Oral components

Abstract

To provide oral compositions that have a high sealing property against dentinal tubules and can sufficiently prevent hyperesthesia.SOLUTION: An oral composition according to the present invention is characterized by containing aluminum lactate, and a dicarboxylic acid compound having 4 or more carbon atoms and no hydroxy group. Further, in the oral composition according to the present invention, the dicarboxylic acid compound preferably has 4 to 6 carbon atoms. Further, in the oral composition according to the present invention, the dicarboxylic acid compound is preferably at least one selected from the group consisting of glutamic acids, succinic acids, adipic acids, fumaric acids and alkali metal salts of these acids.SELECTED DRAWING: Figure 1

Description

Technical Field

[0001] The present invention relates to an oral composition.

Background Art

[0002] Tooth hypersensitivity is a symptom that occurs when the gums recede due to periodontal disease, aging, excessive brushing, etc., and the dentin of the tooth is exposed. When the exposed dentin is stimulated by heat, etc., an unpleasant pain occurs.

[0003] As a technique for preventing tooth hypersensitivity symptoms, a method of alleviating pain transmission and a method of physically blocking open dentinal tubules are known. As a method of physically blocking open dentinal tubules, a method of physically blocking dentinal tubules using aluminum lactate to alleviate tooth hypersensitivity symptoms is known (for example, Patent Document 1). Patent Document 1 discloses an oral composition in which the addition of sodium oxalate to aluminum lactate enhances the sealing property against dentinal tubules.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] However, in conventional oral compositions, the sealing property against dentinal tubules is not sufficient, and it has been difficult to sufficiently prevent tooth hypersensitivity. Therefore, an object of the present invention is to provide an oral composition having a high sealing property against dentinal tubules and capable of sufficiently preventing tooth hypersensitivity.

Means for Solving the Problems

[0006] The oral composition according to the present invention comprises aluminum lactate and It comprises at least one dicarboxylic acid compound selected from the group consisting of glutamic acid, succinic acid, adipic acid, and fumaric acid, The amount of aluminum lactate used is 0.01 to 5% by mass. The amount of the dicarboxylic acid compound is 0.1 to 1% by mass. Furthermore, in the oral composition according to the present invention, it is preferable that the dicarboxylic acid compound is glutamic acid. The oral composition according to the present invention is preferably a dentinal tubule suffocating agent. The oral composition according to the present invention is preferably a toothpaste. [Effects of the Invention]

[0007] According to the present invention, it is possible to provide an oral composition that has high sealing properties for dentinal tubules and can sufficiently prevent hypersensitivity. [Brief explanation of the drawing]

[0008] [Figure 1] This is an electron microscope image showing the state of dentinal tubules in the evaluation method using the oral composition of Example 1. [Figure 2] This is an electron microscope image showing the state of dentinal tubules in the evaluation method using the oral composition of Comparative Example 1. [Figure 3] This is an electron microscope image showing the state of dentinal tubules in the evaluation method using the oral composition of Comparative Example 2.

[0009] Preferred embodiments of the oral composition of the present invention will be described in detail below. In this specification, the oral composition includes toothpastes such as toothpaste paste, powder toothpaste, liquid toothpaste, and liquid toothpaste, as well as lozenges, tablets, creams, ointments, patches, mouthwashes, and chewing gum. Among these, the oral composition of the present invention is preferably applied to toothpaste. Furthermore, the oral composition of the present invention is preferably used as a dentinal tubule suffocating agent.

[0010] The oral composition of the present invention comprises aluminum lactate and a dicarboxylic acid compound having four or more carbon atoms and lacking a hydroxyl group. By including these components, the dentinal tubules can be effectively sealed, and hypersensitivity can be adequately prevented.

[0011] (aluminum lactate) Aluminum lactate is a medicinal ingredient that has traditionally been included in toothpaste as an ingredient to prevent tooth sensitivity. In the oral composition of the present invention, the amount of aluminum lactate is not particularly limited, but is preferably 0.01 to 5% by mass, more preferably 0.1 to 4% by mass, and even more preferably 0.3 to 3% by mass. This allows for more effective sealing of dentinal tubules when used in combination with the dicarboxylic acid compound described later, while maintaining the stability of the formulation.

