TWI281865B - External preparations for beautifying the skin - Google Patents

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

1281865 A7 -------------- — B7___ V. INSTRUCTION DESCRIPTION (/) Technical Field The present invention relates to a skin whitening external preparation containing a specific plant extract. The whitening skin external preparation of the present invention has both an effect of inhibiting tyrosinase activity and inhibiting the production of cyclic adenosine monophosphate (CAMP), has a good effect of suppressing melanin formation, has a whitening effect, and is also excellent in safety. BACKGROUND OF THE INVENTION The pigmentation of skin spots such as dark spots and freckles is caused by abnormal secretion of hormones, ultraviolet rays or inflammatory stimuli, so that the melanin-generating signal transmission pathway in epidermal pigment cells is activated, and melanin produces the main enzyme cheese. As a result of the production and activity of the lysin, excessive melanin is precipitated in the epidermis. In order to prevent such a method of black spots and freckles, a substance which inhibits the activity of tyrosinase which produces melanin as a main enzyme has been used. Specifically, the cream or emulsion obtained by blending with citric acid or ellagic acid (to capture the copper ions necessary for the activity of tyrosinase) is partially coated or hydroquinone a derivative, a resorcinol derivative (having a structure similar to matrix tyrosine and acting as a tyrosinase competition inhibitor), a cream, an emulsion for topical application, or application of a machine other than the above The substance to be transferred, such as L-ascorbic acid (to reduce the dopaquinone of the precursor of melanin to dopa as a melanin-producing machine). The aforementioned substances are substances which inhibit the production of tyrosinase by the tyrosinase which has been produced, or the dopaquinone action which is produced by the activity of tyrosinase. Therefore, it has the difficulty of its own effect and its persistence. Also, regarding L-ascorbic acid, its stability in the original body and the base is not (please read the notes on the back and fill out this page)

This paper scale applies to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) 1281865 A7 ______B7_ V. The invention description (2) is good, so a large amount of application must be applied in order to obtain sufficient effects to prevent dark spots and freckles. In recent years, various active ingredients contained in plant extracts have been emphasized. Various effects such as the antioxidation of polyphenols contained in many plants to antitumor effects have been proposed. There are also various discussions on plant extracts that have a whitening effect. In the Rosaceae rose (R0sa), the plants with whitening effect are known as sakura, rose fruit, etc., but these plant extracts also act to inhibit tyrosinase activity. Can not satisfy the whitening effect and its persistence. On the other hand, 'acting on the information transmission pathway and suppressing the substance that produces itself' has been produced by the squirrel (kakyoku) which inhibits the path of the oxidizing gas, and the chamomile which inhibits the path of the protein kinase C. . However, these transmission pathways have low correlation with melanin production, and it is difficult to obtain a significant effect of suppressing melanin production, and development of a better plant extract pharmacophore is expected. As a result of intensive research on the above-mentioned problems, the present inventors have found that a specific plant extract has both an effect of inhibiting tyrosinase activity and an adenylate cyclase pathway having high affinity for melanin production. The whitening effect and the good effect of suppressing melanin formation are completed, and the present invention has been completed. DISCLOSURE OF THE INVENTION The present invention is a skin external preparation for whitening which is characterized by containing a rose (R. centif〇lia L. or R. gallica L. var centifolia (L. centif〇lia L. or R. gallica L. var centifolia (Losa) belonging to the Rosaceae rose family. .) Reg.) or its solvent extracts for 4 paper sizes applicable to China National Standard (CNS) A4 specifications (210 X 297 mm) -------- order ·------ (please first Read the notes on the back and fill out this page)

• Qin·1281865 A7 _ B7___ V. Invention description ()) is an effective ingredient. Further, the present invention provides a melanin production inhibitor, a tyrosinase activity inhibitor and a cyclic adenosine monophosphate (cAMP) production inhibitor which are characterized by containing the above-mentioned plant or a solvent extract thereof as an active ingredient. BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in detail. The skin whitening external preparation for use in the present invention, the melanin production inhibitor, the tyrosinase activity inhibitor, and the cyclic adenosine monophosphate (cAMP) production inhibitor include the western rose (Rosa) belonging to the Rosaceae rose (Rosa). · centifolia L. or R. gallica L. var centifolia (L·) Reg·) or its solvent extract as an active ingredient. The western rose (English name: Cabbage Rose, ProvanceRose) used in the present invention is a horticultural variety cultivated mainly in the southern part of Europe during the Renaissance period from the Greek Roman period to the Renaissance era. This flower can also be understood from its English name, and is a double-flowered cabbage. Hybrid (R. bifera X R. alba). Western rose (R. centifolia L. or R. gallica L. var centifolia (L.) Reg) can be used directly or after drying, but it can be used in the form of dry powder or solvent extract from the aspects of usability, formulation, etc. It is better. The use of R. centifolia L. or R. gallica L. var centifolia (L.) Reg. is preferred for flower or whole grass, but other parts can be used. The solvent extract of the above plant can be obtained by a usual method, for example, by immersing it with a solvent or heating it under reflux, followed by filtration and concentration. The extraction solvent can be used as long as it is used in the extraction solvent. It is applicable to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) than the paper size. (Please read the back note and fill out this page)

