the skin.

As shown in Table 5, in the case of Comparative Example 2 containing kojic acid in the composition used in Test Example 3 was shown to cause slight irritation to the skin, but the remaining composition shows a distinct cumulative stimulation pattern Although not shown, it was confirmed that the combination of kojic acid, ascorbic acid, tocopherol, ubiquinone and the like at an appropriate concentration is advantageous in terms of skin safety than when used alone.

<Test Example 4: Evaluation of the whitening effect at the human skin level>

Twenty healthy men and women affixed an opaque tape with six holes of 1.5 cm in diameter on the upper forearm of the subject, and was then treated with 1.5 ~ 2 times more ultraviolet light (MED; Minimal Erythema Dose). UVB) was irradiated to induce pigmentation of the skin, and two months after the test substances were applied, the contrast of the skin was measured using a colorimeter. Each test substance was allowed to apply the topical skin preparations of Example 1 and Comparative Examples 1 to 5 twice daily over morning and evening.

Judgment of the effect was determined by obtaining an L * value representing the contrast of the skin as in the animal test. In general, the L * value of Korean skin that does not induce artificial pigmentation is in the range of 50 to 70.

If the test materials are applied, the L * value will gradually increase. The difference in skin color (ΔL *) at the start and completion of the application was calculated according to Equation 4 below to compare the whitening effect on human skin, and the results are shown in Table 6 below.

ΔL * = L * value on the last day of test substance application-L * value before test substance application

Test substance Whitening Effect (ΔL *) Example 1 3.94 Comparative Example 1 1.47 Comparative Example 2 2.93 Comparative Example 3 2.35 Comparative Example 4 1.76 Comparative Example 5 2.41

As shown in Table 6, the composition containing all of the kojic acid, ascorbic acid, tocopherol, ubiquinone, each of the appropriate amount was superior to the skin whitening effect on the human skin compared to the composition containing each component alone Furthermore, it was found that the whitening effect was more effective than kojic acid, which is known to have excellent whitening effect. This means that even if each composition is a lower content than when contained alone, it can provide a higher whitening synergy when combined together in an appropriate composition ratio.

On the basis of the results of the above-described test examples, the skin external preparation compositions for whitening of various formulations having a small irritation to the skin but having an excellent whitening effect are presented. However, it should be noted that the composition of the present invention is not limited only to the following formulation examples.

That is, the whitening skin external composition of the present invention is used for the purpose of treating, improving or preventing skin pigment overdeposition caused by skin pigmentation disorders such as blemishes, freckles, senile pigments, and skin blemishes. There is no particular limitation.

<Formulation example 1: flexible cosmetics>

Flexible longevity according to the present invention was prepared in the composition of Table 7. Components 2 to 8 are mixed and stirred together in purified water to dissolve completely. In addition, what melt | dissolved and completely melt | dissolved components 10-14 together in ethanol is called ethanol part. The ethanol part was slowly added to the water part while stirring and solubilized. Then, the component 15 was added and the pH was adjusted to 4-5 to prepare a flexible cosmetic water.

number Compounding ingredients Content (% by weight) One Purified water To 100 2 glycerin 6.0 3 Butylene Glycol 4.0 4 Propylene glycol 3.0 5 Hyaluronic Acid Extract 1.0 6 Skirt Mushroom Polysaccharides 1.0 7 Kojic acid 0.3 8 Ascorbic Acid 0.3 9 ethanol 8.0 10 Fiji-60 Hydrogenated Castor Oil 0.5 11 Tocopherol 0.2 12 Ubiquinone 0.2 13 antiseptic Quantity 14 incense Quantity 15 Potassium hydroxide Quantity

<Formulation Example 2: Nutrients>

Nutrients according to the present invention was prepared in the composition of Table 8. The components 2 to 9 are mixed and stirred together in purified water and heated to 70 ° C to completely dissolve the water. On the other hand, what melt | dissolved completely by heating to 70 degreeC, mixing and stirring components 10-18 together is used as an oil part. The oil part is added to the water part and first emulsified for 3 minutes using a homogenizer, and then the components 19-20 are added and the second emulsified for 2 minutes. Finally, cooled to room temperature to prepare nutrient cosmetics.

number Compounding ingredients Content (% by weight) One Purified water To 100 2 glycerin 8.0 3 Butylene Glycol 5.0 4 Hyaluronic Acid Extract 3.0 5 Skirt Mushroom Polysaccharides 2.0 6 Xanthan Gum 0.1 7 Carbomer 0.2 8 Kojic acid 0.6 9 Ascorbic Acid 0.6 10 Squalane 8.0 11 Meadowfoam Seed Oil 5.0 12 Polysorbate 60 1.5 13 Sorbitan sesquioleate 0.4 14 Glyceryl Stearate SE 1.0 15 Cetearyl Alcohol 0.8 16 Tocopherol 0.4 17 Ubiquinone 0.4 18 antiseptic Quantity 19 incense Quantity 20 Triethanolamine Quantity

