JPH06312920A - Skin-beautifying agent and skin cosmetic containing the agent - Google Patents

Abstract

PURPOSE:To provide a skin-beautifying agent and skin cosmetic containing phosphoramidon having peptidase inhibiting action as an essential component, having beautifying effect on the skin after ultraviolet irradiation and effective for preventing and treating spots and freckles caused by sunburn, etc. CONSTITUTION:The objective skin-beautifying agent and skin cosmetic are composed of phosphoramidon expressed by formula. Phosphoramidon of formula exhibits excellent effect for preventing and ameliorating pigmentation and has high safety. The skin cosmetic can be used in the form of cream, milky lotion, face lotion, foundation, pack, lotion, gel, solution, stick, etc. Commercially available phosphoramidon can be used for the purpose and the content of phosphoramidon in the skin cosmetic is preferably 0.0001-5%. The skin cosmetic may be properly incorporated, in addition to the phosphoramidon used as an essential component, with lubricant, humectant, thickener, antiseptic, emulsifier, pigment, powder, pH-modifier, drug active component, ultraviolet absorbent, antioxidant, flavor, etc.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a whitening agent and a skin cosmetic, and more particularly to a skin cosmetic having an excellent whitening effect on the skin after ultraviolet irradiation and capable of preventing and treating spots and freckles caused by sunburn. Regarding fees.

[0002]

2. Description of the Related Art Pigments, freckles, and pigmentation on the skin after sunburn are less likely to occur, increase, or disappear with age, which is a problem for middle-aged and older people. Although the pathogenic mechanism of these pigmentation diseases has not been clarified yet,
It is considered that the mechanism of melanin synthesis in epidermal melanocytes was enhanced by the action of sunlight, especially ultraviolet rays, and melanocyte-stimulating hormone. Moreover, it is considered that the delay in keratinization of epidermal keratinocytes (keratinocytes) with aging also causes an increase in the density of melanin granules in the epidermis, that is, a clinically symptomatic increase in pigmentation. These pigmented areas are localized and may be distinctly different from the surrounding normal skin color.

There is a strong demand for the development of a drug capable of recovering such an acquired pigment (ie, melanin) deposit to a normal skin color, and many drugs have been commercialized so far. For example, in recent years, vitamin C has an excellent reducing ability.
Cosmetics containing a (L-ascorbic acid) derivative have also been used. However, this also has a difficulty in stability, and almost no effect is observed for external use. On the other hand, in Europe and America, it is known that hydroquinone has a therapeutic effect on spots and an effect to whiten black skin, but these also have problems in safety of the substance itself (irritation, allergenicity), and Compounding as a drug is problematic in that it may cause vitiligo in some cases. In addition, various components such as isoflavone derivatives (Japanese Patent Laid-Open No. 58-58
225004) and p-hydroxycinnamic acid derivatives as cinnamic acid derivatives (JP-A-59-196813) are known as melanin inhibitors.

[0004]

However, at present, no substance is known that has a sufficient pigmentation preventing / ameliorating effect and compoundability with a cosmetic base. Therefore, an object of the present invention is to provide a component having an excellent whitening effect and useful as a cosmetic, and a skin cosmetic containing the same.

[0005]

The inventors of the present invention have conducted intensive studies to obtain a substance that reduces or eliminates pigmentation due to external stimuli such as ultraviolet rays through the study of the mechanism of melanin production. As a result, phosphoramidon was superior. It has been found that it has an effect of preventing and improving pigmentation, and that good skin cosmetics can be obtained by blending this, and completed the present invention.

That is, the present invention uses the formula (1)

[0007]

[Chemical 2]

A whitening agent comprising phosphoramidon represented by:

The present invention also provides a skin cosmetic containing the above phosphoramidon.

The phosphoramidon used in the present invention is A
ctinomyces and Streptomyces
Tanashiensis MD706-Y4 is known to have a peptidase inhibitory action [Umezawa, S. et al. Tatsuta, K .; ，
Izawa, O .; , Tsuchiya, T .; , & Um
ezawa, H .; Tetrahedron Lette
rs (1972) 1, 97-100, Suda, H .; ，
Aoyagi, T .; Takeuchi, T .; , Ume
zawa, H .; The Journal of Ant
ibiotics (1973) 26, 621-623]
However, nothing is known about the action of the compound on the skin. Such phosphoramidon can be produced according to the above-mentioned document, but commercially available reagents (such as those manufactured by Sigma) can also be used.

