JP2000053529A - Agent for external use for skin - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an agent for external use for skin, markedly improving a skin-beautifying and whitening effect, also excellent in moisture retention effect, stability and safety. SOLUTION: This agent for external use for skin, contains one or two or more kinds selected from the group consisting of L-ascorbic acid and its derivatives, a placental extract, kojic acid and its derivatives, azelaic acid and its derivatives, glucosamine and its derivatives, a hydroquinone glycoside and its derivatives, tranexamic acid and its derivatives, salicylic acid and its derivatives, and Zingiber aromaticum (Zingiberaceae) or its solvent extracts.

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 has remarkably improved skin whitening effect, excellent moisturizing effect, and excellent stability and safety.

[0002]

2. Description of the Related Art Pigments such as skin spots and freckles are stimulated by abnormal hormones and ultraviolet rays, resulting in increased production of melanin in epidermal pigment cells and excessive deposition of melanin on the epidermis. Occurs. Substances that inhibit melanin production, such as L-
A method of administering a large amount of ascorbic acid, a method of injecting glutathione or the like, a method of applying kojic acid, cysteine, or the like in the form of an ointment, a cream, a lotion, and the like, and topically applying the same are employed.

[0003]

However, many of these have problems in terms of stability, safety, odor and the like, and the expected effects are weak and have not been satisfactory. Further, when an external preparation having a moisturizing action is required, it is necessary to separately add a moisturizing agent or the like, and in this case, there is a disadvantage that the skin becomes sticky and the feeling of use is impaired.

[0004]

In view of such circumstances, the present inventors have conducted intensive studies to obtain an external preparation for skin having both an excellent whitening effect and a moisturizing effect. As a result, L-ascorbic acid and L-ascorbic acid Derivative, placenta extract, kojic acid and its derivative, azelaic acid and its derivative, glucosamine and its derivative, hydroquinone glycoside and its derivative, tranexamic acid and its derivative, salicylic acid and its kind selected from the group consisting of its derivative Or two or more, and Lumpuyan (Zingiber aromaticum (Z
ingiberaceae)) can provide a synergistic whitening effect compared to the case of using each alone,
And has a moisturizing effect, found that stability is also improved,
The present invention has been completed.

That is, the present invention relates to L-ascorbic acid and its derivatives, placental extract, kojic acid and its derivatives, azelaic acid and its derivatives, glucosamine and its derivatives, glycosides of hydroquinone and its derivatives, tranexamic acid and One or two or more selected from the group consisting of its derivatives, salicylic acid and its derivatives, and Lumpuyan (Zingibera
ceae)) or a solvent extract thereof.

Hereinafter, the configuration of the present invention will be described in detail. L-ascorbic acid used in the present invention is generally referred to as vitamin C, and due to its strong reducing action, shows an inhibitory action on the tyrosinase reaction, which is the rate-limiting step of melanin action, and shows a reducing action on melanin. Also, L-
Examples of the derivatives of ascorbic acid include L-ascorbic acid monostearate, L-ascorbic acid monopalmitate, L-ascorbic acid monooleate and the like.
Ascorbic acid monoalkyl esters; L-ascorbic acid monophosphate, L-ascorbic acid-2-
L-ascorbic acid monoester derivatives such as sulfate esters; dialkyl esters such as L-ascorbic acid distearate, L-ascorbic acid dipalmitate and L-ascorbic acid dioleate; L-ascorbic acid such as L-ascorbic acid diphosphate ester Diesters; trialkyl esters such as L-ascorbic acid tristearate, L-ascorbic acid tripalmitate and L-ascorbic acid triolate; and ascorbic acid triesters such as L-ascorbic acid triphosphate. Can be. Particularly preferred as L-ascorbic acid and its derivatives are L-ascorbic acid, L-ascorbic acid phosphate, L-ascorbic acid-2-sulfate and salts thereof.

Examples of the kojic acid derivative used in the present invention include kojic acid esters such as kojic acid alkyl ester and kojic acid ethers such as kojic acid alkyl ether.

Examples of the azelaic acid derivative used in the present invention include azelaic acid monoesters such as azelaic acid monoalkyl ester, and azelaic acid diesters such as azelaic acid dialkyl ester.

The glucosamine derivatives used in the present invention include, for example, glucosamine esters such as acetylglucosamine, and glucosamine ethers such as glucosamine methyl ether.

