WO2015022909A1 - Ghg-containing composition and fat absorption inhibitor using same - Google Patents

Ghg-containing composition and fat absorption inhibitor using same Download PDF

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Publication number
WO2015022909A1
WO2015022909A1 PCT/JP2014/070974 JP2014070974W WO2015022909A1 WO 2015022909 A1 WO2015022909 A1 WO 2015022909A1 JP 2014070974 W JP2014070974 W JP 2014070974W WO 2015022909 A1 WO2015022909 A1 WO 2015022909A1
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Prior art keywords
extract
ghg
acid
oil
purple tea
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PCT/JP2014/070974
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French (fr)
Japanese (ja)
Inventor
崇 嘉手苅
下田 博司
村井 弘道
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オリザ油化株式会社
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Publication of WO2015022909A1 publication Critical patent/WO2015022909A1/en

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    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L2/00Non-alcoholic beverages; Dry compositions or concentrates therefor; Their preparation
    • A23L2/52Adding ingredients
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105Plant extracts, their artificial duplicates or their derivatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7024Esters of saccharides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/82Theaceae (Tea family), e.g. camellia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/06Preparations for care of the skin for countering cellulitis
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23VINDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00Food compositions, function of food ingredients or processes for food or foodstuffs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2236/00Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/92Oral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/10Washing or bathing preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • A61Q5/02Preparations for cleaning the hair
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • A61Q5/12Preparations containing hair conditioners

Definitions

  • the present invention relates to a composition which is derived from a plant and contains GHG at a high concentration, and a fat absorption inhibitor using the composition.
  • the present invention is widely used for pharmaceuticals, foods and drinks, cosmetics, and the like.
  • GHG 1,2-di-O-galloyl-4,6-O- (S) -hexahydroxydiphenoyl-b-D-glucose
  • SOD 2 1,2-di-O-galloyl-4,6-O- (S) -hexahydroxydiphenoyl-b-D-glucose
  • Non-patent document 1 Non-patent document 2, Non-patent document 3
  • GHG is blended in food and drink such as functional foods and health foods, it is preferably derived from natural products from the general concept of food safety.
  • a conventionally known natural product containing GHG has a low content, and only a very low content GHG composition can be obtained.
  • even if it is contained in a high concentration it is difficult to obtain a high concentration GHG composition because it is a wild species that is not suitable for cultivation and is difficult to obtain.
  • Hyperlipidemia in which blood neutral fat has exceeded normal levels, have increased rapidly due to overeating, lack of exercise, and increased intake of animal fat.
  • Hyperlipidemia is known to cause diseases such as arteriosclerosis, hypertension, myocardial infarction, and cerebrovascular disorder. To prevent these diseases, an increase in the amount of neutral fat in the blood is caused. It is important for modern people to suppress and even lower the elevated blood neutral fat content to the normal range. Therefore, it is desired to develop an edible material that can be ingested or administered on a daily basis and is effective in adjusting the neutral fat in the blood. As such a material, for example, an extract of bitter gourd is known (Patent Document 1).
  • an object of the present invention is to provide a GHG-containing composition that is a natural product-derived composition containing a high concentration of GHG, and a method for producing the same. Furthermore, it aims at providing the fat absorption inhibitor which uses a novel plant or its extract as an active ingredient.
  • a GHG-containing composition obtained from Kenya purple tea (scientific name: Camellia sinensis, variety TRFK306) and containing GHG.
  • a GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306) and containing 3 to 10% by mass of GHG.
  • a GHG-containing composition characterized in that a Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306) is immersed in a polar solvent (including water), and then heated to reflux to extract GHG in the solvent. Production method. 4).
  • a fat absorption inhibitor containing Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306) and / or its extract as an active ingredient. 5.
  • a fat absorption inhibitor comprising as an active ingredient a GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306). 6).
  • a weight gain inhibitor comprising as an active ingredient a GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306). 7).
  • a method for inhibiting fat absorption of a human by administering to the human a GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306). 8).
  • a method for suppressing weight gain of a human by administering a GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306) to the human.
  • FIG. 2A and FIG. 2B are graphs showing the effects of purple tea extract and orlistat on the blood triglyceride elevation inhibitory effect of purple tea extract of this Example on the effect on blood triglyceride elevation in olive oil-loaded mice. It is. It is a graph which shows the inhibitory effect which acts on the weight gain in the high fat diet-fed mouse
  • the GHG-containing composition of the present invention is a composition obtained from Kenyan purple tea (scientific name: Camelliasinensis, variety name TRFK306, hereinafter simply referred to as “purple tea”), and comprises 3 to 99% by mass of GHG. Contains by content. The shape may be liquid, solid, semi-solid, gel, etc. The solid content of GHG is preferably 3 to 99% by mass. In order to improve the productivity, it is preferably 3 to 30% by mass, and more preferably 3 to 10% by mass. In particular, a GHG-containing composition containing GHG at a content of 3 to 10% by mass can be efficiently obtained by the production method described below.
  • GHG is represented by the following chemical formula (1).
  • Purple tea is a tea tree developed by mating by the Kenyan government and is named variety name TRFK306.
  • the tea leaves of TRFK306 contain anthocyanins and are purple due to this, so they are commonly called “purple tea” or “purple tea”.
  • the present inventors have found that TRFK306 contains a specific component, GHG, at a high concentration.
  • the site of purple tea used in the GHG-containing composition of the present invention is not particularly limited, and leaves, stems, roots, flowers, seeds and the like can be used, but it is particularly preferable to use leaves. This is because a higher concentration of GHG can be obtained.
  • the GHG-containing composition of the present invention preferably comprises, for example, pulverized raw or dried purple tea leaves (hereinafter referred to as “purple tea leaves”) and a polar solvent (including water; the same shall apply hereinafter). ) Can be used for extraction.
  • the purple tea leaves may be appropriately subjected to chemical treatment such as acid or alkali decomposition, enzyme decomposition, etc., and then extracted.
  • the GHG-containing composition can be produced by the method described below. That is, first, as the purple tea leaves, raw or dried purple tea leaves are subjected to chemical treatment such as acid or alkali decomposition, enzyme decomposition or the like.
  • a polar solvent is added to the purple tea leaves and shaken or heated to reflux to extract GHG in the solvent.
  • the said polar solvent is not specifically limited, Water, alcohol, and ketones can be used. These may be used alone or in combination of two or more. Further, among these, it is particularly preferable to use a hydrous alcohol or a hydrous ketone.
  • hydrous alcohol solvent a hydrous solvent such as ethanol, methanol, propanol or the like can be used, and hydrous ethanol is particularly preferable.
  • hydrous ketone solvent hydrous solvents such as acetone, methyl ethyl ketone, diethyl ketone, chloroacetone and the like can be used, and hydrous acetone is particularly preferable.
  • the water content is preferably 20 to 99.9% by mass of ethanol, more preferably 30 to 99% by mass, most preferably 40 to 80% by mass in the case of hydrous ethanol. preferable.
  • hydrous acetone it preferably contains 20 to 99.9% by mass of acetone. This is because the above range is excellent in GHG extraction efficiency.
  • 80% by mass ethanol containing 20% by mass is described as “80% water-containing ethanol”.
  • the heating and refluxing can be performed by a known method using the above-mentioned hydroalcoholic solvent or hydrous ketone solvent.
  • the heating temperature is preferably about 30 to 95 ° C.
  • the reflux time is preferably about 1 to 4 hours.
  • the solvent is distilled off under reduced pressure after extraction. According to this, it is possible to make a composition that does not contain an organic solvent, and it can be adapted to safety standards as a food material for blending into foods and drinks such as functional foods and health foods. is there.
  • stepwise extraction can be performed with a plurality of solvents.
  • the GHG containing composition which contains GHG in high concentration can be manufactured with a sufficient yield.
  • purple tea leaves are added with one of the above hydrous alcohol solvent and the above hydrous ketone solvent, shaken or heated to reflux, and GHG is extracted into the solvent to obtain the first extract.
  • the extract is separated into an extract and a residue not recovered as the extract by centrifugation or the like, and the other unselected solvent is added to the residue, and the mixture is shaken or heated to reflux.
  • GHG is extracted to obtain a second extract.
  • the first extract and the second extract are mixed.
  • the second extract alone can be used as an extract of purple tea leaves.
  • purple tea leaves are subjected to the first extraction treatment with the above-mentioned hydrous alcohol solvent or the above hydrous ketone solvent, thereby extracting characteristics such as physical properties.
  • the other extraction solvent is used in the subsequent second extraction process. Even so, the extraction efficiency can be expected to be improved.
  • the extract obtained by the above method can be used as it is or concentrated to obtain a liquid GHG-containing composition. Furthermore, it can be pulverized by freeze-drying or spray-drying to obtain a powdery composition as a GHG-containing composition. Moreover, it is not limited to these forms.
  • the insoluble matter contained in the extract can be appropriately removed by filtration or the like. The insoluble material may be further pulverized into fine particles.
  • the primary extract from purple tea leaves obtained as described above is fractionated and purified using GHG as an index by ion exchange, size exclusion column chromatography, HPLC, gel filtration, membrane separation, etc. This can also be used as a GHG-containing composition.
  • the GHG-containing composition of the present invention may be added to a pharmaceutically acceptable base or carrier, if necessary, such as tablets, granules, powders, solutions, powders, granules, capsules, jelly-forms, etc. It can be used in the form.
  • the fat absorption inhibitor or weight gain inhibitor of the present invention comprises a GHG-containing composition obtained from purple tea as an active ingredient.
  • the fat absorption inhibitor or weight gain inhibitor of the present invention contains purple tea and / or an extract thereof as an active ingredient. Furthermore, when using an extract of purple tea as the fat absorption inhibitor or weight gain inhibitor of the present invention, the extract can be obtained by the same method as the GHG-containing composition described above.
  • the GHG-containing composition, fat absorption inhibitor and weight gain inhibitor (hereinafter simply referred to as “the present composition”) of the present invention can be used as materials for various foods and drinks.
  • the food and drink include edible oil (salad oil), confectionery (gum, candy, caramel, chocolate, cookie, snack, jelly, gummy, tablet confection etc.), noodles (soba, udon, ramen etc.), and dairy products ( Milk, ice cream, yogurt, etc.), seasonings (miso, soy sauce, etc.), soups, beverages (juice, coffee, tea, tea, carbonated drinks, sports drinks, etc.) and health foods (tablets , Capsules, etc.) and nutritional supplements (nutrient drinks, etc.).
  • the composition or the like may be appropriately blended with these foods and drinks.
  • These foods and drinks can be blended with various ingredients depending on the type, for example, glucose, fructose, sucrose, maltose, sorbitol, stevioside, corn syrup, lactose, citric acid, tartaric acid, malic acid, succinic acid.
  • Acid lactic acid, L-ascorbic acid, dl- ⁇ -tocopherol, sodium erythorbate, glycerin, propylene glycol, glycerin fatty acid ester, polyglycerin fatty acid ester, sucrose fatty acid ester, sorbitan fatty acid ester, propylene glycol fatty acid ester, gum arabic, Food materials such as carrageenan, casein, gelatin, pectin, agar, vitamin Bs, nicotinic acid amide, calcium pantothenate, amino acids, calcium salts, pigments, fragrances and preservatives can be used.
  • this composition having a health maintenance function includes other antioxidants and health food ingredients such as antioxidants, reduced ascorbic acid (vitamin C), vitamin E, reduced glutatin. , Tocotrienol, vitamin A derivative, lycopene, ⁇ -cryptoxanthin, astaxanthin, zeaxanthin, fucoxanthin, uric acid, ubiquinone, coenzyme Q10, folic acid, garlic extract, allicin, sezamin, lignans, catechin, isoflavone, chalcone, tannins, flavonoids , Coumarin, isocoumarins, blueberry extract, arbutin, tannin, anthocyanin, apple polyphenol, grape seed extract, ellagic acid, kojic acid, surge extract health food material, V.
  • antioxidants reduced ascorbic acid (vitamin C)
  • vitamin E reduced glutatin.
  • Tocotrienol vitamin A derivative
  • lycopene ⁇ -cryptoxanthin
  • astaxanthin ze
  • vitamin A V.B1, V.B2 , V.B6, V.B12, VC, VD, VE, VP, Cori , Niacin, pantothenic acid, calcium folate, EPA, oligosaccharide, dietary fiber, squalene, soy lecithin, taurine, donariella, protein, octacosanol, DHA, egg yolk lecithin, linoleic acid, lactoferrin, magnesium, zinc, chromium, selenium, potassium , Heme iron, oyster meat extract, chitosan, chitin oligosaccharide, collagen, chondroitin, turmeric, licorice, kukoshi, keihi, hawthorn, ginger, ganoderma, swordfish extract, suppon, plantain, chamomile, chamomile, dandelion, hibiscus, honey, Boren, royal jelly, lime, lavender, rose
  • the present composition or the like is used as it is, and in the case of an extract, it is spray-dried or freeze-dried together with powdered dextrin, and this is easily converted into a powder, granule, tablet, or solution. ). If necessary, it can also be mixed with a binder such as gum arabic to form a powder or granules, and added to a solid food.
  • a binder such as gum arabic
  • this composition etc. as a raw material of a chemical
  • medical agent may be used for a human and may be used for mammals other than a human.
  • preparation raw material examples include, for example, excipients (glucose, lactose, sucrose, sodium chloride, starch, calcium carbonate, kaolin, crystalline cellulose, cocoa butter, hydrogenated vegetable oil, kaolin, talc, etc.), Binder (distilled water, physiological saline, ethanol water, simple syrup, glucose solution, starch solution, gelatin solution, carboxymethylcellulose, potassium phosphate, polyvinylpyrrolidone, etc.), disintegrant (sodium alginate, agar, sodium bicarbonate, carbonate Calcium, sodium lauryl sulfate, stearic acid monoglyceride, starch, lactose, gum arabic powder, gelatin, ethanol, etc.), disintegration inhibitors (sucrose, stearin, cocoa butter, hydrogenated oil, etc.), absorption accelerators (quaternary ammonium base) , Sodium lauryl sulfate, etc.), a
  • the administration method of this composition and the like can be generally administered orally in the form of tablets, pills, soft / hard capsules, fine granules, powders, granules and the like.
  • the water-soluble preparation can be administered orally as a liquid.
  • parenteral administration may be used.
  • the composition is dispersed in an appropriate solubilizing agent such as ethanol or water, and then applied in a dosage form such as a poultice, lotion, ointment, tincture or cream. be able to.
  • water-soluble preparations such as this composition can be used as they are or in the form of a poultice, lotion, ointment, tincture, cream, etc. with a dispersant, suspension, stabilizer, etc. added. Can be applied.
  • the dose may vary depending on the administration method, medical condition, age of the patient, etc., but for adults, it can usually be administered as 5 to 200 mg as an active ingredient per day, and for children it can usually be administered at about 0.5 to 100 mg.
  • the compounding ratio when using the composition or the like as a drug can be appropriately changed depending on the dosage form, but is usually about 0.01 to 10 wt% when administered orally or by mucosal absorption, parenterally. In the case of administration, it should be about 0.01 to 20 wt%. In addition, since the dose varies depending on various conditions, a dose smaller than the above dose may be sufficient, or it may be necessary to administer beyond the range.
  • the pharmaceutical composition may include other compounds that are commonly used in the pharmaceutical field and compounds that are necessary for molding into a form suitable for oral administration. Examples of such a compound include lactose, starch, hydroxypropylcellulose, kaolin, talc, calcium carbonate and the like.
  • compositions can also be used as cosmetics.
  • Cosmetic forms that can be blended with the present composition include, for example, emulsion, soap, face wash, bath preparation, cream, emulsion, lotion, eau de cologne, shave cream, shave lotion, cosmetic oil, tanning Stop Lotion, Funny Powder, Foundation, Perfume, Pack, Nail Cream, Enamel, Enamel Remover, Eyebrow, Blusher, Eye Cream, Eye Shadow, Mascara, Eyeliner, Lipstick, Lip Cream, Shampoo, Rinse, Hair Dye, Dispersion And cleaning fee.
  • the cosmetic material of the above-described form includes ingredients, oils, higher alcohols, fatty acids, ingredients blended in skin preparations such as cosmetics and quasi-drugs, as long as the effects thereof are not impaired Ultraviolet absorbers, powders, pigments, surfactants, polyhydric alcohols / sugars, polymers, physiologically active ingredients, solvents, antioxidants, fragrances, preservatives and the like can be blended. Examples are listed below, but the present invention is not limited to these examples.
  • Ester-based oil phase components glyceryl tri-2-ethylhexanoate, cetyl 2-ethylhexanoate, isopropyl myristate, butyl myristate, isopropyl palmitate, ethyl stearate, octyl palmitate, isostearic acid Isocetyl, butyl stearate, butyl myristate, ethyl linoleate, isopropyl linoleate, ethyl oleate, isocetyl myristate, isostearyl myristate, isostearyl palmitate, octyldodecyl myristate, isocetyl isostearate, diethyl sebacate, adipine Diisopropyl acid, isoaralkyl neopentanoate, glyceryl tri (capryl / capric)
  • Hydrocarbon oil phase components squalane, liquid paraffin, ⁇ -olefin oligomer, isoparaffin, ceresin, paraffin, liquid isoparaffin, polybutene, microcrystalline wax, petrolatum and the like.
