WO2021112398A1 - Composition comprenant de la vitamine c - Google Patents

Composition comprenant de la vitamine c Download PDF

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Publication number
WO2021112398A1
WO2021112398A1 PCT/KR2020/014311 KR2020014311W WO2021112398A1 WO 2021112398 A1 WO2021112398 A1 WO 2021112398A1 KR 2020014311 W KR2020014311 W KR 2020014311W WO 2021112398 A1 WO2021112398 A1 WO 2021112398A1
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WIPO (PCT)
Prior art keywords
present
vitamin
cosmetic composition
oils
fats
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PCT/KR2020/014311
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English (en)
Korean (ko)
Inventor
전영선
Original Assignee
(주)이시스코스메틱
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Publication of WO2021112398A1 publication Critical patent/WO2021112398A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/46—Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/31—Hydrocarbons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67—Vitamins
    • A61K8/676—Ascorbic acid, i.e. vitamin C
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/52—Stabilizers

Definitions

  • the present invention relates to a stable composition comprising vitamin C.
  • the adverse effects on the skin can be divided into internal factors and external factors.
  • internal factors free radicals generated by stress are mentioned, and the external factors include excessive UV exposure due to environmental pollution.
  • Vitamin C acts as a powerful biological antioxidant in the skin, blood and other tissues, and has a sugar-like structure that accepts two electrons and is easily oxidized to the form of dehydro-L-ascorbic acid (Dehydro-L-ascorbic acid). ) to prevent oxidation or denaturation of biocomponents such as proteins by highly reactive free radicals and peroxides in the living body.
  • vitamin C has a pigmentation inhibitory effect, which is achieved by inhibiting the production of melanin, which is closely related to pigmentation.
  • Vitamin C inhibits the activity of tyrosinase, which is important for the formation of melanin, and reduces the oxidized melanin formed by the oxidation process and changes it into reduced melanin, thereby improving the pigmentation symptoms caused by melanin.
  • the cosmetic composition containing vitamin C has the above useful effects, it is easily oxidized by air, moisture, light, heat, metal ions, oxygen, base, etc. to 2,3-diketo-L-gulonic acid (2 ,3-diketo-L-gulonic acid), oxalic acid, L-threonic acid, L-xylonic acid, L-Lyxonic acid, etc. is oxidized to At this time, there is a big problem in stability and safety in the formulation, such as a drop in potency and discoloration and odor. In addition, it is common that a large amount of pure vitamin C has a poor feeling of use and irritation, and precipitation occurs.
  • An object of the present invention is to provide a composition having high stability of vitamin C, less skin irritation, and excellent skin whitening effect.
  • Another object of the present invention is to provide a method for preparing a vitamin C-containing composition.
  • one or more stabilizers selected from the group consisting of lemon myrtle extract, fullerene and oils and fats were included.
  • the present invention is a first invention.
  • At least one stabilizer selected from the group consisting of lemon myrtle extract, fullerenes and oils and fats
  • composition comprising a.
  • the cosmetic composition of the present invention can be used for skin whitening by the effect of vitamin C.
  • the cosmetic composition may include two or more stabilizers selected from the group consisting of lemon myrtle extract, fullerenes and oils and fats as stabilizers.
  • the cosmetic composition may include lemon myrtle extract and fullerene as stabilizers.
  • the cosmetic composition may include lemon myrtle extract, fullerene and oils and fats as stabilizers.
  • vitamin C included in the cosmetic composition may be pure ascorbic acid.
  • the oils and fats included in the cosmetic composition may be at least one selected from the group consisting of hydrocarbons, silicones, oil-soluble vitamin derivatives, and ester oils.
  • the hydrocarbon may be a C 18-21 alkane.
  • the content of vitamin C may be 30 w/v% or less, preferably 1 to 20 w/v%.
  • the content of oils and fats may be 1 to 20 w/v%.
  • the cosmetic composition may be a functional cosmetic for skin whitening.
  • the present invention is a first invention.
  • At least one stabilizer selected from the group consisting of lemon myrtle extract, fullerenes and oils and fats
  • composition for whitening comprising a.
  • the present invention provides a method for preparing a composition comprising vitamin C, comprising the step of preparing a mixture by mixing vitamin C, lemon myrtle extract and fullerene in an aqueous solvent.
