JP2020093998A - Liquid oral composition - Google Patents

Abstract

To provide a liquid oral composition that reduces bitterness and stimulus peculiar to cetylpyridinium chloride and tranexamic acid and prevents discoloration with time and has good appearance stability.SOLUTION: A liquid oral composition contains following components (A)-(C): (A) cetylpyridinium chloride 0.01-0.1 wt.%, (B) tranexamic acid 0.01-0.1 wt.%, and (C) Apocynum venetum extract 0.00005-0.01 wt.% and has a pH of 5.0-6.5.SELECTED DRAWING: None

Description

The present invention relates to a liquid oral composition, more specifically, a liquid oral composition that reduces bitterness and irritation peculiar to cetylpyridinium chloride and tranexamic acid, and is excellent in appearance stability by suppressing discoloration over time. Regarding things.

BACKGROUND ART Conventionally, a bactericidal agent, an antiplasmin agent, and the like have been incorporated into oral compositions for the prevention or treatment of periodontal diseases. Known bactericides include, for example, quaternary ammonium salt type cationic bactericides such as cetylpyridinium chloride. However, since cetylpyridinium chloride has a peculiar bitterness and also has an irritating property, in order to apply it to the oral cavity, it is required to reduce these as much as possible.

In addition, tranexamic acid and the like are known as antiplasmin agents. However, tranexamic acid also has a peculiar bitterness, and there is also a problem that the appearance turns yellow with time.

In order to solve the problem of bitterness derived from cetylpyridinium chloride, a technique of improving bitterness and irritation by the combined use of a stevia sweetener and improving palatability has been proposed (Patent Document 1), and a method of masking with a flavor component is proposed. It has been proposed (Patent Document 2). However, in these methods, the preparation may become too sweet due to the sweetness of the sweetener, or the sensation of the fragrance itself may deteriorate the usability.

In order to solve the problem of bitterness derived from tranexamic acid, a technique has been proposed in which 1-menthyl acetate is used to improve persistent bitterness in combination with triclosan (Patent Document 3). However, these methods may not suit the taste of the user because l-menthyl acetate itself has a sensation.

Furthermore, a technique of masking bitterness by blending maltitol with cetylpyridinium chloride and tranexamic acid has been proposed (Patent Document 4), but this is also masking of bitterness by increasing sweetness, and therefore the formulation is It may become too sweet and the usability may deteriorate.

Thus, despite the combined use of cetylpyridinium chloride and tranexamic acid, bitterness and irritation is reduced, and the feeling of use is also satisfactory, and an oral composition excellent in appearance stability is still available. Not achieved. Therefore, development of an oral composition satisfying all of these is desired.

Japanese Patent Laid-Open No. 05-000931 JP, 2004-18431, A JP 04-139117A Japanese Patent No. 4044748

An object of the present invention is to provide a composition for liquid oral cavity which reduces bitterness and irritation peculiar to cetylpyridinium chloride and tranexamic acid, and further suppresses discoloration over time and has excellent appearance stability.

In view of such circumstances, as a result of earnest research, the inventors of the present application contained 0.01 to 0.1% by weight of (A) cetylpyridinium chloride and 0.01 to 0.1% by weight of tranexamic acid (B). When the liquid oral composition contains 0.00005 to 0.01% by weight of the extract (C) Rahuma and the pH of the liquid oral composition is 5.0 to 6.5, cetylpyridinium chloride is obtained. Further, they found that the bitterness and irritation peculiar to tranexamic acid are reduced, and further discoloration with time is suppressed, and the present invention was completed.

The present invention also provides a liquid oral composition, which is characterized by not containing ethanol.

The present invention also provides a liquid oral composition, which is a mouthwash.

The liquid composition for oral cavity of the present invention has excellent bitterness and irritation characteristic of cetylpyridinium chloride and tranexamic acid, and further has excellent appearance stability by suppressing discoloration over time.

The component (A) cetylpyridinium chloride used in the present invention is a cationic bactericidal agent contained in a quaternary ammonium compound, and is a substance widely used in the composition for oral cavity for the purpose of sterilizing oral bacteria.

The content of the component (A) is 0.01 to 0.1% by weight, preferably 0.03 to 0.08% by weight, based on the entire liquid oral composition. If it is less than 0.01% by weight, the bactericidal effect in the oral cavity cannot be sufficiently exhibited, and if it exceeds 0.1% by weight, bitterness may be further increased.

The component (B) tranexamic acid used in the present invention is an antiplasmin agent, and is an effective component for antiplasmin and bleeding prevention.

The content of the component (B) is 0.01 to 0.1% by weight, preferably 0.03 to 0.1% by weight, based on the entire liquid oral composition. If it is less than 0.01% by weight, a sufficient anti-inflammatory effect may not be obtained, and if it exceeds 0.1% by weight, the feeling of use may deteriorate and the discoloration with time may become strong.

