JP2000212026A - Preparation for external use for skin - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a preparation for external use for skin exhibiting sufficient drug action of an active oxygen elimination agent, having excellent active oxygen elimination effect and safely and suitably applicable to a biological system by making the preparation include an acerola extract and an active oxygen elimination agent. SOLUTION: The objective preparation contains (A) an acerola extract and (B) an active oxygen elimination agent (e.g. superoxide dismutase, mannitol, carotenoid and animal and vegetable extract containing the same). The extract of the component A can be produced by extracting a fruit of acerola which is a fruit tree belonging to the genus Malpighia with a proper extraction solvent at low temperature, normal temperature or under heating. The compounding amount of the component A is preferably 0.00005-5 wt.%, more preferably 0.00005-1 wt.% in terms of dried solid and that of the component B is preferably 0.00001-10 wt.%, more preferably 0.0001-5 wt.%.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin, and more particularly, to the production of lipid peroxide due to the production of active oxygen in the skin by adding an acerola extract and an active oxygen remover. The present invention relates to an external preparation for skin, such as cosmetics and external medicines, which has an excellent anti-aging effect on the skin and an effect for improving the rough skin, which can prevent skin inflammation, blackening, aging and the like.

[0002]

2. Description of the Related Art Conventionally, skin external preparations such as emulsions, creams, lotions, packs, cleansers, foundations, ointments, and dispersions have been used to prevent the formation of lipid peroxide and prevent skin irritation, blackening, and aging. Various medicinal ingredients have been added to these for the purpose of doing so. In recent years, as one of the causes of skin aging, the adverse effect of active oxygen on the living body has been cited. Active oxygen includes superoxide, singlet oxygen,
Hydroxy radicals, hydrogen peroxide, etc. are known to produce lipid peroxides and damage nuclei, proteins, and enzymes. There is. In addition, in terms of quantity, at least the accumulation of damage caused by active oxygen lowers the biological function, which is a cause of the so-called aging phenomenon. For this reason, various active oxygen removers have been conventionally developed.

[0003]

However, there is a demand for the development of a highly effective active oxygen scavenger for the purpose of defense of the living body and prevention of aging. It must be sufficiently satisfactory from the viewpoint of safety as well as effect. An object of the present invention is to provide a skin external preparation that can sufficiently exert the medicinal effects of an active oxygen removing agent, has an excellent active oxygen removing effect, and is safe and suitable even when applied to a biological system.

[0004]

Means for Solving the Problems The present inventors have improved the efficacy of a medicinal component incorporated in an external preparation for the purpose of preventing the formation of lipid peroxide and the inflammation, darkening and aging of the skin. As a result of diligent studies, the present inventors have found that the combination of an acerola extract and an active oxygen removing agent can sufficiently exert the active oxygen removing effect inherent in the active oxygen removing agent, and completed the present invention. That is, the present invention
An external preparation for skin containing (A) an acerola extract and (B) an active oxygen remover.

[0005]

BEST MODE FOR CARRYING OUT THE INVENTION The acerola extract, which is the component (A) of the external preparation for skin of the present invention, comprises Malpighia.
Acerola (Acerola, scientific name Malpighia emar)
ginata DC; Acerola's scientific name differs in writing in papers and the like depending on the age, region, and researchers. Previously Malpig
hia punicifolia L. and Malpighia glabra L. are confused and used as acerola scientific names.
"TROPI" edited by Steven Nagy et al. In 1980
CAL AND SUBTROPICAL FRUITS "
hia emarginata DC is most suitable. ) The fruit is extracted using an extraction solvent. The extraction treatment is not particularly limited, but the extraction is carried out at a low temperature or at room temperature or with a suitable solvent.

Examples of the above-mentioned extraction solvent include one or more of water; lower monohydric alcohols such as methyl alcohol and ethyl alcohol; and liquid polyhydric alcohols such as glycerin, propylene glycol and 1,3-butylene glycol. Can be used. As an example of a preferable extraction method, after performing extraction at a low temperature using purified water, filtration is performed, and 1,3-butylene glycol is further mixed to a concentration of 20 to 70% (W / W). And a method of performing filtration again.

