JP2011057578A - Peroxide lipid inhibitor and skin external preparation - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a peroxide lipid inhibitor and a skin external preparation which have a high effect, particularly an acne skin external preparation effective for preventing and improving acne since the effect of inhibiting the formation of peroxide lipid by vitamin C or a derivative thereof alone is insufficient and the effect on acne or the like caused by the formation of the peroxide lipid could not have been expected. <P>SOLUTION: An excellent peroxide lipid inhibitor, skin external preparation, and particularly acne skin external preparation can be obtained by using vitamin C or a derivative thereof in combination with sweet tea and/or a tea extract. By further using vitamin C or a derivative thereof and sweet tea and/or a tea extract in combination with a green tea extract, an excellent peroxide lipid inhibitor and skin external preparation, particularly, acne skin external preparation can be obtained. <P>COPYRIGHT: (C)2011,JPO&INPIT

Description

    The present invention relates to a lipid peroxide inhibitor and a skin external preparation, particularly an acne skin external preparation, characterized in that it contains vitamin C or a derivative thereof, strawberry tea and / or black tea extract, and further green tea extract.

    Skin is located in the outermost layer of the body and plays an important role in protecting the living body from the external environment and maintaining the homeostasis of the living body. Therefore, the skin is affected in some way by ultraviolet rays and other various oxidative stresses received in daily life. In particular, sebum is easily oxidized and lipid peroxide is generated. This peroxidation reaction causes various skin modulations (acne, pimples, rough skin, dry skin, wrinkles, spots, dullness, etc.).

    To prevent acne, prevent it from getting worse, and improve symptoms so far: 1. A component containing a component that suppresses sebum secretion: a sebum inhibitor characterized by containing hydroxyflutamide as an active component (see Patent Document 1). 2. A component containing a component that removes a horn plug that closes the pores: a stratum corneum peeling promoter / acne preventive and therapeutic agent containing steroid saponin as an active ingredient (see Patent Document 2). Ingredients that prevent acne-causing fungi and other skin resident bacteria from increasing by stimulating acne: Contains chitin oligosaccharides, chitin or partial degradation products thereof, or chitosan oligosaccharides, chitosan or partial decomposition products effective 3. Acne cosmetics characterized by being blended as an ingredient (see Patent Document 3). Contains an ingredient for suppressing acne inflammation: a topical skin preparation containing an anti-inflammatory agent selected from dipotassium glycyrrhizinate, stearyl glycyrrhetinate, β-glycyrrhetinic acid and glycyrrhetinyl stearate (see Patent Document 4), etc. .

    It is also known to use ascorbic acid as an active agent for treating seborrhea and related skin diseases, particularly acne (see Patent Document 5). However, inhibiting the production of lipid peroxides with vitamin C or its derivatives has been insufficient.

JP-A-6-157242 Japanese Patent No. 4173719 Japanese Patent No. 32533982 Japanese Patent No. 4011802 JP-A-9-110628

    The effect of suppressing the production of lipid peroxide by vitamin C or its derivative alone is insufficient, and an effect on acne and the like caused by the formation of lipid peroxide cannot be expected. This application made it the subject to provide the lipid peroxide production inhibitor and skin external preparation which have a high effect, especially the skin external preparation for acne effective in prevention and improvement of acne.

    By using a combination of vitamin C or a derivative thereof and strawberry tea and / or black tea extract, an excellent lipid peroxide production inhibitor and an external preparation for skin, in particular, an external preparation for skin for acne, and further combining a green tea extract By using it, the present inventors have found an excellent lipid peroxide production inhibitor and a skin external preparation, in particular, an acne skin external preparation, and have completed the present invention.

    According to the present invention, by using vitamin C or a derivative thereof in combination with strawberry tea and / or black tea extract, and further green tea extract, the production of lipid peroxide is suppressed in a synergistic manner. And an external preparation for skin, in particular, an external skin preparation for acne that is effective in preventing and improving acne.

FIG. 1 is a graph showing an evaluation result of a squalene peroxide production inhibitory action by porphyrin-derived singlet oxygen.

