KR102221262B1 - Composition for Improving Wrinkle Using an Extract of Geranium koreanum - Google Patents

Abstract

The present invention discloses a composition for improving skin wrinkles using a round heterozygous extract having an elastase inhibitory activity.

Description

Composition for Improving Wrinkle Using an Extract of Geranium koreanum}

The present invention relates to a composition for improving skin wrinkles using an extract of Geranium koreanum.

With the development of medical technology and the improvement of living standards, people's desire for beauty is strong, and the perception that appearance itself is a social competitiveness is increasing, so preference for skin whitening and skin wrinkle improvement is increasing, and the cosmetic market is expanding (J. .Korean Soc.Food Sci.Nutr., 42(3):355 (2013)).

The skin accounts for about 16% of the human body, and since it is in direct contact with the external environment, it plays an important role in protecting the human body from external harmful factors such as temperature, humidity, and ultraviolet rays. The skin is composed of the epidermis, the dermis, and the subcutaneous tissue under the keratin. The epidermis is a thin protective layer composed of keratinocytes, mainly composed of keratin, immune cells such as melanocytes and Langerhans cells, and Merkel's copuscles that produce and secrete melanin. It prevents external irritation and invasion of pathogens, regulates body temperature, and maintains moisture and lipid components.

The dermis is the connective tissue under the epidermis and is mostly composed of a network of macromolecules called extracellular matrix. This extracellular stroma is made from fibroblasts and consists of fibrous proteins such as collagen and elastin and polysaccharides such as hyaluronic acid.

With age or exposure to UV rays, the action of fibroblasts and the number of cells decrease, resulting in a decrease in the amount of collagen synthesis, and the actions of collagenase and elastase that decompose collagen increase, resulting in loss of skin moisture and skin flexibility. The elasticity decreases.

The most important environmental factor that causes skin aging is ultraviolet rays. When the skin is exposed to UV rays, harmful metabolism is activated, causing chain breakage and abnormal cross-linking of collagen and elastin (Barber et al., 1998; Brenneisen et al., 1998; Masaki et al., 1995; Yamamoto et al., 1995; Yamamoto , 2001; Yasui, Sakurai, 2000), skin tissue damage and skin wrinkles occur (Janssen et al., 1993; Park et al., 1999).

Therefore, a substance having an activity capable of inhibiting collagenase or elastase may have an effect of improving skin wrinkles (Photochem. acd Phptobiol. 2001. 74:283-287).

The present invention discloses the elastase inhibitory activity, etc. of the extracts of round dysentery.

It is an object of the present invention to provide a composition for improving skin wrinkles using a round alligator extract.

Other or specific objects of the present invention will be presented below.

The present invention was completed by confirming that the round shigella extract has a distinct elastase inhibitory activity, as confirmed in the following Examples and Experimental Examples.

In consideration of the foregoing, in one aspect, the present invention can be understood as a composition for improving skin wrinkles including an active ingredient of the round alligator extract.

In the present specification, the term "round heterogeneous grass extract" refers to the extraction target of round heterogeneous leaves, stems, above-ground parts, rhizomes, roots, underground parts, or a mixture thereof: water, lower alcohols having 1 to 4 carbon atoms (methanol, ethanol, butanol, etc.), methylene chloride , Ethylene, acetone, hexane, ether, chloroform, ethyl acetate, butyl acetate, N,N-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), 1,3-butylene glycol, propylene glycol, or a mixed solvent thereof It refers to an extract obtained by leaching using a supercritical extraction solvent such as carbon dioxide or pentane, or a fraction obtained by fractionating the extract, and the extraction method is cold sedimentation in consideration of the polarity of the active substance, the degree of extraction, and the degree of preservation. , Reflux, warming, ultrasonic radiation, supercritical extraction, etc. can be applied. In the case of a fractionated extract, a fraction obtained by suspending the extract in a specific solvent and mixing and policing with a solvent of a different polarity, the crude extract is adsorbed on a column filled with silica gel, etc., and then a hydrophobic solvent, a hydrophilic solvent, or a mixed solvent thereof It means including the fraction obtained as a mobile phase. In addition, the meaning of the extract includes a concentrated liquid extract or a solid extract from which the extraction solvent has been removed by a method such as freeze drying, vacuum drying, hot air drying, spray drying, or the like. Preferably, it means an extract obtained by using water, ethanol or a mixed solvent thereof as an extraction solvent, more preferably an extract obtained by using a mixed solvent of water and ethanol as an extraction solvent.

In addition, in the present specification, the term "active ingredient" refers to an ingredient that can exhibit a desired activity alone or exhibit activity with a carrier that is not itself active.

In addition, in the present specification, "improvement" is meant to include alleviation of symptoms of skin wrinkles, suppression of expression of such symptoms, delay of expression, and removal of expression.

