JPH0812560A - Skin external preparation - Google Patents

Abstract

PURPOSE:To obtain a skin external preparation having suppressing actions on melanogenesis and inhibiting actions on tyrosinase activities, excellent in lightening of the color, beautifying and whitening of pigmentation, dermal stains, ephelides, chloasmata, etc., after sunburn, excellent in safety and useful as an ointment, a cream, etc., for beautifying and whitening by blending an extract of Copaiba therein. CONSTITUTION:This skin external preparation is obtained by blending 0.005-20.0wt.%, preferably 0.01-10.0wt.% extract of Copaiba (botanical name: Copaifera Leguminosae) therein. Furthermore, the Copaiba is a plant growing in an arid grassland, a pasture, etc., in South America, especially the Andes, etc. For example, an extract prepared by immersing a leaf and a stem or a fruit, etc. of the Copaiba or the whole herb thereof in an extracting solvent such as ethanol or refluxing the solvent together with the leaf, etc., therein under heating, filtering the resultant extract solution, concentrating the prepared filtrate, etc., is preferably used as the extract.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION The present invention relates to a copaiba.
The present invention relates to an external preparation for skin, which is effective in inhibiting the production of melanin by blending the extract of a) and preventing and improving pigmentation, spots, freckles, chloasma, etc. after sunburn.

[0002]

BACKGROUND OF THE INVENTION Although there are some unclear points about the mechanism of skin spots and the like, in general, melanin pigments are formed due to hormonal abnormalities and irritation of ultraviolet rays from the sun, and this is the skin. It is thought to be abnormally deposited inside. For the treatment of such spots and bruises, a substance that suppresses melanin production, for example, a method of administering a large amount of vitamin C, a method of injecting glutathione, or the like, or kojic acid, L-ascorbic acid and its derivatives (fatty acid, sulfuric acid) , Phosphate ester, etc.), cysteine or glutathione and its derivatives and the like are applied locally in the form of ointment, cream, lotion and the like. In Europe and America, hydroquinone preparations are used as medicines.

[0003]

However, except for hydroquinone, these compounds show extremely slow effects, and thus the whitening effect is not always sufficient. On the other hand, with regard to hydroquinone, although the effect has been confirmed, it is generally sensitized in Japan,
Not authorized for use. Therefore, in order to improve its safety, an attempt has been made to use higher fatty acid monoesters, alkyl monoethers, etc. (JP-A-58-154507).
However, it is difficult to say that the esters are safe because they are decomposed by a hydrolase in the body, and the 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, Copaiba (Cop)
It was found that an extract of aiba (scientific name: Copaifera Leguminosae) has a melanin production inhibitory effect, and has completed the present invention. Copaiba
There has been no report on the melanin production inhibitory action of the extract of Noritake et al. And its application to a whitening agent has been known at all. The present inventors have completed the present invention based on the above findings.

That is, the present invention is directed to Copai
ba, scientific name: Copaifera Leguminosae). The external preparation of the present invention is preferably a whitening skin external preparation.

The structure of the present invention will be described in detail below. The copaiba used in the present invention is a plant that grows in South America, especially in dry grasslands such as the Andes, grass and the like. The extract used in the present invention is obtained by immersing or heating and refluxing whole Copaiba herb such as leaves, stems or fruits, and then filtering and concentrating. The extraction solvent used in the present invention may be any solvent that is usually used for extraction, and in particular, alcohols such as methanol and ethanol, hydrous alcohols, acetone, and organic solvents such as acetic acid ethyl ester may be used alone or in combination. You can

The amount of the copaiba extract in the present invention is 0.005 to 20.0 as a dry product in the total amount of the external preparation.
%, Preferably 0.01-10.0% by weight.
If it is less than 0.005% by weight, the effect of the present invention is not sufficiently exhibited, and if it exceeds 20.0% by weight, formulation is difficult, which is not preferable. Further, even if it is blended in an amount of 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 added.

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. The present invention is not limited to this. The blending amount is% by weight. Prior to the examples, a test method and results of the melanin suppressing effect and whitening effect of the plant extract of the present invention will be described.

Test Method and Results 1. Sample Preparation Copaiba Stem and Branch 50g
Was immersed in ethanol for 1 week at room temperature and the extract was concentrated to obtain 11.5 g of an ethanol extract. This extract was dissolved in DMSO at a concentration of 1%, the solution was diluted to adjust the concentration, and the following experiment was conducted using this.

2. Cell Culture Method B16 melanoma cultured cells derived from mouse were used. 1
0% FBS and theophylline (0.09 mg / ml)
The cells were cultured in an Eagle MEM medium containing C. in a CO ₂ incubator (95% air, 5% carbon dioxide) at 37 ° C. After 24 hours of culturing, the sample solution was added so as to have a final concentration (concentration of extracted dry matter) of 10 ^-2 to 10 ^-5 % by weight, culturing was continued for 3 days, and the melanin production amount was visually sensed by the following method. The judgment was measured.

3. Visual measurement of melanin amount A diffuser plate was placed on the lid of the plate of the well, the intracellular melanin amount was observed with an inverted microscope, and compared with the case of the sample (reference) to which the copaiba extract 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. The results are also shown in Table 1. Also in the table,
Toxicity means that it is cytotoxic.

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

[0016]

[Table 1]

4. 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 rate of marked efficacy and efficacy among subjects is 80% or more ◯: The rate of marked efficacy and efficacy among subjects is 50% to
In the case of less than 80% Δ: Remarkable and effective proportion of subjects is 30% to
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.

