Composition for oral cavity

Incorporating monoterpenes into oral compositions with phenolic compounds addresses the irritation issue, improving usability by reducing discomfort in the oral cavity.

JP2025134040APending Publication Date: 2025-09-11KOBAYASHI PHARMA CO LTD
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Patent Information

Application Number
JP2025120170
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Filing Date
2025-07-17
Publication Date
2025-09-11

AI Technical Summary

Technical Problem

Oral compositions containing phenolic compounds like thymol and parahydroxybenzoates cause irritation when applied to the oral cavity, leading to poor usability, and existing taste masking agents like saccharin sodium and stevia extract do not provide satisfactory results.

Method used

Incorporating monoterpenes such as camphor and menthol into oral compositions with phenolic compounds to suppress irritation.

Benefits of technology

The inclusion of monoterpenes significantly reduces irritation caused by phenolic compounds, enhancing the overall usability and comfort of the oral composition.

✦ Generated by Eureka AI based on patent content.

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Abstract

To provide a composition for the oral cavity that contains a phenol compound but allows reduction in the irritation perceived when used in the oral cavity.SOLUTION: A composition for the oral cavity contains a monoterpene as well as a phenol compound, reducing the phenol compound-induced irritation.SELECTED DRAWING: None
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Description

[Technical Field]

[0001] The present invention relates to an oral composition which contains a phenolic compound and which reduces the irritation perceived when applied to the oral cavity. [Background technology]

[0002] Thymol (2-isopropyl-5-methylphenol) is known to penetrate biofilms and exhibit bactericidal activity, and is widely used in oral compositions such as dentifrices and mouthwashes. Parahydroxybenzoates are also widely used as preservatives in oral compositions. Various formulation techniques for oral compositions containing phenolic compounds such as thymol and parahydroxybenzoates have been reported. For example, Patent Document 1 describes an oral composition containing a phenolic bactericide such as thymol or a parahydroxybenzoate, an anionic surfactant, and a nonionic surfactant, in which the weight ratio of the nonionic surfactant to the anionic surfactant is 0.1 to 3, and the water content in the composition is 40% by weight or less, which prevents the phenolic bactericide from adsorbing to the container and improves the stability of the phenolic bactericide over time.

[0003] On the other hand, oral compositions containing phenolic compounds such as thymol and parahydroxybenzoic acid esters have the disadvantage of causing irritation when applied to the oral cavity, resulting in a poor usability. Conventionally, a method for reducing the irritation of oral compositions containing phenolic compounds has been known in which sweeteners such as saccharin sodium, stevia extract, and erythritol are incorporated as taste masking agents. However, oral compositions containing such taste masking agents exhibit a sweet taste and do not necessarily provide a satisfactory usability. [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Application Publication No. 11-322554 Summary of the Invention [Problem to be solved by the invention]

[0005] An object of the present invention is to provide an oral composition which contains a phenolic compound but which reduces the irritation perceived when applied to the oral cavity. [Means for solving the problem]

[0006] The present inventors have conducted extensive research to solve the above-mentioned problems and have found that the irritation caused by phenolic compounds can be suppressed by incorporating monoterpenes into an oral composition. Based on this finding and through further research, the present invention has been completed.

[0007] That is, the present invention provides the following aspects. Item 1. An oral composition containing a phenolic compound and a monoterpene. Item 2. The oral composition according to Item 1, wherein the phenolic compound is thymol and / or a parahydroxybenzoic acid ester. Item 3. The oral composition according to Item 1 or 2, wherein the monoterpene is camphor and / or menthol. Item 4. The oral composition according to any one of Items 1 to 3, wherein the monoterpene is contained in an amount of 0.01 to 100 parts by weight per part by weight of the total amount of the phenolic compounds. Item 5. The oral composition according to any one of Items 1 to 4, wherein the content of the phenol compound is 0.001 to 5% by weight. Item 6. The oral composition according to any one of Items 1 to 4, wherein the content of the monoterpene compound is 0.001 to 5% by weight. Item 7. A method for suppressing irritation caused by an oral composition containing a phenolic compound, comprising: A method for suppressing irritation by incorporating a phenolic compound and a monoterpene into an oral composition. [Effects of the Invention]

[0008] According to the present invention, by including a monoterpene together with a phenolic compound in an oral composition, the irritation caused by the phenolic compound can be suppressed when applied to the oral cavity, and an excellent feeling of use can be achieved. DETAILED DESCRIPTION OF THE INVENTION

[0009] 1. Oral composition The oral composition of the present invention is characterized by containing a phenolic compound and a monoterpene. The oral composition of the present invention will be described in detail below.