In addition to the active ingredient, the composition of the present invention may be prepared by including a skin whitening component, a skin wrinkle improvement component, a UV protection component, a skin moisturizing component, and the like known in the art to reinforce and add skin-related activities. Specifically, skin whitening ingredients include arbutin, niacinamide, ascorbyl glucoside, alpha-bisabolol, and oil soluble licorice (Glycyrrhiza) extract, and skin wrinkle improvement ingredients include retinol and retinyl palmi. Tate, adenosine, polyethoxylated amide, etc. are mentioned, and as ultraviolet protection component, dromethrizol, dromethrizol trisiloxane, digaloyl trioleate, dimethicodiethylbenzalmalonate, diethhexylbutami And complexes such as dotriazone and pine bark extract, phosphatidylserine, fingerroot extract powder, and complex extracts such as red ginseng and cornus milk. In addition, as a moisturizing ingredient, AP collagen enzyme decomposition peptide, collactive collagen peptide, N-acetylglucosamine, konjac potato extract, complex extract such as dandelion, rice bran extract, corn germ extract, low molecular weight collagen peptide, ground grass extract powder, phosphatidylserine, hyaluronic acid, etc. Can be mentioned. For other skin whitening ingredients, anti-wrinkle ingredients, UV protection ingredients, and skin moisturizing ingredients, functional cosmetics code according to the Cosmetics Act (“Functional Cosmetics Standards and Test Methods” by the Ministry of Food and Drug Safety), health functional foods in accordance with the Health Functional Foods Act. Reference may be made to Gongjeon (Notification of the Ministry of Food and Drug Safety, "Standards and Specifications for Health Functional Foods.) These ingredients may be included in the composition of the present invention together with one or more of the active ingredients.

The composition of the present invention may contain the active ingredient in an arbitrary amount (effective amount) as long as it can exhibit the effect of improving skin wrinkles depending on the product type, product formulation, etc., and the usual effective amount is based on the total weight of the composition. When it will be determined within the range of 0.001% to 15% by weight. Herein, "effective amount" refers to intended medical/cosmetic effects, such as skin wrinkle improvement effect, when the composition of the present invention is administered to a mammal, preferably a human, to which the composition of the present invention is administered during the administration period according to the advice of a medical expert, etc. It refers to the amount of the active ingredient contained in the composition of the present invention. Such effective amounts can be determined empirically within the range of ordinary skill in the art.

The composition of the present invention can be grasped as a cosmetic composition in a specific aspect.

Even if the composition of the present invention is identified as a cosmetic composition, the cosmetic composition may be classified as a product for its use or legally, and specifically, may be a functional cosmetic having a use such as skin whitening, a non-functional general cosmetic, etc. . The product form can also take any product form, specifically solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing cleansing, oils, powder foundations, emulsion foundations, waxes. It can be formulated as a foundation, spray, or the like. In a specific product form, it may be a flexible lotion, a nutritional lotion, a nutritional cream, a massage cream, an essence, an eye cream, a cleansing cream, a cleansing foam, a cleansing water, a pack, a spray, or a powder formulation.

In addition to the active ingredient, the cosmetic composition of the present invention may include components commonly used in the cosmetic composition, such as stabilizers, solubilizers, surfactants, vitamins, conventional adjuvants such as pigments and perfumes, and carriers.

When the formulation of the present invention is a paste, cream or gel, animal oil, vegetable oil, wax, paraffin, starch, tracanth, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc, or zinc oxide may be used as carrier components. I can.

When the formulation of the present invention is a powder or spray, lactose, talc, silica, aluminum hydroxide, calcium silicate, or polyamide powder may be used as a carrier component. In particular, in the case of a spray, additionally chlorofluorohydrocarbon, propane / May contain propellants such as butane or dimethyl ether.

When the formulation of the present invention is a solution or emulsion, a solvent, a solubilizing agent or an emulsifying agent is used as a carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 ,3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol, fatty acid ester of sorbitan, and the like can be used.

When the formulation of the present invention is a suspension, as a carrier component, a liquid diluent such as water, ethanol or propylene glycol, an ethoxylated isostearyl alcohol, a suspending agent such as polyoxyethylene sorbitol ester, polyoxyethylene sorbitan ester, and crystallites Castle cellulose, aluminum metahydroxide, bentonite, agar, and the like can be used.

When the formulation of the present invention is a surfactant containing cleansing, as a carrier component, aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide Ether sulfates, alkylamidobetaines, fatty alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives or ethoxylated glycerol fatty acid esters may be used.

The cosmetic composition of the present invention can be prepared according to a method for preparing a cosmetic composition conventionally performed in the art, except for including the active ingredient that exhibits skin wrinkle improvement activity and the like.

