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WO2012073601A1 - Inhibiteur de la fixation d'une bactérie induisant une parodontopathie sur les surfaces des dents, inhibiteur de la formation de biofilm buccal, et composition pour des applications orales - Google Patents

Inhibiteur de la fixation d'une bactérie induisant une parodontopathie sur les surfaces des dents, inhibiteur de la formation de biofilm buccal, et composition pour des applications orales Download PDF

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Publication number
WO2012073601A1
WO2012073601A1 PCT/JP2011/073612 JP2011073612W WO2012073601A1 WO 2012073601 A1 WO2012073601 A1 WO 2012073601A1 JP 2011073612 W JP2011073612 W JP 2011073612W WO 2012073601 A1 WO2012073601 A1 WO 2012073601A1
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Prior art keywords
oral
propylene glycol
composition
inhibitor
biofilm
Prior art date
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Ceased
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PCT/JP2011/073612
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English (en)
Japanese (ja)
Inventor
丸山　真達
森嶋　清二
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Lion Corp
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Lion Corp
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Publication date
Application filed by Lion Corp filed Critical Lion Corp
Priority to JP2012546732A priority Critical patent/JP5729391B2/ja
Priority to CN201180057620.3A priority patent/CN103237538B/zh
Priority to KR1020137014630A priority patent/KR101820192B1/ko
Publication of WO2012073601A1 publication Critical patent/WO2012073601A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • 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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/734—Alginic acid
    • 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
    • A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic 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
    • A61K8/33—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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • A61K8/733—Alginic acid; Salts thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • 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
    • A61Q17/005—Antimicrobial preparations

