JPH07252128A - Skin external preparation - Google Patents

Abstract

PURPOSE:To obtain a skin external preparation containing extracts of Bletilla striata Reichb. fil. known as a raw material for galenical medicines having pharacodynamic effects of hemostasis, drainage, mucilaginous property, etc., from ancient times as active ingredients, being safe to skin and capable of preventing, relieving and suppressing liver-spot, ephelis, blackening, etc. CONSTITUTION:An above-ground part such as a leaf part, a stem part or flower part, fruit, a ground bulb part or whole grass of Bletilla striata Reichb. fil., preferably the ground bulb part thereof is, as necessary after drying or pulverizing, extracted using a proper solvent. The resultant extract is blended as an active ingredient to provide the objective skin external preparation. This skin external preparation is effective in prevention of liver-spot, ephelis, dark complexion, etc., or relief of symptom or suppression of exacerbation. Further, the skin external preparation can effectively be used as a cosmetic, a medicated cosmetic or an external medicine in order to carry out beautifying of skin such as recovery of skin after sun-burn or snow-burn. This skin external preparation is excellent in safety as well as stability with the lapse of time.

Description

Detailed Description of the Invention

[0001]

FIELD OF THE INVENTION The present invention relates to an external preparation for the skin, the purpose of which is extremely high in safety for the skin, prevention of spots, freckles, dark skin, etc. or alleviation of symptoms and suppression of aggravation, as well as sunburn and snow. An object of the present invention is to provide a skin external preparation that can be effectively used as a cosmetic, a cosmeceutical, or an external medicine for the purpose of whitening the skin such as recovery of skin after burn.

[0002]

2. Description of the Related Art Stain, freckles, and dark skin are derived from the deposition of skin pigment (melanin), and as it has been said for a long time that "white skin is difficult to remove," these pigmentation symptoms affect women. It is said to be the biggest cause of worries, and whitening cosmetics has been an extremely serious problem. Therefore, the stain,
The topical whitening agent for improving, alleviating or preventing pigmentation symptoms such as freckles has been of great interest to consumers from the viewpoint of basic beauty and treatment. Conventionally, whitening agents such as ascorbic acid, glutathione, and sulfur preparations have been mainly used for such external whitening agents.
In particular, ascorbic acid has long been known to be effective for abnormal pigmentation of the skin such as Lille melanosis. That is, ascorbic acid inhibits tyrosine-tyrosinase action in the mechanism of melanin production in the skin, or inhibits melanin production in order to produce doperquinone by reducing melanin-producing intermediate doperchrome in the opposite direction of its metabolic process. It is said that this suppresses abnormal pigmentation of the skin. Therefore, conventionally, ascorbic acid has been orally administered in the dermatological field for acquired pigmentation such as spots and reel melasma. However, since ascorbic acid is water-soluble and has problems with skin absorbability and oxidative stability, when applied to external preparations such as whitening cosmetics or medical ointments, esterification products with higher fatty acids and phosphoric acid are used. (Fat-soluble ascorbic acid). On the other hand, it has been reported that drugs such as glutathione and sulfur preparations also have an action of inhibiting melanin production, and they have been widely blended in external preparations for the purpose of preventing spots, freckles and the like and for alleviating symptoms.

[0003]

However, even if the above-mentioned ascorbic acid derivative or glutathione is used as a skin external preparation, there is a problem that the whitening effect is not sufficiently satisfied. Further, glutathione and sulfur preparations have a peculiar offensive odor, and when they are mixed with water-soluble cosmetics, precipitation may occur, which is not sufficient for general use as an additive for cosmetics, etc. Were present.

Therefore, in the field of skin external preparations for whitening such as spots, freckles, and dark skin, which are of great interest to consumers for basic beauty, they are extremely safe without causing skin disorders and have symptoms. It has been desired to create a skin external preparation that is extremely effective in alleviating and preventing the above-mentioned problems and is excellent in stability over time.

[0005]

In the present invention, silane (Bl
etilla striata Reichb. fil.) extract is provided as an active ingredient to provide an external preparation for skin, which solves the above conventional problems.

[0006]

The constitution of the external preparation for skin according to the present invention will be described in detail below. In this invention, silane (Bletilla str
iata Reichb. fil.) extract is the active ingredient. Here, silane (Bletilla striata Reichb. Fil.) Means orchid (Orchidacaceae) distributed in Japan and China west of Kanto.
(eae), a perennial herb that has spherical, white, succulent bulbs lined up in a row underground, with several leaves arriving in the lower half of the stem that is about 50 cm in height, and the leaf blades are oblong. 15-30 cm in length and 3-5 in width
Reach cm, sharp on both ends, with many longitudinal veins. The flowers are large, with 3 to 8 flowers, and are plants that are lined up on the top of the stem. still,
Dried subterranean bulbs of this silane (Bletilla striata Reichb.fil.)
ETILLAE TUBER) ”and has been used since ancient times as one of the crude drug prescriptions that have medicinal effects such as hemostasis, drainage, and slime.