1281865 ΚΙ - - - _ _ _ 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 如 如 如 如 如 如 如 如 如 如 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 An organic solvent such as ethane, carbon tetrachloride, acetone, ethyl acetate or hexane is used singly or in combination. The extract obtained by the above solvent extraction may be used as it is, or the concentrated extract may be adsorbed by an adsorption method, such as an ion exchange resin, or adsorbed to a porous polymer (for example, an ADB XAD-2). After the column, the substance is dissolved and concentrated in methanol or ethanol. Further, there is also a method of using a dispensing method such as extracting the obtained extract with water/ethyl acetate. The above-mentioned plant extract obtained as described above has high safety, has a good whitening effect, inhibits melanin formation, inhibits tyrosinase activity, and inhibits the production of cyclic adenosine. When the above-mentioned plant extract is used in combination with a skin external preparation for whitening, it is preferably a dry weight of 0.000001 to 5.0% by weight in the total amount of the external preparation, more preferably 0.00001 to 3.0% by weight, particularly preferably 〇·〇〇. 〇〇ι~1.0% by weight. When the above-mentioned plant extract is used in combination with a skin external preparation for whitening, in addition to the extracts, it is possible to appropriately mix the skin external preparations which are generally used for cosmetics or pharmaceuticals, within the range which does not impair the effects of the present invention. Other ingredients such as oils, humectants, UV absorbers, antioxidants, surfactants, preservatives, humectants, perfumes, water, alcohols, tackifiers, and the like. The ultraviolet absorber of the above paragraph may be appropriately blended with 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxybenzophenone _5-sulfonate sodium, benzotriazolyl Sodium phenol sulfonate, methyl bisbenzotriazolyl tetramethyl butyl phenol 6 This paper scale is applicable to China National Standard (CNS) A4 specification (210 X 297 mm) (please read the notes on the back and fill in the form) This page)

· ϋ ί ini^inn· 一一, I 11 HI flu miim I A7 1281865 V. Illustrative (y) benzophenone derivatives, p-methoxy cinnamic acid octyl ester, di-p-methoxy cinnamic acid mono- a methoxycinnamic acid derivative such as 2-ethylhexanoic acid glyceride or isoamyltrimethoxycinnamic acid trioxane, urinary acid, 4-ter-4'-methoxydiphenylmercapto methane , bis-ethylhexyl hydroxyphenol methoxy phenyl triazine, ethylhexyl triazine, phenyl benzimidazole sulfonic acid, and the like. Further, a metal ion chelating agent such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate or gluconic acid, caffeine, tannin, and valproate may be suitably used. , tranexamic acid and its derivatives, licorice extract, glabddin, various crude drugs, tocopherol acetate, glycyrrhizic acid and its derivatives or its salts, vitamin C, magnesium ascorbyl phosphate, ascorbyl glucoside Other whitening agents such as arbutin, citric acid, resorcinol, ellagic acid, and encrypted column extracts, and sugars such as glucose, fructose, mannose, sucrose, and trehalose. Moreover, the skin external preparation for whitening of the present invention may be a cosmetic material for the skin, a pharmaceutical product, a quasi-medicine product, etc., and particularly, it can be widely applied to a cosmetic material, and the dosage form can be applied to the skin as long as it is suitable for the skin. Any of the solubilizing system, emulsifying system, powder dispersion system, water-oil two-layer system, water-oil-powder three-layer system, ointment, colloid, spray, and the like are applicable. Further, the skin whitening external preparation of the present invention is also used in any form, such as a cosmetic lotion or a foundation of a lotion such as a lotion, a cream, a mask, etc., and can also be used for a cosmetic cosmetic, an aromatic cosmetic, and a bath. Agents, etc. Further, the skin external preparation for whitening of the present invention is not limited to the above dosage form and use form. Example 7 (Please read the phonetic on the back? Please fill out this page again)

Packing----^5J111111 This paper size is applicable to China National Standard (CNS) A4 specification (210 X 297 mm) 1281865 A7 ------ - B7___ V. Invention description (6) Secondly, the following example The invention is described in more detail, but the technical scope of the invention is not limited to the embodiments. Further, the blending amount is % by weight. 0 Before the examples, the effect of inhibiting tyrosinase activity of the plant extract of the present invention, the effect of inhibiting the production of cyclic adenosine monophosphate (cAMp), and the effect of inhibiting melanin production will be described. Test method and evaluation method of whitening effect 〇 [Test method and evaluation method] 1. The flower of R. centifolia L. or R. gallica L. var centifolia (L·) Reg· The water is warmed and extracted to obtain an extract. The extract was concentrated to give 5 g of a plant extract. The above plant extract was dissolved in 70% ethanol to a concentration of 2% by weight as a solution containing a plant extract. These plant extract-containing solutions were diluted and adjusted to prepare a sample solution for the following experiments. 2. Cell culture method B16 melanoma cultured cells derived from rats were used. Dulbecco MEM medium containing 10% FBS and theophylline (0.09 mg/ml), or melanocytes stimulated hormone (α-MSH) (10 nM) in a carbon dioxide incubator (95% air, 5% carbon dioxide) The medium was cultured under conditions of 37 t. 3. Determination of inhibitory effect of tyrosinase activity The cells cultured according to the above 2 methods were sown in 96 trays, and after 24 hours of culture, the sample solution was added to make the final concentration (converted concentration of the extracted dried matter) into 8 paper scales for China. National Standard (CNS) A4 Specification (210 X 297 mm) 1 Pack -------- Order - (Please read the notes on the back and fill out this page)

