JP2011063513A - Anti-aging agent and external preparation for skin - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an external preparation for the skin excellent in anti-aging effect. <P>SOLUTION: The external preparation for the skin comprising vitamin C or a derivative thereof and an extract of Rosa rugosa Thunb. and/or Isodon japonicus is found to be excellent in anti-aging effect. The present invention is completed by further consideration. <P>COPYRIGHT: (C)2011,JPO&INPIT

Description

    The present invention relates to an anti-aging agent and an external preparation for skin, characterized by containing vitamin C or a derivative thereof, and an extract of Hermanus (Rosa rugosa Thunb.) And / or Toki Koshi (Isodon japonicus).

    Conventionally, as factors of skin symptoms such as aging, diseases, stress, wrinkles due to ultraviolet rays, blemishes, reduced skin elasticity, dryness, cellular function decline, melanin production and pigmentation due to ultraviolet rays, decrease and degeneration of dermal matrix components, ultraviolet rays Oxidative damage of cells due to the above. In order to prevent and ameliorate such skin symptoms, various active ingredients have been searched and formulated. In particular, naturally-derived components are known to have various pharmacological and cosmetic effects, and so far, applications of extracts such as plants and fungi to skin external preparations have been studied.

For example, in order to obtain an external preparation for skin having an action for preventing and improving skin aging, the essence of Ponkan (see Patent Document 1) and the extract of Ibukizasou are effective as components having an action of dermal fibroblast activation or proliferation. An anti-aging agent (see Patent Document 2) characterized by being blended as an ingredient, an anti-aging skin external preparation (see Patent Document 3) containing an extract of the genus Birch plant as an active ingredient are disclosed.
JP 2001-131045 A Japanese Patent No. 3544609 JP-A-9-136822

    Various anti-aging agents have been studied for external preparations for skin. However, the effect is not sufficient, and the development of better components has been demanded. Therefore, this invention is providing the outstanding skin external preparation which has an anti-aging effect.

    It has been found that an external preparation for skin containing vitamin C or a derivative thereof and Hermanus and / or a toad extract is excellent in anti-aging effect, and further studies have been made to complete the present invention.

    According to the present invention, there is provided a skin external preparation characterized by containing vitamin C or a derivative thereof, and a hermanus and / or a tocotic extract, and such a skin external preparation has a synergistic effect in an anti-aging effect. Is excellent.

    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 Hermanus used in the present invention is a plant belonging to the genus Rosaceae, which is a deciduous shrub that grows naturally in the sunny coastal sands of the Hokuriku and Tohoku regions from Sanin in Honshu.

    When using the genus in the present invention, there is no particular limitation on the use site, and each site such as leaves, stems, flowers, fruits, roots, and the whole plant can be used, but preferably flowers are used. Good.

    The toad used in the present invention is also known as Enmeso, a plant belonging to the genus Dermatophaceae, which is a perennial that grows on a slightly dry mountain grassland and roadside, and is distributed in Hokkaido, Honshu, Shikoku, Kyushu and Korea.

    When using a toad in the present invention, there are no particular restrictions on the use site, and each site such as leaves, stems, flowers, roots and the whole grass can be used, but preferably the above-ground part is used. .

    In the extraction, it is possible to use herbaceous or toaded raw, but considering the extraction efficiency, it is preferable to carry out extraction after processing such as shredding, drying, and pulverization.

    The extraction can be performed by immersing in an arbitrary extraction solvent for a predetermined time. The extraction solvent may be heated as necessary. In order to increase extraction efficiency, stirring or homogenization in an extraction solvent may be performed. The extraction temperature is suitably about 5 ° C. to the boiling point of the extraction solvent. The extraction time varies depending on the type of extraction solvent and the extraction temperature, but is suitably about 1 hour to 14 days.

    As an extraction solvent, in addition to water, lower alcohols such as methanol, ethanol, propanol and isopropanol; polyhydric alcohols such as 1,3-butylene glycol, propylene glycol, dipropylene glycol and glycerin; ethers such as ethyl ether and propyl ether Solvents such as esters such as butyl acetate and ethyl acetate; ketones such as acetone and ethyl methyl ketone can be used, and water and ethanol are preferable. These may be used alone or in combination of any two or more. Saline, phosphate buffer, phosphate buffered saline, and the like may be used. Furthermore, you may use 1 type, or 2 or more types of supercritical liquids and subcritical liquids, such as water, a carbon dioxide, ethylene, propylene, ethanol, methanol, ammonia.

