Oral components

Abstract

To provide an oral composition with improved photostability of azulene sulfonate and / or a salt thereof.SOLUTION: An oral composition contains (A) azulene sulfonate and / or a salt thereof and (B) isopropylmethylphenol and / or hinokitiol.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to an oral composition with improved photostability of azulenesulfonic acid and / or a salt thereof.

Background Art

[0002] Azulenesulfonic acid and salts thereof are known to have anti-inflammatory effects, epithelial tissue repairing effects and the like, and are widely used in oral compositions such as dentifrices and mouthwashes. However, azulenesulfonic acid and salts thereof have the disadvantage of being easily decomposed by exposure to light. When dissolved, azulenesulfonic acid and salts thereof exhibit a blue to bluish-purple color. When azulenesulfonic acid and salts thereof are decomposed by light exposure, not only the desired effect is attenuated, but also the appearance properties are deteriorated, and even the aesthetic value is impaired.

[0003] Therefore, various formulation techniques for improving the photostability of azulenesulfonic acid and salts thereof have been conventionally studied. For example, Patent Document 1 describes that an aqueous liquid preparation containing at least one selected from organic acids and at least one selected from amino acids as a pH buffering agent for a composition liquid containing an azulene derivative can improve the photostability of the azulene derivative. Further, Patent Document 2 describes that the photostability of azulenes can be improved by incorporating (B) berberines into an aqueous liquid preparation containing (A) azulenes and (C) polyvinylpyrrolidone and / or chondroitins. In recent years, consumers' demands for oral compositions have been diversifying, and development of various formulation prescriptions has been desired accordingly. Therefore, in order to respond to the diversification of formulation prescriptions, further development of formulation techniques for improving the photostability of azulenesulfonic acid and / or a salt thereof has been desired.

Prior Art Literature

Patent Literature

[0004]

Patent Document 1

Patent Document 2

[0005] The object of the present invention is to provide an oral composition having improved photostability of azulene sulfonic acid and / or its salt. [Means for solving the problem]

[0006] The inventors of the present invention conducted diligent research to solve the aforementioned problems and found that by including isopropylmethylphenol and / or hinokitiol together with azulene sulfonic acid and / or its salt in an oral composition, the photostability of azulene sulfonic acid and / or its salt is improved. The present invention was completed by further research based on this finding.

[0007] In other words, the present invention provides inventions in the following embodiments. Item 1. An oral composition containing (A) azulene sulfonic acid and / or a salt thereof, and (B) isopropylmethylphenol and / or hinokitiol. Item 2. The oral composition according to Item 1, further comprising a monohydric lower alcohol and / or a polyhydric alcohol. Item 3. An oral composition according to item 1 or 2, which is a liquid toothpaste, a paste toothpaste, or a mouthwash. [Effects of the Invention]

[0008] According to the present invention, the decomposition of azulene sulfonic acid and / or its salts due to light exposure can be suppressed, thereby improving the storage stability of oral compositions containing azulene sulfonic acid and / or its salts. [Brief explanation of the drawing]

[0009] [Figure 1] In Test Example 1, photographs were taken of the appearance of each oral composition before and after exposure to sunlight. [Figure 2] In Test Example 2, photographs were taken of the appearance of each oral composition after exposure to sunlight. [Modes for carrying out the invention]

[0010] 1. Oral composition The oral composition of the present invention is characterized by containing azulene sulfonic acid and / or a salt thereof, and isopropylmethylphenol and / or hinokitiol. The oral composition of the present invention will be described in detail below.

[0011] [(A) Azulene sulfonic acid and / or its salts] The oral composition of the present invention contains azulene sulfonic acid and / or a salt thereof (sometimes referred to as component (A)).

[0012] Azulene sulfonic acid, also known as 1,4-dimethyl-7-isopropylazulene-3-sulfonic acid, is a known anti-inflammatory component. While there are no particular restrictions on the types of salts of azulene sulfonic acid, as long as they are pharmaceutically acceptable, examples include alkali metal salts such as sodium and potassium salts; alkaline earth metal salts such as calcium and magnesium salts; other metal salts such as aluminum salts; ammonium salts; carboxylate salts such as acetate, trifluoroacetate, butyrate, palmitate, stearate, fumarate, maleate, succinate, malonate, lactate, tartrate, and citrate; organic sulfonates such as methanesulfonate, toluenesulfonate, and tosylate; organic amine salts such as methylamine, triethylamine, triethanolamine, morpholine, piperazine, pyrrolidine, tripyridine, and picoline; and inorganic salts such as hydrochloride, sulfate, nitrate, hydrobromide, and phosphate.

[0013] The oral composition of the present invention may use one component alone from azulene sulfonic acid and its salts as component (A), or it may use two or more components in combination.

[0014] Among component (A), preferred are salts of azulene sulfonic acid, more preferred are alkali metal salts of azulene sulfonic acid, and still more preferred is sodium azulene sulfonate.