  • Animal and vegetable oils and their hydrogenated oils, and naturally occurring waxes beef tallow, hydrogenated beef tallow, lard, hydrogenated tallow, horse oil, hydrogenated horse oil, mink oil, orange luffy oil, fish oil, hydrogenated fish oil, egg yolk oil and other animal oils and Its hardened oil, avocado oil, almond oil, olive oil, cacao butter, kiwi seed oil, apricot oil, kukui nut oil, sesame oil, wheat germ oil, rice germ oil, rice bran oil, safflower oil, shea butter, soybean oil, evening primrose oil , Perilla oil, tea seed oil, camellia oil, corn oil, rapeseed oil, hydrogenated rapeseed oil, palm kernel oil, hydrogenated palm kernel oil,
  • Silicone oil phase components dimethylpolysiloxane, methylphenylpolysiloxane, methylcyclopolysiloxane, octamethylpolysiloxane, decamethylpolysiloxane, dodecamethylcyclosiloxane, methylhydrogenpolysiloxane, polyether-modified organopolysiloxane, dimethyl Siloxane / methylcetyloxysiloxane copolymer, dimethylsiloxane / methylstearoxysiloxane copolymer, alkyl-modified organopolysiloxane, terminal-modified organopolysiloxane, amino-modified silicone oil, amino-modified organopolysiloxane, dimethiconol, silicone gel, acrylic Examples include silicone, trimethylsiloxysilicic acid, and silicone RTV rubber.
  • Fluorine oil phase components perfluoropolyether, fluorine-modified organopolysiloxane, fluorinated pitch, fluorocarbon, fluoroalcohol, fluoroalkyl / polyoxyalkylene co-modified organopolysiloxane, and the like.
  • Lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, isostearyl alcohol, oleyl alcohol, behenyl alcohol, 2-ethylhexanol, hexadecyl alcohol, octyldodecanol and the like can be mentioned.
  • fatty acids Caprylic acid, capric acid, undecylenic acid, lauric acid, myristic acid, palmitic acid, palmitoleic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, linolenic acid, arachidic acid, arachidonic acid, behenic acid , Erucic acid, 2-ethylhexanoic acid and the like.
  • UV absorbers Paraaminobenzoic acid, amyl paraaminobenzoate, ethyldihydroxypropyl paraaminobenzoate, glyceryl paraaminobenzoate, ethyl paraaminobenzoate, octyl paraaminobenzoate, octyldimethyl paraaminobenzoate, ethylene glycol salicylate, salicylic acid Octyl, triethanolamine salicylate, phenyl salicylate, butylphenyl salicylate, benzyl salicylate, homomenthyl salicylate, benzyl cinnamate, octyl paramethoxycinnamate, 2-ethylhexyl paramethoxycinnamate, mono-2-diparamethoxycinnamate Glyceryl ethylhexanoate, isopropyl paramethoxycinnamate, diethanolamine salt of paramethoxycinnam
  • these powders are conventionally known surface treatments such as fluorine compound treatment, silicone treatment, silicone resin treatment, pendant treatment, silane coupling agent treatment, titanium coupling agent treatment, oil agent treatment, N-acylated lysine treatment,
  • the surface treatment may or may not be performed in advance by polyacrylic acid treatment, metal soap treatment, amino acid treatment, lecithin treatment, inorganic compound treatment, plasma treatment, mechanochemical treatment or the like.
  • Anionic surfactant fatty acid soap, ⁇ -acyl sulfonate, alkyl sulfonate, alkyl allyl sulfonate, alkyl naphthalene sulfonate, alkyl sulfate, POE alkyl ether sulfate , Alkylamide sulfate, alkyl phosphate, POE alkyl phosphate, alkylamide phosphate, alkyloylalkyl taurine salt, N-acyl amino acid salt, POE alkyl ether carboxylate, alkyl sulfosuccinate, alkyl sulfoacetic acid Sodium, acylated hydrolyzed collagen peptide salt, perfluoroalkyl phosphate, etc.
  • Cationic surfactant alkyltrimethylammonium chloride, stearyltrimethylammonium chloride, stearyltrimethylammonium bromide, cetostearyltrimethylammonium chloride, distearyldimethylammonium chloride, stearyldimethylbenzylammonium chloride, behenyltrimethylammonium bromide, benzalkonium chloride , Behenic acid amidopropyldimethylhydroxypropylammonium chloride, stearic acid diethylaminoethylamide, stearic acid dimethylaminopropylamide, lanolin derivative quaternary ammonium salts, and the like.
  • Amphoteric surfactants carboxybetaine type, amide betaine type, sulfobetaine type, hydroxysulfobetaine type, amide sulfobetaine type, phosphobetaine type, aminocarboxylate type, imidazoline derivative type, amidoamine type and the like.
  • Nonionic surfactant propylene glycol fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, sorbitan fatty acid ester, POE sorbitan fatty acid ester, POE sorbitol fatty acid ester, POE glycerin fatty acid ester, POE alkyl ether, POE fatty acid ester, POE cured castor Oil, POE castor oil, POE / POP copolymer, POE / POP alkyl ether, polyether-modified silicone lauric acid alkanolamide, alkylamine oxide, hydrogenated soybean phospholipid, and the like.
  • Natural surfactant lecithin, saponin, sugar surfactant and the like.
  • polyhydric alcohols and sugars Ethylene glycol, diethylene glycol, polyethylene glycol, propylene glycol, dipropylene glycol, polypropylene glycol, glycerin, diglycerin, polyglycerin, 3-methyl-1,3-butanediol, 1, 3 -Butylene glycol, sorbitol, mannitol, raffinose, erythritol, glucose, sucrose, fructose, xylitol, lactose, maltose, maltitol, trehalose, alkylated trehalose, mixed isomerized sugar, sulfated trehalose, pullulan and the like. These chemically modified compounds can also be used.
  • Naturally derived polymer compounds such as galactan, gum karaya, gum tragacanth, alginic acid, albumin, casein, curdlan, gellan gum and dextran can also be suitably used.
  • physiologically active ingredients examples include substances that impart some physiological activity to the skin when applied to the skin. For example, whitening ingredients, immunostimulants, anti-aging agents, UV protection agents, slimming agents, tanning agents, antioxidants, hair growth agents, hair restorers, moisturizers, blood circulation promoters, antibacterial agents, bactericides, desiccants, A cooling sensation agent, a warming sensation agent, vitamins, an amino acid, a wound healing promoter, an irritation relaxation agent, an analgesic agent, a cell activator, an enzyme component, etc. are mentioned.
  • suitable ingredients include, for example, ashitaba extract, avocado extract, amateur extract,retea extract, arnica extract, aloe extract, apricot extract, apricot kernel extract, ginkgo biloba extract, fennel extract, turmeric extract, oolong tea extract, ages Extract, Echinacea leaf extract, Ogon extract, Oat extract, Oen extract, Barley extract, Hypericum extract, Oyster extract, Dutch mustard extract, Orange extract, Seawater dried product, Seaweed extract, Hydrolyzed elastin, Hydrolyzed wheat powder, Hydrolyzed silk , Chamomile extract, Carrot extract, Kawara mugwort extract, Licorice extract, Calcade extract, Oyster extract, Kina extract, Cucumber extract, Guanosine, Gardenia extract, Kumazasa extract, Clarae Kiss, walnut extract, grapefruit extract, clematis extract, chlorella extract, mulberry extract, gentian extract, tea extract, yeast extract, burdock extract, fermented rice bran extract
  • Biopolymers such as deoxyribonucleic acid, mucopolysaccharide, sodium hyaluronate, sodium chondroitin sulfate, collagen, elastin, chitin, chitosan, hydrolyzed eggshell membranes, amino acids, hydrolyzed peptides, sodium lactate, urea, sodium pyrrolidonecarboxylate , Moisturizing ingredients such as betaine, whey, trimethylglycine, oily ingredients such as sphingolipid, ceramide, phytosphingosine, cholesterol, cholesterol derivatives, phospholipids, ⁇ -aminocaproic acid, glycyrrhizic acid, ⁇ -glycyrrhetinic acid, lysozyme chloride, guaiazulene, Immunostimulants such as hydrocortisone, vitamin A, vitamin B2, vitamin B6, vitamin C, vitamin D, vitamin E, calcium pantothenate, biotin,
  • Cell activators such as ⁇ -oryzanol and vitamin E derivatives, wound healing agents such as retinol and retinol derivatives, arbutin, kojic acid, placenta extract, sulfur, ellagic acid, linoleic acid, tranexamic acid, glutathione, etc.
  • Whitening agent cephalanthin, licorice extract, red pepper tincture, hinokitiol, garlic iodide extract, pyridoxine hydrochloride, DL- ⁇ -tocopherol, DL- ⁇ -tocopherol acetate, nicotinic acid, nicotinic acid derivative, calcium pantothenate, D-pan Tothenyl alcohol, acetyl pantothenyl ethyl ether, biotin, allantoin, isopropylmethylphenol, estradiol, ethinyl estradiol, capronium chloride, benzalkonium chloride, diphenhydramine hydrochloride, takanal, camphor, salicylic acid, nonyl acid vanillylamide, nonanoic acid vanillylamide, pyroctone Olamine, glyceryl pentadecanoate, L-menthol, mononitroguaiacol, resorcin,
  • antioxidants Sodium bisulfite, sodium sulfite, erythorbic acid, sodium erythorbate, dilauryl thiodipropionate, tocopherol, tolyl biguanide, nordihydroguaiaretic acid, parahydroxyanisole, butylhydroxyanisole, dibutylhydroxy
  • plant extracts having an antioxidant effect such as toluene, ascorbyl stearate, ascorbyl palmitate, octyl gallate, propyl gallate, carotenoid, flavonoid, tannin, lignan, saponin, apple extract and clove extract.
  • the purple tea extract contained 8.70% by mass of GHG.
  • the purple tea extract was further separately prepared twice in the same manner as described above, and the GHG content in the extract was measured by the same method. As a result, the GHG contents were 6.79% by mass and 6.38, respectively. It was mass%. As a result, it was confirmed that the purple tea extract produced by the method of this example contained about 6 to 9% by mass of GHG.
  • ⁇ Test Example 1 Evaluation of effects on blood triglyceride elevation in olive oil-loaded mice> Blood was collected from the orbital venous sac of a fasted mouse (15 hours) using a glass capillary, and 30 minutes later, the purple tea extract (100, 200 mg / kg) of this example was orally administered. One hour later, olive oil (5 mL / kg) was orally administered, and blood was similarly collected from the orbital venous sac at 2, 4 and 6 hours thereafter. Serum was centrifuged from the obtained blood, and triglyceride concentration was measured using an enzymatic method (Triglyceride E-Test Wako, Wako Pure Chemical Industries, Ltd.). The result is shown in FIG.
  • Example 2 Weight gain inhibitory effect in mice fed with high fat diet> Mice (ICR, male, 10 weeks old) were allowed to freely take a high fat diet (High Fat Diet 32) and orally administered purple tea extract (200 mg / kg) once a day. The subject of comparison was a regular diet (CE-2) ad libitum. During this time, body weight was measured daily for 12 days. The result is shown in FIG.
  • Formulation Example 2 Gummy reduced starch syrup 40.0 wt% Granulated sugar 20.0 Glucose 20.0 Gelatin 4.7 Water 9.68 Grape juice 4.0 Grape flavor 0.6 Dye 0.02 Purple tea extract 1.0 100.0wt%
  • Formulation Example 4 Yogurt (hard / soft) Milk 41.5wt% Nonfat dry milk 5.8 Sugar 8.0 Agar 0.15 Gelatin 0.1 Lactic acid bacteria 0.005 Purple tea extract 0.4 Perfume Water residue 100.0wt%
  • Formulation Example 7 Tablet Lactose 54.0 wt% Crystalline cellulose 30.0 Starch degradation product 10.0 Glycerin fatty acid ester 5.0 Purple tea extract 1.0 100.0wt%
  • Formulation Example 8 Oral granules (pharmaceuticals) Purple tea extract 1.0wt% Lactose 30.0 Cornstarch 60.0 Crystalline cellulose 8.0 Polyvinylpyrrolidone 1.0 100.0wt%
  • Formulation Example 9 Tablets Sugar 76.4 wt% Glucose 19.0 Sucrose fatty acid ester 0.2 Purple tea extract 0.5 Purified water 3.9 100.0wt%
  • Formulation Example 10 Cosmetic cream Squalane 20.0 wt% Beeswax 5.0 Refined jojoba oil 5.0 Glycerin 5.0 Glycerol monostearate 2.0 Polyoxyethylene (20) sorbitan- Monostearate 2.0 Purple tea extract 2.0 Preservative appropriate amount Fragrance proper amount Purified water residue 100.0wt%
  • Formulation Example 13 Latex Squalane 4.0 wt% Vaseline 2.5 Cetanol 2.0 Glycerin 2.0 Lipophilic glyceryl monostearate 1.0 Stearic acid 1.0 L-Arginine 1.0 Purple tea extract 0.5 Potassium hydroxide 0.1 Perfume Purified water residue 100.0wt%
  • Formulation Example 15 Shampoo Sodium polyoxyethylene alkyl ether sulfate (E.O2 mol) 15.0 Palm oil aliphatic diethanolamide 5.0 Glycerin 3.0 Purple tea extract 0.4 Ethanol 5.0 Perfume and preservatives Ion exchange water 100.0wt%
  • Formulation Example 16 Hair Cream Liquid Paraffin 20.0wt% Solid paraffin 3.0 Polyoxyethylene cetyl ether (E.O15 mol) 2.0 Sorbitan sesquioleate 1.0 Purple tea extract 0.2 Ethanol 10.0 Potassium hydroxide 0.1 Glycerin 3.0 Perfume and preservatives 100.0wt%
  • Formulation Example 17 Salve Beeswax 5.0wt% Purified lanolin 5.0 Purple tea extract 1.0 Fragrance 0.1 Vaseline residue 100.0wt%
  • the present invention can provide a GHG-containing composition that is a composition derived from a natural product and contains GHG at a high concentration, and a method for producing the same. Furthermore, the fat absorption inhibitor which uses a novel plant or its extract as an active ingredient can be provided.

Abstract

The objective of the present invention is to provide: a 1,2-di-O-galloyl-4,6-O-(S)-hexahydroxydiphenoyl-b-D-glucose (hereinafter abbreviated as "GHG") containing composition that is a composition derived from a natural product and that contains a high concentration of GHG. The GHG-containing composition is characterized by being obtained from purple tea (scientific name: Camellia sinensis, cultivar name TRFK306) from Kenya, and having 3-10 mass% of GHG. The method for producing the GHG-containing composition is characterized by immersing the purple tea (scientific name: Camellia sinensis, cultivar name TRFK306) from Kenya in a polar solvent (including water), and then heating to reflux and extracting the GHG in the solvent.

Description

GHG含有組成物及びそれを用いた脂肪吸収抑制剤GHG-containing composition and fat absorption inhibitor using the same
 本発明は、植物由来であり、且つGHGを高濃度に含有する組成物及びそれを用いた脂肪吸収抑制剤に関する。本発明は医薬品、飲食品及び化粧料等に広く利用される。 The present invention relates to a composition which is derived from a plant and contains GHG at a high concentration, and a fat absorption inhibitor using the composition. The present invention is widely used for pharmaceuticals, foods and drinks, cosmetics, and the like.
 1,2-di-O-galloyl-4,6-O-(S)-hexahydroxydiphenoyl-b -D-glucose (以下、略して「GHG」という。)は、抗酸化作用(DPPHラジカル消去作用、SOD様作用)2)、チロシナーゼ阻害作用3)が既に報告されている(非特許文献1、非特許文献2、非特許文献3)。
 GHGを機能性食品や健康食品などの飲食品に配合する場合、食品安全に関する一般的観念からは、天然物由来のものであることが好ましい。しかしながら、従来知られていたGHGを含む天然物は、その含有量が少なく、非常に低含有のGHG組成物しか得られなかった。また、高濃度に含まれているものであっても、栽培に適さない入手が困難な野生種等であったりして、高濃度GHG組成物を得ることが困難であった。
1,2-di-O-galloyl-4,6-O- (S) -hexahydroxydiphenoyl-b-D-glucose (hereinafter abbreviated as “GHG”) is an antioxidant action (DPPH radical scavenging action, SOD 2) and tyrosinase inhibitory action 3) have already been reported (Non-patent document 1, Non-patent document 2, Non-patent document 3).
When GHG is blended in food and drink such as functional foods and health foods, it is preferably derived from natural products from the general concept of food safety. However, a conventionally known natural product containing GHG has a low content, and only a very low content GHG composition can be obtained. Moreover, even if it is contained in a high concentration, it is difficult to obtain a high concentration GHG composition because it is a wild species that is not suitable for cultivation and is difficult to obtain.