The hydroquinone glycoside used in the present invention includes, for example, hydroquinone α-D-glucose, hydroquinone β-D-glucose, hydroquinone α-L-glucose, hydroquinone β-L-glucose, hydroquinone α-D. -Galactose, hydroquinone β-D-galactose, hydroquinone α-L-
Hexasaccharide glycosides such as galactose and hydroquinone β-L-galactose; hydroquinone α-D-ribose, hydroquinone β-D-ribose, and hydroquinone α-L
-Ribose, hydroquinone β-L-ribose, hydroquinone α-D-arabinose, hydroquinone β-D
Pentacarbon sugar glycosides such as arabinose, hydroquinone α-L-arabinose and hydroquinone β-L-arabinose; hydroquinone α-D-glucosamine, hydroquinone β-D-glucosamine, hydroquinone α-L-
Glucosamine, hydroquinone β-L-glucosamine,
Amino sugar glycosides such as hydroquinone α-D-galactosamine, hydroquinone β-D-galactosamine, hydroquinone α-L-galactosamine, hydroquinone β-L-galactosamine; hydroquinone α-D-glucuronic acid, hydroquinone β-D-glucuronic acid , Hydroquinone α-L-glucuronic acid, hydroquinone β-L-
Glucuronic acid, hydroquinone α-D-galacturonic acid, hydroquinone β-D-galacturonic acid, hydroquinone α-L-galacturonic acid, hydroquinone β-L
-Uronic acid glycosides such as galacturonic acid. Examples of the derivative include an ester such as an acetylated product and an ether such as a methylated product. From the viewpoints of whitening effect, availability and stability, hydroquinone β-D -Glucose (generic name:
Arbutin, hereinafter referred to as arbutin. ) Is preferred.

The tranexamic acid derivative used in the present invention includes a tranexamic acid dimer (trans-4 hydrochloride).
-(Trans-4-aminomethylcyclohexanecarbonyl) aminomethylcyclohexanecarboxylic acid), an ester form of tranexamic acid and hydroquinone (trans-
4-aminomethylcyclohexanecarboxylic acid 4'-hydroxyphenyl ester), an ester of tranexamic acid and gentisic acid (2- (trans-4-aminomethylcyclohexylcarbonyloxy) -5-hydroxybenzoic acid and a salt thereof), tranexamic acid (Trans-4-aminomethylcyclohexanecarboxylic acid methylamide and its salt, trans-4-acetylaminomethylcyclohexanecarboxylic acid and its salt, trans-4- (p-methoxybenzoyl) aminomethylcyclohexanecarboxylic acid and its salt , Trans-4-
Guanidinomethylcyclohexanecarboxylic acid and salts thereof).

The derivatives of salicylic acid used in the present invention include 3-methoxysalicylic acid and salts thereof, 4-methoxysalicylic acid and salts thereof, and 5-methoxysalicylic acid and salts thereof.

In the practice of the present invention, one or more of these may be appropriately selected and blended. Of these, L-ascorbic acid and L-ascorbic acid are particularly preferred.
Ascorbic acid phosphate, L-ascorbic acid-
L-ascorbic acid or its derivative such as 2-sulfate and hydroquinone β-D-glucose.

[0014] L- formula to be incorporated in the external preparation for skin according to the present invention.
Ascorbic acid and its derivatives, placental extract, kojic acid and its derivatives, azelaic acid and its derivatives,
Glucosamine and its derivatives, glycosides of hydroquinone and its derivatives, tranexamic acid and its derivatives, one or two or more kinds selected from the group consisting of salicylic acid and its derivatives are not particularly limited,
Generally, 0.001 to 20.0 with respect to the total amount of the external preparation for skin.
% By weight, preferably 0.01 to 10.0% by weight, particularly preferably 0.1 to 7.0% by weight. When the amount is less than 0.001% by weight, the whitening effect of the external preparation for skin tends to be poor. Conversely, when the amount is more than 20.0% by weight, an increase in the whitening effect cannot be substantially expected. It also tends to be difficult to mix the agent.

According to the present invention, Lumpuyan (Zingiber aroma)
ticum (Zingiberaceae) is a perennial plant that is native to Indonesia, sometimes cultivated medicinally, and is wild in many parts of the country. In the present invention, in particular, the rhizome or the whole plant of the above-mentioned plant is dried and pulverized into a powder, or immersed or heated under reflux with an extraction solvent, and then filtered.
The filtrate can be used after concentration or removal of the solvent,
It is preferable to use it as an extract from the viewpoint of usability.
The extraction solvent used in the present invention may be any solvent that is usually used for extraction, particularly water, alcohols such as methanol, ethanol, propylene glycol, and 1,3-butylene glycol, hydrous alcohols, and urea-containing alcohols. Organic solvents such as acetone and ethyl acetate can be used alone or in combination.

