WO2010085123A2 - Composition applicable à la peau et apte à améliorer la circulation sanguine et de dilater les vaisseaux sanguins - Google Patents

Composition applicable à la peau et apte à améliorer la circulation sanguine et de dilater les vaisseaux sanguins Download PDF

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WO2010085123A2
WO2010085123A2 PCT/KR2010/000441 KR2010000441W WO2010085123A2 WO 2010085123 A2 WO2010085123 A2 WO 2010085123A2 KR 2010000441 W KR2010000441 W KR 2010000441W WO 2010085123 A2 WO2010085123 A2 WO 2010085123A2
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extract
acid
composition
blood circulation
combination
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PCT/KR2010/000441
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English (en)
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WO2010085123A3 (fr
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Dong-Chan Kim
Sun Ok Kim
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Dong-Chan Kim
Sun Ok Kim
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Priority claimed from KR1020090067873A external-priority patent/KR101086504B1/ko
Application filed by Dong-Chan Kim, Sun Ok Kim filed Critical Dong-Chan Kim
Publication of WO2010085123A2 publication Critical patent/WO2010085123A2/fr
Publication of WO2010085123A3 publication Critical patent/WO2010085123A3/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • 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
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/41—Amines
    • A61K8/418—Amines containing nitro groups
    • 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
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • 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
    • 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
    • A61K8/678—Tocopherol, i.e. vitamin E
    • 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
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • 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
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth

Definitions

  • the present invention relates to a composition applicable to skin, useful in promoting blood circulation and vascular relaxation, comprising (1) one or more selected from the group consisting of a licorice root extract, a Curcuma longa extract, a grape extract, a grape seed oil, a grapefruit extract, a bamboo extract, a raspberry extract, a cinnamon extract, a Hovenia dulcis extract, a Japonica extract, an alder extract and a combination thereof; (2) one or more selected from the group consisting of ammonia, nitrite, nitroglycerlin, silver nitrate, magnesium nitrite, ammonium nitrate and a combination thereof; and (3) one or more selected from the group consisting of malic acid, hyaluronic acid, citric acid, vitamin C, tocopherol, aspartic acid, tartaric acid, succinic acid, retinol, glutamic acid, an acid additive and a combination thereof. Also, the present invention relates to a method for improving blood circulation and for
  • Blood circulation in the body is regulated by various factors. Among them are physical elements such as hematocrit, blood viscosity and shear stress around blood vessels, as well as lipid compositions in plasma and corpuscles (platelets). In a normal state, these factors are in homeostasis. In contrast, the interruption of the homeostasis by, for example, a disease such as diabetes, a drug, or smoking induces an excessive aggregation of plasma, platelets, erythrocytes, etc., giving rise to abnormal hemostasis, which blocks blood circulation.
  • blood circulation-improving agents exhibit the effects of delaying the aging of cells and organs, stimulating the growth and regeneration of cells, and alleviating the symptoms attributed to interruption in peripheral blood circulation, such as shoulder pain, neck pain, limb numbness and limb coldness, and the symptoms attributed to the interruption in blood circulation within the head, such as depilation.
  • a variety of medicines have been developed for improvement in blood circulation. However, most of them are in oral dosage forms, which are often difficult to take when the subject suffers from stomach upset, diarrhea, constipation, inappetence, abdominal distention, etc.
  • Adenylyl cyclase catalyzes the conversion of ATP to cAMP. Following the activation of adenylyl cyclase, the resulting cAMP stimulates protein kinase A and inhibits rho kinase, which results in the activation of myosin phosphatase, with the subsequent dephosphylation of myosin. Thus, the myosin is dissociated from the actin, relaxing the smooth muscle.
  • soluble Guanylyl cyclase catalyzes the conversion of ATP to cGMP.
  • the resulting cGMP stimulates protein kinase G, which results in the activation of myosin phosphatase.
  • myosin is dissociated from the actin, relaxing the smooth muscle.
  • an agent which activates adenylyl cyclase and guanylyl cyclase to induce cAMP and cGMP stimulation can be used in the relaxation of the smooth muscle.
  • currently available oral food and medicine products show side effects and must be taken for a long term in order to get a desired result. Further, there are few agents that promise their medicinal effects.
