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
  • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/19—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
  • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
  • A61K8/23—Sulfur; Selenium; Tellurium; 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
  • A61K8/34—Alcohols
• • 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
  • A61K8/34—Alcohols
  • A61K8/347—Phenols
• • 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
  • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
  • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
• • 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
  • A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
  • A61K8/466—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur containing sulfonic acid derivatives; Salts
• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
  • A61K2800/28—Rubbing or scrubbing compositions; Peeling or abrasive compositions; Containing exfoliants
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
  • A61K2800/59—Mixtures
  • A61K2800/596—Mixtures of surface active compounds

Definitions

• the present invention relates to a composition for oral cavity that contains copper ions, has an excellent effect of suppressing the generation of bad breath components as well as an oral biofilm sterilization effect, and is suitable for the suppression of bad breath.
• Patent Document 2 Japanese Patent Application Laid-Open No. 2011-105650 describes a gel-type oral composition that can be used by being applied to the oral cavity.
• Patent Document 3 Japanese Patent Application Laid-Open No. 2003-192555 shows that a dentifrice composition using a special abrasive (specific synthetic amorphous silicate) in combination with a copper compound has an excellent halitosis suppression effect even after long-term storage. Has proposed. However, various factors may be involved in the generation of bad breath, and it is difficult to satisfactorily suppress bad breath, and the bad breath suppression effect on periodontal disease patients is not always sufficient.
• Patent Document 4 Japanese Patent Application Laid-Open No. 2011-98916
• the present invention has been made in view of the above circumstances, and has an object to provide a composition for oral cavity that contains copper ions, is excellent in an oral biofilm sterilization effect and an effect of suppressing the generation of bad breath components, and is suitable for use in suppressing bad breath.
• the present inventors have formulated a combination of a nonionic fungicide and a specific anionic surfactant into a specific amount of copper ions into the oral composition. It has been found that in addition to the biofilm sterilization effect, it has an excellent effect of suppressing the generation of bad breath components, particularly methyl mercaptan.
• composition for oral cavity containing 0.1 to 2% by mass of one or more anionic surfactants selected from the group is excellent in the bactericidal effect of oral biofilm and the effect of suppressing the generation of bad breath components, Even if it is formed, it is found that it suppresses the generation of halitosis components from halitosis-causing bacteria over a long period of time, has a good taste, and is particularly effective for the suppression or removal of halitosis. It came to.
• the three members act synergistically and surprisingly Inhibition of the generation of halitosis components has been enhanced and this has resulted in the generation of halitosis components, in particular methyl mercaptan, over a long period of time, even when the bacteria that cause halitosis have formed biofilms, in addition to the biofilm bactericidal effect. It was possible to impart an excellent action and effect.
• the present invention it is possible to effectively suppress or remove bad breath of a person suffering from periodontal disease, which has been difficult to suppress only by sterilization of a biofilm.
• the combination of the components (A), (B), and (C) was able to give the above-mentioned special effects, and as shown in the comparative examples described later, (A), ( In the absence of any of the components B) and (C), the effect of inhibiting the generation of methyl mercaptan was poor and the effect was inferior (Comparative Examples 1 to 5).
• Patent document 1 is the continuous suppression of the antibacterial and bad breath by a copper compound and a disinfectant, the effect with respect to a biofilm is not examined and is unknown.
• Patent document 2 is the improvement of the gingipaine inhibitory action of a water-soluble copper compound and the biofilm penetration bactericidal effect of a phenolic fungicide in a gel oral composition, and thereby suppression of periodontal disease.
• Patent document 3 is the improvement of the bad breath suppression effect of a copper compound by the special synthetic amorphous silicate as an abrasive
• the present invention is a specific bactericidal biofilm sterilization and suppression of the generation of bad breath components by a combination of the three components (A), (B) and (C). In the toothpaste composition, a particularly remarkable effect can be imparted.
• the present invention provides the following oral composition.