  • the composition of the present invention has high vitamin C stability. Therefore, the composition of the present invention has excellent storage stability and can stably maintain the effect of vitamin C for a long period of time. In addition, the composition of the present invention can ensure stability even when it contains a large amount of vitamin C.
  • composition of the present invention is less irritating when applied to the skin. Therefore, the composition of the present invention can be used without discomfort even for sensitive or weak skin.
  • composition of the present invention exhibits skin whitening, wrinkle improvement, elasticity improvement and antioxidant action. Therefore, it can be usefully used as a cosmetic and pharmaceutical composition.
  • the cosmetic composition of the present invention comprises: (i) vitamin C; and (ii) at least one stabilizing agent.
  • the stabilizer may be at least one selected from the group consisting of lemon myrtle extract, fullerene, and oils and fats.
  • vitamin C means ascorbic acid having the structure of the following formula (I) or a derivative thereof, or a salt or solvate thereof.
  • vitamin C may be pure ascorbic acid.
  • pure ascorbic acid means that the content of the compound of the structure [Formula I], which is not a derivative of ascorbic acid, is 90% or more, preferably 95% or more, more preferably 99% or more with respect to the total vitamin C. .
  • Vitamin C prevents the production of melanin and whitens the skin, and helps to synthesize collagen that makes up the skin, thereby improving wrinkles and improving elasticity. In addition, it also exhibits an antioxidant effect that suppresses free radicals generated due to pollution such as ultraviolet rays and fine dust, and stress.
  • vitamin C is a sensitive substance that is easily destroyed by heat, light, water, and oxygen, it is important to maintain its stability.
  • the cosmetic composition of the present invention has very excellent vitamin C stability, it can effectively exhibit skin whitening, wrinkle improvement, elasticity improvement, and antioxidant effects.
  • lemon myrtle is a plant of the family Myrtaceae, and the scientific name is Backhousia citriodora , lemon scented myrtle, lemon scented ironwood, sweet verbena. It is also called sweet verbena tree, sweet verbena myrtle, lemon scented verbena, lemon scented backhousia, etc. Lemon myrtle is native to the subtropical rain forests of central and southeastern Queensland, Australia.
  • extract includes all substances obtained by extracting the components of a natural product, regardless of the extraction method, extraction solvent, extracted component or the form of the extract, and extracting the material obtained by extracting the component of the natural product It is a broad concept that includes all substances that can be obtained by further processing or processing in other ways.
  • processing or treatment may be, for example, additional fermentation or enzymatic treatment of the extract.
  • an extract is a fraction, an extract or a crude product or purified product of a fraction, or a dilution, concentrate, dried product, fermented product, or mixture thereof, and the like, including extracts of all formulations formable from lemon myrtle. to be.
  • the “lemon myrtle extract” may be an extract of the whole herb, which is the leaf, flower, root, stem, fruit, or a combination thereof, of lemon myrtle, and may be an extract of a part or all of the above-ground part or root part of the herb; Preferably, it may be an extract of lemon myrtle whole plant, and more preferably, it may be an extract of lemon myrtle leaves.
  • the lemon myrtle extract may be prepared using a general preparation method known in the art, and is not particularly limited.
  • a general preparation method known in the art for example, ultrasonic extraction method, supercritical extraction method, vacuum extraction method reflux extraction method, hot water extraction method, low temperature hot water extraction method, high temperature pressure extraction method, low temperature high pressure extraction method, ultra high pressure extraction method, enzyme extraction method, solvent extraction method, cold extraction method, steam distillation method, low temperature high pressure distillation method, It may be prepared by a known method using an elution method, a compression method, a heat extraction method, or an extraction solvent, but is not limited thereto.
  • the lemon myrtle extract may be obtained by low-temperature high-pressure distillation.
  • the lemon myrtle extract may be prepared as an extract using water, an organic solvent, or a mixture thereof as an extraction solvent.
  • the water may include, for example, distilled water, purified water, or sterile water, but is not limited thereto.
  • the organic solvent may include, for example, alcohol, glycerin, butylene glycol, propylene glycol, methyl acetate, ethyl acetate, acetone, benzene, hexane, diethyl ether, and dichloromethane, but is not limited thereto.
  • the lemon myrtle extract is preferably extracted with a solvent selected from the group consisting of water, C 1-6 alcohol, acetone, ether, benzene, chloroform, ethyl acetate, methylene chloride, hexane, cyclohexane, and mixtures thereof. It may be extracted with a solvent.
