Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
  • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
  • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L2/00—Non-alcoholic beverages; Dry compositions or concentrates therefor; Preparation or treatment thereof
  • A23L2/52—Adding ingredients
• • A—HUMAN NECESSITIES
  • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
  • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
  • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
  • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
  • A61K8/20—Halogens; Compounds thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
  • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
  • A61K8/4986—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with sulfur as the only hetero atom
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/67—Vitamins
  • A61K8/676—Ascorbic acid, i.e. vitamin C
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/10—Dispersions; Emulsions
  • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
  • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
  • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q1/00—Make-up preparations; Body powders; Preparations for removing make-up
  • A61Q1/02—Preparations containing skin colorants, e.g. pigments
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
  • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin

Definitions

• the present invention relates to a composition containing salacinol, an external preparation for skin, a cosmetic, and a food and drink.
• Salacinol discovered from a plant of the genus Salacia is a thiosaccharide derivative having a unique structure, and has a structure represented by the formula (1) described later.
• a component obtained from a Salacia plant extract containing a compound represented by the formula (1) is referred to as salacinol. Since salacinol has an ability to inhibit small intestine ⁇ -glucosidase and has an action of slowing the absorption of carbohydrates, research is being conducted as a candidate for a new antidiabetic agent (see, for example, Japanese Patent No. 3030008).
• Salacinol is known to exhibit various physiological activities including melanin production suppression in addition to its ability to inhibit small intestine ⁇ -glucosidase, and is expected to be applied to quasi-drugs and pharmaceutical cosmetics (for example, JP, 2011-88886, JP, 2012-206982, A).
• extract of the plant belonging to the genus Salacia Korean Patent Application to Cosmetics
• application to cosmetics is disclosed (for example, see JP-A-2006-188463).
• the stability of Salacia plant extracts has been studied for the purpose of use as a food (see, for example, “Kotarahim” edited by the Ministry of Agriculture and Fisheries recommended confectionery technology center).
• the invention described in Japanese Patent No. 3030008 is an invention relating to a novel salacinol compound that is useful as an antidiabetic agent, and does not consider the stabilization of salacinol.
• the invention described in Japanese Patent Application Laid-Open No. 2011-88886 is an invention that focuses on the melanin production-inhibiting function of salacinol
• Japanese Patent Application Laid-Open No. 2012-206982 is an invention that focuses on the processing glucosidase inhibitory action of salacinol.
• the stabilization of salacinol has not been studied.
• Kotara Himubutu extract which is a plant extract of the genus Salacia, and its application to whitening cosmetics is disclosed, but focusing on salacinol as an active ingredient
• Kotarahim a confectionery technical center recommended by the Ministry of Agriculture, Fisheries and Technology, examines the application of Kotarahim, a plant extract of the Salacia genus, to foods, and examines its solubility when applied to foods.
• glucosidase inhibitory activity it does not focus on salacinol as an active ingredient, and the stability improvement of salacinol has not been studied.
• the subject of this invention is providing the composition which the decomposition
• Another subject of this invention is providing the skin external preparation, cosmetics, and food-drinks containing the composition containing the salacinol excellent in stability.
• the present inventors have solved the above problems by containing at least one compound selected from citric acid and its salts and a specific magnesium salt. Found to get.
• the present invention is as follows.
• composition according to [1] wherein the content of the compound represented by the formula (1) is 0.001% by mass to 10% by mass with respect to the total amount of the composition.
• composition according to [1] or [2] which has a pH of 8.0 or less.
• [5] A skin external preparation containing the composition according to any one of [1] to [4].
• [6] A cosmetic comprising the composition according to any one of [1] to [4].
• [7] A food or drink comprising the composition according to any one of [1] to [4].
• composition having a pH of 8.0 or less containing a compound represented by the following formula (1) [8] A composition having a pH of 8.0 or less containing a compound represented by the following formula (1).
• composition according to [8] wherein the content of the compound represented by the formula (1) is 0.001% by mass to 10% by mass with respect to the total amount of the composition.
• the inorganic salt of magnesium contains magnesium chloride.
• An external preparation for skin comprising the composition according to any one of [8] to [12].
• a cosmetic comprising the composition according to any one of [8] to [12].
• a food or drink comprising the composition according to any one of [8] to [12].
• denaturation of the salacinol in the composition containing a salacinol is suppressed, and the composition excellent in stability can be provided.
• the skin external preparation, cosmetics, and food / beverage products containing the composition containing the salacinol excellent in stability can be provided.
• composition according to the first aspect of the present invention includes a compound represented by the following formula (1), at least one compound selected from citric acid and a salt thereof, an inorganic salt of magnesium, and 5 or less carbon atoms. And at least one compound selected from organic salts of magnesium having the above organic group.
• the composition according to the second embodiment of the present invention is a composition having a pH of 8.0 or less containing a compound represented by the following formula (1).
• the composition in the second form preferably further contains at least one compound selected from citric acid and salts thereof, and further includes an inorganic salt of magnesium and an organic magnesium having an organic group having 5 or less carbon atoms. More preferably, it contains at least one compound selected from salts.
