KR19990075041A - Whitening cosmetic composition containing ascorbic acid-aminopropanol phosphate diester - Google Patents

Abstract

The present invention relates to a whitening cosmetic composition containing ascorbic acid-aminopropanol phosphate diester (AsA-APPA). According to the present invention, by using AsA-APPA in place of a conventional ascorbic acid or ascorbic acid derivative Whitening improves instability in formulations caused by the use of ascorbic acid, instability in aqueous solution and weak skin safety without losing the effects of inhibiting melanin production of ascorbic acid, promoting the growth of fibroblasts and increasing collagen biosynthesis. Cosmetics can be provided.

Description

Whitening cosmetic composition containing ascorbic acid-aminopropanol phosphate diester

The present invention is ascorbic acid-aminopropanol phosphate diester (Ascorbic acid-

aminopropanol phosphoric acid diester; Hereinafter, the present invention relates to a whitening cosmetic composition containing AsA-APPA. More specifically, L-Ascorbic acid and 3-Aminopropane phosphoric acid are connected in the form of a phosphate diester. A whitening cosmetic composition containing ascorbic acid-aminopropanol phosphate diester, which treats spots and freckles, increases transdermal absorption of ascorbic acid and improves instability and skin safety in the formulation of ascorbic acid. It is about.

In general, ascorbic acid has a strong antioxidant action, collagen biosynthesis effect and fibroblast growth growth effect, in particular, by inhibiting melanin production in the skin by using the antioxidant effect to prevent abnormal pigmentation, such as blemishes, freckles It is used as an external preparation for skin. However, ascorbic acid is easily oxidized and browned under aqueous solution, and the above effects are also lost. Therefore, it is rare to use ascorbic acid alone.

Therefore, in order to solve this problem, ascorbic acid derivatives stabilized by bonding other compounds to hydroxyl groups at the 2,3,5,6 positions of ascorbic acid are used. Such ascorbic acid derivatives are degraded by enzymes when absorbed in vivo, thereby regaining the melanin production inhibitory effect of ascorbic acid, thereby preventing the deposition of spots and freckles. Related patents for ascorbic acid and its derivatives used as active ingredients in whitening cosmetics have been filed in domestic and international papers and patents (Japanese Patent Application Nos. 7-206332 and 7-233038), which are used in cosmetics It is associated with the effect of inhibiting production, preventing freckle and freckles and promoting the regeneration of skin cells.

Conventionally, known ascorbic acid derivatives include ascorbyl-6-monostearate and acyl derivatives such as ascorbyl-2,6-dipalmitate in which two fatty acids are substituted for ascorbic acid. These derivatives are more stable than ascorbic acid, but have not been significantly improved, and because they are crystalline, they are not efficient for external application. In addition, derivatives made of magnesium salts by combining phosphoric acid with ascorbic acid introduced phosphate groups into ascorbic acid, which is a water-soluble substance in itself and hardly absorbed to the dermal layer, and can be stabilized in aqueous solution. Although the percutaneous absorption was promoted, it discolored in an aqueous solution or precipitated as crystals, and there was a problem of generating a precipitate by combining with an external skin component, that is, an anionic polymer material or a surfactant. In order to solve this problem, ascorbic acid-2-O-α-glucoside in which glucose is substituted for the second hydroxyl group of ascorbic acid by microbial fermentation has recently been developed. It is excellent in stability, and hydrolyzed by α-glucotase in vivo to liberate ascorbic acid slowly. Therefore, it is reported that pharmacological action such as inhibiting melanin production and enhancing biosynthesis of collagen is expected, but ascorbic acid- 2-O-α-glucoside has a disadvantage in that it is uncertain that the effect of inhibiting melanin production through absorption and in vivo through the skin and is expensive.

Therefore, the present applicants have repeatedly studied to solve the above problems, it is known that the effect on the proliferation and collagen synthesis of fibroblasts and the stability to the skin is very excellent, it is widely used as an active ingredient of the anti-aging cosmetic composition When the 3-aminopropane phosphate is bound to 2-position of L-ascorbic acid in the form of phosphate diester to prepare ascorbic acid derivatives, the stability and safety are very excellent, and 3-aminopropane phosphate and L-asperate It was found that physiological activity of corbinic acid could be exhibited, and a patent application was filed under the name of "water stable L-ascorbic acid derivative and its preparation method" (Korean Patent No. 97-23005).