  • the concentration of the C 1-6 alcohol may be 10% to 90%, preferably 30% to 90%, and more preferably 50% to 90%.
  • the lemon myrtle extract of the present invention may be purchased commercially, or may be prepared by the known extraction method described above, and preferably extracted in distilled water at low temperature.
  • the lemon myrtle extract may be lemon myrtle distilled water.
  • the lemon myrtle extract can effectively prevent the decomposition and oxidation of vitamin C by external environments such as moisture, temperature, and air by increasing the internal oxidation stability of vitamin C.
  • “Fullerene” is an allotrope of carbon consisting of 60 carbon atoms of the structure of the following [Formula II], and is a carbon-bonded structure having a stable structure that is formed like a soccer ball.
  • Fullerene has insulation, organic solvent solubility, thermal stability, thermal decomposition inhibition, and antioxidant properties, and by utilizing these properties, its application is continuously reviewed in many fields such as magnetic materials, optical materials, superconducting materials, medical care, secondary batteries, and lubricants. is becoming
  • fullerene can effectively prevent decomposition and oxidation of vitamin C by external environments such as moisture, temperature, and air by increasing the internal oxidation stability of vitamin C.
  • oils and fats refer to substances that may exist in the oil phase when the solution is divided into an oil phase and an aqueous phase.
  • oils and fats may include, for example, hydrocarbons, silicones, oil-soluble vitamin derivatives, or ester oils.
  • the cosmetic composition of the present invention may include one or more oils and fats selected from the group consisting of hydrocarbons, silicones, oil-soluble vitamin derivatives, and ester oils.
  • oils and fats effectively prevent decomposition and oxidation by external environments such as moisture, temperature, and air by capturing and stabilizing vitamin C in the inner layer of the water-in-oil dispersion formulation, and the stickiness and slipping phenomenon of vitamin C It is possible to secure stability by using a mechanism to block oxygen on the surface.
  • oils and fats act as a protective agent that prevents contact between vitamin C and external air, thereby preventing oxidation of an aqueous solution in which vitamin C, preferably vitamin C, is dissolved from external oxidizing factors.
  • the hydrocarbon may be a straight-chain or branched alkane, alkene, or alkyne, preferably a C 12-25 alkane, more preferably a C 18-21 alkane.
  • the silicon is a polymer of an organosilicon compound, and refers to a polymer containing silicon as a main component.
  • the oil-soluble vitamin derivative is a vitamin soluble in fat, and includes vitamins A, D, E, and K or derivatives thereof, for example, tocopherol and tocopheryl acetate tocotrienol.
  • the stabilizer may be two or more selected from the group consisting of lemon myrtle extract, fullerenes and oils and fats.
  • the present invention provides a cosmetic composition comprising a lemon myrtle extract and fullerene, a cosmetic composition comprising a lemon myrtle extract and oils and fats, a cosmetic composition comprising a fullerene and fats and oils, or a cosmetic comprising a lemon myrtle extract, fullerene and oils and fats. It may be a composition.
  • the cosmetic composition may include only fullerene as a stabilizer, and may further include a lemon myrtle extract.
  • the cosmetic composition includes lemon myrtle extract, fullerene and oils and fats as stabilizers.
  • the cosmetic composition of the present invention may further include an additional active ingredient functional as a cosmetic in addition to vitamin C.
  • the cosmetic composition of the present invention may further include additional active ingredients effective for whitening, wrinkle improvement, moisturizing, exfoliation, elasticity improvement, antioxidant or oil control, and the like.
  • the cosmetic composition of the present invention may further include vitamin A or vitamin D.
  • the vitamin A and vitamin D have various skin improvement effects including whitening.
  • vitamin A and vitamin D are fat-soluble vitamins, they may also function as stabilizers in the cosmetic composition of the present invention.
  • the content of vitamin C is 50 w/v% or less, preferably 30 w/v% or less, more preferably 20 w/v% or less.
  • the content of vitamin C may be 0.1 w/v% or more, preferably 1 w/v% or more, more preferably 10 w/v% or more.
  • the content of vitamin C may be 10 to 20 w / v%.
  • the content of the lemon myrtle extract may be 90 w/v% or less, preferably 80 w/v% or less, and more preferably 70 w/v% or less.
  • the content of the lemon myrtle extract may be 0.1 w/v% or more, preferably 5 w/v% or more, and more preferably 10 w/v% or more.
