JPH0717847A - Skin external preparation - Google Patents

Abstract

PURPOSE:To provide a skin external preparation synergistically raised in active oxygen-scavenging activity, excellent in effect of preventing wrinkles induced by UV-A radiation, containing a combination of kojic acid and/or its derivative with specific plant extract(s). CONSTITUTION:The skin external preparation containing, as active ingredients, (A) kojic acid and/or a derivative therefrom and (B) at least one kind of extract of plant(s) selected from a group composed of Acacia catechu, Hydrangea serrata, Scutellaria baicalensis, Cinchona succirubra, Potentilla fragarioides L., cucumber, clover, black tea, Betula platyphylla scrub, water melon, stevia, Hedera helix, Thymus vulgaris L., Eugenia caryophyllata, Oenothera tetraptera, Sorbus commixta, banana, Isodon japonicus, Hayflower, Marsh tea, Ilex paraguayensis, melon, apple, lavender, and lemon.

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 characterized by containing kojic acid and / or kojic acid derivative and an extract of a specific plant as an active ingredient. The present invention relates to a skin external preparation having an excellent effect of preventing UV-A-induced wrinkles by synergistically enhancing the active oxygen scavenging action of kojic acid or its derivative by using the plant extract of the above.

[0002]

2. Description of the Related Art Active oxygen is produced in the process in which oxygen molecules are reduced in a living body to become water through superoxide, hydrogen peroxide and hydroxyl radicals. It is known that active oxygen causes damage to biological membranes and tissues and causes various diseases. Skin inflammation and aging are also one of the tissue injuries caused by active oxygen, and along with the adverse effects of the sun, especially ultraviolet rays, research has been extensively conducted in recent years as a key to elucidating the aging mechanism.

It is known that skin aging progresses with aging and is accelerated by external factors such as ultraviolet rays. UV-A (32
0 to 400 nm), UV-B (280 to 320)
nm) and UV-C (200 to 280 nm), but it is ultraviolet rays in the UV-A region that are thought to reach the dermis and induce wrinkles. In addition to the external factors closely related to skin aging, active oxygen has been attracting attention as an internal factor.

Kojic acid is known as a coloring agent (for example, JP-B-56-18569 and JP-B-61-104).
47), but on the other hand, it is also known to have a radical scavenger. However, the action of scavenging active oxygen of kojic acid is not so strong, and therefore a highly effective and highly practical one has been demanded.

[0005]

The present invention synergistically enhances the activity scavenging action of kojic acid or its acid derivative by using an extract of a specific plant in combination, and suppresses wrinkles induced by UV-A or the like. It is an object of the present invention to provide a new external preparation for skin which is excellent in preventing effect.

[0006]

Means for Solving the Problems As a result of intensive studies to achieve the above-mentioned objects, the present inventors have found that Acenyak, Amacha, Ougon, Kina, Kizimushiro, Cucumber, Clover, Black Tea, Shirakaba Stem Scrub, watermelon,
One or more kinds of plant extracts selected from the group consisting of stevia, hollyhock, oleander, clove, evening primrose, rowan, banana, hikoshi, hayflower, marsh tea, mate, melon, apple, lavender, lemon. The present invention has been completed by finding that their combined use with an acid and / or its derivative synergistically enhances their pharmacological properties, active oxygen scavenging action. That is, according to the present invention, kojic acid and / or
Alternatively, there is provided a skin external preparation having an excellent anti-aging effect, which comprises a derivative thereof and an extract of the specific plant as an active ingredient.

[0007]

Detailed Description of the Invention Kojic acid (5-oxy-2-oxymethyl-γ-pyrone) used in the present invention is a pure product of 5-oxy-2-oxymethyl-γ-pyrone, kojic acid. A fermentation broth containing kojic acid as a main component obtained by culturing a known strain having productivity, a concentrated solution of the fermentation broth, and a crystallized extract of kojic acid from the fermentation broth are used. .

