• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    composition for oral care, method of reducing or inhibiting the formation of biofilm in the oral cavity and use of a combination of arginine and zinc oxide and zinc citrate in the preparation of oral care composition. an oral care composition comprising: (a) arginine, in free or salt form; and (b) zinc oxide and zinc citrate. the oral care composition can reduce or inhibit biofilm formation in an oral cavity.
    公开号:BR112016013333B1
    申请号:R112016013333-1
    申请日:2014-12-10
    公开日:2020-12-15
    发明作者:Michael Prencipe；Yun Xu；Xiao Yi Huang
    申请人:Colgate-Palmolive Company；
    IPC主号:
    专利说明:

    Background
    [001] Plaque is a biofilm that adheres to teeth and other oral surfaces, particularly at the gingival margin and is involved in the occurrence of gingivitis, periodontitis, cavities and other forms of periodontal disease. Plaque is cohesive and highly resistant to removal on teeth and / or oral surfaces. Plaque comprises glucans, which are insoluble polysaccharides that provide plaque with its cohesive properties. The bacterial enzyme glycosyltransferase converts dietary sugar into glucans. Plaque mineralizes to form a hard deposit called calculus (or tartar), which becomes a local irritant to the gums, causing gingivitis.
    [002] Various antibacterial agents can slow the growth of bacteria and thus reduce the formation of biofilm on oral surfaces.
    [003] Zinc and other metallic compounds / salts have previously been used as antibacterial agents. Without sticking to the theory, it is believed that free zinc ions provide antibacterial efficacy by inhibiting glucose metabolism and / or interacting with the bacterial cell wall, reducing bacterial colonization (as discussed in Cummins D., J Clin Periodontol 1991; 18; 455461). An insoluble zinc compound, zinc oxide, could also provide great antibacterial efficacy during tooth brushing.
    [004] It would be desirable to provide a composition for oral care which exhibits even better efficacy than the previously known compositions in reducing biofilm. Brief Summary
    [005] An oral care composition is provided comprising: (a) arginine, in its free or salt form; and (b) two or more zinc salts, wherein at least one of said zinc salts is zinc oxide and at least one of said zinc salts is zinc citrate.
    [006] Optionally, a weight ratio of zinc oxide to zinc citrate is 1.5: 1 to 4.5: 1; 1.5: 1 to 4: 1; 1.7: 1 to 2.3: 1; 1.9: 1 to 2.1: 1 or about 2: 1. In addition, the corresponding molar ratios based on these weight ratios can be used.
    [007] Optionally, arginine is present in an amount of 0.5% by weight to 10% by weight, based on the total weight of the composition. Also optionally, arginine is present in an amount of 0.5% by weight to 3% by weight or from 1% by weight to 2.85% by weight, based on the total weight of the composition. Also optionally, arginine is present in an amount of 1.17% by weight to 2.25% by weight based on the total weight of the composition. Despite this also optionally, arginine is present in an amount of 1.4% by weight to 1.6% by weight, based on the total weight of the composition. Still optionally, arginine is present in an amount of about 1.5% by weight, based on the total weight of the composition.
    [008] Optionally, the total concentration of zinc salts in the composition is 0.2% by weight to 5% by weight, based on the total weight of the composition.
    [009] Optionally, the molar ratio of arginine to total zinc salts is 0.05: 1 to 10: 1.
    [010] Optionally, the composition comprises zinc oxide in an amount from 0.5% by weight to 1.5% by weight and zinc citrate in an amount from 0.25% by weight to 0.75% by weight, based on the total weight of the composition. Also optionally, the composition comprises zinc oxide in an amount of about 1% by weight and zinc citrate in an amount of about 0.5% by weight, based on the total weight of the composition.
    [011] Optionally, the composition also comprises one or more abrasives. Also optionally, at least one of said one or more abrasives is silica.
    [012] Optionally, the oral care composition also comprises an anti-calculating agent. Also optionally, the anti-calculating agent is present in an amount of 0.2% by weight to 0.8% by weight, based on the total weight of the composition. Also optionally, the anti-calculating agent is at least one of tetrasodium pyrophosphate and tetrapotassium pyrophosphate.