    Vitamin C or a derivative thereof used in the present invention is not particularly limited. For example, ascorbic acid monofatty acid esters such as L-ascorbic acid monostearate, L-ascorbic acid monopalmitate, L-ascorbic acid monooleate, L- Ascorbic acid monophosphate ester, L-ascorbic acid monoester derivative such as L-ascorbic acid-2-sulfate ester, L-ascorbic acid difatty acid ester derivative such as L-ascorbic acid distearate, L-ascorbic acid dipalmitate, L-ascorbic acid dioleate L-ascorbic acid tristearate, L-ascorbic acid tripalmitate, L-ascorbic acid trifatty acid ester derivatives such as L-ascorbic acid trioleate, L-ascorbic acid triphosphate ester, etc. Ascorbic acid triester derivatives and the like. Among these vitamin C or derivatives thereof, L-ascorbic acid or L-ascorbic acid phosphate ester and salts thereof are particularly preferable.

    The green tea extract used in the present invention is an extract obtained by extracting from tea leaves (Thea sinensis Linne) leaves (green tea) with water, ethanol solution, propylene glycol solution or glycerin solution. Preferably, it is an extract obtained by extraction with 50% ethanol.

    As the black tea extract used in the present invention, it is preferable to use an extract of an ethanol solution of tea made from the leaves of Assamcha (Thea sinensis Linne var. Assamica Pierre).

    It is preferable to use a component obtained by extracting the leaves of Rubus suavissimus in hot water for a while, taking out the leaves, drying them, and extracting the heated ones with hot water.

    Extracts of the above-mentioned solvents for green tea, black tea, and green tea used in the present invention can be used as they are, but they may be left to stand for a certain period of time and used for aging. Alternatively, it can be dissolved again in a polar solvent. Alternatively, it may be used after performing purification treatment such as decolorization, deodorization and desalting, and fractionation treatment by column chromatography or the like within a range not impairing these physiological functions. The said extract of plant and shellfish, its processed material, and the fractionation thing can also be freeze-dried after each processing and fractionation, and can also be melt | dissolved and used for a use solvent. It can also be used by encapsulating in vesicles such as liposomes or microcapsules.

    By using a combination of vitamin C or a derivative thereof, strawberry tea and / or black tea extract, and further green tea extract, it can be used as an excellent lipid peroxide production inhibitor.

    By using a combination of vitamin C or a derivative thereof, strawberry tea and / or black tea extract, and further green tea extract, it can be used as an excellent external preparation for skin.

    It can be used as a skin external preparation for acne that exerts an excellent effect on prevention and improvement of excellent acne by using vitamin C or a derivative thereof in combination with strawberry tea and / or black tea extract and further green tea extract. .

    By using a combination of vitamin C or a derivative thereof, strawberry tea and / or black tea extract, and further green tea extract, it has a squalene peroxide production-inhibiting action due to singlet oxygen generated by porphyrin, and has an excellent anti-acne effect Demonstrate.

    In addition to vitamin C or its derivatives and green tea, black tea, and strawberry tea extracts, acne compositions include pharmaceuticals, quasi drugs, skin cosmetics, hair cosmetics and Arbitrary ingredients that are usually blended in detergents, such as water, oily ingredients, moisturizers, powders, pigments, emulsifiers, solubilizers, gelling agents, detergents, UV absorbers, anti-inflammatory agents, thickeners , PH adjusters, chelating agents, drugs (medicinal ingredients), fragrances, resins, antibacterial and antifungal agents, antioxidants, alcohols, and the like can be appropriately blended. Furthermore, in the range which does not impair the effect of this invention, it can use together with another anti-acne agent or another plant extract.

    The amount of vitamin C or its derivative added to the external preparation for skin can be adjusted depending on the type and purpose, but from the viewpoint of effect and stability, vitamin C or its derivative is converted to solid content with respect to the total amount. , Preferably 0.00001 to 10.0% by mass, more preferably 0.0001 to 5.0% by mass, still more preferably 0.001 to 5.0% by mass, and still more preferably 0.001. It is 001-1.0 mass%.

    The amount of green tea extract added to the external preparation for skin can be adjusted depending on the type and purpose, but from the viewpoint of effectiveness and stability, green tea, black tea, and strawberry tea extract are converted to solid content with respect to the total amount, respectively. Preferably, it is 0.00001-10.0 mass%, More preferably, it is 0.0001-5.0 mass%, More preferably, it is 0.001-5.0 mass%, More preferably, it is 0 0.001 to 1.0% by mass.