  • composition for dermal application activate adenylyl cyclase and gyanylyl cyclase to induce the production of cAMP and cGMP, thereby promoting blood circulation and vasodilation and are thus useful for the improvement of interruption in peripheral blood circulation, limb coldness, Raynaud's phenomenon, impotence, female sexual dysfunction, and depilation attributed to interruption in blood circulation to the head.
  • compositions for dermal application useful in blood circulation and vascular relaxation, comprising (1) one or more selected from the group consisting of a licorice root extract, a Curcuma longa extract, a grape extract, a grape seed oil, a grapefruit extract, a bamboo extract, a raspberry extract, a cinnamon extract, a Hovenia dulcis extract, a Japonica extract, an alder extract and a combination thereof; (2) one or more selected from the group consisting of ammonia, sodium nitrite, nitroglycerlin, silver nitrate, magnesium nitrite, ammonium nitrate and a combination thereof; and (3) one or more selected from the group consisting of malic acid, hyaluronic acid, citric acid, vitamin C, tocopherol, aspartic acid, tartaric acid, succinic acid, retinol, glutamic acid, an acid additive and a combination thereof.
  • composition of the present invention is useful for the treatment of interruption in peripheral blood circulation, limb coldness, Raynaud's phenomenon, impotence, female sexual dysfunction, and depilation attributed to interruption in blood circulation to the head.
  • FIG. 1 shows differences in the maintenance of gel solid state between a conventional gel and the gel of the present invention in a graph (a) and in photographs (b).
  • FIG. 2 shows differences in ability to adsorb active ingredients into the skin between of a conventional gel and the gel of the present invention at 30 min after the application thereof to the skin.
  • FIG. 3 is of photographs showing effects of a conventional gel and the gel of the present invention on blood circulation.
  • FIG. 4 shows a change in pulse height with vascular relaxation in the skin (a) and a pulse height analyzer (b).
  • FIG. 5 is of photographs showing the morphology of normal capillary vessels (a), an increase in blood circulation due to vasodilation (b), and a peripheral blood flow meter (INU Hi-Tek, Korea) (c).
  • FIG. 6 is of photographs showing body temperatures around the ear (a) and in the hand (b) before and after the application of the lotion of the present invention and a thermal imaging camera (FLIR Therma CAM TM, Sweden)(c).
  • FIG. 7 is a graph showing the production of cAMP by a control extract and by the extracts of the present invention.
  • FIG. 8 shows the effect of the composition of the present invention on membrane currents at K + channels.
  • Fig. 9 is of photographs showing peripheral blood around the scalp hair root, before(a), 10 min after(b) and 20 min after (c) the composition was applied to scalp.
  • the present invention pertains to a composition for dermal application, useful in blood circulation and vascular relaxation, comprising (1) one or more selected from the group consisting of a licorice root extract, a Curcuma longa extract, a grape extract, a grape seed oil, a grapefruit extract, a bamboo extract, a raspberry extract, a cinnamon extract, a Hovenia dulcis extract, a Japonica extract, an alder extract and a combination thereof; (2) one or more selected from the group consisting of ammonia, sodium nitrite, nitroglycerlin, silver nitrate, magnesium nitrite, ammonium nitrate and a combination thereof; and (3) one or more selected from the group consisting of malic acid, hyaluronic acid, citric acid, vitamin C, tocopherol, aspartic acid, tartaric acid, succinic acid, retinol, glutamic acid, an acid additive and a combination thereof.
  • the first ingredient of the composition according to the present invention functions to activate adenylyl cyclase to induce the production of cAMP and is one or more selected from the group consisting of a licorice root extract, a Curcuma longa extract, a grape extract, a grape seed oil, a grapefruit extract, a bamboo extract, a raspberry extract, a cinnamon extract, a Hovenia dulcis extract, a Japonica extract, an alder extract and a combination thereof.
  • this ingredient may be contained in an amount of from 2.0 to 20 % by weight based on the total weight of the composition.
  • Licorice is a perennial herb belonging to a legume. Its root is used as a material for sweeteners or for herb medicines. In addition, it is conventionally used for detoxication, anti-inflammation, irritation relief, wound healing, and allergy treatment.
