JPH08133955A - Skin preparation for external use - Google Patents

Abstract

PURPOSE: To obtain a ski preparation for external use formulated with saponin(s) extracted from specific plant (s), excellent in skin beautifying effect, and good in both usability and safety. CONSTITUTION: This skin preparation for external use contains, as active ingredient, 0.001-20wt.% of at least one kind of saponin or its salt extracted from Pulsatilla cernua Spreng., Cyclamen europaeum, Primula officinalli, Achyranthes fauriei Lev. et Van., Fatsia japonica Decne. et Pianch, Caulophyllum robustum Maxim., Clematis chinensis Osbeek, and Anemarrhena asphodeloides Bunge. Besides, combination of the active ingredient with an ascorbic phosphoric ester and/or placenta extract potentiates the skin beautifying effect of this skin preparation, and prevents skin spots and freckle to cause the fine and dampish skin. This skin preparation can be made, by conventional means, into cosmetics and medicinal preparations of such formulations as milky lotion, lotion, cream, jelly, pack, powder, and ointment.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an external preparation for skin which is excellent in whitening effect and has good usability and safety by incorporating saponin obtained from a specific plant.

[0002]

2. Description of the Related Art The skin aging phenomenon represented by pigmentation such as wrinkles and spots on the outer corners of the eyes and freckles appears earlier than other tissues and organs, and is often observed from the mid-twenties. It is considered that this is because the skin is in the outermost layer of the living body and is susceptible to external stimuli (stress) such as ultraviolet rays, oxygen and chemical substances.

Such ultraviolet rays, stains due to stress,
Deposition of melanin pigment such as freckles on the skin is caused by proliferation of pigment cells, which are melanin-producing cells, or enhancement of melanin-producing function in pigment cells. Recent studies have revealed that UV rays and stress increase the number of factors that activate pigment cells in the skin, causing spots and freckles. For the purpose of prevention and whitening, ascorbic acid and its derivatives have been conventionally used.

[0004]

However, it has been difficult for the conventionally used ascorbic acid or its derivative to sufficiently exert the inhibitory effect on pigmentation. Previously, it was clarified that escin, which is one of the triterpenoid saponins, has an anti-pigmenting action, that is, a whitening action (Japanese Patent Application No. 5-246161). The present invention has been made in view of the above-mentioned problems of the prior art, and an object thereof is to provide a skin external preparation that is excellent in whitening effect that can directly and efficiently suppress pigmentation, and that has good usability and safety. To provide.

[0005]

Means for Solving the Problems As a result of intensive studies by the present inventors in order to achieve the above object, it has an excellent whitening effect in blending saponin obtained from a specific plant,
The inventors have found that an external preparation for skin excellent in terms of usability and safety can be obtained, and completed the present invention.

That is, the present invention relates to a skin external preparation characterized by containing one or more saponins obtained from the following plants or salts thereof. (1) Okuna grass (scientific name: Pulsatilla cernua Spreng.
) (2) Cyclamen europaeum (Scientific name: Cyclamen europaeum) (3) Primrose officinal (Scientific name: Primula officinal
i) (4) Hinako no Kozuchi (scientific name: Achyranthes fauriei
Lev.et Van.) (5) Scoop (scientific name: Fatsia japonica Decne.et Pianc
h) (6) Button (scientific name: Caulophyllum robustum
Maxim.) (7) Senninsou (scientific name: Clematis chinensis Osbee
k) (8) Flower bud (scientific name: Anemarrhena asphodeloides Bu
nge)

The structure of the present invention will be described in detail below. The saponin used in the present invention can be obtained by an ordinary method, for example, the following method. That is, without defatting the plant such as turmeric as a raw material, or after defatting with an ordinary fat-soluble organic solvent, water or a lower aliphatic alcohol, or an active ingredient using a hydrous lower aliphatic alcohol at room temperature. Extraction is carried out under heating or under heating, the extract is concentrated by evaporation to remove insoluble substances, and n-butanols are evaporated to dryness. The residue may be dissolved in lower fatty alcohol and then poured into ether with stirring, and the resulting precipitate may be collected by filtration.

The extract thus obtained is a white to brown powder, is easily soluble in water, methanol and dilute methanol, soluble in ethanol, insoluble in chloroform and ether and substantially contains only saponin. It can be used as it is as the saponin of the present invention.

