Oral composition

Abstract

[Problem] To provide an oral composition which more effectively exerts an anti-glycation effect of a gluconate on dentin, exerts a yellowing-inhibiting effect inside a tooth, and exerts an anti-aging effect. [Solution] An oral composition comprising (A) a gluconate and (B) one or more selected from the group consisting of glucose oxidase, papain, amylase, lipase, superoxide dismutase, catalase, and xylanase, the content of the (A) being 0.2 to 5 mass% relative to the total mass of the oral composition, and the enzyme activity amount of the (B) component being 10 to 500 U / g per 1 g of the oral composition.

Description

Technical Field

[0001] This invention relates to oral compositions. Background Technology

[0002] Gluconate is a component that inhibits yellowing of teeth (whitening effect) by suppressing the glycation reaction in dentin.

[0003] For example, Patent Document 1 describes an oral composition comprising sodium fluoride, calcium gluconate, and condensed phosphate.

[0004] Existing technical documents

[0005] Patent documents

[0006] Patent Document 1: Japanese Patent Application Publication No. 2026-1570 Summary of the Invention

[0007] The problem the invention aims to solve

[0008] However, for oral compositions, there is a requirement to exert an inhibitory effect on the formation of aging-causing substances, namely advanced glycation end products (AGEs), which are generated by the binding and denaturation of sugars and proteins (anti-aging effect), and to further enhance the whitening effect.

[0009] The purpose of this invention is to provide an oral composition that more effectively exerts the anti-glycation effect of gluconate on dentin, inhibits yellowing inside teeth, and exerts anti-aging effects.

[0010] Solution for solving the problem

[0011] The tooth surface has a coating of stains and organic matter, which acts as a barrier, making it difficult for gluconate to fully penetrate into the dentin.

[0012] The inventors focused on this point and studied the effect of combining gluconate with a specific enzyme. Their results showed that the specific enzyme reacted with staining substances and organic matter on the tooth surface, removing them, thereby increasing the permeability of the tooth surface and allowing gluconate to easily reach the dentin.

[0013] The present invention has the following aspects.

[0014] [1] An oral composition comprising:

[0015] (A) gluconate, and

[0016] (B) Select one or more from the group consisting of glucose oxidase, papain, amylase, lipase, superoxide dismutase, catalase, and xylanase.

[0017] The content of component (A) is 0.2 to 5% by mass relative to the total mass of the oral composition.

[0018] The enzyme activity of component (B) is 10-500 U / g per 1g of oral composition.

[0019] [2] The oral composition according to [1], wherein the (A) component is one or more selected from the group consisting of calcium gluconate, sodium gluconate, copper gluconate and zinc gluconate.

[0020] [3] The oral composition according to [1] or [2], wherein the ratio expressed as [content (mass%) of component (A)] / [enzyme activity (U / g) of component (B)] is 0.001 to 0.05.

[0021] [4] The oral composition according to any one of [1] to [3] further comprises (C) one or more of the group consisting of polyoxyethylene hydrogenated castor oil and fatty acid amamidopropyl betaine.

[0022] [5] The oral composition according to [4], wherein the content of component (C) is 0.1 to 3 by mass relative to the total mass of the oral composition.

[0023] [6] The oral composition according to any one of [1] to [5] further comprises (D) condensed phosphate.

[0024] [7] The oral composition according to [6], wherein the content of component (D) is 0.1 to 3 by mass relative to the total mass of the oral composition.

[0025] [8] The oral composition according to any one of [1] to [7] further comprises:

[0026] (C) Select one or more from the group consisting of polyoxyethylene hydrogenated castor oil and fatty acid amyl betaine.

[0027] (D) Condensed phosphate,

[0028] The ratio expressed as [(B) enzyme activity (U / g)] / [(C) content (mass%) + (D) content (mass%)] is 14~67.

[0029] The effects of the invention

[0030] According to the present invention, an oral composition can be obtained that more effectively exerts the anti-glycation effect of gluconate on dentin, inhibits yellowing inside the tooth, and exerts anti-aging effects. Detailed Implementation

[0031] The following provides a detailed description of various exemplary embodiments, features, and methods of the present invention. The term "exemplary" as used in this specification means "used as an example, embodiment, or illustration." Any embodiment described as "exemplary" in this specification should not be construed as superior or better than other embodiments.

[0032] Furthermore, to better illustrate the present invention, numerous specific details are shown in the following detailed descriptions. Those skilled in the art will understand that the present invention can be practiced in the same manner even without these specific details. In other instances, to emphasize the spirit of the invention, methods, means, apparatus, and steps well-known to those skilled in the art are not described in detail.

[0033] Unless otherwise stated, all units used in this specification are international standard units, and it should be understood that the numerical values ​​and ranges appearing in this invention include systematic errors that are unavoidable in industrial production.

[0034] In this specification, the word "may" has both the meaning of performing a certain process and the meaning of not performing a certain process.

[0035] In this specification, references to "some specific / preferred embodiments," "other specific / preferred embodiments," and "embodiment" refer to specific elements (e.g., features, structures, properties, and / or characteristics) associated with that embodiment, which are included in at least one embodiment described herein and may or may not be present in other embodiments. Furthermore, it should be understood that the described elements can be combined with various embodiments in any suitable manner.

