JP3415200B2 - External preparation for skin - Google Patents

Description

Description: BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a skin external preparation containing kojic acid and / or a derivative thereof and a specific plant extract as active ingredients. The present invention relates to an external preparation for skin which can improve the stability of kojic acid or a derivative thereof by using a specific plant extract in combination and effectively exhibit their pharmacological actions. [0002] Unlike other organs, 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. In other words, the skin is injured and irritated by being exposed to ultraviolet rays for a long time and causing sunburn, and the skin becomes fragile and causes blistering. When such a condition is repeated, collagen fibers in the subcutaneous tissue are destroyed,
Skin diseases such as pigmentation, rough skin, and development of fine wrinkles are promoted. The wavelength of ultraviolet light that causes inflammation such as erythema on human skin is about 280 to 320 nm, a medium-wave light (UVB wavelength range). Generally, U.S. V. Compounds that selectively absorb ultraviolet rays in the B wavelength range, particularly compounds having a maximum absorption value at 308 nm which is considered to cause erythema, such as benzophenone compounds, salicylic acid derivatives, paraaminobenzoic acid and its esters and silica Ultraviolet absorbers such as cinnamate derivatives have been formulated. [0004] However, these conventionally known sunscreen cosmetics mainly include, as described above, mainly. U.
V. Sunburn is prevented by absorbing ultraviolet light in the B wavelength range, but the effect of preventing sunburn is not always satisfactory. In addition, as an external preparation for effectively preventing inflammation due to sunburn, it not only has no effect at all, but also has a problem of compatibility with other bases, a reduction or coloring of the ultraviolet absorbing ability due to decomposition of the ultraviolet absorbing agent, and Had a problem in terms of safety such as increased skin irritation. On the other hand, various drugs such as vitamin C are used as cosmetics or external preparations for preventing pigmentation, but ultraviolet rays (UV.
However, it has not yet been effective as an external preparation for effectively improving pigmentation of severe symptoms accompanied by inflammation due to region B). Kojic acid, which has been previously developed by the present applicant as an active ingredient for a complexion for external use, is a drug having both of these requirements.
That is, it is known as an ideal whitening agent having an ultraviolet absorbing ability and also having an anti-inflammatory action (for example, JP-B-56-18569, JP-B-61-104747).
JP, JP-B-58-34446, JP-A-55-344
No. 157509). However, although kojic acid has such excellent component characteristics, it has a drawback that it is colored and decomposed with time by ultraviolet rays, and thus its pharmacological action may not be sufficiently exhibited. SUMMARY OF THE INVENTION An 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 together with kojic acid or kojic acid. It is an object of the present invention to provide an external preparation for skin that can exert its original medicinal properties. [0007] Means for Solving the Problems The present inventors, as a result of intensive studies for solving the above problems, Coptis, ON
Di-, Kumaseba, Kurameria, Sabonsou, narcissus, Se
Yarrow, tulip , below mallow,
By combining one or more plant extracts selected from the group consisting of radish, beet, amaryllidaceae, and henna with kojic acid and / or a derivative thereof, their light stability, (light by UVB) Degradability) was improved and a fair-skinned effect was effectively exhibited, and more surprisingly, it was found that a synergistic anti-inflammatory effect was obtained, thereby completing the present invention. [0008] That is, according to the present invention, Coptis, Oh
Mackerel, Kumaseba, Clameria, Soapwort , Narcissus ,
Improvement of photostability of kojic acid or kojic acid derivative, characterized by containing one or more plant extracts selected from the group consisting of yarrow, tulip , below mallow, radishes, beet, gangamana and henna An external preparation for skin having an excellent whitening action and an excellent anti-inflammatory action is provided. 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. A fermentation solution containing kojic acid as a main component obtained by culturing a known 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. used. Examples of the kojic acid derivative include those disclosed in JP-B-60-10005, JP-B1-45472 and JP-B3-74229, and JP-B-58-74229.