  • the content of the lemon myrtle extract may be 10 to 70 w / v%.
  • the content of fullerene may be 5 ppm or less, preferably 3 ppm or less, more preferably 2 ppm or less.
  • the content of fullerene may be 0.01 ppm or more, preferably 0.1 ppm or more, more preferably 1.0 ppm or more.
  • the content of fullerene may be 1.0 to 2 ppm.
  • the content of fullerene may be 0.0005 w/v% or less, preferably 0.0003 w/v% or less, and more preferably 0.0002 w/v% or less.
  • the content of fullerene may be 0.000001 w/v% or more, preferably 0.00001 w/v% or more, and more preferably 0.0001 w/v% or more.
  • the content of fullerene may be 0.0001 w/v% to 0.0002 w/v%.
  • the content of oils and fats may be 50 w/v% or less, preferably 30 w/v% or less, and more preferably 20 w/v% or less.
  • the content of oils and fats may be 0.1 w/v% or more, more preferably 1 w/v% or more. In a specific embodiment of the present invention, the content of oils and fats may be 1 to 20 w/v%.
  • the content of C 18-21 alkane may be 50 w/v% or less, preferably 30 w/v% or less, and more preferably 20 w/v% or less.
  • the content of C 18-21 alkane may be 0.1 w/v% or more, more preferably 1 w/v% or more.
  • the content of C 18-21 alkane may be 1 to 20 w/v%.
  • the content of silicone may be 50 w/v% or less, preferably 30 w/v% or less, and more preferably 20 w/v% or less.
  • the content of silicone may be 0.1 w/v% or more, more preferably 1 w/v% or more.
  • the content of silicone may be 1 to 20 w/v%.
  • the content of the oil-soluble vitamin derivative is 50 w/v% or less, preferably 30 w/v% or less, more preferably 20 w/v% or less.
  • the content of the oil-soluble vitamin derivative may be 0.1 w/v% or more, more preferably 1 w/v% or more. In a specific embodiment of the present invention, the content of the oil-soluble vitamin derivative may be 1 to 20 w/v%.
  • the content of the ester oil may be 50 w/v% or less, preferably 30 w/v% or less, and more preferably 20 w/v% or less.
  • the content of the ester oil may be 0.1 w/v% or more, more preferably 1 w/v% or more. In a specific embodiment of the present invention, the content of ester oil may be 1 to 20 w/v%.
  • the cosmetic composition of the present invention is particularly effective and excellent in whitening, and can be used as a functional cosmetic for skin whitening.
  • the cosmetic composition of the present invention also has excellent anti-wrinkle effect, and can be used as a functional cosmetic for wrinkle improvement.
  • the cosmetic composition of the present invention exhibits excellent stability and can be stored for a long time without decreasing the titer of vitamin C.
  • the cosmetic composition of the present invention exhibits excellent stability at 40° C. or less. Specifically, it was confirmed that the cosmetic composition of the present invention exhibits excellent stability at 5°C. In addition, it was confirmed that the cosmetic composition of the present invention exhibits excellent stability at 25°C. Furthermore, it was confirmed that the cosmetic composition of the present invention exhibits excellent stability at 40°C. Accordingly, the cosmetic composition of the present invention exhibits excellent stability at 5°C to 40°C, 5 to 30°C, or 5 to 25°C.
  • the cosmetic composition of the present invention contains at least one selected from the group consisting of lemon myrtle extract, fullerene, and oil and fat as a stabilizer, skin irritation does not occur and excellent skin whitening effect is maintained.
  • the cosmetic composition of the present invention may be prepared in any formulation conventionally prepared in the art, for example, a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing It may be formulated as cleansing, oil, powder foundation, emulsion foundation, wax foundation and spray, but is not limited thereto. More specifically, it may be prepared in the form of a flexible lotion, a nourishing lotion, a nourishing cream, a massage cream, an essence, a pack, an eye cream, a cleansing cream, a cleansing foam, a cleansing water, a spray, or a powder.
  • a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing It may be formulated as cleansing, oil, powder foundation, emulsion foundation, wax foundation and spray, but is not limited thereto. More specifically, it may be prepared in the form of a flexible lotion, a nourishing lotion, a nourishing cream, a massage cream, an essence, a pack, an eye cream
  • the formulation of the cosmetic composition of the present invention is a paste, cream or gel, animal oil, vegetable oil, wax, paraffin, starch, tracanth, cellulose derivative, polyethylene glycol, bentonite, silica, talc, or zinc oxide is used as a carrier component.
  • lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder, etc. may be used as a carrier component, and in particular, in the case of a spray, additional chlorofluoro propellants such as hydrocarbons, propane/butane or dimethyl ether.
  • a solvent, solubilizer or emulsifier is used as a carrier component, for example, water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzo Eight, propylene glycol, butylene glycol, 1,3-butyl glycol oil, polyoxyethylene hydrogenated castor oil, glycerol, glycerin, aliphatic ester, phenoxyethanol, triethanolamine, polyethylene glycol, beeswax, polysorbate 60, sorbitan Sesquioride, Paraffin, Sorbitan Stearate, Lipophilic Monostearate Glycerin, Stearic Acid, Glyceryl Stearate/PEG-400 Stearate, Carboxypolymer, Sitosterol, Polyglyceryl 2-oleate, Ceramide, Cholesterol , steareth-4
  • a solvent, solubilizer or emulsifier is used as
  • a liquid diluent such as water, ethanol, butylene glycol or propylene glycol, ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester, and polyoxyethylene sorbitan ester
  • Suspending agents such as, microcrystalline cellulose, hydroxyethyl cellulose, sodium hyaluronate, phenoxyethanol, aluminum metahydroxide, bentonite, agar or tracanth may be used.
  • the formulation of the cosmetic composition of the present invention is surfactant-containing cleansing
  • fatty acid amide ether sulfate, alkylamidobetaine fatty alcohol, fatty acid glyceride, fatty acid diethanolamide, vegetable oil, lanolin derivative or ethoxylated glycerol fatty acid ester and the like
  • the cosmetic composition of the present invention may include a cosmetically acceptable additive, for example, may include one or more additives selected from solubilizers, thickeners and surfactants.
  • the cosmetic composition of the present invention may include a solubilizer and a thickener.
  • the solubilizer is, for example, polyglyceryl-10 laurate, polyglyceryl-4 laurate, octyldodeses-16yl, PEG-40 hydrogenated pizza oil, PEG-1-PEG-9 lauryl glygol ethers, C 12-13 pareth 9, heptyl glucose and sorbitan oleate.
  • the solubilizing agent may be at least one selected from polyglyceryl-10 laurate, polyglyceryl-4 laurate, and octyldodeses-16yl.
  • the cosmetic composition of the present invention may include polyglyceryl-10 laurate, polyglyceryl-4 laurate and octyldodeses-16 as solubilizers.
  • the thickener is, for example, hydrophilic silica, polysaccharide, alginate, xanthan gum, carbomer, carboxymethyl cellulose, hydroxyethyl cellulose, hydroxyethylpropylcellulose, hydroxypropylcellulose, polyethylene glycol ester, polyacrylate, poly acrylamide, polyvinyl alcohol, polyvinylpyrrolidone, cyclopentasiloxane, disteadimo hectoride, propylene carbonate, kaolin, calamine, smectide clay, and the like, but is not limited thereto.
  • the thickening agent may be hydroxyethylcellulose.
  • the pharmaceutical composition of the present invention comprises: (i) vitamin C; and (ii) at least one stabilizer.
  • the stabilizer may be at least one selected from the group consisting of lemon myrtle extract, fullerene, and oils and fats.
  • vitamin C in the pharmaceutical composition of the present invention, the description of vitamin C, lemon myrtle extract, fullerene, and oils and fats is the same as described above in the cosmetic composition.
  • the pharmaceutical composition of the present invention may further include a pharmaceutically acceptable carrier in a range that does not impair the effects of the present invention.
  • the type of pharmaceutically acceptable carrier that can be used in the present invention is not particularly limited, and any carrier commonly used in the art may be used.
  • the carrier may include, for example, saline, sterile water, Ringer's solution, buffered saline, albumin injection solution, lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, maltodextrin, glycerol, ethanol, and the like. , but is not limited thereto.
  • the carrier may be used alone or as a mixture of two or more.
  • the pharmaceutical composition of the present invention may further include a pharmaceutically acceptable additive in a range that does not impair the effects of the present invention.
  • a pharmaceutically acceptable additive in a range that does not impair the effects of the present invention.
  • the types of pharmaceutically acceptable additives that can be used in the present invention are not particularly limited, and any additives commonly used in the art may be used.