[0015] The content of component (A) in the oral composition of the present invention may be appropriately set according to the formulation form, use and the like of the oral composition, and for example, it is 0.0001 to 1% by weight, preferably 0.001 to 0.5% by weight, more preferably 0.01 to 0.1% by weight.

[0016] [(B) Isopropylmethylphenol and / or hinokitiol] The oral composition of the present invention further contains isopropylmethylphenol and / or hinokitiol (sometimes referred to as component (B)). Thus, the combined use of azulene sulfonic acid and / or a salt thereof with isopropylmethylphenol and / or hinokitiol can improve the photostability of azulene sulfonic acid and / or a derivative thereof in the oral composition.

[0017] Isopropylmethylphenol (3-methyl-4-isopropylphenol) and hinokitiol are components known as bactericides.

[0018] In the oral composition of the present invention, as component (B), one component selected from isopropylmethylphenol and hinokitiol may be used alone, or two or more thereof may be used in combination.

[0019] From the viewpoint of further improving the photostability of azulene sulfonic acid and / or a derivative thereof, hinokitiol is preferred among component (B).

[0020] In the oral composition of the present invention, the ratio of component (A) to component (B) is determined depending on the respective contents of these two components. For example, the total amount of component (B) may be exemplified by up to 1000 parts by weight per 100 parts by weight of component (A). More specifically, when isopropylmethylphenol is used as component (B), isopropylmethylphenol is preferably 10 to 1000 parts by weight, more preferably 50 to 500 parts by weight, per 100 parts by weight of component (A). Further, when hinokitiol is used as component (B), hinokitiol is preferably 10 to 400 parts by weight, more preferably 50 to 200 parts by weight, per 100 parts by weight of component (A).

[0021] The content of component (B) in the oral composition of the present invention is, for example, 0.0001 to 1% by weight. More specifically, when isopropylmethylphenol is used as component (B), the content of isopropylmethylphenol is preferably 0.001 to 0.5% by weight, more preferably 0.01 to 0.1% by weight. Further, when hinokitiol is used as component (B), the content of hinokitiol is preferably 0.001 to 0.2% by weight, more preferably 0.01 to 0.05% by weight.

[0022] [Monohydric lower alcohol] The oral composition of the present invention may further contain a monohydric lower alcohol. The monohydric lower alcohol is not particularly limited as long as it is applicable to the oral cavity, and examples thereof include monohydric alcohols having 2 to 5 carbon atoms, specifically ethanol, propanol, isopropanol, butanol, and the like. These monohydric lower alcohols may be used alone, or two or more thereof may be used in combination.

[0023] Among these monohydric lower alcohols, ethanol is preferable.

[0024] When the oral composition of the present invention contains a monohydric lower alcohol, the amount is not particularly limited, but for example, it is 0.01 to 15% by weight, preferably 0.1 to 10% by weight, and more preferably 1 to 5% by weight.

[0025] [Polyhydric alcohols] The oral composition of the present invention may further contain a polyhydric alcohol. The polyhydric alcohol is not particularly limited as long as it is applicable in the oral cavity, but examples include dihydric alcohols such as 1,3-butylene glycol, ethylene glycol, propylene glycol, isoprene glycol, diethylene glycol, dipropylene glycol, polyethylene glycol, etc., and glycerin. These polyhydric alcohols may be used individually or in combination of two or more.

[0026] Among these polyhydric alcohols, dihydric alcohols are preferred, and propylene glycol is more preferred.

[0027] When the oral composition of the present invention contains polyhydric alcohols, the amount is not particularly limited, but for example, it is 0.01 to 15% by weight, preferably 0.1 to 10% by weight, and more preferably 1 to 5% by weight.

[0028] [water] The oral composition of the present invention contains water as a base. The amount of water in the oral composition of the present invention may be any remaining amount after removing the added components, and may be set appropriately depending on the formulation form and intended use of the oral composition.

[0029] [Other ingredients] In addition to the components described above, the oral composition of the present invention may contain components commonly used in the art, depending on the form of the oral composition, to the extent that the effects of the present invention are not impaired. Examples of such components include preservatives, bactericides, antibacterial agents, anti-inflammatory agents, abrasives, glucosyltransferase (GTase) inhibitors, plaque inhibitors, dentin hypersensitivity inhibitors, tartar preventive agents, tooth enamel strengthening / remineralizing agents, local anesthetics, blood circulation promoters, thickeners, surfactants, wetting agents, sweeteners, colorants, deodorants, pH adjusters, and the like.

[0030] [pH] The pH of the oral composition of the present invention is not particularly limited, as long as it is within a range that is permissible for application in the oral cavity, but examples include pH 4.0 to 9.0, preferably pH 6.0 to 8.5.