[0036] In this specification, the range of values ​​represented by "value A to value B" refers to the range including the endpoint values ​​A and B.

[0037] In this specification, "oral composition" means a composition intended primarily for use in the oral cavity.

[0038] Oral Compositions

[0039] The oral composition of this embodiment comprises component (A) and component (B).

[0040] <(A) ingredient>

[0041] (A) is a gluconate. (A) is a component that inhibits yellowing of the tooth interior by suppressing glycation reactions in the dentin. (A) and (B) work synergistically to exert an anti-aging effect through whitening and anti-glycation effects within the tooth interior.

[0042] Component (A) can include calcium gluconate, sodium gluconate, copper gluconate, and zinc gluconate. Among these, calcium gluconate is preferred because it readily dissociates from gluconate ions and calcium ions are beneficial to teeth.

[0043] (A) The ingredient may be present in the oral composition as a balanced mixture with gluconolactone.

[0044] (A) The ingredients can be a single type or a combination of two or more types.

[0045] The content of component (A) is 0.2 to 5% by mass relative to the total mass of the oral composition, preferably 0.5 to 5% by mass. By keeping the content of component (A) within the above range, the glycation reaction in the dentin can be inhibited, thereby exerting an inhibitory effect on yellowing of the tooth interior.

[0046] If the content of component (A) is less than 0.2% by mass, the yellowing inhibition effect inside the tooth, the whitening effect inside the tooth, and the anti-aging effect brought about by anti-glycation will not be obtained. If the content of component (A) is greater than 5% by mass, the solubility in solvents will be poor when manufacturing oral compositions.

[0047] In some preferred embodiments, the content of (A) relative to the total mass of the oral composition is preferably 0.3% by mass or more, 0.4% by mass or more, 0.5% by mass or more, 0.6% by mass or more, 0.7% by mass or more, 0.8% by mass or more, 0.9% by mass or more, 1% by mass or more, 1.1% by mass or more, 1.2% by mass or more, 1.3% by mass or more, 1.4% by mass or more, 1.5% by mass or more, 1.6% by mass or more, 1.7% by mass or more, 1.8% by mass or more, 1.9% by mass or more, 2% by mass or more, 2.1% by mass or more, or 2.2% by mass or more, and preferably 4.9% by mass or less, or 4.8% by mass or less. Below 4.7%, 4.6%, 4.5%, 4.4%, 4.3%, 4.2%, 4.1%, 4%, 3.9%, 3.8%, 3.7%, 3.6%, 3.5%, 3.4%, 3.3%, 3.2%, 3.1%, 3%, 2.9%, 2.8%, 2.7%, 2.6%, 2.5%, 2.4%, or 2.3%.

[0048] <(B) Components>

[0049] (B) Component is selected from one or more of the group consisting of glucose oxidase, papain, amylase, lipase, superoxide dismutase, catalase, and xylanase. Component (B) reacts enzymatically with staining substances and organic matter on the tooth surface, removing them and thus increasing the permeability of the tooth surface, allowing component (A) to easily reach the dentin. Therefore, through its whitening and anti-glycation effects within the teeth, it exerts an anti-aging effect.

[0050] (B) The ingredients can be a single type or a combination of two or more types.

[0051] The enzyme activity of component (B) is 10-500 U / g per 1g of oral composition. By keeping the enzyme activity of component (B) within the above range, component (B) reacts with staining substances and organic matter on the tooth surface to remove them, thereby increasing the permeability of the tooth surface and allowing component (A) to easily reach the dentin.

[0052] If the enzyme activity of component (B) is less than 10 U / g, it cannot sufficiently remove stains and organic matter from the tooth surface, thus reducing the permeability of the tooth surface and making it difficult for component (A) to reach the dentin. If the enzyme activity of component (B) is greater than 500 U / g, the taste and odor from the enzyme will easily reduce the user experience.

[0053] In some preferred embodiments, the enzyme activity of component (B) relative to 1g of the oral composition is preferably 20 U / g or more, 30 U / g or more, 40 U / g or more, 50 U / g or more, 60 U / g or more, 70 U / g or more, 80 U / g or more, 90 U / g or more, 100 U / g or more, 110 U / g or more, 120 U / g or more, 130 U / g or more, 140 U / g or more, 150 U / g or more, 160 U / g or more, 170 U / g or more, 180 U / g or more, 190 U / g or more, 200 U / g or more, 210 U / g or more, 220 U / g or more, 230 U / g or more, or 240 U / g. The values ​​are above 250 U / g or above, preferably below 490 U / g, below 480 U / g, below 470 U / g, below 460 U / g, below 450 U / g, below 440 U / g, below 430 U / g, below 420 U / g, below 410 U / g, below 400 U / g, below 390 U / g, below 380 U / g, below 370 U / g, below 360 U / g, below 350 U / g, below 340 U / g, below 330 U / g, below 320 U / g, below 310 U / g, below 300 U / g, below 290 U / g, below 280 U / g, below 270 U / g, or below 260 U / g.

[0054] The enzyme activity of the enzyme contained in component (B) of this invention can be expressed in units of 1 U (Unit) based on the definition of "International Units" of the International Union of Biochemistry in 1964. Here, 1 U refers to the amount of enzyme that, under optimal conditions, can transform 1 μmol of substrate in 1 L of sample at 30°C for 1 minute.