  • the additives may include, but are not limited to, fillers, binders, disintegrants, suspending agents, solvents, antioxidants, pH adjusting agents, wetting agents, sweetening agents and preservatives, for example.
  • the above additives may be used alone or in combination of two or more.
  • compositions of the present invention may be in various formulations suitable for oral or parenteral administration.
  • formulations for oral administration include, for example, tablets, pills, powders, powders, granules, pellets, capsules, troches, lozenges, suspensions, emulsions, syrups and elixirs.
  • formulations for parenteral administration include, for example, injections, suppositories, respiratory inhalants, aerosols, ointments, powders for application, oils, creams and gels, but are not limited thereto.
  • parenteral administration includes, for example, intraperitoneal administration, rectal administration, subcutaneous administration, intravenous administration, intramuscular administration, chest administration, cerebrovascular administration and transdermal administration and hair administration, and the composition is applied to the diseased site or spraying or inhaling, but is not limited thereto.
  • the pharmaceutical composition of the present invention is administered in a pharmaceutically effective amount.
  • pharmaceutically effective amount means an amount sufficient to treat a disease with a reasonable benefit/risk ratio applicable to medical treatment, and the level of an effective amount includes the patient's condition, weight, sex, age, health Condition, severity of disease, sensitivity to drug, administration time, route of administration, rate of excretion, duration of treatment, factors including concomitant drugs and other factors well known in the medical field.
  • the dosage of the pharmaceutical composition of the present invention may be appropriately selected by those skilled in the art.
  • the dosage of the pharmaceutical composition of the present invention may be 0.1 mg/kg to 2,000 mg/kg per day, more preferably 1 mg/kg to 500 mg/kg, based on the content of the extract of the middle head extract.
  • the present invention is not limited thereto. In addition, it does not limit the scope of the present invention of the above dosage.
  • Administration of the pharmaceutical composition of the present invention may be administered once a day, may be administered in several divided doses, may be administered once every several days.
  • the administration period of the pharmaceutical composition of the present invention is well known to those skilled in the art by those skilled in the art that the patient's condition, weight, sex, age, health condition, degree of disease, sensitivity to drugs, factors including concurrent drugs, and other medical fields are well known. factors can be taken into account.
  • the pharmaceutical composition of the present invention may be administered alone or in combination with other therapeutic agents, and may be administered simultaneously or sequentially with other therapeutic agents.
  • the pharmaceutical composition of the present invention may be used in combination with surgery, hormone therapy, chemotherapy, and methods using biological response modifiers.
  • a composition containing vitamin C including the step of preparing a mixture by mixing vitamin C, lemon myrtle extract and fullerene in an aqueous solvent.
  • vitamin C comprising the steps of (a) mixing vitamin C, lemon myrtle extract and fullerene in an aqueous solvent to prepare a mixture, and (b) filling the mixture with oils and fats; compositions can be prepared.
  • step (a) after mixing the oil and fat with other fat-soluble ingredients, it may be peeled together with the mixture of step (a).
  • the oils and fats after the oils and fats are mixed with tocopherol, beta-carotene or both, it may be filled with the mixture of step (a).
  • Example 1 (w/v %)
  • Example 2 (w/v %)
  • Example 3 (w/v %)
  • Example 4 (w/v %)
  • Example 5 (w/v %)
  • Purified water to.100 to.100 to.100 to.100 Lemon Myrtle Distilled Water - 10 30 50 70 fullerene 0.00015 0.00015 0.00015 0.00015 ascorbic acid 15 15 15 15 15 15
  • Octyldodeces-16 0.15 0.15 0.15 0.15 0.15 hydroxyethyl cellulose 0.4 0.4 0.4 0.4 0.4 0.4
  • Purified water, ascorbic acid, distilled lemon myrtle water, fullerene, solubilizers (polyglyceryl-10 laurate, polyglyceryl-4 laurate, octyldodeses-16) and thickening agents (hydroxyethylcellulose) are listed below [Table 2] ] (first mixture).
