Oral treatment compositions to promote gum health.

Description

1 / 42 “ORAL CARE COMPOSITIONS TO PROMOTE GUM HEALTH FIELD OF THE INVENTION

[0001] The present invention relates to oral care compositions comprising a source of stannous ions and a taurate surfactant to promote the oral health of a user's gums. In particular, such oral care compositions are useful for controlling plaque bacteria and / or protecting against bacterial / toxin invasion. BACKGROUND OF THE INVENTION

[0002] Dental plaque (also known as dental biofilm) is a sticky, colorless deposit of bacteria that constantly forms on the tooth surface. Dental plaque is generally composed of bacteria and extracellular polymeric substances (EPS). EPS are biopolymers of microbial origin in which biofilm microorganisms are embedded. J. Bacteriol. 2007, 189(22):7945. Saliva, food, and fluids combine to produce these deposits, which accumulate where teeth and gums meet. Plaque buildup is a major factor in poor oral health, which can lead to cavities and periodontal disease (in the gums), including gingivitis.One of the ways in which toothpaste compositions help prevent and control plaque is through the advantageous use of antibacterial agents, for example, stannous ions; however, the disadvantage and challenge of the formulation is the unintentional reactivity of antibacterial agents with formulation ingredients. This can include oxidative degradation, hydrolysis, adsorption, or... Petition 870260022065, dated 10 / 03 / 2026, page 6 / 103 2 / 42 precipitation of oxyhydroxide species, any of which may affect the bioavailability of the antibacterial agent.

[0003] Sodium lauryl sulfate (SLS) is widely used in toothpaste formulations, offering benefits such as broad compatibility with other ingredients, a neutral taste, and good foaming aesthetics. However, there is ongoing consumer interest in the development of oral care products that do not contain sodium lauryl sulfate. One concern has been that SLS may be a potential source of irritation, scaling, and epithelial barrier dysfunction in the gingiva. Having a strong gingival epithelial barrier function means the gingiva acts as a physical barrier separating biofilm from gingival tissue, providing the first line of defense against bacterial invasion in gingivitis or periodontal disease. Stannous fluoride has a bactericidal and bacteriostatic effect on plaque bacteria.It has also been shown to reduce the virulence of bacterial endotoxin biofilms, such as lipopolysaccharide (LPS) and lipoteichoic acid (LTA), which are associated with the initiation of inflammatory processes involved in periodontal disease and the disruption of epithelial barrier function. Brushing with stannous fluoride toothpaste leads to a reduction in gingivitis and, as a result, to the restoration of barrier function, making the gum tissue more resistant to bacterial attack.

[0004] Thus, there is a continuing need to provide enhanced stannous and fluoride-containing products to help control plaque bacteria on teeth and / or protect against bacterial / toxin invasion, which do not contain sodium lauryl sulfate, but nevertheless have Petition 870260022065, dated 10 / 03 / 2026, p. 7 / 103 3 / 42 adequate stability and aesthetics and do not irritate or compromise the gingival epithelium. SUMMARY OF THE INVENTION

[0005] The present invention relates to a composition for oral care, comprising: (a) from 0.01% to 5%, by weight of the composition, of a source of stannous ions; (b) from 0.1% to 5%, by weight of the composition, of a taurate surfactant represented by formula (I): r2 II I R, C—N—CH2—CH2— SO3'M . (I) wherein R1 is a saturated or unsaturated alkyl chain, linear or branched with 6 to 18 C atoms; R2 is H or methyl, and M is H, sodium or potassium; and, (c) from 0.1% to 2%, by weight of the composition, of a zinc ion source, wherein the zinc ion source comprises at least 95% by weight of a soluble or partially soluble zinc ion source.

[0006] Significant disruption and destabilization of dental biofilm can be achieved by means of an aqueous oral care composition comprising a source of stannous ions and a taurate surfactant. An advantage of the present invention is the optimized deep penetration into the biofilm and / or extermination of bacteria. For this purpose, it has surprisingly been found that the depth of penetration and / or the rate of penetration of stannous ion / zinc ion into biofilms can be increased when Petition 870260022065, dated 10 / 03 / 2026, p. 8 / 103 4 / 42 used in combination with taurate. In summary, the synergistic combination of taurate and the stannous ion source in the oral care composition may be such that optimization is achieved in benefiting gum health.

[0007] One advantage of the present invention is to provide effective antibacterial properties by combining taurate surfactant with a source of stannous and zinc ions. A further advantage of the present invention is to provide oral care compositions with improved deposition / penetration of Sn ions into the biofilm, as well as to provide toxin neutralization impacting the healing recovery of the gingival epithelium.

[0008] Another advantage is that the oral care composition is a toothpaste and preferably provides pleasant sensory experiences, such as taste, foam and mouthfeel.

[0009] It is also an additional advantage that the oral care composition exhibits good stability over a wide pH range. Another advantage is that the oral care compositions have physical and chemical stability over a range of manufacturing, handling, and storage conditions. Another advantage is that the oral care compositions have stable product quality (e.g., consistent visual appearance and no discoloration, etc.) even after three months of storage at 40 °C. Another advantage is that the oral care compositions of the present invention minimize the use of antibacterial agents.

[0010] Another additional advantage is that the oral care compositions of the present invention use Petition 870260022065, dated 10 / 03 / 2026, page 9 / 103 5 / 42 taurate to reduce and / or eliminate the instability and / or discoloration problems of conventional tin-containing toothpastes, as described above. It is also an added advantage that the oral care composition of the present invention surprisingly provides an improved sensory profile and / or reduces potential astringency during and after brushing.

[0011] The present invention further encompasses a method for treating dental biofilm comprising the step of brushing teeth with an oral care composition of the present invention.

[0012] The invention further provides a method for preventing or mitigating plaque formation on dental enamel comprising the step of brushing teeth with an oral care composition of the present invention. DETAILED DESCRIPTION OF THE INVENTION Definitions

[0013] For use in the present invention, the indefinite articles "a" and "an," when used in a claim, are understood to mean one or more of the items claimed or described.

[0014] The terms relieve and relieving are used interchangeably and mean to minimize, avoid, delay and / or treat at least one symptom of gum disease to produce a positive change (i.e., a benefit) for the user.

[0015] The term biofilms for use in the present invention means a bacterial population embedded in a matrix that adheres to each other and / or to surfaces or interfaces in the oral cavity. Petition 870260022065, dated 10 / 03 / 2026, page 10 / 103 6 / 42

[0016] The term comprising, as used herein, means that steps and ingredients beyond those specifically mentioned may be added. This term encompasses the terms consisting of and essentially consisting of. The compositions of the present invention may comprise, consist of, and essentially consist of the essential elements and limitations of the invention described herein, as well as any of the additional or optional ingredients, components, steps, or limitations described herein.

[0017] The term oral care composition or oral care compositions for use in the present invention refers to a product that, in its normal use, is retained in the oral cavity for a sufficient time to come into contact with some or all of the dental surfaces and / or oral tissues for purposes of oral activity. In one example, the composition provides a gum care benefit when used in the oral cavity. The oral care composition of the present invention may be in various forms, including toothpaste, dentifrice, dental gel, dental powders, tablets, mouthwash, mouth rinse, subgingival gel, foam, mousse, chewing gum, lipstick, sponge, dental floss, prophylactic paste, petrolatum gel, denture adhesive or denture product. In one example, the oral composition exists in the form of a paste or gel. In another example, the oral composition exists in the form of a dentifrice.The oral composition can also be incorporated into strips or films for direct application or fixation to oral surfaces, or incorporated into dental floss. Petition 870260022065, dated 10 / 03 / 2026, page 11 / 103 7 / 42

[0018] As used in the present invention, the term dentifrice means paste, gel, powder, tablets or liquid formulations, except where otherwise specified, that are used to clean the surfaces of the oral cavity. Preferably, the dentifrice compositions of the present invention are single-phase compositions, although the compositions may be two-phase or multi-phase compositions. An example of a dentifrice composition is toothpaste (for brushing teeth). The term teeth, as used in the present invention, refers to natural teeth as well as artificial teeth or dental prostheses.

