JP2010090069A - Skin-whitening agent and external preparation for skin - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an external preparation for skin and a skin-whitening agent having excellent skin whitening effect and developing excellent effect for decoloring pigmentation, spot, fleck, chloasma, etc., caused by sunburn, and skin whitening effect. <P>SOLUTION: The external preparation for skin and the skin-whitening agent contains extract of one or more plants selected from the group consisting of Aristolochia gigantea belonging to the genus Aristolochia, family Aristolochiaceae; Barringtonia racemosa belonging to the genus Barringtonia, family Lecythidaceae; Crateva falcate belonging to the genus Crateva, family Capparaceae; Cuphea hyssopifolia belonging to the genus Cuphea, family Lythraceae; Hoya carnosa belonging to the genus Hoya, family Asclepiadaceae; Indigofera suffruticosa belonging to the genus Indigofera, family Legumiosae; and Ixora sunkist belonging to the genus Ixora, family Rubiaceae. <P>COPYRIGHT: (C)2010,JPO&INPIT

Description

  The present invention relates to a whitening agent containing a plant extract as an active ingredient, and further to a skin external preparation containing the same. More specifically, the present invention relates to a whitening agent that is effective in preventing and improving pigmentation, stains, freckles, liver spots, etc. after sunburn, and has an excellent effect on skin whitening, and a skin external preparation containing the same. is there.

  Although there are some unclear points about the mechanism of skin blemishes, etc., in general, melanin pigments are formed due to hormonal abnormalities or stimulation of ultraviolet rays from sunlight, which abnormally deposits in the skin. It is considered a thing. This melanin pigment, which causes skin coloration, is produced in melanogenic granules (melanosomes) in melanocytes (melanocytes) between the epidermis and dermis, and the generated melanin diffuses to neighboring cells by osmotic action .

The biochemical reaction in this melanocyte is estimated as follows. That is, the essential amino acid tyrosine becomes dopaquinone by the action of the enzyme tyrosinase, which is converted into black melanin by the enzymatic or non-enzymatic oxidation action is the melanin pigment production process.
As for the above-mentioned whitening agent that suppresses the production of melanin pigment, various plant-derived extracts have been developed in the hope of safety and mildness of irritation to the skin (for example, Patent Documents 1 to 4). reference).

JP-A-8-3109939 JP-A-7-89843 Japanese Patent Laid-Open No. 9-30954 JP 2003-73224 A

  As described above, for plant-derived whitening agents, it is required to find a new plant that exhibits a new whitening effect. Therefore, the present inventors have dealt with such a conventional situation, and an object thereof is to provide a skin external preparation containing a new plant-derived whitening agent and an extract having a whitening effect.

  As a result of intensive studies in view of the present situation, the present inventors have found that a specific plant extract has an excellent whitening effect, and have completed the present invention.

  The present invention includes Aristolochia gristtea, Aristolochia gigantea, Barringtonia racemosa, Crateva, Crateva, and Crateva. Mexican boxwood (Cuphea hyssopifolia), scallops (Hoya) sakuraran (Hoya carnosa), legumes (Indigofera), scallops (Indigofera suffruticosa), scallops (Ixora) A whitening agent comprising an extract of one or more plants selected from the group consisting of:

  The present invention also relates to the Aristolochia glandtea, Aristolochia gigantea, Crateva falcate, Cpheva, Cuphea, and folia hysso. Extract of one or more plants selected from Hoya, Sakuraya (Hoya carnosa), Indigofera (Indigofera), Indigofera suffruticosa, Rubiaceae (Ixora), Ixora sunkist It is a skin external preparation characterized by including.

  The whitening agent of the present invention has an excellent whitening action, and has an excellent effect on lightening and whitening of pigmentation, stains, freckles, and liver spots after sunburn.