  • solubilizers polyglyceryl-10 laurate, polyglyceryl-4 laurate, octyldodeses-16
  • thickening agents hydroxyethylcellulose
  • Example 6 (w/v %) Example 7 (w/v %) Example 8 (w/v %) Example 9 (w/v %) Example 10 (w/v %) Example 11 (w/v %) Example 12 (w/v %) Example 13 (w/v %) Purified water to.100 to.100 to.100 to.100 to.100 to.100 to.100 Lemon Myrtle Distilled Water 50 50 50 50 50 50 50 50 50 50 50 fullerene 0.00015 0.00015 0.00015 0.00015 0.00015 0.00015 0.00015 0.00015 ascorbic acid 15 15 15 15 15 10 14 18 Polyglyceryl-10 Laurate 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 Polyglyceryl-4 Laurate 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 Octyldodeces-16 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 hydroxyethyl cellulose 0.4 0.4 0.4 0.4 0.4 0.4
  • Examples 14 to 21 were prepared according to the contents described in [Table 3] in the same manner as in Examples 6 to 13.
  • Example 14 (w/v %) Example 15 (w/v %) Example 16 (w/v %) Example 17 (w/v %) Example 18 (w/v %) Example 19 (w/v %) Example 20 (w/v %) Example 21 (w/v %) Purified water to.100 to.100 to.100 to.100 to.100 to.100 to.100 Lemon Myrtle Distilled Water 50 50 50 50 50 50 50 50 50 50 50 50 50 fullerene 0.00015 0.00015 0.00015 0.00015 0.00015 0.00015 0.00015 0.00015 ascorbic acid 15 15 15 15 15 10 14 18 Polyglyceryl-10 Laurate 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 Polyglyceryl-4 Laurate 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 Octyldodeces-16 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 hydroxyethyl cellulose 0.4 0.4 0.4 0.4 0.4
  • Examples 22 to 29 were prepared according to the contents described in [Table 4] in the same manner as in Examples 6 to 13.
  • Example 22 (w/v %) Example 23 (w/v %) Example 24 (w/v %) Example 25 (w/v %) Example 26 (w/v %) Example 27 (w/v %) Example 28 (w/v %) Example 29 (w/v %) Purified water to.100 to.100 to.100 to.100 to.100 to.100 Lemon Myrtle Distilled Water 50 50 50 50 50 50 50 50 50 50 50 50 fullerene 0.00015 0.00015 0.00015 0.00015 0.00015 0.00015 0.00015 0.00015 ascorbic acid 15 15 15 15 15 10 14 18 Polyglyceryl-10 Laurate 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 Polyglyceryl-4 Laurate 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 Octyldodeces-16 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 0.15 hydroxyethyl cellulose 0.4 0.4 0.4 0.4 0.4 0.4 0.4
  • Examples 30 to 37 were prepared according to the contents described in [Table 5] in the same manner as in Examples 6 to 13.
  • Comparative Example 1 (w/v %) Comparative Example 2 (w/v %) Comparative Example 3 (w/v %) Comparative Example 4 (w/v %) Purified water to.100 to.100 to.100 Lemon Myrtle Distilled Water - 70 50 - fullerene - - - - ascorbic acid 15 15 15 15 15 Polyglyceryl-10 Laurate 0.15 0.15 0.15 0.15 Polyglyceryl-4 Laurate 0.15 0.15 0.15 0.15 Octyldodeces-16 0.15 0.15 0.15 0.15 0.15 hydroxyethyl cellulose 0.4 0.4 0.4 0.4 C 18-21 Alkane - - 10 10 tocopherol - - 0.1 0.1 beta-carotene - - 0.1 0.1
  • Comparative Examples 1 and 2 were prepared in the same manner as in Examples 1 to 5, and Comparative Examples 3 and 4 in the same manner as in Examples 6 to 13, according to the contents described in Table 6 below.
