EP3866934A1 - Composition de soin buccal contenant de l'acyl-n-méthylglucamide pour le traitement des caries par réduction de la libération d'acide lactique dans des biofilms buccaux - Google Patents

Composition de soin buccal contenant de l'acyl-n-méthylglucamide pour le traitement des caries par réduction de la libération d'acide lactique dans des biofilms buccaux

Info

Publication number
EP3866934A1
EP3866934A1 EP19783727.1A EP19783727A EP3866934A1 EP 3866934 A1 EP3866934 A1 EP 3866934A1 EP 19783727 A EP19783727 A EP 19783727A EP 3866934 A1 EP3866934 A1 EP 3866934A1
Authority
EP
European Patent Office
Prior art keywords
methylglucamide
acyl
lactic acid
oral
care composition
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP19783727.1A
Other languages
German (de)
English (en)
Inventor
Ingo R. Haeberlein
Brenda Schmid
Melanie N. HAUKE
Jie Yang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
3M Innovative Properties Co
Original Assignee
3M Innovative Properties Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 3M Innovative Properties Co filed Critical 3M Innovative Properties Co
Publication of EP3866934A1 publication Critical patent/EP3866934A1/fr
Withdrawn legal-status Critical Current

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Classifications

    • 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
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • 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
    • A61K8/60—Sugars; 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
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • 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
    • A61K8/731—Cellulose; Quaternized cellulose derivatives
    • 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
    • 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
    • A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • A61K8/817—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a single or double bond to nitrogen or by a heterocyclic ring containing nitrogen; Compositions or derivatives of such polymers, e.g. vinylimidazol, vinylcaprolactame, allylamines (Polyquaternium 6)
    • A61K8/8176—Homopolymers of N-vinyl-pyrrolidones. Compositions of derivatives of such polymers
    • 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
    • A61K2800/74—Biological properties of particular ingredients
    • 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
    • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/87—Application Devices; Containers; Packaging
    • 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
    • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/92—Oral administration

Definitions

  • the invention relates to acyl-N-methylglucamide(s) for use in a method of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm of a living human or animal being and to an oral care composition containing acyl- N-methylglucamide(s) for this use.
  • composition comprises certain acyl-N-methylglucamide(s) dissolved or dispersed in water, optionally in combination with a carrier material.
  • Dental plaque which may include bacteria such as Streptococcus mutans, comprises a biofilm that forms on surfaces in the oral cavity. Dental plaque is at least partly responsible for dental caries, gingivitis, and periodontal diseases.
  • Dental plaque Bacteria in dental plaque metabolize carbohydrates (for example, simple sugars) in the mouth and produce acids that can etch tooth enamel, dentin, and cement. Dental plaque can serve as a substrate for the deposition of tartar or calculus. Build-up of dental plaque and calculus can lead to gingivitis and, ultimately, to periodontal disease.
  • carbohydrates for example, simple sugars
  • a currently available method to remove dental plaque from teeth is mechanical removal with, for example, dental floss or a toothbrush.
  • a toothbrush can aid in removing dental plaque from exposed surfaces of a tooth, and dental floss can aid in removing dental plaque from, for example, interproximal and subgingival surfaces.
  • Proper and regular use of dental floss and a toothbrush can mechanically remove or reduce dental plaque, and can reduce the incidence of dental caries, gingivitis, and periodontal disease.
  • Certain antimicrobial formulations are available (in the form of mouthwashes, rinses, and toothpastes, for example) to aid in the control and treatment of dental plaque, dental caries, gingivitis, and periodontal disease.
  • dental caries results from an imbalance of the metabolic activity in the individual dental biofilm. This reflects the daily clinical experiences that only a small fraction of dental plaque might end up in tooth demineralization. Even more, certain studies with dental biofilm revealed that the bacterial composition of dental plaque does not necessarily indicate the prevailing metabolic (caries) activity of the individual dental plaque.
  • WO 2009/014907 Al provides a dental composition comprising a compound of a certain formula or acceptable salt thereof for inhibiting the formation of biofilm.
  • a compound of a certain formula or acceptable salt thereof for inhibiting the formation of biofilm.
  • N-methyl-d-glucamine is mentioned.
  • WO 00/69890 Al (Stromberg et al.) relates to an oligopeptide protecting against dental caries comprising two arginine residues selected from the group consisting of pentapeptide, hexapeptide, heptapeptide, octapeptide, nonapeptide and decapeptide.
  • CA 986 022 (Goldman et al.) describes a composition suitable for treating teeth for the prevention of plaque which comprises an aqueous solution of N-monochloroglycine buffered to a pH in the range of 9 to 11.5.
  • EP 0 224 599 Al (National Patent Development Corp.) relates to a chemical solution useful in the removal of carious lesions or plaque, said solution being prepared immediately prior to use and formed by mixing DL-2-aminobutyric acid, glycine, sodium hydroxide, sodium chloride, sodium hypochloride in de-ionized water.
  • EP 0 711 543 Al (Unilever) relates to an oral preparation having an anti-caries activity, comprising pyruvic acid or an orally-acceptable salt thereof and urea and/or arginine or a derivative thereof.
  • US 9,750,670 B2 (Pan et al.) provides a composition for oral personal care comprising a tetrabasic zink-amino acid or trialkyl glycine-halide complex, cysteine in free or in orally or cosmetically acceptable salt form.
  • US 2007/0116831 Al (Prakash et al.) describes a dental composition comprising an active dental substance such hydrogen peroxide, one high-potency sweetener such as rebaudioside A, and one sweet taste improving composition, such as an amino acid.
  • US 4,339,432 (Ritchey et al.) relates to an oral mouthwash containing zinc and glycine. It is stated that the astringency of an oral mouthwash composition containing biologically active zinc ions may be reduced by the addition of glycine.
  • WO 2009/014907 Al relates to dental compositions comprising molecules including N-alkyl glucamides.
  • the compositions can be used for prevention of biofilms.
  • an in-vitro human saliva derived microcosm biofilm was used to apply MEGA-9 in mouth rinse formulations twice a day for 1 min each. It was observed that a MEGA-9 concentrations >0.7% accomplishes a significant reduction of biofilm growth without changing the colony forming units of the bacteria in the biofilm.