  • Curcuma longa is a rhizomatous herbaceous perennial plant of the ginger family and is native to tropical South Asia such as India and Okinawa. It is used as a medicinal material with the effects of stimulating bile secretion and evacuation.
  • Curcumin the principal curcuminoid of Curcuma longa, is effective in the reduction of lipid and cholesterol levels in blood.
  • curcumin In vitro experiments and computer remodeling analysis of the present inventors showed that given methylation in the gel composition A or B of Example 1, curcumin further activates adenylyl cyclase so that the interaction between myosin and actin is interrupted to induce muscle relaxation.
  • Curcumin has the following structural formula:
  • curcumin Given methylation, curcumin has the following structural formula:
  • Grape useful in the present invention, is an alkaline food in which glucide, vitamins B1, B2 and C, tartaric acid, citric acid, pectin, potassium and iron are found in abundance. Showing a diuretic effect, potassium is useful in the treatment of edema and the promotion of blood circulation.
  • the glucide of grapes are in a readily digestible form so that it is effective for rapid recuperation from fatigue or of convalescent patients.
  • a grape extract or a grape seed oil may used.
  • a grapefruit extract may be used along with or instead of a grape extract.
  • a bamboo extract as used in the present invention, is known to regulate blood cholesterol by decreasing bad cholesterol while increasing good cholesterol as well as reducing a triglyceride level in blood.
  • the bamboo extract is useful for blood circulation because it functions to prevent excessive blood coagulation, improve the elasticity of the blood vessels, and heal wounds on the blood vessels.
  • a raspberry extract is abundant in phytoestrogen so that it is effective in preventing prostate cancer and pancreas cancer. Also, its abundant polyphenols play as scavengers of reactive oxygen species and make the blood vessels smooth, thus preventing the occurrence of diseases of adult people.
  • Cinnamon is a small evergreen tree belonging to the family Lauraceae, native to southern China and northern Vietnam. Its bark is used as an herb medicine with the effects of preventing blood discharge, platelet aggregation, and skin darkening.
  • a cinnamon extract is prescribed for cold, pain and convulsion thanks to its medicinal effects of perspiration, fever removal, peptic and antiemetic.
  • Hovenia dulcis is a hardy tree with large leaves, belonging to the family Rhamnaceae.
  • a Hovenia dulcis extract is known to protect and help recover the liver from substances such as alcohol. Particularly, it is effective in the treatment of hangover, such as headache, dizziness, foul breath, and thirst after drinking.
  • the composition of the present invention may contain an extract from the plant species japonica.
  • an extract from Swertia japonica and/or alder (Alnus japonica) may be used.
  • Swertia japonica is a biennial herb belonging to the family Gentianaceae among which are Swertiae Herba and Atractylodes macrocephala Koidzumi. The herb is known to stimulate the secretion of gastric juice.
  • Alder Alder (Alnus japonica) is a deciduous tree belonging to the family Betulaceae. Its extract is known to have the functions of mitigate hangover and detoxifying and protecting the liver from alcohol.
  • a solvent such as water, an organic solvent or a combination thereof
  • the extracts may be obtained simultaneously from a mixture of all the sources. Alternatively, the extracts may be mixed after they are individually prepared from respective sources in optimal conditions.
  • the extracts useful in the present invention may be obtained using typical methods known in the art or may be commercially available.
  • the plants are dried and pulverized.
  • a polar solvent such as water, lower alcohol of C1 ⁇ C4 (e.g., methanol, ethanol, butanol, etc.) or a mixture thereof the volume of which is 2- to 20-fold larger than the weight of the pulverized plant
  • extracts are prepared using an extraction method such as hot water extraction, cold precipitation, cold extraction under reflux, or ultrasonication.
  • the dried powder of the plants is added to water which is then heated at 70°C or higher, preferably at 80°C or higher and more preferably at 90°C or higher for 2 hrs and preferably for 3 hrs or longer, followed by filtration to afford an extract.
  • Higher temperatures reduce the time to heat, but may destroy effective ingredients.
  • lower temperatures may not guarantee the complete extraction of effective ingredients from the plants. Hence, it is important to control the heating temperature and time.
  • the extracts thus obtained may be used after being dried or as they are.
