JPH0930929A - Skin preparation for external use - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a skin preparation for external use having the action to inhibit melanin formation and tyrosinase activity and prevent and ameliorate the pigmentation, spots and freckles after sunburn and liver spots. SOLUTION: A plant in Woodfordia in Lythreceae, particularly Sidowayah (Woodfordia fructicosa) growing in the savanna or stock farms in Indonesia is extracted and the extract is used as an active ingredient in an amount of 0.005-20wt.%, preferably 0.01-10wt.%, on the dry basis in the total skin preparation. In addition, conventional skin color lightener, moisturizer, antioxidant, oily components, ultraviolet absorber, surfactant, thickener, alcohols, powdery components, colorants, aqueous components, water and a variety of skin nutrients are appropriately formulated to prepare ointment, cream, emulsion, lotion, pack, bath medicine and the like All of the whole plant bodies such as flower, leaf, stem are soaked in an extractant such as methanol or they are heated under reflux, then the soaking or extraction solution is filtered and concentrated to give this extract.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION The present invention relates to Lythraceae
The present invention relates to a skin external preparation effective by inhibiting the formation of melanin by incorporating an extract of a plant of the genus Woodfordia, and preventing and improving pigmentation, spots, freckles, chloasma, etc. after sunburn.

[0002]

2. Description of the Related Art Although there are some unclear points about the mechanism of the occurrence of skin spots and the like, melanin pigments are generally formed due to hormonal abnormalities and stimulation of ultraviolet rays from sunlight. It is believed to be abnormally deposited within. This melanin pigment, which causes skin coloring, is produced in melanin-producing granules (melanosomes) in melanocytes (melanocytes) between the epidermis and dermis,
The generated melanin diffuses into adjacent cells by the osmotic effect. The biochemical reaction in this melanocyte is presumed to be as follows. That is, tyrosine, which is an essential amino acid, is converted into dopaquinone by the action of the enzyme tyrosinase, and the process in which it is converted to black melanin via a red pigment and a colorless pigment by an enzymatic or non-enzymatic oxidative action is a melanin pigment production process. Therefore, suppressing the action of tyrosinase, which is the first step of the reaction, is important for suppressing melanin production.

[0003]

However, compounds that suppress the tyrosinase action, except for hydroquinone, have very slow onset of their effects, so that the effect of improving skin pigmentation is not sufficient. On the other hand, although hydroquinone is recognized as having an effect, its use is generally restricted because of its sensitizing properties. Therefore, in order to improve its safety, attempts have been made to use higher fatty acid monoesters or alkyl monoethers (JP-A-58-154507), but the esters are decomposed by a hydrolase in the body. Therefore, it is not always safe, and ethers have not been sufficiently satisfactory in terms of safety.

[0004]

The inventors of the present invention investigated the melanin production inhibitory effect of various substances as a solution to these problems, and as a result, Lythra
The present inventors have found that an extract of a plant of the genus Woodfordia of the family Ceae) has a melanin production inhibitory action and a tyrosinase inhibitory action, and completed the present invention. Lysoraceae (Lythraceae) Udfordia (W
There has been no report about the melanin production inhibitory action of extracts of the oodfordia) plant, and its application to external preparations for skin has not been known at all. The present inventors have completed the present invention based on the above findings.

That is, the present invention relates to Lythracea
e) A skin external preparation characterized by containing an extract of a plant of the genus Woodfordia.

The structure of the present invention will be described in detail below. The plant of the genus Woodfordia of the family Lythraceae used in the present invention is Sidowaya (S
Idowayah, scientific name: Woodfordia fruticosa) is suitable. These are plants that grow especially on dry grasslands and pastures in Indonesia. The extract used in the present invention is obtained by immersing or heating and refluxing whole plants such as flowers, leaves, stems including rhizomes, fruits, etc. with the extraction solvent, filtering and concentrating. The extraction solvent used in the present invention is not particularly limited as long as it is a solvent usually used for extraction. In particular, an organic solvent such as alcohols such as methanol and ethanol, aqueous alcohols, acetone, and ethyl acetate is used alone or in combination. Can be.