Definitions

  • the present invention relates to a tooth surface adhesion inhibitor of periodontal disease-causing bacteria excellent in the effect of suppressing periodontal disease-causing bacteria in the oral cavity, and the effect of inhibiting periodontal disease-causing bacteria in the oral cavity and biofilm.
  • the present invention relates to an oral biofilm formation inhibitor and a composition for oral cavity, which have a high bactericidal effect and are effective in preventing and improving periodontal diseases.
  • Periodontal disease is considered to be an infectious disease caused by colonization of pathogenic bacteria in the oral cavity, and it is important to eliminate infected pathogenic bacteria for the prevention and improvement of periodontal disease. For this reason, various bactericides and antibiotics are used, but pathogenic bacteria that cause periodontal disease form biofilms and are known to be resistant to bactericides and antibiotics. Therefore, isopropylmethylphenol, a nonionic bactericidal agent that penetrates into the biofilm and sterilizes it, has been developed as a technology that has a high biofilm suppression effect that causes periodontal disease. There was room for.
  • propylene glycol alginate is known as a binder for oral compositions, and has been disclosed to have an effect of improving liquid separation of dentifrice (Patent Document 1) and an effect of adjusting viscosity with time (Patent Document). 2, 3). Moreover, it is disclosed that it can be mix
  • Patent Document 7 discloses a combination of propylene glycol alginate and triclosan, but the biofilm bactericidal effect is not sufficient and improved. There was room for. Furthermore, it is disclosed that propylene glycol alginate has an effect of masking the taste derived from essential oils, specifically, a masking action of thymol having an antibacterial action (Patent Document 8).
  • the present invention has been made in view of the above circumstances, and the tooth surface adhesion inhibitor of the periodontal disease-causing bacteria and the tooth surface adhesion-inhibiting effect of the periodontal disease-causing bacteria, which are excellent in the tooth surface adhesion-inhibiting effect of the periodontal disease-causing bacteria. It is an object of the present invention to provide an oral biofilm formation inhibitor and an oral composition that are excellent in aging and exhibit a high biofilm bactericidal effect.
  • propylene glycol alginate is effective as a tooth surface adhesion inhibitor for periodontal disease-causing bacteria.
  • the present inventors have combined the use of propylene glycol alginate and isopropylmethylphenol, and by blending these two components in the oral composition, it is excellent in the effect of suppressing periodontal disease causative bacteria. And it discovered that the high bactericidal effect with respect to an oral biofilm was exhibited, and the formulation excellent in the formation inhibitory effect of an oral biofilm was obtained.
  • the bactericidal effect with respect to the said oral biofilm could be further strengthened by mix
  • the dentifrice composition containing a poorly water-soluble disinfectant such as isopropylmethylphenol has a bactericidal effect on the oral biofilm, the effect is still not a sufficient level and there is room for improvement, In addition, bacteria remain in the oral cavity even after brushing, and the bacteria may adversely affect the periodontal tissue by attaching and multiplying in the oral cavity again.
  • the present inventors examined non-bactericidal plaque control means, and added alginic acid propylene glycol ester to the tooth surface of periodontal disease-causing bacteria, particularly Porphyromonas gingivalis. It has been found that there is a previously unknown effect of suppressing adhesion and it is useful for plaque control.
  • the mechanism of action is not clear, but both components act synergistically, and can suppress the initial adhesion of periodontopathic bacteria, which is the initial stage of formation of periodontopathic biofilm.
  • the preparation is coated on the tooth surface and isopropylmethylphenol is sufficiently retained, and the biofilm permeability of isopropylmethylphenol is further improved. This prevents the remaining in the interdental and gingival margins where cleaning is not possible. It is presumed to exert an excellent bactericidal effect even on periodontopathic biofilms with high drug barrier performance.
  • propylene glycol alginate has an effect of suppressing periodontal disease-causing adhesion to the tooth surface and enhances the biofilm bactericidal effect.
  • the present invention provides the following preparation and oral composition.
  • An oral biofilm formation inhibitor comprising (A) propylene glycol alginate and (B) isopropylmethylphenol.
  • An oral composition comprising (A) propylene glycol alginate and (B) isopropylmethylphenol.
  • a tooth surface adhesion inhibitor for periodontal disease-causing bacteria that effectively suppresses the adhesion of periodontal disease-causing bacteria to the tooth surface.
  • an oral biofilm formation inhibitor and an oral composition that are excellent in the effect of suppressing adhesion of periodontal disease-causing bacteria to the oral cavity and the biofilm bactericidal effect and can suppress the formation of biofilms are provided. it can. These preparations are effective in preventing and improving periodontal diseases.
  • the present invention relates to (A) a tooth surface adhesion inhibitor of periodontal disease-causing bacteria containing propylene glycol alginate as an active ingredient, and (A) oral biotechnology containing propylene glycol alginate and (B) isopropylmethylphenol as active ingredients.