  • WO 2017/205230 Al describes a dental paste comprising (i) a compound of Formula I, (ii) a compound of Formula II and (iii) a dental abrasive.
  • the dental paste can be used as prophy paste and for inhibiting biofilm formation on a surface in the oral cavity.
  • the compound according to Formula I has the following structure: HOCH2- (CHOH-)nCH2NR 1 R 2 with R 1 being H or an alkyl group, R 2 being C(0)R 3 , wherein R 3 is a C3-C9 alkyl group and n being an integer from about 2 to about 5.
  • the compound according to Formula II has the following structure: HOCH2-(CHOH-) m CH2NHR 4 with R 4 being H or an alkyl group, and n being an integer from about 2 to about 5.
  • R 4 being H or an alkyl group
  • n being an integer from about 2 to about 5.
  • WO 90/04789 Al (Meito Sangyo) describes reagents for diagnosis of periodontal disease of bacteroides gingivalis consisting of particles of latex sensitized with B. gingivalis fimbrial antigen or an antibody to it.
  • WO 00/27438 (Unilever) relates to a bactericidal and non-bactericidal solution for removing biofilms.
  • the composition comprises a detergent and a salt or salt-forming acid.
  • detergents are listed such as cetylpyridinium chloride (CPC), cetylpyridinium bromide (CPB), hexadecyltrimethylammonium bromide (CTAB), benzalkonium chloride, octanonyl -methyl -glucamide (MEGA-8), sodium dodecyl sulfact (SDS), etc. wherein SDS and CPB are said to be preferred.
  • a biofilm matrix such as dental plaque may contribute to the isolation of bacteria from the protective effect of antimicrobial compounds and, thus, may interfere with the function of antimicrobial formulations such as mouthwashes, rinses, and toothpastes.
  • composition should be easy in administering and simple in use. Ideally, the composition should be easy to prepare and reasonable in price of manufacturing.
  • composition should not have undesired side effects like bad taste or being astringent.
  • the invention features acyl-N-methylglucamide(s) and an oral care composition containing acyl-N-methylglucamide(s) for use in a method of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a living human being or animal as described in the present text and claims.
  • the invention features a composition, in particular an oral care composition, for use in a method of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a living human being or animal, the composition comprising acyl-N-methylglucamide(s) or mixtures thereof as described in the present text and claims, which are dissolved or dispersed in water and being present in an amount of at least 0.1 wt.% with respect to the composition.
  • the invention is also related to a kit of parts as described in the present text and claims for use in a method of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a living human being or animal, the kit of parts containing Part A comprising acyl-N-methylglucamide(s) or mixtures thereof, Part B comprising water, and optionally Part C comprising an application device.
  • the invention is also directed to the use of certain acyl-N-methylglucamide(s) or mixtures thereof for producing a composition or a kit of parts as described in the present text and claims for use in a method of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a living human being or animal.
  • the acyl-N-methylglucamide(s) and oral care composition described in the present text are particularly useful for treating caries of patients having xerostomia, that is, patients having a reduced salivary flow.
  • acyl-N-methylglucamide(s) and oral care composition are particularly useful for treating caries being located in dental interstices, that is, in the region between two adjacent teeth (interproximal region).
  • composition is understood to be a mixture of two or more components.
  • a “dental or oral care composition” is a composition which is to be used in the dental field (including restorative and prosthodontic work) including the orthodontic area.
  • the composition should be not detrimental to the patient's health and thus free of hazardous and toxic components being able to migrate out of the composition.
  • Commercially available products have to fulfil certain requirements such as those given in DIN EN ISO 1942:2011-03.
  • An oral care composition is a composition for use in the oral environment, i.e. for treating the surfaces of soft and hard dental tissue.
  • An oral care composition is not intended to be administered with the intention to be swallowed by the patient.
  • a "dental surface” or“dental hard tissue” refers to tooth structures (e. g., enamel, dentin, and cementum) and bone.
  • A“tooth structure” is any tooth structure, prepared or ready for preparation by the dentist. It can be a single tooth or two or more teeth. A tooth structure is also referred to as hard dental tissue in contrast to soft dental tissue (e.g. gingival).
  • “Caries” is understood as tooth decay, also known as dental caries which is a demineralization and/or breakdown of teeth due to acids made by bacteria.
  • “Dental plaque” is understood as is a biofilm or mass of bacteria that grows on surfaces within the mouth.
  • the term“biofilm” refers to a matrix containing bacteria.
  • a biofilm in an oral cavity can include bacteria, epithelial cells, leukocytes, macrophages and other oral exudate.
  • A“paste” is a substance that behaves as a solid until a sufficiently large load or stress is applied, at which point it flows like a fluid.
  • Pastes typically consist of a suspension of granular material in a background fluid. The individual grains are jammed together like sand on a beach, forming a disordered, glassy or amorphous structure, and giving pastes their solid-like character. Pastes can be classified by their viscosity or their consistency comparable to dental impression material.
  • A“toothpaste” (dentifrice) is a cleaning agent for the daily individual care. It is typically used as a prophylactic measure against caries, gingivitis or periodontitis.
  • a“prophylaxis paste” is a product which is used by a profession such as a dentist or a dental hygienist to remove adherent deposits such as stain, plaque or tartar which may stick to the surface of a natural tooth, artificial tooth crown or bridge or filling material.
  • a prophylaxis paste is therefore typically used on slowly rotating paste carrier (sometimes also referred to as prophy cups). Most of the commercially available prophylaxis pastes have a different viscosity compared to tooth pastes.
  • A“gel” is typically a colloidal system in which a porous matrix of interconnected particles spans the volume of a liquid medium.
  • gels are apparently solid, jelly- like materials. Both by weight and volume, gels are mostly liquid in composition and thus exhibit densities similar to liquids, however, have the structural coherence of a solid.
  • An example of a common gel is edible gelatine. Many gels display thixotropy, that is, they become fluid when agitated, but re-solidify when resting.
  • A“film forming agent” is a substance which will cause a composition containing it to change from a liquid stage to a solid stage in such a manner as to form a film or coating on a surface.
  • A“solvent” means a liquid which is able to at least partially disperse or dissolve a component at ambient conditions (e.g. 23°C).
