Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
  • A61K8/42—Amides
• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
  • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
  • A61K8/9783—Angiosperms [Magnoliophyta]
  • A61K8/9789—Magnoliopsida [dicotyledons]
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Definitions

• the present invention relates to a composition for oral cavity which has an excellent effect of improving the stickiness in the oral cavity, which also causes bad breath, and has an excellent refreshing feeling imparting effect, which is suitable for suppressing bad breath.
• compositions have been proposed.
• plant extracts such as Lamiaceae and Citrus are known as bad breath suppressing ingredients
• oral compositions containing plant extracts as active ingredients for preventing bad breath are proposed in addition to these.
• Patent Documents 1 to 3 Japanese Patent Laid-Open No. 2005-289918, Japanese Patent No. 5776364, Japanese Patent Laid-Open No. 2016-112634.
• the composition for oral cavity containing these plant extracts is effective for reducing bad breath-causing components such as volatile sulfur, methyl mercaptan and the like, and has an effect of preventing bad breath as breath (interpersonal).
• JP 2005-289918 A Japanese Patent No. 5776364 JP 2016-112634 A JP 2014-125440 A Japanese Patent Laying-Open No. 2015-182983 JP 2016-102076 A Special table 2014-507440 gazette Special table 2012-508741 gazette Special table 2011-520925 JP 2013-112634 A
• the conventional composition for oral cavity aimed at suppressing bad breath cannot provide a sufficient effect that can eliminate the above-mentioned bad breath anxiety, and improvement has been desired.
• This invention is made
• the present inventors have improved the discomfort such as stickiness in the oral cavity, which is considered to be the main cause of bad breath anxiety, and a feeling of cleanliness. Considering that it is effective to enhance the feeling, further studies were made focusing on these points.
• a specific component is selected from the plant extract and the cooling sensation agent, and both components are used in a specific amount and in a specific ratio, the stickiness in the oral cavity is improved and persists over time. It has been found that an excellent effect that gives a refreshing feeling can be obtained. And when the combination system of both components is blended in the composition for oral cavity, the effect of improving the sticky feeling in the oral cavity is excellent, and the above-mentioned sustained and excellent refreshing effect is exerted.
• the single use of the component (A) or the component (B) has almost no effect on improving the stickiness feeling in the oral cavity and the effect of imparting a refreshing feeling (Comparative Example 1). ⁇ 15). Therefore, from this result, it was not considered that the combined effect was improved by using both in combination, but as is clear from the examples described later, in the present invention, the components (A) and (B) When combined, both components are in a specific range and the mass ratio of (A) / (B) is in a specific range, both components act synergistically, suppressing oral irritation and improving the sticky feeling Both the refreshing effect was enhanced and the effect was remarkable.
• Such operational effects of the present invention are specific to the combination of the components (A) and (B), and instead of the component (B), menthol, peppermint oil or Monomenthyl succinate is inferior when used in combination with component (A) (Comparative Examples 16 to 18), and N-substituted-p-menthane-carboxamide other than component (B) may be used in combination with component (A). inferior.
• Patent Documents 4 to 9 JP 2014-125440, JP 2015-182983, JP 2016-102076, JP 2014-507440, JP 2012-508741, JP 2011-11 No.
• Patent Document 10 Japanese Patent Laid-Open No. 2013-112634
• An oral composition containing a mixture of p-menthane-3,8-diol isomers is disclosed.
• the present invention improves the sticky feeling in the oral cavity and imparts a refreshing feeling by the combined use of the components (A) and (B), and its technical idea cannot be predicted from Patent Documents 4 to 10.
• the present invention provides the following oral composition.
• An oral composition containing 0.00001 to 0.01% by mass of one or more selected from (B-2), wherein (A) / (B) is 0.02 to 100 as a mass ratio.
• the plant extract is rosemary, oxon, carrot, sage, licorice, sugar beet, salmon, peanut, olive, tea, yellowfin, black mushroom, salamander, thyme, birch, peonies, flamingo, asenyaku, turmeric, clove, stevia , Mucloj, Marjoram, Melissa, Perilla, Laurel, Eucalyptus, Cola, Luo Hanhua, Camellia, Clove, Allspice, Suou, Shikon, Diou, Forsythia, Chimpi, Keihi, Oregano, Basil, Naginata Koju, Buttonpi and Seitakamiirobaran
• the composition for oral cavity according to [1] which is an extract of one or more kinds of plants.
• the present invention it is possible to provide an oral composition having an excellent effect of improving the stickiness in the oral cavity that also causes bad breath, an excellent refreshing effect, and good usability.
• the composition for oral cavity of the present invention has a high feeling of bad breath suppression and can be suitably used for the suppression of bad breath.
