WO2002005757A1

WO2002005757A1 - External preparations for beautifying the skin

Info

Publication number: WO2002005757A1
Application number: PCT/JP2001/006185
Authority: WO
Inventors: Rikako Furuya; Osamu Moro; Ohji Ifuku; Kenichi Umishio
Original assignee: Shiseido Company, Ltd.
Priority date: 2000-07-19
Filing date: 2001-07-17
Publication date: 2002-01-24
Also published as: JP2002029959A; KR100825839B1; CN1229094C; KR20020047148A; CN1443056A; TWI281865B; JP4233734B2

Abstract

External preparations for beautifying the skin, which contain as the active ingredient R. centifolia L. or R. gallica L. var. centifolia (L.) Reg., both of which belong to the genus Rosa of the family Rosaceae, or solvent extracts thereof. The preparations exhibit inhibitory activities against tyrosinase and the production of cyclic AMP (cAMP), have excellent melanism-inhibiting and beautifying effects, and are excellent in safety.

Description

Specification

Skin whitening preparation for external use

Technical field

The present invention relates to a skin whitening external preparation containing a specific plant extract. The skin whitening preparation of the present invention has both a tyrosinase activity inhibitory effect and a cyclic AMP (cAMP) production inhibitory effect, has an excellent melanin production inhibitory effect, a whitening effect, and is excellent in safety. is there. Background art

Pigmentation of skin spots, freckles, etc., is caused by abnormal secretion of hormones, ultraviolet rays, inflammatory stimuli, etc., which activates the melanin production signal transduction pathway in epidermal pigment cells to produce and activate tyrosinase, the main enzyme of melanin production. Increased expression results from excessive deposition of melanin on the epidermis.

As a means for preventing such spots and freckles, substances that inhibit the activity of tyrosinase, the main enzyme of melanin production, have been conventionally used. Specifically, creams containing kojic acid, ellagic acid, etc., which have the mechanism of action to capture copper ions essential for the expression of tyrosinase activity, topical application such as lotions, and substrate tyrosine The topical application of creams and lotions containing a hydroquinone derivative, resorcinol derivative, etc., which has a similar structure to that of tyrosinase competition inhibitor, or a substance with an action mechanism other than the above, Administration of L-ascorbic acid has been performed with the mechanism of suppressing melanin production by reducing dopaquinone, a melanin precursor, to dopa.

The above-mentioned substances act on produced tyrosinase or on dopaquinone produced by expressing tyrosinase activity, and do not inhibit tyrosinase production itself. Therefore, the effect itself and its There was a drawback that the continuity was weak. In addition, L-ascorbic acid has poor stability in the drug substance and the base, and a large amount of L-ascorbic acid is required to sufficiently prevent spots and freckles.

In recent years, various active ingredients contained in plant extracts have been receiving attention. Various effects have been reported, including antioxidant effects of polyphenols contained in many plants, including antitumor effects. A variety of plant extracts having a whitening effect are also being sought.

Roses (Rosaceae) Rosaaceae (Rosa) are known as whitening plants that have a whitening effect, such as Kinsakurako and Yatsumi. These plant extracts also have the effect of inhibiting tyrosinase activity. It was a mechanism, and the whitening effect and its persistence were not satisfactory.

On the other hand, as a substance that acts on the signal transduction pathway and inhibits the production itself, there have been reported camilles having a nitric oxide pathway inhibitory action and a protein kinase C pathway inhibitory action. However, these transduction pathways have low involvement in melanin production, and it is difficult to obtain remarkable inhibition of melanin production. Therefore, the development of better plant extract medicinal agents has been expected.

The present inventors have conducted intensive studies in view of the above circumstances, and as a result, the extract of a specific plant has both an inhibitory effect on tyrosinase activity and an inhibitory effect on the adenylate cyclase pathway, which is highly involved in melanin production, and has an excellent whitening effect. The inventors have found that there is an excellent melanin production inhibitory effect, and have completed the present invention. Disclosure of the invention

That is, the present invention relates to Rosaceae (R. centif olia L. or R. gall ica L. var. Centif olia (L.) Reg.) Or a solvent thereof belonging to the genus Rosa (Rosa). An external preparation for whitening skin characterized by containing an extract as an active ingredient.

The present invention also comprises the above plant or a solvent extract thereof as an active ingredient. A melanin production inhibitor, a tyrosinase activity inhibitor, and a cyclic AMP (cAMP) production inhibitor are provided. BEST MODE FOR CARRYING OUT THE INVENTION

Hereinafter, the present invention will be described in detail.

