Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
  • A61K8/41—Amines
  • A61K8/416—Quaternary ammonium compounds
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/46—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
  • A61K8/466—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur containing sulfonic acid derivatives; Salts
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Definitions

• the invention relates to an oral care composition containing certain ammonium alkyl sulfonate or carbonate components.
• the oral care compositions and in particular the ammonium alkyl sulfonate or carbonate components contained therein were found to be effective for treating caries or reducing the risk of getting caries lesions 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.
• 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 organic 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.
• US 5,624,906 (Vermeer) relates to an oral hygiene composition
• a certain amount of a specific aldonamide compound a certain amount of a humectant, a certain amount of a cosurfactant and a certain amount of water.
• the composition is said to have improved foam, viscosity, clarity and taste.
• the composition is for removing, loosening and retarding the further development of plaque and calculus on dental surfaces.
• US 2008/0187500 Al is directed to a solid-state method of producing functionalized moieties.
• the obtained hybrid organic/inorganic system includes a functionalized calcium phosphate and a surfactant.
• the system is intended to improve the remineralization of decalcified enamel, to enhance the occlusion of exposed dentinal tubules and to decrease dentinal hypersensitivity.
• WO 2015/195124 Al (Colgate-Palmolive) describes a dentifrice comprising a zinc-amino acid complex, a soluble phosphate salt and a dentifrice base which includes water. It is described that a composition comprising a certain amount of the zinc -amino acid complex is suitable to reduce or inhibit the formation of biofilms.
• US 2007/0264296 Al (Myntti) describes a solvating system for breakdown of biofilm matrices, removal of biofilms from a surface or both, wherein the system comprises a solution of water, a metal ion sequestering agent and a solvating agent for an extracellular polysaccharide matrix.
• sequestering agent mild acids such as citric acid or lactic acid can be sued.
• the solvating agent can be selected from anionic surfactants, non-ionic surfactants, cationic surfactants and zwitterionic surfactants.
• the metal ion sequestering agent removes the ion which bridges the extracellular polysaccharide matrix and binds the polymer chains together and the solvating agent then surrounds and suspends the unbound polymer.
• the solvating system is said to be particularly useful for use on human tissue which cause chronic conditions such as rhinosinusitis.
• 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.
• Such components should be easy in administering and simple in use.
• the components should be easy to obtain or prepare and reasonable in price of manufacturing or purchase.
• the components should not have undesired side effects like bad taste or being astringent.
• the components of the respective composition should in particular be active if used and/or applied in a permanent treatment.
• the invention features an oral care composition for treating caries or reducing the risk of getting caries, the oral care composition comprising an ammonium alkyl sulfonate or carbonate component and optionally amino acid(s) contained in a solvent and/or carrier, the ammonium alkyl sulfonate or carbonate component being characterized by the following formula: RAS -S SVNiCH jz CHzVA (I) with
• the invention is also related to a kit of parts comprising the oral care composition as described in the present text and claims and an application device.
• Described is also a method of using the ammonium alkyl sulfonate or carbonate component or the kit of parts as described in the present text and claims for the production of an oral care composition.
• a further aspect of the invention is directed to the use of the ammonium alkyl sulfonate or carbonate component in a method for treating caries or reducing the risk of caries, the method comprising the step of bringing the ammonium alkyl sulfonate or carbonate component in contact with an oral biofilm and/or hard dental tissue in the mouth of a living human being or animal as described in the present text and claims.
• the treatment is particular effective if the oral care composition is applied to marginal regions of the hard dental tissue.
• marginal regions of hard dental tissue are interproximal areas of teeth, e.g. the area between two neighbouring teeth, fissures being present on the surface of a tooth, marginal gap between a dental restoration (e.g. dental filling or dental crown) and the tooth substance.
• a dental restoration e.g. dental filling or dental crown
• a “dental or oral care composition” is a composition which is to be used in the dental field 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 dental products have to fulfil certain requirements such as those given in DIN EN ISO 1942:2011-03.
• a “dental surface” or “hard dental 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 produced by bacteria.
• Biofilm is understood as a biofilm or mass of bacteria that grows on surfaces within the mouth.
• biofilm refers to a matrix containing bacteria.
• a biofilm in an oral cavity can include bacteria, epithelial cells, leukocytes, macrophages and further 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 “film forming component” 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 definition of the term “film former” can also be found in DIN 55945 (1999-07-00).