    The extract of the above-mentioned Hermanus or toad used in the present invention can be used as it is, but it may be left standing for a certain period of time and aged, or the concentrated and dried product may be used as water or polar It can also be dissolved in a solvent and used again. 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 vitamin C or a derivative thereof together with a hermanus and / or a toads extract, it has a synergistically excellent anti-aging effect and can be used as an anti-aging agent and a skin external preparation.

    An anti-aging agent containing vitamin C or a derivative thereof, and a hermanus and / or a toco-kichi extract has a human epidermal keratinocyte activation action, and exhibits an excellent effect in preventing and improving aging symptoms.

    An external preparation for skin containing vitamin C or a derivative thereof, and a hermanus and / or a tocotic extract exhibits an anti-aging effect.

    Each of these agents is not limited at all in terms of its form and the presence or absence of other components, as long as it contains vitamin C or a derivative thereof, and a hermanus and / or a toads extract as active ingredients. As for the form, any form such as liquid, paste, gel, solid or powder can be selected according to its use and the like, vehicle (excipient), solvent, Or other general additives (an antioxidant, a coloring agent, a dispersing agent etc.) can be included arbitrarily.

    The dosage form of the external preparation for skin is arbitrary, and can be provided, for example, as a solubilization system such as lotion, a dispersion system such as calamine lotion, or an emulsification system such as cream or emulsion. Furthermore, it can also be provided in various dosage forms such as aerosol form, ointment or poultice filled with propellant.

    Specifically, various cosmetics such as emulsions, creams, lotions, lotions, packs, cosmetic liquids, cleaning agents or makeup cosmetics; liquids, ointments, powders, granules, aerosols, patches or poultices Various forms of cosmetics, quasi-drugs, or external medicines can be exemplified.

    In addition to vitamin C or its derivative and hermanus and / or toads extract, each of these agents includes pharmaceuticals, quasi-drugs, skin cosmetics, hair cosmetics and washings as required and necessary. Optional ingredients that are usually blended into the material such as water, oily ingredients, humectants, powders, pigments, emulsifiers, solubilizers, gelling agents, cleaning agents, UV absorbers, anti-inflammatory agents, thickeners, A pH adjuster, a chelating agent, a drug (medicinal component), a fragrance, a resin, a fungicide, a fungicide, an antioxidant, an alcohol, or the like can be appropriately blended. Furthermore, in the range which does not impair the effect of this invention, it is also possible to use together with other anti-aging agents, plants other than Hermanus or Hikikoshi or extracts thereof.

    The amount of vitamin C or a derivative thereof added to the external preparation for skin can be adjusted depending on the type and purpose, but from the viewpoint of effect and stability, the total amount is preferably 0.0001 in terms of solid content. It is -20.0 mass%, More preferably, it is 0.001-15.0 mass%, More preferably, it is 0.01-15.0 mass%.

    The blending amount of the Hermanus extract into the external preparation for skin can be adjusted depending on the type and purpose, but from the viewpoint of the effect and stability, the total amount is preferably 0.0001 to 20 in terms of solid content. It is 0.0 mass%, More preferably, it is 0.001-15.0 mass%, More preferably, it is 0.01-15.0 mass%.

    The blending amount of the extract of the toad skin into the external preparation for skin can be adjusted depending on the type and purpose, but from the viewpoint of the effect and stability, the total amount is preferably 0.0001 to 20 in terms of solid content. It is 0.0 mass%, More preferably, it is 0.001-15.0 mass%, More preferably, it is 0.01-15.0 mass%.

    In the following, a preparation example of a hermanus or a tocotic extract, a test method for evaluating the anti-aging effect using vitamin C or a derivative thereof in combination with a hermanus and / or a tocotic extract will be described in more detail. The target range is not limited by these.

[Extract 1]
Hermanus flowers were dried and pulverized, 20 times the sample weight of ethanol was added and extracted at room temperature with stirring for 3 hours, and then insolubles were removed by filtration. After concentration under reduced pressure, freeze-drying was performed to obtain Extract 1.

[Extract 2]
The above-ground part of the toad was dried and pulverized, 20% of the sample weight of 50% ethanol was added, extracted at room temperature with stirring for 3 hours, and then insolubles were removed by filtration. After concentration under reduced pressure, lyophilization was performed to obtain Extract 2.