In addition, the present applicant is a cosmetic that can exhibit the stability, skin safety, fibroblast proliferation effect and melanin production inhibitory effect in the aqueous phase of L-ascorbic acid derivative, ie, AsA-APPA, prepared by the method described in the above-mentioned document. As a result of repeated studies to develop the present invention, it was found that the above object can be achieved when the AsA-APPA is contained in an amount of 0.005 to 10% by weight based on the total weight of the composition.

Accordingly, it is an object of the present invention to provide a whitening cosmetic which is excellent in stability and safety while containing AsA-APPA, inhibiting melanin production, promoting fibroblast growth and increasing collagen biosynthesis.

In order to achieve the above object, the whitening cosmetic of the present invention is characterized by containing AsA-APPA in an amount of 0.005 to 10% by weight based on the total weight of the composition.

The above and other objects, features and advantages of the present invention will become apparent to those skilled in the art from the following detailed description.

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

The present invention uses AsA-APPA in which 3-aminopropane phosphoric acid is bound to L-ascorbic acid as an ascorbic acid derivative in a whitening cosmetic that inhibits melanin production.

In other words, AsA-APPA has the effect of inhibiting melanin production of ascorbic acid, prevents ascorbic acid from being easily oxidized and browned in aqueous solution, increases transdermal absorption of ascorbic acid, and forms ascorbic acid. Ascorbic acid derivatives with improved instability and skin safety.

AsA-APPA used in the whitening cosmetics of the present invention is a 2-chlorotetrahydro-2H-1,3,2-oxazaphosphorine-P-oxide obtained by the intermediate process of 3-aminopropane phosphate synthesis. It is obtained by directly reacting with ascorbic acid using the property of ring opening. That is, AsA-APPA reacts 3-amino-1-propanol and phosphorus oxychloride at an equivalent ratio of 1: 1 to 1.3 in an organic solvent in an organic solvent at a temperature of 0 to 5 ° C. for 1 to 2 hours, thereby allowing 2-chloro After preparing tetrahydro-2H-1,3,2-oxazaphosphorin-P-oxide, it is reacted with L-ascorbic acid protected with 5,6-hydroxyl group in the presence of an organic solvent, and then hydrolyzed. Prepared by crystallization with a polar organic solvent, represented by the following formula (1).

(Ⅰ)

AsA-APPA is contained in an amount of 0.005 to 10% by weight, preferably 0.01 to 3.0% by weight based on the total weight of the composition in order to obtain the desired effect in the present invention.

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 ingredients in addition to the above-mentioned AsA-APPA can be appropriately selected by those skilled in the art without difficulty according to the formulation or purpose of use of other cosmetics.

Hereinafter, after briefly showing a production example of AsA-APPA, examples and comparative examples will be described in detail the configuration and effect of the present invention. However, the present invention is not limited only to these examples.

[Production Example]: L-ascorbic acid, 3-aminopropanol phosphate diester>

10 g (0.046 mol) of 5,6-isopropylidene ascorbic acid, which protected the 5,6-hydroxyl group of L-ascorbic acid using an isopropylidene group, was dissolved in 100 ml of chloroform, and then, 12.9 mL (0.093 mol) of ethylamine was added dropwise. 8.6 g (0.055 mol) of 2-chlorotetrahydro-2H-1,3,2-oxazaphosphorine-P-oxide dissolved in 20 ml of chloroform was added dropwise. After completion of the dropwise addition, the mixture was stirred at room temperature overnight, the organic layer was washed with an aqueous solution of phosphoric acid, dried over anhydrous sodium sulfate and activated carbon, and decolorized. The reaction solution was filtered and the filtrate was concentrated under reduced pressure, and the obtained residue was dissolved in 30 ml of purified water and stirred for 3 hours at 50 ° C in a thermostat. 150 ml of isopropanol was added to the stirred reaction solution to obtain crystals, and the obtained crystals were dried in vacuo to obtain L-ascorbic acid and 3-aminopropanol phosphate diester as 6 g of a white solid.