[0019] The term partially soluble or partially soluble in water, as used herein, means that a compound has a solubility of 1 g / 1,000 ml or more in water at 25°C. The term insoluble, as used herein, means that a compound has a solubility of less than 0.1 g / 1,000 ml at 25°C.

[0020] The term effective amount, as used in the present invention, refers to an amount of a compound or composition sufficient to induce a positive benefit, or an oral health benefit, and / or an amount low enough to avoid serious side effects, that is, to provide an adequate benefit-risk ratio, within the good judgment of one skilled in the art. In one example, effective amount means at least 0.01% of the material, by weight of the composition, and alternatively, at least 0.1%.

[0021] As used in the present invention, the words preferred, preferably and their variants refer to embodiments of the invention that provide Petition 870260022065, dated 10 / 03 / 2026, p. 12 / 103 8 / 42 certain benefits under certain circumstances. However, other embodiments may also be preferred under the same circumstances or under different circumstances. Furthermore, the mention of one or more preferred embodiments does not imply that other embodiments are not useful and is not intended to exclude other embodiments from the scope of the invention.

[0022] The term substantially free, as used herein, refers to an unintentional amount of that material that is added to the composition or an amount of a material that is less than 0.05%, 0.01% or 0.001% of the composition. The term essentially free of, as used herein, means that the indicated material is not deliberately added to the composition or, preferably, is not present in analytically detectable amounts. This includes compositions in which the indicated material is present only as an impurity of one of the other deliberately added materials. The term free, for use in the present invention, refers to the fact that no reasonably detectable amount of that material is present in the composition.

[0023] The term total water content, as used herein, means both free water and water that is bound by other components in the oral care formulation.

[0024] All percentages, parts and ratios are based on the total weight of the compositions of the present invention, except where otherwise specified. All weights mentioned that refer to ingredients mentioned herein are based on the active content and therefore do not include solvents or by-products that may be included in Petition 870260022065, dated 10 / 03 / 2026, page 13 / 103 9 / 42 commercially available materials, except where otherwise indicated. The term weight percentage may be denoted as % by weight in this document. All molecular weights, as used in this document, are weight-average molecular weights expressed in grams / mol, except where otherwise specified.

[0025] All measurements mentioned in the present invention are made at 25°C (i.e., room temperature) unless otherwise specified. Oral care compositions

[0026] It has been surprisingly discovered that the combination of stannous ion (i.e., an antibacterial agent), a source of soluble or partially soluble zinc ions, and a taurate amino acid-based surfactant in an oral care composition is particularly useful for controlling plaque bacteria and maintaining barrier integrity and function, i.e., promoting gum health benefits for users. In particular, the surprising finding was that the penetration of stannous ion into biofilms is considerably improved when combined with taurate. Without wanting to get bogged down in theory, the surfactant Taurate is derived from an amino acid containing carboxylic and amine groups. Stannous ions are believed to bind strongly to these chemical moieties of the amino acid to positively influence the penetration of stannous ions into biofilms.

[0027] It was also surprisingly discovered that the penetration depth and / or penetration rate of stannous and / or zinc ions into biofilms can be increased, or markedly increased, when formulated Petition 870260022065, dated 10 / 03 / 2026, p. 14 / 103 10 / 42 with taurate surfactant, compared to other anionic surfactants such as SLS. In short, the presence of taurate in combination with a source of stannous ions and a source of soluble or partially soluble zinc ions in an oral care composition aids in the effectiveness of the composition in mediating the harmful effects of bacteria on gingival biofilms.

[0028] In one aspect, the present invention is directed to an oral care composition comprising: (a) from 0.01% to 5%, by weight of the composition, of a source of stannous ions; (b) from 0.1% to 5%, by weight of the composition, of a taurate surfactant represented by formula (I) o r2 II I R,--C—N—CH2—CH2—SOfM. (I) where R1 is a saturated or unsaturated, linear or branched alkyl chain with 6 to 18 carbon atoms; R2 is H or methyl, and M is H, sodium or potassium; and, (c) from 0.1% to 2%, by weight of the composition, of a zinc ion source, wherein the zinc ion source comprises at least 95% by weight of a soluble or partially soluble zinc ion source. Source of stannous ions

[0029] The present invention relates to the oral care compositions mentioned above which comprise, in a preferred example, the source of stannous ions present in Petition 870260022065, dated 10 / 03 / 2026, p. 15 / 103 11 / 42 quantity of 0.01% to 5%, preferably 0.05% to 4%, or more preferably 0.1% to 2%, by weight of the composition, to provide antibacterial efficacy. The stannous ion source used in the present invention may include any safe and effective stannous salt. Suitable examples of stannous ion sources are selected from soluble stannous salts and, preferably, selected from the group consisting of stannous chloride, stannous fluoride, stannous acetate, stannous gluconate, stannous oxalate, stannous sulfate, stannous lactate, stannous tartrate, stannous iodide, stannous chlorofluoride, stannous hexafluorozirconate, stannous citrate, stannous malate, stannous glycinate, stannous carbonate, stannous phosphate, stannous pyrophosphate, stannous metaphosphate and combinations thereof; Preferably, the source of stannous ions is selected from stannous chloride, stannous fluoride, or a combination thereof.

[0030] In a preferred example, the stannous ion source comprises stannous chloride. In another preferred example, the stannous ion source comprises stannous fluoride. In a particularly preferred example, the stannous ion source comprises a combination of stannous fluoride and stannous chloride.

[0031] In some examples, the oral care composition of the present invention is substantially free of stannous oxide from an insoluble stannous ion source, preferably essentially free of stannous oxide, more preferably free of stannous oxide. Petition 870260022065, dated 10 / 03 / 2026, page 16 / 103 12 / 42 Surfactant taurate

[0032] The oral care composition of the present invention contains a taurate surfactant as the main surfactant. Taurate is represented by formula (I): R2 II I Ri--C—N — CH2—CH2— SO3-M+, (I) wherein R1 is a saturated or unsaturated alkyl chain, linear or branched with 6 to 18 C atoms; R2 is H or methyl, and M is H, sodium or potassium.

[0033] Preferably, R1 is a saturated or unsaturated alkyl chain, linear or branched, with 8 to 18 C atoms. Optionally, but preferably, the taurate surfactant of the present invention comprises one or more selected from the group consisting of potassium cocoyl taurate, potassium methyl cocoyl taurate, sodium methyl caproyl taurate, sodium cocoyl taurate, sodium lauroyl taurate, sodium methyl cocoyl taurate, sodium methyl lauroyl taurate, sodium methyl myristoyl taurate, sodium methyl oleoyl taurate, and combinations thereof. Source of soluble or partially soluble zinc ions

[0034] Optionally, but preferably, the oral care composition may additionally comprise 0.1% to 5%, preferably 0.2% to 2%, by weight of the composition, of a zinc ion source, wherein the zinc ion source comprises at least 95% by weight of a Petition 870260022065, dated 10 / 03 / 2026, page 17 / 103 13 / 42 source of soluble or partially soluble zinc ions. In some embodiments, the oral care composition comprises a source of zinc ions consisting of a soluble or partially soluble source of zinc ions.