The saponin used in the present invention also has a whitening effect as a salt thereof. Examples of the salt include alkaline earth metal salts such as sodium salt and potassium salt, basic amino acids or alkanolamines, and esters thereof. The compounding amount is usually 0.001 to 20.0% by weight, preferably 0.1% to the total amount of the external preparation for skin.
001 to 5.0% by weight.

The saponin and salts thereof used in the present invention are used in combination with ascorbic acid phosphate and / or placenta extract to further enhance the whitening effect. In that case, the compounding amount of ascorbic acid phosphate and / or placenta extract can be appropriately selected, but it is usually 0.00 based on the total amount of the skin external preparation.
It is 1 to 20.0% by weight, preferably 0.01 to 5.0% by weight. These can be used alone or in combination of two or more. The saponins and salts thereof used in the present invention have no adverse effect locally or systemically.

The external preparation for skin of the present invention comprises an emulsion, lotion, cream, jelly, pack, powder, and
Cosmetics and pharmaceutical preparations of various dosage forms such as ointments can be prepared. Furthermore, the external preparation for skin of the present invention includes, in addition to the above essential components, polysaccharides, cholesterols, plant extracts such as licorice, glycyrrhizic acid and its derivatives, glycyrrhetinic acid and its derivatives, hinokitiol, tocopherol and its derivatives, and ascorbine. Acids and their derivatives, kojic acid and its derivatives, arbutin, hydroquinones, tranexamic acid, phospholipids such as flavonoids, retinol and phosphatidylcholine, antioxidants such as butylhydroxytoluene, ultraviolet absorbers, excipients, oils, metal ions A blocking agent, a pH adjuster, a surfactant, a preservative, a moisturizer, a fragrance, water, an alcohol, a thickener, a coloring agent and the like can be appropriately added as required.

[0012]

EXAMPLES First, prior to the examples, the effectiveness of the present invention will be shown by giving examples of efficacy tests of the active ingredient of the present invention. Tables 1-3
Based on the prescription, the lotion was adjusted by a conventional method and the whitening effect was examined.

<Test method> 40 women aged 28 to 50 years old having spots, freckles, etc. on the face were made into a panel, and 5 people were made into a group, and each component-containing lotion was applied to the face once a day for 3 months every day. After application, the whitening effect after use was evaluated based on the following evaluation criteria.

<Criteria> Remarkable effect: Pigmentation was not noticeable. Effective: Pigmentation was significantly reduced. Slightly effective: Pigmentation became slightly thin. Ineffective: No change in pigmentation. <Judgment> A: When the rate of marked efficacy and efficacy among the subjects is 80% or more B: The rate of marked efficacy and efficacy among the subjects is 65 to 8
In the case of 0% C: Remarkably effective and effective ratio among subjects is 50 to 6
In the case of 5% D: When the ratio of markedly effective and effective in the subjects is less than 50% <Results> The results are shown in Tables 1 to 3 together with the prescription.

[0015]

[Table 1]

[0016]

[Table 2]

[0017]

[Table 3]

From these results, it is understood that the external preparation for skin of the present invention has an excellent whitening effect. Next, the present invention will be described in more detail with reference to examples. The present invention is not limited to this. The blending amount is% by weight.

Example 1 Vanishing Cream Stearic Acid 5.0 Stearyl Alcohol 4.0 Stearic Acid Butyl Alcohol Ester 8.0 Glycerin Monostearic Acid Ester 2.0 Okinagusa Saponin 0.5 Propylene Glycol 10.0 Glycerin 4.0 Caustic Potassium 0 2 Preservative / antioxidant Proper amount Perfume Proper amount Ion-exchanged water Residual (production method) Propylene glycol, caustic potash, and Okinagusa saponin are dissolved in ion-exchanged water and heated to 70
Keep at ℃ (water phase). Mix other ingredients, heat and melt to 70
Keep at ℃ (oil phase). The oil phase is gradually added to the water phase, and after the addition is completed, the temperature is kept for a while to cause the reaction. After that, the mixture is uniformly emulsified with a homomixer and cooled to 30 ° C while stirring well.

Example 2 Neutral Cream Stearyl Alcohol 7.0 Stearic Acid 2.0 Lanolin 2.0 Squalane 5.0 2-Octyldodecyl Alcohol 6.0 Polyoxyethylene (25 mol) Cetyl Alcohol Ether 3.0 Glycerin Mono Stearic acid ester 2.0 Ascorbic acid phosphoric acid ester 3.0 Cyclamensaponin 1.0 Preservative / antioxidant Suitable amount Ion-exchanged water Residual (production method) Ascorbic acid phosphoric acid ester and cyclamensaponin are added and heated. And maintain at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). Add the oil phase to the water phase and perform pre-emulsification, homogenize with a homomixer, and stir well until 30
Cool to ° C.