Component (C) used in the present invention is an extract of Rahuma. Rafuma (Apocynum Venetum L.) is a perennial plant that belongs to the genus Bascurcumon of the oleander family and mainly grows in northwestern China. The component (C) can be used in any part such as leaves, stems, roots, and may be a crushed product, shredded product, or a dried product thereof.

The above plant extract can be obtained by a conventional method using an extraction solvent. Examples of the solvent to be extracted include water, lower alcohols (methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 2-butanol, etc.), liquid polyhydric alcohols (1,3-butylene glycol, propylene). Glycol, glycerin, etc.), ketones (acetone, methyl ethyl ketone, etc.), acetonitrile, esters (ethyl acetate, butyl acetate, etc.), hydrocarbons (hexane, heptane, etc.), ethers (ethyl ether, tetrahydrofuran, propyl ether, etc.) Is mentioned. These solvents may be used alone or in combination of two or more. A polar solvent such as water or a lower alcohol is preferable, and water is particularly preferable.

The extract may be used as it is as an extracted solution, and if necessary, it may be subjected to treatments such as concentration, dilution, filtration, decolorization with activated carbon, deodorization, ethanol precipitation and the like. Furthermore, the extracted solution may be concentrated to dryness, spray-dried, freeze-dried and the like and used as a dried product.

The content of the component (C) is 0.00005 to 0.01% by weight, preferably 0.0001 to 0.01% by weight, based on the entire liquid oral composition. If it is less than 0.00005% by weight, a sufficient bitterness-suppressing effect cannot be obtained, and if it exceeds 0.01% by weight, an astringent taste derived from the extract may be generated.

The pH of the liquid oral composition of the present invention is in the range of 5.0 to 6.5, and preferably in the range of 5.0 to 6.3, as described above. If the pH is higher than 6.5, the effect of suppressing discoloration over time becomes insufficient, and the appearance stability may be poor.
The above pH was measured immediately after the composition was prepared using a pH meter (model number F-51) manufactured by Horiba Ltd., and the value after 3 minutes at 20°C was shown.
The pH can be adjusted within the above range depending on the course, but a pH adjusting agent may be added if necessary. The pH adjuster is not particularly limited, and examples thereof include citric acid, sodium citrate, sodium monohydrogen phosphate, sodium dihydrogen phosphate, and the like, and one or more of these can be used.

The liquid composition for oral cavity of the present invention is not particularly limited as to the content of ethanol, but preferably it does not contain ethanol. This can further reduce irritation.

The liquid oral composition of the present invention is prepared as a liquid preparation in which the contained components are solubilized, and for example, it is used as a raw mouthwash, a mouthwash, a mouthwash, or a concentrated type, which is diluted when used. It can be prepared as a mouthwash, liquid dentifrice, etc. Of these, the mouth rinse is particularly preferable. In addition, especially in mouthwash, bitterness, irritation, etc. are more strongly expressed than paste-like preparations such as dentifrice, but in the present invention, bitterness, irritation is reduced in such liquid preparation, and a good feeling of use is obtained. Can be granted.

The liquid composition for oral cavity of the present invention may contain any component used in a usual composition for oral cavity, in addition to the above-mentioned components, within the range where the intended effect is not impaired. For example, wetting agents, surfactants, solvents, sweeteners, coloring agents, flavors, preservatives, thickeners, active ingredients and the like can be mentioned. However, it is not limited to these examples.

Next, the present invention will be described in more detail with reference to examples. However, the present invention is not limited to these. The content is% by weight.

Below, the example of manufacture of the solvent extract using Rahuma is shown.

Production Example 1 Hot water extract of Rahuma Purified water (10 L) was added to 150 g of dried Rahuma leaf, and extraction was performed at 95 to 100° C. for 2 hours. The filtrate was concentrated under reduced pressure and freeze-dried to obtain 11.5 g of a hot water extract of Rahuma.

Production Example 2 50% ethanol extract of Rahuma To 100 g of dried Rahuma leaf was added 3 L of a 50 (v/v)% ethanol aqueous solution, and the mixture was extracted at room temperature for 5 days. The filtrate was concentrated to dryness under reduced pressure to obtain 5.5 g of 50% ethanol extract of Rahuma.

According to the compositions shown in Tables 1 to 3, the liquid oral compositions (mouthwashes) of Examples 1 to 13 and Comparative Examples 1 to 6 were prepared by a conventional method, and the obtained liquid oral compositions were as follows. Evaluation was performed according to the method.