[0035] Preferably, the source of soluble or partially soluble zinc ions is selected from the group consisting of zinc citrate, zinc chloride, zinc sulfate, zinc gluconate, zinc lactate, and combinations thereof. More preferably, the source of zinc ions is selected from zinc citrate, zinc gluconate, zinc lactate, and combinations thereof.

[0036] However, preferred zinc sources are soluble zinc sources, such as zinc chloride or zinc sulfate. More preferred zinc sources are those where the zinc is already combined with a suitable chelating agent in the form of a salt or other complex, such as zinc citrate, zinc gluconate, zinc lactate, and zinc glycinate. Especially preferred sources of zinc ions are zinc citrate, zinc gluconate, zinc lactate, and mixtures thereof. Preferably, the oral care composition may comprise a soluble zinc ion source of 0.1% to 1.5%, preferably 0.15% to 1%, more preferably 0.2% to 0.55% by weight of the composition.

[0037] Preferably, the oral care composition of the present invention is substantially free of, preferably essentially free of, more preferably free of any insoluble or moderately soluble zinc compounds. Insoluble or moderately soluble zinc compounds, such as zinc oxide, zinc phosphate Petition 870260022065, dated 10 / 03 / 2026, page 18 / 103 14 / 42 or zinc carbonate are not suitable as a source of zinc for the oral composition of the present invention. Fluoride Ion Source

[0038] The compositions may optionally, but preferably, include an effective amount of an anticaries agent as a source of fluoride ions. The fluoride ion may be present in a sufficient amount to result in a fluoride ion concentration in the composition at 25 °C and / or, in one embodiment, may be used in amounts of about 0.0025% to about 5% by weight of the composition, preferably from about 0.005% to about 2.0%, preferably from 0.5% to about 1.5% by weight of the composition, to provide anticaries efficacy. Representative sources of fluoride ions include stannous fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, and zinc fluoride, or mixtures thereof. In one aspect, the oral care compositions of the present invention may have a dual source of fluoride ions, specifically sodium monofluorophosphate and an alkali metal fluoride.Alternatively, the oral care compositions of the present invention may contain a dual fluoride ion source that is a combination of stannous fluoride and sodium fluoride. Without delving into theory, such an approach may provide an improvement in average fluoride absorption.

[0039] In some preferred examples, the source of fluoride ions is selected from stannous fluoride, sodium monofluorophosphate, sodium fluoride, or combinations thereof.

[0040] In one aspect, the oral care composition of the present invention does not contain amine fluoride. Petition 870260022065, dated 10 / 03 / 2026, page 19 / 103 15 / 42 (also called olaflur), regulatory in some regions. Secondary surfactant due to restrictions

[0041] The oral care compositions in this document may include a secondary surfactant, other than the surfactant Taurate. The composition may include a secondary surfactant in a content of about 0.01% to about 10%, about 0.025% to about 9%, about 0.05% to about 5%, about 0.1% to about 2.5%, about 0.5% to about 2%, or about 0.1% to about 1%, by weight, of the composition.

[0042] Preferably, the secondary surfactant is an amphoteric surfactant, for example, selected from the group consisting of betaine surfactants.Non-limiting examples of amphoteric surfactants may be a betaine or a sultaine selected from the group consisting of: almondamidopropyl betaine, apricotamidopropyl betaine, avocadoamidopropyl betaine, babassuamidopropyl betaine, behenamidopropyl betaine, canolamidopropyl betaine, capryl / capramidopropyl betaine, cocoamidopropyl betaine, coco / oleamidopropyl betaine, coco / sunfloweramidopropyl betaine, cupuassuamidopropyl betaine, isostearamidopropyl betaine, lauramidopropyl betaine, meadowfoamamidopropyl betaine, leiteamidopropyl betaine, visãomidopropyl betaine, myristamidopropyl betaine, olivamidopropyl betaine, palmaamidopropyl betaine, palmitamidopropyl betaine, palmamidopropyl betaine, ricinoleamidopropyl betaine, sesame starch propyl betaine, shea butter starch propyl betaine, soy starch propyl betaine, stearamidopropyl betaine. Petition 870260022065, dated 10 / 03 / 2026, page 20 / 103 16 / 42 seboamidopropyl betaine, undecyleneamidopropyl betaine, wheat germamidopropyl betaine, cocamidopropyl hydroxysultain (CAPHS), lauramidopropyl hydroxysultain (LAPHS), oleamidopropyl hydroxysultain (OAPHS), seboamidopropyl hydroxysultain (TAPHS), and combinations thereof, preferably selected from the group consisting of cocamidopropyl betaine, lauramidopropyl betaine, oleamidopropyl betaine, seboamidopropyl betaine, cocamidopropyl hydroxysultain and combinations thereof; and more preferably, selected from cocamidopropyl betaine, lauramidopropyl betaine or a combination thereof.

[0043] In addition, the secondary surfactant may also be a nonionic surfactant or another anionic surfactant other than SLS taurate or sulfate. In some embodiments, the secondary surfactant in the oral care compositions of the present invention may be nonionic surfactants that are, for example, compounds produced by the condensation of alkylene oxide groups (of a hydrophilic nature) with a hydrophobic organic compound that may be aliphatic or alkylaromatic in nature. Examples of suitable nonionic surfactants may include Pluronics® which are poloxamers, alkyl phenol polyethylene oxide condensates, products derived from the condensation of ethylene oxide with the reaction product of propylene oxide and ethylenediamine, aliphatic alcohol ethylene oxide condensates, long-chain tertiary amine oxides, long-chain tertiary phosphine oxides, long-chain dialkyl sulfoxides, and combinations of these materials.Suitable anionic surfactants as the surfactant. Petition 870260022065, dated 10 / 03 / 2026, page 21 / 103 17 / 42 secondary components of the present invention may include sarcosinates, isethionates, alkyl phosphates, etc.

[0044] In alternative embodiments, the composition contains less than 0.05% by weight of any secondary surfactant. In some preferred embodiments, the composition is essentially free of, preferably free of, any secondary surfactant, for example, betaine.

[0045] In one aspect, the composition of the present invention is substantially free of sodium lauryl sulfate (SLS). Preferably, the composition of the present invention is essentially free of, more preferably free of, sodium lauryl sulfate (SLS). Without wanting to get bogged down in theory, such an approach may provide an improvement in the consumer's sensory experience by reducing irritation of the oral tissue. Abrasive containing calcium

[0046] The compositions of the present invention may optionally, and in some respects preferably, comprise from about 5% to about 50%, preferably from about 10% to about 50%, by weight of the composition, of a calcium-containing abrasive, wherein the calcium-containing abrasive is preferably selected from the group consisting of calcium carbonate, calcium glycerophosphate, dicalcium phosphate, tricalcium phosphate, calcium orthophosphate, calcium metaphosphate, calcium polyphosphate, calcium oxyapatite, sodium carbonate and mixtures thereof; wherein the calcium-containing abrasive is more preferably calcium carbonate. Preferably, the composition comprises from about 15% to about 50%, preferably from about 15% to about Petition 870260022065, dated 10 / 03 / 2026, page 22 / 103 18 / 42 of 40%, preferably from about 15% to about 25%, by weight, of the composition, of an abrasive containing calcium.