[0010] [Phenol compounds] The oral composition of the present invention contains a phenolic compound. In this specification, the term "phenolic compound" is a general term for compounds having a phenol skeleton.

[0011] The type of phenolic compound used in the present invention is not particularly limited as long as it is applicable to the oral cavity, and examples thereof include thymol, parahydroxybenzoic acid esters, and the like.

[0012] Specific examples of the parahydroxybenzoic acid ester include methyl parahydroxybenzoate, ethyl parahydroxybenzoate, propyl parahydroxybenzoate, isopropyl parahydroxybenzoate, and butyl parahydroxybenzoate.

[0013] These phenol compounds may be used alone or in combination of two or more.

[0014] Among these phenolic compounds, thymol, methyl parahydroxybenzoate, and ethyl parahydroxybenzoate are preferred.

[0015] The content of phenolic compounds in the oral composition of the present invention may be appropriately determined depending on the type of phenolic compound used, the form of the oral composition, etc., and may be, for example, 0.001 to 5 wt% in total. From the viewpoint of more effectively suppressing irritation caused by phenolic compounds, the total amount of phenolic compounds in the oral composition of the present invention is preferably 0.005 to 2 wt%, more preferably 0.01 to 1 wt%, and even more preferably 0.05 to 0.3 wt%.

[0016] [Monoterpene] The oral composition of the present invention contains a monoterpene in addition to a phenolic compound. The coexistence of the phenolic compound and the monoterpene makes it possible to suppress the irritation caused by the phenolic compound.

[0017] Monoterpenes are known compounds that have a structure containing two isoprene units in the molecule and have cooling and refreshing effects.

[0018] The type of monoterpene used in the present invention is not particularly limited, as long as it is applicable to the oral cavity. Examples include alcohol-based monoterpenes such as menthol, geraniol, linalool, borneol, cineole, and terpineol; aldehyde-based monoterpenes such as citral, citronellal, perillaldehyde, and safranal; and ketone-based monoterpenes such as camphor, menthone, carbomenthone, and ionone. When optical isomers exist, these monoterpenes may be d-, l-, or dl-isomers. These monoterpenes may be used alone or in combination of two or more.

[0019] Furthermore, in the oral composition of the present invention, the monoterpene may be used in the form of an essential oil containing a monoterpene. The essential oil containing a monoterpene can be appropriately selected from known essential oils and used, and examples of essential oils containing menthol include peppermint oil, peppermint oil, and spearmint oil. In addition, when an essential oil containing a monoterpene is used, the description of the content or ratio of the monoterpene in this specification refers to the value converted into the amount of monoterpene contained in the essential oil.

[0020] These monoterpenes may be used alone or in combination of two or more.

[0021] Among these monoterpenes, from the viewpoint of more effectively suppressing the irritation caused by phenolic compounds, preferred are ketone-based monoterpenes and alcohol-based monoterpenes, and even more preferred are camphor and menthol.

[0022] In the oral composition of the present invention, the ratio of monoterpenes to phenolic compounds may be appropriately set depending on the types of phenolic compounds and monoterpenes used, and may be, for example, 0.01 to 100 parts by weight in total of monoterpenes per 1 part by weight of the total amount of phenolic compounds. From the viewpoint of more effectively suppressing the irritation caused by phenolic compounds, the total amount of monoterpenes is preferably 0.1 to 30 parts by weight, more preferably 0.5 to 20 parts by weight, and even more preferably 1 to 10 parts by weight, per 1 part by weight of the total amount of phenolic compounds.

[0023] The content of the monoterpene in the oral composition of the present invention is, for example, 0.001 to 5% by weight. From the viewpoint of more effectively suppressing the irritation caused by phenolic compounds, the content of the monoterpene in the oral composition of the present invention is preferably 0.01 to 3% by weight, more preferably 0.05 to 2% by weight, and even more preferably 0.1 to 1% by weight.

[0024] [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, but examples thereof 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 alone or in combination of two or more.

[0025] When a monohydric lower alcohol is contained in the oral composition of the present invention, the content is not particularly limited, but may be, for example, 0.01 to 5% by weight, preferably 0.1 to 4% by weight, and more preferably 0.5 to 3% by weight.

[0026] [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 is applicable to the oral cavity, and examples thereof include ethylene glycol, 1,3-butylene glycol, propylene glycol, isoprene glycol, diethylene glycol, dipropylene glycol, polypropylene glycol, and glycerin. Among these polyhydric alcohols, glycerin is preferred. These polyhydric alcohols may be used alone or in combination of two or more.