The amount (content) of the acerola extract in the external preparation for skin of the present invention is preferably 0.00005 to 5% by weight as dry solid content (hereinafter, "% by weight" is simply indicated by "%"). And more preferably 0.0005 to
1%. If the amount (content) of this acerola extract is less than 0.00005%, a sufficient effect may not be obtained, and even if it exceeds 5%, the effect is further increased. Absent.

The active oxygen remover which is the component (B) of the external preparation for skin of the present invention includes carotenoids such as superoxide dismutase (SOD), mannitol, beta-carotene, astaxanthin and lutein, and animals and plants containing these. Extract, hydroquinone and its derivatives and salts thereof, bilirubin, cholesterol, tryptophan, histidine, quercetin, quercitrin, catechin and its derivatives, rutin and its derivatives, taurine, thiotaurine, soybean and egg-derived phospholipids, eggshell membrane extraction , Placenta extract, gallic acid and its derivatives, stevia, glabridine, glabrene, liquiritin, isoliquiritin, and liquorice extract containing them, yeast extract, ougon extract, seaweed extract, tolmentilla extract , Arhat extract, ginkgo extract, ganoderma extract, grape seed extract, calyx extract, green tea, black tea, tea extract such as oolong tea, peonies extract, gentian extract, hawthorn extract, rosemary extract , Mocca extract, saxifrage extract, yasajitsu extract, gennoshoko extract, red pepper extract, melissa extract, parsley extract, dicoppi extract, retinol and its derivatives (retinol palmitate, retinol acetate, etc.), retinal and its Derivatives, vitamin A such as dehydroretinal; thiamines (thiamine hydrochloride, thiamine sulfate, etc.), riboflavins (riboflavin, riboflavin acetate, etc.), pyridoxines (pyridoxine hydrochloride, pyridoxine dioctanoate, etc.), flavin adenine nucleotides , Cyanocobalami , Folates,
Vitamin B such as nicotinic acid (nicotinamide, benzyl nicotinate), choline; vitamin C such as ascorbic acid and derivatives thereof; vitamin D such as ergocalciferol, cholecalciferol, dihydroxystanal; tocopherol And its derivatives (dl
-Α (β, γ) -tocopherol, dl-α-tocopherol acetate, dl-α-tocopherol nicotinate,
Linoleic acid-dl-α-tocopherol, succinic acid dl
-Α-tocopherol) and vitamin Es such as ubiquinones. One or more of these active oxygen removing agents are appropriately selected and blended.

The above ascorbic acid and its derivatives are
L-ascorbic acid, L-ascorbyl palmitate,
L-ascorbyl dipalmitate, L-isopalmitate
-Ascorbyl, L-ascorbyl diisopalmitate, L-ascorbyl tetraisopalmitate, L-ascorbyl stearate, L-ascorbyl distearate, L-ascorbyl isostearate, L-ascorbyl diisostearate, L-ascorbyl myristate, di-ascorbyl L-ascorbyl myristate, L-ascorbyl isomyristate, L-ascorbyl diisomyristate, L-ascorbyl oleate, L-dioleic acid
-Ascorbyl, L-ascorbyl 2-ethylhexanoate, sodium L-ascorbate,
Potassium L-ascorbate, magnesium L-ascorbate, calcium L-ascorbate, aluminum L-ascorbate, sodium L-ascorbate, sodium L-ascorbate Potassium, magnesium L-ascorbate sulfate, calcium L-ascorbate sulfate, L-
Aluminum ascorbate sulfate, sodium L-ascorbate, potassium L-ascorbate, L
-Magnesium ascorbate, calcium L-ascorbate, aluminum L-ascorbate and the like.

Among these active oxygen scavengers, particularly preferred are vitamin C and its derivatives and salts thereof, carotenoids such as superoxide dismutase, mannitol, beta-carotene and astaxanthin, rutin and its derivatives, glabridine, Grabrene, liquiritin, isoliquiritin, and liquorice extract, ginkgo extract, grape seed extract, calyx extract, yasadtsu extract, zikkopi extract, and placenta extract containing them.