The present inventors have found that Lumpuyan (Zingiber aro)
maticum (Zingiberaceae)) or a solvent extract thereof has already been found to have a whitening effect (Japanese Patent Application Laid-Open No. 9-71522).
Ascorbic acid and its derivatives, placenta extract, kojic acid and its derivatives, etc. and Lumpuyan (Zingiber aromati
cum (Zingiberaceae)) or a solvent extract thereof, the whitening effect is synergistically improved, and the problems such as the stability of the conventionally known whitening agent are eliminated, and the moisturizing effect is imparted. It is a new thing that can be done.

The amount of Lumpuyan or its solvent extract is not particularly limited, but is generally 0.0001 to 20.0% by weight, preferably 0.01 to 10% by weight, as a dry solid content based on the total amount of the external preparation for skin. 0.0% by weight. If the amount is less than 0.0001% by weight, the whitening effect and moisturizing effect of the external preparation for skin tend to be insufficient, and the effect of suppressing the skin irritation of the external preparation tends to be poor.
Even if it is added in excess of 0% by weight, an increase in the effect cannot be substantially expected, and it tends to be difficult to incorporate it into an external preparation for skin.

The skin whitening effect of the present invention can be further enhanced by further blending an ultraviolet ray protective agent with the external preparation for skin of the present invention. The ultraviolet ray protective agent used in the present invention is a substance that absorbs ultraviolet rays physicochemically.
And an “ultraviolet ray blocking agent” that is a substance that scatters and reflects ultraviolet rays by physical action, and these can be used alone or in combination of two or more.

Examples of the ultraviolet absorber include paraaminobenzoic acid (hereinafter abbreviated as PABA), PABA monoglycerin ester, N, N-dipropoxy PABA ethyl ester, N, N-diethoxy PABA ethyl ester,
N, N-dimethyl PABA ethyl ester, N, N-dimethyl PABA butyl ester, N, N-dimethyl PA
Benzoic acid UV absorbers such as BA amyl ester, anthranilic acid UV absorbers such as homomenthyl-N-acetylanthranilate, amyl salicylate, menthyl salicylate, homomenthyl salicylate, octyl salicylate, phenyl salicylate, benzyl salicylate, p- Salicylic acid ultraviolet absorbers such as isopropanol phenyl salicylate, octyl cinnamate, ethyl-4-isopropyl cinnamate, methyl-2,5
-Diisopropylcinnamate, ethyl-2,4-diisopropylcinnamate, methyl-2,4-diisopropylcinnamate, propyl-p-methoxycinnamate, isopropyl-p-methoxycinnamate, isoamyl-p-methoxycinnamate, octyl -P-methoxycinnamate (2-ethylhexyl-p-methoxycinnamate), 2-ethoxyethyl-p-methoxycinnamate, cyclohexyl-p-methoxycinnamate, ethyl-α-cyano-β-phenylcinnamate,
2-ethylhexyl-α-cyano-β-phenylcinnamate, glyceryl mono-2-ethylhexanoyl-diparamethoxycinnamate, 3,4,5-trimethylcinnamate 3-methyl-4- [methylbis (trimethylsiloxy ) Silyl] butyl and other cinnamic acid ultraviolet absorbers;
4-dihydroxybenzophenone, 2,2'-dihydroxy-4-methoxybenzophenone, 2,2'-dihydroxy-4,4'-dimethoxybenzophenone, 2,
2,4,4'-tetrahydroxybenzophenone, 2-
Hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxy-4'-methylbenzophenone, 2
-Hydroxy-4-methoxybenzophenone-5-sulfonate, 4-phenylbenzophenone, 2-ethylhexyl-4'-phenyl-benzophenone 2-carboxylate, 2-hydroxy-4-n-octoxybenzophenone, 4-hydroxy- Benzophenone-based ultraviolet absorbers such as 3-carboxybenzophenone, 3- (4′-
Methylbenzylidene) d, l-camphor, 3-benzylidene d, l-camphor, urocanic acid, urocanic acid ethyl ester, 2-phenyl-5-methylbenzoxanol, 2,2-hydroxy-5-methylphenylbenzotriazole, 2- (2'-hydroxy-5'-t
-Octylphenyl) benzotriazole, 2- (2 ′)
-Hydroxy-5'-methylphenylbenzotriazole, dibenzarazine, dianisoylmethane, 4-ter
t-butyl-4'-methoxydibenzoylmethane, 5-
(3,3-dimethyl-2-norbornylidene) -3-pentan-2-one and the like. Of these, particularly preferred are 4-tert-butyl-4'-methoxydibenzoylmethane, octyl-p-methoxycinnamate, 2-hydroxy-4-methoxybenzophenone, and 2-hydroxy-4-methoxybenzophenone-5.
-Sulfonates and the like.

