Oral components

Abstract

This invention relates to an oral composition that contains an azulene compound and can effectively suppress discoloration even under light exposure. [Solution] The following components (A) to (C): (A) One or more azulene compounds selected from azulene, azulene sulfonic acid, and azulene sulfonate salts. (B) Sodium saccharin (C) One or more fragrance components selected from eugenol, geraniol, linalool, camphor, anethole, thymol, terpinolene, and cineole. An oral composition containing the above, wherein the mass ratio ((B) / (A)) of the content of component (B) to the content of component (A) is 3 or more and 50 or less.

Description

TECHNICAL FIELD

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

BACKGROUND ART

[0002] Conventionally, compounds such as azulene are known as one of the components that provide desired pharmacological actions such as anti-inflammatory action and bactericidal action, and have been used in various compositions for application to the oral cavity.

[0003] For example, Patent Document 1 discloses a liquid composition containing azulene sulfonate having an anti-inflammatory effect, cetylpyridinium, and a weakly acidic substance, and attempts to suppress adsorption of azulene sulfonate to the inner wall of a plastic container. Further, Patent Document 2 discloses an oral composition containing azulene sulfonic acid and / or a salt thereof, a quaternary ammonium salt, a monoterpene, and propylene glycol in specific amounts, and aims to suppress the formation of insoluble matter after storage.

PRIOR ART DOCUMENTS

PATENT DOCUMENTS

[0004]

PATENT DOCUMENT 1

PATENT DOCUMENT 2

SUMMARY OF THE INVENTION

PROBLEMS TO BE SOLVED BY THE INVENTION

[0005] Incidentally, azulene compounds such as azulene and sodium azulene sulfonate have low photostability, and thus easily cause photolysis, which may lead to discoloration of the composition. However, in any of the above patent documents, the composition still has to be stored under light-shielded conditions.

[0006] Therefore, the present invention relates to an oral composition that contains an azulene compound and can effectively suppress discoloration even under light exposure. [Means for solving the problem]

[0007] Therefore, the inventors conducted diligent research to solve the above problems and have found an oral composition that effectively enhances the photostability of the azulene compound and effectively suppresses discoloration of the composition even during storage under light exposure, by containing an azulene compound and sodium saccharin in a specific mass ratio, and further containing a specific fragrance component.

[0008] In other words, the present invention comprises the following components (A) to (C): (A) One or more azulene compounds selected from azulene, azulene sulfonic acid, and azulene sulfonate salts. (B) Sodium saccharin (C) One or more fragrance components selected from eugenol, geraniol, linalool, camphor, anethole, thymol, terpinolene, and cineole. The present invention provides an oral composition containing the above, wherein the mass ratio ((B) / (A)) of the content of component (B) to the content of component (A) is 3 or more and 50 or less. [Effects of the Invention]

[0009] The oral composition of the present invention effectively enhances the photostability of the azulene compound, effectively suppressing discoloration of the composition even during storage under light exposure. Therefore, the container for filling the oral composition is not limited to whether or not it is made of a light-shielding material, allowing for greater freedom in selecting the type of container. [Brief explanation of the drawing]

[0010] [Figure 1]These are photographs of the oral compositions in the examples before and after storage, filled into transparent containers, for evaluation of the discoloration suppression effect. (a1-1) shows the oral composition of Example 1 before storage, and (a1-2) shows the oral composition of Example 1 after storage. (a2-1) shows the oral composition of Example 2 before storage, and (a2-2) shows the oral composition of Example 2 after storage. (a3-1) shows the oral composition of Example 8 before storage, and (a3-2) shows the oral composition of Example 8 after storage. (a4-1) shows the oral composition of Example 9 before storage, and (a4-2) shows the oral composition of Example 9 after storage. [Figure 2] These are photographs of the oral compositions of comparative examples before and after storage, filled in transparent containers, for evaluation of the discoloration suppression effect. (b1-1) shows the oral composition of Comparative Example 1 before storage, and (b1-2) shows the oral composition of Comparative Example 1 after storage. (b2-1) shows the oral composition of Comparative Example 2 before storage, and (b2-2) shows the oral composition of Comparative Example 2 after storage. (b3-1) shows the oral composition of Comparative Example 3 before storage, and (b3-2) shows the oral composition of Comparative Example 3 after storage. (b4-1) shows the oral composition of Comparative Example 5 before storage, and (b4-2) shows the oral composition of Comparative Example 5 after storage. [Modes for carrying out the invention]

[0011] The present invention will be described in detail below. In this invention, "composition under light exposure" means a composition that is exposed to light, such as natural light or artificial lighting, and includes, for example, a composition that is stored in a container that does not have light-shielding properties and is exposed to light.