  • propylene glycol alginate is a tooth surface adhesion inhibitor of periodontal disease-causing bacteria.
  • Propylene glycol ester of alginic acid is obtained by esterifying propylene glycol to a carboxyl group constituting alginic acid in order to enhance acid resistance and salt resistance of alginic acid.
  • Duckroid manufactured by Food Chemifa Co., Ltd. A product commercialized under a trade name such as kelp acid can be used.
  • Alginic acid propylene glycol ester is a quantitative ratio of ⁇ -D-mannuronic acid (M) and ⁇ -L-guluronic acid (G) constituting alginic acid (M / G ratio, molar ratio, hereinafter the same), sequence order, number (Molecular weight) and the molecular structure differing in the degree of esterification of the carboxyl group and the like, and the viscosity of the aqueous solution due to the difference in the molecular structure can take various values.
  • the propylene glycol alginate used in the present invention is not limited to these molecular structures and viscosities.
  • the constituent ratio of ⁇ -D-mannuronic acid (M) and ⁇ -L-guluronic acid (G) (M / (G ratio) is preferably greater than 1.0, particularly preferably greater than 1.0 and 2 or less.
  • the degree of esterification of the carboxyl group is preferably 40% or more, particularly preferably 70 to 95%. The higher the degree of esterification, the higher the effect. If the degree of esterification is less than 40%, there is a possibility that sufficient antifouling effect of periodontal disease-causing bacteria and enhanced biofilm bactericidal effect cannot be obtained. There is nothing in the market that exceeds 95%.
  • the viscosity at 20 ° C. (hereinafter the same) of an aqueous solution of 1% (mass%, hereinafter the same) by a BL type viscometer described later is 10 to 1,300 mPa ⁇ s, particularly 10 to 200 mPa. -It is preferable that it is the range of s. Those having a viscosity of less than 10 mPa ⁇ s are not commercially available. If the viscosity exceeds 1,300 mPa ⁇ s, there is a possibility that the adhesion suppressing effect of periodontal disease-causing bacteria and the enhancement effect of the biofilm bactericidal effect cannot be sufficiently obtained. .
  • the component (A) for example, the following commercially available products can be used.
  • Kimiloid LV 1% aqueous solution viscosity 90 mPa ⁇ s (rotor No.
  • the viscosity is a value measured by a BL type viscometer Specifically, it is a measured value by the following method. Further, the propylene glycol alginate can be used alone or in combination of two or more depending on the type of product.
  • Viscosity measurement method (Duck Lloyd, Food Chemifa Corporation) 4 g of propylene glycol alginate is collected and placed in a 600 mL beaker, and 396 g of purified water is added little by little while stirring with a stir bar. First, dissolve well with a small amount of water. Thereafter, the mixture is allowed to swell for 1 hour, and after 1 hour, the mixture is stirred for 1 minute at 12,000 rpm with a high-speed stirrer (homomixer). This solution is put into a 300 mL tall beaker and allowed to stand in a 20 ° C. water bath. When the foam rises and the beaker solution is clear, remove the foam with a spoon.
  • thermometer is put in a beaker to confirm that the test solution has reached 20 ° C., and the viscosity is measured.
  • Viscometer Tokyo Keiki BL type viscometer rotor: No. 1 Rotation speed: 60rpm Measurement time: 1 minute
  • Viscosity measurement method (Kimiloid, Kimlicum, Kimika Co., Ltd.) Take 297 g of purified water in a 300 mL tall beaker and add 3.0 g of alginate propylene glycol ester with stirring with a stirrer or three-one motor to completely dissolve. Next, after standing for 1 hour in a 20 ° C. constant temperature water bath (confirm that the aqueous solution of propylene glycol alginate reached 20 ° C.), a BL type viscometer (manufactured by Tokyo Keiki Co., Ltd.) was used for exactly 1 minute later. Measure the viscosity. The rotor used and the number of rotations were changed according to the viscosity range shown below.
  • Rotor No. 1 Rotation speed 60rpm When the viscosity is more than 80 mPa ⁇ s and not more than 160 mPa ⁇ s: Rotor No. 1, rotation speed 30rpm When the viscosity is more than 160 mPa ⁇ s and not more than 400 mPa ⁇ s: Rotor No. 2, rotation speed 60rpm When the viscosity exceeds 400 mPa ⁇ s and is 800 mPa ⁇ s or less: Rotor No. 2, rotation speed 30rpm When the viscosity exceeds 800 mPa ⁇ s and is 1,600 mPa ⁇ s or less: Rotor No. 3, rotation speed 60rpm
  • component (B) isopropylmethylphenol used in combination with alginate propylene glycol ester is a nonionic fungicide with a broad antibacterial spectrum, and Takasago Fragrance Co., Ltd., Ogawa Fragrance Co., Osaka Kasei Co., Ltd., Sumitomo Pharmaceutical Co., Ltd. Products that have been commercialized by companies can be used.
  • the mass ratio of the component (A) / component (B) in the combination system is not particularly limited, but is preferably 0.4 to 20, particularly 1 to 10. If the mass ratio of the component (A) / component (B) is less than 0.4 or exceeds 20, the adhesion inhibitory effect of periodontal disease-causing bacteria and the biofilm bactericidal effect may not be sufficiently exhibited.
  • composition for oral cavity of the present invention contains a combination system of the above-mentioned (A) propylene glycol alginate and (B) isopropylmethylphenol as active ingredients.
