Oral composition
By blending laurylpyridinium chloride with macrocyclic musk compounds, aliphatic unsaturated ketones, or aliphatic unsaturated alcohols, the oral composition effectively reduces irritation and astringency, addressing the challenges posed by laurylpyridinium chloride in oral formulations.
Patent Information
- Application Number
- JP2023207225
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2023-12-07
- Publication Date
- 2025-06-19
AI Technical Summary
Laurylpyridinium chloride, effective in killing Fusobacterium contributing to plaque formation, exhibits strong irritation and astringency, posing challenges in formulating oral compositions with improved usability.
Blending laurylpyridinium chloride with macrocyclic musk compounds, aliphatic unsaturated ketones, or aliphatic unsaturated alcohols reduces irritation and astringency, enhancing the composition's usability.
The blending of laurylpyridinium chloride with specific compounds significantly reduces irritation and astringency, leading to an improved oral composition that is more palatable and effective in preventing periodontal disease.
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Abstract
Description
Technical Field
[0001] The present disclosure relates to oral compositions and the like. Specifically, it relates to an oral composition and the like containing (A) laurylpyridinium chloride, and at least one selected from the group consisting of (B) (B-1) macrocyclic musk compounds, (B-2) aliphatic unsaturated ketones having 5 to 10 carbon atoms, and (B-3) aliphatic unsaturated alcohols having 5 to 10 carbon atoms.
Background Art
[0002] Among quaternary ammonium salts that are bactericides, cetylpyridinium chloride (also referred to as "CPC") has high bactericidal activity against periodontal disease-causing bacteria and has been widely used in oral compositions. However, CPC has bitterness and irritation, which has been a problem when formulating it into oral compositions. Therefore, conventionally, methods for improving the usability with various additives have been developed to reduce the bitterness or irritation derived from CPC (Patent Documents 1 to 6).
[0003] Patent Document 1 describes a method for improving the bitterness of cationic bactericides such as CPC by blending l-menthol and chlorobutanol.
[0004] Patent Document 2 describes a method for suppressing the bitterness of CPC and improving the usability by blending low concentrations of ethyl maltol and l-menthol in a liquid oral composition.
[0005] Patent Document 3 describes a method for improving the bitterness of CPC by blending anethole, eugenol, linalool, and menthol at a predetermined concentration.
[0006] Patent Document 4 describes a method for improving the discomfort of the aftertaste caused by CPC by blending specific plant extracts such as Nigaki and hops.
[0007] Patent Document 5 describes a method for improving the bitterness and irritation of cationic bactericides such as CPC by a combination of high-sweetness sweeteners and specific fragrance components.
[0008] Patent Document 6 describes a method for improving the specific bitterness and irritation of CPC by blending limonene, polyoxyethylene hydrogenated castor oil, propylene glycol, and xylitol at a predetermined concentration.
[0009] On the other hand, recent research has shown that for the prevention of periodontal disease, it is important to suppress the formation of plaque, which is the cause of periodontal disease, and laurylpyridinium chloride (also referred to as "dodecylpyridinium chloride" or "DPC") is effective in killing Fusobacterium, which contributes to plaque formation by coaggregating with various bacteria (Patent Document 7). However, compared with CPC, DPC has a stronger irritation and a specific astringency, so there are still problems in the usability with the conventional methods for reducing bitterness or irritation of CPC, which has been a drawback in product development.
[0010] In recent years, a method has been developed to improve the strong bitterness that occurs when CPC and DPC are used in combination by blending methyl paraben, sodium saccharin, menthol, etc. (Patent Documents 8 and 9).
Prior Art Documents
Patent Documents
[0011]
Patent Document 1
Patent Document 2
Patent Document 3
Patent Document 4
Patent Document 5
Patent Document 6
[0012] [Non-Patent Document 1] Alternative Mechanisms of Astringency - What is the Role of Saliva?(DOI:https: / / doi.org / 10.1111 / jtxs.12022) [Summary of the Invention] [Problems to be Solved by the Invention]
[0013] An object of the present invention is to provide an oral composition containing laurylpyridinium chloride with reduced irritation and astringency. [Means for Solving the Problems]
[0014] The present inventors have found that by blending (A) laurylpyridinium chloride and at least one selected from the group consisting of (B) (B-1) macrocyclic musk compounds, (B-2) aliphatic unsaturated ketones having 5 to 10 carbon atoms, and (B-3) aliphatic unsaturated alcohols having 5 to 10 carbon atoms, the irritation and astringency of DPC are reduced, and further improvements have been made.