[0012] (Dicarboxylic acid compounds) The oral composition of the present invention contains a dicarboxylic acid compound. The dicarboxylic acid compound used in this invention has four or more carbon atoms and does not have a hydroxyl group. By using such a dicarboxylic acid compound in combination with aluminum lactate, it is possible to achieve high sealing performance for dentinal tubules. In this invention, the number of carbon atoms in the dicarboxylic acid compound is 4 or more, but more preferably 4 to 6. If the number of carbon atoms is less than the lower limit, the sealing effect of aluminum lactate on dentinal tubules cannot be sufficiently promoted.

[0013] Furthermore, in this invention, the dicarboxylic acid compound is a compound that does not have a hydroxyl group. However, if a dicarboxylic acid compound having a hydroxyl group is used, it may not be able to promote the sealing effect of aluminum lactate on dentinal tubules, and in some cases, it may even be inhibited. Also, the dicarboxylic acid compound is preferably an acidic amino acid. Thereby, the blocking property of aluminum lactate against dentinal tubules can be more effectively promoted. Examples of the acidic amino acid that can be used as the dicarboxylic acid compound of the present invention include glutamic acid, aspartic acid, and the like. Further, the dicarboxylic acid compound is preferably a chelating agent. Thereby, the blocking property of aluminum lactate against dentinal tubules can be more effectively promoted. Examples of the chelating agent that can be used as the dicarboxylic acid compound of the present invention include succinic acid, glutaric acid, adipic acid, glutamic acid, aspartic acid, fumaric acid, or alkali metal salts thereof.

[0014] Examples of the dicarboxylic acid compound having 4 or more carbon atoms and no hydroxy group include succinic acid, glutaric acid, adipic acid, glutamic acid, aspartic acid, fumaric acid, or alkali metal salts of these acids. Among these, as the dicarboxylic acid compound, it is preferable to use at least one selected from the group consisting of succinic acid, adipic acid, glutamic acid, fumaric acid, or alkali metal salts of these acids. Thereby, the blocking property of aluminum lactate against dentinal tubules can be more effectively promoted.

[0015] The blending amount of the dicarboxylic acid compound is preferably 0.001 to 5% by mass, more preferably 0.1 to 2% by mass, and even more preferably 0.3 to 1% by mass. Thereby, while maintaining the stability of the preparation, the blocking property of aluminum lactate against dentinal tubules can be more effectively promoted. Also, when the blending amount of aluminum lactate is 1, the blending amount of the dicarboxylic acid compound is preferably 0.0017 to 8.3, more preferably 0.17 to 3.3, and even more preferably 0.5 to 1.7. Thereby, the dentinal tubules can be more effectively blocked, and hypersensitivity can be sufficiently prevented.

[0016] (Other components) In addition to the above components, the oral composition of the present invention may contain, for example, abrasive agents, humectants, solvents, binders, flavors, excipients, sweeteners, pH adjusters, preservatives, emulsifiers, solubilizers, foaming agents, lubricants, surfactants, oils, pigments, antioxidants, and other drugs, etc., which can be appropriately formulated. These additives are commonly used in pharmaceutical compositions, oral compositions or food formulation design, and can be appropriately selected within the range that does not impair the effects of the present invention, and can be formulated in appropriate amounts. Examples of such additives include the following.

[0017] Examples of abrasive agents include silica-based abrasive agents such as silica gel, precipitated silica, pyrogenic silica, hydrated silicic acid, anhydrous silicic acid, zeolite, aluminosilicate, zirconosilicate, calcium hydrogen phosphate for toothpaste such as dicalcium phosphate dihydrate and dicalcium phosphate anhydride, calcium pyrophosphate, magnesium phosphate tribasic, tricalcium phosphate, aluminum hydroxide, alumina, light calcium carbonate, heavy calcium carbonate, magnesium carbonate, zirconium silicate, synthetic resin-based abrasive agents, etc. One or more of these can be used in combination.

[0018] Examples of humectants include glycerin, diglycerin, polyglycerin, 1,3-butylene glycol, polyethylene glycol, 1,2-pentanediol, 1,3-hexanediol, propylene glycol, dipropylene glycol, isopropylene glycol, polypropylene glycol, ethylene glycol, diethylene glycol, triethylene glycol, maltitol, reduced starch syrup, lactitol, palatinite, erythritol, sorbitol, mannitol, xylitol, xylose, trehalose, glucose, lactose, mannose, maltose, fructose, inositol, pentaerythritol, maltotriose, starch hydrolyzate, starch hydrolyzate reduced alcohol, and other polyhydric alcohols. One or more of these can be used in combination.

