TW202302067A - Composition for oral cavity - Google Patents

Abstract

The purpose of the present invention is to provide a composition for the oral cavity that, while containing a phenol compound, exhibits a suppression of the irritation perceived upon use in the oral cavity. The irritation caused by phenol compounds can be suppressed by the incorporation in the composition for the oral cavity of a monoterpene in addition to the phenol compound.

Description

oral composition

The present invention relates to a composition for oral cavity containing a phenolic compound and suppressing the irritation sensed when applied to the oral cavity.

Thymol (thymol, 2-isopropyl-5-methylphenol) is known to penetrate into biofilms to exhibit a bactericidal effect, and is widely used in oral compositions such as dentifrices and mouthwashes. In addition, parabens are widely used in oral compositions as preservatives. Conventionally, there have been various reports on formulation techniques for oral compositions containing phenolic compounds such as thymol and parabens. For example, in Patent Document 1, it is described that a phenolic fungicide such as thymol or a paraben, an anionic surfactant, and a nonionic surfactant are contained, and that the nonionic surfactant is The composition for oral cavity in which the weight ratio of the surfactant is 0.1 to 3 and the water content in the composition is 40% by weight or less prevents the container adsorption of the phenolic fungicide and improves the stability of the phenolic fungicide over time.

On the other hand, in the case of an oral composition containing a phenolic compound such as thymol or a paraben, there is a disadvantage that irritation occurs when it is applied in the oral cavity, and the usability decreases. Conventionally, as a method of reducing the irritation of oral compositions containing phenolic compounds, a method of preparing sweeteners such as saccharin sodium (saccharin sodium), stevia extract, and erythritol as a taste-masking agent is known. However, in oral compositions formulated with such a taste-masking agent, sweetness appears, and a satisfactory usability cannot necessarily be obtained. [Prior art literature] [Patent Document]

[Patent Document 1] Japanese Patent Laid-Open No. 11-322554

[Problems to be Solved by the Invention] An object of the present invention is to provide an oral composition containing a phenolic compound, in which the irritation sensed when applied to the oral cavity is suppressed. [Means to solve the problem]

As a result of diligent research by the present inventors to solve the above-mentioned problems, it was found that the irritation caused by the phenolic compound can be suppressed by containing both a phenolic compound and a monoterpene in an oral composition. The present invention was completed by further repeated studies based on the above findings.

That is, the present invention provides the inventions of the embodiments disclosed below. Item 1. A composition for oral cavity 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 paraben. Item 3. The oral composition according to Item 1 or Item 2, wherein the monoterpene is camphor and/or menthol. Item 4. The oral composition according to any one of Items 1 to 3, which contains 0.01 to 100 parts by weight of the monoterpene relative to 1 part by weight of the total amount of the phenolic compound. Item 5. The oral composition according to any one of Items 1 to 4, wherein the content of the phenol compound is 0.001% by weight 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% by weight to 5% by weight. Item 7. A method for suppressing irritation, which is a method for suppressing irritation of an oral composition containing a phenolic compound, wherein Phenolic compounds and monoterpenes are formulated in oral compositions. [Effect of the invention]

According to the present invention, by containing both the phenolic compound and the monoterpene in the composition for oral cavity, the stimulation of the phenolic compound can be suppressed when applied to the oral cavity, and an excellent usability can be provided.

1. Oral composition The composition for oral cavity of this invention is characterized by containing a phenolic compound and a monoterpene. Hereinafter, the oral composition of the present invention will be described in detail.

[phenolic compound] The composition for oral cavity of this invention contains a phenolic compound. In this specification, a phenol compound is a generic term for compounds having a phenol skeleton.

The type of the phenolic compound used in the present invention is not particularly limited as long as it can be applied in the oral cavity, and examples thereof include thymol, paraben, and the like.

Specific examples of parabens include methyl paraben, ethyl paraben, propyl paraben, isopropyl paraben, and butyl paraben. .