[0015] This disclosure includes, for example, the subject matter described in the following items. Item 1. (A) Laurylpyridinium chloride, and An oral composition containing at least one selected from the group consisting of (B)(B-1) a macrocyclic musk compound, (B-2) an aliphatic unsaturated ketone having 5 to 10 carbon atoms, and (B-3) an aliphatic unsaturated alcohol having 5 to 10 carbon atoms. Item 2. (B-1) is at least one selected from the group consisting of ω-pentadecalactone, muscone, and ethylene brassylate, (B-2) is at least one selected from the group consisting of 6-methyl-5-hepten-2-one and 4-methyl-3-penten-2-one, and / or The oral composition according to Item 1, wherein (B-3) is at least one selected from the group consisting of cis-3-hexenol, trans-2-hexenol, and cis-2-pentenol. Item 3. The oral composition according to Item 1 or 2, wherein the content of (A) is 3 to 200,000 parts by mass with respect to 1 part by mass of (B) in the oral composition. Item 4. When (B-1) is contained, the content of (A) is 100 to 200,000 parts by mass with respect to 1 part by mass of (B-1) in the oral composition, When (B-2) is contained, the content of (A) is 3 to 5000 parts by mass with respect to 1 part by mass of (B-2) in the oral composition, and / or The oral composition according to any one of Items 1 to 3, wherein when (B-3) is contained, the content of (A) is 3 to 5000 parts by mass with respect to 1 part by mass of (B-3) in the oral composition. Item 5. The oral composition according to any one of Items 1 to 4, containing 0.01 to 0.5% by mass of (A). Item 6. When (B-1) is contained, the content of (B-1) in the oral composition is 0.0000001 to 0.001% by mass, When (B-2) is contained, the content of (B-2) in the oral composition is 0.000002 to 0.01% by mass, and / or When containing (B-3), the oral composition according to any one of Items 1 to 5, wherein the content of (B-3) is 0.000002 to 0.01% by mass. Item 7. Furthermore, the oral composition according to any one of Items 1 to 6, which contains (C) an alkali metal acetate.
Advantages of the Invention
[0016] There is provided an oral composition containing laurylpyridinium chloride with reduced irritation and astringency.
Modes for Carrying Out the Invention
[0017] Hereinafter, each embodiment included in the present disclosure will be described in more detail. The oral composition included in the present disclosure contains (A) laurylpyridinium chloride and at least one selected from the group consisting of (B) (B-1) a macrocyclic musk compound, (B-2) an aliphatic unsaturated ketone having 5 to 10 carbon atoms, and (B-3) an aliphatic unsaturated alcohol having 5 to 10 carbon atoms. In the present specification, the oral composition may be referred to as "the oral composition of the present disclosure". Further, each component of (A) and (B) may be referred to as "(A) component", "(B) component", etc. Further, each component of (B) component may be referred to as "(B-1) component", "(B-2) component", "(B-3) component", etc.
[0018] In the present specification, the "macrocyclic musk compound" refers to a compound having a 14- to 18-membered macrocyclic structure, having 14 to 18 carbon atoms in the macrocyclic musk compound, and may contain an oxygen atom. The oxygen atom may form a ring together with 14 to 18 carbon atoms, or may have an oxygen atom as a substituent of the ring. The number of atoms forming the macrocyclic structure in the macrocyclic musk compound may be, for example, 15, 16, or 17. In other words, the macrocyclic musk compound may have a 15-membered, 16-membered, or 17-membered macrocyclic structure. Among them, the number of atoms forming the macrocyclic structure in the macrocyclic musk compound is preferably 15 to 17. In other words, the macrocyclic musk compound preferably has a 15- to 17-membered macrocyclic structure. The upper or lower limit of the carbon number range in the macrocyclic musk compound may be, for example, 15, 16, or 17. Among them, 14 to 17 is preferable, and 15 to 16 is more preferable. The number of oxygen atoms contained in the macrocyclic musk compound is preferably 1 to 5. The upper or lower limit of this range may be, for example, 2, 3, 4, or 5. Among them, 1 to 4 is preferable. The oxygen atom may be contained in the macrocyclic structure or in the side chain. The macrocyclic musk compound may or may not have 1 to 3 unsaturated bonds (double bonds between carbon atoms). The macrocyclic musk compound may have 1 to 3 carbonyl groups. Among them, the number of carbonyl groups is preferably 1 to 2. Examples of the macrocyclic musk compound include ω-pentadecalactone, muscone, ethylene brassylate, 3-methyl-4-cyclopentadecen-1-one, civetone, cyclopentadecanone, 5-cyclohexadecen-1-one, cyclohexadecanone, 11(12)-cyclopentadecenolide, 9-cyclopentadecenolide, cyclohexadecanolide, ethylene dodecanedioate, 12-oxahexadecanolide, 11-oxahexadecanolide, 10-oxahexadecanolide, ambrettolide, etc. These can be blended alone or in combination of two or more. Among them, ω-pentadecalactone, muscone, and ethylene brassylate are preferable, and ω-pentadecalactone is more preferable.