1281865 A7 V. Inventive Note (7) HT7~10'5 wt%, and continue to culture. After 3 days of culture, the cells were washed with PBs, PBS containing 1% Triton was added, and DOPA was added to make the final soil ρ, and the absorbance (475 nm) after 0 minutes and 60 minutes was measured for ImM 〇. The sample to which the plant extract was added (control group: 70% ethanol) was compared according to the following criteria. Further, the same test as above was carried out using the extract of Rosa canina L. (ethanol extract) which is also belonging to the genus Rosa (Rosaceae) as a reference example. The results are shown in Table 1. Further, Table 1 shows the results of the culture of a medium containing melanocyte-stimulating hormone (α-MSH), but the same results were obtained when using theophylline. (Criteria for judging) 〇: The tyrosinase activity inhibitory effect was excellent compared with the control group. △ ·· The tyrosinase activity inhibitory effect was slightly better than the control group. X: No tyrosinase activity inhibitory effect. -------- Order ------ 23⁄4 first read the back of the note and then fill out this page) Table 1 sample solution g solution concentration (weight 〇 / (〇 - 0 10·7 1〇- 6 10·5 Western 啬 啬 X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X X The plate was incubated for 24 hours, and then added to the sample solution so that the final concentration (converted concentration of the extract dried product) was 1 〇 2 to 10 - 4% by weight, and the culture was continued. After 3 days of culture, the plate was placed on the lid of the 96-well plate. Diffuser plate, observe cells with inverted microscope 9

1281865 A7 B7 V. The amount of melanin in the invention u) is compared with the sample without the addition of plant extract (control group: 70% ethanol), and is evaluated according to the following criteria. Further, the same test as above was carried out using the extract of Rosa canina L. (Rosin canina L.) which is also Rosaceae as a reference example. The results are shown in Table 2. Further, Table 2 shows the results of culture of a medium containing melanocyte-stimulating hormone (-MSH), but the same results were obtained when using theophylline. (Criteria for judging) 〇: White compared with the control group (melanin production inhibition is good). △: slightly whiter than the control group (melanin production inhibition is slightly better). X: As white as the control group (no melanin production inhibition). Table 2

Sample solution concentration (% by weight) 0 10'5 1〇·4 10'3 1〇-2 Western rose extract XX Δ 〇〇 wild rose extract XXXXX 5 · Determination of inhibition effect of cyclosporine production from rats B16 melanoma cell culture cells were seeded in a 12-well plate and cultured in Dabeck MEM medium containing 10% FBS in a carbon dioxide incubator (95% air, 5% carbon dioxide) at 37 ° C for 24 hours. Thereafter, the medium was evacuated, and a melanocyte-stimulating hormone (-MSH, 0.1 nM) and a sample solution were added to obtain a final concentration (converted concentration of the extract dried matter) of 10-1 to 10-3 wt% of the blood-free medium. After culturing for 30 minutes, the medium was removed and the cells were collected in TE buffer and transferred to 10 paper size national standard (CN5) A4 specifications (21〇x 297 public). (Please read the notes on the back and fill out this page. )

Pack - ϋ up n · one mouth, —im an Bn n flu 11 1281865 A7 B7 V. Inventive Note (?) 1·5ιη1 micro-test tube, after boiling, use the ring pity gland (camP) to determine the kit (Ama Amoxicilne Co., Ltd.) The amount of cyclic adenosine monophosphate (cAMP) in the liquid was measured. Further, the same test as described above was carried out using the extract of Rosa canina L. (Ethanol extract) which is also belonging to the Rosaceae (R0sa) as a reference example. The sample (control group: 70% ethanol) which was not added with the plant extract was evaluated according to the following criteria. The results are shown in Table 3. (Criteria for Judgment) 〇·· Compared with the control group, the cyclophosphamide g: (cAMP) has a better inhibitory effect. △: The inhibition of cyclic adenosine monophosphate (CAMP) production was slightly better than that of the control group. X: acyclic adenosine monophosphate (cAMP) produces an inhibitory effect. (Please read the notes on the back and fill out this page)

Table 3 Sample solution sample solution concentration (weight 0 10'3 10·2 5x10*2 ιο·ι Western rose extract XX Δ 〇〇 wild rose extract XXXXX · 111! 1 Φ 6_ whitening effect test (test method) to expose For the back skin of 20 subjects in the summer sunshine for 4 hours (1 day, 2 hours, 2 days), the test sample solution shown below was applied once in the morning and evening for 4 weeks, and the following criteria were used. Evaluation. The average number of evaluation points of 20 subjects is shown in Table 4. 11 This paper scale applies to China National Standard (CNS) A4 specification (210 X 297 mm) 1281865 A7 ___ B7 V. Description of invention (θ (Test sample solution) Mixing component (% by weight) (alcohol phase) 95% ethanol 25.0 Polyethylene oxide (25 mol) Hardened castor oil ether 2.0 Methylparaben 0.1 Dibutylhydroxytoluene 0.01 Spice 0.05 (aqueous phase) Glycerin 2.0 1,3-butanediol 1.0 Ion exchange water remaining agent (shown in Table 4. The amount shown in the table is dry weight) (Preparation method) The aqueous phase and the alcohol phase are separately prepared and mixed. And make it soluble. Method) The lightening effect after use was judged according to the following criteria. (Comment) 4: It was confirmed to have a significant lightening effect after continuous application. 3: It was confirmed to have a lightening effect after continuous application. : It is considered to have a slight lightening effect after being applied. 1: It is considered to have no lightening effect after being applied. --------Book----- (Please read the notes on the back first) Fill in this page again)