    [013] An oral care composition is also provided for use in reducing or inhibiting biofilm formation in an oral cavity.
    [014] A method is also provided to reduce or inhibit biofilm formation in an oral cavity, the method comprising bringing the oral cavity into contact with an oral care composition.
    [015] There is also provided a use, in an oral care composition, of a combination of: (a) arginine, in its free or salt form; and (b) two or more zinc salts, wherein at least one of such zinc salts is zinc oxide and at least one of such zinc salts is zinc citrate; to reduce or inhibit biofilm formation in an oral cavity.
    [016] Optionally, a weight ratio of zinc oxide to zinc citrate is 1.5: 1 to 4.5: 1; 1.5: 1 to 4: 1; 1.7: 1 to 2.3: 1; 1.9: 1 to 2.1: 1 or about 2: 1. Also, the corresponding molar ratios based on these weight ratios can be used.
    [017] Optionally, arginine is present in an amount of 0.5% by weight to 10% by weight, based on the total weight of the composition. Also optionally, arginine is present in an amount of 0.5% by weight to 3% by weight or from 1% by weight to 2.85% by weight, based on the total weight of the composition. Also optionally, arginine is present in an amount of 1.17% by weight to 2.25% by weight based on the total weight of the composition. Despite this also optionally, arginine is present in an amount of 1.4% by weight to 1.6% by weight, based on the total weight of the composition. Still optionally, arginine is present in an amount of about 1.5% by weight, based on the total weight of the composition.
    [018] Optionally, the total concentration of zinc salts in the oral care composition is 0.2% by weight to 5% by weight, based on the total weight of the composition.
    [019] Optionally, the molar ratio of arginine to the total zinc salts in the oral care composition is 0.05: 1 to 10: 1. Also, the corresponding molar ratios based on these weight ratios can be used.
    [020] Optionally, zinc oxide is present in the oral care composition in an amount of 0.5% by weight to 1.5% by weight and zinc citrate is present in the oral composition in an amount of 0.25 % by weight up to 0.75% by weight, based on the total weight of the composition. Also optionally, zinc oxide is present in the oral care composition in an amount of about 1% by weight and zinc citrate is present in the oral composition in an amount of about 0.5% by weight, based on total weight of the composition.
    [021] Other areas of applicability of the present invention will become apparent from the detailed description provided below. It should be understood that the detailed description and specific examples, while indicating the preferred embodiment of the invention, are for the purpose of illustration only and are not intended to limit the scope of the invention. Detailed Description
    [022] The following description of the preferred mode (s) is merely exemplary in nature and is in no way intended to limit the invention, its application or uses.
    [023] As used throughout the description, ranges are used as abbreviated forms to describe each and every value that is within the range. Any value within the range can be selected as the end value of the range. In addition, all references cited in this document are incorporated herein by reference in their entirety. In the event of a conflict between a definition in the present disclosure and that of a cited reference, the present disclosure prevails.
    [024] Unless otherwise specified, all percentages and quantities expressed in this document and throughout the specification should be understood as referring to weight percentages. The quantities given are based on the active weight of the material.
    [025] As used in this description, the phrase “free or salt arginine” means that arginine can be present as the free amino acid or as a salt of the amino acid. Examples of suitable arginine salts include, but are not limited to, arginine bicarbonate, arginine phosphate and arginine hydrochloride.
    [026] The present inventors have surprisingly found that the addition of arginine to an oral care composition comprising a zinc salt improves the effectiveness of the oral care composition by reducing biofilm. The present inventors have also unexpectedly found that there is a more adequate concentration of arginine in which the effectiveness in reducing the biofilm of the oral care composition containing zinc salt is optimized.
    [027] In a first aspect, an oral care composition is provided comprising: (a) arginine, in free or salt form; and (b) two or more zinc salts, wherein at least one of said zinc salts is zinc oxide and at least one of said zinc salts is zinc citrate.
