JPH101438A - External preparation for skin - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a preparation for external use for skin, comprising an extract of a specific myrsinaceous plant or 1,4-benzoquinones contained in the extract as an active ingredient and having preventing effects on aging, antiinflammatory and beautifying and whitening effects together. SOLUTION: This preparation for external use comprises an extract of Ardisia japonica Blume, Ardisia quinquegona Blume and Ardisia sieboldi Miq. or 1,4-benzoquinones contained in the extract as an active ingredient. The blending concentration of the extract in the preparation for external use is about 0.1-1μM expressed in terms of the 1,4-benzoquinones and about 0.001-10wt.% in a state of a crude extract of the plant. The active ingredient has good scavenging actions on active oxygen species and further antiinflammatory actions based on inhibiting actions on 5-lipoxygenases and beautifying and whitening actions based on inhibiting actions, etc., on tyrosinases. The preparation is effective in reducing and preventing aging diseases of the skin mainly caused by oxidative stress, dermatitis, pigmentation such as dermal stains, ephelides or nevus Ota, blackening, etc., due to sunburn.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an external preparation for skin having an anti-aging effect, an anti-inflammatory effect and a whitening effect. More specifically, the present invention relates to an external preparation for skin comprising an extract of a specific Aspergillus or a 1,4-benzoquinone contained in the extract.

[0002]

2. Description of the Related Art Skin is exposed to various stresses existing in the environment, such as heat, ultraviolet rays, and various chemical substances. As a result, inflammatory reactions such as erythema and edema, allergic reactions, and blackening due to melanin production occur on the skin. As a result of being subjected to the stress for a long period of time, wrinkles and wrinkles of the skin occur, and elasticity decreases. It has been revealed that such aging symptoms progress.

[0003] Therefore, active ingredients that prevent the above-mentioned inflammation and the like and prevent darkening and aging of the skin have been sought, and attempts have been made to provide external skin preparations containing them. For example, anti-inflammatory agents include β-glycyrrhetinic acid, glycyrrhizic acid, salts and derivatives thereof, allantoin and its derivatives, azulene, ε-aminocaproic acid, hydrocortisone, and the like. Antihistamines such as phenylamine are used, and as whitening agents, ascorbic acid and its derivatives, kojic acid and its derivatives, hydroquinone derivatives such as arbutin and the like are used.
In recent years, aging of skin due to oxidative stress has been highlighted, and elimination agents for active oxygen species such as vitamin E and superoxide dismutase have been added.

[0004] However, many of the above-mentioned components which have been conventionally used are unstable to light and heat, etc., and their actions and effects are insufficient. In order to obtain, it was necessary to blend a considerably large amount.
Furthermore, there are few components that can exhibit all effects together with anti-aging, anti-inflammatory, and whitening. To achieve these effects evenly, it is necessary to use various types of components in combination, and depending on the components used in combination, In some cases, the stability and action of each may be reduced.

[0005]

SUMMARY OF THE INVENTION The present invention has been made to solve the above-mentioned problems, and has only the effects of anti-aging, anti-inflammatory and whitening by containing only a small amount and a small number of active ingredients. Another object of the present invention is to provide an external preparation for skin that is excellent in stability and safety.

[0006]

Various studies have been carried out to solve the above-mentioned problems. As a result, it has been found that an extract of a specific plant belonging to the family Astragalus has a combination of an anti-aging effect, an anti-inflammatory effect and a whitening effect. By including the extract in a skin external preparation, good results were obtained, and the present invention was completed.

[0007] Among plants belonging to the family Astridaceae, it is known that extracts such as roots of Manryou ( Ardisia crenata Sims) have both a whitening effect and an anti-inflammatory effect (JP-A-4-346912). the study of, Ardisia japonica (Ardisia japonica Blume), Shishiakuchi (a.
quinquegona Blume) and mokutachibana ( A. siebold)
i Miq.) extract has excellent skin anti-aging, anti-inflammatory and whitening effects.

Namely, in the present invention, Ardisia japonica (Ardisia japonica Blume), Shishiakuchi (A. Quinque
gona Blume) and mokutachibana ( A. sieboldi Miq.)
One or two or more types are selected from each of the above extracts to be contained in the external preparation base. As the site used for extracting the plant, any site such as leaf, bark, flower, fruit, root, rhizome, etc. may be used, but leaves are particularly preferable. Each of these parts may be cut into raw pieces and subjected to extraction, but it is most preferable to dry, pulverize and extract as a powder in terms of extraction efficiency.