• the term “film former” is often used in varnishes.
• the substance hydroxyethyl methacrylate (HEMA) cannot be regarded as a film former according to this definition.
• a “film” is a thin sheet or strip of a preferably flexible material. A coating of a surface with a material typically results in a film.
• 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 “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). “Critical Micelle Concentration (CMC)” means the concentration of a component above which micelles are spontaneously formed.
• ammonium alkyl sulfonate or carbonate component is abbreviated as AASC component.
• 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.
• “And/or” means one or both.
• the expression component A and/or component B refers to a component A alone, component B alone, or to both component A and component B.
• additive(s) means that the term should include the singular and plural form.
• additive(s) means one additive and more additives (e.g. 2, 3, 4, etc.).
• AASC component also includes a composition containing the AASC component.
• the composition described in the present text provides an effective means for treating caries or reducing the risk of getting caries lesions.
• an in-vitro human saliva derived microcosm biofilm was used to apply the AASC component described in the present text using different treating schemes.
• the AASC component functions either as a biofdm metabolism control agent or as an agent for modifying the structure of the biofdm or as a kind of cell membrane modifying agent. Independent of the mechanism, the AASC component is effective for treating caries or reducing the risk of getting caries lesions.
• the cell membrane modifying agent primarily refers to the cell membrane of the cells of the bacteria forming the biofdm and of the extra-cellular membranes constituting the biofilm.
• the oral care composition described in the present text containing an AASC component as agent for treating caries or reducing the risk of getting caries is designed to move from a plaque formation inhibition composition or dental plaque removal composition or biofdm reducing composition to a composition allowing the control of the metabolic balance on dental plaque.
• the invention shows that the AASC component is effective to accomplish caries activity control in a dental biofdm, i.e. being able to influence the metabolic balance of the dental biofilm.
• the AASC component proposed in the present text is easily available at reasonable costs and not harmful to the patient.
• the AASC component is very effective, if it is used in an amount of the critical micelle concentration or above.
• AASC components may have already been suggested as surfactants in various compositions, however, the particular use and effect which can be obtained by these components as described in the present text has not been suggested before.
• ammonium alkyl sulfonate component (AASC) contained in the oral care composition described in the present text is in particular provided for use in a method or therapy of treating caries or reducing the risk of caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm of a human or animal being.
• the AASC components described in the present text have a zwitter ionic structure.
• Mixtures of AASC components can be used, if desired.
• the AASC component can also be characterized by the following parameters alone or in combination: a) Molecular weight: 180 to 800 g /mol; b) CMC at 20-25 °C: 2 to 350 mM in water.
• AASC component having a molecular weight in the above range was found to be beneficial because it typically allows an easier dissolution of the component in a solvent or carrier material, if desired. It may also help to facilitate the interaction of the AASC component with the cell membranes of the lactic acid reducing bacteria located in a biofilm.
• CMC critical micelle concentration
• the AASC component is typically present in the oral care composition in an amount effective for reducing the lactic acid release of lactic acid releasing bacteria by 50% or more compared to a control composition not containing the AASC component, in particular if the AASC component is used in a permanent application scheme.
• Range 0.5 to 100 mmol or 1 to 50 mmol; with respect to 100 g solvent or carrier component.
• the AASC component is used in combination with water.
• the oral care composition comprises one or more of the AASC components and water.
• Water is used for dissolving the AASC component, at least partially. Water is typically present in an amount sufficient to fully dissolve the AASC component and other optional components being present in the oral care composition.
• the AASC component may be present in the form of micelles.
• An AASC component containing oral care composition may comprise water in the following amounts: Lower limit: at least 5 or at least 10 or at least 20 wt.%;
• the ratio of AASC component to water is typically at least 0.00001 / 100, or at least 0.001 / 100, or at least 0.01 / 100 with respect to weight.
• the ratio of AASC component to water can be in a range of 0.00001 / 100 to 5 / 100, or in a range of 0.001 / 100 to 3 / 100, or in a range of 0.01 / 100 to 2 / 100 with respect to weight.
• the AASC component may also be used in combination with a carrier component.
• the oral care composition may comprise one or more AASC components, one or more carrier components and optionally water.
• 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 AASC component containing composition to support the application and/or to trigger the release of the active agent(s) contained in the composition.
• the carrier component is typically present in the following amount(s):
• Suitable carrier components are gel-forming agents or paste-forming agents.
