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 a cationic surfactant. 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 halitosis. 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 formulation 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 the stability of sodium copper chlorophyllin over time is good.

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 diligent research, the inventors discovered that the long-term stability of sodium copper chlorophyllin can be improved by using it in combination with a cationic surfactant, and further improvements were made.

[0007] This disclosure includes, for example, the following subjects: Section 1. This is an oral composition containing copper chlorophyllin sodium and a cationic surfactant. In the composition, the mass ratio of the copper chlorophyllin sodium and the cationic surfactant is 70:1 to 1:30. An oral composition wherein the water content in the composition is 5% by mass or less. Section 2. The oral composition described in item 1, which is a non-aqueous composition. Section 3. The oral composition according to claim 1 or 2, wherein the content of the cationic surfactant in the composition is 0.001 to 0.5% by mass. Section 4. The oral composition according to any one of claims 1 to 3, wherein the content of copper chlorophyllin sodium in the composition is 0.5% by mass or less. Section 5. The oral composition according to any one of claims 1 to 4, wherein the cationic surfactant is a quaternary ammonium salt type cationic surfactant and / or an amino acid-based cationic surfactant. [Effects of the Invention]

[0008] An oral composition is provided in which copper chlorophyllin sodium exhibits good long-term stability. [Modes for carrying out the invention]

[0009] This disclosure encompasses oral compositions containing copper chlorophyllin sodium and a cationic surfactant. In this specification, such oral compositions may be referred to as "the oral compositions of this disclosure."

[0010] Examples of cationic surfactants used in this disclosure include quaternary ammonium salt type cationic surfactants and amino acid-based cationic surfactants. Cationic surfactants can be used individually or in combination of two or more types.

[0011] Examples of quaternary ammonium salts that constitute quaternary ammonium salt-type cationic surfactants include alkylpyridinium salts, benzethonium salts, benzalkonium salts, monoalkyltrimethylammonium salts, and dialkyldimethylammonium salts. Examples of salts include chloride salts and bromide salts. Examples of alkyl groups in alkylpyridinium salts, monoalkyltrimethylammonium salts, or dialkyldimethylammonium salts include alkyl groups having 8 to 22 carbon atoms. 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, or 21. More specifically, for example, it may be 9 to 21. Examples of quaternary ammonium salt type cationic surfactants include cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, stearyltrimethylammonium chloride, cetyltrimethylammonium chloride, stearyltrimethylammonium chloride, behenyltrimethylammonium chloride, distearyldimethylammonium chloride, laurylbenzyldimethylammonium chloride, hexadecyltrimethylammonium bromide, and stearyltrimethylammonium bromide. Among these, cetylpyridinium chloride, benzalkonium chloride, and benzethonium chloride are preferred.

[0012] Examples of amino acid-based cationic surfactants include mono-N-long-chain acyl basic amino acid lower alkyl ester salts. Examples of basic amino acids that constitute amino acid-based cationic surfactants include natural amino acids such as ornithine, lysine, and arginine. Synthetic amino acids such as α,γ-diaminobutyric acid can also be used. These may be optically active or racemic. The acyl group of the mono-N-long-chain acyl basic amino acid lower alkyl ester salt is preferably a saturated or unsaturated higher fatty acid residue having 8 to 22 carbon atoms. The upper or lower limit of the carbon number may be, for example, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, or 21. More specifically, it may be 9 to 21. Examples include single higher fatty acid residues such as lauroyl, myristoyl, palmitoyl, and stearoyl groups; and natural mixed higher fatty acid residues such as coconut oil fatty acid residues and beef tallow higher fatty acid residues. Examples of lower alkyl esters include alkyl esters having 1 to 8 carbon atoms. Specifically, these include methyl esters, ethyl esters, propyl esters, butyl esters, pentyl esters, hexyl esters, heptyl esters, octyl esters, and the like. Lower alkyl esters are preferably in salt form, and examples include inorganic salts such as hydrochloride, bromate, sulfate, and phosphate; and organic salts such as glycolate, acetate, lactate, succinate, tartrate, citrate, acidic amino acid salts, higher fatty acid salts, L- or DL-pyrrolidone carboxylate salts, pyroglutamate, and p-toluenesulfonate. Among these, hydrochloride, L- or DL-pyrrolidone carboxylate salts, and acidic amino acid salts are preferred. Examples of amino acid-based cationic surfactants include N-coconut oil fatty acid acyl-L-arginine ethyl DL-pyrrolidone carboxylate.