[0047] Preferably, the abrasive containing calcium is calcium carbonate. More preferably, the abrasive containing calcium is selected from the group consisting of finely ground natural chalk, ground calcium carbonate, precipitated calcium carbonate, and combinations thereof. Some non-limiting examples of the percentages by weight of the calcium-containing abrasive include about 15%, about 20%, about 25%, or about 30% by weight of the composition, preferably wherein the calcium-containing abrasive is calcium carbonate. Silica-based abrasive

[0048] Dental abrasives based on silica, of various types, are preferred due to their unique benefits of exceptional tooth cleaning and polishing performance without undue abrasion of enamel or dentin. The silica-based abrasive polishing materials of the present invention, as well as other abrasives, generally have an average particle size in the range of about 0.1 to about 30 microns, preferably about 5 to about 15 microns. For example, the silica-based abrasives used in the present invention are precipitated silica (e.g., sodium silicate solution by acid destabilization to produce very fine particles), such as those in the ZEODENT® series from Huber Engineered Materials (e.g., ZEODENT® 103, 124, 113, 115, 163, 165, 167). It is recognized that some of these silicas (e.g., synthetic amorphous silica) can perform both thickening and abrasive functions, but they are included in Petition 870260022065, dated 10 / 03 / 2026, page 23 / 103 19 / 42 present invention under the term abrasive for the purposes of the present invention. Preferably, the oral care composition comprises from 1% to 35%, more preferably from 5% to 25%, by weight of the composition, of abrasive. pH

[0049] The pH of the oral care composition may range from about 4.0 to about 9.0, preferably from about 4.3 to about 8.0, more preferably from about 4.6 to about 7.5. In some examples, the composition has a pH ranging from 4.0 to 4.9. In alternative examples, the composition may have a pH ranging from 5.0 to 6.0. In other examples, the composition has a pH ranging from 6.1 to 7.3. In some other examples, the composition may have a pH ranging from 7.5 to 9.0. A method for evaluating the pH of oral care is described below. For clarification purposes, although the analytical method describes testing the oral care composition when freshly prepared, for the purposes of the present invention claim, the pH can be taken at any time during the reasonable life cycle of the product (including, but not limited to, the time when the product is purchased from a store and taken to the user's home). pH modifying agent

[0050] The oral care compositions of the present invention may include an effective amount of a pH modifying agent, wherein, preferably, the pH modifying agent is a pH buffering agent. The pH modifying agents, as used in the present invention, refer to agents that can be used to adjust the pH of the oral care compositions to the pH range identified above. The compositions may comprise Petition 870260022065, dated 10 / 03 / 2026, page 24 / 103 20 / 42 approximately 0.001% to approximately 5%, by weight of the composition, of pH modifying agent. pH modifying agents may include alkali metal hydroxides, ammonium hydroxide, organic ammonium compounds, carbonates, sesquicarbonates, borates, silicates, phosphates, imidazole and mixtures thereof. Specific pH adjusters include monosodium phosphate (monobasic sodium phosphate, or MSP), trisodium phosphate (tribasic sodium phosphate dodecahydrate, or TSP), sodium benzoate, benzoic acid, sodium hydroxide, potassium hydroxide, alkali metal carbonate salts, sodium carbonate, imidazole, pyrophosphate salts, tripolyphosphate salts, sodium gluconate, lactic acid, sodium lactate, citric acid, sodium citrate, and phosphoric acid.Without adhering to theory, phosphate may also have chelating activity for calcium ions and therefore provide some stabilization of monofluorophosphate (in those formulations containing monofluorophosphate).

[0051] A method for evaluating oral care pH is described. pH is measured by a pH meter with an automatic temperature compensation (ATC) probe. The pH meter is capable of reading down to 0.001 pH units. The pH electrode can be selected from one of the following (i) combinations of Orion Ross Sure-Flow: Glass body - VWR #34104-834 / Orion #8172BN or VWR#10010-772 / Orion #8172BNWP; Epoxy body VWR #34104-830 / Orion #8165BN or VWR#10010-770 / Orion #8165BNWP; Semimicro, epoxy body - VWR #34104-837 / Orion #8175BN or VWR#10010-774 / Orion #3175BNWP; or (ii) Orion Perfect combination: VWR #34104-843 / Orion #8203BN semi-micro, Petition 870260022065, dated 10 / 03 / 2026, page 25 / 103 21 / 42 glass body; or (iii) suitable equivalent. The self-temperature compensating probe is a Fisher Scientific, Cat. No. 13-620-16.

[0052] A 25% by weight aqueous oral care paste is prepared with deionized water and then centrifuged for 10 minutes at 15,000 revolutions per minute using a SORVALL RC 28S centrifuge and an SS-34 rotor (or equivalent gravitational force, at 24149g of force). The pH is assessed in the supernatant after one minute, or when the reading stabilizes. After each pH assessment, the electrode is washed with deionized water. Any excess water is wiped off with a laboratory-grade tissue. When not in question, the electrode is kept immersed in a pH 7 buffer solution or an appropriate electrode storage solution. Humectants

[0053] The oral care compositions of the present invention may include humectants present in amounts of 0% to 70% or 15% to 55% by weight of the compositions. Humectants prevent the oral care compositions from hardening upon exposure to air, and certain humectants may also impart a desirable sweetness of taste to the oral care compositions. Suitable examples of humectants may include glycerin, sorbitol, polyethylene glycol, propylene glycol, xylitol, trimethyl glycine, and mixtures thereof. Other examples may include other edible polyhydric alcohols. In some examples, the humectant is selected from sorbitol, glycerin, and combinations thereof. In a preferred example, the humectant is sorbitol. In another preferred example, the Petition 870260022065, dated 10 / 03 / 2026, page 26 / 103 22 / 42 The humectant is glycerin. In one example, the composition comprises from 10% to 66%, or alternatively from 30% to 55%, of humectant, by weight of the composition. Water

[0054] The oral care compositions described herein may include from 10% to 60%, by weight of the composition, of the total water content. In some examples, the oral care compositions may include from 10% to 50%, or preferably from 10% to 40%, by weight of the composition, of the total water content. The term total water content, for use in the present invention, means the total amount of water present in the composition, added separately or present as a solvent or vehicle for other raw materials, but excluding that which may be present as water of crystallization in certain inorganic salts. Preferably, the water is USP water.

[0055] Water is commonly used as a carrier material in oral care compositions due to its many benefits. For example, water is useful as a processing aid, is benign to the oral cavity, and helps in the rapid foaming of toothpastes. Water can be added as a single ingredient or can be present as a vehicle for other common raw materials, for example, sorbitol. Thickening system

[0056] The oral care compositions of the present invention may comprise a thickening system. Preferably, the oral care composition comprises from about 0.5% to about 10%, preferably from about 0.8% to about 5%, more preferably from about 1% to Petition 870260022065, dated 10 / 03 / 2026, page 27 / 103 23 / 42 approximately 5%, by weight of the composition, of a thickening system. More preferably, the thickening system comprises a thickening polymer, a thickening silica, or a mixture thereof. Even more preferably, when the thickening system comprises a thickening polymer, the thickening polymer is selected from carboxymethylcellulose, a linear sulfated polysaccharide, a natural gum, or mixtures thereof.Even more preferably, when the thickening system comprises a thickening polymer, the thickening polymer is selected from the group consisting of: (a) from about 0.01% to about 3% of a carboxymethylcellulose (CMC), by weight, of the composition, preferably from about 0.1% to about 2.5%, more preferably from about 0.5% to about 1.7%, by weight, of the composition, of CMC; (b) from about 0.01% to about 2.5%, preferably from about 0.05% to about 2%, more preferably from about 0.1% to about 1.5%, by weight, of the composition, of a linear sulfated polysaccharide, preferably wherein the linear sulfated polysaccharide is a carrageenan; (c) from about 0.01% to about 3%, preferably from about 0.1% to about 2%, more preferably from about 0.2% to about 1.8%, by weight, of the composition of a natural gum; or (d) mixtures thereof.