    The amount of black tea extract added to the external preparation for skin can be adjusted according to the type and purpose, but from the viewpoint of effectiveness and stability, green tea, black tea, and strawberry tea extract are converted to solid content with respect to the total amount, respectively. Preferably, it is 0.00001-10.0 mass%, More preferably, it is 0.0001-5.0 mass%, More preferably, it is 0.001-5.0 mass%, More preferably, it is 0 0.001 to 1.0% by mass.

    The amount of strawberry tea extract added to the external preparation for skin can be adjusted depending on the type and purpose, but from the viewpoint of effect and stability, green tea, black tea, and strawberry tea extract are converted to solid content with respect to the total amount, respectively. Preferably, it is 0.00001-10.0 mass%, More preferably, it is 0.0001-5.0 mass%, More preferably, it is 0.001-5.0 mass%, More preferably, it is 0 0.001 to 1.0% by mass.

    Hereinafter, preparation examples of vitamin C or a derivative thereof, green tea, black tea, and strawberry tea extract, and a test method for evaluating the anti-acne effect will be described in more detail. However, the technical scope of the present invention is limited by these. Is not to be done.

<Vitamin C or its derivative>
L-(+)-ascorbic acid with a commercially available reagent level was used as vitamin C or a derivative thereof.

<Green tea extract>
It is an extract obtained by extracting with 50% ethanol from tea leaves (Thea sinensis Linne) leaves (green tea).

<Black tea extract>
A 1,3-butylene glycol solution is added to an ethanol solution of a product made from the leaves of Assamcha (Thea sinensis Linne var. Assamica Pierre) (tea).

<Sweet tea extract>
After immersing the leaves of Rubus suavissimus in boiling water for a while, the leaves were taken out, dried, and further heated and extracted with hot water. The components obtained were dissolved in 50% by mass of 1,3-butylene glycol solution. Is.

[Example 1]
<Evaluation of squalene peroxide production inhibitory action by porphyrin-derived singlet oxygen>
In 500 μL of a squalene solution (30 mM) prepared in a mixture of methanol: chloroform = 1: 1, 500 μL of a sample solution prepared to the concentration shown in Table 1 with any organic solvent, and in a mixture of methanol: chloroform = 1: 1 After adding 500 μL of the prepared hematoporphyrin solution (15 μM) and mixing well, UVA is irradiated at ² mW / cm ² for 10 minutes. (This is used as a reaction solution.) 40 μL of the reaction solution is sampled separately, and 5 μL of a saturated potassium iodide solution is added. Further, a mixed solution of chloroform: acetic acid: ethanol = 4: 4: 1 is added to a total volume of 5 mL. After reacting in the dark for 30 minutes, the absorbance at 359 nm was measured. When the absorbance after addition of the sample after correction with the absorbance without hematoporphyrin is (A) and the absorbance when the sample is added is (B), the inhibition rate of squalene peroxide production by porphyrin-derived singlet oxygen is Defined in
Inhibition rate (%) = {(A) − (B) / (A)} × 100

    The results are shown in Table 1 and FIG.

    From the results shown in Table 1, by using a combination of vitamin C or a derivative thereof, strawberry tea and / or black tea extract, and further green tea extract, squalene peroxide production-inhibiting action by porphyrin-derived singlet oxygen is shown and synergistic. It was found that it has an excellent anti-acne effect.

    Next, a prescription example is shown about the other external preparation for skin of this invention.

[Example 2]
Skin preparation for acne (lotion type)
(1) Ethanol 5.00 (mass%)
(2) Methyl paraoxybenzoate 0.02
(3) Concentrated glycerin 3.00
(4) 1,3-butylene glycol 1.00
(5) Ascorbic acid derivative 0.01
(6) Green tea extract 0.01
(7) Black tea extract 0.01
(8) Green tea extract 0.01
(9) Purified water 100.00 The remaining manufacturing method: (1), (2), (6), and (7) are uniformly dissolved to obtain an alcohol phase. The mixture is uniformly mixed with stirring in an aqueous phase obtained by adding (3) to (5) and (8) to (9) in advance.