The skin whitening agent for external use, melanin production inhibitor, tyrosinase activity inhibitor, and cyclic AMP (cAMP) production inhibitor of the present invention are R. centifolia belonging to the family Rosaceae and Rosa. L. or R. gallica L. var. Centifolia (L.) Reg.) Or a solvent extract thereof as an active ingredient.

The cabbage rose (Cabbage Rose, Provanc e Rose) used in the present invention is a horticultural species cultivated mainly in the southern part of Europe from the Greek-Roman era to the Renaissance era. It is a heavy valve and is of hybrid origin (R. bifera X R. alba).

Centifolia L. or R. gallica L. var. Centifolia (L.) Reg.) Can be used either raw or dried. Force S, Usability, Formulation etc. Therefore, it is preferable to use it as a dry powder or a solvent extract.

It is preferable to use flowers or whole plants as the site of R. centifolia L. 7; this is R. gallica L. var. Centifolia (L.) Reg. It can also be used.

The solvent extract of the above plant can be obtained by a conventional method. For example, it can be obtained by immersing or heating under reflux with an extraction solvent, followed by filtration and concentration. As the extraction solvent, any solvent can be used as long as it is a solvent generally used for extraction. Examples of the solvent include water, alcohols such as methanol, ethanol, propylene glycol, 1,3-butylene glycol and glycerin, and hydrous alcohols. Black form, dichloroethane, carbon tetrachloride, acetone, ethyl acetate, hexane And the like can be used alone or in combination. The extract obtained by extraction with the above solvent is used as is, or the concentrated extract is subjected to an adsorption method, for example, after removing impurities using an ion exchange resin, or a column of a porous polymer (for example, Amberlite XAD-2). After adsorption, elution with methanol or ethanol and concentration can also be used. A partitioning method, for example, an extract extracted with ethyl acetate or the like is also used. The plant extract thus obtained is highly safe and has excellent whitening effect, melanin production inhibitory effect, tyrosinase activity inhibitory effect, and cyclic AMP (cAMP) production inhibitory effect.

When the above-mentioned plant extract is used in combination with an external preparation for whitening skin, it is preferable to add 0.001 to 5.0% by weight, more preferably 0.000% by weight, as a dry weight in the total amount of the external preparation. 1 to 3.0% by weight, particularly preferably 0.00001 to: L. 0% by weight.

When the above plant extract is used in combination with a skin whitening agent for external use, in addition to these extracts, other extracts usually used for skin external agents such as cosmetics and pharmaceuticals may be used as long as the effects of the present invention are not impaired. Components such as an oil, a wetting agent, an ultraviolet absorber, an antioxidant, a surfactant, a preservative, a humectant, a fragrance, water, an alcohol, a thickener, and the like can be appropriately added as needed.

Examples of the ultraviolet absorbers described in the preceding paragraph include 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxybenzophenone-15-sodium sulfonate, sodium benzotriazolylbutylphenol sulfonic acid, and methylene bis. Benzotriazoinoletetramethinolebutynolepheno, such as benzophenone derivatives, otatyl paramethoxycinnamate, mono-2-diparamethoxycinnamate glyceryl hexanoate, isopentyl trimethoxycinnamate trisiloxane, etc. Methoxycinnamic acid derivatives, perocanic acid, 4-tert-4'-methoxydibenzoinolemethane, bis-ethylenoxyhexynoleoxyphenolene methoxy phenyl triazine, ethylhexyl triazone, phenylbenziimi Dazole sulfonic acid and the like can be appropriately compounded as needed.

Furthermore, sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, dalconic acid, caffeine, tannin, verapamil, tranexamic acid and derivatives thereof, licorice Extracts, grabradine, various crude drugs, drugs such as tocopherol acetate, glycyrrhizic acid and its derivatives or their salts, vitamin C, magnesium ascorbate phosphate, darcoside ascorbate, arbutin, kojic acid, resorcinol, ellagic acid, and potato extract Other whitening agents such as foodstuffs, sugars such as gnorecose, fructose, mannose, sucrose, trehalose and the like can also be appropriately blended.

In addition, the skin whitening agent for external use of the present invention can be widely applied to cosmetics, pharmaceuticals, quasi-drugs, and the like, particularly preferably applied to the outer skin. Any solution that is applicable to any of the following: solution system, solubilization system, emulsification system, powder dispersion system, water-oil-two-layer system, water-oil-powder three-layer system, ointment, gel, azole, etc. Is applied.

The form of use of the skin whitening external preparation of the present invention is also optional. For example, in addition to facial cosmetics and foundations such as lotions, emulsions, creams, and packs, makeup cosmetics, aromatic cosmetics, It can be used as a bath agent and the like.

In addition, the form which the skin whitening agent for external use of the present invention can take is not limited to the above dosage form and use form. Example

Next, the present invention will be described in more detail with reference to examples, but the technical scope of the present invention is not limited by these examples. In addition, all compounding amounts are weight%.

