JP2846364B2 - External preparation for preventing rough skin - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Application Field] The present invention relates to an external preparation for preventing rough skin,
More specifically, the present invention relates to an external preparation for effectively preventing skin roughness due to sunburn.

[Conventional technology and its problems]

Kojic acid inhibits the action of tyrosinase present in the skin of the human body and exhibits an excellent inhibitory action on melanin production, and it has been already clarified by long-term studies of the present inventors that kojic acid is an active ingredient. External preparations such as light-skinned cosmetics and ointments have also been proposed (for example,
No. 18569, JP-B-61-1047).

By the way, human skin is adversely affected by excessive ultraviolet irradiation, that is, the skin is damaged by long-term exposure to ultraviolet rays and causes sunburn, erythema is caused, and the skin becomes a state of burn (sunburn), becomes brittle and changes in water bubbles. It leads to a hospital. In addition, the melanin formation of pigment cells is promoted and the skin darkens, and if this state is further repeated,
Collagen fibers in the subcutaneous tissue are destroyed,
Pigmentation such as spots and freckles and aging of the skin are promoted.

It is known that such a wavelength that causes erythema and burns on human skin is a medium-wave light (UVB wavelength range) of about 280 to 320 nm.

Therefore, cosmetics aimed at preventing sunscreen are generally U.S.
A compound that selectively absorbs ultraviolet light having a wavelength in the VB range, and a compound that has a maximum absorption value at 308 nm, which is particularly supposed to cause erythema, such as salicylic acid, paraaminobenzoic acid and its esters, and silica skin derivatives. It is known to incorporate

However, conventionally known sunscreen cosmetics, as described above, mainly prevent sunburn by absorbing ultraviolet rays having a wavelength in the UVB range, but the effect of sunburn prevention is not necessarily sufficient. However, it is not only completely ineffective as an external preparation for effectively preventing erythema and burns due to sunburn, but also has problems such as salicylic acid causing side effects on the skin.

On the other hand, various drugs have been used as external preparations for preventing skin roughness, but no suitable external preparations for preventing erythema and burns due to sunburn have been found yet.

[Object of the invention]

Accordingly, an object of the present invention is to provide an external preparation for preventing skin roughness for effectively preventing skin roughness due to sunburn.

[Means for solving the problem]

The present invention has been proposed to achieve the above-mentioned object, and has as its gist a skin roughness inhibitor containing kojic acid and β-carotene as essential components.

(Description of preferred embodiments of the invention)

An important technical feature of the skin roughness inhibitor of the present invention is that kojic acid and β-carotene are used in combination as essential components.

Kojic acid As previously described, kojic acid is excellent in the melanin production inhibitory action.
As described in detail in Japanese Patent No. 569, it may be used as an active ingredient of fair-skinned cosmetics or as an external preparation such as an ointment as disclosed in JP-B-61-1047. It has been known.

As kojic acid, A pure product of 5-oxy-2-oxymethyl-γ-pyrone represented by, a fermentation solution containing kojic acid as a main component obtained by culturing a strain having a kojic acid-producing ability, a concentrated solution of the fermentation solution,
And a product obtained by extracting kojic acid from the fermentation solution and crystallizing the same.

Examples of such a strain having a kojic acid-producing ability include, for example, Aspergillus albus, Aspergillus candidas, Aspergillus alize, Aspergillus nidulans, Aspergillus parasiteicas, Aspergillus awamori, Aspergillus tamari, Aspergillus newpus, Aspergillus newpus and Aspergillus newpus Strains of the genus Aspergillus, such as Aspergillus wench, Aspergillus glaucus, Aspergillus crubeidas, Aspergillus fumigatus, Aspergillus dicantus, strains of the genus Penicillium such as Penicillium dalay, strains of the genus Escaliciatus such as Escalikia coli. , Acetobacter
Strains of the genus Acetobacter, such as gluconicus and Acetobacter xytinum, and strains of the genus Gluconobacter, such as gluconobacter rosius gluconobacter gurnicus, are preferably used.