• [1] (A) 0.001 to 0.2% by mass of copper ions, (B) 0.01 to 1% by mass of a nonionic fungicide, and (C) 0.1 to 2 of one or more anionic surfactants selected from acyl taurine, acyl amino acids and salts thereof. mass%
• the composition for oral cavity to contain [2] (A) The composition for oral cavity according to [1], wherein the copper ion source is one or more water-soluble copper compounds selected from copper gluconate, copper citrate, copper sulfate and copper chloride. [3] (B) The oral composition according to [1] or [2], wherein the nonionic fungicide is isopropylmethylphenol.
• composition for oral cavity that contains copper ions and is excellent in the effect of suppressing the generation of bad breath components together with the bactericidal effect of oral biofilm and suitable for the suppression of bad breath.
• This composition for oral cavity can also be used effectively for suppressing or removing bad breath of a person suffering from periodontal disease.
• the composition for oral cavity of this invention contains (A) copper ion, (B) nonionic fungicide, and (C) specific anionic surfactant.
• copper ion means a copper ion of a copper compound dissolved in a liquid medium (water or the like) of the composition, and is not an insoluble copper compound existing in a solid state in the composition.
• Copper ion is a bad breath suppression or removal agent, and acts as a generation inhibitor of methyl mercaptan, a bad breath component. It is preferable that the copper containing compound used as a copper ion source is a water-soluble copper compound.
• the water-soluble copper compound is a compound having a water solubility at 25 ° C. of 5 g / 100 mL or more, and preferably a water-soluble copper salt such as copper gluconate, copper citrate, copper sulfate, copper chloride, more preferably copper gluconate. , Copper citrate, copper sulfate, especially copper gluconate, copper citrate. These may be used alone or in combination of two or more.
• (A) component can also use the copper ion derived from the solution which melt
• the above solution can also be used as a source of ions.
• copper ions obtained by dissolving water-insoluble copper oxide in an acidic aqueous solution such as dilute hydrochloric acid can also be used.
• copper of a copper-containing compound formed by dissolving a metal complex in the system and copper of a copper-containing compound solubilized using a surfactant can also be used as the copper ion of the present invention.
• the blending amount of (A) copper ions is 0.001 to 0.2% (mass%, the same applies hereinafter) of the entire composition, preferably 0.005 to 0.15%, more preferably 0.01 to 0.1%.
• a sufficient bad breath removing effect is exhibited and a methyl mercaptan generation suppressing effect is exhibited.
• it exceeds 0.2% the metallic taste of copper is enhanced, making it difficult to suppress, and the taste of the preparation becomes poor.
• the preparation stability after storage may be inferior.
• the nonionic bactericide has a biofilm bactericidal action and acts as a generation inhibitor of methyl mercaptan, which is a bad breath component.
• the nonionic fungicide is preferably isopropylmethylphenol or triclosan, more preferably isopropylmethylphenol (3-methyl-4-isopropylphenol).
• the blending amount of the (B) nonionic fungicide is 0.01 to 1%, preferably 0.05 to 0.5% of the whole composition. If it is less than 0.01%, a sufficient biofilm sterilizing effect and a methyl mercaptan generation suppressing effect are inferior.
• the upper limit amount is not particularly limited, but if it is 1% or less, it is sufficiently dissolved in the preparation, and if it exceeds 1%, the solubility is lowered and the action may be inferior.
• Component (C) is one or more anionic surfactants selected from acyl taurine, acyl amino acids, and salts thereof.
• the component (C) acts as a generation inhibitor of methyl mercaptan, which is a bad breath component. Moreover, it contributes also to the improvement of the biofilm sterilization effect by (B) component.
• As the component (C) those selected from acyl taurine and salts thereof are particularly preferable from the viewpoint of the above-described effects.
• the component (C) preferably has an acyl group having 8 to 18 carbon atoms, particularly 12 to 16 carbon atoms, and is selected from acyl taurine salts and acyl amino acid salts having the acyl group. Salts are preferred.
