Liquid oral composition

Abstract

The present application provides a liquid oral composition comprising component (a): copper gluconate, component (b): zinc chloride and component (c): L-sodium aspartate.

Description

Technical Field

[0001] This invention relates to a liquid oral composition. Background Technology

[0002] As a technique for incorporating metal compounds into oral preparations, there are techniques described in Patent Documents 1 to 5.

[0003] Patent Document 1 (Japanese Patent Application Publication No. 2003-137755) discloses an oral composition containing a compound that releases one or more metal ions selected from copper, zinc, aluminum, iron, and tin. This composition is formulated with one or more compounds selected from L-menthol derivatives and N-ethyl-p-menthane-3-carboxamide (claim 1). As a specific example of the oral composition, a mouthwash is described, containing specific amounts of specific ingredients including copper gluconate and zinc chloride (Example 26). According to this document, the metallic taste of the oral composition is improved, resulting in a pleasant user experience and high commercial value (paragraph 0023).

[0004] In Patent Document 2 (Japanese Patent Application Publication No. 2000-159647), as a technology for improving the user experience of a toothpaste composition (paragraph 0003), a toothpaste composition is described, which is formed by combining one or more selected from amino acids and their salts and proteins in a toothpaste composition containing one or more selected from condensed phosphates, bicarbonates and bisulfates and a water-soluble transition metal compound (claim 1).

[0005] Patent document 3 (Japanese Patent Application Publication No. 2019-108276) discloses an oral composition containing pyrrolidone carboxylic acid or its inorganic base salt, and zinc oxide (claim 1). According to this document, an oral composition can be provided that improves the whitening effect on the root surface of teeth and its persistence, and reduces the impact of metallic taste on the user experience (paragraph 0009).

[0006] Patent Document 4 (Japanese Patent Application Publication No. 2022-99623) and Patent Document 5 (Japanese Patent Application Publication No. 2022-99624) disclose oral compositions that use water-soluble copper salts such as copper gluconate, which have deodorizing effects, and are widely used in dental flossers or mouthwashes to prevent halitosis (paragraph 0002 of Patent Document 4, paragraph 0002 of Patent Document 5). The aim of these documents is to provide oral compositions containing water-soluble copper salts that suppress metallic taste (paragraph 0006 of Patent Document 4, paragraph 0006 of Patent Document 5), and to describe oral compositions containing water-soluble copper salts and specific plant extracts (claim 1 of Patent Document 4, claim 1 of Patent Document 5).

[0007] Existing technical documents

[0008] Patent documents

[0009] Patent Document 1: Japanese Patent Application Publication No. 2003-137755

[0010] Patent Document 2: Japanese Patent Application Publication No. 2000-159647

[0011] Patent Document 3: Japanese Patent Application Publication No. 2019-108276

[0012] Patent Document 4: Japanese Patent Application Publication No. 2022-99623

[0013] Patent Document 5: Japanese Patent Application Publication No. 2022-99624 Summary of the Invention

[0014] According to the research of the inventors, it has been newly discovered that when copper gluconate and zinc chloride are added to the oral composition, the metallic taste increases and the user experience decreases. In order to suppress this decrease in user experience, for example, when a metal chelating agent is further added to the composition, the halitosis suppression effect is reduced.

[0015] Therefore, the present invention provides a technology that suppresses the metallic taste of liquid oral compositions while providing excellent halitosis suppression.

[0016] According to the present invention, the following liquid oral composition and method for suppressing metallic taste are available.

[0017] [1] A liquid oral composition comprising the following components (a) to (c):

[0018] (a) Copper gluconate

[0019] (b) Zinc chloride

[0020] (c) Sodium L-aspartate.

[0021] [2] The liquid oral composition as described in [1], wherein the content of the above component (c) is 0.1% by mass or more and 2% by mass or less relative to the total liquid oral composition.

[0022] [3] The liquid oral composition as described in [1] or [2], wherein the mass ratio (c) / ((a)+(b)) of the content of the above-mentioned component (c) in the liquid oral composition to the total content of the above-mentioned components (a) and (b) is 0.1 or more and 20 or less.

[0023] [4] The liquid oral composition as described in any one of [1] to [3] is a metallic taste inhibitor.

[0024] [5] The liquid oral composition as described in any one of [1] to [4] is a mouthwash.

[0025] [6] A method for suppressing metallic taste, comprising the step of incorporating the following ingredient (c) into a liquid oral composition comprising the following ingredients (a) and (b),

[0026] (a) Copper gluconate

[0027] (b) Zinc chloride

[0028] (c) Sodium L-aspartate.