[0031] [Dosage form / form] The dosage form of the oral composition of the present invention is not particularly limited, as long as it can be applied inside the oral cavity, but examples include liquid or semi-solid forms (gel or paste).

[0032] The form of the oral composition of the present invention is not particularly limited as long as it can be applied to the oral cavity and remain there for a certain period of time. Examples include oral hygiene agents such as liquid toothpaste, tooth paste, mouthwash (liquid toothpaste and mouthwash are sometimes referred to as mouth rinse, mouthwash, dental rinse, etc.), oral fresheners (mouth spray, etc.), and oral ointments. Among these, liquid toothpaste, tooth paste, and mouthwash are preferred.

[0033] Furthermore, the container for containing the oral composition of the present invention is not particularly limited, and for example, tube containers, bottle containers, etc., can be used. Another form of container for containing the oral composition of the present invention is a light-transmitting transparent container. Here, transparent containers include both colorless transparent containers and colored transparent containers. Since the azulene sulfonic acid and / or salt thereof in the oral composition of the present invention is photostable, the decomposition of the azulene sulfonic acid and / or salt thereof can be suppressed even when exposed to light while contained in a transparent container.

[0034] 2. Method for improving the photostability of azulene sulfonic acid and / or its salts The present invention further provides a method for improving the photostability of an oral composition containing azulene sulfonic acid and / or a salt thereof, comprising: (A) azulene sulfonic acid and / or a salt thereof and (B) isopropylmethylphenol and / or hinokitiol.

[0035] In the method for improving the photostability of the present invention, the type and amount of azulene sulfonic acid and / or therein, the amount of isopropylmethylphenol and / or hinokitiol, other components that can be included and their amounts, pH, dosage form and form of the oral composition, etc., are as described in the "1. Oral Composition" section above. [Examples]

[0036] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples.

[0037] Test Example 1 The oral compositions shown in Table 1 were prepared. 5 ml of the obtained oral composition was placed in a 20 ml transparent glass container and stored indoors in direct sunlight for 1 day. The appearance of the oral composition was observed before and after storage, and the photostability of sodium azulene sulfonate was evaluated according to the following criteria. ·Judgment criteria S: Almost no discoloration of the oral composition is observed after storage. A: The oral composition has faded slightly after storage, but still exhibits a bluish-purple hue. B: The oral composition has faded after storage and exhibits a light bluish-purple hue. C: The oral composition has faded significantly after storage and is almost transparent.

[0038] The results obtained are shown in Table 1 and Figure 1. When sodium azulene sulfonate was contained alone, significant decomposition (fading) occurred upon exposure to sunlight (Comparative Example 1), but when sodium azulene sulfonate and isopropylmethylphenol were contained, decomposition (fading) due to sunlight exposure was suppressed. Although detailed results are omitted, it was confirmed that the oral compositions of Examples 1 and 2 could suppress the decomposition (fading) of sodium azulene sulfonate even when stored indoors in direct sunlight for a longer period of time.

[0039] [Table 1]

[0040] Test Example 2 The oral compositions shown in Table 2 were prepared. 5 ml of the obtained oral composition was filled into a 20 ml transparent glass container and stored indoors in direct sunlight for 2 days. The appearance of the oral composition was observed before and after storage, and the photostability of sodium azulene sulfonate was evaluated using the same criteria as in Test Example 1. Note that Test Example 2 was conducted on a different day than Test Example 1. Although detailed results are omitted, it was confirmed that the decomposition (discoloration) of sodium azulene sulfonate could be suppressed even when the oral compositions of Examples 3 and 4 were stored indoors in direct sunlight for a longer period of time.

[0041] The results obtained are shown in Table 2 and Figure 2. These results also confirm that when sodium azulene sulfonate and isopropylmethylphenol are included, decomposition (fading) due to sunlight exposure can be suppressed (Example 3). Furthermore, when sodium azulene sulfonate and hinokitiol are included, the inhibitory effect against decomposition (fading) due to sunlight exposure is high, and it was confirmed that significantly superior photostability can be achieved (Example 4).

[0042] [Table 2]

[0043] Prescription examples Liquid toothpaste and toothpaste were prepared with the compositions shown in Tables 3 and 4. The obtained liquid toothpaste and toothpaste were evaluated using the same method as in Test Example 1, and it was confirmed that the photostability of sodium azulene sulfonate was improved in both cases.

[0044] [Table 3]

[0045] [Table 4]

Claims

1. An oral composition containing (A) azulene sulfonic acid and / or a salt thereof, and (B) isopropylmethylphenol.

2. An oral composition comprising (A) azulene sulfonic acid and / or a salt thereof, and (B) hinokitiol, wherein the pH is 6.0 to 9.

0.

3. Furthermore, the oral composition according to claim 1 or 2 contains a monohydric lower alcohol and / or a polyhydric alcohol.

4. The oral composition according to claim 1 or 2, which is a liquid toothpaste, a paste toothpaste, or a mouthwash.

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