• gel-forming or paste-forming agents 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.
• the carrier component is a film-forming agent.
• Film-forming agents are suitable to improve adherence of the quaternary ammonium alkyl component(s) contained in the composition descnbed in the present text to hard dental tissue, such as a tooth surface.
• film-forming agent(s) are present, the components contained in the composition described in the present text are typically dissolved or dispersed in the film forming component(s) and form together with the film forming component(s) a film or coating on the surface of hard dental tissue.
• the molecular weight (Mw) of the film-forming agent can vary over a wide range (e.g. 2,000 to 1,200,000 g/mol). Typical ranges include 10,000 to 500,000 or 20,000 to 300,000 g/mol.
• the molecular weight can be determined by GPC technology, using e g. a polystyrene standard.
• the film forming component might not be able to form a sufficiently durable film or coating. Thus, the effect of a delayed release of the AASC component might not be obtained.
• components like 2-hydroxyethyl acrylate (HEMA), which are sometimes classified as film-forming agents, are not suitable as film forming component in the sense of the present text.
• the film caused or produced by the film-forming agent typically has a thickness in a range of 0.5 pm to 100 pm or 10 pm to 50 pm.
• 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.
• natural film-forming agents include shellac, mastix, sandarac, tolubalsam, dammar resin, benzoe resin, keratin, maizin, gum Arabic and gelatines.
• semi-synthetic film-forming agents include gelatines treated with formaldehyde and salol (acetaldehyde phenol condensate).
• Typical cellulose derivatives include cellulose acetate phthalate, hydroxyethylcellulose, hydroxy- propylcellulose, methylcellulose, ethylcellulose and hydroxypropylmethyl cellulose phthalate.
• poly (meth)acry late s 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 ydrolysed , polyvinyl acetate phthalate (e.g. hydroxypropyl- and hydroxypropyl-methylcellulose), homo- and copolymers of poly vinylacetate, homo- and copolymers of polyvinylpropionate, styrene acrylics, ethylene vinyl acetate, poly(hydroxyethyl methacrylate, poly(vinylethylene glycol acrylate, polyvinyl alcohol(s).
• polyvinyl ydrolysed polyvinyl acetate phthalate (e.g. hydroxypropyl- and hydroxypropyl-methylcellulose), homo- and copolymers of poly vinylacetate, homo- and copolymers of polyvinylpropionate, styrene acrylics, ethylene vinyl acetate, poly(hydroxyethyl methacrylate, poly(vinylethylene glycol acrylate, polyvinyl alcohol(s).
• film -forming agent(s) include (e.g. fully or partially ydrolysed) 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.
• film-forming agents which are sometimes preferred include polyvinyl alcohol, gelatine, polyacrylic acid, partially neutralized polyacrylic acid and mixtures thereof.
• a film-forming agent is present, it is typically present in the following amounts:
• Tipper limit utmost 90 or utmost 80 or utmost 70 wt.%;
• the AASC component is used in combination with abrasive particles.
• the oral care composition may comprise one or more AASC components, abrasive particles and optionally carrier component(s) and water.
• abrasive particles which may be present include perlite, bentonite, silica, alumina, aluminium hydroxide, ilmenite (FcTiO,), 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 AASC component is used in combination with certain amino acids.
• the oral care composition comprises one or more AASC components, one or more amino acids, water, optionally carrier component(s) and optionally abrasive particles.
• the amino component(s) are used for modifying the structure of the oral biofilm and thus have an influence on the overall environment where the lactic acid producing bacteria are located.
• the amino acid(s) may have a direct impact on the metabolism of the lactic acid releasing bacteria.
• ammo acids were found to be useful for achieving the desired results: glycine, leucine, isoleucine, 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.
• the amino acids might be in D- or L-configuration, wherein the L-configuration is preferred.
• the following amino acids were found to be not effective for reducing the lactic -acid release of bacteria in a biofilm: proline, arginine, histidine, aspartic acid, glutamine, tyrosine and are therefore not suggested for this particular use.
• the AASC component containing oral care composition described in the present text does typically not contain these amino acids in an effective amount, e.g. more than 0.5 wt.% or more than 0.3 wt.% or more than 0.1 wt.%.
• amino acids selected from glycine, leucine, isoleucine, methionine, phenylalanine, serine, threonine, valine, tryptophan and mixtures thereof may be present in an amount sufficient for achieving the desired result.