    [028] In some embodiments, arginine is present in the oral care composition in an amount of 0.5% by weight to 3% by weight; from 0.75% by weight to 2.9% by weight; from 1% by weight to 2.85% by weight; from 1.17% by weight to 2.25% by weight; from 1.3% by weight to 2% by weight; from 1.4% by weight to 1.6% by weight; or about 1.5% by weight, based on the total weight of the composition.
    [029] In any of the above modalities, the molar ratio of arginine: total zinc salts in the oral care composition can be 0.05: 1 to 10: 1; from 0.08: 1 to 5: 1; 0.1: 1 to 1: 1; from 0.4: 1 to 0.8: 1 or about 0.65: 1.
    [030] Examples of suitable zinc salts that can be used in the compositions of any of the above include (but are not limited to): zinc oxide, zinc citrate, zinc lactate, zinc chloride, zinc acetate, zinc gluconate, zinc glycinate, zinc sulfate, sodium zinc citrate and mixtures thereof. In any of the above aspects, at least one of one or more zinc salts can be zinc oxide. In the compositions at least one of said zinc salts is zinc oxide and at least one of said zinc salts is zinc citrate. In any of the above embodiments, the total concentration of the zinc salts in the composition can be from 0.2% by weight to 5% by weight; from 0.5% by weight to 2.5% by weight; from 0.8% by weight to 2% by weight; or about 1.5% by weight, based on the total weight of the composition.
    [031] In any of the above embodiments, the composition may comprise zinc oxide in an amount of 0.5% by weight to 1.5% by weight and zinc citrate in an amount of 0.25% by weight at 0 , 75% by weight, based on the total weight of the composition. Alternatively, the compositions may comprise zinc oxide in an amount from 0.75% by weight to 1.25% by weight and zinc citrate in an amount from 0.4% by weight to 0.6% by weight, based on in the total weight of the composition. Alternatively, the compositions may comprise zinc oxide in an amount of about 1% by weight and zinc citrate in an amount of about 0.5% by weight, based on the total weight of the composition.
    [032] In any of the above modalities, the oral care composition may also comprise one or more abrasives. Suitable abrasives that can be included in the compositions include, but are not limited to: silica abrasives, aluminum oxide, aluminum silicate, calcined alumina, bentonite, other siliceous materials, insoluble phosphates, natural calcium carbonate (NCC), carbonate precipitated calcium (PCC) and mixtures thereof. In some embodiments, at least one of one or more abrasives is an abrasive silica. Examples of abrasive silicas include, but are not limited to, precipitated or hydrated silicas having an average particle size of up to about 20 microns (such as Zeodent 105 and Zeodent 114 marketed by JM Huber Chemicals Division, Havre de Grace, Md. 21078 ); Sylodent 783 (marketed by Davison Chemical Division of W.R. Grace &Company); or Sorbosil AC 43 (from PQ Corporation). In some embodiments, at least one of the one or more abrasives is a calcium carbonate abrasive, such as precipitated calcium carbonate (PCC) or natural calcium carbonate (NCC).
    [033] In any of the above embodiments, the compositions may also comprise an anti-calculating agent (for the control of tartar). Suitable anticalculating agents include, but are not limited to: phosphates and polyphosphates, polyaminopropanesulfonic acid (AMPS), polyolefin sulfonates, polyolefin phosphates, diphosphonates such as azacycloalkane-2,2-diphosphonates (eg, azacycloeptane-2,2 acid -diphosphonic), N-methyl azacyclopentane-2,3-diphosphonic acid, ethane-1-hydroxy-1,1-diphosphonic acid (EHDP) and ethane-1-amino-1,1-diphosphonate, phosphonoalkane carboxylic acids e. Useful inorganic phosphate and polyphosphate salts include monobasic, dibasic and tribasic sodium phosphates, tetrasodium pyrophosphate (TSPP), tetrapotassium pyrophosphate, sodium tripolyphosphate, tetrapolyphosphate, sodium trimetaphosphate and same hexamethasphates. Other useful tartar control agents include polycarboxylate polymers and polyvinyl methyl methyl / maleic anhydride (PVM / MA) copolymers, such as GANTREZ®. In some embodiments, the anticalculation agent is at least one of tetrasodium pyrophosphate and tetrapotassium pyrophosphate. In some embodiments, the anti-calculating agent is present in the composition in an amount of 0.2% by weight to 0.8% by weight; 0.3% by weight to 0.7% by weight; 0.4% by weight to 0.6% by weight; or about 0.5% by weight, based on the total weight of the composition.