  • organic solvents useful in the extraction include alcohols such as methanol, ethanol, isopropanol and butanol, ethylene, acetone, ether, hexane, chloroform, ethyl acetate, DMF (N,N-dimethylformamide), DMSO (dimethylsulfoxide), and a combination thereof.
  • the plants are first finely pulverized.
  • a solvent such as water, a dehydrated or hydrated lower alcohol of C1 ⁇ C4, ethyl acetate, acetone or hexane is added in an amount of 2 to 20-volumes based on the weight of the pulverized plant, followed by heating at 40 ⁇ 100°C for 1 ⁇ 5 hrs in an extractor equipped with a condenser or by immersing at room temperature for 1 to 30 days.
  • the extraction mixture is filtered through a nylon membrane or using cold filtration to remove particles therefrom.
  • the extract thus obtained can be used as it is or may be freeze-dried, vacuum dried, hot-air dried or spray dried.
  • the alcohol concentrate may be suspended in water and fractioned with a non-polar solvent such as hexane, chloroform or ethylacetate to give a fraction useful in the present invention.
  • a non-polar solvent such as hexane, chloroform or ethylacetate
  • the fraction may be further purified through silica gel column chromatography with a mixture of a polar solvent such as methanol, ethanol, propanol or isopropanol and non-polar solvent such as ethyl acetate, hexane, dichloromethane or chloroform serving as a mobile phase, so as to isolate active ingredients effective for blood circulation and vascular relaxation.
  • a polar solvent such as methanol, ethanol, propanol or isopropanol
  • non-polar solvent such as ethyl acetate, hexane, dichloromethane or chloroform serving as a mobile phase, so as to isolate active ingredients effective for blood circulation and vascular relaxation.
  • the second ingredient of the composition according to the present invention functions to activate guanylyl cyclase to induce the production of cGMP and is one or more selected from the group consisting of ammonia, sodium nitrite such as potassium nitrite or sodium nitrite, nitroglycerin, silver nitrate, magnesium nitrite, ammonium nitrate and a combination thereof.
  • this ingredient may be contained in an amount of from 2.0 to 20 % by weight based on the total weight of the composition.
  • the third ingredient of the composition according to the present invention is one or more acid selected from the group consisting of malic acid, hyaluronic acid, citric acid, vitamin C, tocopherol, aspartic acid, tartaric acid, succinic acid, retinol, glutamic acid, an acid additive and a combination thereof.
  • this ingredient may be contained in an amount of from 2.0 to 20 % by weight based on the total weight of the composition.
  • the composition of the present invention is preferably in the form of a lotion or gel. Because most of the conventional agents for improving blood circulation are in oral dosage forms, they are often difficult to take when the subject suffers from stomach unpleasantness, diarrhea, constipation, inappetence, abdominal distention, etc. If they have an acidic ingredient, the currently used gels or lotions are readily to liquefy so that their ingredients diffuse into the air.
  • xanthan gum is used to overcome the drawbacks of the conventional gel or lotion composition.
  • xanthan gum functions to maintain the integrity of the gel or lotion for a long period of time and to stabilize the ingredients, so that they stably remain on the skin and continuously penetrate into the skin (see FIG. 1).
  • xanthan gum is contained in an amount of from 0.1 to 2.0 % by weight based on the total weight of the composition of the present invention.
  • Xanthan gum is produced by fermentation of glucose by the pathogenic bacterium Xanthomonas campestris .
  • Xanthan gum is a polysaccharide consisting of a main chain of ⁇ -(1->4)-glucan frequently with a side chain composed of mannose and glucuronic acid at a ratio of 2:2:2 mannose: glucose: glucuronic acid.
  • xanthan gum is prepared as an odorless, white or creamy powder which is soluble in water but not in ethanol or ether. Because it is highly viscous when dissolved, xanthan gum is used as a suspending agent, a stabilizer and an emulsifier in cosmetics and foods.
  • a preferred embodiment of the present invention is a composition comprising of xanthan gum optionally in combination with glycerin which allows the active ingredients to remain on the skin for a long period of time and to continuously penetrate into the skin, thereby improving blood circulation and vascular relaxation.