• the amino acids contained in the AASC component containing 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.
• the AASC component containing oral care 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.
• the AASC component containing oral care 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% or more than 50% compared to the situation before the oral care composition described in the present text was used.
• a suitable method for determining the effectiveness is described in the example section.
• amino acid(s) selected from glycine, leucine, isoleucine, methionine, phenylalanine, serine, threonine, valine, tryptophan and mixtures thereof are typically present in the following amounts:
• Range 0.1 to 15 or 1 to 12 or 2 to 10 wt.%; wt.% with respect to the whole AASC component containing oral care composition.
• 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 methionine in an amount of 0.1 to 10 wt.%; or phenylalanine in an amount of 0.1 to 5 wt.%; or serine in an amount of 0.1 to 10 wt.%; or threonine in an amount of 0.1 to 10 wt.%; or valine in an amount of 0.1 to 8 wt.%; or tryptophan in an amount of 0.1 to 2 wt.%; wt.% with respect to the whole AASC component containing oral care composition.
• glycine in an amount of 1 to 10 wt.%; or leucine in an amount of 1 to 5 wt.%; or isoleucine in an amount of 2 to 5 wt.%; or methionine in an amount of 2 to 10 wt.%; or phenylalanine in an amount of 1 to 5 wt.%; or serine in an amount of 1 to 10 wt.%; or threonine in an amount of 6 to 10 wt.%; or valine in an amount of 3 to 8 wt.%; or tryptophan in an amount of 0.5 to 2 wt.%; wt.% with respect to the whole AASC component containing oral care composition.
• the ratio of amino acid(s) 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(s) 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 AASC component to amino acid(s) is typically at least 1 / 500 or at least 1 / 100 or at least 1 / 10 with respect to weight. If present, the ratio of AASC component to amino acid(s) can be in a range of 1 / 500 to 1 / 1, or in a range 1 / 100 to 1 / 2, or in a range of 1 / 10 to 1 / 5 with respect to weight.
• the following ratio of amino acid to AASC component was found to be particularly useful: per 1 wt.% amino acid the AASC component is present in an amount of 50 to 200 pMol or 70 to 180 pMol or 90 to 160 pMol.
• AASC component is used in combination with any of the other amino acids mentioned, in particular phenylalanine, serine, isoleucine or methionine.
• the AASC component containing oral care composition described in the present text may also comprise additive(s).
• additive(s) One or more additives can be present, if desired. If present, additive(s) are typically present in the following amount(s):
• Additive(s) which might be present include stabilizer(s), colourant(s), phosphate releasing agent(s), calcium releasing agent(s), anti-microbial agent(s), buffer(s), humectant(s), preservative agent(s), flavour additive(s) and mixtures thereof.
• the composition might contain one or more stabilizer(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 overtime.
• 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 0.01 to 3 wt.% or 0.1 to 1 wt.% with respect to the weight of the whole composition.
• stabilizer(s) examples include copolymers of 2,5-fiirandione with 1,9-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 comprises one or more colourants.
• a colourant there is no need for a colourant to be present at all.
• a colourant is present, it is typically present in an amount of at most 5 wt.% or of at most 3 wt.% or of at most 1 wt.% with respect to the whole composition. Typical ranges include 0.01 wt.% to 5 wt.% or 0.1 wt.% to 3 wt.% with respect to the whole composition.
• 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.
• a phosphate releasing agent there is no need for a phosphate releasing agent to be present at all. If a phosphate releasing agent is present, it is typically present in an amount of at most 5 wt.% or of at most 3 wt.% or of at most 2 wt.% with respect to the whole composition. 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.
• the composition comprises anti-microbial agent(s). However, there is no need for an anti-microbial agent to be present at all.
• an anti-microbial agent it is present, it is typically present in an amount of at most 2 wt.% or of at most
• an anti-microbial agent might help reducing health risks for professionals in the dental offices and laboratories as well as for patients.
• Useful anti-microbial agents include chlorhexidine or derivatives thereof and aldehydes (glutaraldehyde, 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 digluconate, CAS 18472-51-0) or as a pure compound or as a salt.
• water- based solutions e.g. a 20 % aqueous solution of CHX digluconate, 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), arabens dine (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.
• the composition can comprise one or more buffer(s) as an additive. However, there is no need for a buffer to be present at all.