<Example 1 and Comparative Examples 1-5> Cream

ingredient Example 1 Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Cetostearyl alcohol 1.0 1.0 1.0 1.0 1.0 1.0 Lipophilic Monostearic Acid Glycerin 1.0 1.0 1.0 1.0 1.0 1.0 Monostearic acid polyoxyethylene sorbitan (E.O. 20) 1.5 1.5 1.5 1.5 1.5 1.5 Self-emulsifying monoglycerate glycerin 1.0 1.0 1.0 1.0 1.0 1.0 Tri (capryl, capric acid) glycerin 6.0 6.0 6.0 6.0 6.0 6.0 Liquid paraffin 7.0 7.0 7.0 7.0 7.0 7.0 Squalane 3.0 3.0 3.0 3.0 3.0 3.0 Tocopheryl Acetate 1.0 1.0 1.0 1.0 1.0 1.0 Allantoin 0.3 0.3 0.3 0.3 0.3 0.3 glycerin 7.0 7.0 7.0 7.0 7.0 7.0 Propylene glycol 7.0 7.0 7.0 7.0 7.0 7.0 Xanthan Gum 0.5 0.5 0.5 0.5 0.5 0.5 antiseptic handful handful handful handful handful handful incense handful handful handful handful handful handful Ascorbic Acid (AsA) - - 0.5 - - 0.25 Aminopropanol phosphate (APPA) - - - 0.5 - 0.25 AsA-APPA (production example) 0.5 - - - - Magnesium Ascrobyl Phosphate - - - - 0.5 - Purified water to100 to100 to100 to100 to100 to100

[Manufacturing method]

After heating and dissolving an aqueous phase and an oil phase, respectively, these were mixed and stirred, cooled to room temperature, and molded into a product.

<Example 2 and Comparative Examples 6 to 10> Flexible Cosmetics

ingredient Example 2 Comparative Example 6 Comparative Example 7 Comparative Example 8 Comparative Example 9 Comparative Example 10 Purified water to 100 to 100 to 100 to 100 to 100 to 100 Polyoxyethylene octyldodecyl ether-16 0.5 0.5 0.5 0.5 0.5 0.5 Polysorbate (20) 0.5 0.5 0.5 0.5 0.5 0.5 glycerin 10.0 10.0 10.0 10.0 10.0 10.0 Propylene glycol 9.0 9.0 9.0 9.0 9.0 9.0 Polyethylene Glycol 4000 3.0 3.0 3.0 3.0 3.0 3.0 Allantoin 0.3 0.3 0.3 0.3 0.3 0.3 Carboxymethyl Cellulose Sodium 0.2 0.2 0.2 0.2 0.2 0.2 Ascorbic Acid (AsA) - - 0.5 - - 0.25 Aminopropanol phosphate (APPA) - - - 0.5 - 0.25 AsA-APPA (production example) 0.5 - - - - - Magnesium Acroville Phosphate - - - - 0.5 - ethanol 7.0 7.0 7.0 7.0 7.0 7.0 incense handful handful handful handful handful handful antiseptic handful handful handful handful handful handful

[Manufacturing method]

After heating and dissolving carboxymethylcellulose sodium in purified water and cooling to room temperature, the remaining water-soluble component was added, the ethanol part was added and mixed, and it shape | molded into the product.

<Example 3> Oil-in-water type makeup oil cosmetic

ingredient Example 3 Ozokerite 3.0 Hexyllaurate 6.0 Cetyldimethicone copolyol 3.0 Silicone gel 20.0 Trimethylsiloxysilicate 3.0 Acrylic-Silicone Copolymer 4.0 Cyclomethicone 15.0 Colorant 15.0 Purified water to 100 glycerin 5.0 AsA-APPA 0.5 antiseptic handful incense handful

[Manufacturing method]

First, the oil phase was completely heated and dissolved, and then cyclomethicone and colorant were added and dispersed in a homomixer. At this time, the colorant was mixed with 70.0% by weight of titanium dioxide, 20.0% by weight of iron oxide and 10.0% by weight of talc uniformly and then pulverized twice. Next, the heated and dissolved aqueous phase was added to the oil phase, mixed, stirred, emulsified, cooled and molded into a product.

Test Example 1 Proliferation of Fibroblasts

Fibroblasts were cultured by removing the epidermis from the skin obtained from the neonatal epidermis by adding Type 1 collagenase. The culture medium was Dulbecco's Modified Eagle's Media (DMEM).

Fibroblasts were measured by MTT method. As a result, AsA-APPA shows a proliferative effect of fibroblasts to a concentration of 10mM, it can be seen that there is little cytotoxicity.

Test Example 2: Human safety of AsA-APPA

Hereinafter, in order to determine the safety of the human body of AsA-APPA-containing cosmetics of the present invention, it was confirmed that AsA-APPA is a raw material without toxicity and irritation as a cosmetic through the following experiments.