[0013] In the oral compositions of this disclosure, the mass ratio of sodium copper chlorophyllin to cationic surfactant can be, for example, about 70:1 to 1:30. The upper or lower limits of this range may 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 may be about 60:1 to 1:25.

[0014] 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 may be about 0.001 to 0.45% by mass.

[0015] 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 this 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 contained, the total amount of the cationic surfactants can be within the above range.

[0016] 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, in the case where an amount of water that is difficult to remove as inevitable impurities is contained in the composition, it is included in the "non-aqueous composition" in this specification.

[0017] The oral composition of the present disclosure contains the above-described components and may further contain known components that can be incorporated into the oral composition. Examples of such known components include hydrocarbon oils, polyhydric alcohols, surfactants other than cationic surfactants, abrasives, humectants, 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.

[0018] Examples of hydrocarbon oils include paraffin, squalane, microcrystalline wax, petrolatum, ceresin, limonene, turpentine oil, and the like. 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. Hydrocarbon oils can be used alone or in combination of two or more.

[0019] Examples of polyhydric alcohols include glycerin, propanediol, butylene glycol, polyethylene glycol, and the like. 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. Preferably, the polyethylene glycol has an average number of added moles of ethylene oxide units (EO) of 4 to 20 (4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20). Among the polyhydric alcohols, glycerin is preferred. Polyhydric alcohols can be used individually or in combination of two or more.

[0020] Examples of surfactants include nonionic surfactants, anionic surfactants, and amphoteric surfactants. Among these, nonionic surfactants are preferred. Surfactants can be used individually or in combination of two or more.

[0021] 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; 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; polyglycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, polyoxyethylene fatty acid esters, alkyl glucosides, polyoxyethylene hydrogenated castor oil (POE hydrogenated castor oil), polyoxyethylene hydrogenated castor oil fatty acid esters, glycerin fatty acid esters, and polyoxyethylene propylene block copolymers. Among these, polyglycerin fatty acid esters, alkyl glucosides, polyoxyethylene hydrogenated castor oil, polyoxyethylene hydrogenated castor oil fatty acid esters, and polyoxyethylene alkyl ethers are preferred, with polyglycerin fatty acid esters being more preferred.

[0022] Examples of polyglycerol fatty acid esters include esters of polyglycerol with saturated or unsaturated fatty acids having 8 to 24 carbon atoms. The upper or lower limit of the carbon number 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 saturated or unsaturated. Furthermore, the fatty acid may be straight-chain or branched-chain. Examples of such fatty acids 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, isomarugaric acid, isoleic acid, isolinoleic acid, and isobéhenic acid. Among these, capric acid, lauric acid, myristic acid, stearic acid, oleic acid, and isostearic acid are preferred. Natural fatty acids, such as coconut oil fatty acids and palm oil fatty acids, containing these fatty acids, may also be used. Furthermore, the polyglycerin fatty acid ester is preferably a mono, di, tri, tetra, penta, or cycloester compound of the fatty acid and polyglycerin, and more preferably a mono, di, or triester compound. The polyglycerin preferably contains an average of 4 to 12 glycerin units. The upper or lower limit of glycerin units may be, for example, 5, 6, 7, 8, 9, 10, or 11. More specifically, it may be, for example, 5 to 11. Preferred polyglycerin fatty acid esters include, for example, 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, and polyglyceryl-n trimiristate (where n represents the number of glycerin units). More preferably, polyglyceryl-n myristate is used.

[0023] The form of the oral composition disclosed herein is not particularly limited, but can be in the form (dosage form) of, for example, an ointment, paste, paste, gel, liquid, spray, mouthwash, liquid toothpaste, toothpaste, or topical application. The oral compositions disclosed herein can be used, for example, as pharmaceuticals or quasi-drugs. Furthermore, the oral compositions disclosed herein can also be used, for example, as carriers for oral compositions.

[0024] The oral compositions of this disclosure can be prepared by conventional methods by combining sodium copper chlorophyllin, a cationic surfactant, and other components as needed.

[0025] The stability over time can be evaluated by observing the change in the amount of copper chlorophyllin sodium over time using absorbance (405 nm), as shown in the examples described later. For example, the oral composition of this disclosure preferably has an absorbance ratio (%) of 90% or more between the absorbance of a sample left at 55°C for 3 weeks and the absorbance of a sample left at 5°C for 3 weeks. The lower limit of this range may be, for example, 91%, 92%, 93%, 94%, or 95%.