(Evaluation method)
Approximately 10 mL of the liquid oral composition of the sample shown in the table by 10 specialist panelists was rinsed for 30 seconds, and after rinsing for 30 seconds, (1) bitterness and (2) irritation, the following criteria Was evaluated according to.

(1) Bitterness (evaluation standard)
4 points: No bitterness is felt 3 points: Little bitterness is felt 2 points: Bitterness is felt 1 point: Bitterness is strongly felt (criteria)
⊚: Average point is 3.5 points or more and 4.0 points or less ○: Average point is 3.0 points or more and less than 3.5 points Δ: Average point is 2.0 points or more and less than 3.0 points x: Average point is Less than 2.0 points

(2) Stimulation (evaluation criteria)
4 points: No irritation at all 3 points: Almost no irritation 2 points: irritation is felt 1 point: irritation is strongly felt (criteria)
⊚: Average point is 3.5 points or more and 4.0 points or less ○: Average point is 3.0 points or more and less than 3.5 points Δ: Average point is 2.0 points or more and less than 3.0 points x: Average point is Less than 2.0 points

(3) Appearance stability (no discoloration)
Each sample shown in the table was stored in a constant temperature bath at 40° C. for 3 months, and then the appearance stability (discoloration) was visually observed and evaluated according to the following criteria. The evaluation was based on colorless and transparent water.
(Criteria)
⊚: No discoloration at all, colorless and transparent ○: Slightly pale yellow discoloration is seen, but there is no problem ×: Clearly yellow discoloration is seen

The details of the raw materials used are as follows.
・Cetylpyridinium chloride (manufactured by Fuji Film Wako Pure Chemical Industries)
・Tranexamic acid (Kyowa Pharma Chemical Co., Ltd.)

In Tables 1 and 2 above, when the liquid oral compositions of the present invention of Examples 1 to 13 are used, the bitterness and irritancy peculiar to cetylpyridinium chloride and tranexamic acid are reduced, and further, discoloration over time is caused. It was suppressed and had excellent appearance stability.

In Table 3 above, when the content of the component (A) is more than 0.1% by weight (Comparative Example 1) or when the content of the component (B) is more than 0.1% by weight (Comparative Example 2), Alternatively, when the content of the component (C) was less than 0.00005% by weight (Comparative Example 3), bitterness and irritation could not be suppressed. Moreover, when the content of the component (C) was more than 0.01% by weight (Comparative Example 4), an astringent taste derived from a plant appeared and the bitterness could not be suppressed. Furthermore, when the pH of the liquid oral composition was higher than 6.5 (Comparative Examples 5 and 6), discoloration of tranexamic acid occurred over time, and the appearance stability was deteriorated.

(Example 14)
(Component) (% by weight)
1. Cetylpyridinium chloride 0.04
2. Tranexamic acid 0.03
3. Rafuma 50% ethanol extract (Production Example 2) 0.004
4. Glycerin 4.0
5. Propylene glycol 4.0
6. Polyoxyethylene hydrogenated castor oil 0.4
7. Xylitol 3.0
8. Citric acid 0.03
9. Sodium citrate 0.27
10. Perfume 0.1
11. Methylparaben 0.1
12. Purified water Residual (preparation method)
Prepared in the same manner as in Examples 1-13.
pH=6.2

(Example 15)
(Component) (% by weight)
1. Cetylpyridinium chloride 0.06
2. Tranexamic acid 0.04
3. Rafuma 50% ethanol extract (Production Example 2) 0.007
4. Glycerin 7.0
5. Propylene glycol 4.0
6. Polyoxyethylene hydrogenated castor oil 0.5
7. Sorbitol 5.0
8. Sodium monohydrogen phosphate 0.05
9. Sodium dihydrogen phosphate 0.25
10. Perfume 0.15
11. Methylparaben 0.1
12. Purified water Residual (preparation method)
Prepared in the same manner as in Examples 1-13.
pH=5.9

When the liquid oral compositions shown in Examples 14 and 15 were evaluated, the bitterness and irritancy peculiar to cetylpyridinium chloride and tranexamic acid were reduced, and further, discoloration over time was suppressed and the appearance stability was excellent. ..

ADVANTAGE OF THE INVENTION According to this invention, the bitterness and irritation peculiar to cetylpyridinium chloride and tranexamic acid are reduced, the discoloration over time is suppressed, and the liquid oral composition excellent in appearance stability can be provided.

Claims (3)

The following components (A) to (C);
(A) Cetylpyridinium chloride 0.01 to 0.1% by weight
(B) Tranexamic acid 0.01 to 0.1% by weight
(C) Rafuma extract 0.00005-0.01% by weight
And a pH of 5.0 to 6.5. The liquid oral composition according to claim 1, which does not contain ethanol. The liquid oral composition according to claim 1 or 2, which is a mouthwash.