    Each effect was evaluated using the said extract. Note that * and ** described in each evaluation result indicate that the significance probability P value in the t-test is less than 5% (P <0.05), and less than 1% significance (P <0.01). ) Is represented by **.

[Example 1]
<Evaluation of human epidermal keratinocyte activation effect>
Human epidermal keratinocytes HaCaT were seeded in a 96-well microplate so as to be 2.0 × 10 ⁴ cells per well. Dulbecco's modified Eagle medium (DMEM) supplemented with 5% by weight fetal bovine serum (FBS) was used as the seeding medium. After 24 hours, the medium was replaced with a culture medium in which the sample was added to each concentration shown in Table 1 in a 5% by mass FBS-added DMEM medium, and further cultured for 24 hours. Next, the MTT reagent adjusted with the culture medium so that it might be set to 100 microgram / mL was added to the cell except the supernatant, and it culture | cultivated for about 2 hours. Finally, formazan produced in 2-propanol was extracted and the absorbance at 550 nm was measured. At the same time, the absorbance at 650 nm was measured as turbidity, and the cell activation effect was evaluated using the difference between the two measured values.
The evaluation results are shown in Tables 1 to 3 as relative values when the cell activation effect in the control with no sample added is taken as 100.

    Evaluation results of human keratinocyte activating effect of ascorbic acid / Hananus extract

    From the results shown in Table 1, an excellent anti-aging effect was recognized in the external preparation for skin using both ascorbic acid and a hermanus extract.

    Evaluation results of human epidermis keratinocyte activation by ascorbic acid and abalone extract

    From the results shown in Table 2, an excellent anti-aging effect was recognized for the external preparation for skin using a combination of ascorbic acid and a toad extract.

    Evaluation results of human keratinocyte activating effect of ascorbic acid, hermanus extract, and toad wolfberry extract

    From the results shown in Table 3, the external preparation for skin using the ascorbic acid / Hananus extract / hikokoshi extract in combination was synergistically excellent in anti-aging effect.

    Then, the formulation example of the skin external preparation which mix | blended ascorbic acid or its derivative (s) and the extract 1 and / or the extract 2 obtained by the said preparation method is shown.

[Example 2]
Emulsion (1) Squalane 10.0 (mass%)
(2) Methylphenylpolysiloxane 4.0
(3) Hydrogenated palm kernel oil 0.5
(4) Hydrogenated soybean phospholipid 0.1
(5) Polyoxyethylene monostearate
Sorbitan (20E.O.) 1.3
(6) Sorbitan monostearate 1.0
(7) Glycerin 4.0
(8) Methyl paraoxybenzoate 0.1
(9) Carboxyvinyl polymer 0.15
(10) Remainder 100 (11) Ascorbic acid 0.043
(12) Extract 1 0.043
(13) Extract 2 0.043
(14) Arginine (1% by mass aqueous solution) 20.0
Production method: The oil phase components (1) to (6) are heated and dissolved at 80 ° C. On the other hand, the aqueous phase components (7) to (11) are dissolved by heating at 80 ° C. The oil phase component is added to this while stirring and uniformly emulsified with a homogenizer. After cooling, (12) to (14) are sequentially added at 40 ° C. and mixed uniformly.

[Example 3]
Lotion (1) Ethanol 15.0 (mass%)
(2) Polyoxyethylene (40E.O.) hydrogenated castor oil 0.3
(3) Fragrance 0.1
(4) Purified water 100 (5) Citric acid 0.02
(6) Sodium citrate 0.1
(7) Glycerin 1.0
(8) Hydroxyethyl cellulose 0.1
(9) Ascorbic acid 0.043
(10) Extract 1 0.043
(11) Extract 2 0.043
Production method: (2) and (3) are dissolved in (1). Further, after sequentially adding (4) to (9), the mixture is sufficiently stirred, and (10) and (11) are added and mixed uniformly.

[Example 4]
Cream (1) Squalane 10.0 (mass%)
(2) Stearic acid 2.0
(3) Hydrogenated palm kernel oil 0.5
(4) Hydrogenated soybean phospholipid 0.1
(5) Cetanol 3.6
(6) Lipophilic glyceryl monostearate 2.0
(7) Glycerin 10.0
(8) Methyl paraoxybenzoate 0.1
(9) Arginine (20 mass% aqueous solution) 15.0
(10) Purified water 100 (11) Ascorbic acid 0.0625
(12) Carboxyvinyl polymer (1% by weight aqueous solution) 15.0
(13) Extract 1 0.0625
Production method: The oil phase components (1) to (6) are heated and dissolved at 80 ° C. On the other hand, the aqueous phase components (7) to (11) are dissolved by heating at 80 ° C. The oil phase component is added to this while stirring and uniformly emulsified with a homogenizer. Add (12), stir, cool and add (13) at 40 ° C. and mix uniformly.