• a numerical range indicated by using “to” indicates a range including the numerical values described before and after “to” as the minimum value and the maximum value, respectively.
• the amount of each component in the composition means the total amount of the plurality of substances present in the composition unless there is a specific notice when there are a plurality of substances corresponding to each component in the composition. To do.
• embodiments of the present invention will be described more specifically.
• composition of the present invention is called salacinol, and 1,4-Dioxy-1,4-[(S)-[(2S, 3S)- 2,4-dihydroxy-3- (sulfoxy) butyl] episulfoniumlide] -D-arabinitol Inner Salt (IUPAC name), CAS No .; 20000399-47-9.
• salacinol a compound obtained by any of biosynthesis, chemical synthesis, and extraction and purification from plants can be used in the present invention.
• Examples of a method for obtaining salacinol by extraction and purification from a plant include a method for isolation and purification from a plant of the genus Salacia or an extract of the plant of the genus Salacia using a known method, for example, preparative chromatography.
• the plant of the genus Salacia is a plant belonging to the Decinum family that grows mainly in India and Southeast Asia. More specifically, the plants belonging to the genus Salacia include Salacia reticulata, Salacia oblonga, Salacia prinoides, Salacia chinensisia and Salacia chinensisia. ), Salacia burunoniana, Salacia grandiflora, Salacia macrosperma, and the like.
• the plants belonging to the genus Salacia include Salacia reticulata, Salacia oblonga, Salacia prinoides, Salacia chinensisia and Salacia chinensisia. ), Salacia burunoniana, Salacia grandiflora, Salacia macrosperma, and the like.
• the composition of this invention may contain the salacinol isolated and purified from the extract of the plant of the genus Salacia as the salacinol.
• the extract of the plant of the genus Salacia is an extract from the edible part such as the root, stem, leaf, flower, fruit of the plant of the genus Salacia, the root of the plant of the genus Salacia, the stem, the leaf, the flower, Extracts from pulverized edible parts such as fruits, extracts from roots, trunks, leaves, flowers, fruits, etc. of edible parts such as fruits, and extracts from the genus Salacia Used to mean dry powder (extract powder) obtained by drying.
• two or more types of sites of the genus Salacia may be mixed and used.
• extract powder obtained by drying an extract extracted from a site selected from roots and trunks is more preferably used.
• the extract powder of the genus Salacia can preferably be obtained by drying an extract obtained by solvent extraction from the edible part of the genus Salacia.
• the solvent used for the extraction of salacinol include water, alcohol, and ketone.
• a solvent used for the extraction of salacinol a mixed solvent obtained by mixing two or more kinds of solvents may be used.
• the alcohol include methanol, ethanol and the like.
• ethanol acetone, methyl ethyl ketone, cyclohexane and the like are preferable.
• a solvent used for extraction of salacinol water, alcohol, a mixed solvent of water and alcohol, a mixed solvent of water and ketone, etc. are preferable, and a mixed solvent of water, alcohol, and water and alcohol is more preferable.
• hot water at 50 ° C. to 98 ° C., ethanol, and a mixed solvent of water and ethanol are more preferable.
• the alcohol content in the mixed solvent of water and alcohol is preferably 30% by mass to 90% by mass, and more preferably 40% by mass to 70% by mass.
• salacinol when obtained by synthesis, it can be synthesized by a known synthesis method, for example, a method described in JP-T 2009-528299 (International Publication No. 2007/098567).
• the content of salacinol in the composition of the present invention is preferably in the range of 0.001% by mass to 10% by mass and more preferably 0.03% by mass to 3% by mass with respect to the total amount of the composition. preferable. Within the above-described content range, the physiological effectiveness of salacinol can be more effectively obtained, and formulation can be further facilitated. In addition, from the viewpoint of formulation, the composition is more suitable for applications such as external preparations for skin, cosmetics, and foods and drinks, and the feeling of use when applied to external preparations for skin and cosmetics becomes better. The content of salacinol in the composition can be confirmed by detection under the following conditions by high performance liquid chromatography.
• composition of the present invention contains at least one compound selected from citric acid and salts thereof.
• at least one compound selected from citric acid and a salt thereof may hereinafter be abbreviated as a citric acid compound.
• Citric acid and citrate in the present invention may be hydrates or anhydrides.
• Examples of the salt when citric acid is a salt include alkali metal salts, alkaline earth metal salts, transition metal salts, ammonium salts, and the like.
• citric acid compound which can be used for this invention is illustrated below, this invention is not limited to the following compounds.
• examples of the citric acid compound include citric acid, sodium citrate, potassium citrate, calcium citrate, aluminum citrate, zinc citrate, iron citrate, diammonium citrate, and ammonium dihydrogen citrate.
• the content of the citric acid compound in the composition of the present invention is preferably 0.1% by mass to 10% by mass, and 0.4% by mass to 5% by mass with respect to the total amount of the composition. It is more preferable that In the composition of the present invention, only one type of citric acid compound may be used, or two or more types may be used in combination.
• the composition of the present invention contains at least one compound selected from an inorganic salt of magnesium and an organic salt of magnesium having an organic group having 5 or less carbon atoms.
