JPH03188011A - Cosmetic - Google Patents

Abstract

PURPOSE:To obtain a beautifying agent having excellently beautifying effects, high stability and safety, preventing and improving sunburn, stain and freckle of the skin, containing kojic acid and N,N'-diacetylcystine dimethyl. CONSTITUTION:0.001-5wt.% kojic acid and/or derivative thereof and 0.0001-5wt.% N,N'-diacetylcystine dimethyl are contained as essential components, properly blended with an aqueous component, powder, a surfactant, an oil agent, a humectant, an alcohol, a pH adjuster, an antiseptic, a dyestuff, an antioxidant, a thickening agent, perfume, etc., used in common cosmetics and prepared by a conventional procedure to give the objective substance. The substance can be processed into milky lotion, cream, toilet lotion, pack, ointment, dispersion, granule, cleaning agent, etc.

Description

[Detailed Description of the Invention] [Industrial Application Field] The present invention provides kojic acid and/or its derivatives and N, N'
- A novel cosmetic containing diacetylcystine dimethyl, having an excellent whitening effect, and having high stability and safety.

[Problems to be solved by conventional techniques and inventions] Conventionally,
Whitening cosmetics are widely used to obtain beauty effects such as preventing dark skin, age spots, and freckles, and these whitening cosmetics mainly contain whitening agents such as ascorbic acid, glutathione, and colloidal sulfur. It is blended. However, since ascorbic acid is susceptible to oxidation, it is difficult to expect a certain level of effect to be achieved, and glutathione and colloidal sulfur have the drawbacks of producing a characteristic off-odor and precipitation.

For this reason, there has recently been a wide search for skin-whitening agents from nature, and for example, kojic acid or its derivatives are known to have excellent skin-whitening effects (Japanese Patent Laid-Open No. 53
-18739, JP-A-56-7776, JP-A-56
-79616, JP-A-59-33207, etc.).

However, when these kojic acids or their derivatives are added to cosmetics at high concentrations with the expectation of higher whitening effects,
The stability of the product deteriorated, and it was not sufficiently satisfactory for actual use.

For this reason, there has been a desire for cosmetics that have excellent whitening effects and are highly stable and safe.

[Means to solve the problem]

Under these circumstances, the present inventors have conducted extensive research and have found that the combination of kojic acid and/or its derivatives and N,N'-diacetylcystine dimethyl has a synergistic whitening effect and is stable and safe. They discovered that cosmetics with excellent properties can be obtained and completed the present invention.

That is, the present invention provides a whitening cosmetic containing kojic acid and/or a derivative thereof and N,N'-diacetylcystine dimethyl.

In the present invention, kojic acid or a derivative thereof used as an active ingredient has the following general formula (I) (wherein R1 and R
2 may be the same or different and have a hydrogen atom or a carbon number of 3
~22 acyl group or alkyl group).

Kojic acid may be extracted and purified from fermentation products by microorganisms such as Aspergillus, Penicillium, Acetobacter, etc., or it may be an extract without the purification process, or it may be obtained by synthesis. But that's fine.

Further, as the kojic acid derivative, those synthesized from the above-mentioned kojic acid can be used, and examples of its ester include kojic acid monobutyrate, kojic acid monocaprate, and kojic acid monopalmitate.

Monoesters such as kojic acid monostearate, kojic acid monocinnamate, or kojic acid monobenzoate; diesters such as kojic acid dibutyrate, kojic acid dipalmitate, kojic acid distearate, or kojic acid dioleate, and the like.

These kojic acids and their derivatives can be used alone or in combination of two or more, and o, oooi,
~5% by weight (hereinafter simply expressed as %), especially 0.01~3
．． It is preferable to mix 0%. If it is less than 0.0001%, a sufficient whitening effect cannot be obtained, and if it exceeds 5%, the stability of the product over time often decreases, which is not preferable.

In addition, N,N'-diacetylcystine dimethyl, which is another essential component of the present invention, is represented by the following structural formula: It is known to have activating and whitening effects (Clinical Dermatology 9 (
6) p. 444). In the present invention, this N,
N'-diacetylcystine dimethyl is present at 0.0% in the entire composition.
0001 to 5%, particularly preferably 0.01 to 3.0%. If it is less than 0.0001%, a sufficient whitening effect cannot be obtained, and if it exceeds 5%, the stability of the product decreases, which is not preferable.

Furthermore, in addition to the above-mentioned essential ingredients, the cosmetic of the present invention also includes aqueous ingredients, powders, surfactants, oils, humectants, alcohols, pH! Ill conditioners, preservatives, pigments, antioxidants, thickeners, fragrances, and the like can be added as appropriate.

The cosmetic of the present invention can be produced by blending kojic acid and/or its derivatives, which are essential ingredients, with N,N'-diacetylcystine dimethyl, according to a conventional method.
It can be applied as a cream, lotion, bag, ointment, dispersion, granule, cleansing agent, etc.

〔Example〕

Next, the present invention will be further explained with reference to Examples, but the present invention is not limited to these Examples.

Example 1 A milky lotion having the composition shown in Table 1 was produced and evaluated for whitening effect. The results are shown in Tables 2 and 3.

Margin below <Manufacturing method> A, (6) to (9) and one are heated and mixed and kept at 70°C.

B. Heat and mix (1) to (5), αQ and (11) and maintain at 70°C.

Add C and B to A and mix, then add (support) and mix uniformly, then add 03) to uniformly emulsify, and cool to 30°C to obtain a milky lotion.