[0012] The oral composition of the present invention contains one or more azulene compounds selected from azulene, azulene sulfonic acid, and azulene sulfonate as component (A). Since such component (A) has low photostability, it may easily decompose in photos and cause discoloration of the composition. For this reason, compositions containing it usually need to be stored under light shielding conditions, such as by filling them into light-shielding containers. However, with the oral composition of the present invention, photostability is effectively enhanced, and discoloration of the composition can be effectively suppressed even under light exposure.

[0013] 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.

[0014] Among component (A), from the viewpoint of fully exhibiting the effect of suppressing discoloration of the composition under light exposure due to 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.

[0015] The content of component (A) in the oral composition of the present invention is preferably 0.001 mass% or more, more preferably 0.005 mass% or more, still more preferably 0.01 mass% or more, even more preferably 0.015 mass% or more, and is preferably 0.03 mass% or less, more preferably 0.028 mass% or less, still more preferably 0.025 mass% or less, from the viewpoint of effectively exhibiting the discoloration suppressing effect of the composition under light exposure. The content of component (A) in the oral composition of the present invention is preferably 0.001 mass% or more and 0.03 mass% or less, more preferably 0.005 to 0.028 mass%, still more preferably 0.01 to 0.028 mass%, even more preferably 0.015 to 0.025 mass%.

[0016] The oral composition of the present invention contains sodium saccharin as component (B). Sodium saccharin is a component also known as a so-called sweetener, but by using it in combination with the perfume component of component (C) described later while maintaining a specific mass ratio with the above component (A), it unexpectedly effectively enhances the light stability of component (A), and can exhibit an excellent effect of suppressing discoloration of the composition even under light exposure.

[0017] The content of component (B) in the oral composition of the present invention is preferably 0.1 mass% or more, more preferably 0.12 mass% or more, still more preferably 0.14 mass% or more, even more preferably 0.15 mass% or more, and is preferably 0.5 mass% or less, more preferably 0.45 mass% or less, still more preferably 0.4 mass% or less, even more preferably 0.35 mass% or less, from the viewpoint of effectively exhibiting the discoloration suppressing effect of the composition under light exposure. The content of component (B) in the oral composition of the present invention is preferably 0.1 mass% or more and 0.5 mass% or less, more preferably 0.12 to 0.45 mass%, still more preferably 0.14 to 0.4 mass%, even more preferably 0.15 to 0.35 mass%.

[0018] The mass ratio of the content of component (B) to the content of component (A) ((B) / (A)), from the viewpoint of effectively exerting the discoloration inhibitory effect of the composition under exposure to light by acting synergistically with component (C), is 3 or more, preferably 4 or more, more preferably 5 or more, and 50 or less, preferably 25 or less, more preferably 13 or less. The mass ratio of the content of component (B) to the content of component (A) ((B) / (A)) is 3 to 50, preferably 4 to 25, and more preferably 5 to 13.

[0019] The oral composition of the present invention contains, as component (C), one or two or more perfume ingredients selected from eugenol, geraniol, linalool, camphor, anethole, thymol, terpinolene, and cineole. Such component (C) acts synergistically with component (B) which maintains a specific mass ratio with the above component (A), so that the discoloration inhibitory effect of the composition under exposure to light can be further enhanced. Among component (C), from the viewpoint of achieving effective and enhanced discoloration inhibitory effect, one or two or more selected from eugenol, geraniol, camphor, anethole, thymol, and terpinolene are preferred, one or two or more selected from eugenol, geraniol, anethole, and thymol are more preferred, and one or two selected from anethole and thymol are even more preferred.

[0020] From the viewpoint of effectively enhancing the effect of suppressing discoloration of the composition under light exposure, the content of component (C) in the oral composition of the present invention is preferably 0.0001% by mass or more, more preferably 0.0005% by mass or more, even more preferably 0.0008% by mass or more, preferably 0.1% by mass or less, more preferably 0.08% by mass or less, even more preferably 0.05% by mass or less, and even more preferably 0.01% by mass or less. Furthermore, the content of component (C) in the oral composition of the present invention is preferably 0.0001% by mass or more and 0.1% by mass or less, more preferably 0.0005 to 0.08% by mass, even more preferably 0.0008 to 0.05% by mass, and even more preferably 0.0008 to 0.01% by mass.

