KR101127279B1 - A composition comprising novel black ginseng leaf and the extract thereof showing anti-oxidative activity prepared by novel process - Google Patents

Abstract

The present invention is a method for producing a neutrophil width through the process of repeating the drying and steaming at an appropriate temperature and time by washing the ginseng leaf more than 4 years old with an ultrasonic cleaner and using a high temperature and high pressure to shorten the time, The present invention relates to a composition containing the black trifoliate and its extract prepared from the preparation method, and the composition exhibits an excellent antioxidant effect. Thus, the composition is a skin external pharmaceutical composition for the prevention and treatment of skin diseases caused by oxidative stress and the skin caused by oxidative stress. It can be used as a cosmetic composition for the prevention and improvement of diseases.

Black leaf, mass production, augmentation width, antioxidant

Description

A composition comprising novel black ginseng leaf and the extract contents showing anti-oxidative activity prepared by novel process}

An object of the present invention is to reduce the time compared to the method for producing augmentation width from ginseng leaf and the method, containing black ginseng leaf and its extract as an active ingredient provided from a novel method for producing black ginseng leaf using high temperature and high pressure that can be mass-produced It is to provide an antioxidant composition.

Most of the studies on ginseng conducted so far have been conducted on ginseng roots, so most of the ginseng leaves have been discarded.

Accordingly, the present invention is about 2 to 3 times more saponin content than ginseng root (Yahara et al., Chem . Pharm ., Bull. , 24 (9) , p.2204, 1976) Manufacture of new black leaf which can be mass-produced with shorter time compared to this method and the method of augmentation width from ginseng leaf to develop into economical raw materials such as medicine, health functional food, food additives and cosmetics using leaf Provide a method.

To capture the $ 3.5 billion global ginseng market, Korean bio venture companies are working hard to develop new global ginseng-related materials worth $ 3.5 billion annually. So far, the only company that has standardized ginseng as a functional food and is making a profit in the global market is “Pharmaton,” a company owned by Boehringer Ingelheim, Switzerland. National research on ginseng and commercialization of the venture industry are in progress.

Korean red ginseng has a historical record of about 1,000 years ago (there is a record of red ginseng in Goryeo-do, written by the Chinese Song Dynasty). have. In general, the numerical objectives of herbal medicines are known as: 1) reducing side effects such as toxicity, 2) altering herbal properties and enhancing drug efficacy, 3) improving storage and storage, and 4) correcting taste and odor and color. In general, red ginseng undergoes a second ingredient conversion during an appropriate heat treatment process, thereby generating new active ingredients unique to red ginseng or fresh ginseng, and some active ingredients increase in content. As such, new ingredients that do not exist in ginseng are produced according to the processing method of ginseng, and new processed ginsengs having better effects on various physiological activities including anticancer activity can be developed compared to ginseng (Okamura N. et al. , Biol . Pharm. Bull. , 17 (2) , p.270, 1994).

In China, it develops a method of mass-producing Rg3, a ginseng saponin, which is rarely present in white ginseng and is present in red ginseng, and is used for anticancer treatment under the trade name 'Shenyi'.

In Korea, the representative product of functional ginseng is 'Seonsam' developed by bio venture company Ginseng Science in 1998.It was developed as Sesamsamjeong in 2001 and recognized in domestic health functional food market. It has been established as a leader in functional ginseng (Keum YS et al., Antioxidant and anti-tumor promoting activities of the methanol extract of heat-processed ginseng, Cancer Lett ., 150 (1) , pp. 41-48, 2000).

In addition, 'Hwangsam EX' co-developed by Korea Research Institute of Biotechnology and Bio-Venture Company, 'Vitgin', 'Naengsam Farming Ginseng Farming Co.' Recently, various types of processed ginseng are being developed, such as Biomax, which was developed jointly with UPI in the US, Six Plus of CJ, and Yellow Ginseng of Ildong Pharm.

In recent years, as a result of efforts to further increase the active ingredient content of ginseng, black ginseng using the principle of gujeunggupo, the most representative method of using water and fire, has been developed. (Korean Patent Laid-Open Publication No. 2003-0005089; Manufacturing method of black ginseng and black rice ginseng), The laboratory has applied for a standardized manufacturing method of black ginseng that can be shortened in time and mass production compared to this method (Korea) Patent Application No. 10-2006-0044066; Novel manufacturing method of black ginseng and composition containing the same).

     In this way, in the era of premium ginseng, the present inventors tried to overcome the limitation that research on ginseng and processed ginseng until now is mostly limited to roots. We have developed a method of manufacturing black ginseng leaves, which are processed ginseng leaves produced using the principle, and a standardized manufacturing method of black ginseng leaves using high temperature and high pressure, which is much shorter in time and capable of mass production. The present invention was completed by confirming that the red ginseng exhibited 4-5 times stronger antioxidant effect than the conventional red ginseng.

An object of the present invention is an antioxidant containing a black ginseng leaf and its extract provided from a method for preparing a neutrophil width using ginseng leaves and a novel method for producing black ginseng leaves using high temperature and high pressure, which is shorter in time and capable of mass production. It is to provide a composition for.

In order to achieve the above object, the present invention is effective in extracting the black and three leaf extracts obtained through a novel method for producing black leaves using the principle of augmentation through the process of drying, steaming, heating and drying ginseng leaf Provided is a skin external pharmaceutical composition for the prevention and treatment of skin diseases caused by oxidative stress, and a cosmetic composition for the prevention and improvement of skin diseases caused by oxidative stress.

In addition, the present invention contains black and three leaves extract as an active ingredient obtained through a novel method for producing black leaves using high temperature and high pressure to mass production through drying, steaming, heating and drying ginseng leaf Provided is a skin composition for preventing and treating skin diseases caused by oxidative stress and a cosmetic composition for preventing and improving skin diseases caused by oxidative stress.

Hereinafter, the present invention will be described in detail.

The black trilobite of the present invention can be prepared through the following process.