  • composition of the present invention may further comprise one or more selected from the group consisting of animal fat, vegetable fat, lipid, wax, paraffin, starch, tragacanth, cellulose derivatives, polyethylene glycol, silicon, bentonite, silica, talc, zinc oxide, allantoin, dipotassium glycyrrhizate, glycereth-26, glucose, and a combination thereof as a structural ingredient for gel or lotion.
  • composition of the present invention may further comprise a transdermal penetration enhancer.
  • transdermal penetration enhancer is intended to refer to an agent which helps a desired ingredient penetrate into vascular endothelial cells at a high rate.
  • lecithin, phospholipids or liposomes serve as transdermal penetration enhancers in cosmetics.
  • composition of the present invention may further comprise an oil selected from the group consisting of vegetable oil, mineral oil, silicon oil, synthetic oil and a combination thereof.
  • oil useful in the present invention include mineral oil, cyclomethicone, squalane, octyldodecyl myristate, olive oil, vitis vinifera seed oil, macadamia nut oil, glyceryloctanoate, castor oil, ethylhexyl isononanoate, dimethicone, cyclopentasiloxane, and sunflower seed oil.
  • a surfactant and/or a higher alcohol may be contained in an amount of from 0.1 to 5 % by weight in the composition of the present invention.
  • the surfactant useful in the present invention may be a typical one such as a non-ionic surfactant, an anionic surfactant, a cationic surfactant, an amphiphatic surfactant, and phospholipid.
  • surfactant examples include sorbitan sesquioleate, polysorbate 60, glyceryl stearate, lipophilic glycerylstearate, sorbitan oleate, sorbitan stearate, DEA-cetylphosphate, sorbitan stearate/sucrose cocoate, glycerylstearate/polyethylene glycol-100 stearate, ceteareth-6 olivate, arachidiylalcohol/vehenylalcohol/arachidyl glycoside, and polypropyleneglycol-26-buteth-26/polyethylene glycol-40 hydrogenated caster oil.
  • the higher alcohol useful in the present invention has 12 to 20 carbon atoms in length. It may be selected from the group consisting of cetyl alcohol, stearyl alcohol, octyldodecanol, isostearyl alcohol and a combination thereof.
  • a thickener may be added in an amount of from 0.001 to 5 % by weight. It is selected from a group consisting of carbomer, xanthan gum, bentonite, magnesiumaluminum silicate, cellulose gum, dextrin palmitate and a combination thereof.
  • composition of the present invention may further comprise cosmetically active ingredients such as higher fatty acid and vitamins, an antioxidant (butylhydroxyanisole, propyl gallate, erythorbic acid, tocopherylacetate, butyrated hydroxytoluene, etc.), a preservative (methylparaben, butylparaben, propylparaben, phenoxyethanol, imidazolidinylurea, chlorphensin, etc.), a colorant, a pH adjuster (triethanolamine, citric acid, sodium citrate, malic acid, sodium malate, fumaric acid, sodium fumarate, succinic acid, sodium succinate, sodium hydroxide, sodium hydrogen phosphate, etc.), a moisturizing agent (glycerin, sorbitol, propylene glycol, butyrene glycol, hexylene glycol, diglycerin, betain, glycereth-26, methylgluces-20, etc.), and a lubricant.
  • composition of the present invention may further comprise essential ingredients for the skin, an aromatic, whether natural or synthetic, and other additives.
  • composition of the present invention is safe to the skin.
  • composition of the present invention functions to improve blood circulation and vascular relaxation. Thus, it is useful in the improvement of interruption in peripheral blood circulation, limb coldness, Raynaud's phenomenon, impotence, female sexual dysfunction, and depilation attributed to interruption in blood circulation to the head.
  • composition of the present invention shows the promotion of hair regrowth or the prevention of hair loss.
  • promotion of hair regrowth and “prevention of hair loss” are intended to have the same meaning.
  • the composition of the present invention was found to activate K + channels as measured through a patch clamp technique in which membrane currents at K + channels were increased in the presence of the composition as shown in the following examples (FIG. 8).
  • This is attributed to the fact that the composition of the present invention stimulates cAMP to activate protein kinase G which leads to the phosphorylation of K + channels.
  • membrane currents are induced at the activated channels.
  • SUR sulfonylurea receptor
  • the present invention pertains to a method for improving blood circulation and for enlarging blood vessels, comprising applying the composition to the skin.