Example 3 Cold Cream Solid Paraffin 5.0 Beeswax 10.0 Liquid Paraffin 41.0 Glycerin Monostearic Acid 2.0 Ester Polyoxyethylene (20 mol) Sorbitan Monolauric Acid Ester 2.0 Placenta Extract 1.0 Seisei Primrose saponin 2.0 Butylhydroxytoluene 0.4 Soap powder 0.1 Borax 0.2 Ion-exchanged water Residual fragrance Suitable amount Preservative Suitable amount (production method) Soap powder, borax, placenta extract and primrose primrose saponin are added to ion-exchanged water and heated. Melt and keep at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is stirred into the water phase and gradually added to carry out the reaction. After completion of the reaction, emulsify the mixture uniformly with a homomixer, and after emulsification, cool to 30 ° C. while stirring well.

Example 4 Emulsion Stearic acid 2.5 Cetyl alcohol 1.5 Liquid paraffin 10.0 Polyoxyethylene (10 mol) monooleate 2.0 Polyethylene glycol 1500 3.0 Triethanolamine 1.0 Primrose Extract 0.05 Ascorbic acid phosphate 0.1 Ion-exchanged water Residual fragrance Suitable amount Preservative Suitable amount (Production method) Ion-exchanged water with polyethylene glycol 150
0, triethanolamine, ascorbic acid phosphoric acid ester and primrose extract are added and dissolved by heating to maintain the temperature at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase, preliminary emulsification is performed, and the mixture is uniformly emulsified with a homomixer. After emulsification, the mixture is cooled to 30 ° C. with thorough stirring.

Example 5 Emulsion Polyoxyethylene (20 mol) Behenyl ether 2.0 Sorbitan monopalmitate 1.5 Isostearyl palmitate 5.0 Isostearyl myristate 3.0 MC stearic acid 2.0 Cetanol 1.0 Beeswax 2.0 Liquid paraffin 3.0 Glycerin 2.0 Propylene glycol 5.0 Placenta extract 5.0 Arbutin 3.0 Pasque extract 0.2 Ion-exchanged water Residual fragrance Amount Preservative / antioxidant Amount (Production method) Ion Propylene glycol, placenta extract, arbutin and sage extract are added to the exchanged water and dissolved by heating to maintain the temperature at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase, preliminary emulsification is performed, and the mixture is uniformly emulsified with a homomixer. After emulsification, the mixture is cooled to 30 ° C. with thorough stirring.

Example 6 Lotion (alcohol phase) 95% ethanol 10.0 polyoxyethylene hydrogenated castor oil 2.0 propylene glycol 4.0 oleyl alcohol 0.1 lecithin 2.5 (water phase) glycerin 0.8 Primrose saponin 0.1 Cyclamen saponin 0.1 Ion-exchanged water Residual UV absorber Appropriate amount (manufacturing method) The water phase and alcohol phase are adjusted and solubilized.

Example 7 Peel-off type pack (alcohol phase) 95% ethanol 10.0 polyoxyethylene (15 mol) oleyl alcohol ether 2.0 okinagusa saponin 0.5 preservative proper amount perfume proper amount (water phase) polyvinyl alcohol 12. 0 Glycerin 3.0 Polyethylene glycol 1500 1.0 Tranexamic acid 1.0 Ion-exchanged water Residual (manufacturing method) The water phase is adjusted at 80 ° C and cooled to 50 ° C.
Then, the alcohol phase adjusted at room temperature is added, and the mixture is uniformly mixed and allowed to cool.

Example 8 Vanishing Cream Stearic Acid 5.0 Stearyl Alcohol 4.0 Stearic Acid Butyl Alcohol Ester 8.0 Glycerin Monostearic Acid Ester 2.0 Sennin Sousaponin 0.5 Propylene Glycol 10.0 Glycerin 4.0 Caustic Potassium 0 2 Preservatives / antioxidants Appropriate amount Perfume Appropriate amount Ion-exchanged water Residual (production method) Add propylene glycol, caustic potash, and sennen saponin to ion-exchanged water and heat to 7
Keep at 0 ° C (aqueous phase). Mix other ingredients and heat to melt
Keep at 0 ° C (oil phase). The oil phase is gradually added to the water phase, and after the addition is completed, the temperature is kept for a while to cause the reaction. After that, the mixture is uniformly emulsified with a homomixer and cooled to 30 ° C while stirring well.