  After washing three to seven years old, preferably 4-6 years old, ginseng leaves of the present invention three times for 10 minutes with an ultrasonic cleaner, 12 to 36 hours at a temperature of 30 to 70 ° C, preferably 40 to 60 ° C, preferably The first drying step of drying for 20 to 28 hours; Primary steaming step of steaming for 1 to 5 hours, preferably 2 to 4 hours at a temperature of 60 to 120 ℃, preferably 85 to 105 ℃ except for the preheating time in a steamer; A secondary drying process step of drying at a temperature of 40 to 80 ° C., preferably 50 to 70 ° C. for 6 to 18 hours, preferably 9 to 15 hours; It is characterized in that it comprises a steaming and drying step of repeating the steaming step and the second drying step nine times, it is possible to produce a processed phosphorus leaf (hereinafter referred to as BGL-1) of 14% or less moisture.

In addition, 3 to 7 years old, preferably 4-6 years old ginseng leaf of the present invention after washing three times for 10 minutes with an ultrasonic cleaner, 12 to 36 hours at a temperature of 30 to 70 ℃, preferably 40 to 60 ℃, Preferably the first drying step of drying for 20 to 28 hours; A primary steaming step of steaming for 1 to 5 hours, preferably 2 to 4 hours at a temperature of 95 to 155 ° C, preferably 110 to 145 ° C under pressure; Characterized in that it comprises a secondary drying step of drying for 6 to 18 hours, preferably 9 to 15 hours at a temperature of 40 to 80 ℃, preferably 50 to 70 ℃, the moisture content within 14%, Processed ginseng leaves (hereinafter referred to as BGL-2) using high temperature and high pressure, which can be shortened in time and mass-produced, can be produced.

The method for obtaining the extract of BGL-1 prepared by the above method will be described in detail. After grinding the BGL-1 prepared by the above method, about 3 to 7 times, preferably 4 to 6 times, BGL-1 After adding a mass of water and leaving it to stand at room temperature for 3 to 7 hours, 0.5-2 L of methanol was added, followed by extraction under reflux three times for three hours. The extracted solution was cooled to room temperature, filtered, and methanol was removed using a vacuum condenser to obtain an extract of BGL-1 (hereinafter referred to as BGLE-1) prepared by the method of the present invention.

In addition, the method of obtaining the extract of the BGL-2 prepared by the above method in detail, after grinding the BGL-2 prepared by the above production method, about 3 to 7 times of the black trilobite 1, preferably 4 to 6 After adding twice the mass of water and leaving it to stand at room temperature for 3 to 7 hours, 0.5-2 L of methanol was added and the mixture was refluxed three times for three hours. The extracted solution was cooled to room temperature, filtered, and methanol was removed using a vacuum condenser to obtain an extract of BGL-2 (hereinafter, referred to as BGLE-2) prepared by the method of the present invention.

The black trifoliate or extract thereof prepared by the above manufacturing method is dried through a drying method common in the art such as shade drying or freeze drying, and then pulverized and powdered into fine particles, preferably a particle size of about 50 μm to 200 μm. It can be prepared into compositions such as pills, capsules, tablets, etc. using excipients or carriers well known in the art through the process of the conversion.

The black trilobite produced by the production method of the present invention can be used as a raw material for various preparations by grinding into fine powder, preferably a powder of about 50 ~ 200㎛ size using a herbal medicine grinder.

Black ginseng leaf prepared by the above method contains about 2-3 times more saponin content than ginseng root. Among these saponin components, Rg5 has anticancer effect, antidiabetic effect, etc. Since it exhibits various pharmacological activities such as antistress effect, hepatoprotective effect and antioxidant effect, the black trilobite of the present invention may exhibit various physiological activities as above.

Black ginseng leaf extract prepared by the production method of the present invention exhibits a strong antioxidant effect, it is characterized by a strong antioxidant effect compared to red ginseng and black ginseng extract.

Therefore, the present invention provides a skin external pharmaceutical composition for the prevention and treatment of skin diseases caused by oxidative stress containing the black trifoliate and its extract as an active ingredient prepared from the preparation method and the extraction method.

In another aspect, the present invention provides a cosmetic composition for the prevention and improvement of skin diseases caused by oxidative stress containing black trifoliate and its extract as an active ingredient prepared from the production method and extraction method.

Skin diseases caused by the oxidative stress include skin diseases such as skin aging, wrinkles, blemishes, freckles, dermatitis, acne.

The black trifoliate and its extract may be used in an amount of 0.001 to 90% by weight, preferably 0.01 to 10% by weight, based on the total weight of the skin external pharmaceutical composition or cosmetic composition.

The skin external pharmaceutical composition containing the black trifoliate and extracts thereof of the present invention is a skin external preparation having an antioxidant effect of cream, gel, patch, spray, ointment, warning agent, lotion agent, linen agent, pasta agent or cataplasmase agent. It may be prepared and used as a pharmaceutical composition in the form of external preparations for skin, but is not limited thereto.

Preferred dosages of the black trilobite and extracts thereof of the present invention vary depending on the condition and weight of the patient, the extent of the disease, the form of the drug, the route of administration and the duration, and may be appropriately selected by those skilled in the art. However, for the preferred effect, black ginseng and its extract of the present invention is preferably administered at 0.0001 to 100 mg / kg, preferably at 0.001 to 10 mg / kg. Administration may be administered once a day or may be divided several times. The dosage does not limit the scope of the invention in any aspect.

In addition, the black trifoliate of the present invention and extracts thereof may be used in a variety of cosmetics and face wash having an antioxidant effect.

 Products to which the composition can be added include, for example, cosmetics such as lotion, skin, lotion, nourishing lotion, nourishing cream, massage cream, essence, pack, etc., and cleansing, face wash, soap, treatment, essence, etc. have.

Cosmetics of the present invention comprises a composition selected from the group consisting of water-soluble vitamins, oil-soluble vitamins, polymer peptides, polymer polysaccharides, sphingolipids and seaweed extract.