  • the blending amount of propylene glycol alginate is not particularly limited, but is preferably 0.02 to 1%, particularly preferably 0.05 to 0.5% of the whole oral composition. If the blending amount is less than 0.02%, there is a possibility that sufficient adhesion inhibitory effect of periodontal disease-causing bacteria and enhancement effect of biofilm sterilization by isopropylmethylphenol may not be obtained. If it exceeds 1%, the adhesion inhibitory effect of periodontal disease-causing bacteria is saturated, so that the improvement of the adhesion inhibitory effect cannot be expected, and the enhancement effect of biofilm sterilization by isopropylmethylphenol may be reduced.
  • the blending amount of isopropylmethylphenol is not particularly limited, but is preferably 0.005 to 0.1%, particularly 0.01 to 0.1% of the entire composition. If the blending amount is less than 0.005%, the bactericidal effect on the biofilm may not be sufficiently exhibited. If it exceeds 0.1%, the solubility of isopropylmethylphenol itself is poor, so that the biofilm sterilization effect may be reduced by precipitation.
  • the mass ratio of the component (A) / (B) is the same as described above.
  • the oral composition of the present invention may further contain at least one anionic surfactant selected from alkyl sulfates and acyl sarcosinates as component (C).
  • component (C) is not particularly limited, but as the alkyl sulfate salt, an alkali metal salt of a higher alkyl sulfate ester having 8 to 18 carbon atoms, and as the acyl sarcosine salt, the acyl group has a carbon number of acyl group. 8 to 18 acyl sarcosine salts can be used, and sodium lauryl sulfate and / or sodium lauroyl sarcosine are particularly preferably used.
  • the blending amount of the anionic surfactant is not particularly limited, but is preferably 0.05 to 3%, particularly preferably 0.1 to 2.0% of the whole composition. If the blending amount is less than 0.05%, the biofilm sterilization effect may not be improved, and if it exceeds 3%, the enhancement effect of periodontopathic biofilm sterilization effect is saturated, and more biofilms There is a possibility that the bactericidal effect cannot be obtained, and the adhesion surface of the periodontal disease-causing bacteria is affected, and the periodontal disease-causing bacteria adhesion suppressing effect may be reduced.
  • the oral composition of the present invention is in the form of liquid, paste, gel, etc., and is used for toothpastes such as toothpaste, toothpaste, liquid toothpaste, mouthwash, gel, ointment, mouth freshener, gargle Can be prepared in various dosage forms such as tablets for oral use, pasta for oral cavity, gum, etc., and known ingredients other than the above ingredients are blended within a range that does not impair the effects of the present invention, and prepared by ordinary methods. Can do.
  • various abrasives, wetting agents, binders, surfactants, sweeteners, coloring agents, preservatives, fragrances, pH adjusters, and other active ingredients are included as optional components. it can.
  • abrasives precipitated silica, silica gel, aluminosilicate, zeolite, zirconosilicate, dicalcium phosphate dihydrate and anhydride, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, tertiary phosphorus
  • examples thereof include magnesium oxide, insoluble sodium metaphosphate, insoluble potassium metaphosphate, titanium oxide, hydroxyapatite, and synthetic resin-based abrasive (mixing amount: usually 5 to 50%).
  • wetting agent examples include glycerin, sorbitol, propylene glycol, polyethylene glycol, 1,3-butylene glycol, erythritol, xylit, maltite, lactit, trehalose, tornale and the like (blending amount: usually 0 to 50%, especially 5 ⁇ 45%).
  • Binders include carrageenan, sodium carboxymethylcellulose, sodium alginate, polyacrylic acid, sodium polyacrylate, carboxyvinyl polymer, polyvinyl alcohol, polyvinylpyrrolidone, xanthan gum, tara gum, guar gum, locust bean gum, gellan gum, gelatin, curdlan , Gum arabic, agar, pectin, pullulan, etc. (blending amount: usually 0.1 to 5%).
  • surfactant examples include anionic surfactants other than the component (C), nonionic surfactants, cationic surfactants, and amphoteric surfactants, and one or more of these are used. Also good.
  • anionic surfactant include lauroylmethyl taurine, acylamino acid salts, sodium dodecylbenzenesulfonate, ⁇ -sulfo fatty acid alkyl ester / sodium, and alkyl phosphate ester salts.
  • nonionic surfactant examples include polyoxyethylene sorbitan fatty acid ester, sucrose fatty acid ester, sorbitan fatty acid ester, polyoxyethylene polyoxypropylene block copolymer type activator, polyoxyethylene fatty acid ester, fatty acid monoglyceride and the like.
  • Amphoteric surfactants include betaine acetate-type amphoteric surfactants such as alkyldimethylaminoacetic acid betaines and fatty acid amidopropyldimethylaminoacetic acid betaines, and imidazoline types such as N-fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salts.
  • amphoteric surfactants examples include amphoteric surfactants and amino acid type surfactants such as N-fatty acid acyl-L-alginate salts.
  • amino acid type surfactants such as N-fatty acid acyl-L-alginate salts.
  • cationic surfactant examples include alkylammonium and alkylbenzylammonium salts (blending amount: usually 0.1 to 5%).
  • sweetener examples include saccharin, saccharin sodium, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl hydrochalcone, perilartine, xylitol, maltitol, sucralose, reduced palatinose, erythritol, aspartame and the like.
  • colorant examples include blue No. 1, yellow No. 4, titanium dioxide and the like.
  • preservative examples include sodium benzoate, p-hydroxybenzoate ester, alkyldiaminoethylglycine hydrochloride, potassium sorbate and the like.
