Oral components

Abstract

To provide an oral composition that contains an azulene compound while effectively inhibiting color change thereof.SOLUTION: An oral composition comprising the following components (A) and (B): (A) one or two or more azulene compounds selected from azulene, azulene sulfonic acid and a salt thereof, and guaiazulene; and (B) one or two or more nicotinic acid compounds selected from nicotinic acid, isonicotinic acid, chloronicotinic acid, and salts thereof.SELECTED DRAWING: None

Description

Technical Field

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

Background Art

[0002] Conventionally, various components have been used in agents and compositions intended for application to the oral cavity to provide desired pharmacological effects such as anti-inflammatory action and alveolar bone resorption inhibitory action, and compounds such as azulene are one of such components. For example, Patent Document 1 discloses an agent for inhibiting the production of AGEs (Advanced Glycation End Products) for oral use, which comprises azulene compounds such as sodium azulenesulfonate and azulene as active ingredients, and is intended to suppress inflammatory reactions caused by AGEs.

Prior Art Documents

Patent Documents

[0003]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0004] Meanwhile, azulene compounds such as azulene and sodium azulenesulfonate have low photostability, and thus easily cause photolysis, which may lead to discoloration during storage of the composition. However, the technique described in the above Patent Document 1 does not focus at all on suppressing such discoloration of the composition caused by the azulene compounds, and no investigations have been made in this regard.

[0005] Accordingly, the present invention relates to an oral composition that can effectively suppress discoloration while containing an azulene compound.

Means for Solving the Problems

[0006] Therefore, the inventors conducted diligent research to solve the above problems and found an oral composition that effectively enhances the photostability of the azulene compound and effectively suppresses discoloration during storage of the composition by containing an azulene compound and a specific nicotinic acid compound.

[0007] In other words, the present invention comprises the following components (A) and (B): (A) One or more azulene compounds selected from azulene, azulene sulfonic acid and its salts, and guaiazulene. (B) One or more nicotinic acid compounds selected from nicotinic acid, isonicotinic acid, chloronicotinic acid, and salts thereof. This invention provides an oral composition containing [a specific ingredient]. [Effects of the Invention]

[0008] The oral composition of the present invention effectively enhances the photostability of the azulene compound, effectively suppressing unwanted discoloration of the composition during storage, and allowing the azulene compound to fully exhibit its inherent anti-inflammatory and other effects. Therefore, the container for filling the oral composition is not limited to being made of a light-shielding material, increasing the freedom of choice in selecting the type of container. Furthermore, even after storage, it can be used while enjoying a pleasant flavor without perceiving unpleasant tastes such as excessive saltiness or bitterness. [Brief explanation of the drawing]

[0009] [Figure 1] In Test Example 1, the images show the oral composition before and after storage, both filled into transparent containers. Figure 1(A) is a photograph of Example 1, where (a1) shows the oral composition before storage and (a2) shows the oral composition after storage. Figure 1(B) is a photograph of Comparative Example 1, where (b1) shows the oral composition before storage and (b2) shows the oral composition after storage. [Figure 2]In Test Example 2, the images show the oral composition before and after storage, both filled into transparent containers. Figure 2(A) is a photograph of Example 21, where (a1) shows the oral composition before storage and (a2) shows the oral composition after storage. Figure 2(B) is a photograph of Comparative Example 4, where (b1) shows the oral composition before storage and (b2) shows the oral composition after storage. [Modes for carrying out the invention]

[0010] The present invention will be described in detail below. In this invention, "good flavor" means that when the oral composition is applied, it provides a pleasant sensation without the perception of unpleasant tastes such as saltiness or bitterness.

[0011] The oral composition of the present invention contains, as component (A), one or more azulene compounds selected from azulene, azulene sulfonic acid and its salts, and guaiazulene. Since such component (A) has low photostability, it may easily decompose in photos and cause discoloration of the composition. However, with the oral composition of the present invention, photostability can be effectively increased, effectively suppressing discoloration of the composition and allowing component (A) to fully exhibit the desired effects, such as its anti-inflammatory properties.

