JP2018095574A - Oral composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an oral composition that exhibits a bactericidal effect with thymol, and has a refreshing use feeling with good palatability, and also excellent storage stability.SOLUTION: An oral composition contains (A) thymol 0.005 mass% or more, (B) menthol, (C) ascorbic acid phosphate ester magnesium, and (D) silica abrasive.SELECTED DRAWING: None

Description

  The present invention relates to a composition for oral cavity which has a bactericidal effect by thymol, has a good feeling of use, and is excellent in storage stability.

  In oral diseases such as caries and periodontal disease, sterilizing the causative bacteria is one of the important prevention methods. In oral compositions, thymol is known as a component having bactericidal power, but if this component is added, the unique odor and flavor may deteriorate the feeling of use such as refreshing and may be irritating. Therefore, the use of thymol as a fungicide was limited.

  Menthol is generally blended as a fragrance in oral compositions, and menthol has a refreshing feeling imparting effect, odor, and taste masking effect, but these effects are not fully exhibited depending on the blended ingredients, and many If it is added too much, its irritation becomes strong and painful irritation occurs, which may make it unusable for use.

  On the other hand, ascorbic acid phosphate ester such as magnesium ascorbate phosphate (APM) or a salt thereof is used in an oral composition as an active ingredient for prevention or suppression of periodontal diseases such as gingivitis. However, there is a problem in that it is difficult to stabilize and formulation discoloration easily occurs.

  In addition, the following patent documents 1-4 are mentioned as a prior art document relevant to this invention.

  Patent Document 1 (International Publication No. 2013/13396) discloses ascorbic acid phosphate ester or a salt thereof, a specific nonionic surfactant such as polyoxyethylene hydrogenated castor oil, isopropylmethylphenol, triclosan, and the like. By combining with an aromatic compound selected from thymol, the solubility of ascorbic acid phosphate ester or its salt in the neutral region of pH 8.0 or lower is improved, and the odor and dust during low-temperature storage are suppressed, resulting in a clear appearance A composition for oral cavity in which is maintained is disclosed.

Patent Document 2 (Japanese Patent Application Laid-Open No. 2012-131751) discloses a dentifrice composition comprising a combination of an ascorbic acid phosphate ester having a different pH range to be stabilized or a salt thereof and an alkali unstable periodontal disease preventive component, A technique for improving the stability of both components over time in a region of pH 8.0 or less by combining a silica-based abrasive is proposed, and thymol is described as an example of a fragrance that can be added.
Patent Document 3 (Japanese Patent No. 3582537) discloses the use of ascorbic acid phosphate and a specific monoterpenoid or specific phenylpropanoid and menthol in combination to absorb ascorbic acid phosphate into the mucosa. In addition, a composition for oral cavity that can effectively prevent the active oxygen produced excessively by the biological defense reaction and prevent / treat the destruction of gingival tissue in periodontal disease is disclosed.
Patent Document 4 (Japanese Patent Laid-Open No. 2013-129600) contains (A) an ascorbic acid phosphate or a salt thereof, (B) a silica-based abrasive, and (C) an alkali metal inorganic salt, and has a pH at 25 ° C. (D) Mensofuran and / or Mentone is blended with the dentifrice composition having a 6.0 to 8.0, so that a unique metallic taste when using the dentifrice composition, It describes that the astringency is improved and the usability can be improved.

International Publication No. 2013/133096 JP 2012-131751 A Japanese Patent No. 3582537 JP 2013-129600 A

  However, in the conventional technology, when thymol is blended as a bactericidal agent in an oral composition, lack of refreshment due to its specific odor and irritation, and improvements in terms of palatability and feeling of use have been desired.

  The present invention has been made in view of the above circumstances, and has an object to provide an oral composition that has a bactericidal effect by thymol, has a refreshing and good feeling of use, and is excellent in storage stability. To do.