  • Perfumes include natural oils such as peppermint oil, spearmint oil, eucalyptus oil, wintergreen oil, clove oil, thyme oil, sage oil, cardamom oil, rosemary oil, marjoram oil, lemon oil, nutmeg oil, lavender oil, paracres oil, etc.
  • pH adjusting agents examples include phthalic acid, phosphoric acid, citric acid, succinic acid, acetic acid, fumaric acid, malic acid, carbonic acid and their potassium salts, sodium salts or ammonium salts, ribonucleic acid and salts thereof, sodium hydroxide, etc. 1 type (s) or 2 or more types can be used.
  • active ingredients include cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, chlorhexidine hydrochloride, alkyldiaminoethylglycine hydrochloride, hinokitiol, and other fungicides, tranexamic acid, epsilon-aminocaproic acid, azulene, allantoin, allantochlorohydroxyaluminum, Allantoin dihydroxyaluminum, glycyrrhetin salts, glycyrrhetinic acid, dihydrocholesterol, hydrocholesterol and other anti-inflammatory agents, dextranase, lysozyme chloride, amylase, protease, mutanase, lytic enzyme, lytechenzyme, etc., sodium fluoride, monofluorolin Sodium fluoride, fluorides such as stannous fluoride, vitamins such as ascorbate and tocophe
  • the blending amount is mass%.
  • Alginic acid propylene glycol ester-1 Product name: Kimiroid BF Viscosity 20 mPa ⁇ s (rotor No. 1, 60 rpm) M / G ratio 1.3, degree of esterification 80% Alginic acid propylene glycol ester-2
  • Kimiloid NLS-K Viscosity 55 mPa ⁇ s (rotor No. 1, 60 rpm) M / G ratio 1.3
  • degree of esterification 80% Alginic acid propylene glycol ester-3 Product name: Kimiroid MV, manufactured by Kimika Co., Ltd. Viscosity: 148 mPa ⁇ s (rotor No.
  • a solution suspended in anaerobic conditions 80 vol% nitrogen, 10 vol% carbon dioxide, 10 vol% hydrogen
  • PBS manufactured by Wako Pure Chemical Industries, Ltd.
  • the adherent carrier was immersed in human unstimulated saliva filtered with a 0.45 ⁇ m filter for 1 hour (37 ° C.) using a hydroxyapatite (HA) plate (manufactured by Asahi Optical Co., Ltd.) having a diameter of 7 mm and a thickness of 3.5 mm.
  • the HA surface was coated with saliva components and subjected to the test.
  • the saliva-coated HA plate was washed once with PBS (manufactured by Wako Pure Chemical Industries, Ltd.) and then immersed in 2 mL of a test composition having the composition shown in Tables 1 to 3 for 5 minutes. After the treatment, the plate was washed once with PBS, and then the HA plate was immersed in the aforementioned Porphyromonas gingivalis solution for 30 minutes (37 ° C.). Thereafter, the HA plate was washed three times with 1 mL of PBS, and then the adhered bacteria were dispersed by sonication (200 ⁇ A, 10 seconds) in 4 mL of PBS, and 10-fold serial dilution was performed using PBS.
  • PBS manufactured by Wako Pure Chemical Industries, Ltd.
  • Adhesion inhibition rate (%) ((number of adherent bacteria in control ⁇ number of adherent bacteria in test composition) / (number of adherent bacteria in control)) ⁇ 100
  • Adhesion inhibition rate is 80% or more and 100% or less
  • Adhesion inhibition rate is 60% or more and less than 80%
  • Adhesion suppression rate is 0% or more and less than 40%
  • THBHM Composition of THBHM: Expressed by mass in 1 liter.
  • Todd Hewitt Broth Becton and Dickinson: 30g / L Hemin (Sigma Aldrich): 5mg / L Menadion (Wako Pure Chemical Industries, Ltd.): 1mg / L Distilled water: Residue (Med up so that the total amount becomes 1 L, and autoclaved at 121 ° C. for 20 minutes.)
  • alginic acid propylene glycol ester exhibits an excellent effect of suppressing adhesion of periodontal disease-causing bacteria.
  • model biofilm What was treated for 4 hours with human unstimulated saliva obtained by filtering a hydroxyapatite (HA) plate (manufactured by Asahi Optical Co., Ltd.) having a diameter of 7 mm and a thickness of 3.5 mm with a 0.45 ⁇ m filter.
  • a basal medium mucin culture solution (BMM) * 3 was used as a model biofilm carrier and a culture solution.
  • the strains used to make the model biofilms are Actinomyces viscosus ATCC 43146, Veilonella parvula ATCC17745, and VEC. (Porphyromonas gingivalis) ATCC 33277 was used.
  • model biofilm was transferred to a 24-well multiplate (manufactured by Sumitomo Bakelite Co., Ltd.), added with 2 mL of the test composition shown in Tables 2 and 3, and immersed for 3 minutes. After washing 6 times with 1 mL of Kojunkaku Kogyo Co., Ltd., it was dispersed by sonication (200 ⁇ A, 10 seconds) in a test tube (diameter 13 mm ⁇ 100 mm) to which 4 mL of the same buffer was added.
  • Bactericidal rate of periodontal disease bacteria is 1,000 or more ⁇ : Bactericidal rate of periodontal disease bacteria is 100 or more and less than 1,000 ⁇ : Bactericidal rate of periodontal disease bacteria is 10 or more and 100 Less than: ⁇ : Bactericidal rate of periodontal disease bacteria is 1 or more and less than 10 ⁇ : Bactericidal rate of periodontal disease bacteria is less than 1
  • alginic acid propylene glycol ester exhibits an excellent effect of suppressing adhesion of periodontal disease-causing bacteria.
  • the combined use of propylene glycol alginate and isopropylmethylphenol is superior in the effect of suppressing the adhesion of periodontal disease-causing bacteria and improves the biofilm bactericidal effect. From this, it was confirmed that the combined system has an excellent effect of suppressing the formation of oral biofilm.
  • composition for oral cavity of the following prescription example was prepared by a conventional method.
  • the raw materials used were the same as described above, and the propylene glycol alginate used was Kimika Co., Ltd., trade name: Kimiloid BF.
  • Kimika Co., Ltd. trade name: Kimiloid BF.

