Composition for oral cavity

Abstract

To provide a composition for the oral cavity with improved solubility of salicylic acid and / or a derivative thereof.SOLUTION: A composition for the oral cavity contains salicylic acid and / or a derivative thereof and a water-soluble metal compound. The composition has improved solubility of the salicylic acid and / or derivative thereof, inhibiting the opacification caused by insolubilization of the salicylic acid and / or the derivative thereof.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to an oral composition in which the solubility of salicylic acid and / or its derivative is improved.

Background Art

[0002] Salicylic acid and its derivatives (hereinafter referred to as salicylic acids) are known to have an anti-inflammatory and analgesic effect and are widely used in oral compositions such as dentifrices and mouthwashes. Conventionally, various reports have been made on the formulation techniques of oral compositions containing salicylic acids. For example, Patent Document 1 describes that an oral composition containing a salicylic acid derivative and specific N-substituted-p-menthane-3-carboxamides can have excellent flavor and storage stability.

[0003] On the other hand, salicylic acids are hardly soluble in water, and when formulated in an oral composition, there is a drawback that they cannot be sufficiently dissolved and turbidity occurs. Conventionally, in order to suppress the turbidity of oral compositions containing salicylic acids, improvements have been made in manufacturing conditions or formulation prescriptions, such as increasing the stirring time, adding heat treatment, or adding a surfactant. However, increasing the stirring time or adding heat treatment in the manufacturing process leads to an increase in manufacturing time and cost, and furthermore, the addition of a surfactant may adversely affect the taste of the oral composition or cause a decrease in the bactericidal action of the oral composition. Therefore, the development of a formulation technique for simply dissolving salicylic acids in an oral composition by a simple method is desired.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] An object of the present invention is to provide an oral composition in which the solubility of salicylic acid and / or its derivative is improved.

Means for Solving the Problems

[0006] The present inventors intensively studied to solve the above problems, and as a result, in an oral composition, by containing a water-soluble metal compound together with salicylic acid and / or its derivative, the solubility of salicylic acid and / or its derivative is improved, and salicylic acid and / or its derivative can be easily dissolved even at room temperature, and it was found that cloudiness caused by insolubilization of salicylic acid and / or its derivative can be suppressed. The present invention has been completed by further studies based on such findings.

[0007] That is, the present invention provides the inventions of the following aspects. Item 1. An oral composition containing (A) salicylic acid and / or its derivative, and (B) a water-soluble metal compound. Item 2. The oral composition according to Item 1, wherein the component (B) is a water-soluble alkali metal salt and / or a water-soluble aluminum salt. Item 3. The oral composition according to Item 1 or 2, wherein the component (B) is at least one selected from the group consisting of sodium saccharin, sodium aspartate, sodium fluoride, sodium monofluorophosphate, potassium nitrate, and aluminum lactate. Item 4. The oral composition according to any one of Items 1 to 3, wherein the content of the component (A) is 0.001 to 1% by weight. Item 5. The oral composition according to any one of Items 1 to 4, wherein the content of the component (B) is 0.001 to 1% by weight. Item 6. A method for improving the solubility of salicylic acid and / or its derivative in an oral composition, A method for improving solubility, comprising blending (A) salicylic acid and / or its derivative and (B) a water-soluble metal compound in an oral composition.

Effects of the Invention

[0008] According to the present invention, by a simple method of including a water-soluble metal compound together with salicylic acid and / or its derivative in an oral composition, the solubility of salicylic acid and / or its derivative can be improved, and cloudiness caused by insolubilization of salicylic acid and / or its derivative can be suppressed.

Brief Description of the Drawings

[0009]

Figure 1

Modes for Carrying Out the Invention

[0010] 1. Oral composition The oral composition of the present invention is characterized by containing salicylic acid and / or its derivative (sometimes referred to as component (A)), and a water-soluble metal compound (sometimes referred to as component (B)). Hereinafter, the oral composition of the present invention will be described in detail.

[0011] [(A) Salicylic acid and / or its derivative] The oral composition of the present invention contains salicylic acid and / or its derivative. Salicylic acid and its derivative are known components that are known to have an anti-inflammatory and analgesic effect.