  Hereinafter, the present invention will be described in detail. Plants used in the present invention include Aristolochia gristine, Aristolochia gigantea, Barringtonia barringtonia, Barringtonia racemosa, Crateva fate, Crateva (Cuphea) Mexican boxwood willow (Cuphea hyssopifolia), scallop family (Hoya) sakuraran (Hoya carnosa), legume family (Indigofera) nanbankonatsunagi (Indigofera suffruticosa), Rubiaceae sangtanka (Ixora) sunkist).

  Aristolochia gigantea, Aristolochia gigantea, has a bud-like resemblance to a pipe, and some related plants have the name of pipe casserole.

  Barringtonia racemosa is one of the mangrove trees and is called sagaribana because it hangs a little pink flower from white in the middle of summer.

  Crateva falcate is a tree that grows along Okinawa's limestone areas and rivers.

  Cuphea hyssopifolia (Cuphea) is a plant that can be admired by bordering and potting of flower beds.

  Hoya carnosa, a genus of the genus Haga, is a vine and rooted tree that grows on rocks. The flowers are light red and fragrant.

  Indigofera savruticosa (Indigofera) has been cultivated and used mainly in Yaeyama as a raw material for indigo.

  Ixora sunkist (Ixora) is a flowering tree imported for ornamental purposes, and has smaller flowers than Sandanka.

  The plant extract of the present invention has never been reported to have a whitening effect, and was first discovered by the present inventors.

  None of the plants used in the whitening agent of the present invention has been reported to have a whitening effect. In addition, among the plants used in the whitening agent of the present invention, there is no report for external use except for the genus Barringtonia (Barringtonia racemosa).

  The plant extract used in the present invention is obtained by immersing or heating and refluxing the above-mentioned plant leaves, stems, flowers, bark, seeds or fruits, whole plants, etc. together with an extraction solvent, followed by filtration and concentration.

  Among them, Aristolochia gigantea, Sagaribana (Barringtonia racemosa), Sakuraran (Hoya carnosa), Nanban Komatsugi (Indigofera suffruticosa) are preferably extracts from leaves, and Crateva falcate is preferably an extract from leaf stems. Extracts from whole plants are preferred for Ixora sunkist and Mexican cottonwood (Cuphea hyssopifolia).

  The extraction solvent used in the present invention may be any solvent as long as it is usually used for extraction, and in particular, alcohols such as methanol, ethanol and 1,3-butylene glycol, hydrous alcohols, organic solvents such as acetone and ethyl acetate. Can be used alone or in combination, but alcohols such as methanol, ethanol and 1,3-butylene glycol are particularly preferred. An extraction solvent containing a large amount of water is not preferable because extraction of the active ingredient is suppressed. Moreover, in this invention, the skin external preparation can be mix | blended with the 1 or 2 or more types of solvent extract chosen from the said plant.

  The whitening agent of the present invention is a blended material consisting essentially of one or more of the above plant extracts, but may contain other components. This whitening agent is mix | blended with a skin external preparation, and the skin external preparation of this invention is provided.

  The whitening agent of the present invention can be used in various fields, and can be suitably used particularly in the fields of cosmetics, pharmaceuticals, quasi drugs and the like.

  The compounding quantity of the plant extract in the skin external preparation of this invention is 0.0001-5.0 mass% as a dry substance in the external preparation whole quantity, Preferably it is 0.001-1.0 mass%. When the amount is less than 0.0001% by mass, the effect referred to in the present invention is not sufficiently exerted, and when it exceeds 5.0% by mass, it is not preferable because it is difficult to formulate, and a significant improvement in the effect is not observed.

  The skin external preparation of the present invention is produced by blending the whitening agent according to the present invention with the base of the skin external preparation. In addition to the essential components described above, the external preparation for skin of the present invention includes components that are usually used in external preparations for skin, such as cosmetics and pharmaceuticals, such as moisturizers, antioxidants, oily components, ultraviolet absorbers, surfactants, A viscous agent, alcohols, a powder component, a colorant, an aqueous component, water, various skin nutrients, and the like can be appropriately blended as necessary.

