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
  • A61K8/33—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
  • A61K8/34—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
  • A61K8/46—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
  • 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 an isopropylmethylphenol-containing dentifrice composition which has an antibacterial effect on bacteria in the oral cavity for a long time and is suitable for the prevention or control of caries and periodontal disease.
• an oral composition such as a dentifrice containing a bactericidal agent or an antibacterial agent to sterilize oral bacteria that cause oral diseases such as dental caries and periodontal disease, and, as a preferable preventive measure, go to bed
• a dentifrice containing a bactericidal agent or an antibacterial agent to sterilize oral bacteria that cause oral diseases such as dental caries and periodontal disease, and, as a preferable preventive measure, go to bed
• it is widely known that it is recommended to brush before it is difficult to completely kill pathogenic bacteria in the oral cavity.
• the number of bacteria in the oral cavity tends to increase overnight because the temperature and humidity at which bacteria can easily propagate are maintained. Therefore, it is considered effective if, for example, the teeth are brushed before going to bed, and if the antibacterial effect continues even after waking up overnight.
• the antibacterial power by the conventional dentifrice composition has a problem in durability and is not sufficient, and a dentifrice composition having an antibacterial effect which lasts for a long time, for example, sleeps overnight and gets up even when getting up A thing was desired.
• Patent documents 1 and 2 Japanese Patent Laid-Open No. 2011-98916, Japanese Patent Laid-open No. 2011-989178 propose a blended dentifrice composition, but the sustainability of the bactericidal activity is not mentioned and is unknown. is there.
• Patent Document 3 Japanese Patent No. 55688766 proposes a deashing inhibitor using isopropylmethylphenol and arabitol in combination, and is to be combined with a surfactant and an oral composition such as a mouthwash and the like Is disclosed.
• tea extract such as green tea as a compounding component for oral cavity composition not only to improve the feeling of use but also to prevent dental caries and halitosis by its antibacterial action
• Patent Documents 4 to 7 Patent No. 222419, Patent No. 5067529, Japanese Patent Application Laid-Open No. 2006-199661, and International Publication No. WO 2013/100089, but no mention is made of the durability of the antibacterial effect.
• JP, 2011-98916, A JP, 2011-98918, A Patent No. 5568876 gazette Japanese Patent Application Laid-Open No. 11-222419 Patent No. 5067529 JP, 2006-199661, A International Publication No. 2013/100089
• the present invention has been made in view of the above circumstances, and it is an object of the present invention to provide a dentifrice composition in which the antibacterial effect on bacteria in the oral cavity lasts for a long time.
• the present inventor combines isopropylphenol of an oral bactericide, a specific anionic surfactant and tea extract in combination with a dentifrice composition, It has been found that the durability of the antibacterial effect is remarkably improved, and the antibacterial effect can be imparted immediately after brushing teeth and can be sustained even after a long time, and that the stimulation and unpleasant taste are suppressed and the feeling in use becomes good. That is, according to the present invention, the dentifrice composition containing (A) isopropylmethylphenol, (B) ⁇ -olefin sulfonate, and (C) tea extract can provide a long-lasting antibacterial effect on oral bacteria. The present invention has been made based on the finding that the composition can be sustained over time and can impart low irritation and good taste.
• the durability of the antibacterial effect of the oral cavity antibacterial agent is not sufficient, and the antibacterial effect of tea extract is weak and the durability is also poor.
• surfactants such as anionic surfactants, which are general components of dentifrice compositions, are generally known to have a cleaning action and to some extent have an antibacterial effect, but the surfactant It could not provide a satisfactory antimicrobial effect.
• the three people unexpectedly act synergistically to give oral bacteria, in particular, pathogenic bacteria such as periodontal disease.
• the durability of the antibacterial effect was remarkably improved, and it was possible to impart an excellent antibacterial effect which lasts even after a long period of time immediately after brushing teeth.