• at least one compound selected from an inorganic salt of magnesium and an organic salt of magnesium having an organic group having 5 or less carbon atoms may hereinafter be abbreviated as a magnesium salt compound.
• the magnesium salt compound used in the present invention may be an inorganic salt or an organic salt.
• the organic salt of magnesium in the present invention has an organic group having 1 to 5 carbon atoms.
• the molecular weight of the magnesium salt compound is preferably 500 or less, and more preferably 300 or less.
• the magnesium salt compound used in the composition is appropriately selected according to the dosage form of the composition, the application mode including the composition, other components contained in the composition, and the like.
• the composition may contain only one type of magnesium salt compound or two or more types. When the composition contains two or more magnesium salt compounds, it may contain only two or more magnesium inorganic salts, or may contain only two or more organic magnesium salts. One or more species and one or more organic salts of magnesium may be used in combination.
• the magnesium salt compound may be a hydrate or an anhydride.
• the form of the magnesium salt compound is not limited as long as the magnesium molar amount necessary for exhibiting the stabilizing effect of salacinol is present in the composition. From the viewpoint of the effect on the content, an inorganic salt of magnesium and an organic salt of magnesium having an organic group having 5 or less carbon atoms are used as the magnesium salt compound in the present invention.
• the inorganic salt of magnesium used in the present invention is a salt obtained by reacting an inorganic acid or an inorganic base with magnesium.
• the inorganic acid include hydrochloric acid, nitric acid, phosphoric acid, sulfuric acid and the like.
• the inorganic base include sodium hydroxide.
• the inorganic salt of magnesium that can be used in the present invention include magnesium chloride, magnesium hydroxide, magnesium carbonate, magnesium nitrate, magnesium sulfate, magnesium hydrogen phosphate, magnesium phosphate, trimagnesium phosphate, basic magnesium carbonate, and peroxide.
• the organic salt of magnesium used in the present invention is a salt obtained by reacting an organic acid with magnesium.
• the organic acid used to obtain the organic salt of magnesium include organic acids having an organic group having 1 to 5 carbon atoms, preferably organic acids having an organic group having 2 to 5 carbon atoms, More preferred are organic acids having 4 organic groups.
• the organic acid include formic acid (1), acetic acid (2), lactic acid (3), aspartic acid (4), pyroglutamic acid (5) and the like.
• the numerical value in () after the compound name indicates the number of carbons contained in the organic group of the organic acid.
• acetic acid (2), lactic acid (3), aspartic acid (4), pyroglutamic acid (5), and the like are preferable as the organic acid.
• an organic salt of magnesium if the organic group contained in the molecule has 6 or more carbon atoms, there is a concern about generation of malodor caused by a free organic acid, irritation to the skin, etc.
• a magnesium salt having an organic group having 5 or less carbon atoms is used. Examples of the organic salt of magnesium include magnesium acetate, magnesium lactate, magnesium aspartate, magnesium pyroglutamate and the like, and magnesium aspartate, magnesium pyroglutamate and the like are preferable.
• a thickener etc. with low salt tolerance may be used together.
• a magnesium salt compound to be used it is preferable to select a magnesium salt having a low molecular weight and high solubility in a solvent used in the preparation.
• the magnesium salt has a solubility in water at 25 ° C. of 0.1 g / 100 ml or more. It is preferable to select a compound, and it is more preferable to select a magnesium salt compound having a solubility in water of 1 g / 100 ml or more.
• the type of magnesium salt compound to be used can be appropriately changed according to the emulsion stability and irritation.
• the content of the magnesium salt compound in the composition is preferably 0.1% by mass to 10% by mass and more preferably 0.2% by mass to 5% by mass with respect to the total amount of the composition.
• the pH of the composition of the present invention is preferably 8.0 or less, more preferably 7.0 or less, and still more preferably in the range of 3.0 to 6.0.
• the pH of the composition can be appropriately adjusted by a known method according to the formulation of the composition.
• the composition of the present invention can contain water. There is no restriction
• Milli-Q water is ultrapure water obtained by a Milli-Q water production apparatus, which is an ultrapure water production apparatus manufactured by Merck Millipore.
• the composition of the present invention can be prepared by carrying out a stirring and mixing step of dissolving and mixing salacinol, a citric acid compound, and a magnesium salt compound in a solvent according to the dosage form. Moreover, you may prepare by containing a salacinol, a citric acid compound, and a magnesium salt compound suitably in formulation of a final dosage form. Any preparation is included in the composition of the present invention as long as it contains salacinol, a citric acid compound, and a magnesium salt compound.
• a manufacturing method of the composition of this invention if the said component is contained, there will be no restriction
• compositions such as a skin external preparation and cosmetics, containing the composition of this invention
• examples of the method for producing an emulsified composition include a conventional emulsifier method in water, an emulsifier method in oil, and an alternate addition method.
• the emulsified composition is an oil-in-water type emulsified composition
• a method of preparing by a one-step emulsification operation of emulsifying by applying an emulsification method using a normal emulsification apparatus utilizing a shearing action is mentioned.