Prior to the examples, the tyrosinase activity inhibiting effect, the cyclic AMP (cAMP) production inhibiting effect, the melanin production inhibiting effect and the beauty of the plant extract of the present invention are described. The test method and evaluation method for the white effect will be described.

[Test method and evaluation method]

1. Sample preparation

50 g of flowers of R. centifolia L. or R. gallica L. var. Centifolia (L.) Reg.) Were warm-extracted with water to obtain an extract. The extract was concentrated to obtain 5 g of a plant extract.

The above plant extract was dissolved in 70% ethanol to a concentration of 2% by weight to obtain a plant extract-containing solution. The concentration of the plant extract-containing solution was adjusted by diluting the solution, and this was used as a sample solution, and the following experiment was performed.

2. Cell culture method

B16 melanoma cultured cells from mice were used. 1 0% FBS and Teofi Li down (0. 0 9 mg / ml) , or Meranosai preparative stimulating hormone (α- MSH) C 0 ₂ incubator base one coater with Dulbecco's MEM medium containing (Ι Ο ηΜ) (9 5 % The cells were cultured at 37 ° C in air, 5% carbon dioxide).

3. Measurement of tyrosinase activity inhibitory effect

The cells cultured by the above second method were seeded in 96 plates, the final concentration (dry extract in terms of concentration) of the sample solution after 24 hours incubation was added to a 1 0 one ⁷ to 1 0 ⁵ wt%, further Culture was continued. After 3 days of culture, the cells were washed with PBS, PBS containing l% Triton was added, and DOPA was added to a final concentration of 1 mM.

The absorbance (475 nm) at 0 and 60 minutes after the addition was measured. It was compared with a sample to which no plant extract was added (control; 70% ethanol) and evaluated according to the following criteria. As a reference example, an extract of rose (Rosa canina L.) belonging to the same genus Rosaceae (Rosa) (extracted with ethanol) , The same test as above was performed. Table 1 shows the results. Table 1 shows the results in a medium containing melanosite-stimulating hormone (α-MSH). The same results were obtained when theophylline was used.

(Judgment criteria)

〇: Superior in tyrosinase activity inhibitory effect compared to control.

Δ: Slightly superior to tyrosinase activity inhibitory action compared to control.

X: No tyrosinase activity inhibitory action. table 1

4. Visual judgment of melanin amount (melanin production suppression effect)

Seeded cells cultured in the second method in 9 6 plates, the final concentration (dry extract in terms of concentration) of the sample solution 2 4 hours of culture was added to a 1 0 ² to 1 0 ⁵ wt% The culture was further continued. After 3 days of culture, place a diffusion plate on the lid of a 96-well plate, observe the amount of melanin in the cells with an inverted microscope, and compare with the sample without added plant extract (control; 70% ethanol) And evaluated according to the following criteria. In addition, as a reference example, the same test as described above was performed on an extract (Rosa canina L.) extract (ethanol extracted) belonging to the same genus Rosaceae (Rosa). Table 2 shows the results. Table 2 shows the results in a medium containing melanosite-stimulating hormone (a-MSH), but the same results were obtained when theophylline was used.

(Judgment criteria) 〇: Whiter than control (excellent in inhibiting melanin production).

Δ: slightly whiter than control (slightly superior in melanin production inhibitory action), X: whiteness comparable to control (no melanin production inhibitory action). Table 2

5. Cyclic AMP (c AMP) production inhibitory effect measurement

Seeded with B 1 6 melanoma culture cells from mice 1 2 © El plates, 1 0% C_〇 Dar Beck co MEM medium containing FBS ₂ Inkyubeta one (95% air, 5% carbon dioxide) inside, Culture was performed at 37 ° C. The medium was aspirated after 24 hours incubation, Meranosai preparative stimulating hormone (a- MSH, 0. 1 ηΜ) , and I the sample solution to a final concentration of 1 0- ^1-1 0- ^3% by weight (dry extract in terms of concentration) Serum-free medium added as above. After incubation for 30 minutes, remove the medium, collect the cells with TE buffer, transfer to a 1.5 mL microtube, boil, and then cycle the amount of cyclic AMP (cAMP) in this solution. The measurement was performed using an AMP (cAMP) measurement kit (manufactured by Amersham). In addition, as a reference example, the same test as above was performed on an extract (ethanol extracted) of Novara (Rosa canina L.) belonging to the same Rosaceae (Rosa). It was compared with a sample to which no plant extract was added (control; 70% ethanol) and evaluated according to the following criteria. Table 3 shows the results.