[0012] Examples of azulene sulfonates include alkali metal salts such as sodium salts and potassium salts; alkaline earth metal salts such as calcium salts and magnesium salts; metal salts other than alkali metal salts and alkaline earth metal salts such as aluminum; ammonium salts; carboxylate salts such as acetate, palmitate, stearate, fumarate, and citrate; organic amine salts such as methylamine salt, triethylamine salt, triethanolamine salt, morpholine salt, piperazine salt, pyrrolidine salt, tripyridine salt, and picoline salt; and inorganic salts such as hydrochloride salt, sulfate salt, nitrate salt, hydrobromide salt, and phosphate salt.

[0013] Among the components (A), from the viewpoint of exhibiting a sufficient discoloration-inhibiting effect with component (B) described later, one or more selected from azulene and azulene sulfonate are preferred, azulene sulfonate is more preferred, and sodium azulene sulfonate is even more preferred.

[0014] From the viewpoint of effectively exhibiting a discoloration-inhibiting effect, the content of component (A) in the oral composition of the present invention is preferably 0.001% by mass or more, more preferably 0.005% by mass or more, even more preferably 0.01% by mass or more, even more preferably 0.015% by mass or more, preferably 0.03% by mass or less, more preferably 0.025% by mass or less, and even more preferably 0.02% by mass or less. Furthermore, the content of component (A) is preferably 0.001% by mass or more and 0.03% by mass or less, more preferably 0.005 to 0.025% by mass, even more preferably 0.01 to 0.02% by mass, and even more preferably 0.015 to 0.02% by mass.

[0015] The oral composition of the present invention contains, as component (B), one or more nicotinic acid compounds selected from nicotinic acid, isonicotinic acid, chloronicotinic acid, and salts thereof. By including such component (B), the photostability of component (A) can be effectively enhanced, and the discoloration suppression effect in the composition can be fully exhibited.

[0016] Here, examples of the salt of component (B) include alkali metal salts such as sodium salts and potassium salts; and alkaline earth metal salts such as calcium salts and magnesium salts.

[0017] Among the components (B), from the viewpoint of exhibiting an effective and efficient discoloration-inhibiting effect, one or more selected from nicotinic acid and nicotinate salts are preferred, and more specifically, one or two selected from nicotinic acid and sodium nicotinate are more preferred.

[0018] The content of component (B) may vary depending on the type of the aforementioned component (A), but from the perspectives of effectively exerting the discoloration inhibiting effect and effectively maintaining favorable flavor, in the oral composition of the present invention, it is preferably 0.005 mass% or more, more preferably 0.01 mass% or more, still more preferably 0.05 mass% or more, even more preferably 0.35 mass% or more, further preferably 1.4 mass% or more, preferably 6 mass% or less, more preferably 5 mass% or less, still more preferably 4 mass% or less, even more preferably 3 mass% or less, and further preferably 2 mass% or less. The content of component (B) is preferably 0.005 mass% to 6 mass%, more preferably 0.01 to 5 mass%, still more preferably 0.05 to 4 mass%, even more preferably 0.35 to 3 mass%, and further preferably 1.4 to 2 mass%.

[0019] Further, when the oral composition of the present invention is a liquid oral composition such as a mouthwash or a liquid dentifrice, the content of component (B) in the oral composition of the present invention is preferably 0.01 mass% or more, more preferably 0.05 mass% or more, still more preferably 0.3 mass% or more, preferably 1.95 mass% or less, more preferably 1.5 mass% or less, and still more preferably 0.65 mass% or less. When the oral composition of the present invention is a liquid oral composition such as a mouthwash or a liquid dentifrice, the content of component (B) in the oral composition of the present invention is preferably 0.01 to 1.95 mass%, more preferably 0.05 to 1.5 mass%, and still more preferably 0.3 to 0.65 mass%. On the other hand, when the oral composition of the present invention is a dentifrice composition such as a toothpaste or a powder dentifrice, the content is preferably 0.01 mass% or more, more preferably 0.35 mass% or more, still more preferably 0.4 mass% or more, even more preferably 1.3 mass% or more, preferably 5 mass% or less, more preferably 4 mass% or less, and still more preferably 1.95 mass% or less. When the oral composition of the present invention is a dentifrice composition such as a toothpaste or a powder dentifrice, the content of component (B) in the oral composition of the present invention is preferably 0.01 to 5 mass%, more preferably 0.35 to 4 mass%, still more preferably 0.4 to 1.95 mass%, and even more preferably 1.3 to 1.95 mass%.