This paper scale applies to China National Standard (CNS) A4 specification (210 X 297 mm) 1281865 A7 ________B7 V. Invention description (Π) Table 4 Comparative examples 1 2 3 4 5 6 1 2 Western rose - - - - _ 0.1 1.0 野蔷微1.0 - - - 看• 营实- 1.0 - - • - Ascorbic acid - - 3.0 - • • Ascorbyl phosphonium 餻 - - - 1.0 _ _ Sodium acid phosphate sodium - - - - 1.0 _ • Placenta Extract - - - - per 1.0 • Jing 1.00 1.10 1.10 1.35 1.35 1.15 1.60 2.20 As is apparent from Table 4, the present invention has a good whitening effect. In particular, the present invention was found to be quite good in whitening effect even when compared with the ascorbic acid derivative and the placenta extract compounding which are known to have a skin whitening effect. Hereinafter, examples of the combination of the whitening skin external preparations of the various dosage forms of the present invention will be described as examples. Further, the blending amount of the plant extract is a dry residue. Example 3 vanishing cream 13 This paper scale applies to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) - Packing---- (Please read the notes on the back and fill out this page)

Ingredients (heavy stomach%) (1) Stearic acid 6.0 (2) Sorbitol monostearate 2.0 (3) Polyepoxyether (20 mol) Sorbitol monostearate 1.5 ( 4) Arbutin 7.0 (5) Sodium bisulfite 0.03 (6) Propylene glycol 7.0 (7) Glycerin 3.0 (8) Western rose extract (water extract) 1.0 (9) Pair of ethyl benzoate 0.1 (10) Butyl benzoate 0.1 (11) Thiosulfate 〇. 〇 1 (12) Perfume 0.1 (13) Ion-exchanged water 72.16 (manufacturing method) 1281865 A7 B7 V. Description of invention (will be (4), (6) (7), (8) is added to (13), heated and kept at 70QC (aqueous phase). In addition, (1)~(3), (5), (9)~(12) are mixed and heated and melted. The heat is kept at 7 〇. (: (oil phase). The oil phase is added to the water phase to carry out pre-emulsification, homogenized by a homogenizer, and then cooled to 30 ° C under full agitation to obtain mildew. Cream combination with ingredients (% by weight) (1) Stearyl alcohol 5.0 (2) Stearic acid 2.0 (3) Aqueous lanolin 2.0 (4) 2-Pipe methoxy benzophenone 2.0 (5) Angle Squalane 5.0 (6) 2-octyldodecanol 6. 〇 (7) polyethylene oxide (25 Mo Cetyl ether 3.0 (8) Glycerol monostearate 2.0 (9) Placenta extract 0.1 (10) Propylene glycol 2.0 (11) 1,3-butanediol 3.0 (12) Western rose extract (water extract) 5.0 (13) Perfume 0.2 (14) 1,2-pentanediol 0.5 (15) butyl p-hydroxybenzoate 0.1 (16) times bovine acid extension 0.01 (17 medlar exchange water 65.69 (manufacturing method) (9) ~(12), (16) are added to (17), heated and kept at 7 ° C (aqueous phase). In addition, (1) ~ (8), (13) ~ (15) are mixed, heated and melted. The temperature is maintained at 7〇t (oil phase). The oil phase is added to the water phase for pre-emulsification, homogenized by a homogenizer, and then cooled to 30 ° C with sufficient agitation to obtain a neutral cream. Applicable to China National Standard (CNS) A4 specification (210 X 297 mm) Γ% first read the back of the a thing and then fill out this page: > ---I 1 · · 1281865 A7 ______ B7 V, invention description (β Example 5 Cold cream with ingredients (% by weight) (1) Solid paraffin 5.0 (2) Beeswax 5.0 (3) Vaseline 5.0 (4) Liquid paraffin 20.0 (5) Squalane 10.0 (6) Glycerol monostearate · 2.0 (7) Polyethylene oxide (20) Ear) Sorbitol monolaurate 2.0 (8) Citrate 2.0 (9) 2-Sodium methoxy benzophenone-5-sulfonate 3.5 (1 〇) soap powder 0.1 (11)» 0.2 (12 sprinkle rosehip extract (water extract) 0.1 (13 hazelnut exchange water 44.55 (14) perfume 0.2 (15) ethyl p-hydroxybenzoate 0.2 (16) butyl p-hydroxybenzoate 0.1 (17) Base toluene 0.05 (manufacturing method) ---- (Please read the notes on the back and fill out this page)