[0055] The enzyme activities of each enzyme in this invention are determined by the following method. It should be noted that, in any case, 2.0 g of the oral composition is suspended in 20 mL of phosphate buffer, centrifuged, and the resulting supernatant is used as the test solution. It is then appropriately diluted according to the enzyme activity value before use.

[0056] <Glucose oxidase>

[0057] The enzyme activity of glucose oxidase was determined by the following method.

[0058] 0.1 mL of the test solution was added to 0.3 mL of a substrate solution containing 18% glucose, and the mixture was reacted in a thermostat maintained at 30°C for 3 minutes. Then, o-phenylenediamine was used as an indicator to determine the amount of hydrogen peroxide generated, thus calculating the hydrogen peroxide content.

[0059] One unit (U) of glucose oxidase activity is defined as the amount of enzyme that generates 1 μmol of hydrogen peroxide per minute.

[0060] Papain

[0061] The enzyme activity of papain was determined by the following method.

[0062] The test solution was mixed with casein solution and reacted in a constant temperature bath at 37°C for 10 minutes. Trichloroacetic acid solution was then added to stop the reaction, and the amount of soluble peptides generated was determined by absorbance.

[0063] One unit (U) of papain's enzyme activity is defined as the amount of amino acid produced per minute equivalent to 1 μg of tyrosine.

[0064] <Amylase>

[0065] The enzyme activity of amylase was determined by the following method.

[0066] The test solution was mixed with a substrate containing a cross-linked starch polymer with an insoluble blue pigment. After reacting in a constant temperature bath at 37°C for 15 minutes, 1N sodium hydroxide solution was added to stop the reaction, and the absorbance was measured.

[0067] One unit (U) of amylase activity is defined as the amount of reducing sugar produced per minute equivalent to 1 μmol of glucose.

[0068] Superoxide dismutase

[0069] The enzyme activity of superoxide dismutase was determined by the following method.

[0070] The test solution was mixed with a reaction solution containing water-soluble tetrazolium salt, and then xanthine oxidase solution was added. The mixture was reacted in a thermostat maintained at 37°C for 20 minutes. The resulting formazan (…) was then measured. formazan ) The absorbance of the pigment.

[0071] One unit (U) of superoxide dismutase enzyme activity is defined as the amount of enzyme that removes 50% of superoxide.

[0072] Xylanase

[0073] The enzyme activity of xylanase was determined by the following method.

[0074] The test solution was mixed with xylan solution and reacted in a constant temperature bath at 40°C for 10 minutes. Then, 3,5-dinitrosalicylic acid test solution was added and heated to develop color. The amount of reducing sugar generated was determined by absorbance.

[0075] One unit (U) of xylanase enzyme activity is defined as the amount of reducing sugar produced per minute equivalent to 1 μmol xylose.

[0076] Catalase

[0077] The enzyme activity of catalase was determined by the following method.

[0078] After reacting the test solution with hydrogen peroxide solution at 25°C for 1 minute, a reaction stop solution is added to stop the reaction, and the amount of residual hydrogen peroxide is determined by absorbance.

[0079] One unit (U) of catalase activity is defined as the amount of enzyme that breaks down 1 μmol of hydrogen peroxide per minute.

[0080] <Lipase>

[0081] After reacting the test solution with a p-nitrophenyl palmitate solution at 37°C for 10 minutes, the amount of p-nitrophenol generated was determined by absorbance.

[0082] One unit (U) of lipase activity is defined as the amount of enzyme that produces 1 μmol of fatty acid per minute.

[0083] The enzyme activity of each enzyme is expressed as the enzyme activity (U / g) per gram of enzyme preparation.

[0084] In some preferred embodiments, the ratio, expressed as [content (mass%) of component (A)] / [enzyme activity (U / g) of component (B)], is preferably 0.001 to 0.05. By setting the ratio in this way, component (A) and component (B) work synergistically, and based on the whitening effect and anti-glycation effect inside the teeth, an anti-aging effect can be easily achieved.

[0085] In some preferred embodiments, the ratio expressed as [content (mass%) of component (A)] / [enzyme activity (U / g) of component (B)] is preferably 0.005 or more, 0.01 or more, 0.015 or more, 0.02 or more, or 0.025 or more, and preferably 0.045 or less, 0.04 or less, 0.035 or less, or 0.03 or less.

[0086] <(C) Ingredients>

[0087] In some preferred embodiments, the oral composition of the present invention may further comprise (C) selected from one or more of the group consisting of polyoxyethylene hydrogenated castor oil and fatty acid amamidopropyl betaine. The stability of component (B) is improved by the adhesion of component (C) to the surface of component (B). This promotes the enzymatic reaction of component (B) with staining substances and organic matter on the tooth surface, facilitating their removal, thereby further enhancing the permeability of the tooth surface and allowing component (A) to more easily reach the dentin.

[0088] The average repeat number of oxyethylidenes in the polyoxyethylene hydrogenated castor oil is preferably 10 to 60, more preferably 15 to 40, and even more preferably 18 to 25. If the average repeat number of oxyethylidenes is above the lower limit mentioned above, the hydrophilicity of the polyoxyethylene hydrogenated castor oil becomes higher, the structural deformation caused by the hydrophobic interaction with component (B) is suppressed, and the stereostructure stability of component (B) becomes higher. If the average repeat number of oxyethylidenes is below the upper limit mentioned above, a balance with the hydrophobic group is maintained, and appropriate adsorption to the interface is maintained, thereby stably maintaining the surrounding environment of component (B). Commercially available polyoxyethylene hydrogenated castor oil can be used, such as NIKKOL (registered trademark) HCO-20, 40, 60 (manufactured by Nikko Chemical Co., Ltd.). The average repeat number of oxyethylidenes mentioned above can be determined by gel filtration chromatography.