 一方、近年、過食、運動不足、動物性脂肪の摂取量の増加等により、血中の中性脂肪が正常値を超えた状態、いわゆる高脂血症の人が急増している。高脂血症は、動脈硬化、高血圧、心筋梗塞、脳血管障害等の疾病の原因となることが知られており、これらの疾病を予防するために、血中の中性脂肪量の上昇を抑制し、更には上昇した血中の中性脂肪量を正常範囲に低下させることが、現代人にとって重要になっている。そのため、日常的に摂取或いは投与が可能であり、血中の中性脂肪の調整に有効な可食性素材の開発が望まれている。このような素材として例えばニガウリの抽出物等が知られている(特許文献1)。 On the other hand, in recent years, people with so-called hyperlipidemia, in which blood neutral fat has exceeded normal levels, have increased rapidly due to overeating, lack of exercise, and increased intake of animal fat. Hyperlipidemia is known to cause diseases such as arteriosclerosis, hypertension, myocardial infarction, and cerebrovascular disorder. To prevent these diseases, an increase in the amount of neutral fat in the blood is caused. It is important for modern people to suppress and even lower the elevated blood neutral fat content to the normal range. Therefore, it is desired to develop an edible material that can be ingested or administered on a daily basis and is effective in adjusting the neutral fat in the blood. As such a material, for example, an extract of bitter gourd is known (Patent Document 1).
特開2006-117658号公報JP 2006-117658 A
 このような背景の下、本発明者は、GHGがケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)に高濃度に含有し、更に、ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)及びその抽出物に脂肪、特にトリグリセリドの血中への吸収を抑制する作用を有することを見出し、本発明を完成した。
 即ち、本発明は、天然物由来の組成物であってGHGを高濃度含有するGHG含有組成物、並びにその製造方法を提供することを目的とする。
 更に、新規な植物またはその抽出物を有効成分とする脂肪吸収抑制剤を提供することを目的とする。
Under such a background, the present inventor has found that GHG is contained in a high concentration in Kenyan purple tea (scientific name: Camellia sinensis, cultivar name TRFK306), and further Kenyan purple tea (scientific name: Camellia sinensis, cultivar name TRFK306). ) And its extract have the effect of inhibiting the absorption of fat, particularly triglycerides, into the blood, and the present invention has been completed.
That is, an object of the present invention is to provide a GHG-containing composition that is a natural product-derived composition containing a high concentration of GHG, and a method for producing the same.
Furthermore, it aims at providing the fat absorption inhibitor which uses a novel plant or its extract as an active ingredient.
 上記課題を解決するための本発明の技術的特徴は以下のとおりである。
1.ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)から得られ、GHGを含有することを特徴とするGHG含有組成物。
2.ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)から得られ、GHGを3~10質量%含有することを特徴とするGHG含有組成物。
3.ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)を極性溶媒(水をも含む)に浸漬し、その後、加熱還流して溶媒中にGHGを抽出することを特徴とするGHG含有組成物の製造方法。
4.ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)及び/またはその抽出物を有効成分とする脂肪吸収抑制剤。
5.ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)から得られるGHG含有組成物を有効成分とする脂肪吸収抑制剤。
6.ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)から得られるGHG含有組成物を有効成分とする体重増加抑制剤。
7.ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)から得られるGHG含有組成物をヒトに投与することにより、当該ヒトの脂肪吸収を抑制する方法。
8.ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)から得られるGHG含有組成物をヒトに投与することにより、当該ヒトの体重増加を抑制する方法。
The technical features of the present invention for solving the above-described problems are as follows.
1. A GHG-containing composition obtained from Kenya purple tea (scientific name: Camellia sinensis, variety TRFK306) and containing GHG.
2. A GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306) and containing 3 to 10% by mass of GHG.
3. A GHG-containing composition characterized in that a Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306) is immersed in a polar solvent (including water), and then heated to reflux to extract GHG in the solvent. Production method.
4). A fat absorption inhibitor containing Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306) and / or its extract as an active ingredient.
5. A fat absorption inhibitor comprising as an active ingredient a GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306).
6). A weight gain inhibitor comprising as an active ingredient a GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306).
7). A method for inhibiting fat absorption of a human by administering to the human a GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306).
8). A method for suppressing weight gain of a human by administering a GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306) to the human.
本実施例の紫茶抽出物のHPLCクロマトグラムである。It is a HPLC chromatogram of the purple tea extract of a present Example. 本実施例の紫茶抽出物におけるオリーブ油負荷マウスにおける血中トリグリセリド上昇に及ぼす作用の評価を示すもので、図2AおよびBは、紫茶抽出物およびオーリスタットの血中トリグリセリド上昇抑制作用を示すグラフである。FIG. 2A and FIG. 2B are graphs showing the effects of purple tea extract and orlistat on the blood triglyceride elevation inhibitory effect of purple tea extract of this Example on the effect on blood triglyceride elevation in olive oil-loaded mice. It is. 本実施例の紫茶抽出物の高脂肪食飼育マウスにおける体重増加に及ぼす抑制作用を示すグラフであるIt is a graph which shows the inhibitory effect which acts on the weight gain in the high fat diet-fed mouse | mouth of the purple tea extract of a present Example.
 以下、本発明を詳細に説明する。 Hereinafter, the present invention will be described in detail.
 本発明のGHG含有組成物は、ケニア産紫茶(学名:Camelliasinensis、品種名TRFK306、以下単に「紫茶」とする。)から得られた組成物であって、GHGを3~99質量%の含有量で含有する。その形状は液状、固形状、半固形状、ゲル状などであってよく、そのGHGの固形分換算含有量としては、3~99質量%であることが好ましいが、飲食品や化粧料の素材として使用する場合には、その生産性を良好にするため、3~30質量%であることが好ましく、さらには3~10質量%であることが好ましい。特に、3~10質量%の含有量でGHGを含有するGHG含有組成物は、下記に説明する製造方法により効率よく得ることができる。 The GHG-containing composition of the present invention is a composition obtained from Kenyan purple tea (scientific name: Camelliasinensis, variety name TRFK306, hereinafter simply referred to as “purple tea”), and comprises 3 to 99% by mass of GHG. Contains by content. The shape may be liquid, solid, semi-solid, gel, etc. The solid content of GHG is preferably 3 to 99% by mass. In order to improve the productivity, it is preferably 3 to 30% by mass, and more preferably 3 to 10% by mass. In particular, a GHG-containing composition containing GHG at a content of 3 to 10% by mass can be efficiently obtained by the production method described below.
 GHGは、下記化学式(1)で表される。 GHG is represented by the following chemical formula (1).
Figure JPOXMLDOC01-appb-C000001
Figure JPOXMLDOC01-appb-C000001
 紫茶は、ケニア政府によって交配によって開発されたチャノキであり、品種名TRFK306と名づけられている。このTRFK306の茶葉はアントシアニンを含有し、これにより紫色をしているため、通称「紫茶」或いは「パープルティ」と呼ばれている。更にTRFK306には特異成分であるGHGを高濃度に含有していることが本発明者によって見出された。
 本発明のGHG含有組成物に使用する紫茶の部位は特に限定されず、葉、茎、根、花、種子等を使用することができるが、特に葉を用いることが好ましい。より高濃度のGHGを得ることができるからである。
Purple tea is a tea tree developed by mating by the Kenyan government and is named variety name TRFK306. The tea leaves of TRFK306 contain anthocyanins and are purple due to this, so they are commonly called “purple tea” or “purple tea”. Furthermore, the present inventors have found that TRFK306 contains a specific component, GHG, at a high concentration.
The site of purple tea used in the GHG-containing composition of the present invention is not particularly limited, and leaves, stems, roots, flowers, seeds and the like can be used, but it is particularly preferable to use leaves. This is because a higher concentration of GHG can be obtained.
 本発明のGHG含有組成物は、好ましくは例えば、生のままの、又は乾燥させた紫茶の葉(以下「紫茶葉」という。)を粉砕し、極性溶媒(水をも含む。以下同じ。)を用いて抽出する方法により得ることができる。その紫茶葉には、抽出効率をよくするため、適宜、酸又はアルカリ分解、酵素分解等の化学的処理を施して、それから抽出してもよい。 The GHG-containing composition of the present invention preferably comprises, for example, pulverized raw or dried purple tea leaves (hereinafter referred to as “purple tea leaves”) and a polar solvent (including water; the same shall apply hereinafter). ) Can be used for extraction. In order to improve the extraction efficiency, the purple tea leaves may be appropriately subjected to chemical treatment such as acid or alkali decomposition, enzyme decomposition, etc., and then extracted.
 具体的には、GHG含有組成物は以下に説明する方法により製造することができる。
 即ち、先ず、上記紫茶葉として、生のままの、又は乾燥させた紫茶葉に酸又はアルカリ分解、酵素分解等の化学的処理を施す。
Specifically, the GHG-containing composition can be produced by the method described below.
That is, first, as the purple tea leaves, raw or dried purple tea leaves are subjected to chemical treatment such as acid or alkali decomposition, enzyme decomposition or the like.
 そして、上記紫茶葉に極性溶媒を添加して、振とうあるいは加熱還流し、その溶媒中にGHGを抽出する。 Then, a polar solvent is added to the purple tea leaves and shaken or heated to reflux to extract GHG in the solvent.
 このとき、上記極性溶媒は特に限定されないが、水、アルコール類、ケトン類を用いることができる。尚、これらは1種のみ用いても良いし2種以上を混合して用いてもよい。
 更に、これらのうち特に含水アルコールまたは含水ケトンを用いることが好ましい。
At this time, although the said polar solvent is not specifically limited, Water, alcohol, and ketones can be used. These may be used alone or in combination of two or more.
Further, among these, it is particularly preferable to use a hydrous alcohol or a hydrous ketone.
 含水アルコール系溶媒としては、エタノール、メタノール、プロパノール等の含水溶媒を用いることができ、特に、含水エタノールが好ましい。また、含水ケトン系溶媒としては、アセトン、メチルエチルケトン、ジエチルケトン、クロロアセトン等の含水溶媒を用いることができ、特に、含水アセトンが好ましい。 As the hydrous alcohol solvent, a hydrous solvent such as ethanol, methanol, propanol or the like can be used, and hydrous ethanol is particularly preferable. Further, as the hydrous ketone solvent, hydrous solvents such as acetone, methyl ethyl ketone, diethyl ketone, chloroacetone and the like can be used, and hydrous acetone is particularly preferable.
 その含水率としては、含水エタノールの場合には、エタノールを20~99.9質量%含むものであることが好ましく、30~99質量%含むものであることが更に好ましく、40~80質量%含むものであることが最も好ましい。含水アセトンの場合には、アセトンを20~99.9質量%含むものであることが好ましい。上記範囲がGHGの抽出効率が優れているからである。なお、以下、含水溶媒の含水率の表記については、簡便化のため、例えば、20質量%で含水させた80質量%エタノールのことを「80%含水エタノール」と表記する。 The water content is preferably 20 to 99.9% by mass of ethanol, more preferably 30 to 99% by mass, most preferably 40 to 80% by mass in the case of hydrous ethanol. preferable. In the case of hydrous acetone, it preferably contains 20 to 99.9% by mass of acetone. This is because the above range is excellent in GHG extraction efficiency. Hereinafter, with respect to the description of the water content of the water-containing solvent, for the sake of simplicity, for example, 80% by mass ethanol containing 20% by mass is described as “80% water-containing ethanol”.
 本発明のGHG含有組成物の製造方法において、その加熱還流は、上記含水アルコール系溶媒又は含水ケトン系溶媒を用いて、周知の方法で行うことができる。その加熱温度は30~95℃程度、還流時間は1~4時間程度であることが好ましい。 In the method for producing a GHG-containing composition of the present invention, the heating and refluxing can be performed by a known method using the above-mentioned hydroalcoholic solvent or hydrous ketone solvent. The heating temperature is preferably about 30 to 95 ° C., and the reflux time is preferably about 1 to 4 hours.
 また、本発明のGHG含有組成物の製造方法において、必要に応じて適宜、振とう、攪拌等を行っても良い。 Further, in the method for producing a GHG-containing composition of the present invention, if necessary, shaking, stirring, etc. may be performed.
 また、本発明のGHG含有組成物の製造方法においては、抽出後、上記溶媒を減圧留去することが好ましい。これによれば、有機溶媒を含まない組成物とすることができ、機能性食品や健康食品などの飲食品に配合するための食品素材として、その安全性の基準等に適合させることが可能である。 In the method for producing a GHG-containing composition of the present invention, it is preferable that the solvent is distilled off under reduced pressure after extraction. According to this, it is possible to make a composition that does not contain an organic solvent, and it can be adapted to safety standards as a food material for blending into foods and drinks such as functional foods and health foods. is there.
 本発明のGHG含有組成物の製造方法においては、複数の溶媒で段階的な抽出を行うことができる。これにより、GHGを高濃度に含有するGHG含有組成物を、より収率よく製造することができる。 In the method for producing a GHG-containing composition of the present invention, stepwise extraction can be performed with a plurality of solvents. Thereby, the GHG containing composition which contains GHG in high concentration can be manufactured with a sufficient yield.
 具体的には、例えば、紫茶葉を上記含水アルコール系溶媒及び上記含水ケトン系溶媒のいずれか一方を添加し、振とうあるいは加熱還流して、その溶媒中にGHGを抽出して第1抽出物を得る。遠心分離等により抽出物とその抽出物として回収されなかった残渣に分離し、その残渣に、上記溶媒のうち選択しなかった他方を添加して、振とうあるいは加熱還流して、その溶媒中にGHGを抽出して第2抽出物を得る。そして、前記第1抽出物と第2抽出物とを混合する。なお、この第2抽出物の単独でも紫茶葉の抽出物として利用可能であることはいうまでもない。 Specifically, for example, purple tea leaves are added with one of the above hydrous alcohol solvent and the above hydrous ketone solvent, shaken or heated to reflux, and GHG is extracted into the solvent to obtain the first extract. Get. The extract is separated into an extract and a residue not recovered as the extract by centrifugation or the like, and the other unselected solvent is added to the residue, and the mixture is shaken or heated to reflux. GHG is extracted to obtain a second extract. Then, the first extract and the second extract are mixed. Needless to say, the second extract alone can be used as an extract of purple tea leaves.
 このように、複数の溶媒で段階的な抽出を行うことにより、紫茶葉が、上記含水アルコール系溶媒又は上記含水ケトン系溶媒による第1の抽出処理を受けることによって、その物性等の特性が抽出のために好適なものに変化することが考えられるので、続く第2の抽出処理の際には、上記含水アルコール系溶媒又は上記含水ケトン系溶媒を用いる場合はもとより、それ以外の溶媒を用いる場合であっても、その抽出効率が改善されることが期待できる。 Thus, by performing stepwise extraction with a plurality of solvents, purple tea leaves are subjected to the first extraction treatment with the above-mentioned hydrous alcohol solvent or the above hydrous ketone solvent, thereby extracting characteristics such as physical properties. In the case of using the above-mentioned hydrous alcohol solvent or the above hydrous ketone solvent, the other extraction solvent is used in the subsequent second extraction process. Even so, the extraction efficiency can be expected to be improved.
 上記の方法で得られる抽出物は、これを、そのまま又は濃縮して液体状のものをGHG含有組成物とすることもできる。更に凍結乾燥又は噴霧乾燥により粉末化して粉末状のものをGHG含有組成物とすることもできる。
 また、これらの形態に制限されるものでもない。抽出物中に含まれる不溶物は、適宜、濾過などで除くことができる。不溶物はさらに粉砕し、微細粒子状にしてもよい。
The extract obtained by the above method can be used as it is or concentrated to obtain a liquid GHG-containing composition. Furthermore, it can be pulverized by freeze-drying or spray-drying to obtain a powdery composition as a GHG-containing composition.
Moreover, it is not limited to these forms. The insoluble matter contained in the extract can be appropriately removed by filtration or the like. The insoluble material may be further pulverized into fine particles.
 また、上記のようにして得られる紫茶葉からの一次的抽出物を、イオン交換、サイズ排除カラムクロマト法、HPLC法、ゲルろ過、膜分離等により、GHGを指標にして分画、精製して、これをGHG含有組成物とすることもできる。 The primary extract from purple tea leaves obtained as described above is fractionated and purified using GHG as an index by ion exchange, size exclusion column chromatography, HPLC, gel filtration, membrane separation, etc. This can also be used as a GHG-containing composition.
 本発明のGHG含有組成物は、必要に応じて、薬学的に許容される基材や担体を添加して、錠剤、顆粒剤、散剤、液剤、粉末、顆粒、カプセル剤、ゼリー状剤等の形態にして利用することができる。 The GHG-containing composition of the present invention may be added to a pharmaceutically acceptable base or carrier, if necessary, such as tablets, granules, powders, solutions, powders, granules, capsules, jelly-forms, etc. It can be used in the form.
 本発明の脂肪吸収抑制剤または体重増加抑制剤は、紫茶から得られるGHG含有組成物を有効成分とする。
 また、本発明の脂肪吸収抑制剤または体重増加抑制剤は、紫茶及び/またはその抽出物を有効成分とする。
 更に、本発明の脂肪吸収抑制剤または体重増加抑制剤として紫茶の抽出物を用いる場合、上記抽出物は、上述したGHG含有組成物と同様の方法により得ることができる。
The fat absorption inhibitor or weight gain inhibitor of the present invention comprises a GHG-containing composition obtained from purple tea as an active ingredient.
The fat absorption inhibitor or weight gain inhibitor of the present invention contains purple tea and / or an extract thereof as an active ingredient.
Furthermore, when using an extract of purple tea as the fat absorption inhibitor or weight gain inhibitor of the present invention, the extract can be obtained by the same method as the GHG-containing composition described above.