[0020] The mass ratio of the content of component (A) to the content of component (B) ((A) / (B)) is preferably 0.00025 or more, more preferably 0.00125 or more, still more preferably 0.0025 or more, even more preferably 0.005 or more, preferably 3 or less, more preferably 2 or less, still more preferably 1 or less, and even more preferably 0.65 or less, from the viewpoints of effectively exerting the discoloration inhibitory effect and maintaining a favorable flavor. The mass ratio of the content of component (A) to the content of component (B) ((A) / (B)) is preferably 0.00025 to 3, more preferably 0.00125 to 2, still more preferably 0.0025 to 1, and even more preferably 0.005 to 0.65.

[0021] The oral composition of the present invention contains water. The water in the present invention means all water contained in the oral composition, including not only purified water and the like blended into the oral composition, but also water contained in each blended component. By containing such water, while the respective components described above are favorably dissolved or dispersed, the photostability of component (A) is effectively enhanced to sufficiently exert the discoloration inhibitory effect, and the desired action and effect by component (A) can also be effectively provided while maintaining a favorable flavor.

[0022] Specifically, when the oral composition of the present invention is a liquid oral composition such as a mouthwash or liquid toothpaste, the water content in the oral composition of the present invention is preferably 50% by mass or more, more preferably 70% by mass or more, even more preferably 80% by mass or more, preferably 99.7% by mass or less, more preferably 99.5% by mass or less, and even more preferably 99.4% by mass or less. Also, when the oral composition of the present invention is a liquid oral composition such as a mouthwash or liquid toothpaste, the water content in the oral composition of the present invention is preferably 50 to 99.8% by mass, more preferably 70 to 99.5% by mass, and even more preferably 80% to 99.4% by mass. Furthermore, when the oral composition of the present invention is a toothpaste or powder toothpaste, the water content is preferably 5% by mass or more, more preferably 10% by mass or more, preferably 60% by mass or less, and more preferably 55% by mass or less in the oral composition of the present invention.

[0023] Furthermore, if the oral composition of the present invention is a toothpaste composition such as a toothpaste paste or toothpaste powder, its moisture content can be calculated from the amount of water added and the amount of water in the added components, but it can also be measured using, for example, a Karl Fischer moisture meter. As a Karl Fischer moisture meter, for example, a trace moisture measuring device (manufactured by Hiranuma Sangyo Co., Ltd.) can be used. With this device, 5g of the oral composition can be taken, suspended in 25g of anhydrous methanol, and 0.02g of this suspension can be taken out to measure its moisture content.

[0024] In addition to the above components, the oral composition of the present invention may contain one or more surfactants selected from anionic surfactants and nonionic surfactants.

[0025] Examples of anionic surfactants include, specifically, sulfate ester salts such as alkyl sulfates and polyoxyalkylene alkyl ether sulfates; fatty acid salts such as oleates and laurates; alkyl sulfonates such as alkylbenzene sulfonates, α-olefin sulfonates, and hydroxyalkane sulfonates; alkyl phosphates such as alkyl phosphates; fatty acid ester salts of higher fatty acid sulfonated monoglycerides and isethionic acid; polyoxyethylene monoalkyl phosphates; N-acyl amino acids, N-acyl taurines, and one or more selected from these salts. Among these, sulfate ester salts such as alkyl sulfates and polyoxyalkylene alkyl ether sulfates are preferred as anionic surfactants.

[0026] Examples of nonionic surfactants include, specifically, one or more selected from polyoxyethylene hydrogenated castor oil; sucrose fatty acid esters; polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan monostearate; sorbitan fatty acid esters; glycerin fatty acid esters such as glyceride monostearate; alkyl glucosides; polyoxyethylene monoalkyl (or alkenyl) ethers such as polyoxyethylene stearyl ether, polyoxyethylene polyoxypropylene copolymers, polyoxyethylene alkylphenyl ethers such as polyoxyethylene nonylphenyl ether; fatty acid alkanolamides such as coconut oil fatty acid diethanolamide; and polyethylene glycol fatty acid esters.