[0089] The number of carbon atoms in fatty acid amamidopropyl betaine is preferably 10 to 16, more preferably 12 to 14, and even more preferably 12 to 13. If the number of carbon atoms in fatty acid amamidopropyl betaine is above or below the aforementioned lower limit, the hydrophobicity of fatty acid amamidopropyl betaine becomes higher, suppressing excessive interaction of component (B) with the surface, and the stability of the stereostructure of component (B) becomes higher. If the number of carbon atoms in fatty acid amamidopropyl betaine is below the aforementioned upper limit, the hydrophilicity of fatty acid amamidopropyl betaine becomes higher, and the dispersibility with coloring substances and organic matter becomes higher. Furthermore, if the number of carbon atoms in fatty acid amamidopropyl betaine is below the aforementioned upper limit, the dispersibility of component (B) with coloring substances and organic matter becomes higher, and the stability of the enzyme activity of component (B) becomes higher.

[0090] Fatty acid amamidopropyl betaine preferably has an alkyl group having 10 to 16 carbon atoms. Examples of such fatty acid amamidopropyl betaine include coconut oil fatty acid amamidopropyl betaine and lauric acid amamidopropyl betaine. Among these, coconut oil fatty acid amamidopropyl betaine is preferred. Commercially available products can be used as fatty acid amamidopropyl betaine, such as ENAGCOL (registered trademark) C-30B manufactured by LION SPECIALTY CHEMICALS CO., LTD., and NIKKOL (registered trademark) AM-3130N manufactured by Nikko Chemical Co., Ltd.

[0091] (C) The ingredients can be a single type or a combination of two or more types.

[0092] The content of component (C) is preferably 0.1 to 3% by mass relative to the total mass of the oral composition. By keeping the content of component (C) within the above range, the effect of component (B) can be improved.

[0093] In some preferred embodiments, the content of (C) relative to the total mass of the oral composition is preferably 0.2% by mass or more, 0.3% by mass or more, 0.4% by mass or more, 0.5% by mass or more, 0.6% by mass or more, 0.7% by mass or more, 0.8% by mass or more, 0.9% by mass or more, 1% by mass or more, 1.1% by mass or more, 1.2% by mass or more, 1.3% by mass or more, 1.4% by mass or more, or 1.5% by mass or more, and preferably 2.9% by mass or less, 2.8% by mass or less, 2.7% by mass or less, 2.6% by mass or less, 2.5% by mass or less, 2.4% by mass or less, 2.3% by mass or less, 2.2% by mass or less, 2.1% by mass or less, 2% by mass or less, 1.9% by mass or less, 1.8% by mass or less, 1.7% by mass or less, or 1.6% by mass or less.

[0094] <(D) Component>

[0095] In some preferred embodiments, the oral composition of the present invention may further comprise (D) condensed phosphate. The chelating effect of component (D) enhances the stability of component (B). This promotes the enzymatic reaction of component (B) with staining substances and organic matter on the tooth surface, facilitating their removal, thereby further improving the permeability of the tooth surface and allowing component (A) to more easily reach the dentin.

[0096] Examples of condensed phosphates include, for example, chain-like polyphosphates (e.g., pyrophosphate, tripolyphosphate, highly polymerized polyphosphate), cyclic metaphosphates (e.g., trimetaphosphate, tetrametaphosphate, hexametaphosphate), and phytates. Preferably, at least one of pyrophosphate, tripolyphosphate, hexametaphosphate, and phytates is selected.

[0097] Examples of salts include inorganic alkali salts such as sodium and potassium salts, alkaline earth metal salts such as calcium and magnesium salts, and organic alkali salts such as triethylammonium salts, triethanolamine salts, pyridinium salts, and diisopropylammonium salts. Among these, alkali metal salts or alkaline earth metal salts are preferred, and sodium or potassium salts are more preferred.

[0098] In some preferred embodiments, examples of condensed phosphates include potassium pyrophosphate, sodium pyrophosphate, sodium tripolyphosphate, potassium tripolyphosphate, sodium hexametaphosphate, sodium phytate, and potassium phytate.

[0099] In some preferred embodiments, the condensed phosphate can be a water-soluble condensed phosphate, such as an alkali metal pyrophosphate, an alkali metal tripolyphosphate, or a polyphosphate with a higher degree of polymerization. As a preferred embodiment, potassium salts or mixtures of sodium and potassium salts can also be used, but the sodium form of such salts is preferred. All physical forms, such as hydrated or dehydrated forms, can be used.

[0100] The content of component (D) is preferably 0.1 to 3% by mass relative to the total mass of the oral composition. By setting the content of component (D) within the above range, the stability of component (B) is improved, making it easier to remove stains and organic matter from the tooth surface, thereby further improving the permeability of the tooth surface, and making it easier for component (A) to reach the dentin.

[0101] (D) The component can be a single condensed phosphate or a combination of two or more.

