JPH11189512A - Preparation for external use for skin - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a preparation for external use for skin that can very effectively prevent and improve the skin blackening caused by skin pigmentation and can be safely used without any damage to skin. SOLUTION: The plant body of Pajaro bobo is extracted with a polar solvent and the extract is formulated to a preparation for external use for skin, preferably in an amount of 0.001-20 wt.% on the dry basis of the whole amount of the external preparation.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin, and more particularly, to an external preparation for skin which suppresses the production of melanin and has an effect of preventing or improving pigmentation after sunburn, spots and freckles, etc. Things.

[0002]

2. Description of the Related Art Pigmentation in the skin due to spots, freckles and darkening of the skin after sunburn is the result of a marked increase in melanin production due to the activation of pigment cells (melanocytes) present in the skin. Especially for middle-aged people, it is one of the serious skin problems. In general, melanin is converted from tyrosine to dopa and dopa to dopaquinone by the action of the enzyme tyrosinase biosynthesized in melanocytes, and then formed via intermediates such as 5,6-dihydroxyindole, and then formed around melanocytes. Are sent to the basal cells (keratinocytes) and stored there.

[0003] Therefore, in order to prevent or improve the pigmentation of the skin, it is conceivable to inhibit the melanin production process or to bleach the already produced melanin in light color. Various whitening components have been conventionally proposed based on such a concept. For example, as a compound that inhibits tyrosinase activity and suppresses melanin production, a sulfur compound represented by glutathione is exemplified. Hydrogen peroxide, hydroquinone, vitamins, and the like have been used to bleach the generated melanin in light color. In addition, topical administration of vitamin A acid or vitamin A has been performed to reduce melanin in keratinocytes. Alternatively, in consideration of safety and the like, many attempts have been made to use a conventionally known natural product such as an extract from a plant as a whitening component.

[0004]

As described above, there are various whitening ingredients which prevent and improve pigmentation. However, ascorbic acids are easily oxidized and unstable in systems containing a large amount of water such as moist skin external preparations, causing discoloration and odor.Hydrogen peroxide has problems in stability and safety during storage, Glutathione and sulfur emit a remarkable off-flavor and are not suitable for use in external preparations for skin. In addition, in the case of a conventionally known natural product such as an extract from a plant, the action is slow, so that the blackening of the skin may not be sufficiently effectively prevented. On the other hand, although the effect of hydroquinone on improving pigmentation has been recognized for some time, its use is generally restricted due to safety problems such as skin irritation.

The present invention has been made in view of such circumstances, and not only can it prevent or improve the skin blackening due to pigmentation extremely effectively, but also can be used safely without any harm to the skin. An object of the present invention is to provide a skin external preparation that can be used.

[0006]

Means for Solving the Problems In order to solve these problems, the present inventors screened a wide variety of plant extracts for the effect of inhibiting melanin production using cultured cells. It has been found that an extract of Pajaro bobo has melanin production inhibitory activity, and based on this finding, the present invention has been completed.

That is, according to the present invention, Pajaro Bobo (Pa
An external preparation for skin characterized by containing an extract of Jaro bobo).

[0008] The solvent for extracting the extract is preferably a polar solvent.

The content of the extract in the external preparation for skin is 0.001 to 20.0% by weight in terms of dry weight.
It is preferred that

Further, the external preparation for skin of the present invention can be suitably used as a cosmetic.

[0011]

DESCRIPTION OF THE PREFERRED EMBODIMENTS The present invention will be described below in detail.

The topical skin preparation of the present invention is characterized by containing an extract of Pajaro bobo.

The pajaro bobo (Pa) used in the present invention
Jaro bobo) is a plant from Peru in South America, and its scientific name is written as Salix chilensis.

Pajaro Bobo contains various components having an effect of suppressing melanin production. Although the mechanism of action for suppressing melanin production is not always clear, it is presumed that, for example, melanin production is suppressed by inhibiting tyrosinase activity. By this effect, it is considered that the external preparation for skin of the present invention can prevent the occurrence of pigmentation on the skin, improve the progress of pigmentation, and prevent the skin from being darkened. That is, the topical skin preparation of the present invention is characterized by containing such components derived from Pajaro Bobo.
Therefore, the external preparation for skin of the present invention may contain shreds, crushed products, pulverized products and the like of Pajaro Bobo, but preferably contains an extract obtained by extracting the above components with a solvent as an active ingredient. To be contained. In addition, the component can be obtained from any part of the plant of Pajaro Bobo,
Leaves, stems, branches or nuts, or the whole plant of Pajaro bobo can be used for extraction and the like.