  Others, disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, sequestering agents such as gluconic acid, caffeine, tannin, verapamil, tranexamic acid and its derivatives, licorice extract, grabrizine , Hot water extract of fire spine fruit, various herbal medicines, drugs such as tocopherol acetate, glycyrrhizic acid and its derivatives or salts thereof, vitamin C, magnesium ascorbate phosphate, glucoside ascorbate, arbutin, kojic acid, alkoxysalicylic acid and / Or other whitening agents such as salts thereof, saccharides such as glucose, fructose, mannose, sucrose, trehalose and the like can be appropriately blended.

  The skin external preparation of the present invention may be any one as long as it is used in conventional skin external preparations such as ointments, creams, emulsions, lotions, packs, bath preparations, etc., and the dosage form is not particularly limited.

The present invention will be described in more detail with reference to the following examples, but the present invention is not limited thereto. Unless otherwise specified, the amount is shown in mass%.
Prior to the examples, the test method and the results regarding the melanin production inhibitory effect of the plant extract of the present invention will be described.

1. Sample Preparation The following plants used in this example were all from Okinawa, but are not limited thereto.
(1) 72 mL of methanol was added to 7.18 g of Aristolochia gigantea leaves, and after immersion for 7 days at room temperature, methanol in the filtrate was distilled off to obtain 1.093 g of a dry solid.
(2) 72 mL of methanol was added to 7.16 g of the leaves of Barringtonia racemosa, immersed for 7 days at room temperature, and then filtered. The methanol in the filtrate was distilled off to obtain 0.910 g of a dry solid.
(3) 71 mL of methanol was added to 7.03 g of leaves and stems of Crateva falcata, and after immersion for 7 days at room temperature, filtration was performed. The methanol in the filtrate was distilled off to obtain 0.712 g of a dry solid.
(4) 71 mL of methanol was added to 7.03 g of the whole plant of Cuphea hyssopifolia, and it was immersed for 7 days at room temperature and then filtered. The methanol in the filtrate was distilled off to obtain 0.761 g of a dry solid.
(5) 69 mL of methanol was added to 6.84 g of leaves of Hoya carnosa, and after soaking for 7 days at room temperature, filtration was performed. The methanol in the filtrate was distilled off to obtain a dry solid 0.397.
(6) 49 mL of methanol was added to 4.88 g of leaves of Indigofera suffruticosa, and after immersion for 7 days at room temperature, filtration was performed. The methanol in the filtrate was distilled off to obtain 0.541 g of a dry solid.
(7) 63 mL of methanol was added to 6.28 g of whole plant of Ixora sunkist, and after immersion for 7 days at room temperature, it was filtered. The methanol in the filtrate was distilled off to obtain 1.037 g of a dry solid.

2. Melanin production inhibitory effect test method and the results The resulting plant methanol extract was used as a test sample, and the melanin production inhibitory effect was measured and evaluated by the following method.

(1) Cell culture method Mouse-derived B16 melanoma culture cells were used. The cells were cultured in an Eagle's MEM medium containing 10% FBS in a CO ₂ incubator (95% air, 5% carbon dioxide) at 37 ° C. After 24 hours of culturing, the sample solution was added so that the final concentration (concentration in terms of dried extract) was 10 ppm and 30 ppm, and the culture was further continued for 3 days. The cytotoxicity and melanin production were measured by the following methods.

(2) Measurement of cytotoxicity The medium was aspirated and removed 3 days after the addition of the test substance solution, and then an E-MEM medium containing 10% Alama Blue solution was added and reacted at 37 ° C. After 30 minutes, fluorescence was measured at an excitation wavelength of 544 nm and a measurement wavelength of 590 nm, and the relative value of the number of cells was taken as the relative value of the number of cells. Was calculated. The higher the% cell number, the lower the cytotoxicity. When it was less than 80%, it was judged as “toxic”.