[Example 5]
Essence (1) Purified water 100 balance (mass%)
(2) Glycerin 10.0
(3) Sucrose fatty acid ester 1.3
(4) Carboxyvinyl polymer (1% by weight aqueous solution) 17.5
(5) Sodium alginate (1% by weight aqueous solution) 15.0
(6) Polyglyceryl monolaurate 1.0
(7) Ascorbic acid 0.0625
(8) Macadamia nut oil fatty acid phytosteryl 3.0
(9) N-lauroyl-L-glutamic acid di (phytosteryl-2-octyldodecyl) 2.0
(10) Hardened palm oil 2.0
(11) Squalane (from olive) 1.0
(12) Behenyl alcohol 0.75
(13) Beeswax 1.0
(14) Jojoba oil 1.0
(15) 1,3-butylene glycol 10.0
(16) L-arginine (10% by mass aqueous solution) 2.0
(17) Extract 2 0.0625
Production method: The aqueous phase components (1) to (7) are mixed and dissolved by heating at 75 ° C. On the other hand, the oil phase components (8) to (14) are mixed and dissolved by heating at 75 ° C. Next, the oil phase component is added to the aqueous phase component and preliminary emulsification is performed, followed by uniform emulsification with a homomixer. After cooling, add (15) at 50 ° C and (16) and (17) at 40 ° C, and mix uniformly.

[Example 6]
Aqueous gel (1) Carboxyvinyl polymer 0.5 (mass%)
(2) Ascorbic acid 0.043
(3) Purified water 100 (4) Sodium hydroxide (10% by mass aqueous solution) 0.5
(5) Ethanol 10.0
(6) Methyl paraoxybenzoate 0.1
(7) Fragrance 0.1
(8) Polyoxyethylene (60E.O.) hydrogenated castor oil 1.0
(9) Extract 1 0.043
(10) Extract 2 0.043
Production method: (1) and (2) are added to (3), and after stirring uniformly, (4) is added. After stirring uniformly, (6) previously dissolved in (5) is added. After stirring uniformly, (7) to (8) previously mixed are added, and finally (9) and (10) are added, and stirred and mixed uniformly.

[Example 7]
Cleansing fee (1) Squalane 81.0 (mass%)
(2) Polyoxyethylene glyceryl isostearate 15.0
(3) The balance which makes purified water 100 (4) Ascorbic acid 0.043
(5) Extract 1 0.043
(6) Extract 2 0.043
Manufacturing method: (1) and (2) are uniformly dissolved. (3) to (6) are sequentially added to this and mixed uniformly.

[Example 8]
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 purified water 100 (8) Ascorbic acid 0.043
(9) Extract 1 0.043
(10) Extract 2 0.043
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, add (9) and (10) at 40 ° C. and mix uniformly.

[Example 9]
Makeup base cream (1) Squalane 10.2 (mass%)
(2) Cetanol 2.0
(3) Glycerin tri-2-ethylhexanoate 2.5
(4) Lipophilic glyceryl monostearate 1.0
(5) Propylene glycol 11.0
(6) Sucrose fatty acid ester 1.3
(7) The balance which makes purified water 100 (8) Ascorbic acid 0.043
(9) Titanium oxide 1.0
(10) Bengala 0.1
(11) Yellow iron oxide 0.4
(12) Fragrance 0.1
(13) Extract 1 0.043
(14) Extract 2 0.043
Production method: The oil phase components (1) to (4) are mixed and dissolved by heating at 75 ° C. On the other hand, the aqueous phase components (5) to (8) are mixed and dissolved by heating at 75 ° C., and the pigments (9) to (11) are added thereto and uniformly dispersed with a homomixer. The oil phase component is added to the water phase component and emulsified with a homomixer. After cooling, the components (12) to (14) are added at 40 ° C. and mixed uniformly.

