JPH11246338A - Antiaging agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an antiaging agent which keeps the skin taut and elastic and can maintain the skin in a fresh state. SOLUTION: This antiaging agent contains a solvent extract from a gromwell (botanical name: Lithospermum erythrorhizon Siebold et Zuccarini). The extract from the gromwell possesses elastase inhibitory effect and prevents skin from aging. The extract from the gromwell on this invention is blended in an amount of 0.0005-20.0 wt.%, preferably 0.001-10.0 wt.%, based on the whole weight of the preparation for external use in the dry basis. When it is less than 0.0005 wt.%, the effect on this invention is not efficiently exerted and when it is more than 20.0 wt.%, it is not favorable due to the difficulty of pharmaceutical manufacturing. Further, even when the amount of more than 10.0 wt.% is blended, the very great improvement of the effect is not observed.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an anti-aging agent,
More specifically, the present invention relates to an anti-aging agent that has an elastase inhibitory action, maintains skin firmness and elasticity, and can maintain a youthful skin condition. The anti-aging agent of the present invention, including basic cosmetics, makeup cosmetics, hair cosmetics,
It can be suitably used as a bath agent and the like.

[0002]

2. Description of the Related Art Conventionally, the necessity of an anti-aging agent has been considered, but the mechanism and definition of aging have not been clarified. The measurement of the moisturizing state and the measurement of the elasticity of the skin have been performed, and the skin color has been visually observed for judgment. However, in recent years, research on aging has been advanced, and aging is an important factor as a cause of skin aging macroscopically, and furthermore, drying, oxidation, sunlight (ultraviolet rays)
The effects of aging have also been cited as direct factors related to skin aging. Specific phenomena of skin aging include:
It is known that collagen and elastin in skin dermis are reduced, mucopolysaccharides such as hyaluronic acid are reduced, and cells are damaged by ultraviolet rays. Of these, elastin forms crosslinks and contributes to the elasticity of tissues.However, elastin, which is an elastin-disrupting enzyme, is overexpressed by UV exposure and aging, and elastin is denatured and destroyed. However, it is thought to lead to a decrease in skin elasticity. Therefore, it is important to prevent the aging of the skin by suppressing the action of elastase and preventing denaturation / destruction of elastin which gives the skin elasticity and firmness. That is, the present invention provides an anti-aging agent that has the effect of suppressing the activity of elastase and restoring and maintaining the firmness and elasticity of the skin, thereby preventing skin aging and maintaining a youthful skin condition. The purpose is to:

[0003]

Means for Solving the Problems In view of the above problems, the present inventors examined elastase inhibitory activity of a wide variety of substances.
The present inventors have found that the solvent extract of ni) has excellent elastase inhibitory activity, and have completed the present invention.

[0004] That is, the present invention relates to Murasaki (scientific name: Lithos
permum erythrorhizon (Siebold et Zuccarini) as an active ingredient.

Hereinafter, the configuration of the present invention will be described in detail. The moraki (Borginaceae) plant used in the present invention is a murasaki (scientific name: Lithospermum erythrorhizon Sie)
The bold et Zuccarini) extract, which is also referred to as a sicon extract, is obtained by immersing or heating to reflux with an extraction solvent from the roots of the plant, followed by filtration and concentration. The extraction solvent used in the present invention may be any solvent that is generally used for extraction, and particularly methanol, ethanol or 1,3
-Alcohols such as butylene glycol, aqueous alcohols, and organic solvents such as acetone and ethyl acetate can be used alone or in combination.

The amount of the extract of purple in the present invention is 0.0005-20.
0% by weight, preferably 0.001 to 10.0% by weight. If the amount is less than 0.0005% by weight, the effects of the present invention cannot be sufficiently exerted. Further, even if the content is 10.0% by weight or more, the effect is not so much improved.

[0007] Since the purple extract used in the present invention exhibits excellent elastase inhibitory activity on human skin, the anti-aging agent containing the purple extract prevents aging of the skin, It can maintain youthful and healthy skin condition.

[0008] In addition to the above essential components, the anti-aging agent of the present invention includes components commonly used in external preparations for skin such as cosmetics and pharmaceuticals, for example, whitening agents, moisturizing agents, antioxidants, oily components,
An ultraviolet absorber, a surfactant, a thickener, an alcohol, a powder component, a coloring material, an aqueous component, water, various skin nutrients, and the like can be appropriately compounded as necessary.