Such phosphoramidon is preferably blended in the skin cosmetic of the present invention in an amount of 0.00001 to 10% by weight (hereinafter simply referred to as%), particularly 0.0001 to 5%.

In addition to the above essential ingredients, the skin cosmetic of the present invention also contains various optional ingredients used in ordinary cosmetics, quasi drugs, pharmaceuticals, etc., such as oils, moisturizers, thickeners and antiseptics. Agents, emulsifiers, pigments, powders, pH adjusters, medicinal components, ultraviolet absorbers, antioxidants, fragrances and the like can be appropriately added.

Specific examples of the oil agent include liquid paraffin, petrolatum, paraffin wax, squalane, beeswax, carnauba wax, olive oil, lanolin, higher alcohols, fatty acids, synthetic ester oils of higher alcohols and fatty acids, silicone oils, and the like. Examples of moisturizers include sorbitol, xylitol, glycerin, maltitol, propylene glycol, sodium pyrrolidonecarboxylate, polyoxypropylene fatty acid ester, polyethylene glycol, and the like, and thickeners include carboxyvinyl polymer, carboxymethylcellulose, polyvinyl alcohol, carrageenan. , Water-soluble polymers such as gelatin, and electrolytes such as sodium chloride and potassium chloride. Preservatives include methylparaben, ethylparaben, propylpa Ben, butyl paraben, sodium benzoate and the like can be mentioned. As the emulsifier, polyoxyethylene alkyl ether, polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, polyoxyethylene glycerin fatty acid ester. , Nonionic surfactants such as polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitol fatty acid ester, etc., powders such as talc, sericite, mica, kaolin, silica, bentonite, vermiculite, zinc white, mica, mica. Examples include titanium, titanium oxide, magnesium oxide, zirconium oxide, barium sulfate, red iron oxide, iron oxide, ultramarine blue, and the like, and examples of pH adjusters include buffering agents such as citric acid-sodium citrate. Examples of the medicinal component include arbutin, kojic acid, vitamin C and its derivatives, placenta extract, dipotassium glycyrrhizinate, allantoin, vitamin E derivative, pantethenic acid derivative, yoquinin, and various plant extracts.

The skin cosmetic of the present invention can be manufactured by a conventional method. Further, the skin cosmetics to be the subject of the present invention are not limited to general skin cosmetics, but include quasi drugs, external medicines, and the like, and their dosage forms are creams, emulsions, and lotions. , Foundation, pack,
A lotion form, a gel form, a solution form, a stick form, etc. can be arbitrarily selected according to the purpose.

[0015]

[Action and effect of the invention] Phosphoramidon has the action of extinguishing pigmentation generated by stimulation with ultraviolet rays,
A cosmetic containing this has an excellent whitening effect, an effect of preventing and treating spots and freckles due to sunburn and the like, and is highly safe.

[0016]

EXAMPLES The present invention will be described in more detail below with reference to examples, but the present invention is not limited thereto.

Example 1 (Extinction Effect on UVB Pigment Spots) After carefully shaving the back hair of 20 brown guinea pigs with a hair clipper and a shaver, UV rays in the UVB region were applied twice as much as the minimum erythema dose (MED). Irradiation was performed once a day for 3 days, and the amount of pigment spot elimination was examined by continuously applying the evaluation test to the test site twice a day for one month for the induced pigment spots. Phosphoramidon (Sigma) 1% as a sample
The contained 80% ethanol solution was used, and only 80% ethanol was used as a control. Evaluation was measured by a color difference meter, obtained were calculated L ^* value from Munsell values, from the sample application site [Delta] L ^* (aging) samples uncoated (solvent only = control) site of [Delta] L ^* (aging ) Was subtracted (ΔΔL ^* ). In addition,
ΔΔL ^* is expressed by the following formula. ΔΔL ^* = (L ^* _1- L ^* ₀ )-(L ' ^* _1- L' ^* ₀ ) L ^* ₀ ; sample-applied test site before application L ' ^* ₀ ; sample-unapplied test site before application L ^* ₁ ; Sample-applied test site after 1 month of continuous application L ' ^* ₁ ; Sample-unapplied test site after 1 month of continuous application The evaluation was shown by the average value of the evaluation points of 20 test animals.

[0018]

[Table 1]

As a result, as shown in Table 2, the composition containing phosphoramidon was found to have a clear effect of eliminating pigment spots as compared with the control.