[0029] It should be noted that any combination of these components, or any scheme derived by transforming the present invention into methods, apparatuses, etc., is also valid as a form of the present invention.

[0030] According to the present invention, the metallic taste of liquid oral composition can be suppressed, while its halitosis suppression effect is excellent. Detailed Implementation

[0031] The embodiments of the present invention will be described below. In this embodiment, the composition may contain each component individually or in combination of two or more components.

[0032] In this specification, the "~" sign indicating a numerical range means above and below, with both values ​​at either end included.

[0033] (Liquid oral composition)

[0034] In this embodiment, the liquid oral composition comprises the following components (a) to (c).

[0035] (a) Copper gluconate

[0036] (b) Zinc chloride

[0037] (c) Sodium L-aspartate

[0038] The liquid oral composition in this embodiment contains the above-mentioned components (a) to (c), thus it can suppress the metallic taste of the liquid oral composition and obtain an excellent halitosis suppression effect.

[0039] Furthermore, in this embodiment, the liquid oral composition is also suitable as a metallic taste inhibitor.

[0040] The following is an explanation of each component.

[0041] (ingredient (a))

[0042] Ingredient (a) is copper gluconate. Ingredient (a) may be a commercially available product, for example.

[0043] The content of component (a) in the liquid oral composition is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, even more preferably 0.03% by mass or more, and even more preferably 0.08% by mass or more, relative to the total liquid oral composition. This improves the halitosis suppression effect.

[0044] Furthermore, the content of component (a) in the liquid oral composition is preferably 10% by mass or less, more preferably 1% by mass or less, even more preferably 0.5% by mass or less, even more preferably 0.3% by mass or less, and even more preferably 0.2% by mass or less, relative to the total liquid oral composition. This improves the metallic taste suppression effect. Additionally, the content of component (a) in the liquid oral composition can be below its solubility in the solvent.

[0045] (Component (b))

[0046] Ingredient (b) is zinc chloride. Ingredient (b) may be a commercially available product, for example.

[0047] The content of component (b) in the liquid oral composition is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, even more preferably 0.03% by mass or more, and even more preferably 0.08% by mass or more, relative to the total liquid oral composition. This improves the halitosis suppression effect.

[0048] Furthermore, the content of component (b) in the liquid oral composition is preferably 10% by mass or less, more preferably 1% by mass or less, even more preferably 0.5% by mass or less, even more preferably 0.3% by mass or less, and even more preferably 0.2% by mass or less, relative to the total liquid oral composition. This improves the metallic taste suppression effect. Additionally, the content of component (b) in the liquid oral composition can be below its solubility in the solvent.

[0049] The mass ratio (b) / (a) of the content of component (b) to the content of component (a) in the liquid oral composition is preferably 0.1 or more, more preferably 0.3 or more, even more preferably 0.5 or more, and preferably 10 or less, more preferably 5 or less, and even more preferably 3 or less. This allows for a more ideal effect in suppressing metallic taste and halitosis.

[0050] (Component (c))

[0051] Ingredient (c) is sodium L-aspartate. Ingredient (c) may be a commercially available product, for example.

[0052] The content of component (c) in the liquid oral composition is preferably 0.1% by mass or more, more preferably 0.2% by mass or more, even more preferably 0.5% by mass or more, and even more preferably 0.8% by mass or more, relative to the total liquid oral composition. This improves the effect of suppressing metallic taste.

[0053] Furthermore, the content of component (c) in the liquid oral composition is preferably 2% by mass or less, more preferably 1.5% by mass or less, and even more preferably 1.2% by mass or less, relative to the total liquid oral composition. This improves the metallic taste suppression effect. Additionally, the content of component (c) in the liquid oral composition can be below its solubility in the solvent.

[0054] The mass ratio (c) / ((a)+(b)) of the content of component (c) in the liquid oral composition to the total content of components (a) and (b) is preferably 0.1 or more, more preferably 1 or more, further preferably 3 or more, and preferably 20 or less, more preferably 10 or less, and further preferably 7 or less. This improves the effect of suppressing metallic taste.

[0055] Liquid oral compositions may also contain ingredients other than those in (a) to (c).

[0056] For example, a liquid oral composition may also contain at least one compound selected from copper compounds other than component (a) and zinc compounds other than component (b).

[0057] In addition, the liquid oral composition specifically contains water.

[0058] (water)

[0059] The water content in a liquid oral composition can be, for example, the remainder after excluding components other than water from the liquid oral composition.