As an extraction solvent, in addition to water, methanol,
One or more alcohols such as ethanol, propanol, isopropanol, 1,3-butylene glycol, and propylene glycol, and highly polar organic solvents such as ethyl acetate and acetone can be used. Is most preferred.

The extract can be added to the external preparation base as it is, but it can be diluted with a solvent such as water or alcohol,
It can also be added after treatment such as decolorization and deodorization. Furthermore, the method of Fukuyama et al. (Chem. Pharm.
Bull. 43 (8) 1391-1394 (1995)) or the like, and may be contained as a fraction having a higher concentration of the active ingredient. In particular, when 1,4-benzoquinones fractionated by the above-mentioned purification operation are contained, they have extremely high activity, so that a sufficient effect can be exerted at a low concentration.

In the present invention, in addition to extracts such as Aspergillus oryzae or 1,4-benzoquinones isolated therefrom, other active oxygen species scavengers, anti-inflammatory agents, whitening agents, etc.
General external preparations such as oils, humectants, ultraviolet absorbers, fragrances, preservatives, and raw materials for cosmetics can also be contained.

[0012]

The extracts of Aspergillus oryzae and the like, and the 1,4-benzoquinones isolated therefrom, have good elimination of reactive oxygen species and, in addition, 5-lipoxygenase inhibitory activity. It has an anti-inflammatory action based on tyrosinase and a whitening action by tyrosinase inhibitory action and the like. Therefore, the external preparation for skin according to the present invention is useful for improving and preventing aging symptoms of the skin mainly due to oxidative stress, treating and preventing inflammation in the skin, and pigmentation diseases such as spots, freckles, and nevus of Ota. In the improvement and prevention of blackening due to sunburn and sunburn, it has excellent action and effects.

An effective effect is recognized when the compounding concentration in the external preparation is about 0.1 to 1 μM in terms of 1,4-benzoquinone. Even in the state of a crude plant extract, 0.001 to 10
Sufficient effects are observed with a blending of about weight%.

[0014]

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a lotion, an emulsion,
It can be provided as a skin external preparation in the form of a gel, cream, ointment or the like. In addition, it can be provided as a skin cosmetic such as lotion, milky lotion, cream and the like.

[0015]

EXAMPLES The present invention will be described in more detail with reference to Examples.

[Example 1] Skin lotion (1) Ethanol 10.0 (wt%) (2) Hydroxyethylcellulose 1.0 (3) Aspergillus niger leaf ethanol extract 5.0 (4) Purified water 84.0 Production method: (1) to (4) are mixed and made uniform.

Example 2 Skin Emulsion (1) Stearic acid 0.2 (% by weight) (2) Cetanol 1.5 (3) Vaseline 3.0 (4) Liquid paraffin 7.0 (5) Polyoxy Ethylene (10E.O.) monooleic acid 1.5 ester (6) Tocopherol acetate 5.0 (7) Glycerin 5.0 (8) Methyl parahydroxybenzoate 0.1 (9) Triethanolamine 1.0 (10 ) Purified water 71.7 (11) Sciatica leaf methanol extract 2.0 (12) Motachibana leaf ethyl acetate extract 2.0 Production method: Mix and heat the oil phase components of (1) to (6) Dissolve and keep at 70 ° C. On the other hand, the aqueous phase components (7) to (10) are mixed and heated to be uniform, and the temperature is set to 70 ° C. The oil phase component is gradually added to the aqueous phase component while stirring to emulsify, and after cooling, (11) and (12) are added at 40 ° C.

Example 3 Skin Gel (1) Dipropylene glycol 10.0 (% by weight) (2) Carboxyvinyl polymer 0.5 (3) Potassium hydroxide 0.1 (4) Methyl paraoxybenzoate 0.1 (5) Purified water 84.3 (6) Ascorbic acid phosphate magnesium salt 4.0 (7) 1,4-benzoquinone-containing fraction ethanol solution 1.0 (1,4-benzoquinone content; (100 μM) Production method: After dissolving (2) uniformly in (5), dissolve (4) in (1) and then add (3) to increase the viscosity, (6), (7) )
Is added.