• lauroylmethyl taurine salt lauroyl sarcosine salt, particularly lauroylmethyl taurine salt are preferable.
• These salts are alkali metal salts, alkaline earth metal salts, organic amine salts and the like, among which alkali metal salts, particularly sodium salts are preferred.
• acyl taurine salt examples include sodium lauroylmethyl taurate, myristoyl methyl taurine sodium, coconut oil fatty acid methyl taurine sodium and the like.
• acyl amino acid salt examples include sodium lauroyl sarcosine, sodium lauroyl glutamate, sodium lauroyl aspartate and the like. Commercially available products can be used.
• NIKKOL LMT (lauroyl methyl taurine sodium, manufactured by Nikko Chemicals Co., Ltd.), NIKKOL MMT (myristoyl methyl taurine sodium, manufactured by Nikko Chemicals Co., Ltd.), Soypon SLP (lauroyl sarcosine) Sodium, manufactured by Kawaken Fine Chemical Co., Ltd.), Amisoft LS-11 (sodium lauroyl glutamate, manufactured by Ajinomoto Healthy Supply Co., Ltd.) and the like can be used.
• the blending amount of component (C) is 0.1 to 2%, preferably 0.3 to 1.5% of the whole composition. If the blending amount is less than 0.1%, the effect of suppressing the generation of methyl mercaptan cannot be sufficiently obtained, and the biofilm sterilization effect tends to be low. When it exceeds 2%, the metallic taste of copper derived from the component (A) becomes strong, and the taste of the preparation is lowered.
• anionic surfactants other than the above component (C) may be blended as long as the effects of the present invention are not hindered.
• alkyl sulfates such as sodium lauryl sulfate are not blended.
• (Blending amount 0%) is better, and when blending, the amount is preferably 0.5% or less, particularly 0.2% or less, particularly 0.1% or less of the whole composition.
• the oral composition of the present invention preferably further contains (D) an organic acid having 10 or less carbon atoms or a salt thereof.
• (D) component is mix
• the organic acid has 10 or less carbon atoms, preferably 4 to 6 carbon atoms, and tricarboxylic acid, dicarboxylic acid or a salt thereof having the carbon number can be used, and the salt is an alkali metal salt.
• hydroxy acid such as citric acid, tartaric acid, malic acid and salts thereof are preferable. These may be used alone or in combination of two or more.
• the blending amount of component (D) is preferably 0.01 to 3%, more preferably 0.1 to 2% of the entire composition. Within this range, the taste improving effect is more excellent, and a sufficient methyl mercaptan generation suppressing effect is exhibited.
• the oral composition of the present invention is particularly suitable as a dentifrice composition such as toothpaste, liquid dentifrice, and toothpaste, especially as a toothpaste composition. It can mix
• a general abrasive for oral cavity can be used.
• silica-based abrasives such as silicic anhydride such as precipitated silica and pyrogenic silica, aluminosilicate, zirconosilicate, titanium-binding silica, dicalcium phosphate dihydrate or anhydrous, monobasic calcium phosphate
• examples thereof include calcium phosphate-based abrasives such as tertiary calcium phosphate, calcium carbonate, calcium hydroxide, aluminum hydroxide, insoluble sodium metaphosphate, and synthetic resin-based abrasives, and general silica-based abrasives for dentifrices are suitable.
• the blending amount of these abrasives is usually 2 to 40%, particularly 10 to 30%.
• wetting agent examples include sugar alcohols such as sorbit and xylit, and polyhydric alcohols such as glycerin and propylene glycol.
• sugar alcohols such as sorbit and xylit
• polyhydric alcohols such as glycerin and propylene glycol.
• the blending amount of the wetting agent is usually 5 to 50%, particularly 10 to 40%.
• an organic binder or an inorganic binder can be used as the binder.
• the organic binder include cellulose derivatives such as sodium carboxymethylcellulose, methylcellulose, hydroxymethylcellulose, and hydroxyethylcellulose, gums such as xanthan gum, alginic acid derivatives such as sodium alginate, carrageenan, polyvinyl alcohol, and sodium polyacrylate.