The amount (content) of the active oxygen remover in the external preparation for skin of the present invention is preferably 0.00001.
-10%, more preferably 0.0001-5%.
When a plant extract or the like is used as it is, it is converted to a dry solid content. If the active oxygen remover is within this range, when combined with the acerola extract, it does not affect the acerola extract in the external preparation for skin, and has good stability over time and excellent skin aging. An effect of preventing and improving skin roughness can be obtained. That is, the active oxygen remover is affected by the acerola extract, and improves the effect of preventing lipid peroxidation due to the generation of active oxygen in the skin and inflammation, blackening, and aging of the skin. In addition, the active oxygen remover can be used alone or in combination of two or more.

The skin external preparation of the present invention is prepared by blending the essential components (A) and (B) with various types of bases known as ordinary skin external preparations according to a conventional method. be able to. Examples of the form of the skin external preparation are not particularly limited, for example, milky lotion, cream, lotion, pack,
It can be used as skin care cosmetics such as detergents, makeup cosmetics such as lipsticks, foundations, etc., cosmetics for the scalp, ointments, topical pharmaceuticals such as dispersions, etc. , Paste, mousse,
Gel, powder, solution, solubilizing, emulsifying, powder dispersing and multi-layered can be used.

In addition to the components (A) and (B), the external preparation for skin of the present invention usually contains cosmetics, quasi-drugs, and external medicines as long as the effects of the present invention are not impaired. Ingredients used in the formulation, i.e., water, oils, surfactants, metal soaps, gelling agents, powders, alcohols, water-soluble polymers, film-forming agents, resins, UV protection agents, clathrate compounds, antibacterial Agents, fragrances, deodorants, salts, pH regulators, cooling agents, animal / microbial extracts, plant extracts, blood circulation enhancers, astringents, antiseborrheic, whitening, anti-inflammatory, humectants, One or more of anti-inflammatory agents, keratolytic agents, enzymes, hormones, vitamins, and the like can be appropriately added.

[0014]

EXAMPLES Next, the present invention will be described in more detail with reference to Reference Examples, Test Examples and Examples, but the present invention is not limited thereto.

Reference Example 1 Production of acerola extract Acerola (Acerola, scientific name: Malpighia emarginat)
aDC) was added with purified water, extracted at low temperature for one day, and then filtered to obtain an acerola extract (dry solid content: 1.7%).

Reference Example 2 Manufacture of Japanese gourd extract 10 g of Japanese gougon (Scarabae root) is cut into small pieces, and 100 ml of absolute ethanol is added thereto.
Extracted for days and filtered to give a pentagon extract (dry solids 1.0%).

Reference Example 3 Production of bovine placenta extract 1 kg of bovine placenta of 3 to 4 months of pregnancy is frozen, thawed to remove impurities after washing, 5 l of purified water is added, extracted under reduced pressure and low temperature for 3 days, and filtered to extract placenta extract (3.5% dry solids).

Test Example 1 Superoxide removal activity measurement test The acerola extract and the active oxygen remover listed in Table 1 were used alone or as a mixture to prepare a sample. After dilution with water, the superoxide removal activity was measured by the following measurement method.

(Measurement method) A substrate solution [3.0] was added to 2.4 ml of 0.05 M sodium carbonate buffer (pH 10.2).
mM xanthine (dissolved in 0.05 M sodium carbonate buffer)] 0.1 ml, 3.0 mM EDTA 0.1
ml, 0.15% (w / v) bovine serum albumin.
1 ml, 0.1 ml of 0.75 mM nitro blue tetrazolium and 0.1 ml of each test sample were mixed,
For 10 minutes. Next, an enzyme solution [xanthine oxidase solution (about 0.04 units / m in purified water)
The reaction was started by adding 0.1 ml and the reaction was carried out at 25 ° C.
And then incubated with 6 mM CaCl ₂
The reaction is stopped by adding 0.1 ml. Then 560 nm
The absorbance (A) at is measured. As a control, absorbance (B) of a sample to which purified water was added instead of the test sample, and to each sample blank, 0.1 ml of 6 mM CaCl ₂ was added to stop the reaction, and then 0.1 ml of xanthine oxidase was added.
The absorbance (C) of the sample to which was added was measured, and the superoxide removal rate was calculated from the following equation. Table 1 shows the results.

