Oral composition and dentin protective agent

Abstract

An oral composition and a dentin protective agent according to the present disclosure are characterized by containing calcium silicate having an Si / Ca ratio of 1.15 to 2.3.

Description

Oral composition and dentin protective agent

[0001] The present disclosure relates to oral compositions and dentin protective agents.

[0002] Generally, dental caries occurs when bacteria in dental plaque on the tooth surface metabolize sugars in food and drink to produce acid, which decalcifies hydroxyapatite in the enamel and dentin. For example, oral compositions disclosed in Patent Document 1 have been known. This oral composition contains (A) a pharmacologically acceptable zinc compound and (B) a pharmacologically acceptable aldehyde compound. This oral composition effectively prevents dental caries by effectively inhibiting mineral elution from tooth tissue and maintaining the acid resistance of the enamel, dentin, etc.

[0003] Japanese Patent Application Publication No. 11-228368

[0004] In recent years, the risk of root caries and tooth sensitivity due to exposed dentin caused by gingival recession has become a particular problem for the elderly. Dentin erosion is caused by the demineralization of hydroxyapatite and the breakdown of collagen, an organic substance contained in dentin. It is difficult to prevent dentin erosion using conventional demineralization prevention techniques alone. Therefore, effective protection of dentin has been sought.

[0005] As a result of research aimed at solving the above-mentioned problems, the present inventors have newly discovered that calcium silicate having a specific Si / Ca ratio exhibits excellent dentin protection. Various aspects for solving the above-mentioned problems will be described below.

[0006] The oral composition of Aspect 1 is characterized by containing calcium silicate having a Si / Ca ratio of 1.15 or more and 2.3 or less. Aspect 2 is the oral composition of Aspect 1 for protecting dentin.

[0007] The dentin protective agent of aspect 3 is characterized by containing calcium silicate having a Si / Ca ratio of 1.15 or more and 2.3 or less.

[0008] The oral composition and dentin protective agent of the present disclosure can exert an excellent protective effect on dentin.

[0009]

[0033] The oral composition and dentin protective agent according to the present disclosure are described below in detail. Since the oral composition and dentin protective agent contain similar components, only the dentin protective agent will be described below.

[0010] In the present disclosure, the oral composition refers to a composition intended primarily for use in the oral cavity. The oral composition of the present disclosure includes not only oral preparations that are expelled from the oral cavity after use, but also ingestible foods and beverages. The dentin protective agent is not limited to those intended for use in the oral cavity.

[0011] The dentin protective agent contains calcium silicate having a Si / Ca ratio of 1.15 or more and 2.3 or less. The components constituting the dentin protective agent will be described below.

[0012] <Calcium silicate> Calcium silicate is a compound of calcium oxide (CaO) and silicon dioxide (SiO ２ ), water, etc. are bonded in various combinations, and x(CaO)·y(SiO ２ ) z (H ２ In the dentin protective agent of the present disclosure, calcium silicate having a Si / Ca ratio within a predetermined range is used as a raw material.

[0013] The Si / Ca ratio of calcium silicate is 1.15 or more and 2.3 or less. The upper limit of the Si / Ca ratio of calcium silicate is preferably 2.2, more preferably 2.1. The lower limit of the Si / Ca ratio of calcium silicate is preferably 1.2, more preferably 1.3. The upper or lower limit of this range may be, for example, 1.15, 1.2, 1.25, 1.3, 1.35, 1.4, 1.45, 1.5, 1.55, 1.6, 1.65, 1.7, 1.75, 1.8, 1.85, 1.9, 1.95, 2.0, 2.05, 2.1, 2.15, 2.2, 2.25, or 2.3.

[0014] The Si / Ca ratio of calcium silicate can be measured using energy dispersive X-ray spectroscopy (SEM-EDX). More specifically, the Si / Ca ratio of calcium silicate used as a raw material is measured by the following method.

[0015] (1) Affix conductive carbon tape to the sample stage and sprinkle calcium silicate on it. (2) Remove excess powder with a blower and perform elemental analysis using energy dispersive X-ray spectroscopy (SEM-EDX).

[0016] (3) Each sample is measured four times, and the average Si / Ca ratio is calculated from the number of Si and Ca atoms. The Si / Ca ratio of calcium silicate can be adjusted appropriately by changing the ratio of silicon dioxide and calcium oxide that make up the molecule.