    [034] In any of the above modalities, the oral care composition can be a toothpaste, a toothpaste, a gel, a dental powder, a mouthwash, a mouthwash, a tablet, a tablet, an aerosol, a gum or a film. In certain embodiments, the oral care composition is a toothpaste, a gel or a dental powder.
    [035] In a second aspect, an oral care composition is provided according to any of the above modalities, for use in reducing or inhibiting the formation of biofilm in an oral cavity.
    [036] In a third aspect, a method is provided to reduce or inhibit the formation of biofilm in an oral cavity, the method comprising bringing the oral cavity into contact with an oral care composition according to any of the above modalities.
    [037] In a fourth aspect, use is made, in an oral care composition, of a combination of: (a) arginine, in free or salt form; and (b) two or more zinc salts, wherein at least one of said zinc salts is zinc oxide and at least one of said zinc salts is zinc citrate; to reduce or inhibit biofilm formation in an oral cavity.
    [038] According to the fourth aspect, the oral care composition can be a composition according to any of the modalities as described above for the first aspect.
    [039] Oral care compositions can also comprise additional ingredients. These additional ingredients may include, but are not limited to, diluents, bicarbonate salts, pH modifying agents, surfactants, foam modulators, thickening agents, humectants, sweeteners, flavorings, pigments, additional antibacterial agents, anti-caries agents and mixtures thereof. .
    [040] In some embodiments, oral care compositions comprise at least one bicarbonate salt useful, for example, to provide a “clean feeling” in teeth and gums due to effervescence and carbon dioxide release. Any orally acceptable bicarbonate can be used, including, without limitation, alkali metal bicarbonates, such as sodium and potassium bicarbonates, ammonium bicarbonate and the like. One or more additional bicarbonate salts are optionally present in a total amount of about 0.1% by weight to about 50% by weight, for example, from about 1% by weight to 20% by weight, by the total weight composition.
    [041] In some embodiments, oral care compositions comprise at least one pH-modifying agent. Said agents include acidifying agents to lower the pH, basifying agents to increase the pH and buffering agents to control the pH within a desired range. For example, one or more compounds selected from acidifying, basifying and buffering agents can be included to provide a pH of 2 to 10 or in various illustrative modalities, 2 to 8, 3 to 9, 4 to 8, 5 to 7 , 6 to 10, 7 to 9, etc. Any orally acceptable pH modifying agent can be used, including without limitation, carboxylic, phosphoric and sulfonic acids, acid salts (eg, monosodium citrate, disodium citrate, monosodium maleate, etc.), alkali metal hydroxides such as sodium hydroxide , carbonates such as sodium carbonate, bicarbonates, sesquicarbonates, borates, silicates, phosphates (e.g., monosodium phosphate, trisodium phosphate), imidazole and the like. One or more pH modifying agents are optionally present in a total amount effective to maintain the composition in an orally acceptable pH range.
    [042] Oral care compositions can also comprise at least one surfactant. Any orally acceptable surfactant, most of which are anionic, non-ionic or amphoteric, can be used. Suitable anionic surfactants include, without limitation, water soluble salts of C8-20 alkyl sulfates, sulfonated monoglycerides of C8-20 fatty acids, taurates and the like. Illustrative examples of these and other classes include sodium lauryl sulfate, coconut monoglyceride sodium sulfonate, sodium lauryl sarcosinate, sodium lauryl isothionate, sodium lauryl ether carboxylate and sodium dodecyl benzenesulfonate. Suitable nonionic surfactants include, without limitation, poloxamers, polyoxyethylene sorbitan esters, fatty alcohol ethoxylates, alkylphenol ethoxylates, tertiary amine oxides, tertiary phosphine oxides, dialkyl sulfoxides and the like. Suitable amphoteric surfactants include, without limitation, derivatives of C8-20 aliphatic secondary and tertiary amines having an anionic group such as carboxylate, sulfate, sulfonate, phosphate or phosphonate. Betaines can also be used, a suitable example of which is cocoamidopropyl betaine. One or more surfactants are optionally present in a total amount of about 0.01 wt% to about 10 wt%, for example, from about 0.05 wt% to about 5 wt% or about from 0.1% by weight to about 2% by weight by the total weight of the composition.