[0020]

(Equation 1)

[0021]

[Table 1]

As is evident from the results in Table 1, the acerola extract alone had superoxide removing activity, but when used in combination with the SOD and pentagon extract, it exhibited a synergistic effect and exhibited an activity. It was shown to be very effective for oxygen removal.

Embodiment 1 FIG. Cream A cream (composition 1 of the present invention,
2 and Comparative products 1 to 4) were prepared, and their beautiful skin effect and skin aging prevention effect were examined. The results are also shown in Table 2.

[0024]

[Table 2]

(Production method) A. Components (1)-(7), (11) and (12) are mixed and heated to 70 ° C. B. Components (8) and (13) are mixed and heated to 70 ° C. C. Add B to A, mix, cool and cool (9) and (1).
0) was added and mixed uniformly to obtain a cream.

(Test Method) 25 per test cream
A panel consisting of 15 women aged 55 to 55
After washing the face for 12 weeks, an appropriate amount of the test cream was applied to the face. The skin and skin aging prevention effects of the application were evaluated according to the following criteria.

(Evaluation criteria) Beautifying effect: <Evaluation> <Contents> Effective The dullness of the skin became less noticeable. Slightly effective Skin dullness became less noticeable. Ineffective No change from before use.

Skin Aging Prevention Effect: <Evaluation> <Contents> Effective Skin peeling and gloss were improved. Slightly effective Skin glue, gloss slightly improved. Ineffective No change from before use.

As shown in the results in Table 2, the product of the present invention 1 (comprising an acerola extract and an active oxygen scavenger Melissa extract) and the product of the present invention 2 (acerola extract, an active oxygen scavenger Melissa extract and acetic acid- dl-α-tocopherol) cream is applied to the skin to prevent the occurrence of “dullness” on the skin, to make the skin beautiful, and to improve the skin shine and gloss and to prevent skin aging. It became clear to do.

Embodiment 2 Preparation Example of Lotion (Formulation) (%) (1) Glycerin 6.0 (2) 1,3-butylene glycol 5.5 (3) Polyoxyethylene (20EO) Sorbitan 1.5 Monolaurate ( 4) Ethyl alcohol 9.0 (5) Acerola extract * 1 10.0 (6) Mannitol * 2 0.5 (7) Preservative appropriate amount (8) Perfume appropriate amount (9) Purified water remaining amount * 1 Reference example 1 * 2 manufactured by Sigma

(Production method) A. Components (3), (4), (7) and (8) are mixed and dissolved. B. Components (1), (2), (5), (6) and (9) are mixed and dissolved. C. A and B were mixed and made uniform to obtain a lotion.

Embodiment 3 Preparation Example of Emulsion (Formulation) (%) (1) Polyoxyethylene (10EO) Sorbitan 1.0 Monostearate (2) Polyoxyethylene (60EO) Sorbitan 0.5 Tetraoleate (3) ) Glyceryl monostearate 1.0 (4) Stearic acid 0.5 (5) Behenyl alcohol 0.5 (6) Squalane 8.0 (7) Acerola extract * 1 3.0 (8) Astaxanthin * 2 0.02 (9) Preservative 0.1 (10) Carboxyvinyl polymer 0.1 (11) Sodium hydroxide 0.05 (12) Ethyl alcohol 5.0 (13) Remaining purified water (14) Perfume appropriate amount * 1 Reference example * 2 manufactured by Sigma

(Production method) A. The components (9) to (13) are mixed by heating and kept at 70 ° C. B. Components (1) to (6) and (8) are mixed by heating and kept at 70 ° C. C. Add A to B, mix and emulsify uniformly. D. After cooling C, (7) and (14) were added and mixed uniformly to obtain an emulsion.

Embodiment 4 Preparation example of ointment (Formulation) (%) (1) Stearic acid 18.0 (2) Cetanol 4.0 (3) Triethanolamine 2.0 (4) Glycerin 5.0 (5) Acerola extract * 12 0.0 (6) Licorice extract * 2 0.5 (7) Purified water balance * 1 Produced in Reference Example 1 * 2 Maruzen Pharmaceutical Co., Ltd.