The water-soluble vitamins may be any compound that can be incorporated into cosmetics, but preferably vitamin B1, vitamin B2, vitamin B6, pyridoxine, pyridoxine, vitamin B12, pantothenic acid, nicotinic acid, nicotinic acid amide, folic acid, vitamin C, vitamin H, and the like. Their salts (thiamine hydrochloride, sodium ascorbate salt, etc.) and derivatives (ascorbic acid-2-sodium phosphate salt, ascorbic acid-2-magnesium phosphate salt, etc.) may also be used in the water-soluble vitamins that can be used in the present invention. Included. The water-soluble vitamins can be obtained by conventional methods such as microbial transformation, purification from microorganism culture, enzyme or chemical synthesis.

The oil-soluble vitamin may be any compound that can be incorporated into cosmetics, but preferably vitamin A, carotene, vitamin D2, vitamin D3, vitamin E (d1-alpha tocopherol, d-alpha tocopherol, d-alpha tocopherol), and the like. And derivatives thereof (ascorbic palmitate, ascorbic stearate, ascorbic acid dipalmitate, dl-alpha tocopherol acetate, dl-alpha tocopherolvitamin E, dl-pantothenyl alcohol, D-pantothenyl alcohol, pantotenylethyl Ethers, etc.) are also included in the oil-soluble vitamins used in the present invention. Oil-soluble vitamins can be obtained by conventional methods such as microbial transformation, purification of microorganism culture, enzyme or chemical synthesis.

The polymer peptide may be any compound as long as it can be incorporated into cosmetics. Preferably, collagen, hydrolyzed collagen, gelatin, elastin, hydrolyzed elastin, keratin and the like can be given. Polymeric peptides can be purified and obtained by conventional methods such as purification from microbial cultures, enzymatic methods or chemical synthesis methods, or can be purified and used from natural products such as dermis and pig silk such as pigs and cattle.

The polymer polysaccharide may be any compound as long as it can be blended into cosmetics. Preferably, hydroxyethyl cellulose, xanthan gum, sodium hyaluronate, chondroitin sulfate or a salt thereof (sodium salt, etc.) may be mentioned. For example, chondroitin sulfate or its salt, etc. can be normally purified from a mammal or fish.

The sphingolipid may be any compound as long as it can be blended into cosmetics. Preferably, ceramide, phytosphingosine, sphingosaccharide lipid, etc. may be mentioned. Sphingo lipids can usually be purified from mammals, fish, shellfish, yeasts or plants by conventional methods or obtained by chemical synthesis.

The seaweed extract may be any compound as long as it can be blended into cosmetics. Preferably, the seaweed extract may include brown algae extract, red algae extract, green algae extract, and the like. Also, calginine, arginic acid, sodium arginate, Potassium arginate and the like are also included in the seaweed extract used in the present invention. Seaweed extract can be obtained by purification from seaweed by conventional methods.

The cosmetic of the present invention may be blended with other essential ingredients, if necessary, in combination with the essential ingredients.

Other components that may be added include fats and oils, moisturizers, emollients, surfactants, organic and inorganic pigments, organic powders, ultraviolet absorbers, preservatives, fungicides, antioxidants, plant extracts, pH adjusters, alcohols, pigments, flavorings, Blood circulation accelerators, cooling agents, restriction agents, purified water and the like.

Examples of the fat or oil component include ester fats, hydrocarbon fats, silicone fats, fluorine fats, animal fats, and vegetable fats and oils.

As ester fats and oils, glyceryl tri2-ethylhexanoate, cetyl 2-ethylhexanoate, isopropyl myristate, butyl mystinate, isopropyl palmitate, ethyl stearate, octyl palmitate, isocetyl isostearate, and stearic acid Butyl, ethyl linoleate, isopropyl linoleate, ethyl oleate, isocetyl acid isocetyl, isostyl acid isostearyl, isostaryl palmitate, octylate acid octyldodecyl, isostearic acid isetyl, diethyl sebacate, adipine Acid isopropyl, isoalkyl neopentane, tri (capryl, capric acid) glyceryl, trimethyl ethyl trimethylol propane, triisostearic acid trimethylol propane, tetra 2-ethylhexanoic penta erythritol Cetyl caprylate, lauric acid decyl, hexyl laurate, decyl myristin, myristin acid myristyl, myritic acid cetyl, stearyl stearate, decyl oleate, rininooleic acid , Isostearyl laurate, isotridecyl myristin, isocetyl palmitate, octyl stearate, isocetyl stearate, isodecate oleate, octylate decyl oleate, octyl dodecyl linoleate, isopropyl isopropyl acid, 2 -Cetostearyl ethylhexanoate, stearyl 2-ethylhexanoate, hexyl isostearate, ethylene glycol dioctanoate, ethylene glycol dioleate, propylene glycol dicapric acid, propylene glycol dicacapate, capric acid Propylene Glycol, Dipentane Neopentyl Glycol, Dioctanoate Neopentyl Glycol, Tricaprylic Acid Glyceryl, Triundecyl Glyceryl, Triisopalmitinate Glyceryl, Triisostearate Glyceryl, Neopentane Octyldodecyl Isostearyl octanoate, octyl isononate, hexyl decyl neodecanoate, octyl dodecyl neodecanoate, isocetyl isostearate, isostearyl isostearate, Sothete octylate, polyglycerol oleate, polyglycerine isostearate, triisocetyl citrate, triisoalkyl citrate, triisoctyl citrate, lauryl lactate, myritic lactate, octyl lactate, octyl lactate, tricitric acid Ethyl, acetyl triethyl citrate, acetyl tributyl citrate, trioctyl citrate, diisostearyl malic acid, 2-ethylhexyl hydroxystearate, di2-ethylhexyl succinate, diisobutyl adipicate, diisopropyl sebacinate, Dioctyl sebacate, cholesteryl stearate, cholesteryl isostearate, cholesteryl hydroxystearate, cholesteryl oleate, dihydrocholesteryl oleate, physteryl isostearate, phytic oleate, 12-Steloylhydroxystearate isocetyl, 12-Steloylhydroxystearate stearyl, 12-steal One hydroxy stearic acid and the like esters such as cetearyl source.