(Judgment criteria)

〇: Superior to cyclic AMP (c AMP) production inhibitory effect than control. Δ: Slightly superior to cyclic AMP (c AMP) production inhibitor as compared to control.

X: No cyclic AMP (cAMP) production inhibitory action. Table 3

6. Whitening effect test

(Test method)

The test sample solution shown below was applied to the back skin of 20 subjects exposed to the sunlight in summer for 4 hours (2 hours a day for 2 days) once a day in the morning and evening for 4 weeks. Evaluation was performed according to the criteria. Table 4 shows the results of the average value of the evaluation points of the 20 subjects.

(Test sample solution)

Ingredients

(Alcohol phase)

9 5% ethanol 25.0

Polyoxyethylene (25 mol)

Hydrogenated castor oil ether 2.0

Methyl paraben 0.1

Djibutinorehi Droxytonoren 0.01

Fragrance 0.05

(Aqueous phase)

Glycerin 2.0 1,3-butylene glycol cornole 1.0

Ion exchange water residue

Chemicals (shown in Table 4. In the table, the amount is dry weight.)

(Formulation method)

After preparing the aqueous phase and the alcohol phase respectively, mixing and solubilizing _c

(Evaluation method)

The lightening effect after use was determined based on the following criteria

(Score)

After 4 consecutive applications, a lightening effect was remarkably observed.

After three consecutive applications, a lightening effect was observed.

After two consecutive applications, a slight lightening effect was observed.

After one continuous application, no lightening effect was observed. Table 4

As is clear from Table 4, the product of the present invention, especially _c it can be seen that an excellent whitening effect, even compared already Asukorubin acid derivatives are known to a skin whitening effect, the placental extract formulation examples, The product of the present invention is excellent in whitening effect Was observed.

Hereinafter, examples of the formulation of the skin whitening external preparation of the present invention in various dosage forms will be described as Examples. The amount of the plant extract is the amount of the dried residue. Example 3 Burnishing cream

Ingredients (% by weight)

(1) Stearic acid 6.0

(2) Sorbitan monostearate 2.0

(3) Polyoxyethylene (20 mol)

Sorbitan monostearate 1.5

(4) Arbutin

(5) Sodium bisulfite 0.03

(6) Propylene glycol Cornole 7.0

(7) Glycerin 3.0

(8) Parasitic extract (water extract) 1.0

(9) Etilparaben 0.1

(10) Butyl paraben 0.1

(11) Thiotaurin 0.01

(12) Fragrance 0.1

(13) Ion-exchanged water 72. 1 6

(Formulation method)

(4), (6), (7), and (8) were added to (13), and the mixture was heated and maintained at 70 ° C (aqueous phase). On the other hand, (1) to (3), (5), (9) to (; 12) were mixed, heated and melted, and kept at 70 ° C (oil phase). The oil phase was added to the aqueous phase, pre-emulsified, homogenized uniformly with a homomixer, and cooled to 30 ° C with good stirring to obtain a burnishing cream. Example 4 Neutral cream Ingredients (% by weight)

(1) Stearinole alcohol 5.0

(2) Stearic acid 0

(3) Hydrogenated lanolin 0

(4) 2-Hydroxy-1- 4-methoxybenzophenone 0

(5) Squalane 0

(6) 2-octyl deserial call 0

(7) Polyoxyethylene (25 mol)

Setino Leano Reconoreethenore 3 0

(8) Glycerin monostearate 20

(9) Placental extract G1

(10) Propylene Darcol 20

(11) 1,3 Butylene recall 3 0

(12) Rose extract (water extract) 5 0

(13) Fragrance 0 2

(14) 1, 2 —pentanediol 0 5

(15) Butyl paraben 0 1

(16) Hipotaurine 0 0 1

(17) Ion exchange water 6 5 6 9

(Formulation method)

(9) to (12) and (16) were added to (17), and the mixture was heated and maintained at 70 ° C (aqueous phase). On the other hand, (1) to (8) and (13) to (; 15) were mixed, heated and melted, and kept at 70 ° C (oil phase). The oil phase was added to the aqueous phase, pre-emulsified, homogenized uniformly with a homomixer, and cooled to 30 ° C with thorough stirring to obtain a neutral cream. Example 5 Cold cream

Ingredients (% by weight) (1) Solid paraffin 5.0

(2) Beeswax 5.0

(3) Vaseline 5.0

(4) Liquid paraffin 20.0

(5) Squalane 1 0.0

(6) Glycerin monostearate 2.0

(7) Polyoxyethylene (20 mol)