The medium composition of these strains is usually sucrose, sucrose, brown sugar, glucose, starch, maltose, glycerin, mannitol, rhamnose, xylose, gluconic acid, arabinose, dihydroxyacetone, inosit, lactose, ethanol, etc. The carbon source is about 2 to 15% (weight%, the same applies hereinafter), the nitrogen source is about 0.1 to 1% such as ammonium sulfate, polypeptone, sodium nitrate, baker's yeast extract, brewer's yeast extract, and the magnesium source such as magnesium sulfate is about 0.01-0.05%, potassium hydrogen phosphate,
Phosphorus and potassium sources such as potassium dihydrogen phosphate are 0.01 to 0.1%,
Other inorganic salts such as ferric sulfate, ferric chloride, sodium chloride, and calcium chloride having about 0.001 to 0.005% can be used.

β-carotene β-carotene is Is a compound having a molecular weight of 537 and a melting point of 183 ° C, and is known as a pigment having a vitamin A effect.

This β-carotene is acne (acne) together with other caroloid-series compounds, for example, α-carotene, γ-carotene, β-carotene-4,4′-dione, β-apo-8′-carotylol and the like. It is disclosed in Japanese Patent Application Laid-Open (JP-A) No. 61-501030 that it can be used as a drug for treating or preventing the disease. However, acne is mainly due to abnormal secretion from the body, especially abnormal gonadal function, which causes male hormones to increase sebaceous gland proliferation and excretion of sebum, while Es
It is a skin abnormality that trogen causes to reduce the sebaceous glands and reduce excretion of the skin, and the development process and state are completely different from skin abnormalities such as erythema and burns caused by sunburn. In the present invention, by using the above β-carotene in combination with kojic acid, a synergistic skin roughness prevention effect is achieved, and even when other carotene is used in combination with kojic acid, an excellent skin roughness prevention effect is obtained. Even when it is seen that no specific combination is used, a specific synergistic effect is observed for a specific combination in the present invention. In addition, the external preparation of the present invention significantly suppresses the color change observed in the preparation of kojic acid over a long period of time, and is excellent in commercial value.

In the present invention, as a cosmetic compound, by using together known kojic acid and β-carotene, while preventing inflammation such as erythema and burns associated with sunburn, which was hitherto unknown at all, It has been found that the composition has an effective pharmacological action as an external preparation for improving inflammation.

Preparation of external preparation The external preparation of the present invention is usually used as an ointment (cream), but it may be used in the form of emulsion, pasta, poultice or lotion.

In any of them, the mixing ratio of kojic acid is 0.01 to 10.0% by weight, preferably 0.1% by weight, based on the whole external preparation.
5 to 5.0% by weight, and the mixing ratio of β-carotene to kojic acid is 0.
01 to 5.0, preferably 0.1 to 1.0.

In preparing the ointment, a hydrophilic component such as glycerin or sorbite, and kojic acid are added to purified water to prepare an aqueous phase. Separately from this, beeswax, paraffin, microcrystalline wax, ceresin, high-grade Β-carotene is added to oil components such as fatty acids, solid oils such as hardened oils, semi-solid oils such as petrolatum, lanolin, and glycerides, liquid oils such as squalane, liquid paraffin, various ester oils, preservatives, and surfactants. To prepare the oil phase. The aqueous phase thus prepared is heated to about 70 to 75 ° C. while gently stirring, and then the oil phase, which has been heated to the same degree, is gradually added to obtain an ointment.

What is important in preparing the external preparation is that when the external preparation is obtained by mixing a previously prepared aqueous phase and an oil phase, kojic acid is added to the aqueous phase and the oil phase is added. That is, β-carotene is added to the part. By adding both components to the aqueous phase and the oil phase in advance,
Even when these are mixed to prepare an external preparation, the active ingredients are integrated without being separated, and a suitable external preparation is formed.