[0027] From the viewpoint of ensuring that the discoloration-inhibiting effect in the present invention is fully exerted without being hindered, the surfactant content in the oral composition of the present invention is usually 0.05% by mass or more, preferably 0.1% by mass or more, more preferably 0.3% by mass or more, usually 5% by mass or less, preferably 3% by mass or less, and more preferably 2% by mass or less. Furthermore, the surfactant content in the oral composition of the present invention is usually 0.05 to 5% by mass, preferably 0.1 to 3% by mass, and more preferably 0.3 to 2% by mass.

[0028] More specifically, when the oral composition of the present invention is a liquid oral composition such as a mouthwash or liquid toothpaste, the content of such surfactant 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 3% by mass or less, more preferably 2% by mass or less, and even more preferably 1.5% by mass or less. Furthermore, when the oral composition of the present invention is a liquid oral composition such as a mouthwash or liquid toothpaste, the content of such surfactant in the oral composition of the present invention is preferably 0.05 to 3% by mass, more preferably 0.1 to 2% by mass, and even more preferably 0.3 to 1.5% by mass. Furthermore, when the oral composition of the present invention is a toothpaste composition such as a toothpaste or tooth powder, the content of such surfactant in the oral composition of the present invention is preferably 0.3% by mass or more, more preferably 0.5% by mass or more, even more preferably 0.8% by mass or more, preferably 5% by mass or less, more preferably 3% by mass or less, and even more preferably 2% by mass or less.

[0029] The oral composition of the present invention may contain, in addition to the above-mentioned components, sugar alcohols such as sorbitol, erythritol, xylitol, or mannitol; fluorine-containing compounds such as sodium fluoride, stannous fluoride, or sodium monofluorophosphate; binders; humectants such as glycerin, propylene glycol, or polyethylene glycol; pH adjusters such as sodium hydroxide; abrasives; disinfectants; fragrances; sweeteners; preservatives, etc., to the extent that they do not impair the effects of the present invention.

[0030] The pH of the oral composition of the present invention at 25°C is preferably 5 or higher, more preferably 5.7 or higher, even more preferably 6 or higher, preferably 9.5 or lower, more preferably 9 or lower, even more preferably 8.5 or lower, and even more preferably 8 or lower, from the viewpoint of effectively exhibiting a discoloration-inhibiting effect and maintaining a good flavor. Furthermore, the pH of the oral composition of the present invention at 25°C is preferably 5 to 9.5, more preferably 5 to 9, even more preferably 5.7 to 8.5, and even more preferably 6 to 8.

[0031] The container for filling the oral composition of the present invention is not limited to a container made of a light-shielding material such as a metallic layer of aluminum, but can also be made of a material without a metallic layer or a transparent material, as it does not require consideration of the discoloration of the oral composition over time. Therefore, the oral composition of the present invention is a highly useful oral composition because it allows for greater freedom in selecting the type of container for filling it. [Examples]

[0032] The present invention will be described in detail below based on examples. Unless otherwise specified in the table, the content of each component is expressed in mass percent.

[0033] [Test Example 1: Examples 1-20, Comparative Examples 1-3] Each oral composition was prepared according to the formulations shown in Tables 1-3. Then, each obtained oral composition was measured and evaluated according to the following method.

[0034] Evaluation of the discoloration suppression effect Ten g of each obtained oral composition was filled into a transparent container (container body material: polystyrene) and stored for one week at 25°C while being illuminated by a fluorescent lamp with a color temperature of 6700K. For both the oral composition before and after storage, the absorbance of each was measured using a microplate recorder (TECAN, Sunrise Rainbow Thermo, tunable absorbance microplate reader) while the composition was still filled in its container, with an Abs of 577. nm The values ​​were measured, and the resulting values ​​were introduced into the following formula to calculate the color change rate (%), which was used as an evaluation index. A smaller value for the discoloration rate of the applied color indicates superior discoloration suppression. Color change rate (%) = {(Absorbance of oral composition before storage Abs577 nm - Absorbance of oral composition after storage: Abs577 nm Absorbance of oral composition before storage: Abs 577 nm}×100