The extraction can be performed by a general method. For example, leaves, stems, branches and the like of Pajaro Bobo are immersed in an extraction solvent or heated to reflux with an extraction solvent, and then filtered to remove plant residues, thereby having an effect of preventing or improving pigmentation. Can be obtained. Plants used for extraction may be subjected to treatment such as shredding and pulverization as needed before extraction. Further, the obtained extract may be further purified, concentrated, and the like, if necessary.

The extraction solvent is not particularly limited as long as it is a polar solvent usually used for extraction. Preferably, the extraction solvent is an alcohol such as methanol or ethanol, an aqueous alcohol, an organic solvent such as ether, acetone or ethyl acetate or water alone. Alternatively, two or more kinds can be used in combination. In the total amount of the external preparation for skin of the present invention, the content of Pajaro Bobo is preferably calculated by converting the extract to dry weight,
0.001 to 20.0% by weight, particularly preferably 0.01
１10.0% by weight. If the amount is less than 0.001% by weight, the effect of the present invention is not sufficiently exhibited, and even if the amount exceeds 20.0% by weight, the effect cannot be expected to be improved as much as the amount thereof.

The external preparation for skin of the present invention includes, in addition to the above-mentioned extract or dried product thereof, components usually used in external preparations for skin, for example, aqueous components, water, oily components, alcohols, hydrocarbons, Higher fatty acids, waxes, humectants, antioxidants, ultraviolet absorbers, surfactants, thickeners, powder components, coloring agents, fragrances, preservatives, anti-inflammatory agents, pH adjusters, sequestering agents, sugars Various skin nutrients, agents such as whitening ingredients other than the present extract or a dried product thereof, and the like can be appropriately compounded as necessary.

Specifically, alcohols such as ethanol, propanol, cetanol, stearyl alcohol, glycerin, propylene glycol, and butylene glycol; hydrocarbons such as petrolatum, squalane, and liquid paraffin; and higher fatty acids such as stearic acid and oleic acid Etc., waxes such as gay wax, hyaluronic acid etc. as humectants, tocopherol, tocopherol acetate, butylhydroxyl toluene etc. as antioxidants, benzophenone derivatives etc. as ultraviolet absorbers, polyoxyethylene cetyl ether, mono as surfactants Polyethylene glycol stearate, glyceryl monostearate, polyoxyethylene sorbitan monolaurate, polyoxyethylene lauryl ether, polyoxyethylene poly Oxypropylene glycol, fatty acid monoglyceride, polyoxyethylene hydrogenated castor oil, sodium lauryl sulfate, alkylsulfosuccinate, quaternary alkylamine, glycine betaine, alkyl betaine, etc., gum arabic, carboxyvinyl polymer, xanthan gum, guar gum as a thickener, Cationized guar gum, polyvinyl alcohol, etc., talc, silica gel, titanium oxide, acrylic acid-methacrylic acid copolymer, etc. as powder components, paraben, chlorhexidine gluconate, etc. as preservatives, dipotassium glycylate, tranexamic acid and the like as anti-inflammatory agents Derivatives, p
H adjusters such as citrates and acetates, sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, gluconic acid, etc., and sugars such as glucose, fructose, mannose, Sucrose, trehalose, sulfated trehalose and the like can be mentioned. In addition to these, caffeine, tannin, verapamil, licorice extract, glabridine, various crude drugs, glycyrrhizic acid and its derivatives or salts, 4- (1,1-dimethylethyl) -4 ′
-Methoxy-dibenzoylmethane, potassium hydroxide and the like.

As whitening agents other than Pajaro bobo extract, vitamin C, magnesium phosphate ascorbate,
Ascorbic acid glucoside, arbutin, kojic acid and the like can be mentioned.

The external preparation for skin of the present invention can be used for preventing or improving pigmentation of the skin, and for such purposes, the uses of pharmaceuticals, quasi-drugs or cosmetics are particularly limited. Not something.

The dosage form of the present invention is arbitrary, and any dosage form conventionally used for this type of external preparation for skin may be used, for example, solution, ointment, cream, emulsion, lotion,
Packs, aqueous gels, oil gels, bath agents and the like.

[0022]

EXAMPLES Examples of the present invention will be described below, but the present invention is not limited to these examples. First, a production example of a pajaro bobo extract contained in the external preparation for skin of the present invention and its melanin production inhibitory effect will be described.