Example 9 Cold Cream Solid Paraffin 5.0 Beeswax 10.0 Liquid Paraffin 41.0 Glycerin Monostearic Acid 2.0 Ester Polyoxyethylene (20 mol) Sorbitan Monolauric Acid Ester 2.0 Placenta Extract 1.0 Hana Sugesaponin 2.0 Butylhydroxytoluene 0.4 Soap powder 0.1 Borax 0.2 Ion-exchanged water Residual fragrance Suitable amount Preservative Suitable amount (Production method) Soap powder, borax, placenta extract and Hanasagesaponin are added to ion-exchanged water and heated. Dissolve 70
Keep at ℃ (water phase). Mix other ingredients, heat and melt to 70
Keep at ℃ (oil phase). The oil phase is stirred into the water phase and gradually added to carry out the reaction. After completion of the reaction, emulsify the mixture uniformly with a homomixer, and after emulsification, cool to 30 ° C. while stirring well.

Example 10 Lotion (alcohol phase) 95% ethanol 10.0 polyoxyethylene hydrogenated castor oil 2.0 propylene glycol 4.0 oleyl alcohol 0.1 lecithin 2.5 (water phase) glycerin 0.8 Senninsou 0.1 Hanasagesaponin 0.1 Ion-exchanged water Residual UV absorber Appropriate amount (manufacturing method) An aqueous phase and an alcohol phase are adjusted and solubilized.

Example 11 Peel-off type pack (alcohol phase) 95% ethanol 10.0 polyoxyethylene (15 mol) oleyl alcohol ether 2.0 sennin soupaponin potassium salt 5.0 preservative proper amount perfume proper amount (water phase) polyvinyl alcohol 12.0 Glycerin 3.0 Polyethylene glycol 1500 1.0 Tranexamic acid 1.0 Ion-exchanged water Residual (manufacturing method) The water phase is adjusted at 80 ° C and cooled to 50 ° C.
Then, the alcohol phase adjusted at room temperature is added, and the mixture is uniformly mixed and allowed to cool.

Example 12 Vanishing Cream Stearic Acid 5.0 Stearyl Alcohol 4.0 Stearic Acid Butyl Alcohol Ester 8.0 Glycerin Monostearic Acid Ester 2.0 Hinata Nokozuchi Saponin 0.5 Propylene Glycol 10.0 Glycerin 4.0 Caustic Potassium 0.2 Preservative / antioxidant Proper amount Perfume Proper amount Ion-exchanged water Residue (Production method) Propylene glycol, caustic potash, and Hinata nokozuchi saponin are added to ion-exchanged water, dissolved and heated to 70 ° C (water phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is gradually added to the water phase, and after the addition is completed, the temperature is kept for a while to cause the reaction. After that, the mixture is uniformly emulsified with a homomixer and cooled to 30 ° C while stirring well.

Example 13 Neutral Cream Stearyl Alcohol 7.0 Stearic Acid 2.0 Lanolin 2.0 Squalane 5.0 2-Octyldodecyl Alcohol 6.0 Polyoxyethylene (25 mol) Cetyl Alcohol Ether 3.0 Glycerin Mono Stearic acid ester 2.0 Ascorbic acid phosphoric acid ester 3.0 Yatsude saponin sodium salt 1.0 Preservatives / antioxidants Appropriate amount Ion-exchanged water Residual (manufacturing method) Propylene glycol, ascorbic acid phosphoric acid ester and yatsude saponin Add sodium salt and heat to keep at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase to carry out preliminary emulsification, and the mixture is uniformly emulsified with a homomixer and then cooled to 30 ° C. with thorough stirring.

Example 14 Cold Cream Solid Paraffin 5.0 Beeswax 10.0 Liquid Paraffin 41.0 Glycerin Monostearic Acid 2.0 Ester Polyoxyethylene (20 mol) Sorbitan Monolauric Acid Ester 2.0 Placenta Extract 1.0 Louis I-button saponin 2.0 Butylhydroxytoluene 0.4 Soap powder 0.1 Borax 0.2 Ion-exchanged water Residual fragrance Suitable amount Preservative Suitable amount (Production method) Soap powder, borax, placenta extract and Louis I-button saponin in ion-exchanged water Addition by heating and melting and maintaining at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is stirred into the water phase and gradually added to carry out the reaction. After completion of the reaction, emulsify the mixture uniformly with a homomixer, and after emulsification, cool to 30 ° C. while stirring well.

