Oral composition

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 technology]

[0002] Conventionally, various ingredients have been used in agents and compositions to be applied to the oral cavity to achieve desired pharmacological effects such as anti-inflammatory effects and alveolar bone resorption inhibitory effects, and compounds such as azulene are one such ingredient. For example, Patent Document 1 discloses an oral AGE (Advanced Glycation End Products) production inhibitor that contains azulenes such as sodium azulene sulfonate and azulene as active ingredients, and aims to suppress inflammatory responses caused by AGEs. [Prior art documents] [Patent documents]

[0003] [Patent Document 1] Japanese Patent Publication No. 2022-164911 Summary of the Invention [Problem to be solved by the invention]

[0004] However, azulene compounds such as azulene and sodium azulene sulfonate have low photostability and are therefore susceptible to photodecomposition, which may result in discoloration of the composition during storage. However, the technology of Patent Document 1 does not pay any attention to or consider at all how to suppress discoloration of the composition caused by the azulene compound.

[0005] Therefore, the present invention relates to an oral composition that contains an azulene compound and yet can effectively inhibit discoloration. [Means for solving the problem]

[0006] Therefore, the present inventors conducted extensive research to solve the above problems and discovered an oral composition that contains an azulene compound and a specific nicotinic acid compound, thereby effectively increasing the photostability of the azulene compound and effectively suppressing discoloration of the composition during storage.

[0007] That is, the present invention provides a composition comprising 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 The present invention provides an oral composition containing the above. [Effects of the Invention]

[0008] The oral composition of the present invention can effectively increase the photostability of the azulene compound and effectively suppress unwanted discoloration of the composition during storage, thereby allowing the azulene compound to fully exert its inherent effects, such as anti-inflammatory activity, etc. Therefore, the container for filling the oral composition can be freely selected without being limited to whether it is made of a light-shielding material or not, and this allows for greater freedom in the selection of the type of container. Furthermore, even after storage, the product can be used while enjoying a pleasant flavor without perceiving unpleasant tastes such as excessive saltiness or bitterness. [Brief explanation of the drawings]

[0009] [Figure 1] 1A and 1B are photographs of the oral composition filled in a transparent container before and after storage in Test Example 1. Fig. 1(A) is a photograph of Example 1, where (a1) shows the oral composition before storage and (a2) shows the oral composition after storage. Fig. 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]2A and 2B are photographs of the oral composition filled in a transparent container before and after storage in Test Example 2. Fig. 2(A) is a photograph of Example 21, where (a1) shows the oral composition before storage and (a2) shows the oral composition after storage. Fig. 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. DETAILED DESCRIPTION OF THE INVENTION

[0010] The present invention will be described in detail below. In the present invention, "good flavor" means that when the oral composition is applied, it is accompanied by a pleasant feeling without the perception of unpleasant tastes such as salty or bitter.

[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. Component (A) has low photostability and may easily undergo photodecomposition, causing discoloration of the composition. However, the oral composition of the present invention can effectively increase photostability and effectively inhibit discoloration of the composition, allowing component (A) to fully exert its inherent desired effects, such as anti-inflammatory activity.

[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 salts; ammonium salts; carboxylates such as acetates, palmitates, stearates, fumarates, and citrates; organic amine salts such as methylamine salts, triethylamine salts, triethanolamine salts, morpholine salts, piperazine salts, pyrrolidine salts, tripyridine salts, and picoline salts; and inorganic acid salts such as hydrochlorides, sulfates, nitrates, hydrobromides, and phosphates.

[0013] Among the components (A), from the viewpoint of achieving a sufficient discoloration suppression effect by the component (B) described below, one or more selected from azulene and azulene sulfonates are preferred, azulene sulfonates are more preferred, and sodium azulene sulfonate is even more preferred.

[0014] From the viewpoint of effectively exhibiting the 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, still 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. 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 still 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 containing such component (B), the photostability of component (A) can be effectively increased, and the discoloration-inhibiting effect of the composition can be fully exerted.

[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] Of the components (B), one or more selected from nicotinic acid and nicotinic acid salts are preferred from the viewpoint of exhibiting an effective and efficient discoloration suppression effect, 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 component (A), but from the viewpoint of effectively exerting the discoloration-inhibiting effect and effectively maintaining a good flavor, the content in the oral composition of the present invention is preferably 0.005% by mass or more, more preferably 0.01% by mass or more, even more preferably 0.05% by mass or more, still more preferably 0.35% by mass or more, even more preferably 1.4% by mass or more, preferably 6% by mass or less, more preferably 5% by mass or less, even more preferably 4% by mass or less, still more preferably 3% by mass or less, and even more preferably 2% by mass or less. The content of component (B) is preferably 0.005% by mass or more and 6% by mass or less, more preferably 0.01 to 5% by mass, even more preferably 0.05 to 4% by mass, even more preferably 0.35 to 3% by mass, and even more preferably 1.4 to 2% by mass.