  • the composition of the present invention promotes blood circulation at peripheral vessels and improves blood circulation across the body to prevent limb coldness and a decrease in body temperature.
  • Glycerin, xanthan gum, allantoin, dipotassium glycyrrhizate, Glycereth-26, glucose, a Curcuma longa extract, a grape extract, a bamboo extract, hyaluronic acid, nitrous acid (sodium salt), tocopherol, aspartic acid, citric acid and methylparaben were mixed at a predetermined ratio using a stirrer or mixer under an aseptic condition and then heated at 50 ⁇ 100°C to give preparation #1.
  • Glycerin, xanthan gum, allantoin, dipotassium glycyrrhizate, glycereth-26, a licorice root extract, a Raspberry extract, a cinnamon extract, a Hovenia dulcis extract, a Japonica extract, phosphatidylcholine lipoid, retinol, chrysin, nitrous acid (sodium salt), aspartic acid, citric acid and methylparaben were mixed at a predetermined ratio using a stirrer or mixer under an aseptic condition and heated at 50 ⁇ 100°C to give preparation #1.
  • Xanthan gum, glycerin, sodium nitrite, citric acid (trace), tocopherol, a Curcuma longa extract and a bamboo extract were mixed at a predetermined ratio with a suitable amount of water using a stirrer or mixer under an aseptic condition, heated at 50 ⁇ 100°C, emulsified and cooled to 50°C, followed by adding an aromatic and cooling to 30°C to afford gel composition A.
  • Xanthan gum glycerin, chrysin, retinol, an acid (ascorbic acid, glutamic acid), sodium nitrite (trace), citric acid (trace), tocopherol, a Curcuma longa extract and a bamboo extract mixed at a predetermined ratio with distilled water using a stirrer or mixer under an aseptic condition, heated at 50 ⁇ 100°C, emulsified and cooled to 50°C, followed by adding an aromatic and cooling to 30°C.
  • xanthan gum gel was assayed for suitability as a trap material.
  • Carbopol gel; Cabopol gel and materials; Trans gel; Trans gel and materials; Xanthan gum gel; Xanthan gum gel and materials; KY gel; and KY gel and materials were analyzed for maintenance (%) of materials in gel solid state.
  • Carbopol and TEA gel were observed for maintenance in solid state.
  • the Carbopol and TEA gel was observed to sustain its structure in the absence of the materials, but to rapidly collapse in the presence of the materials.
  • the structure of the xanthan gum and glycerin remained unchanged irrespective of the presence of the materials, indicating that xanthan gum makes a great contribution to resistance to acid (FIG. 1b).
  • the gel or lotion compositions according to the present invention were assayed for vascular relaxation. In this regard, 30 min after the gel composition prepared in Example 1 and a control gel composition were applied thereto, the respective hands were analyzed for peripheral vascular expansion.
  • Age two persons in their twenties, four persons in their thirties, one person in his forties, two persons in their fifties
  • Age two persons in their twenties, two persons in their thirties, two persons in their forties
  • the subjects to which the gel composition of the present invention were applied kept their hands in red colors whereas the hands of the subject in the control group turned pale in color due to vascular contraction, implying that the gel or lotion compositions according to the present invention have greater ability to moisturize the skin and penetrate active ingredients into the skin than do the control composition (FIG. 2).
  • the gel compositions according to the present invention were measured for effect on blood circulation. Subjects were observed for dermal color and analyzed for pulse height using a pulse height analyzer (FIG. 4b) before and 5 min after the gel composition prepared in Example 1 was applied thereto.
  • a pulse height analyzer FIG. 4b
  • Age two persons in their twenties, eight persons in their thirties, four persons in their forties
  • the gel compositions according to the present invention were evaluated for effects on blood circulation and vascular relaxation.
  • a capillary blood flow-measuring system FIG. 5c
  • an examination was made of peripheral blood flow through capillary vessels before and 5 min after the application of the gel composition prepared in Example 1 to the hands.
  • Age four persons in their thirties, two persons in their forties, four persons in their fifties
  • FIG. 5a shows the morphology of normal capillary vessels and their morphological changes.
  • a definite increase in blood flow was observed in the subjects 5 min after the gel composition according to the present invention was applied thereto, as shown in FIG. 5b, in comparison with the subjects before the application.