In the present invention, the compounding amount of the extract of the plant of the genus Woodfordia of the family Lythraceae is 0.005 to 20% as a dry product in the total amount of the external preparation.
It is 0% by weight, preferably 0.01 to 10.0% by weight. If the amount is less than 0.005% by weight, the effects of the present invention are not sufficiently exhibited, and if the amount is more than 20.0% by weight, it is not preferable because formulation is difficult. Further, even if the content is 10.0% by weight or more, the effect is not so much improved.

In addition to the above-mentioned essential components, the external preparation for skin of the present invention is a component that is usually used in external preparations for skin such as cosmetics and pharmaceuticals, for example, other whitening agents, moisturizers, antioxidants and oily components. , UV absorber, surfactant, thickener,
Alcohols, powder components, coloring materials, aqueous components, water, various skin nutrients and the like can be appropriately blended as necessary.

In addition, sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, gluconic acid, caffeine, tannin, verapamil, tranexamic acid and its derivatives, licorice extraction Substance, glabridin, hot water extract of fruits of fire thorns, various crude drugs, tocopherol acetate,
Drugs such as glycyrrhizic acid and its derivatives or salts thereof, vitamin C, magnesium ascorbate phosphate,
Other whitening agents such as ascorbic acid glucoside, arbutin, kojic acid, glucose, fructose, mannose,
Sugars such as sucrose and trehalose can also be appropriately blended.

The external preparation for skin of the present invention may be any ointment, cream, emulsion, lotion, pack, bath agent or the like as long as it is a conventional external preparation for skin, and its form is not particularly limited.

[0011]

Next, the present invention will be described in more detail by way of examples. Note that the present invention is not limited by this. The blending amount is% by weight. Prior to Examples, test methods and results of the melanin suppressing effect, tyrosinase activity inhibiting effect and whitening effect of the plant extract of the present invention will be described.

Test Method and Results 1. Sample preparation (1) Sidowayah (scientific name: Woodfordia
Fruticosa) extract 50 g of flower parts of Sidowayah were immersed in methanol at room temperature for 4 days, and the extract was concentrated to obtain 5.8 g of a methanol extract. This extract was dissolved in DMSO at 1%, the concentration was adjusted by diluting this solution, and the following experiment was performed using this.

2. Cell culture method B16 melanoma cultured cells derived from mice were used. 1
0% FBS and theophylline (0.09 mg / ml)
The cells were cultured in an Eagle MEM medium containing C.sub.2 in a CO.sub.2 incubator (95% air, 5% carbon dioxide) at 37.degree. After 24 hours of culturing, the sample solution was added so that the final concentration (concentration of extracted dry matter) was 10 −2 to 10 −5% by weight, and the culturing was continued for another 3 days. The determination and the tyrosinase activity inhibitory effect were measured.

3. Visual perception of melanin amount Place a diffusion plate on the lid of the well plate and observe the intracellular melanin amount with an inverted microscope.
e) The comparison was made with the sample (standard) to which the extract of the plant of the genus Woodfordia was not added. The results are shown in Table 1. In addition, as a reference example, the same test as above was carried out on an extract of Kaigai (Lamiaceae, Odorikosou Subfamily), which is already known to have an action of suppressing melanin production. Table 1 also shows the results. Further, in the table, "toxic" means that it is cytotoxic.

<Judgment Criteria> ◯: White (amount of melanin) Δ: Slightly white (amount of melanin) ×: Reference (amount of melanin)