(2-1) Acute oral toxicity test

In 10 ICR mice, each of 5 males and females weighing 20 to 33 g, 10 ml / kg of white pale yellow powder AsA-APPA was diluted in saline at 50% concentration and administered once orally. -10 mg / kg of physiological saline was administered to 10 ICR mice, each of 5 males and females weighing 20 to 33 g, to the control group (AsA-APPA dose: 0 g / kg). On the day of administration, change the general condition every hour up to 6 hours, and observe the change of general condition (clinical symptoms), addiction symptoms, and deaths every day from the next day to 14 days. The weight change was observed. When the animals died during the observation period, they were necropsied immediately, and the animals surviving until the end of the observation period were autopsied after the end of the examination, and the internal organs were visually examined. As a result, no dead animals were observed over the entire test period, and no significant difference was observed in the weight change group compared to the control group. In addition, no abnormality was observed in the autopsy findings in each of the test and control animals. AsA-APPA was LD ₅₀ (Lethal Dose) value over 5 g / kg by Litchfield-Wilcoxon method in acute oral exposure.

(2-2) Acute dermal toxicity test

Ten 10 ICR mice, each weighing 20 to 30 g, were treated with 10 ml of white pale yellow powder, AsA-APPA, 4 ml / kg diluted in saline at 50% concentration and administered once percutaneously (AsA). -APPA dose: 2 g / kg) and 10 ICR mice each of 5 males and females weighing 20 to 30 g were administered 4 ml / kg of saline to the control group (AsA-APPA dose: 0 g / kg) It was. About 24 hours before administration, hair on the back of the skin without any abnormalities was depilated to a size of 1.5 × 1.5 cm 2. It was fixed with non-irritating tape and applied for 24 hours. On the day of dosing, change the general condition every hour up to 6 hours, and observe the change of general condition (clinical symptoms), addiction symptoms, and deaths every day from the next day to 14 days. Weight change was observed. When the animals died during the observation period, they were necropsied immediately, and the animals surviving until the end of the observation period were autopsied after the end of the examination, and the internal organs were visually examined. As a result, no dead animals were observed over the entire test period, and no significant difference was observed in the weight change group compared to the control group. In addition, no abnormality was observed in the autopsy findings in each of the test and control animals. AsA-APPA was more than 2 g / kg LD ₅₀ (Lethal Dose) by Litchfield-Wilcoxon method in acute transdermal exposure.

(2-3) Primary skin irritation test

Twelve New Zealand White male rabbits were used as test and control groups. 24 hours before application of the test substance, the hairs on the back are removed, and about 2.5 cm x 2.5 cm in size, the scalp and two skin and the two skin and skin areas around the spine, the left compartment is the control compartment, the right compartment Silver was used as a test compartment for applying the test substance. The test compartment per animal was coated with 1.0 ml of AsA-APPA (0.5 ml / site) diluted with physiological saline at 50% concentration, and 1.0 ml of physiological saline was applied to the control compartment. After application, the application part was covered with gauze and fixed with a non-irritating tape and applied for 24 hours. After the application period was finished, the application part was lightly washed with physiological saline.

24 hours and 72 hours after application of the test substance, irritation such as erythema, skin formation, and edema formation was observed. As a result of evaluation of skin reaction determined by Korean Food and Drug Safety Notice No. 96-8, "Toxicity Test Standards for Drugs," no edema and crust formation were observed, and the skin primary irritation index PII (Draize The Primary Irritation Index was found to be 0.13 (almost non-irritant).

(2-4) Eye irritation test

Nine New Zealand White species rabbits were used as test and control groups. 0.1 ml of AsA-APPA was diluted with physiological saline at a 10% concentration in the right eye of each rabbit, and three of them were rinsed thoroughly with lukewarm physiological saline after 20-30 seconds, and the other six were not washed. . After application of the test substance, 1, 2, 3, 4, and 7 days after the application of the test substance, the corneal haze and its extent, iris response, conjunctival redness, edema, and the degree of discharge were observed. Evaluation of eye irritation of eye mucosal reactions using grades of ocular lesions in the "Toxicity Testing Standards of Drugs" and the degree of irritation of the results according to the commonly used eye irritation classification table. Afterwards, no adverse reactions were observed, so the mucosal irritation rate (MOI) was 0.0 for washing and 0.0 for no washing.