Examples of the kojic acid derivative include, for example, Japanese Patent Publication No. 60-10005, Japanese Patent Publication No. 1-45472, Japanese Patent Publication No. 3-74229, and Japanese Patent Publication No. 58-221.
No. 51, Japanese Patent Publication No. 58-22152, an esterification product of kojic acid and -CH at the 2-position of kojic acid.
Known compounds such as a kojic acid derivative in which a kojic acid molecule is stabilized by binding a saccharide to the ₂ OH group can be used alone or in combination of two or more kinds.

Specific examples of plant extracts used in combination with kojic acid and / or its acid derivatives include the following.

Uncaria gambir Roxburgh (Ru
biaceae)) is native to Malay and is cultivated in Java, Sumatra, Borneo, etc. Gambir Extract
As the extract, an extract obtained by extracting from leaves and young shoots with a 1,3-butylene glycol solution or an ethanol solution can be preferably used.

As the armature extract (Hydrangea Extract), the armature (Hydrangea serrata Seringe var.
(Hungerberg sugimoto) leaves and branch tips are added with purified water, ethanol or a mixed solution thereof, and the extract is obtained by cold or hot digestion, or a powder obtained by drying the extract is preferably used.

Scutellaria baicalensis Geor
gi (Labiatae)) is from China, and is also known as Scutellaria baicalensis, and it has been used in Chinese medicine to eliminate hyperemia. As the extract (Scutellaris Root Extract), the roots of Scutellaria baicalensis excluding the pericarp are purified and extracted with ethanol or a mixture thereof, which is preferably mixed with 1,3-butylene glycol or ethanol. it can.

The plants of the genus Cinchona are wild in the Andes Mountains in Peru, Polyvia and Ecuador, and there are more than 400 species. Quina extract (Cinc
As honaExtract, Kina (Cinchona succirubra P
avon et Klotzch (Rubiaceae)) or other extract obtained by extracting from the bark of a plant of the same genus with purified water, propylene glycol, ethanol, or a mixture thereof.

Potentillae anserinae
Is a plant with many pinnate leaves, usually grown in moist clay soils, with long branches and dense silvery-haired hair, with long, fruitless bright yellow flowers. The extract (Potentilla Extra
As ct), leaf extract can be preferably used.

Cucumber Extrac
t) is a fruit obtained by squeezing the fruit of cucumber (Cucumis sativus), or concentrated in an extract obtained by extracting the fruit with purified water or 1,3-butylene glycol, propylene glycol, or a mixture thereof. What added glycerin can be used conveniently.

Clover (Trifolium pratense) has 15
It is a legume perennial that grows up to 50 cm in height and has three leaves. The flowers have a white round shape and are rich in nectar. As the extract (Clover Blossom Extract),
Those extracted from flowers can be preferably used.

As the tea extract (Fermented Tea Extract), there is Assamcha (Teasinesis L. var assamica Pie
An extract obtained by slightly drying leaves of rre (Theaceae: Camelliaceae)), fermenting, further drying, and extracting the minced ones with an ethanol solution can be suitably used.

Birch (Betula alba L., Bet)
ula leuta L., Folia betula) is a plant of the birch family,
Widely distributed in the northern temperate zone of the Northern Hemisphere. The extract (Birch
Extracts, Birch Leaf Extracts, Birch Bark Extracts) are preferably extracts extracted from leaves, bark and xylem with purified water, ethanol, propylene glycol, 1,3-butylene glycol and the like. Further, as the oil-soluble extract, an extract obtained by extracting an ethanol extract from bark with squalane can be preferably used.

Watermelon (Citrullus battich Forsk) is
It is a first-year climbing herb of the Cucurbitaceae family. As the extract, those extracted from fruits or seeds can be preferably used.

Stevia (Stevia rebandiona Bertoni)
Is an Asteraceae perennial native to South America. As the extract, one extracted from whole grass can be preferably used.