[Example 10]
Emulsion foundation (1) Methylpolysiloxane 2.0 (mass%)
(2) Squalane 5.0
(3) Octyldodecyl myristate 5.0
(4) Cetanol 1.0
(5) Polyoxyethylene (20E.O.)
Sorbitan monostearate 1.3
(6) Sorbitan monostearate 0.7
(7) 1,3-butylene glycol 8.0
(8) Xanthan gum 0.1
(9) Methyl paraoxybenzoate 0.1
(10) Remainder 100 (11) Ascorbic acid 0.043
(12) Titanium oxide 9.0
(13) Talc 7.4
(14) Bengala 0.5
(15) Yellow iron oxide 1.1
(16) Black iron oxide 0.1
(17) Fragrance 0.1
(18) Extract 1 0.043
(19) Extract 2 0.043
Production method: The oil phase components (1) to (6) are mixed and dissolved by heating at 75 ° C. On the other hand, the aqueous phase components (7) to (11) are mixed and dissolved by heating at 75 ° C., and the pigments (12) to (16) are added thereto and uniformly dispersed with a homomixer. Add oil phase ingredients and emulsify. After cooling, components (17) to (19) are sequentially added at 40 ° C. and mixed uniformly.

[Example 11]
Water-in-oil emollient cream (1) Liquid paraffin 34.0 (mass%)
(2) Microcrystalline wax 2.0
(3) Vaseline 5.0
(4) Diglycerin oleate 5.0
(5) Sodium chloride 1.3
(6) Potassium chloride 0.1
(7) Propylene glycol 3.0
(8) 1,3-butylene glycol 5.0
(9) Methyl paraoxybenzoate 0.1
(10) Ascorbic acid 0.043
(11) The balance of 100 purified water (12) Fragrance 0.1
(13) Extract 1 0.043
(14) Extract 2 0.043
Production method: Dissolve (5) and (6) in a part of (11) to 50 ° C., and gradually add to (4) heated to 50 ° C. with stirring. After mixing this, it disperse | distributes uniformly to (1)-(3) heated and melt | dissolved at 70 degreeC. (7) to (10) are added to the remainder of (11) heated and dissolved at 70 ° C. while stirring and emulsified with a homomixer. After cooling, add (12) to (14) at 40 ° C. and mix uniformly.

[Example 12]
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 0.043
(7) Extract 1 0.043
(8) Extract 2 0.043
(9) 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. Add (6) to (9) at 40 ° C. and mix uniformly.

[Example 13]
Bath agent (1) Fragrance 0.3 (mass%)
(2) Ascorbic acid 0.044
(3) Extract 1 0.043
(4) Extract 2 0.043
(5) Sodium bicarbonate 50.0
(6) Sodium sulfate 49.57
Production method: (1) to (6) are mixed uniformly.

[Example 14]
Hair wax (1) Stearic acid 3.0 (mass%)
(2) Microcrystalline wax 2.0
(3) Cetyl alcohol 3.0
(4) Highly polymerized methylpolysiloxane 2.0
(5) Methylpolysiloxane 5.0
(6) Poly (oxyethylene / oxypropylene)
Methylpolysiloxane copolymer 1.0
(7) Methyl paraoxybenzoate 0.1
(8) 1,3-butylene glycol 7.5
(9) Arginine 0.7
(10) Remainder 100 (11) Ascorbic acid 0.043
(12) Extract 1 0.043
(13) Extract 2 0.043
(14) Fragrance 0.1
Production method: The oil phase components (1) to (6) are mixed and heated and dissolved at 75 ° C. On the other hand, the aqueous phase components (7) to (11) are dissolved by heating at 75 ° C., the oil phase component is added, and the mixture is emulsified with a homomixer. After cooling, the components (12) to (14) are added at 40 ° C. and mixed uniformly.

[Example 15]
Hair artic (1) Ethanol 50.0 (mass%)
(2) Remainder 100 (3) Ascorbic acid 0.043
(4) Extract 1 0.043
(5) Extract 2 0.043
(6) Fragrance 0.1
Production method: Components (1) to (6) are mixed and homogenized.

    The skin external preparations shown in Examples 2 to 15 were compositions having an anti-aging effect.

    The composition containing the vitamin C of the present invention or a derivative thereof and the extract of “Hamanus” and / or “Hikikoshi” shows an excellent anti-aging effect and is useful as an anti-aging agent and a skin external preparation.

Claims (2)

  An anti-aging agent characterized by comprising vitamin C or a derivative thereof and an extract of Hermanus (Rosa rugosa Thunb.) And / or Toki Koshi (Isodon japonicus).   A topical skin preparation characterized by comprising vitamin C or a derivative thereof and an extract of hermanus (Rosa rugosa Thunb.) And / or a toad (Isodon japonicus).