  • a solvent typically has a viscosity below 5 or below 1 or below 0.1 Pa*s at 23°C.
  • A“particle” means a substance being a solid having a shape which can be geometrically determined. Particles can typically be analysed with respect to e.g. grain size.
  • the mean particle size of a powder can be obtained from the cumulative curve of the grain size distribution and is defined as the arithmetic average of the measured grain sizes of a certain powder mixture. Respective measurements can be done using commercially available granulometers (e.g. CILAS Laser Diffraction Particle Size Analysis Instrument).
  • Ambient conditions mean the conditions which the inventive solution is usually subjected to during storage and handling.
  • Ambient conditions may, for example, be a pressure of 900 to 1100 mbar, a temperature of 10 to 40 °C and a relative humidity of 10 to 100 %. In the laboratory ambient conditions are adjusted to 20 to 25 °C and 1,000 to 1,025 mbar.
  • a composition is“essentially or substantially free of’ a certain component, if the composition does not contain said component as an essential feature. Thus, said component is not wilfully added to the composition either as such or in combination with other components or ingredient of other components.
  • a composition being essentially free of a certain component usually does not contain that component at all. However, sometimes the presence of a small amount of the said component is not avoidable e.g. due to impurities contained in the raw materials used.
  • Adding an“(s)” to a term means that the term should include the singular and plural form.
  • the term“additive(s)” means one additive and more additives (e.g. 2, 3, 4, etc.).
  • Fig. 1 shows a SEM picture of an untreated human saliva derived biofilm.
  • Fig. 2 shows a SEM picture of a human saliva derived biofilm, which has been treated with MEGA-9.
  • the composition described in the present text provides an effective means for reducing the risk of caries.
  • the cell membrane modifying agent primarily refers to the cell membrane of the cells of the bacteria forming the biofilm and of the extra-cellular membranes constituting the biofilm.
  • acyl-N-methylglucamide(s) and oral care composition described in the present text are designed to move from a plaque formation inhibition agent or composition or dental plaque removal composition or biofilm reducing composition to an agent or composition allowing the control of the metabolic balance on dental plaque.
  • the invention shows that certain acyl-N-methylglucamide(s) are effective to accomplish caries activity control in a dental biofilm without being antimicrobial, i.e. being able to influence the metabolic balance of the dental biofilm.
  • acyl-N- methylglucamide(s) proposed in the present text are easily available at reasonable costs and essentially non-toxic to the patient.
  • the oral care composition described in the present text for use in a method or therapy of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm of a human or animal being comprises certain acyl-N- methylglucamide(s) or mixtures thereof.
  • acyl-N-methylglucamide(s) can be characterized by the following formula:
  • MEGA-9 MEGA-9, MEGA- 10, MEGA- 11 or MEGA-12.
  • MEGA-9 MEGA-9 is sometimes preferred.
  • MEGA-9 has the following structure:
  • MEGA-9 N-Methyl-N-Nonanoylglucamide (CAS# 85261-19-4).
  • glucamides such as MEGA-8 are less effective than MEGA-9, MEGA- 10, MEGA- 11 or MEGA- 12 for reducing the lactic acid release of lactic acid releasing bacteria in the mouth of a patient, or essentially non-effective at all.
  • the reduction of the lactic acid release can be determined as described in the example section.
  • acyl-N-methylglucamide(s) are typically present in an aqueous composition in an amount of at least 0.1 wt.% with respect to the whole composition.
  • acyl-N-methylglucamide(s) include:
  • Tipper limit utmost 10 or utmost 8 or utmost 5 wt.%;
  • Range 0.1 to 10 or 0.2 to 8 or 0.3 to 5 wt.%;
  • the acyl-N-methylglucamide(s) may be used and applied together with water.
  • the oral care composition also comprises water.
  • Water is used for dissolving the acyl-N-methylglucamide(s) contained in the composition, at least partially.
  • Water is typically present in an amount sufficient to fully dissolve the acyl-N- methylglucamide(s) and other optional components being present in the composition. It has been found that the desired effect of reducing the lactic-acid release can be achieved more effectively, if the acyl-N-methylglucamide(s) are present in dissolved form in the composition.
  • composition may comprise water in the following amounts:
  • Range 30 to 98 or 40 to 95 or 50 to 90 wt.%
  • the ratio of acyl-N-methylglucamide(s) to water is typically at least 0.1 / 100, or at least 0.3 / 100, or at least 0.5 / 100 with respect to weight.
  • the ratio of the acyl-N-methylglucamide(s) to water can be in a range of 0.1 / 100 to 10 / 100, or in a range 0.3 / 100 to 8 / 100, or in a range of 0.5 / 100 to 5 / 100 with respect to weight.
  • acyl-N-methylglucamide(s) may be used and applied together with carrier component(s).
  • the oral care composition may also comprise one or more carrier components.
  • the nature and structure of the carrier component is not particularly limited, unless the desired result cannot be achieved.
  • Carrier components may help to adjust the rheological properties of the composition.
  • Suitable carrier components are gel-forming components, paste-forming components or film-forming components.
  • gel-forming or paste-forming components include Irish moss, carboxymethyl cellulose, gum tragacanth, gum arabic, gum Karaya, sodium alginate, hydroxyethyl cellulose, methyl and ethyl cellulose, carrageenan, xanthan gum, polyvinyl pyrrolidone, and mixtures thereof.
  • Film formers or film forming agents can be classified as natural film former, semi synthetic film formers, cellulose derivatives, poly(meth)acrylates and vinyl polymers.
  • Examples of natural film forming components include shellac, mastix, sandarac, tolubalsam, dammar resin, benzoe resin, keratin, maizin, gum Arabic and gelatines.
  • semi -synthetic film forming components examples include gelatines treated with formaldehyde and salol (acetaldehyde phenol condensate).
  • Typical cellulose derivatives include cellulose acetate phthalate, hydroxyethylcellulose, hydroxypropylcellulose, methylcellulose, ethylcellulose and hydroxypropylmethyl cellulose phthalate.
  • poly(meth)acrylates examples include copolymers of (meth)acrylic esters and amino functional (meth)acrylates, copolymers of (meth)acrylic acid and methyl methacrylate, polyacrylamide, polyacrylic acid and salts thereof, in particular partial salts thereof, including sodium salts.
