Oral composition

Abstract

[Problem] To provide an oral composition which inhibits irritation to the outer and inner parts of teeth by peroxide, more effectively exerts an anti-glycation action of a gluconate on dentin, exerts a yellowing inhibition effect on the inner part of teeth, 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 a peroxide and a peroxide generator, the content of the (A) component being 0.2 to 5 mass% relative to the total mass of the oral composition, and the active oxygen amount of the (B) component being 0.001 to 2.5 mass%.

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] In addition, to improve safety and user experience, it is also necessary to suppress the irritation to the inside and outside of teeth caused by peroxides.

[0010] The purpose of this invention is to provide an oral composition that inhibits the external and internal irritation of teeth caused by peroxides, more effectively exerts the anti-glycation effect of gluconate on dentin, exerts an inhibitory effect on yellowing of the tooth interior, and exerts an anti-aging effect.

[0011] Solution for solving the problem

[0012] 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.

[0013] The inventors focused on this point and studied the effect of combining gluconate with peroxide. Their results showed that peroxide generates reactive oxygen species, which react with and remove staining substances and organic matter on the tooth surface, thereby increasing the permeability of the tooth surface and allowing gluconate to easily reach the dentin.

[0014] The inventors have also discovered that when gluconate and peroxide are used together, the irritation to the inside and outside of the tooth is mitigated.

[0015] The present invention has the following aspects.

[0016] [1] An oral composition comprising:

[0017] (A) gluconate, and

[0018] (B) Select one or more from the group consisting of peroxides and peroxide-generating agents.

[0019] The content of component (A) is 0.2 to 5% by mass relative to the total mass of the oral composition.

[0020] The reactive oxygen species content of component (B) is 0.001 to 2.5% by mass.

[0021] [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.

[0022] [3] The oral composition according to [1] or [2], wherein one or more of the group consisting of peroxides and peroxide generating agents is one or more of the group consisting of hydrogen peroxide, urea peroxide, phthalimide peroxyhexanoic acid, and a combination of glucose oxidase and glucose.

[0023] [4] The oral composition according to any one of [1] to [3], wherein the ratio expressed as [content of (A) component (mass%)] / [active oxygen content of (B) component (mass%)] is 0.2 to 500.

[0024] [5] The oral composition according to any one of [1] to [4] further comprises (C) polyethylene glycol.

[0025] [6] The oral composition according to [5], wherein the average molecular weight of component (C) is 300 to 1100.

[0026] [7] The oral composition according to [5] or [6], wherein the content of component (C) is 10 to 50% by mass relative to the total mass of the oral composition.

[0027] [8] The oral composition according to any one of [1] to [7], wherein the content of component (A) is 0.5 to 5 by mass relative to the total mass of the oral composition.

[0028] [9] The oral composition according to any one of [1] to [8], wherein the active oxygen content of component (B) is 0.5 to 2.5 by mass.

[0029] The effects of the invention

[0030] According to the present invention, an oral composition is available that can suppress the external and internal irritation of teeth caused by peroxides, more effectively exert the anti-glycation effect of gluconate on dentin, exert the effect of inhibiting yellowing inside teeth, and exert the effect of anti-aging. 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) works synergistically with (B) to exert an anti-aging effect through whitening and anti-glycation effects within the tooth interior. Additionally, (A) mitigates the external and internal irritation to the tooth caused by peroxides.

[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 peroxides and peroxide generating agents. Component (B) generates reactive oxygen species on the tooth surface, which react with and remove staining substances and organic matter on the tooth surface, thereby increasing the permeability of the tooth surface and allowing component (A) to easily reach the dentin. Thus, through the whitening effect and anti-glycation effect inside the tooth, it exerts an anti-aging effect.

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

[0051] Peroxides can be categorized as either inorganic or organic.

[0052] Examples of inorganic peroxides include hydrogen peroxide, urea peroxide (urea peroxide: CO(NH2)·H2O2), calcium peroxide, magnesium peroxide, ammonium persulfate, potassium persulfate, potassium chlorate, potassium bromate, potassium superphosphate, perborate, and percarbonate. Among these, hydrogen peroxide and urea peroxide are preferred.