Hedera helix is a perennial plant of the family Araliaceae, which is a stringy evergreen shrub that grows on trees and walls. As the extract (Ivy Extract) originating from Europe in the Caucasus region, propylene glycol, 1,3-butylene glycol extracted from stems and leaves and those extracted with an aqueous solution thereof can be preferably used.

Thymus vulgaris L. is a shrub that grows in southern Europe, is 40 cm in height, has oval-shaped leaves of gray-green, and has small, pale red or bluish purple flowers. As the extract (Thyme Extract), an extract obtained by extracting propylene glycol, butylene glycol or an aqueous solution thereof from whole grass can be preferably used.

Clove (Syzygium aromaticum Merrill
et Perry, Eugenia caryophyllata Thunberg) is native to the Moluccas, Sumatra, Java, Ambon, Madagascar, Zanzibar, West Indies, etc.,
It is an evergreen tree in the family Amphitaceae. The extract (Clove Extr
As act), those obtained from buds can be preferably used.

[Evening Primrose (Oenothera tertraptera Cav.Oeno
thera hookeri) has thin stems, folds of yellow flowers,
A plant that grows up to a height of 1 m, it grows mainly in the dry hills of Europe and America. The extract (Ev
As the ening Primrose Extract), those extracted from whole grass can be preferably used.

Rowan (Sorbus aucuparia) is a deciduous tree and is found mainly in Europe. It has compound leaves, and the hair is dense on the back side of the leaves. The flowers are white and shaped like an umbrella, with bright red berries. The extract (Mountain A
As the sh Extract), a fruit extract can be preferably used.

Banana (Musa sapientum) is a perennial plant that is cultivated in many tropical and subtropical countries.
As the extract (Banana Extract), a fruit extract can be preferably used.

Hikiokoshi (Isodon japonicus Hara) is a plant of the Lamiaceae family and is a perennial plant that grows naturally in various parts of Japan, such as south of southern Hokkaido and Korea. Black squirrel (Isodon t
richocarpus Kubo) grows in the mountains of Hokkaido, east of Fukui, Honshu. Both species are dried whole plants and
is Herba). The extract (Isodonis HerbaEx
tract), foliage from ethanol, purified water, 1,
An extract obtained by extraction with 3-butylene glycol or the like, or an extract obtained by extracting with ethyl acetate, distilling off ethyl acetate and then adding ethanol or purified water can be preferably used.

Hayflower Extract
As the), flowers of hay flower (Graminis) can be preferably used.

Marsh tea (Ledi polustris)
An evergreen shrub commonly found in marshes or wetlands in northern, eastern Europe, northern Asia, and North America, with open branches, hard lanceolate leaves, and white or pink vermicular flowers. As the extract (Marsh Tea Extract), those obtained from leaves can be preferably used.

Mate (Ilex peraguariensis) is a shrub in the wild, but sometimes it reaches a height of 20 m. Alternate leaves, white flowers gather on the axils and bloom.
The fruit is a small black-purple succulent fruit with four seeds. As the extract (Mate Extract), those extracted from leaves can be preferably used.

[0031] Melon (Cucumis melo L.) is an annual herbaceous plant of the family Cucurbitaceae, and as the extract (Melon Extract), those extracted from fruits and seeds can be preferably used.

Apple (Pyrus malus L.) is a plant of the family Rosaceae, which is a deciduous tree cultivated in various places. As the extract (Apple Extract), a liquid obtained by squeezing the fruit and concentrating the liquid, or concentrated glycerin, or an extract obtained by extracting from the fruit with 1,3-butylene glycol or propylene glycol is preferable. Can be used.

Lavandula officinalis is a semi-shrub, native to the western Mediterranean, Dalmatia and Greece, and currently cultivated in southern France, England, Italy, Hungary, Spain and North Africa. It has cotton-like or spear-shaped blue-green leaves, and purple flowers with a unique smell bloom. As an extract (Lavender Extract),
Extracts from flowers can be preferably used.

