Oral composition

Abstract

To provide an oral composition that contains sodium copper chlorophylline with good stability over time.SOLUTION: An oral composition contains sodium copper chlorophylline and at least one cationic surfactant selected from the group consisting of cetylpyridinium chloride, benzalkonium chloride, and DL-pyrrolidonecarboxylic acid salt of N-cocoyl-L-arginine ethyl ester. In the composition, the mass content ratio of the sodium copper chlorophylline and the cationic surfactant is 70: 1-1: 30. In the composition, the content of water is 5 mass% or less.SELECTED DRAWING: None

Description

Technical Field

[0001] The present disclosure relates to oral compositions and the like. More specifically, it relates to non-aqueous oral compositions and the like.

Background Art

[0002] Sodium copper chlorophyllin is a component having an effect of preventing gingivitis and bad breath. However, it is known to be hygroscopic and to deteriorate during long-term storage in a hygroscopic state, and its instability in the presence of water has been a problem in pharmaceutical development (Patent Documents 1 and 2).

Prior Art Documents

Patent Documents

[0003]

Patent Document 1

Patent Document 2

Summary of the Invention

Problems to be Solved by the Invention

[0004] An object of the present disclosure is to provide an oral composition in which sodium copper chlorophyllin has good stability over time.

Means for Solving the Problems

[0005] The present inventors considered that in order to stably incorporate sodium copper chlorophyllin into an oral composition, it is preferable that the water content in the composition is low, and conducted studies. However, it was found that even when the water content in the composition is low, sodium copper chlorophyllin decreases over time.

[0006] As a result of intensive studies, the inventors of the present invention have found that the stability over time of sodium copper chlorophyllin may be improved by using sodium copper chlorophyllin and a cationic surfactant in combination, and have further made improvements.

[0007] The present disclosure includes, for example, the subject matter described in the following items. Item 1. A composition for oral use containing sodium copper chlorophyllin and at least one cationic surfactant selected from the group consisting of cetylpyridinium chloride, benzalkonium chloride, and N-coconut oil fatty acyl-L-arginine ethyl · DL-pyrrolidone carboxylate, wherein in the composition, the mass ratio of the content of the sodium copper chlorophyllin to the content of the cationic surfactant is 70:1 to 1:30, and the water content in the composition is 5% by mass or less. A composition for oral use. Item 2. The composition for oral use according to Item 1, which is a non-aqueous composition. Item 3. The composition for oral use according to Item 1 or 2, wherein the content of the cationic surfactant in the composition is 0.001 to 0.5% by mass. Item 4. The composition for oral use according to any one of Items 1 to 3, wherein the content of the sodium copper chlorophyllin in the composition is 0.5% by mass or less.

Advantages of the Invention

[0008] A composition for oral use with good stability over time of sodium copper chlorophyllin is provided.

Modes for Carrying Out the Invention

[0009] The present disclosure includes a composition for oral use containing sodium copper chlorophyllin and a cationic surfactant. In this specification, the composition for oral use may be referred to as "the composition for oral use of the present disclosure".

[0010] Examples of the cationic surfactant used in the present disclosure include cetylpyridinium chloride, benzalkonium chloride, N-coconut fatty acid acyl-L-arginine ethyl · DL-pyrrolidone carboxylate, and the like. These can be used alone or in combination of two or more.

[0011] In the oral composition of the present disclosure, the mass ratio of sodium copper chlorophyllin and the cationic surfactant can be, for example, about 70:1 to 1:30. The upper or lower limit of this range can be, for example, about 60:1, 50:1, 40:1, 30:1, 20:1, 10:1, 5:1, 3:1, 2:1, 1:1, 1:2, 1:4, 1:6, 1:8, 1:10, 1:15, 1:20, or 1:25. Specifically, for example, it can be about 60:1 to 1:25.

[0012] In the oral composition of the present disclosure, the content of sodium copper chlorophyllin can be, for example, about 0.5% by mass or less. The upper or lower limit of this range can be, for example, about 0.001, 0.003, 0.005, 0.01, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.12, 0.14, 0.16, 0.18, 0.2, 0.22, 0.24, 0.25, 0.26, 0.27, 0.28, 0.29, 0.3, 0.35, 0.4, or 0.45% by mass. Specifically, for example, it can be about 0.001 to 0.45% by mass.