(2-5) Skin sensitization test

Three male and female guinea pigs (Hartley Albino Guinea Pig) each weighing 300 to 360 g were subjected to Magnuson and Kligman's test methods (Guinea Pig Maximization test). To determine the sample concentration to be used for the induction test (test substance concentration in the light stimulus category) and the challenge test (test substance concentration in the non-irritant category), the concentration of the test substance was changed to 6.25%, 12.5%, At 25.0%, primary stimulation was performed on each of three male and female guinea pigs. Samples of three concentrations for each animal were coated with AsA-APPA 0.5ml / site on each of the two left and right sites (2.5 × 2.5㎝) around the spine, covered with a gauze and fixed with a non-irritating tape for 24 hours. .

Next, intradermal injection was performed in which each male and female was injected with 0.1 mL of a 25% AsA-APPA with a 26gauge 1/2 inch needle.

On the 7th day of intradermal injection, the same area was depilated, followed by pretreatment with 10% SLS solution (based on petrolatium), followed by 0.5 ml / site application of AsA-APPA on the same area, covered with gauze, and well-coated with a non-irritating tape. Fixed and applied for 48 hours. After two weeks of patching, the test substance was applied to the left back of the depilated experimental animals, and on the right side, physiological saline was applied and applied in the same manner. After 24 hours of application, the solution was lightly washed with saline solution. The control group used physiological saline instead of the test substance and the rest of the test procedure was performed in the same manner. As a result, at 24, 48 and 72 hours after patch removal, no skin symptoms such as erythema, edema and crust formation were observed in both the control and test groups, and skin sensitization was based on Kligman's criteria. It was a highly safe substance in the category 1 sensitization category.

(2-6) Human patch test

Thirty healthy women aged 20 to 30 years were tested according to CTFA guidelines (The Cosmetic, Toiletry and Fragrance Association. Inc. Washington, D.C., 20036, 1991). 20 μl of the test substance (10% in Patch base) prepared in the Finn Chamber was added dropwise, washed with 70% ethanol, dried, and fixed on the back of the test site with a micropore tape. . The patch is applied for 24 hours, and after removing the patch, the test areas are marked with a marking pen. After 30 minutes and 24 hours, the skin reaction of each test site is observed and the International Contact Dermatitis Research Group : It was determined according to the regulations of ICDRG). As a result, human skin primary irritation was almost absent and suspicious erythema response was 1%, but all disappeared after 48 hours. Average reactivity (MS) was 0.42.

[Test result]

Test substance % Reactivity, N = 30 24 hours 48 hours Average reactivity AsA-APPA One 0 0.42 Patch base One 0 0.42

*

(2-7) Repeat insult human patch test

Twenty healthy women aged 20 to 30 years were tested according to CTFA guidelines (The Cosmetic, Toiletry and Fragrance Association. Inc. Washington, D.C., 20023, 1991). After wiping the back part of the test site with 70% propyl alcohol and drying, 20 μl of a test substance (10% in patch base) prepared in a pin chamber was added dropwise, and the application site was marked with a marking pan on the upper left. The application was carried out three times for nine times every 24 hours. After the application of the induction period for 3 weeks, the Challenge Insult Patch was performed after about 2 weeks. At this stage, the original test site and the new test site were simultaneously performed, but were observed for 96 hours after the closed patch for 48 hours. The skin reaction of each test site was observed at 24, 48 and 72 hours after patch removal, and was determined according to the regulations of the International Contact Dermatitis Research Group (ICDRG). As a result, the cumulative stimulation by cumulative patch showed no significant stimulus response in the microstimulus range and there was no sensitization. The average responsiveness of the induction period was 0.14 and the average responsiveness of the challenge period was 0.

[Test result]

sample Induction period Average reactivity (%) n = 20 Challenge Period Average reactivity (%) n = 20 1 week 2 weeks 3 weeks 24 hours 48 hours 72 hours AsA-APPA One - - 0.14 - - - 0 Patch base - One - 0.14 - - - 0

The test results of (2-1) to (2-7) are summarized in Table 1 below.

Experienced person result Judgment Acute Oral Toxicity Test LD ₅₀ ＞ 5g / Kg Non-toxic Acute dermal toxicity test LD ₅₀ ＞ 2g / Kg Non-toxic Skin Primary Stimulation Experiment PII = 0.13 Almost irritant Eye mucosal stimulation experiment M.O.I = 0 Irritant Skin sensitization experiment Klingman Rating: Level 1 Weak sensitivity Human patch experiment MS = 0.42 Irritant Cumulative Stimulation Experiment MS = 0.14 Irritant

AsA-APPA was confirmed to be a safe substance as an external preparation for skin in the above toxicity and skin safety experiments.