4. Measurement of tyrosinase activity Before measurement, the medium in the wells is removed and washed twice with 100 μl of PBS. 45 μl of 1% Triton-X in each well
(Rohm and Haas product name, surfactant) containing PBS is added. Shake the plate for 1 minute, break the cell membrane well, and use a microplate reader for 475n.
The absorbance at m was measured, and this was taken as the absorbance at 0 minutes. Then, 5 μl of 10 mM L-DOPA solution was quickly added, and the mixture was transferred to an incubator at 37 ° C. and reacted for 60 minutes. The plate was shaken for 1 minute, and the absorbance (475 nm) at 60 minutes was measured. The tyrosinase activity ratio (%) was defined as the ratio of the absorbance difference of the sample with the plant extract to the absorbance difference between the time of 0 minute and the time of 60 minutes in the case of the sample to which no plant extract was added (control). Table 1 shows the results. Further, as a reference example, the same test as above was carried out on an ethanol extract of mussel, which is already known to have a tyrosinase activity inhibitory action. Table 1 also shows the results. In the table, "toxic" means that cytotoxicity was observed, and "-" means that no significant difference was observed within a risk rate of 5% as compared with the control.

[0017]

[Table 1] Test Melanin production Visual evaluation Tyrosinase activity rate (%) Concentration (% by weight) 10-5 10-4 10-3 10-2 10-5 10-4 10-3 10-2 Sidowaya extract △ ○ ○ Toxicity 74 61 45 Toxicity Kaigai extract × × × × − − − 55

5. Whitening test [Test method] 40 subjects exposed to sunlight in summer for 4 hours (2 hours per day for 2 days) each sample from 5 days after the day of sun exposure to the skin of the upper arm inner skin Was applied once each morning and evening for 4 weeks. The panel was divided into 8 groups, and 5 groups were prepared, and the tests were conducted according to the formulations shown below. (Alcohol phase) 95% Ethyl alcohol 55.0% by weight Polyoxyethylene (25 mol) hydrogenated castor oil ether 2.0 Antioxidant / preservative proper amount Fragrance proper amount drug (listed in Table 2) (water phase) glycerin 5.0 Sodium hexametaphosphate Suitable amount Ion-exchanged water Residue <Production method> An aqueous phase and an alcohol phase are prepared, respectively, and then both are mixed and solubilized.

[Evaluation Method] The lightening effect after use was judged based on the following judgment criteria. <Judgment criteria> ：: When the ratio showing significant effect and effectiveness among the subjects is 80% or more 割 合: The ratio showing significant effect and effectiveness among the subjects is 50% or more
Less than 80% △: The proportion of the test subjects showing excellent and effective is 30% or more
When less than 50% x: When the ratio of markedly effective or effective among the subjects is less than 30%

Samples having the blending composition described in the above test method were prepared and the whitening effect was compared using the agents shown in Table 2.
The results are shown in Table 2.

[0021]

[Table 2]

The Sidowayaya extract in Table 2 was obtained by heating and reducing flowers in ethanol, filtering and concentrating and drying.

As is clear from Table 2, the effect after exposure to sunlight was found to be that the addition of the Sidowaya extract prevented excessive melanin pigment deposition and prevented darkening. It was

Example 1 Cream (Formulation) Stearic acid 5.0% by weight Stearyl alcohol 4.0 Isopropyl myristate 18.0 Glycerin monostearate 3.0 Propylene glycol 10.0 Sidowaya methanol extract 0.01 Caustic potash 0.2 Sodium bisulfite 0.01 Preservative Suitable amount Fragrance Suitable amount Ion-exchanged water Residual (production method) Propylene glycol, Sidowaya methanol extract and caustic potash are added to ion-exchanged water and dissolved, and heated to 70 ° C (water phase) ). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is gradually added to the water phase, and after the addition is completed, the temperature is maintained for a while to cause a reaction. Then, it is uniformly emulsified with a homomixer and cooled to 30 ° C. with thorough stirring.

Example 2 Cream (Formulation) Stearic acid 2.0% by weight Stearyl alcohol 7.0 Hydrogenated lanolin 2.0 Squalane 5.0 2-Octyldodecyl alcohol 6.0 Polyoxyethylene (25 mol) cetyl alcohol ether 3.0 Glycerin monostearate 2.0 Propylene glycol 5.0 Sidowaya ethanol extract 0.05 Sodium bisulfite 0.03 Ethylparaben 0.3 Fragrance suitable amount Ion-exchanged water Residual (production method) Propylene glycol in ion-exchanged water And add
Heat and maintain at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is added to the aqueous phase to carry out preliminary emulsification, and the mixture is uniformly emulsified with a homomixer and then cooled to 30 ° C. with thorough stirring.

