JPH06256152A - Skin cosmetic - Google Patents

Abstract

PURPOSE:To provide a novel skin cosmetic capable of effectively preventing the blacking of skins and excellent also on the point of safety. CONSTITUTION:A skin cosmetic contains glabridin and an active oxygen- eliminating agent and prevents the generation of inflammations and the production and deposition of skin melanin caused by external irritations such as UV rays due to the synergistic action of the essential ingredients.

Description

Detailed Description of the Invention

[0001]

INDUSTRIAL APPLICABILITY The present invention can suppress inflammation caused by external stimuli such as ultraviolet rays and the production or deposition of skin melanin, and prevent erythema (sunburn), skin blackening, spots, freckles and the like. It relates to skin cosmetics.

[0002]

2. Description of the Related Art In the final stage of the process of darkening the skin color, tyrosine, which is one of the amino acids, produces the black pigment melanin by the action of tyrosinase. Therefore, it has been conventionally attempted to prevent pigment deposition by applying various agents having an action of inhibiting the action of tyrosinase, such as glutathione, vitamin C or its derivatives, to the skin. However, these drugs are not always satisfactory in terms of stability and effectiveness in topical application.

In addition to tyrosinase, this is a cause and trigger of melanin production, for example, activation of melanocytes by ultraviolet rays, involvement of various chemical mediators due to inflammation, involvement of active oxygen species produced by ultraviolet rays, and sebum. This is because it has been difficult to sufficiently prevent the deposition of melanin even by applying a drug that merely inhibits the action of tyrosinase, as reported by the involvement of peroxides and the like.

[0004]

DISCLOSURE OF THE INVENTION The object of the present invention is to effectively prevent skin blackening, which is associated with many factors as described above, and is also excellent in safety. To provide new skin cosmetics.

[0005]

The skin cosmetic according to the present invention is characterized in that it contains glabridin and an active oxygen scavenger as essential active ingredients, and the synergistic action of these essential ingredients causes external stimuli such as ultraviolet rays. It suppresses inflammation and skin melanin production and deposition. Glabridin, which is one of the active ingredients constituting the skin cosmetic of the present invention, is a compound having a structural formula of the following chemical formula 1, and is naturally a kind of licorice, Glycyrrhizaglabra Linne var.
It is contained in a very small amount (commonly known as Russia, Afghan and Turkish liquorice).

[0006]

[Chemical 1]

It has been confirmed that glabridin has a pharmacological action such as an antibacterial action, an antioxidative action, an anticarious action and an antiplasmin action, and is also known to have a melanin production inhibiting action (special feature). Kaihei 1-311
011). However, the previously confirmed melanin production-inhibitory action of glabridine is only when glabridine is used alone, and the effect of using it in combination with an active oxygen scavenger and other physiologically active substances has not been known.

When glabridin is extracted from licorice to be used as a raw material for producing cosmetics of the present invention, first, the root portion of licorice or its water extraction residue (for example, the residue obtained by extracting glycyrrhizin) is extracted with an organic solvent. As the extraction solvent, lower aliphatic alcohols such as methanol and ethanol; lower aliphatic ketones such as acetone; ethers such as dioxane and ethyl ether; halogenated hydrocarbons such as methylene chloride and chloroform; ethyl acetate, propyl acetate, etc. Esters such as butyl acetate; hydrocarbons such as hexane and benzene; and mixtures of two or more of these organic solvents can be used. The licorice to be extracted is immersed in about 5 to 15 times the amount of the above solvent, and allowed to stand at room temperature or heated under reflux. The extract obtained by distilling off the solvent from the extract usually contains about 5 to 10% of glabridin and can be used as it is in the cosmetic of the present invention, but it was purified to improve its purity. By using the ones, it is possible to obtain a cosmetic material which is more excellent in use effect and less colored.

Purification of the extract can be carried out by, for example, a method in which normal phase silica gel chromatography and reverse phase chromatography are carried out, followed by crystallization from acetone. According to this method, pure glabridin is relatively easily prepared. Can be obtained. In addition, the purification can be performed by employing any organic compound purification means such as column chromatography using a synthetic adsorbent or liquid-liquid countercurrent extraction.

Preferred specific examples of the active oxygen scavenger contained in the skin cosmetic of the present invention together with glabridin include:
Superoxide dismutase, catalase, β-
Carotene, baicalin, baicalein, melissa extract, nephew extract, sage extract, rosemary extract, eleuterococcus extract, ginkgo extract, clove extract, kujin extract, hamamelis extract, sowakuhi extract, basil extract , Panax ginseng extract,
There are enzymes such as Touki extract, Senkyu extract and the like, active oxygen scavenging enzymes, and plant extracts.