[0060] Furthermore, the water content in the liquid oral composition is preferably 50% by mass or more, more preferably 60% by mass or more, and even more preferably 70% by mass or more, and preferably 99.9% by mass or less, more preferably 99.8% by mass or less, and even more preferably 99% by mass or less, relative to the total liquid oral composition.

[0061] Liquid oral compositions are, for example, aqueous compositions, preferably aqueous compositions containing 50% by mass or more of water.

[0062] (ethanol)

[0063] Liquid oral compositions may further contain ethanol.

[0064] The ethanol content in the liquid oral composition is preferably 0.1% by mass or more, more preferably 1% by mass or more, and even more preferably 2% by mass or more. This provides a pleasant and comfortable user experience.

[0065] Furthermore, the ethanol content in the liquid oral composition is preferably 30% by mass or less, more preferably 20% by mass or less, even more preferably 10% by mass or less, even more preferably 7.5% by mass or less, and even more preferably 5% by mass or less. This can suppress strong irritation to the oral cavity. From this point of view, it is also preferable that the liquid oral composition does not contain ethanol, that is, the ethanol content is 0% by mass, or the liquid oral composition contains ethanol and its content is 5% by mass or less.

[0066] (Other ingredients)

[0067] Without impairing the effects of the present invention, the liquid oral composition may also contain components other than those described above.

[0068] Examples of the aforementioned components include, for instance, pharmaceutical ingredients, binders, humectants, flavoring agents, preservatives, colorants, pH adjusters, solvents other than those mentioned above, solubilizers, base agents, cleaning agents, adsorbents, etc., which may be appropriately selected according to the dosage form. Specific examples of added components are shown below, but the components that can be incorporated into the present invention are not limited to these.

[0069] As medicinal ingredients, examples include one or more of the following: antibacterial agents, anti-inflammatory agents, blood circulation promoters, tartar deposit inhibitors, pigment removers, sensory hypersensitivity inhibitors, vitamins, and tartar-degrading enzymes. There are no restrictions on these medicinal ingredients as long as they can be used in pharmaceuticals, etc.

[0070] Among the medicinal ingredients, as bactericides, examples include one or more selected from isopropyl methylphenol, cetylpyridinium chloride, benzalkonium chloride, benzyl chloride, juniper alcohol, chlorhexidine hydrochloride, alkyl diaminoethyl glycine hydrochloride, sodium lauroyl sarcosinate, and triclosan.

[0071] As anti-inflammatory agents, examples include one or more selected from β-glycyrrhetinic acid, glycyrrhetinic acid, glycyrrhizic acid, diammonium glycyrrhizate, disodium glycyrrhizate, trisodium glycyrrhizate, dipotassium glycyrrhizate, monoammonium glycyrrhizate, ε-aminocaproic acid, sodium azulene sulfonate hydrate, allantoin, allantoin dihydroxyaluminate, epidihydrocholesterol, dihydrocholesterol, and hydrochloric acid lysozyme.

[0072] Examples of blood circulation promoters include sodium chloride.

[0073] Examples of dental calculus inhibitors include one or more of disodium hydrogen phosphate, disodium dihydrogen pyrophosphate, sodium pyrophosphate, anhydrous sodium pyrophosphate, tetrasodium pyrophosphate (anhydrous), disodium hydrogen phosphate, sodium hydrogen phosphate hydrate, disodium hydrogen phosphate (crystal), trisodium phosphate, and sodium polyphosphate.

[0074] Examples of pigment removers include one or more of macrogol (Macrogol 200, Macrogol 300, Macrogol 400, Macrogol 600, Macrogol 1000, Macrogol 1500, Macrogol 1540, Macrogol 4000, Macrogol 6000, Macrogol 20000, etc.), sodium polyphosphate, and polyvinylpyrrolidone.

[0075] Examples of inhibitors of hypersensitivity include at least one selected from potassium nitrate and water-soluble aluminum salts.

[0076] As a vitamin preparation, examples include one or more selected from ascorbic acid, L-ascorbic acid, sodium ascorbate, sodium L-ascorbate, pyridoxine hydrochloride, DL-α-tocopherol acetate, tocopherol acetate, dl-α-tocopherol nicotinic acid, and tocopherol nicotinic acid ester.

[0077] Examples of dental plaque-degrading enzymes include glucanase.