  • vinyl polymers include polyvinyl pyrrolidon, polyvinyl acetate phthalate (e.g. hydroxypropyl- and hydroxypropyl-methylcellulose), homo- and copolymers of polyvinylacetate, homo- and copolymers of polyvinylpropionate, styrene acrylics, ethylene vinyl acetate, poly(hydroxyethyl methacrylate, poly(vinylethylene glycol acrylate, polyvinyl alcohol(s).
  • polyvinyl pyrrolidon polyvinyl acetate phthalate (e.g. hydroxypropyl- and hydroxypropyl-methylcellulose), homo- and copolymers of polyvinylacetate, homo- and copolymers of polyvinylpropionate, styrene acrylics, ethylene vinyl acetate, poly(hydroxyethyl methacrylate, poly(vinylethylene glycol acrylate, polyvinyl alcohol(s).
  • film forming component(s) include (e.g. fully or partially hydrolyzed) polyvinylalcohol,, polymethylvinylether, polyvinylpyrrolidone, (e.g. aqueous) acrylic resin dispersions (e.g. EudragitTM, commercially available from Rohm), gelatine, polysaccharides (e.g. agarose), polyacrylamide, copolymers of vinylpyrrolidinone and acrylamide, hydrophilic cellulose derivatives (e.g.
  • hydroxyethylcellulose hydroxypropylcellulose, methylcellulose
  • homo- and copolymers of polyvinylacetate homo- and copolymers of polyvinylpropionate, styrene acrylics, ethylene vinyl acetate, polyurethanes, hydroxylated acrylates such as poly(hydroxyethyl methacrylate), poly(vinylethylene glycol acrylate), and combinations and mixtures thereof.
  • composition described in the present text may also comprise abrasive particles.
  • abrasive particles examples include perlite, bentonite, silica, alumina, aluminium hydroxide, ilmenite (FeTiCh), zircon oxide, zircon silicate, calcium carbonate, sodium bicarbonate, titanium dioxide, precipitated lime, chalk, flour of pumice, zeolites, talcum, kaolin, kieselguhr, aluminium oxide, silicates and mixtures thereof.
  • the carrier component is typically present in the following amount(s):
  • acyl-N-methylglucamide(s) may be used and applied together with certain amino acid(s).
  • the oral care composition described in the present text for use in a method or therapy of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm of a living human or animal being may also comprise one or more amino acids.
  • amino acids were found to be useful for achieving the desired results: glycine, leucine, isoleucine, lysine, methionine, phenylalanine, serine, threonine, valine, tryptophan and mixtures thereof, with the following amino acids being sometimes preferred: glycine, phenylalanine, serine, isoleucine, leucine, methionine, with glycine and phenylalanine being sometimes being even more preferred.
  • the amino acids may be natural or synthetic.
  • amino acids might be in D- or L-configuration, wherein the L-configuration is preferred.
  • the composition described in the present text does typically not contain these amino acids in an effective amount, e.g. more than 0.5 or more than 0.3 or more than 0.1 wt.%.
  • amino acids selected from glycine, leucine, isoleucine, lysine, methionine, phenylalanine, serine, threonine, valine, tryptophan and mixtures thereof are present in an amount sufficient for achieving the desired result.
  • the amino acids contained in the oral care composition are used in a therapeutically effective amount being sufficient to influence the lactic acid release metabolism of lactic acid releasing bacteria in an oral biofilm.
  • composition and the amino acids contained therein are used for a time period being sufficient to influence the lactic acid release metabolism of lactic acid releasing bacteria in an oral biofilm.
  • composition and the amino acids contained therein are typically present in an amount and applied for a time period effective to reduce the lactic acid release of lactic acid producing bacteria by more than 40% or more than 45% compared to the situation before the oral care composition described in the present text was used.
  • amino acids are typically present in the following amounts:
  • Range 0.1 to 15 or 1 to 12 or 2 to 10 wt.%;
  • glycine in an amount of 0.1 to 10 wt.%; or
  • leucine in an amount of 0.1 to 5 wt.%; or
  • isoleucine in an amount of 0.1 to 5 wt.%; or
  • lysine in an amount of 0.1 to 10 wt.%; or
  • methionine in an amount of 0.1 to 10 wt.%; or
  • phenylalanine in an amount of 0.1 to 5 wt.%; or
  • threonine in an amount of 0.1 tolO wt.%; or
  • valine in an amount of 0.1 to 8 wt.%; or
  • tryptophan in an amount of 0.1 to 2 wt.%
  • glycine in an amount of 1 to 10 wt.%; or
  • lysine in an amount of 5 to 10 wt.%;
  • phenylalanine in an amount of 1 to 5 wt.%;
  • tryptophan in an amount of 0.5 to 2 wt.%; wt.% with respect to the whole composition.
  • the ratio of amino acid to water is typically at least 0.1 / 100, or at least 1.5 / 100, or at least 2 / 100 with respect to weight.
  • the ratio of amino acid to water can be in a range of 0.1 / 100 to 15 / 100, or in a range / 1.5 to 100 to 12 / 100, or in a range of 2 to 100 to 10 to 100 with respect to weight.
  • the ratio of the acyl-N-methylglucamide(s) to amino acid is typically at least 1 / 0.5 or at least 1 / 1 or at least 1 / 2.
  • the ratio of the acyl-N-methylglucamide(s) to amino acid can be in a range of 1 / 0.5 to 0.1 / 5, or in a range 1 / 1 to 1 / 5, or in a range of 1 / 2 to 1 / 5 with respect to weight.
  • the acyl-N-methylglucamide(s) may be used and applied together with additive(s).
  • the oral care composition described in the present text may also comprise additive(s).
  • One or more additives can be present, if desired.
  • additive(s) are typically present in the following amount(s):
  • Range 0.01 to 10 or 0.1 to 8 or 0.5 to 6 wt.%;
  • Additive(s) which might be present include stabilizer(s), fluoride releasing agent(s), colourant(s), phosphate releasing agent(s), calcium releasing agent(s), anti microbial agent(s), buffer(s), surfactant(s), humectant(s), preservative agent(s), flavour additive(s) and mixtures thereof.