• composition for oral cavity of the present invention comprises (A) a plant extract, (B) N- (4-cyanomethylphenyl) -2-isopropyl-5-methylcyclohexanecarboxamide (B-1) and N- (2- ( One or more selected from 2-pyridinyl) ethyl) -2-isopropyl-5-methylcyclohexanecarboxamide (B-2) is contained in a specific amount and a specific ratio.
• a plant extract is an extract of a plant, and when used in combination with the component (B), it reduces the stickiness in the oral cavity.
• the plant that is the raw material of the extract is rosemary, hornon, carrot, sage, licorice, sugar beet, persimmon (especially persimmon tannin), jujube, olive (particularly olive leaf), tea, yellowfin (particularly bark) (Owaku), Kuromoji, Salamander, Thyme, Birch, Peonies, Vultures, Asenyaku, Turmeric, Clove, Stevia, Mukuroji, Marjoram, Melissa, Perilla, Laurel, Eucalyptus, Cola, Arachon, Camellia, Clove, Allspice, Suo, Shikon , Daio, Forsythia, Chinpi, Keihi, Oregano, Basil, Naginata Koju, Buttonpi, Seikamirobaran and the like.
• rosemary, oxon, carrot, sage, licorice, sugar beet, salmon, jujube, olive, tea, yellowfin, black moji, salamander are preferred, more preferably rosemary, oxon, carrot, sage, licorice, toki, Salmon, jujube, olive, tea, yellowfin, and more preferred are rosemary, orange, carrot, sage, and liquorice.
• a method for extracting a plant extract a known method can be adopted, and it can be performed under normal extraction conditions. Specifically, a plant extract is obtained by extracting a raw material plant, particularly a powder obtained by pulverizing leaves and stems, using a polar solvent, a nonpolar solvent, or a mixed solvent of a polar solvent and a nonpolar solvent. Obtainable.
• the extraction solvent examples include polar solvents such as water, ethyl ether, ethylene chloride, dioxane, acetone, ethanol, methanol, ethyl acetate, propylene glycol, butylene glycol, and glycerin, or n-hexane, petroleum ether, ligroin, and cyclohexane.
• Non-polar solvents such as carbon tetrachloride, chloroform, dichloromethane, 1,2-dichloroethane, toluene and benzene, or a mixed solvent thereof.
• Preferred extraction solvents are water, lower monohydric alcohols having 1 to 5 carbon atoms (particularly methanol, ethanol, propanol, isopropanol, etc.), glycols (particularly propylene glycol, butylene glycol, etc.), or a mixed solvent thereof.
• the mixed solvent preferably has a mixing ratio of water and lower monohydric alcohol or glycol of 10:90 to 90:10 (mass ratio).
• the extraction solvent may be water alone.
• the plant extract extracted using the said solvent by using an extraction residue as a raw material can also be used.
• a commercial item can also be used for such (A) plant extract. Specifically, commercially available products such as Maruzen Pharmaceutical Co., Ltd. and Yamada Yakuken Co., Ltd. can be used.
• the blending amount of the plant extract (A) is 0.00001 to 0.05 (mass%, the same applies hereinafter) of the whole composition as a pure extract excluding the extraction solvent, preferably 0.0001 to 0.005% More preferably, it is 0.0002 to 0.005%. If the blending amount is less than 0.00001%, the effect of improving the sticky feeling is inferior. If it exceeds 0.05%, the stimulation is too strong.
• Component (B) is composed of N- (4-cyanomethylphenyl) -2-isopropyl-5-methylcyclohexanecarboxamide (B-1) and N- (2- (2-pyridinyl) ethyl) -2-isopropyl-5 It is selected from methylcyclohexanecarboxamide (B-2), preferably N- (4-cyanomethylphenyl) -2-isopropyl-5-methylcyclohexanecarboxamide (B-1).
• the component (B-1) or the component (B-2) may be used, and the components (B-1) and (B-2) are used in terms of the effect. Also good.
• the blending amount of component (B) is 0.00001 to 0.01%, preferably 0.00003 to 0.005% of the entire composition. If it is less than 0.00001%, the effect of improving the sticky feeling and the effect of imparting a refreshing feeling are inferior. If it exceeds 0.01%, the irritation may be too strong and the aftertaste may deteriorate.
• the blending amounts of the component (B-1) and the component (B-2) can be set within the range of the blending amount of the component (B).
• (A) / (B) indicating the blending ratio of the component (A) and the component (B) is 0.02 to 100, preferably 0.05 to 20, more preferably, as a mass ratio. 0.2-5.
• both the effect of improving stickiness and the effect of imparting a refreshing feeling are excellent, and the stimulation is satisfactorily suppressed. If it is less than 0.02, the effect of imparting a refreshing feeling will not be sufficiently maintained, and the stimulation will also be strong. If it exceeds 100, the stimulation becomes stronger.