• Examples of a normal emulsifier include a stirrer stirring, an impeller stirring, a homomixer, and a continuous flow type shearing device. Further, after the emulsification operation using the above-described normal emulsification apparatus, the high-pressure dispersion step is carried out by a method such as emulsification operation using an emulsification apparatus such as a high-pressure homogenizer or an ultrasonic disperser. You may apply the method of performing the two-stage emulsification operation which uses the emulsifier more than a kind sequentially.
• the composition of the present invention is prepared as an aqueous composition
• it is usually prepared by stirring the mixture containing the composition of the present invention and, if necessary, additives in the range of 15 ° C to 45 ° C.
• the temperature condition for preparing the aqueous composition is not limited to the above-described range, and may be prepared by appropriately heating and stirring the mixture according to the solubility of the additive contained in the aqueous composition. Good.
• a sterilization step can be performed.
• the sterilization step may be performed at any stage in each step of preparing the composition of the present invention.
• sterilization method examples include sterilization methods such as dry heat sterilization and steam sterilization, electron beam sterilization, sterilization using ionizing radiation, sterilization methods using electromagnetic waves such as high-frequency sterilization, and ethylene oxide gas (EOG) sterilization.
• EOG ethylene oxide gas
• the sterilization method is appropriately selected depending on the types of components contained in the composition. Depending on the purpose, two or more sterilization steps can be performed.
• a sterilization method applied to the composition of the present invention a sterilization method selected from dry sterilization, heat sterilization such as steam sterilization, and filter sterilization is preferable.
• the decomposition or modification of salacinol which is an active ingredient contained in the composition, is suppressed. That is, at least one of a decrease in content due to decomposition of salacinol in the composition and a decrease in effectiveness due to modification of salacinol are effectively suppressed, and the stability of salacinol is excellent. Therefore, the composition of the present invention contains salacinol as an active ingredient, and since salacinol maintains an effect stably over a long period of time as an active ingredient, it can be used in various dosage forms. Examples of the dosage form to which the composition of the present invention can be applied include external preparations for skin, cosmetics, foods and drinks, and the like.
• Examples of the external preparation for skin include ointments, creams, gels, and poultices.
• Examples of cosmetics include aqueous cosmetics, emulsified cosmetics, and powder cosmetics.
• Examples of the food and drink include health foods, drinks, beverages and the like having forms such as tablets, granules, capsules, and powders.
• the external preparation for skin of the present invention contains the composition of the present invention.
• the composition of the present invention is locally applied to the skin as an external preparation for skin, the whitening effect can be expected due to the physiological activity of suppressing melanin production caused by local salacinol.
• the amount of the composition of the present invention contained in the external preparation for skin of the present invention varies depending on the type and purpose of the dosage form and cannot be specified unconditionally, but the content of salacinol is relative to all the components of the external preparation for skin.
• the composition is preferably contained in an amount of 0.001% by mass to 10% by mass, more preferably 0.03% by mass to 3% by mass.
• the external preparation for skin of the present invention can further contain an additive component that is usually used in the field of external preparation for skin, if necessary.
• an additive component that is usually used in the field of external preparation for skin, if necessary.
• other components that can be used in the external preparation for skin other components in the cosmetics described later can be similarly exemplified.
• the cosmetic of the present invention contains the composition of the present invention.
• Cosmetics include lotion, beauty liquid, milky lotion, cream, cream pack / mask, pack, base makeup cosmetics, cosmetics for hair washing, fragrance cosmetics, liquid body cleansers, UV care cosmetics, deodorant cosmetics, oral care cosmetics, etc. Of cosmetics.
• the cosmetic of the present invention can be obtained, for example, by mixing the composition of the present invention and components used in combination, if necessary, by stirrer stirring, impeller stirring, stirring using a homomixer or the like. .
• the production method for preparing the cosmetic of the present invention as an emulsified composition or an aqueous composition can be carried out in the same manner as described in the preparation of the composition of the present invention.
• Content in the composition in the cosmetics of this invention is suitably selected according to the dosage form of cosmetics, and the intended purpose.
• the content of the salacinol may be contained in an amount ranging from 0.001% by mass to 10% by mass with respect to the total amount of the cosmetic. More preferably, the composition is contained in an amount ranging from 0.03% to 3% by mass. Since the composition of the present invention described above is excellent in the stability of salacinol, which is an active ingredient, it can be suitably used in cosmetics.
• the cosmetic of the present invention can be expected to exhibit a whitening effect due to salacinol.
• the cosmetics of the present invention may appropriately contain additive components that are usually used in the field of cosmetics, depending on the form.
• Other components can be contained in the composition of the present invention and the cosmetic containing the composition of the present invention as an oil-soluble or water-soluble additive component depending on the properties of the components.
• other components include one or more components selected from pearl luster materials, preservatives, antioxidants, dyes, thickeners, and pH adjusters.
• a fragrance flavor, an antibacterial agent, a moisturizer, various oil-based components, an ultraviolet absorber, an active oxygen remover, an antioxidant, an antimicrobial agent, a hair restorer, a mineral, an amino acid, etc. can be used.
• other components that can be used in the cosmetic of the present invention will be described.