[0078] Examples of adhesives include one or more of the following: pullulan, gelatin, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, sodium carboxymethylcellulose, carrageenan, sodium alginate, xanthan gum, sodium polyacrylate, gum arabic, guar gum, locust bean gum, polyvinyl alcohol, carboxyvinyl polymers, tackifying anhydrous silica, and bentonite.

[0079] From the viewpoint of easy rinsing of the mouth, liquid oral compositions are preferably free of xanthan gum, and more preferably free of binders.

[0080] Here, "free of xanthan gum or binder" specifically means that the liquid oral composition does not contain xanthan gum or binder intentionally, and more specifically, that the content of xanthan gum or binder is less than 0.001% by mass relative to the total liquid oral composition.

[0081] As a humectant, any commercially available humectant used as a raw material for pharmaceuticals, food, or cosmetics is acceptable. Examples include polyols. More specifically, examples include one or more selected from sorbitol, glycerin, concentrated glycerin, ethylene glycol, propylene glycol, 1,3-butanediol, propylene glycol (1,3-propanediol), polyethylene glycol, polypropylene glycol, sodium hyaluronate, and hydrolyzed collagen.

[0082] From the viewpoint of reducing irritation to the oral cavity, the humectant is preferably selected from at least one of glycerin and propylene glycol, more preferably glycerin.

[0083] As flavoring agents, examples include one or more selected from monosodium glutamate (MSG), saccharin, sodium saccharin, sucrose, glucose, fructose, lactose, honey, aspartame, stevia, sucralose, inositol, D-sorbitol, D-mannitol, arabinitol, raffinose, lactulose, lactitol, xylitol, erythritol, reduced paragine, paragine, palatinit (registered trademark), acesulfame potassium, trehalose, maltose, maltodextrin or maltitol, neohesperidin dihydrochalcone, perilla syrup, p-methoxycinnamonaldehyde, and semathymidine.

[0084] From the viewpoint that the flavoring agent has a strong sweetness and can be flavored with a small amount, the flavoring agent is preferably selected from at least one of xylitol, sodium saccharin and saccharin, and more preferably selected from at least one of xylitol and sodium saccharin.

[0085] Examples of preservatives include parabens selected from sodium benzoate, methylparaben, ethylparaben, butylparaben, isopropylparaben, propylparaben, isobutylparaben, benzylparaben, etc.; alcohols such as phenoxyethanol; sorbic acid, benzoic acid, dehydroacetic acid, propionic acid and their salts; ethylenediaminetetraacetic acid salt; and one or more of alkyldiamine ethylglycine hydrochloride.

[0086] The amount of preservative in the liquid oral composition may be, for example, 0.01 to 1% by mass relative to the total liquid oral composition.

[0087] As coloring agents, examples include natural pigments such as safflower red pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, red yeast rice pigment, red cabbage blue pigment, carotene pigment, hibiscus pigment, cocoa pigment, spirulina blue pigment, and tamarind pigment; legally permitted pigments such as Red No. 3, Red No. 104, Red No. 105, Red No. 106, Yellow No. 4, Yellow No. 5, Green No. 3, and Blue No. 1; and one or more of riboflavin and titanium dioxide.

[0088] Examples of pH adjusters include one or more acids or bases and buffers such as acetic acid, hydrochloric acid, sulfuric acid, nitric acid, citric acid, phosphoric acid, malic acid, gluconic acid, maleic acid, succinic acid, glutamic acid, pyrophosphate, tartaric acid, acetic acid, sodium hydroxide, potassium hydroxide, sodium acetate, sodium carbonate, sodium citrate, sodium bicitrate, phosphoric acid, sodium phosphate, sodium hydrogen phosphate, sodium dihydrogen phosphate, and potassium dihydrogen phosphate.

[0089] The amount of preservative in the liquid oral composition may be, for example, 0.001 to 1% by mass relative to the total liquid oral composition.

[0090] In addition to water and ethanol, other solvents that can be used include lower alcohols such as propanol.

[0091] To promote the dissolution of the aforementioned additives or active ingredients in water, solubilizers may also be added. Examples of such solubilizers include polyols such as dipropylene glycol.

[0092] Examples of base agents include sodium bicarbonate.

[0093] Sodium polyphosphate can be cited as an example of a cleaning agent.

[0094] Examples of adsorbents include β-cyclodextrin.

[0095] Furthermore, in addition to the above-mentioned components, without prejudice to the contents of this invention, components suitable for use in oral compositions such as liquid oral compositions may also be appropriately incorporated.

[0096] (pH)

[0097] The pH of the liquid oral composition is preferably 4.0 or higher, more preferably 4.5 or higher, and even more preferably 4.7 or higher. This inhibits tooth demineralization.