• the present invention it is preferable to further blend one or more selected from (C) menthyl monosuccinate, N- ⁇ (ethoxycarbonyl) methyl ⁇ -p-menthane-3-carboxamide and menthyl lactate.
• the component (C) is preferably menthyl monosuccinate and N- ⁇ (ethoxycarbonyl) methyl ⁇ -p-menthane-3-carboxamide, more preferably menthyl monosuccinate.
• the blending amount of the component (C) is preferably 0.0001 to 0.01%, more preferably 0.0003 to 0.005% of the entire composition. Within this range, the effect of improving the stickiness is further improved. If it exceeds 0.01%, the irritation may become strong and the aftertaste may deteriorate.
• the composition for oral cavity of the present invention is prepared in the form of solid, liquid, liquid, paste, gel, etc., and is used for toothpastes such as toothpastes, liquid dentifrices, liquid dentifrices, moisturized dentifrices, mouthwashes, and refreshments in the mouth. It is possible to use various dosage forms such as an agent, but in particular, a dentifrice or a mouthwash, especially a dentifrice is suitable, and a toothpaste containing an abrasive is good.
• the manufacturing method can employ a conventional method according to the dosage form.
• an appropriate well-known component can be mix
• examples thereof include abrasives, binders, wetting agents, surfactants, sweeteners, preservatives, pH adjusters, fragrances, and medicinal ingredients.
• examples include a wetting agent, a surfactant, a sweetener, an antiseptic, a pH adjuster, a fragrance, and a medicinal component.
• abrasives examples include calcium phosphate compounds such as dicalcium phosphate dihydrate or anhydrous, primary calcium phosphate, tertiary calcium phosphate, and calcium pyrophosphate; precipitated silica, aluminosilicate, zirconosilicate, titanium-bonded silica, etc.
• Silica-based abrasives; calcium carbonate-based abrasives such as calcium carbonate; calcium hydroxide, aluminum hydroxide, tribasic magnesium phosphate, magnesium carbonate, calcium sulfate, bentonite, hydroxyapatite, and one or two of these More than seeds can be blended.
• silica-based abrasives and calcium carbonate-based abrasives mainly composed of silicates such as precipitated silica, aluminosilicate, zirconosilicate, and titanium-bonded silica, especially silica-based materials such as precipitated silica. Abrasives are preferred.
• the abrasive is preferably abrasive particles having a particle size of 1 to 40 ⁇ m, and the BET specific surface area is preferably 80 to 250 square meters per gram.
• the particle size is a value measured by a particle size distribution measuring device (manufactured by Nikkiso Co., Ltd., Microtrac particle size distribution meter, dispersion medium: water).
• a particle size distribution measuring device manufactured by Nikkiso Co., Ltd., Microtrac particle size distribution meter, dispersion medium: water.
• silica-based abrasive commercially available products can be used.
• the blending amount of the abrasive is preferably 8 to 70%, particularly 10 to 50% of the whole composition.
• the abrasive may be granular, and granules can be blended as an abrasive component.
• the granule is a particle obtained by forming a water-insoluble powder into a granule, and may be a granule obtained by crushing silica gel or a granulated product using a binder for granulation.
• the above-mentioned abrasive particles having a particle diameter of 1 to 40 ⁇ m and the above-mentioned granules may be used in combination.
• binder As binder, xanthan gum, sodium carboxymethylcellulose, sodium polyacrylate, sodium alginate, polyvinylpyrrolidone, carrageenan, methylcellulose, sodium hydroxyethylcellulose, tragacanth gum, caraya gum, arabiya gum, locust bean gum, polyvinyl alcohol, carboxyvinyl polymer, carbopol Organic binders such as bee gum and propylene glycol alginate, and inorganic binders such as thickening silica and aluminum silicate can be blended. These can be used alone or in combination of two or more.
• the blending amount of the binder is preferably 0.8 to 5%, particularly 1 to 3%, and in the case of an inorganic binder, 0.5 to 10% of the whole composition. %, Particularly 1 to 8% is preferred.
• wetting agent examples include sugar alcohols such as sorbit and xylit, and polyhydric alcohols such as propylene glycol and glycerin.
• the blending amount is usually 5 to 50%, particularly 20 to 45% of the whole composition.
• the surfactant examples include an anionic surfactant, a nonionic surfactant, and an amphoteric surfactant.
• an anionic surfactant is preferable.
• Anionic surfactants include alkyl sulfates, ⁇ -olefin sulfonates, hydrogenated coconut fatty acid monoglyceride monosulfate, lauryl sulfoacetate, N-acyl taurine salts such as N-methyl-N-acyl taurate, Examples include acyl amino acid salts such as acyl sarcosine salt and N-acyl-L-glutamate. These can be used alone or in combination of two or more.
