Oral composition

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 technology 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 into 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 further, 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 technology 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] The object of the present invention is to provide an oral composition in which the solubility of salicylic acid and / or its derivatives is improved. [Means for solving the problem]

[0006] The inventors of the present invention conducted diligent studies to solve the aforementioned problems and found that by including a water-soluble metal compound together with salicylic acid and / or its derivatives in an oral composition, the solubility of salicylic acid and / or its derivatives can be improved, making it possible to easily dissolve salicylic acid and / or its derivatives even at room temperature, and suppressing the clouding caused by the insolubilization of salicylic acid and / or its derivatives. The present invention was completed by further studies based on this finding.

[0007] In other words, the present invention provides inventions in the following embodiments. Item 1. An oral composition containing (A) salicylic acid and / or its derivatives, and (B) a water-soluble metal compound. Item 2. The oral composition according to Item 1, wherein the (B) component 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 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. An oral composition according to any one of items 1 to 3, wherein the content of component (A) is 0.001 to 1% by weight. Item 5. An oral composition according to any one of items 1 to 4, wherein the content of component (B) is 0.001 to 1% by weight. Item 6. A method for improving the solubility of salicylic acid and / or its derivatives in oral compositions, A method for improving the solubility of an oral composition, comprising (A) salicylic acid and / or its derivatives and (B) a water-soluble metal compound. [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 derivatives in an oral composition, the solubility of salicylic acid and / or its derivatives can be improved, and turbidity caused by the insolubilization of salicylic acid and / or its derivatives can be suppressed. [Brief explanation of the drawing]

[0009] [Figure 1] These are images showing the appearance of various liquid preparations (Examples 1-10, Comparative Examples 1-4, Reference Example 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 derivatives (sometimes referred to as component (A)) and a water-soluble metal compound (sometimes referred to as component (B)). The oral composition of the present invention will be described in detail below.

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

[0012] The types of salicylic acid derivatives are not particularly limited, as long as they are applicable in the oral cavity, but examples include 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, salicylic acid amide, and the like.

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

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

[0015] Regarding the content of the component (A) in the oral composition of the present invention, it may be appropriately set according to the type of the 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 the component (A) and more effectively suppressing the generation of insoluble matters, as the content of the component (A) in the oral composition of the present invention, 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 can be mentioned.

[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 co-existing the component (A) with the water-soluble metal compound, the solubility of the component (A) can be improved, and it becomes possible to suppress the cloudiness 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 is applicable 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 turbidity 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 component (B) to component (A) can be appropriately set depending on the types of component (A) and component (B) used, but for example, a ratio of 0.01 to 50 parts by weight of component (B) per 1 part by weight of component (A) is appropriate. From the viewpoint of further improving the solubility of component (A) and more effectively suppressing turbidity caused by the insolubilization of component (A), a ratio of 0.5 to 10 parts by weight, more preferably 1 to 5 parts by weight, of component (B) per 1 part by weight of component (A) is appropriate.

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

[0027] [Monovalent 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 in the oral cavity, but examples include monohydric alcohols having 2 to 5 carbon atoms, specifically ethanol, propanol, isopropanol, butanol, etc. Among these monohydric lower alcohols, ethanol is preferred. These monohydric lower alcohols may be used individually or in combination of two or more.

[0028] When the oral composition of the present invention contains a monohydric lower alcohol, the amount is not particularly limited, but for example, it may be 0.01 to 5% by weight, preferably 0.1 to 4% by weight, and more preferably 0.5 to 3% by weight.

[0029] [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 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 preferred. These polyhydric alcohols may be used individually or in combination of two or more.

[0030] When the oral composition of the present invention contains polyhydric alcohols, the amount is not particularly limited, but for example, it is 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 water content in the oral composition of the present invention may be any remaining amount after removing the added components, and can be appropriately set depending on the form of the oral composition, etc., but examples include 10 to 99.9% by weight, preferably 15 to 99% by weight, more preferably 35 to 98% by weight, and even more preferably 40 to 88% by weight.

[0032] [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 other than component (A), abrasives, glucosyltransferase (GTase) inhibitors, plaque inhibitors, hypersensitivity inhibitors, tartar preventive agents, tooth enamel strengthening / remineralizing agents, local anesthetics, blood circulation promoters, thickeners, wetting agents, sweeteners, colorants, deodorants, pH adjusters, and the like.

[0033] [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 3.5 to 8, preferably pH 3.7 to 7.5.

[0034] [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).

[0035] 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.

[0036] One aspect of the oral composition of the present invention is that it has a transparent appearance. In the oral composition of the present invention, the solubility of component (A) is improved, thereby suppressing turbidity caused by the insolubilization of component (A). However, in another aspect of the oral composition of the present invention, discoloration or turbidity caused by other components (such as insoluble additives) may occur.

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

[0038] In the method for improving solubility of the present invention, the type and amount of salicylic acid and / or its derivatives, the type and amount of water-soluble metal compounds, other components that can be included and their amounts, pH, oral dosage form, form, etc., are as described in the "1. Oral Composition" section above. [Examples]

[0039] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples.

[0040] Test example Liquid formulations with the compositions shown in Tables 1 and 2 were prepared. Specifically, a first solution was prepared by dissolving methyl salicylate in ethanol. Separately, a second solution was prepared by dissolving a metal compound in purified water. A liquid formulation was prepared by mixing sorbitol solution and concentrated glycerin, and then mixing the first and second solutions into this mixture. The liquid formulations were prepared without heating.

[0041] The appearance of the obtained liquid was visually observed, and the degree of turbidity was evaluated according to the following criteria. <Criteria for determining the degree of cloudiness> 6: Methyl salicylate is completely dissolved and has a colorless, transparent appearance. 5: The methyl salicylate is slightly undissolved, but the substance is nearly colorless and transparent. 4: The methyl salicylate is slightly undissolved, resulting in a transparent appearance with slightly reduced clarity. 3: Methyl salicylate is dissolved to some extent, but the appearance is semi-transparent. 2: The methyl salicylate is not dissolved, resulting in a cloudy, translucent appearance. 1: Methyl salicylate is not dissolved, resulting in a cloudy, opaque appearance.

[0042] The results are shown in Tables 1 and 2. Figure 1 shows photographs of the appearance of each liquid preparation. When methyl salicylate was included in the absence of a water-soluble metal compound, the methyl salicylate could not dissolve, resulting in significant turbidity and a transparent or translucent appearance (Comparative Examples 1-4). In particular, when methyl salicylate and citric acid were included, the methyl salicylate could not dissolve, and significant turbidity was observed (Comparative Example 4). In contrast, when a water-soluble metal compound was included along with methyl salicylate, the methyl salicylate dissolved sufficiently, resulting in a transparent appearance (Examples 1-10).

[0043] [Table 1]

[0044] [Table 2]

[0045] Manufacturing example Toothpastes with the compositions shown in Tables 3-6 and mouthwashes with the compositions shown in Tables 7-9 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. An oral composition comprising (A) salicylic acid and / or a derivative thereof, and (B) a water-soluble metal compound.

2. 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. 3. The oral composition according to claim 1, 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 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 component (B) is 0.001 to 1% by weight.

6. 1. A method for increasing the solubility of salicylic acid and / or its derivatives in an oral composition, comprising: A method for improving solubility of an oral composition, comprising blending (A) salicylic acid and / or a derivative thereof and (B) a water-soluble metal compound.

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