[0057] The thickening polymer may also include non-colloidal microcrystalline cellulose, colloidal microcrystalline cellulose, or a mixture thereof. Non-colloidal microcrystalline cellulose, typically called microcrystalline cellulose or MCC, is a purified, partially depolymerized cellulose, for example, AVICEL® PH 102 or PH 105. Colloidal microcrystalline cellulose is obtained by reducing Petition 870260022065, dated 10 / 03 / 2026, page 28 / 103 24 / 42 the particle size of microcrystalline cellulose and stabilizing the particles to prevent the formation of hard aggregates, for example, AVICEL® CL 611 or RC 591.

[0058] Preferably, when the thickening system comprises a thickening silica, the thickening silica is from about 0.01% to about 8%, preferably from about 0.1% to about 5%, preferably from about 1% to about 3%, by weight, of the composition.

[0059] Preferably, the linear sulfated polysaccharide is a carrageenan (also known as carrageenan). Examples of carrageenan include kappa-carrageenan, iotacarrageenan, lambda-carrageenan, or mixtures thereof.

[0060] In one aspect, thickening silica is obtained from a sodium silicate solution by destabilizing it with acid to produce very fine particles. A commercially available example is the ZEODENT® brand silicas, available from Huber Engineered Materials (e.g., ZEODENT® 103, 124, 113, 115, 163, 165 and 167).

[0061] In one aspect, CMC is prepared from cellulose by treatment with alkali and monochloroacetic acid or its sodium salt. Different varieties are commercially characterized by viscosity. A commercially available example is CMC of the Aqualon™ brand close to Ashland Special Ingredients (e.g., Aqualon™ 7H3SF; Aqualon™ 9M3SF; Aqualon™ TM9A; Aqualon™ TM12A). Preferably, a natural gum is selected from the group consisting of karaya gum, gum arabic (also known as acacia gum), tragacanth gum, xanthan gum, and mixtures thereof. Preferably, the natural gum is a Petition 870260022065, dated 10 / 03 / 2026, p. 29 / 103 25 / 42 Xanthan gum. Xanthan gum is a polysaccharide secreted by the bacterium Xanthomonas camestris. In general, xanthan gum is composed of repeating pentasaccharide units, comprising glucose, mannose, and glucuronic acid in a molar ratio of 2:2:1, respectively. The chemical formula (of the monomer) is C35H49O29. In one aspect, xanthan gum is available from CP Kelco Inc. (Okmulgee, USA).

[0062] In one aspect, the thickening polymer is selected from the group consisting of a carboxymethylcellulose, a linear sulfated polysaccharide, a natural gum and mixtures thereof. Viscosity

[0063] Preferably, the oral care compositions of the present invention have a viscosity range of about 200,000 centipoises to about 850,000 centipoises (cP). A method for evaluating viscosity is described. The viscometer is a Brookfield® viscometer, model DV-I Prime, with a Brookfield Helipath holder. The viscometer is placed in the Helipath holder and leveled using a bubble level. Spindle E is fixed, and the viscometer is set to 2.5 RPM. Separate the spindle, zero the viscometer, and install spindle E. Then, lower the spindle until the crosshead is partially submerged in the paste before starting the measurement. Simultaneously turn on the power switch on the viscometer and the helipath to start the spindle's downward rotation. Set a timer for 48 seconds and turn on the timer at the same time as the motor and the helipath. Take a reading after 48 seconds. The reading is in cP. Petition 870260022065, dated 10 / 03 / 2026, p. 30 / 103 26 / 42 Dye

[0064] The compositions of the present invention may include a colorant. Titanium dioxide is an example of a colorant. Titanium dioxide is a white powder that imparts opacity to the compositions. The colorant, for example, titanium dioxide, may generally comprise from about 0.25% to about 5% by weight of the composition. Flavoring agent

[0065] The toothpaste composition of the present invention may include from 0.01% to 5%, preferably from 0.1% to 2%, by weight of the composition, of a flavoring agent. Examples of suitable flavoring agents that may be used in the toothpaste composition include those described in U.S. Patent No. 8,691,190; Haught, JC, from column 7, line 61, to column 8, line 21. In some examples, the flavoring agent may be selected from methyl salicylate, menthol, eugenol, and cineole. In some examples, the toothpaste composition may comprise a flavor and aroma mixture that is free or substantially free of methyl salicylate, menthol, eugenol, and cineole. Sweetener

[0066] The toothpaste compositions of the present invention may include a sweetening agent. The sweetening agent is generally present in the toothpaste compositions in proportions of 0.005% to 5% by weight of the composition. Suitable examples of sweeteners include saccharin, dextrose, sucrose, lactose, xylitol, maltose, levulose, aspartame, sodium cyclamate, D-tryptophan, dihydrochalcones, acesulfame, sucralose, neotame, and mixtures thereof. Other examples of sweeteners Petition 870260022065, dated 10 / 03 / 2026, page 31 / 103 Suitable 27 / 42 configurations are described in U.S. Patent No. 8,691,190; Haught, JC from Column 9, row 18 to Column 10, row 18. Other ingredients

[0067] The present oral care composition may comprise the usual and conventional auxiliary components known to those skilled in the art. Optional ingredients include, for example, but are not limited to, anti-plaque agent, anti-sensitivity agent, whitening and oxidizing agent, anti-inflammatory agent, anti-calculus agent, chelating agent, tooth-adhering agent, analgesic and anesthetic agent. It will be understood that the components selected for the oral care compositions need to be chemically and physically compatible with each other.

[0068] Preferably, the oral care composition of the present invention is essentially free of glycyrrhetinic acid and its salt. Method of use

[0069] In one aspect, the present invention relates to a method for treating dental biofilm. The method comprises the step of brushing / cleaning the teeth with an oral care composition according to the present invention. The method comprises placing a subject's teeth in contact with the oral care compositions according to the present invention.

[0070] In another aspect, the present invention also relates to a method for controlling plaque bacteria in an individual, comprising administering to the oral cavity of an individual an oral care composition according to the present invention, preferably wherein the Petition 870260022065, dated 10 / 03 / 2026, p. 32 / 103 28 / 42 administration should occur at least once a day, preferably at least twice a day. Testing methods Test method 1: Assay for measuring the enhanced endotoxin neutralization of the antibacterial agent in biofilms

[0071] To determine the enhanced endotoxin neutralization of the antibacterial agent in biofilms, the following assay is used to evaluate the LPS binding efficiency of stannous ions via measurement of a fluorescent dye that is bound to LPS lipid A in plaque biofilms in situ for oral care compositions of the present invention and controls. Details of the invention are described below. (a) Substrate for biofilm growth

[0072] Hydroxyapatite (HA) discs are used for in situ biofilm growth. HA discs are designed having three parallel grooves (i.e., 200 µm wide; 200 µm deep for double-sided grooves; While 500 µm wide and 500 µm deep for the intermediate groove) on each disc. When fixing the discs in an individual's mouth, keeping these grooves vertical mimics the interproximal space between teeth, the hard-to-clean area where plaque tends to accumulate. This design allows for the collection of untouched plaque from the grooves. The HA discs are manufactured by Shanghai Beierkang Biomedicine Limited. (b) Using the splint

[0073] Human individuals use the splint. Each patient uses up to 12 HA discs in the splint to ensure that Petition 870260022065, dated 10 / 03 / 2026, page 33 / 103 29 / 42 at least 9 HA discs are available after 48 hours. In a specific example, and with reference to Figure 2, the HA disc has three parallel grooves (the grooves on the two sides are 300 pm wide and 300 pm deep; while the intermediate groove (between the two side grooves) is 500 pm wide and 500 pm deep). The intermediate groove is designed wider and deeper than the two side grooves so that the HA disc can be more easily separated into two identical half-discs for head-to-head comparison purposes. Further details of HA discs are described in US2017 / 0056531 (e.g., paragraphs

[0019] to

[0020] ).