  • the picture of FIG. 5b which shows an increase in blood flow through capillary vessels was taken of the subject in his fifties who suffered from hyperlipidemia.
  • the lotion compositions according to the present invention were evaluated for ability to induce vasodilation.
  • the composition prepared in Example 1 was applied in an amount of 1 g to each the ear and the hand, followed by monitoring thermal changes using a thermal imaging camera.
  • the body heat from the subject was increased after the application of the lotion composition of the present invention, in comparison with that measured before the application (FIG. 6a).
  • the hand of the subject who suffered from limb coldness was observed to increase in temperature after the application of the lotion composition of the present invention thereto (FIG. 6b).
  • the extracts used in the gel or lotion composition of the present invention were assayed for ability to produce cAMP.
  • human embryonic kidney cells were treated with 1 ⁇ M of the adenylyl cyclase activator forskolin (control), 1 mg/ml of a Curcuma longa extract, and 1 mg/ml of a mixture of a Curcuma longa extract, a bamboo extract and a japonica extract, followed by the measurement of cAMP level.
  • HEK cells were stimulated for 20 min with an agonist in the presence of the phosphodiesterase inhibitor Ro 20-1724 (5 ⁇ M), followed by terminating the reaction by three cycles of freezing and thawing.
  • the sample thus obtained was centrifuged for 4 min at 12,000x g, 4°C according to the method of Brown et al.
  • Adenylyl cyclase activity was assessed by measurement of cAMP levels in the HEK cells using a specific cAMP-binding protein isolated from bovine adrenal cortex to detect cellular cAMP by competition with a standard amount of 3 H-labeled cAMP. Bound 3 H-cAMP present in the supernatant was quantitatively analyzed using a liquid scintillation counter.
  • cAMP production was increased by 25% upon treatment with the Curcuma longa extract and by 50% upon treatment with the mixture of the Curcuma longa extract, the bamboo extract and the japonica extract, in comparison with the control forskolin (FIG. 7).
  • EXAMPLE 8 Ability of the Composition to Promote Hair Regrowth or to Prevent Hair Loss I
  • composition according to the present invention activates the K + channel responsible for the activity of hair follicles.
  • composition A was used in an amount of 0.1 mg/ml as an effector while pinacidil (50 ⁇ M) served as a K + channel opener in myocytes.
  • compositions of the present invention activated K + channels. That is, the compositions of the present invention stimulate cAMP and cGMP to activate protein kinase G which leads to the phosphorylation of K + channels. This mechanism is also found in the activation of SUR (sulfonylurea receptor) 2B K + channels. Showing an activity to activate K+ channels, therefore, the compositions of the present invention are effective for the promotion of hair regrowth or the prevention of hair loss.
  • SUR sulfonylurea receptor
  • composition (A) of Example 1-1 and 3g of composition (B) of Example 1-2 were combined and mixed to produce the test composition.
  • a concentration of peripheral blood around the hair root was low, and thickness, color and density of visible peripheral blood vessels was very low (Fig 9a).
  • a peripheral blood around the hair root was highly concentrated and had an increased thickness and density in comparison with those of the subjects before the application (Fig. 9).
  • the study is designed to evaluate the dermal irritancy contact with intact skin of rabbits.
  • This test system is recommended by ISO 10993-10 : Biological Evaluation of Medical Devices-Part 10L Tests for Irritation and Delayed-type Hypersensitivity .
  • the negative control vehicle sterile water
  • each patch was placed on either side of the rabbit's spine, in the opposite fashion as the test sample preparation (one caudally and one cranially).
  • Each patch was secured to each of the 4 sites using an elastic bandage covered by adhesive tape or stockinet. Bandages remained in place for 24 hours and were removed.
  • the test and control sites were rinsed with lukewarm water to remove any residual matter.
  • the sites exposed to the test article were examined for signs of dermal irritancy at 1, 24, 48, and 72 hours after patch removal. The observations were rated on an numerical scale using the scoring system in below Table 1 (Scoring Criteria) and Table 2(Primary Irritation Response Categories).
  • the mean skin reaction score was calculated by adding together the scores for the test material for erythema and edema at the 24, 48, and 72 hour points and dividing by six.