The composition of the present invention can be recognized as a food composition in another specific aspect.

The food composition of the present invention can be prepared in any form, for example, beverages such as tea, juice, carbonated beverages, ion beverages, processed oils such as milk, yogurt, gums, rice cakes, Korean sweets, bread, snacks, noodles, etc. Foods, tablets, capsules, pills, granules, liquids, powders, flakes, pastes, syrups, gels, jelly, and health functional food preparations such as bars can be prepared. In addition, the food composition of the present invention can be classified as a product as long as it conforms to the enforcement regulations at the time of manufacture and distribution in terms of legal and functional classification. For example, it may be a health functional food in accordance with the Health Functional Food Act, or soy milk, fermented beverages, special purpose foods, etc. according to each food type according to the Food Sanitation Act's Food Code (Notice of the Ministry of Food and Drug Safety, Food Standards and Standards).

The food composition of the present invention may contain food additives in addition to the active ingredients. Food additives are generally understood as substances that are mixed or infiltrated by being added to food in manufacturing, processing, or preserving food. Since they are taken daily and long-term with food, their safety must be ensured. In the Food Additives Code according to the Food Sanitation Act (notified by the Ministry of Food and Drug Safety, standards and standards for food additives), food additives that are guaranteed to be safe are classified into chemical synthetic products, natural additives, and mixed preparations.

These food additives can be classified into sweeteners, flavoring agents, preservatives, emulsifiers, acidulants, thickeners, etc. in terms of functionality.

The sweetener may be used in an amount to give the food a suitable sweet taste, and may be natural or synthetic. Preferably, a natural sweetener is used, and examples of the natural sweetener include sugar sweeteners such as corn syrup solids, honey, sucrose, fructose, lactose, and maltose.

Flavoring agents can be used to enhance taste or aroma, and both natural and synthetic can be used. Preferably, it is the case of using a natural one. In the case of using natural ones, the purpose of nutrient enhancement can be combined in addition to flavor. As a natural flavoring agent, it may be obtained from apples, lemons, tangerines, grapes, strawberries, peaches, or the like, or from green tea leaves, roundtails, bamboo leaves, cinnamon, chrysanthemum leaves, jasmine, and the like. It is also possible to use those obtained from ginseng (red ginseng), bamboo shoots, aloe vera, and ginkgo. The natural flavoring agent may be a liquid concentrate or a solid extract. In some cases, synthetic flavoring agents may be used, and synthetic flavoring agents may include esters, alcohols, aldehydes, terpenes, and the like.

As a preservative, sodium calcium sorbate, sodium sorbate, potassium sorbate, calcium benzoate, sodium benzoate, potassium benzoate, EDTA (ethylenediaminetetraacetic acid), etc. can be used, and as an emulsifier, acacia gum, carboxymethylcellulose, xanthan gum, Pectin, etc. may be mentioned, and as the acidulant, arithmetic, malic acid, fumaric acid, adipic acid, phosphoric acid, gluconic acid, tartaric acid, ascorbic acid, acetic acid, phosphoric acid, and the like can be used. In addition to the purpose of enhancing taste, the acidulant may be added so that the food composition has an appropriate acidity for the purpose of inhibiting the growth of microorganisms.

As the thickening agent, a suspending agent, a settling agent, a gel-forming agent, a swelling agent, and the like may be used.

In addition to the food additives described above, the food composition of the present invention may include a physiologically active substance or minerals known in the art for the purpose of supplementing and reinforcing functionality and nutritional properties and ensuring stability as a food additive.

Examples of such bioactive substances include catechins contained in green tea, vitamins such as vitamin B1, vitamin C, vitamin E, and vitamin B12, tocopherol, dibenzoyl thiamine, and the like, and minerals include calcium preparations such as calcium citrate, magnesium stearate. Magnesium preparations such as, iron preparations such as iron citrate, chromium chloride, potassium iodide, selenium, germanium, vanadium, and zinc.

In the food composition of the present invention, the food additive described above may be included in an appropriate amount to achieve the purpose of addition according to the product type.

With respect to other food additives that may be included in the food composition of the present invention, reference may be made to the food code or the food additive code.

The composition of the present invention can be understood as a pharmaceutical composition in a specific embodiment.

The pharmaceutical composition of the present invention may be prepared in an oral dosage form or a parenteral dosage form according to an administration route by a conventional method known in the art, including a pharmaceutically acceptable carrier in addition to the active ingredient. Here, "pharmaceutically acceptable" means that the application (prescription) does not have toxicity beyond adaptable without inhibiting the activity of the active ingredient.