[0098] In addition, the pH of the liquid oral composition is preferably 7.0 or less, more preferably 6.5 or less, even more preferably 6.0 or less, and even more preferably 5.5 or less.

[0099] The pH of the liquid oral composition can be measured at 25°C using a commercially available pH meter.

[0100] (Liquid formulation)

[0101] Liquid oral compositions are specifically liquid formulations. Liquid formulations are specifically oral administration formulations.

[0102] Specific examples of liquid oral compositions include mouthwash, liquid toothpaste, and oral cooling agents. Mouthwash is preferred. This allows for convenient and easy suppression of halitosis in daily life.

[0103] (Manufacturing method)

[0104] In this embodiment, the liquid oral composition includes, for example, the formulation components (a) to (c) and the process of appropriately incorporating other components.

[0105] (Methods for suppressing metallic taste)

[0106] In this embodiment, the method for suppressing metallic taste includes the step of incorporating the above-mentioned component (c) into a liquid oral composition containing the above-mentioned components (a) and (b).

[0107] According to the above method, the reduction in halitosis suppression effect of the liquid oral composition can be inhibited, while its metallic taste can be effectively suppressed.

[0108] The embodiments of the present invention have been described above, but these are merely examples of the present invention, and various configurations other than those described above may also be used.

[0109] Example

[0110] The following examples and comparative examples illustrate this embodiment in detail, but this embodiment is not limited to these examples.

[0111] (Example 1, Comparative Example 1)

[0112] The ingredients listed in Table 1 were mixed to prepare mouthwashes for each example, and the methods described below were used for evaluation. Details of the ingredients listed in each table are shown below.

[0113] (a) Copper gluconate: Healcious Cu, manufactured by Fusang Chemical Industry Co., Ltd.

[0114] p-Hydroxybenzoate: MEKKINS M, manufactured by Ueno Pharmaceutical Co., Ltd.

[0115] (Preparation method of mouthwash)

[0116] The ingredients listed in Table 1 were mixed to obtain the mouthwashes for each example.

[0117] The pH of the obtained mouthwash at 25°C was measured using a pH meter (Horiba Seisakusho Co., Ltd., LAQUA F-72).

[0118] (Evaluation Method)

[0119] The metallic taste of each mouthwash sample was evaluated using the following methods.

[0120] One participant evaluated the user experience. Each participant held 10 mL of mouthwash in their mouth for 20 seconds, rinsed thoroughly, and then spat it out. The following rating scale was used for evaluation.

[0121] Scoring criteria:

[0122] 5: No metallic taste was detected.

[0123] 4: Almost no metallic taste was detected.

[0124] 3: There is a slight metallic taste, but it is within acceptable limits.

[0125] 2: I can smell a metallic taste

[0126] 1: I noticed a very strong metallic smell.

[0127] Each participant provided one evaluation, and the evaluation was conducted based on the obtained score according to the following evaluation criteria. The evaluation results are shown in Table 1.

[0128] A: 4.0 points or above

[0129] B: 3.0 or above but less than 4.0

[0130] C: Less than 3.0 points

[0131] [Table 1]

[0132]

[0133] According to Table 1, Example 1, which combines ingredients (a) to (c), effectively suppresses the metallic taste of the mouthwash. Furthermore, by using the mouthwash of Example 1, a halitosis suppression effect can be achieved.

[0134] This application claims priority based on Japanese Patent Application No. 2024-029638, filed on February 29, 2024, the entire disclosure of which is incorporated herein by reference.

Claims

1. A liquid oral composition comprising the following components (a) to (c): (a) Copper gluconate, (b) Zinc chloride, (c) Sodium L-aspartate.

2. The liquid oral composition according to claim 1, wherein, The content of component (c) is 0.1% by mass or more and 2% by mass or less relative to the total liquid oral composition.

3. The liquid oral composition according to claim 1 or 2, wherein, The mass ratio (c) / ((a)+(b)) of the content of component (c) in the liquid oral composition to the total content of components (a) and (b) is 0.1 or more and 20 or less.

4. The liquid oral composition according to any one of claims 1 to 3, wherein it is a metallic taste inhibitor.

5. The liquid oral composition according to any one of claims 1 to 4, wherein it is a mouthwash.

6. A method for suppressing metallic taste, comprising the step of incorporating component (c) into a liquid oral composition comprising components (a) and (b) thereof, (a) Copper gluconate, (b) Zinc chloride, (c) Sodium L-aspartate.

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