In addition, sequestering agents such as disodium edetate, trisodium edetate, sodium citrate, sodium polyphosphate, sodium metaphosphate, gluconic acid, caffeine, tannin, verapamil, tranexamic acid and derivatives thereof, and licorice extract Products, glabridine, hot water extract of fire thorn fruit, various crude drugs, tocopherol acetate,
Drugs such as glycyrrhizic acid and its derivatives or salts thereof, vitamin C, magnesium ascorbate phosphate,
Other whitening agents such as ascorbic acid glucoside, arbutin, kojic acid, glucose, fructose, mannose,
Sugars such as sucrose and trehalose can also be appropriately blended.

The present invention can be widely applied to cosmetics and quasi-drugs applied to the outer skin, particularly preferably cosmetics, and its dosage form is also aqueous solution type, solubilizing type and emulsifying type. A wide range of dosage forms can be used, such as powder, oil-liquid, gel, ointment, aerosol, water-oil two-layer systems, water-oil-powder three-layer systems, and the like. In other words, if it is a basic cosmetic, face wash, lotion,
It can be widely applied to various forms such as emulsions, creams, gels, essences (packs, masks), etc. In addition, if it is makeup cosmetics,
As a toiletry product such as a foundation, it can be widely applied to forms such as body soap and soap. Furthermore, quasi-drugs can be widely applied to various ointments and the like. And in these dosage forms and forms,
The form that the anti-aging agent of the present invention can take is not limited.

[0011]

EXAMPLES Next, the anti-aging agent of the present invention will be described in more detail with reference to examples, but the present invention is not limited to these examples. The compounding amount is% by weight. Prior to the examples, a test method for the elastase inhibitory activity of the plant extract of the present invention and the results thereof will be described.

1. Preparation of sample 200 g of purple and 400 g of purified water and 60 g of ethanol
Add 0 g and heat dissolve at 50 ° C. After cooling, filtration and solvent extraction gave 2 g of an extract. This extract was dissolved in DMSO at 2%, the concentration was adjusted by diluting this solution, and the following experiment was performed using this.

2. Test Method for Elastase Inhibitory Activity and Results The elastase activity was measured as follows according to the method of Fujie et al. As a reaction buffer, 0.1 M
This was performed using HEPES, 0.5 M NaCl (pH 7.4). Methoxy-succinyl as an elastase substrate
-alanyl-alanyl-prolyl-valine-p-nitroanilide (BA
CHEMFEINCHEMIKALIEN AG)
It was dissolved in DMSO to 80 mM, dispensed in 20 μl aliquots, and stored frozen (−80 ° C.). At the time of use, it was used after being diluted to 8 mM with a reaction buffer. Elastase is elastase derived from human leukocytes (ELAST).
IN PRODUCT CO., INC.)
And dissolved in a reaction buffer to give a concentration of 10 μg / ml.
The resulting solution was dispensed in aliquots and stored frozen (-80 ° C). At the time of use, it was diluted to 5 μg / ml with a reaction buffer and used. 96-well plate (CORNING 25860)
In each case, 25 μl of 8 mM elastase substrate was dispensed, and 50 μl of the inhibitor was further added. Next, 25 μl of 5 μg / ml elastase was added on ice, and the mixture was immediately incubated at 37 ° C. for 20 minutes. afterwards,
The absorbance was measured at 415 nm. However, the inhibition rate is based on the following function.

[0014]

## EQU1 ## Inhibition rate (%) = 100− (in the presence of inhibitor / no inhibitor) × 100

The results are shown in FIG. In addition, as a reference example, a test substance similar to that described above was used for an in vivo substance exhibiting elastase inhibitory activity and fetal bovine serum (manufactured by GIBCO) and compared. FIG. 1 also shows the results.

Hereinafter, examples of compounding of various dosage forms of the anti-aging agent according to the present invention will be described.

Example 1 Cream (Formulation) Stearic acid 3.0% by weight Stearyl alcohol 5.0 Isopropyl myristate 18.0 Glycerin monostearate 3.0 Propylene glycol 10.0 Murasaki extract 0.01 Caustic potash 0.0 2 Sodium bisulfite 0.01 Preservatives Appropriate amount Fragrance Appropriate amount Ion-exchanged water Residue (Preparation method) Add propylene glycol, purple extract and caustic potash to ion-exchanged water, dissolve and heat to 70 ° C (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is gradually added to the water phase, and after the addition is completed, the temperature is maintained for a while to cause a reaction. Thereafter, the mixture is uniformly emulsified with a homomixer and cooled to 30 ° C. while stirring well.