(3) Measurement of the amount of melanin The medium is removed by suction, washed 3 times with a buffer (phosphate buffer 50 mM, pH 6.8), 1M NaOH is added to lyse the cells, and the absorbance at 475 nm is measured. did. Using this value as a relative value of the melanin amount, the melanin amount ratio (%) of the test substance added group to the test substance non-added group (only the solvent added) was calculated. The lower the melanin content ratio, the higher the melanin production inhibitory effect.
The results of the melanin ratio (%) using each plant extract are shown in Table 1. Table 1 shows the amount of melanin when each plant extract is added as a percentage based on the amount of control melanin. A case where only a solvent containing no plant extract was added was used as a control.

Table 1 shows that the plant extracts used in the present invention all have an excellent melanin-inhibiting action and are useful as whitening agents.
Below, the formulation example of the skin external preparation by this invention of various dosage forms is demonstrated as an Example.

Formulation Example 1 Lotion Mass%
Trimethylglycine 1.0
This whitening agent (Aristolochia extract dry residue) 1.0
Glycerin 1.0
1,3-butylene glycol 5.0
Sodium alginate 0.1
Ethyl alcohol 5.0
Polyoxyethylene polyoxypropylene decyl tetradecyl ether 0.2
Sodium hexametaphosphate Appropriate amount Citric acid Appropriate amount Sodium citrate Appropriate amount Phenoxyethanol Appropriate perfume Appropriate amount Purified water Residue

Formulation Example 2 Lotion Mass%
Whitening agent (residue of Sabagaribana extract) 5.0
Glycerin 2.0
1,3-butylene glycol 4.0
Polyoxyethylene methyl glucoside 1.0
PEG / PPG-14 / 7 dimethyl ether 3.0
Erythritol 1.0
Polyoxyethylene hydrogenated castor oil 0.5
Polyglyceryl diisostearate 0.3
Triethylhexanoin 0.3
EDTA 3 sodium appropriate amount citric acid appropriate amount sodium citrate appropriate amount phenoxyethanol appropriate amount purified water remainder

Formulation Example 3 Lotion Mass%
Tranexamic acid 1.0
4-methoxysalicylate potassium 1.0
Lipoic acid 0.1
Clam leaf extract 0.1
Hipotaurine 0.1
Clara extract 0.1
Tounin extract 0.1
Beech bud extract 0.1
This whitening agent (Kobano Sandanka extract dry residue) 0.01
Magnesium ascorbate phosphate 0.1
Thiotaurine 0.1
Green tea extract 0.1
Western mint extract 0.1
Iris Root Extract 1.0
Trimethylglycine 1.0
Glycerin 1.0
1,3-butylene glycol 5.0
Hydroxyethyl cellulose 0.05
Ethyl alcohol 5.0
Polyoxyethylene polyoxypropylene decyl tetradecyl ether 0.2
EDTA 3 sodium appropriate amount citric acid appropriate amount sodium citrate appropriate amount phenoxyethanol appropriate amount perfume appropriate amount purified water residue

Formulation Example 5 Latex Mass%
Dipotassium glycyrrhizinate 0.05
Tocopherol acetate 0.5
Whitening agent (Mexico boxwood extract dry residue) 0.0005
Sodium L-glutamate 0.05
Fennel extract 0.1
Yeast extract 0.1
Giant extract 0.1
Hydroxypropyl-β-cyclodextrin 0.1
Glycerin 6.0
1,3-butylene glycol 5.0
Polyoxyethylene methyl glucoside 3.0
Sunflower oil 1.0
Squalane 2.0
Isododecane 4.0
Dimethylpolysiloxane 3.0
Xanthan gum 0.1
Carboxyvinyl polymer 0.1
Acrylic acid / alkyl methacrylate copolymer 0.1
Ethyl alcohol 5.0
Potassium hydroxide Appropriate amount Sodium hexametaphosphate Appropriate amount Bengala Appropriate amount Yellow iron oxide Appropriate amount Ethylparaben Appropriate perfume Appropriate amount Purified water Residue