• a buffer is present, it is typically present in an amount of at most 5 wt.% or of at most 3 wt.% or of at most 2 wt.% with respect to the whole composition. 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(hydroxymethyl)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(hydroxyl- methyl)methane (BIS-TRIS), 2-(cyclohexylamino)ethane sulfonic acid (CHES), 2-[4-(2-hydroxyethyl-l- piperazine)] ethane sulfonic acid (HEPES), 3-[4-(2-hydroxyethyl-l-piperazinyl)]propane sulfonic acid (HEPPS), 2-morpholinoethane sulfonic acid (MES), 3-morpholinoethane
• the composition might contain one or more humectant(s) as an additive. However, there is no need for a humectant to be present at all.
• a humectant is present, it is typically present in an amount of at most 5 wt.% or of at most 3 wt.% or of at most 2 wt.% with respect to the whole composition. Typical ranges include 0.01 wt.% to 5 wt.% or 0.1 wt.% to 3 wt.% with respect to the whole composition.
• humectant(s) examples 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.
• an AASC component containing oral care composition comprises: Component A (AASC) in an amount of 0.00001 to 5 wt.%;
• Component B (water) in an amount of 5 to 98 wt.%;
• Component C (carrier component) in an amount of 0 to 90 wt.%
• Component D (amino acid) in an amount of 0 to 15 wt.%
• Component E additive in an amount of 0 to 10 wt.%; wt.% with respect to the whole composition.
• an AASC containing oral care composition comprises:
• Component C (carrier component) in an amount of 1 to 90 wt.%;
• Component D (amino acid) in an amount of 0 to 15 wt.%
• Component E additive in an amount of 0 to 10 wt.%; wt.% with respect to the whole composition.
• an AASC containing oral care composition comprises:
• Component A in an amount of 0.00001 to 5 wt.%;
• Component B (water) in an amount of 5 to 98 wt.%;
• Component C (carrier component) in an amount of 1 to 90 wt.%;
• Component D (amino acid) in an amount of 0.1 to 15 wt.%;
• Component E additive in an amount of 0 to 10 wt.%; wt.% with respect to the whole composition.
• 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.
• the AASC component described in the present text is particularly useful for producing an oral care composition.
• the AASC component containing oral care composition described in the present text can typically be produced as follows:
• the AASC component is provided and mixed with the other components of the oral care composition such as water, the carrier component(s), amino acid(s) and the additive(s), if present.
• the mixing is done by dissolving or dispersing the AASC component in the carrier component(s) and additive(s), if desired, with the aid of a mixing device.
• the mixing can also 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 invention is also directed to a kit of parts for use in a method or therapy of treating or reducing the risk of getting caries.
• the kit of parts typically comprises
• Part A comprising the AASC component described in the present text
• Part B comprising water for dissolving or dispersing the AASC component, optionally in combination with a carrier component, and optionally 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.
• AASC component containing oral care composition described in the present text in combination with a dental tray, mouth guard or clear tray aligner, providing the AASC 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 botles, tubes, vessels or foil bags (including glass or plastic botles, e.g. equipped with a screw cap), blisters, syringes, etc.
• the packaging device might be designed for single-use or repeated use.
• the AASC component can be used and applied in different forms or shapes.
• the AASC component is provided in a liquid, e g. in the form of an oral rinse or a mouth wash.
• the composition is provided as part of a gel.
• the composition is provided as part of a paste, e.g. in the form of a toothpaste.
• the composition is provided as part of a gum, e.g. in the form of a chewing gum.
• the composition is provided in a form which results in a coating after application.
• Such an application typically contains a film forming agent.
• preventive care products where the AASC component described in the present text can be used include prophy pastes, prophy powder, varnishes, coatings, etc.
• the AASC component has to be brought in contact with the oral biofilm or hard dental tissue.
• 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: at least 2-times for 1 to 5 min within 24 hours; at least 3 -times for 1 to 5 min within 24 hours.
• the oral care composition is applied in a continuous or permanent application scheme.
• Possible daily repeating schemes for a continuous application scheme are: at least 1 hour within 24 hours; at least 5 hours within 24 hours.
• AASC component is provided in the form of a gel or varnish to be applied either directly on the surface of the tooth structure or with the help of an application device.
• the AASC component described in the present text is applied to form a coating or fdm which can persist on a tooth surface for at least 1, 2, 3 or 5 or 10 days up to 12 months or even longer.