Hydrocarbon-based fats and oils, such as squalene, a liquid paraffin, alpha-olefin oligomer, isoparaffin, ceresin, paraffin, a liquid isoparaffin, polybutene, microcrystal wax, and a vaseline, etc. are mentioned as a hydrocarbon-type fats and oils.

Examples of the silicone-based oils and fats include polymethylsilicone, methylphenylsilicone, methylcyclopolysiloxane, octamethylpolysiloxane, decamethylpolysiloxane, dodecamethylcyclosiloxane, dimethylsiloxane, methylcetyloxysiloxane copolymer, dimethylsiloxane and methylsteoxysiloxane copolymer, and alkyl. Modified silicone oil, amino modified silicone oil and the like.

Examples of the fluorine-based oil include perfluoropolyether and the like.

Animal or vegetable oils include avocado oil, almond oil, olive oil, sesame oil, rice bran oil, soybean oil, soybean oil, corn oil, rapeseed oil, almond oil, palm kernel oil, palm oil, castor oil, sunflower oil, grape seed oil. , Cottonseed oil, Palm oil, Cucumber nut oil, Wheat germ oil, Rice germ oil, Shea butter, Walnut colostrum oil, Marker demia nut oil, Meadow home oil, Egg yolk oil, Uji, Horse oil, Mink oil, Orange rape oil, Jojoba oil And animal or plant fats and oils such as candeler wax, carnava wax, liquid lanolin and hardened castor oil.

Examples of the moisturizing agent include a water-soluble low molecular moisturizer, a fat-soluble molecular moisturizer, a water-soluble polymer, and a fat-soluble polymer.

Water-soluble low molecular humectants include serine, glutamine, sorbitol, mannitol, pyrrolidone-sodium carboxylate, glycerin, propylene glycol, 1,3-butylene glycol, ethylene glycol, polyethylene glycol B (polymerization degree n = 2 or more), polypropylene Glycol (polymerization degree n = 2 or more), polyglycerol B (polymerization degree n = 2 or more), lactic acid, lactic acid salt, etc. are mentioned.

Examples of the fat-soluble low molecular humectants include cholesterol and cholesterol esters.

Examples of the water-soluble polymer include carboxyvinyl polymer, polyasparaginate, tragacanth, xanthan gum, methyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, carboxymethyl cellulose, water soluble chitin, chitosan, and dextrin. Can be.

Examples of the fat-soluble polymers include polyvinylpyrrolidone-eicosene copolymers, polyvinylpyrrolidone-hexadecene copolymers, nitrocellulose, dextrin fatty acid esters, polymer silicones, and the like.

Examples of the emollient include long-chain acyl glutamic acid cholesteryl esters, hydroxy stearic acid cholesterol, 12-hydroxystearic acid, stearic acid, rosin acid, lanolin fatty acid cholesteryl esters, and the like.

As surfactant, nonionic surfactant, anionic surfactant, cationic surfactant, amphoteric surfactant, etc. are mentioned.

As the nonionic surfactant, self-emulsifying glycerin monostearate, propylene glycol fatty acid ester, glycerin fatty acid ester, polyglycerol fatty acid ester, sorbitan fatty acid ester, POE (polyoxyethylene) sorbitan fatty acid ester, POE sorbitan fatty acid ester, POE Glycerin fatty acid ester, POE alkyl ether, POE fatty acid ester, POE hardened castor oil, POE castor oil, POE / POP (polyoxyethylene / polyoxypropylene) copolymer, POE / POP alkyl ether, polyether modified silicone, lauric acid Alkanolamide, alkylamine oxide, hydrogenated soybean phospholipid, etc. are mentioned.

Anionic surfactants include fatty acid soaps, alpha-acyl sulfonates, alkyl sulfonates, alkyl allyl sulfonates, alkyl naphthalene sulfonates, alkyl sulfates, POE alkyl ether sulfates, alkylamide sulfates, alkyl phosphates, POE alkylphosphates, and alkylamides. Phosphates, alkyloylalkyltaurine salts, N-acylamino acid salts, POE alkyl ether carboxylate salts, alkyl sulfosuccinate salts, sodium alkyl sulfo acetates, acylated hydrolyzed collagen peptide salts, perfluoroalkyl phosphate esters, and the like. Can be.

As cationic surfactant, alkyl trimethylammonium chloride, stearyl trimethyl ammonium chloride, stearyl trimethyl ammonium chloride, cetostearyl trimethyl ammonium chloride, distearyl dimethyl ammonium chloride, stearyl dimethyl benzyl ammonium bromide, behenyl trimethyl ammonium chloride, chloride Benzalkonium, diethylaminoethyl stearate, dimethylaminopropyl stearate, lanolin derivatives, quaternary ammonium salts, and the like.

Examples of amphoteric surfactants include the carboxybetaine type, the amide betain type, the sulfobetain type, the hydroxysulfobetain type, the amide sulfobetain type, the phosphobetaine type, the aminocarboxylate type, the imidazoline derivative type, and the amideamine type. An amphoteric surfactant etc. are mentioned.

Examples of the organic and inorganic pigments include inorganic pigments such as silicic acid, silicic anhydride, magnesium silicate, talc, sericite, mica, kaolin, Bengala, clay, bentonite, titanium mica, titanium oxide, bismuth chloride, zirconium oxide, magnesium oxide, Inorganic pigments such as calcium sulfate, barium sulfate, magnesium sulfate, calcium carbonate, magnesium carbonate, iron oxide, chromium oxide, chromium oxide, chromium hydroxide, Polyamide, polyester, polypropylene, polystyrene, polyurethane, vinyl resin, urea resin, phenol resin, fluorine resin, silicon resin, acrylic resin, melamine resin, epoxy resin, polycarbonate resin, divinylbenzene, styrene copolymer, Organic pigments such as silk powder, cellulose, CI pigment yellow, CI pigment orange, and composite pigments of these inorganic pigments and organic pigments;

As organic powder, Metal soaps, such as a calcium stearate; Alkyl phosphate metal salts such as sodium cetylinate, zinc lauryl acid and calcium laurate; Acylamino acid polyvalent metal salts such as N-lauroyl-beta-alanine calcium, N-lauroyl-beta-alanine zinc, and N-lauroylglycine calcium; Amide sulfonic acid polyvalent metal salts, such as N-lauroyl-taurine calcium and N-palmitoyl-taurine calcium; N-epsilon-lauroyl-L-lysine, N-epsilon-palmitolyzine, N-alpha-paratoylol nitin, N-alpha-lauroyl arginine, N-alpha-cured fatty acid acyl arginine -Acyl basic amino acid; N-acyl polypeptides, such as N-lauroyl glycyl glycine; Alpha-amino fatty acids such as alpha-aminocaprylic acid and alpha-aminolauric acid; Polyethylene, polypropylene, nylon, polymethyl methacrylate, polystyrene, divinylbenzene-styrene copolymer, ethylene tetrafluoride and the like.