No. 22151, JP-B-58-22152, Kojic acid obtained by stabilizing a kojic acid molecule by bonding a saccharide to an esterified product of kojic acid and a -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. Specific plant extracts used in combination with kojic acid and / or its derivatives include the following. [0011] Spinach (Coptis japonica Makino (Ranu
nculaceae)) is a small perennial plant that is often found in the mountains of the Sea of Japan side of Hokkaido and Honshu. Its extract (Japanese Copti
s Extract) is extracted from the rhizome with the roots almost removed from spinach or other congeners,
Those obtained by concentration can be suitably used. Itohimehagi (Polygala tenuifolia Will)
d) is a perennial herb of the smelt family. Onji (Poly
The term "galae Radix" means its root, and as an ondi extract, one obtained by extraction with ethanol, purified water or the like can be suitably used. [0014] Cumaceba is a plant belonging to the genus Platinimisium of the leguminous family, Platinumium trinitatis.
(Platymiscium trinitatis), which has long been used as a tonic. As its extract,
Those extracted with water, ethanol, propylene glycol or the like can be suitably used. [0015] Clameria (Rhatany) is a small shrub from South America, the extract of which is preferably used from its roots. Saponaria officinalis is a perennial herb native to Europe and is a herb that reaches a height of 30 to 60 cm. The extract (Saponaria Extract) includes propylene glycol,
An extract obtained by extracting with 1,3-butylene glycol or an aqueous solution thereof can be suitably used. Narcissus (Narcissus tazetta L. var. Ch)
inensis Roemer) is a perennial herb of the Amaryllidaceae family, and its extract can be suitably used when extracted from bulbs. Achillea millefo
lium L.) is a perennial plant of the Asteraceae family and its extract (Milfoi
l Extract) can be preferably used one extracted from whole grass. [0021] Tulip (Tulipa gesneriana L.)
Is a perennial herb of the lily family and its extract (Tulip Extract
As ()), those extracted from flowers can be suitably used. Below oil (Althaea officinalis)
L.) is native to Europe and native to salty swamps on the eastern Mediterranean coast. It is a perennial plant with a height of 1.5 to 2 m. As the extract (Althea Extract), extract obtained from roots with purified water, 1,3-butylene glycol, propylene glycol, ethanol, or a mixture thereof can be suitably used. The radish is Japanese cabbage radish, and an extract thereof extracted from seeds can be suitably used. Beet (Beta vulgares L.) is a perennial plant belonging to the family Acalyptaceae. As its extract (Beet Extract), those extracted from leaves and stems can be suitably used. Amaryllidaceae (Lycoris radiata Herbert)
Is a perennial herb of the Amaryllidaceae family, the extract of which is obtained by extracting a bulb with purified water or the like can be suitably used. As the henna extract (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 leaves and stems can be suitably used. In the present invention, the amount of the kojic acid and / or a derivative thereof and the plant extract may be in the range of cosmetics such as creams, lotions, emulsions, packs, lotions, essences, ointments, cataplasms and plasters. In any case where it is used as an external preparation such as a preparation, the plant extract is 0.0001 to 20% by weight, preferably 0.01 to 10% by weight, and kojic acid and / or its derivative is contained in the whole preparation. It is added 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. As mentioned above, for example, cataplasms, plasters, pastes, creams, ointments, aerosols, emulsions, It is widely used in known forms as pharmaceuticals such as lotions, emulsions, essences, packs, gels, powders, foundations, sun care, bath salts, quasi-drugs, and cosmetics. When preparing the external preparation of the present invention, various known active ingredients usually used, for example, carpronium chloride, cefanlanthine, vitamin E, vitamin E nicotinate, nicotinic acid, nicotinamide, benzyl nicotinate, Peripheral vasodilators such as ginger tincture and pepper tincture, cooling agents such as camphor and meenthol, antibacterial agents such as hinokitiol, benzalkonium chloride, undecylenic acid, anti-inflammatory agents such as lysozyme chloride, glycyrrhizin, allantoin, ascorbic acid, A fairing agent such as arbutin, a placenta extract, a liver extract, various extracts derived from animals, plants and microorganisms such as a lactic acid bacterium culture extract can be appropriately added and used. The above-mentioned pharmaceuticals, quasi-drugs, and cosmetics include known active ingredients, surfactants, base ingredients such as oils and fats, and, if necessary, known humectants, preservatives, and antioxidants. Agents, UV absorbers / scatterers, chelating agents, pH adjusters,