  • the mean for the vehicle controls were calculated in the same manner.
  • the vehicle control mean score is subtracted from the test material mean score to obtain the Primary Irritation score. All the scores for each animal were added and the sum was then divided by the number of animals (3) to obtain the Primary Irritation Index.
  • test material elicited a negligible Primary Irritation Response with a Primary Irritation Index of 0.4, as shown in Table 3(Primary Irritation Test Results). All raw data, documentation, protocols and final reports generated for this study are retained in the archives for a minimum of five (5) years at Ethox International, Inc., STS Life Sciences Division, 7500 West Henrietta Road, Rush, New York 14543.
  • Score is sum of erythema and edema 24, 48 and 72 hour scores/6

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Abstract

La présente invention porte sur une composition pour application dermique, utile pour favoriser la circulation sanguine et la relaxation vasculaire. Elle comprend (1) un ou plusieurs éléments choisis dans le groupe constitué par un extrait de racine de réglisse, un extrait de Curcuma longa, un extrait de raisin, une huile de pépin de raisin, un extrait de pomelo, un extrait de bambou, un extrait de framboise, un extrait de cannelle, un extrait de Hovenia dulcis, un extrait de Japonica, un extrait d'aulne, et une combinaison de ceux-ci ; (2) un ou plusieurs éléments choisis dans le groupe constitué par l'ammoniac, le nitrite de sodium, la nitroglycérine, le nitrate d'argent, le nitrite de magnésium, le nitrate d'ammonium et une combinaison de ceux-ci ; et (3) un ou plusieurs éléments choisis dans le groupe constitué par l'acide malique, l'acide hyaluronique, l'acide citrique, la vitamine C, le tocophérol, l'acide aspartique, l'acide tartrique, l'acide succinique, le rétinol, l'acide glutamique, et additif acide et une combinaison de ceux-ci. L'invention porte sur une méthode permettant d'améliorer la circulation sanguine et de dilater les vaisseaux sanguins par application de la composition sur la peau.
PCT/KR2010/000441 2009-01-22 2010-01-22 Composition applicable à la peau et apte à améliorer la circulation sanguine et de dilater les vaisseaux sanguins WO2010085123A2 (fr)

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KR20090005301 2009-01-22
KR10-2009-0005301 2009-01-22
KR1020090067873A KR101086504B1 (ko) 2009-01-22 2009-07-24 혈행개선 및 혈관확장 기능을 가지는 피부 도포용 조성물
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140031311A1 (en) * 2012-01-18 2014-01-30 Edward M. Lichten Treatment of reynaud's disease
US11253545B2 (en) 2019-05-24 2022-02-22 Brian Brazzo Compositions comprising silver nitrate, hyaluronic acid and allantoin and methods for use thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000201650A (ja) * 1999-01-12 2000-07-25 Kyowa Hakko Kogyo Co Ltd 育毛食品および経口育毛剤
JP2006282597A (ja) * 2005-03-31 2006-10-19 Naris Cosmetics Co Ltd 毛乳頭細胞増殖促進剤、血管内皮増殖因子（ｖｅｇｆ）産生促進剤、養毛・育毛剤
KR100794447B1 (ko) * 2005-12-12 2008-01-16 남종현 발모촉진제 및 그의 제조방법

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000201650A (ja) * 1999-01-12 2000-07-25 Kyowa Hakko Kogyo Co Ltd 育毛食品および経口育毛剤
JP2006282597A (ja) * 2005-03-31 2006-10-19 Naris Cosmetics Co Ltd 毛乳頭細胞増殖促進剤、血管内皮増殖因子（ｖｅｇｆ）産生促進剤、養毛・育毛剤
KR100794447B1 (ko) * 2005-12-12 2008-01-16 남종현 발모촉진제 및 그의 제조방법

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140031311A1 (en) * 2012-01-18 2014-01-30 Edward M. Lichten Treatment of reynaud's disease
US8835406B2 (en) * 2012-01-18 2014-09-16 Edward M. Lichten Treatment of reynaud's disease
US11253545B2 (en) 2019-05-24 2022-02-22 Brian Brazzo Compositions comprising silver nitrate, hyaluronic acid and allantoin and methods for use thereof

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