  • the composition might contain one or more stabilize ⁇ s) as an additive.
  • the storage stability of the dental composition might be improved. That is, the individual components of the composition do not separate over time.
  • a composition is defined as storage-stable, if the components do not separate from each other within 6 months or 12 months or 24 months or 36 months at ambient conditions.
  • a stabilizer is present, it is typically, present in a low amount.
  • Amounts, found to be useful, include 0.001 to 5 wt.% or 0.01 to 3 wt.% or 0.1 to 1 wt.% with respect to the weight of the whole composition. Typical ranges include from 0.01 wt.% to 5 wt.% or from 0.1 wt.% to 3 wt.% with respect to the whole composition.
  • stabilizer(s) examples include copolymers of 2,5-furandione with l,9-decadiene and methoxyethene (e.g. StabilizeTM, International Specialty Products (ISP) Comp.) and carboxy vinyl polymers (e.g. CarbopolTM, Lubrizol Advanced Materials Comp.).
  • Stabilizers typically have a mean particle size below 500 pm or below 250 pm or below 100 pm.
  • the composition can comprise one or more fluoride releasing agents as an additive.
  • Typical ranges include 0.01 wt.% to 5 wt.% or 0.1 wt.% to 3 wt.% with respect to the whole composition.
  • fluoride releasing agents include sodium fluoride, potassium fluoride, stannous fluoride, N,N,N’ -Tris(2-hydroxyethyl)-N’ -octadecyl- 1 ,3-diaminopropan- dihydrofluorid (amine fluoride), sodium monofluorophosphate and mixtures thereof.
  • the composition comprises one or more colourants.
  • a colourant may allow an easy detection in a patient's mouth (especially compared to oral tissue and/or tooth substance) and control whether after the treatment all residues of the composition have been removed.
  • a blue, green or violet colour may be suitable.
  • Colouring of the dental composition can be achieved by incorporating colorants or pigments (organic and inorganic) into the composition.
  • colourants include red iron oxide 3395, BayferroxTM 920 Z Yellow, NeazoponTM Blue 807 (copper phthalocyanine-based dye) or Helio Fast Yellow ER and mixtures thereof.
  • the composition comprises one or more phosphate releasing agent(s) as an additive.
  • Typical ranges include 0.01 wt.% to 5 wt.% or 0.1 wt.% to 3 wt.% with respect to the whole composition.
  • phosphate and/or calcium releasing agent(s) examples include calcium pyrophosphate, calcium carbonate, dicalcium phosphate dehydrate, amorphous calcium phosphate, casein phosphopeptide, calcium sodium phosphosilicate, trimetaphosphate, and mixtures thereof.
  • composition comprises anti-microbial agent(s).
  • Typical ranges include 0.01 wt.% to 2 wt.% or 0.1 wt.% to 1 wt.% with respect to the whole composition.
  • an anti-microbial agent might help reducing health risks for professionals in the dental offices and laboratories as well as for patients.
  • ETseful anti-microbial agents include chlorhexidine or derivatives thereof and aldehydes (glutaraldyde, phthalaldehyde) and chlorhexidine or its derivatives and salts of phenolics or acids. It can also be preferred to use acid adducts of chlorhexidine or its derivatives like e.g., acetates, gluconates, chlorides, nitrates, sulphates or carbonates.
  • Chlorhexidine and its derivatives are commercially available in water-based solutions (e.g. a 20 % aqueous solution of CHX di gluconate, CAS 18472-51-0) or as a pure compound or as a salt.
  • water-based solutions e.g. a 20 % aqueous solution of CHX di gluconate, CAS 18472-51-0
  • pure Chlorohexidine compound CAS 55-56-1
  • CHX salts like CHX diacetate monohydrate (CAS 56-95-1) or CHX dihydrochloride (CAS 3697-42-5) are preferred.
  • CHX also seems to be especially suited as an additive due in part to its well-known and proven anti-microbial action against Gram-positive and Gram-negative microorganisms including the oral Streptococci and Lactobacilli.
  • CHX is bacteriostatic for Mycobaterium.
  • CHX is also active against yeasts including Candida albicans and viruses including HIV, HBV, HCV, Influenza- and Herpes virus.
  • a further advantage of CHX is its low toxicity.
  • Preferred anti-microbial agents include hexitidin, cetypyridiniumcloride (CPC), chlorhexidin (CHX), triclosan, stannous chloride, benzalkonium chloride, non-ionic or ionic surfactants (e.g. quaternary ammonium compounds), alcohols [monomeric, polymeric, mono-alcohols, poly-alcohols (e. g. xylitol, sorbitol), aromatic (e. g. phenol)], antimicrobial peptides (e. g. histatins), bactericins (e. g. nisin), antibiotics (e. g. tetracycline), aldehydes (e.
  • inorganic and organic acids e. g. benzoic acid, salicylic acid, fatty acids
  • derivative of such acids such as esters (e. g. p-hydroxy benzoate or other parabenes, laurizcidin), enzymes (e. g. lysozyme, oxidases), proteins (e. g. enamel matrix protein, proline rich proteins), fluoride, EDTA, essential oils (e. g. thymol).
  • composition can comprise one or more buffer(s) as an additive.
  • Typical ranges include 0.1 wt.% to 5 wt.% or 1 wt.% to 3 wt.% with respect to the whole composition.
  • buffers examples include acetic acid/acetate, tris(hydroxy- methyl)aminomethane (TRIS), N-(2-acetamido)-2-aminoethane sulfonic acid (ACES), N- (2-acetamido)imminodiacetate (ADA), N,N-bis(2-hydroxyethyl)-2-aminoethane sulfonic acid (BES), 2,2-bis-(hydroxyethyl)-iminotris(hydroxylmethyl)methane (BIS-TRIS), 2- (cyclohexylamino)ethane sulfonic acid (CHES), 2-[4-(2-hy droxy ethyl- 1- piperazine)]ethane sulfonic acid (HEPES), 3-[4-(2-hydroxyethyl-l-piperazinyl)]propane sulfonic acid (HEPPS), 2-morpholinoethane sulfonic acid (TRIS), N-(
  • the dental composition comprises one or more surfactant(s) as an additive.