 本発明のGHG含有組成物、脂肪吸収抑制剤及び体重増加抑制剤(以下、単に「本組成物等」とする。)は、各種飲食品の素材として使用することができる。飲食品としては、例えば、食用油(サラダ油)、菓子類(ガム、キャンディー、キャラメル、チョコレート、クッキー、スナック、ゼリー、グミ、錠菓等)、麺類(そば、うどん、ラーメン等)、乳製品(ミルク、アイスクリーム、ヨーグルト等)、調味料(味噌、醤油等)、スープ類、飲料(ジュース、コーヒー、紅茶、茶、炭酸飲料、スポーツ飲料等)をはじめとする一般食品や、健康食品(錠剤、カプセル等)、栄養補助食品(栄養ドリンク等)が挙げられる。これらの飲食品に本組成物等を適宜配合するとよい。 The GHG-containing composition, fat absorption inhibitor and weight gain inhibitor (hereinafter simply referred to as “the present composition”) of the present invention can be used as materials for various foods and drinks. Examples of the food and drink include edible oil (salad oil), confectionery (gum, candy, caramel, chocolate, cookie, snack, jelly, gummy, tablet confection etc.), noodles (soba, udon, ramen etc.), and dairy products ( Milk, ice cream, yogurt, etc.), seasonings (miso, soy sauce, etc.), soups, beverages (juice, coffee, tea, tea, carbonated drinks, sports drinks, etc.) and health foods (tablets , Capsules, etc.) and nutritional supplements (nutrient drinks, etc.). The composition or the like may be appropriately blended with these foods and drinks.
 これら飲食品には、その種類に応じて種々の成分を配合することができ、例えば、ブドウ糖、果糖、ショ糖、マルトース、ソルビトール、ステビオサイド、コーンシロップ、乳糖、クエン酸、酒石酸、リンゴ酸、コハク酸、乳酸、L-アスコルビン酸、dl-α-トコフェロール、エリソルビン酸ナトリウム、グリセリン、プロピレングリコール、グリセリン脂肪酸エステル、ポリグリセリン脂肪酸エステル、ショ糖脂肪酸エステル、ソルビタン脂肪酸エステル、プロピレングリコール脂肪酸エステル、アラビアガム、カラギーナン、カゼイン、ゼラチン、ペクチン、寒天、ビタミンB類、ニコチン酸アミド、パントテン酸カルシウム、アミノ酸類、カルシウム塩類、色素、香料、保存剤等の食品素材を使用することができる。さらに、健康維持機能をもった本組成物等には、他の抗酸化物質や健康食品素材などの配剤、(例えば、抗酸化物質、還元型アスコルビン酸(ビタミンC)、ビタミンE、還元型グルタチン、トコトリエノール、ビタミンA誘導体、リコピン、β-クリプトキサンチン、アスタキサンチン、ゼアキサンチン、フコキサンチン、尿酸、ユビキノン、コエンザイムQ10、葉酸、ニンニクエキス、アリシン、セザミン、リグナン類、カテキン、イソフラボン、カルコン、タンニン類、フラボノイド類、クマリン、イソクマリン類、ブルーベリーエキス、アルブチン、タンニン、アントシアニン、リンゴポリフェノール、ブドウ種子エキス、エラジ酸、コウジ酸、サージ抽出物健康食品素材、V.(ビタミン)A、V.B1、V.B2、V.B6、V.B12、V.C、V.D、V.E、V.P、コリン、ナイアシン、パントテン酸、葉酸カルシウム、EPA、オリゴ糖、食物繊維、スクアレン、大豆レシチン、タウリン、ドナリエラ、プロテイン、オクタコサノール、DHA、卵黄レシチン、リノール酸、ラクトフェリン、マグネシウム、亜鉛、クロム、セレン、カリウム、ヘム鉄、カキ肉エキス、キトサン、キチンオリゴ糖、コラーゲン、コンドロイチン、ウコン、カンゾウ、クコシ、ケイヒ、サンザシ、生姜、霊芝、シジミエキス、スッポン、オオバコ、カミツレ、カモミール、セイヨウタンポポ、ハイビスカス、ハチミツ、ボーレン、ローヤルゼリー、ライム、ラベンダー、ローズヒップ、ローズマリー、セージ、ビフィズス菌、フェーカリス菌、ラクリス、小麦胚芽油、ゴマ油、シソ油、大豆油、中鎖脂肪酸、アガリクス、イチョウ葉エキス、ウコン、コンドロイチン、玄米胚芽エキス、レイシ、タマネギ、DHA、 EPA、 DPA、 甜茶、冬虫夏草、ニンニク、蜂の子、パパイヤ、プーアル、プロポリス、メグスリの木、ヤブシタケ、ロイヤルゼリー、ノコギリヤシ、ヒアルロン酸、コラーゲン、ギャバ、ハープシールオイル、サメ軟骨、グルコサミン、レシチン、ホスファチジルセリン、田七ニンジン、桑葉、大豆抽出物、エキナセア、エゾウコギ、大麦抽出物、オリーブ葉、オリーブ実、ギムネマ、バナバ、サラシア、ガルシニア、キトサン、セントジョーンズワート、ナツメ、ニンジン、パッションフラワー、ブロッコリー、プラセンタ、ハトムギ、ブドウ種子、ピーナッツ種皮、ビルベリー、ブラックコホシュ、マリアアザミ、月桂樹、セージ、ローズマリー、ラフマ、黒酢、ゴーヤー、マカ、紅花、亜麻、ウーロン茶、花棘、カフェイン、カプサイシン、キシロオリゴ糖、グルコサミン、ソバ、シトラス、食物繊維、プロテイン、プルーン、スピルリナ、大麦若葉、核酸、酵母、椎茸、梅肉、アミノ酸、深海鮫抽出物、ノニ、カキ肉、スッポン、シャンピニオン、オオバコ、アセロラ、パイナップル、バナナ、モモ、アンズ、メロン、イチゴ、ラズベリー、オレンジ、フコイダン、メシマコブ、クランベリー、コンドロイチン硫酸、亜鉛、鉄、セラミド、シルクペプチド、グリシン、ナイアシン、チェストツリー、セラミド、L-システイン、L-カルニチン、赤ワイン葉、ミレット、ホーステール、ビオチン、センテラアジアティカ、ハスカップ、ピクノジェノール、フキ、ルバーブ、クローブ、ローズマリー、カテキン、プーアル、クエン酸、ビール酵母、メリロート、ブラックジンガー、ショウガ、ガジュツ、ナットウキナーゼ、ベニコウジ、トコトリエノール、ラクトフェリン、シナモン、韃靼ソバ、ココア、ユズ種子エキス、シソの実エキス、ライチ種子エキス、月見草エキス、黒米エキス、α-リポ酸、ギャバ、生コーヒー豆エキス、フキエキス、キウイ種子エキス、温州みかんエキス、アカショウガエキス、アスタキサンチン)なども配合することができる。 These foods and drinks can be blended with various ingredients depending on the type, for example, glucose, fructose, sucrose, maltose, sorbitol, stevioside, corn syrup, lactose, citric acid, tartaric acid, malic acid, succinic acid. Acid, lactic acid, L-ascorbic acid, dl-α-tocopherol, sodium erythorbate, glycerin, propylene glycol, glycerin fatty acid ester, polyglycerin fatty acid ester, sucrose fatty acid ester, sorbitan fatty acid ester, propylene glycol fatty acid ester, gum arabic, Food materials such as carrageenan, casein, gelatin, pectin, agar, vitamin Bs, nicotinic acid amide, calcium pantothenate, amino acids, calcium salts, pigments, fragrances and preservatives can be used. In addition, this composition having a health maintenance function includes other antioxidants and health food ingredients such as antioxidants, reduced ascorbic acid (vitamin C), vitamin E, reduced glutatin. , Tocotrienol, vitamin A derivative, lycopene, β-cryptoxanthin, astaxanthin, zeaxanthin, fucoxanthin, uric acid, ubiquinone, coenzyme Q10, folic acid, garlic extract, allicin, sezamin, lignans, catechin, isoflavone, chalcone, tannins, flavonoids , Coumarin, isocoumarins, blueberry extract, arbutin, tannin, anthocyanin, apple polyphenol, grape seed extract, ellagic acid, kojic acid, surge extract health food material, V. (vitamin) A, V.B1, V.B2 , V.B6, V.B12, VC, VD, VE, VP, Cori , Niacin, pantothenic acid, calcium folate, EPA, oligosaccharide, dietary fiber, squalene, soy lecithin, taurine, donariella, protein, octacosanol, DHA, egg yolk lecithin, linoleic acid, lactoferrin, magnesium, zinc, chromium, selenium, potassium , Heme iron, oyster meat extract, chitosan, chitin oligosaccharide, collagen, chondroitin, turmeric, licorice, kukoshi, keihi, hawthorn, ginger, ganoderma, swordfish extract, suppon, plantain, chamomile, chamomile, dandelion, hibiscus, honey, Boren, royal jelly, lime, lavender, rosehip, rosemary, sage, bifidobacteria, faecalis, lacris, wheat germ oil, sesame oil, perilla oil, soybean oil, medium chain fatty acid, agaricus, ginkgo biloba , Turmeric, chondroitin, brown rice germ extract, litchi, onion, DHA, EPA, DPA, 甜 tea, cordyceps, garlic, bee, papaya, puer, propolis, megs, tree, yabushitake, royal jelly, saw palmetto, hyaluronic acid, collagen , GABA, harpseal oil, shark cartilage, glucosamine, lecithin, phosphatidylserine, paddy carrot, mulberry leaf, soy extract, echinacea, sorghum, barley extract, olive leaf, olive fruit, gymnema, banaba, salacia, garcinia, Chitosan, St. John's wort, jujube, carrot, passion flower, broccoli, placenta, pearl barley, grape seed, peanut seed coat, bilberry, black cohosh, maria thistle, laurel, sage, rosemary, raffma, black vinegar, -Yah, Maca, safflower, flax, oolong tea, flower spine, caffeine, capsaicin, xylo-oligosaccharide, glucosamine, buckwheat, citrus, dietary fiber, protein, prune, spirulina, barley young leaves, nucleic acid, yeast, shiitake, plum meat, amino acid, Deep sea bream extract, noni, oyster meat, suppon, champignon, plantain, acerola, pineapple, banana, peach, apricot, melon, strawberry, raspberry, orange, fucoidan, mesimacob, cranberry, chondroitin sulfate, zinc, iron, ceramide, silk Peptide, Glycine, Niacin, Chest Tree, Ceramide, L-Cysteine, L-Carnitine, Red Wine Leaf, Millet, Horsetail, Biotin, Centella Asiatica, Hascup, Pycnogenol, Fuki, Rhubarb, Clove, Rosemary, Catech , Puer, citric acid, brewer's yeast, merirot, black zinger, ginger, gadget, nattokinase, becouge, tocotrienol, lactoferrin, cinnamon, persimmon buckwheat, cocoa, yuzu seed extract, perilla seed extract, lychee seed extract, evening primrose extract, black rice Extract, α-lipoic acid, GABA, fresh coffee bean extract, Japanese bursa extract, kiwi seed extract, Unshu mandarin orange extract, red ginger extract, astaxanthin) and the like.
 具体的な製法としては、本組成物等をそのまま、抽出物の場合は粉末デキストリンとともにスプレードライまたは凍結乾燥し、これを粉末、顆粒、打錠または溶液にすることで容易に食品(インスタント食品等)に含有させることができる。また必要に応じてアラビアガム等のバインダーと混合して粉末状あるいは顆粒状にし、固形食品に添加することも可能である。 As a specific production method, the present composition or the like is used as it is, and in the case of an extract, it is spray-dried or freeze-dried together with powdered dextrin, and this is easily converted into a powder, granule, tablet, or solution. ). If necessary, it can also be mixed with a binder such as gum arabic to form a powder or granules, and added to a solid food.
 本組成物等は、薬品(医薬品および医薬部外品を含む。)の素材として用いてもよい。
 薬品製剤用の原料に、本組成物を適宜配合して製造することができる。尚、上記薬品は、ヒトに用いても良いし、ヒト以外の哺乳類動物に用いても良い。本組成物等に配合しうる製剤原料としては、例えば、賦形剤(ブドウ糖、乳糖、白糖、塩化ナトリウム、デンプン、炭酸カルシウム、カオリン、結晶セルロース、カカオ脂、硬化植物油、カオリン、タルク等)、結合剤(蒸留水、生理食塩水、エタノール水、単シロップ、ブドウ糖液、デンプン液、ゼラチン溶液、カルボキシメチルセルロース、リン酸カリウム、ポリビニルピロリドン等)、崩壊剤(アルギン酸ナトリウム、カンテン、炭酸水素ナトリウム、炭酸カルシウム、ラウリル硫酸ナトリウム、ステアリン酸モノグリセリド、デンプン、乳糖、アラビアゴム末、ゼラチン、エタノール等)、崩壊抑制剤(白糖、ステアリン、カカオ脂、水素添加油等)、吸収促進剤(第四級アンモニウム塩基、ラウリル硫酸ナトリウム等)、吸着剤(グリセリン、デンプン、乳糖、カオリン、ベントナイト、硅酸等)、滑沢剤(精製タルク、ステアリン酸塩、ポリエチレングリコール等)などが挙げられる。
You may use this composition etc. as a raw material of a chemical | medical agent (a pharmaceutical and a quasi-drug are included).
It can be produced by appropriately blending the present composition with a raw material for a pharmaceutical preparation. In addition, the said chemical | medical agent may be used for a human and may be used for mammals other than a human. Examples of the preparation raw material that can be blended in the present composition include, for example, excipients (glucose, lactose, sucrose, sodium chloride, starch, calcium carbonate, kaolin, crystalline cellulose, cocoa butter, hydrogenated vegetable oil, kaolin, talc, etc.), Binder (distilled water, physiological saline, ethanol water, simple syrup, glucose solution, starch solution, gelatin solution, carboxymethylcellulose, potassium phosphate, polyvinylpyrrolidone, etc.), disintegrant (sodium alginate, agar, sodium bicarbonate, carbonate Calcium, sodium lauryl sulfate, stearic acid monoglyceride, starch, lactose, gum arabic powder, gelatin, ethanol, etc.), disintegration inhibitors (sucrose, stearin, cocoa butter, hydrogenated oil, etc.), absorption accelerators (quaternary ammonium base) , Sodium lauryl sulfate, etc.), adsorbent ( Glycerin, starch, lactose, kaolin, bentonite, silicic acid, etc.), lubricants (purified talc, stearates, polyethylene glycol, and the like) and the like.
 本組成物等の投与方法は、一般的には、錠剤、丸剤、軟・硬カプセル剤、細粒剤、散剤、顆粒剤等の形態で経口投与することができる。また、水溶性製剤は、液剤として経口的に投与することができる。さらに非経口投与であってもよい。非経口剤として投与する場合は、本組成物等をエタノールや水など適当な可溶化剤に分散させた後、パップ剤、ローション剤、軟膏剤、チンキ剤、クリーム剤などの剤形で適用することができる。また本組成物等の水溶性製剤は、そのままで、あるいは分散剤、懸濁剤、安定剤などを添加した状態で、パップ剤、ローション剤、軟膏剤、チンキ剤、クリーム剤などの剤形で適用することができる。  The administration method of this composition and the like can be generally administered orally in the form of tablets, pills, soft / hard capsules, fine granules, powders, granules and the like. The water-soluble preparation can be administered orally as a liquid. Furthermore, parenteral administration may be used. When administered as a parenteral preparation, the composition is dispersed in an appropriate solubilizing agent such as ethanol or water, and then applied in a dosage form such as a poultice, lotion, ointment, tincture or cream. be able to. In addition, water-soluble preparations such as this composition can be used as they are or in the form of a poultice, lotion, ointment, tincture, cream, etc. with a dispersant, suspension, stabilizer, etc. added. Can be applied.
 投与量は、投与方法、病状、患者の年齢等によって変化し得るが、大人では、通常、1日当たり有効成分として5~200mg、子供では通常0.5~100mg程度投与することができる。 The dose may vary depending on the administration method, medical condition, age of the patient, etc., but for adults, it can usually be administered as 5 to 200 mg as an active ingredient per day, and for children it can usually be administered at about 0.5 to 100 mg.
 本組成物等を薬品として使用する際の配合比は、剤型によって適宜変更することが可能であるが、通常、経口または粘膜吸収により投与される場合は約0.01~10wt%、非経口投与による場合は、0.01~20wt%程度にするとよい。なお、投与量は種々の条件で異なるので、前記投与量より少ない量で十分な場合もあるし、また、範囲を超えて投与する必要のある場合もある。医薬組成物は、本組成物等以外に、医薬分野において常用される既知の他の化合物、および経口投与に適した形態に成型するのに必要な化合物を包含していてもよい。そのような化合物と しては、例えば、乳糖、デンプン、ヒドロキシプロピルセルロース、カオリン、タルク、炭酸カルシウムなどが挙げられる。 The compounding ratio when using the composition or the like as a drug can be appropriately changed depending on the dosage form, but is usually about 0.01 to 10 wt% when administered orally or by mucosal absorption, parenterally. In the case of administration, it should be about 0.01 to 20 wt%. In addition, since the dose varies depending on various conditions, a dose smaller than the above dose may be sufficient, or it may be necessary to administer beyond the range. In addition to the present composition and the like, the pharmaceutical composition may include other compounds that are commonly used in the pharmaceutical field and compounds that are necessary for molding into a form suitable for oral administration. Examples of such a compound include lactose, starch, hydroxypropylcellulose, kaolin, talc, calcium carbonate and the like.