  As a result of intensive studies to achieve the above object, the present inventor has (B) menthol and (C) ascorbic acid phosphate ester in an oral composition containing 0.005% by mass or more of (A) thymol. When combined with magnesium and (D) silica-based abrasives, (A) the sterilization effect by thymol is exhibited and its specific odor is masked, and the irritation derived from the components (A) and (B) is also suppressed and refreshed. The present inventors have found that it is possible to give a good feeling of use with excellent palatability and to prevent the discoloration of the preparation over time, to stabilize the flavor and to give good storage stability, and to achieve the present invention.

  In the present invention, when the (B) component and the (C) component are used in combination with the (A) thymol, which is a bactericidal agent, the combined system of the (B) and (C) components is a masking agent for idiosyncratic odors and a stimulating agent. Acting as an inhibitor, the unique and unique odor of the component (A) is appropriately masked, and the irritation derived from the components (A) and (B) is alleviated, whereby simple addition of a general oral flavor Thus, it is possible to give a feeling of use with good palatability and excellent refreshing feeling that cannot be achieved. Furthermore, in this case, when the components (A), (B), and (C) are combined, the storage stability is lowered, for example, the preparation is discolored due to browning or the flavor is deteriorated. However, by using the (D) component in combination, the usability is improved without causing the above-mentioned problems related to storage stability, and (A), (B), (C), (D) A particularly remarkable effect can be imparted by a combination of components.

Accordingly, the present invention provides the following oral composition.
[1] (A) 0.005% by mass or more of thymol,
(B) menthol,
An oral composition comprising (C) magnesium ascorbate phosphate and (D) a silica-based abrasive.
[2] Containing 0.005 to 1% by mass of component (A) as a bactericide, 0.05 to 2% by mass of component (B), 0.02 to 1% by mass of component (C), (D ) The composition for oral cavity according to [1], containing 5 to 30% by mass of the component.
[3] The composition for oral cavity according to [1] or [2], wherein the content of abrasives other than (D) silica-based abrasive is 0 to 10% by mass.
[4] The composition for oral cavity according to any one of [1] to [3], wherein the blending mass ratio represented by (B) / (A) is 0.4 to 80.
[5] The composition for oral cavity according to any one of [1] to [4], wherein the composition has a pH at 7.5C of 7.5 to 9.5.
[6] The composition for oral cavity according to any one of [1] to [5], which is a toothpaste.

  ADVANTAGE OF THE INVENTION According to this invention, the thymol containing oral composition which has the bactericidal effect by thymol, has a refreshing and favorable feeling of use, and is excellent also in storage stability can be provided.

  The composition for oral cavity of the present invention contains (A) thymol at a specific amount or more and (B) menthol, (C) magnesium ascorbate phosphate (APM) and (D) a silica-based abrasive. It is. Hereinafter, each component will be described in detail.

  (A) Thymol is a component blended as a bactericidal agent. Thymol may be used as a single thymol or may be used as an essential oil containing thymol such as thyme oil.

  The blending amount of (A) thymol is 0.005% by mass or more of the entire composition, preferably 0.01-2% by mass, more preferably 0.01-1% by mass, and still more preferably 0.02-%. 0.5% by mass. As the blending amount of the component (A) increases, the bactericidal effect increases. When the blending amount of the component (A) is less than 0.005% by mass, the bactericidal effect is not sufficiently obtained. On the other hand, although there is no restriction | limiting in particular about the upper limit of a compounding quantity, It is suitable to set it as 2 mass% or less from the point of own specific odor, irritation | stimulation, and the discoloration suppression of a formulation. In addition, what is necessary is just to use so that content of thymol may become in the said range when using the essential oil containing thymol.

  (B) Menthol increases the refreshing feeling during use and acts as a masking agent for a specific odor derived from the component (A), and L-menthol can be used. As the component (B), one isolated or synthesized from essential oil containing menthol may be used, or the essential oil may be used as it is.