[Example 3]
Acne skin external preparation (milky lotion type)
(1) Glyceryl tri-2-ethylhexanoate 8.00 (mass%)
(2) Self-emulsifying glyceryl monostearate 2.50
(3) Behenyl alcohol 0.50
(4) Concentrated glycerin 5.00
(5) Purified water 100.00 The remainder (6) Xanthan gum (1 wt% aqueous solution) 20.00
(7) Ascorbic acid derivative 0.01
(8) Green tea extract 0.01
(9) Black tea extract 0.01
(10) Green tea extract 0.01
(11) Ethanol 4.00
(12) Methyl paraoxybenzoate 0.15
Production method: The oil phases (1) to (3) and the aqueous phases (4) to (6) are dissolved by heating up to 80 ° C., respectively. Both phases are mixed and uniformly emulsified using a homomixer. After cooling to 45 ° C., the aqueous phase (7) and (10) and the alcohol phase combined with (8), (9), (11), and (12) are added and stirred uniformly.

[Example 4]
Skin preparation for acne (cream type)
(1) Squalane 10.00 (mass%)
(2) Stearic acid 2.00
(3) Hydrogenated palm kernel oil 0.50
(4) Hydrogenated soybean phospholipid 0.10
(5) Cetanol 3.60
(6) Lipophilic glyceryl monostearate 2.00
(7) Glycerin 10.00
(8) Methyl paraoxybenzoate 0.10
(9) 1% by weight carboxyvinyl polymer aqueous solution 15.00
(10) Purified water 100.00 The remainder (11) 10 wt% L-arginine aqueous solution 3.00
(12) Ascorbic acid derivative 0.01
(13) Green tea extract 0.01
(14) Black tea extract 0.01
(15) Green tea extract 0.01
Production method: The oil phase components (1) to (6) are dissolved by heating to 80 ° C. On the other hand, (7) to (10) are dissolved by heating to 80 ° C. To this is added the oil phase with stirring, then (11) is added, and the mixture is uniformly emulsified with a homogenizer, cooled to 45 ° C., (12) to (15) are added, and the mixture is stirred uniformly.

[Example 5]
Cleansing fee (1) Squalane 81.0 (mass%)
(2) Polyoxyethylene glyceryl isostearate 15.0
(3) Purified water 100 (4) Ascorbic acid derivative 0.01
(5) Green tea extract 0.01
(6) Black tea extract 0.01
(7) Green tea extract 0.01
Manufacturing method: (1) and (2) are uniformly dissolved. To this, (3) to (7) are sequentially added and mixed uniformly.

[Example 6]
Facial cleansing foam (1) Stearic acid 16.0 (mass%)
(2) Myristic acid 16.0
(3) Lipophilic glyceryl monostearate 2.0
(4) Glycerin 25.0
(5) Sodium hydroxide 7.5
(6) Palm oil fatty acid amidopropyl betaine 1.0
(7) The balance which makes 100 purified water (8) Ascorbic acid derivative 0.01
(9) Green tea extract 0.01
(10) Black tea extract 0.01
(11) Green tea extract 0.01
Production method: The oil phase components (1) to (4) are heated and dissolved at 80 ° C. On the other hand, the aqueous phase components (5) to (8) are heated and dissolved at 80 ° C., and mixed and stirred uniformly with the oil phase component. After cooling, (9) to (11) are sequentially added at 40 ° C. and mixed uniformly.

Pack (1) Remainder water (100%)
(2) Polyvinyl alcohol 12.0
(3) Ethanol 17.0
(4) Glycerin 9.0
(5) Polyethylene glycol (average molecular weight 1000) 2.0
(6) Ascorbic acid derivative 0.01
(7) Green tea extract 0.01
(8) Black tea extract 0.01
(9) Green tea extract 0.01
(10) Fragrance 0.1
Production method: (2) and (3) are mixed, heated to 80 ° C, and then dissolved in (1) heated to 80 ° C. After evenly dissolving, add (4) and (5) and cool with stirring. (6) to (10) are sequentially added at 40 ° C. and mixed uniformly.

    By using vitamin C or a derivative thereof in combination with strawberry tea and / or black tea extract, and further green tea extract, a lipid peroxide production inhibitor and an external preparation for skin that exhibit a synergistically excellent lipid peroxide inhibitory effect, It is particularly useful as a skin external preparation for acne that is effective in preventing and improving acne.

Claims (5)

  A lipid peroxide production inhibitor characterized by containing vitamin C or a derivative thereof and strawberry tea and / or black tea extract.   Furthermore, the lipid peroxide production inhibitor of Claim 1 containing a green tea extract.   An external preparation for skin characterized by containing vitamin C or a derivative thereof and strawberry tea and / or black tea extract.   Furthermore, the skin external preparation of Claim 1 containing a green tea extract.   The skin external preparation according to claim 3 or 4, which is for acne.

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