• the component (A) has a unique unpleasant taste and the component (B) has a unique stimulus or bitterness
• these components unexpectedly interact with each other to cause the aforementioned unpleasant taste.
• the combination of the components (A), (B) and (C) gives a specific and remarkable action and effect as an antibacterial agent for oral cavity, and such action and effect, in particular, the durability of the antibacterial effect is As apparent from the results of the comparative examples described later, it was inferior if any of the components (A), (B) or (C) was lacking (comparative examples 2 to 5).
• the durability (after 8 hours) of the antimicrobial effect is inferior even if the antimicrobial agent triclosan and the components (B) and (C) are blended (comparative example) 3) Even if the components (A) and (C) are blended and the anionic surfactant sodium lauryl sulfate is further blended, if the component (B) is not blended, durability of the antimicrobial effect (8) After time) was inferior (comparative example 4).
• the present invention provides the following dentifrice composition.
• the present invention it is possible to provide a dentifrice composition in which the antibacterial effect on bacteria in the oral cavity lasts for a long time and the feeling of use is good.
• the dentifrice composition of the present invention can prevent the increase of bacteria in the oral cavity, which may cause oral diseases such as caries and periodontal disease, for a long time, since the antibacterial effect continues after use, and is more effective. And oral cavity diseases such as dental caries and periodontal disease can be prevented or suppressed.
• the dentifrice composition of the present invention contains (A) isopropylmethylphenol, (B) ⁇ -olefin sulfonate and (C) tea extract.
• Isopropylmethylphenol is an antibacterial agent, and its blending amount is preferably 0.001 to 0.1% (% by mass, hereinafter the same) of the whole composition, and more preferably 0.01 to 0.06. %. When the amount is 0.001% or more, a sufficient antibacterial effect is exhibited, and when it is 0.1% or less, unique unpleasant taste by itself is sufficiently suppressed.
• the (B) ⁇ -olefin sulfonate acts as an agent for improving the antimicrobial activity of the (A) component in combination with the (C) tea extract, and also as an inhibitor of the unpleasant taste of the (A) component.
• an alkali metal salt such as sodium or potassium of an ⁇ -olefinsulfonic acid having 10 to 16 carbon atoms, particularly 14 to 16 carbon atoms can be used.
• it is an ⁇ -olefin sulfonate having 14 carbon atoms, particularly a sodium salt (general name: sodium tetradecene sulfonate).
• trade name “K Lipolan PJ-400CJ” manufactured by Lion Specialty Chemicals Co., Ltd. can be used.
• the content of the (B) ⁇ -olefin sulfonate is preferably 0.1 to 2%, more preferably 0.3 to 1% of the total composition. If the blending amount is 0.1% or more, a sustained antibacterial effect can be sufficiently obtained. If it is 2% or less, the stimulation and bitter taste by itself are sufficiently suppressed, resulting in a feeling of use of low irritation.
• Tea extract acts as an agent for improving the antimicrobial activity of component (A) in combination with component (B), and also an inhibitor of unpleasant taste of component (A) and stimulation of component (B). Acts as well.
• the tea extract commercially available products or those obtained by known methods can be used. Specifically, green tea may be used as the raw material.
• the extraction solvent may be a hydrophilic solvent, and water, lower monohydric alcohols such as ethanol and propanol, polyhydric alcohols such as 1,3-butylene glycol and propylene glycol, etc. may be mentioned, and one kind selected from these A solvent or two or more mixed solvents can be used. Extraction conditions and post-processing can adopt a usual method.
• Commercially available products include green tea extract ("Japanese ism" manufactured by Maruzen Pharmaceutical Co., Ltd.) and the like.
• the blending amount of (C) tea extract is preferably 0.0007 to 0.01%, more preferably 0.001 to 0.005% of the whole composition as a pure extract extract excluding a solvent.
• a sustained antibacterial effect is fully acquired as a compounding quantity is 0.0007% or more, deterioration of a taste (oating taste) can be prevented as it is 0.01% or less, and a feeling of use can be maintained favorably.