Test Example 1 The whitening effect of the test substance was examined by pricking the backs of colored guinea pigs and utilizing the fact that pigmentation occurs when irradiated with ultraviolet rays under anesthesia. For ultraviolet irradiation, FL2O3 manufactured by Toho ■
- Three BLB lamps and three PL2O3/E30 lamps were irradiated at the same time, and the amount of ultraviolet rays was 4.8 x 10'er
g/cm2. 24 hours before UV irradiation, immediately after irradiation, and 24 hours after irradiation, 4 locations on the back of the guinea pig (2X
0.2 cm of samples ■ to ■ were thoroughly rubbed onto a 2 cm). However, before irradiation, the application site was thoroughly washed with warm water. Seven days after irradiation, the degree of pigmentation at each site was observed and judged based on the following criteria. The results are shown in Table 2.

<Evaluation criteria> Pigmentation rating; 0: No pigmentation observed at all.

1: Very slight pigmentation is observed.

2: Pigmentation is observed, but the border with the non-irradiated area is unclear.

3: Pigmentation is observed, and the border with the non-irradiated area is clear.

Whitening effect; 8 or more out of 10 guinea pigs with a pigmentation score of 1 or less: Excellent Effect 6 or more animals: Effective 4 or more animals: Fairly effective 3 or less animals: Ineffective Clear from table 2 in the margins below Table 2 As shown, the emulsion of the present invention containing a combination of kojic acid and N,N'-diacetylcystine dimethyl (sample 2) was compared with sample 2 which did not contain any of these, as well as kojic acid or N,N'-diacetylcystine dimethyl. - Even when compared with samples ① and ①, which contained diacetylcystine dimethyl alone, it showed a remarkable anti-pigmentation effect.

Test Example 2 Usage Effect Test A panel of 15 women between the ages of 23 and 44 were asked to apply an appropriate amount of the emulsions of Samples ■ to ■ to their faces twice a day, once in the morning and once in the evening, after washing their faces for 12 weeks. A test was conducted and evaluated based on the following criteria.

Evaluation criteria: Yes Effective: Bleeding and freckles are no longer noticeable.

Slightly effective. Blends and freckles are now less noticeable.

No effect: No change.

Table 3 It has excellent results and shows a remarkable whitening effect.

Example 2 Lotion: Formula> (1) Glycerin (2) 1,3-butylene glycol (3) Polyoxyethylene solpicum monolaurate (20B, 0.) (%) 5.0 6.5 1.2 (4) Ethyl alcohol 8.0 (6) Roudic acid (7) N, N'-diacetylcystine dimethyl (8) Preservative (9) Fragrance 2.0 0.2 Appropriate amount Appropriate amount As is clear from Table 3, The emulsion of the present invention (sample ■) is
The effect of making spots and freckles less noticeable is found not only when compared with sample ■ which does not contain any of these, but also when compared with samples ■ and ■ which contain only rosic acid or N,N'-diacetylcystine dimethyl.
100.0$1) -Maru Falcos ■Production method> A, (3), (4), (8) and (9) are mixed and dissolved.

B, (1), (2), (5) to (7) and αO are mixed and dissolved.

C, A and B were mixed and made uniform to obtain a lotion.

Example 3 Cream: <Formulation> (1) Beeswax (2) Cethanol (3) Reduced lanolin (4) Squalane (5) Glycerin monostearate (%) 6.0 5.0 5.0 30.0 4.0 (8) Roudic acid (9) N, N'-diacetylcystine dimethyl αQ inositol αD preservative Q21 fragrance 1.0 1.0 0.1 0.3 0.05 Total 100
Production method> Mix A, (1) to (7), 0υ and α-ri, heat and keep at 70°C.

Mix B, (8) to αO and α■, heat and maintain at 70t.

B was added to C and A, mixed, and then cooled to obtain cream.

Example 4 Pack: Prescription> (%) (1)
Polyvinyl alcohol 20.0 (2
) Ethanol 20.0 (
3) Glycerin 5.0 (
4) Kaolin 6,
0 (6) Roudic acid (7) N, N'-diacetylcystine dimethyl (8) Preservative (9) Fragrance Total 00 ◆2] Manufacturing method manufactured by Gatefosse> A, (1), (3) to (7) ) and 0 mouth, mix at 70℃
Heat to and stir.

Mix B, (2), (8) and (9).

B was added to C and A, mixed, and then cooled to obtain 1<tsuku.

Example 5 Cleaning agent: Formula> (%) (1)
Stearic acid 10.0 (2
) Palmitic acid 8.0 (3)
Myristic acid 12.0 (4
) Lauric acid 4,0 (
5) Oleyl alcohol 1.5 (
6) Purified lanolin 1.0 (
7) Fragrance 0.1 (
8) Preservative 0.2 (9
) Glycerin 18.000
Potassium hydroxide 6.000 Kojic acid 0.20ZN
, N'-diacetylcystine dimethyl
0.1 Manufacturing method> Mix A, (9), α1 and α, and heat to 70°C.

Mix B, (1) to (6) and (8) and heat to 70°C.

B was added to C18 and kept at 70°C for a while, and after the saponification reaction was completed, it was cooled to 50°C, and (7), 0υ and (Corporate) were added and cooled to obtain a cleaning agent.

〔Effect of the invention〕

As detailed above, the cosmetic of the present invention has an excellent whitening effect and is therefore effective in preventing and improving skin darkening caused by sunburn, age spots, and freckles.

Furthermore, the cosmetic composition of the present invention is stable and safe, so it can be used with confidence.

that's all

Claims (1)

[Claims] 1. A whitening cosmetic containing kojic acid and/or its derivatives and N,N'-diacetylcystine dimethyl.