Various additives such as fragrances and coloring agents can be used in combination. The following are examples and test examples of the effects thereof, which do not limit the present invention in any way. <Test Example 1> Stability test with time Preparation of the following emulsion base containing the active ingredients shown in Table 1 was prepared. (In this test, 100 g of the solvent was added to 10 g of the original plant, After stirring at room temperature for 3 hours, a plant extract evaporated to dryness was used), and the stability test of kojic acid or a kojic acid derivative was performed. The specimen is ultraviolet (UV
-Stored at 50 ° C for 2 months while irradiating. One month after the start of storage, the content of kojic acid or a derivative thereof (kojic acid glucoside as a representative example) was determined for each sample, and the time-dependent change from the test start date was measured. The quantification of the active ingredient was performed by a high performance liquid chromatography (ultraviolet spectrophotometer detector: wavelength 270 nm). Emulsion base (% by weight) used in the test (A) Polyoxyethylene behenyl ether (20E.0.) 0.50 Polyoxyethylene bite tetraoleate (60E.0.) 1.00 Lipophilic type Glycerin monostearate 1.00 Stearic acid 0.50 Behenyl alcohol 0.50 Natural vitamin E 0.02 Preservatives Appropriate amount (B) 1,3-butylene glycol 5.00 Carboxyvinyl polymer 0.01 N-lauroyl-L- Sodium glutamate 0.50 The components belonging to the production method (A) are dissolved by heating (oil phase) and separately (B)
Was dissolved by heating (aqueous phase). The aqueous phase was added to the oil phase, stirred and emulsified, and then cooled to obtain an emulsion base. [0035] <Test Example 2> Inhibition of UV erythema A yellow-brown guinea pig weighing about 300 g was used for the test.
The day before the experiment, the ventral part of the guinea pig was depilated. Experiment 3
A tape with two small holes (diameter 12 mm) was applied to the hair removal part, and an ultraviolet lamp (H-400-F, Toshiba) was set to 20 cm.
Irradiation was performed for 40 seconds from the above distance. Immediately after the irradiation, 50 mg / site of a sample (containing the following cream base and the active ingredient described in Table 2) was applied to the suspension for 30 seconds.
100 ml of a solvent was added to 0 g, and the mixture was stirred at room temperature for 3 hours and then evaporated to dryness. Three hours after ultraviolet irradiation, macroscopic observation was carried out. Three points of erythema with a clear boundary were irradiated, two points of erythema with an indistinct boundary, and one point of slight erythema were observed. Those without erythema were judged as 0 points and compared. Table 2 shows the results. Further, after determining the erythema intensity, the test site was irradiated with UV-B once a day for 90 seconds, 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 consecutive days, and on the 20th day, the degree of coloring of the skin was determined. Test cream base (% by weight) (A) Polyoxyethylene glycol monostearate (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 Preservatives Appropriate amount Flavoring amount Fine amount (B) 1,3-butylene glycol 5.00 Purified water The components belonging to the residue (A) are heated and dissolved (oil phase) and separated. ,
The component belonging to the component (B) was heated and dissolved (aqueous phase). The aqueous phase was added to the oil phase, and the mixture was stirred and emulsified and then cooled to obtain a vanishing cream base. Criteria 3: No pigmentation is observed. 2: Slight pigmentation is observed. 1: Moderate pigmentation is observed. 0: Same as control site (untreated). -1: Stronger pigmentation than control site (untreated) is observed. [0039] [0040] Prescription Examples The following are prescription examples of the present invention. In addition, in the formulation examples, "appropriate amount" means an amount that makes the entire formulation 100% by weight. <Formulation Example 1> Cream (% by weight) 1. Polyethylene glycol monostearate (40E.0.) 