 更に、本組成物等を化粧料として用いることもできる。
 本組成物等を配合しうる化粧料の形態としては、例えば、乳液、石鹸、洗顔料、入浴剤、クリーム、乳液、化粧水、オーデコロン、ひげ剃り用クリーム、ひげ剃り用ローション、化粧油、日焼け止めローション、おしろいパウダー、ファンデーション、香水、パック、爪クリーム、エナメル、エナメル除去液、眉墨、ほお紅、アイクリーム、アイシャドー、マスカラ、アイライナー、口紅、リップクリーム、シャンプー、リンス、染毛料、分散液、洗浄料等が挙げられる。
Furthermore, this composition etc. can also be used as cosmetics.
Cosmetic forms that can be blended with the present composition include, for example, emulsion, soap, face wash, bath preparation, cream, emulsion, lotion, eau de cologne, shave cream, shave lotion, cosmetic oil, tanning Stop Lotion, Funny Powder, Foundation, Perfume, Pack, Nail Cream, Enamel, Enamel Remover, Eyebrow, Blusher, Eye Cream, Eye Shadow, Mascara, Eyeliner, Lipstick, Lip Cream, Shampoo, Rinse, Hair Dye, Dispersion And cleaning fee.
 上記形態の化粧料には、本発明による本組成物の他に、その作用効果を損なわない範囲で化粧品、医薬部外品などの皮膚外用剤に配合される成分、油分、高級アルコール、脂肪酸、紫外線吸収剤、粉体、顔料、界面活性剤、多価アルコール・糖、高分子、生理活性成分、溶媒、酸化防止剤、香料、防腐剤等を配合することができる。
 例を以下に羅列するが、本発明はこれらの例に限定されるものではない。
In addition to the present composition according to the present invention, the cosmetic material of the above-described form includes ingredients, oils, higher alcohols, fatty acids, ingredients blended in skin preparations such as cosmetics and quasi-drugs, as long as the effects thereof are not impaired Ultraviolet absorbers, powders, pigments, surfactants, polyhydric alcohols / sugars, polymers, physiologically active ingredients, solvents, antioxidants, fragrances, preservatives and the like can be blended.
Examples are listed below, but the present invention is not limited to these examples.
(1)油分の例
 エステル系の油相成分:トリ2-エチルヘキサン酸グリセリル、2-エチルヘキサン酸セチル、ミリスチン酸イソプロピル、ミリスチン酸ブチル、パルミチン酸イソプロピル、ステアリン酸エチル、パルミチン酸オクチル、イソステアリン酸イソセチル、ステアリン酸ブチル、ミリスチン酸ブチル、リノール酸エチル、リノール酸イソプロピル、オレイン酸エチル、ミリスチン酸イソセチル、ミリスチン酸イソステアリル、パルミチン酸イソステアリル、ミリスチン酸オクチルドデシル、イソステアリン酸イソセチル、セバシン酸ジエチル、アジピン酸ジイソプロピル、ネオペンタン酸イソアラキル、トリ(カプリル・カプリン酸)グリセリル、トリ2-エチルヘキサン酸トリメチロールプロパン、トリイソステアリン酸トリメチロールプロパン、テトラ2-エチルヘキサン酸ペンタエリスリトール、カプリル酸セチル、ラウリン酸デシル、ラウリン酸ヘキシル、ミリスチン酸デシル、ミリスチン酸ミリスチル、ミリスチン酸セチル、ステアリン酸ステアリル、オレイン酸デシル、リシノレイン酸セチル、ラウリン酸イソステアリル、ミリスチン酸イソトリデシル、ミリスチン酸イソセチル、ミリスチン酸イソステアリル、パルミチン酸イソセチル、パルミチン酸イソステアリル、ステアリン酸オクチル、ステアリン酸イソセチル、オレイン酸イソデシル、オレイン酸オクチルドデシル、リノール酸オクチルドデシル、イソステアリン酸イソプロピル、2-エチルヘキサン酸セトステアリル、2-エチルヘキサン酸ステアリル、イソステアリン酸ヘキシル、ジオクタン酸エチレングリコール、ジオレイン酸エチレングリコール、ジカプリン酸プロピレングリコール、ジ(カプリル・カプリン酸)プロピレングリコール、ジカプリル酸プロピレングリコール、ジカプリン酸ネオペンチルグリコール、ジオクタン酸ネオペンチルグリコール、トリカプリル酸グリセリル、トリウンデシル酸グリセリル、トリイソパルミチン酸グリセリル、トリイソステアリン酸グリセリル、ネオペンタン酸オクチルドデシル、オクタン酸イソステアリル、イソノナン酸オクチル、ネオデカン酸ヘキシルデシル、ネオデカン酸オクチルドデシル、イソステアリン酸イソセチル、イソステアリン酸イソステアリル、イソステアリン酸オクチルデシル、ポリグリセリンオレイン酸エステル、ポリグリセリンイソステアリン酸エステル、炭酸ジプロピル、炭酸ジアルキル(C12-18)、クエン酸トリイソセチル、クエン酸トリイソアラキル、クエン酸トリイソオクチル、乳酸ラウリル、乳酸ミリスチル、乳酸セチル、乳酸オクチルデシル、クエン酸トリエチル、クエン酸アセチルトリエチル、クエン酸アセチルトリブチル、クエン酸トリオクチル、リンゴ酸ジイソステアリル、ヒドロキシステアリン酸2-エチルヘキシル、コハク酸ジ2-エチルヘキシル、アジピン酸ジイソブチル、セバシン酸ジイソプロピル、セバシン酸ジオクチル、ステアリン酸コレステリル、イソステアリン酸コレステリル、ヒドロキシステアリン酸コレステリル、オレイン酸コレステリル、オレイン酸ジヒドロコレステリル、イソステアリン酸フィトステリル、オレイン酸フィトステリル、12-ステアロイルヒドロキシステアリン酸イソセチル、12-ステアロイルヒドロキシステアリン酸ステアリル、12-ステアロイルヒドロキシステアリン酸イソステアリル等が挙げられる。
 炭化水素系の油相成分:スクワラン、流動パラフィン、α-オレフィンオリゴマー、イソパラフィン、セレシン、パラフィン、流動イソパラフィン、ポリブテン、マイクロクリスタリンワックス、ワセリン等が挙げられる。
 動植物油とその硬化油、および天然由来のロウ:牛脂、硬化牛脂、豚脂、硬化豚脂、馬油、硬化馬油、ミンク油、オレンジラフィー油、魚油、硬化魚油、卵黄油等の動物油およびその硬化油、アボカド油、アルモンド油、オリーブ油、カカオ脂、キウイ種子油、杏仁油、ククイナッツ油、ゴマ油、小麦胚芽油、コメ胚芽油、コメヌカ油、サフラワー油、シアバター、大豆油、月見草油、シソ油、茶実油、ツバキ油、トウモロコシ油、ナタネ油、硬化ナタネ油、パーム核油、硬化パーム核油、パーム油、硬化パーム油、ピーナッツ油、硬化ピーナッツ油、ヒマシ油、硬化ヒマシ油、ヒマワリ油、ブドウ種子油、ホホバ油、硬化ホホバ油、マカデミアナッツ油、メドホーム油、綿実油、硬化綿実油、ヤシ油、硬化ヤシ油等の植物油およびその硬化油、ミツロウ、高酸価ミツロウ、ラノリン、還元ラノリン、硬化ラノリン、液状ラノリン、カルナバロウ、モンタンロウ等のロウ等が挙げられる。
 シリコーン系の油相成分:ジメチルポリシロキサン、メチルフェニルポリシロキサン、メチルシクロポリシロキサン、オクタメチルポリシロキサン、デカメチルポリシロキサン、ドデカメチルシクロシロキサン、メチルハイドロジェンポリシロキサン、ポリエーテル変性オルガノポリシロキサン、ジメチルシロキサン・メチルセチルオキシシロキサン共重合体、ジメチルシロキサン・メチルステアロキシシロキサン共重合体、アルキル変性オルガノポリシロキサン、末端変性オルガノポリシロキサン、アミノ変性シリコーン油、アミノ変性オルガノポリシロキサン、ジメチコノール、シリコーンゲル、アクリルシリコーン、トリメチルシロキシケイ酸、シリコーンRTVゴム等が挙げられる。
 フッ素系の油相成分:パーフルオロポリエーテル、フッ素変性オルガノポリシロキサン、フッ化ピッチ、フルオロカーボン、フルオロアルコール、フルオロアルキル・ポリオキシアルキレン共変性オルガノポリシロキサン等が挙げられる。
(1) Examples of oil components Ester-based oil phase components: glyceryl tri-2-ethylhexanoate, cetyl 2-ethylhexanoate, isopropyl myristate, butyl myristate, isopropyl palmitate, ethyl stearate, octyl palmitate, isostearic acid Isocetyl, butyl stearate, butyl myristate, ethyl linoleate, isopropyl linoleate, ethyl oleate, isocetyl myristate, isostearyl myristate, isostearyl palmitate, octyldodecyl myristate, isocetyl isostearate, diethyl sebacate, adipine Diisopropyl acid, isoaralkyl neopentanoate, glyceryl tri (capryl / capric acid), trimethylolpropane tri-2-ethylhexanoate, trimethylol triisostearate Propane, pentaerythritol tetra-2-ethylhexanoate, cetyl caprylate, decyl laurate, hexyl laurate, decyl myristate, myristyl myristate, cetyl myristate, stearyl stearate, decyl oleate, cetyl ricinoleate, isolaurate Stearyl, isotridecyl myristate, isocetyl myristate, isostearyl myristate, isocetyl palmitate, isostearyl palmitate, octyl stearate, isocetyl stearate, isodecyl oleate, octyldodecyl linoleate, octyldodecyl isoleate, isopropyl isostearate Cetostearyl 2-ethylhexanoate, stearyl 2-ethylhexanoate, hexyl isostearate, ethyleneglycol dioctanoate , Ethylene glycol dioleate, propylene glycol dicaprate, propylene glycol di (capryl / capric acid), propylene glycol dicaprylate, neopentyl glycol dicaprate, neopentyl glycol dioctanoate, glyceryl tricaprylate, glyceryl triundecylate, triiso Glyceryl palmitate, glyceryl triisostearate, octyldodecyl neopentanoate, isostearyl octanoate, octyl isononanoate, hexyldecyl neodecanoate, octyldodecyl neodecanoate, isocetyl isostearate, isostearyl isostearate, octyldecyl isostearate, polyglycerin olein Acid ester, polyglycerol isostearate, dipropyl carbonate, charcoal Dialkyl (C12-18), triisocetyl citrate, triisoaralkyl citrate, triisooctyl citrate, lauryl lactate, myristyl lactate, cetyl lactate, octyl decyl lactate, triethyl citrate, acetyl triethyl citrate, acetyl tributyl citrate, Trioctyl citrate, diisostearyl malate, 2-ethylhexyl hydroxystearate, di-2-ethylhexyl succinate, diisobutyl adipate, diisopropyl sebacate, dioctyl sebacate, cholesteryl stearate, cholesteryl isostearate, cholesteryl hydroxystearate, olein Cholesteryl acid, dihydrocholesteryl oleate, phytosteryl isostearate, phytosteryl oleate, 12-stearoyl hydroxystearate Cetyl, 12-stearoyl-hydroxystearic acid stearyl 12-stearoyl-hydroxystearic acid isostearate, and the like.
Hydrocarbon oil phase components: squalane, liquid paraffin, α-olefin oligomer, isoparaffin, ceresin, paraffin, liquid isoparaffin, polybutene, microcrystalline wax, petrolatum and the like.
Animal and vegetable oils and their hydrogenated oils, and naturally occurring waxes: beef tallow, hydrogenated beef tallow, lard, hydrogenated tallow, horse oil, hydrogenated horse oil, mink oil, orange luffy oil, fish oil, hydrogenated fish oil, egg yolk oil and other animal oils and Its hardened oil, avocado oil, almond oil, olive oil, cacao butter, kiwi seed oil, apricot oil, kukui nut oil, sesame oil, wheat germ oil, rice germ oil, rice bran oil, safflower oil, shea butter, soybean oil, evening primrose oil , Perilla oil, tea seed oil, camellia oil, corn oil, rapeseed oil, hydrogenated rapeseed oil, palm kernel oil, hydrogenated palm kernel oil, palm oil, hydrogenated palm oil, peanut oil, hydrogenated peanut oil, castor oil, hydrogenated castor oil , Vegetable oils such as sunflower oil, grape seed oil, jojoba oil, hardened jojoba oil, macadamia nut oil, medhome oil, cottonseed oil, hardened cottonseed oil, coconut oil, hardened coconut oil and its hardened , Beeswax, high acid value beeswax, lanolin, reduced lanolin, hydrogenated lanolin, liquid lanolin, carnauba wax and montan wax.
Silicone oil phase components: dimethylpolysiloxane, methylphenylpolysiloxane, methylcyclopolysiloxane, octamethylpolysiloxane, decamethylpolysiloxane, dodecamethylcyclosiloxane, methylhydrogenpolysiloxane, polyether-modified organopolysiloxane, dimethyl Siloxane / methylcetyloxysiloxane copolymer, dimethylsiloxane / methylstearoxysiloxane copolymer, alkyl-modified organopolysiloxane, terminal-modified organopolysiloxane, amino-modified silicone oil, amino-modified organopolysiloxane, dimethiconol, silicone gel, acrylic Examples include silicone, trimethylsiloxysilicic acid, and silicone RTV rubber.
Fluorine oil phase components: perfluoropolyether, fluorine-modified organopolysiloxane, fluorinated pitch, fluorocarbon, fluoroalcohol, fluoroalkyl / polyoxyalkylene co-modified organopolysiloxane, and the like.
(2)高級アルコールの例
 ラウリルアルコール、ミリスチルアルコール、セチルアルコール、ステアリルアルコール、イソステアリルアルコール、オレイルアルコール、ベヘニルアルコール、2-エチルヘキサノール、ヘキサデシルアルコール、オクチルドデカノール等が挙げられる。
(2) Examples of higher alcohols Lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, isostearyl alcohol, oleyl alcohol, behenyl alcohol, 2-ethylhexanol, hexadecyl alcohol, octyldodecanol and the like can be mentioned.
(3)脂肪酸の例
 カプリル酸、カプリン酸、ウンデシレン酸、ラウリン酸、ミリスチン酸、パルミチン酸、パルミトレイン酸、ステアリン酸、イソステアリン酸、オレイン酸、リノール酸、リノレン酸、アラキン酸、アラキドン酸、ベヘン酸、エルカ酸、2-エチルヘキサン酸等が挙げられる。
(3) Examples of fatty acids Caprylic acid, capric acid, undecylenic acid, lauric acid, myristic acid, palmitic acid, palmitoleic acid, stearic acid, isostearic acid, oleic acid, linoleic acid, linolenic acid, arachidic acid, arachidonic acid, behenic acid , Erucic acid, 2-ethylhexanoic acid and the like.
(4)紫外線吸収剤の例
 パラアミノ安息香酸、パラアミノ安息香酸アミル、パラアミノ安息香酸エチルジヒドロキシプロピル、パラアミノ安息香酸グリセリル、パラアミノ安息香酸エチル、パラアミノ安息香酸オクチル、パラアミノ安息香酸オクチルジメチル、サリチル酸エチレングリコール、サリチル酸オクチル、サリチル酸トリエタノールアミン、サリチル酸フェニル、サリチル酸ブチルフェニル、サリチル酸ベンジル、サリチル酸ホモメンチル、ケイ皮酸ベンジル、パラメトキシケイ皮酸オクチル、パラメトキシケイ皮酸2-エチルヘキシル、ジパラメトキシケイ皮酸モノ2-エチルヘキサン酸グリセリル、パラメトキシケイ皮酸イソプロピル、パラメトキシヒドロケイ皮酸ジエタノールアミン塩、ジイソプロピル・ジイソプロピルケイ皮酸エステル混合物、ウロカニン酸、ウロカニン酸エチル、ヒドロキシメトキシベンゾフェノン、ヒドロキシメトキシベンゾフェノンスルホン酸及びその塩、ジヒドロキシメトキシベンゾフェノン、ジヒドロキシメトキシベンゾフェノンジスルホン酸ナトリウム、ジヒドロキシベンゾフェノン、ジヒドロキシジメトキシベンゾフェノン、ヒドロキシオクトキシベンゾフェノン、テトラヒドロキシベンゾフェノン、ブチルメトキシジベンゾイルメタン、2、4、6-トリアニリノ-p-(カルボ-2-エチルヘキシル-1-オキシ)-1、3、5-トリアジン、2-(2-ヒドロキシ-5-メチルフェニル)ベンゾトリアゾール、メチル-O-アミノベンゾエート、2-エチルヘキシル-2-シアノ-3、3-ジフェニルアクリレート、フェニルベンゾイミダゾール硫酸、3-(4-メチルベンジリデン)カンフル、イソプロピルジベンゾイルメタン、4-(3、4-ジメトキシフェニルメチレン)-2、5-ジオキソ-1-イミダゾリジンプロピオン酸2-エチルヘキシル等、およびこれらの高分子誘導体やシラン誘導体等が挙げられる。
(4) Examples of UV absorbers Paraaminobenzoic acid, amyl paraaminobenzoate, ethyldihydroxypropyl paraaminobenzoate, glyceryl paraaminobenzoate, ethyl paraaminobenzoate, octyl paraaminobenzoate, octyldimethyl paraaminobenzoate, ethylene glycol salicylate, salicylic acid Octyl, triethanolamine salicylate, phenyl salicylate, butylphenyl salicylate, benzyl salicylate, homomenthyl salicylate, benzyl cinnamate, octyl paramethoxycinnamate, 2-ethylhexyl paramethoxycinnamate, mono-2-diparamethoxycinnamate Glyceryl ethylhexanoate, isopropyl paramethoxycinnamate, diethanolamine salt of paramethoxyhydrocinnamic acid, diisopropyl diisopropylcinnamic acid Stealth mixture, urocanic acid, ethyl urocanate, hydroxymethoxybenzophenone, hydroxymethoxybenzophenone sulfonic acid and its salts, dihydroxymethoxybenzophenone, dihydroxymethoxybenzophenone sodium disulfonate, dihydroxybenzophenone, dihydroxydimethoxybenzophenone, hydroxyoctoxybenzophenone, tetrahydroxybenzophenone, Butylmethoxydibenzoylmethane, 2,4,6-trianilino-p- (carbo-2-ethylhexyl-1-oxy) -1,3,5-triazine, 2- (2-hydroxy-5-methylphenyl) benzotriazole , Methyl-O-aminobenzoate, 2-ethylhexyl-2-cyano-3, 3-diphenyl acrylate, phenylbenzimidazole sulfate, 3- (4-methylbenzylidene) can Examples include full, isopropyldibenzoylmethane, 4- (3,4-dimethoxyphenylmethylene) -2, 5-dioxo-1-imidazolidinepropionate 2-ethylhexyl, and the like, polymer derivatives, silane derivatives, and the like.