• the oil component can be appropriately selected from components generally used in cosmetics as long as the stability of salacinol is not impaired.
• desirable oils that can be used in cosmetics include polar oils such as hydrocarbon oils and ester oils, silicone oils, and liquid oils that are liquid at room temperature.
• Thickeners include quince seed, carrageenan, gum arabic, caraya gum, xanthan gum, gellan gum, tamarind gum, locust bean gum, tragacanth gum, pectin, starch, cyclodextrin, methylcellulose, ethylcellulose, carboxymethylcellulose, sodium alginate, polyvinyl alcohol, polyvinyl Examples include pyrrolidone, carboxyvinyl polymer, sodium polyacrylate, and the like.
• Examples of the pH adjuster include lactic acid, glycolic acid, succinic acid, tartaric acid, malic acid, potassium carbonate, triethanolamine, monoethanolamine, and other organic acids or salts thereof, hydrochloric acid, perchloric acid, carbonic acid, phosphoric acid and the like.
• Inorganic acids and salts thereof, sodium hydrogen carbonate, ammonium hydrogen carbonate, sodium hydroxide, potassium hydroxide and the like can be mentioned. It is not limited to these compounds, What is necessary is just to select and use a well-known pH adjuster suitably according to the objective.
• the citric acid compound contained in the composition of the present invention has a pH adjusting function.
• a citric acid compound may be used for the pH adjustment
• the exemplified pH adjusting agent described above may be used
• the citric acid compound and the aforementioned pH adjusting agent may be used in combination.
• a pH adjuster can be used individually or in combination of 2 or more types.
• moisturizing agent examples include agar, diglycerin, distearyldimonium hectorite, butylene glycol, polyethylene glycol, propylene glycol, hexylene glycol, yokuinine extract, petrolatum, urea, hyaluronic acid, ceramide, phospholipid, lipid, isoflavone.
• active oxygen scavengers include superoxide dismutase (SOD), mannitol, lutein and derivatives thereof, bilirubin, cholesterol, tryptophan, histidine, quercetin, quercitrin, catechin, catechin derivatives, gallic acid, gallic acid derivatives, and ogon extract.
• SOD superoxide dismutase
• mannitol lutein and derivatives thereof
• bilirubin cholesterol, tryptophan, histidine
• quercetin quercitrin
• catechin catechin derivatives
• gallic acid gallic acid derivatives
• ogon extract ogon extract.
• Ginkgo biloba extract Yukinoshita extract
• Melissa extract, Gennoshoko extract, Boppi extract Parsley extract
• Tormentilla extract Rakan fruit extract, seaweed extract
• Yashajitsu extract Zicopi extract and the like.
• antioxidants include vitamin A such as retinol, retinoic acid, retinol acetate, retinol palmitate, retinyl acetate, retinyl palmitate, tocopheryl retinoic acid, vitamin C and its derivatives, kinetin, retinoin, tocopherol, and tocotrienol.
• vitamin E such as vitamin E and its derivatives, sesamin, astaxanthin, lycopene, resveratrol, pterostilbene, ⁇ -lipoic acid, coenzyme Q10, flavonoids, erythorbic acid, propyl gallate, BHT (di-n-butylhydroxytoluene), Examples thereof include BHA (butylhydroxyanisole), tretinoin, polyphenol, SOD, phytic acid, koki extract, soybean extract, black tea extract, tea extract, age extract and the like.
• amino acids examples include glutamic acid, L-aspartic acid, L-alanine, L-cysteine, glycine, L-isoleucine, L-leucine, lysine and the like, and salts thereof.
• the various active ingredients that can be used in the cosmetics described above may be used alone or in combination of two or more.
• the food / beverage products of this invention contain the composition of this invention.
• salacinol since salacinol exhibits physiological activities such as ⁇ -glucosidase inhibitory ability and melanin production inhibitory function in the small intestine, when taken orally as a food or drink, it exerts a preventive effect on diabetes and a melanin production inhibitory effect. Can be expected.
• the various forms which can be mainly supplied to a body by an oral route can be taken.
• the food and drink of the present invention are, for example, powdered foods, granular foods, sheet foods, bottled foods, canned foods, retort foods, capsule foods, tablet foods, liquid foods, drinks, etc. It can be used as food and drink such as food, nutritional supplements and foods for specified health use.
• the food / beverage products of this invention take the form of a functional food, it can be set as the form of common foodstuffs, such as an energy drink, a nourishing tonic, a palatability drink, and a frozen dessert.
• the form of the functional food the form of nutritional supplements such as tablets, granules, and capsules can also be suitably exemplified.
• the form of the food / beverage products containing the composition of this invention is not restrict
• the food or drink of the present invention can optionally contain other components generally used in food and drink.
• other components that can be used in the food and drink of the present invention include colorants, preservatives, thickening stabilizers, antioxidants, color formers, bleaches, fungicides, gum bases, bitters, enzymes, and gloss.
• the pH of the food or drink of the present invention is preferably 8.0 or less, more preferably 7.0 or less, as in the case of the composition described above. More preferably, it is set to 0 to 6.0. Any pH adjuster that can be used to adjust pH in food and drink can be used as long as it is usually used in the food field.