Sorbitan monolaurate 2.0

(8) Kojic acid 2.0

(9) 2-hydroxy-1-4-methoxybenzophenone

One 5-sodium sulfonate 3.5

(10) Stone powder 0.1

(11) Borax 0.2

(12) Rosemosa extract (water extract) 0.1

(13) Ion-exchanged water 44.5 5

(14) Fragrance 0.2

(15) Ethilparaben 0.2

(16) Butyl paraben 0.1

(17) Butyl hydroxytoluene 0.0 5

(Formulation method)

(8), (10), (11) and (12) were added to (13), and the mixture was dissolved by heating and kept at 70 ° C (aqueous phase). On the other hand, (1) to (7), (9) and (14) to (17) were mixed, melted by heating, and kept at 70 ° C (oil phase). The oil phase was gradually added to the aqueous phase while stirring, and after the reaction _{c was} completed, the mixture was uniformly emulsified with a homomixer. After the emulsification, the mixture was cooled to 30 ° C. while stirring well to obtain a cold cream. Example 6 Nutrition cream Ingredients (% by weight)

(1) Dimethyl distearyl chloride

Criteria for ammonia processing 2.0

(2) Polyoxyethylene

Methyl polysiloxane polymer 0.1

(3) Liquid paraffin 1 0.0

(4) Vaseline 5.0

(5) Cetyl octanoate 20.0

(6) L-sodium glutamate 0.0 1

(7) Dipropylene glycol 5.0

(8) Methylparaben 0.2

(9) Sodium hyaluronate 0.0 5

(10) Vitamin E acetate 0.02

(11) Parasitic extract (water extract) 2.0

(12) Ion-exchanged water 5 5.6.2

(Formulation method)

After heating (2), (3) and (5) to 50 ° C, (4) and (10) were added, and (1) was added to the completely dissolved oil phase parts to perform uniform dispersion. To (12), add the aqueous phase parts, in which (6), (7), (8), (9), and (11) are dissolved, to 50 ° C and add them to HM. Then, the mixture was cooled to room temperature to obtain a water-in-oil emulsion composition. Example 7 Emulsion

Ingredients (% by weight)

(1) Polyoxyethylene (10 mol)

Estoleno monooleate 2.0

(2) Octyl paramethoxycinnamate 3.5

(3) Liquid paraffin 2.0 (4) Cyclopentadimethy ^ / siloxane 1.0

(5) Squalane 3.0

(6) 1,3-butylene glycol5.0

(7) Arbutin 2.0

(8) Sodium bisulfite 0.03

(9) Glycerin 2.0

(10) Ethanol 5.0

(11) Carboxyl polymer 0.3

(12) Hydroxypropyl cellulose 0.1

(13) Hydrogenium hydroxide 0.15

(14) Etinole Paraben 0.1

(15) 1,2-pentanediol 1.0

(16) Paramecium extract (water extract) 0.5

(17) Ion exchange water 72.02

(18) Fragrance 0.3

(Formulation method)

(17) and (10) are dissolved by heating (16) and (7), and (6), (8), (9), (11) and (13) (Aqueous phase). On the other hand, (1)-(5), (14), (15).

(18) was mixed, heated and melted, and kept at 70 ° C (oil phase). Add oil phase to water phase, pre-emulsify, homogenize homogeneously with homomixer, and after emulsification, mix well

After cooling to 30 ° C, an emulsion was obtained. Example 8 Emulsion

Ingredients (% by weight)

(1) Polyoxyethylene (20 mol) Polyoxy

Propylene (2 mol) Cetyl alcohol 1.0

(2) Octyl-p-methoxycinnamate 3.5 (3) “Silicone KF966” (20 cs) 2.0

(Shin-Etsu Chemical Co., Ltd.)

(4) Liquid paraffin (medium viscosity) 3.0

(5) 4-1-tert-Ptinolemethoxydibenzoinolemethane 0.3

(6) Glyceryl tri-2-ethylhexanoate 1.0

(7) Arbutin 2.0

(8) Sodium bisulfite 0.0 3

(9) Glycerin 2.0

(10) Ethanore 3.0

(11) Carboxyvinyl polymer 0.3

(12) Hydroxypropyl cellulose 0.1

(13) Potassium hydroxide 0.1

(14) 1,2-pentanediol 2.0

(15) Phenoxyethanol 0.2

(16) Acacia rose extract (hydrous alcohol extract) 0.1

(17) Ion exchange water 79. 3 7

(Formulation method)

(17) and (10) are dissolved in (16) and (7) by heating, and (6), (8), (9), (11)-(13) and (15) are dissolved. , Kept at 70 ° C (aqueous phase). On the other hand, (1) to (5) and (14) were mixed, heated and melted, and kept at 70 ° C (oil phase). The oil phase was added to the aqueous phase, pre-emulsified, homogeneously emulsified with a homomixer, and after emulsification, cooled to 30 ° C with good stirring to obtain an emulsion. Example 9 Emulsion

Ingredients (% by weight)

(1) Polyoxyethylene (20 mol) Polyoxy

Propylene (2 monoles) Cetyl alcohol 1.0 1

(2) Paramethoxycinnamic acid mono-2-

Glycerinol hexanoate 2.0

(3) “Silicone KF 96” (20 cs) 2.0

(Shin-Etsu Chemical Co., Ltd.)

