JPH08310939A - Beautifying and whitening dermal preparation for external use - Google Patents

Abstract

PURPOSE: To obtain a beautifying and whitening dermal preparation for external use, having controlling actions on the melanogenesis and inhibiting actions on tyrosinase activities and effective in preventing and reducing pigmentation, dermal stains, ephelides, liver sots, etc., after sunburn. CONSTITUTION: This dermal preparation for external use contains 0.005-20wt.%, preferably 0.01-10wt.% plant extract of the genus Equisetum of the family Equisetaceae (except Equisetum giganteum). The plant extract is prepared by immersing the plant, especially a leaf, a stem, a fruit, etc., or the whole herb of Equisetum arvense L., Equisetum hyemale L. or Equisetum debile Roxb. together with an extracting solvent such as methanol or refluxing under heating, then filtering the resultant extract and concentrating the prepared extract. The plant extract is further suitably blended with usually used ingredients and prepared into an ointment, a cream, a milky lotion, a lotion, a pack, a bathing agent, etc.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention suppresses the production of melanin by incorporating a plant extract of the genus Equisetum of the family Equisetum,
The present invention relates to an external preparation for whitening skin, which is effective in preventing and improving pigmentation, stains, freckles, and liver spots 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. This melanin pigment, which causes skin coloring, is produced in the melanogenic granules (melanosomes) in the melanocytes (melanocytes) between the epidermis and the 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, the process in which tyrosine, which is an essential amino acid, becomes dopaquinone by the action of the enzyme tyrosinase, and this is converted to black melanin via the red and colorless pigments by the enzymatic or non-enzymatic oxidation action is the melanin pigment formation process. Therefore, suppressing the action of tyrosinase, which is the first step of the reaction, is important for suppressing melanin production.

[0003]

However, except for hydroquinone, the compounds that suppress the action of tyrosinase show extremely slow effects, and therefore the effect of improving skin pigmentation is not sufficient. On the other hand, although the effect of hydroquinone is tentatively recognized, its use is generally limited because of its sensitizing property. 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]

Therefore, as a solution to these problems, the present inventors investigated a melanin production inhibitory effect on various substances, and as a result, a plant extract of Equisetum spp. Was found to have a melanin production inhibitory effect. Further, they found that they have a tyrosinase inhibitory action, and completed the present invention. Regarding the melanin production inhibitory effect of the plant extract of the genus Equisetum,
setum giganteum) was recently reported by the applicant of the present application and found to be applied to a whitening agent (Japanese Patent Application No. 7-78478), but the whitening effect on other plants has never been reported. unknown. The present inventors have completed the present invention based on the above findings.

That is, the present invention is based on the family Equiseata.
e) Horsetail (Equisetum) (excluding Cora de Cavallo (Equisetum giganteum). } The whitening skin external preparation characterized by mix | blending the plant extract of these.

The structure of the present invention will be described in detail below. Equiseatae used in the present invention (Eqseatae)
uisetum plants are especially horsetail (Equisetum arvense)
L.), horsetail (Equisetum hyemale L.) or Taiwan dogdogsa (Equisetum debile Roxb.).

[0007] These plants are widely distributed all over the world, and are plants that especially grow in dry grasslands and grasses. The plant extract used in the present invention is obtained by immersing or heating and refluxing the whole plant such as leaves, stems or fruits of these plants, followed by filtration and concentration. 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

[0008] In the present invention, the compounding amount of the plant of the genus Equisetum of the family Equisetum is 0.005 as a dry product in the total amount of the external preparation.
˜20.0% by weight, preferably 0.01 to 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 whitening agent for skin whitening of the present invention also contains components that are usually used in external skin external agents such as cosmetics and pharmaceuticals, such as other whitening agents and moisturizers.
Antioxidants, oily components, UV absorbers, surfactants, thickeners, 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 whitening skin of the present invention includes, for example, ointments, creams, emulsions, lotions, packs, bath agents and the like.
Any conventional skin external preparation may be used,
The dosage form is not particularly limited.

[0012]

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 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. Preparation of Sample 50 g of stems and branches of Equisetum sp. Plants were immersed in ethanol at room temperature for 1 week, and the extract was concentrated to obtain 5.2 g of ethanol extract. This extract was added to DMSO 1
%, The solution was diluted to adjust the concentration, and the following experiment was performed 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 another 3 days, and the melanin production amount was visually sensed by the following method. The determination and the tyrosinase activity inhibitory effect were measured.

3. Visual measurement of the amount of melanin Place a diffusion plate on the lid of the well plate, observe the intracellular melanin amount with an inverted microscope, and in the case of the sample (reference) to which the plant extract of Equisetum spp. Is added Compared with. The results are shown in Table 1. Also, as a reference example,
The same test as described above was carried out also on an extract of mussel (Lamiaceae, Odorikosou subfamily), which is already known to have a melanin production inhibitory action. The results are also shown in Table 1.

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

4. Measurement of tyrosinase activity Before the measurement, the medium in the wells is removed, and the wells are washed twice with 100 μl of PBS. 45 μl of 1% Triton-X in each well
PBS containing (trade name of Rohm and Haas, surfactant) is added. Shake the plate for 1 minute to break the cell membrane well, then use a microplate reader to 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 inhibition rate (%) was defined as the decrease in the absorbance difference of the plant extract-added sample with respect to the absorbance difference at 0 minutes and 60 minutes in the case of the sample to which the plant extract was not 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. The results are also shown in Table 1. In the table, − means that no significant difference was observed within the risk rate of 5% as compared with the control.