<Formulation Example 3: Nutrition Cream>

Nutritional cream according to the invention was prepared in the composition of Table 9 below. The components 1 to 10 are mixed and stirred together, and heated to 70 ° C to completely dissolve the water. On the other hand, what melt | dissolved completely by heating to 70 degreeC, mixing and stirring components 11-21 together is called an oil part. The oil part is added to the water part and first emulsified for 3 minutes using a homogenizer, and then components 22 to 23 are added and the second emulsified for 2 minutes. Finally, the cream is cooled to room temperature.

number Compounding ingredients Content (% by weight) One Purified water To 100 2 glycerin 8.0 3 Butylene Glycol 6.0 4 Propylene glycol 4.0 5 Hyaluronic Acid Extract 3.0 6 Skirt Mushroom Polysaccharides 5.0 7 Xanthan Gum 0.1 8 Carbomer 0.1 9 Kojic acid 1.0 10 Ascorbic Acid 0.5 11 Vegetable squalane 6.0 12 Cetyloctanoate 4.0 13 Caprylic Capric Triglyceride 3.0 14 Cyclomethicone 5.0 15 Cetaarylglucoside 2.0 16 Sorbitan stearate 0.5 17 Glyceryl Stearate SE 1.5 18 Cetearyl Alcohol 2.0 19 Tocopherol 0.5 20 Ubiquinone 0.2 21 antiseptic Quantity 22 incense Quantity 23 Triethanolamine Quantity

<Formulation Example 4: Essence>

Essence according to the present invention was prepared in the composition of Table 10 below. The components 1 to 12 are mixed and stirred together, and heated to 70 占 폚 to completely dissolve the water. On the other hand, what melt | dissolved completely by heating to 70 degreeC, mixing and stirring components 13-25 together is used as an oil part. The oil part is added to the water part and first emulsified for 3 minutes using a homogenizer. Then, components 26 to 27 are added and second emulsified for 2 minutes. Finally, the essence is prepared by cooling to room temperature.

number Compounding ingredients Content (% by weight) One Purified water To 100 2 glycerin 4.0 3 Butylene Glycol 4.0 4 Fiji-8 2.0 5 Betaine 1.0 6 Hyaluronic Acid Extract 5.0 7 Skirt Mushroom Polysaccharides 8.0 8 Cellulose gum 0.1 9 Carbomer 0.1 10 Kojic acid 1.0 11 Ascorbic Acid 1.0 12 Ascorbic Glucoside 0.5 13 Propylene Glycol Monostearate 2.0 14 Hydrogenated Polydecene 2.0 15 Caprylic Capric Triglyceride 2.0 16 Dimethicone 1.0 17 Cyclomethicone 1.0 18 Polyglyceryl-3 Methylglucose Distearate 1.5 19 Glyceryl Stearate SE 1.0 20 Tocopherol 0.5 21 Tocopheryl Acetate 0.3 22 Tocopherylolinate 0.3 23 Ubiquinone 0.2 24 Butylated hydroxytoluene Quantity 25 antiseptic Quantity 26 incense Quantity 27 Triethanolamine Quantity

<Formulation example 5: ampoules>

Ampoules according to the present invention were prepared with the composition shown in Table 11 below. First, the components 1-10 were heated and heated to 70 degreeC, mixing and stirring together, and the water part was made into water parts, The components 11-24 were heated and heated to 70 degreeC while mixing and stirring together, and it was made into oil parts. The oil part is added to the water part, emulsified for 5 minutes using a homogenizer, and cooled to room temperature to prepare an emulsion. The powder is prepared by uniformly mixing the components 25 to 28 in the completely dried solid silver powder state. The ampoules are packaged separately into powders and liquids, mixed separately just before using 8.5 ml of emulsion and 0.6 g of powder separately, and then dissolved by a pump or an eyedropper and applied to the skin.

number Compounding ingredients Content (% by weight) latex One Purified water To 100 2 Diglycerin 3.0 3 Butylene Glycol 3.0 4 Fiji-75 1.0 5 Trehalos 3.0 6 Hyaluronic Acid Extract 5.0 7 Skirt Mushroom Polysaccharides 8.0 8 Seaweed Extract 3.0 9 Cellulose gum 0.1 10 Xanthan Gum 0.1 11 Propylene Glycol Monostearate 1.0 12 Vegetable squalane 3.0 13 Hydrogenated Polydecene 2.0 14 Cyclomethicone 2.0 15 Dimethicone Copolyol 1.0 16 Polyglyceryl-3 Methylglucose Distearate 1.5 17 Glyceryl Stearate 0.8 18 Tocopherol 2.0 19 Tocopheryl Acetate 1.0 20 Tocopherylolinate 0.5 21 Ubiquinone 1.0 22 Butylated hydroxytoluene Quantity 23 antiseptic Quantity 24 incense Quantity Powder 25 D-mannitol To 100 26 Ascorbic Acid 20.0 27 Magnesium Ascorbyl Phosphate 10.0 28 Kojic acid 35.0