    [043] Oral care compositions may comprise at least one foam modulator, useful for example to increase the amount, thickness or stability of the foam generated by the composition upon shaking. An orally acceptable foam modulator can be used, including without limitation, polyethylene glycols (PEGs), also known as polyoxyethylenes. High molecular weight PEGs are suitable, including those having an average molecular weight of 200,000 to 7,000,000, for example, 500,000 to 5,000,000 or 1,000,000 to 2,500,000. One or more PEGs are optionally present in a total amount of from about 0.1 wt% to about 10 wt%, for example from about 0.2 wt% to about 5 wt% or about 0.25% by weight to about 2% by weight, based on the total weight of the composition.
    [044] Oral care compositions may comprise at least one thickening agent, useful for example to provide desired consistency and / or mouthfeel to the composition. Any orally acceptable thickening agent can be used, including without limitation, carbomers, also known as carboxyvinyl polymers, carrageenans, also known as Irish moss and more particularly 1-carrageenan (iota-carrageenan), cellulosic polymers such as hydroxyethylcellulose, carboxymethylcellulose (CMC ) and salts thereof, for example, CMC sodium, natural gums such as karaya, xanthan, gum arabic and tragacanth, colloidal magnesium aluminum silicate, colloidal silica and the like. A preferred class of thickening and gelling agents includes a class of acrylic acid homopolymers cross-linked with an alkyl ether of pentaerythritol or an alkyl ether of sucrose or carbomers. Carbomers are commercially available from B.F. Goodrich as the Carbopol® series. Particularly preferred carbopols include Carbopol 934, 940, 941, 956, 974P and mixtures thereof. Silica thickeners such as DT 267 (from PPG Industries) can also be used. One or more thickening agents are optionally present in a total amount of from about 0.01% by weight to 15% by weight, for example from about 0.1% by weight to about 10% by weight or from about 0 , 2% by weight to about 5% by weight, based on the total weight of the composition.
    [045] The compositions may comprise at least one viscosity modifier, useful for example to help inhibit fixation or separation of ingredients or to promote redispersibility by stirring a liquid composition. Any orally acceptable viscosity modifier can be used, including without limitation, mineral oil, petrolatum, clays and organomodified clays and the like. One or more viscosity modifying agents are optionally present in a total amount of about 0.01% by weight to about 10% by weight, for example, from about 0.1% by weight to about 5% by weight , by the total weight of the composition.
    [046] The compositions can also comprise at least one humectant. Any orally acceptable humectant can be used, including without limitation, polyhydric alcohols such as glycerin, sorbitol (optionally as a 70% by weight solution in water), xylitol or low molecular weight polyethylene glycols (PEGs). Most humectants also work as sweeteners. One or more humectants are optionally present in a total amount of about 1% by weight to about 70% by weight, for example, from about 1% by weight to about 50% by weight, from about 2% by weight. weight at about 25% by weight or from about 5% by weight to about 15% by weight, by the total weight of the composition.
    [047] Oral care compositions may comprise at least one sweetener, useful for example to improve the taste of the composition. One or more sweeteners are optionally present in a total amount depending heavily on the particular sweetener (s) selected, but typically 0.005% by weight to 5% by weight, by the total weight of the composition, optionally 0.005% by weight at 0.2% by weight, also optionally 0.05% by weight at 0.1% by weight, by the total weight of the composition.