Lemon (Citrus limon Burmann fil.) Originates from the foothills of the western Himalayas of India, but is currently mainly produced in the United States and Italy. The extract (Lemon
Extract), the fruit is purified water, glycerin, 1,
An extract obtained by leaching with or squeezing with 3-butylene glycol, propylene glycol or the like or a fruit juice obtained by squeezing and filtering and then adding concentrated glycerin can be preferably used.

In the present invention, the amount of the kojic acid and / or its derivative and the plant extract compounded is such that creams, lotions, milky lotions, packs, lotions, essences and other cosmetics, ointments and poultices are used. In any case of using it as an external preparation such as plaster, 0.0001 to 20% by weight, preferably 0.01 to 10% by weight, of a plant extract extract, kojic acid and / or its derivative relative to the whole preparation Is blended in the range of 0.001 to 10% by weight, preferably 0.1 to 5% by weight.

The external preparation for skin of the present invention is not particularly limited as long as it is suitable for external application, and examples thereof include poultices, plasters, pastes, creams, ointments and aerosols, as mentioned above. It is widely used in the form known as pharmaceuticals such as emulsions, lotions, emulsions, essences, packs, gels, powders, foundations, sun care and bath salts, quasi drugs, and cosmetics.

In the case of producing the external preparation of the present invention, various known active ingredients usually used, for example, carpronium chloride, cepharanthin, vitamin E, vitamin E nicotinate, nicotinic acid, nicotinic acid amide, benzyl nicotinate, and ginger. Cooling agents such as tincture, capsicum tincture, antibacterial agents such as hinokitiol, benzalkonium chloride, undecylenic acid, antiphlogistics such as lysozyme chloride, glycyrrhizin and allantoin, whitening agents such as ascorbic acid and arbutin, placenta extract, liver extract Various extracts derived from animals, plants and microorganisms such as lactic acid bacterium culture extracts can be appropriately added and used.

In addition to known active ingredients, base agents such as surfactants and oils and fats, known moisturizers, antioxidants, ultraviolet rays, etc. may be added to the above-mentioned drugs, quasi-drugs and cosmetics. Various additives such as an absorbent / scattering agent, a chelating agent, a pH adjusting agent, a fragrance and a coloring agent can be used in combination.

[0039]

EXAMPLES Next, examples and test examples for showing the effects thereof will be shown, but these do not limit the present invention at all.

<Test Example 1> Active oxygen scavenging test SOD activity of the external preparation for skin of the present invention The active ingredient shown in Table 1 was added to a lotion base consisting of the following formulation examples, and a formulation was prepared by the method of McCord et al. The SOD activity in was measured. In this test, 10 plants were
After adding 100 ml of the solvent to g and stirring at room temperature for 3 hours,
Evaporated and dried plant extract was used. Also, in the prescription example,
The blending ratio (appropriate amount) of purified water means a numerical value of 100% by weight as a whole.

(Wt%) 1. Polyoxyethylene hydrogenated castor oil (60E.0.) 8.00 2. Ethanol 15.00 3. Behenyl alcohol 1.00 4. Paraoxybenzoic acid ester 0.10 5. Citric acid 0.10 6. Sodium citrate 0.30 7.1,3-butylene glycol 4.00 8. Disodium edetate 0.01 9. Purified water Suitable amount

[0042]

[0043]

[0044]

[0045]

[0046]

[0047]

[0048]

<Test Example 2> The half face method is used.
Wa improvement effect test 1) Test method The active ingredient shown in Table 2 was mixed with the essence base (Example 7), and a woman (35 to 55 years old) with small wrinkles was applied to the face twice a day in the morning and evening. After continuous application, the degree of improvement of small wrinkles was examined after 3 months. The face was applied to the left and right by the half-face method, and one side was coated with the essence containing the active ingredient, and the other side was coated with the essence containing no active ingredient (only the base) for evaluation. In this test, a plant extract was used in which 100 g of the solvent was added to 10 g of the original plant, the mixture was stirred at room temperature for 3 hours, and then evaporated to dryness.