Examples of the ultraviolet absorber include paraaminobenzoic acid, ethyl paraaminobenzoate, amyl paraaminobenzoic acid, octyl paraaminobenzoate, ethylene glycol salicylate, phenyl salicylate, octyl salicylate, benzyl salicylate, butylphenyl salicylate, homomentyl salicylic acid and benzyl cinnamic acid. , Paramethoxy cinnamic acid-2-ethoxyethyl, paramethoxy cinnamic acid octyl, diparamethoxy cinnamic acid mono-2-ethylhexaneglyceryl, paramethoxy cinnamic acid isopropyl, diisopropyl diisopropyl cinnamic acid ester mixture, wuro Canonic acid, ethyl urokanoate, hydroxymethoxybenzophenone, hydroxymethoxybenzophenonesulfonic acid and salts thereof, dihydroxymethoxybenzophenone, dihydroxymethoxybenzophenone sodium sulfonate, dihydroxybenzophenone , Tetrahydroxybenzophenone, 4- tert -butyl-4'-methoxydibenzoylmethane, 2,4,6-trianilino- p- (carbo-2'-ethylhexyl-1'-oxy) -1 , 3,5-triazine, 2- (2-hi And the like can be mentioned hydroxy-5-methylphenyl) benzotriazole.

As fungicides, hinokithiol, trichloric acid, trichlorohydroxydiphenyl ether, chlorhexidine gluconate, phenoxyethanol, resorcin, isopropylmethylphenol, azulene, salicylic acid, zinphylthione, benzalkonium chloride, Photosensitizer No. 301, mononitrourecosodium sodium, undecylenic acid, etc. are mentioned.

Examples of the antioxidant include butylhydroxyanisole, propyl gallic acid, and erythorbic acid.

Examples of the pH adjuster include citric acid, sodium citrate, malic acid, sodium malate, fmaric acid, sodium pmarate, succinic acid, sodium succinate, sodium hydroxide, sodium dihydrogen phosphate, and the like.

Examples of the alcohol include higher alcohols such as cetyl alcohol.

In addition, the compounding component which may be added other than this is not limited to this, Moreover, Although all said components can be mix | blended within the range which does not impair the objective and effect of this invention, Preferably it is 0.01-5% weight percentage with respect to a total weight, More preferably 0.01-3% by weight.

The cosmetic of the present invention may take the form of a solution, an emulsion, a viscous mixture or the like.

Ingredients included in the cosmetic composition of the present invention may include components commonly used in cosmetic compositions in addition to the black trifolium and its extract as an active ingredient, for example, stabilizers, solubilizers, vitamins, pigments and flavors and Such conventional adjuvants and carriers.

The cosmetic composition of the present invention may be prepared in any formulation commonly prepared in the art, and includes, for example, emulsion, cream, lotion, pack, foundation, lotion, beauty solution, hair cosmetic, and the like.

Specifically, the cosmetic composition of the present invention skin lotion, skin softener, skin toner, astringent, lotion, milk lotion, moisturizing lotion, nutrition lotion, massage cream, nutrition cream, moisture cream, hand cream, foundation, essence, nutrition essence, Formulations of packs, soaps, cleansing foams, cleansing lotions, cleansing creams, body lotions and body cleansers.

When the formulation of the present invention is a paste, cream or gel, animal fiber, plant fiber, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide may be used as the carrier component .

In the case where the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as a carrier component. Especially, in the case of a spray, a mixture of chlorofluorohydrocarbons, propane / Propane or dimethyl ether.

In the case of the solution or emulsion of the present invention, a solvent, a solvent or an emulsifier is used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, , 3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan fatty acid esters.

When the dosage form of the present invention is a suspension, liquid carrier diluents such as water, ethanol or propylene glycol, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystalline Cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.

When the formulation of the present invention is an interfacial active agent-containing cleansing, the carrier component may include aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, linolenic derivatives or ethoxylated glycerol fatty acid esters.

Hereinafter, the present invention will be described in detail with reference to the following examples and experimental examples.

However, the following Examples and Experimental Examples are only illustrative of the present invention, and the content of the present invention is not limited by the following Experimental Examples.

Comparative Example  1. Preparation of Red Ginseng Extract

Take 20 g of red ginseng purchased from Geumsan, crush it, add 100 ml of water, and leave it at room temperature for 5 hours, extract it under reflux three times for 3 hours by adding 1 liter of methanol. The extracted solution is cooled to room temperature, filtered and concentrated under reduced pressure. Methanol was removed using, and 8.1 g of red ginseng extract was obtained. 200 g of water was added and suspended in 8.1 g of red ginseng extract, and then 200 ml of ether was added to remove the nonpolar material. 200 ml of saturated butanol was added to the remaining aqueous layer to extract saponins present in ginseng, and then, butanol was removed by a vacuum condenser to obtain 1.3 g of butanol extract containing a large amount of ginseng saponin (hereinafter referred to as RGRE-1). This RGRE-1 was used as a comparative sample of the antioxidant experiment of the invention.

Comparative Example  2. Preparation of Black Ginseng Extract

A black ginseng extract (hereinafter referred to as BGRE-1) prepared by the method of preparing Korean Patent Application No. 10-2006-0044066 (a method for preparing a new black ginseng and a composition containing the same) was used as a comparative sample for antioxidant experiments.