  • Typical ranges include 0.01 wt.% to 5 wt.% or 0.1 wt.% to 3 wt.% with respect to the whole composition.
  • surfactant(s) which can be used include water-soluble salts of alkyl sulphates and alkyl ether sulphates having 8 to 18 carbon atoms in the alkyl moiety, water-soluble salts of sulfonated monoglycerides of fatty acids having 8 to 18 carbon atoms in the alkyl radical and mixtures thereof. More specific examples include sodium lauryl sulphate and sodium coconut monoglyceride sulfonates.
  • composition might contain one or more humectant(s) as an additive.
  • humectant(s) which can be used include glycerine, sorbitol, mannitol, xylitol, propylene glycol, polyethylene glycol and mixtures thereof.
  • preservative agent(s) examples include sodium benzoate, citric acid and its salts, and combinations thereof.
  • flavour additive(s) examples include peppermint, spearmint, and combinations thereof.
  • the composition comprises:
  • Component A (acyl-N-methylglucamide) in an amount of 0.1 to 10 wt.%;
  • Component B (water) in an amount of 30 to 98 wt.%;
  • Component C (carrier component) in an amount of 0 to 50 wt.%;
  • Component D (amino acid) in an amount of 0 to 15 wt.%
  • Component E additive in an amount of 0 to 10 wt.%
  • the composition comprises:
  • Component A (acyl-N-methylglucamide) in an amount of 0.1 to 10 wt.%;
  • Component B (water) in an amount of 30 to 98 wt.%;
  • Component C (carrier component) in an amount of 1 to 50 wt.%;
  • Component D (amino acid) in an amount of 0 to 15 wt.%
  • Component E additive in an amount of 0 to 10 wt.%
  • the composition comprises:
  • Component A (acyl-N-methylglucamide) in an amount of 0.1 to 10 wt.%;
  • Component B (water) in an amount of 30 to 98 wt.%;
  • Component C (carrier component) in an amount of 1 to 50 wt.%;
  • Component D (amino acid) in an amount of 0.1 to 15 wt.%;
  • Component E additive in an amount of 0.1 to 10 wt.%
  • the composition typically has a pH value in the range of 6 to 8. Thus, the composition is essentially neutral.
  • the composition can also be characterized by its viscosity. Depending on its chemical formulation, the viscosity may vary over a huge range.
  • the viscosity is typically in a range of 1 to 10 mPa*s or 1 to 1,000 mPa*s at 23 °C.
  • the viscosity is typically in a range of 2,000 to 200,000 mPa*s at 23°C.
  • the viscosity of liquids can be measured using a Physica MCR 301 Rheometer (Anton Paar, Graz, Austria) with a cone/plate geometry CP25-1 under controlled shear rate at 23 °C (e.g. 100 s 1 ). The diameter is 25 mm, the cone angle 1°, and the separation between the cone tip and the plate 49 pm.
  • the viscosity of pastes can be determined using a Physica MCR 301 Rheometer (Anton Paar, Graz, Austria) with a plate/plate geometry (PP15) at a constant shear rate of 1 s 1 in rotation at 28 °C.
  • the diameter of the plates is 10 mm and the gap between the plates is set to 2.0 mm.
  • composition described in the present text can typically be produced as follows:
  • Acyl-N-methylglucamide is provided and mixed with water, the optional carrier component(s), amino acid(s) and the optional additive(s).
  • the mixing is done by dissolving or dispersing the amino acid(s) in the carrier component(s) and additive(s), if desired, with the aid of a mixing device.
  • the mixing can be accomplished shortly before the use of the oral care composition or the oral care composition can already be provided in a mixed and storage stable form.
  • the present invention is also directed to a kit of parts for use in a method or therapy of treating caries by reducing the caries activity or reducing the lactic acid release in an oral biofilm.
  • the kit of parts typically comprises
  • Part A comprising the acyl-N-methylglucamide(s)
  • Part B comprising water for dissolving or dispersing the acyl-N-methylglucamide(s), optionally in combination with a carrier component
  • Part C comprising an application device.
  • the other components such as amino acid(s), carrier component(s) or additive(s) as described in the present text can be present in Part A or Part B or Part A and Part B, as desired.
  • Providing the components of the composition in separated parts can be beneficial to improve the storage stability.
  • the practitioner Before use, the practitioner will prepare the oral care composition by combining the respective components of the individual parts.
  • the application of the oral care composition can be done by various means and/or using various devices.
  • Possible application devices include cups, sponges, brushes, dental trays, syringes, mouth guards, and clear tray aligners.
  • Clear tray aligners can straighten a dental patient’s teeth without the need for using wires and brackets of traditional braces.
  • the aligners typically consist of a sequence of clear, removable trays that fit over the teeth to straighten them.
  • composition or kit of parts described in the present text in combination with a dental tray, mouth guard or clear tray aligner can be advantageous, as these kinds of devices are typically worn for a longer period of time (e.g. 10 min to 12 hrs) and thus are well suited for applying the oral care composition described in the present text for a longer period of time, if desired.
  • compositions described in the present text for use of the composition described in the present text in combination with a dental tray, mouth guard or clear tray aligner, providing the composition in the form of a paste or gel was found to be advantageous.
  • the oral care composition described in the present text is typically packaged in a suitable packaging device.
  • the size and shape of the packaging device typically depends on the form how the composition is provided. Suitable packaging devices include sealable bottles, tubes, vessels or foil bags (including glass or plastic bottles, e.g. equipped with a screw cap), blisters, syringes, etc.
  • the packaging device might be designed for single-use or repeated use.
  • the acyl-N-methylglucamide is used for producing an oral care composition or a kit of parts for a particular use as described in the present text.
  • the acyl-N-methylglucamide is used as an agent effective to reduce the lactic acid release of lactic acid producing bacteria in an oral biofilm.
  • the oral care composition or kit of parts described in the present text is designed or intended for use in a method or therapy of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm of a living human or animal being.
  • composition described in the present text may be provided in different forms or shapes.
  • the composition is provided as liquid, e.g. in the form of an oral rinse or a mouth wash.
  • the composition is provided as gel.
  • the composition is provided as paste, e.g. in the form of a tooth paste.