[0017] The average particle size (D50) of calcium silicate determined by a wet laser diffraction scattering method is not particularly limited, and is, for example, 5 μm or more and 35 μm or less.

[0018] The upper or lower limit of the range may be, for example, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, or 35 μm.

[0019] The degree of aggregation of calcium silicate is not particularly limited. For example, the degree of aggregation of calcium silicate is 0.5% or more and 15% or less. The upper or lower limit of this range may be, for example, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 6.5, 7, 7.5, 8, 8.5, 9, 9.5, 10, 10.5, 11, 11.5, 12, 12.5, 13, 13.5, 14, 14.5, or 15%.

[0020] The degree of aggregation of calcium silicate is determined by the following method using a sieve: The powder is placed on the top sieve of a three-stage sieve shown in Table 1 below, and is vibrated for a predetermined time and with a predetermined strength. The amount of powder that has formed clumps due to the vibration is calculated using the following formula.

[0021] If most of the measured particle size of the calcium silicate sample is smaller than the mesh size of the sieve (lower row) described below, a standard sieve is used, and the sample is vibrated for a specified time and strength, and the degree of aggregation is evaluated from the amount of sample charged and the amount remaining on the sieve.

[0022]

[0023] Coagulation degree (%) = (amount remaining on top sieve / amount of sample added + amount remaining on middle sieve / amount of sample added × 3 / 5 + amount remaining on bottom sieve / amount of sample added × 1 / 5) × 100. The content of calcium silicate in the dentin protective agent is not particularly limited. The content of calcium silicate is, for example, 0.1% by mass or more and 20% by mass or less.

[0024] The upper or lower limit of the range may be, for example, 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20% by weight.

[0025] <Other Components> The dentin protective agent may contain other components in addition to the components described above, depending on the intended application, form, use, etc., such as medicinal ingredients, surfactants, abrasives, humectants, thickeners, stabilizers, preservatives, sweeteners, pH adjusters, antioxidants, flavorings, colorants, etc. As each of these components, known components that are incorporated into dentin protective agents can be used. These components may be used alone or in combination of two or more.

[0026] Examples of the medicinal ingredient include a bactericide, a blood circulation promoter, an anti-inflammatory agent, a bleeding improving agent, a tissue repair agent, a remineralizing agent, a hypersensitivity suppressant, etc. Specific examples of the medicinal ingredient include bactericides such as anionic bactericides such as sodium cocoyl sarcosinate and sorbic acid, cationic bactericides such as chlorhexidine hydrochloride, chlorhexidine gluconate, benzalkonium chloride and benzethonium chloride, amphoteric bactericides such as dodecyldiaminoethylglycine, halogenated diphenyl ethers such as triclosan (2',4,4'-trichloro-2-hydroxy-diphenyl ether), phenolic bactericides such as isopropylmethylphenol, and hinokitiol.

[0027] Examples of blood circulation promoters include vitamin E compounds such as dl-α-tocopherol acetate, tocopherol succinate, and tocopherol nicotinate, and enzymes such as dextranase, amylase, protease, mutanase, lysozyme, and bacteriolytic enzyme (retic enzyme).

[0028] Examples of anti-inflammatory agents include epsilon aminocaproic acid, dipotassium glycyrrhizinate, β-glycyrrhetinic acid, etc. Examples of anti-bleeding agents include tranexamic acid, ascorbic acid, etc.

[0029] Examples of tissue repair agents include allantoin, etc. Examples of remineralizing agents include fluorine compounds such as sodium fluoride, etc. Examples of dentin hypersensitivity inhibitors include nitrates (potassium nitrate), aluminum lactate, hydroxyapatite, tin fluoride, arginine, etc.

[0030] Other examples include plant extracts extracted with water-soluble solvents, chlorophyll, sodium chloride, zinc chloride, potassium nitrate, etc. Specific examples of surfactants include nonionic surfactants, anionic surfactants, cationic surfactants, and amphoteric surfactants.