[0012] The type of the derivative of salicylic acid is not particularly limited as long as it is applicable in the oral cavity. For example, methyl salicylate, ethyl salicylate, acetylsalicylic acid, sulfosalicylic acid, glycol salicylate, ethylene glycol salicylate, dipropylene glycol salicylate, titanium salicylate, 2-ethylhexyl salicylate, homomenthyl salicylate, phenyl salicylate, salicylamide, etc. can be mentioned.

[0013] In the oral composition of the present invention, as component (A), one kind may be selected from salicylic acid and its derivatives and used alone, or two or more kinds may be used in combination.

[0014] Among the components of (A), salicylic acid derivatives are preferred, methyl salicylate and ethyl salicylate are more preferred, and methyl salicylate is even more preferred.

[0015] Regarding the content of component (A) in the oral composition of the present invention, it may be appropriately set according to the type of component (A) used, the form of the oral composition, the degree of anti-inflammatory and analgesic effects to be imparted, etc. For example, 0.001 to 1% by weight can be mentioned. From the viewpoint of sufficiently dissolving component (A) and more effectively suppressing the generation of insoluble substances, the content of component (A) in the oral composition of the present invention is preferably 0.005 to 0.5% by weight, more preferably 0.01 to 0.3% by weight, and even more preferably 0.05 to 0.15% by weight.

[0016] [(B) Water-soluble metal compound] The oral composition of the present invention contains a water-soluble metal compound in addition to the component (A). By coexisting the component (A) with a water-soluble metal compound, the solubility of the component (A) can be improved, and it becomes possible to suppress the turbidity caused by the insolubilization of the component (A).

[0017] In the present invention, the water-soluble metal compound refers to a metal compound that can be dissolved at room temperature. Specifically, metal compounds that can be dissolved at 0.03 g / ml or more in purified water at 20°C can be mentioned.

[0018] The type of the water-soluble metal compound is not particularly limited as long as it can be applied in the oral cavity. For example, water-soluble alkali metal salts, water-soluble alkaline earth metal salts, water-soluble aluminum salts, etc. can be mentioned.

[0019] Examples of the water-soluble alkali metal salts include water-soluble sodium salts such as sodium saccharin, sodium aspartate, sodium glutamate, sodium fluoride, sodium monofluorophosphate, sodium nitrate, sodium lactate, sodium polyphosphate, sodium polyacrylate, sodium alginate, sodium citrate, and sodium phosphate; and water-soluble potassium salts such as potassium saccharin, potassium aspartate, potassium glutamate, potassium fluoride, potassium monofluorophosphate, potassium nitrate, potassium lactate, and dipotassium glycyrrhizinate.

[0020] Examples of the water-soluble alkaline earth metal salts include water-soluble calcium salts such as calcium lactate, calcium chloride, and calcium phosphorylated oligosaccharide; and water-soluble magnesium salts such as magnesium lactate, magnesium chloride, and magnesium phosphate.

[0021] Examples of the water-soluble aluminum salts include aluminum lactate and aluminum chloride.

[0022] These water-soluble metal compounds may be in the form of solvates such as hydrates.

[0023] In the oral composition of the present invention, one kind of water-soluble metal compound may be used alone as the component (B), or two or more kinds of water-soluble metal compounds may be used in combination.

[0024] Among the component (B), from the viewpoint of further improving the solubility of the component (A) and more effectively suppressing the cloudiness caused by the insolubilization of the component (A), preferably, water-soluble alkali metal salts, water-soluble aluminum salts, more preferably, sodium saccharin, sodium aspartate, sodium fluoride, sodium monofluorophosphate, potassium nitrate, aluminum lactate; still more preferably, sodium saccharin, sodium aspartate, sodium fluoride, potassium nitrate, and aluminum lactate.

[0025] In the oral composition of the present invention, the ratio of the component (B) to the component (A) may be appropriately set according to the types of the component (A) and the component (B) to be used, etc. For example, per 1 part by weight of the total amount of the component (A), the total amount of the component (B) is 0.01 to 50 parts by weight. From the viewpoint of further improving the solubility of the component (A) and more effectively suppressing the turbidity caused by the insolubilization of the component (A), per 1 part by weight of the total amount of the component (A), the total amount of the component (B) is preferably 0.5 to 10 parts by weight, more preferably 1 to 5 parts by weight.