Comparative Example  3. Ginseng leaf  Preparation of Extract

      Take 5 years old ginseng leaf grown in Geumsan and wash it twice with ultrasonic cleaner for 15 minutes. Take 50g of dried ginseng leaf at 60 ℃ for 10 hours, grind it, add 100ml of water, and leave it at room temperature for 5 hours. 1 L of methanol (20% water) was added thereto, and the mixture was refluxed three times for 3 hours. The extracted solution was cooled to room temperature, filtered, and methanol was removed using a vacuum concentrator to obtain 17.98 g of ginseng leaf extract.

17.98 g of this ginseng leaf extract was suspended in 500 ml of water, and 500 ml of ether was added to remove the nonpolar material. 500 ml of saturated butanol was added to the remaining aqueous layer to extract saponin present in ginseng four times, and then, butanol was removed with a reduced pressure concentrator to extract butanol extract containing a large amount of ginseng saponin (crude saponin extract, hereinafter referred to as CGLE-1). ) 9.19 g was obtained. The above CGLE-1 was used as a comparative sample of the antioxidant experiment.

Example  One. Black trilobite  Produce

1-1. To the gut width  By way

After purchasing 5-year-old ginseng leaf grown in Geumsan, it was put in an ultrasonic cleaner and washed repeatedly three times for 15 minutes. The washed ginseng leaves were first dried at 50 ° C. for 24 hours. The ginseng leaves dried at low temperature for 24 hours were placed in Onggi using a steamer and steamed for 3 hours at 95 ° C except for the preheating time. The preheating time is typically 30 minutes from the time the steam erupts from the pot.

After maintaining the internal temperature of the dryer with a built-in hot wire 60 ℃ ginseng leaf was evenly dried for 12 hours while rotating the pen.

     This steaming and drying process was repeated nine times to produce BGL-1 having a water content of 14% or less, in which the green ginseng leaf turned black.

1-2. Method by high temperature and high pressure

After purchasing 5-year-old ginseng leaf grown in Geumsan, it was put in an ultrasonic cleaner and washed three times in total for 3 minutes. The washed ginseng leaves were first dried at 50 ° C. for 24 hours, and further steamed at 110-145 ° C. for 3 hours under pressure.

After maintaining the internal temperature of the dryer with a built-in heating wire at 60 ℃, evenly rotating the ginseng leaves for 12 hours while rotating the pen to prepare a BGL-2 of the present invention having a moisture content of 14% or less.

Example  2. Black leaf  Preparation of Extract

      50 g of black trilobite prepared by the two methods of the amplification width and high temperature and high pressure of Example 1-1 and 1-2 were respectively added, and 100 ml of water was added and left at room temperature for 5 hours, followed by 80% methanol (20% water). 1 liter was added and refluxed three times for 3 hours, and the extracted solution was cooled to room temperature, filtered, and methanol was removed using a vacuum concentrator to obtain black leaf extract (BGLE-1; 17.85 g and BGLE-2). ; 18.12 g). 500 ml of water was added to the black trifolium extract to suspend and 500 ml of ether was added to remove the nonpolar material. 500 ml of saturated butanol was added to the remaining aqueous layer, followed by extraction of saponin present in ginseng four times, followed by removal of butanol using a reduced pressure concentrator to obtain a butanol extract (crude saponin extract) containing a large amount of ginseng saponin (quasi-amplification method; 9.16g (Hereinafter referred to as BGLBE-1 and high temperature and high pressure method; 9.35g, hereinafter referred to as BGLBE-2). This black trilobite crude saponin was used as a sample for saponin analysis and antioxidant experiment.

Example  3. Black leaf  Saponin ingredient analysis

In order to analyze the components of ginseng saponin present in the black trifoliate extract, 20 mg of the black trifoliate butanol extract obtained in Example 2 was dissolved in 1 ml of methanol, and the filtrate was filtered with a 0.45 μm filter. The components were analyzed at.

As a result of analyzing the components, Rb1 0.5-1mg, Rb2 + Rb3 1.4-2.1mg, Rc 0.5-1.2mg, Rd 2.1-2.5mg, Re 1.0-1.5mg, Rg1 0.4-0.9 It was confirmed that mg, Rk1 is 3.7mg, Rg5 is 4.7mg, Rg3 (S) + Rg3 (R) 25-32mg is present.

In particular, Rg5, which is produced specifically by steaming, has an anti-anxiety effect (Cha HY et al., Biol) . Pharm Bull., 28 (9) , pp1621-5, 2006), brain function improvement effect (Kang JS et al., Arch Pharm Res. , 28 (3) , pp335-342, 2005), antidiabetic effect (Kordella T et al., Diabetes Forecast, 57 (1) , pRG5-8, 2004), Hepatitis C inhibitory effect (Neuberger J et al., The Royal College of Physicians of London and the British Society of Gastroenterology., 49 , Suppl 1 : I1-21, 2001), Rg3 has anti-stress effect (Chung BC et al., Pharmacol Res. , 54 (1) , pp46-9, 2006), anti-cancer effect (Huang C. et al., Sichuan Da Xue Xue Bao Yi Xue Ban, 37 (1) , pp 60-2, 2006), hepatoprotective effect (Kim DH et al., Biol Pharm Bull., 28 (10) , pp1992-4, 2005), antioxidant effect (Sun YX et al., J Agric Food Chem ., 51 (9) , pp2555-8, 2003), angiogenesis inhibitory effect (Qui H et al., Zhonghua Wai Ke Za Zhi , 40 (8 ), pp606-8, 2002), vasorelaxation (Schini-Kerth VB et al., Eur J Pharmacol . , 367 (1) , pp51-7, 1999), platelet aggregation inhibitory activity (Lee HK et al., Biol Pharm Bull., 21 (1) , pp79-80, 1998), etc., are known to exhibit various physiological activities. Therefore, black saponins containing a large amount of these saponins can expect various physiological activities as described above.