[0053] Examples of organic peroxides include alkyl peroxides and aryl peroxides. Preferred examples include: (a) peroxybenzoic acid and its cyclically substituted derivatives, such as alkyl peroxybenzoic acid, or peroxy-α-naphthoic acid and magnesium monoperoxyphthalate; (b) aliphatic or substituted aliphatic peroxides, such as peroxylauric acid, peroxystearic acid, ε-phthaliminoperoxyhexanoic acid [phthaliminoperoxyhexanoic acid (PAP)], o-carboxybenzoiminoperoxyhexanoic acid, N-nonenamide peroxyhexanoic acid and N-nonenyl... (c) Aliphatic and aromatic aliphatic peroxydicarboxylic acids, such as 1,12-disperoxycarboxylic acid, 1,9-disperoxyazelic acid, disperoxysepiacetic acid, disperoxytetrazoic acid, disperoxyphthalic acid, 2-decyldisperoxybutane-1,4-diacid, N,N-terephthaloyldi(6-aminoperoxyhexanoic acid); (d) aliphatic or aromatic hydrogen peroxide compounds, such as tert-butylhydrogen peroxide, cumene hydroperoxide, etc. Among these, phthalimide peroxyhexanoic acid is preferred.

[0054] As peroxide generating agents, substances that can generate inorganic or organic peroxides when used in a dental cleaning composition can be listed. For example, glucose oxidase generates hydrogen peroxide by reacting with glucose. Therefore, the combination of glucose oxidase and glucose is included in component (B) as an inorganic peroxide generating agent. As peroxide generating agents, in addition to combinations of glucose oxidase and glucose, other examples include combinations of lactose oxidase and lactose, galactose oxidase and galactose, uricase oxidase and uric acid, ethanol oxidase and ethanol, cholesterol oxidase and cholesterol, glycolate oxidase and glycolic acid, malate oxidase and malic acid, hexose oxidases other than glucose oxidase and hexose, gluconolactone oxidase and gluconolactone, amine oxidases and various amines, choline oxidases and choline, xanthine oxidases and xanthine, oxalate oxidases and oxalate, sarcosine oxidases and sarcosine, pyranose oxidases and pyranose, glycerol oxidases and glycerol, and amino acid oxidases and amino acids.

[0055] (B) The ingredients can be a single type or a combination of two or more types.

[0056] The reactive oxygen content of component (B) is 0.001 to 2.5% by mass relative to the total mass of the oral composition, preferably 0.5 to 2.5% by mass. By keeping the reactive oxygen content of component (B) within the above range, glycation reaction in dentin can be inhibited, thereby exerting an inhibitory effect on yellowing of the tooth interior.

[0057] If the reactive oxygen species content of component (B) is less than 0.001% 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 reactive oxygen species content of component (B) is greater than 2.5% by mass, it may cause damage to the tooth surface and gums, reducing safety and user experience.

[0058] In this specification, the amount of active oxygen in component (B) of the dental cleaning composition is a value determined using a known iodine titration method.

[0059] Specifically, acetic acid solution is added to the sample to create acidic conditions. When potassium iodide is added, the peroxide reacts with the potassium iodide to produce iodine. The solution turns blue when starch aqueous solution is added as an indicator. The amount of iodine produced is titrated with a standard sodium thiosulfate solution. The endpoint is reached when the blue color disappears and the solution becomes colorless. Based on the volume of sodium thiosulfate used in the titration, the content of reactive oxygen species in the sample (in mass%) is calculated.

[0060] In some preferred embodiments, the reactive oxygen species content of component (B) is preferably 0.05% by mass or more, 0.1% by mass or more, 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, or 1.2% by mass or more, and preferably less than 2.4% by mass, less than 2.3% by mass, less than 2.2% by mass, less than 2.1% by mass, less than 2% by mass, less than 1.9% by mass, less than 1.8% by mass, less than 1.7% by mass, less than 1.6% by mass, less than 1.5% by mass, less than 1.4% by mass, or less than 1.3% by mass.

[0061] In some preferred embodiments, the ratio, expressed as [content of component (A) (mass%)] / [reactive oxygen content of component (B) (mass%)], is preferably 0.2 to 500. By setting the ratio in this way, component (A) and component (B) work synergistically, and based on the whitening and anti-glycation effects inside the teeth, an anti-aging effect is easily achieved.

[0062] In some preferred embodiments, the ratio expressed as [content (mass%) of component (A)] / [reactive oxygen content (mass%) of component (B)] is preferably 0.5 or more, 1 or more, 5 or more, 10 or more, 20 or more, 30 or more, 40 or more, 50 or more, 60 or more, 70 or more, 80 or more, 90 or more, 100 or more, 110 or more, 120 or more, 130 or more, 140 or more, 150 or more, 160 or more, 170 or more, 180 or more, 190 or more, or 200 or more. The values ​​are: above 210, above 220, above 230, above 240, or above 250, preferably below 490, below 480, below 470, below 460, below 450, below 440, below 430, below 420, below 410, below 400, below 390, below 380, below 370, below 360, below 350, below 340, below 330, below 320, below 310, below 300, below 290, below 280, below 270, or below 260.