• the AASC component is applied together with film -forming agent(s). Suitable film-forming agents are described above.
• the AASC component containing oral care composition described in the present text does typically not comprise the following components alone or in combination: oxidizing components in an amount of more than 0.5 wt.%; heavy metal components comprising Zn, Sn or Cu in an amount of more than 0.1 wt.%; fluoride anions in an amount of more than 0.1 wt.%; wt.% with respect to the whole composition.
• composition 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 that the composition does not contain abrasive particles at all. Common to most of these abrasive particles 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 impact 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, Sn or Cu (e.g. less than 0.1 or less than 0.05 or less than 0.01 wt.% heavy metal ions) or do not contain heavy metal component) s) at all.
• heavy metal components may have a negative impact, 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.
• compositions described in the present text are essentially free of fluoride component(s), e.g. they do not contain fluoride ions in an amount of greater than 0.05 or greater than 0.01 wt.% or do not contain fluoride component(s) at all.
• compositions described in the present text are essentially free of organic acids not being amino acids, in particular carboxylic acids, e.g. they do not contain organic acids in an amount of greaterthan 0.05 or greater than 0.01 wt.% or do not contain organic acids at all.
• compositions described in the present text should be sufficiently biocompatible, that is, the composition should not produce a toxic, injurious, or immunological response in living tissue.
• the AASC component described in the present text for use in a method of treating caries or reducing the risk of getting 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 AASC component being applied in combination with water, the AASC component being contained in an amount of at least 0.0001 wt.% with respect to the weight of the whole composition, the composition having a pH in the range of 6 to 8 and having a viscosity of 1 to 1,000 mPa*s at 23°C.
• Embodiment 2 Embodiment 2
• the AASC as described in the present text for use in a method of treating caries or reducing the risk of getting 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 AASC component being applied in combination with water and gel-forming or paste-forming component(s), the ratio of the AASC component to water being in a range of 0.0001: 100 to 5: 100 with respect to weight, the composition having a pH in the range of 6 to 8 and having a viscosity of 2,000 to 20,000 mPa*s at 23°C.
• Embodiment 3 Embodiment 3
• the AASC component as described in the present text for use in a method of treating caries or reducing the risk of getting 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 AASC component being applied in combination with water and amino acid(s), the ratio of the AASC component to water being in a range of 0.0001: 100 to 5:100 with respect to weight, the amino acid(s) being selected from glycine, leucine, isoleucine, methionine, phenylalanine, serine, threonine, valine, tryptophan and mixtures thereof, the method of treating caries or reducing the risk of getting caries by reducing the lactic acid release comprising the step of applying the composition being applied to the oral biofilm for at least 1 min.
• the AASC as described in the present text for use in a method of treating caries or reducing the risk of getting 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 AASC component being applied in combination with water, the ratio of the AASC component to water being in a range of 0.0001: 100 to 5:100 with respect to weight, the composition having a pH in the range of 6 to 8, the method of treating caries or reducing the risk of getting caries by reducing the lactic acid release comprising the steps of applying AASC to the oral biofilm and/or hard dental tissue according to either of the following application schemes: at least 2 times for at least ! min within 24 hours, for at least 1 hour within 24 hours, or for at least 2 days.
• the AASC component as described in the present text for use in a method of treating caries or reducing the risk of getting 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 AASC component being applied in combination with water and amino acid(s), the ratio of the AASC component to water being in a range of 0.0001: 100 to 5:100 with respect to weight, the amino acid being selected from 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 methionine in an amount of 0.1 to 10 wt.%; or phenylalanine in an amount of 0.1 to 5 wt.%; or serine in an amount of 0.1 to 10 wt.%; or threonine in an amount of 0.1 tolO wt.%; or valine in an amount of
• the AASC component as described in the present text for use in a method of treating caries or reducing the risk of getting 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 AASC component being applied in combination with film-forming, gel-forming or paste-forming component(s), the AASC component being applied to the oral biofilm and/or hard dental tissue for at least 2 days.