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Abstract

L'invention concerne : un inhibiteur de la fixation d'une bactérie induisant une parodontopathie sur les surfaces des dents qui possède un excellent effet inhibiteur de la fixation de la bactérie induisant une parodontopathie sur les surfaces des dents ; un inhibiteur de formation de biofilm buccal qui possède un excellent effet inhibiteur de la fixation de la bactérie induisant une parodontopathie sur les surfaces des dents et peut présenter un effet élevé de stérilisation du biofilm ; et une composition pour des applications orales. L'invention concerne également un inhibiteur de la fixation d'une bactérie induisant une parodontopathie sur les surfaces des dents qui comprend (A) un ester de propylène glycol d'acide alginique ; un inhibiteur de la formation de biofilm buccal qui comprend (A) un ester de propylène glycol d'acide alginique et (B) de l'isopropylméthylphénol ; et une composition pour des applications orales qui est caractérisée en ce qu'elle comprend (A) un ester de propylène glycol d'acide alginique et (B) de l'isopropylméthylphénol.
PCT/JP2011/073612 2010-11-30 2011-10-14 Inhibiteur de la fixation d'une bactérie induisant une parodontopathie sur les surfaces des dents, inhibiteur de la formation de biofilm buccal, et composition pour des applications orales Ceased WO2012073601A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2012546732A JP5729391B2 (ja) 2010-11-30 2011-10-14 歯周病原因菌の歯面付着抑制剤、口腔バイオフィルム形成抑制剤及び口腔用組成物
CN201180057620.3A CN103237538B (zh) 2010-11-30 2011-10-14 牙周病原菌的齿面附着抑制剂、口腔生物膜形成抑制剂及口腔用组合物
KR1020137014630A KR101820192B1 (ko) 2010-11-30 2011-10-14 치주병 원인균의 치면 부착 억제제, 구강 바이오필름 형성 억제제 및 구강용 조성물