2.00 2. Self-emulsifying glyceryl monostearate 5.00 Stearic acid 5.00 4. Behenyl alcohol 1.00 5. Liquid paraffin 10.00 6. Glyceryl trioctanoate 10.00 7. Paraoxybenzoate 0.20 8.1 1,3-butylene glycol 5.00 9. Disodium edetate 0.01 10. Kojic acid 1.00 11. Orange (water extract) 0.50 12. Onji (ethanol extract) 0.10 13. Purified water qs production method A. Heat and dissolve 1-6. B. Heat and dissolve 7-13. C. Add B to A, emulsify, stir and cool. D. After cooling, C is filled into a container, and is used as a product after inspection. Directions and dosage Apply appropriate amount to face. <Formulation Example 2 > Lotion (% by weight) Polyoxyethylene hydrogenated castor oil (60E.0.) 8.00 2. 2. Ethanol 15.00 Kojic acid glucoside 7.00 4. Coomaseva (1: 1 extract of water and propylene glycol) 2.00 5. 5. Clameria (water extract) 0.50 6. Paraoxybenzoic acid ester 0.10 7. citric acid 0.10 Sodium citrate 0.30 9.1,3-butylene glycol 4.00 10. 10. Disodium edetate 0.01 Purified water qs production method A. 1 to 11 are uniformly stirred and dissolved. B. A is filled in a container, and is used as a product after inspection. Directions and dosage Apply appropriate amount to face. <Formulation Example 3 > Ointment (% by weight) 1. Polyethylene glycol monostearate (40E.0.) 2.00 2. Self-emulsifying glyceryl monostearate 5.00 Stearic acid 5.00 4. Behenyl alcohol 1.00 5. Liquid paraffin 10.00 6. Glyceryl trioctanoate 10.00 7. Paraoxybenzoate 0.20 8.1 1,3-butylene glycol 5.00 9. Disodium edetate 0.01 10. Kojic acid 1.00 11. 11. Soap (1,3-butylene glycol extract) 0.10 Sage (propylene glycol extract) 0.40 13. 13. Daffodil (water extract) 1.00 Purified water qs production method A. Heat and dissolve 1-6. B. Heat and dissolve 7-14. C. Add B to A, emulsify, stir and cool. D. After cooling, C is filled into a container, and is used as a product after inspection. Directions and dosage Apply appropriate amount to face. <Formulation Example 5> Poultice (% by weight) Polyacrylic acid 30.00 2. Kojic acid 0.50 3. 3. Achillea millefolium (water extract) 0.10 Maronier (propylene glycol extract) 0.05 5. Tea (ethanol extract) 0.05 6. 6. Sodium polyacrylate 7.00 Aluminum chloride 0.30 8. Concentrated glycerin 20.00 9. 9. Sorbitan monooleate 1.00 Titanium oxide 4.00 11. Purified water Proper quantity production method A. 1 to 5, 9 and 11 are heated and dissolved. B. Heat and dissolve 6 to 8 and 10. C. Add B to A and stir uniformly to mix. D. After cooling, C was applied to a coating agent to obtain a product after inspection. Usage and dosage Remove the liner and apply to the affected area. <Formulation Example 4 > Bath agent (% by weight) Liquid paraffin 65.00 2. 2. Glycerin monostearate di-2-heptylundecanoate 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 Vitamin E 0.20 7. 7. Kojic acid monopalmitate 2.00 Tulip (water extract) 3.00 9. Perfume 1.00 10. Dye fine amount 11. Ethanol qs production method A. 1 to 9 are mixed and dissolved. B. Add 10 to 11 and dissolve. C. Add B to A and stir uniformly. D. C was filled in a soft capsule to obtain a product after inspection. Usage and dosage Put appropriate amount of water in the bathtub. <Formulation Example 5 > Essence (% by weight) 1.1% Carboxyvinyl polymer solution 10.00 Glycerin 20.00 3. 3. Hyaluronic acid 0.50 Ethanol 7.00 5. 5. Kojic acid galactamide 3.00 6. 6. Kojic acid 2.00 7. Below mallow (2: 1 extract of water and ethanol) 1.00 Radish (water extract) 0.20 9. Beet (water extract) 0.10 10. Amaryllidaceae (water extract) 0.01 11. Henna (water extract) 0.01 12. Purified Water Proper Production Method The above components were mixed, uniformly stirred and dissolved to produce an essence. Directions and dosage Apply appropriate amount to face. It was confirmed that each of the skin external preparations of Formulation Examples 1 to 5 was a preparation having an effect satisfying the object of the present invention. According to the present invention, by using kojic acid and / or a derivative thereof in combination with at least one extract of a specific plant, it is possible to stabilize kojic acid and / or a derivative thereof by photolysis. An external preparation for the skin is provided which enhances the properties and exhibits an excellent effect on the ultraviolet erythema suppression action and the like.

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Claims (1)

(57) and [Claims 1] kojic acid and / or derivatives thereof, Coptis, Onji, Kumaseba, Kurameria, Sabonsou, scan
An external preparation for skin, characterized by containing one or more plant extracts selected from the group consisting of narcissus , achillea millefolium, tulip , below-flower, radish, beet, gigantea and henna.