[0023]

[Production Example] Production of Pajaro Bobo extract 1000 g of leaves, stems and branches of Pajaro Bobo
The mixture was extracted with 0 L of 80% methanol for 5 days at room temperature, and the obtained extract was filtered to remove insolubles. Then, the solvent was distilled off using an evaporator, and further concentrated to dryness with a vacuum pump to obtain 152 g of the concentrate. I got

<Melanin production inhibitory effect on pigment cells> (Test method) Plastic culture flask (25 cm 2)
In an Eagle MEM medium containing 10% fetal bovine serum,
× 104 mouse melanoma cells (B16 cells) were seeded and cultured under conditions of 5% carbon dioxide and 37 ° C.
The next day, the DMSO solution of the Pajaro bobo extract was converted to a dry weight, and the concentration in the medium was 1 × 10 −3 to 5 ×.
10-2 (W / V%) was added, and the cells were further cultured for 2 days. After completion of the culture, the medium was removed, and the cells were washed with an equilibrated phosphate buffered saline (PBS). The cells were detached using a solution containing trypsin and EDTA, and the cells were collected using a centrifuge. After washing the cells with PBS, 1N
Sodium hydroxide was added and dissolved by heating. After cooling, chloroform was added and stirred, followed by centrifugation again. The supernatant thus obtained was measured at an absorbance of 400 nm, and the amount of melanin was determined from a calibration curve previously prepared using synthetic melanin. Table 1 shows the results. In addition, the number of cells was calculated assuming that the number of cells of the control (only added DMSO) was 100%. The amount of melanin was converted into the amount of melanin per a fixed number of cells, and the control without addition of the extract was determined as 100% (each n = 5). Table 1 shows the obtained results.

[0025]

[Table 1]

As is clear from the results shown in Table 1, it was revealed that the extract of Pajaro bobo had an effect of suppressing melanin production on pigment cells, and that the effect was remarkable even in a small amount. At this time, no toxicity to the pigment cells was observed.

[0027]

Example 1 Oil-in-water cream (Production method) The components (A) shown in Table 2 were mixed and heated to 80 ° C. Separately from (A), each component of (B) was mixed and heated to 80 ° C. Thereafter, the component (B) was added to the component (A) and the mixture was emulsified with stirring, and then cooled to 35 ° C. to obtain an oil-in-water cream.

[0028]

[Table 2]

<Actual use test> Next, in order to demonstrate how the cosmetic of the present invention is superior in preventing and improving skin pigmentation, the oil-in-water cream shown in Example 1 was used. And a long-term continuous use test was conducted to confirm the effect. As a comparative product, an oil-in-water cream prepared by replacing the Pajaro Bobo extract in the cream of Example 2 with purified water was used.

(Test Method) Forty female volunteers suffering from black and white, spots, and freckles were divided into two statistically equivalent groups, and the face of Group A was subjected to the oil-in-water type of Example 1 of the present invention. The cream was used, and a comparative oil-in-water cream was used on the face of Group B for 3 months. The improvement effect on the pigmentation three months later was evaluated by visual observation, and comparison between groups was performed. Table 3 shows the results. The effective rate is
A case where an effect slightly higher than the improvement was recognized was regarded as effective.

[0031]

[Table 3]

As shown in the results in Table 3, the cosmetic of the present invention has a significantly more effective effect of preventing and improving skin pigmentation and an excellent whitening effect as compared with the comparative cosmetic. It became clear. In addition, in the product application part of the present invention,
No undesirable reactions were observed on the skin during the test period,
The cosmetics of the present invention were also confirmed to be highly safe.

[0033]

Example 2 Emulsion (Preparation method) Component (A) and component (B) shown in
Dissolve with stirring at 0 ° C. After the component (A) was added to the component (B) and pre-emulsification was performed, the mixture was uniformly emulsified with a homomixer. After emulsification, the mixture was cooled to 30 ° C. with stirring to obtain an emulsion.

[0034]

[Table 4]

[0035]

Example 3 Lotion (Preparation method) The components of (A) shown in Table 5 were mixed and dissolved at room temperature. On the other hand, each component of (B) was also mixed and dissolved at room temperature. The component (B) was added to the component (A) and solubilized to obtain a lotion.

[0036]

[Table 5]

[0037]

Example 4 Packing Charge (Production Method) The component (A) was dispersed and dissolved at room temperature. The component (B) was added thereto and uniformly dissolved to obtain a pack material.

[0038]

[Table 6]

Industrial Applicability The external preparation for skin of the present invention can suppress the production of melanin, effectively prevent or ameliorate skin pigmentation based on the melanin, and can be used safely without any harm to the skin. can do. Further, the external preparation for skin of the present invention can be used as a cosmetic having an excellent whitening effect.

Claims (4)

[Claims] 1. Pajaro bobo
An external preparation for skin, characterized by containing the extract of o). 2. The external preparation for skin according to claim 1, wherein the extract is extracted with a polar solvent. 3. The external preparation for skin according to claim 1, wherein the extract is contained in an amount of 0.001 to 20% by weight in terms of dry weight based on the total amount of the external preparation. 4. The composition according to claim 1, which is a cosmetic.
An external preparation for skin according to Item.