<Formulation Example 6: Ointment>

Ointments according to the invention were prepared in the composition of Table 12 below. The components 1 to 7 are mixed and stirred together, and heated to 70 ° C to completely dissolve the water. On the other hand, what melt | dissolved completely by heating to 70 degreeC, mixing and stirring components 8-20 together is made into an oil part. The oil part is added to the water part and first emulsified for 4 minutes using a homogenizer, and then component 21 is added and the second emulsified for 3 minutes. Finally, the ointment is prepared by cooling to room temperature.

number Compounding ingredients Content (% by weight) One Purified water To 100 2 glycerin 8.0 3 Butylene Glycol 4.0 4 Hyaluronic Acid Extract 5.0 5 Skirt Mushroom Polysaccharides 3.0 6 Kojic acid 2.0 7 Ascorbic Acid 1.0 8 Liquid paraffin 15.0 9 Caprylic Capric Triglyceride 5.0 10 Vaseline 10.0 11 Polysorbate 60 1.2 12 Sorbitan sesquioleate 0.3 13 Glyceryl Stearate SE 1.0 14 Cetearyl Alcohol 3.0 15 paraffin 5.0 16 Beeswax 4.0 17 Tocopherol 1.0 18 Ubiquinone 0.5 19 Butylated hydroxytoluene Quantity 20 antiseptic Quantity 21 incense Quantity

As can be seen from the above, the present invention uses an ascorbic acid and its derivatives, tocopherol and its derivatives, ubiquinone and the like in an external preparation for skin whitening containing kojic acid in an appropriate amount, thereby causing skin abnormalities, sensitization, A safe skin whitening agent which is safe without side effects such as mutagenicity and shows excellent whitening effect could be applied to various formulations.

The whitening effect of the skin external preparation composition for whitening according to the present invention, ascorbic acid, tocopherol and ubiquinone, which have excellent antioxidant ability, complementarily act to prevent browning and reduction of titer of kojic acid, This is because it effectively inhibited sinease activity. Therefore, the whitening skin external preparation composition according to the present invention can reduce the blending content of kojic acid used to achieve the same degree of whitening effect.

As described above, the whitening skin external preparation composition according to the present invention effectively inhibits melanin production by using kojic acid, ascorbic acid and its derivatives, tocopherol and its derivatives, ubiquinone and the like as an active ingredient. It is excellent in effect and can effectively improve and prevent skin pigmentation such as blemishes, freckles and sunburn on the skin.

In addition, the topical skin preparation composition for whitening according to the present invention has no skin side effects and is excellent in stability in terms of formulation.

Claims (10)

0.01 to 5.0% by weight of kojic acid to the total weight of the composition, 0.01 to 5.0% by weight of the ascorbic acid and its derivatives, 0.01 to 5.0% by weight of the tocopherol and its derivatives, and ubiquinone 0.01 to 1.0 wt% based on the total weight, The active ingredient to help the whitening is contained in 0.1 to 10% by weight based on the total weight of the composition as a whole, the ascorbic acid derivative is magnesium ascorbyl phosphate, sodium ascorbyl phosphate, ascorbyl glucoside, aminopropyl asco Bilphosphate or a mixture of two or more thereof, and the tocopherol derivative is tocopheryl acetate, tocopheryl linoleate, tocopheryl nicotinate, tocopheryl glucoside, tocopheryl succinate or a mixture of two or more thereof. Skin external preparation composition for whitening. The method of claim 1, The kojic acid is 0.1 to 2.0% by weight relative to the total weight of the composition, ascorbic acid and its derivatives to 0.1 to 3.0% by weight, tocopherol and its derivatives to 0.1 to 3.0% by weight, ubiquinone It is contained in 0.05 to 0.5% by weight based on the total weight, The whitening composition for skin whitening, characterized in that the active ingredient to help the whitening is contained in an amount of 0.1 to 10% by weight based on the total weight of the composition. delete delete The method of claim 1, The whitening skin external composition is a skin care composition for whitening, characterized in that it has a flexible cosmetics, nourishing cosmetics, massage cream, nutrition cream, essence, pack, gel, ampoule or skin adhesive type cosmetic formulation. The method of claim 1, The skin whitening composition for skin whitening has a transdermal dosage form such as lotion, ointment, gel, cream, patch or spray. The method of claim 5, The ampoule is packaged separately from each other in a powder and a liquid, the skin and the external preparation composition for whitening, characterized in that the powder and the emulsion are mixed with each other immediately before use to take an appropriate amount with a pump or an eyedropper and apply it to the skin. The method of claim 7, wherein The powder is a topical kojic acid of claim 1, the ascorbic acid of claim 1 and its derivatives, excipients or mixtures of one or more thereof. The method of claim 7, wherein The liquid external preparation for skin whitening, characterized in that the liquid is a transparent or opaque cosmetic having flowability. The method of claim 8, The excipient is hyaluronic acid, locust bean gum, cellulose gum, xanthan gum, carrageenan, karaya gum, tragacanth gum, tamarindus indica seed gum, guar gum, queen's seed gum, D-mannitol, betaine, trehalose, dextrin Whitening skin external composition, cyclodextrin or a mixture of one or more thereof.