These phenolic compounds may be used alone or in combination of two or more.

Among these phenolic compounds, thymol, methyl p-hydroxybenzoate, and ethyl p-hydroxybenzoate are preferably mentioned.

The content of the phenolic compound in the oral composition of the present invention may be appropriately set according to the type of the phenolic compound used, the form of the oral composition, etc., for example, 0.001 wt. based on the total amount of the phenolic compound %~5% by weight. From the viewpoint of more effectively suppressing the irritation of phenolic compounds, the total amount of phenolic compounds in the oral composition of the present invention is preferably 0.005% by weight to 2% by weight, more preferably 0.01% by weight. % by weight to 1% by weight, more preferably 0.05% by weight to 0.3% by weight.

[Monoterpene] The oral composition of the present invention also contains monoterpenes in addition to phenolic compounds. Stimulation by the phenolic compound can be suppressed by allowing the phenolic compound to coexist with the monoterpene.

The so-called monoterpene is a well-known component which has a structure including two isoprene units in a molecule|numerator, and has cooling action etc.

The type of monoterpene used in the present invention is not particularly limited as long as it can be applied in the oral cavity, for example, menthol, geraniol, linalool, borneol, cineole, pine oil Alcohol-based monoterpenes such as alcohol; aldehyde-based monoterpenes such as citral, citronellal, perillaldehyde, and saffron; ketone-based monoterpenes such as camphor, menthone, carvomenthone, and ionone ene etc. When optical isomers exist, these monoterpenes may be any of d-body, l-body, and d1-body. These monoterpenes may be used alone or in combination of two or more.

In addition, in the composition for oral cavity of this invention, as a monoterpene, you may use it in the state containing the essential oil of a monoterpene. The essential oil containing monoterpene can be appropriately selected from known ones, and examples of the essential oil containing menthol include peppermint oil, peppermint oil, spearmint oil and the like. In addition, when using the essential oil containing a monoterpene, description about the content or ratio of a monoterpene in this specification is the value converted into the amount of the monoterpene contained in the said essential oil.

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

Among these monoterpenes, from the viewpoint of more effectively suppressing the stimulation of phenolic compounds, preferably ketone-based monoterpenes and alcohol-based monoterpenes are used, more preferably camphor and menthol are used.

In the oral composition of the present invention, the ratio of the monoterpene to the phenolic compound may be appropriately set according to the type of the phenolic compound and the monoterpene to be used, for example, 1 to the total amount of the phenolic compound. Parts by weight and monoterpenes are 0.01 parts by weight to 100 parts by weight in total. From the viewpoint of more effectively suppressing the irritation of phenolic compounds, the total amount of monoterpenes is preferably 0.1 parts by weight to 30 parts by weight, more preferably 1 part by weight of the total amount of phenolic compounds 0.5 to 20 parts by weight can be mentioned, more preferably 1 to 10 parts by weight can be mentioned.

As content of the monoterpene in the composition for oral cavity of this invention, 0.001 weight% - 5 weight% is mentioned, for example. From the viewpoint of more effectively suppressing the irritation of phenolic compounds, the content of monoterpene in the oral composition of the present invention is preferably 0.01% by weight to 3% by weight, more preferably 0.05% by weight ~2% by weight, more preferably 0.1% by weight~1% by weight.

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

When the oral composition of the present invention contains a monohydric lower alcohol, the content is not particularly limited, for example, 0.01% by weight to 5% by weight, preferably 0.1% by weight to 4% by weight, and more preferably 0.5% by weight to 3% by weight.

[Polyol] The oral composition of the present invention may further include polyhydric alcohols. The polyhydric alcohol is not particularly limited as long as it can be applied in the oral cavity, for example, ethylene glycol, 1,3-butanediol, propylene glycol, isopropylene glycol, diethylene glycol, dipropylene glycol, polypropylene glycol, glycerin, etc. . Among these polyhydric alcohols, glycerin is preferably used. These polyols may be used alone or in combination of two or more.