[0074] The discs can be positioned so that the indentation is in the interdental space between the teeth (since this area is prone to plaque formation (given the difficulty of cleaning, etc.)). Individuals remove the splint only during meals (the splint is stored in an opaque container under humid conditions) and to perform oral hygiene procedures. Immediately afterwards, the splint is used again. Individuals are asked to use a straw when drinking. (c) In situ release of biofilms from the HA disc

[0075] All HA discs are removed from the splint after 48 hours using forceps. The forceps are used to hold the edge of the HA chips and transfer the HA disc to a 2 mL centrifuge tube containing phosphate-buffered saline (PBS). The forceps are thoroughly washed (water; 75% alcohol; and then deionized water) before each disc transfer. Petition 870260022065, dated 10 / 03 / 2026, page 34 / 103 30 / 42 (d) Preparation of toothpaste supernatants

[0076] 15 grams of deionized water are added to 5 grams of toothpaste from test samples. After vigorous shaking, the mixture is centrifuged at 12,000 rpm for 20 minutes. The supernatant is prepared one day before use and stored at 4°C. (e) Confocal laser scanning microscopy

[0077] After the HA discs are removed from the splint. The HA discs are used for ex vivo treatment by the different compositions of the invention and control. After being treated with the supernatant in question and labeled with the microbial fluorescent probe and the stannous fluorescent probe, the biofilms in the grooves are measured by confocal laser scanning microscopy (CLSM) (as described below). Preferably, the neutralized LPS fluorescent probe is BODIPY-TR-cadaverine (BC) (available from Thermo Fisher). Preferably, the microbial fluorescent probe is the Molecular Probes™ LIVE / DEAD® BacLight™ system (available from Thermo Fisher). (f) Disc preparation

[0078] The HA discs are rinsed in PBS solution, and each HA disc is divided into two halves using forceps. After that, each disc half is placed statically in 500 to 1000 pl of PBS solution for 1 minute. Each disc is treated for two minutes with PBS solution or toothpaste supernatant. Each disc is washed, each held by forceps, shaken ten times back and forth in 1 ml of PBS solution, and then this washing cycle is repeated. Then, each disc is immersed statically in 500 to 1000 pl of PBS solution for 5 minutes. Petition 870260022065, dated 10 / 03 / 2026, page 35 / 103 31 / 42 (g) Staining and fluorescence microscopy

[0079] The neutralization effect of LPS was evaluated using BODIPY-TR-cadaverine (BC), a fluorescent dye that is bound to lipid A, thus suppressing its fluorescence. BC is displaced by agents with an affinity for this lipid. When LPS is bound by other ions, for example, tin, BC is released from LPS and its fluorescence is proportional to the amount of free (unbound) BC present. Therefore, the fluorescence level indicates the amount of neutralized (bound) LPS versus free (unbound) LPS, and the effectiveness of an antibacterial agent in reducing biofilm toxicity. The greater the amount of bound LPS, the lower its toxicity.

[0080] After treatment and immersion, each disc is stained with the BODIPY-TR-cadaverine (BC) probe together with the Syto-9 probe (containing 5 μM BC probe and 5 μM Sn probe) for 30 minutes in the dark. After staining, each disc is immersed in 500 to 1000 μL of PBS solution statically for 2 minutes. The discs are washed again, holding each disc with tweezers, agitated five times back and forth in 1 mL of PBS solution, and then the cycle is repeated. For samples stained with SYTO-9 / BC dye, the following parameters are used: Xex = 488 nm / 543 nm, Xem = 500 / 580 nm, 20X objective lens and scanning from the bottom of the bacteria to the surface to 60 μM with a step size = 3 μη. (h) Confocal laser scanning microscopy

[0081] The Leica™ TCS SP8 AOBS spectral confocal microscope is used. The confocal system consists of a Leica™ DM6000B upright microscope and a microscope Petition 870260022065, dated 10 / 03 / 2026, page 36 / 103 The Leica™ DMIRE2 32 / 42 inverted microscope features a vertical stand for slide-mounted sample applications, while the inverted stand, with a 37°C incubation chamber and CO2 enrichment accessories, provides live-cell applications. The microscopes share an interchangeable laser scanning head and, in addition to their own electromotor-driven stages, a high-precision galvanometer-driven Z-stage, which facilitates rapid focal plane (Z) imaging. Besides epifluorescence, the microscopes support various transmitted light contrast methods, including bright-field, polarizing light, and differential interference contrast, and are equipped with Leica™ 5x, 20x, 40x, 63x (oil and dry), and 100x (oil) objective lenses.

[0082] The laser detection and scanning system is described. The TCS SP8 AOBS confocal system is equipped with four lasers (one diode laser, one argon laser, and two helium lasers), thus enabling the excitation of a wide range of fluorochromes within the UV, visible, and ultraviolet ranges of the electromagnetic spectrum. The laser scanning head design, which incorporates tunable acoustic-optical filters (AOTF), an acoustic-optical dichroic beam (AOBS), and four prism spectrophotometer detectors, enables the excitation and detection of three fluorochromes simultaneously. The upright microscope also has a light transmission detector that makes it possible to superimpose a transmitted light image onto a fluorescence recording.

[0083] Leica™ Confocal software is used. Confocal microscopy is controlled using a Pentium PC. Petition 870260022065, dated 10 / 03 / 2026, p. 37 / 103 A standard 33 / 42 microscope equipped with two monitors runs Leica™ Confocal software. Leica Confocal software provides an interface for capturing, processing, and analyzing multidimensional image series, including 3D reconstruction and measurement, physiological recording and analysis, time-lapse, fluorochrome colocalization, photo-brightening techniques such as FRAP and FRET, spectral blending, and multicolor restoration. Regarding image analysis, samples stained with the SYTO-9 / BC probe are selected to quantify the fluorescence intensity of red and green pixels. Efficacy of neutralizing LPS endotoxin

[0084] Using the software, the fluorescence intensity ratio (FIR) bound LPS / bacterial cell was calculated. This fluorescence intensity ratio indicates the relative amount of bound (neutralized) LPS per unit of bacteria, and the effectiveness of an agent in reducing biofilm toxicity. The higher the fluorescence intensity ratio, the greater the effectiveness in neutralizing LPS endotoxin. Rate of penetration of the active ingredient into the biofilm.

[0085] Using the software, the pixel overlap of the green bacterial probes and the red stannous probes is identified, and then this value is divided by all non-black pixels (which includes non-overlapping stannous probes) to provide a percentage of stannous colocalization in the bacteria. Generally, the higher this stannous colocalization percentage, the greater the effectiveness of the oral care product in delivering stannous to the bacteria. (See Xiang J, Li H, Pan B, Chang J, He Y, He Petition 870260022065, dated 10 / 03 / 2026, page 38 / 103 34 / 42 T, Strand R, Shi Y, Dong W. (2018) Penetration and Bactericidal Efficacy of Two Oral Care Products in an Oral Biofilm Model. Am J Dent, Vol 31, Issue 1: 53-60). Test Method 2: EC50 Test (Irritation) - 2D cell-based method for evaluating oral irritation.

[0086] Half the maximum effective concentration (EC50) is a toxic unit that measures the concentration of a formula or toxicant that induces a response halfway between the baseline and the maximum after a specified exposure time. (1) Cell line culture and test preparation:

[0087] Human gingival epithelial cells (HGE) are maintained in an incubator at 37°C with 5% CO2 and 95% humidity. Dulbecco's modified Eagle medium (DMEM, Gibco) containing 10% fetal calf serum, 1% penicillin-streptomycin, is used as the complete culture medium, which was changed every 2 to 3 days.