Example 4 Skin Cream (1) Beeswax 6.0 (% by weight) (2) Cetanol 5.0 (3) Reduced Lanolin 8.0 (4) Squalane 27.5 (5) Glyceryl fatty acid ester 4.0 (6) Lipophilic glyceryl monostearate 2.0 (7) Polyoxyethylene (20E.O.) sorbitan 5.0 Monolaurate (8) Propylene glycol 5.0 (9) Paraoxybenzoic acid Methyl 0.1 (10) Purified water 30.4 (11) Retinol palmitate 1.0 (12) 50% by weight of Aspergillus niger leaf Propylene 3.0 Glycol extract (13) 50% by weight of Motachibana leaf 1,3-butylene 3.0 Glycol extract Production method: Mix and dissolve the oil phase components (1) to (7) and heat to 75 ° C. On the other hand, the aqueous phase components (8) to (10) are mixed and dissolved, and heated to 75 ° C. Next, the oil phase component is added to the water phase component and pre-emulsified, and then uniformly emulsified by a homomixer. After cooling, (11) to (13) are added at 40 ° C.

Example 5 Oil-in-water emulsion ointment (1) White petrolatum 25.0 (% by weight) (2) Stearyl alcohol 25.0 (3) Glycerin 12.0 (4) Sodium lauryl sulfate 1.0 (5) Methyl paraoxybenzoate 0.1 (6) Purified water 33.9 (7) Retinoic acid 0.5 (8) Extract of 50% by weight of Aspergillus niger leaf propanol 1.5 (9) Extraction of ethanol by 60% by weight of Sicicuti leaf Material 0.5 (10) Motachibana leaf 60% by weight ethanol extract 0.5 Production method: Mix and dissolve the oil phase components of (1) to (4) to make uniform,
Heat to 75 ° C. On the other hand, the aqueous phase components (5) and (6) were mixed and dissolved, heated to 75 ° C., added with the oil phase component and emulsified, cooled, and then cooled to 40 ° C. at (7) to (10). ) Is added and mixed.

[Example 6] Lotion (1) Ethanol 10.0 (wt%) (2) 1,3-butylene glycol 5.0 (3) Methyl parahydroxybenzoate 0.1 (4) Mokutachibana whole tree ethanol Extract 0.5 (5) Fragrance 0.1 (6) Purified water 84.3 Production method: (1) to (5) are sequentially added to (6) and uniformly mixed and dissolved.

Example 7 Emollient cream (water-in-oil type) (1) Liquid paraffin 30.0 (% by weight) (2) Microcrystalline wax 2.0 (3) Vaseline 5.0 (4) Diglyceryl geo Leic acid ester 5.0 (5) Sodium L-glutamate 1.6 (6) L-serine 0.4 (7) Propylene glycol 3.0 (8) Methyl parahydroxybenzoate 0.1 (9) Purified water 52. 4 (10) Aspergillus bark, leaf 50% by weight propylene 0.2 glycol extract (11) Siciakuchi leaf, flower, fruit 1,3-butylene 0.2 glycol extract (12) Fragrance 0.1 Production method: (5) , (6) dissolved in a part of (9) to 50 ° C.
Add slowly to (4) heated to 0 ° C. with stirring. This was previously mixed and uniformly dispersed in (1) to (3), which were heated and dissolved at 70 ° C., and (7) and (8) were dissolved in the remainder of (9) and heated to 70 ° C. Add while stirring and emulsify with a homomixer. After cooling, (10) to (12) are added and mixed at 40 ° C.

Of the above embodiments, the first and third embodiments
Were evaluated for their anti-aging, anti-inflammatory and whitening effects. At that time, in Example 1, the ethanol extract of Aspergillus niger leaves (3) was replaced with the same amount of tocopherol acetate in Comparative Example 1 and in Example 3, the fraction containing (1,7) -benzoquinones in (7) was used. The same evaluation was performed with Comparative Example 2 in which the ethanol solution was replaced with ethanol.