[0026] As the content of the component (B) in the oral composition of the present invention, for example, 0.001 to 1% by weight can be mentioned. From the viewpoint of further improving the solubility of the component (A) and more effectively suppressing the turbidity caused by the insolubilization of the component (A), the content of the component (B) in the oral composition of the present invention is preferably 0.005 to 0.8% by weight, more preferably 0.05 to 0.5% by weight, and still more preferably 0.1 to 0.4% by weight.

[0027] [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 can be applied in the oral cavity. For example, monohydric alcohols having 2 to 5 carbon atoms, specifically, ethanol, propanol, isopropanol, butanol, etc. can be mentioned. Among these monohydric lower alcohols, ethanol is preferably mentioned. These monohydric lower alcohols may be used alone or in combination of two or more.

[0028] When the oral composition of the present invention contains a monohydric lower alcohol, its content is not particularly limited. For example, 0.01 to 5% by weight, preferably 0.1 to 4% by weight, and still more preferably 0.5 to 3% by weight can be mentioned.

[0029] [Polyhydric alcohol] The oral composition of the present invention may further contain a polyhydric alcohol. The polyhydric alcohol is not particularly limited as long as it can be applied in the oral cavity. Examples thereof include ethylene glycol, 1,3-butylene glycol, propylene glycol, isoprene glycol, diethylene glycol, dipropylene glycol, polypropylene glycol, glycerin, and the like. Among these polyhydric alcohols, glycerin is preferably mentioned. These polyhydric alcohols may be used alone or in combination of two or more.

[0030] When the oral composition of the present invention contains a polyhydric alcohol, the content thereof is not particularly limited. For example, it may be 0.1 to 50% by weight, preferably 1 to 40% by weight, and more preferably 10 to 35% by weight.

[0031] [Water] The oral composition of the present invention contains water as a base. The content of water in the oral composition of the present invention may be the remainder excluding the added components, and is appropriately set according to the form of the oral composition and the like. For example, it may be 10 to 99.9% by weight, preferably 15 to 99% by weight, more preferably 35 to 98% by weight, and still more preferably 40 to 88% by weight.

[0032] [Other Containing Components] In addition to the components described above, the oral composition of the present invention may contain components commonly used in the art according to the form of the oral composition, as long as the effects of the present invention are not impaired. Examples of such components include preservatives, bactericides, antibacterial agents, anti-inflammatory agents other than component (A), abrasives, glucosyltransferase (GTase) inhibitors, plaque inhibitors, hypersensitivity inhibitors, tartar preventives, dentin strengthening / remineralizing agents, local anesthetics, blood circulation promoters, thickeners, wetting agents, sweeteners, pigments, deodorants, pH adjusters, and the like.

[0033] [pH] Regarding the pH of the oral composition of the present invention, there is no particular limitation as long as it is within the range acceptable for application in the oral cavity. For example, pH 3.5 to 8, preferably pH 3.7 to 7.5 can be mentioned.

[0034] [Dosage form · Form] Regarding the dosage form of the oral composition of the present invention, there is no particular limitation as long as it can be applied in the oral cavity. For example, liquid or semi-solid form (gel-like, paste-like) can be mentioned.

[0035] Regarding the form of the oral composition of the present invention, there is no particular limitation as long as it can be applied in the oral cavity and stay in the oral cavity for a certain period of time. For example, oral hygiene agents such as liquid dentifrices, paste dentifrices, mouthwashes (liquid dentifrices and mouthwashes are sometimes generally referred to as mouth rinses, mouth washes, dental rinses, etc.), oral fresheners (mouth sprays, etc.), and oral ointments can be mentioned. Among these, preferably liquid dentifrices, paste dentifrices, and mouthwashes can be mentioned.

[0036] In one aspect of the oral composition of the present invention, it can have a transparent appearance. Although the white turbidity caused by the insolubilization of the component (A) is suppressed by improving the solubility of the component (A) in the oral composition of the present invention, in another aspect of the oral composition of the present invention, coloring or white turbidity caused by other components (insoluble additive components, etc.) may occur.

[0037] 2. Method for improving solubility of salicylic acid and / or its derivative The present invention further provides a method for improving the solubility of salicylic acid and / or its derivative in an oral composition, which comprises blending (A) salicylic acid and / or its derivative and (B) a water-soluble metal compound in the oral composition.

