JPH10316530A - Skin preparation for external use for whitening - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a skin preparation for external use for whitening, capable of suppressing melanization and effective in prevention and improvement of pigmentation, liver spot, freckle, chloasma, etc., after suburn by using a specific plant of the family Solanaceae as an active ingredient. SOLUTION: This skin preparation for external use for whitening is obtained by formulating an extract of a plant belonging to the genus Solanum of the family Solanaceae. Jurubeba paiz (scientific name: Solanum paniculatum) is especially preferably used as the plant. The above extract is preferably formulated in an amount of 0.0005-10.0 wt.% in the skin preparation. The skin preparation for external use can properly be formulated, as necessary, with the other beautifying agent, humectant, antioxidant, oily component, ultraviolet light absorbent, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to eggplant (Solanaceae)
By adding an extract of the family Solanum, the production of melanin is suppressed and pigmentation after sunburn is reduced.
The present invention relates to a whitening skin external preparation effective for preventing and improving spots, freckles, liver spots, and the like.

[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.

[0003] This melanin pigment, which causes skin coloring, is produced in melanin-producing granules (melanosomes) in melanocytes (melanocytes) between the epidermis and the dermis, and the produced melanin is penetrated by neighboring cells. Spread to The biochemical reaction in this melanocyte is estimated as follows.

That is, tyrosine, which is an essential amino acid, is converted into dopaquinone by the action of the enzyme tyrosinase, which is converted into black melanin via a red pigment and a colorless pigment by an enzymatic or non-enzymatic oxidative action in the process of producing melanin pigment. is there.

[0005] Therefore, suppressing the action of tyrosinase, which is the first step of the reaction, is important for suppressing the production of melanin.

[0006]

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.

[0007] On the other hand, although hydroquinone has been recognized as having an effect, its use is generally restricted because of its sensitizing properties. In order to improve the safety, attempts have been made to use monoesters or alkyl monoethers of higher fatty acids (Japanese Patent Application Laid-Open No. 58-154507), but the esters are decomposed by hydrolytic enzymes in the body. Therefore, it is not always safe, and ethers have not yet been obtained that are sufficiently satisfactory in terms of safety.

The present inventors have studied the effect of inhibiting melanin production on a wide variety of substances to solve these problems. As a result, the extract of a plant belonging to the genus Solanum of the family Solanaceae was found to inhibit melanin production. It has been found that it has an action and a tyrosinase inhibitory action, and has completed the present invention.

The Solanaceae family Solanum
) A report on an extract of a genus plant has been reported so far as an example of a skin external preparation for improving acne skin (Japanese Patent Application Laid-Open No. 56-1).
54500), but has a melanin production inhibitory action,
No application to whitening agents is known. The present inventors have completed the present invention based on the above findings.

An object of the present invention is to provide a highly safe whitening skin external preparation which has excellent melanin production inhibitory activity and tyrosinase inhibitory activity.

[0011]

That is, the present invention is an external preparation for skin whitening characterized by incorporating an extract of a plant of the genus Solanum in the family Solanaceae.

The present invention also relates to the eggplant (Solanaceae)
The present invention provides the skin whitening agent for external use, wherein the plant of the genus Solanum is Jurubeba paiz (scientific name: Solanum paniculatum).

Furthermore, the present invention relates to a plant of the present invention, wherein the amount of the extract of the plant of the genus Solanum of the family Solanaceae is 0.0
005 to 10.0% by weight of the skin whitening agent for skin whitening.

[0014]

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS The configuration of the present invention will be described below in detail.

As the Solanaceae plant of the genus Solanum used in the present invention, jurubeba paiz (scientific name: Solanum paniculatum) is preferred. It is a plant that grows especially on dry grasslands, pastures and the like in Brazil.

The Solanaceae family Solanam
The melanin production inhibitory action and the tyrosinase inhibitory action of the extract of the genus plant are the effects discovered for the first time by the present inventors, and their application to whitening agents and skin externalizing agents for whitening is not known at all.