• the blending ratio of the (B) component or the (C) component to the (A) component, or the blending ratio of the (B) component and the (C) component is not particularly limited. It can be set within the range that satisfies the blending amount of
• the dentifrice composition of the present invention can be prepared by a usual method as toothpaste, liquid toothpaste such as liquid toothpaste, moistened toothpaste, etc., and is particularly suitable as a toothpaste.
• other known components can be blended as needed in a range that does not impair the effects of the present invention.
• a surfactant other than the abrasive, the wetting agent, the caking agent, and the component (B), and if necessary, the colorant, the sweetener, the preservative, the flavor, the components other than the components (A) and (C) An active ingredient etc. can be mix
• blended may be conventional amounts as long as the effects of the present invention are not impaired.
• polishing agent examples include precipitated silica, silica-based polishing agents such as aluminosilicate and zirconosilicate, calcium phosphate-based compounds, calcium carbonate, and synthetic resin-based polishing agents. Silica-based polishing agents are particularly preferable.
• the blending amount of the abrasive is usually 2 to 50%, particularly 10 to 30%.
• the wetting agent may, for example, be a sugar alcohol such as sorbite or xylite, glycerin, propylene glycol, or a polyhydric alcohol such as polyethylene glycol having an average molecular weight of 160 to 400 (average molecular weight described in Quasi-drug raw material standard 2006).
• the blending amount of the wetting agent is usually 5 to 50%, particularly 10 to 30%.
• An organic or inorganic caking agent can be blended as a caking agent.
• cellulose derivatives such as sodium carboxymethyl cellulose, methyl cellulose and hydroxymethyl cellulose
• alginic acid derivatives such as propylene glycol alginate
• gums such as xanthan gum
• organic caking agents such as carrageenan, polyvinyl alcohol and sodium polyacrylate
• gelability Inorganic binders such as thickening silica such as silica, gelling aluminum silica and the like can be mentioned.
• the blending amount of the caking agent is usually 0.1 to 10%, particularly 0.1 to 5%.
• a combination of an organic caking agent and an inorganic caking agent is preferable, and the compounding amount of the organic caking agent is 5% or less, in particular 3% or less, and the compounding amount of the inorganic caking agent is 5% or less Especially 2% or less is good.
• anionic surfactants other than the component (B), nonionic surfactants, cationic surfactants, and amphoteric surfactants can be blended.
• Anionic surfactants include alkyl sulfates such as lauryl sulfate.
• Nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters, sugar alcohol fatty acid esters, sorbitan fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene hydrogenated castor oil, etc. Examples thereof include polyoxyethylene fatty acid esters, polyoxyethylene higher alcohol ethers, and fatty acid alkanolamides.
• the cationic surfactant includes alkyl ammonium type, alkyl benzyl ammonium salt and the like.
• Amphoteric surfactants include betaine acetates such as alkyl betaines and fatty acid amidopropyl betaines, betaines such as alkyl imidazolinium betaines, imidazolines and imidazolium betaines.
• the content of the surfactant is usually 0 to 10%, particularly 0.1 to 5%.
• the preferred blending amount of anionic surfactants other than the component (B), in particular lauryl sulfate, is 1 to 5%, particularly 1 to 3%.
• the preferred blending amount of the nonionic surfactant is 0 to 2%.
• Blue No. 1 Yellow No. 4, titanium dioxide and the like can be mentioned.
• saccharin sodium etc. are mentioned.
• the preservative include p-hydroxybenzoic acid esters such as methylparaben and butylparaben, benzoic acid or salts thereof, and the like.
