JP7549566B2 - Oral Composition - Google Patents

Description

The present invention relates to an oral composition.

Conventionally, copper chlorophyllin sodium has been used in various oral compositions since it is an ingredient expected to have an effect of preventing or improving bad breath.
For example, Patent Document 1 discloses an oral solid preparation containing a specific blend ratio of effervescent components, which are carbonates and organic acids, and copper chlorophyllin sodium, and attempts to synergistically enhance the effect of preventing bad breath by effervescence in the mouth. Patent Document 2 discloses an oral composition containing a nitroimidazole derivative and copper chlorophyllin sodium, and aims to improve the effect of preventing bad breath by suppressing the production of volatile sulfur compounds (VSCs) by Fusobacterium nucleatum and Bacteroides gingivalis.

Japanese Patent Application Publication No. 10-236935 Special Publication No. 6-35376

Specific examples of volatile sulfur compounds (VSCs) that cause bad breath include hydrogen sulfide, methyl mercaptan, and dimethyl sulfide, each of which is known to emit a unique odor. The present inventors have discovered that by suppressing the generation of methyl mercaptan, which has a low threshold and emits a unique "bloody" odor and can also be metabolized to dimethyl sulfide, a volatile sulfur compound (VSC) that also has a low threshold, the satisfaction of suppressing bad breath can be increased, particularly for oral cavities with symptoms of protein leakage from the gums.
However, in all of the above patent documents, there is still room for further study regarding suppressing bad breath while focusing on suppressing the generation of methyl mercaptan.

That is, the present invention relates to an oral composition that suppresses the generation of volatile sulfur compounds (VSCs), particularly methyl mercaptan, for a long period of time, thereby exerting an excellent effect in suppressing bad breath and providing a high level of satisfaction.

The inventors conducted various studies and discovered an oral composition that contains specific amounts of sodium copper chlorophyllin and erythritol in a specific mass ratio, thereby significantly suppressing the generation of volatile sulfur compounds (VSCs), particularly methyl mercaptan, and improving the effect of suppressing bad breath.

Thus, the present invention relates to a composition comprising the following components (A) and (B):
The present invention provides an oral composition comprising: (A) 0.001% by mass or more and 0.5% by mass or less of sodium copper chlorophyllin; and (B) erythritol, wherein the mass ratio ((B)/(A)) of the content of component (B) to the content of component (A) is 500 or more and 55,000 or less.

The oral composition of the present invention can significantly suppress the generation of volatile sulfur compounds (VSCs), particularly methyl mercaptan, in the oral cavity, and can extremely effectively reduce the unpleasant sensation caused by bad breath.

The present invention will be described in detail below.
The oral composition of the present invention contains 0.001% by mass or more and 0.5% by mass or less of copper chlorophyllin sodium as component (A). In the oral composition of the present invention, erythritol as component (B) described later has a specific mass ratio with respect to copper chlorophyllin sodium as component (A), so that the generation of methyl mercaptan in the oral cavity can be effectively reduced, and the effect of suppressing bad breath can be dramatically improved.

The content of component (A) in the oral composition of the present invention is 0.001% by mass or more, preferably 0.003% by mass or more, and more preferably 0.005% by mass or more, from the viewpoint of achieving a bad breath suppressing effect. The content of component (A) in the oral composition of the present invention is 0.5% by mass or less, preferably 0.3% by mass or less, and more preferably 0.1% by mass or less, from the viewpoint of suppressing unpleasant sensations such as metallic taste. The content of component (A) in the oral composition of the present invention is 0.001% by mass or more and 0.5% by mass or less, preferably 0.003 to 0.3% by mass, and more preferably 0.005 to 0.1% by mass.

The oral composition of the present invention contains erythritol as component (B). Component (B), in combination with component (A), effectively reduces the generation of methyl mercaptan in the oral cavity, thereby synergistically enhancing the effect of suppressing bad breath.

From the viewpoint of improving the bad breath suppression effect, the content of component (B) in the oral composition of the present invention is preferably 5% by mass or more, more preferably 10% by mass or more, even more preferably 20% by mass or more, and preferably 55% by mass or less, more preferably 50% by mass or less, and even more preferably 45% by mass or less. The content of component (B) in the oral composition of the present invention is preferably 5 to 55% by mass, more preferably 10 to 50% by mass, and even more preferably 20 to 45% by mass.

The mass ratio ((B)/(A)) of the content of component (B) to the content of component (A) is 500 or more, preferably 1000 or more, more preferably 1500 or more, and 55000 or less, preferably 27500 or less, more preferably 14000 or less, from the viewpoint of enhancing the synergistic effect of components (A) and (B) and improving the bad breath suppression effect.