[0038] In the method for improving solubility of the present invention, regarding the type and blending amount of salicylic acid and / or its derivative, the type and blending amount of the water-soluble metal compound, other components that can be blended and their blending amounts, pH, oral dosage form, form, etc., they are as described in the column of "1. Oral composition" above.

Examples

[0039] Examples are shown below to more specifically explain the present invention, but the present invention is not limited thereto.

[0040] Test example Solutions having the compositions shown in Tables 1 and 2 were prepared. Specifically, a first solution in which methyl salicylate was dissolved in ethanol was prepared. Separately, a second solution in which a metal compound was dissolved in purified water was prepared. A sorbit solution and concentrated glycerin were mixed, and the first solution and the second solution were mixed therewith to prepare a solution. The preparation of the solution was carried out without heating.

[0041] The appearance of the obtained solution was visually observed, and the degree of turbidity was evaluated according to the following criteria. <Criteria for judging the degree of turbidity> 6: Methyl salicylate is completely dissolved and has a colorless and transparent appearance. 5: Methyl salicylate is slightly undissolved, but has a substantially colorless and transparent appearance. 4: Methyl salicylate is slightly undissolved and has a transparent appearance with slightly reduced transparency. 3: Methyl salicylate is dissolved to some extent and has a translucent appearance. 2: Methyl salicylate is undissolved and has a turbid translucent appearance. 1: Methyl salicylate is undissolved and has a turbid opaque appearance.

[0042] The results are shown in Tables 1 and 2. Also, photographs of the appearance of each solution are shown in FIG. 1. When methyl salicylate was included in the absence of a water-soluble metal compound, methyl salicylate could not be dissolved and significant turbidity was observed, and the appearance was transparent or translucent (Comparative Examples 1 to 4). In particular, even when methyl salicylate and citric acid were included, methyl salicylate could not be dissolved and significant turbidity was observed (Comparative Example 4). In contrast, when a water-soluble metal compound was included together with methyl salicylate, methyl salicylate could be sufficiently dissolved and had a transparent appearance (Examples 1 to 10).

[0043]

Table 1

[0044]

Table 2

[0045] Production example A dentifrice having the composition shown in Tables 3 to 6 and a mouthwash having the composition shown in Tables 7 to 9 were prepared.

[0046]

Table 3

[0047]

Table 4

[0048]

Table 5

[0049]

Table 6

[0050]

Table 7

[0051]

Table 8

[0052]

Table 9

Claims

1. (A) Salicylic acid and / or its derivatives, and (B) a water-soluble metal compound, wherein the derivative of salicylic acid is at least one selected from the group consisting of methyl salicylate, ethyl salicylate, sulfosalicylic acid, dipropylene glycol salicylate, titanium salicylate, 2-ethylhexyl salicylate, homomenthyl salicylate, phenyl salicylate, and salicylamide, An oral composition which is a dentifrice (however, excluding those containing thymol, sugar alcohol, and anethole).

2. The oral composition according to claim 1, wherein the component (B) is a water-soluble alkali metal salt and / or a water-soluble aluminum salt.

3. The oral composition according to claim 1 or 2, wherein the component (B) is at least one selected from the group consisting of sodium saccharin, sodium aspartate, sodium fluoride, sodium monofluorophosphate, potassium nitrate, and aluminum lactate.

4. The oral composition according to any one of claims 1 to 3, wherein the content of the component (A) is 0.001 to 1% by weight.

5. The oral composition according to any one of claims 1 to 4, wherein the content of the component (B) is 0.001 to 1% by weight.

6. A method for improving the solubility of salicylic acid and / or its derivatives in an oral composition (however, excluding those containing thymol, sugar alcohol, and anethole), wherein (A) salicylic acid and / or its derivatives and (B) a water-soluble metal compound are blended into the oral composition, wherein the derivative of salicylic acid is at least one selected from the group consisting of methyl salicylate, ethyl salicylate, sulfosalicylic acid, dipropylene glycol salicylate, titanium salicylate, 2-ethylhexyl salicylate, homomenthyl salicylate, phenyl salicylate, and salicylamide, and the oral composition is a dentifrice, the method for improving solubility.

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