(4) Squalane 3.0

(5) 1, 3—butylene glycol Cornole 5.0

(6) Ascorbic acid 2-Darcoside 3.0

(7) Polyethylene glycol 400 3.0

(8) Glycerin 2.0

(9) Ethanol 5.0

(10) Ripoxybininole polymer 0.3

(11) Hydroxypropyl senorelose 0.1

(12) Potassium hydroxide 0.1

(13) Butyl paraben 0.1

(14) Phenoxyethanol 0.4

(15) Thiotaurin 0.02

(16) Parasitic extract (dry powder) 0.01

(17) Ion exchange water 72. 87

(18) Fragrance 0.1

(Formulation method)

Dissolve (15), (16) and (6) in (17) and (9), and further dissolve (5), (7), (8), (10)-(12), (14) Dissolved and kept at 70 ° C (aqueous phase). On the other hand, (1) to (4) and (13) and (18) were mixed, melted by heating, and kept at 70 ° C (oil phase). The oil phase was added to the aqueous phase, pre-emulsified, homogenized uniformly with a homomixer, and after emulsification, cooled to 30 ° C with good stirring to obtain an emulsion. Example 10 Emulsion Ingredients (% by weight)

(1) Polyoxyethylene (20 mol) Polyoxy

Propylene (2 mol) Cetyl alcohol 0

(2) “Silicone KF 96” (20 cs) 20

(Shin-Etsu Chemical Co., Ltd.)

(3) Liquid paraffin (medium viscosity) 3.0

(4) Methylene bis-benzotriazolinole

Tetramethylbutylphenol 0

(5) 1,3-butylene glycol 5 0

(6) Glycerin 20

(7) Ethanol 40

(8) Carboxybule polymer 0 3

(9) Hydroxypropyl senorelose 0 1

(10) Hydrogenium hydroxide 0 05

(11) 1,2-pentanediol 10

(12) Butyl paraben 0 1

(13) Kojic acid 30

(14) Rosemary extract 0 00

(1,3-butylene glycol extract)

(15) Deionized water 77.449

(Formulation method)

(13) was dissolved in (15) by heating, and (14), (5) and (10) were further dissolved and kept at 70 ° C (aqueous phase). On the other hand, (1) to (4) and (11) and (12) were mixed, heated and melted, and kept at 70 ° C (oil phase). The oil phase was added to the aqueous phase, pre-emulsified, homogenized uniformly with a homomixer, and after emulsification, cooled to 30 ° C with good stirring to obtain an emulsion. Example 1 1 Emulsion

Ingredients (% by weight)

(1) Stearic acid... 5

(2) Setinoreanorekonore). 5

(3) Beeswax ί. 0

(4) Polyoxyethylene (20 mol)

Estoleno monooleate 0

(5) Glycerin monostearate 10

(6) Ethanol 30

(7) Arbutin 1 0 0

(8) Sodium bisulfite 0 0 3

(9) 1, 3—butylene glycol 50

(10) Polyethylene glycol 400 200

(11) Seymour rose extract 0 0 0 0 5

(1,3-butylene glycol extract)

(12) Ion exchange water 7 3 2 1 9 5

(13) Fragrance 0 1 5

(14) Methyl paraben 0 3

(15) Butyl paraben 0 2

(16) Thiotaurin 0 1

(Formulation method)

(7), (9), (10), and (16) were added to (12), and the mixture was dissolved by heating and maintained at 70 ° C (aqueous phase). (11) was added to (6) and dissolved (alcohol phase). On the other hand, (1) to (5), (8), (13), (14), and (15) were mixed, heated and melted and kept at 70 ° C (oil phase). _{C The} oil phase was added to the aqueous phase. The mixture was pre-emulsified and homogenized uniformly with a homomixer. The alcohol phase was added while stirring this. Thereafter, the mixture was cooled to 30 ° C with stirring to obtain an emulsion. Example 1 2 Emulsion

Ingredients (% by weight)

(1) Microcrystalline wax 1.0

(2) Beeswax 1.0

(3) Vaseline 2.0

(4) Liquid paraffin 1 0.0

(5) Squalane 5.0

(6) Jojoba oil 5.0

(7) Sorbitan sesquioleate 4.0

(8) Polyoxyethylene (20 mol)

Sonolebitan monooleic acid estenole 1.0

(9) Arbutin 5.0

(10) Sodium bisulfite 0.0 3 (11) Tranexamic acid 5.0

(12) 1, 3-butylene glycol5.0

(13) Sorbitol 2.0

(14) Rosemary extract 0.000 0 1

(1,3-butylene glycol extract)

(15) Bisechino hexinoleoxy

Phenol methoxyphenyl triazine 1.5

(16) Ion-exchanged water 52.0.