When the composition for oral cavity of the present invention contains a polyhydric alcohol, its content is not particularly limited, for example, 0.1% by weight to 50% by weight, preferably 1% by weight to 40% by weight, and more preferably 10% by weight. % by weight to 35% by weight.

[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 appropriately set according to the form of the oral composition, as long as it is the remainder after removing the added components, for example, 10% by weight to 99.9% by weight, Preferably it is 15 weight% - 99 weight%, More preferably, it is 35 weight% - 98 weight%, More preferably, it is 40 weight% - 88 weight%.

[other containing ingredients] The composition for oral cavity of the present invention may contain components generally used in the technical field according to the form of the composition for oral cavity, in addition to the above-mentioned components, within the range not impairing the effect of the present invention. Examples of such components include antiseptics, bactericides, antibacterial agents, anti-inflammatory agents, abrasives, glucosyltransferase (glycosyltransferase, GTase) inhibitors, plaque inhibitors, hyperesthesia inhibitors, calculus preventive agents, Dentin strengthening/remineralizing agents, local anesthetics, blood circulation accelerators, thickeners, humectants, sweeteners, pigments, deodorants, pH regulators, etc.

[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 in the oral cavity, and examples include liquid or semisolid forms (gel, paste).

The form of the composition for oral cavity of the present invention is not particularly limited as long as it is a form that can be applied in the oral cavity and can be retained in the oral cavity for a fixed period of time. Examples include: liquid dentifrice, toothpaste, mouthwash (liquid Dental rinses, mouthwashes are generally sometimes called mouth rinses, mouth washes, dental rinses, etc.), mouth fresheners (mouth sprays, etc.) ), oral hygiene agents such as ointments for the oral cavity. Among these, liquid dentifrices, toothpastes, and mouthwashes are preferred.

2. Stimulus inhibition method The present invention further provides an irritation suppression method, which is a method for suppressing irritation of an oral composition containing a phenolic compound, wherein a phenolic compound and a monoterpene are blended in the oral composition.

In the stimulation suppression of the present invention, regarding the type or compounded amount of the phenolic compound, the type or compounded amount of the monoterpene, other components that can be compounded or their compounded amount, pH, oral dosage form, form, etc., as described in "1. As described in the column "composition for oral cavity". [Example]

Examples are shown below to describe the present invention more specifically, but the present invention is not limited thereto.

Test case Liquid preparations with the compositions shown in Table 1 and Table 2 were prepared according to a conventional method. 500 µl of the obtained liquid preparation was brought into the mouth of an evaluator trained in the taste test, and the irritation was evaluated according to the following judgment criteria. ＜Criteria for judging irritation＞ 6: The tongue does not feel hot stimulation at all. 5: The tongue hardly feels hot stimulation. 4: After about 10 seconds after containing it in the mouth, the tongue will feel some hot stimulation. 3: When about 5 seconds have elapsed since it was contained in the mouth, the tongue felt a hot stimulation. 2: After about 2 to 3 seconds after being contained in the mouth, the tongue will feel a burning sensation 1: Immediately after being contained in the mouth, a burning sensation is felt on the tongue.

The results are shown in Table 1 and Table 2. Stimulation was confirmed when thymol or parabens (methylparaben or ethylparaben) were included in the absence of camphor or menthol (Comparative Examples 1 to 5 ). On the other hand, when thymol or a paraben and camphor or menthol were contained together, stimulation was suppressed (Example 1-Example 12). In particular, when 1 part by weight or more of camphor or menthol was included with respect to 1 part by weight of thymol or a paraben, the stimulation-inhibiting effect was remarkably confirmed (Examples 2 to 6 and embodiment 8 to embodiment 12).

[Table 1] comparative example Example 1 2 1 2 3 4 5 6 7 8 9 Thymol 0.05 0.1 0.1 0.1 0.1 0.1 0.05 0.3 1 0.1 0.1 dl-camphor - - 0.05 0.1 0.3 1 0.3 0.3 0.3 - - 1-menthol - - - - - - - - - 0.1 0.3 ethanol 2.5 2.5 2.5 2.5 2.5 2.5 2.5 2.5 2.5 2.5 2.5 concentrated glycerin 30 30 30 30 30 30 30 30 30 30 30 Sorbitol liquid (sorbitol concentration 70% by weight) 30 30 30 30 30 30 30 30 30 30 30 purified water The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part Total (weight%) 100 100 100 100 100 100 100 100 100 100 100 Ratio of monoterpene to 1 part by weight of phenolic compound (parts by weight) - - 0.5 1 3 10 6 1 0.3 1 3 Stimulant evaluation results 2 1 4 5 6 6 6 6 3 5 6

[Table 2] comparative example Example comparative example Example comparative example Example Reference example 3 10 4 11 5 12 1 2 Thymol - - - - 0.1 0.1 - - Methylparaben 0.1 0.1 - - - - - - Ethyl p-hydroxybenzoate - - 0.1 0.1 - - - - dl-camphor - 0.3 - 0.3 - 0.1 0.1 - 1-menthol - - - - - - - 0.1 ethanol 2.5 2.5 2.5 2.5 2.5 2.5 2.5 2.5 concentrated glycerin 30 30 30 30 - - 30 30 Sorbitol liquid (sorbitol concentration 70% by weight) 30 30 30 30 - - 30 30 purified water The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part The remaining part Total (weight%) 100 100 100 100 100 100 100 100 Ratio of monoterpene to 1 part by weight of phenolic compound (parts by weight) - 3 - 3 - 1 - - Stimulant evaluation results 2 4 2 4 1 5 6 6

Manufacturing example Toothpaste with the composition shown in Table 3 and mouthwash with the composition shown in Table 4 were prepared. Irritation was confirmed using the obtained toothpaste and mouthwash, and the irritation caused by the phenolic compound was reduced in both.

[Table 3] Toothpaste Manufacturing example 1 Manufacturing example 2 Thymol 0.1 0.3 parabens 0.1 0.1 dl-camphor 0.25 1 1-menthol 0.8 0.8 concentrated glycerin 30 30 Sorbitol 30 30 Anhydrous silicic acid 5 5 Hydrous Silicic Acid 15 15 sodium lauryl sulfate 1 1 ethanol 2.5 2.5 cetylpyridinium chloride 0.05 0.05 POE hardened castor oil 1 1 spices 0.9 0.9 purified water The remaining part The remaining part Total (weight%) 100 100

[Table 4] Mouthwash Manufacturing example 3 Manufacturing Example 4 Thymol 0.1 0.3 parabens 0.1 0.1 dl-camphor 0.25 1 1-menthol 0.8 0.8 concentrated glycerin 10 10 Propylene Glycol 5 5 ethanol 10 10 POE hardened castor oil 1 1 cetylpyridinium chloride 0.05 0.05 spices 0.9 0.9 citric acid 0.01 0.01 trisodium citrate 0.1 0.1 purified water the remains the remains Total (weight%) 100 100

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Claims (7)

An oral composition containing phenolic compounds and monoterpenes. The oral composition according to claim 1, wherein the phenolic compound is thymol and/or paraben. The oral composition according to claim 1 or claim 2, wherein the monoterpene is camphor and/or menthol. The oral composition according to any one of claim 1 to claim 3, wherein the monoterpene is contained in an amount of 0.01 to 100 parts by weight relative to 1 part by weight of the total amount of the phenolic compound. The composition for oral cavity according to any one of claim 1 to claim 4, wherein the content of the phenolic compound is 0.001% by weight to 5% by weight. The oral composition according to any one of claim 1 to claim 4, wherein the content of the monoterpene compound is 0.001% by weight to 5% by weight. A method for suppressing irritation, which is a method for suppressing irritation of an oral composition containing a phenolic compound, wherein Phenolic compounds and monoterpenes are formulated in oral compositions.