• pH adjusters examples include organic acids selected from gluconic acid, L-tartaric acid, malic acid, lactic acid, adipic acid, succinic acid, acetic acid, fumaric acid, phytic acid, and derivatives thereof, sodium bicarbonate List inorganic acids such as (sodium hydrogen carbonate), sodium carbonate, sodium hydroxide, calcium hydroxide, disodium hydrogen phosphate, sodium dihydrogen phosphate, dipotassium hydrogen phosphate, potassium dihydrogen phosphate, potassium carbonate Can do.
• the organic acid may take the form of a salt such as sodium salt, potassium salt, magnesium salt and the like.
• a pH adjuster can be used individually or in combination of 2 or more types.
• ingredients that can be used in food and drink applications include milk protein, soy protein, egg albumin protein, etc., or egg white oligopeptides, soy hydrolysates, mixtures of amino acids alone, and the like thereof.
• the food and drink of the present invention include natural liquid foods, semi-digested nutritional foods and nutritional foods, drinks, capsules, enteral nutritional supplements, etc. that contain sugars, fats, trace elements, vitamins, emulsifiers, fragrances, etc. It can take the form of a workpiece.
• nutritional additives such as amino acids, vitamins, minerals, sweeteners, spices, fragrances, and pigments are used to improve nutritional balance and flavor at the time of ingestion. May be blended.
• the food / beverage products of this invention can be manufactured based on the manufacturing method of the above-mentioned composition.
• the content of the composition of the present invention in the food and drink of the present invention is appropriately selected according to the purpose, but from the viewpoint of fully expressing the effectiveness of salacinol, the content of salacinol in the food and drink of the present invention
• the food / beverage products of the present invention can be expected to exhibit ⁇ -glucosidase inhibitory ability in the small intestine and whitening effect due to salacinol.
• composition of the present invention is excellent in the stability of salacinol as an active ingredient, has little fear of alteration or reduction of salacinol as an active ingredient, and can be expected to have a long-term effect due to the addition of salacinol. It can be suitably used for foods and drinks, and its application range is wide.
• Example 1 The salacinol-containing composition of Example 1 was prepared by stirring the components described in the following composition 1 at 25 ° C. for 30 minutes.
• Composition 1 Salacinol [compound represented by formula (1)] 0.3 g ⁇ Citric acid [citric acid compound] 0.12 g ⁇ Sodium citrate dihydrate [citric acid compound] 0.56 g ⁇ Magnesium chloride [magnesium salt compound] 0.5g ⁇ Water [solvent] 98.5g
• the pH of the composition was 5.5.
• the composition was allowed to stand for 2 weeks in a temperature atmosphere of 70 ° C., and heated with aging. Thereafter, the content of salacinol in the composition after heating was measured in the same manner as the composition immediately after preparation. Assuming that the content of salacinol in the composition immediately after preparation was 100, the residual rate (%) of salacinol in the composition after heating was found to be 82%.
• Reference Example 1 A composition of Reference Example 1 was prepared in the same manner as in Example 1 except that the composition 1 did not contain a citric acid compound and the amount of the solvent was increased in an amount equal to the amount of citric acid decreased.
• the residual rate (%) of salacinol was determined in the same manner as in Example 1, in Reference Example 1 containing no citric acid compound, the residual rate was 76%.
• Reference Example 2 A composition of Reference Example 2 was prepared in the same manner as in Example 1 except that the composition 1 did not contain magnesium chloride and the amount of the solvent was increased in the same amount as the reduced amount of magnesium chloride.
• the residual ratio (%) of salacinol was determined in the same manner as in Example 1, the residual ratio of salacinol was 73% in the composition of Reference Example 2 containing no magnesium chloride. From these results, it can be seen that the composition of Example 1 has better stability of salacinol than Reference Example 1 and Reference Example 2.
• the aqueous phase composition A obtained above was stirred with a homogenizer (model name: HP93, manufactured by SMT Co., Ltd.) while maintaining the temperature at 70 ° C. (10000 rpm), and the oil phase composition A was added to the aqueous phase composition A.
• a preliminary emulsion was obtained.
• the obtained preliminary emulsified product was cooled to about 40 ° C., and high-pressure emulsification was performed at 200 MPa using an optimizer HJP-25005 (manufactured by Sugino Machine Co., Ltd.).
• HJP-25005 manufactured by Sugino Machine Co., Ltd.
• it filtered with the micro filter with an average hole diameter of 1 micrometer, and prepared the astaxanthin containing emulsion composition (astaxanthin content rate: 0.3 mass%).
• the obtained astaxanthin emulsion composition was diluted to 1% by mass with milli-Q water, and the particle size of the dispersed particles was measured using a particle size analyzer FPAR-1000 (manufactured by Otsuka Electronics Co., Ltd.). there were.
• An equivalent emulsified composition can be obtained by replacing the Haematococcus alga extract with a krill extract.
• each component used in the aqueous phase composition B is weighed in a container according to the above composition, heated and mixed with stirring in a thermostatic bath at 70 ° C., confirmed to be well mixed, held at 70 ° C., Phase composition B was obtained.