[0019] The upper or lower limit of the carbon number range in aliphatic unsaturated ketones having 5 to 10 carbon atoms may be, for example, 6, 7, 8, or 9. Among them, 6 to 8 is preferable. The aliphatic unsaturated ketone having 5 to 10 carbon atoms may be linear or branched. Among them, being branched is preferable. Moreover, the aliphatic unsaturated ketone having 5 to 10 carbon atoms may have 1 to 3 unsaturated bonds (double bonds between carbon atoms). Among them, the number of unsaturated bonds is preferably 1. The aliphatic unsaturated ketone having 5 to 10 carbon atoms may have 1 to 3 carbonyl groups. Among them, the number of carbonyl groups is preferably 1. Examples of the aliphatic unsaturated ketone having 5 to 10 carbon atoms include 6-methyl-5-hepten-2-one, 4-methyl-3-penten-2-one, 1-penten-3-one, 1-hexen-3-one, 4-hexen-3-one, 5-methyl-3-hexen-2-one, 1-hepten-3-one, 3-hepten-2-one, 6-methyl-3-hepten-2-one, 5-methyl-2-hepten-4-one, 6-methyl-3,5-heptadien-2-one, 1-octen-3-one, 2-octen-4-one, 3-octen-2-one, 4-octen-3-one, 1,5-octadien-3-one, 3,5-octadien-2-one, 3-nonen-2-one, 2-nonen-4-one, 5-nonen-2-one, 8-nonen-2-one, 3-decen-2-one, 2,5-dimethyl-2-octen-6-one, etc. These can be blended alone or in combination of two or more. Among them, 6-methyl-5-hepten-2-one and 4-methyl-3-penten-2-one are preferable, and more preferably 6-methyl-5-hepten-2-one.
[0020] The upper or lower limit of the carbon number range in aliphatic unsaturated alcohols having 5 to 10 carbon atoms may be, for example, 6, 7, 8, or 9. Among them, 5 to 6 is preferable. The aliphatic unsaturated alcohol having 5 to 10 carbon atoms may be linear or branched. Among them, being linear is preferable. The aliphatic unsaturated alcohol having 5 to 10 carbon atoms may have 1 to 3 unsaturated bonds (double bonds between carbon atoms). Among them, the number of unsaturated bonds is preferably 1. The aliphatic unsaturated alcohol having 5 to 10 carbon atoms may have 1 to 3 hydroxyl groups. Among them, the number of hydroxyl groups is preferably 1. Examples of the aliphatic unsaturated alcohol having 5 to 10 carbon atoms include cis-3-hexenol, trans-2-hexenol, cis-2-pentenol, 1-penten-3-ol, cis-2-hexenol, trans-3-hexenol, cis-4-hexenol, hexa-2,4-dienol, 1-hepten-3-ol, cis-3-heptenol, cis-4-heptenol, 6-methyl-5-hepten-2-ol, cis-2-octenol, cis-3-octenol, 1-octen-3-ol, cis-4-octenol, 1-nonen-3-ol, trans-2-nonen-4-ol, cis-3-nonenol, cis-6-nonenol, 2,6-nonadienol, 3,6-nonadienol, trans-2-decenol, cis-4-decenol, 9-decenol, citronellol, geraniol, linalool and the like. These can be blended alone or in combination of two or more. Among them, cis-3-hexenol, trans-2-hexenol and cis-2-pentenol are preferable, and cis-3-hexenol is more preferable.
[0021] In the oral composition of the present disclosure, the component (B) contains at least one selected from the group consisting of (B-1) a macrocyclic musk compound, (B-2) an aliphatic unsaturated ketone having 5 to 10 carbon atoms, and (B-3) an aliphatic unsaturated alcohol having 5 to 10 carbon atoms, and more preferably includes a combination of two or more. For example, it may contain (B-1) a macrocyclic musk compound and (B-2) an aliphatic unsaturated ketone having 5 to 10 carbon atoms, it may contain (B-1) a macrocyclic musk compound and (B-3) an aliphatic unsaturated alcohol having 5 to 10 carbon atoms, it may contain (B-2) an aliphatic unsaturated ketone having 5 to 10 carbon atoms and (B-3) an aliphatic unsaturated alcohol having 5 to 10 carbon atoms, or it may contain (B-1) a macrocyclic musk compound, (B-2) an aliphatic unsaturated ketone having 5 to 10 carbon atoms, and (B-3) an aliphatic unsaturated alcohol having 5 to 10 carbon atoms.