  (B) 0.05-2 mass% of the whole composition is preferable, and, as for the compounding quantity of menthol, 0.1-1.2 mass% is more preferable. When the blending amount of component (B) is 0.05% by mass or more, a sufficient masking effect and refreshing feeling can be obtained. Moreover, it is suitable for suppression of irritation | stimulation that the compounding quantity of (B) component is 2 mass% or less. When the blending amount of the component (B) is too large, the stimulus of the component (B) itself is strongly expressed when used in combination with the component (A), and the stimulus may not be suppressed even when the component (C) is blended. In addition, when using the essential oil containing a menthol, what is necessary is just to use so that content of a menthol may be in the said range.

  In the present invention, the blending mass ratio represented by (B) / (A) is preferably 0.4 to 80, and more preferably 0.8 to 80. By making this ratio within the above-mentioned range, it is possible to obtain a good feeling of use that is not excessively irritating while suppressing a specific odor and obtaining a refreshing feeling.

(C) Ascorbic acid phosphate magnesium (APM) is a component that acts as a masking agent for specific odors and an irritation suppressor in combination with component (B).
(C) Ascorbic acid phosphate magnesium may include a magnesium salt of a derivative having a phosphate group at any of positions 2, 3, 5, and 6 of ascorbic acid. For example, ascorbic acid-2-phosphate, ascorbic acid-3-phosphate, ascorbic acid-5-phosphate, ascorbic acid-6-phosphate, ascorbic acid-2-polyphosphate, ascorbic acid- Mention may be made of magnesium salts of ascorbic acid phosphate derivatives such as 3-polyphosphate, ascorbic acid-5-polyphosphate, and ascorbyl-6-polyphosphate. As the component (C), one kind selected from these may be used alone or two or more kinds may be used in appropriate combination. In particular, ascorbic acid-2-phosphate magnesium is preferable in terms of stability of the composition. Preferably used.

  Although the compounding quantity of (C) component is not restrict | limited in particular, 0.02-1 mass% of the whole composition is preferable, More preferably, it is 0.1-0.6 mass%. When the blending amount of the component (C) is 0.02% by mass or more, sufficient masking ability and stimulation suppression effect are obtained, and when it is 1% by mass or less, sufficient preparation discoloration suppressing effect and flavor stability are obtained. can get.

  In the present invention, the blending mass ratio represented by (C) / (B) is preferably 0.01 to 10, more preferably 0.05 to 6, still more preferably 0.2 to 3, ~ 2 is particularly preferred. When the blending mass ratio is within the above range, the refreshing feeling, the specific odor masking ability, and the stimulus suppressing effect are further improved, and the effect of suppressing the discoloration of the preparation and the flavor stability are further improved.

  In addition, [(A) + (B)] / (C) indicating the ratio of the total amount of the components (A) and (B) to the amount of the component (C) is 0.1 to 25 in terms of mass ratio. Preferably, 0.3 to 23 is more preferable, and 0.5 to 5 is particularly preferable. By making this ratio within the above-mentioned range, a refreshing feeling, a specific odor masking ability, a stimulus suppressing effect can be obtained, and a preparation which hardly changes color can be obtained.

  Examples of (D) silica-based abrasives include precipitated silica, silica gel, aluminosilicate, and the like. (D) As for the compounding quantity of a component, 5-30 mass% of the whole composition is preferable, and 8-22 mass% is more preferable. When the blending amount of the component (D) is 5% by mass or more, the discoloration of the preparation can be sufficiently suppressed and the flavor can be stabilized. When the blending amount of the component (D) is 30% by mass or less, it is possible to secure an appropriate polishing force and hardness of the preparation.

  In the present invention, (D) abrasives other than silica-based abrasives, specifically, calcium phosphate-based abrasives such as dicalcium phosphate, aluminum hydroxide, calcium carbonate, and the like are within the range that does not hinder the effects of the present invention. However, it is preferable not to mix them. (D) When mix | blending abrasives other than a component, the compounding quantity considers the deterioration of the flavor accompanying time-lapse | temporality, and discoloration of an agent, 7 mass% or less, Especially 5 mass% or less are preferable, 0 mass% is More preferred.