[0021] The mass ratio ((C) / (A)) of the content of component (C) to the content of component (A) is preferably 0.003 or more, more preferably 0.005 or more, even more preferably 0.008 or more, even more preferably 0.03 or more, preferably 10 or less, more preferably 5 or less, even more preferably 1 or less, and even more preferably 0.5 or less, from the viewpoint of effectively enhancing the effect of suppressing discoloration of the composition under light exposure. Furthermore, the mass ratio ((C) / (A)) of the content of component (C) to the content of component (A) is preferably 0.003 to 10, more preferably 0.005 to 5, even more preferably 0.008 to 1, and even more preferably 0.03 to 0.5.

[0022] The oral composition of the present invention contains water. In this invention, water refers to the total water content in the oral composition, including not only purified water or the like that blended into the oral composition, but also the water contained in each of the blended components. By including such water, the above-mentioned components are dissolved or dispersed well, the photostability of component (A) is effectively enhanced, the discoloration suppression effect of the composition under light exposure is fully exhibited, and the desired effects of component (A) are effectively brought about.

[0023] Specifically, when the oral composition of the present invention is a toothpaste composition such as a toothpaste or tooth powder, the water content 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 25% by mass or more, preferably 60% by mass or less, more preferably 55% by mass or less, and even more preferably 50% 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 water content in the oral composition of the present invention is preferably 60% by mass or more, more preferably 80% by mass or more, even more preferably 90% by mass or more, even more preferably 95% by mass or more, preferably 99.7% by mass or less, even more preferably 99.5% by mass or less, even more preferably 99.4% by mass or less, and even more preferably 98.5% by mass or less.

[0024] 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.

[0025] In addition to the above components, the oral composition of the present invention may contain one or more surfactants selected from anionic surfactants, cationic surfactants, nonionic surfactants, and amphoteric surfactants.

[0026] For example, as anionic surfactants, anionic surfactants other than sulfate esters, such as alkyl sulfates and polyoxyalkylene alkyl ether sulfates, are preferred. Specifically, examples include 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.

[0027] From the viewpoint of ensuring that the surfactant content is fully exerted without hindering the discoloration suppression effect of the composition under light exposure, 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. More specifically, when the oral composition of the present invention is a toothpaste composition such as a toothpaste or toothpaste powder, the amount 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 2.8% by mass or less, more preferably 2.5% by mass or less, and even more preferably 1.8% 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 amount 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 0.2% by mass or more, preferably 1.8% by mass or less, more preferably 1% by mass or less, and even more preferably 0.5% by mass or less.

[0028] When the oral composition of the present invention is a toothpaste composition such as a toothpaste paste or a toothpaste powder, in order to provide an appropriate viscosity and ensure a good feel as a toothpaste composition, a binder may be included in addition to the above components. Specifically, such binders include, for example, polymer-based binders such as carboxyvinyl polymer and acrylic acid / (meth)acrylate alkyl copolymer; hydroxycellulose derivatives such as hydroxyethylcellulose, hydroxypropylcellulose, and hydroxypropyl methylcellulose; and one or more selected from sodium carboxymethylcellulose, ethylcellulose, sodium alginate, carrageenan, xanthan gum, sodium polyacrylate, pectin, agar, tragacanth gum, gum arabic, guar gum, karaya gum, locust bean gum, gela gum, tamarid gum, psyllium seed gum, etc. In particular, one or more cellulose-based binders selected from carboxymethylcellulose sodium, hydroxyethylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose are preferred.

[0029] When the oral composition of the present invention is a toothpaste composition such as a toothpaste or a toothpaste powder, the amount of binder in the oral composition of the present invention is preferably 0.05 to 3% by mass, more preferably 0.1 to 2.5% by mass, and even more preferably 0.3 to 2% by mass.

[0030] When the oral composition of the present invention is a toothpaste or toothpaste powder, in order to provide an appropriate viscosity and ensure a good feel as a toothpaste composition, it may also contain water-insoluble powders in addition to the above components. Note that "water-insoluble" means that the amount that dissolves in 100g of water (at 20°C) is 1g or less.