Two or more of these active oxygen scavengers may be contained in the cosmetic of the present invention. In the skin, active oxygen is generated when it receives ultraviolet rays in the presence of oxygen.
The generated active oxygen is normally erased by enzymes such as superoxide dismutase and catalase in the body, but the active oxygen is not completely erased in the skin whose function is deteriorated due to aging, damage, etc. Causes denaturation of collagen, decomposition of hyaluronic acid, and peroxidation of lipids. Thereby, the skin further deteriorates.
In addition, lipid peroxide generated by active oxygen causes an increase in inflammatory factors and induces a melanin production system due to inflammation. Furthermore, it is known that some reactive oxygen species directly participate in the melanogenesis cycle generated from tyrosine and promote melanogenesis. The active oxygen scavengers used in the present invention are known to prevent the above-mentioned undesired biological reactions caused by active oxygen, and this action acts synergistically with the action of glabridin to maintain favorable skin. -Helps to form and also prevents blackening of the skin.

The preferred amount of glabridin in the skin cosmetic of the present invention varies depending on the kind of the cosmetic, but it is usually about 0.001 to 10% by weight, particularly preferably about 0.01 to 1.0% by weight. %. Further, the preferable blending amount of the active oxygen scavenger is about 0.01 to 10% by weight, particularly preferably about 0.05 to 5% by weight, and further about 10 to 2000% by weight with respect to glabridin. It is desirable to mix them as follows.

The cosmetic of the present invention is any cosmetic that can advantageously utilize the melanin production inhibitory action by the combined use of glabridin and an active oxygen scavenger, such as lotion, emulsion, cream, pack, soap, body shampoo. And the like. Cosmetic ingredients other than glabridine and active oxygen scavengers, such as oils and fats, surfactants, thickeners, pigments, fragrances, preservatives, ethanol, polyhydric alcohols, etc., are essential depending on the type of the cosmetic. It can be arbitrarily selected within a range not impairing the action of the two components.

[0014]

【Example】

[Preparation example of glabridin] 500 g of licorice root shredded pieces were immersed in 5 liters of ethyl acetate and heated under reflux for 2 hours to extract ethyl acetate-soluble components. The same operation was repeated for the extraction residue obtained by separating the extract, and a total of 9 liters of extract was obtained. The solvent of the extract was distilled off under reduced pressure to obtain 13.1 g of an extract containing glabridin. Next, the extract was dissolved in chloroform, sprinkled on silica gel (Wakogel C-300, product of Wako Pure Chemical Industries, Ltd.), and then dried. The dried product was stacked and packed on a column previously packed with 1 kg of silica gel and eluted with a chloroform / methanol mixture (30: 1) to collect a glabridin-containing fraction. The solvent of this fraction was distilled off under reduced pressure to obtain 5.8 g of a solid substance, which was then dissolved in a small amount of methanol, sprinkled with reverse phase silica gel (ODSG-3, product of Mito Chemical Research Laboratory) and dried. , And stacked and packed on a column previously packed with 800 g of reverse phase silica gel. A water-acetonitrile mixture (30:70) was passed through this column as an elution solvent, and a glabridin-containing fraction was collected. The solvent was distilled off from this fraction under reduced pressure, the obtained solid substance (4.3 g) was dissolved in 40 ml of acetone, and the mixture was allowed to stand at 5 ° C. for 3 days to obtain 3.8 g of crystals of glabridin. In each of the following examples, crystals of the above purified glabridin were used as glabridin.

Example 1 A lotion was prepared according to the formulation shown in Table 1. In this case, the glabridin crystals according to the above-mentioned production example are first dissolved in an ethanol / 1,3-butylene glycol mixed solution, and a surfactant (polyoxysorbitan monolaurate; 20E.
O.), perfume and para-oxybenzoic acid ester were added and dissolved, then purified water and other components were added and stirred to homogenize. In addition, 3 used as an active oxygen scavenger
50 kinds of plant extracts are used for the coarsely crushed raw materials.
An extract obtained by adding a wt% ethanol aqueous solution, allowing the mixture to stand at room temperature for 7 days with occasional stirring, and then clarified by filtration.

[0016]

[Table 1] Lotion formulation (unit:% by weight) Note 1: Prescription 4 is a comparative example

Next, the use effect of each of the above lotions was tested by the following method. Test method for erythema suppressing effect: The back of a brown guinea pig was shaved, a 0.1% solution of oxsoralen was applied thereto, and after 30 minutes, UVA 1 J / cm ² was irradiated. Immediately after the irradiation, 5 sections with a size of 2 cm × 2 cm are determined for each irradiation site, and in each section, A: the above lotion as it is B: lotion without glabridin from the above formulations 1 to 3 C: the above lotion formulation Toner lotion from which active oxygen scavenger is removed from 1 to 3 D: Toner lotion from which both glabridin and active oxygen scavenger are removed from formulations 1 to 3 E: Apply one of the lotions of formulation 4 After 24 hours, the erythema-suppressing effect was determined by visual observation (using the color of the skin not treated with PUVA as the reference color).