• the AASC component as described in the present text for use in a method of treating caries or reducing the risk of getting caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a human being or animal, the AASC component being selected from 3-(N,N-Dimethyloctylammonio)-propane-sulfonate, 3- (Decyldimethylammonio) -propane -sulfonate, 3-(Dodecyldimethylammonio)-propane-sulfonate, 3-(4- Heptyl)phenyl-3-hydroxypropyl)dimethylammomo-propane-sulfonate, Amidosulfobetaine-14,
• the method of treating caries or reducing the risk of getting caries comprising the step of bringing the AASC component into contact with the oral biofilm according to either of the following application schemes: at least 2 times for at least 1 min within 24 hours, or for at least 1 hour within 24 hours, or for at least for 2 days.
• the AASC component as described in the present text for use in a method of treating caries or reducing the risk of getting caries by reducing the lactic acid release of lactic acid producing bacteria in an oral biofilm in the mouth of a human being or animal, the AASC component being applied in combination with water and amino acid(s), the AASC component being selected from 3-(N,N-Dimethyloctylammonio)-propane-sulfonate, 3- (Decyldimethylammonio) -propane -sulfonate, 3-(Dodecyldimethylammonio)-propane-sulfonate, 3-(4- Heptyl)phenyl-3-hydroxypropyl)dimethylammonio-propane-sulfonate, Amidosulfobetaine-14,
• 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)- Nicotmamide-adenine-dinucleotide (NAD)- Phenazine Methosulphate (PMS) - Thiazolyl blue tetrazolium bromide (MTT) - enzyme assay.
• LDH Lactic acid dehydrogenase
• NAD Nicotmamide-adenine-dinucleotide
• PMS Phenazine Methosulphate
• MTT Thiazolyl blue tetrazolium bromide
• biofilm samples were washed (in three steps, each lasting 30 sec) in 1.5 ml PBS-solution.
• 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.
• a compound should lower the lactic acid release in permanent application of at least 50 % in comparison to the untreated biofilm control and should also lower lactic acid release in the periodic application of at least 5 %.
• Negative number indicates that the release of lactic acid was reduced, a positive number indicates that the release of lactic acid was increased.
• the CMC can be determined by light scattering (increases with concentration of component), surface tension (decreases with concentration of component) and dye solubilization (increases with concentration of component).
• a simple dye solubilization method for the determination of CMC involves the solubilization of a dye in a detergent solution only in the presence of micelles.
• the amount of dye is directly proportional to the micelle concentration.
• the CMC is determined by plotting optical density of the solubilized dye against detergent concentration. The points of inflection on the plot of observed data versus detergent concentration corresponds to the CMC of a typical detergent.
• Bovine sample disks of about 10 x 10 mm (+/- 2mm) were incubated in a 24 well plate containing 1.8 ml medium in an incubator at 37°C and 60 rpm circular movement.
• the treatment composition described below were added by pipetting and removed by a suction pump.
• Biofilms were grown in an MCM (mucine containing medium plus 1 % sucrose) human derived saliva bioflm system.
• Fresh medium MCM-1% sucrose
• CMC critical micellar concentration
• Fresh medium (MCM-1% sucrose and Treatment Composition) for storage for about 14h at 37 °C.
• the reduction in the lactic acid release should be at least 50 or at least 60%.
• Bovine sample disks were incubated in a 24 well plate containing 1.8 ml medium in an incubator at 37°C and 60 rpm circular movement.
• the Treatment Compositions described below were added by pipetting and removed by a suction pump.
• Biofilms were grown in a MCM (mucine containing medium plus 1 % sucrose) human derived saliva biofilm system.
• Fresh medium (MCM-1% sucrose) for about 14h at 37 °C.
• Day 2 2 min treatment with Treatment Composition after 24 and 31 hours and fresh medium (MCM-1% sucrose) after 22, 24, 28, and 31 hours.
• Day 3 2 min treatment with Treatment Composition after 48 hours and fresh medium (MCM-1% sucrose) after 46 and 48 hours.
• the reduction in the lactic acid release should be at least 5 or at least 8%.
• TCx Treatment Compositions to be used for the Permanent Exposure Procedure and the Periodic Exposure Procedure were prepared by dissolving the respective AASC components in a liquid carrier medium (water or MCM) in the amounts given below in Table 2.
• MCM liquid carrier medium
• the AASC component was dissolved in MCM.
• the AASC component was dissolved in water.
• Ammonia alkyl sulfonate (AASC) components are effective to lower the lactic acid release from in vitro human saliva microcosm biofdm.

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• 2020
  • 2020-09-23 WO PCT/IB2020/058877 patent/WO2021059151A1/en unknown
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