(5)粉体・顔料の例
 赤色104号、赤色201号、黄色4号、青色1号、黒色401号等の色素、黄色4号ALレーキ、黄色203号BAレーキ等のレーキ色素、ナイロンパウダー、シルクパウダー、ウレタンパウダー、テフロン(登録商標)パウダー、シリコーンパウダー、ポリメタクリル酸メチルパウダー、セルロースパウダー、デンプン、シリコーンエラストマー球状粉体、ポリエチレン末等の高分子、黄酸化鉄、赤色酸化鉄、黒酸化鉄、酸化クロム、カーボンブラック、群青、紺青等の有色顔料、酸化亜鉛、酸化チタン、酸化セリウム等の白色顔料、タルク、マイカ、セリサイト、カオリン、板状硫酸バリウム等の体質顔料、雲母チタン等のパール顔料、硫酸バリウム、炭酸カルシウム、炭酸マグネシウム、珪酸アルミニウム、珪酸マグネシウム等の金属塩、シリカ、アルミナ等の無機粉体、ステアリン酸アルミニウム、ステアリン酸マグネシウム、パルミチン酸亜鉛、ミリスチン酸亜鉛、ミリスチン酸マグネシウム、ラウリン酸亜鉛、ウンデシレン酸亜鉛等の金属セッケン、ベントナイト、スメクタイト、窒化ホウ素等が挙げられる。これらの粉体の形状(球状、棒状、針状、板状、不定形状、燐片状、紡錘状等)および粒子径に特に制限はない。なおこれらの粉体は、従来公知の表面処理、例えばフッ素化合物処理、シリコーン処理、シリコーン樹脂処理、ペンダント処理、シランカップリング剤処理、チタンカップリング剤処理、油剤処理、N-アシル化リジン処理、ポリアクリル酸処理、金属セッケン処理、アミノ酸処理、レシチン処理、無機化合物処理、プラズマ処理、メカノケミカル処理等によって事前に表面処理されていてもいなくても構わない。
(5) Examples of powders and pigments Red 104, Red 201, Yellow 4, Blue 1, Black 401 and other dyes, Yellow 4 AL lake, Yellow 203 BA lake and other lake dyes, nylon powder , Silk powder, urethane powder, Teflon (registered trademark) powder, silicone powder, polymethyl methacrylate powder, cellulose powder, starch, silicone elastomer spherical powder, polyethylene powder, yellow iron oxide, red iron oxide, black Colored pigments such as iron oxide, chromium oxide, carbon black, ultramarine and bitumen, white pigments such as zinc oxide, titanium oxide and cerium oxide, extender pigments such as talc, mica, sericite, kaolin and barium sulfate plate, titanium mica Pearl pigments such as barium sulfate, calcium carbonate, magnesium carbonate, aluminum silicate, metal salts such as magnesium silicate, Inorganic powders such as Rica and alumina, metal soaps such as aluminum stearate, magnesium stearate, zinc palmitate, zinc myristate, magnesium myristate, zinc laurate, zinc undecylenate, bentonite, smectite, boron nitride, etc. It is done. There are no particular restrictions on the shape of these powders (spherical, rod-like, needle-like, plate-like, irregular shape, flake-like, spindle-like, etc.) and particle diameter. These powders are conventionally known surface treatments such as fluorine compound treatment, silicone treatment, silicone resin treatment, pendant treatment, silane coupling agent treatment, titanium coupling agent treatment, oil agent treatment, N-acylated lysine treatment, The surface treatment may or may not be performed in advance by polyacrylic acid treatment, metal soap treatment, amino acid treatment, lecithin treatment, inorganic compound treatment, plasma treatment, mechanochemical treatment or the like.
(6)界面活性剤の例
 アニオン性界面活性剤:脂肪酸セッケン、α-アシルスルホン酸塩、アルキルスルホン酸塩、アルキルアリルスルホン酸塩、アルキルナフタレンスルホン酸塩、アルキル硫酸塩、POEアルキルエーテル硫酸塩、アルキルアミド硫酸塩、アルキルリン酸塩、POEアルキルリン酸塩、アルキルアミドリン酸塩、アルキロイルアルキルタウリン塩、N-アシルアミノ酸塩、POEアルキルエーテルカルボン酸塩、アルキルスルホコハク酸塩、アルキルスルホ酢酸ナトリウム、アシル化加水分解コラーゲンペプチド塩、パーフルオロアルキルリン酸エステル等が挙げられる。
 カチオン性界面活性剤:塩化アルキルトリメチルアンモニウム、塩化ステアリルトリメチルアンモニウム、臭化ステアリルトリメチルアンモニウム、塩化セトステアリルトリメチルアンモニウム、塩化ジステアリルジメチルアンモニウム、塩化ステアリルジメチルベンジルアンモニウム、臭化ベヘニルトリメチルアンモニウム、塩化ベンザルコニウム、塩化ベヘニン酸アミドプロピルジメチルヒドロキシプロピルアンモニウム、ステアリン酸ジエチルアミノエチルアミド、ステアリン酸ジメチルアミノプロピルアミド、ラノリン誘導体第四級アンモニウム塩等が挙げられる。
 両性界面活性剤:カルボキシベタイン型、アミドベタイン型、スルホベタイン型、ヒドロキシスルホベタイン型、アミドスルホベタイン型、ホスホベタイン型、アミノカルボン酸塩型、イミダゾリン誘導体型、アミドアミン型等が挙げられる。
 ノニオン性界面活性剤:プロピレングリコール脂肪酸エステル、グリセリン脂肪酸エステル、ポリグリセリン脂肪酸エステル、ソルビタン脂肪酸エステル、POEソルビタン脂肪酸エステル、POEソルビット脂肪酸エステル、POEグリセリン脂肪酸エステル、POEアルキルエーテル、POE脂肪酸エステル、POE硬化ヒマシ油、POEヒマシ油、POE・POP共重合体、POE・POPアルキルエーテル、ポリエーテル変性シリコーンラウリン酸アルカノールアミド、アルキルアミンオキシド、水素添加大豆リン脂質等が挙げられる。
 天然系界面活性剤:レシチン、サポニン、糖系界面活性剤等が挙げられる。
(6) Examples of surfactants Anionic surfactant: fatty acid soap, α-acyl sulfonate, alkyl sulfonate, alkyl allyl sulfonate, alkyl naphthalene sulfonate, alkyl sulfate, POE alkyl ether sulfate , Alkylamide sulfate, alkyl phosphate, POE alkyl phosphate, alkylamide phosphate, alkyloylalkyl taurine salt, N-acyl amino acid salt, POE alkyl ether carboxylate, alkyl sulfosuccinate, alkyl sulfoacetic acid Sodium, acylated hydrolyzed collagen peptide salt, perfluoroalkyl phosphate, etc. are mentioned.
Cationic surfactant: alkyltrimethylammonium chloride, stearyltrimethylammonium chloride, stearyltrimethylammonium bromide, cetostearyltrimethylammonium chloride, distearyldimethylammonium chloride, stearyldimethylbenzylammonium chloride, behenyltrimethylammonium bromide, benzalkonium chloride , Behenic acid amidopropyldimethylhydroxypropylammonium chloride, stearic acid diethylaminoethylamide, stearic acid dimethylaminopropylamide, lanolin derivative quaternary ammonium salts, and the like.
Amphoteric surfactants: carboxybetaine type, amide betaine type, sulfobetaine type, hydroxysulfobetaine type, amide sulfobetaine type, phosphobetaine type, aminocarboxylate type, imidazoline derivative type, amidoamine type and the like.
Nonionic surfactant: propylene glycol fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, sorbitan fatty acid ester, POE sorbitan fatty acid ester, POE sorbitol fatty acid ester, POE glycerin fatty acid ester, POE alkyl ether, POE fatty acid ester, POE cured castor Oil, POE castor oil, POE / POP copolymer, POE / POP alkyl ether, polyether-modified silicone lauric acid alkanolamide, alkylamine oxide, hydrogenated soybean phospholipid, and the like.
Natural surfactant: lecithin, saponin, sugar surfactant and the like.
(7)多価アルコール、糖の例
 エチレングリコール、ジエチレングリコール、ポリエチレングリコール、プロピレングリコール、ジプロピレングリコール、ポリプロピレングリコール、グリセリン、ジグリセリン、ポリグリセリン、3-メチル-1、3-ブタンジオール、1、3-ブチレングリコール、ソルビトール、マンニトール、ラフィノース、エリスリトール、グルコース、ショ糖、果糖、キシリトール、ラクトース、マルトース、マルチトール、トレハロース、アルキル化トレハロース、混合異性化糖、硫酸化トレハロース、プルラン等が挙げられる。またこれらの化学修飾体等も使用可能である。
(7) Examples of polyhydric alcohols and sugars Ethylene glycol, diethylene glycol, polyethylene glycol, propylene glycol, dipropylene glycol, polypropylene glycol, glycerin, diglycerin, polyglycerin, 3-methyl-1,3-butanediol, 1, 3 -Butylene glycol, sorbitol, mannitol, raffinose, erythritol, glucose, sucrose, fructose, xylitol, lactose, maltose, maltitol, trehalose, alkylated trehalose, mixed isomerized sugar, sulfated trehalose, pullulan and the like. These chemically modified compounds can also be used.
(8)高分子の例
 アクリル酸エステル/メタクリル酸エステル共重合体(プラスサイズ、互応化学社製)、酢酸ビニル/クロトン酸共重合体(レジン28-1310、NSC社製)、酢酸ビニル/クロトン酸/ビニルネオデカネート共重合体(28-2930、NSC社製)、メチルビニルエーテルマレイン酸ハーフエステル(ガントレッツES、ISP社製)、T-ブチルアクリレート/アクリル酸エチル/メタクリル酸共重合体(ルビマー、BASF社製)、ビニルピロリドン/ビニルアセテート/ビニルプロピオネート共重合体(ルビスコールVAP、BASF社製)、ビニルアセテート/クロトン酸共重合体(ルビセットCA、BASF社製)、ビニルアセテート/クロトン酸/ビニルピロリドン共重合体(ルビセットCAP、BASF社製)、ビニルピロリドン/アクリレート共重合体(ルビフレックス、BASF社製)、アクリレート/アクリルアミド共重合体(ウルトラホールド、BASF社製)、ビニルアセテート/ブチルマレエート/イソボルニルアクリラート共重合体(アドバンテージ、ISP社製)、カルボキシビニルポリマー(カーボポール、BFGoodrich社製)、アクリル酸・メタクリル酸アルキル共重合体(ペミュレン、BF Goodrich社製)等のアニオン性高分子化合物や、ジアルキルアミノエチルメタクリレート重合体の酢酸両性化物(ユカフォーマー、三菱化学社製)、アクリル酸オクチルアクリルアミド/アクリル酸ヒドロキシプロピル/メタクリル酸ブチルアミノエチル共重合体(AMPHOMER、NSC社製)等の両性高分子化合物、ビニルピロリドン/ジメチルアミノエチルメタクリレートの4級化物(GAFQUAT、ISP社製)、メチルビニルイミダゾリウムクロリド/ビニルピロリドン共重合体(ルビコート、BASF社製)等のカチオン性高分子化合物、ポリビニルピロリドン(ルビスコールK、BASF社製)、ビニルピロリドン/酢酸ビニル共重合体(ルビスコールVA、BASF社製)、ビニルピロリドン/ジメチルアミノエチルメタクリレート共重合体(コポリマー937、ISP社製)、ビニルカプロラクタム/ビニルピロリドン/ジメチルアミノエチルメタクリレート共重合体(コポリマーVC713、ISP社製)等のノニオン性高分子化合物等がある。また、セルロースまたはその誘導体、ケラチン及びコラーゲンまたはその誘導体、アルギン酸カルシウム、プルラン、寒天、ゼラチン、タマリンド種子多糖類、キサンタンガム、カラギーナン、ハイメトキシルペクチン、ローメトキシルペクチン、グアーガム、アラビアゴム、結晶セルロース、アラビノガラクタン、カラヤガム、トラガカントガム、アルギン酸、アルブミン、カゼイン、カードラン、ジェランガム、デキストラン等の天然由来高分子化合物も好適に用いることができる。
(8) Examples of polymers Acrylic ester / methacrylic acid ester copolymer (plus size, manufactured by Kyoyo Chemical), vinyl acetate / crotonic acid copolymer (resin 28-1310, manufactured by NSC), vinyl acetate / croton Acid / vinyl neodecanate copolymer (28-2930, manufactured by NSC), methyl vinyl ether maleic acid half ester (Gantrez ES, manufactured by ISP), T-butyl acrylate / ethyl acrylate / methacrylic acid copolymer (rubymer) , BASF), vinyl pyrrolidone / vinyl acetate / vinyl propionate copolymer (Rubicol VAP, BASF), vinyl acetate / crotonic acid copolymer (Rubiset CA, BASF), vinyl acetate / croton Acid / vinyl pyrrolidone copolymer (Rubiset CAP, manufactured by BASF), vinyl pyrrolidone / acrylate copolymer (Rubiflex, BA SF), acrylate / acrylamide copolymer (Ultrahold, BASF), vinyl acetate / butyl maleate / isobornyl acrylate copolymer (Advantage, ISP), carboxy vinyl polymer (Carbopol, BF Goodrich), anionic polymer compounds such as acrylic acid / alkyl methacrylate copolymer (Pemulene, BF Goodrich), and acetic acid amphoteric products of dialkylaminoethyl methacrylate polymers (Yukaformer, Mitsubishi Chemical) Amphoteric polymer compounds such as octyl acrylate acrylate / hydroxypropyl acrylate / butylaminoethyl methacrylate copolymer (AMPHOMER, NSC), quaternized vinylpyrrolidone / dimethylaminoethyl methacrylate (GAFQUAT, ISP) , Methyl vinyl imidazolium chloride Cationic polymer compounds such as vinyl / vinylpyrrolidone copolymer (rubicoat, manufactured by BASF), polyvinylpyrrolidone (rubiscol K, manufactured by BASF), vinylpyrrolidone / vinyl acetate copolymer (rubiscol VA, manufactured by BASF) ), Nonionic polymer compounds such as vinylpyrrolidone / dimethylaminoethyl methacrylate copolymer (copolymer 937, manufactured by ISP), vinylcaprolactam / vinylpyrrolidone / dimethylaminoethyl methacrylate copolymer (copolymer VC713, manufactured by ISP), etc. There is. Cellulose or derivatives thereof, keratin and collagen or derivatives thereof, calcium alginate, pullulan, agar, gelatin, tamarind seed polysaccharide, xanthan gum, carrageenan, high methoxyl pectin, low methoxyl pectin, guar gum, gum arabic, crystalline cellulose, arabino Naturally derived polymer compounds such as galactan, gum karaya, gum tragacanth, alginic acid, albumin, casein, curdlan, gellan gum and dextran can also be suitably used.