    [048] The compositions may also comprise a flavoring agent, useful for example to improve the taste of the composition. Any natural or synthetic orally acceptable flavoring can be used, including without limitation aromas of tea, vanilla, sage, marjoram, parsley oil, mint oil, cinnamon oil, wintergreen oil (methylsalicylate), mint oil, clove oil , bay oil, anise oil, eucalyptus oil, citrus oils, oils and fruit essences including those derived from lime, orange, lemon, grapefruit, apricot, banana, grape, apple, strawberry, cherry, pineapple, etc., flavors derived from grains and dried fruits such as coffee, cocoa, peanuts, almonds, etc., absorbed and encapsulated flavorings and the like. Also included within the flavorings of this document are ingredients that provide fragrance and / or sensory effect in the mouth, including refreshing or stimulating effects. Said ingredients include illustratively menthol, menthyl acetate, menthol lactate, camphor, eucalyptus oil, eucalyptol, anethole, eugenol, cassia, oxanone, α-irinone, guaietol propylene, thymol, linalool, benzaldehyde, cinnamaldehyde, N- ethyl-p-mentan-3-carboxamine, N, 2,3-trimethyl-2-isopropylbutanamide, 3- (1-menthoxy) -propane-1,2-diol, cinnamaldehyde glycerol acetal (GCA), menthol glycerol acetal (MGA ) and the like. One or more flavorants are optionally present in a total amount of from about 0.01% by weight to about 5% by weight, for example, from about 0.03% by weight to about 2.5% by weight, optionally from about 0.05% by weight to about 1.5% by weight, also optionally from about 0.1% by weight to about 0.3% by weight, by the total weight of the composition.
    [049] The compositions can comprise at least one dye. The dyes in this document include pigments, inks, red inks and agents that provide a particular shine or reflectivity such as pearlescent agents. Any orally acceptable dye can be used, including without limitation talc, mica, magnesium carbonate, magnesium silicate, magnesium aluminum silicate, titanium dioxide, red, yellow, brown and black iron oxides, ferric ammonium ferrocyanide, violet manganese, overseas, titanium mica, bismuth oxychloride and the like. One or more dyes are optionally present in a total amount of from about 0.001% by weight to about 20% by weight, for example, from about 0.01% by weight to about 10% by weight or from about 0 , 1% by weight to about 5% by weight, based on the total weight of the composition.
    [050] The compositions can also comprise an additional antibacterial agent or preservative, such as chlorhexidine, trichlanosane, quaternary ammonium compounds (e.g., benzalkonium chloride), or parabens such as methylparaben or propylparaben. One or more additional antibacterial agents or preservatives can optionally be present in the composition in a total amount of about 0.01% by weight to about 0.5% by weight, optionally from about 0.05% by weight to about 0.1% by weight, based on the total weight of the composition.
    [051] Oral care compositions can also comprise a source of fluoride ions. Sources of fluoride ion include, but are not limited to: stannous fluoride, sodium fluoride, potassium fluoride, potassium monofluorophosphate, sodium monofluorophosphate, ammonium monofluorophosphate, sodium fluorosilicate, ammonium fluorosilicate as amurine fluoride (N'- octadecyltrimethylenediamine-N, N, N'-tris (2-ethanol) - dihydrofluoride), ammonium fluoride and combinations thereof. In certain embodiments, the fluoride ion source includes stannous fluoride, sodium fluoride, amine fluorides, sodium monofluorophosphate, as well as mixtures thereof. In certain embodiments, the oral care composition may also contain a source of fluoride ions or an ingredient that supplies fluoride in sufficient quantities to supply about 50 to about 5000 ppm of fluoride ion, for example, from about 100 to about 1000 , from about 200 to about 500 or about 250 ppm of fluoride ion. Fluoride ion sources can be added to the compositions at a level of about 0.001% by weight to about 10% by weight, for example, from about 0.003% by weight to about 5% by weight, 0.01% by weight to about 1% by weight, or from about 0.05% by weight. However, it should be understood that the weights of fluoride salts to provide the appropriate level of fluoride ion will obviously vary based on the weight of the counterion in the salt and one skilled in the art can readily determine said amounts. A preferred fluoride salt can be sodium fluoride.
    [052] The compositions may comprise a saliva stimulating agent useful, for example, in improving dry mouth. Any orally acceptable saliva stimulating agent can be used, including without limitation food acids such as citric, lactic, malic, succinic, ascorbic, adipic, fumaric and tartaric acids and mixtures thereof. One or more saliva stimulating agents are optionally present in a total amount effective for saliva stimulation.