The extract used in the present invention may be any of the above-mentioned plant branches, roots, leaves, stems including rhizomes, fruits, flowers, etc., or
After immersing the whole plant with the extraction solvent or heating to reflux,
It is obtained by filtration and concentration. The extraction solvent used in the present invention is not particularly limited as long as it is generally a solvent used for extraction.For example, an organic solvent such as alcohols such as methanol and ethanol, aqueous alcohols, acetone, and ethyl acetate alone may be used alone. Alternatively, it is preferable to use them in combination.

The amount of the extract of the plant of the genus Solanum of the family Solanaceae in the present invention is 0.0005 to 10.0% by weight, preferably 0.01 to 5% by weight of the total amount of the external preparation as a dry matter. 0.0% by weight. 0.0005
If the amount is less than 10% by weight, the effects of the present invention are not sufficiently exhibited, and if the amount is more than 10.0% by weight, it is difficult to formulate the composition, which is not preferable. Further, even if the content is 5.0% by weight or more, the effect is not so greatly improved.

In addition to the above essential components, the skin whitening preparation of the present invention contains components usually used in skin external preparations such as cosmetics and pharmaceuticals, for example, other whitening agents, humectants, and the like.
Antioxidants, oily components, UV absorbers, surfactants, thickeners, alcohols, powder components, coloring materials, aqueous components, water,
Various skin nutrients and the like can be appropriately compounded as needed.

In addition, sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, gluconic acid, caffeine, tannin, verapamil, tranexamic acid and derivatives thereof, and licorice extract Products, glabridine, hot water extract of fire thorn fruit, 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 whitening skin external preparation of the present invention includes, for example, ointments, creams, emulsions, lotions, packs, bath preparations, etc.
Any conventional skin external preparation may be used,
The dosage form is not particularly limited.

[0022]

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 compounding amount is% by weight. Prior to the examples, test methods and results regarding 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 its results" Sample preparation Root part 100 of jurubeba paiz
g of the extract was immersed in ethanol at room temperature for one week, and the extract was concentrated to obtain 1.6 g of an ethanol extract. This extract is
After dissolving 1% in MSO and diluting this solution to adjust the concentration, 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)
Was cultured in a CO2 incubator (95% air, 5% carbon dioxide) at 37 ° C. in an Eagle MEM medium containing After 24 hours of culture, the sample solution is added to a final concentration (concentration in terms of dry extract) of 10 ^-2 to 10 ^-5 % by weight, and the culture is further continued for 3 days. Judgment and the tyrosinase activity inhibitory effect were measured.

3. Visual measurement of the amount of melanin Place the diffusion plate on the lid of the well plate, observe the amount of melanin in the cells with an inverted microscope, and examine the sample without the extract of the Solanaceae family (reference). Compared to the case. The results are shown in "Table 1". In addition, as a reference example, the same test as described above was performed on a scallop extract (Lamiaceae, Scrophulariaceae) already known to have a melanin production inhibitory action. The results are shown in Table 1 together.

<Judgment Criteria> A: White compared to the standard (melanin content is smaller than the standard) C: Slightly white compared to the standard (melanin content is slightly smaller than the standard) C: Standard Comparable

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. Thereafter, 5 μl of a 10 mM L-DOPA solution was quickly added, and the mixture was transferred to a 37 ° C. incubator 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). The results are shown in Table 1. In addition, as a reference example, the same test as described above was conducted on an ethanol extract of oyster, which is already known to have a tyrosinase activity inhibitory action. The results are shown in Table 1 together. In the table,-
Means that no significant difference was observed within 5% of the risk compared to the control. A blank column means that the test was not performed because a tyrosinase activity inhibitory effect was observed at a lower concentration.