  • the composition is provided as gum, e.g. in the form of a chewing gum.
  • the composition For reducing the lactic acid release of lactic-acid releasing bacteria in an oral biofilm, the composition has to be brought in contact with the biofilm.
  • the oral biofilm is typically located on tooth surfaces, in particular hard dental tissue.
  • the bringing into contact can be achieved by different means, including rinsing, spraying, brushing, swabbing, coating or combinations thereof.
  • the bringing into contact is typically done for a time period being sufficient for causing the desired effect.
  • the bringing into contact is typically done for a duration of at least 1 min or of at least 2 min or at least 3 min or at least 4 min.
  • the step of bringing into contact can be repeated several times.
  • the oral care composition is applied in periodic application scheme.
  • Possible daily repeating schemes for a periodic application scheme are:
  • the oral care composition is applied in a continuous application scheme.
  • All components used in the dental composition of the invention should be sufficiently biocompatible, that is, the composition should not produce a toxic, injurious, or immunological response in living tissue.
  • composition described in the present text does typically not comprise the following components alone or in combination:
  • compositions described in the present text are essentially free of abrasive particles, in particular free of the abrasive particles described in the text above.
  • Essentially free means less than 1 or less than 0.5 or less than 0.1 wt.% or do not contain abrasive particles at all. Common to most of these substances is typically a comparable high hardness, e.g. above about Mohs 4 or above about 5.
  • compositions described in the present text are essentially free of oxidizing component(s) (e.g. less than 0.5 or less than 0.3 or less than 0.1 wt.%) or do not contain oxidizing components at all.
  • Oxidizing component(s) which are typically not present are peroxide, hypochlorite, perborate, persulfate, peroxyphosphate, peroxycarbonate.
  • oxidizing components have a negative effect in that they may react with the amino acids being present in the composition having the result that the reaction products are no longer suitable for acting as a metabolism modifying agent.
  • compositions described in the present text are essentially free of heavy metal component(s), in particular those comprising Zn or Cu (e.g. less than 0.1 or less than 0.05 or less than 0.01 wt.%) or do not contain heavy metal component(s) at all.
  • compositions described in the present text are essentially free of acidic substances such as carboxylic or phosphoric acid components.
  • heavy metal components may have a negative effect, too, in that they may react with the amino acids being present in the composition (e.g. by forming insoluble complexes) having the result that the reaction products are no longer suitable for acting as a metabolism modifying agent.
  • Embodiment 1 An oral care composition for use in a method of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a living human or animal, the composition comprising
  • acyl-N-methylglucamide in an amount of at least 0.1 wt.%, preferably of 0.1 to 10 wt.%,
  • composition having a pH in the range of 6 to 8.
  • compositions for use in a method of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a living human or animal being, the composition comprising
  • acyl-N-methylglucamide in an amount of at least 0.1 wt.%, preferably of 0.1 to 10 wt.%,
  • the ratio of acyl-N-methylglucamide to water being in a range of 0.1 : 100 to 10: 100 with respect to weight
  • composition having a pH in the range of 6-8,
  • An oral care composition for use in a method of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a living human or animal being, the composition comprising acyl-N-methylglucamide in an amount of at least 0.1 wt.%, preferably of 0.1 to 10 wt.%,
  • the ratio of acyl-N-methylglucamide to water being in a range of 0.1 : 100 to 10: 100 with respect to weight
  • composition having a pH in the range of 6-8 and
  • compositions for use in a method of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a living human or animal being, the composition comprising
  • acyl-N-methylglucamide in an amount of at least 0.1 wt.%, preferably of 0.1 to 10 wt.%,
  • amino acid(s) selected from glycine, leucine, isoleucine, lysine, methionine, phenylalanine, serine, threonine, valine, tryptophan and mixtures thereof, preferably in an amount of 0.1 to 15 wt.%,
  • the method of reducing the lactic acid release comprising the step of applying the composition to the oral biofilm for at least 1 min,
  • An oral care composition for use in a method of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a living human or animal, the composition comprising acyl-N-methylglucamide in an amount of at least 0.1 wt.%, and
  • composition having a pH in the range of 6 to 8,
  • the method of treating caries by reducing the lactic acid release comprising the steps of applying the composition to the oral biofilm according to either of the following application schemes:
  • compositions for use in a method of treating caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a living human or animal, the composition comprising
  • acyl-N-methylglucamide in an amount of at least 0.1 wt.%
  • glycine in an amount of 0.1 to 10 wt.%; or
  • leucine in an amount of 0.1 to 5 wt.%; or
  • isoleucine in an amount of 0.1 to 5 wt.%; or
  • lysine in an amount of 0.1 to 10 wt.%; or
  • methionine in an amount of 0.1 to 10 wt.%; or
  • phenylalanine in an amount of 0.1 to 5 wt.%; or
  • threonine in an amount of 0.1 tolO wt.%; or
  • valine in an amount of 0.1 to 8 wt.%; or
  • tryptophan in an amount of 0.1 to 2 wt.%; or
  • composition having a pH in the range of 6 to 8,
  • the method of treating caries by reducing the lactic acid release comprising the steps of applying the composition to the oral biofilm with the aid of an application device selected from a dental tray, mouth guard or clear tray aligner,
  • compositions can be used in a method or therapy described in the present text.
  • TSx Treatment Solutions
  • the Treatment Solutions (TSx) had the following composition:
  • the MCM media containing alkylmethylglucamides had the following composition:
  • the accumulation of lactic acid in the supernatant (0.75 ml PBS-solution with 5% sucrose per each biofilm sample disc) was measured by using the Lactic acid dehydrogenase (LDH)- Nicotinamid- adenin-dinukleotid (NAD)- Phenazine Methosulphate (PMS) - Thiazolyl blue tetrazolium bromide(MTT) - enzyme assay.
  • LDH Lactic acid dehydrogenase
  • NAD Nicotinamid- adenin-dinukleotid
  • PMS Phenazine Methosulphate
  • the biofilm samples were washed (in three steps, each lasting 30 sec) in 1.5 ml PBS-solution. After 30 min the accumulated amount of lactic acid in the supernatant was measured by analyzing 50 m ⁇ of the supernatant.