    [053] The compositions can include anti-sensitivity agents, for example, potassium salts such as potassium nitrate, potassium bicarbonate, potassium chloride, potassium citrate and potassium oxalate; capsaicin; eugenol; strontium salts; chloride salts and combinations thereof. Said agents can be added in effective amounts, for example, from about 1% by weight to about 20% by weight based on the total weight of the composition, depending on the agent chosen.
    [054] The composition can also comprise an antioxidant. An orally acceptable antioxidant can be used, including butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), vitamin A, carotenoids, vitamin E, flavonoids, polyphenols, ascorbic acid, herbal antioxidants, chlorophyll, melatonin and mixtures thereof. Examples
    [055] The experiments were carried out in order to evaluate the effectiveness of the biofilm reduction of compositions containing different concentrations of arginine.
    [056] In all Examples, below, the methodology used was the University of Manchester biofilm growth inhibition model. The protocol for this model is as follows: (1) the plaque was collected from four healthy volunteers and grouped together as an inoculum. The optical density of the inoculum was equal to 0.3 absorbance at 610 nm; (2) sterile hydroxyapatite (PAH) discs were incubated under anaerobic conditions at 37 ° C for 24 hours with 1 ml of artificial sterile saliva (with 0.01% by weight of sucrose) and 1 ml of saliva grouped in a microplate 24 wells; (3) for each test toothpaste (and for each control) a treatment solution of 1 part of toothpaste: 2 parts of sterile water by weight was prepared. Each freshly prepared treatment solution was added to three wells and allowed to come in contact with the PAH disk in it for 10 minutes; (4) the liquid phase of each well was then removed and replaced with 2 mL of sterile artificial saliva; (5) the discs were then kept at 37 ° C under anaerobic conditions for 8 days; (6) at intervals of 2.4 and 8 days, the discs were collected aseptically and transferred to pre-reduced thioglycolate medium (4.5 ml per disc); (7) 100 μl of the dilution, 10-4, 10-5 and 10-6 were plated in duplicate for each disc on Neomycin / Vancomycin Agar (NV) for total gram-negative anaerobes; (8) The plates were spread over the surface using a sterile distributor and were incubated anaerobically at 37 ° C for 72 hours, after which the number of colonies on each plate was counted.
    [057] The log10 CFU / ml (where CFU = colony forming units) for each test or control toothpaste was calculated. A lower log10 CFU / ml indicates that the tested toothpaste is more effective in inhibiting biofilm growth.
    [058] The test results are shown in Example 1, below. Example 1
    [059] In the first cycle of biofilm reduction tests, formulations such as those listed in Table 1 were evaluated for their ability to reduce biofilm growth. The results obtained using the University of Manchester Biofilm Growth Inhibition methodology (above) are shown in Table 1, with the average log10 CFU / ml obtained from the disk incubated for 8 days in step 6 of the method. In the results below, formulas that share the same letter for “statistical significance” do not show a significant difference in their biofilm reduction effectiveness.
    [060] Table 1


    [061] The results as shown in Table 1 showed that the formulas containing arginine improved the effectiveness in reducing biofilm. As shown in Table 1, above, the formula containing 1.5 wt% arginine outperformed all other tested formulas, as indicated by a significantly lower value of Log10 CFU / ml mean. This was followed by the formula with 1.0% by weight of arginine and then by the formulas containing 0.5% by weight and 3.0% by weight of arginine.
    权利要求:
    Claims (14)
    [0001]
    1. Composition for oral care, characterized by the fact that it comprises: a. arginine, in free or salt form; and b. zinc oxide and zinc citrate, in which arginine is present in an amount of 1% by weight to 2.25% by weight, based on the total weight of the composition.
    [0002]
    2. Oral care composition according to claim 1, characterized by the fact that arginine is present in an amount of 1.17% by weight to 2.25% by weight, based on the total weight of the composition.
    [0003]
    3. Oral care composition according to claim 2, characterized by the fact that arginine is present in an amount of 1.4% by weight to 1.6% by weight, based on the total weight of the composition.