[0013] In the oral composition of the present disclosure, the content of the cationic surfactant can be, for example, about 0.001 to 0.5% by mass. The upper or lower limit of the range can be, for example, about 0.002, 0.003, 0.004, 0.005, 0.01, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, 0.12, 0.14, 0.16, 0.18, 0.2, 0.22, 0.24, 0.25, 0.26, 0.27, 0.28, 0.29, 0.3, 0.35, 0.4, or 0.45% by mass. Specifically, for example, it may be about 0.002 to 0.45% by mass. In the oral composition of the present disclosure, when two or more cationic surfactants are included, the total amount of the cationic surfactants can be within the above range.

[0014] The oral composition of the present disclosure may contain water as long as the stability of sodium copper chlorophyllin over time is not impaired. Specifically, for example, the water content is preferably about 5% by mass or less. The upper limit of the range of the water content may be about 4, 3, 2, 1, or 0.5% by mass. Further, the oral composition of the present disclosure is more preferably a composition that does not contain water (i.e., a non-aqueous composition). However, the case where an amount of water that is difficult to remove as an inevitable impurity is contained in the composition is included in the "non-aqueous composition" in this specification.

[0015] The oral composition of the present disclosure contains the above-described components and can further contain known components that can be formulated into the oral composition. Examples of such known components include hydrocarbon oils, polyhydric alcohols, surfactants other than cationic surfactants, abrasives, wetting agents, foaming agents, fragrances, activators, sweeteners, preservatives, colorants, pH adjusters, stabilizers, flavoring agents, astringents, thickeners, other medicinal agents, and the like. Such known components can be used alone or in combination of two or more.

[0016] Examples of hydrocarbon oils include paraffin, squalane, microcrystalline wax, petrolatum, ceresin, limonene, turpentine oil, etc. Among them, squalane and paraffin are preferred, and paraffin is more preferred. As squalane, either animal squalane or vegetable squalane can be used, and for example, shark squalane, olive squalane, etc. can be preferably used. As paraffin, liquid paraffin is preferred, and light liquid paraffin is more preferred. In this specification, light liquid paraffin refers to those having a specific gravity of 0.830 to 0.870 and a viscosity of less than 37 mm 2 / s. The viscosity is calculated by the capillary viscometer method according to the description in the 17th revised Japanese Pharmacopoeia. The kinematic viscosity of light liquid paraffin can be, for example, less than about 45 mm 2 / s. The hydrocarbon oil can be used alone or in combination of two or more.

[0017] Examples of polyhydric alcohols include glycerin, propanediol, butylene glycol, polyethylene glycol, etc. As propanediol, either propylene glycol (1,2-propanediol) or 1,3-propanediol can be preferably used. As butylene glycol, 1,3-butylene glycol is preferred. As polyethylene glycol, the average number of added moles of ethylene oxide units (EO) is preferably 4 to 20 (4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20). Among them, as the polyhydric alcohol, glycerin is preferred. The polyhydric alcohol can be used alone or in combination of two or more.

[0018] Examples of surfactants include nonionic surfactants, anionic surfactants, zwitterionic surfactants, etc. Among them, nonionic surfactants are preferred. The surfactant can be used alone or in combination of two or more.

[0019] Examples of nonionic surfactants include, for example, sugar fatty acid esters such as sucrose fatty acid ester and maltose fatty acid ester; sugar alcohol fatty acid esters such as maltitol fatty acid ester; sorbitan fatty acid esters such as sorbitan monolaurate; polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan monolaurate and polyoxyethylene sorbitan monostearate; fatty acid alkanolamides such as lauric acid diethanolamide; polyoxyethylene alkyl ethers such as polyoxyethylene stearyl ether and polyoxyethylene oleyl ether; polyethylene glycol fatty acid esters such as polyethylene glycol monooleate and polyethylene glycol monolaurate; alkyl glucosides such as lauryl glucoside and decyl glucoside; polyglycerol fatty acid esters, polyoxyethylene glycerol fatty acid esters, polyoxyethylene fatty acid esters, alkyl glucosides, polyoxyethylene hydrogenated castor oil (POE hydrogenated castor oil), polyoxyethylene hydrogenated castor oil fatty acid ester, glycerol fatty acid ester, polyoxyethylene propylene block copolymer, etc. Among them, polyglycerol fatty acid esters, alkyl glucosides, polyoxyethylene hydrogenated castor oil, polyoxyethylene hydrogenated castor oil fatty acid ester, and polyoxyethylene alkyl ether are preferred, and polyglycerol fatty acid esters are more preferred.

[0020] Examples of polyglycerol fatty acid esters include esters of saturated or unsaturated fatty acids having 8 to 24 carbon atoms and polyglycerol. The upper or lower limit of the number of carbon atoms may be, for example, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, or 23. More specifically, for example, it may be 9 to 23. The fatty acid may be a saturated fatty acid or an unsaturated fatty acid. Further, the fatty acid may be a linear fatty acid or a branched fatty acid. Examples of the fatty acid include capric acid, lauric acid, myristic acid, stearic acid, palmitic acid, palmitoleic acid, margaric acid, oleic acid, linoleic acid, behenic acid, isocapric acid, isolauric acid, isomyristic acid, isostearic acid, isopalmitic acid, isopalmitoleic acid, isomargaric acid, isooletic acid, isolinoleic acid, isobehenic acid, etc. Among them, capric acid, lauric acid, myristic acid, stearic acid, oleic acid, and isostearic acid are preferable. Also, natural fatty acids such as coconut oil fatty acid and palm oil fatty acid containing these fatty acids may be used. Further, the polyglycerol fatty acid ester is preferably a mono, di, tri, tetra, penta, or cycloester compound of the fatty acid and polyglycerol, and more preferably a mono, di, or triester compound. Polyglycerol preferably contains an average of 4 to 12 glycerol units. The upper or lower limit of the glycerol units may be, for example, 5, 6, 7, 8, 9, 10, or 11. More specifically, for example, it may be 5 to 11. Examples of the preferable polyglycerol fatty acid ester include polyglyceryl-n caprate, polyglyceryl-n laurate, polyglyceryl-n myristate, polyglyceryl-n stearate, polyglyceryl-n oleate, polyglyceryl-n dimyristate, polyglyceryl-n distearate, polyglyceryl-n diisostearate, polyglyceryl-n trilaurate, polyglyceryl-n trimyristate (n represents the number of glycerol units), etc. More preferably, it is polyglyceryl-n myristate.

[0021] The form of the oral composition of the present disclosure is not particularly limited, and for example, it can be in the form (dosage form) of an ointment, paste, pasta, gel, liquid, spray, mouthwash, liquid dentifrice, toothpaste, coating agent, etc. The oral composition of the present disclosure can be used, for example, as pharmaceuticals and quasi-drugs. Further, the oral composition of the present disclosure can be used, for example, as a carrier for oral compositions.

[0022] The oral composition of the present disclosure can be prepared by a conventional method by combining sodium copper chlorophyllin and a cationic surfactant, and optionally other components.

[0023] As shown in the examples described later, the stability over time can be evaluated by confirming the change over time in the amount of sodium copper chlorophyllin by absorbance (405 nm). For example, in the oral composition of the present disclosure, the ratio (%) of the absorbance of the product stored at 55°C for 3 weeks to the absorbance of the product stored at 5°C for 3 weeks is preferably about 90% or more. The lower limit of this range may be, for example, about 91, 92, 93, 94, or 95%.

[0024] 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.

[0025] Also, regarding the various characteristics (properties, structures, functions, etc.) described for each of the above-described embodiments of the present disclosure, they may be combined in any manner when specifying the subject matter included in the present disclosure. That is, the present disclosure includes all subject matters consisting of any combination of the combinable characteristics described in this specification.

Examples

[0026] The content of the present disclosure will be specifically described using the following examples and the like. However, the present disclosure is not limited thereto in any way. In the following, unless otherwise specified, the experiments are conducted under atmospheric pressure and normal temperature conditions. Also, unless otherwise specified, "%" means "% by mass". Further, the compounding amount values of each component described in each table indicate "% by mass" unless otherwise specified.