[0063] <(C) Ingredients>

[0064] In some preferred embodiments, the oral composition of the present invention may further comprise (C) polyethylene glycol. Component (C) serves to soothe the irritation to the outer and inner surfaces of the teeth caused by component (B). Additionally, it further enhances the whitening effect.

[0065] The average molecular weight of component (C) is preferably 300-1100, more preferably 400-1000. If the average molecular weight of component (C) is above the lower limit above, it exhibits excellent adhesion and retention, and tends to remain in the oral cavity for an extended period. If the average molecular weight of component (C) is below the upper limit above, its penetration rate into stains and organic matter deposited on the tooth surface increases, causing these stains to swell further. Consequently, component (B) is more easily accessible, further enhancing the whitening effect. The average molecular weight of component (C) is a value determined by gel permeation chromatography (GPC).

[0066] In some preferred embodiments, the average molecular weight of component (C) is preferably 350 or more, 400 or more, 450 or more, 500 or more, 550 or more, 600 or more, 700 or more, or 750 or more, and preferably 950 or less, 900 or less, 850 or less, or 800 or less.

[0067] Examples of components (C) include polyethylene glycol 200 (average molecular weight 190-210), polyethylene glycol 300 (average molecular weight 280-320), polyethylene glycol 400 (average molecular weight 380-420), polyethylene glycol 600 (average molecular weight 570-630), and polyethylene glycol 1000 (average molecular weight 950-1050). Polyethylene glycol can be a manufactured substance or a commercially available product.

[0068] (C) The ingredients can be a single type or a combination of two or more types.

[0069] The content of component (C) is preferably 10 to 50% by mass relative to the total mass of the oral composition. By keeping the content of component (C) within the above range, it is easier to alleviate the external and internal irritation of the teeth caused by component (B).

[0070] In some preferred embodiments, the content of (C) relative to the total mass of the oral composition is preferably 11% by mass or more, 12% by mass or more, 13% by mass or more, 14% by mass or more, 15% by mass or more, 16% by mass or more, 17% by mass or more, 18% by mass or more, 19% by mass or more, 20% by mass or more, 21% by mass or more, 22% by mass or more, 23% by mass or more, 24% by mass or more, or 25% by mass or more, preferably 49% by mass or less, 48% by mass or less, or 4% by mass or less. Less than 7% by mass, less than 46% by mass, less than 45% by mass, less than 44% by mass, less than 43% by mass, less than 42% by mass, less than 41% by mass, less than 40% by mass, less than 39% by mass, less than 38% by mass, less than 37% by mass, less than 36% by mass, less than 35% by mass, less than 34% by mass, less than 33% by mass, less than 32% by mass, less than 31% by mass, less than 30% by mass, less than 29% by mass, less than 28% by mass, less than 27% by mass, or less than 26% by mass.

[0071] <Other Ingredients>

[0072] 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 (such as calcium phosphate), binders (such as thickening silica, polyvinylpyrrolidone, etc.), humectants (such as glycerin), sweeteners (such as saccharin), flavorings, pH adjusters, preservatives, pharmaceutically active ingredients (such as sodium pyrophosphate, sodium monofluorophosphate, etc.), and surfactants (such as sodium lauryl sulfate).

[0073] As a solvent, water can be listed. As water, purified water, sterile purified water, water for injection, etc. can be listed.

[0074] The water content in oral compositions can be appropriately set according to the product form and method of use of the oral composition.

[0075] 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.

[0076] 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.

[0077] Dosage Forms of Oral Compositions

[0078] 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.

[0079] 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.

[0080] 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.

[0081] 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.

[0082] 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.

[0083] Methods for manufacturing oral compositions

[0084] 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.

[0085] 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.

[0086] The resulting toothpaste can be manufactured into a product by storing it in a specified container (laminated tube).

[0087] 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 suitable for toothpaste compositions can be used as the container. Examples of containers include plastic containers made of polyethylene, polypropylene, polyethylene terephthalate, and nylon.

[0088] 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.

[0089] 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.

[0090] Methods for cleaning teeth

[0091] The present invention provides a method for cleaning teeth, comprising applying the oral composition of the present invention to the tooth surface.

[0092] 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.

[0093] Example

[0094] 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.

[0095] It should be noted that in the following examples, unless otherwise specified, "%" as the unit of content means "mass %".