[0028]

[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 ----------- -------------------------------------------------- ----------- Jurbeba Pits × ○ 90 106 Extract Kaikai Extract × × × × − − − 55 ------------------- -------------------------------------------------- ---

5. Whitening effect test [Test method] The day when 40 subjects were exposed to sunlight with artificial light (UV-A + UV-B) for 30 minutes (10 minutes a day for 3 days) on the inner skin of the upper arm. After 5 days, each sample was applied once in the morning and evening for 4 weeks. Divide the panel into 8 groups,
The test was performed according to the following formulation as five groups. (Alcohol phase) 95% ethyl alcohol 55.0% by weight Polyoxyethylene (25 mol) hydrogenated castor oil ether 2.0 Antioxidant / preservatives Appropriate amount Perfume Appropriate amount Drug (Table 2) (Aqueous phase) Glycerin 5.0 Sodium hexametaphosphate Appropriate amount Ion-exchange water Residue <Production method> Prepare an aqueous phase and an alcohol phase, respectively, and then mix and solubilize both.

[Evaluation method] The lightening effect after use was determined based on the following 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
Less than 50% ×: The proportion of subjects showing excellent and effective is less than 30%

A sample having the composition described in the above test method was prepared, and the whitening effects were compared using the agents shown in Table 2.
The results are shown in "Table 2".

[0032]

[Table 2] ---------------------------------------------- ------------- Drug compounding amount (% by weight) Effect --------------------------- -------------------------------- No additive-× Hydroquinone 1.0 △ Juluveva / Pits extract 0.1 ○ Jurbeva-Pits extract 1.0 ○ Jurbeva-Pits extract 5.0 ◎ -------------------------------- ---------------------------

The extract of Jurbaba-Paitz in Table 2 was obtained by heating and reducing the roots of Jurbaba-Paitz in ethanol, followed by filtration, concentration and drying.

As is clear from Table 2, the effect after exposure to sunlight shows that the addition of the extract of jurubeba pits prevents the deposition of excessive melanin pigments and prevents blackening. It was recognized that.

Examples of the skin whitening external preparation of the present invention are shown below. The Jurbaba-Paitz extract is obtained by reducing the roots by heating in each extraction solvent, filtering, concentrating and drying.

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 Dulbeva Pits Methanol Extract 0.0 01 Caustic potash 0.2 Preservatives Appropriate amount Fragrance Appropriate amount Ion-exchanged water Residue (Preparation method) Propylene glycol, julbeva-pitts methanol extract and caustic potash are added and dissolved in ion-exchanged water, and heated to 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 water phase, and after the addition is completed, the temperature is maintained for a while to cause a reaction. Thereafter, the mixture is uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well.

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 Jurbeba pitts ethanol extract 0.05 Ethylparaben 0.3 Perfume Appropriate amount Ion-exchanged water Residue (Production method)
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 water phase, pre-emulsified, homogenized with a homomixer, and cooled to 30 ° C. with good 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 2-Ethylhexyl paramethoxycinnamate 1.5 Borax 0.2 Jurbeva-Paithe acetone extract 0.05 Julubeba-Paitz ethanol extract 0.05 Ethylparaben 0.3 Perfume Appropriate amount Ion-exchange water residue ( Production method) Soap powder and borax are added to ion-exchanged water, heated and dissolved, 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 gradually added to the aqueous phase while stirring to carry out the reaction. After completion of the reaction, the mixture is uniformly emulsified with a homomixer, and cooled to 30 ° C. while stirring well after emulsification.