(17) Fragrance 0.2

(18) Ethilparaben 0.1

(19) Butyl paraben 0.1

(20) Djibutinolehi Droxitolen 0.05 (Production method) (9) and (11) to (; 14) were added to (16), and the mixture was heated and maintained at 70 ° C (aqueous phase). On the other hand, (1) to (8), (10), (15) and (17) to (20) were mixed, dissolved by heating, and kept at 70 ° C (oil phase). While stirring the oil phase, the water phase was gradually added to the oil phase, and the mixture was uniformly emulsified with a homomixer. After emulsification, the mixture was cooled to 30 ° C. while stirring well to obtain an emulsion. Example 13 Emulsion

Ingredients (% by weight)

(1) Isopropyl alcohol 10.0

(2) Diglyceryl diisostearate 0 5

(3) POE modified dimethyl polysiloxane xanthine 0

(4) Octamethylcyclotetrasiloxane 250

(5) Decamethylcyclopentasiloxane 1 5 0

(6) Trimethylsiloxycyanic acid 50

(7) Yurikuri oil 3 0

(8) Fragrance 0 0 5

(9) Dipropylene glycolone 20

(10) Seymour rose extract 0 0 0 2

(Propylene dalicol extract)

7 0

(12) Sodium bisulfite 0 0 3

Ben 0 1

(14) Edetate trisodium 0 1

(15) Ion exchange water 3 0 7 1 8

(16) Potassium chloride 0 5

(Formulation method)

Dissolve (1) to (8) (oil phase), dissolve (9) to (16) (aqueous phase), and add aqueous phase to oil phase And emulsified to obtain an emulsion _c Example 14

Ingredients (% by weight)

A. Oil phase

Dimethinolepolysiloxane 0 5

Decamethylcyclopentasiloxane 10

Jojoba oil 0 5

B. Aqueous phase

0

Saiyou para extract (water extract) 0 0 0 5

Alkyl-modified carboxyvinyl polymer, 05

Canolepoxy vinyl polymer 0 3

Gum arabic 0 0 5

Echinoreanorekonore 8 0

Trisodium edetate 0 1

Met Paraben 0 1

Phenoxyethanol 0 2

Deionized water 8 8 0 4 5

C. Neutralization

ΚΟΗ 0 5

(Formulation method)

Dissolved (II) phase 'The dissolved (II) phase was added, emulsified, and neutralized with the (C) phase to obtain an emulsion. Example 15 Jelly

Ingredients (% by weight) (1) 95% ethanol 0 0

(2) Dipropylene glycol Cornole 0 0

(3) Glycerin 5 0

(4) Polyoxyethylene (15 mol)

Talent Reino Reanoreko-Nore-Tenore 2 0

(5) Arbutin 0 5

(6) Sodium bisulfite 0 0 3

(7) Ascorbic acid distearate 0 5

(8) Carboxyul polymer (Carbopol 941) 0

(9) Caustic potash 0 1 5

(10) L—Arginine 0 1

(11) Seymour rose extract 0 0 0 1

(50% 1, 3-Petit Lendacol extract)

(12) Fragrance 0.1

(13) Fenoki Shetano 0.4

(14) Ion-exchanged water 7 0.2 1 9

(Formulation method)

(11), (5), (3) and (8) were uniformly dissolved in (14) (aqueous phase). On the other hand, (1) ^ (2), (4), and (6), (7), (12), and (13) were dissolved and added to the aqueous phase. Then, the mixture was neutralized and thickened by (9) and (10) to obtain jelly. Example 1 6 peel-off type pack

Ingredients (% by weight)

(Alcohol phase)

9 5% Ethano 10.0

Polyoxyethylene (15 mol)

Oleyl alcohol ether 2.0 Etylhexyltriazone 0

Methyl paraben 0 3

Phenoxy ethanol

Fragrance 0 2

(Aqueous phase)

Seymour rose extract 0

(50% 1,3-butylene glycol extract)

Ten

Sodium bisulfite 0 0 3

Polyvinyl alcohol 1 2 0

Glycerin 3 0

Polyethylene glycol 1 5 0 0 1 0

Deionized water 6 8 1 7

(Formulation method)

Prepare an aqueous phase at 80 ° C, cool to 50 ° C, add the alcohol phase prepared at room temperature, mix uniformly, and allow to cool. Example 17 Pack with powder

