JP2023165258A - Oral composition - Google Patents

Abstract

To suppress the disproportionation of cetylpyridinium chloride hydrate (CPC) even with a relatively high level of the CPC.SOLUTION: An oral composition contains cetylpyridinium chloride hydrate of 0.1 mass% or more, and further contains polyoxyethylene hydrogenated castor oil with an average number of added moles of ethylene oxide ranging from 35 to 45, and polyoxyethylene sorbitan stearate.SELECTED DRAWING: None

Description

TECHNICAL FIELD The present invention relates to oral compositions.

BACKGROUND ART Oral compositions for the prevention and treatment of periodontitis and stomatitis have been known.
Patent Document 1 discloses an oral composition containing cetylpyridinium chloride, also called cetylpyridinium chloride hydrate.

Japanese Patent Application Publication No. 2011-73970

By the way, in oral compositions containing cetylpyridinium chloride hydrate (hereinafter also referred to as CPC), as the concentration of CPC increases, CPC becomes non-uniform. If CPC becomes non-uniform, the concentration of CPC will vary in the oral composition, and there is a possibility that the bactericidal action of CPC will vary.

The oral composition for solving the above problems contains 0.1% by mass or more of cetylpyridinium chloride hydrate, and further contains polyoxyethylene hardened castor having an average number of added moles of ethylene oxide of 35 to 45. The gist is that it contains oil and polyoxyethylene sorbitan stearate.

In the oral cavity composition, the content of the polyoxyethylene hydrogenated castor oil is preferably 0.5% by mass or more and 3% by mass or less.
In the oral cavity composition, the content of the polyoxyethylene sorbitan stearate is preferably 0.5% by mass or more and 3% by mass or less.

In the oral composition, the content of hydroxyethylcellulose is preferably 1% by mass or more and 3% by mass or less, and the content of crystalline cellulose is preferably 5% by mass or more and 20% by mass or less.

In the oral composition, the content of the cetylpyridinium chloride hydrate is preferably 0.3% by mass or more.

According to the oral composition of the present invention, it is possible to suppress non-uniformity of CPC even when the concentration of CPC is relatively high.

Embodiments of the oral cavity composition according to the present invention will be described.
The oral composition contains 0.1% by mass or more of CPC, and further contains polyoxyethylene hydrogenated castor oil having an average added mole number of ethylene oxide of 35 or more and 45 or less, and polyoxyethylene sorbitan stearate.

When the oral composition contains CPC at a relatively high concentration of 0.1% by mass or more, the bactericidal action of CPC can be suitably expressed. Further, by containing polyoxyethylene hydrogenated castor oil having an average added mole number of ethylene oxide of 35 or more and 45 or less and polyoxyethylene sorbitan stearate, it is possible to suppress non-uniformity of CPC.

Each component constituting the oral composition will be explained below.
<CPC>
CPC is commonly used as a disinfectant. The CPC is not particularly limited, and any known CPC can be used.

The content of CPC is preferably 0.3% by mass or more. When the content of CPC is 0.3% by mass or more, the concentration of CPC becomes higher, so that the bactericidal action of CPC can be expressed more suitably.

<Polyoxyethylene hydrogenated castor oil>
Polyoxyethylene hydrogenated castor oil has an average number of added moles of ethylene oxide of 35 or more and 45 or less. The average number of added moles of ethylene oxide is preferably 40. The above polyoxyethylene hydrogenated castor oil is generally used as a nonionic surfactant.

The above-mentioned polyoxyethylene hydrogenated castor oil is not particularly limited, and any known polyoxyethylene hydrogenated castor oil can be used.
A specific example of the above-mentioned polyoxyethylene hydrogenated castor oil includes polyoxyethylene hydrogenated castor oil (hereinafter also referred to as POE hydrogenated castor oil 40) in which the average number of added moles of ethylene oxide is 40.

The content of POE hydrogenated castor oil 40 is not particularly limited, but is preferably 0.5% by mass or more and 3% by mass or less. When the content of POE hydrogenated castor oil 40 is within the above numerical range, non-uniformity of CPC can be more suitably suppressed.

<Polyoxyethylene sorbitan stearate>
Polyoxyethylene sorbitan stearate is commonly used as a nonionic surfactant. The polyoxyethylene sorbitan stearate is not particularly limited, and known polyoxyethylene sorbitan stearate (hereinafter also referred to as polysorbate 60) can be used.

The content of polysorbate 60 is not particularly limited, but is preferably 0.5% by mass or more and 3% by mass or less. When the content of polysorbate 60 is within the above numerical range, non-uniformity of CPC can be suitably suppressed.

<Other ingredients>
Oral compositions may contain other ingredients other than those mentioned above, such as bactericides, antibacterial agents, surfactants, wetting agents, thickeners, stabilizers, and preservatives, depending on the application purpose, form, use, etc. , a sweetener, a pH adjuster, an antioxidant, a flavoring agent, a coloring agent, etc. may be added. As each of these components, known components that are incorporated into oral compositions can be used. These components may be used alone or in combination of two or more.

Specific examples of fungicides include, in addition to the above-mentioned CPC, hinokitiol and the like.
Specific examples of antibacterial agents include parabens, sodium benzoate, triclosan, chlorhexidine hydrochloride, chlorhexidine gluconate, minocycline hydrochloride, isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, and the like.

Specific examples of surfactants include nonionic surfactants, anionic surfactants, and amphoteric surfactants.
(Nonionic surfactant)
Specific examples of nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters and maltose fatty acid esters, sugar alcohol fatty acid esters such as maltitol fatty acid esters, and sorbitan fatty acid esters such as sorbitan stearate and sorbitan monolaurate. , polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan laurate (also referred to as polysorbate 20), polyoxyethylene sorbitan oleate (also referred to as polysorbate 80), fatty acid alkanolamides such as lauric acid diethanolamide, polyoxyethylene Polyoxyethylene alkyl ethers such as stearyl ether and polyoxyethylene oleyl ether, polyethylene glycol fatty acid esters such as polyethylene glycol monooleate and polyethylene glycol monolaurate, alkyl glycosides such as lauryl glycoside and decyl glycoside, polyglycerin fatty acid esters, polyoxy Ethylene glycerin fatty acid ester, polyoxyethylene fatty acid ester, alkyl glucosides, polyoxyethylene hydrogenated castor oil (with an average added mole number of ethylene oxide of 10, 20, 60), glycerin fatty acid ester, polyoxyethylene propylene block copolymer, etc. can be mentioned.

(Anionic surfactant)
Specific examples of anionic surfactants include sulfuric acid ester salts such as sodium lauryl sulfate and sodium polyoxyethylene lauryl ether sulfate, sulfosuccinates such as sodium lauryl sulfosuccinate and sodium polyoxyethylene lauryl ether sulfosuccinate, and cocoyl sarcosine. Examples include sodium, acyl amino acid salts such as sodium lauroylmethylalanine, sodium cocoylmethyltaurate, and the like.

(Ampholytic surfactant)
Specific examples of amphoteric surfactants include amino acid type amphoteric surfactants such as N-lauryldiaminoethylglycine and N-myristyldiethylglycine, alkyldimethylaminoacetic acid betaine, and N-alkyl-N'-carboxymethyl-N'. -hydroxyethylethylenediamine salt, and betaine-based amphoteric surfactants such as 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine.

The content of surfactants other than POE hydrogenated castor oil 40 and polysorbate 60 is not particularly limited, but is preferably less than 1% by mass.
When the content of surfactants other than POE hydrogenated castor oil 40 and polysorbate 60 is less than 1% by mass, solid-liquid separation of each component in the oral composition can be suitably suppressed.

Specific examples of wetting agents include propylene glycol, glycerin, sorbitol, polyethylene glycol, 1,3-butylene glycol, water, alcohol, and the like.

Among these, it is preferable to contain at least one of propylene glycol and glycerin.
The content of the wetting agent is not particularly limited, but is preferably 35% by mass or more, more preferably 40% by mass or more, and even more preferably 45% by mass or more. Further, it is preferably 90% by mass or less, more preferably 85% by mass or less, and even more preferably 80% by mass or less.

The content of propylene glycol is not particularly limited, but is preferably 5% by mass or more, more preferably 10% by mass or more, and even more preferably 15% by mass or more. Moreover, it is preferably 35% by mass or less, more preferably 30% by mass or less, and even more preferably 25% by mass or less.

The content of glycerin is not particularly limited, but is preferably 15% by mass or more, more preferably 20% by mass or more, and even more preferably 25% by mass or more. Further, it is preferably 45% by mass or less, more preferably 40% by mass or less, and even more preferably 35% by mass or less.

Specific examples of the thickener include sodium polyacrylate, carrageenan, sodium carboxymethylcellulose, sodium alginate, xanthan gum, hydroxyethylcellulose, crystalline cellulose, hydroxypropylmethylcellulose, methylcellulose, propylene glycol alginate, and the like. Thickeners are also called binders.

Among these, it is preferable to contain hydroxyethyl cellulose and crystalline cellulose.
Although the content of hydroxyethyl cellulose is not particularly limited, it is preferably 1% by mass or more and 3% by mass or less.

The content of crystalline cellulose is not particularly limited, but is preferably 5% by mass or more, more preferably 8% by mass or more, and even more preferably 10% by mass or more. Further, it is preferably 20% by mass or less, more preferably 18% by mass or less, and even more preferably 15% by mass or less.

When the content of hydroxyethyl cellulose and crystalline cellulose is within the above numerical range, it becomes easy to adjust the viscosity of the oral composition and make it into a paste or gel.
Specific examples of the stabilizer include sodium edetate, sodium thiosulfate, sodium sulfite, calcium lactate, lanolin, triacetin, castor oil, magnesium sulfate, and the like.

Specific examples of preservatives include 1,2-dibromo-2,4-dicyanobutane, photosensitizers, isothiazolone derivatives, hydantoin derivatives, parabens, sodium benzoate, phenol, and the like.

Specific examples of sweeteners include saccharin, saccharin sodium, acesulfame potassium, stevia extract, palatinose, palatinit, erythritol, maltitol, xylitol, lactitol, and the like.

Specific examples of the pH adjuster include citric acid, phosphoric acid, malic acid, pyrophosphoric acid, lactic acid, tartaric acid, glycerophosphoric acid, acetic acid, nitric acid, or chemically possible salts thereof, sodium hydroxide, and the like.

Specific examples of antioxidants include tocopherols, dibutylhydroxytoluene, butylhydroxyanisole, gallic acid esters, and the like.
The fragrance may be a natural fragrance or a synthetic fragrance. Further, it may be a single fragrance or a mixed fragrance.

Specific examples of fragrances include l-menthol, d-carvone, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate, citronellyl acetate, methyl eugenol, cineol, Linalool, ethyl linalool, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, perilla oil, wintergreen oil, clove oil, eucalyptus oil, pimento oil, d-camphor, d-borneol, Examples include fennel oil, cinnamon oil, cinnamaldehyde, peppermint oil, and vanillin.

Specific examples of colorants include legal pigments such as Green No. 1, Green No. 3, Blue No. 1, Yellow No. 4, Yellow No. 5, Red No. 102, Red No. 3, copper chlorofin sodium, titanium oxide, etc. Can be mentioned.

<Application form, dosage form, and use of oral composition>
The application form of the oral composition is not particularly limited, and it can be used, for example, as a pharmaceutical, a designated quasi-drug, a quasi-drug, or a cosmetic.

The dosage form of the oral composition is not particularly limited, but it can be used as a paste, ointment, or gel.
Applications of oral compositions include, for example, oral coatings for the tongue and other areas, gingival anti-inflammatory agents, periodontal disease therapeutics, denture attachments, implant care agents, and the like.

<Action and effect>
The effect of the oral cavity composition of this embodiment will be explained.
In the oral composition, when the content of CPC is 0.1% by mass or more, CPC tends to become non-uniform. In other words, CPC tends to become non-uniform in the oral composition. When the content of CPC is 0.3% by mass or more, CPC becomes more likely to become non-uniform. When the oral composition contains POE hydrogenated castor oil 40 and polysorbate 60, non-uniformity of CPC can be suppressed. It is presumed that the mechanism of suppressing the non-uniformity of CPC is that the polarity of CPC is suitably relaxed by POE hydrogenated castor oil 40 and polysorbate 60, thereby suppressing aggregation of CPC.

Moreover, as another method of suppressing non-uniformity of CPC, it is possible to include a surfactant other than POE hydrogenated castor oil 40 and polysorbate 60. However, when the content of surfactant is increased, the oral composition becomes more prone to solid-liquid separation. Therefore, simply increasing the surfactant content may reduce the handling properties of the oral composition.

The effects of the oral cavity composition of this embodiment will be explained.
(1) Polyoxyethylene hydrogenated castor oil containing 0.1% by mass or more of cetylpyridinium chloride hydrate and having an average added mole number of ethylene oxide of 35 to 45, and polyoxyethylene sorbitan stearate. contains.

Therefore, even if the concentration of CPC is relatively high, such as 0.1% by mass or more, it is possible to suppress non-uniformity of CPC. Furthermore, since variations in the concentration of CPC in the oral composition can be suppressed, variations in the bactericidal action can be suppressed.

(2) The content of polyoxyethylene hydrogenated castor oil is 0.5% by mass or more and 3% by mass or less. Therefore, non-uniformity of CPC can be suitably suppressed.
(3) The content of polyoxyethylene sorbitan stearate is 0.5% by mass or more and 3% by mass or less. Therefore, non-uniformity of CPC can be suitably suppressed.

(4) The content of hydroxyethyl cellulose is 1% by mass to 3% by mass, and the content of crystalline cellulose is 5% by mass to 20% by mass. Therefore, it becomes easy to adjust the viscosity of the oral composition and make it gel-like.

(5) The content of CPC is 0.3% by mass or more. Therefore, the bactericidal effect of CPC can be expressed more suitably. Moreover, even if the content of CPC is 0.3% by mass or more, non-uniformity of CPC can be suppressed.

(6) The content of surfactants other than POE hydrogenated castor oil 40 and polysorbate 60 is less than 1% by mass. Therefore, solid-liquid separation of each component in the oral composition can be suppressed.

Examples will be given below to make the structure and effects of the present invention more concrete, but the present invention is not limited to these Examples.
The oral compositions of Examples 1 to 6 and Comparative Examples 1 to 6 shown in Table 1 were produced by mixing the respective components according to a conventional method.

In Table 1, the numbers written on the right side of each component mean the content (mass%) of each component, which was blended so that the total amount with the remaining water was 100% by mass. The oral composition had a gel-like form.

In Table 1, POE hydrogenated castor oil 60 means polyoxyethylene hydrogenated castor oil having an average number of added moles of ethylene oxide of 60.

(Evaluation test)
The oral compositions of Examples 1 to 6 and Comparative Examples 1 to 6 were evaluated for the presence or absence of non-uniformity and the presence or absence of solid-liquid separation. The evaluation method and evaluation results are shown below.

(Method for evaluating the presence or absence of non-uniformity)
25 g of each of the oral compositions of Examples 1 to 6 and Comparative Examples 1 to 6 was collected and filled into an aluminum laminate tube with a diameter of 22 mm. After attaching a cap to the laminate tube and sealing it, it was left to stand for one month under constant temperature conditions of 55°C. Thereafter, the oral composition was squeezed out of the laminated tube. In the squeezed oral composition, the concentration of CPC contained in the oral composition was measured at three locations: 1 g from the tip, 2 g from the tip, and 3 g from the tip. Known high performance liquid chromatography was used to measure the concentration of CPC. The coefficient of variation (hereinafter also referred to as CV value) of the concentration at the three locations was calculated, and when the CV value was 1.5 or less, it was considered uniform (◯). When the CV value was more than 1.5, it was classified as non-uniform (x). The results are shown in Table 1.

(Evaluation method for presence or absence of solid-liquid separation)
In the evaluation method for the presence or absence of non-uniformity, the presence or absence of solid-liquid separation was visually confirmed when the oral composition was squeezed out from the laminated tube after being left for one month under a constant temperature condition of 55°C. If solid-liquid separation was not confirmed, it was determined that there was no solid-liquid separation (○). If solid-liquid separation was confirmed, it was determined that solid-liquid separation was present (x). The results are shown in Table 1. Note that for oral compositions in which solid-liquid separation was confirmed, the presence or absence of non-uniformity was not evaluated.

(Evaluation results)
From Table 1, it was confirmed that Comparative Examples 1 to 6 did not contain POE hydrogenated castor oil 40 or polysorbate 60, and the CPC was non-uniform. Moreover, in Comparative Example 3, since the content of POE hydrogenated castor oil 60 was as large as 1% by mass, solid-liquid separation occurred.

On the other hand, in Examples 1 to 6, since POE hydrogenated castor oil 40 and polysorbate 60 were contained, the CPC did not become non-uniform. Further, no solid-liquid separation occurred.

Claims (5)

Contains 0.1% by mass or more of cetylpyridinium chloride hydrate,
Furthermore, an oral composition characterized by containing polyoxyethylene hydrogenated castor oil having an average added mole number of ethylene oxide of 35 or more and 45 or less, and polyoxyethylene sorbitan stearate. The oral composition according to claim 1, wherein the content of the polyoxyethylene hydrogenated castor oil is 0.5% by mass or more and 3% by mass or less. The oral composition according to claim 1, wherein the content of the polyoxyethylene sorbitan stearate is 0.5% by mass or more and 3% by mass or less. The oral composition according to claim 1, wherein the content of hydroxyethyl cellulose is 1% by mass or more and 3% by mass or less, and the content of crystalline cellulose is 5% by mass or more and 20% by mass or less. The oral composition according to any one of claims 1 to 4, wherein the content of the cetylpyridinium chloride hydrate is 0.3% by mass or more.