[0031] Specific examples of nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters and maltose fatty acid esters, sugar alcohol fatty acid esters such as maltitol fatty acid esters, sorbitan fatty acid esters such as sorbitan stearate and sorbitan monolaurate, polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan laurate (also called polysorbate 20), polyoxyethylene sorbitan stearate (also called polysorbate 60), and polyoxyethylene sorbitan oleate (also called polysorbate 80), fatty acid alkanolamides such as lauric acid diethanolamide, polyoxyethylene sorbitan oleate (also called polysorbate 8 ... Examples of suitable olefin stearyl ethers include polyoxyethylene alkyl ethers such as polyoxyethylene oleyl ether, polyethylene glycol fatty acid esters such as polyethylene glycol monooleate and polyethylene glycol monolaurate, alkyl glycosides such as lauryl glycoside and decyl glycoside, polyglycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, polyoxyethylene fatty acid esters, alkyl glucosides, polyoxyethylene hydrogenated castor oil (those with an average number of moles of ethylene oxide added of 10, 20, 40, or 60), glycerin fatty acid esters, and polyoxyethylene propylene block copolymers.

[0032] Specific examples of anionic surfactants include sulfate ester salts such as sodium lauryl sulfate and polyoxyethylene lauryl ether sodium sulfate, sulfosuccinates such as sodium lauryl sulfosuccinate and polyoxyethylene lauryl ether sodium sulfosuccinate, acylamino acid salts such as sodium cocoyl sarcosine and sodium lauroyl methyl alanine, and sodium cocoyl methyl taurate.

[0033] Specific examples of cationic surfactants include quaternary alkylammonium salts such as cocoyl arginine ethyl PCA, cetyltrimethylammonium chloride, distearyldimethylammonium chloride, stearyldimethylbenzylammonium chloride, and stearyltrimethylammonium chloride, and chlorhexidine gluconate.

[0034] Specific examples of amphoteric surfactants include amino acid amphoteric surfactants such as N-lauryldiaminoethylglycine and N-myristyldiethylglycine, and betaine amphoteric surfactants such as alkyldimethylaminoacetic acid betaine, N-alkyl-N'-carboxymethyl-N'-hydroxyethylethylenediamine salt, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, and cocamidopropyl betaine.

[0035] Specific examples of abrasives include calcium carbonate, calcium phosphate, dibasic calcium phosphate, calcium pyrophosphate, insoluble sodium metaphosphate, titanium oxide, amorphous silica, crystalline silica, abrasive silica, thickening silica, aluminosilicate, aluminum oxide, titanium oxide, aluminum hydroxide, resin, etc. The above-mentioned silica is also called silicic anhydride.

[0036] Specific examples of humectants include propylene glycol, glycerin, sorbitol, polyethylene glycol, 1,3-butylene glycol, water, and alcohol.

[0037] Specific examples of thickeners include sodium polyacrylate, carrageenan, sodium carboxymethylcellulose, sodium alginate, xanthan gum, hydroxyethyl cellulose, crystalline cellulose, hydroxypropylmethylcellulose, methylcellulose, propylene glycol alginate, etc. Thickeners are also called binders.

[0038] Specific examples of stabilizers include sodium edetate, sodium thiosulfate, sodium sulfite, calcium lactate, lanolin, triacetin, castor oil, magnesium sulfate, and the like.

[0039] Specific examples of preservatives include 1,2-dibromo-2,4-dicyanobutane, photosensitizers, isothiazolone derivatives, hydantoin derivatives, parabens, sodium benzoate, and phenol.

[0040] Specific examples of sweeteners include saccharin, saccharin sodium, acesulfame potassium, stevia extract, palatinose, palatinit, erythritol, maltitol, xylitol, and lactitol.

[0041] Specific examples of pH adjusters include citric acid, phosphoric acid, malic acid, pyrophosphoric acid, lactic acid, tartaric acid, glycerophosphoric acid, acetic acid, nitric acid, or chemically acceptable salts thereof, sodium hydroxide, and the like.

[0042] Specific examples of antioxidants include tocopherols, dibutylhydroxytoluene, butylhydroxyanisole, and gallic acid esters. The fragrance may be a natural fragrance or a synthetic fragrance. It may also be a single fragrance or a blended fragrance.

[0043] Specific examples of fragrances include 1-menthol, d-carvone, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate, citronellyl acetate, methyl eugenol, cineole, linalool, ethyl linalool, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, perilla oil, wintergreen oil, clove oil, eucalyptus oil, pimento oil, d-camphor, d-borneol, fennel oil, cinnamon oil, cinnamon aldehyde, peppermint oil, and vanillin.