2) Test Results As a result of judging the degree of improvement of small wrinkles before the use of essence, the essence of the present invention was found to have a clear effect of reducing wrinkles. In addition, no skin abnormality was observed due to continuous use. The results are shown in Table 2.

[0051]

[0052]

[0053]

[Prescription example] The prescription example of the present invention is given below. In the prescription examples, the “appropriate amount” means an amount that makes the entire prescription 100% by weight.

<Formulation Example 1> Cream (% by weight) 1. Polyethylene glycol monostearate (40E.0) 2.00 2. Self-emulsifying glyceryl monostearate 5.00 3. Stearic acid 5.00 4. Behenyl alcohol 1.00 5. Liquid paraffin 10.00 6. Glyceryl trioctanoate 10.00 7. Paraoxybenzoic acid ester 0.20 8.1,3-butylene glycol 5.00 9. Disodium edetate 0.01 10. Kojic acid 1.00 11. Acacia catechu (ethanol extract) 0.50 12. Amacha (1: 1 mixed extract of water and ethanol) 0.10 13. Purified water Proper amount Manufacturing method A. Heat 1 to 6 to dissolve. B. 7 to 13 are heated and dissolved. C. Add B to A, emulsify, stir, and cool. D. After C is cooled, it is filled in a container to be a product after inspection. How to use and dose Rub on face appropriately.

<Formulation Example 2> Emulsion (wt%) 1. Monostearic acid Polyoxyethylene sorbitan (20E.0.) 2.00 2. Tetraoleic acid Polyoxyethylene sorbit (60E.0.) 0.50 3. 3. Lipophilic glyceryl monostearate 1.00 4. Stearic acid 0.50 5. Behenyl alcohol 0.50 6. Avocado oil 4.00 7. Glyceryl trioctanoate 4.00 8. Paraoxybenzoic acid ester 0.20 9.1,3-butylene glycol 5.00 10. Xanthan gum 0.14 11. Disodium edetate 0.01 12. Kojic acid 4.00 13. Ougon (1: 1 mixed liquid extract of ethanol and 1,3-butylene glycol) 5.00 14. Purified water Proper amount Manufacturing method A. Heat 1 to 7 to dissolve. B. Dissolve 8 to 14 by heating. C. Add B to A, emulsify, stir, and cool. D. After cooling C, it was filled in a container, and it was a product after inspection. How to use and dose Rub on face appropriately.

<Prescription Example 3> Lotion (% by weight) 1. Polyoxyethylene hydrogenated castor oil (60E.0.) 8.00 2. Ethanol 15.00 3. Kojic acid glucoside 7.00 4. Quina (propylene glycol extract) 2.00 5. Kizimushiro (water extract) 0.50 6. Paraoxybenzoic acid ester 0.10 7. Citric acid 0.10 8. Sodium citrate 0.30 9.1,3-butylene glycol 4.00 10. Disodium edetate 0.01 11. Purified water Proper amount Manufacturing method A. 1 to 11 are uniformly stirred and dissolved. B. A is filled in a container and the product is obtained after the inspection. How to use and dose Rub on face appropriately.

<Formulation Example 4> Ointment (wt%) 1. Polyethylene glycol monostearate (40E.0) 2.00 2. Self-emulsifying glyceryl monostearate 5.00 3. Stearic acid 5.00 4. Behenyl alcohol 1.00 5. Liquid paraffin 10.00 6. Glyceryl trioctanoate 10.00 7. Paraoxybenzoic acid ester 0.20 8.1,3-butylene glycol 5.00 9. Disodium edetate 0.01 10. Kojic acid 1.00 11. Cucumber (water extract) 0.10 12. Coro bar (ethanol extract) 0.40 13. Black tea (ethanol extract) 1.00 14. Purified water Proper amount Manufacturing method A. Heat 1 to 6 to dissolve. B. 7 to 14 are heated and dissolved. C. Add B to A, emulsify, stir, and cool. D. After C is cooled, it is filled in a container to be a product after inspection. How to use and dose Rub on face appropriately.