[0102] In some preferred embodiments, the content of (D) relative to the total mass of the oral composition is preferably 0.2% by mass or more, 0.3% by mass or more, 0.4% by mass or more, 0.5% by mass or more, 0.6% by mass or more, 0.7% by mass or more, 0.8% by mass or more, 0.9% by mass or more, 1% by mass or more, 1.1% by mass or more, 1.2% by mass or more, 1.3% by mass or more, 1.4% by mass or more, or 1.5% by mass or more, and preferably 2.9% by mass or less, 2.8% by mass or less, 2.7% by mass or less, 2.6% by mass or less, 2.5% by mass or less, 2.4% by mass or less, 2.3% by mass or less, 2.2% by mass or less, 2.1% by mass or less, 2% by mass or less, 1.9% by mass or less, 1.8% by mass or less, 1.7% by mass or less, or 1.6% by mass or less.

[0103] In some preferred embodiments, the ratio, expressed as [enzyme activity of component (B) (U / g)] / [content of component (C) (mass%) + content of component (D) (mass%)], is preferably 14 to 67. By setting the ratio in this way, components (C) and (D) enhance the stability of component (B), thereby promoting the enzymatic reaction of component (B) with staining substances and organic matter on the tooth surface, making them easier to remove, thus further improving the permeability of the tooth surface, and making it easier for component (A) to reach the dentin.

[0104] In some preferred embodiments, the ratio expressed as [enzyme activity of component (B) (U / g)] / [content of component (C) (mass%) + content of component (D) (mass%)] is preferably 15 or more, 16 or more, 17 or more, 18 or more, 19 or more, 20 or more, 21 or more, 22 or more, 23 or more, 24 or more, 25 or more, 26 or more, 27 or more, 28 or more, 29 or more, 30 or more, 31 or more, 32 or more, 33 or more, 34 or more, 35 or more, 36 or more, 37 or more, 38 or more, 39 or more, or 40 or more, preferably 66 or less, 65 or less, 64 or less, 63 or less, 62 or less, 61 or less, 60 or less, 59 or less, 58 or less, 57 or less, 56 or less, 55 or less, 54 or less, 53 or less, 52 or less, 51 or less, 50 or less, 49 or less, 48 ​​or less, 47 or less, 46 or less, or 45 or less.

[0105] <Other Ingredients>

[0106] In the oral composition of the present invention, other ingredients commonly used in oral compositions may be incorporated as needed, without impairing the effects of the present invention. Examples of optional ingredients that may be incorporated include solvents, abrasives (abrasive silica, etc.), binders (thickening silica, xanthan gum, etc.), humectants (sorbitol, glycerin, etc.), sweeteners (saccharin, etc.), flavorings, pH adjusters, preservatives (methylparaben, etc.), active ingredients (sodium monofluorophosphate, etc.), and surfactants other than ingredient (C) (sodium lauryl sulfate, etc.).

[0107] As a solvent, water can be listed. As water, purified water, sterile purified water, water for injection, etc. can be listed.

[0108] The water content in oral compositions can be appropriately set according to the product form and method of use of the oral composition.

[0109] For example, when the oral composition is toothpaste, the water content is preferably 5 to 90% by mass, more preferably 10 to 60% by mass, and even more preferably 15 to 50% by mass, relative to the total mass of the oral composition.

[0110] When the oral composition is a mouthwash or spray, the water content relative to the total mass of the oral composition is preferably 70-99% by mass, more preferably 75-95% by mass, and even more preferably 80-90% by mass.

[0111] Dosage Forms of Oral Compositions

[0112] The oral composition of this embodiment can be manufactured into any suitable dosage form known in the conventional method. Examples of dosage forms include liquids (solutions, emulsions, suspensions, slurries, etc.), semi-solids (gels, ointments, pastes, etc.), and solids (tablets, granules, capsules, films, mixtures, molten solids, waxy solids, elastic solids, soft capsules, etc.). In this embodiment, the dosage form of the oral composition is preferably a liquid or semi-solid.

[0113] The oral composition of this embodiment can be widely used in oral applications. Examples of solid dosage forms include troche tablets, gummies, chewing gum, and dental cleaning agents. Examples of semi-solid dosage forms include toothpaste and gel-based dental cleaning agents. Examples of liquid dosage forms include mouthwash, liquid dental cleaning agents, and mouthwashes (sprays, etc.). From the viewpoint of effectiveness and stability, toothpaste and gel-based dental cleaning agents are preferred.

[0114] In this embodiment, when the oral composition is a semi-solid, and the oral composition is prepared into a liquid state, the pH (25°C) of the oral composition is preferably 5.0 to 9.0, more preferably 6.0 to 8.0. This maintains effectiveness and stability. The pH can be measured immediately after preparation of the oral composition using a pH meter (model Hm-30S) manufactured by Toa Denpa Kogyo Co., Ltd., after 3 minutes at 25°C. The pH can be adjusted by adding the described pH adjuster, component composition, etc.

[0115] The oral composition of this embodiment can be adjusted to an appropriate viscosity, for example, depending on the dosage form. When the dosage form is, for example, a paste, gel, or ointment, the viscosity at 25°C, measured using a BH viscometer, is preferably 1 Pa·s to 300 Pa·s, more preferably 20 Pa·s to 150 Pa·s.