[0026] In this specification, the term "comprising" includes both "consisting essentially of" and "consisting of." Furthermore, this disclosure encompasses all any combination of the constituent elements described herein.

[0027] Furthermore, the various characteristics (properties, structure, function, etc.) described in each embodiment of this disclosure above may be combined in any way to identify the subject matter covered by this disclosure. In other words, this disclosure covers all subject matter consisting of any combination of the combinable characteristics described herein. [Examples]

[0028] The contents of this disclosure will be specifically explained using the following examples. However, this disclosure is not limited in any way to these examples. Unless otherwise specified below, experiments were conducted under atmospheric pressure and room temperature conditions. Unless otherwise specified, "%" means "mass%". Also, unless otherwise specified, the blending amounts of each component listed in each table are also in "mass%".

[0029] Composition preparation The compositions were prepared according to the formulations shown in Table 1 below, filled into toothpaste tubes in 40g portions, and left for 1 or 3 weeks at 5°C and 55°C as an accelerated condition. The content of each component in the serums listed in Table 1 was 35% by mass of glycerin, 5% by mass of polyglyceryl-10 myristate, and 60% by mass of light liquid paraffin. The kinematic viscosity of the light liquid paraffin was 12.56 mm². 2 A sample with a kinematic viscosity of / s (40℃) and a density (specific gravity) of 0.843 was used. The viscosity of the light liquid paraffin calculated from this kinematic viscosity and density was 10.59 mm². 2 It was / s.

[0030] [Table 1]

[0031] Preparation of samples for UV-Vis absorbance measurement For Examples 1-4 and 7 (5°C, 55°C), samples for measurement were prepared according to the following procedure. 30 mL of isopropanol / methanol (9:1) mixture was added to 1 g of the sample and shaken vigorously for 30 minutes. After shaking, isopropanol / methanol (9:1) mixture was added to the solution to make a total volume of 100 mL, which was used as the sample for measurement. For the samples left standing at Examples 5, 6, and 8, and Comparative Examples 1 and 2 (5°C, 55°C), the samples for measurement were prepared according to the following procedure. 10 mL of isopropanol / methanol (9:1) mixture was added to 2 g of the sample and shaken vigorously for 30 minutes. After shaking, isopropanol / methanol (9:1) mixture was added to the solution to make a total volume of 25 mL, which was used as the sample for measurement.

[0032] UV-visible absorbance measurement An isopropanol / methanol (9:1) mixture was used as a control solution, and the absorbance (405 nm) was measured. The ratio (%) of the absorbance of the sample left at 55°C for one week to the absorbance of the sample left at 5°C for one week, and the ratio (%) of the absorbance of the sample left at 55°C for three weeks to the absorbance of the sample left at 5°C for three weeks, were calculated to evaluate the stability of copper chlorophyllin sodium. The results are shown in Table 1.

[0033] As shown in Table 1, in Examples 1 to 8, the ratio of the absorbance of the sample left at 55°C to the absorbance of the sample left at 5°C was 90% or more at both the first and third weeks, indicating that copper chlorophyllin sodium has good long-term stability.

[0034] Composition preparation Compositions were prepared according to the formulations shown in Table 2 below, and the stability of sodium copper chlorophyllin was evaluated in the same manner as in Example 5, etc. The content of each component in the serums listed in Table 2 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.

[0035] [Table 2]

[0036] As shown in Table 2, when benzalkonium chloride or N-coconut oil fatty acid acyl-L-arginine ethyl / DL-pyrrolidone carboxylate was used instead of cetylpyridinium chloride (Examples 9 and 10), the ratio of the absorbance of the sample left at 55°C to the absorbance of the sample left at 5°C was 90% or more at both the first and third weeks, indicating that copper chlorophyllin sodium exhibits good long-term stability.

Claims

1. An oral composition comprising sodium copper chlorophyllin and a cationic surfactant, In the composition, the content mass ratio of the copper chlorophyllin sodium to the cationic surfactant is 70:1 to 1:30, An oral composition, wherein the water content in the composition is 5% by mass or less.

2. The oral composition of claim 1 , which is a non-aqueous composition.

3. 3. The oral composition according to claim 1, wherein the content of the cationic surfactant in the composition is 0.001 to 0.5% by mass.

4. The oral composition according to any one of claims 1 to 3, wherein the content of the copper chlorophyllin sodium in the composition is 0.5 mass% or less.

5. The oral composition according to any one of claims 1 to 4, wherein the cationic surfactant is a quaternary ammonium salt-type cationic surfactant and / or an amino acid-based cationic surfactant.