[0027] When a polyhydric alcohol is contained in the oral composition of the present invention, the content is not particularly limited, but may be, for example, 0.1 to 50% by weight, preferably 1 to 40% by weight, and more preferably 10 to 35% by weight.

[0028] [water] The oral composition of the present invention preferably 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 depending on the form of the oral composition, etc., but may be, for example, 10 to 99.9 wt %, preferably 15 to 99 wt %, more preferably 35 to 98 wt %, and even more preferably 40 to 88 wt %.

[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, as long as 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, hypersensitivity inhibitors, anti-tartar agents, tooth strengthening / remineralizing agents, local anesthetics, blood circulation promoters, thickeners, humectants, sweeteners, colorants, deodorizers, and pH adjusters.

[0030] [Dosage form / shape] The dosage 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 examples thereof include liquid and semi-solid forms (gel, paste).

[0031] 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, and examples thereof include oral hygiene agents such as liquid dentifrices, toothpastes, mouthwashes (liquid dentifrices and mouthwashes are sometimes commonly called mouth rinses, mouthwashes, dental rinses, etc.), mouth fresheners (mouth sprays, etc.), oral ointments, etc. Of these, liquid dentifrices, toothpastes, and mouthwashes are preferred.

[0032] 2. Stimulus suppression method The present invention further provides a method for suppressing irritation caused by an oral composition containing a phenolic compound, which comprises blending a phenolic compound and a monoterpene into the oral composition.

[0033] In the irritation suppression of the present invention, the type and amount of phenolic compound, the type and amount of monoterpene, other ingredients that can be added and their amounts, pH, oral dosage form, shape, etc. are as described in the section "1. Oral Composition" above. [Example]

[0034] The present invention will be explained in more detail below by showing examples, but the present invention is not limited to these examples.

[0035] Test Example Liquid preparations having the compositions shown in Tables 1 and 2 were prepared according to conventional methods. 500 μl of the resulting liquid preparations were placed in the mouths of evaluators trained in taste testing, and irritation was evaluated according to the following criteria. <Criteria for irritation> 6: I don't feel any tingling sensation on my tongue at all. 5: There is almost no tingling sensation on the tongue. 4: After about 10 seconds of putting it in your mouth, you will feel a slight tingling sensation on your tongue. 3: About 5 seconds after putting it in your mouth, you will feel a tingling sensation on your tongue. 2: After about 2-3 seconds of putting it in your mouth, you will feel a tingling sensation on your tongue. 1: Immediately after putting it in your mouth, you will feel a tingling sensation on your tongue.

[0036] The results are shown in Tables 1 and 2. When thymol or a parahydroxybenzoic acid ester (methyl parahydroxybenzoate or ethyl parahydroxybenzoate) was contained in the absence of camphor or menthol, irritation was observed (Comparative Examples 1 to 5). In contrast, when camphor or menthol was contained together with thymol or a parahydroxybenzoic acid ester, irritation was suppressed (Examples 1 to 12). In particular, when 1 part by weight or more of camphor or menthol was contained per part by weight of thymol or a parahydroxybenzoic acid ester, a significant irritation suppressing effect was observed (Examples 2 to 6 and 8 to 12).

[0037] [Table 1]

[0038] [Table 2]

[0039] Manufacturing example Toothpastes having the compositions shown in Table 3 and mouthwashes having the compositions shown in Table 4 were prepared. Irritation was confirmed using the obtained toothpastes and mouthwashes, and it was found that the irritation caused by phenolic compounds was reduced in both cases.

[0040] [Table 3]

[0041] [Table 4]

Claims

1. An oral composition containing a phenolic compound and a monoterpene.

2. The oral composition according to claim 1 , wherein the phenolic compound is thymol and / or a parahydroxybenzoic acid ester.

3. The oral composition according to claim 1 or 2, wherein the monoterpene is camphor and / or menthol.

4. 4. The oral composition according to claim 1, wherein the monoterpene is contained in an amount of 0.01 to 100 parts by weight per part by weight of the total amount of the phenolic compounds.

5. The oral composition according to any one of claims 1 to 4, wherein the content of the phenolic compound is 0.001 to 5% by weight.

6. The oral composition according to any one of claims 1 to 4, wherein the content of the monoterpene compound is 0.001 to 5% by weight.

7. A method for suppressing irritation caused by an oral composition containing a phenolic compound, comprising: A method for suppressing irritation by incorporating a phenolic compound and a monoterpene into an oral composition.

Citation Information

Patent Citations

  • Composition for oral cavity

    JP1999322554A