[0088] One day before the test, 20,000 cells / well are seeded in a 96-well plate and incubated at 37°C with 5% CO2 and 95% humidity for 24h. (2) Toothpaste preparation:

[0089] 6 + / -0.001 g of toothpaste is added to 18 ml of DMEM in a sterilized 100 ml beaker. The sample is stirred at 500 rpm for 20 min using a magnetic stir bar. The paste is then transferred to a sterilized 50 ml tube and centrifuged at 15,000 rpm for 15 min. The supernatant is diluted with DMEM to provide a 25 mg / ml core stock solution. The core stock solution is further diluted with DMEM to the dosage solutions according to the table below. Petition 870260022065, dated 10 / 03 / 2026, page 39 / 103 35 / 42 ID Final Concentration (mg / ml) Stock (mg / ml) Stock Volume (µl) Medium Volume (µl) Final Volume (µl) 1 14.063 25 450 350 800 2 12.500 25 400 400 800 3 10.938 25 350 450 800 4 9.375 25 300 500 800 5 7.813 25 250 550 800 6 6.250 25 200 600 800 7 4.688 25 150 650 800 8 3.125 25 100 700 800 9 1.563 25 50 750 800 10 0.781 25 25 775 800 (3) Dosage of plaque solutions:

[0090] The medium is removed from the 96-well plate. 150µl of selected dosage solutions are added to the 96-well plate. There is a duplicate for each dosage solution concentration. The cell is incubated with serial concentrations of toothpaste dosage solutions for 30 min at 37°C with 5% CO2 and 95% humidity. (4) CCK8 test for evaluating HGE cell viability:

[0091] The working solution of the Cell Counting Kit-8 (CCK8, from DOJINDO) is prepared by diluting the CCK8 reagent with DMEM (CCK8: DMEM=1:10). The toothpaste dosage solution is then carefully removed from the 96-well plate. 100µl of the CCK8 working solution is added to each well, and the cell is continuously incubated for 1.5 ha at 37°C, 5% CO2, and 95% humidity. Then, the 96-well plate... Petition 870260022065, dated 10 / 03 / 2026, page 40 / 103 36 / 42 wells are read by SpectraMax i3 (Molecular Devices) for absorbance at 450 nm at room temperature. (5) Data processing:

[0092] The initial OD value is deducted from the OD of the blank control (the wells without cells), which is then followed by normalization with the average OD of the positive control (the wells with cells only). The data are then processed by GraphPad to generate the 30-min EC50 for each toothpaste. Examples

[0093] The following examples and descriptions clarify in more detail the embodiments within the scope of the present invention. These examples are provided for illustrative purposes only and should not be considered a limitation of the present invention, since many variations thereof are possible without departing from its character and scope. Example A: Preparing Examples 1 to 4

[0094] Formulation Examples 1 to 4 are toothpaste compositions shown below with component quantities in % by weight. Examples 1 to 3 are comparative formulations, while Example 4 is an inventive formulation according to the present invention. Example 4 is made with a stannous ion source, a soluble zinc ion source, and a taurate surfactant (SMCT). In parallel, comparative formulation Examples 1 and 2 are made without a stannous ion source and use SLS and SMCT surfactants, respectively. Example 3 is a formulation containing a stannous ion source and sodium lauryl sulfate (SLS) surfactant, but without taurate surfactant. All compositions are prepared by mixing the components described in the Table. Petition 870260022065, dated 10 / 03 / 2026, page 41 / 103 37 / 42 1, in the proportions indicated. A commercial comparative formulation containing insoluble zinc ion and a stannous ion source is also prepared, namely, Comparative Example 5. Table 1: Examples of Formulation 1 to 4 Name Ex. 1 (Comparative) Ex. 2 (Comparative) Ex. 3 (Comparative) Ex. 4 (of the invention) Water qsp qsp qsp qsp Glycerin - - - - Sorbitol (70%) 65.200 65.200 48.000 48.00 Stannous fluoride - - - - Stannous chloride in silica (10%) - - 1.290 1.29 Sodium fluoride 0.321 0.321 0.321 0.321 Sodium gluconate - - 1.064 1.064 Sodium hydroxide (50%) - - 0.900 0.900 Monosodium phosphate 0.400 0.400 - - Trisodium phosphate 0.930 0.930 - - Sodium saccharin 0.300 0.300 0.500 0.500 Xanthan gum - - 0.875 0.875 Carrageenan - - 1.500 1.500 Carbomer 0.220 0.220 - - Sodium carboxymethyl cellulose (CMC) 0.700 0.700 - - Sodium citrate - - - - Zinc citrate - - 0.533 0.533 Titanium dioxide - - - - Hydrated silica 16.000 16.000 16.000 16.000 Sodium lauryl sulfate (29%) 5.000 - 5.000 - Petition 870260022065, dated 10 / 03 / 2026, page 42 / 103 38 / 42 Sodium Methyl Cocoyl Taurate (SMCT) (29%) - 5,000 - 5,000 Flavorings 1,000 1,000 1,000 1,000 Total 100,000 100,000 100,000 100,000 Example B: Improve endotoxin neutralization and stannous (Sn) penetration into the biofilm.

[0095] Test method 1 is conducted to measure the neutralization of bacterial endotoxin in biofilms of the examples of the present invention and comparators, as well as to measure the penetration rate of active Sn into biofilms that neutralizes the endotoxin. The results are presented in Table 2 and Table 3. Table 2 - Neutralization of bacterial endotoxins in biofilm Treatment Fluorescence intensity ratio (FIR) LPS bound / bacterial cell Cluster* Negative control (Phosphate buffer solution) 0.1033 D Comparative example 1 0.1267 D Comparative example 2 0.1300 D Comparative example 3 1.0833 B Example of the invention 4 1.8833 A 1 Comparative example 5 0.8500 C * Means for groups in homogeneous subsets, those that do not share a letter are significantly different (alpha = 0.05) and average sample size = 6. Student-Newman-Keuls Method1 Comparative Example 5 is a commercially available toothpaste from Colgate® Total™sf (LOT 1249US56C1), with the Petition 870260022065, dated 10 / 03 / 2026, page 43 / 103 39 / 42 Ingredients: water, sorbitol, hydrated silica, glycerin, PEG-12, tetrasodium pyrophosphate, flavor and aroma, sodium lauryl sulfate, zinc phosphate, cellulose gum, sodium citrate, stannous fluoride; microcrystalline cellulose, sodium saccharin, cocamidopropyl betaine, xanthan gum, citric acid, sucralose, titanium dioxide. Table 3 - Rate of penetration of active Sn into biofilm Treatment % of Sn penetration Grouping* Negative control (Phosphate buffer solution) 0.11 D Comparative example 1 1.53 D Comparative example 2 1.67 D Comparative example 3 75.24 B Example of the invention 4 84.43 A 1 Comparative example 5 64.00 C Same as above.

[0096] The results in Table 2 demonstrate a Significantly higher Fluorescence Intensity Ratio (FIR) of LPS / bound bacterial cell with biofilms treated with Examples of the invention 4 (i.e., compositions containing Sn + Zinc Citrate + Taurate), compared to Comparative Example 3 (i.e., compositions of Zinc Citrate Sn + SLS) and Comparative Example 5 (commercial formulation containing Sn, insoluble Zinc Phosphate + SLS and co-surfactant cocamidopropyl betaine). Furthermore, Comparative Examples 1 and 2 (i.e., without a Sn source) have no effect on endotoxin neutralization, regardless of the type of surfactant, taurate or SLS. Interestingly, the example Petition 870260022065, dated 10 / 03 / 2026, page 44 / 103 Comparative example 3, which contains a soluble / partially soluble zinc source (i.e., zinc citrate), has improved bacterial toxin neutralization and stannous penetration versus competitive example 5, which contains an insoluble zinc ion source, which is zinc phosphate.