Example 2 Cream (Formulation) Stearic acid 2.0% by weight Stearyl alcohol 7.0 Hydrogenated lanolin 3.0 Squalane 4.0 2-octyldodecyl alcohol 6.0 Polyoxyethylene (25 mol) cetyl alcohol ether 3.0 Glycerin monostearate 2.0 Propylene glycol 6.0 Murasaki extract 0.05 Sodium bisulfite 0.03 Ethyl paraben 0.3 Perfume Appropriate amount Ion-exchanged water Residue (Production method) Add propylene glycol to ion-exchanged water ,
Heat and maintain at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is added to the water phase, pre-emulsified, homogenized with a homomixer, and cooled to 30 ° C. with good stirring.

Example 3 Cream (Formulation) 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 0.0 Soap powder 0.1 Borax 0.2 Purple extract 0.1 Sodium bisulfite 0.03 Ethyl paraben 0.3 Perfume Appropriate amount Ion-exchange water residue (Preparation method) Add soap powder and borax to ion-exchange water and heat and dissolve And maintain at 70 ° C. (aqueous phase). The other components are mixed, melted by heating 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 4 Emulsion (Formulation) 2.5% by weight of stearic acid Cetyl alcohol 1.5 Vaseline 5.0 Liquid paraffin 10.0 Polyoxyethylene (10 mol) monooleate 2.0 Polyethylene glycol 1500 0 Triethanolamine 1.0 Carboxyvinyl polymer 0.05 (Product name: Carbopol 941, BFGoodrich Chemical company) Murasaki extract 3.0 Sodium bisulfite 0.01 Ethyl paraben 0.3 Perfume Appropriate amount Ion-exchanged water residue (Production method) ) The carboxyvinyl polymer is dissolved in a small amount of ion-exchanged water (phase A). Polyethylene glycol 1500 and triethanolamine are added to the remaining ion-exchanged water, dissolved by heating, and kept at 70 ° C. (aqueous phase). The other components are mixed, melted by heating and kept at 70 ° C. (oil phase). The oil phase is added to the water phase, pre-emulsification is performed, the phase A is added, and the mixture is uniformly emulsified with a homomixer.

Example 5 Emulsion (Formulation) Microcrystalline wax 1.0% by weight Beeswax 2.0 Lanolin 20.0 Liquid paraffin 10.0 Squalane 5.0 Sorbitan sesquioleate 4.0 Polyoxyethylene (20 mol) ) Sorbitan monooleate 1.0 Propylene glycol 7.0 Murasaki extract 10.0 Sodium bisulfite 0.01 Ethyl paraben 0.3 Perfume Appropriate amount Ion-exchanged water Residue (Production method) Add propylene glycol 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). While stirring the oil phase, the aqueous phase is gradually added thereto, and the mixture is uniformly emulsified with a homomixer. After emulsification, cool to 30 ° C with good stirring.

Example 6 Jelly (Formulation) Weight% 95% Ethyl alcohol 10.0 Dipropylene glycol 15.0 Polyoxyethylene (50 mol) Oleyl alcohol ether 2.0 Carboxyvinyl polymer 1.0 (Product name: Carbopol) 940, BFGoodrich Chemical company) Caustic soda 0.15 L-arginine 0.1 Purple extract 7.0 Sodium 2-hydroxy-4-methoxybenzophenonesulfonate 0.05 Ethylenediaminetetraacetate trisodium 2 water 0.05 Methylparaben 0 .2 Perfume Appropriate amount Ion-exchanged water Residue (Preparation method) Carbopol 940 was uniformly dissolved in ion-exchanged water, while Murasaki extract and polyoxyethylene (50 mol) oleyl alcohol ether were dissolved in 95% ethanol. To be added. Next, after adding other components, the mixture is neutralized with caustic soda and L-arginine to increase the viscosity.

Example 7 Essence (Formulation) Weight% (A phase) Ethyl alcohol (95%) 10.0 Polyoxyethylene (20 mol) octyldodecanol 1.0 Pantothenyl ethyl ether 0.1 Purple extract 1 0.5 methyl paraben 0.15 (phase B) potassium hydroxide 0.1 (phase C) glycerin 5.0 dipropylene glycol 10.0 sodium bisulfite 0.03 carboxyvinyl polymer 0.2 (trade name: Carbopol 940, BFGoodrich Chemical company) Purified water Residue (Preparation method) Dissolve A phase and C phase uniformly, and add A to C phase
Add phases and solubilize. Next, after adding the phase B, filling is performed.