    [0004]
    4. Oral care composition according to claim 3, characterized by the fact that arginine is present in an amount of 1.5% by weight, based on the total weight of the composition.
    [0005]
    5. Oral care composition according to any of the preceding claims, characterized by the fact that the total concentration of zinc salts in the composition is 0.2% by weight to 5% by weight, based on the total weight of the composition .
    [0006]
    6. Oral care composition according to any of the preceding claims, characterized in that the molar ratio of arginine to total zinc salts is 0.05: 1 to 10: 1.
    [0007]
    7. Oral care composition according to any one of the preceding claims, characterized in that the composition comprises zinc oxide in an amount of 0.5% by weight to 1.5% by weight and zinc citrate in a amount from 0.25% by weight to 0.75% by weight, based on the total weight of the composition.
    [0008]
    8. Oral care composition according to claim 7, characterized in that the composition comprises zinc oxide in an amount of 1% by weight and zinc citrate in an amount of 0.5% by weight, based on in the total weight of the composition.
    [0009]
    9. Oral care composition according to claim 6, characterized by the fact that the weight ratio of zinc oxide to zinc citrate is 1.5: 1 to 4.5: 1, optionally 1.5: 1 to 4: 1; 1.7: 1 to 2.3: 1; 1.9: 1 to 2.1: 1 or 2: 1.
    [0010]
    10. Oral care composition according to any one of the preceding claims, characterized in that it comprises a source of fluoride ion selected from stannous fluoride, sodium fluoride, potassium fluoride, potassium monofluorophosphate, sodium monofluorophosphate, ammonium monofluorophosphate , sodium fluorosilicate, ammonium fluorosilicate, amine fluoride, ammonium fluoride and combinations thereof.
    [0011]
    11. Oral care composition according to claim 10, characterized in that the source of fluoride ion comprises stannous fluoride.
    [0012]
    12. Oral care composition according to claim 10, characterized by the fact that the fluoride ion source is present in the composition in an amount ranging from 0.01% to 1% by weight of the composition.
    [0013]
    13. Oral care composition for use in reducing or inhibiting biofilm formation in an oral cavity, characterized by the fact that the oral care composition is to be contacted with the oral cavity, where the oral care composition is as defined in any of claims 1 to 12.
    [0014]
    14. Use of a combination of: a. arginine, in free or salt form; and b. zinc oxide and zinc citrate; characterized by the fact that it is in the preparation of an oral care composition as defined in claim 1 to reduce or inhibit biofilm formation in an oral cavity.
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    同族专利:
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    IL245796A|2019-02-28|
    US20200009031A1|2020-01-09|
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    PL3082724T3|2019-01-31|
    PH12016501033B1|2016-07-04|
    MX2016007543A|2016-10-04|
    EP3082724B1|2018-08-15|
    ES2696448T3|2019-01-15|
    PH12016501033A1|2016-07-04|
    US11260002B2|2022-03-01|
    BR112016013333A2|2018-06-26|
    JP2017500324A|2017-01-05|
    RU2676679C1|2019-01-10|
    AR098885A1|2016-06-22|
    IL245796D0|2016-07-31|
    CN104721226A|2015-06-24|
    MX364540B|2019-04-30|
    EP3082724A1|2016-10-26|
    CL2016001547A1|2017-02-03|
    KR20160098260A|2016-08-18|
    WO2015094849A1|2015-06-25|
    US10441517B2|2019-10-15|
    ZA201602589B|2020-02-26|
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    法律状态:
    2019-08-13| B06U| Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]|
    2020-06-16| B06A| Patent application procedure suspended [chapter 6.1 patent gazette]|
    2020-09-24| B09A| Decision: intention to grant [chapter 9.1 patent gazette]|
    2020-12-15| B16A| Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]|Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 10/12/2014, OBSERVADAS AS CONDICOES LEGAIS. |
    优先权:
    申请号 | 申请日 | 专利标题
    CN201310703017.9A|CN104721226B|2013-12-19|2013-12-19|Oral care compositions|
    CN201310703017.9|2013-12-19|
    PCT/US2014/069486|WO2015094849A1|2013-12-19|2014-12-10|Oral care composition|
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