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

[0020] From the viewpoint of effectively exerting the discoloration-inhibiting effect and maintaining a good flavor, 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, even more preferably 0.0025 or more, still more preferably 0.005 or more, and preferably 3 or less, more preferably 2 or less, even more preferably 1 or less, and still more preferably 0.65 or less. 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, even more preferably 0.0025 to 1, and still more preferably 0.005 to 0.65.

[0021] The oral composition of the present invention contains water. In the present invention, water refers to the total amount of water contained in the oral composition, including not only purified water or the like contained in the oral composition but also the water contained in each of the components contained therein. By including such water, the components contained therein can be well dissolved or dispersed, while effectively increasing the photostability of component (A) to fully exhibit the discoloration-inhibiting effect, maintaining a good flavor, and effectively achieving the desired effects of component (A).

[0022] Specifically, when the oral composition of the present invention is a liquid oral composition such as a mouthwash or liquid dentifrice, the content of water 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, and 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. Furthermore, when the oral composition of the present invention is a liquid oral composition such as a mouthwash or liquid dentifrice, the content of water 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 dentifrice composition such as a toothpaste or a tooth powder, the content of water in the oral composition of the present invention is preferably 5% by mass or more, more preferably 10% by mass or more, and preferably 60% by mass or less, more preferably 55% by mass or less. Also, when the oral composition of the present invention is a dentifrice composition such as a toothpaste or a tooth powder, the content of water in the oral composition of the present invention is preferably 5 to 60% by mass, more preferably 10 to 55% by mass.

[0023] When the oral composition of the present invention is a dentifrice composition such as a toothpaste or a tooth powder, the water content can be calculated from the amount of water contained in the composition and the amount of water contained in the ingredients, but it can also be measured using a Karl Fischer moisture meter. For example, a trace moisture analyzer (manufactured by Hiranuma Sangyo Co., Ltd.) can be used as the Karl Fischer moisture meter. With this device, 5 g of the oral composition is suspended in 25 g of anhydrous methanol, and 0.02 g of this suspension is taken and the water content is measured.

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

[0025] Specific examples of anionic surfactants include 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; higher fatty acid sulfonated monoglyceride salts, fatty acid ester salts of isethionic acid; polyoxyethylene monoalkyl phosphates; N-acyl amino acids, N-acyltaurines, and salts thereof. Among these, sulfate ester salts such as alkyl sulfates and polyoxyalkylene alkyl ether sulfates are preferred as anionic surfactants.

[0026] Specific examples of nonionic surfactants include 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 monostearate glyceride; alkyl glucosides; polyoxyethylene monoalkyl (or alkenyl) ethers such as polyoxyethylene stearyl ether, polyoxyethylene polyoxypropylene copolymers, polyoxyethylene alkyl phenyl ethers such as polyoxyethylene nonyl phenyl ether; fatty acid alkanolamides such as coconut oil fatty acid diethanolamide; and polyethylene glycol fatty acid esters.

[0027] The content of the surfactant 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, and usually 5% by mass or less, preferably 3% by mass or less, more preferably 2% by mass or less, from the viewpoint of fully exerting the discoloration-inhibiting effect of the present invention without inhibiting it. The content of the surfactant in the oral composition of the present invention is usually 0.05 to 5% by mass, preferably 0.1 to 3% by mass, 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 dentifrice, the content of the 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. When the oral composition of the present invention is a liquid oral composition such as a mouthwash or liquid dentifrice, the content of the 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. When the oral composition of the present invention is a dentifrice composition such as a toothpaste or a tooth powder, the content of the 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, and preferably 5% by mass or less, more preferably 3% by mass or less, and even more preferably 2% by mass or less. When the oral composition of the present invention is a dentifrice composition such as a toothpaste or a tooth powder, the content of the surfactant in the oral composition of the present invention is preferably 0.3 to 5% by mass, more preferably 0.5 to 3% by mass, and even more preferably 0.8 to 2% by mass.

[0029] In addition to the above-mentioned components, the oral composition of the present invention may contain, within the scope that does not inhibit the effects of the present invention, for example, 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.