Further, as an ultraviolet ray blocking agent, titanium oxide (TiO ₂ ), talc (MgSiO ₂ ), carmine (FeO ₂ ), bentonite, kaolin, zinc oxide (Z
nO) and the like.

When such an ultraviolet ray protective agent is blended, the blending amount is usually 0.01 to 30.
0% by weight, more preferably 0.1 to 20.0%.
% By weight.

In addition to the above essential components, the skin external preparation of the present invention also contains other components usually used in skin external preparations such as cosmetics and pharmaceuticals, such as oils, wetting agents, antioxidants, surfactants, and preservatives. An agent, a humectant, a fragrance, water, alcohol, a thickener and the like can be appropriately compounded as needed.

The dosage form of the external preparation for skin according to the present invention is arbitrary. For example, it can take any dosage form such as a solubilizing system such as a lotion, an emulsifying system such as an emulsion or a cream, or an ointment or a dispersion. it can.

[0024]

EXAMPLES Next, the present invention will be described in more detail with reference to examples, but it goes without saying that the technical scope of the present invention is not limited to these examples. In addition, in the following examples, the compounding amount is% by weight.

Examples 1 to 8, Comparative Examples 1 to 9 (alcohol phase) 95% ethanol 25.0% by weight Polyoxyethylene (25 mol) hydrogenated castor oil ether 2.0 2-hydroxy-4-methoxy benzophenone-5 -Sulfonate 3.0 Preservative / Antioxidant Appropriate amount Fragrance Appropriate amount Chemical (Table 1 and Table 2) (Aqueous phase) Glycerin 2.0 Propylene glycol 1.0 Ion-exchanged water Residue [Production method] Aqueous phase, alcohol phase Is prepared and solubilized.

Examples 1 to 8 and Comparative Examples 1 to 9 obtained
The whitening effect and the moisturizing effect were determined from use tests such as the skin whitening effect, the removal of spots, and freckles on the skin by the cumulative application using the lotion. The test method and evaluation method are as follows. The results are shown in Tables 1 and 2.

(1) Whitening Effect (Test Method) The sample lotions of Examples 1 to 8 and Comparative Examples 1 to 9 were taken in the morning with a test group of 20 subjects suffering from darkness, spots, freckles, etc. I had it applied to my face every day for a month. Three months later, the whitening effect was examined, and the degree of black and white, spots, and freckles before and after the start was evaluated on a seven-point scale.

(Judgment Criteria) 1: No black and white, no stain, no freckles. 2: Black, spots, freckles are slight. 3: There is slight darkness, spots, and freckles. 4: Medium-to-mild darkness, spots, and freckles. 5: Black, spots, freckles are moderate. 6: Dark and black, spots and freckles are moderately high. 7: Black, spots, freckles are high.

(Judgment) ：: The ratio (effective rate) of those who improved by two or more steps among the examinees was 80% or more. ：: The ratio (effective rate) of the test subjects who improved by two or more stages is 50% or more and less than 80%. Δ: The ratio (effective rate) of the test subjects who improved two or more stages is 30% or more and less than 50%. X: The ratio (effective rate) of persons who improved two or more stages among the test subjects is less than 30%.

(2) Moisturizing effect The amount of UV irradiation was changed beforehand, and the MED (minimum erythema amount) was measured in advance by using 1.44 MED for two FL40SE lamps and two BLB lamps (manufactured by Toshiba) for 20 healthy persons. The abdomen was irradiated. A 2 × 2 cm site irradiated with UV, a site where the samples of Examples 1 to 8 and Comparative Examples 1 to 9 are applied,
The site to which the sample having the same formulation as that of the examples and comparative examples was applied except for the drug, and the site to which nothing was applied (control) were determined, and application was continued for one week. One week later, the skin conductance was measured in a thermo-hygrostat (SKICON-200; manufactured by IBS Co., Ltd.) to determine the water content of the stratum corneum.

When the water content of the stratum corneum at the site where the drug-removed sample was applied was set to 1, the value of the water content of the stratum corneum at the site where the sample of each Example and Comparative Example was applied, and the water content of the control stratum corneum were Tables 1 and 2 also show the average value of the water content of the stratum corneum at the site where the sample of each example was applied when the value was 1.