The oral composition of the present invention preferably further contains glycyrrhetinic acid (C), which contributes to the plaque formation inhibitory effect and anti-inflammatory effect brought about by glycyrrhetinic acid, maintains the health of the gums, prevents or improves periodontal disease itself, and eliminates the generation of VSCs at the source, and in particular effectively inhibits the generation of methyl mercaptan, which is believed to further enhance the bad breath suppressing effect of the present invention.
Examples of such component (C) include α-glycyrrhetinic acid, β-glycyrrhetinic acid, etc. Among these, β-glycyrrhetinic acid is preferred.

The content of component (C) in the oral composition of the present invention is preferably 0.001% by mass or more, more preferably 0.005% by mass or more, and even more preferably 0.01% by mass or more, from the viewpoint of preventing or improving periodontal disease itself and effectively enhancing the effect of suppressing bad breath. The content of component (C) in the oral composition of the present invention is preferably 1% by mass or less, more preferably 0.7% by mass or less, and even more preferably 0.5% by mass or less, from the viewpoint of ensuring good solubility or dispersibility of component (C). The content of component (C) in the oral composition of the present invention is preferably 0.001 to 1% by mass, more preferably 0.005 to 0.7% by mass, and even more preferably 0.01 to 0.5% by mass.

The mass ratio ((B)/(C)) of the content of component (B) to the content of component (C) is 10 or more, preferably 50 or more, more preferably 150 or more, and is 55,000 or less, preferably 27,500 or less, more preferably 10,000 or less, from the viewpoint of enhancing the synergistic effect of components (A) and (B) and dramatically improving the bad breath suppression effect.

The oral composition of the present invention preferably contains water (D). This allows the above-mentioned components to be dissolved or dispersed well, while also increasing the diffusibility of the oral composition after application in the oral cavity, resulting in an excellent effect of suppressing bad breath.

The content of component (D) in the oral composition of the present invention is preferably 1% by mass or more, more preferably 5% by mass or more, even more preferably 8% by mass or more, and is preferably 99% by mass or less, more preferably 98% by mass or less.
Furthermore, when the oral composition of the present invention is in the form of a dentifrice composition such as a paste-like toothpaste, the content of component (D) in the oral composition of the present invention is preferably 1 to 65% by mass, more preferably 5 to 60% by mass, and even more preferably 8 to 50% by mass. When the oral composition of the present invention is in the form of a liquid oral composition such as a mouthwash, mouth spray, or liquid dentifrice, the content of component (D) in the oral composition of the present invention is preferably 70 to 99% by mass, more preferably 75 to 99% by mass, and even more preferably 80 to 98% by mass.

In addition, the water of component (D) in the present invention means the total water contained in the oral composition, including not only the purified water etc. directly blended into the oral composition, but also the water contained in each of the blended components.
The content of component (D) can be determined by calculation from the amount of water blended and the amount of water in the blended components, but can also be measured, for example, with a Karl Fischer moisture meter.

The oral composition of the present invention may further contain hydrogel particles (E), which allows the hydrogel particles to penetrate into localized areas such as gingival sulci and periodontal pockets, and allows each of the components contained in the component (E) to follow the penetrated components and reach deep into the localized areas, thereby effectively enhancing the halitosis suppressing effect.
The term "hydrogel" refers to a water-containing swollen body formed by mixing a gel-forming agent with water as a solvent, and which is insoluble in water.
Examples of the gel-forming agent to be incorporated in component (E) include one or more selected from seaweed extracts such as agar, κ-carrageenan, ι-carrageenan, λ-carrageenan, furcellaran, alginates, and propylene glycol alginate; plant seed mucilages such as guar gum, locust bean gum, tamarind seed polysaccharides, tara gum, and cassia gum; plant fruit mucilages such as pectin and arabinogalactan; microbially produced mucilages such as xanthan gum, scleroglucan, pullulan, dextran, gellan gum, and curdlan; animal proteins such as gelatin, albumin, and casein; plant proteins such as soybean protein and wheat protein; cellulose and derivatives thereof such as microcrystalline cellulose; and starch and derivatives thereof such as starch, starch phosphate, and starch glycolate. Among these, from the viewpoint of imparting appropriate destructive properties while facilitating penetration into local sites, one or more selected from κ-carrageenan, agar, and gellan gum are preferred, with agar being particularly preferred.
The content of the gel-forming agent in component (E) is preferably 0.25 to 5 mass %, more preferably 0.5 to 4.5 mass %, and even more preferably 1 to 4 mass %.

In addition to the above components, component (E) may contain, to the extent that the effects of the present invention are not impaired, for example, thickening polymers such as polyvinylpyrrolidone, polyacrylic acid, and carboxyvinyl polymer; pH adjusters; medicinal ingredients; colorants; preservatives; fragrances, etc.