[0096] <Ingredients Used>

[0097] [(A) Ingredient]

[0098] Calcium gluconate: manufactured by Zhengzhou Ruipu Biological Engineering Co., Ltd.

[0099] Sodium gluconate: manufactured by Jungbunzlauer Shandong Fuyang Bio-tech and Xingfa Group.

[0100] Copper gluconate: manufactured by Hebei Chuanghai Biotechnology Co., Ltd.

[0101] Zinc gluconate: manufactured by Hebei Chuanghai Biotechnology Co., Ltd.

[0102] [(B) Component]

[0103] Hydrogen peroxide: manufactured by Evonik.

[0104] Urea peroxide: manufactured by Shanxi Shundu Group Co., Ltd.

[0105] Phthalimide peroxyhexanoic acid: manufactured by Shandong Look Chemical Co., Ltd.

[0106] [(C) Component]

[0107] Polyethylene glycol 400: (manufactured by LiaoNing Oxiranpharm, trade name: PEG-400).

[0108] Polyethylene glycol 600: (manufactured by LiaoNing Oxiranpharm, trade name: PEG-600).

[0109] Polyethylene glycol 1000: (Sanyo Chemical Industry Co., Ltd., trade name: PEG-1000).

[0110] [water]

[0111] Purified water.

[0112] [Common Ingredients (Optional Ingredients)]

[0113] Sodium pyrophosphate: Manufactured by Hubei Xingfa Chemicals Group.

[0114] Sodium saccharin: Henan Kaifeng Pingmei Shenma Xinghua Fine Chemical Co., Ltd.

[0115] Sodium lauryl sulfate (K12), manufactured by Dongming Juhua Chemical Co., Ltd.

[0116] Thickening silica: Made by Evonik, product number: Zeodent (registered trademark) 165.

[0117] Calcium phosphate: Manufactured by Hebei Chuanghai Biotechnology Co., Ltd.

[0118] Sodium monofluorophosphate: manufactured by Hubei Xingfa Chemical Group Co., Ltd.

[0119] Polyvinylpyrrolidone: Manufactured by Hefei TNJ Chemical Industry Co., Ltd.

[0120] Fragrance composition: Fragrance composition A as described in Table 4.

[0121] Glycerin: Produced by Wilmar International Limited.

[0122] <Examples 1-15, Comparative Examples 1-3>

[0123] Using the above-mentioned ingredients as raw materials, toothpaste compositions having the formulations shown in Tables 1-4 below were prepared. Water-soluble ingredients (excluding binders, fragrance compositions, surfactants, and abrasives in Tables 1-4) 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.

[0124] Empty columns in the table indicate that the ingredient was not mixed. The "balance" of purified water indicates that the total amount of the toothpaste composition is 100%.

[0125] The obtained toothpaste composition was evaluated as follows. The results are recorded in the table.

[0126] <Evaluation Methods>

[0127] Evaluation Method 1: Yellowing Inhibition Test of Bovine Teeth

[0128] The anti-yellowing effect of the oral compositions of Examples 1-15 and Comparative Examples 1-3 was evaluated by the following methods.

[0129] 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.

[0130] 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).

[0131] <Step A>

[0132] 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.

[0133] <Step B>

[0134] 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.

[0135] The saccharification solution was prepared using PBS (pH 7.4) to ensure it contained 9% ribose.

[0136] The toothpaste composition was diluted 3 times with the above-mentioned saccharification solution, centrifuged, and the resulting supernatant was used as the test solution.

[0137] The stained dentin blocks were immersed in 2 mL of the test solution and reacted at 37°C for 7 days.

[0138] 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).

[0139] 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 performed on a fixed area in the center of the test surface.

[0140] It can be said that the lower the ΔE value, the higher the effect of inhibiting internal yellowing.

[0141]

[0142] (L1,a1,b1: before saccharification, L2,a2,b2: after saccharification)

[0143] Those with a ΔE value below 12 are considered qualified.

[0144] Evaluation Method 2: AGEs (Advanced Glycation End Products) Formation Inhibition Assay

[0145] The toothpaste compositions of Examples 1-15 and Comparative Examples 1-3 were evaluated for their AGEs generation inhibition effect by the following method.

[0146] The saccharification solution was prepared using PBS (pH 7.4) to ensure it contained 9% ribose.

[0147] The toothpaste composition was diluted 3 times with the above-mentioned saccharification solution, centrifuged, and the resulting supernatant was used as the test solution.

[0148] 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:

[0149] (i) Saccharified solution (without toothpaste composition: saccharification control),

[0150] (ii) Test solution.