Example 15 Emulsion Stearic Acid 2.5 Cetyl Alcohol 1.5 Liquid Paraffin 10.0 Polyoxyethylene (10 mol) Monooleate 2.0 2.0 Polyethylene Glycol 1500 3.0 Triethanolamine 1.0 Yatsude Extract Substance 0.05 Ascorbic acid phosphoric acid 0.1 Ion-exchanged water Residual fragrance Suitable amount Preservative Suitable amount (Production method) Polyethylene glycol, triethanolamine, ascorbic acid phosphoric acid ester and yam extract are added to ion-exchanged water and dissolved by heating. Keep at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase, preliminary emulsification is performed, and the mixture is uniformly emulsified with a homomixer. After emulsification, the mixture is cooled to 30 ° C. with thorough stirring.

Example 16 Emulsion Polyoxyethylene (20 mol) Behenyl ether 2.0 Sorbitan monopalmitate 1.5 Isostearyl palmitate 5.0 Isostearyl myristate 3.0 MC stearic acid 2.0 Cetanol 1.0 Beeswax 2.0 Liquid paraffin 3.0 Glycerin 2.0 Propylene glycol 5.0 Placenta extract 5.0 Arbutin 3.0 Luyou button extract 0.2 Ion-exchanged water Residual fragrance Suitable amount Preservative / antioxidant Suitable amount (Production method ) Polyethylene glycol, triethanolamine, placenta extract, arbutin and peony extract are added to ion-exchanged water and dissolved by heating and kept at 70 ° C (aqueous phase). The other ingredients are mixed, heated and melted and maintained at 70 ° C. (oil phase). The oil phase is added to the aqueous phase and pre-emulsified and homogenized with a homomixer. After emulsification, mix well at 30 ° C.
Cool down.

Example 17 Lotion (Alcohol phase) 95% Ethyl alcohol 10.0 Polyoxyethylene hydrogenated castor oil 2.0 Propylene glycol 4.0 Oleyl alcohol 0.1 Lecithin 2.5 (Aqueous phase) Glycerin 0.8 Hinata Kozuchi saponin 0.1 Luis button saponin 0.1 Ion-exchanged water Residual UV absorber Appropriate amount (manufacturing method) The water phase and alcohol phase are adjusted and solubilized.

Example 18 Peel-off type pack (alcohol phase) 95% ethanol 10.0 polyoxyethylene (15 mol) oleyl alcohol ether 2.0 yatsudesaponin 5.0 preservative proper amount perfume proper amount (water phase) polyvinyl alcohol 12. 0 Glycerin 3.0 Polyethylene glycol 1500 1.0 Tranexamic acid 1.0 Ion-exchanged water Residual (manufacturing method) The water phase is adjusted at 80 ° C and cooled to 50 ° C.
Then, the alcohol phase adjusted at room temperature is added, and the mixture is uniformly mixed and allowed to cool.

[0037]

As explained above, the external preparation for skin of the present invention has the action of the essential components characteristic of the present invention.
It has an excellent whitening effect, prevents skin spots and freckles, and makes the skin moisturized and highly safe.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification code Internal reference number FI technical display location A61K 35/78 ADA W 8217-4C

Claims (3)

[Claims] 1. An external preparation for skin, which comprises one or more saponins obtained from the following plants or salts thereof. (1) Okuna grass (scientific name: Pulsatilla cernua Spreng.
) (2) Cyclamen europaeum (Scientific name: Cyclamen europaeum) (3) Primrose officinal (Scientific name: Primula officinal
i) (4) Hinako no Kozuchi (scientific name: Achyranthes fauriei
Lev.et Van.) (5) Scoop (scientific name: Fatsia japonica Decne.et Pianc
h) (6) Button (scientific name: Caulophyllum robustum
Maxim.) (7) Senninsou (scientific name: Clematis chinensis Osbee
k) (8) Flower bud (scientific name: Anemarrhena asphodeloides Bu
nge) 2. The external preparation for skin according to claim 1, wherein the content of saponin or its salt is 0.001 to 20.0% by weight based on the total weight of the external preparation. 3. The external preparation for skin according to claim 1, which is an external preparation for whitening.