First, as an effect of preventing skin aging, the effect on the occurrence of wrinkles in hairless mice was evaluated.
In the evaluation, five hairless mice were used as one group, and the examples and the comparative examples were applied to the back once a day for each group.
The hairless mice were irradiated with long-wavelength ultraviolet light (UVA) for 50 weeks at J / cm ² / week, the occurrence of wrinkles on the back skin of the hairless mouse was observed, and scored according to the criteria shown in Table 1. At this time, a group to which only purified water was applied was used as a control. The results are shown in Table 2 by calculating the average value of each group and showing the relationship with the number of UVA irradiation days.

[Table 1]

Next, the anti-inflammatory effect was determined by injecting a carrageenan aqueous solution subcutaneously into the back of a group of 5 hairless mice to induce inflammation. It was applied to the back skin, and the state of improvement of inflammation was observed and evaluated. At this time, the group to which only purified water was applied was used as a control. The state of improvement of inflammation was evaluated in three stages of “improvement”, “slight improvement”, and “no improvement”, and the number of hairless mice that obtained each evaluation was shown in Table 3.

Subsequently, the effect of improving skin roughness was evaluated. 1 female panelist with significant skin irritation
In each group, each of Examples and Comparative Examples was given 2 times a day.
The skin was used continuously for one month with a blind for one month, and the skin symptoms after one month were observed and compared with those before the start of use. The skin roughening symptoms were scored according to the criteria shown in Table 4 to give a score of 2
The average value of 0 subjects was calculated and is shown in Table 5.

[Table 4]

Finally, the effect of improving pigmentation symptoms was evaluated. A group of 20 female panelists with remarkable pigmentation symptoms such as spots and freckles was used as a group, and the examples and comparative examples were each used twice a day blindly for one month for each group, and the skin after one month was used. The state of pigmentation was observed and compared with that before use. The state of pigmentation was evaluated according to the criteria shown in Table 6, and the average value of 20 persons was calculated.

[Table 6]

[0028]

[Table 2] In Table 2, in the control group, generation of deep wrinkles was observed in almost all hairless mice by UVA irradiation for 50 weeks. In the group to which the examples of the present invention were applied, a good effect of preventing the generation of wrinkles due to UVA was recognized, and even after irradiation for 50 weeks, only the generation of minute wrinkles was observed. On the other hand, the wrinkle progression was slower in the control group than in the control group, but the preventive effect was smaller than in the control group, and the hairless group showed moderate wrinkle appearance after 50 weeks. Mice were also seen.

[0029]

[Table 3] Also in Table 3, in the control group, almost no hairless mice showed improvement in inflammation after one week, and only one case showed a slight improvement tendency. In the group to which Example was applied, improvement was observed in all cases, and improvement was observed in 3 cases in the group to which Example 1 was applied and 4 cases in the group to which Example 3 was applied. On the other hand, the improvement of the group to which the comparative example was applied was insufficient and no improvement was observed.

[0030]

[Table 5] From Table 5, in the group using the examples of the present invention, favorable skin roughness and improvement of the pigmentation symptom were recognized, the skin condition was recovered to almost a good condition, and the pigmentation was also improved to a slight extent. Is shown. On the other hand, in the group using the comparative example, the tendency of improvement of the rough skin and the pigmentation symptom is observed, but the skin condition has not recovered to a point where it can be said to be healthy, and slight to moderate pigmentation is still observed. The effect was inadequate.

In the above-mentioned use test, there was no paneler who recognized skin irritation and skin sensitization in the use groups of Examples 1 and 3 of the present invention. Further, when Examples 1 to 7 of the present invention were stored at 25 ° C. for 3 months, none of them showed any change in state.

[0032]

As described in detail above, according to the present invention, it is possible to provide an external preparation for skin having both effects of anti-aging, anti-inflammatory and whitening, and excellent in stability and safety.

Claims (3)

[Claims] 1. An Aspergillus oryzae plant, Arbus japonica ( Ar
disia japonica Blume) and A. quinquegona
An external preparation for skin, characterized by containing one or more selected from extracts of Blume) and A. sieboldi Miq. 2. An Aspergillus oryzae plant, Arbus japonica ( Ar
disia japonica Blume) and A. quinquegona
Blume) and 1,4-benzoquinones contained in the extract of A. sieboldi Miq.
An external preparation for skin, characterized by containing a seed or two or more kinds. 3. The external preparation for skin according to claim 1, wherein the external preparation for skin is a cosmetic for skin.