[0116] In addition, when the oral composition is in liquid form, the viscosity at 25°C as measured by a BH viscometer should be 1000 mPa·s or less, and is particularly preferably 0.7 to 1000 mPa·s.

[0117] Methods for manufacturing oral compositions

[0118] The method for manufacturing the oral composition of the present invention is not particularly limited, and it can be manufactured by mixing the above-mentioned ingredients. The mixing order of the ingredients is not particularly limited, but uniform mixing is preferred.

[0119] When the oral composition of the present invention is a toothpaste composition, it can be manufactured by any suitable method known in the past. Specifically, as a method for manufacturing the toothpaste composition, for example, the following manufacturing method can be listed: first, the components soluble in a solvent are manufactured, then insoluble components other than these are mixed, and defoaming is performed as needed, for example, by reducing pressure.

[0120] The resulting toothpaste can be manufactured into a product by storing it in a specified container (laminated tube).

[0121] There are no particular limitations on the shape or material of the container that can hold the toothpaste composition of the present invention. Any suitable container known in the past that is generally applicable to toothpaste compositions can be used as the container. Examples of containers made of materials such as polyethylene, polypropylene, polyethylene terephthalate, and nylon include, for instance.

[0122] When the oral composition of the present invention is a liquid oral composition, the manufacturing method thereof may be, for example, the following method: the raw material components are added sequentially to a solvent such as purified water and stirred to dissolve them uniformly.

[0123] There are no particular limitations on the shape or material of the container for holding the oral composition containing the liquid of the present invention. Generally, it can be used in containers applied to oral compositions. Specifically, such containers can be laminated containers containing layers of polyethylene, ethylene methacrylate copolymer, polyethylene terephthalate, aluminum, glass vapor deposited layer, polyvinyl alcohol, ethylene ethylene alcohol copolymer, acrylonitrile copolymer, paper, recycled plastic, etc.; or polyethylene containers, polyethylene terephthalate containers, polypropylene containers; or bag containers containing linear polyethylene, low-density polyethylene, high-density polyethylene, etc., of polyethylene or polypropylene. Tubular containers, mechanical or pressure differential dispenser containers, pillow-type packaging, and other film packaging containers can also be used as various containers commonly used in oral compositions.

[0124] Methods for cleaning teeth

[0125] The present invention provides a method for cleaning teeth, comprising applying the oral composition of the present invention to the tooth surface.

[0126] When the oral composition of the present invention is a liquid dosage form such as a mouthwash, for example, a method of holding an appropriate amount in the mouth for 10 to 30 seconds and rinsing can be described. When the oral composition of the present invention is a solid dosage form such as a toothpaste or a semi-solid dosage form such as toothpaste, for example, an appropriate amount can be applied (attached) to the teeth and then brushed.

[0127] Example

[0128] The embodiments of the present invention will be described in detail below with reference to examples. Those skilled in the art will understand that the following examples are merely illustrative and should not be considered as limiting the scope of the invention. Where specific conditions are not explicitly stated in the examples, general conditions or conditions specified by the manufacturer are followed. Unless otherwise specified by the manufacturer, the reagents or equipment used are generally commercially available products.

[0129] It should be noted that in the following examples, unless otherwise specified, "%" as the unit of content means "mass %".

[0130] <Ingredients Used>

[0131] [(A) Ingredient]

[0132] Calcium gluconate: manufactured by Zhengzhou Ruipu Biological Engineering Co., Ltd.

[0133] Sodium gluconate: manufactured by Jungbunzlauer Shandong Fuyang Bio-tech and Xingfa Group.

[0134] Copper gluconate: Manufactured by Hebei Chuanghai Biotechnology Co., Ltd.

[0135] Zinc gluconate: manufactured by Hebei Chuanghai Biotechnology Co., Ltd.

[0136] [(B) Component]

[0137] Glucose oxidase: manufactured by Zhongnuo Biotechnology Development Jiangsu Co., Ltd.

[0138] Papain: Produced by Nanning Dongheng Huadao Biotechnology Co., Ltd.

[0139] Amylase: manufactured by Novonesis.

[0140] Superoxide dismutase: manufactured by Shenzhen Siyomicro Bio-tech Co., Ltd.

[0141] Catalase: Manufactured by Guangdong VTR Bio-Tech Co., Ltd.

[0142] Xylanase: Produced by Nanning Dongheng Huadao Biotechnology Co., Ltd.

[0143] [(C) Component]

[0144] Polyoxyethylene hydrogenated castor oil: manufactured by AOKI OIL INDUSTRIAL, trade name: BLAUNON (registered trademark) RCW-20, average repeat number of oxyethylene: 10~40.

[0145] Coconut oil fatty acid amamidopropyl betaine: manufactured by Evonik, trade name: Tego (registered trademark) BetainCK OK MB.

[0146] [(D) component]

[0147] Sodium pyrophosphate: Manufactured by Taihei Chemical Industry Co., Ltd., product name "Sodium pyrophosphate (anhydrous)".

[0148] Sodium tripolyphosphate: Manufactured by Taihei Chemical Industry Co., Ltd.

[0149] Sodium metaphosphate: Manufactured by Hubei Xingfa Chemicals Group Co., Ltd.

[0150] [water]

[0151] Purified water.