[0019]

[Table 1] ─────────────────────────────────── Test Melanin production Visual evaluation Tyrosinase activity inhibition rate ( %) ──────── ──────────────────────── concentration (wt%) 10 ^-5 10 ^-4 10 ^-3 10 ^{- 2} 10 ^-5 10 ^-4 10 ^-3 10 ^-2 ─────────────────────────────────── Horsetail extraction Substance × × × ○ − − 36 98 Horse mackerel extract × × × ○ − − 37 97 Taiwan Indigo extract × × × ○ − − 38 98 Clam shell 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 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.

[0023]

[Table 2] ───────────────────────────────────────────────────────────────────────────────────────────────────────────────────────────────────────────────────────────────────── ──────────────────────── Additive- × Hydroquinone 1.0 △ Horsetail extract 0.1 ○ Horsetail extract 1.0 ○ Horsetail extract 10.0 ◎ Horse mackerel extract 0.1 ○ Horse mackerel extract 1.0 ○ Horse mackerel extract 10.0 ◎ Thai one dog dougosa extract 0.1 ○ Thai one dog dougosa extract 1.0 ○ Thai one dog dougosa extract Thing 10.0 ◎ ──────────────────────────────

The extract of horsetail, horsetail and Taiwan dogdogosa shown in Table 2 was obtained by heating and reducing the whole plants of these plants in ethanol, filtering and concentrating and drying.

As is clear from Table 2, the effect after exposure to sunlight is that the addition of horseradish, horsetail or Taiwan dogdogsa extract prevents excessive deposition of melanin pigment and produces a black color. It was accepted to prevent this.

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 Sugina methanol extract 0.01 Caustic potash 0 .2 Sodium bisulfite 0.01 Preservative Suitable amount Perfume Suitable amount Ion-exchanged water Residual (production method) Dissolve propylene glycol, horse mackerel methanol extract and caustic potash in ion-exchanged water and heat to 7
Keep at 0 ° C (aqueous phase). Mix other ingredients and heat to melt
Keep at 0 ° 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 Toxa 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 Soap powder 0.1 Borax 0.2 Taiwan Inudogusa acetone extract 0.05 Horsetail ethanol extract 0.05 Sodium hydrogen sulfite 0.03 Ethylparaben 0.3 Perfume proper amount Ion-exchanged water Residue (production method) Ion-exchange Soap powder and borax are added to water, dissolved 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% by weight 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) Toxa 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% 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 Taiwan Inudogusa acetone extract 10.0 Sodium hydrogen sulfite 0.01 Ethylparaben 0.3 Fragrance appropriate amount Ion-exchanged water Residue (production method) Propylene glycol And add
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 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 Horse mackerel 50% ethanol aqueous solution extract 7.0 2-Hydroxy-4-methoxybenzophenone sodium sulfonate 0.05 Ethylenediaminetetraacetate ・ 3 sodium ・ 2 water 0 .05 Methylparaben 0.2 Fragrance Appropriate amount Ion-exchanged water Residue (production method) Carbopol 940 is uniformly dissolved in ion-exchanged water, while horseradish 50% ethanol aqueous solution extract and polyoxyethylene (50 mol) oleyl are added to 95% ethanol. Alcohol 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 Toxamethanol 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) 5.0% by weight dipropylene glycol Polyoxyethylene (60 moles) hydrogenated castor oil 5.0 (Phase B) Thai one dog dog methanol extract 0.01 Olive oil 5.0 Tocopherol acetate 0.2 Ethylparaben 0.2 Perfume 0.2 (C phase) 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) Phases A, B, and C 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 octanoate 2.0 horse mackerel ethanol extract 1.0 preservative appropriate amount perfume appropriate amount (production method) Talc-black iron oxide powder components are thoroughly mixed with a blender. Then, an oily component of squalane to isocetyl octoate, an extract of horse mackerel ethanol, a preservative and a fragrance are added and kneaded well, then filled into a container and molded.

Example 10 Emulsion type foundation (cream type) (Prescription) (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 Toxa 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.

[0036]

Industrial Applicability As described above, the whitening skin external preparation of the present invention has a melanin production inhibitory action and a tyrosinase activity inhibitory action, and is effective in treating pigmentation, stains, freckles, melasma, etc. after sunburn. It is an external preparation for whitening skin, which has excellent effects on lightening and whitening, and is also excellent in safety.

Claims (3)

[Claims] 1. A genus Equisea (Equiseatae)
setum) {However, Cora de Cavallo (Equisetum gigante
um) is excluded. } The whitening skin external preparation characterized by mix | blending the plant extract of these. 2. A plant of the genus Equisetum, belonging to the family Equisetum, is Equisetum (Eq.
uisetum arvense L.), horsetail (Equisetum hyemale)
L.) or Taiwan Indogusa (Equisetum debile Rox)
b.) The external preparation for whitening skin according to claim 1. 3. The compounding amount of the plant extract of the horse mackerel genus Equisetum is 0.005 to 20.0% by weight.
A skin external preparation for whitening as described.