• each component used in the oil phase composition B is weighed in a container according to the above composition, heated and mixed for 5 minutes while stirring on a 150 ° C. hot plate, and confirmed to be well mixed.
• Composition B was obtained.
• the obtained aqueous phase composition B was added to the oil phase composition B, mixed with stirring, and dispersed for a predetermined time using an ultrasonic homogenizer to obtain a coarse dispersion.
• the obtained coarse dispersion was further emulsified at a high pressure of 200 MPa using an ultrahigh pressure emulsifier (Altimizer, manufactured by Sugino Machine Co., Ltd.), and a lycopene-containing composition (lycopene content: 0.17% by mass) ) was prepared.
• an ultrahigh pressure emulsifier Altimizer, manufactured by Sugino Machine Co., Ltd.
• a lycopene-containing composition lycopene content: 0.17% by mass
• the obtained lycopene-containing emulsion composition was diluted by 1 mass% with MilliQ water, and the particle size of the dispersed particles was measured using a particle size analyzer FPAR-1000 (manufactured by Otsuka Electronics Co., Ltd.). there were.
• a cosmetic was prepared as follows using the astaxanthin-containing emulsion composition and the lycopene emulsion composition prepared by the above method as appropriate.
• Example 2 lotion
• a lotion having the following composition 2 was prepared by a conventional method and adjusted with sodium hydroxide so that the pH was 5.5 (total amount: 100% by mass).
• [Composition 2] [Content (% by mass)]
• Salacinol [compound represented by formula (1)] 0.3
• Arbutin 2.0 Dipotassium glycyrrhizinate 1.0
• Dipropylene glycol 4.0 Polyoxyethylene methyl glucoside 1.0 1,3-butylene glycol 4.0
• Polyethylene glycol 1.0 Ethanol 2.0 Polyoxyethylene hydrogenated castor oil (60 EO) 0.2 Phenoxyethanol 0.3
• Glycerin mono-2-ethylhexyl ether 0.2 Oryzanol 0.01
• Polyoxyethylene phytosterol (NIKKOL BPS-20 : Product name, manufactured by Nikko Chemicals Co., Ltd.) 0.03
• N-acetyl-L-hydroxyproline 1.0
• Water-soluble collagen 1.0
• composition 3 A cosmetic liquid having the following composition 3 was prepared by a conventional method, and the pH of the cosmetic liquid was adjusted to 6.2 using sodium citrate (total amount: 100% by mass).
• Composition 3 [Content (% by mass)]
• Salacinol [compound represented by formula (1)] 1.0 Phosphoric acid-L-ascorbyl magnesium 2.0 Dipotassium glycyrrhizinate 1.0 Dipropylene glycol 4.0 Glycerin 5.0 Diglycerin 2.0 1,2-pentanediol 2.0 Phenoxyethanol 0.5 Methyl paraoxybenzoate 0.1 Alkali Neges Relatus B-16 Polymer 0.05 Oryzanol 0.01 Polyoxyethylene phytosterol (NIKKOL BPS-20 : Product name, manufactured by Nikko Chemicals Co., Ltd.) 0.03 Polyoxyethylene hydrogenated castor oil (60 EO) 0.2 Camellia extract 0.01 Lecithin 0.05 Citric acid [citric acid compound] 0.7 Sodium citrate [
• Example 4 Cream
• a cream having the following composition 4 was prepared by a conventional method, and the pH of the cream was adjusted to 6.4 using sodium hydroxide (total amount: 100% by mass).
• Composition 4 [Content (% by mass)]
• Salacinol [compound represented by formula (1)] 0.1 Arbutin 2.0
• Phosphoric acid-L-ascorbyl magnesium 0.1 1,2-pentanediol 3.0 Dipropylene glycol 7.0
• Polyethylene glycol 6000 [Molecular weight: 6000] 1.0 Sodium hyaluronate 0.5 Trimethylglycine 0.5 1,3-butylene glycol 3.0 Xanthan gum 0.5
• Acrylic acid / alkyl methacrylate copolymer 0.7
• Squalane 0.5 Shea fat 1.0
• Sara honey bee 1.0
• Behenyl alcohol 1.0
• composition 5 A sunscreen agent having the following composition 5 was prepared by a conventional method, and the pH of the sunscreen agent was adjusted to 7.0 using sodium hydroxide (total amount: 100% by mass).
• Composition 5 [Content (% by mass)]
• Salacinol [compound represented by formula (1)] 0.3
• Surface-treated titanium oxide fine particles HXMT-100ZA: trade name, 6.0 (Taika Co., Ltd., average primary particle size 15 nm)
• Aluminum hydroxide 1.0 Isostearic acid 0.5 Sorbitan sesquioleate 1.0 Dipotassium glycyrrhizinate 0.5 Phosphoric acid-L-ascorbyl magnesium 0.1
• Krill extract 0.5 Water-soluble collagen 1.0
• Citric acid [citric acid compound] 0.7 Sodium citrate [citric acid compound
• Example 6 Latex
• An emulsion having the following composition 6 was prepared by a conventional method, and the pH of the emulsion was adjusted to 6.6 using sodium citrate (total amount: 100% by mass).