  • Comparative Example 1 (w/v %) Comparative Example 2 (w/v %) Comparative Example 3 (w/v %) Comparative Example 4 (w/v %) Purified water to.100 to.100 to.100 Lemon Myrtle Distilled Water - 70 50 - fullerene - - - - ascorbic acid 15 15 15 15 15 Polyglyceryl-10 Laurate 0.15 0.15 0.15 0.15 Polyglyceryl-4 Laurate 0.15 0.15 0.15 0.15 Octyldodeces-16 0.15 0.15 0.15 0.15 0.15 hydroxyethyl cellulose 0.4 0.4 0.4 0.4 C 18-21 Alkane - - 10 10 tocopherol - - 0.1 0.1 beta-carotene - - 0.1 0.1
  • Example 1 Example 2
  • Example 3 Example 4
  • Example 5 Example 6
  • Example 7 Early 100% 100% 100% 100% 100% 100% 100% 100% 100% 1 month later 5°C 98.20% 97.10% 98.10% 97.20% 98.20% 98.3 97.5 25°C 95.20% 96.50% 97.30% 97.90% 95.20% 97.4 98.8
  • Example 8 Example 9 Example 10 Example 11 Example 12 Example 13 Early 100% 100% 100% 100% 100% 100% 100% 100% 1 month later 5°C 98.4 99.2 94.5 94.8 93.4 94.1 25°C 97.6 98.8 96.8 93.7 92.1 95.4
  • Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Early 100% 100% 100% 100% 100% 1 month later 5°C 88.5% 92.80% 87.5 84.2 25°C 65.10% 75.20% 94.4 90.2
  • Example 6 Example 7
  • Example 8 Example 9
  • Example 10 Example 11
  • Example 12 Example 13 Early 100% 100% 100% 100% 100% 100% 100% 100% 100% 100% 1 month later 40°C 93.4% 91.1% 92.4% 94.4% 90.8% 93.6% 94.6% 92.5%
  • Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Early 100% 100% 100% 100% 100% 1 month later 40°C 50.5% 61.5% 68.8% 64.8%
  • Example 11 At the first visit, after wiping the test site with 70% ethanol and drying, 15 ⁇ l of the cosmetic composition of Example 11, Example 12 or Example 13 was applied to the back of the subject in a Finn chamber and fixed with plaster.
  • the skin reaction of the test site was visually assessed by a dermatologist 30 minutes after the patch was removed.
  • the skin reaction of the test site was visually evaluated by a dermatologist.
  • the stimulation index was calculated by calculating the scores of the subjects determined at the 2nd, 3rd and 4th visits according to Equation 1 below.
  • the cosmetic composition of Example 11 had a stimulation index of 0.016
  • the cosmetic composition of Example 12 had a stimulation index of 0.021
  • the cosmetic composition of Example 13 had a stimulation index of 0.016, and all were determined to be non-irritating.
  • Example 11 At visit 1, the cosmetic composition of Example 11, Example 12 or Example 13 was applied to the face. Then, facial pictures were taken using a VISIA®CR (Canfield, USA). One of the hyperpigmented lesions on the left and right sides of the facial area was found and marked on the photograph, and the melanin level (M-value) was measured using Mexameter® MX 18 (CK electronic GmbH, Germany).
  • Example 11 At visit 2 (two weeks after visit 1) and visit 3 (after 4 weeks from visit 1), the cosmetic composition of Example 11, Example 12 or Example 13 was applied as in the 1st visit. Then, facial photography was performed using VISIA®CR. Melanin levels in hyperpigmented lesions were measured with Mexameter® MX 18 at the same site as indicated at Visit 1.
  • a dermatologist evaluated the presence or absence of adverse reactions (irritating symptoms such as pruritus and erythema), and no special skin abnormalities occurred during the test period.
  • the degree of improvement in hyperpigmentation was calculated by calculating the melanin level measured at the first visit, the second visit and the third visit by Equation 2 below, and the results are shown in Table 14.

Abstract

La présente invention concerne une composition cosmétique comprenant : (i) de la vitamine C ; et (ii) au moins un type d'agent stabilisant choisi dans le groupe constitué par un extrait de myrte de citron, des fullerènes et de l'huile et des graisses. La composition de la présente invention a une stabilité élevée de vitamine C. Ainsi, la composition de la présente invention présente une excellente stabilité au stockage et peut ainsi conserver de manière stable les effets de la vitamine C pendant une longue période. De plus, la composition de la présente invention peut garantir une stabilité même lorsqu'elle contient une grande quantité de vitamine C.
PCT/KR2020/014311 2019-12-06 2020-10-20 Composition comprenant de la vitamine c WO2021112398A1 (fr)

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KR102455132B1 (ko) 2020-10-27 2022-10-18 (주)이시스코스메틱 레몬머틀 추출물이 포함된 화장료 조성물 및 그 제조 방법
KR102546787B1 (ko) * 2020-11-12 2023-06-23 주식회사 라피끄 순수비타민 c를 고함량 함유하는 화장료 조성물
KR102379257B1 (ko) * 2021-09-29 2022-03-28 코스맥스 주식회사 아스코르브산을 포함하는 유분산 고형 화장료 조성물 및 이의 제조 방법

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