Formulation Example 6 Daytime Milk Emulsion Mass%
Dipotassium glycyrrhizinate 0.1
This whitening agent (Nanbankonatsu extract dry residue) 0.005
Tocopherol acetate 0.1
1,3-butylene glycol 5.0
Squalane 0.5
Isododecane 10.0
Isohexadecane 25.0
Dimethylpolysiloxane 2.0
Polyoxyethylene / methylpolysiloxane copolymer 1.5
Trimethylsiloxysilicic acid 1.0
4-t-butyl-4′-methoxydibenzoylmethane 1.0
2-Ethylhexyl paramethoxycinnamate 5.0
Diparamethoxycinnamate mono-2-ethylhexanoate glyceryl 1.0
Silicone coated fine particle titanium oxide 4.0
Dimethyl distearyl ammonium hectorite 0.5
Spherical polyethylene powder 3.0
Talc 5.0
EDTA 3 sodium appropriate amount phenoxyethanol appropriate amount perfume appropriate amount purified water remainder

Formulation Example 7 Latex Mass%
L-Arginine 0.1
Royal Jelly Extract 0.1
Yeast extract 0.1
This whitening agent (Sakuraran extract dry residue) 0.005
Stearyl glycyrrhetinate 0.05
Tocopherol acetate 0.1
Acetylated sodium hyaluronate 0.1
Glycerin 5.0
Dipropylene glycol 7.0
Polyethylene glycol 1500 2.0
Liquid paraffin 7.0
Vaseline 3.0
Behenyl alcohol 1.0
Batyl alcohol 2.0
Jojoba oil 1.0
Stearic acid 0.5
Isostearic acid 0.5
Behenic acid 0.5
Tetra-2-ethylhexanoic acid pentaerythritol 3.0
Cetyl 2-ethylhexanoate 3.0
Glycerol monostearate 1.0
Polyoxyethylene glycerol monostearate 1.0
Carboxyvinyl polymer 0.15
Sodium hexametaphosphate Appropriate potassium hydroxide Appropriate methylparaben Appropriate fragrance Appropriate purified water Residual

Formulation Example 8 Latex Mass%
Ascorbic acid glucoside 1.5
Tranexamic acid 1.0
Tocopherol acetate 0.1
Sodium hyaluronate 0.05
This whitening agent (Gyoboku extract dry residue) 0.0003
Pantothenyl ethyl ether 0.1
Stearyl glycyrrhetinate 0.1
Glycerin 7.0
1,3-butylene glycol 5.0
Polyethylene glycol 20000 0.5
Vaseline 2.0
Jojoba oil 3.0
Squalane 2.0
Phytosteryl hydroxystearate 0.5
Behenyl alcohol 0.5
Batyl alcohol 0.2
Dimethylpolysiloxane 2.0
Tetra-2-ethylhexanoic acid pentaerythrit 0.1
Polyoxyethylene hydrogenated castor oil 1.0
Polyoxyethylene glyceryl isostearate 3.0
4-t-butyl-4'-methoxydibenzoylmethane 0.1
Diparamethoxycinnamic acid mono-2-ethylhexanoate glyceryl 0.1
Xanthan gum 0.1
Carboxyvinyl polymer 0.2
Ethanol 5.0
Potassium hydroxide Appropriate amount Sodium pyrosulfite Appropriate amount Sodium hexametaphosphate Appropriate amount EDTA 3 sodium Appropriate amount Yellow iron oxide Appropriate amount Paraoxybenzoate Appropriate amount Purified water

Formulation Example 9 Cream Mass%
Whitening agent (dry residue of Aristolochia extract) 0.0005
Potassium 4-methoxysalicylate 3.0
Propylene glycol 5.0
Glycerin 8.0
Stearic acid 2.0
Stearyl alcohol 7.0
Hydrogenated Lanolin 2.0
Squalane 5.0
2-Octyldodecyl alcohol 6.0
Polyoxyethylene cetyl alcohol ether 3.0
Glycerin monostearate ester 2.0
Potassium hydroxide appropriate amount ethyl paraben appropriate amount perfume appropriate amount ion-exchanged water remainder