[0044] Specific examples of colorants include legally designated dyes such as Green No. 1, Green No. 3, Blue No. 1, Yellow No. 4, Yellow No. 5, Red No. 102, and Red No. 3, copper chlorophine sodium, and titanium oxide.

[0045] <Application forms, dosage forms, and uses of the dentin protective agent and oral composition> The application forms of the dentin protective agent and oral composition are not particularly limited, and they can be used, for example, as pharmaceuticals, quasi-drugs, cosmetics, and foods.

[0046] The dosage form of the dentin protective agent and oral composition is not particularly limited, and can be in the form of an ointment, paste, spray, gel, liquid, suspension, gum, etc., by containing a solvent such as water, alcohol, or hydrocarbon.

[0047] The type of water used as a solvent is not particularly limited, and for example, distilled water, pure water, ultrapure water, purified water, tap water, etc. can be used. The type of alcohol used as a solvent is not particularly limited, and for example, ethanol can be used. A mixture of water and alcohol can also be used. The type of hydrocarbon used as a solvent is not particularly limited, and for example, gelled hydrocarbon, paraffin, squalane, etc. can be used.

[0048] The dentin protective agent and oral composition can be used for any known purpose, as appropriate, including, for example, a masticatory agent, an oral dissolving agent, an oral disintegrating agent, a tongue care agent, a mouth freshener, a toothpaste, a mouthwash, a gargle, a liquid dentifrice, a biofilm dispersant, an agent for preventing bad breath, a gum massage agent, an oral moisturizing agent, a tongue coating remover, an oral application agent, an oral disinfectant, a throat disinfectant, an oral throat agent, a periodontal disease treatment agent, a denture wearing agent, a denture coating agent, a denture stabilizer, a denture preservative, a denture cleaner, and an implant care agent.

[0049] <Effects of the present embodiment> The dentin protective agent and oral composition exhibit excellent dentin protective effects due to the above-mentioned components. More specifically, the caries prevention effect can be improved by improving the dentin demineralization inhibition rate. Furthermore, the hypersensitivity prevention effect can be improved by improving the dentin tubule occlusion rate.

[0050] <Effects of this embodiment> The effects of the dentin protective agent and oral composition of this embodiment will be described. (1) The dentin protective agent and oral composition of this embodiment contain calcium silicate as the calcium silicate raw material, with a Si / Ca ratio of 1.15 or more and 2.3 or less. Therefore, the protective effect of dentin can be improved. This results in improved effects of improving the acid resistance of dentin, caries prevention, and hypersensitivity prevention. In particular, in elderly people, root caries and hypersensitivity of dentin exposed by gingival recession can be prevented.

[0051] (2) Conventionally, fluoride has been commonly used to prevent dental caries and hypersensitivity, but fluoride is less effective on dentin due to its structural characteristics, and sufficient effects have not been achieved. The dentin protective agent and oral composition of the present embodiment can improve the caries prevention effect and hypersensitivity prevention effect without relying on fluoride.

[0052] <Other Examples of the Present Embodiment> The above-described embodiment can be modified as follows: The present embodiment and the following modified examples can be combined with each other within the scope of technical compatibility.

[0053] The dentin protective agent and oral composition of this embodiment may be applied to domestic animals other than humans, such as pets and livestock.

[0054] Examples will be provided below to more specifically describe the configuration and effects of the present disclosure, but the present disclosure is not limited to these examples. The dentin protective agents of Examples 1 and 2 and Comparative Examples 1 to 3 shown in Table 2 were produced according to conventional methods. Specifically, calcium silicate having the Si / Ca ratio shown in Table 2 was dissolved in water to a concentration of 10% by mass to prepare aqueous solutions of the dentin protective agents. The Si / Ca ratios of calcium silicate in Table 2 were measured using the energy dispersive X-ray spectroscopy (SEM-EDX) described above, and represent the average of four measurements for each sample. For reference, the maximum and minimum measured values ​​of the Si / Ca ratios of the calcium silicate used in Examples 1 and 2 are shown.

[0055] (Evaluation Test) The dentin protective effect of the dentin protective agents of Examples 1 and 2 and Comparative Examples 1 to 3 was evaluated by measuring the dentinal tubule sealing ability and demineralization inhibitory ability using the methods described below. The evaluation methods and evaluation results are shown below.