Column: Shiseido C18 column (5㎛, 1504.6mm) Flow rate 1ml / min Detector ELSD-LT detector Solvent A; CH ₃ CN: H ₂ O: 5% CH ₃ COOH = 15: 80: 5, B; CH ₃ CN: H ₂ O = 80:20
0 minutes (0% B), 0-10 minutes (30% B), 10-25 minutes (50% B), 25-40 (100% B), 40-50 minutes (100% B), 50-55 Minute (0% B), 55-58 minutes (0% B) Temperature 40 degrees

Experimental Example  1. Antioxidant Experiment

In order to measure the antioxidant activity of the black trilobite extract, the radical scavenging ability test was carried out using the ginseng leaf extract of Comparative Example 1 and the black tricot extract of Example 2 using TOSC (Total Oxyradical Scavenging Capacity) assay. It was.

TOSC assays are described in Winston et al., Free Radic. Biol Med ., Feb, 24 (3), pp480-493, 1998) and modified by the same authors (Regoli and Winston, Toxicol Appl Pharmacol ., Apr 15, 156 (2) , pp96-105, 1999). Peroxyl radicals were generated by thermal homolysis of ABAP (2,2'-azobisamidinopropane) at 35 ° C (Winston et al., Free Radic). Biol Med ., Feb, 24 (3), pp 480-493, 1998), the hydroxyl radical is the Fenton reaction using Fe and ascorbate (Fenton reaction; Winston and Cederbaum et al., Alcholol Clin Exp Res, 9 (2) , pp95-102, 1985), peroxynitrite was generated through spontaneous decomposition of SIN-1. Each reactive oxygen species generated reacts with α-keto-γ-methiolbutyric acid (KMBA) to generate ethylene gas, which does not show any temperature-dependent difference. It has been reported (Winston et al., Free Radic Biol Med . , 24 (3), pp 480-493, 1998; Regoli and Winston et al., Toxicol Appl Pharmacol ., 156 (2), pp 96-105, 1999).

The reaction proceeded by putting the final volume of 1 ml of the reaction solution into a sealed 10 ml container with rubber septum. Ethylene gas generation detection takes a predetermined volume of air in the head space of the reaction vessel and is equipped with a gas chromatography equipped with a Poropack N column and a flame ionization detector (FID). Was analyzed.

As a result of the experiment, the area under the kinetic curve (AUC) was obtained by integrating a graph obtained from the experimental measurements, and the TOSC value was calculated through Equation 1 below. (See Table 2 and Table 3)

TOSC = 100-(∫SA / ∫CA × 100)

∫SA = range integrated from the curve of the sample response

(integrated area from the curve of the sample reaction)

∫CA = integrated range from curve of control response

(integrated area from the curve of the control reaction)

For a sample having no oxyradical scavenging capacity, ∫SA / ∫CA = 1 and a value of TOSC = 0. Conversely, when ∫SA → 0, the TOSC value approaches 100. The value of TOSC is compared with the value in the control, so it is theoretically unaffected by the sensitivity of the instrument, reagents used, or other reaction conditions.

GC equipped with Poropack N column and FID (flame ionizing detector) for the detection of ethylene gas was placed in an oven at 60 ° C, injector 180 ° C and detector 180. It was fixed at 캜 and helium was injected into the column at a rate of 30 ml / min as the mobile phase. For the determination of the ethylene gas in the vial, 150 μl of air in the vial was taken with a gas-tight syringe using the head-space technique, and then gas-tight. The test was performed by injecting a syringe into an injector.

Total Oxyradical Scavenging Ability (TOSC) on Peroxyl Radicals of Ginseng and Black Leaves sample
(Antioxidant) TOSC value according to concentration Specific TOSC Value (TOSC / mg) RGRE-1 Concentration
(mg / ml) 0.0125 0.025 0.05 0.1 423 ± 88 TOSC value 3.69 31.27 38.87 41.3 BGRE-1 Concentration
(mg / ml) 0.0125 0.025 0.05 0.1 476 ± 91 TOSC value 8.10 32.35 45.33 51.80 CGLE-1 Concentration
(mg / ml) 0.0125 0.025 0.05 0.1 991 ± 93 TOSC value 10.3 24.8 55.3 58.3 BGLGE-1 Concentration
(mM) 0.0125 0.025 0.05 0.1 2045 ± 448 TOSC value 36.2 49 58.0 61.5   BGLGE-2 Concentration
(mg / ml) 0.0125 0.025 0.05 0.1 2240 ± 467 TOSC value 38.1 56.0 60.0 68.4 Glutathione
(GSH,
glutathione) Concentration
(mg / ml) 0.0125 0.025 0.05 0.1 940 ± 19 TOSC value 12.4 22.8 47.3 56.4

Total Oxygen Radical Scavenging Ability (TOSC) on Peroxidation of Ginseng and Black Ginseng Leaves sample
(Antioxidant) TOSC value according to concentration Specific TOSC value
(TOSC / mg) RGRE-1 Concentration
(mg / ml) 0.0125 0.025 0.05 0.1 232 ± 24 TOSC value 17.0 31.27 38.87 41.3 BGRE-1 Concentration
(mg / ml) 0.0125 0.025 0.05 0.1 405 ± 39 TOSC value 8.10 32.35 45.33 51.80 CGLE-1 Concentration
(mg / ml) 0.0125 0.025 0.05 0.1 856 ± 291 TOSC value 17.0 21.4 45.8 44.8 BGLGE-1 Concentration
(mM) 0.0125 0.025 0.05 0.1 1694 ± 396 TOSC value 19.4 38.2 41.6 49.6 BGLGE-2 Concentration
(mg / ml) 0.0125 0.025 0.05 0.1 1792 ± 27.7 TOSC value 21.8 44.8 47.6 52.8 Glutathione
(GSH,
glutathione) Concentration
(mg / ml) 0.0125 0.025 0.05 0.1 347 ± 3 TOSC value 4.2 8.5 17.4 34.3

As confirmed in Korean Patent Application No. 10-2006-0044066 (a method for preparing a new black ginseng and a composition containing the same), BGRE-1 has peroxyl radicals and peroxide nitrates at a concentration of 0.2 mg / ml or less. peroxynitrite) has been reported to exhibit high antioxidant activity. In particular, the scavenging ability (peroxynitrite) BGRE-1 showed about 1.7 times higher activity than RGRE-1.