[0030] From the viewpoint of effectively exerting the discoloration-inhibiting effect and maintaining a good flavor, the pH of the oral composition of the present invention at 25°C is preferably 5 or more, more preferably 5.7 or more, even more preferably 6 or more, and preferably 9.5 or less, more preferably 9 or less, even more preferably 8.5 or less, and still more preferably 8 or less. The pH of the oral composition of the present invention at 25°C is preferably 5 or more and 9.5 or less, more preferably 5 or more and 9 or less, 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, and even if the container is made of a material without a metallic layer or a transparent material, there is no need to consider discoloration of the oral composition over time. Therefore, the oral composition of the present invention is a highly useful oral composition, as it allows for greater freedom in selecting the type of container for filling it. [Example]

[0032] The present invention will be described in detail below with reference to the following examples. Unless otherwise specified in the tables, the content of each component is expressed in mass %.

[0033] Test Example 1: Examples 1 to 20, Comparative Examples 1 to 3 Each oral composition was prepared according to the formulation shown in Tables 1 to 3. Then, using each of the obtained oral compositions, measurements and evaluations were carried out according to the following methods.

[0034] <Evaluation of discoloration prevention effect> 10 g of each of the obtained oral compositions was filled into a transparent container (container body material: polystyrene) and stored in an environment of 25°C for 1 week while being irradiated with a fluorescent light source lamp with a color temperature of 6700K. The absorbance (Abs577) of both the oral compositions before and after storage was measured using a microplate recorder (TECAN, variable wavelength absorbance microplate reader, Sunrise Rainbow Thermo) while still filled in the container. nm The value obtained was used in the following formula to determine the color change rate (%), which was used as an index for evaluation. The smaller the value of the discoloration rate, the better the discoloration suppression effect. Color change rate (%) = {(Absorbance Abs577 of oral composition before storage nm -Optical absorbance Abs577 of oral composition after storage nm ) / Absorbance Abs577 of oral composition before storage nm}×100

[0035] Flavor Evaluation The obtained oral composition was applied to the oral cavity of three expert panelists, and immediately afterwards, the degree of unpleasant taste felt in the oral cavity was evaluated according to the following criteria, and the results of the discussion between the three expert panelists were used as the evaluation index. 2: The saltiness and bitterness were quite strong, but not enough to cause any problems when using the product. 1: There was a slight salty or bitter taste, but it was not enough to cause any problems when using the product. 0: No salty or bitter taste

[0036] The results obtained are shown in Tables 1 to 3. Furthermore, for Example 1 and Comparative Example 1, photographs of the oral compositions both before and after storage are shown in FIG.

[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 formulation shown in Table 4. Next, in the same manner as in Test Example 1, 10 g of each of the obtained oral compositions was filled into a transparent container (container body material: polystyrene) and stored for one week in an environment of 25°C while irradiated with a fluorescent light source lamp with a color temperature of 6700 K. Photographs of the oral composition both before and after storage are shown in FIG.

[0041] [Table 4]

[0042] As is clear from the results in FIGS. 1 and 2, the oral composition of the present invention can effectively prevent discoloration during storage, even though it contains an azulene compound.

[0043] Test Example 3: Examples 22 and 23, Comparative Examples 5 and 6 According to the formulations shown in Table 5, mouthwashes Example 22 and Comparative Example 5, and dentifrices Example 23 and Comparative Example 6 were prepared. Next, the effect of these mouthwashes and dentifrices on improving gingival inflammation was evaluated according to the following method. The results are shown in Table 5.

[0044] <Evaluation of the effectiveness of mouthwashes in improving gingival inflammation> Twenty men and women in their 40s to 60s with mild gingivitis rinsed their mouths with 20 ml of the resulting mouthwash four times a day for approximately 30 seconds each time for eight weeks. Next, dental hygienists measured the gingival inflammation index (GI) of all teeth at the start of the study, and calculated the average value, which was designated as the "initial GI average." Similar measurements were also performed at the end of the study, and the average value was calculated, which was designated as the "8-week GI average." The difference between the "average GI value after 8 weeks" and the "average GI value at the beginning" was calculated to obtain the "change in gingival inflammation index," which was used as an index for evaluating the mouthwash's effect in improving gingival inflammation.

[0045] <Evaluation of the gingival inflammation suppression effect of toothpaste> Twenty men and women in their 40s to 60s with mild gingivitis were asked to brush their teeth with 1 g of the resulting toothpaste three times a day for approximately three minutes each time for 12 weeks. Next, dental hygienists measured the gingival inflammation index (GI) of all teeth at the start of the study, and calculated the average value, which was designated as the "initial GI average." Similar measurements were also performed at the end of the study, and the average value was calculated, which was designated as the "12-week GI average." The difference between the "average GI value after 12 weeks" and the "average GI value at the beginning" was calculated to obtain the "variation in the gingival inflammation index," which was used as an index for evaluating the toothpaste's effect in improving gingival inflammation.

[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 comprising:

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

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

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