In addition, from the viewpoint of facilitating the penetration of component (E) into a localized area, it is preferable that the shape of component (E) is a shape of a body of revolution composed of curved surfaces. Here, "body of revolution composed of curved surfaces" refers to a closed figure composed of a virtual axis and a continuous curve rotated around a virtual axis.

The average particle size of component (E) is preferably 50 to 500 μm, more preferably 100 to 400 μm, and even more preferably 140 to 290 μm, from the viewpoint of allowing component (E) to penetrate deep into the localized area and for each of the contained components to reach thereto, thereby effectively enhancing the bad breath suppression effect.

The content of component (E) in the oral composition of the present invention is preferably 2% by mass or more, more preferably 4% by mass or more, even more preferably 5% by mass or more, preferably 15% by mass or less, more preferably 12% by mass or less, and even more preferably 10% by mass or less, from the viewpoint of allowing component (E) to penetrate deep into the localized area and allowing each contained component to reach therein, thereby effectively enhancing the bad breath suppression effect. The content of component (E) in the oral composition of the present invention is preferably 2 to 15% by mass, more preferably 4 to 12% by mass, and even more preferably 5 to 10% by mass.

The oral composition of the present invention may contain one or more surfactants (F) selected from anionic surfactants (f1), nonionic surfactants (f2), and amphoteric surfactants (f3) in order to dissolve or disperse the above-mentioned components well, while also increasing the diffusibility of the oral composition after application to the oral cavity, and to exert an excellent effect of suppressing bad breath.

Examples of the anionic surfactant of component (f1) include one or more selected from alkyl sulfate ester salts such as lauryl sulfate, myristyl sulfate, palmityl sulfate, stearyl sulfate, octyl sulfate, and capryl sulfate; fatty acid salts such as oleate and laurate; alkyl sulfonates such as alkylbenzenesulfonate, α-olefinsulfonate, and hydroxyalkanesulfonate; acylamino acid salts such as acyl glutamate and acyl sarcosine salt; acyltaurates such as lauryl methyl taurine salt; alkyl phosphates such as alkyl phosphates; higher fatty acid sulfonated monoglyceride salts, fatty acid ester salts of isethionic acid; and polyoxyethylene monoalkyl phosphates.
Among these, from the viewpoint of further enhancing the effect of suppressing bad breath, it is preferable to use one or more selected from alkyl sulfate ester salts, acylamino acid salts, and acyltaurine salts.

Examples of the nonionic surfactant of component (f2) include one or more selected from polyoxyethylene hydrogenated castor oil; polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monomyristate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate, and polyoxyethylene sorbitan monooleate; sucrose fatty acid esters; sorbitan fatty acid esters; glycerin fatty acid esters such as glyceride monostearate; alkyl glucosides; polyglycerin fatty acid esters such as decaglyceride monostearate and decaglyceride monomyristate; polyoxyethylene alkylphenyl ethers; fatty acid alkanolamides such as coconut oil fatty acid diethanolamide; and polyethylene glycol fatty acid esters.
Among these, from the viewpoint of further enhancing the effect of suppressing bad breath, one or more selected from polyoxyethylene hydrogenated castor oil and polyoxyethylene sorbitan fatty acid ester are preferred.

Examples of the amphoteric surfactant of component (f3) include one or more selected from acetate betaines such as lauryl dimethylamino acetate betaine; imidazolinium betaines such as 2-alkyl-N-carboxymethyl-N-hydroxyethyl-N-imidazolium betaine; alkyl sulfobetaines such as lauryl sulfobetaine and lauryl hydroxysulfobetaine; coconut oil fatty acid amidoalkyl betaines such as coconut oil fatty acid amidopropyl betaine; and long-chain alkyl imidazoline betaine salts such as N-alkyl-1-hydroxyethyl imidazoline betaine sodium.
Among these, from the viewpoint of further enhancing the effect of suppressing bad breath, one or more selected from coconut oil fatty acid amidoalkylbetaine and alkylsulfobetaine are preferred.

From the viewpoint of effectively enhancing the effect of suppressing bad breath, the content of component (F) in the oral composition of the present invention is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, even more preferably 0.3% by mass or more, preferably 4% by mass or less, more preferably 3% by mass or less, and even more preferably 2.5% by mass or less.

The oral composition of the present invention may contain, in addition to the above-mentioned components, for example, a pH adjuster such as sodium hydroxide, a flavoring, a sweetener, a coloring, etc., within the range that does not impair the effects of the present invention.

The pH of the oral composition of the present invention at 25°C is preferably 7 or more, more preferably 7.5 or more, even more preferably 7.8 or more, even more preferably 8 or more, preferably 10 or less, more preferably 9.5 or less, even more preferably 9 or less, and even more preferably 8.5 or less, from the viewpoint of maintaining a good usability and effectively enhancing the bad breath suppressing effect.