(Production method) Heat and mix a part of components (3), (4) and (7),
Keep at ° C. B. Heat mix components (1) and (2) and maintain at 75 ° C. C. Add A slowly to B. D. C was cooled and dissolved in the rest of (7) while cooling (5), (6)
Was added to obtain an ointment.

Each of the lotion of Example 2, the lotion of Example 3, and the ointment of Example 4 has excellent stability over time, and when applied to the skin, the skin is improved in terms of radiance and luster, and dullness of the skin is improved. It prevented skin aging.

Example 5 Preparation Example of Cleaning Agent (Formulation) (%) (1) Stearic acid 10.0 (2) Palmitic acid 8.0 (3) Myristic acid 12.0 (4) Lauric acid 4.0 ( 5) Oleyl alcohol 1.5 (6) Purified lanolin 1.0 (7) Perfume appropriate amount (8) Preservative 0.1 (9) Potassium hydroxide 6.0 (10) Acerola extract * 1 0.5 (11) ) Oregon extract * 2 0.5 (12) Remaining purified water * 1 Manufactured in Reference Example 1 * 2 Manufactured in Reference Example 2

(Production method) Heat and mix components (9) and (12) and maintain at 70 ° C. B. Components (1) to (6) and (8) are mixed by heating and kept at 70 ° C. C. Add A to B and maintain at 70 ° C. for a while. After the saponification reaction is completed, cool to 50 ° C. and mix components (7), (10) and
(11) was added, and the mixture was cooled to obtain a washing agent. The cleansing agent of Example 5 was excellent in stability over time, and when applied to the skin, moisturized and excellent in moisturizing properties by applying to the skin, and prepared the texture of the skin, and gave a shine and a luster.

Embodiment 6 Preparation Example of Pack (Formulation) (%) (1) Polyvinyl alcohol 20.0 (2) Ethyl alcohol 20.0 (3) Glycerin 5.0 (4) Kaolin 6.0 (5) Acerola extract * 1 1. 0 (6) Saxifraga extract * 2 0.2 (7) Preservative appropriate amount (8) Fragrance 0.05 (9) Remaining purified water * 1 Produced in Reference Example 1 * 2 Produced by Ichimaru Falcos

(Production method) A. Mix components (1), (3), (4) and (9),
And stir. B. Mix components (2), (7) and (8). C. B is added to A, mixed and cooled (5),
(6) was uniformly dispersed to obtain a pack. The pack of Example 6 was excellent in stability over time, and by applying to the skin, improved skin abrasion and gloss, and prevented dull skin and aging of the skin.

Embodiment 7 FIG. Preparation method of lip balm A lip balm was prepared according to the following formulation and the following method. (Prescription) (%) (1) Microcrystalline wax 9.0 (3) Solid paraffin 8.0 (4) Vaseline 15.0 (5) Cetyl ethylhexanoate 15.0 (6) Liquid paraffin 8.0 (6) ) Castor oil remaining amount (7) Acerola extract * 1 0.02 (8) Beta-carotene * 2 0.01 (9) BHT * 3 0.002 (10) Perfume appropriate amount * 1 Produced in Reference Example 1 * 2 Wako Pure Chemicals * 3 Sigma

(Production method) A. Components (1) to (6) are heated and dissolved at 100 to 110 ° C. B. A is mixed with the components (7) to (10) at 90 ° C. with stirring. C. B was cooled and molded to obtain a lip balm. The lip balm of Example 7 was excellent in stability over time, feeling in use, and finish, and was applied to the lips to keep the lips smooth and prevent roughening.

Embodiment 8 FIG. Preparation method of powder foundation (Prescription) (%) (1) Mica 50.0 (2) Titanium oxide 15.0 (3) Nylon powder 5.0 (4) Remaining kaolin (5) Color pigment 3.0 (6) ) 2-Ethylhexyl paramethoxycinnamate 2.0 (7) Dimethylpolysiloxane 2.0 (8) Squalane 3.0 (9) Glyceryl trioctanoate 2.0 (10) Vaseline 1.0 (11) Acerola extract * 1 0.02 (12) Bovine placenta extract * 2 0.5 (13) BHA * 3 0.005 (14) Perfume appropriate amount * 1 Manufactured in Reference Example 1 * 2 Manufactured in Reference Example 3 * 3 Sigma

(Production Method) A. Mix components (1) to (5). B. Components obtained by heating and dissolving the components (6) to (14) are added, mixed and pulverized. C. B was filled in a metal plate and press-molded to obtain a powder foundation. The powder foundation of Example 8 has stability over time,
It was excellent in use feeling and finish and applied to the skin to suppress dullness and roughness of the skin and prevent aging of the skin.