(8), (10), (11) and (12) are added to (13), dissolved by heating and kept at 7 ° C (aqueous phase). Further, (1) to (7) and (9) '(14) to (17) were mixed, heated and melted, and kept at 7 ° C (oil phase). The oil phase was gradually added to the aqueous phase under agitation to cause a reaction. After the completion of the reaction, the mixture was uniformly emulsified by a homogenizer, and then emulsified, and then thoroughly stirred and cooled to 3 ° C to obtain a cold cream. This paper scale is suitable for Chinese National Standard (Cns) A4 specification (210 X 297 public love - Example 6 Nutrition Cream with ingredients (% by weight) (1) Chlorinated One A$•=: Painting 雠Montmorillonite 2.0 (2) Polyethylene oxide/methyl polyoxane polymer 0.1 (3) liquid paraffin 10.0 (4) squalane 5.0 (5) cetyl octanoate 20.0 (6) sodium L-ascorbate 0.01 (7) dipropylene glycol 5.0 (8) methyl p-hydroxybenzoate 0.2 (9) sodium hyaluronate 0.05 (10) vitamin E acetate 0.02 (11) western rose extract (water extract) 2.0 (12) ion exchange water 55.62 (method of preparation) After (2), (3), and (5) are heated to 50 ° C, (4) and (10) are completely dissolved to form an oil phase portion, and (1) is added to uniformly disperse, and then one is added thereto. The aqueous phase (6), (7), (8), (9), (11) is dissolved in (I2) (heated to 50 ° C), and homogenized to make uniform emulsification. Cool to room temperature to obtain an aqueous emulsified composition in oil. Example 7 Emulsion compounding component (% by weight) (1) Polyethylene oxide (10 mol) Monooleate 2.0 (2) Octyl p-methoxycinnamate 3.5 (3) Liquid paraffin 2.0 (4) Cyclopentyl dimethyl decane 1.0 (5) squalane 3.0 (6) 1,3-butanediol 5.0 (7) Arbutin 2.0 (8) Sodium bisulfite 0.03 (9) Glycerin 2.0 16 1281865 A7 ____B7 V. INSTRUCTIONS (W). This paper scale applies the Chinese National Standard (CNS) A4 specification (210 X 297 mm) (please read the notes on the back and fill out this page)

1281865 A7 ___ B7 V. INSTRUCTIONS (K) (10) Ethanol 5.0 (11) Carboxyvinyl polymer 0.3 (12) Hydroxypropyl cellulose 0.1 (13) Sodium hydroxide 0.15 (14) Ethyl p-hydroxybenzoate 0.1 (15) 1,2-pentanediol 1.0 (16) Western rose extract (water extract) 0.5 (17) ion-exchanged water 72.02 (18) Spice 0.3 (method of production) Heat dissolve (16) and (17) In (17) and (10), (6), (8), (9), (11) to (13) are further dissolved and kept at 70 ° C (aqueous phase). Further, (1) to (5), (14), (15), and (18) were mixed, heated and melted, and kept at 70 ° C (oil phase). The oil phase was added to the aqueous phase, pre-emulsified, homogenized by a homogenizer, and emulsified and then agitated to cool to 30 ° C to obtain an emulsion. Example 8 Emulsion Mixing Ingredient (% by weight) (1) Polyepoxyethylene (20 mol) polypropylene oxide (2 mol) residual wax alcohol i ^ (2) Octyl-p-methoxycinnamic acid Ester 3.5 (3) "Anthrone KF96" (20cs) (manufactured by Shin-Etsu Chemical Co., Ltd.) 2.0 (4) Liquid Dendrobium (Medium Viscosity) 3.0 (5) 4-tert-Butylmethoxydiphenylmethylmethane 0.3 (6) Triethyl 2-ethylhexanoate 1.0 (7) Arbutin 2.0 (8) Sodium bisulfite 〇.〇3 (9) Glycerin 2.0 (10) Ethanol 3.0 (11) Carboxyvinyl polymer 0.3 (12) Hydroxypropyl fiber 0.1 (13) Sodium hydroxide 0.1 (14) 1,2-Pentanediol 2.0 (15) Phenoxyethanol 0.2 17 This paper scale applies to China National Standard (CNS) A4 specification (210 X 297 mm) (please Read the notes on the back and fill out this page.)

I nnnm - - - a T f flu II m —I— ii — I 1 il — A7 0.1 79.37 (% by weight) 1.0 2.0 2.0 3.0 5.0 3.0 3.0 2.0 5.0 0.3 0.1 0.1 0.1 0.4 0.02 0.01 72.87 0.1 1281865 ____B7 V. DESCRIPTION OF THE INVENTION (U) (16) Western rose extract (aqueous alcohol extract) (Hazelnut exchange water (preparation method) (16) and (7) are heated and dissolved in (17) and (1), and then (6), (8), (9), (11) to (13), (15) dissolve and keep at 70 ° C (aqueous phase). In addition, mix (1) ~ (5), (14) It is heated and melted and kept at 70 ° C (oil phase). The oil phase is added to the aqueous phase, pre-emulsified, homogenized by a homogenizer, and emulsified and then agitated to a temperature of 3 ° C to obtain an emulsion. Example 9 Emulsion Mixing Ingredients (1) Polyethylene oxide (20 mol) polypropylene oxide (2 mol) cetyl alcohol (2) p-methoxycinnamic acid mono-2-ethylhexanoic acid glycerol Ester (3) "Anthrone KF96" (2〇cs) (manufactured by Shin-Etsu Chemical Co., Ltd.) (4) Squalane (5) 1,3-butanediol (6) Ascorbic acid 2-glucoside (7) Polyethylene Alcohol 400 (8) Glycerol (9) Ethanol (10) Carboxyvinyl polymer (11) Hydroxyl Propylcellulose (u) sodium hydroxide (!3) butylparaben (14) phenoxyethanol (15) thiotaurine (16 sprinkle rose extract (dry powder) (17) ion Exchange water (18) Perfume (preparation method) Dissolve (15), (16) and (6) in (17) and (9), and then (5), (7) ' (8), (10) ~ (12), (14) dissolve and keep warm at 7 (rC (aqueous phase). In addition -------- set-------- (please read the notes on the back and fill out this page)