[0056] (Brushing treatment and dentinal tubule occlusion test) (1) Dentin from the root surface of an extracted bovine tooth was excised and embedded in resin (polymethyl methacrylate), and then polished with waterproof abrasive paper to expose the surface, creating a bovine tooth block.

[0057] (2) The bovine tooth block is immersed in a 2% (w / w) citric acid solution for 2 minutes. (3) After immersion in distilled water, it is subjected to ultrasonic treatment. (4) A part of the tooth surface is covered with varnish to make it a healthy surface.

[0058] (5) Using a brushing machine, brush for 30 seconds in the sample solution (*1). *1: Sample solution (aqueous solution containing 10% (w / w) calcium silicate, 0.5% (w / w) sodium carboxymethylcellulose, and 10% (w / w) glycerin). (6) Lightly wash the surface with distilled water and immerse in artificial saliva (*2) (8 hours, 37°C).

[0059] *2: Artificial saliva (CaCl ２ : 1.5mM, KH ２ P.O. ４ : 0.9 mM, KCl: 130 mM, HEPES: 20 mM, pH 7.0 (KOH)) (7) Wash the surface with distilled water.

[0060] (8) Brush the surface in the sample solution for 30 seconds using a brushing machine. (9) Lightly rinse the surface with distilled water and immerse it in artificial saliva (16 hours, 37°C). (10) Rinse the surface with distilled water.

[0061] (The above steps (5) to (10) are repeated twice.) (11) After removing the varnish, the sample surface is observed using a laser microscope at the same magnification to determine the number of unoccluded dentinal tubules. The dentinal tubule occlusion rate is calculated using the following formula.

[0062] Dentinal tubule occlusion rate (%) = {[Number of dentinal tubules (healthy surface)] - [Number of dentinal tubules (treated surface)] / [Number of dentinal tubules (healthy surface)]} x 100 The effectiveness of dentinal tubule occlusion was evaluated according to the following criteria. The results are shown in Table 2.

[0063] 3: When the dentinal tubule occlusion rate is more than 70% 2: When the dentinal tubule occlusion rate is more than 50% and 70% or less 1: When the dentinal tubule occlusion rate is 50% or less (Decalcification Inhibition Test) Samples after brushing treatment in the dentinal tubule occlusion test were used.

[0064] (1) A portion of the tooth surface is covered with varnish to create a healthy surface. (2) The tooth is immersed in a decalcifying solution (0.87 M citric acid solution, pH 1.36) for 2 hours. (3) After removing the varnish, the surface is lightly washed with distilled water, and the difference in level with the reference surface is measured using a laser microscope. The decalcification inhibition rate is calculated using the following formula.

[0065] Decalcification inhibition rate (%) = {[step (healthy surface)] - [step (treated surface)] / [step (healthy surface)]} x 100 The effectiveness of decalcification inhibition was evaluated according to the following criteria. The results are shown in Table 2.

[0066] 3: Decalcification inhibition rate exceeds 70% 2: Decalcification inhibition rate exceeds 50% and is 70% or less 1: Decalcification inhibition rate is 50% or less

[0067]

[0068] (Evaluation Results) As can be seen from Table 2, in each of the comparative examples, the dentinal tubule occlusion rate was 50% or less. In contrast, in each of the examples, the dentinal tubule occlusion rate exceeded 50%. Furthermore, in each of the examples, the decalcification inhibition rate exceeded 70%. Therefore, it was confirmed that the configurations of each example provided particularly excellent dentin protection effects.

[0069] (Additional Notes) Next, the technical ideas that can be understood from the above-mentioned embodiments and other examples will be additionally described. (a) An oral composition or dentin protective agent, characterized in that it contains calcium silicate having a Si / Ca ratio of 1.2 or more and 2.2 or less.

[0070] (b) The oral composition or dentin protective agent used for preventing dentin caries or dentin hypersensitivity.

Claims

1. An oral composition comprising calcium silicate having a Si / Ca ratio of 1.15 or more and 2.3 or less.

2. The oral composition according to claim 1, which is for protecting dentin.

3. A dentin protective agent characterized by containing calcium silicate having a Si / Ca ratio of 1.15 or more and 2.3 or less.

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