[0152] [Common Ingredients (Optional Ingredients)]

[0153] Sorbitol solution (70% by mass aqueous solution): manufactured by ROQUETTE.

[0154] Glycerin: Produced by Wilmar International Limited.

[0155] Thickening silica: Made by Evonik, product number: Zeodent (registered trademark) 165.

[0156] Abrasive silica: Made by Evonik, trade name: Zeodent (registered trademark) 103.

[0157] Xanthan gum: Produced by Xinjiang Meihua Amino Acid Co., Ltd.

[0158] Sodium monofluorophosphate: manufactured by Hubei Xingfa Chemical Group Co., Ltd.

[0159] Sodium lauryl sulfate (K12), manufactured by Dongming Juhua Chemical Co., Ltd.

[0160] Sodium saccharin: Henan Kaifeng Pingmei Shenma Xinghua Fine Chemical Co., Ltd.

[0161] Methylparaben: manufactured by FUSHIMI Pharmaceutical Co., Ltd.

[0162] Fragrance composition: Fragrance composition A as described in Table 6.

[0163] <Examples 1-20, Comparative Examples 1-3>

[0164] Using the above-mentioned ingredients as raw materials, toothpaste compositions having the formulations shown in Tables 1-5 below were prepared. Water-soluble ingredients (excluding binders, fragrance compositions, surfactants, and abrasives in Tables 1-5) were added to purified water and stirred. Then, binders, fragrance compositions, surfactants, and abrasives were added, and the mixture was further stirred under reduced pressure (4 kPa) to obtain the toothpaste composition. A 5L capacity kneader (manufactured by Ishiyama Works Co., Ltd.) was used in the manufacturing process.

[0165] Empty columns in the table indicate that the ingredient was not mixed. The "balance" of purified water indicates that the total amount of the oral composition is 100%.

[0166] The obtained oral compositions were evaluated as follows. The results are recorded in the table.

[0167] <Evaluation Methods>

[0168] Evaluation Method 1: Yellowing Inhibition Test of Bovine Teeth

[0169] The anti-yellowing effect of the oral compositions of Examples 1-20 and Comparative Examples 1-3 was evaluated by the following methods.

[0170] The attached gingiva and root portion of the extracted tooth are removed to create a dentin block containing enamel and dentin. A block approximately 6mm × 6mm × 3mm in size is cut from the center of the crown, with the enamel surface serving as the test surface. The test surface is polished using water-resistant abrasive paper (#800, #2000, #4000) to homogenize the surface.

[0171] Alternately perform steps A and B below to allow stain to adhere to the test surface. Perform steps A and B three times each day for two days (a total of six times each).

[0172] <Step A>

[0173] Add 300 μL of saliva (Medix Biochemica USA Inc., product number: 991-05-P) to the test surface, seal it with a sealant, and incubate at 37°C for 2 hours.

[0174] <Step B>

[0175] Add 300 μL of black tea extract from Brisk tea bags (manufactured by Unilever Japan Co., Ltd.) according to the conditions stated on the packaging to the test surface after step A above, and incubate at 37°C for 1 hour.

[0176] The saccharification solution was prepared using PBS (pH 7.4). The saccharification solution contained 9% ribose, 5% glucose, 1% casein, 1% starch, 1% xylan, and 0.5% trioleic acid glyceride.

[0177] The oral composition was diluted 3 times with the above-mentioned saccharification solution, centrifuged, and the resulting supernatant was used as the test solution.

[0178] The stained dentin blocks were immersed in 2 mL of the test solution and reacted at 37°C for 7 days.

[0179] Brush 50 times using an automatic grinding tester (Miyagawa Shoten Co., Ltd., load 200g, temperature 37°C) equipped with a flat-cut toothbrush (PC Clinica, manufactured by Lion Corporation).

[0180] The test surface was photographed before the reaction (before saccharification) and after the reaction (after saccharification and washing) using a digital microscope (KEYENCE VHX-2000). The values ​​of L*, a*, and b* were determined by image analysis, and ΔE was calculated using the following formula. Measurements were also taken for a fixed area in the center of the test surface.

[0181] It can be said that the lower the ΔE value, the higher the effect of inhibiting internal yellowing.

[0182]

[0183] (L1,a1,b1: before saccharification, L2,a2,b2: after saccharification)

[0184] Those with a ΔE value below 12 are considered qualified.

[0185] Evaluation Method 2: AGEs (Advanced Glycation End Products) Formation Inhibition Assay

[0186] The oral compositions of Examples 1-20 and Comparative Examples 1-3 were evaluated for their AGEs generation inhibition effects by the following methods.

[0187] The saccharification solution was prepared using PBS (pH 7.4). The saccharification solution contained 5% glucose, 1% casein, 1% starch, 1% xylan, and 0.5% trioleic acid glyceride.

[0188] The oral composition was diluted 3 times with the above-mentioned saccharification solution, centrifuged, and the resulting supernatant was used as the test solution.

[0189] Two dentin blocks, prepared using the same method as evaluation method 1 after staining, were each immersed in 2 mL of the following solution and reacted at 37°C for 7 days:

[0190] (i) Glycated solution (without oral composition: glycated control),

[0191] (ii) Test solution.