[0032]

[Table 1] {Example 1 2 3 4 5 6 7 8}マ グ ネ シ ウ ム Magnesium L-ascorbic acid phosphate 1.0 − − − − − − − Placenta Extract − 1.0 − − − − − − − Arbutin − − 1.0 − − − − − − Kojic acid − − − 1.0 − − − − Azelaic acid − − − − 1.0 − − − Glucosamine − − − − − − 1.0 − − Tranexamic acid − − − − − − − 1.0 − Salicylic acid − − − − − − − 1.0 1.0 Lumpuyan 80% ethanol aqueous solution Reflux extract (as dry solid content) 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0 ─────────── ─────────────────────── Whitening effect ◎ ○ ◎ ○ ○ ○ ○ ○ Moisturizing effect Removed sample 1.4 1.2 1.4 1.2 1.2 1.2 1.3 1.3 vs control 2 1.3 2 1.3 1.3 1.3 1.5 1.5 ────────────────────────────── ────

[0033]

[Table 2] Comparative Example 1 2 3 4 5 6 7 8 9マ グ ネ シ ウ ム Magnesium L-ascorbic acid phosphate 2.0 − − − − − ---Placental extract-2.0-------Arbutin--2.0------Kojic acid---2.0-----Azelaic acid----2.0----Glucosamine-- − − − 2.0 − − − Tranexamic acid − − − − − − 2.0 − − Salicylic acid − − − − − − − 2.0 − Lumpuyan 80% ethanol aqueous solution Reflux extract (as dry solids) − − − − − − − − 2.0 ─────────────────────────────────── Whitening effect ○ × × × × △ △ ○ Moisturizing effect vs. chemical removal sample 1 1 1 1 1 1 1 1 1.1 ───────────────────────────── ──────

As is clear from Tables 1 and 2, the Example has a synergistic skin whitening effect and has both the whitening and moisturizing effects as compared with the Comparative Example. Admitted.

Example 9 Vanishing cream stearic acid 6.0% by weight sorbitan monostearate 2.0 polyoxyethylene (20 mol) sorbitan monostearate 1.5 arbutin 7.0 sodium bisulfite 0.03 propylene glycol 10.0 Rumpuyan 80% ethanol aqueous solution Reflux extract (as dry solids) 1.0 Preservative / antioxidant appropriate amount Perfume appropriate amount Ion-exchange water residue (Production method) Ion-exchange water 80% ethanol aqueous solution reflux extract and arbutin And propylene glycol, and heat to maintain 70 ° C. (aqueous phase). The other components are mixed, heated and melted and kept at 70 ° C. (oil phase). The oil phase is added to the water phase to perform preliminary emulsification, and after uniform emulsification with a homomixer, the mixture is cooled to 30 ° C. while stirring well.

Example 10 Neutral Cream Stearyl Alcohol 7.0% by Weight Stearic Acid 2.0 Hydrogenated Lanolin 2.0 2-Hydroxy-4-methoxybenzophenone 3.5 Squalane 5.0 2-Octyldodecyl Alcohol 6.0 Polyoxyethylene (25 mol) Cetyl alcohol ether 3.0 Glycerin monostearate 2.0 Placenta extract 0.1 Propylene glycol 5.0 Lumpuyan 80% ethanol aqueous solution Reflux extract (as dry solid content) 10.0 Perfume Appropriate amount Preservative / antioxidant Appropriate amount Ion-exchanged water Residue (Preparation method) Add 80% ethanol aqueous solution reflux extract, placenta extract and propylene glycol to ion-exchanged water and heat to 70 ° C (aqueous phase). The other components are mixed, heated and melted and kept at 70 ° C. (oil phase). The oil phase is added to the water phase to perform preliminary emulsification, and after uniform emulsification with a homomixer, the mixture is cooled to 30 ° C. while stirring well.

Example 11 Cold cream Solid paraffin 5.0% by weight Beeswax 10.0 Vaseline 15.0 Liquid paraffin 41.0 Glycerin monostearate 2.0 Polyoxyethylene (20 mol) Sorbitan monolaurate 2 2.0 Kojic acid 2.0 4-tert-Butyl-4'-methoxydibenzoylmethane 3.5 Soap powder 0.1 Borax 0.2 Lumpuyan 80% ethanol aqueous solution Reflux extract (as dry solid content) 0.1 Ion Exchanged water Residual fragrance Appropriate amount Preservative / antioxidant Appropriate amount (Preparation method) Add 80% aqueous solution of Lumpuyan ethanol reflux, kojic acid, soap powder and borax to ion-exchanged water.
Heat and maintain at 70 ° C (aqueous phase). The other components are mixed, heated and melted and kept at 70 ° C. (oil phase). The oil phase is gradually added to the aqueous phase while stirring to carry out the reaction. After completion of the reaction, the mixture is uniformly emulsified with a homomixer, and cooled to 30 ° C. while stirring well after emulsification.