• peppermint oil As flavoring agents, peppermint oil, spearmint oil, anise oil, eucalyptus oil, wintergreen oil, cassia oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, mint oil, cardamom oil, coriander oil, mandarin oil, Lime oil, lavender oil, rosemary oil, laurel oil, camomile oil, caraway oil, marjoram oil, bay oil, lemongrass oil, origanum oil, pine needle oil, neroli oil, rose oil, jasmine oil, grapefruit oil, sweetie Processing of natural flavors such as oil, soy sauce, iris concrete, absolute peppermint, absolute rose, orange flower, and processing of these natural flavors (pre-cut, pre-cut, fractional distillation, liquid extraction, essence, powder flavor And the like), and menthol, karl , Anethole, cineole, methyl salicylate, cinnamic aldehyde, eugenol, 3-l-menthoxy
• the known perfume materials used can be used in combination and are not limited to the perfumes described in the examples.
• the blending amount of the flavor is not particularly limited, it is preferable to use 0.00001 to 1% of the above-mentioned flavor material in the composition, and the flavoring fragrance using the above-mentioned flavor material has 0. It is preferable to use 1 to 2%.
• those known as medicinal ingredients for oral cavity for example, cationic bactericidal agents such as cetyl pyridinium chloride, anti-inflammatory agents such as tranexamic acid, allantoin, fluorine-containing compounds such as sodium fluoride and sodium monofluorophosphate , Enzymes, plant extracts, anti-calculus agents, anti-plaque agents and the like. These can be blended in effective amounts.
• Example Comparative Example
• the dentifrice composition (toothpaste) having the composition shown in Tables 1 to 3 was prepared by a conventional method and evaluated by the following method. The results are shown in the table.
• the culture solution was prepared by dissolving 30 g of trypticase soy broth (manufactured by Difco) in 1 L of purified water, 5 mg / L of hemin (manufactured by Sigma), 1 mg / L of vitamin K (manufactured by Wako Pure Chemical Industries, Ltd.) The one to which was added was used.
• As oral bacteria Streptococcus mutans strain ATCC 25175, Streptococcus sanguinis strain ATCC 10556, Actinomyces naes Landi strain ATCC 51655, Fusobacterium nucleatum strain ATCC 10953 and Bayionella parvula strain ATCC 17745, respectively, each of these 5 species is 2 ⁇ .
• model biofilm (1-2) Evaluation Method of Antibacterial Effect Immediately after Application
• the formed above-mentioned model biofilm is dispersed after adding an evaluation drug (double mass of artificial saliva * to a dentifrice composition to be evaluated, dispersed, and centrifuged) Soaked in 2 mL for 3 minutes and washed 6 times with 1 mL of sterile saline.
• the model biofilm is dispersed in sterile saline by sonication (200 ⁇ A, 10 seconds) in 4 mL of sterile saline, and 50 ⁇ L is spread on Bacteroides agar plate until colonies can be confirmed with naked eyes Anaerobic culture (80 vol% nitrogen, 10 vol% carbon dioxide, 10 vol% hydrogen) was performed.
• the model biofilm is dispersed in sterile saline by sonication (200 ⁇ A, 10 seconds) in 4 mL of sterile saline, and 50 ⁇ L can be spread on Bacteroides agar plates, and colonies can be confirmed visually Anaerobic culture was carried out (80 vol% nitrogen, 10 vol% carbon dioxide, 10 vol% hydrogen). The number of grown colonies was counted to determine the viable count (cfu) of the remaining Porphyromonas gingivalis bacteria, and the number was determined according to the following criteria.
• ⁇ Evaluation criteria> ⁇ : cfu is less than 10 7 ⁇ : cfu 10 7 to 10 8 less than ⁇ : cfu 10 8 or more
• the collected saliva samples were respectively diluted, and after anaerobic culture, the number of oral bacteria (Log (cfu / mL)) was measured.
• the numbers of oral bacteria of the samples A, B and C were a, b and c, respectively.
• saliva samples A, B, and C were collected in the same manner as described above except that the dentifrice composition was not used and the water was dipped in a toothbrush.

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• 2017
  • 2017-11-29 JP JP2017228839A patent/JP7031253B2/ja active Active
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