Pigmentation-inhibiting effect test method: According to the erythema-inhibiting effect test method, a brown guinea pig treated with PUVA was prepared.
After 1 week, the area where pigmentation was observed was divided into 5 sections of 2 cm x 2 cm, and one of the above-mentioned lotions A to E was applied to each section once every morning and evening for 10 consecutive days. After 10 days, the effect of suppressing pigmentation was judged by visual observation (PU
The standard color is the color of the skin that is not VA-treated).

The results are shown in Tables 2 and 3. The lotion of the present invention containing both glabridine and an active oxygen scavenger is a lotion (D) containing neither glabridin nor an active oxygen scavenger or a comparative example lotion of Formulation 4 using magnesium ascorbate phosphate. It can be seen that the effect of suppressing erythema due to ultraviolet rays and the effect of suppressing pigmentation are remarkably superior to those of (E). Further, it can be seen that the lotion of the present invention shows an excellent use effect even when compared with the application examples (B, C) of lotion containing only one of glabridin and the active oxygen scavenger. No inflammation or other skin disorders were observed.

[0020]

[Table 2] Cosmetic lotion basic formulation Erythema suppressing effect Formulation 1 PUVA-untreated skin ≧ A >> C = B >> D = E Formulation 2 PUVA-untreated skin = A >> C ≧ B >> D = E Formulation 3 PUVA-untreated skin ≧ A >> C ≧ B >> D = E

[0021]

[Table 3] Basic lotion formulation Pigmentation suppression effect Formulation 1 Skin not treated with PUVA = A >>C>B>E> D Formulation 2 Skin not treated with PUVA = A >>C>E>B> D Formulation 3 Skin not treated with PUVA = A >>C>E>B> D

Example 2 A cream was produced according to the formulation shown in Table 4. At the time of production, the raw materials in the same table group were first melted at 70 ° C., mixed with the raw materials, and then heated to 78 ° C. Next, this was gradually added to the raw material heated to 75 ° C. with stirring to carry out preliminary emulsification. After that, apply a homogenizer to completely emulsify,
After cooling to 50 ° C, was added and cooled to 30 ° C. In addition, the prescription 8 is a comparative example.

[0023]

[Table 4] Cream prescription (unit:% by weight)

(Note 1) Surfactant A: self-emulsifying glycerin monostearate Surfactant B: sorbitan monostearate carboxyvinyl polymer: 1% aqueous solution

Next, each of the above creams was tested for its use effect by the following method. Pigmentation suppression effect test method: The back of a brown guinea pig was depilated, and the depilated site was divided into 4 sections of 2 cm x 2 cm, which were irradiated with UVB at 1 J / cm ² for 2 days. Four
Since pigment deposition was observed after a day, A: the above cream as it was in each compartment B: cream excluding glabridin from the above cream formulation C: cream excluding the active oxygen scavenger from the above cream formulation D: formulation Apply one of the 7 creams once a day for 10 consecutive days,
After a day, the effect of suppressing pigmentation was judged by visual observation (U
The standard color is the color of the skin that is not VB treated).

Erythema inhibitory effect test method: According to the pigmentation inhibitory effect test method, the above-mentioned creams A to D were applied to each compartment on the back of the UVB-treated brown guinea pig, and after 24 hours, the effect of suppressing erythema. Was judged by visual observation (UV
B: The color of the skin not treated is the standard color).

The results are shown in Tables 5 and 6. Comparing the case of applying the cream of the present invention containing glaburidine and the active oxygen scavenger with the application example of the cream excluding glabridine or the active oxygen scavenger, the former is either the erythema suppressing effect and the pigmentation suppressing effect by ultraviolet rays. Was also found to be superior to the latter. In addition, no inflammation or other skin disorders were observed.

[0028]

[Table 5] Cream basic formulation Pigmentation suppressing effect Formulation 5 UVB-untreated skin = A >>C>B> D Formulation 6 UVB-untreated skin ≧ A >>C>B> D Formulation 7 UVB-untreated skin ≧ A >>C>B> D

[0029]

[Table 6] Cream basic formulation Erythema suppressing effect Formulation 5 UVB-untreated skin ≧ A >> C ≧ B >> D Formulation 6 UVB-untreated skin ≧ A >> C ≧ B >> D Formulation 7 UVB-untreated skin ≧ A >> C ≧ B ≫ D

[0030]

Industrial Applicability As described above, the cosmetic of the present invention containing glabridin and an active oxygen scavenger can effectively prevent skin inflammation and pigmentation due to ultraviolet rays, and no undesirable side effects are observed. .

Claims (1)

[Claims] 1. A skin cosmetic, which comprises glabridin and an active oxygen scavenger as essential components.