18 1281865

V. INSTRUCTIONS (I?) ' Mix (1) to (4) and (13), (18) and heat and melt at 70 ° C (oil phase). The oil phase is added to the aqueous phase, pre-emulsified, homogenized by a homogenizer, and emulsified and then agitated to cool to 3 (TC to obtain an emulsion. Example 10 emulsion compounding component (% by weight) (1) Polycyclic ring Ethylene oxide (20 mol) polyepoxypropanol (2 mol) Esterol ^ ^ (2) "Anthrone KF96" (20cs) (manufactured by Shin-Etsu Chemical Co., Ltd.) 2*0 (3) Liquid stone Impurity viscosity) 30 (4) Methyl bis-benzotriazolyl tetramethyl butyl phenol L0 (5) 1,3-butanediol 5 〇 (6) glycerol 2.0 (7) Ethanol 4.0 (8) Carboxyvinyl polymer 0.3 (9) Hydroxypropyl cellulose α 1 (10) Sodium hydroxide 〇〇 5 (11) 1,2-pentanediol 1 () (12) butyl benzoate αι (13 citric acid 3.0 (14 ) Western rose extract (1,3-butanediol extract) 0.001 (15) ion-exchanged water 77.449 (manufacturing method) (13) is dissolved in (15) by heating, and then (14), (5) ~ ( 1〇) Dissolved and kept at 7 ° C (aqueous phase). Further, (1) to (4) and (11), (12) were mixed and heated to melt and kept at 7 ° C (oil phase). The oil phase is added to the aqueous phase, pre-emulsified, homogenized to homogenize, and emulsified Sufficient agitation under cooling to 30 ° C to the emulsion. 19 paper scale applicable Chinese National Standard (CNS) A4 size (210 X 297 mm) (Please read the back of the precautions to fill out this page)

--------Book·--- ---- 1281865 Α7 Β7 V. Description of invention (β Example 11 emulsion compounding ingredients (% by weight) (1) stearic acid 1.5 (2) cetyl alcohol 0.5 (3) Beeswax 2.0 (4) Polyethylene oxide (20 mol) Monooleate 1.0 (5) Glycerol monostearate 1.0 (6) Ethanol 3.0 (7) Arbutin 10.0 (8) Sodium bisulfite 0.03 (9) 1,3-butanediol 5.0 (10) polyethylene glycol 400 2.0 (11) western rose extract (1,3-butanediol extract) 0.0005 (12 gardenia exchange water 73.2195 (13) spices 0.15 (14) methyl p-hydroxybenzoate 0.3 (15) p-butyl benzoate 0.2 (16) thiotaurine 0.1 (manufacturing method) (7), (9) and (10), (16) Add (12), heat to dissolve and keep warm in -------- order---- (please read the notes on the back and fill out this page)

Qin·7 (TC (aqueous phase). Further, (11) is added to dissolve in (6) (alcohol phase). In addition, (1) to (5), (8), (13), (14), (15) mixing, heating and melting and maintaining at 7 ° C (oil phase). The oil phase is added to the aqueous phase, pre-emulsified, homogenized by a homogenizer, and added to the alcohol phase with full agitation. The mixture was cooled to 30 ° C under stirring to obtain an emulsion. (% by weight) 1.5 0.5 2.0 10.0 Example 12 Emulsion compounding ingredients (1) Microcrystalline wax (2) Wax (3) Vaseline (4) Liquid paraffin 20 Paper size Applicable to China National Standard (CNS) A4 specification (210 X 297 mm) 1281865 A7 ___B7 V. Description of invention (θ) (5) Squalane 5.0 (6) Jojoba oil 5.0 (7) Sorbitan half Oleate 4.0 (8) Polyethylene oxide (20 mol) Sorbitol monooleate 1.0 (9) Arbutin 5.0 (10) Sodium bisulfite 0.03 (11 hemolytic acid 5.0 (12) 1,3-butanediol 5.0 (13) Sorbitol 2.0 (14) Western rose extract (1,3-butanediol extract) 0.00001 (15) bis-ethylhexylhydroxyl 1.5 phenol methoxyphenyl Sancha (16 dice exchange water 52.01999 (17) Material 0.2 (18) ethyl p-hydroxybenzoate 0.1 (19) p-butyl benzoate 0.1 (20) dibutyl hydroxy toluene 0.05 (manufacturing method) (9), (11) ~ (14) added (16 ), heated and kept at 70 ° C (aqueous phase). In addition, (1) ~ (8), (10), (15), (17) ~ (20) mixed, heated and melted and kept at 70 ° C (Oil phase). The oil phase was agitated and the oil phase was slowly added to the aqueous phase. The mixture was uniformly emulsified by a homogenizer, and after emulsification, it was thoroughly stirred to cool to 30 ° C to obtain an emulsion. Ingredients (% by weight) (1) Isopropyl glycol 10.0 (2) Diglyceryl diisostearate 0.5 (3) POE denatured dimethyl polyoxane 1.0 (4) Octylmethylcyclotetraoxane 25.0 ( 5) Dodecylcyclopentaoxane 15.0 (6) Trimethylsiloxylic acid 5.0 (7) Eucalyptus oil 3.0 (8) Spices 〇.〇5 21 This paper scale applies to China National Standard (CNS) A4 Specifications (210 X 297 mm) (Please read the notes on the back and fill out this page) 1% loaded