[0192] After the reaction, 6N HCl solution (20 μL / mg tooth weight) was added to the dentin block, and hydrolysis was carried out at 110°C for 16 hours. The resulting solution was measured using a microplate reader (FlexStation 3, Molecular Devices). The fluorescence at 385 nm produced by irradiation with 335 nm excitation light (measurement index: pentosidine) was measured. The obtained fluorescence intensity was compared with that of 9% ribose solution and various test solutions.

[0193] The amount of AGEs generated was calculated as a relative value with the fluorescence intensity of the glycation control group set to "1".

[0194] It can be said that the lower the relative AGEs value, the higher the anti-aging effect.

[0195] Relative AGEs value = (fluorescence intensity of each experimental group) / (fluorescence intensity of the glycation control group)

[0196] A relative value below 0.8 is considered acceptable.

[0197] [Table 1]

[0198]

[0199] [Table 2]

[0200]

[0201] [Table 3]

[0202]

[0203] [Table 4]

[0204]

[0205] [Table 5]

[0206]

[0207] As shown in Tables 1-4, the oral compositions of Examples 1-20 exhibit excellent effects in inhibiting internal yellowing and AGEs formation.

[0208] As shown in Table 5, in Comparative Example 1, where the content of component (A) was 0.1% by mass, the effects of inhibiting internal yellowing and inhibiting AGEs formation were both poor.

[0209] In Comparative Example 2, which does not contain component (B), the effects of inhibiting internal yellowing and inhibiting AGEs formation are worse than those of the Example.

[0210] (B) In Comparative Example 3, where the enzyme activity of component B was 2 U / g, the inhibition effects on internal yellowing and AGEs formation were worse than those of the Example.

[0211] As can be seen from the above, the oral composition of the present invention has excellent effects in inhibiting yellowing of the tooth interior and anti-aging.

[0212] Furthermore, in Example 1 above, flavoring compositions B to X, as described in Tables 6 to 8, were used to replace flavoring composition A. Other toothpaste compositions with the same composition were prepared, and all showed excellent effects in inhibiting yellowing of teeth and anti-aging. The compositions of flavorings 1 to 9 and solvent 1, as described in Tables 6 to 8, are shown in Tables 9 to 18.

[0213] It should be noted that "removing a% fore-fraction" in the table refers to removing the initial a% when fractionating essential oils, and "removing b% fore-fraction / rear fraction" refers to removing the initial b% and the final b% when fractionating essential oils.

[0214] [Table 6]

[0215]

[0216] [Table 7]

[0217]

[0218] [Table 8]

[0219]

[0220] [Table 9]

[0221]

[0222] [Table 10]

[0223]

[0224] [Table 11]

[0225]

[0226] [Table 12A]

[0227]

[0228] [Table 12B]

[0229]

[0230] [Table 13]

[0231]

[0232] [Table 14]

[0233]

[0234] [Table 15A]

[0235]

[0236] [Table 15B]

[0237]

[0238] [Table 16A]

[0239]

[0240] [Table 16B]

[0241]

[0242] [Table 16C]

[0243]

[0244] [Table 16D]

[0245]

[0246] [Table 16E]

[0247]

[0248] [Table 16F]

[0249]

[0250] [Table 16G]

[0251]

[0252] [Table 16H]

[0253]

[0254] [Table 16I]

[0255]

[0256] [Table 16J]

[0257]

[0258] [Table 17]

[0259]

[0260] [Table 18]

[0261]

[0262] It should be noted that the technical means of the present invention have been described through specific examples, but those skilled in the art will understand that the present invention is not limited thereto.

[0263] The embodiments of the present invention have been described above, but these descriptions are exemplary and not exhaustive, and are not limited to the disclosed embodiments. Various modifications and variations will be apparent to those skilled in the art without departing from the scope and spirit of the described embodiments. The terminology used in this specification is chosen to best explain the principles of the embodiments, practical applications, or market improvements, or to enable those skilled in the art to understand the embodiments disclosed herein.

Claims

1. An oral composition comprising: (A) gluconate, and (B) Select one or more from the group consisting of glucose oxidase, papain, amylase, lipase, superoxide dismutase, catalase, and xylanase. The content of component (A) is 0.2 to 5% by mass relative to the total mass of the oral composition. The enzyme activity of component (B) is 10-500 U / g per 1g of oral composition.

2. The oral composition according to claim 1, wherein, The component (A) is selected from one or more of the group consisting of calcium gluconate, sodium gluconate, copper gluconate and zinc gluconate.

3. The oral composition according to claim 1, wherein, The ratio expressed as [content of component (A) (mass%)] / [enzyme activity of component (B) (U / g)] is 0.001~0.

05.

4. The oral composition according to claim 1, further comprising (C) one or more selected from the group consisting of polyoxyethylene hydrogenated castor oil and fatty acid amamidopropyl betaine.

5. The oral composition according to claim 4, wherein, The content of component (C) is 0.1 to 3% of the total mass of the oral composition.

6. The oral composition according to claim 1, further comprising (D) condensed phosphate.

7. The oral composition according to claim 6, wherein, The content of component (D) is 0.1 to 3% of the total mass of the oral composition.

8. The oral composition according to claim 1, further comprising: (C) Select one or more from the group consisting of polyoxyethylene hydrogenated castor oil and fatty acid amyl betaine. (D) Condensed phosphate, The ratio expressed as [(B) enzyme activity (U / g)] / [(C) content (mass%) + (D) content (mass%)] is 14~67.

Images