Example 3 Cream (Formulation) Solid paraffin 5.0% by weight Beeswax 10.0 Vaseline 15.0 Liquid paraffin 41.0 Glycerin monostearate 2.0 Polyoxyethylene (20 mol) sorbitan monolaurate 2 0.0 Soap powder 0.1 Borax 0.2 Sidowaya acetone extract 0.05 Sodium hydrogen sulfite 0.03 Ethylparaben 0.3 Perfume proper amount Ion-exchanged water Residual (production method) Soap powder and borax are added to ion-exchanged water, Melt by heating and keep at 70 ° C (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is gradually added to the aqueous phase while stirring to carry out the reaction. After the reaction is completed, the mixture is uniformly emulsified with a homomixer, and after emulsification, the mixture is cooled to 30 ° C. with thorough stirring.

Example 4 Emulsion (formulation) Stearic acid 2.5 wt% Cetyl alcohol 1.5 Vaseline 5.0 Liquid paraffin 10.0 Polyoxyethylene (10 mol) monooleate 2.0 Polyethylene glycol 1500 3. 0 triethanolamine 1.0 carboxyvinyl polymer 0.05 (trade name: Carbopol 941, BFGoodrich Chemical company) Sidowaya acetic acid ethyl ester extract 0.01 sodium bisulfite 0.01 ethylparaben 0.3 perfume proper amount ion-exchanged water Residual (manufacturing method) The carboxyvinyl polymer is dissolved in a small amount of ion-exchanged water (phase A). Polyethylene glycol 1500 and triethanolamine are added to the remaining ion-exchanged water, dissolved by heating, and kept at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is added to the water phase to perform preliminary emulsification, the phase A is added, and the mixture is uniformly emulsified with a homomixer. After the emulsification, the mixture is cooled to 30 ° C. while stirring well.

Example 5 Emulsion (Formulation) Microcrystalline wax 1.0% by weight Beeswax 2.0 Lanolin 20.0 Liquid paraffin 10.0 Squalane 5.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 mol) ) Sorbitan monooleate 1.0 Propylene glycol 7.0 Sidowaya acetone extract 10.0 Sodium hydrogen sulfite 0.01 Ethylparaben 0.3 Perfume suitable amount Ion-exchanged water Residue (production method) Add propylene glycol to ion-exchanged water ,
Heat and maintain at 70 ° C. (aqueous phase). The other components are mixed, heated and melted and kept at 70 ° C. (oil phase). While stirring the oil phase, the aqueous phase is gradually added thereto, and the mixture is uniformly emulsified with a homomixer. After emulsification, cool to 30 ° C with good stirring.

Example 6 Jelly (formulation) 95% ethyl alcohol 10.0 wt% dipropylene glycol 15.0 polyoxyethylene (50 mol) oleyl alcohol ether 2.0 carboxyvinyl polymer 1.0 (trade name: Carbopol 940, BFGoodrich Chemical company) Caustic soda 0.15 L-arginine 0.1 Sidowaya 50% ethanol aqueous solution extract 7.0 2-Hydroxy-4-methoxybenzophenone sulfonate sodium 0.05 Ethylenediaminetetraacetate / 3sodium / dihydrate 0 .05 Methylparaben 0.2 Fragrance Appropriate amount Ion-exchanged water Residual (production method) Carbopol 940 was uniformly dissolved in ion-exchanged water, while Sidowaya 50% ethanol aqueous solution extract and polyoxyethylene (50 mol) oleyl in 95% ethanol. Arcor Was dissolved ether, is added to the aqueous phase.
Next, after adding other components, the mixture is neutralized with caustic soda and L-arginine to increase the viscosity.