Formulation Example 10 Cream Mass%
4-methoxysalicylate potassium 1.0
3-O-ethylascorbic acid 1.0
This whitening agent (dried residue of Sagaribana extract) 0.0001
Coenzyme Q10 0.03
Tranexamic acid 2.0
Tocopherol acetate 0.1
Sodium hyaluronate 0.05
Pantothenyl ethyl ether 0.1
Stearyl glycyrrhetinate 0.1
Glycerin 7.0
1,3-butylene glycol 5.0
Polyethylene glycol 20000 0.5
Vaseline 2.0
Behenyl alcohol 0.5
Batyl alcohol 0.2
Squalane 2.0
Phytosteryl hydroxystearate 0.5
Jojoba oil 3.0
Tetra-2-ethylhexanoic acid pentaerythrit 1.0
Dimethylpolysiloxane 2.0
Polyoxyethylene glyceryl isostearate 1.5
Polyoxyethylene hydrogenated castor oil 1.0
Carboxyvinyl polymer 0.2
Xanthan gum 0.1
Ethanol 5.0
Sodium hexametaphosphate Appropriate amount Yellow iron oxide Appropriate amount EDTA3 sodium Appropriate amount Potassium hydroxide Appropriate amount Paraoxybenzoate Appropriate amount Purified water Residue

Formulation Example 11 Two-layer type daytime milk emulsion
Tranexamic acid 2.0
4-methoxysalicylate potassium 1.0
This whitening agent (cobano sandanka extract dry residue) 0.0001
Dipotassium glycyrrhizinate 0.02
Glutathione 1.0
Thiotaurine 0.05
Clara extract 1.0
Dipropylene glycol 5.0
Dimethylpolysiloxane 5.0
Isohexadecane 25.0
Polyoxyethylene / methylpolysiloxane copolymer 2.0
Dimethyl distearyl ammonium hectorite 0.5
Butylethylpropanediol 0.5
2-Ethylhexyl paramethoxycinnamate 7.5
Trimethylsiloxysilicate 5.0
Spherical polyalkyl acrylate powder 5.0
Dextrin palmitate coated fine particle zinc oxide 15.0
EDTA3 sodium appropriate amount methylparaben appropriate amount phenoxyethanol appropriate amount perfume appropriate amount purified water remainder

Formulation Example 12 Gel Mass%
Potassium 4-methoxysalicylate 0.1
Nettle extract 0.1
This whitening agent (Mexico boxwood extract dry residue) 0.0003
Dipotassium glycyrrhizinate 0.1
Ascorbic acid glucoside 2.0
Tocopherol acetate 0.1
Ogon Extract 0.1
Yukinoshita extract 0.1
Glycerin 2.0
1,3-butylene glycol 5.0
Polyethylene glycol 1500 3.0
Polyethylene glycol 20000 3.0
Agar powder 1.5
Xanthan gum 0.3
Acrylic acid / alkyl methacrylate copolymer 0.05
Cetyl octanoate 3.0
Dimethylpolysiloxane 5.0
Sodium hexametaphosphate Appropriate amount Dibutylhydroxytoluene Appropriate amount Yellow iron oxide Appropriate amount Citric acid Appropriate amount Sodium citrate Appropriate amount Sodium hydroxide Appropriate amount Phenoxyethanol Appropriate perfume Appropriate amount Purified water Residue

Claims (2)

  Aristolochia gristine (Aristolochia gigantea), Sagaribana (Barringtonia) Sagaribana (Barringtonia racemosa), Cleetaceae (Crateva) selected from the group consisting of hyssopifolia), Hoya carnosa, Legumaceae, Indigofera, Indigofera suffruticosa, Ixora, Ixora sunkist A whitening agent comprising one or more plant extracts.   Aristolochia Aristolochia gigantea, Aristolochia gigantea, Crateva, Crateva falcate, Candva, Cuphea, H, and H It contains one or more plant extracts selected from carnosa), legumes Indigofera sambaruin (Indigofera suffruticosa), Ixora sunkist, Ixora sunkist A topical skin preparation.