     As a result, CGLE-1, an unprocessed ginseng leaf extract, showed more than two times higher antioxidant activity against peroxyl radicals and peroxynitrite than previously known black ginseng. In addition, BGLGE-1 and BGLGE-2, which steamed the ginseng leaf by the augmentation width and high temperature and high pressure method, showed more than twice as strong antioxidant effect as CGLE-1 showing high antioxidant activity (see Table 2 and Table 3). .

In other words, the black ginseng leaf extract (BGLGE-1 and BGLGE-2) prepared by the method of the present invention showed more than twice as strong antioxidant effect as the unprocessed ginseng leaf extract (CGLE-1), and the black ginseng extract (BGRE Compared with -1), it showed 4-5 times stronger antioxidant effect.

In addition, it was found that BGLGE-1 and BGLGE-2 exhibited strong antioxidant activity compared to glutathione (GSH, glutathione), which shows antioxidant activity in the human body.

Experimental Example  2. Acute Toxicity Test

Acute toxicity test was performed using 6-week-old specific pathogen-free (SPF) SD rats from the Korean Center for Experimental Animals. Two animals of each group were orally administered to the black trilobite extract of Example 2 at a dose of 1 g / kg. After administration of the test substance, mortality, clinical symptoms, and changes in body weight were observed. Hematological and hematological examinations were performed. Necropsy was performed to visually observe abnormalities in organs and thoracic organs.

As a result, no clinical symptoms or dead animals were found in all animals treated with the test substance, and no toxic changes were observed in weight changes, blood tests, blood biochemical tests, and autopsy findings.

As a result, the extract of the present invention did not show a change in toxicity even in rats up to 1 g / kg, respectively, the minimum lethal dose (LD ₅₀ ) was determined to be a safe substance of more than 1 g / kg.

The preparation example of the cosmetic composition comprising the black trifoliate or extract thereof of the present invention will be described, but the present invention is not intended to be limited thereto, but is intended to be described in detail.

Formulation example  1. Preparation of Hydrophilic Ointment

Raw material weight%   Black Leaf or Black Leaf 9.00   White vaseline 36.00   Stearyl alcohol 31.00   Ethyl (or methyl) p-oxybenzoate a very small amount   Propylene glycol 19.00   Sodium lauryl sulfate 2.40   Propyl p-oxybenzoate a very small amount system 100.00

Formulation example  2. Flexible Cosmetics skin Manufacturing

Raw material weight%   Black Leaf or Black Leaf 2.0 1,3-butylene glycol 2.00 glycerin 3.00 Oleyl alcohol 2.00 Polysorbate 20 1.00 ethanol 6.00 antiseptic a very small amount incense a very small amount Purified water Balance system 100.00

Formulation example  3. Milk croissant  Produce

Raw material weight%   Black Leaf or Black Leaf 5.0 1,3-butylene glycol 4.00 glycerin 3.00 Oleyl alcohol 0.05 Polysorbate 20 1.00 antiseptic a very small amount incense a very small amount Purified water Balance system 100.00

Formulation example  4. Manufacturing of Nutritional Cream

Raw material weight%  Black Leaf or Black Leaf 2.0 Vaseline 5.00 Liquid paraffin 30.00 Beeswax 3.00 Polysorbate 60 1.00 Sorbitan sesquioleate 1.00 1,3-butylene glycol 5.00 glycerin 5.00 antiseptic a very small amount incense a very small amount Purified water Balance system 100.00

Formulation example  5. Massage  Manufacture of cream

Raw material weight%   Black Leaf or Black Leaf 7.0 glycerin 5.00 Triethanolamine 0.50 Tocopheryl acetate 1.00 Liquid paraffin 5.00 Squalane 5.00 Macadamia Nut Oil 15.00 Polysorbate 60 1.00 Sorbitan sesquioleate 1.00 Carboxy vinyl polymer 0.20 antiseptic a very small amount incense a very small amount Purified water Balance system 100.00

As described above, the present invention is a black man using a high temperature and high pressure that can be produced in a short time, mass production is possible compared to the conventional method of producing augmentation width using a ginseng leaf that is discarded even more than the ginseng root saponin content The present invention relates to a composition containing the black trifoliate and extracts thereof prepared from the method for producing trifoliate, and the composition exhibits a strong antioxidant effect and is a skin external pharmaceutical composition for preventing and treating skin diseases caused by oxidative stress and oxidative stress. Provided is a cosmetic composition for preventing and improving skin diseases.

Claims (6)

After washing the 4-6 years old ginseng leaf, the first drying step of drying for 20 to 28 hours at a temperature of 40 to 60 ℃; Primary steaming step of steaming for 2 to 4 hours at a temperature of 85 to 105 ℃ in the steamer; Secondary drying step of drying for 9 to 15 hours at a temperature of 50 to 70 ℃; Method for producing a processed ginseng leaf having a moisture of 14% or less, characterized in that it comprises a steaming and drying step of repeating the steaming step and the second drying step nine times. After washing the 4-6 years old ginseng leaf, the first drying step of drying for 20 to 28 hours at a temperature of 40 to 60 ℃; Primary steaming step of steaming for 2 to 4 hours at a temperature of 110 to 145 ℃ under pressure; Method for producing a processed ginseng leaf having a moisture of 14% or less, characterized in that it comprises a secondary drying process step of drying for 9 to 15 hours at a temperature of 50 to 70 ℃. The processed ginseng leaf prepared by the method of claim 1 or 2 is pulverized, and 2 to 7 times the mass of the processed ginseng leaf is added and left for 3 to 7 hours. The mixed solvent of water and methanol is extracted as Method of extracting processed ginseng leaf extract. delete delete Cosmetic composition for the prevention and improvement of blemishes, freckles containing the processed ginseng leaf extract obtained by the method of claim 3 as an active ingredient.