[0022] When the oral composition of the present disclosure contains (B-1) a macrocyclic musk compound, in the oral composition of the present disclosure, the content of (A) lauryl pyridinium chloride is preferably about 100 to 200,000 parts by mass with respect to 1 part by mass of the (B-1) macrocyclic musk compound. The upper or lower limit of this range may be, for example, about 200, 300, 400, 500, 600, 700, 800, 900, 1000, 2000, 3000, 4000, 5000, 6000, 7000, 8000, 9000, 10000, 11000, 12000, 13000, 14000, 15000, 16000, 17000, 18000, 19000, 20000, 25000, 30000, 35000, 40000, 45000, 50000, 55000, 60000, 65000, 70000, 75000, 80000, 85000, 90000, 95000, 100000, or 150000 parts by mass. More specifically, it may be about 200 to 150,000 parts by mass. When the oral composition of the present disclosure contains (B-2) an aliphatic unsaturated ketone having 5 to 10 carbon atoms, in the oral composition of the present disclosure, the content of (A) laurylpyridinium chloride is preferably about 3 to 5000 parts by mass with respect to 1 part by mass of the aliphatic unsaturated ketone having 5 to 10 carbon atoms. The upper or lower limit of the range may be, for example, about 4, 5, 6, 7, 8, 9, 10, 20, 30, 40, 50, 60, 70, 80, 90, 100, 150, 200, 250, 300, 350, 400, 450, 500, 550, 600, 650, 700, 750, 800, 850, 900, 950, 1000, 1100, 1200, 1300, 1400, 1500, 2000, 2500, 3000, 3500, 4000, or 4500 parts by mass. More specifically, it may be about 4 to 4500 parts by mass. When the oral composition of the present disclosure contains (B-3) an aliphatic unsaturated alcohol having 5 to 10 carbon atoms, in the oral composition of the present disclosure, the content of (A) laurylpyridinium chloride is preferably about 3 to 5000 parts by mass with respect to 1 part by mass of the aliphatic unsaturated alcohol having 5 to 10 carbon atoms. The upper or lower limit of the range may be, for example, about 4, 5, 6, 7, 8, 9, 10, 20, 30, 40, 50, 60, 70, 80, 90, 100, 150, 200, 250, 300, 350, 400, 450, 500, 550, 600, 650, 700, 750, 800, 850, 900, 950, 1000, 1100, 1200, 1300, 1400, 1500, 2000, 2500, 3000, 3500, 4000, or 4500 parts by mass. More specifically, it may be about 3 to 4500 parts by mass. When the oral composition of the present disclosure contains two or more selected from the group consisting of (B-1) a macrocyclic musk compound, (B-2) an aliphatic unsaturated ketone having 5 to 10 carbon atoms, and (B-3) an aliphatic unsaturated alcohol having 5 to 10 carbon atoms, the content of (A) laurylpyridinium chloride with respect to 1 part by mass of (B-1) the macrocyclic musk compound, (B-2) the aliphatic unsaturated ketone having 5 to 10 carbon atoms, or (B-3) the aliphatic unsaturated alcohol having 5 to 10 carbon atoms in the oral composition of the present disclosure is preferably within the above range respectively. For example, in the oral composition of the present disclosure, the content of (A) laurylpyridinium chloride may be about 3 to 200,000 parts by mass with respect to 1 part by mass of the component (B). The upper or lower limit of the range may be, for example, about 4, 5, 6, 7, 8, 9, 10, 20, 30, 40, 50, 60, 70, 80, 90, 100, 150, 200, 300, 400, 500, 600, 700, 800, 900, 1000, 2000, 3000, 4000, 5000, 6000, 7000, 8000, 9000, 10,000, 11,000, 12,000, 13,000, 14,000, 15,000, 16,000, 17,000, 18,000, 19,000, 20,000, 25,000, 30,000, 35,000, 40,000, 45,000, 50,000, 55,000, 60,000, 65,000, 70,000, 75,000, 80,000, 85,000, 90,000, 95,000, 100,000, or 150,000 parts by mass. More specifically, it may be about 4 to 150,000 parts by mass.
[0023] In the oral composition of the present disclosure, it is preferable that (A) laurylpyridinium chloride is contained in an amount of about 0.01 to 0.5% by mass. The upper or lower limit of the range may be, for example, about 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14, 0.15, 0.2, 0.25, 0.3, 0.35, 0.4, or 0.45% by mass. More specifically, it may be about 0.02 to 0.45% by mass.
[0024] When the oral composition of the present disclosure contains (B-1) a macrocyclic musk compound, in the oral composition of the present disclosure, (B-1) the macrocyclic musk compound is preferably contained in an amount of about 0.0000001 to 0.001% by mass. The upper or lower limit of the range may be, for example, about 0.0000002, 0.0000003, 0.0000004, 0.0000005, 0.0000006, 0.0000007, 0.0000008, 0.0000009, 0.000001, 0.000002, 0.000003, 0.000004, 0.000005, 0.000006, 0.000007, 0.000008, 0.000009, 0.00001, 0.00002, 0.00003, 0.00004, 0.00005, 0.00006, 0.00007, 0.00008, 0.00009, 0.0001, 0.0002, 0.0003, 0.0004, 0.0005, 0.0006, 0.0007, 0.0008, or 0.0009% by mass. More specifically, it may be about 0.0000002 to 0.0009% by mass. When the oral composition of the present disclosure contains (B-2) an aliphatic unsaturated ketone having 5 to 10 carbon atoms, in the oral composition of the present disclosure, (B-2) the aliphatic unsaturated ketone having 5 to 10 carbon atoms is preferably contained in an amount of about 0.000002 to 0.01% by mass. The upper or lower limit of the range may be, for example, about 0.00001, 0.00002, 0.00003, 0.00004, 0.00005, 0.00006, 0.00007, 0.00008, 0.00009, 0.0001, 0.0002, 0.0003, 0.0004, 0.0005, 0.0006, 0.0007, 0.0008, 0.0009, 0.001, 0.002, 0.003, 0.004, 0.005, 0.006, 0.007, 0.008, or 0.009% by mass. More specifically, it may be about 0.00001 to 0.009% by mass. When the oral composition of the present disclosure contains (B-3) an aliphatic unsaturated alcohol having 5 to 10 carbon atoms, in the oral composition of the present disclosure, the content of (B-3) the aliphatic unsaturated alcohol having 5 to 10 carbon atoms is preferably about 0.000002 to 0.01% by mass. The upper limit or the lower limit of the said range may be, for example, about 0.00001, 0.00002, 0.00003, 0.00004, 0.00005, 0.00006, 0.00007, 0.00008, 0.00009, 0.0001, 0.0002, 0.0003, 0.0004, 0.0005, 0.0006, 0.0007, 0.0008, 0.0009, 0.001, 0.002, 0.003, 0.004, 0.005, 0.006, 0.007, 0.008, or 0.009% by mass. More specifically, it may be about 0.00001 to 0.009% by mass. When the oral composition of the present disclosure contains two or more selected from the group consisting of (B-1) a macrocyclic musk compound, (B-2) an aliphatic unsaturated ketone having 5 to 10 carbon atoms, and (B-3) an aliphatic unsaturated alcohol having 5 to 10 carbon atoms, the content of (B-1) the macrocyclic musk compound, (B-2) the aliphatic unsaturated ketone having 5 to 10 carbon atoms, or (B-3) the aliphatic unsaturated alcohol having 5 to 10 carbon atoms in the oral composition of the present disclosure is preferably within the above range, respectively. For example, in the oral composition of the present disclosure, the total amount of component (B) may be about 0.0000001 to 0.01% by mass. The upper or lower limit of this range may be, for example, 0.0000002, 0.0000003, 0.0000004, 0.0000005, 0.0000006, 0.0000007, 0.0000008, 0.0000009, 0.000001, 0.000002, 0.000003, 0.000004, 0.000005, 0.000006, 0.000007, 0.000008, 0.000009, 0.00001, 0.00002, 0.00003, 0.00004, 0.00005, 0.00006, 0.00007, 0.00008, 0.00009, 0.0001, 0.0002, 0.0003, 0.0004, 0.0005, 0.0006, 0.0007, 0.0008, or about 0.0009% by mass. More specifically, it may be about 0.0000002 to 0.009% by mass.
[0025] The oral composition of the present disclosure may contain (C) an alkali metal acetate. In the present specification, the component (C) may be referred to as “component (C)” or the like. Examples of the (C) alkali metal acetate include sodium acetate, potassium acetate, etc. The alkali metal acetate can be blended alone or in combination of two or more. Among them, sodium acetate is preferred.
[0026] When the oral composition of the present disclosure contains (C) an alkali metal acetate, in the oral composition of the present disclosure, the content of (A) laurylpyridinium chloride is preferably about 0.03 to 5 parts by mass with respect to 1 part by mass of the (C) alkali metal acetate. The upper or lower limit of the range may be, for example, about 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14, 0.15, 0.16, 0.17, 0.18, 0.19, 0.2, 0.25, 0.3, 0.35, 0.4, 0.45, 0.5, 0.55, 0.6, 0.65, 0.7, 0.75, 0.8, 0.85, 0.9, 0.95, 1, 1.5, 2, 2.5, 3, or 4 parts by mass. More specifically, it may be about 0.04 to 4 parts by mass.
[0027] In the oral composition of the present disclosure, the (C) alkali metal acetate is preferably contained in an amount of about 0.005 to 1.0% by mass. The upper or lower limit of the range may be, for example, about 0.01, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.11, 0.12, 0.13, 0.14, 0.15, 0.2, 0.25, 0.3, 0.35, 0.4, 0.45, 0.5, 0.6, 0.7, 0.8, or 0.9% by mass. More specifically, it may be about 0.01 to 0.9% by mass, or may be about 0.05 to 0.5% by mass.
[0028] The oral composition of the present disclosure can further suppress irritation and astringency by blending (C) sodium acetate.
[0029] The composition of the present disclosure can be, for example, a solid composition, a liquid composition, etc. Among them, a liquid composition is preferable.
[0030] In addition, the oral composition of the present disclosure can also be used, for example, as a pharmaceutical, quasi-drug, or cosmetic. The form of the oral composition of the present disclosure is not particularly limited, but can be, for example, in the form (dosage form) of an ointment, paste, pasta, gel, liquid, spray, mouthwash, liquid dentifrice, toothpaste, coating agent, etc.
[0031] The oral composition of the present disclosure contains (A) laurylpyridinium chloride, (B) at least one selected from the group consisting of (B-1) macrocyclic musk compounds, (B-2) aliphatic unsaturated ketones having 5 to 10 carbon atoms, and (B-3) aliphatic unsaturated alcohols having 5 to 10 carbon atoms, and (C) an alkali metal acetate. In addition, optional components that can be formulated in the oral composition may be further formulated singly or in combination of two or more, as long as the effects of the present invention are not impaired. Examples of the optional components include surfactants, fragrances, sweeteners, binders, wetting agents, preservatives, colorants, pH adjusters, medicinal components, bases, abrasives, stabilizers, and the like.
[0032] As the surfactant, for example, a nonionic surfactant, an anionic surfactant, or an amphoteric surfactant can be blended. Specifically, examples of the nonionic surfactant include sugar fatty acid esters such as sucrose fatty acid ester, maltose fatty acid ester, lactose fatty acid ester; fatty acid alkanolamides; glycerin fatty acid esters; sorbitan fatty acid esters; fatty acid monoglycerides; polyoxyethylene alkyl ethers with a polyoxyethylene addition coefficient of 8 to 10 and an alkyl group having 13 to 15 carbon atoms; polyoxyethylene alkyl phenyl ethers with a polyoxyethylene addition coefficient of 10 to 18 and an alkyl group having 9 carbon atoms; diethyl sebacate; polyoxyethylene hydrogenated castor oil; fatty acid polyoxyethylene sorbitan, alkyl glucosides having 8 to 16 carbon atoms in the alkyl group, and the like. Examples of the anionic surfactant include sulfate esters such as sodium lauryl sulfate, sodium polyoxyethylene lauryl ether sulfate; sulfosuccinates such as sodium lauryl sulfosuccinate, sodium polyoxyethylene lauryl ether sulfosuccinate; acyl amino acid salts such as sodium cocoyl sarcosinate, sodium lauroyl methyl alaninate; sodium cocoyl methyl taurine, and the like. Examples of the amphoteric ion surfactant include betaine type surfactants such as lauryldimethylaminoacetic acid betaine, coconut oil fatty acid amidopropyldimethylaminoacetic acid betaine; imidazoline type surfactants such as N-cocoyl-N-carboxymethyl-N-hydroxyethyl ethylenediamine sodium; amino acid type surfactants such as N-lauryl diaminoethyl glycine, and the like. Further, coconut oil fatty acid monoethanolamide, coconut oil fatty acid diethanolamide, coconut oil fatty acid amide betaine, coconut oil fatty acid amidopropyl betaine, and N-coconut oil fatty acid acyl-L-arginine ethyl dl-pyrrolidone carboxylate are also preferably exemplified. These surfactants can be blended alone or in combination of two or more. The blending amount is usually about 0.1 to 5% by mass based on the total amount of the composition.
[0033] As the fragrance, for example, menthol, carboxylic acid, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate, citronellyl acetate, methyl eugenol, cineole, 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, star anise oil, cinnamon oil, cinnamaldehyde, mint oil, vanillin, ethyl vanillin, maltol, ethyl maltol, lactones having 6 to 12 carbon atoms, caryophyllene, germacrene, viridiflorol, etc. can be used. These can be used alone or in combination of two or more. Also, these can be blended in an amount of, for example, about 0.001 to 1.5% by mass based on the total amount of the composition.
[0034] As the sweetener, for example, sodium saccharin, acesulfame potassium, stevioside; stevia sweeteners such as rebaudioside, sucralose, neohesperidin dihydrochalcone, perillartine, thaumatin, aspartyl phenylalanyl methyl ester, p-methoxycinnamic aldehyde, glycyrrhizin and other licorice sweeteners can be blended. These can be used alone or in combination of two or more. Also, these can be blended in an amount of, for example, about 0.001 to 1% by mass based on the total amount of the composition.
[0035] As the binder, for example, cellulose derivatives such as sodium carboxymethyl cellulose, carboxymethyl ethyl cellulose salt, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, etc., microbial-produced polymers such as xanthan gum, gellan gum, etc., natural polymers or natural rubbers such as tragacanth gum, karaya gum, gum arabic, carrageenan, dextrin, etc., synthetic polymers such as polyvinyl alcohol, polyvinyl pyrrolidone, etc., inorganic binders such as thickening silica, veegum, etc., cationic binders such as O-[2-hydroxy-3-(trimethylammonio)propyl] hydroxyethyl cellulose chloride, etc. can be used alone or in combination of two or more.
[0036] As the wetting agent, for example, sorbitol, glycerin, propylene glycol, xylitol, maltitol, lactitol, polyoxyethylene glycol, etc. can be blended alone or in combination of two or more. Further, these can be blended in an amount of, for example, about 5 to 20% by mass based on the total amount of the composition.
[0037] As the preservative, for example, parabens such as methylparaben, ethylparaben, propylparaben, butylparaben, etc., sodium benzoate, phenoxyethanol, alkyl diaminoethyl glycine hydrochloride, chlorobutanol, etc. can be blended alone or in combination of two or more.
[0038] As the colorant, for example, legal dyes such as Blue No. 1, Yellow No. 4, Red No. 202, Green No. 3, etc., mineral-based pigments such as ultramarine, reinforced ultramarine, dark blue, etc., titanium oxide, etc. can be blended alone or in combination of two or more.
[0039] As the pH adjuster, for example, 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, etc. can be blended. These can be blended alone or in combination of two or more so that the pH of the composition is in the range of, for example, 4 to 9. The blending amount of the pH adjuster is exemplified by about 0.01 to 2% by weight.
[0040] As the medicinal ingredient, a bactericide other than laurylpyridinium chloride may be blended. For example, cationic bactericides such as cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate, etc., amphoteric bactericides such as dodecyldiaminoethylglycine, nonionic bactericides such as triclosan, isopropylmethylphenol, hinokitiol, etc. may be mentioned. Furthermore, medicinal ingredients other than bactericides can also be blended. For example, vitamin E compounds such as aluminum lactate, potassium nitrate, dl-α-tocopherol acetate, succinic acid tocopherol, or tocopherol nicotinate, sodium fluoride, glycyrrhizinate, etc. may be blended. The medicinal ingredients can be blended alone or in combination of two or more kinds.
[0041] As the base, for example, alcohols, silicon, apatite, white petrolatum, paraffin, liquid paraffin, microcrystalline wax, squalane, plastic base, etc. can be blended alone or in combination of two or more kinds.
[0042] As the abrasive, for example, calcium carbonate, magnesium carbonate, dibasic calcium phosphate, tribasic calcium phosphate, magnesium phosphate, silica, zeolite, sodium metaphosphate, aluminum hydroxide, magnesium hydroxide, calcium pyrophosphate, bengala, calcium sulfate, anhydrous silicic acid, etc. can be blended alone or in combination of two or more kinds.
[0043] As the stabilizer, for example, sodium edetate, sodium thiosulfate, sodium sulfite, calcium lactate, lanolin, triacetin, castor oil, magnesium sulfate, etc. can be blended alone or in combination of two or more kinds.
[0044] In addition, the oral composition of the present disclosure may contain extracts of plants such as Japanese honewort, hops, althea, Japanese mugwort, gentiana, and Chinese corktree. Furthermore, it may contain quassin, iso-alpha acids, tujon, gentiopicroside, berberine, etc., which are these bitter components. As the above plant extracts or their bitter components, those obtained by extracting raw material plants using an appropriate extraction solvent such as water or ethanol by adopting a usual method can be used. Those commercially available as extracts, oils, extracts, etc. may also be used. Alternatively, synthetic products can also be used.
[0045] The oral composition of the present disclosure can be produced by a known method or a method easily conceived from a known method. For example, it can be prepared by appropriately mixing (A) lauryl pyridinium chloride, (B) at least one selected from the group consisting of (B-1) macrocyclic musk compounds, (B-2) aliphatic unsaturated ketones having 5 to 10 carbon atoms, and (B-3) aliphatic unsaturated alcohols having 5 to 10 carbon atoms, and (C) an alkali metal acetate and other components as required.
[0046] In this specification, “astringency” refers to a sensation perceived by a chemical response with receptors present in the oral mucosal epithelium or by friction generated by a decrease in the lubricity of the oral mucosal epithelium (Non-Patent Document 1). Note that “astringency” is a sensation of a different nature from “bitterness” perceived by a response with bitter receptors present in taste buds.
[0047] In addition, in this specification, “comprising” includes “consisting essentially of” and “consisting of” (The term “comprising” includes “consisting essentially of” and “consisting of.”). Further, the present disclosure includes all arbitrary combinations of the constituent elements described in this specification.
[0048] Moreover, for each of the embodiments of the present disclosure described above, various characteristics (properties, structures, functions, etc.) may be combined in any way when specifying the subject matter encompassed by the present disclosure. That is, the present disclosure encompasses all subject matters consisting of any combination of the combinable characteristics described in this specification.
Example
[0049] The content of the present disclosure will be specifically described using the following examples. However, the present disclosure is not limited thereto in any way. In the following, unless otherwise specified, experiments are conducted under atmospheric pressure and normal temperature conditions. Also, unless otherwise specified, "%" means "mass%". Further, the compounding amount values of each component described in each table indicate "mass%" unless otherwise specified.
[0050] <Sensory evaluation> Liquid oral compositions were prepared by a conventional method with the compounding amounts shown in Tables 1 and 2.
[0051]
Table 1
[0052]
Table 2
[0053] Four monitors were each asked to hold 10 mL of the prepared liquid oral composition in their mouths and use it for 20 seconds, and the irritation and astringency during use, as well as the irritation and astringency 1 minute after use, were evaluated according to a five-level evaluation criterion. <Evaluation criterion: Irritation, astringency> 5: Feels very strong 4: Feels strong 3: Feels 2: Barely feels 1: Doesn't feel at all
[0054] The evaluation values of the four people were tabulated and the average value was calculated. The results are shown together with Table 2. ◎: Average score less than 2.0 〇: Average score is 2.0 or more and less than 3.0 ×: Average score is 3.0 or more and less than 4.0 ××: Average score is 4.0 or more
[0055] As shown in Table 2, by blending lauryl pyridinium chloride and specific compounds (ω-pentadecalactone, muscone, ethylene brassylate, 6-methyl-5-hepten-2-one, 4-methyl-3-penten-2-one, cis-3-hexenol, trans-2-hexenol, cis-2-pentenol), it was confirmed that the irritation and astringency during use and 1 minute after use were reduced. On the other hand, when γ-undecalactone and vanillin were blended, the irritation and astringency were not suppressed.
[0056] Formulation examples are shown below.
[0057]
Table 3
[0058]
Table 4
[0059]
Table 5
[0060]
Table 6
[0061]
Table 7
[0062]
Table 8
[0063]
Table 9
[0064]
Table 10
[0065]
Table 11
Claims
1. (A) Laurylpyridinium chloride, and (B) An oral composition containing at least one selected from the group consisting of (B-1) a macrocyclic musk compound, (B-2) an aliphatic unsaturated ketone having 5 to 10 carbon atoms, and (B-3) an aliphatic unsaturated alcohol having 5 to 10 carbon atoms.
2. (B-1) is at least one selected from the group consisting of ω-pentadecalactone, muscone, and ethylene brassylate, (B-2) is at least one selected from the group consisting of 6-methyl-5-hepten-2-one and 4-methyl-3-penten-2-one, and / or (B-3) is at least one selected from the group consisting of cis-3-hexenol, trans-2-hexenol, and cis-2-pentenol. The oral composition according to claim 1.
3. In the oral composition, the content of (A) is 3 to 200,000 parts by mass with respect to 1 part by mass of (B). The oral composition according to claim 1 or 2.
4. When (B-1) is contained, in the oral composition, the content of (A) is 100 to 200,000 parts by mass with respect to 1 part by mass of (B-1), When (B-2) is contained, in the oral composition, the content of (A) is 3 to 5000 parts by mass with respect to 1 part by mass of (B-2), and / or When (B-3) is contained, in the oral composition, the content of (A) is 3 to 5000 parts by mass with respect to 1 part by mass of (B-3). The oral composition according to claim 1 or 2.
5. The oral composition according to claim 1 or 2, containing 0.01 to 0.5% by mass of (A).
6. When (B-1) is contained, in the oral composition, the content of (B-1) is 0.0000001 to 0.001% by mass, When containing (B-2), in the oral composition, the content of (B-2) is 0.000002 to 0.01% by mass, and / or The oral composition according to claim 1 or 2, when containing (B-3), wherein the content of (B-3) in the oral composition is 0.000002 to 0.01% by mass.
7. Furthermore, the oral composition according to claim 1 or 2, which contains (C) an alkali metal acetate.
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