[0035] 《Flavor Evaluation》 Immediately after applying the obtained oral composition to the oral cavity of three expert panelists, the degree of unpleasant taste perceived in the oral cavity was evaluated sensorily according to the following criteria, and the results of the discussion among the three expert panelists were used as the evaluation index. 2: I felt a strong salty and bitter taste, but it wasn't to a degree that would cause any problems in terms of use. 1: I noticed a slight salty and bitter taste, but it wasn't enough to cause any problems in terms of use. 0: I didn't taste any saltiness or bitterness at all.

[0036] The results obtained are shown in Tables 1 to 3. Figure 1 also shows photographs of both the oral composition before and after storage for Example 1 and Comparative Example 1.

[0037] [Table 1]

[0038] [Table 2]

[0039] [Table 3]

[0040] [Test Example 2: Example 21, Comparative Example 4] Each oral composition was prepared according to the formulations shown in Table 4. Next, in the same manner as in Test Example 1, 10 g of each obtained oral composition was filled into a transparent container (container body material: polystyrene) and stored for one week at 25°C while being illuminated by a fluorescent light source with a color temperature of 6700K. Figure 2 shows photographs of both the oral composition before and after storage.

[0041] [Table 4]

[0042] As is clear from the results in Figures 1 and 2, the oral composition of the present invention can effectively suppress discoloration during storage, even while containing an azulene compound.

[0043] [Test Example 3: Examples 22-23, Comparative Examples 5-6] Examples 22 and Comparative Example 5, which are mouthwashes, and Examples 23 and Comparative Example 6, which are toothpastes, were prepared according to the formulations shown in Table 5. Next, the effectiveness of each of these mouthwashes and toothpastes in improving gingival inflammation was evaluated according to the method described below. The results are shown in Table 5.

[0044] Evaluation of the effectiveness of mouthwash in improving gingival inflammation. Twenty men and twenty women aged 40 to 60 with mild gingivitis used 20 ml of the prepared mouthwash to rinse their mouths four times a day for approximately 30 seconds each time for eight weeks. Next, a dental hygienist measured the gingival inflammation index (GI) of all teeth at the start of the study and calculated the average value, which was defined as the "initial average GI." The same measurement was performed at the end of the study and calculated the average value, which was defined as the "average GI after 8 weeks." The difference between the obtained "average GI after 8 weeks" and the "average GI at the beginning" was calculated to determine the "change in gingival inflammation index," which was used as an indicator to evaluate the gingival inflammation-improving effect of the mouthwash.

[0045] Evaluation of the anti-gingival inflammation effect of toothpaste Twenty men and twenty women aged 40 to 60 with mild gingivitis were instructed to use 1g of the prepared toothpaste to brush their teeth three times a day for approximately 3 minutes each time for 12 weeks. Next, a dental hygienist measured the gingival inflammation index (GI) of all teeth at the start of the study and calculated the average value, which was defined as the "initial average GI." The same measurement was performed at the end of the study and calculated the average value, which was defined as the "average GI after 12 weeks." The difference between the obtained "average GI after 12 weeks" and the "average GI at the beginning" was calculated to determine the "change in gingival inflammation index," which was used as an indicator to evaluate the gingival inflammation-improving effect of toothpaste.

[0046] [Table 5]

Claims

1. The following components (A) and (B): (A) One or more azulene compounds selected from azulene, azulene sulfonic acid and its salts, and guaiazulene. (B) One or more nicotinic acid compounds selected from nicotinic acid, isonicotinic acid, chloronicotinic acid, and salts thereof. An oral composition containing [a specific ingredient].

2. The oral composition according to claim 1, wherein the mass ratio ((A) / (B)) of the content of component (A) to the content of component (B) is 0.00025 or more and 3 or less.

3. The oral composition according to claim 1 or 2, wherein the content of component (A) is 0.001% by mass or more and 0.03% by mass or less.

4. The oral composition according to claim 1 or 2, wherein the content of component (B) is 0.005% by mass or more and 6% by mass or less.

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