Example 12 Emulsion Polyoxyethylene (20 mol) Polyoxypropylene (2 mol) Cetyl alcohol 1.0% by weight Octyl-p-methoxycinnamate 3.5 Silicone KF96 (20cs) (manufactured by Shin-Etsu Chemical Co., Ltd.) 2 0.0 Liquid paraffin (medium viscosity) 3.0 Propylene glycol 5.0 Arbutin 2.0 Sodium bisulfite 0.03 Glycerin 2.0 Ethanol 15.0 Carboxyvinyl polymer 0.3 Hydroxypropyl cellulose 0.1 KOH Preservative Appropriate amount Rumpuyan hydrous alcohol extract (as dry solids) 20.0 Ion-exchanged water Residue (Preparation method) Heat-dissolve Rumpuyan hydrous alcoholic extract and arbutin in ion-exchanged water and ethanol, and further dissolve propylene glycol or lower water-soluble components Dissolve
Keep at 0 ° C. (aqueous phase). The other oil components are mixed, heated and melted and kept at 70 ° C. (oil phase). The oil phase is added to the water phase, preliminarily emulsified, homogenized with a homomixer, emulsified, and cooled to 30 ° C. while stirring well.

Example 13 Emulsion Polyoxyethylene (20 mol) Polyoxypropylene (2 mol) Cetyl alcohol 1.0% by weight Silicone KF96 (20cs) (manufactured by Shin-Etsu Chemical Co., Ltd.) 2.0 Liquid paraffin (medium viscosity) 0 Propylene glycol 5.0 Ascorbic acid 5.0 4-tert-Butyl-4'-methoxydibenzoylmethane 3.5 Glycerin 2.0 Ethanol 15.0 Carboxyvinyl polymer 0.3 Hydroxypropylcellulose 0.1 KOH Suitable amount Preservative Rumpuyan 80% ethanol aqueous solution reflux extract (as dry solids) 7.0 Ion-exchanged water residue (Preparation method) Heat-dissolve the Rumpuyan 80% ethanol aqueous reflux extract in ion-exchanged water and ethanol, and further dissolve below propylene glycol Dissolve the water-soluble components of (Aqueous phase). Mix with other oily ingredients, heat and melt to 70
C (oil phase). The oil phase is added to the water phase, preliminarily emulsified, and uniformly emulsified by a homomixer. After emulsification, the mixture is cooled to 30 ° C. while stirring well.

Example 14 Emulsion Polyoxyethylene (20 mol) Polyoxypropylene (2 mol) Cetyl alcohol 1.0% by weight Silicone KF96 (20cs) (manufactured by Shin-Etsu Chemical Co., Ltd.) 2.0 Liquid paraffin (medium viscosity) 0 Propylene glycol 5.0 Glycerin 2.0 2-Hydroxy-4-methoxybenzophenone 3.5 Ethanol 15.0 Carboxyvinyl polymer 0.3 Hydroxypropylcellulose 0.1 KOH Appropriate amount Preservative Appropriate placenta extract 5.0 Lumpuyan 80 % Ethanol aqueous solution reflux extract (as dry solid content) 7.0 ion-exchanged water residue (Preparation method) Heat-dissolve 80% ethanol aqueous solution reflux extract and placenta extract in ion-exchanged water and ethanol, and further dissolve below propylene glycol Dissolve the water-soluble components of Keep (water phase). Mix with other oily ingredients,
Heat to melt and maintain at 70 ° C (oil phase). The oil phase is added to the water phase, preliminarily emulsified, and uniformly emulsified by a homomixer. After emulsification, the mixture is cooled to 30 ° C. while stirring well.

Example 15 Emulsion Polyoxyethylene (20 mol) Polyoxypropylene (2 mol) Cetyl alcohol 1.0% by weight Silicone KF96 (20cs) (manufactured by Shin-Etsu Chemical Co., Ltd.) 2.0 Liquid paraffin (medium viscosity) 0 Propylene glycol 5.0 Glycerin 2.0 Ethanol 15.0 Carboxyvinyl polymer 0.3 Hydroxypropylcellulose 0.1 KOH qs Preservative qs Kojic acid 3.0 Lumpuyan 80% ethanol aqueous solution Reflux extract (as dry solids) 3.0 Ion-exchanged water Residue (Preparation method) Ion-exchanged water, a reflux extract of 80% aqueous Lumpuyan ethanol solution and kojic acid are dissolved by heating, and water-soluble components such as propylene glycol or less are further dissolved and kept at 70 ° C (water phase). Mix with other oily ingredients, heat and melt to 7
Keep at 0 ° C. (oil phase). The oil phase is added to the water phase, preliminarily emulsified, and uniformly emulsified by a homomixer. After emulsification, the mixture is cooled to 30 ° C. while stirring well.