[0031] Examples of such water-insoluble powders include, for example, one or more selected from hydrated silicic acid, anhydrous silicic acid, silica gel, aluminosilicate, zirconosilicate, calcium phosphate such as dicalcium phosphate and tricalcium phosphate, magnesium phosphate, calcium carbonate such as light calcium carbonate and heavy calcium carbonate, aluminum hydroxide, alumina, zeolite, calcium pyrophosphate, sodium polyphosphate, magnesium carbonate, and magnesium acetate, and may be in hydrated or anhydrous form as appropriate.

[0032] When the oral composition of the present invention is a toothpaste composition such as a toothpaste or a toothpaste powder, the content of water-insoluble powder in the oral composition of the present invention is preferably 0.1 to 35% by mass, more preferably 0.5 to 30% by mass, even more preferably 1 to 25% by mass, even more preferably 5 to 20% by mass, and still more preferably 8 to 15% by mass.

[0033] From the viewpoint of fully exhibiting the effect of suppressing discoloration of the composition under light exposure without hindering it, the oral composition of the present invention may further contain one or more sugar alcohols selected from erythritol, sorbitol, mannitol, and xylitol. The content of such sugar alcohols in the oral composition of the present invention is preferably 1 to 50% by mass, more preferably 2 to 48% by mass, and even more preferably 3 to 46% by mass. More specifically, for example, if the oral composition of the present invention is a toothpaste composition such as a toothpaste or a toothpaste powder, the content of such sugar alcohol in the oral composition of the present invention is preferably 7% by mass or more, more preferably 18% by mass or more, even more preferably 35% by mass or more, preferably 50% by mass or less, more preferably 48% by mass or less, and even more preferably 46% by mass or less.

[0034] From the viewpoint of fully exhibiting the effect of suppressing discoloration of the composition under light exposure without hindering it, the oral composition of the present invention may further contain one or more polyhydric alcohols selected from glycerin, propylene glycol, and polyethylene glycol. The content of such polyhydric alcohols in the oral composition of the present invention is preferably 0.1 to 10% by mass, more preferably 0.5 to 9% by mass, and even more preferably 1 to 7% by mass. More specifically, for example, if the oral composition of the present invention is a toothpaste composition such as a toothpaste or toothpaste powder, the content of such polyhydric alcohol in the oral composition of the present invention is preferably 1% by mass or more, more preferably 3.5% by mass or more, even more preferably 4% by mass or more, preferably 10% by mass or less, more preferably 9% by mass or less, and even more preferably 7% by mass or less.

[0035] The oral composition of the present invention may contain, in addition to the above components, fluorine-containing compounds such as sodium fluoride, stannous fluoride, or sodium monofluorophosphate; pH adjusters such as sodium hydroxide; disinfectants; preservatives, etc., to the extent that they do not inhibit the effects of the present invention.

[0036] The pH of the oral composition of the present invention at 25°C is preferably 5 or higher, more preferably 5.5 or higher, even more preferably 6 or higher, preferably 9 or lower, more preferably 8.5 or lower, even more preferably 8 or lower, even more preferably 7.5 or lower, and still more preferably 7 or lower, from the viewpoint of effectively exhibiting the effect of suppressing discoloration of the composition under light exposure and effectively suppressing the formation of unwanted precipitates. Furthermore, the pH of the oral composition of the present invention at 25°C is preferably 5 to 9, more preferably 5.5 to 8.5, even more preferably 6 to 8, even more preferably 6 to 7.5, and still more preferably 6 to 7.

[0037] The viscosity of the oral composition of the present invention at 25°C is preferably 1000 dPa·s or more, more preferably 1500 dPa·s or more, even more preferably 2000 dPa·s or more, preferably 10000 dPa·s or less, more preferably 8000 dPa·s or less, and even more preferably 7000 dPa·s or less. Furthermore, the viscosity of the oral composition of the present invention at 25°C is preferably 1000 to 10000 dPa·s, more preferably 1500 to 8000 dPa·s, and even more preferably 2000 to 7000 dPa·s. The viscosity of oral compositions refers to the value measured using a digital viscometer (TVB-10 viscometer, manufactured by Toki Sangyo Co., Ltd.) and a T-bar stage (TS-20, manufactured by Toki Sangyo Co., Ltd.) under the conditions of rotor TC, rotation speed of 2.5 rpm, and 1 minute.