The oral composition of the present invention includes (A) thymol, (B) other fragrance in addition to natural fragrance added as a general oral fragrance, and fragrance processed from natural fragrance, and Known perfume materials used in oral compositions such as simple flavors and blended flavors can be used singly or in combination of two or more. The blending amount of the fragrances other than the components (A) and (B) is preferably 0.01 to 2% by mass, more preferably 0.05 to 1% by mass, based on the flavor stability. When it is within this range, sufficient flavor stability can be obtained.
In addition, as a fragrance | flavor, the fragrance | flavor raw material containing (A) thymol and (B) menthol is included in the amount of above-mentioned (A) and (B) component, and can be used within the range of each compounding quantity.

  The composition for oral cavity of the present invention is prepared in a usual manner as a dentifrice such as a toothpaste, a liquid toothpaste, a moisturized toothpaste, etc. in the form of liquid, paste, etc. Other optional components according to the mold can be blended within a range not impairing the effects of the present invention. For example, a binder, a thickener, a surfactant, a sweetener, an antiseptic, a colorant, (A) thymol, and (B) an active ingredient other than magnesium ascorbyl phosphate may be blended.

  Examples of the thickener include sugar alcohols such as sorbitol, and polyhydric alcohols such as propylene glycol and glycerin. The compounding quantity of a thickener is 5-50 mass% normally.

  Examples of the binder include cellulose derivatives such as sodium carboxymethyl cellulose, gums such as xanthan gum, and carrageenan. The compounding amount of the binder is usually 0 to 5% by mass, particularly 0.1 to 5% by mass.

As the surfactant, an anionic surfactant, a cationic surfactant, a nonionic surfactant, and an amphoteric surfactant can be blended.
Examples of the anionic surfactant include alkyl sulfates such as sodium lauryl sulfate. Examples of nonionic surfactants include polyhydric acids such as sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, sugar alcohol fatty acid esters such as sucrose fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, and polyoxyethylene glycerin fatty acid esters. Examples include alcohol fatty acid esters, polyoxyethylene alkyl ethers, polyoxyethylene fatty acid esters such as polyoxyethylene hydrogenated castor oil, and fatty acid alkanolamides. Examples of the cationic surfactant include alkylammonium type, and examples of the amphoteric surfactant include betaine type and imidazoline type. The compounding amount of these surfactants is preferably 0.1 to 10% by mass, particularly 0.5 to 5% by mass, based on the entire composition.

  Examples of the sweetener include saccharin sodium, and examples of the antiseptic include paraoxybenzoic acid ester, benzoic acid and salts thereof. As a coloring agent, a well-known pigment | dye can be used for oral cavity compositions.

  As an active ingredient (medicinal ingredient), a publicly known medicinal ingredient blended in a composition for oral cavity can be used. Examples include fluorine-containing compounds such as sodium fluoride and sodium monofluorophosphate, tranexamic acid, epsilon aminocaproic acid, anti-inflammatory agents such as allantoin, and enzymes such as dextranase. In addition, the said active ingredient can mix | blend an effective amount in the range which does not prevent the effect of this invention.

  The pH of the composition may vary, but the pH at 25 ° C. is preferably 7.5 to 9.5, more preferably 8.0 to 9.1. By making pH of a composition into said range, stability of (C) component can be improved more. In addition, you may adjust pH of a composition using a well-known pH adjuster. Examples of the pH adjuster include citric acid, malic acid and alkali metal salts thereof, sodium hydroxide, potassium hydroxide, disodium hydrogen phosphate, sodium dihydrogen phosphate, hydrochloric acid and the like.

  EXAMPLES Hereinafter, although an Example, a comparative example, a formulation example is shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example. In the following examples, “%” means “% by mass” unless otherwise specified.

[Examples 1-17, Comparative Examples 1-5]
An oral composition (toothpaste) was prepared by a conventional method using the components shown in Tables 2 to 4 and having the compositions shown in Table 1. The obtained composition for oral cavity was used as a test preparation, and the usability and storage stability were evaluated by the following methods. The results are shown in Tables 2-4.
Moreover, all the compositions for oral cavity of an Example confirmed that the bactericidal power was high.