[0097] The results in Table 3 demonstrate a significantly greater penetration of Sn ion into the biofilm for Examples of the invention 4 containing stannous and taurate vs. Comparative Examples 3 and 5 containing stannous and SLS.

[0098] The use of taurate without a source of stannous ions, Comparative Example 2, has a very low FIR of the bound LPS / bacterial cell, indicating that the surfactant taurate does not neutralize bacterial endotoxins (LPS).

[0099] The surprising combination of tin and taurate has a significant improvement in the neutralization of bacterial endotoxin, due to the increased penetration of stannous ions into the biofilm. Example 3: EC50 irritation test

[0100] Test Method 2 is conducted to measure half the maximum effective concentration (EC50) of the invention's examples and comparators. EC50 measures the concentration of a formula or toxicant that induces a response halfway between baseline and maximum after a specified exposure time. The higher the numerical score, the better, showing that the cells are more tolerant / less irritated and not harmed. Table 4 - EC50 irritation test Treatment EC50 (mg / ml) Grouping * Comparative example 1 5,807 B Petition 870260022065, dated 10 / 03 / 2026, page 45 / 103 41 / 42 Comparative example 2 8.002 A Comparative example 3 5.406 B Example of the invention 4 6.998 A Comparative example 5 5.683 B * Same as above.1 Same as above.

[0101] As demonstrated in Table 4, compositions containing taurate surfactant demonstrate significantly greater tolerance to irritation of human gingival epithelial cells for Examples of the invention 4 and Comparative Example 2 (compositions containing taurate surfactant).

[0102] The surprising combination of tin and taurate has a significant improvement in neutralizing bacterial endotoxin from the penetration of the stannous ion into the biofilm, while causing less irritation and disruption of the gingival epithelium barrier, which, if compromised, will allow bacterial toxins to infiltrate and cause inflammation of the gums.

[0103] The dimensions and values ​​disclosed herein should not be understood as strictly limited to the exact numerical values ​​mentioned. Instead, except where otherwise specified, each of these dimensions is intended to mean both the value mentioned and a range of functionally equivalent values ​​around that value. For example, a dimension disclosed as 40 mm is intended to mean approximately 40 mm.

[0104] Each document cited in the present invention, including any patent or patent application referenced or related, and any patent application or Petition 870260022065, dated 10 / 03 / 2026, page 46 / 103 42 / 42 patent in which this application claims priority or benefit thereof, is hereby incorporated in its entirety into the present invention by reference, except where expressly excluded or otherwise limited. Mention of any document is not an admission that it constitutes prior art relating to any invention disclosed or claimed in the present invention, or that it alone, or in any combination with any other reference or references, teaches, suggests or reveals any such invention. Furthermore, if there is a conflict between any meaning or definition of a term in this document and any meaning or definition of the same term in a document incorporated by reference, the meaning or definition ascribed to that term in this document shall prevail.

[0105] Although specific embodiments of the present invention have been illustrated and described, it will be evident to those skilled in the art that various other alterations and modifications can be made without departing from the spirit and scope of the invention. Therefore, it is intended to cover in the appended claims all such alterations and modifications that are within the scope of the present invention. Petition 870260022065, dated 10 / 03 / 2026, p. 47 / 103

Claims

1 / 4 CLAIMS 1. Oral care composition characterized by comprising: (a) 0.01% to 5% by weight of the composition of a stannous ion source; (b) 0.1% to 5% by weight of the composition of a taurate surfactant represented by the formula: r2 II I Rj--C—N — CH2—CH2 — SO3-M+, wherein R1 is a saturated or unsaturated alkyl chain, linear or branched with 6 to 18 C atoms; R2 is H or methyl, and M is H, sodium or potassium; and (c) 0.1% to 2% by weight of the composition of a zinc ion source, wherein the zinc ion source comprises at least 95% by weight of a soluble or partially soluble zinc ion source.

2. Oral care composition, according to claim 1, characterized in that R1 is a saturated or unsaturated alkyl chain, linear or branched, with 8 to 18 C atoms, optionally wherein the taurate surfactant comprises one or more of potassium cocoyl taurate, potassium methyl cocoyl taurate, sodium methyl caproyl taurate, sodium cocoyl taurate, sodium lauroyl taurate, sodium methyl cocoyl taurate, sodium methyl lauroyl taurate, sodium methyl myristoyl taurate, sodium methyl oleoyl taurate.

3. Oral care composition, according to any of the preceding claims, characterized in that the source of soluble or partially soluble zinc ions (Petition 870260022065, dated 10 / 03 / 2026, page 91 / 103 2 / 4) is selected from the group consisting of zinc citrate, zinc chloride, zinc sulfate, zinc gluconate, zinc lactate and combinations thereof; and in which, more preferably, the source of zinc ions is selected from the group consisting of zinc citrate, zinc gluconate, zinc lactate and combinations thereof.

4. Oral care composition, according to any of the preceding claims, characterized in that the composition is substantially free of insoluble zinc compounds selected from zinc oxide, zinc phosphate or zinc carbonate.

5. Oral care composition, according to any of the preceding claims, characterized in that the source of stannous ions is selected from soluble stannous salts and, preferably, selected from the group consisting of stannous chloride, stannous fluoride, stannous acetate, stannous gluconate, stannous oxalate, stannous sulfate, stannous lactate, stannous tartrate, stannous iodide, stannous chlorofluoride, stannous hexafluorozirconate, stannous citrate, stannous malate, stannous glycinate, stannous carbonate, stannous phosphate, stannous pyrophosphate, stannous metaphosphate and combinations thereof; wherein, preferably, the source of stannous ions is selected from stannous chloride, stannous fluoride, or a combination thereof.

6. Oral care composition, according to any of the preceding claims, characterized by additionally comprising 0.5% to 5%, preferably 0.5% to 1.5%, by weight of the composition, of a source of fluoride ions; preferably, the source of fluoride ions is selected from the group consisting of stannous fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate and zinc fluoride, or mixtures thereof.

7. Oral care composition, according to any of the preceding claims, characterized by being substantially free of sodium lauryl sulfate (SLS).

8. Oral care composition, according to any of the preceding claims, characterized by comprising from 10% to 60%, preferably from 10% to 40%, by weight of the composition, of the total water content.

9. Oral care composition, according to any of the preceding claims, characterized by further comprising from 0.01% to 5%, by weight of the composition, of a thickening system, wherein the thickening system is selected from a thickening polymer, a thickening silica or a combination thereof.

10. Oral care composition, according to any of the preceding claims, characterized by further comprising from 1% to 35%, more preferably from 5% to 25%, by weight of the composition, of an abrasive, wherein the abrasive is selected from a calcium-containing abrasive, a silica abrasive or a combination thereof; and wherein, more preferably, the abrasive is a silica abrasive.

11. Oral care composition, according to any of the preceding claims, characterized in that the composition is free of glycyrrhetinic acid and its salt. Petition 870260022065, dated 10 / 03 / 2026, pp. 93 / 103 4 / 4 12. Oral care composition, according to any of the preceding claims, characterized in that the composition has a pH ranging from 4.0 to 9.0, preferably from 4.3 to 8.0 and more preferably from 4.6 to 7.

5.

13. Oral care composition, according to any of the preceding claims, characterized by being a monophasic toothpaste.

14. Use of a composition for oral care, as defined in any one of claims 1 to 13, characterized by the fact that it is for the manufacture of a composition for the treatment of dental biofilm.

15. Use of a composition for oral care, as defined in any of claims 1 to 13, characterized by being for the manufacture of a composition to prevent or mitigate plaque formation on tooth enamel. Petition 870260022065, dated 10 / 03 / 2026, pp. 94 / 103