Ingredients (% by weight)

(Alcohol phase)

95% ethanol 5.0

Methyl paraben 0.1

1, 2-pentanediol 2.0

Fragrance 0.3

Ascorbic acid diol 1.0

(Aqueous phase)

Seymour rose extract 3.0 (50% 3-butylene 'recall extract)

Ten

Dipropylene glycol 3 0

Polyethylene glycol 1 500 0 5

Zinc flower 1 5 0

Power Olin 8 0

Ion exchange water 6 1 1

(Formulation method)

The aqueous phase was uniformly prepared at room temperature. Then, the alcohol phase prepared at room temperature was added!] And mixed uniformly to obtain a pack containing powder. Example 18 Water-absorbing ointment

Ingredients (% by weight)

(1) Vaseline 40.0

(2) Stearyl alcohol 18.0

(3) Mokuro 20.0

(4) Polyoxyethylene (10 mol)

Monooleate 0.25

(5) Glycerin monostearate 0.25

(6) Placental extract 0.5

(7) Chinese rose extract (ethanol extract) 0.5

(8) Deionized water 20.5

(Formulation method)

(6) and (7) were added to (8) and kept at 70 ° C (aqueous phase). On the other hand, (1) to (5) were mixed and dissolved at 70 ° C (oil phase). The oil phase was added to the aqueous phase, and the mixture was uniformly emulsified with a homomixer and then cooled to obtain a water-absorbing ointment. Example 1 9 Lotion

Ingredients (% by weight)

(Aqueous phase)

Deionized water 83. 6098 Glycerin 5.0

1,3 Butylene Gri Cornore 2.0

Ascorbic acid 2-Gnorecoside 1.0

Rose extract (water extract) 0.0 1

Brilliant Blue 0.00002 Edetate 0.1

Caustic force 0.2

Sodium taenoate 0.15

Cuic acid 0.03

(Alcohol phase)

Ethanol (95%) .7.0

Polyoxyethylene (60 mol) hydrogenated castor oil ether 0.3

Vitamin E acetate 0.1

Spice 0.05

Methyl paraben 0.1 5

Phenoxyethanol 0.3

(Formulation method)

After uniformly dissolving the aqueous phase and the alcohol phase, the alcohol phase was added to the aqueous phase and mixed uniformly. Example 20 Lotion

Ingredients (% by weight)

(Aqueous phase) Two

Ion exchange water 7 9 6 6 4 7

Glycerin 5 0

Polyethylene glycol 4 0 0 2 0

Xylitol 0 5

Asconolevic acid 1-glucoside 1 0

Rose extract (water extract) 0 0 0 5

First green 0 0 0 0 3

Metaphosphoric acid 0 1

0

Sodium alginate 0 1

Hyaluronic acid 0 1

Trimethyldaricin 3 0

Caustic force 0 4

Sodium lactate 0 1

Lactic acid 0 0 3

(Ph. Anorecol)

Ethanol (95%) 70

P O E Oleino Leano Reconoreethenore 0 3

Vitamin E acetate 0

Perfume 0 0 5

Methyl paraben 0 1 5

Phenoxyethanol 0 3

(Formulation method)

After the aqueous phase and the alcohol phase were each dissolved uniformly, the alcohol phase was added to the aqueous phase and mixed uniformly. In the skin lightening effect test, all of the skin whitening external preparations of Examples 3 to 20 were used. Excellent effects were observed. Industrial applicability

As described in detail above, according to the present invention, it has both a tyrosinase activity inhibitory effect and a cyclic AMP (cAMP) production inhibitory effect, and has an excellent melanin production inhibitory effect and a highly safe whitening agent having a whitening effect. An external preparation for skin is provided.

Claims

The scope of the claims

1. Contains rose (R. cent ifolia L. or R. gallica L. var. Centifolia (L.) Reg.) Belonging to the family Nora (Rosaceae) and the genus Rosa or a solvent extract thereof as an active ingredient. An external preparation for skin whitening, characterized in that:

2. Rosaceae (R. centifolia L. or R. gallica L. var. Centifolia (L.) Reg.) Belonging to the genus Rosa (Rosa). A melanin production inhibitor characterized by containing as a component.

3. Rosaceae (R. centifolia L. or f. R. gallica L. var. Centifolia (L.) Reg.) Belonging to the genus Rosa (Rosa) A tyrosinase activity inhibitor, which is contained as an active ingredient.

4. Rosaceae (R. centifolia L. or R. gallica L. var. Centifolia (L.) Reg.) Belonging to the genus Rosa or a solvent extract thereof as an active ingredient A cyclic AMP (cAMP) production inhibitor, characterized in that: