JPH0717848A - Topical skin - Google Patents

Abstract

(57) [Summary] [Objective] By using a specific plant extract in combination with kojic acid and / or a derivative thereof, the stability of kojic acid or a kojic acid derivative by photolysis can be increased, and kojic acid or a kojic acid derivative is originally An external preparation for skin that exerts the medicinal effect of [Composition] Consists of kojic acid and / or its derivative and Coptis chinensis, Onji, Cuckon, Coacebana, Clameria, Saponsou, Salvia, Narcissus, Achillea millefolium, Aesculus hippocastanum, Cha, Tulip, Birodoaoi, Red radish, Beetroot, Himaburna and Henna. A skin external preparation characterized by containing one or more plant extracts selected from the group.

Description

Detailed Description of the Invention

[0001]

FIELD OF THE INVENTION The present invention relates to an external preparation for skin containing kojic acid and / or a derivative thereof and an extract of a specific plant as an active ingredient. More specifically, by using a specific plant extract in combination, The present invention relates to a skin external preparation capable of improving the stability of kojic acid or its derivatives and effectively expressing their pharmacological actions.

[0002]

2. Description of the Related Art Unlike other organs, the skin is susceptible to external influences, that is, physical factors such as sunlight, temperature and humidity, or chemical factors such as detergents. Among them, the adverse effect of ultraviolet rays contained in sunlight on the skin is particularly serious. That is, exposure to ultraviolet rays for a long time causes sunburn, which damages the skin, causes inflammation, and weakens the skin, resulting in blistering. When such a state is repeated, collagen fibers in the subcutaneous tissue are destroyed,
It promotes skin diseases such as pigmentation, rough skin, and fine wrinkles.

Since the wavelength of ultraviolet rays which causes inflammation such as erythema on human skin is a medium wave ray (UVB wavelength range) of about 280 to 320 nm, it is not suitable for cosmetics intended to prevent sunburn. Generally, U.S.P. V. Compounds that selectively absorb ultraviolet rays in the B wavelength range, particularly compounds that have a maximum absorption site at 308 nm, which is said to cause erythema, such as benzophenone compounds, salicylic acid derivatives, para-aminobenzoic acid and its esters and silicates. UV absorbers such as cinnamic acid derivatives have been incorporated.

However, these conventionally known sunscreen cosmetics are mainly used as described above. U.
V. Although it is intended to prevent sunburn by absorbing ultraviolet rays in the B wavelength range, it has been difficult to say that the effect of sunburn prevention is necessarily sufficient. Further, not only does it show no effect as an external preparation that effectively prevents inflammation due to sunburn, but it also has a problem of compatibility with other bases, deterioration of ultraviolet absorption capacity due to decomposition of ultraviolet absorbent and coloring, Had problems in terms of safety, such as increased skin irritation. On the other hand, various chemicals such as vitamin C are used as cosmetics or external preparations for preventing pigmentation, but ultraviolet rays (U.V.
It has not yet been effective as an external preparation for effectively improving pigmentation of severe symptoms accompanied by inflammation due to (B region).

Kojic acid, which was previously developed by the applicant as an active ingredient for a topical whitening agent, is a drug satisfying these requirements,
That is, it is known as an ideal whitening agent having an ultraviolet absorbing ability and also having an anti-inflammatory effect (for example, JP-B-56-18569 and JP-B-61-10447).
JP-B, JP-B-58-34446, JP-A-55-
No. 157509). However, although kojic acid has such excellent component characteristics, it has a drawback of being colored and decomposed with time by ultraviolet rays, and in some cases, its pharmacological action is not sufficiently exerted.

[0006]

The object of the present invention is to enhance the stability of kojic acid or a kojic acid derivative by photolysis by using an extract of a specific plant in combination, and to improve the stability of kojic acid or a kojic acid derivative. An object is to provide an external preparation for skin that exerts its medicinal effect regardless of its effect.

[0007]

Means for Solving the Problems As a result of intensive studies for solving the above problems, the present inventors have found that Coptis, Onji, Cuckoo, Coomassea, Clameria, Sophora sinensis, Salvia, Narcissus, Yarrow, Horse chestnut, By using one or more kinds of plant extracts selected from the group consisting of tea, tulip, velvet aoi, radish, beet, hemlock, and henna in combination with kojic acid and / or its derivative, their photostability, ( Photodegradability by UVB) is improved,
The present invention has been completed by finding that the skin-whitening effect is effectively exerted and, surprisingly, that a synergistic anti-inflammatory effect is obtained.

[0008] That is, according to the present invention, Coptis, Onji, Cuckon, Coomassea, Clameria, Saboursou,
Salvia, narcissus, yarrow, horse chestnut, tea, tulip, velvet aoi, radish, beet, hemibana, henna, a kojic acid characterized by containing one or more kinds of plant extracts selected from the group consisting of or There is provided a skin external preparation having an improved light stability of a kojic acid derivative and an excellent anti-inflammatory effect.

[0009]

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. .

As the kojic acid derivative, for example, those disclosed in Japanese Examined Patent Publication No. 60-10005, Japanese Examined Patent Publication No. 1-45472 and Japanese Examined Patent Publication No. 3-74229, Japanese Examined Patent Publication No. 58-
No. 22151 and Japanese Patent Publication No. 58-22152, Kojic acid having a stabilized kojic acid molecule by binding a saccharide to the esterified product of kojic acid and the -CH ₂ OH group at the 2-position of kojic acid. Known compounds such as derivatives can be used alone or in combination of two or more. The following can be illustrated as a specific plant extract used together with kojic acid and / or its derivative (s).

Coptis japonica Makino (Ranu
nculaceae)) is a small perennial plant found in the mountains of the Sea of Japan side of Hokkaido and Honshu. The extract (Japanese Copti
As s Extract), after adding water from the rhizome except for the roots of Coptis or other plants of the same genus,
What was obtained by concentrating can be used conveniently.

[0012] Polygala tenuifolia Will
d) is a perennial herb belonging to the family Hemelidae. Onji (Poly
galae Radix) means the root thereof, and as the Ondi extract, those obtained by extraction with ethanol, purified water and the like can be preferably used.

Kudzu (Pueraria lobata Willd) is a vine perennial herb of the legume family and has a diameter of 10 to 2 underground.
There are storage roots up to 0 cm. Cuckle (Puer)
ariae Radix) means the storage root thereof, and as the extract, those obtained by extraction with ethanol, purified water and the like can be preferably used.

[0014] Cumaceba is a plant of the genus Platymiscium of the family of the legume, Platymiscium trinitatis.
(Platymiscium trinitatis), which has been used as a tonic since ancient times. As the extract,
Those extracted with water, ethanol, propylene glycol or the like can be preferably used.

Clameria (Rhatany) is a small shrub from South America, and its extract is preferably one extracted from roots.

Saponaria officinalis is a perennial herb native to Europe and a height of 30 to 60 cm. As the extract (Saponaria Extract), propylene glycol from the leaves of soapless,
An extract obtained by extracting with 1,3-butylene glycol or an aqueous solution thereof can be preferably used.

Sage (Salvia officinalis L.) is a perennial plant of the Labiatae family, is native to Europe and is cultivated in the Mediterranean coast and all over Japan, and is generally called salvia in Japan. As the extract (Salvia Extract), the one extracted from whole grass with purified water, propylene glycol, 1,3-butylene glycol, ethanol or the like can be preferably used. Further, as the oil-soluble extract thereof, those extracted with a dark blue liquid of persic oil and liquid paraffin can be preferably used.

Narcissus tazetta L. var. Ch
inensis Roemer) is a perennial herb of the family Amaryllidaceae, and the extract thereof can be preferably used extracted from bulbs.

Achillea millefo
lium L.) is a perennial of the Asteraceae family and its extract (Milfoi
As l Extract), those extracted from whole grass can be preferably used.

Horse chestnut (Aesculus hippocastanum L.)
It is said to be horse chestnut, which is native to the Balkan Peninsula. It is well known as a roadside tree in Japan and is widely cultivated. Horse Chestnut Extract, Horse
As se Chestnut Extract Powder), those obtained by extracting fruits or leaves with propylene glycol, 1,3-butylene glycol, purified water, ethanol or the like can be preferably used.

Tea (Thea sinensis L.) is an evergreen shrub cultivated in various places and is widely used as a beverage. As the tea extract, tea branches and leaves are subjected to dry distillation under reduced pressure, and ethanol or glycerin and purified water are added to the fraction, or tea leaves extracted with ethanol can be preferably used.

Tulip (Tulipa gesneriana L.)
Is a perennial herb of the lily family, Tulip Extract
As), those extracted from flowers can be preferably used.

Bellows Aoi (Althaea officinalis
L.) is native to Europe and grows naturally in the salt marshes of the eastern Mediterranean region. It is a perennial plant with a height of 1.5 to 2 m. As the extract (Althea Extract), the one obtained by extracting from the root with purified water, 1,3-butylene glycol, propylene glycol, ethanol, or a mixed solution thereof can be preferably used.

The radish is radish radish, and the extract thereof can be suitably used as the extract.

[0025] Beet (Beta vulgares L.) is a perennial plant of the family Chenopodiaceae, and as its extract (Beet Extract), those extracted from leaves and stems can be preferably used.

Limulus radiata Herbert
Is a perennial herb of the family Amaryllidaceae, and the extract thereof is preferably obtained by extracting bulbs with purified water or the like.

As the henna extract, shrubs (Lawsonia alba, Lawsonia Spinosa L., Lawsonia L.) produced in tropical regions such as North America and India are used.
Those obtained by drying the leaves and trunk of the above can be preferably used.

In the present invention, the amounts of the kojic acid and / or its derivative and the plant extract to be blended are the same for cosmetics such as creams, lotions, emulsions, packs, lotions and essences, ointments, poultices and plasters. When used as an external preparation such as an agent, the plant extract is 0.0001 to 20% by weight, preferably 0.01 to 10% by weight, and kojic acid and / or a derivative thereof is contained in the whole preparation. It is compounded 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 as mentioned above, for example, poultice, plaster, paste, cream, ointment, aerosol, emulsion, It is widely used in the form known as pharmaceuticals such as lotions, emulsions, essences, packs, gels, powders, foundations, sun cares, bath salts, quasi drugs, and cosmetics.

In the case of producing the external preparation of the present invention, various known active ingredients which are usually used, for example, carpronium chloride, cefanthanthine, vitamin E, vitamin E nicotinate, nicotinic acid, nicotinic acid amide, benzyl nicotinate, Peripheral vasodilators such as Ginkgo tincture, Capsicum tincture, camphor, cooling agents such as meenthol, antibacterial agents such as hinokitiol, benzalkonium chloride, undecylenic acid, anti-inflammatory agents such as lysozyme chloride, glycyrrhizin and allantoin, ascorbic acid, A whitening agent such as arbutin, a placenta extract, a liver extract, various extracts derived from animals, plants and microorganisms such as lactic acid bacterium culture extract can be appropriately added and used.

In addition to the known active ingredients and base components such as surfactants and oils and fats, known moisturizers, preservatives, and antioxidants for the above-mentioned pharmaceuticals, quasi drugs, and cosmetics Agent, UV absorber / scattering agent, chelating agent, pH adjusting agent,
Various additives such as fragrances and colorants can be used in combination.

[0032]

EXAMPLES Examples and test examples of their effects will be given below, but these do not limit the present invention in any way.

<Test Example 1> Stability test with time Preparation of the following emulsion bases containing the active ingredients shown in Table 1 (In this test, 10 g of the original plant was added to 100 ml of the solvent, After stirring at room temperature for 3 hours, the dried plant extract was evaporated) and the stability test of kojic acid or kojic acid derivative was carried out. The sample is ultraviolet light (UV
-B) was irradiated and stored at 50 ° C for 2 months. One month after the start of storage, the content of kojic acid or its derivative (kojic acid glucoside as a representative example) was determined for each sample, and the change over time from the test start date was measured. The quantitative determination of the active ingredient was carried out by a high performance liquid chromatography method (ultraviolet spectrophotometer detector: wavelength 270 nm).

Emulsion base used in the test (% by weight) (A) Polyoxyethylene behenyl ether (20E.0.) 0.50 Tetraoleic acid polyoxyethylene bit (60E.0.) 1.00 Lipophilic type Glycerin monostearate 1.00 Stearic acid 0.50 Behenyl alcohol 0.50 Natural vitamin E 0.02 Preservative Suitable amount (B) 1,3-butylene glycol 5.00 Carboxyvinyl polymer 0.01 N-lauroyl-L- Sodium glutamate 0.50 Heat-dissolve components belonging to the production method (A) (oil phase), and separately (B)
The components belonging to (1) were dissolved by heating (aqueous phase). The aqueous phase was added to the oil phase, the mixture was stirred and emulsified, and then cooled to obtain an emulsion base.

[0035]

<Test Example 2> UV Erythema Suppressing Action A yellow-brown guinea pig having a body weight of about 300 g was used for the test.
The ventral part of the guinea pig was depilated on the day before the experiment. Experiment 3
Put a tape with two small holes (diameter 12 mm) on the hair removal part, and put an ultraviolet lamp (H-400-F, Toshiba) at 20 cm.
Irradiation for 40 seconds from the distance. Immediately after irradiation, 50 mg / site of a sample (the following cream base and the active ingredient described in Table 2) was applied to the seeds for 30 seconds (the plant extract in this test was prepared by
100 ml of the solvent was added to 0 g, the mixture was stirred at room temperature for 3 hours, and then evaporated to dryness was used). Visual observation was performed 3 hours after UV irradiation, and 3 points of erythema with clear boundaries of the irradiated area, 2 points of erythema with unclear boundaries, and 1 point of slight erythema were observed. Those without erythema were judged as 0 points and compared. The results are shown in Table 2. Further, after the erythema intensity was determined, the test site was irradiated with UV-B once a day for 90 seconds and every three days for a total of three times. From the irradiation start date, the sample was continuously applied three times a day for 20 days, and the degree of skin coloring was determined on the 20th day.

Cream base for testing (% by weight) (A) Monostearic acid Polyoxyethylene glycol (40E.0.) 2.00 Self-emulsifying glyceryl monostearate 5.00 Stearic acid 5.00 Behenyl alcohol 1.00 Liquid paraffin 1.00 Glycerin trioctanoate 10.00 Preservative Suitable amount Perfume Small amount (B) 1,3-butylene glycol 5.00 Purified water Residue (A) The ingredients belonging to (heat) are dissolved (oil phase) separately. ,
A component belonging to the component (B) was dissolved by heating (aqueous phase). The aqueous phase was added to the oil phase, the mixture was emulsified with stirring, and then cooled to obtain a vanishing cream base.

Criterion 3: No pigmentation is observed. 2: Slight pigmentation is observed. 1: Medium pigmentation is observed. 0: No change from control site (no treatment) -1: Stronger pigmentation than the control site (no treatment) is observed.

[0039]

[0040]

[0041]

[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. Ouren (water extract) 0.50 12. Onji (ethanol extract) 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. Polyethylene sorbitan monostearate (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. Kudzu (ethanol extract) 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.

<Formulation 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. Coomassever (1: 1 extract of water and propylene glycol) 2.00 5. Clameria (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 (% 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. Soapless (1,3-butylene glycol extract) 0.10 12. Sage (propylene glycol extract) 0.40 13. Narcissus (water 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. Achillea millefolium (water extract) 0.10 4. Horse chestnut (propylene glycol extract) 0.05 5. Cha (ethanol extract) 0.05 6. Sodium polyacrylate 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. 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. Tulip (water extract) 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. Ballowed Aoi (2: 1 extract of water and ethanol) 1.00 8. Radish (water extract) 0.20 9. Beet (water extract) 0.10 10. Higanbana (water extract) 0.01 11. Henna (water 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.

[0049]

INDUSTRIAL APPLICABILITY According to the present invention, the stability of kojic acid and / or its derivative by photolysis is increased by using kojic acid and / or its derivative in combination with at least one kind of extract of a specific plant. Also, there is provided an external preparation for the skin, which exhibits an excellent effect of suppressing erythema of ultraviolet rays and the like.

Claims (1)

[Claims] 1. Kojic acid and / or a derivative thereof, and Coptis, Ondi, Cuckon, Coomassea, Clameria, Sophora sinensis, Salvia, Narcissus, Achillea millefolium,
A skin external preparation characterized by containing one or more kinds of plant extracts selected from the group consisting of horse chestnut, tea, tulip, bellows mallow, radish, beet, hempflower, and henna.