(1) Evaluation of feeling of use Three test subjects collect about 1g of each composition on a toothbrush, brush their teeth for 3 minutes, and determine the refreshing feeling, specific odor masking ability and irritation when using the following evaluation criteria. Adopt the most evaluation points.

<Exhilaration>
◎: Feel strongly ○: Feel △: Feel a little ×: Don't feel

<Unique odor masking ability>
◎: Peculiar odor of thymol is masked and palatability is good. ○: Peculiar odor of thymol is slightly felt but not uncomfortable. △: Peculiar odor of thymol is felt but it is durable. ×: Peculiar odor of thymol. And poor taste

<Stimulus>
◎: No sense of irritation is observed and the feeling of use is excellent ○: Some irritation is recognized but there is no problem as the feeling of use △: There is considerable irritation and the feeling of use is slightly bad ×: Strong irritation and bad feeling of use

(2) Evaluation of storage stability Each composition filled in the tube was stored at 50 ° C. for one month, and then the composition was taken out of the tube onto paper and visually evaluated for discoloration according to the following evaluation criteria.
In addition, three test subjects brushed their teeth using about 1 g of each composition after storage in the same manner as described above, evaluated the flavor stability according to the following evaluation criteria, and adopted the most evaluation points. In addition, the thing stored at -5 degreeC was used as a control article corresponding to immediately after manufacture, and the comparative evaluation was carried out.

<discoloration>
◎: Same color in the adjacent comparison with the control product ○: Some color difference was recognized in the adjacent comparison with the control product, but the difference cannot be recognized in the distance comparison △: With the control product Although a slight color difference was recognized in the comparison of the distance between the two, it is a level that is not a problem. ×: The color is clearly different from the control product.

<Flavor stability>
A: Flavor of the same level as compared to the control product ○: A slight change in flavor was observed compared to the control product, but there was no problem in use ×: Change in flavor compared to the control product Is obvious and has problems in use with deteriorating odor and taste

Details of the raw materials used are as follows.
(A) Thymol: manufactured by Takasago International Corporation (B) menthol: 1-menthol, manufactured by Takasago International Corporation (C) APM: magnesium ascorbyl 2-phosphate ester, Wako Pure Chemical Industries, Ltd. Made (D) abrasive silica: Taki Chemical Co., Ltd. calcium hydrogen phosphate (comparative product): Taihei Chemical Industry Co., Ltd. calcium carbonate (compared product): Calfine Co., Ltd. The composition is as shown in Table 5.

Comparative Examples 1 and 2 were blended with abrasives other than (D) silica-based abrasives, but discolored after storage at 50 ° C. for 1 month, resulting in poor flavor stability.
In Comparative Example 3, since the component (B) was not blended, it was confirmed that there was no refreshing feeling and the specific odor of thymol was not masked.
In Comparative Example 4, since the component (C) was not blended, it was confirmed that the irritation caused by the combination of the component (A) and the component (B) was not suppressed.
In Comparative Example 5, since the component (B) and the component (C) were not blended, there was no refreshing feeling and it was confirmed that the specific odor of thymol was not masked.

  Hereinafter, the composition of the fragrance is shown.

  Hereinafter, a prescription example is shown.

Claims (6)

(A) 0.005% by mass or more of thymol,
(B) menthol,
An oral composition comprising (C) magnesium ascorbate phosphate and (D) a silica-based abrasive.   As a bactericidal agent, it contains 0.005 to 1% by mass of component (A), 0.05 to 2% by mass of component (B), 0.02 to 1% by mass of component (C), and component (D). The composition for oral cavity of Claim 1 containing 5-30 mass%.   Furthermore, content of abrasive | polishing agents other than (D) silica type abrasive | polishing agent is 0-10 mass%, The composition for oral cavity of Claim 1 or 2.   The composition for oral cavity according to any one of claims 1 to 3, wherein a blending mass ratio represented by (B) / (A) is 0.4 to 80.   The composition for oral cavity according to any one of claims 1 to 4, wherein the pH of the composition at 25 ° C is 7.5 to 9.5.   It is a toothpaste, The composition for oral cavity of any one of Claims 1-5.