[0020]

[Table 2]

[0021]

Table 2 Example 2 (Cream) (Composition) (%) (1) Glycerin monostearate 5.0 (2) Polyethylene glycol monostearate 2.0 (3) Squalane 8.0 (4) Stearyl alcohol 5 0.0 (5) Glyceryl trioctanoate 8.0 (6) Dimethylpolysiloxane (50cs) 0.5 (7) Glycerin 5.0 (8) Citric acid 0.5 (9) Sodium citrate 0.5 (10) Phosphoramidon 1.0 (11) 6-amino-n-caproic acid 0.5 (12) Purified water Remaining amount (13) Preservative proper amount (14) Perfume proper amount

[0022]

Table 3 Example 3 (Essence) (Composition) (%) (1) 1,3-butylene glycol 8.0 (2) glycerin 4.0 (3) xanthan gum 0.3 (4) sodium chondroitin sulfate 0. 1 (5) Sodium hyaluronate 0.1 (6) Ethanol 3.0 (7) Polyoxyethylene polyoxypropylene decyl tetradecyl ether 0.5 (8) Phosphoramidon 0.01 (9) Glycine 0.5 (10) Purified water Remaining amount (11) Preservative Suitable amount (12) Perfume Suitable amount

[0023]

Table 4 Example 4 (Emulsion) (Composition) (%) (1) Polyoxyethylene sorbitan tristearate 1.0 (2) Glyceryl oleate 1.0 (3) Glyceryl monostearate 0.5 (4 ) Squalane 6.0 (5) Glyceryl trioctanoate 2.0 (6) Cetyl octanoate 2.0 (7) Stearyl alcohol 2.0 (8) Octyl methoxycinnamate 2.0 (9) 1,3-butylene Glycol 5.0 (10) Glycerin 3.0 (11) Phosphoramidon 0.5 (12) Nicotinic acid amide 1.0 (13) Purified water remaining amount (14) Preservative proper amount (15) Perfume proper amount

[0024]

Table 6 Example 5 (lotion) (composition) (%) (1) 1,3-butylene glycol 6.0 (2) glycerin 4.0 (3) sodium hyaluronate 0.1 (4) ethanol 5 0.0 (5) Polyoxyethylene-oleyl ether (20 EO) 0.3 (6) Disodium edetate 0.1 (7) Sodium citrate 1.0 (8) Phosphoramidon 0.5 (9) Chloride Ammonium 0.5 (10) L-ascorbic acid phosphate magnesium 3.0 (11) Purified water residual amount (12) Preservative appropriate amount (13) Perfume appropriate amount

[0025]

Table 7 Example 6 (Cream foundation) (Composition) (%) (1) Dimethylpolysiloxane (6cs) 10.0 (2) Methylphenylpolysiloxane 3.0 (3) Octamethylcyclotetrasiloxane 10. 0 (4) polyoxyalkylene-modified silicone 5.0 (5) titanium oxide 5.0 (6) sericite 2.0 (7) talc 3.0 (8) red iron oxide 0.4 (9) iron oxide yellow 7 (10) Iron oxide black 0.1 (11) Glycerin 5.0 (12) Phosphoramidon 0.25 (13) 6-Amino-n-caproic acid 0.5 (14) Purified water Residual amount (15) Preservative Appropriate amount (16) Perfume Appropriate amount

[0026]

Table 8 Example 7 (pack) (composition) (%) (1) dipropylene glycol 3.0 (2) polyethylene glycol 3.0 (3) 1,3-butylene glycol 1.0 (4) glycerin 2 0.0 (5) Sodium pyrrolidonecarboxylate 1.0 (6) Phosphoramidon 0.2 (7) Lactic acid 0.5 (8) Sodium lactate 0.5 (9) Polyvinyl alcohol 12.0 (10) Ethanol 3.0 ( 11) Polyoxyethylene polyoxypropylene decyl tetradecyl ether 0.3 (12) Purified water remaining amount (13) Preservative proper amount (14) Perfume proper amount

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁵ Identification number Internal reference number FI Technical indication location A61K 31/70 ADS 8314-4C (72) Inventor Genji Imogawa 1022-89 Himurocho, Utsunomiya City, Tochigi Prefecture

Claims (2)

[Claims] 1. The following formula (1): A whitening agent consisting of phosphoramidon. 2. A skin cosmetic containing the phosphoramidon according to claim 1.