(9)生理活性成分の例
 生理活性成分としては、皮膚に塗布した場合に皮膚に何らかの生理活性を与える物質が挙げられる。例えば、美白成分、免疫賦活剤、老化防止剤、紫外線防御剤、スリミング剤、ひきしめ剤、抗酸化剤、発毛剤、育毛剤、保湿剤、血行促進剤、抗菌剤、殺菌剤、乾燥剤、冷感剤、温感剤、ビタミン類、アミノ酸、創傷治癒促進剤、刺激緩和剤、鎮痛剤、細胞賦活剤、酵素成分等が挙げられる。これらの好適な配合成分の例としては、例えばアシタバエキス、アボカドエキス、アマチャエキス、アルテアエキス、アルニカエキス、アロエエキス、アンズエキス、アンズ核エキス、イチョウエキス、ウイキョウエキス、ウコンエキス、ウーロン茶エキス、エイジツエキス、エチナシ葉エキス、オウゴンエキス、オウバクエキス、オウレンエキス、オオムギエキス、オトギリソウエキス、オドリコソウエキス、オランダカラシエキス、オレンジエキス、海水乾燥物、海藻エキス、加水分解エラスチン、加水分解コムギ末、加水分解シルク、カモミラエキス、カロットエキス、カワラヨモギエキス、甘草エキス、カルカデエキス、カキョクエキス、キナエキス、キューカンバ-エキス、グアノシン、クチナシエキス、クマザサエキス、クララエキス、クルミエキス、グレープフルーツエキス、クレマティスエキス、クロレラエキス、クワエキス、ゲンチアナエキス、紅茶エキス、酵母エキス、ゴボウエキス、コメヌカ発酵エキス、コメ胚芽油、コンフリーエキス、コラーゲン、コケモモエキス、サイシンエキス、サイコエキス、サイタイ抽出液、サルビアエキス、サボンソウエキス、ササエキス、サンザシエキス、サンショウエキス、シイタケエキス、ジオウエキス、シコンエキス、シソエキス、シナノキエキス、シモツケソウエキス、シャクヤクエキス、ショウブ根エキス、シラカバエキス、スギナエキス、セイヨウキズタエキス、セイヨウサンザシエキス、セイヨウニワトコエキス、セイヨウノコギリソウエキス、セイヨウハッカエキス、セ-ジエキス、ゼニアオイエキス、センキュウエキス、センブリエキス、ダイズエキス、タイソウエキス、タイムエキス、茶エキス、チョウジエキス、チガヤエキス、チンピエキス、トウキエキス、トウキンセンカエキス、トウニンエキス、トウヒエキス、ドクダミエキス、トマトエキス、納豆エキス、ニンジンエキス、ニンニクエキス、ノバラエキス、ハイビスカスエキス、バクモンドウエキス、パセリエキス、蜂蜜、ハマメリスエキス、パリエタリアエキス、ヒキオコシエキス、ビサボロール、ビワエキス、フキタンポポエキス、フキノトウエキス、ブクリョウエキス、ブッチャーブルームエキス、ブドウエキス、プロポリス、ヘチマエキス、ベニバナエキス、ペパーミントエキス、ボダイジュエキス、ボタンエキス、ホップエキス、マツエキス、マロニエエキス、ミズバショウエキス、ムクロジエキス、メリッサエキス、モモエキス、ヤグルマギクエキス、ユーカリエキス、ユキノシタエキス、ヨクイニンエキス、ヨモギエキス、ラベンダーエキス、リンゴエキス、レタスエキス、レモンエキス、レンゲソウエキス、ローズエキス、ローズマリーエキス、ローマカミツレエキス、ローヤルゼリーエキス等を挙げることができる。
 また、デオキシリボ核酸、ムコ多糖類、ヒアルロン酸ナトリウム、コンドロイチン硫酸ナトリウム、コラーゲン、エラスチン、キチン、キトサン、加水分解卵殻膜などの生体高分子、アミノ酸、加水分解ペプチド、乳酸ナトリウム、尿素、ピロリドンカルボン酸ナトリウム、ベタイン、ホエイ、トリメチルグリシンなどの保湿成分、スフィンゴ脂質、セラミド、フィトスフィンゴシン、コレステロール、コレステロール誘導体、リン脂質などの油性成分、ε-アミノカプロン酸、グリチルリチン酸、β-グリチルレチン酸、塩化リゾチーム、グアイアズレン、ヒドロコールチゾン等の免疫賦活剤、ビタミンA、ビタミンB2、ビタミンB6、ビタミンC、ビタミンD、ビタミンE、パントテン酸カルシウム、ビオチン、ニコチン酸アミド、ビタミンCエステル等のビタミン類、アラントイン、ジイソプロピルアミンジクロロアセテート、4-アミノメチルシクロヘキサンカルボン酸等の活性成分、トコフェロール、カロチノイド、フラボノイド、タンニン、リグナン、サポニン等の抗酸化剤、α-ヒドロキシ酸、β-ヒドロキシ酸などの細胞賦活剤、γ-オリザノール、ビタミンE誘導体などの血行促進剤、レチノール、レチノール誘導体等の創傷治癒剤、アルブチン、コウジ酸、プラセンタエキス、イオウ、エラグ酸、リノール酸、トラネキサム酸、グルタチオン等の美白剤、セファランチン、カンゾウ抽出物、トウガラシチンキ、ヒノキチオール、ヨウ化ニンニクエキス、塩酸ピリドキシン、DL-α-トコフェロール、酢酸DL-α-トコフェロール、ニコチン酸、ニコチン酸誘導体、パントテン酸カルシウム、D-パントテニルアルコール、アセチルパントテニルエチルエーテル、ビオチン、アラントイン、イソプロピルメチルフェノール、エストラジオール、エチニルエストラジオール、塩化カプロニウム、塩化ベンザルコニウム、塩酸ジフェンヒドラミン、タカナール、カンフル、サリチル酸、ノニル酸バニリルアミド、ノナン酸バニリルアミド、ピロクトンオラミン、ペンタデカン酸グリセリル、L-メントール、モノニトログアヤコール、レゾルシン、γ-アミノ酪酸、塩化ベンゼトニウム、塩酸メキシレチン、オーキシン、女性ホルモン、カンタリスチンキ、シクロスポリン、ジンクピリチオン、ヒドロコールチゾン、ミノキシジル、モノステアリン酸ポリオキシエチレンソルビタン、ハッカ油、ササニシキエキス、プラセンタ、ユズ種子エキス、ブルーベリーエキス、リンゴンベリーエキス、カンカニクジュヨウエキス、黒米エキス、生コーヒー豆エキス、レスベラトロール、キウイ種子エキス、イチゴ種子エキス、桜エキス等の育毛剤などが挙げられる。
(9) Examples of physiologically active ingredients Examples of physiologically active ingredients include substances that impart some physiological activity to the skin when applied to the skin. For example, whitening ingredients, immunostimulants, anti-aging agents, UV protection agents, slimming agents, tanning agents, antioxidants, hair growth agents, hair restorers, moisturizers, blood circulation promoters, antibacterial agents, bactericides, desiccants, A cooling sensation agent, a warming sensation agent, vitamins, an amino acid, a wound healing promoter, an irritation relaxation agent, an analgesic agent, a cell activator, an enzyme component, etc. are mentioned. Examples of these suitable ingredients include, for example, ashitaba extract, avocado extract, amateur extract, altea extract, arnica extract, aloe extract, apricot extract, apricot kernel extract, ginkgo biloba extract, fennel extract, turmeric extract, oolong tea extract, ages Extract, Echinacea leaf extract, Ogon extract, Oat extract, Oen extract, Barley extract, Hypericum extract, Oyster extract, Dutch mustard extract, Orange extract, Seawater dried product, Seaweed extract, Hydrolyzed elastin, Hydrolyzed wheat powder, Hydrolyzed silk , Chamomile extract, Carrot extract, Kawara mugwort extract, Licorice extract, Calcade extract, Oyster extract, Kina extract, Cucumber extract, Guanosine, Gardenia extract, Kumazasa extract, Clarae Kiss, walnut extract, grapefruit extract, clematis extract, chlorella extract, mulberry extract, gentian extract, tea extract, yeast extract, burdock extract, fermented rice bran extract, rice germ oil, comfrey extract, collagen, bilberry extract, saicin extract, psycho extract Extract Kizuta extract, hawthorn extract, elderberry extract, yarrow extract, mint extract, sage extract, mallow extract, senki Sue extract, assembly extract, soybean extract, tiso extract, thyme extract, tea extract, clove extract, chigaya extract, chimpi extract, touki extract, toshinsen extract, tonin extract, spruce extract, dokudami extract, tomato extract, natto extract, carrot extract, garlic extract, Novara extract, hibiscus extract, bacmond extract, parsley extract, honey, hamamelis extract, parietalia extract, toad extract, bisabolol, loquat extract, dandelion extract, burdock extract, bukuro extract, butcher bloom extract, grape extract, propolis, loofah extract, Safflower extract, peppermint extract, bodaige extract, button extract, hop extract, pine extract, marronnier extract, mizubasho Kiss, Mukuroji extract, Melissa extract, Peach extract, Cornflower extract, Eucalyptus extract, Yukinoshita extract, Yokuinin extract, Artemisia extract, Lavender extract, Apple extract, Lettuce extract, Lemon extract, Lotus root extract, Rose extract, Rosemary extract, Roman chamomile extract And royal jelly extract.
Biopolymers such as deoxyribonucleic acid, mucopolysaccharide, sodium hyaluronate, sodium chondroitin sulfate, collagen, elastin, chitin, chitosan, hydrolyzed eggshell membranes, amino acids, hydrolyzed peptides, sodium lactate, urea, sodium pyrrolidonecarboxylate , Moisturizing ingredients such as betaine, whey, trimethylglycine, oily ingredients such as sphingolipid, ceramide, phytosphingosine, cholesterol, cholesterol derivatives, phospholipids, ε-aminocaproic acid, glycyrrhizic acid, β-glycyrrhetinic acid, lysozyme chloride, guaiazulene, Immunostimulants such as hydrocortisone, vitamin A, vitamin B2, vitamin B6, vitamin C, vitamin D, vitamin E, calcium pantothenate, biotin, nicotinamide, vitamin C ester Vitamins, active ingredients such as allantoin, diisopropylamine dichloroacetate, 4-aminomethylcyclohexanecarboxylic acid, antioxidants such as tocopherol, carotenoid, flavonoid, tannin, lignan, saponin, α-hydroxy acid, β-hydroxy acid, etc. Cell activators, blood circulation promoters such as γ-oryzanol and vitamin E derivatives, wound healing agents such as retinol and retinol derivatives, arbutin, kojic acid, placenta extract, sulfur, ellagic acid, linoleic acid, tranexamic acid, glutathione, etc. Whitening agent, cephalanthin, licorice extract, red pepper tincture, hinokitiol, garlic iodide extract, pyridoxine hydrochloride, DL-α-tocopherol, DL-α-tocopherol acetate, nicotinic acid, nicotinic acid derivative, calcium pantothenate, D-pan Tothenyl alcohol, acetyl pantothenyl ethyl ether, biotin, allantoin, isopropylmethylphenol, estradiol, ethinyl estradiol, capronium chloride, benzalkonium chloride, diphenhydramine hydrochloride, takanal, camphor, salicylic acid, nonyl acid vanillylamide, nonanoic acid vanillylamide, pyroctone Olamine, glyceryl pentadecanoate, L-menthol, mononitroguaiacol, resorcin, γ-aminobutyric acid, benzethonium chloride, mexiletine hydrochloride, auxin, female hormone, cantalis tincture, cyclosporine, zinc pyrithione, hydrocortisone, minoxidil, monostearic acid Polyoxyethylene sorbitan, peppermint oil, Sasanishiki extract, placenta, yuzu seed extract, bull Berry extract, lingonberry extract, C. tubulosa extract, black rice extract, green coffee bean extract, resveratrol, kiwi seed extract, strawberry seed extract, and the like hair tonic such as cherry extract.
(10)酸化防止剤の例
 亜硫酸水素ナトリウム、亜硫酸ナトリウム、エリソルビン酸、エリソルビン酸ナトリウム、チオジプロピオン酸ジラウリル、トコフェロール、トリルビグアナイド、ノルジヒドログアヤレチン酸、パラヒドロキシアニソール、ブチルヒドロキシアニソール、ジブチルヒドロキシトルエン、ステアリン酸アスコルビル、パルミチン酸アスコルビル、没食子酸オクチル、没食子酸プロピル、カロチノイド、フラボノイド、タンニン、リグナン、サポニン、リンゴエキスやチョウジエキスなどの酸化防止効果の認められる植物エキス等が挙げられる。
(10) Examples of antioxidants Sodium bisulfite, sodium sulfite, erythorbic acid, sodium erythorbate, dilauryl thiodipropionate, tocopherol, tolyl biguanide, nordihydroguaiaretic acid, parahydroxyanisole, butylhydroxyanisole, dibutylhydroxy Examples include plant extracts having an antioxidant effect such as toluene, ascorbyl stearate, ascorbyl palmitate, octyl gallate, propyl gallate, carotenoid, flavonoid, tannin, lignan, saponin, apple extract and clove extract.
(11)溶媒の例
 精製水、エタノール、低級アルコール、エーテル類、LPG、フルオロカーボン、N-メチルピロリドン、フルオロアルコール、揮発性直鎖状シリコーン、次世代フロン等が挙げられる。
(11) Examples of solvents Purified water, ethanol, lower alcohol, ethers, LPG, fluorocarbon, N-methylpyrrolidone, fluoroalcohol, volatile linear silicone, next-generation chlorofluorocarbon and the like.
 以下に、本発明を具体化した実施例について説明する。本発明は下記実施例に限定されない。
〈実施例:紫茶抽出物(GHG含有組成物)の作製〉
 紫茶葉50gを50%エタノール水溶液500mLに浸漬し、撹拌しながら40℃で2時間加熱還流することにより抽出した。吸引ろ過により抽出液400mLを得た。抽出液を濃縮・乾固し紫茶抽出物を16.6g得た。
Examples that embody the present invention will be described below. The present invention is not limited to the following examples.
<Example: Production of purple tea extract (composition containing GHG)>
Extraction was performed by immersing 50 g of purple tea leaves in 500 mL of 50% ethanol aqueous solution and heating to reflux at 40 ° C. for 2 hours with stirring. 400 mL of extract was obtained by suction filtration. The extract was concentrated and dried to obtain 16.6 g of purple tea extract.
〈紫茶抽出物の成分分析〉
 紫茶抽出物について、下記の条件でHPLC分析を行ったところ、27.5minの箇所に緑茶やウーロン茶、紅茶などの一般のお茶には含まれない紫茶抽出物に特有成分のピークを確認した(図1の矢印部分)。
〈サンプル調整〉
 紫茶抽出物350mgを30%メタノール水溶液に溶解し、メスフラスコで20mLに定容した。溶液を2倍希釈し、フィルターろ過後HPLC分析を行った。HPLCの分析条件は以下のとおりである。
〈HPLC分析条件〉
流速:0.7 mL/min
移動相A:0.3%TFA水溶液
移動相B:アセトニトリル
グラジエント:下記表1のとおり
カラム:SunFire C18, 4.6×150 mm (Waters) または同等品
カラム温度:30℃
サンプル注入量:10μL
検出波長:280 nm
<Ingredient analysis of purple tea extract>
When the purple tea extract was subjected to HPLC analysis under the following conditions, a peak of a specific component of the purple tea extract not contained in general tea such as green tea, oolong tea and black tea was confirmed at 27.5 min ( Arrow portion in FIG. 1).
<Sample adjustment>
350 mg of purple tea extract was dissolved in 30% aqueous methanol solution, and the volume was adjusted to 20 mL with a volumetric flask. The solution was diluted 2 times, filtered and subjected to HPLC analysis. The analysis conditions of HPLC are as follows.
<HPLC analysis conditions>
Flow rate: 0.7 mL / min
Mobile phase A: 0.3% TFA aqueous solution Mobile phase B: Acetonitrile gradient: As shown in Table 1 below: Column: SunFire C18, 4.6 x 150 mm (Waters) or equivalent Column temperature: 30 ° C
Sample injection volume: 10 μL
Detection wavelength: 280 nm
Figure JPOXMLDOC01-appb-T000002
Figure JPOXMLDOC01-appb-T000002
 上記特有成分について分離精製を行いNMR分析を行った。その結果を表2に示す。表2に示すように、NMR分析値と文献値とを比較した結果、既知成分1,2-di-O-galloyl-4,6-O-(S)-hexahydroxydiphenoyl-b -D-glucose(GHG)と同定した。 The above specific components were separated and purified and subjected to NMR analysis. The results are shown in Table 2. As shown in Table 2, as a result of comparison between NMR analysis values and literature values, the known component 1,2-di-O-galloyl-4,6-O- (S) -hexahydroxydiphenoyl-b -D-glucose (GHG ).
Figure JPOXMLDOC01-appb-T000003
Figure JPOXMLDOC01-appb-T000003
 GHG精製品を標準物質として、HPLCによる定量分析を行った結果、紫茶抽出物中にはGHGが8.70質量%含有していた。
 上述した方法と同様にして紫茶抽出物を更に別途更に2回調整し同様の方法にて抽出物中のGHG含有量を測定した結果GHGの含有量はそれぞれ6.79質量%、6.38質量%であった。これにより、本実施例の方法にて製造された紫茶抽出物には約6~9質量%のGHGを含有することが確認された。
As a result of quantitative analysis by HPLC using GHG purified product as a standard substance, the purple tea extract contained 8.70% by mass of GHG.
The purple tea extract was further separately prepared twice in the same manner as described above, and the GHG content in the extract was measured by the same method. As a result, the GHG contents were 6.79% by mass and 6.38, respectively. It was mass%. As a result, it was confirmed that the purple tea extract produced by the method of this example contained about 6 to 9% by mass of GHG.