The oral composition of the present invention may be in the form of a liquid oral composition such as a mouthwash, mouth spray, or liquid dentifrice, or may be in the form of a dentifrice composition such as a powder dentifrice or toothpaste.

The oral composition of the present invention is particularly effective in removing bad breath caused by proteins leaching from blood, gums, and other tissues. Therefore, when the oral composition of the present invention is applied to an oral cavity in which there is at least one of the following problems with the gums: "swelling," "bleeding," "thinning," or "receding gums," and where there is a condition in which proteins leak from the gums, such as periodontal disease, gingivitis, or alveolar pyorrhea, it is possible to realize a remarkable effect. In this way, the method of using the oral composition of the present invention is highly useful as a method for suppressing dental bad breath.

The present invention will be described in detail below with reference to examples. Unless otherwise indicated in the table, the content of each component is expressed as mass %.

[Examples 1 to 3, Comparative Examples 1 to 4]
The components shown in Table 1 were mixed to prepare various oral compositions (pH 6.7 to 7.0 at 25° C.).
Next, using the obtained oral composition, the amounts (ppm) of hydrogen sulfide ( _H2S ), methyl mercaptan ( _CH3SH ), and dimethyl sulfide (( _CH3 ) _2S ) generated, and the total VSC amount (ppm) were measured according to the methods described below, and based on the obtained values, the relative ratio (%) of each component to the control (amount of each component in the control) and the relative ratio (%) of the total VSC amount to the control (amount of VSC in the control) were calculated.
The results are shown in Table 1.

<<Measurement of VSC>>
The VSC was measured using Oralchroma (registered trademark).
Specifically, saliva was collected at rest and cooled on ice, and 1.5 mL of the saliva was then collected and placed in a glass vial. Next, 1.5 mL of the obtained oral compositions (Examples 1 to 3 and Comparative Examples 1 to 3) were added to the glass vial and stirred for 10 seconds using a vortex. After that, the samples were cultured at 37°C to obtain saliva treated with each oral composition. In addition, water (Comparative Example 4) was added instead of the oral composition to serve as a control.
Next, 0.5 mL of the gas phase of the control was injected into Oralchroma, and the amounts of hydrogen sulfide ( _H2S ), methyl mercaptan ( _CH3SH ), and dimethyl sulfide (( _CH3 ) _2S ) generated were measured every hour. In the control where water (Comparative Example 4) was added instead of the oral composition, the measured value at the point when the amounts of hydrogen sulfide ( _H2S ), methyl mercaptan ( _CH3SH ), and dimethyl sulfide (( _CH3 ) _2S ) generated reached the measurement limit value of Oralchroma was set to 100, and the amounts of hydrogen sulfide ( _H2S ), methyl mercaptan ( _CH3SH ), and dimethyl sulfide (( _CH3 ) _2S ) generated in each oral composition-treated saliva at that point were calculated to determine the respective amounts (%) relative to the control.
Similarly, the VSC, which is the total amount of hydrogen sulfide (H ₂ S), methyl mercaptan (CH ₃ SH), and dimethyl sulfide ((CH ₃ ) ₂ S), was also determined.

[Example 4, Comparative Example 5]
The components shown in Table 2 were mixed to prepare each oral composition.
The hydrogel particles (average particle size: 50 to 500 μm) were prepared by heating and mixing the components listed in the footnotes of Table 2 and spraying the mixture into the gas phase.
Next, using the obtained oral composition, 90 panelists who had at least one of the following problems regarding their gums: "swelling,""bleeding,""thinning," or "receding gums" brushed their teeth three times a day for 28 days, and then performed a sensory evaluation of the feel in the oral cavity according to the following items (1) to (3).
Each item was rated on a three-point scale: very good, good, or average (no response allowed), and the percentage (%) of people who gave each rating out of the total number of panelists was calculated.
The results are shown in Table 3.

(1) Taste and aroma (2) Refreshing feeling in the mouth (3) Suppression of bad breath

Claims (3)

The following components (A) , (B) , and (D) :
(A) Sodium copper chlorophyllin 0.003 % by mass or more and 0.01 % by mass or less (B) Erythritol 10% by mass or more and 20 % by mass or less
(D) Water 8% by mass or more and 74.39% by mass or less
and wherein the mass ratio of the content of component (B) to the content of component (A) ((B)/(A)) is 500 or more and 2000 or less. The oral composition according to claim 1 further contains glycyrrhetinic acid (C). The oral composition according to claim 2, wherein the content of component (C) is 0.001% by mass or more and 1% by mass or less.