When the pharmaceutical composition of the present invention is prepared in an oral dosage form, powders, granules, tablets, pills, dragees, capsules, solutions, gels, syrups, suspensions, wafers according to a method known in the art together with a suitable carrier It can be prepared in a formulation such as. At this time, examples of suitable pharmaceutically acceptable carriers include sugars such as lactose, glucose, sucrose, dextrose, sorbitol, mannitol, and xylitol, starches such as corn starch, potato starch, wheat starch, cellulose, methylcellulose, ethylcellulose, Celluloses such as sodium carboxymethylcellulose and hydroxypropylmethylcellulose, polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, magnesium stearate, mineral oil, malt, gelatin, talc, polyol, vegetable Yu, etc. are mentioned. In the case of formulation activity, if necessary, it can be formulated including diluents and/or excipients such as fillers, extenders, binders, wetting agents, disintegrants, and surfactants.

When the pharmaceutical composition of the present invention is prepared in a parenteral dosage form, it may be formulated in the form of an injection, a transdermal administration, a nasal inhalation and a suppository according to a method known in the art together with a suitable carrier. When formulated as an injection, suitable carriers include sterile water, ethanol, polyols such as glycerol or propylene glycol, or mixtures thereof, preferably Ringer's solution, PBS (phosphate buffered saline) containing triethanol amine, or sterile water for injection. , An isotonic solution such as 5% dextrose may be used. When formulated into a transdermal dosage form, it may be formulated in the form of an ointment, cream, lotion, gel, external solution, pasta, liniment, air roll, and the like. In the case of nasal inhalants, it can be formulated in the form of an aerosol spray using suitable propellants such as dichlorofluoromethane, trichlorofluoromethane, dichlorotetrafluoroethane, and carbon dioxide, and the bases of the suppositories are witepsol and tween. (tween) 61, polyethylene glycols, cacao butter, laurin paper, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene stearates, sorbitan fatty acid esters, and the like can be used.

Regarding the formulation of a pharmaceutical composition, it is known in the art, and specifically, reference may be made to Remington's Pharmaceutical Sciences (19th ed., 1995). This document is considered as part of this specification.

The preferred dosage of the pharmaceutical composition of the present invention is in the range of 0.001 mg/kg to 10 g/kg per day, preferably 0.001 mg/kg to 1 g, depending on the patient's condition, weight, sex, age, patient severity, and route of administration. May be in the /kg range. Administration can be made once a day or divided into several times. Such dosage should not be construed as limiting the scope of the invention in any aspect.

As described above, according to the present invention, it is possible to provide a composition for improving skin wrinkles using a round alligator extract. The composition of the present invention may be commercialized as food or cosmetics.

Figure 1 is a result of the elastase inhibitory activity of the round yijilweed extract.

Hereinafter, the present invention will be described with reference to Examples and Experimental Examples. However, the scope of the present invention is not limited to these Examples and Experimental Examples.

<Example> Preparation of round dysentery extract

After adding 10 times the weight of 70% ethanol to the powder (extraction site: root), immersing it for 24 hours, extracting twice, and filtering, the filtrate was concentrated under reduced pressure and freeze-dried to obtain a solid extract of round allium grass. Was prepared.

<Experimental Example> Anti-wrinkle activity in skin wrinkles of the extract of round alligator-Elastase inhibitory activity test

After adding the example samples diluted by concentration in 50 mM Tris-Cl buffer (pH 8.5), 1 mg/ml N-succinyl-(Ala) ₃ -p-nitroanilide as the substrate was added to 50 mM Tris-Cl buffer (pH 8.5) I did. 0.6U/ml PPE (porcine pancreas elastase) was added, mixed well, reacted at 25°C, and absorbance was measured at 405 nm using an ELISA reader, and ursolic acid was used as a positive control.

While the results are shown in Fig. 1, the IC ₅₀ , which is a 50% inhibitory concentration of elastase, is shown in Table 1 below. The result is the result of repeated experiment 3 times for each concentration.

Elastase inhibitory activity (IC ₅₀ , μg/ml) division Elastase inhibition assay(㎍/ml)) Round Alliger Extract 243.5 ursolic acid 33.67

As shown in Fig. 1 and the table above, the sample clearly showed an elastase inhibitory activity, and the IC ₅₀ of the sample was 243.5 μg/ml. _{The IC 50} of ursolic acid, a positive control group, was 33.67 ㎍/ml.

Claims (4)

A composition for improving skin wrinkles, comprising an active ingredient of a mixed solvent extract of water and ethanol from the roots of round allodynia having an elastase inhibitory activity.
The method of claim 1,
The composition, characterized in that the water and ethanol mixed solvent is 70% ethanol.
The method according to claim 1 or 2,
The composition is a composition, characterized in that the food composition.
The method according to claim 1 or 2,
The composition is a composition, characterized in that the cosmetic composition.

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