• anionic surfactants containing a sulfonic acid group are preferable from the viewpoint of foaming and foam quality, and alkyl sulfates and ⁇ -olefin sulfonates are more preferable.
• the salt include sodium salt, potassium salt, ammonium salt and the like, and sodium salt is particularly preferable.
• the alkyl sulfate the alkyl group preferably has 12 to 14 carbon atoms. Specific examples of the alkyl sulfate include sodium lauryl sulfate and sodium myristoyl sulfate.
• alkali metal salts such as sodium and potassium of ⁇ -olefin sulfonate having 14 to 16 carbon atoms can be used, and among them, ⁇ -olefin sulfonate having 14 carbon atoms, particularly sodium. Salts (generic name; sodium tetradecene sulfonate) are preferred.
• the amount of the surfactant, particularly an anionic surfactant is preferably 0.6 to 2.5%, more preferably 1 to 2.5% of the whole composition. In the case of a mouthwash, 0 to 1.0%, particularly 0 to 0.3% of the whole composition is preferable.
• sweetener examples include saccharin sodium, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, perilartin, glycyrrhizin, thaumatin, asparatylphenylalanine methyl ester and the like.
• preservative examples include paraoxybenzoic acid ester and sodium benzoate.
• pH adjuster examples include organic acids such as citric acid and lactic acid and salts thereof; inorganic compounds such as hydrochloric acid, sodium hydroxide, potassium hydroxide, disodium hydrogen phosphate, and sodium dihydrogen phosphate.
• fragrance known oral fragrances such as menthol, anethole, carvone, eugenol, limonene, n-decyl alcohol, citronellol, ⁇ -terpineol, citronellyl acetate, cineol, linalool, ethyl linalool, vanillin, thymol, spearmint oil, Peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, pimento oil, cinnamon oil, perilla oil, winter green oil, clove oil, eucalyptus oil and the like.
• Medicinal ingredients include enzymes such as dextranase, amylase, protease, mutanase; anti-inflammatory agents such as tranexamic acid, epsilon aminocaproic acid, azulene, glycyrrhizinate, glycyrrhetinate; sodium chloride, vitamins, allantoins, etc.
• enzymes such as dextranase, amylase, protease, mutanase
• anti-inflammatory agents such as tranexamic acid, epsilon aminocaproic acid, azulene, glycyrrhizinate, glycyrrhetinate
• sodium chloride vitamins, allantoins, etc.
• Cell activators such as isopropylmethylphenol, cetylpyridinium chloride, benzalkonium chloride, hinokitiol, lysozyme chloride; water-soluble copper compounds such as copper chlorophyll and copper gluconate; calculus prophylaxis; blood circulation promoters such as vitamin E Amino acids such as alanine, glycine and proline can be blended.
• the compounding quantity of a medicinal ingredient can be made into an effective quantity in the range which does not inhibit the effect of this invention.
• inorganic compounds such as titanium mica, titanium oxide, bentonite; cellulose-based organic powders such as crystalline cellulose; natural polymer compounds such as agar, gelatin, starch, glucomannan; polyvinyl acetate, acrylic resin Synthetic polymers such as polyurethane, polyester, polyvinyl chloride, nylon powder, polyethylene powder or copolymers thereof; waxes such as carnauba wax, rosin, rice wax, microcrystalline wax, beeswax, paraffin wax; cetanol, Higher alcohols such as stearyl alcohol; polyisobutylene, polybutadiene, silicone, and natural rubber can be blended as long as the effects of the present invention are not impaired.
• the solvent purified water is generally used.
• a lower monohydric alcohol having 1 to 3 carbon atoms such as ethanol may be blended. The amount of the lower monohydric alcohol is preferably 0 to 10% of the entire composition.
• Dentifrice compositions (toothpaste) or mouthwashes having the compositions shown in Tables 1 to 6 were prepared by conventional methods and stored in ordinary oral preparation containers (toothpaste: laminate tube, mouthwash: bottle). . These were used as samples and evaluated by the methods shown below. The results are shown in Tables 1-6.
• the numerical value of the blending amount of the component (A) in the table is the pure extract amount excluding the extraction solvent.
• B1 N- (4-cyanomethylphenyl) -2-isopropyl-5-methylcyclohexanecarboxamide >> Product name: Ebacool G-180, manufacturer: Givadan Japan Co., Ltd.
• B2 N- (2- (2-pyridinyl) ethyl) -2-isopropyl-5-methylcyclohexanecarboxamide >> Product name: Evercool G-190, Manufacturer: Givaudan Japan
• a prescription example is shown below.
• the raw materials used are the same as described above.

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• 2018
  • 2018-05-30 JP JP2019521283A patent/JP7264049B2/ja active Active
  • 2018-05-30 CN CN201880035202.6A patent/CN110691583A/zh active Pending
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