[0020]

[Table 2] ────────────────────────── Drug compounding amount (% by weight) Effect ────────── ──────────────── Additive- × Hydroquinone 1.0 △ Copaiba extract 0.1 ○ Copaiba extract 1.0 ○ Copaiba extract 10.0 ◎ ──── ──────────────────────

The copaiba extract of Table 2 was obtained by heating and reducing whole grass of Copaiba 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 copaiba extract prevents excessive deposition of melanin pigment and prevents 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 Copaiba methanol extract 0.01 Caustic potash 0 .2 Sodium hydrogen sulfite 0.01 Preservative proper amount Perfume proper amount Ion-exchanged water Residual (production method) Propylene glycol, copaiba methanol extract and caustic potash are added to ion-exchanged water and dissolved, and heated and kept at 70 ° C (water phase). The other ingredients are mixed, heated and melted and maintained 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 the 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 Copaiba ethanol extract 0.05 Sodium bisulfite 0.03 Ethylparaben 0.3 Perfume proper amount Ion-exchanged water Residue (production method) Propylene glycol is added to ion-exchanged water In addition,
Heat to maintain 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained 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 Copaiba acetone extract 0.05 Copaiba ethanol extract 0.05 Sodium bisulfite 0.03 Ethylparaben 0.3 Perfume suitable amount Ion-exchanged water Residual (production method) Soap to ion-exchanged water The powder and borax are added, melted by heating and kept at 70 ° C. (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is stirred into the water phase and gradually added 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) Copaiba acetic acid ethyl ester extract 0.01 Sodium hydrogen sulfite 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 were added to the remaining ion-exchanged water, and the mixture was heated and dissolved and maintained at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase for preliminary emulsification, the phase A is added and the mixture is homogenized with a homomixer, and after emulsification, the mixture is cooled to 30 ° C. while being well stirred.

Example 5 Emulsion (Formulation) Microcrystalline wax 1.0 wt% 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 Copaiba acetone extract 10.0 Sodium bisulfite 0.01 Ethylparaben 0.3 Perfume proper amount Ion-exchanged water Residue (production method) Add propylene glycol to ion-exchanged water,
Heat to maintain 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and kept at 70 ° C. (oil phase). While stirring the oil phase, the aqueous phase is gradually added to this and the mixture is uniformly emulsified with a homomixer. After emulsification, cool to 30 ° C while stirring well.

Example 6 Jelly (formulation) 95% ethyl alcohol 10.0% by weight 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 Copaiba 50% ethanol aqueous solution extract 7.0 2-Hydroxy-4-methoxybenzophenone sulfonate sodium 0.05 Ethylenediaminetetraacetate ・ 3 sodium ・ 2 water 0 .05 Methylparaben 0.2 Fragrance Suitable amount Ion-exchanged water Residual (production method) Carbopol 940 is uniformly dissolved in ion-exchanged water, while Copaiba 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 Copaiba Methanol Extract 1.5 Methylparaben 0.15 (Phase B) Potassium hydroxide 0.1 (Phase C) Glycerin 5.0 Dipropylene glycol 10.0 Sodium bisulfite 0.03 Carboxyvinyl polymer 0.2 (trade name: Carbopol 940 , BFGoodrich Chemical company) Purified water Residual (manufacturing method) A phase and C phase are uniformly dissolved, and A is added to C phase.
Add phase and solubilize. Next, phase B is added and then 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) Copaiba 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,
Phase B is added to the phase to solubilize it. Next, this is added to phase C 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 octoate 2.0 copaiba ethanol extract 1.0 preservative appropriate amount perfume appropriate amount (manufacturing process) Talc to black iron oxide powder components are thoroughly mixed with a blender. Then, an oily component of squalane to isocetyl octoate, a copaiba ethanol extract, an antiseptic and a fragrance are added and kneaded well, then filled into a container and molded.

Example 10 Emulsion type foundation (cream type) (Formulation) (Powder part) Titanium dioxide 10.3 wt% 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 (Aqueous phase) Purified water 50.0 1,3-Butylene glycol 4.5 Copaiba Ethanol extract 1.5 Sorbitan sesquioleate ester 3.0 Preservative proper amount Perfume proper amount (Production method) After heating and stirring the aqueous phase, the powder portion thoroughly mixed and pulverized is added and subjected to a homomixer treatment. Further, the heated and mixed oil phase is added and subjected to a homomixer treatment, and then a fragrance is added with stirring and cooled to room temperature.

[0033]

Industrial Applicability As described above, the external preparation for skin of the present invention has an action of suppressing melanin production, and is excellent in lightening pigmentation, spots, freckles, melasma, and whitening after sunburn. It is an external preparation for the skin that is effective and safe.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁶ Identification number Internal reference number FI Technical indication location A61K 35/78 ADA C 8217-4C (72) Inventor Masako Naganuma 1050 Shinba-cho, Kohoku-ku, Yokohama-shi, Kanagawa Address Shiseido Daiichi Research Center (72) Inventor Minoru Fukuda 1050 Shinba-cho, Kohoku Ward, Yokohama City, Kanagawa Prefecture Shiseido Daiichi Research Center

Claims (3)

[Claims] 1. Copaiba (scientific name: Copa)
ifera Leguminosae) an external preparation for skin characterized by being blended with the extract. 2. The compounding amount of the copaiba extract is 0.005.
The external preparation for skin according to claim 1, which is ˜20.0% by weight. 3. The external preparation for skin according to claim 1, which is an external preparation for whitening skin.