[0038] 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.

[0039] Furthermore, the present invention is also highly useful as a method for suppressing discoloration of an oral composition containing the above component (A) under light exposure. Specifically, this method involves adding one or more azulene compounds (A) selected from azulene, azulene sulfonic acid, and azulene sulfonate salts, and saccharin sodium (B) in a mass ratio ((B) / (A)) of 3 to 50, and adding one or more fragrance components (C) selected from eugenol, geraniol, linalool, anethole, camphor, thymol, terpinolene, and cineole, to suppress discoloration of an oral composition under light exposure. The content and quantitative relationships of each component are the same as described above.

[0040] With the method of the present invention, even if the oral composition containing the above component (A) is filled into a container made of a material that does not have a metallic layer or a container made of a transparent material, discoloration of the oral composition under light exposure can be effectively suppressed, so there is no need to worry about storage in environments exposed to light. [Examples]

[0041] 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.

[0042] [Examples 1-15, Comparative Examples 1-6] Each oral composition (Table 1: viscosity at 25°C = approximately 2500 dPa·s, pH = approximately 6.7; Table 2: pH = approximately 6.5) was prepared according to the formulations shown in Tables 1 and 2. Then, the discoloration-inhibiting effect of each obtained oral composition was evaluated according to the method described below. The oral compositions shown in Table 1 correspond to liquid oral compositions, and the oral compositions shown in Table 2 correspond to toothpaste compositions. A corresponding evaluation method for the discoloration-inhibiting effect was used for each. The results are shown in Tables 1 and 2.

[0043] Evaluation of the discoloration suppression effect 1. Evaluation of the discoloration suppression effect when the oral composition is a liquid oral composition. 80 mL of each obtained oral composition was filled into a transparent container (container body material: polyethylene terephthalate or polystyrene) and stored for one week at 25°C while being illuminated with an LED (Light Emitting Diode) light source lamp. For both the oral composition before and after storage, the absorbance (Abs) of each was measured using a microplate recorder (TECAN, Sunrise Rainbow Thermo, a tunable absorbance microplate reader) while the oral composition was still filled in its container. 577nm The values ​​were measured, and the percentage of color change was calculated by substituting the obtained values ​​into the following formula. Next, based on the obtained color change rate values, the color change rate values ​​of each oral composition were recalculated as the color change suppression effect (%) value, with the color change suppression effect of Comparative Example 1 set to 0%, and this was used as an evaluation index. Color change rate (%) = {(Absorbance of oral composition before storage Abs 577nm - Absorbance of oral composition after storage (Abs) 577nm Absorbance of oral composition before storage (Abs) 577nm}×100

[0044] Figures 1 and 2 show photographs of both the oral compositions before and after storage for Examples 1-2, 8-9, and Comparative Examples 1-3 and 5.

[0045] 2. Evaluation of the discoloration-inhibiting effect when the oral composition is a toothpaste composition. 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. The L*, a*, and b* values ​​were measured for both the oral composition before and after storage using a spectrophotometer (CM-700d, manufactured by Konica Minolta Optics, Inc.). The color difference formula (ΔE*ab = [(ΔL*)) 2 +(Δa*) 2 +(Δb*) 2 The color difference before and after storage was calculated according to (1 / 2), and the discoloration suppression effect of each oral composition was calculated when the discoloration suppression effect of Comparative Example 6 was set to 0%.

[0046] [Table 1]

[0047] [Table 2]

Claims

1. The following components (A) to (C): (A) One or more azulene compounds selected from azulene, azulene sulfonic acid, and azulene sulfonate salts. (B) Sodium saccharin (C) One or more fragrance components selected from eugenol, geraniol, linalool, camphor, anethole, thymol, terpinolene, and cineole. An oral composition containing the above, wherein the mass ratio of the content of component (B) to the content of component (A) ((B) / (A)) is 3 or more and 50 or less.

2. The oral composition according to claim 1, wherein the content of component (B) is 0.1% by mass or more and 0.5% by mass or less.

3. The oral composition according to claim 1 or 2, wherein the mass ratio ((C) / (A)) of the content of component (C) to the content of component (A) is 0.003 or more and 10 or less.

4. 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.

5. The oral composition according to claim 1 or 2, wherein the content of component (C) is 0.0001% by mass or more and 0.1% by mass or less.

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