[0019] Preferred solvents include organic solvents such as alcohol and water, such as ethanol, propyl alcohol, and isopropyl alcohol. These solvents can be used individually or in combination of two or more.

[0020] Examples of binders include carrageenan (ι, λ, κ), alginic acid, sodium alginate, propylene glycol alginate, calcium-containing sodium alginate, potassium alginate, calcium alginate, ammonium alginate, and other alginates and their derivatives, xanthan gum, guar gum, agar, sodium carboxymethylcellulose, hydroxyethylcellulose, sodium polyacrylate, etc., and one or more of these can be used in combination.

[0021] Examples of fragrances include l-menthol, anethole, menthone, cineole, limonene, carvone, methyl salicylate, ethyl butyrate, eugenol, thymol, cinnamic aldehyde, and trans-2-hexenal, and one or more of these can be used in combination. These components may be blended individually, or essential oils containing them may be blended. In addition to the above fragrance components, other fragrance components such as aliphatic alcohols and their esters, terpene hydrocarbons, phenol ethers, aldehydes, ketones, and lactones, as well as essential oils, may be blended to the extent that they do not interfere with the effects of the present invention.

[0022] Examples of excipients include sucrose, lactose, starch, glucose, crystalline cellulose, mannitol, sorbitol, xylitol, erythritol, palatinitol, palatinose, maltitol, trehalose, lactitol, lactulose, reduced starch sugar, reduced isomaltoligosaccharide, coupling sugar, gum base, gum arabic, gelatin, cetyl methylcellulose, light anhydrous silicic acid, magnesium aluminate, calcium aluminometasilicate, sodium bicarbonate, and calcium phosphate.

[0023] Examples of sweeteners include sodium saccharin, aspartame, trehalose, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, and perillartin. One or more of these can be used in combination.

[0024] Examples of pH adjusting agents include citric acid, phosphoric acid, pantothenic acid, malic acid, pyrophosphate, lactic acid, tartaric acid, glycerophosphate, acetic acid, nitric acid, or chemically possible salts thereof such as disodium hydrogen phosphate, or sodium hydroxide. These can be used individually or in combination of two or more to ensure the pH of the composition is within an appropriate range.

[0025] Examples of preservatives include parahydroxybenzoic acid esters, benzoic acid and its salts, salicylic acid and its salts, sorbic acid and its salts, phenoxyethanol, alkyldiaminoethylglycine hydrochloride, etc., and one or more of these can be used in combination.

[0026] Examples of emulsifiers include polyoxyethylene alkyl ethers, polyoxyethylene fatty acid esters, polyoxyethylene sorbitan fatty acid esters, sorbitan fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, polyoxyethylene hydrogenated castor oil, sodium stearoyl lactylate, soybean phospholipids, and alkyltrimethylammonium chloride. Examples of solubilizing agents include esters, polyethylene glycol derivatives, polyoxyethylene hydrogenated castor oil, sorbitan fatty acid esters, and sulfated fatty alcohols.

[0027] Examples of foaming agents include sodium lauryl sulfate, sodium lauroyl sarcosinate, sodium alkyl sulfosuccinate, sodium coconut oil fatty acid monoglycerin sulfonate, sodium α-olefin sulfonate, N-acyl amino acid salts such as N-acyl glutamate, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, maltitol fatty acid esters, sucrose fatty acid esters, polyglycerin fatty acid esters, fatty acid diethanolamide, polyoxyethylene sorbitan monostearate, polyoxyethylene hydrogenated castor oil, and polyoxyethylene fatty acid esters. One or more of these can be used in combination. Examples of lubricants include magnesium stearate, sucrose fatty acid esters, talc, and hydrogenated oils. Examples of oils other than the essential oils used as antibacterial components and the oils used as fragrances include coconut oil, olive oil, sesame oil, peanut oil, parsley oil, parsley seed oil, and safflower oil.

[0028] Examples of surfactants include sodium lauryl sulfate, sodium α-olefin sulfonate, sodium dodecylbenzenesulfonate, sodium lauryl sulfoacetate, sodium N-lauroyl sarcosinate, N-acyl glutamate, sucrose fatty acid esters, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene block copolymer, alkyl glycosides, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, alkyldimethylamine oxide, lauryl ethanolamide, sodium cocoyl sarcosinate, and sodium N-lauroyl methyl taurate solution.

[0029] In addition to the ingredients mentioned above, the product may also contain, for example, dyes such as Blue No. 1, pigments such as titanium dioxide, antioxidants such as dibutylhydroxytoluene, chelating agents such as edetates, and flavoring agents such as tea extract and tea distillate.