  • the lactic acid was quantified by the lactic acid specific enzyme assay described above. Known correlation between measured enzyme activity and amount of lactic acid was used to translate measured enzyme activity into the amount of lactic acid present in sample of the supernatant.
  • the mass of biofilm was determined as follows: Filter papers were put into 1.5 ml- reaction tubes and weighted. The biofilm, that was grown on the enamel disks was carefully wiped off with the pre-weighted filter papers. The filter papers containing the wet biofilms were placed back into the respective reaction tube and re-weighted. The wet biomass is calculated from the difference in weight.
  • Biofilms were grown in a MCM (mucine containing medium containing 1 % sucrose) human derived saliva biofilm system.
  • Exposure Procedure 1 is summarized as follows:
  • Bovine sample disks are incubated in a 24 well plate containing 1.8 ml medium in an incubator at 37°C and 60 rpm circular movement. Medium and/ or treatment solutions were added by pipetting and removed by a suction pump.
  • Bovine sample disks are incubated in a 24 well plate containing 1.8 ml medium in an incubator at 37°C and 60 rpm circular movement. Medium and/or treatment solutions were added by pipetting and removed by a suction pump.
  • Example 1 Human saliva derived biofilm model show reduction in lactic acid release by
  • the biofilms were grown in continuous presence of sucrose and were treated 4 times within 50 h with water and 2% MEGA-9 in water respectively, in accordance to Exposure Procedure 1.
  • Table 4 results of Exposure Procedure 1, 4 treatments within 50 h.
  • Example 2 Human saliva derived biofilm model show reduction in lactic acid release by
  • the biofilms were grown in continuous presence of sucrose and MEGA 8, 9, 10 and 12, according to Exposure Procedure 2.
  • Table 5 results of exposure procedure 2, continuous exposure.
  • Fig. 1 a scanning electron microscope (SEM) picture of a human saliva derived biofilm is shown. Inter biofilm membrane-like structure for inter biofilm compartmentation is visible.
  • Fig. 2 an SEM picture of a human saliva derived biofilm is shown which has been treated with MEGA-9 according to Exposure Procedure 1. Compared to Fig. 1, the membrane-like structure for inter biofilm compartmentation is clearly different.
  • Fig. 1 and Fig. 2 where obtained with a scanning electron microscope from Zeiss Leo 1530VP using the following conditions: Samples prepared by ethanol-HMDS dehydration, sputtering of samples with Platinum (Voltage 1,2 kV; SE- detector. The scaling factor is 20k).

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Abstract

L'invention concerne un ou plusieurs acyl-N-méthylglucamides et une composition de soin buccal contenant un ou plusieurs acyl-N-méthylglucamides destinés à être utilisé dans un procédé de traitement des caries par réduction de la libération d'acide lactique de bactéries produisant de l'acide lactique dans un biofilm buccal dans la bouche d'un homme ou d'un animal. L'invention concerne également un kit d'éléments destiné à être utilisé dans un procédé de traitement des caries par réduction de la libération d'acide lactique de bactéries produisant de l'acide lactique dans un biofilm buccal, le kit d'éléments comprenant un élément A comprenant certains acyl-N-méthylglucamides ou mélanges de ceux-ci, un élément B comprenant de l'eau, et éventuellement un élément C comprenant un dispositif d'application.
EP19783727.1A 2018-10-18 2019-10-08 Composition de soin buccal contenant de l'acyl-n-méthylglucamide pour le traitement des caries par réduction de la libération d'acide lactique dans des biofilms buccaux Withdrawn EP3866934A1 (fr)

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PCT/IB2019/058572 WO2020079531A1 (fr) 2018-10-18 2019-10-08 Composition de soin buccal contenant de l'acyl-n-méthylglucamide pour le traitement des caries par réduction de la libération d'acide lactique dans des biofilms buccaux

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US8557A (en) 1851-12-02 Railroad-switch
DK136455B (da) 1972-11-20 1977-10-17 Nat Patent Dev Corp Tandplejemiddel.
US4339432A (en) 1979-06-20 1982-07-13 Lever Brothers Company Oral mouthwash containing zinc and glycine
EP0224599A1 (fr) 1985-11-06 1987-06-10 National Patent Development Corporation Solution chimique à utiliser dans le traitement des dents
WO1990004789A1 (fr) 1988-10-17 1990-05-03 Meito Sangyo Kabushiki Kaisha Reactif et procede de diagnostic immunologique des maladies du periodonte
EP0711543B1 (fr) 1994-11-11 2003-02-19 Unilever Plc Compositions orales
EP1124584A1 (fr) 1998-11-06 2001-08-22 Universite De Montreal Solutions bactericides et non bactericides servant a eliminer des films biologiques
SE9901773D0 (sv) 1999-05-17 1999-05-17 Nicklas Stroemberg Förebyggande av karies i tänderna
US20070116831A1 (en) 2005-11-23 2007-05-24 The Coca-Cola Company Dental Composition with High-Potency Sweetener
ATE516794T1 (de) 2006-09-13 2011-08-15 3M Innovative Properties Co Dentalzusammensetzungen mit organogelatoren, produkte und verfahren
JP5453260B2 (ja) 2007-07-25 2014-03-26 スリーエム イノベイティブ プロパティズ カンパニー 被膜形成歯科用組成物及び関連する方法
WO2009014907A1 (fr) 2007-07-25 2009-01-29 3M Innovative Properties Company Composition dentaire thérapeutique et procédés afférents
US9750670B2 (en) 2012-12-19 2017-09-05 Colgate-Palmolive Company Zinc amino acid complex with cysteine
WO2017187421A1 (fr) * 2016-04-28 2017-11-02 The Regents Of The University Of California Compositions pour la gestion de la formation de plaque dentaire
WO2017205230A1 (fr) 2016-05-26 2017-11-30 3M Innovative Properties Company Dentifrices thérapeutiques et procédés et kits associés
EP3478067B1 (fr) * 2016-06-29 2020-06-03 Clariant International Ltd Composition coprenant a glucanamide cyclique pour inhiber des micro-organismes
US11464717B2 (en) * 2017-02-10 2022-10-11 Evonik Operations Gmbh Oral care composition containing at least one biosurfactant and fluoride

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