· I stupid | A7 1281865 ___ B7 V. Description of invention (〆) (9) Dipropylene glycol 2.0 (10) Western rose extract (propylene glycol extract) 0.002 (11) Androside 7.0 (12) Sodium bisulfite 0.03 ( 13)) Methylparaben 0.1 (14) Trisodium edetate 0.1 (15) Ion-exchanged water 30.718 (16) Sodium chloride 0.5 (Preparation method) Dissolve (1) to (8) (oil phase), (9) to (16) are dissolved (aqueous phase), and then the oil phase is added to the aqueous phase and emulsified: to obtain an emulsion. Example 14 Emulsion* Compatible Ingredient (% by weight) A. Oil Phase Dimethylpolyoxane 0.5 Dodecamethylcyclopentaoxane 1.0 Jojoba Oil 0.5 B Ice Phase Arbutin 1.0 Western Rose Extract ( Water extract) 0.005 alkyl-denatured carboxyvinyl polymer 0.05 thiol ethylene base polymer 0.3 acacia 0.05 ethyl alcohol 8.0 trisodium edetate 0.1 methyl p-hydroxybenzoate 0.1 phenoxyethanol 0.2 (15) Ion exchange water 88.045 C. Neutralization of potassium hydroxide 0.15 (manufacturing method) 1 loading -------- order --- (please read the notes on the back and fill out this page)

The dissolved (A) phase is added to the dissolved (B) phase, and after emulsification, the (C) phase is neutralized to obtain an emulsion. 22 This paper size is applicable to China National Standard (CNS) A4 specification (210 X 297 mm) A7 1281865 ___ B7 V. Inventive Note (>1) Example 15 Colloidal Composition ίRay%) (1) 95% Ethanol 10.0 (2 Dipropylene glycol 1.0 (3) Glycerol 5.0 (4) Polycyclohexane (15 mol) Ether ether 2.0 (5) Arbutin 0.5 (6) Sodium bisulfite 0.03 (7) Ascorbyl distearate 0.5 ( 8) Carboxyvinyl polymer 1 A (Jiabobo Road 941) • 1 · (9) Sodium hydroxide 0.15 (10) L-arginine 0.1 (11) Western rose extract (5〇% U-butanediol) Extract) 0.001 (12) Perfume 0.1 (13) Phenoxyethanol 0.4 (M) Ion-exchanged water 70.219 (Preparation method) (11), (5), (3) and (8) are uniformly dissolved in (H) (water box). Further, (2), (4), and (6), (7), (12), and (13) are dissolved in (1) and added to the aqueous phase. Then, the colloids are obtained by neutralizing the (9) and (10) and adding the viscosity. Example 16 Peel-off mask compounding component (% by weight) (alcohol phase) 95% ethanol 10.0 Polyethylene oxide (15 mol) Oleic ether 2.0 Ethylhexyl triazinone 1.0 Pair of methyl benzoate 0.3 benzene Oxyethanol 0.3 Fragrance 1.0 (aqueous phase) Western Rose Extract (50% 1,3-butanediol extract) 1.0 23 -------- Order *--- (Please read the notes on the back first) Fill in this page again)

This paper size is applicable to China National Standard (CNS) A4 specification (210 X 297 mm) 1281865 A7 B7 V. Description of invention (y) Arbutin 1.0 Sodium bisulfite 0.03 Polyvinyl alcohol 12.0 Glycerin 3.0 Polyethylene glycol 1500 1.0 Ion exchange water 68.17 (manufacturing method) The aqueous phase was prepared at 80 ° C and cooled at 50 ° C. The alcohol phase, which was prepared at room temperature, was then uniformly mixed and allowed to cool. Example 17 Powder-containing mask compounding component (% by weight) (alcohol phase) 95% ethanol 5.0 methylparaben 0.1 1,2-pentanediol 2.0 perfume 0.3 ascorbic acid dioleate 1.0 ice phase) Western rose extract (50% 1,3-butanediol extract) 1.0 Arbutin 1.0 Dipropylene glycol 3.0 Polyethylene glycol 1500 0.5 Zinc white 15.0 Kaolin 8.0 Ion exchange water 61.1 (Preparation method) The aqueous phase was uniformly prepared at room temperature. Then, the alcohol phase prepared at room temperature was added and uniformly mixed to obtain a powder-containing mask. Example 18 Water-absorbing ointment with ingredients (% by weight) (1) Vaseline 40.0 (2) Stearyl alcohol 18.0 24 This paper scale is applicable to China National Standard (CNS) A4 specification (210 X 297 mm) -------- ----- (Please read the notes on the back and fill out this page)