[0027] Preparation of Composition According to the formulation shown in Table 1 below, the composition was prepared and filled into toothpaste tubes at 40 g each, and left at 5°C and in an environment of 55°C as the accelerated condition for 1 or 3 weeks. In the serum described in Table 1, the content of each component was 35% by mass of glycerin, 5% by mass of polyglyceryl-10 myristate, and 60% by mass of light liquid paraffin. The light liquid paraffin had a kinematic viscosity of 12.56 mm 2 / s (40°C) and a density (specific gravity) of 0.843. The viscosity of the light liquid paraffin calculated from the kinematic viscosity and density was 10.59 mm 2 / s.

[0028]

Table 1

[0029] Preparation of Sample for Ultraviolet-Visible Absorbance Measurement For the samples left at 5°C and 55°C of Examples 1 to 4 and 7, measurement samples were prepared according to the following procedure. 30 mL of an isopropanol / methanol (9:1) mixed solution was added to 1 g of the sample and shaken strongly for 30 minutes. The isopropanol / methanol (9:1) mixed solution was added to the solution after shaking to make the total volume 100 mL, which was used as the measurement sample. For the samples left at 5°C and 55°C of Examples 5, 6 and 8, Comparative Examples 1 and 2, measurement samples were prepared according to the following procedure. 10 mL of an isopropanol / methanol (9:1) mixed solution was added to 2 g of the sample and shaken strongly for 30 minutes. The isopropanol / methanol (9:1) mixed solution was added to the solution after shaking to make the total volume 25 mL, which was used as the measurement sample.

[0030] Ultraviolet-Visible Absorbance Measurement Using an isopropanol / methanol (9:1) mixture as a control solution, the absorbance (405 nm) was measured. The ratios (%) of the absorbance of the samples stored at 55°C for one week to the absorbance of the samples stored at 5°C for one week, and the ratios (%) of the absorbance of the samples stored at 55°C for three weeks to the absorbance of the samples stored at 5°C for three weeks were calculated to evaluate the stability of sodium copper chlorophyllin. The results are shown in Table 1.

[0031] As shown in Table 1, in Examples 1 to 8, the ratios of the absorbance of the samples stored at 55°C to the absorbance of the samples stored at 5°C were 90% or more at both the first week and the third week, indicating that the stability of sodium copper chlorophyllin over time was good.

[0032] Preparation of Composition According to the formulation shown in Table 2 below, a composition was prepared, and the stability of sodium copper chlorophyllin was evaluated in the same manner as in Example 5 and the like. In the serum described in Table 2, the content of each component was 35% by mass of glycerin, 5% by mass of polyglyceryl-10 myristate, and 60% by mass of light liquid paraffin. The results are shown in Table 2.

[0033]

Table 2

[0034] As shown in Table 2, when cetylpyridinium chloride was replaced with benzalkonium chloride or N-cocoyl-L-arginine ethyl·DL-pyrrolidone carboxylate (Examples 9 and 10), the ratios of the absorbance of the samples stored at 55°C to the absorbance of the samples stored at 5°C were 90% or more at both the first week and the third week, indicating that the stability of sodium copper chlorophyllin over time was good.

Claims

1. A dental composition containing sodium copper chlorophyllin and a cationic surfactant, wherein the cationic surfactant is at least one selected from the group consisting of cetylpyridinium chloride, benzalkonium chloride, and N-coconut oil fatty acyl-L-arginine ethyl DL-pyrrolidone carboxylate, in the composition, the mass ratio of the sodium copper chlorophyllin to the cationic surfactant is 70:1 to 1:30, in the composition, the water content is 5% by mass or less, and the form is an ointment, paste, pasta, gel, liquid, spray, mouthwash, liquid dentifrice, dentifrice, or coating agent, a dental composition.

2. The dental composition according to claim 1, comprising a hydrocarbon oil, a polyhydric alcohol, and a nonionic surfactant.

3. The dental composition according to claim 1 or 2, which is a non-aqueous composition.

4. In the composition, the content of the cationic surfactant is 0.001 to 0.5% by mass, the dental composition according to any one of claims 1 to 3.

5. In the composition, the content of the sodium copper chlorophyllin is 0.5% by mass or less, the dental composition according to any one of claims 1 to 4.

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