Example 16 Emulsion Stearic acid 1.5% by weight Cetyl alcohol 0.5 Beeswax 2.0 Polyoxyethylene (20 mol) Monooleate 1.0 Glycerin monostearate 1.0 Ethanol 10.0 Arbutin 20.0 Sodium bisulfite 0.03 Propylene glycol 5.0 80% aqueous solution of lumpuyan ethanol Reflux extract (as dry solids) 1.0 Ion-exchanged water Residual perfume Appropriate amount Preservative / antioxidant Appropriate amount (Method) To the water are added a reflux extract of 80% aqueous Lumpuyan ethanol, arbutin and propylene glycol, and the mixture is dissolved by heating and maintained at 70 ° C (aqueous phase). Add the flavor to ethanol and dissolve (alcohol phase). The other oil components are mixed, heated and melted and kept at 70 ° C. (oil phase). The oil phase is added to the water phase, pre-emulsified, and homogenized uniformly with a homomixer. Add alcohol phase while stirring. Then, cool to 30 ° C with stirring.

Example 17 Emulsion Microcrystalline wax 1.0% by weight Beeswax 2.0 Lanolin 2.0 Liquid paraffin 20.0 Squalane 10.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 mol) Sorbitan mono Oleic acid ester 1.0 Arbutin 5.0 Sodium bisulfite 0.03 Tranexamic acid 5.0 Propylene glycol 7.0 Lumpuyan 80% aqueous ethanol reflux extract (as dry solids) 0.0001 Octyl-p-methoxycinnamate 3.5 Ion-exchanged water Residual perfume Appropriate amount Preservative / Antioxidant Appropriate amount (Preparation method) Add 80% ethanol aqueous solution of Rumpuyan reflux extract, arbutin, tranexamic acid and propylene glycol to ion-exchanged water and heat to 70 ° C ( Aqueous phase). The other components are mixed, dissolved by heating and kept at 70 ° C. (oil phase). While stirring the oil phase, the aqueous phase is gradually added to the oil phase, and the mixture is uniformly emulsified with a homomixer. After emulsification, cool to 30 ° C with good stirring.

Example 18 Jelly 95% ethanol 10.0% by weight Dipropylene glycol 15.0 Polyoxyethylene (15 mol) Oleyl alcohol ether 2.0 Salicylic acid 0.5 Sodium bisulfite 0.03 Ascorbic acid distearate 0.5 Carboxyvinyl polymer 1.0 (trade name: Carbopol 941) Caustic potash 0.15 L-arginine 0.1 Lumpuyan 80% ethanol aqueous solution Reflux extract (as dry solid content) 2.0 Perfume Appropriate preservative Appropriate ion-exchanged water Residue (Preparation method) Lumppuyan 80% aqueous ethanol reflux extract, arbutin and carbopol 941 were uniformly dissolved in ion-exchanged water, while dipropylene glycol and polyoxyethylene (15 mol) oleyl alcohol ether in 95% ethanol were used. Dissolve the other ingredients and add to the aqueous phase. Then, it is neutralized with caustic potash and L-arginine to thicken.

Example 19 Peel-off type pack (alcohol phase) 95% ethanol 10.0% by weight polyoxyethylene (15 mol) oleyl alcohol ether 2.0 4-tert-butyl-4′-methoxydibenzoylmethane 3.5 Preservatives Appropriate amount Perfume Appropriate amount (aqueous phase) Lumpuyan 80% ethanol aqueous solution Reflux extract (as dry solids) 3.0 Azelaic acid 1.0 Sodium bisulfite 0.03 Polyvinyl alcohol 12.0 Glycerin 3.0 Polyethylene glycol 1500 1 0.0 ion-exchanged water residue (Preparation method) Prepare an aqueous phase at 80 ° C and cool to 50 ° C.
Next, the alcohol phase prepared at room temperature is added, mixed uniformly, and allowed to cool.

Example 20 Pack with Powder (Alcohol Phase) 95% Ethanol 2.0% by Weight Preservatives Appropriate Perfume Appropriate Coloring Appropriate Ascorbic Acid Dioleate 1.0 (Aqueous Phase) Rumpuyan 80% Ethanol Reflux Extract (Dry Solid) 7.0) Arbutin 1.0 Propylene glycol 7.0 Zinc flower 25.0 Kaolin 20.0 Ion-exchanged water Residue (Preparation method) An aqueous phase is uniformly prepared at room temperature. Next, the alcohol phase prepared at room temperature is added and mixed uniformly.