• Composition 6 [Content (% by mass)] ⁇ Oil phase component ⁇ Haematococcus alga extract 0.2 Astaxanthin-containing emulsion composition (krill extract) [Composition prepared by Preparation Method 1 described above] 0.4 Squalane 8.0 Jojoba oil 7.0 Cetyl alcohol 1.5 ⁇ Water phase ingredient ⁇ Salacinol [compound represented by formula (1)] 1.0 Glycerol monostearate 2.0 Polyoxyethylene cetyl ether 3.0 Polyoxyethylene soorbitan monooleate 2.0 1,3-butylene glycol 1.0 Glycerin 2.0 Sucrose stearate 0.1 Polyglyceryl oleate-10 0.1 Polyglyceryl stearate-2 0.1 Phenoxyethanol 0.2 Collagen 1.0 Oryzanol 0.01 Polyoxyethylene phytoste
• Example 7 Jerry-like serum
• a jelly-like serum having the following composition 7 was prepared by a conventional method, and the pH of the jelly-like serum was adjusted to 7.6 using sodium citrate (total amount: 100% by mass).
• Salacinol Compound represented by formula (1)] 1.0 Haematococcus alga extract 0.1 Astaxanthin-containing emulsion composition (krill extract) [Composition prepared by Preparation Method 1 described above] 0.2 Ceramide III, VI mixture 1.0 Hydrolyzed collagen 1.0 Acetylhydroxyproline 1.0 Ethylhexyl glycerin 0.1 Oleic acid 0.5 1,3-butylene glycol 1.0 Glycerin 2.0 Sucrose 0.1 Polyglyceryl oleate-10 0.1 Polyglyceryl stearate-2 0.1 Phenoxyethanol 0.2 Collagen 1.0 Oryzanol 0.01 Polyoxyethylene phytosterol (NIKKOL BPS-20 : Product name, manufactured by Nikk
• composition 8 [Content (% by mass)]
• Salacinol [compound represented by formula (1)] 0.3 Talc (OTS-2 TALK JA-46R : Daito Kasei Kogyo Co., Ltd.) 18 Titanium oxide (OTS-2 TiO 2 CR-5 : Daito Kasei Kogyo Co., Ltd.) 9.0 Iron oxide yellow (OTS-2 YELLOW LLXLO : Daito Kasei Kogyo Co., Ltd.) 2.3 Iron oxide red (OTS-2 RED R-516L: Daito Kasei Kogyo Co., Ltd.) 0.15 Iron oxide black (OTS-2 BLACK BL-100: Daito Kasei Kogyo Co., Ltd.
• composition 9 Liquid foundation
• Composition 9 [Content (% by mass)]
• Salacinol [compound represented by formula (1)] 0.5 Dipotassium glycyrrhizinate 0.2 Specific red composite pigment * 1 0.5 Extender * 2 15.0 Colorant pigment * 3 2.0 Pearl pigment * 4 3.0 Cyclomethicone 25.0 Dimethicone polyol 5.0 Lauryl PEG-9 polydimethylsiloxyethyl dimethicone 3.0 PEG-9 polydimethylsiloxyethyl dimethicone 1.2 Squalane 0.1 Sorbitan sesquiisostearate 1.0 Distemalimonium Hectorite 0.8 Ethyl hexyl methoxycinnamate 2.5 Hematococcus prubiaris oil 0.1 Tocopherol 0.1 Damask rose flower oil trace amount fragrance appropriate amount
• Example 10 Face wash
• a face wash having the following composition 10 was prepared by a conventional method, and the pH of the face wash was adjusted to 6.3 using sodium citrate (total amount: 100% by mass).
• [Composition 10] [Content (% by mass)] Salacinol [compound represented by formula (1)] 1.0 Myristic acid K 2.0 Palmitic acid K 0.5 Stearic acid K 0.5 (Lauramide / Myristamide) DEA 1.0 Cocoylglycine Na 10.0 Lauro Anjo Na 13.0 PEG-32 3.0 Butylene glycol 15.0 Glycerin 10.0 Sorbitol 5.0 Potassium hydroxide appropriate amount Glyceryl stearate 1.5 Hematococcus spurbiaris oil 0.05 Astaxanthin-containing emulsion composition (krill extract) 0.05 [Composition prepared by Preparation Method 1 described above] Lycopene-containing emulsion composition [Composition prepared by the above-described preparation method 2] 0.1 Water-soluble collagen 1.0 Tocopherol 0.5
• Example 11 Soft drink
• a soft drink having the following composition 11 was prepared by a conventional method, and the pH of the soft drink was adjusted to 3.0 using sodium citrate (total amount: 100% by mass).
• Composition 11 [Content (% by mass)]
• Salacinol Compound represented by formula (1)] 1.0 Fructose dextrose liquid sugar 30.0 Orange juice 20.0 Ascorbic acid 0.2
• Citric acid Citric acid
• Magnesium chloride Magnesium salt compound] 0.1 Emulsifier 0.5 Perfume Appropriate amount Sodium citrate [Citrate compound] Appropriate amount of purified water Remaining amount

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