[0030] Furthermore, the oral composition of the present invention, which combines the above components, can be manufactured in accordance with conventional methods.

[0031] Furthermore, the resulting toothpaste or other composition can be used by filling it into aluminum tubes, laminate tubes, glass-coated tubes, plastic tubes, plastic bottles, aerosol containers, etc.

[0032] The oral composition of the present invention has been described above, but the present invention is not limited thereto. For example, in addition to the components described above, the oral composition of the present invention may contain any other components having any function. [Examples]

[0033] Next, specific embodiments of the present invention will be described. <Preparation of oral compositions> (Examples 1-6, Comparative Examples 1-9) Oral compositions (aqueous solutions) were prepared with concentrations of aluminum lactate and dicarboxylic acid compounds or monocarboxylic acid compounds as shown in Table 1. Each oral composition was then pH-adjusted to 7 using sodium hydroxide.

[0034] <Evaluation Method> Dentin sections approximately 1 cm in length and width were prepared from the roots of bovine teeth, and their surfaces were polished with a file. The dentin sections were immersed in a 10% phosphoric acid solution and a 10% hypochlorite solution for 30 seconds, then washed once and three times, respectively, and finally subjected to ultrasonic treatment to open the dentinal tubules. Open dentin sections were immersed in the oral compositions of each example and comparative example for 60 minutes while being stirred. Afterward, they were washed, dried, and platinum vapor deposition was performed, and the opening state was observed using an electron microscope. The surface opening state was evaluated by determining the area of ​​the opening using image analysis software (image-j), calculating the sealing rate, and evaluating it according to the following criteria. A: Lockdown rate over 80% B: Lockdown rate between 50% and less than 80% C: Lockdown rate between 25% and less than 50% D: Lockdown rate between 5% and 25% E: Lockdown rate less than 5% These results are shown in Table 1. Furthermore, Figures 1 to 3 show electron microscope images illustrating the state of dentinal tubules in the evaluation method using each of the oral compositions in Example 1, Comparative Examples 1 and 2.

[0035] [Table 1]

[0036] As can be seen from Table 1 and Figure 2, in Comparative Example 1, the oral composition containing only aluminum lactate had deposits on the edges of the dentinal tubules, and although there was a slight tendency to seal them, the effect was insufficient. Furthermore, in the oral compositions of Examples 1 to 4, aluminum lactate is combined with glutamic acid, fumaric acid, succinic acid, and adipic acid, respectively, and it can be seen that the sealing effect by aluminum lactate is promoted (see Figure 1). Furthermore, in the oral composition of Example 5, the concentration of glutamic acid was increased, but similar results were obtained. Furthermore, in the oral composition of Example 6, when the concentration of glutamic acid was reduced, a sufficient promotion of sealing was observed compared to Comparative Example 1, but the sealing promotion effect was not as strong as that of the oral composition of Example 1.

[0037] Furthermore, in the oral compositions of Comparative Examples 2 to 5, the effects of glutamic acid, fumaric acid, succinic acid, and adipic acid were examined individually, but no septic effect was observed at all. Furthermore, in the oral compositions of Comparative Examples 6 and 7, when malic acid and tartaric acid, which are dicarboxylic acids having a hydroxyl group, were combined with aluminum lactate, the sequestering of aluminum lactate was inhibited. Furthermore, in the oral composition of Comparative Example 8, when oxalic acid, a dicarboxylic acid with 2 carbon atoms, was combined with aluminum lactate, the sequestering of aluminum lactate was inhibited. Furthermore, in the oral composition of Comparative Example 9, serine having one hydroxyl group and one carboxyl group was combined with aluminum lactate, but the result was that it neither inhibited nor promoted the sealing by aluminum lactate.

Claims

1. Aluminum lactate and It comprises at least one dicarboxylic acid compound selected from the group consisting of glutamic acid, succinic acid, adipic acid, and fumaric acid, The amount of aluminum lactate used is 0.01 to 5% by mass. An oral composition wherein the amount of the dicarboxylic acid compound is 0.1 to 1% by mass.

2. The oral composition according to claim 1, wherein the dicarboxylic acid compound is glutamic acid.

3. An oral composition according to claim 1 or 2, which is a dentinal tubule sealing agent.

4. An oral composition according to any one of claims 1 to 3, which is a toothpaste.

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