Example 21 Water Absorbing Ointment Vaseline 40.0 wt% Stearyl Alcohol 18.0 Mokurou 20.0 Polyoxyethylene (10 mol) Monooleate 0.25 Glycerin Monostearate 0.25 Placenta Extract 0 Rumpuyan 80% ethanol aqueous solution reflux extract (as dry solids) 10.0 Ion-exchanged water residue (Preparation method) Add Rumpuyan 80% ethanol aqueous solution reflux extract and placenta extract to ion-exchanged water and keep at 70 ° C (water phase). Other components are mixed and dissolved at 70 ° C. (oil phase). Add the oil phase to the aqueous phase, after homogenizing uniformly with a homomixer,
Cooling.

Example 22 Solid foundation (formulation)% by weight Talc 43.1 Kaolin 15.0 Sericite 10.0 Zinc white 7.0 Titanium dioxide 3.8 Yellow iron oxide 2.9 Black iron oxide 0.2 Lumpuyang dried Powder 0.1 Glucosamine 1.0 Squalane 8.0 Isostearic acid 4.0 POE sorbitan monooleate 3.0 Isocetyl octanoate 2.0 Preservatives Appropriate amount Fragrance Appropriate amount (Production method) Powdery components of talc to glucosamine are thoroughly mixed with a blender Then, an oily component of squalane to isocetyl octanoate, a preservative, and a flavor are added thereto, and the mixture is kneaded well, and then filled and molded into a container.

In the same skin whitening and moisturizing effect tests as in Examples 1 to 8, all the skin external preparations obtained in Examples 9 to 22 showed the same effect as Examples 1 to 8. .

[0050]

As described above, the external preparation for skin according to the present invention is a highly safe external preparation for skin with significantly improved skin whitening effect. Further, since the external preparation for skin of the present invention has a moisturizing effect, a sufficient moisturizing effect can be obtained even when the amount of the moisturizing agent is reduced, and a good feeling of use without stickiness can be obtained. . Furthermore, the whitening effect can be further enhanced by blending an ultraviolet ray protective agent.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 31/19 603 A61K 31/19 603 31/35 601 31/35 601 31/375 31/375 31/60 31/60 31/70 602 31/70 602 607 607 35/50 35/50 35/78 35/78 C X

Claims (9)

[Claims] 1. L-ascorbic acid and a derivative thereof,
One or two selected from the group consisting of placenta extract, kojic acid and its derivatives, azelaic acid and its derivatives, glucosamine and its derivatives, hydroquinone glycosides and its derivatives, tranexamic acid and its derivatives, salicylic acid and its derivatives An external preparation for skin, characterized by containing at least one species and Lumpuyan (Zingiber aromaticum (Zingiberaceae)) or a solvent extract thereof. 2. The external preparation for skin according to claim 1, which comprises L-ascorbic acid or a derivative thereof, and lumpuyan or a solvent extract thereof. 3. The external preparation for skin according to claim 2, wherein the L-ascorbic acid and a derivative thereof are L-ascorbic acid, L-ascorbic acid phosphate, L-ascorbic acid-2-sulfate or a salt thereof. . 4. The external preparation for skin according to claim 1, wherein the hydroquinone glycoside and its derivative are hydroquinone β-D-glucose. 5. A hydroquinone β-D-glucose,
2. A method according to claim 1, which comprises Lumpuyan or a solvent extract thereof.
The topical skin preparation according to the above. 6. L-ascorbic acid and its derivatives,
One or two selected from the group consisting of placenta extract, kojic acid and its derivatives, azelaic acid and its derivatives, glucosamine and its derivatives, hydroquinone glycosides and its derivatives, tranexamic acid and its derivatives, salicylic acid and its derivatives The external preparation for skin according to claim 1, wherein the amount of at least one kind is 0.001 to 20.0% by weight based on the total amount of the external preparation for skin. 7. Lumpuyan (Zingiber aromaticum (Zin)
giberaceae)) or its solvent extract in the total amount of the external preparation for skin is 0.0001 to 20.0 as a dry solid content.
2. The external preparation for skin according to claim 1, which is contained by weight. 8. The external preparation for skin according to claim 1, which is an external preparation for skin whitening. 9. The method according to claim 1, further comprising an ultraviolet protection agent.
The topical skin preparation according to the above.