<Formulation Example 5> Pap agent (% by weight) 1. Polyacrylic acid 30.00 2. Kojic acid 0.50 3. Shirakaba trunk scrub (1: 1 mixed liquid extract of water and ethanol) 0.10 4. Watermelon (ethanol extract) 0.05 5. Stevia (water extract) 0.05 6. Polyacrylic acid soda 7.00 7. Aluminum chloride 0.30 8. Concentrated glycerin 20.00 9. Sorbitan monooleate 1.00 10. Titanium oxide 4.00 11. Purified water Suitable amount manufacturing method A. 1 to 5, 9 and 11 are heated and dissolved. B. Heat 6 to 8 and 10 to dissolve. C. Add B to A, stir evenly, and mix. D. After cooling C, it was applied to a coating agent, and after inspection, a product was obtained. Usage and dose: Remove the liner and apply to the affected area.

<Formulation Example 6> Bath agent (% by weight) 1. Liquid paraffin 65.00 2. Di-2-heptyl undecanoic acid Glycerin monostearate 5.00 3. Polyoxyethylene (2E.0.) Glycerin monostearate 2.00 4. Polyoxyethylene (9E.0.) Monooleate 2.00 5. Polyoxyethylene (3E.0.) Lauryl ether 5.00 6. Vitamin E 0.20 7. Kojic acid monopalmitate 2.00 8. Prickly pear (1: 1 mixed extract of propylene glycol and water) 3.00 9. Fragrance 1.00 10. Minute amount of dye 11. Ethanol Proper amount production method A. Mix and dissolve 1 to 9. B. Add 10 to 11 and dissolve. C. Add B to A and stir uniformly. D. C was filled in a soft capsule, and a product was obtained after the inspection. Dosage and dosage Put an appropriate amount in the bath and take a bath.

<Formulation Example 7> Essence (% by weight) 1.1% carboxyvinyl polymer solution 10.00 2. Glycerin 20.00 3. Hyaluronic acid 0.50 4. Ethanol 7.00 5. Galactimide kojic acid 3.00 6. Kojic acid 2.00 7. Tachijakoso (water extract) 1.00 8. Clove (water extract) 0.20 9. Evening primrose (ethanol extract) 0.10 10. Rowan (water extract) 0.01 11. Banana (ethanol extract) 0.01 12. Purified water Appropriate amount Production method The above components were mixed, uniformly stirred, and dissolved to produce essence. Usage and dose Appropriate amount Rub on face. It was confirmed that each of the external preparations for skin of Formulation Examples 1 to 7 is a preparation having an effect satisfying the object of the present invention.

[0061]

Industrial Applicability According to the present invention, there is provided a novel skin preparation for external use, which comprises kojic acid and / or a derivative thereof and a specific plant extract as active ingredients. It is highly effective and can very effectively improve damaged skin due to sunburn, and can prevent skin aging such as fine wrinkles.

Claims (1)

[Claims] 1. Kojic acid and / or a derivative thereof, and Acenyak, Amacha, Ougon, Kina, Kijimushiro, Cucumber, Clover, Black tea, Birch trunk scrub, Watermelon, Stevia, Ivy, Ivy, Periwinkle, Evening grass, Rowan, Banana An external preparation for skin, which comprises, as an active ingredient, one or more kinds of plant extracts selected from the group consisting of Hikioko, Hayflower, Marsh tea, mate, melon, apple, lavender, and lemon.