Test Example 3: Skin Safety

Skin safety was compared with respect to the whitening cosmetics prepared in Examples 1 to 2 and Comparative Examples 1 to 10. About the safety of skin, it carried out according to the normal patch test and evaluated by the following criteria. The results are shown in Table 2.

Judgment criteria +++: Very irritating, not suitable for use in cosmetics

++: It is not recommended to use because of severe irritation

+: Slightly irritating and requires attention

±: almost no stimulus

-: No irritation at all, good for sensitive skin

=: No repeated stimulus results

Example 1 Example 2 Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Comparative Example 5 Comparative Example 6 Comparative Example 7 Comparative Example 8 Comparative Example 9 Comparative Example 10 Judgment ＝ － ＝ － ＝ ± ± ＝ + ± ± －

From Table 2, it can be seen that AsA-APPA-containing cosmetics are not irritating to the skin.

Test Example 4: Whitening effect

In order to test the whitening effect of the cosmetic of the present invention, 10 healthy adults and men and women were set up, and after attaching a piece of 4 holes of a circular hole having a diameter of 1.5 cm to the lower arms of both arms, Philips TL20W / 12UV at a distance of 10 cm The lamp and the TL20W / 09UV lamp were irradiated with ultraviolet rays once a day for 1.5 days each at 1.5 MED, and then the subjects were divided into groups A and B, and cream A (group 1 and comparative examples 1 to 5) was placed in group A. After applying the flexible cosmetics (Example 2 and Comparative Examples 6 to 10) twice a day for 6 weeks, the whitening efficacy was visually determined and the results are shown in Table 3.

Test Product Valid effect experience Slightly effect no effect Example 1 2 2 6 Example 2 One 3 6 Comparative Example 1 - - 10 Comparative Example 2 3 One 6 Comparative Example 3 - One 9 Comparative Example 4 One 3 6 Comparative Example 5 One 2 7 Comparative Example 6 - - 10 Comparative Example 7 One 2 7 Comparative Example 8 - One 9 Comparative Example 9 One One 8 Comparative Example 10 - One 9

As can be seen from Table 3, AsA-APPA-containing cosmetics (Examples 1 and 2) have a lower whitening effect than ascorbic acid-containing cosmetics (Comparative Example 2 and Comparative Example 7), but known substances Compared with the phosphorus magnesium ascorbyl phosphate-containing cosmetics (Comparative Example 4 and Comparative Example 9), it was found that almost similar whitening effect was obtained.

Test Example 5: Water Stability

In order to evaluate the stability in the aqueous solution of the cosmetics of Example 2 and Comparative Example 9, discoloration for each of the temperature of 5 ℃, 25 ℃, 45 ℃ under the same conditions as magnesium acrovil phosphate known to be the most stable to date And whether or not precipitation was observed visually, the results are shown in Table 4.

· Discoloration · Precipitation

0-none 0-none 1-very little 1-very little

2-slightly 2-slightly

3-somewhat (not serious) 3-something (not serious)

4-many changes 4-many changes

Sample name Temperature (℃) 5 days 10 days 15th 30 days discoloration Sedimentation discoloration Sedimentation discoloration Sedimentation discoloration Sedimentation Example 2 5 0 0 0 0 0 0 0 0 25 0 0 0 0 0 0 0 0 45 0 0 One 0 One 0 2 0 Comparative Example 9 5 0 One 0 One 0 2 0 2 25 0 0 0 One One 2 One 2 45 One 0 One One One 2 One 2

AsA-APPA aqueous solution of Table 4 showed little precipitation formation or browning at 5 ° C and 25 ° C, and changed color to pale yellow enough to be visually observed only when stored at 45 ° C for 30 days. It was found that the stability was greatly improved compared to the crowville phosphate.

As described above, by using AsA-APPA as an ascorbic acid derivative used in whitening cosmetics to prevent blemishes and freckles, it has the effect of inhibiting melanin production of ascorbic acid and easily oxidizes ascorbic acid in aqueous solution. It is possible to provide a whitening cosmetic that prevents browning, increases percutaneous absorption, and improves instability and skin safety in the formulation.

Claims (1)

A whitening cosmetic composition comprising ascorbic acid-aminopropanol phosphoric acid diester, a derivative of ascorbic acid, in an amount of 0.005 to 10% by weight, based on the total weight of the composition. Cosmetic composition.