Example 7 Beauty Serum (Formulation) (Phase A) Ethyl Alcohol (95%) 10.0% by Weight Polyoxyethylene (20 mol) Octyldodecanol 1.0 Pantotenyl Ethyl Ether 0.1 Sidowaya Methanol Extraction Substance 1.5 Methylparaben 0.15 (Phase B) Potassium hydroxide 0.1 (Phase C) Glycerin 5.0 Dipropylene glycol 10.0 Sodium hydrogen sulfite 0.03 Carboxyvinyl polymer 0.2 (trade name: Carbopol 940, BFGoodrich Chemical company) Purified water Residue (production method) Phases A and C are uniformly dissolved, and A is added to phase C.
Add phases and solubilize. Next, after adding the phase B, filling is performed.

Example 8 Pack (formulation) (Phase A) Dipropylene glycol 5.0% by weight Polyoxyethylene (60 mol) hydrogenated castor oil 5.0 (Phase B) Sidowaya methanol extract 0.01 Olive oil 5. 0 Tocopherol acetate 0.2 Ethylparaben 0.2 Perfume 0.2 (Phase C) Sodium hydrogen sulfite 0.03 Polyvinyl alcohol 13.0 (Saponification degree 90, degree of polymerization 2,000) Ethanol 7.0 Purified water Residual ( Manufacturing method) A phase, B phase, and C phase are uniformly dissolved, respectively.
Add phase B to phase and solubilize. Next, this is added to the C phase and then filled.

Example 9 Solid Foundation (Formulation) Talc 43.1% by weight Kaolin 15.0 Sericite 10.0 Zinc white 7.0 Titanium dioxide 3.8 Yellow iron oxide 2.9 Black iron oxide 0.2 Squalane 8 0.0 Isostearic acid 4.0 POE sorbitan monooleate 3.0 Isocetyl octanoate 2.0 Sidowaya ethanol extract 1.0 Preservative proper amount Fragrance appropriate amount (manufacturing method) Talc to black iron oxide powder components are thoroughly mixed with a blender. Then, an oily component of squalane to isocetyl octoate, an ethanol extract of Sidowaya, an antiseptic and a fragrance are added, and the mixture is well kneaded and then filled into a container and molded.

Example 10 Emulsion type foundation (cream type) (Formulation) (Powder part) Titanium dioxide 10.3% by weight Sericite 5.4 Kaolin 3.0 Yellow iron oxide 0.8 Bengala 0.3 Black iron oxide 0.2 (oil phase) decamethylcyclopentasiloxane 11.5 liquid paraffin 4.5 polyoxyethylene-modified dimethylpolysiloxane 4.0 (water phase) purified water 50.0 1,3-butylene glycol 4.5 side Waya ethanol extract 1.5 Sorbitan sesquioleate 3.0 3.0 Preservative proper amount Perfume proper amount (Production method) After heating and stirring the aqueous phase, a powder portion thoroughly mixed and pulverized is added and treated with a homomixer. Further, the oil phase mixed by heating is added, and the mixture is treated with a homomixer. Then, a fragrance is added with stirring, and the mixture is cooled to room temperature.

[0034]

Industrial Applicability As described above, the external preparation for skin of the present invention has a melanin production inhibitory action and a tyrosinase activity inhibitory action, and causes pigmentation, stains, freckles, melasma, etc. after sunburn. It has an excellent whitening effect and also has excellent safety.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification code Internal reference number FI Technical display location A61K 35/78 AED A61K 35/78 AEDC // C12N 9/99 C12N 9/99 (72) Inventor Masako Naganuma 1050 Shinba-cho, Kohoku-ku, Yokohama-shi, Kanagawa Shiseido Daiichi Research Center Co., Ltd.

Claims (3)

[Claims] 1. An external preparation for skin, comprising an extract of a plant of the genus Woodfordia of the family Lythraceae. 2. A plant of the genus Woodfordia of the family Lythraceae is Sidowaya.
ah, scientific name: Woodfordia fruticosa), The external preparation for skin according to claim 1. 3. The compounding amount of the extract of the plant of the genus Woodfordia of the family Lythraceae is 0.00.
The external preparation for skin according to claim 1, which is 5 to 20.0% by weight.