 〈試験例1:オリーブ油負荷マウスにおける血中トリグリセリド上昇に及ぼす作用の評価〉
 絶食(15時間)したマウスの眼窩静脈嚢より,ガラスキャピラリーを用いて採血を行い,その30分後に,上記本実施例の紫茶抽出物(100, 200 mg/kg)を経口投与した。1時間後にオリーブ油(5 mL/kg)を経口投与し,その後2,4および6時間目において眼窩静脈嚢から同様に採血を行った。得られた血液から血清を遠心分離し,トリグリセリド濃度を酵素法(トリグリセリドE-テストワコー,和光純薬工業社製)を用いて測定した。その結果を図2のAに示す。
 更に、紫茶抽出物(100, 200 mg/kg)に変えて紫茶抽出物(400 mg/kg)及び抗肥満薬として知られるオールスタットの5w/v %アラビアガム懸濁液(10, 20mg/kg)を用いて同様の試験を行った。その結果を図2のBに示す。
<Test Example 1: Evaluation of effects on blood triglyceride elevation in olive oil-loaded mice>
Blood was collected from the orbital venous sac of a fasted mouse (15 hours) using a glass capillary, and 30 minutes later, the purple tea extract (100, 200 mg / kg) of this example was orally administered. One hour later, olive oil (5 mL / kg) was orally administered, and blood was similarly collected from the orbital venous sac at 2, 4 and 6 hours thereafter. Serum was centrifuged from the obtained blood, and triglyceride concentration was measured using an enzymatic method (Triglyceride E-Test Wako, Wako Pure Chemical Industries, Ltd.). The result is shown in FIG.
Furthermore, instead of purple tea extract (100, 200 mg / kg), purple tea extract (400 mg / kg) and allstat 5w / v% gum arabic suspension known as anti-obesity drug (10, 20mg / kg) was used for the same test. The result is shown in FIG.
 〈結果及び試験例1における実施例の効果〉
 図2Aに示すように、オリーブ油投与マウス(control)の血中トリグリセリドは、非投与マウス(Normal)と比較して上昇した。これに対し、紫茶抽出物(100, 200 mg/kg)をあらかじめ投与したマウスにおいては、血中トリグリセリドの上昇を抑制する傾向が認められた。また、図2Bに示すように、400 mg/kgの紫茶抽出物を投与したマウスでは、オリーブ油投与4および6時間目において有意な血中トリグリセリドの低下が認められた。抗肥満薬のオーリスタットは10および20 mg/kgで有意な血中トリグリセリドの上昇抑制作用を示した。
 以上により、本実施例の紫茶抽出物(GHG含有組成物)は、脂肪吸収抑制剤、血中トリグリセリドの上昇抑制剤として使用することができることが確認された。
<Results and Effects of Examples in Test Example 1>
As shown in FIG. 2A, blood triglycerides in olive oil-administered mice (control) increased compared to non-administered mice (Normal). In contrast, in mice pre-administered with purple tea extract (100, 200 mg / kg), there was a tendency to suppress the rise in blood triglycerides. In addition, as shown in FIG. 2B, in the mice administered with 400 mg / kg purple tea extract, a significant decrease in blood triglycerides was observed at 4 and 6 hours after olive oil administration. The anti-obesity drug orlistat significantly increased blood triglycerides at 10 and 20 mg / kg.
From the above, it was confirmed that the purple tea extract (GHG-containing composition) of this example can be used as a fat absorption inhibitor and a blood triglyceride rise inhibitor.
〈試験例2:高脂肪食飼育マウスにおける体重増加抑制作用〉
 マウス(ICR,雄,10週齢)に,高脂肪食(High Fat Diet 32)を自由摂取させるとともに,紫茶抽出物(200 mg/kg)を1日1回経口投与した。比較対象には通常食(CE-2)自由摂取させた。この間12日間にわたり体重を毎日測定した。その結果を図3に示す。
<Test Example 2: Weight gain inhibitory effect in mice fed with high fat diet>
Mice (ICR, male, 10 weeks old) were allowed to freely take a high fat diet (High Fat Diet 32) and orally administered purple tea extract (200 mg / kg) once a day. The subject of comparison was a regular diet (CE-2) ad libitum. During this time, body weight was measured daily for 12 days. The result is shown in FIG.
〈結果及び試験例2における実施例の効果〉
 図3に示すように、高脂肪食を摂取させたマウス(Control)の体重は、実験開始7日目から、通常食飼育マウスの体重を上回った。これに対し、紫茶抽出物(200 mg/kg)を経口投与したマウスの体重は、他のグループと比較して明らかな低値を示した。以上により、本実施例の紫茶抽出物(GHG含有組成物)は、高脂肪食マウスにおける体重抑制作用を有し、これにより、ダイエット剤(体重抑制剤)として使用することができることが確認された。
<Results and Effects of Examples in Test Example 2>
As shown in FIG. 3, the body weight of the mouse (Control) fed with the high fat diet exceeded the body weight of the normal diet-fed mice from the 7th day of the experiment. On the other hand, the body weight of the mice to which purple tea extract (200 mg / kg) was orally administered showed a clearly low value as compared with other groups. From the above, it was confirmed that the purple tea extract (GHG-containing composition) of this example has a body weight-suppressing action in high-fat diet mice and can be used as a dieting agent (body weight-suppressing agent). It was.
 以下に本発明の効果に起因する紫茶抽出物(GHG含有組成物)の配合例を挙げるが、下記配合例は本発明を限定するものではない。
 配合例1:チューインガム
      砂糖                 53.0wt%
      ガムベース              20.0
      グルコース              10.0
      水飴                 16.0
      香料                  0.5
      紫茶抽出物               0.5  
                        100.0wt%
Although the compounding example of the purple tea extract (GHG containing composition) resulting from the effect of this invention is given to the following, the following compounding example does not limit this invention.
Formulation Example 1: Chewing gum Sugar 53.0wt%
Gum base 20.0
Glucose 10.0
Minamata 16.0
Fragrance 0.5
Purple tea extract 0.5
100.0wt%
 配合例2:グミ
      還元水飴               40.0wt%
      グラニュー糖             20.0
      ブドウ糖               20.0
      ゼラチン                4.7
      水                   9.68
      ブドウ果汁               4.0
      ブドウフレーバー            0.6
      色素                  0.02
      紫茶抽出物               1.0  
                        100.0wt%
Formulation Example 2: Gummy reduced starch syrup 40.0 wt%
Granulated sugar 20.0
Glucose 20.0
Gelatin 4.7
Water 9.68
Grape juice 4.0
Grape flavor 0.6
Dye 0.02
Purple tea extract 1.0
100.0wt%
 配合例3:キャンディー
      砂糖                 50.0wt%
      水飴                 33.0
      水                  14.4
      有機酸                 2.0
      香料                  0.2
      紫茶抽出物               0.4  
                        100.0wt%
Formulation Example 3: Candy Sugar 50.0wt%
Minamata 33.0
Water 14.4
Organic acid 2.0
Fragrance 0.2
Purple tea extract 0.4
100.0wt%
 配合例4:ヨーグルト(ハード・ソフト)
      牛乳                 41.5wt%
      脱脂粉乳                5.8
      砂糖                  8.0
      寒天                  0.15
      ゼラチン                0.1
      乳酸菌                 0.005
      紫茶抽出物               0.4  
      香料                   微量  
      水                    残余  
                        100.0wt%
Formulation Example 4: Yogurt (hard / soft)
Milk 41.5wt%
Nonfat dry milk 5.8
Sugar 8.0
Agar 0.15
Gelatin 0.1
Lactic acid bacteria 0.005
Purple tea extract 0.4
Perfume
Water residue
100.0wt%
 配合例5:清涼飲料
      果糖ブドウ糖液糖           30.0wt%
      乳化剤                 0.5
      紫茶抽出物               0.05
      香料                   適量
      精製水                  残余  
                        100.0wt%
Formulation Example 5: Soft drink Fructose glucose liquid sugar 30.0wt%
Emulsifier 0.5
Purple tea extract 0.05
Perfume
Purified water residue
100.0wt%
 配合例6:ソフトカプセル
      ブドウ種子油             87.0wt%
      乳化剤                12.0
      紫茶抽出物               1.0  
                        100.0wt%
Formulation Example 6: Soft capsule Grape seed oil 87.0wt%
Emulsifier 12.0
Purple tea extract 1.0
100.0wt%
 配合例7:錠剤
      乳糖                 54.0wt%
      結晶セルロース            30.0
      澱粉分解物              10.0
      グリセリン脂肪酸エステル        5.0
      紫茶抽出物               1.0  
                        100.0wt%
Formulation Example 7: Tablet Lactose 54.0 wt%
Crystalline cellulose 30.0
Starch degradation product 10.0
Glycerin fatty acid ester 5.0
Purple tea extract 1.0
100.0wt%
 配合例8:顆粒内服剤(医薬品)
      紫茶抽出物               1.0wt%
      乳糖                 30.0
      コーンスターチ            60.0
      結晶セルロース             8.0
      ポリビニールピロリドン         1.0  
                        100.0wt%
Formulation Example 8: Oral granules (pharmaceuticals)
Purple tea extract 1.0wt%
Lactose 30.0
Cornstarch 60.0
Crystalline cellulose 8.0
Polyvinylpyrrolidone 1.0
100.0wt%
 配合例9:錠菓
      砂糖                 76.4wt%
      グルコース              19.0
      ショ糖脂肪酸エステル          0.2
      紫茶抽出物               0.5
      精製水                 3.9  
                        100.0wt%
Formulation Example 9: Tablets Sugar 76.4 wt%
Glucose 19.0
Sucrose fatty acid ester 0.2
Purple tea extract 0.5
Purified water 3.9
100.0wt%
 配合例10:化粧クリーム
      スクワラン              20.0wt%
      ミツロウ                5.0
      精製ホホバ油              5.0
      グリセリン               5.0
      グリセリンモノステアレート       2.0
      ポリオキシエチレン(20)ソルビタン-
      モノステアレート            2.0
      紫茶抽出物               2.0
      防腐剤                  適量
      香料                   適量
      精製水                  残余  
                        100.0wt%
Formulation Example 10: Cosmetic cream Squalane 20.0 wt%
Beeswax 5.0
Refined jojoba oil 5.0
Glycerin 5.0
Glycerol monostearate 2.0
Polyoxyethylene (20) sorbitan-
Monostearate 2.0
Purple tea extract 2.0
Preservative appropriate amount Fragrance proper amount
Purified water residue
100.0wt%
 配合例11:化粧水
      エタノール               5.0wt%
      グリセリン               2.0
      1,3-ブチレングリコール         2.0
      ポリエチレンオレイルエーテル      0.5
      クエン酸ナトリウム           0.1
      クエン酸                0.1
      紫茶抽出物               0.1
      精製水                  残余  
                        100.0wt%
Formulation Example 11: Lotion Ethanol 5.0 wt%
Glycerin 2.0
1,3-Butylene glycol 2.0
Polyethylene oleyl ether 0.5
Sodium citrate 0.1
Citric acid 0.1
Purple tea extract 0.1
Purified water residue
100.0wt%
 配合例12:ボディージェル
      マカデミアナッツ油           2.0wt%
      ミリスチン酸オクチルドデシル     10.0
      メチルフェニルポリシロキサン      5.0
      ベヘニルアルコール           3.0
      ステアリン酸              3.0
      バチルアルコール            1.0
      モノステアリン酸グリセリル       1.0
      テトラオレイン酸ポリオキシエチレンソルビット
                          2.0
      水素添加大豆リン脂質          1.0
      セラミド                0.1
      パルミチン酸レチノール         0.1
      防腐剤                  適量
      ツボクサ抽出物             1.0
      紫茶抽出物               1.0
      1、3-ブチレングリコール       5.0
      精製水                  残余  
                        100.0wt%
Formulation Example 12: Body Gel Macadamia Nuts Oil 2.0wt%
Octyldodecyl myristate 10.0
Methylphenylpolysiloxane 5.0
Behenyl alcohol 3.0
Stearic acid 3.0
Batyl alcohol 1.0
Glyceryl monostearate 1.0
Tetraoleic acid polyoxyethylene sorbit 2.0
Hydrogenated soybean phospholipid 1.0
Ceramide 0.1
Retinol palmitate 0.1
Preservative Appropriate amount Clover extract 1.0
Purple tea extract 1.0
1,3-butylene glycol 5.0
Purified water residue
100.0wt%
 配合例13:乳液
      スクワラン               4.0wt%
      ワセリン                2.5
      セタノール               2.0
      グリセリン               2.0
      親油型モノステアリン酸グリセリン    1.0
      ステアリン酸              1.0
      L-アルギニン             1.0
      紫茶抽出物               0.5
      水酸化カリウム             0.1
      香料                   微量
      精製水                  残余  
                        100.0wt%
Formulation Example 13: Latex Squalane 4.0 wt%
Vaseline 2.5
Cetanol 2.0
Glycerin 2.0
Lipophilic glyceryl monostearate 1.0
Stearic acid 1.0
L-Arginine 1.0
Purple tea extract 0.5
Potassium hydroxide 0.1
Perfume
Purified water residue
100.0wt%
 配合例14:浴用剤(液状)
      プロピレングリコール         50.0wt%
      エタノール              20.0
      硫酸ナトリウム             5.0
      紫茶抽出物               0.5
      ラノリン                0.5
      アボガド油               0.5
      色素                  1.5
      香料                 22.0  
                        100.0wt%
Formulation Example 14: Bath agent (liquid)
Propylene glycol 50.0wt%
Ethanol 20.0
Sodium sulfate 5.0
Purple tea extract 0.5
Lanolin 0.5
Avocado oil 0.5
Dye 1.5
Fragrance 22.0
100.0wt%
配合例15:シャンプー
   ポリオキシエチレンアルキルエーテル硫酸ナトリウム
     (E.O2モル)            15.0
     ヤシ油脂肪族ジエタノールアミド      5.0
     グリセリン                3.0
     紫茶抽出物                0.4
     エタノール                5.0
     香料及び防腐剤               適量
     イオン交換水                残余  
                        100.0wt%
Formulation Example 15: Shampoo Sodium polyoxyethylene alkyl ether sulfate (E.O2 mol) 15.0
Palm oil aliphatic diethanolamide 5.0
Glycerin 3.0
Purple tea extract 0.4
Ethanol 5.0
Perfume and preservatives
Ion exchange water
100.0wt%
配合例16:ヘヤークリーム
     流動パラフィン             20.0wt%
     固形パラフィン              3.0
     ポリオキシエチレンセチル エーテル
                   (E.O15モル)
                          2.0
     ソルビタンセスキオレート         1.0
     紫茶抽出物                0.2
     エタノール               10.0
     水酸化カリウム              0.1
     グリセリン                3.0
     香料及び防腐剤               適量 
                        100.0wt%
Formulation Example 16: Hair Cream Liquid Paraffin 20.0wt%
Solid paraffin 3.0
Polyoxyethylene cetyl ether (E.O15 mol)
2.0
Sorbitan sesquioleate 1.0
Purple tea extract 0.2
Ethanol 10.0
Potassium hydroxide 0.1
Glycerin 3.0
Perfume and preservatives
100.0wt%
配合例17:軟膏剤
     サラシミツロウ              5.0wt%
     精製ラノリン               5.0
     紫茶抽出物                1.0
     香料                   0.1
     ワセリン                  残余  
                        100.0wt%
Formulation Example 17: Salve Beeswax 5.0wt%
Purified lanolin 5.0
Purple tea extract 1.0
Fragrance 0.1
Vaseline residue
100.0wt%
 以上、説明したように、本発明は、天然物由来の組成物であってGHGを高濃度で含有するGHG含有組成物、並びにその製造方法を提供することができる。更に、新規な植物またはその抽出物を有効成分とする脂肪吸収抑制剤を提供することができる。 As described above, the present invention can provide a GHG-containing composition that is a composition derived from a natural product and contains GHG at a high concentration, and a method for producing the same. Furthermore, the fat absorption inhibitor which uses a novel plant or its extract as an active ingredient can be provided.

Claims (6)

  1.  ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)から得られ、1,2-di-O-galloyl-4,6-O-(S)-hexahydroxydiphenoyl-b -D-glucose (以下、略して「GHG」という。)を含有することを特徴とするGHG含有組成物。 1,2-di-O-galloyl-4,6-O- (S) -hexahydroxydiphenoyl-b -D-glucose (abbreviated below) obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306) GGH containing composition characterized by containing "GHG").
  2.  ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)から得られ、GHGを3~10%質量含有することを特徴とするGHG含有組成物。 GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306) and containing 3 to 10% by mass of GHG.
  3.  ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)を極性溶媒(水をも含む)に浸漬し、その後、加熱還流して溶媒中にGHGを抽出することを特徴とするGHG含有組成物の製造方法。 A GHG-containing composition characterized in that purple tea from Kenya (scientific name: Camellia sinensis, variety TRFK306) is immersed in a polar solvent (including water) and then heated to reflux to extract GHG in the solvent. Production method.
  4.  ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)及び/またはその抽出物を有効成分とする脂肪吸収抑制剤。 A fat absorption inhibitor containing Kenya purple tea (scientific name: Camellia sinensis, variety TRFK306) and / or its extract as an active ingredient.
  5.  ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)から得られるGHG含有組成物を有効成分とする脂肪吸収抑制剤。 Fat absorption inhibitor containing GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306) as an active ingredient.
  6.  ケニア産紫茶(学名:Camellia sinensis、品種名TRFK306)から得られるGHG含有組成物を有効成分とする体重増加抑制剤。 A weight gain inhibitor comprising as an active ingredient a GHG-containing composition obtained from Kenyan purple tea (scientific name: Camellia sinensis, variety TRFK306).
PCT/JP2014/070974 2013-08-12 2014-08-08 Ghg-containing composition and fat absorption inhibitor using same WO2015022909A1 (en)

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