1281865 A7 _ B7 V. INSTRUCTIONS (Factory (3) Wood wax 20.0 (4) Polycyclohexane (10 mol) Monooleate 0.25 (5) Glycerol monostearate 0.25 (6) Placenta extract 0.5 (7) Western rose extract (ethanol extract) 0.5 (8) Ion exchange water 20.5 (manufacturing method) Add (6), (7) to (8) and keep at 7 (TC (aqueous phase). In addition, (1) ~ (5) at 7 (TC mixed dissolution (oil phase). The oil phase is added to the aqueous phase, uniformly homogenized by a homogenizer, and then cooled to obtain a water-absorbing ointment. Example 19 Cosmetic water-containing ingredients (% by weight) (aqueous phase) Ion exchange water 83.6098 Glycerin 5.0 1,3-butanediol 2.0 Ascorbic acid-2-glucoside 1.0 Western rose extract (water extract) 0.01 Brilliant blue 0.0002 edetate 0.1 Sodium hydroxide 0.2 Sodium citrate 0.15 Citric acid 0.03 (alcohol phase) 95% ethanol 7.0 polyethylene oxide (60 mol) hardened castor oil ether acetate 0.3 vitamin E acetate 0.1 perfume 〇.〇5 p-methyl benzoic acid methyl ester 0.15 phenoxyethanol 0.3 (Method) 25 This paper scale applies to China National Standard (CNS) A4 specification (210 X 297 mm) (please read the back first) Note: Please fill in this page) Pack ------------------------ 1281865 A7 ~^^ _-_B7___ V. Description of the invention (蚪) Uniform the aqueous and alcohol phases After dissolution, the alcohol phase was added to the aqueous phase and uniformly mixed. Example 20 Cosmetic water-containing ingredients (% by weight) Ice-phase) Ion-exchanged water 79.6647 Glycerin 5.0 Polyethylene glycol 400 2.0 Xylitol 0.5 Ascorbic acid-2-vine view 1.0 Western rose extract (water extract) 0.005 Fast green 0.0003 Metaphosphoric acid 0.1 Oxycholinium 0.1 Sodium arginate 0.1 Hyaluronic acid 0.1 Trimethylglycerol 3.0 Sodium hydroxide 0.4 Sodium lactate 0.1 Lactic acid 0.03 (alcohol phase) 95 %ethanol7.0 POE oleyl ether 0.3 Vitamin E acetate 0.1 Fragrance 0.05 Methylparaben 0.15 Phenoxyethanol 0.3 (Manufacturing Method) 1 Pack--------Book----- (Read first Note on the back and fill out this page)

After uniformly dissolving the aqueous phase and the alcohol phase, the alcohol phase is added to the aqueous phase and uniformly mixed. Any of the skin external preparations for whitening of the above Examples 3 to 20 was found to have good effects in the whitening effect test. 26 The paper scale applies to the Chinese National Standard (CNS) A4 specification (210 X 297 mm) 1281865 A7 _ B7_ V. INSTRUCTION DESCRIPTION (β) INDUSTRIAL APPLICABILITY As described above, according to the present invention, A whitening skin external preparation having high safety, which has both a tyrosinase activity inhibitory effect and a cyclic adenosine monophosphate (cAMP) production inhibitory effect, and has a good effect of suppressing melanin formation and a whitening effect. --------Book----- (Please read the notes on the back and fill out this page)

Qin · This paper scale applies to China National Standard (CNS) A4 specification (210 X 297 mm)

Claims (1)

1281865 C8 D8 VI. Application for Patent Scope; Patent Application No. 090117406 Patent Application Revision/Replacement 2Q07.01 1· A composition for external use of skin for whitening, characterized by containing a rose belonging to the family Rosaceae (Rosa) A dried powder of R. centifolia L. or R. gallica L. var centifolia (L.) Reg. or a solvent extract thereof as an active ingredient; a solvent selected for the extract At least one selected from the group consisting of water, alcohols, aqueous alcohols, chloroform, dichloroethane, carbon tetrachloride, acetone, ethyl acetate, and hexane. .2. A melanin production inhibitor composition characterized by containing a rose (R. centifolia L. or R. gallica L. var centifolia (L.) Reg belonging to the Rosa genus (Rosaceae). .) a dry powder or a solvent extract thereof as an active ingredient; the solvent used in the extract is selected from the group consisting of water, alcohols, aqueous alcohols, chloroform, dichloroethane, carbon tetrachloride, acetone, acetic acid At least one of a group consisting of ethyl ester and hexane. A tyrosinase activity inhibitor composition characterized by containing a rose (R. centifolia L. or R. gallica L. var centifolia (L. cent.) belonging to the genus Rosa of the Rosaceae family. a dry powder of Reg) or a solvent extract thereof as an active ingredient; the solvent used in the extract is selected from the group consisting of water, alcohols, aqueous alcohols, chloroform, dichloroethane, carbon tetrachloride, acetone And at least one of the group consisting of ethyl acetate and hexane. 4. A cyclic adenosine monophosphate (cAMP) production inhibitor composition characterized by containing a rose (Rosa) belonging to the Rosaceae rose (R. This paper scale is applicable to the Chinese National Standard (CNS) A4 specification. (210 X 297 mm) --------------------------.......... ----------£0. (Please read the notes on the back and fill out this page) 5 6 8 8 12 A8B8C8D8 VI. Patent application scope centifolia L· or R· gallica L_ var centifolia (L· ) a dry powder of Reg.) or a solvent extract thereof as an active ingredient; the solvent used in the extract is selected from the group consisting of water, alcohols, aqueous alcohols, chloroform, dichloroethane, carbon tetrachloride, acetone And at least one of the group consisting of ethyl acetate and hexane. ...........r-r......—— (Please read the notes on the back and fill out this page) -1 tl 2 This paper scale applies to China National Standard (CNS) A4 Specifications (210 X 297 mm)