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2014157547A1 (ja) * 2013-03-27 2017-02-16 ライオン株式会社 口腔用組成物
JP2017119639A (ja) * 2015-12-28 2017-07-06 花王株式会社 Ｔｒｐｖ４活性化剤
JP2021175714A (ja) * 2020-05-01 2021-11-04 サンスター株式会社 口腔用組成物

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2562437B (en) 2016-01-28 2022-05-25 Kimberly Clark Co Anti-adherent composition against DNA viruses and method of inhibiting the adherence of DNA viruses to a surface
US11168287B2 (en) 2016-05-26 2021-11-09 Kimberly-Clark Worldwide, Inc. Anti-adherent compositions and methods of inhibiting the adherence of microbes to a surface
WO2019107335A1 (fr) * 2017-11-30 2019-06-06 ライオン株式会社 Inhibiteur de formation de biofilm buccal et composition à usage oral

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH04139118A (ja) * 1990-10-01 1992-05-13 Lion Corp 口腔用組成物
JPH1171250A (ja) * 1997-08-29 1999-03-16 Lion Corp 口腔用組成物
JPH1171251A (ja) * 1997-08-29 1999-03-16 Lion Corp 口腔用組成物
JP2006176479A (ja) * 2004-12-24 2006-07-06 Lion Corp 歯磨剤組成物
JP2008156309A (ja) * 2006-12-26 2008-07-10 Lion Corp 口腔用組成物
JP2009520802A (ja) * 2005-12-21 2009-05-28 マクニール−ピーピーシー・インコーポレーテツド 親水コロイドを用いた、精油の味覚マスキング
JP2009149535A (ja) * 2007-12-19 2009-07-09 Lion Corp 口腔用組成物
JP2009155271A (ja) * 2007-12-27 2009-07-16 Lion Corp 口腔用組成物

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4763441B2 (ja) * 2004-12-10 2011-08-31 花王株式会社 歯垢形成抑制剤並びにそれを含む口腔剤組成物及び食品

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH04139118A (ja) * 1990-10-01 1992-05-13 Lion Corp 口腔用組成物
JPH1171250A (ja) * 1997-08-29 1999-03-16 Lion Corp 口腔用組成物
JPH1171251A (ja) * 1997-08-29 1999-03-16 Lion Corp 口腔用組成物
JP2006176479A (ja) * 2004-12-24 2006-07-06 Lion Corp 歯磨剤組成物
JP2009520802A (ja) * 2005-12-21 2009-05-28 マクニール−ピーピーシー・インコーポレーテツド 親水コロイドを用いた、精油の味覚マスキング
JP2008156309A (ja) * 2006-12-26 2008-07-10 Lion Corp 口腔用組成物
JP2009149535A (ja) * 2007-12-19 2009-07-09 Lion Corp 口腔用組成物
JP2009155271A (ja) * 2007-12-27 2009-07-16 Lion Corp 口腔用組成物

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPWO2014157547A1 (ja) * 2013-03-27 2017-02-16 ライオン株式会社 口腔用組成物
JP2017119639A (ja) * 2015-12-28 2017-07-06 花王株式会社 Ｔｒｐｖ４活性化剤
JP2021175714A (ja) * 2020-05-01 2021-11-04 サンスター株式会社 口腔用組成物
JP7630917B2 (ja) 2020-05-01 2025-02-18 サンスター株式会社 口腔用組成物

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JPWO2012073601A1 (ja) 2014-05-19
KR101820192B1 (ko) 2018-01-18
CN103237538A (zh) 2013-08-07
CN103237538B (zh) 2016-01-20
MY162054A (en) 2017-05-31
JP5729391B2 (ja) 2015-06-03

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