Example 4 Emulsion (Formulation) 2.5% by weight of stearic acid Cetyl alcohol 1.5 Vaseline 5.0 Liquid paraffin 10.0 Polyoxyethylene (10 mol) monooleate 2.0 Polyethylene glycol 1500 0 Triethanolamine 1.0 Carboxyvinyl polymer 0.05 (trade name: Carbopol 941, BFGoodrich Chemical company) Eggplant (scientific name: Solanum melongena) 0.01 Real ethyl acetate extract Placenta extract 1.0 ethyl Paraben 0.3 Perfume Appropriate amount Ion exchange water residue (Preparation method) Dissolve the carboxyvinyl polymer in a small amount of ion exchange water (A phase). 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 Kinginnabisubi (scientific name: Solanum aculeatissimum) 10.0 Acetone extract of fruit of kojic acid 1.0 Ethylparaben 0.3 Perfume Appropriate amount Ion-exchanged water Residue (Preparation method) ) Add propylene glycol to deionized 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% by weight Dipropylene glycol 15.0 Polyoxyethylene (50 mol) Oleyl alcohol ether 2.0 Carboxyvinyl polymer 1.0 (Product name: Carbopol) 940, BFGoodrich Chemical company) Caustic soda 0.15 L-arginine 0.1 Scientific name: Solanum lyratumm 7.0 A 50% ethanol aqueous solution of fruit of sodium 2-hydroxy-4-methoxybenzophenonesulfonate 0.05 Ethylenediaminetetraacetate, trisodium, 2 water 0.05 methylparaben 0.2 Perfume Appropriate amount Ion-exchanged water Residue (Preparation method) Carbopol 940 is uniformly dissolved in ion-exchanged water, while 50% of fermented fruit in 95% ethanol % Ethanol aqueous solution extraction Things, polyoxyethylene (50 mol) oleyl alcohol ether were dissolved, 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 Serum (Prescription) (Phase A) Ethyl alcohol (95%) 10.0% by weight Polyoxyethylene (20 mol) octyldodecanol 1.0 Pantothenyl ethyl ether 0.1 Jurbeva pitts Methanol extract 1.5 Ascorbic acid glucoside 1.5 Arbutin 3.0 Methyl paraben 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 Residue (Preparation method) Dissolve A phase and C phase uniformly, and add A to C phase
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) Dulbeva pitts methanol extract 0.01 Olive oil 5.0 Tocopherol acetate 0.2 Ethyl paraben 0.2 Fragrance 0.2 (C phase) Ascorbic acid 2-glucoside 2.0 Polyvinyl alcohol 13.0 (Saponification degree 90, polymerization degree 2,000) Ethanol 7.0 Purified water residue (Production method) A phase, B phase, and C phase are each dissolved uniformly,
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 octoate 2.0 Dulbeba / Peats ethanol extract 1.0 Preservatives Appropriate amount Fragrance Appropriate amount (Production method) Powder component of talc to black iron oxide in a blender Mix well, add the oily components of squalane to isocetyl octanoate, ethanolic extract of juleba pits, preservatives, and fragrance, knead well, fill into a container, and mold.

Example 10 Emulsion type foundation (cream type) (prescription) (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 (aqueous phase) purified water 50.0 1,3-butylene glycol 4.5 jurubeba・ Peats ethanol extract 1.5 Sorbitan sesquioleate 3.0 Preservatives Appropriate amount Flavors Appropriate amount (Preparation method) After heating and stirring the aqueous phase, a well mixed and pulverized powder portion is added, followed by homomixer treatment. 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.

[0046]

As described above, the external preparation for whitening skin of the present invention has an inhibitory effect on melanin production and an inhibitory effect on tyrosinase activity, and is effective in preventing pigmentation, spots, freckles, liver spots, etc. after sunburn. It has excellent effects on lightening and whitening, and also has excellent safety.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁶ Identification symbol FI // A61K 35/78 ADA A61K 35/78 ADAR (72) Inventor Masahiro Ota 1050 Nippa-cho, Kohoku-ku, Yokohama-shi, Kanagawa Pref. Shiseido Daiichi Research Center

Claims (3)

[Claims] The present invention relates to a solanaceae family of solanum.
m) An external preparation for whitening skin, comprising an extract of a genus plant. 2. The solanum of the Solanaceae family.
m) The skin whitening preparation according to claim 1, wherein the genus plant is jurubeba paiz (scientific name: Solanum paniculatum). 3. A solanum (Solanaceae) family of solanum.
m) The amount of the extract of the genus plant is 0.0005 to 10.0.
The skin whitening agent for whitening according to claim 1 or 2, which is in weight%.