The silane used in the present invention (Blet
(illa striata Reichb. fil.) is not particularly limited, and leaves, stems, above-ground parts such as flowers, fruits, underground bulbs, or whole plants can be arbitrarily used, More desirably, the underground bulb portion is preferably used. Such silane (Bletilla striata Reichb. Fil.) Is dried if necessary, pulverized, and extracted with an appropriate solvent. Any solvent can be used without particular limitation as long as it is a solvent generally used for plant extraction, such as a polar solvent, a non-polar solvent or a mixed solvent thereof.

Specific examples of the polar solvent include water, alcohols such as methanol, ethanol, isopropanol, n-propanol, isobutanol, n-hexanol, methylamyl alcohol, 2-ethylbutanol and n-octanol, ethylene glycol, Polyhydric alcohols such as ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, propylene glycol, propylene glycol monomethyl ether, propylene glycol monoethyl ether, triethylene glycol, 1,3-butylene glycol and hexylene glycol, or derivatives thereof, acetone , Methylacetone,
One or more mixed solvents of ketones such as methyl ethyl ketone, methyl isobutyl ketone and methyl-n-propyl ketone, esters such as ethyl acetate and isopropyl acetate, ethers such as ethyl ether, isopropyl ether and n-butyl ether. Is exemplified as a preferred embodiment, but is not particularly limited.

As the non-polar solvent, petroleum ether, n-
Hexane, n-pentane, n-butane, n-octane,
Examples of suitable solvents include aliphatic hydrocarbons such as cyclohexane, carbon tetrachloride, chloroform, dichloromethane, trichloroethylene, benzene, toluene and the like, or a mixed solvent of two or more thereof, but the invention is not particularly limited thereto.
Further, the mixed solvent of the polar solvent and the non-polar solvent described above can be used without limitation in the present invention.

In the present invention, silane (Bletilla str
(iata Reichb. fil.) extract may be used as it is in the form of a filtrate, or may be used in the form of a powder by evaporating the solution to dryness, and any appropriate one may be adopted. Further, the liquid or powder may be used as it is as an external preparation for skin, but more preferably, it is mixed with a known excipient or diluent, or any other compounding material, and granules, emulsions, It is used after being prepared into a dosage form such as a solution or suspension. As the external preparation for skin in the final form of the present invention, even a cosmetic applied to healthy skin for the purpose of beauty, or a medicinal product having a specific use purpose such as spots, relief of freckles, and recovery of skin after sunburn. It may be a cosmetic (quasi drug) or a drug intended for the treatment of spots and the like, and any form can be adopted. In addition, when preparing these dosage forms, ascorbic acid and its derivatives known as whitening agents, sulfur preparations, glutathione, etc., or known additives such as moisturizers, UV absorbers, vitamins, etc. It can also be used in combination as appropriate as long as the effect of the above is not impaired.

Further, in such a skin external preparation,
At any stage of the manufacturing process, the silane (Bletilla s
triata Reichb. fil.) extract may be blended in any amount. The blending amount may be 0.001% by weight or more, more preferably 0.01% by weight or more as a dry weight, and may be appropriately set depending on the purpose of use and the dosage form.

(Prescription Example) Hereinafter, the constitution of the external preparation for skin according to the present invention will be described in detail with reference to a prescription example. (Formulation Example 1) Lotion formulation weight% Silane (Bletilla striata Reichb. Fil.) 10.0 Ethanol extract of underground bulb Glycerin 6.0 1,3 Butylene glycol 4.0 Polyoxyethylene polyoxypropylene 1.0 Decyl Tetradecyl ether Preservative Suitable amount Fragrance Suitable amount Purified water Balance 100.0

(Formulation example 2) Cream formulation weight% Silane (Bletilla striata Reichb. Fil.) 0.1 Ethanol extract of subterranean bulb (dry product) Stearyl alcohol 5.0 Stearic acid 2.0 Hydrogenated lanolin 3. 0 Squalane 10.0 Octyldodecanol 10.0 Propylene glycol 5.0 Polyoxyethylene cetyl ether 2.4 Glycerin monostearate 1.6 Preservative proper amount Fragrance proper amount Purified water balance 100.0

(Formulation Example 3) Emulsion type weight% Silane (Bletilla striata Reichb. Fil.) 0.2 Ethanol extract of whole plant (dry matter) Squalane 5.0 Vaseline 2.0 Beeswax 0.5 Sorbitan sesquiolein Acid ester 0.5 Polyoxyethylene oleyl ether 0.8 Glycerin 5.0 Carboxyvinyl polymer 0.2 Potassium hydroxide 0.1 Preservative proper amount Fragrance proper amount Purified water balance 100.0

[0015]

EXAMPLES The effects of the external preparation for skin according to the present invention will be further clarified below with reference to Examples. However,
The present invention is not limited to the following examples. (Example 1) Silane (Bletilla striata Reichb. Fil.)
Add 50 ml of ethanol to 100 g of dry ground material of underground bulb,
It was immersed at room temperature for a whole day and night for extraction, and the extract was filtered and ethanol was concentrated to obtain 0.82 g of the extract, which was used as the whitening agent of Example 1. (Comparative Example 1) Ascorbic acid phosphate magnesium salt was used as the whitening agent of Comparative Example 1. (Comparative Example 2) Reduced glutathione was used as the whitening agent of Comparative Example 2.

[0016]

[Test example]

(Test Example 1) Measurement of tyrosinase biosynthesis inhibitory activity B16 melanoma 4F5 (RIKEN Cell Bank) cultured in 10% FBS-DMEM was seeded on a 96 well plate at 5 × 10 ⁴ cells / well (total amount 195 μl), The cells were cultured under the conditions of 37 ° C and 5% -CO ₂ for 24 hours. The whitening agents obtained in the above Examples and Comparative Examples were added to the final concentrations of 5, 10, 50 and 100, respectively.
, 50% ethanol / PBS solution to 500ppm, sterilized by filtration with 0.2μm membrane filter, and add 5μl each.
It was cultured for 24 hours. After completion, remove the culture solution and use 1% Tr
After solubilizing the cell membrane with 50 μl of iton X-100 / PBS solution,
100 μl of 10 mM L-DOPA was added as a substrate and reacted at 37 ° C. for 4 hours. The reaction was stopped by adding 50 μl of methanol to this reaction system, and a wavelength of 47
Absorbance at 5 nm was measured. As a control, the absorbance of the reaction system without the addition of the whitening agent of the Examples and Comparative Examples was measured, and the tyrosinase biosynthesis inhibition rate (%) was calculated from these absorbances based on the following equation. A: Absorbance without addition of whitening agent of Examples and Comparative Examples (475 nm) B: Absorbance with addition of whitening agent of Examples and Comparative Examples (475 nm) Table 1 shows the results.

[0017]

[Table 1]

(Test Example 2) Measurement of cell viability B16 melanoma 4F5 (RIKEN Cell Bank) cultured in 10% FBS-DMEM was seeded on a 96 well plate at 5 × 10 ⁴ cells / well (total volume: 195 μl). ), And was cultured for 24 hours under the conditions of 37 ° C and 5% -CO ₂ . The whitening agents obtained in the above Examples and Comparative Examples were added to the final concentrations of 5, 10, 50 and 100, respectively.
, 50% ethanol / PBS solution to 500ppm, sterilized by filtration with 0.2μm membrane filter, and add 5μl each.
It was cultured for 24 hours. The viability of the cultured cells was measured by the MTT test method. First, remove the culture solution and
D-MEM medium containing 10% 5 mg / ml MTT solution was added to the cells. This was reacted at 37 ° C for 4 hours. After the reaction, 0.04
After adding 100 μl of N hydrochloric acid-isopropanol solution and developing color for 30 minutes, the absorbance at wavelengths of 570 nm and 655 nm was measured. As a control, the absorbance was measured without adding the whitening agent of the Examples and Comparative Examples, and the cell viability (%) was calculated from these absorbances based on the following formula. C: Absorbance when the whitening agents of Examples and Comparative Examples were added (value at 570 nm-value of 655 nm) D: Absorbance when no whitening agents of Examples and Comparative Examples were added (value at 570 nm-value of 655 nm) The results are shown in Table 2.

[0019]

[Table 2]

As is clear from the results of Test Example 1, the whitening agents of the Examples have a low concentration of 500 ppm,
The inhibitory effect on tyrosinase biosynthesis was about 50%. Moreover, it was confirmed that the whitening agents of the Examples exhibit a significantly higher tyrosinase biosynthesis inhibitory rate than the ascorbic acid ester and glutathione that have been conventionally used as whitening agents, and a sufficient whitening effect is expressed. . further,
Sufficient tyrosinase biosynthesis inhibitory effect was observed at 500 ppm
At the level of concentration, no toxicity to cells was observed, indicating that the whitening agents of the examples are highly safe.

[0021]

As described above in detail, since the present invention is an external preparation for skin characterized by containing a silane (Bletilla striata Reichb. Fil.) Extract as an active ingredient, it is also clear from the results of the above test examples. As described above, it is extremely safe for the skin, and exhibits an effective tyrosinase biosynthesis inhibitory effect, preventing spots, freckles, dark skin, etc. or relieving symptoms or suppressing aggravation, as well as sunburn and skin after snowburn. It has an excellent effect that it can be effectively and versatilely used as a cosmetic, a cosmeceutical, or an external medicine for the purpose of whitening the skin such as recovery.

 ─────────────────────────────────────────────────── ─── Continuation of the front page (72) Inventor Noriyuki Fujiwara 5-12, 12kencho, Chuo-ku, Osaka City Mandom Central Research Institute, Inc.

Claims (1)

[Claims] 1. Silane (Bletilla striata Reichb. Fi
l.) A skin external preparation characterized by comprising an extract as an active ingredient.