• the inorganic binder include gelling silica and gelling aluminum silica.
• the amount of binder is usually 0.1 to 10%, particularly 0.2 to 8%, and the amount of organic binder is 0.1 to 5%, particularly 0.5 to 3%.
• the blending amount of the inorganic binder is preferably 0.1 to 8%, particularly 0.5 to 5%.
• nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters, sugar alcohol fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene hydrogenated castor oil and the like.
• sugar fatty acid esters such as sucrose fatty acid esters, sugar alcohol fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene hydrogenated castor oil and the like.
• examples include oxyethylene fatty acid esters, polyoxyethylene higher alcohol ethers such as polyoxyethylene stearyl ether, and fatty acid alkanolamides such as lauric acid diethanolamide.
• Examples of the cationic surfactant include alkylammonium types such as distearylmethylammonium chloride and alkylbenzylammonium salts.
• Examples of the amphoteric surfactant include alkyl betaines, betaine acetate types such as alkyldimethylaminoacetic acid betaines and fatty acid amidopropyl betaines, betaine types such as alkylimidazolinium betaines, and imidazoline types.
• the blending amount of these surfactants is preferably 0 to 10%, particularly 0.01 to 5%.
• the nonionic surfactant may be blended in an amount of 0.01% or less, or 0% without blending.
• Sweeteners include sodium saccharin and the like, and colorants include blue No. 1, yellow No. 4, and titanium dioxide.
• Examples of the preservative include paraoxybenzoic acid esters such as methyl paraoxybenzoate, benzoic acid, and salts thereof.
• Perfumes are peppermint oil, spearmint oil, anise oil, eucalyptus oil, wintergreen oil, cassia oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, peppermint oil, cardamom oil, coriander oil, mandarin oil, lime Oil, lavender oil, rosemary oil, laurel oil, camomil oil, caraway oil, marjoram oil, bay oil, lemongrass oil, origanum oil, pine needle oil, neroli oil, rose oil, jasmine oil, grapefruit oil, sweetie oil , Sardine oil, Iris concrete, absolute peppermint, absolute rose, orange flower, and other natural fragrances, and processing of these natural fragrances (front reservoir cut, rear reservoir cut, fractional distillation, liquid-liquid extraction, essence, powder flavor Perfume, menthol, carvone Anethole, cineol, methyl salicylate, cinnamic aldehyde, eugenol, 3-l-
• Active ingredients include cationic fungicides such as cetylpyridinium chloride and benzalkonium chloride, anti-inflammatory agents such as tranexamic acid, epsilon aminocaproic acid, allantoin, enzymes such as dextranase, sodium fluoride, sodium monofluorophosphate, etc. Fluorine-containing compounds, vitamins such as ascorbic acid and tocopherol acetate, and plant extracts such as dipotassium glycyrrhizinate, potassium nitrate, aluminum lactate, sodium chloride and thyme.
• the above-mentioned arbitrary active ingredient can be blended in an effective amount as long as the effects of the present invention are not hindered.
• Toothpaste compositions having the compositions shown in Tables 1 to 3 were prepared by conventional methods and evaluated by the following methods. The results are shown in the table.
• HA hydroxyapatite
• Methyl mercaptan concentration is less than 1/10 ⁇ : Methyl mercaptan concentration is 1/10 or more and less than 1/4 ⁇ : Methyl mercaptan concentration is 1/4 or more and less than 1/2 ⁇ : Methyl mercaptan concentration is 1/2 or more

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• 2019
  • 2019-05-28 WO PCT/JP2019/021053 patent/WO2019230707A1/ja active Application Filing
  • 2019-05-28 JP JP2020522204A patent/JP7298601B2/ja active Active
  • 2019-05-28 KR KR1020207019113A patent/KR20210014618A/ko not_active Application Discontinuation
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