[0151] 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 (Molecular Devices, Flex Station3). The fluorescence at 385 nm produced by irradiation with 335 nm excitation light (as measured by pentosidine) was measured. The fluorescence intensity was compared with that of 9% ribose solution and other test solutions.

[0152] The amount of AGEs generated was calculated as a relative value with the fluorescence intensity of the glycation control group set to "1".

[0153] It can be said that the lower the relative AGEs value, the higher the anti-aging effect.

[0154] Relative AGEs value = (fluorescence intensity of each experimental group) / (fluorescence intensity of the glycation control group)

[0155] A relative value below 0.8 is considered acceptable.

[0156] Evaluation Method 3: Stimulation Inhibition Effect on Teeth

[0157] Ten subjects were used. Approximately 1g of the toothpaste composition was applied to a toothbrush. The stimulation during brushing for 3 minutes was assessed. The score was set as follows: no stimulation was not felt at all (4 points), slight stimulation was felt (3 points), stimulation was felt (2 points), and strong stimulation was felt (1 point). The average score was calculated.

[0158] The higher the score, the greater the stimulus-inhibition effect.

[0159] [Table 1]

[0160]

[0161] [Table 2]

[0162]

[0163] [Table 3]

[0164]

[0165] [Table 4]

[0166]

[0167] As shown in Tables 1-3, the toothpaste compositions of Examples 1-15 exhibit excellent effects in inhibiting internal yellowing and AGEs formation. Furthermore, they also demonstrate excellent irritation inhibition.

[0168] As shown in Table 4, 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.

[0169] In Comparative Example 2, which does not contain component (B), the effects of inhibiting internal yellowing and inhibiting AGEs formation were both poor.

[0170] (B) In Comparative Example 3, where the reactive oxygen species content of component B was 0.0005% by mass, the effects of inhibiting internal yellowing and inhibiting AGEs formation were both poor.

[0171] 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.

[0172] Furthermore, in Example 1 above, flavoring compositions B to X as described in Tables 5 to 7 were used to replace flavoring composition A, and toothpaste compositions with the same composition were prepared. The results showed excellent inhibition of yellowing of the teeth and anti-aging effects. The compositions of flavorings 1 to 9 and solvent 1 as described in Tables 5 to 7 are shown in Tables 8 to 17.

[0173] 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.

[0174] [Table 5]

[0175]

[0176] [Table 6]

[0177]

[0178] [Table 7]

[0179]

[0180] [Table 8]

[0181]

[0182] [Table 9]

[0183]

[0184] [Table 10]

[0185]

[0186] [Table 11A]

[0187]

[0188] [Table 11B]

[0189]

[0190] [Table 12]

[0191]

[0192] [Table 13]

[0193]

[0194] [Table 14A]

[0195]

[0196] [Table 14B]

[0197]

[0198] [Table 15A]

[0199]

[0200] [Table 15B]

[0201]

[0202] [Table 15C]

[0203]

[0204] [Table 15D]

[0205]

[0206] [Table 15E]

[0207]

[0208] [Table 15F]

[0209]

[0210] [Table 15G]

[0211]

[0212] [Table 15H]

[0213]

[0214] [Table 15I]

[0215]

[0216] [Table 15J]

[0217]

[0218] [Table 16]

[0219]

[0220] [Table 17]

[0221]

[0222] 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.

[0223] 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 peroxides and peroxide-generating agents. The content of component (A) is 0.2 to 5% by mass relative to the total mass of the oral composition. The reactive oxygen species content of component (B) is 0.001 to 2.5% by mass.

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 group consisting of one or more peroxides and peroxide generating agents is further divided into one or more groups consisting of hydrogen peroxide, urea peroxide, phthalimide peroxyhexanoic acid, and a combination of glucose oxidase and glucose.

4. The oral composition according to claim 1, wherein, The ratio, expressed as [content of component (A) (mass%)] / [active oxygen content of component (B) (mass%)], is 0.2 to 500.

5. The oral composition according to claim 1, further comprising (C) polyethylene glycol.

6. The oral composition according to claim 5, wherein, The average molecular weight of component (C) is 300~1100.

7. The oral composition according to claim 5, wherein, The content of component (C) is 10 to 50% by mass relative to the total mass of the oral composition.

8. The oral composition according to claim 1, wherein, The content of component (A) is 0.5 to 5% of the total mass of the oral composition.

9. The oral composition according to claim 1, wherein, The reactive oxygen species content of component (B) is 0.5 to 2.5% by mass.

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