[0045]

As described above, by combining the acerola extract with the active oxygen scavenger, the original effects of the active oxygen scavenger can be fully exhibited.
Therefore, the external preparation for skin of the present invention has an extremely high improvement and prevention effect against lipid peroxide generation, inflammation, blackening, aging and the like caused by active oxygen generation in the skin. Since the skin external preparation of the present invention can sufficiently exhibit the performance inherent in an active oxygen remover, it is extremely useful in cosmetics and medical treatment.

Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat II (Reference) A61P 39/06 A61K 31/00 639C A61K 35/78 35/78 CN (72) Inventor Yuki Hata Sakaemachi, Kita-ku, Tokyo 48-18 Inside Kose Research Center (72) Inventor Shizuka Uehara 48-18 Sakaemachi, Kita-ku, Tokyo Inside Kose Research Center (72) Inventor Ichiro Sasaki 48-18 Sakaemachi, Kita-ku, Tokyo (72) Inventor Kenichi Nagamine 2-5-1-203 Misumicho, Higashimurayama-shi, Tokyo (72) Inventor Takashi Kito 1-2-1-25-103 Namiki, Kawaguchi-shi, Saitama F-term ( Reference) 4C083 AA071 AA082 AA111 AA112 AB032 AB242 AB432 AB442 AC012 AC022 AC072 AC102 AC122 AC131 AC242 AC342 AC352 AC422 AC442 AC471 AC472 AC491 AC542 AC581 AC791 AC841 AD072 AD092 AD112 AD152 AD391 AD411 AD471 AD491 AD512 AD571 AD621 AD622 CC63 CC07 CC12 CC13 CC23 DD17 DD23 DD31 EE12 FF05 4C088 AA02 AA06 AA12 AB02 AB12 AB19 AB32 AB38 AB40 AB45 AB51 AB55 AB56 AB60 AB66 AB67 BA08 CA06 CA08 MA08 MA11 MA63 NA07 ZA89

Claims (3)

[Claims] 1. An external preparation for skin comprising (A) an acerola extract and (B) an active oxygen remover. 2. An active oxygen scavenger comprising superoxide dismutase, mannitol, carotenoids and animal and plant extracts containing them, hydroquinone and its derivatives and salts thereof, bilirubin, cholesterol,
Tryptophan, histidine, quercetin, quercitrin, catechin and its derivatives, rutin and its derivatives, taurine, thiotaurine, soybean and egg-derived phospholipids, eggshell membrane extract, placenta extract, gallic acid and its derivatives, stevia extract, Gravlidine, glabrene, liquiritin, isoliquiritin and liquorice extract containing them, yeast extract, seaweed extract, seaweed extract, tormentilla extract, arhat extract, ginkgo extract, ganoderma extract, grape seed extract, Citrus extract, tea extract, peony extract, gentian extract,
Hawthorn extract, rosemary extract, mocca extract,
Saxifraga extract, Jasage extract, Geno ginger extract, Persimmon extract, Melissa extract, Parsley extract, Dicopi extract, vitamins A and their derivatives and their salts, vitamins B and their derivatives and their Salts, vitamins C and derivatives thereof, salts thereof, vitamins D and derivatives thereof, salts thereof, vitamins E and derivatives thereof, salts thereof, glutathione and derivatives thereof and salts thereof, dibutylhydroxytoluene and butyl 3. The external preparation for skin according to claim 1, which is selected from hydroxyanisole. 3. The composition according to claim 1, wherein the amount of the acerola extract is 0.00005 to 5% by weight as dry solids, and the amount of the active oxygen remover is 0.00001 to 10% by weight. External preparation for skin.