When the external preparation is an emulsion, a humectant such as glycerin, a pH adjuster, etc. are added to the purified water, mixed by heating, and ethanol and kojic acid are added to prepare an aqueous phase. Solid oils such as paraffin, semi-solid oils such as petrolatum and lanolin, liquid oils such as squalane, liquid paraffin, various ester oils, and β with preservatives and surfactants
-Mix carotene and heat mix to prepare oil phase.
Next, the oil phase is added to the aqueous phase for pre-emulsification, and a protective colloid such as carboxyvinyl polymer or carboxymethyl cellulose is added thereto, and the mixture is uniformly emulsified with a homomixer to form an emulsion.

In the case of a poultice, a humectant such as glycerin, a film agent such as polyvinyl alcohol, veegum and the like are added to purified water to swell, and β-carotene, a perfume, an ethanol in which a preservative and the like are dissolved are added to form a paste. Knead until it becomes
As a poultice, kojic acid may be added at any time.

Further, in the case of a lotion, a humectant such as glycerin or propylene glycol is dissolved in alcohol in purified water, and the two are mixed and solubilized at room temperature.
In this case, kojic acid and β-carotene may be added at any time.

Further, also in a lotion, a humectant such as glycerin or propylene glycol is dissolved in alcohol in purified water, and both are mixed and solubilized at room temperature. In this case as well, kojic acid and β-carotene are used in both cases. You may mix at a time.

In the present invention, it is recommended to add an ultraviolet absorber, particularly a medium-wave light absorber, in order to more effectively prevent skin roughness due to sunburn. Examples of such ultraviolet absorbers include oxybenzone and salts thereof, phenyl salicylate, ethyl paraamidobenzoate, homomenthyl salicylate, isopropyl-P-methoxycinnamate, 2-ethoxyethyl-P-methoxycinnamate,
Urocanic acid and salts thereof are exemplified, and 0.1% of the whole external preparation is included.
It is blended at a ratio of about 001 to 10.0% by weight.

〔Example〕

 Hereinafter, the present invention will be described based on examples.

Example 1 (%) A. Cetanol 0.5 Vaseline 2.0 Liquid paraffin 7.0 Self-emulsifying glyceryl monostearate 2.5 Polyoxyethylene sorbitan 1.5 Monostearate (20E.O.) Octyldodecanol 5.0 β-Carotene 0.5 B. Propylene glycol 5.0 Glycerin 5.0 Purified water 100100 g C. Kojic acid 1.0 As described above, a cream was prepared by mixing 1% by weight of kojic acid (KA) and 0.5% by weight of β-carotene in the entire cream, and the replica score of 1, was irradiated by ultraviolet irradiation. The cream was applied 0.3 ± 0.1 to 30 subjects having skin evaluated as 2.
g The composition was applied twice a day, every 12 hours, and the surface state of the skin at the start of application and one week after application was taken as a replica, and the results were observed with a stereoscopic microscope (20 times).

The replica uses a quick-drying silicone-based synthetic rubber on the skin surface, takes a negative replica, and fills it with a polysulfide-based synthetic rubber to take a positive replica (Kumaya et al.,
SCCJ.Vol 19, No.1 (1985) P.9-19).

 Table 1 shows the results.

Example 2 Example 2 was repeated except that the amount of kojic acid (KA) was changed to 0.5% by weight.

Comparative example 1 It carried out like Example 1 except not mix | blending (beta) -carotene.

 Table 1 shows the results.

Comparative Example 2 Example 1 was repeated except that kojic acid was not added and β-carotene was added at 1% by weight.

 Table 1 shows the results.

[Effects of the Invention] According to the present invention, the improvement of damaged skin such as erythema and burns due to sunburn can be extremely effectively achieved by applying an external preparation combining kojic acid and β-carotene.

Claims (1)

(57) [Claims] 1. An external preparation for preventing rough skin, comprising kojic acid and β-carotene as essential components.