Example 8 Pack Weight% (Formulation) (A phase) Dipropylene glycol 5.0 Polyoxyethylene (60 mol) hydrogenated castor oil 5.0 (B phase) Murasaki extract 0.01 Olive oil 5.0 Acetic acid Tocopherol 0.2 Ethylparaben 0.2 Perfume 0.2 (Phase C) Sodium bisulfite 0.03 Polyvinyl alcohol 13.0 (Saponification degree 90, Degree of polymerization 2,000) Ethanol 7.0 Purified water residue (Production method) A phase, B phase, and C phase are each dissolved uniformly,
Add phase B to phase and solubilize. Next, this is added to the C phase and then filled.

Example 9 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 Squalane 8 0.0 Isostearic acid 4.0 POE sorbitan monooleate 3.0 Isocetyl octoate 2.0 Murasaki extract 1.0 Preservatives Appropriate amount Fragrance Appropriate amount The oily components of squalane to isocetyl octanoate, murasaki extract, preservatives, and fragrances are added to the mixture, kneaded well, and the mixture is filled into a container and molded.

Example 10 Emulsion type foundation (cream type) (prescription) wt% (powder part) Titanium dioxide 10.3 Sericite 5.4 Kaolin 3.0 Yellow iron oxide 0.8 Bengala 0.3 Black iron oxide 0.2 (oil phase) Decamethylcyclopentasiloxane 11.5 Liquid paraffin 4.5 Polyoxyethylene-modified dimethylpolysiloxane 4.0 (aqueous phase) Purified water 50.0 1,3-butylene glycol 4.5 Murasaki Extract 1.5 Sorbitan sesquioleate 3.0 Preservatives Appropriate amount Flavors Appropriate amount (Preparation method) After heating and stirring the aqueous phase, a well-mixed and pulverized powder portion is added, followed by homomixer treatment. Further, the oil phase mixed by heating is added, and the mixture is treated with a homomixer. Then, a fragrance is added with stirring, and the mixture is cooled to room temperature.

Comparative Example 1 Comparative Example 1 was prepared by replacing the purple extract in the formulation of Example 10 with water. For each of the cosmetics obtained in Example 10 and Comparative Example 1, the following monitor test was performed. Table 1 shows the results.

Monitor test A healthy adult woman 1 randomly selected from the ages of 25 to 57 years
With 00 subjects as subjects, the improvement effect on wrinkles and fine wrinkles after using each cosmetic on the facial skin for one month every day was examined.

(A) Effect on wrinkles and fine wrinkles The condition of the skin was visually observed and evaluated based on the following evaluation criteria. (Evaluation criteria) A: Disappeared cleanly. B: Slightly less noticeable. C: No change. D: Increased a little. E: Increased.

(B) Effect on skin firmness and tarmi The condition of the skin was visually observed and evaluated based on the following evaluation criteria. (Evaluation criteria) A: Very improved. B: Improved. C: No change. D: It became somewhat noticeable. E: It became noticeable.

In the above monitor test, when using the cosmetics obtained in Example 10 and Comparative Example 1, no subject had any abnormal skin.

[0032]

[Table 1] ──────────────────────────────────── Wrinkles and small wrinkles Effect (person) Effect on person (person) ─────────────── Ｃ ABCD EABCDE ── ────────────────────────────────── Example 10 18 42 31 9 0 12 41 35 12 0 Comparative Example 1 0 31 35 20 14 0 21 61 4 14 ────────────────────────────────────

As is clear from the results shown in Table 1, when the cosmetic obtained in Example 10 was used, Comparative Example 1 was used.
It is recognized that wrinkles and fine wrinkles and skin firmness and skin thinning were improved as compared with the case where the cosmetic obtained in the above was used. This indicates that blending the purple extract as an active ingredient is a very useful formulation.

[0034]

As described above, according to the present invention,
By containing the purple extract as an active ingredient, an anti-aging agent exhibiting an excellent anti-aging effect can be provided.
That is, the purple extract exhibits elastase inhibitory activity, thereby suppressing the degeneration of elastin, which is an elastic fiber, and has elasticity, can maintain skin without wrinkles and sagging, and prevents skin aging, An anti-aging agent having an excellent cosmetic effect of maintaining a youthful skin condition is provided.

[Brief description of the drawings]

FIG. 1 is a diagram showing the elastase inhibitory activity of a purple extract in comparison with fetal calf serum.

Claims (3)

[Claims] 1. A purple (Borginaceae) murasaki (scientific name: Lithospermum erythrorhizon Siebold et Zucc)
arini) as an active ingredient. 2. The anti-aging agent according to claim 1, which is an elastase inhibitor. 3. A purple (Borginaceae) murasaki (scientific name: Lithospermum erythrorhizon Siebold et Zucc)
arini), which comprises a solvent extract of arini).