JP2002308747A - Foamable solid composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a foamable solid composition for the oral cavity having quality stability of a product improved by suppressing the reaction of a carbonic acid salt with an organic acid under preservation, and further having suppressed acidity when being used, and excellent feel in use. SOLUTION: This foamable solid composition for the oral cavity is characterized in that the composition comprises (A) the carbonic acid salt, and (B) a partially neutralized organic acid partially neutralized so that the pH of a solution obtained by dissolving the neutralized organic acid in water may be 3.5-5.0, and surface-coated with a water-soluble polymer.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a partially neutralized solubilized carbonate and water having a pH of 3.5 to 5.0 when dissolved in water.
The present invention also relates to an effervescent oral solid composition containing a partially neutralized organic acid whose surface is coated with a water-soluble polymer.

[0002]

2. Description of the Related Art Conventionally, a solid foamable oral composition is a solid preparation containing a carbonate and an organic acid as a foaming component, and has an excellent refreshing sensation when placed directly in the oral cavity. There are known oral compositions (for example, JP-A-3-279321). In addition, an oral composition containing a foaming component, a heat absorbing agent and 1-menthol to obtain an excellent refreshing sensation, and a solid preparation containing a large amount of a heat absorbing agent to enhance the refreshing sensation (JP-A-7-238008) Gazette) is also known.

[0003] In the form of such an effervescent solid preparation, solid carbonates and organic acids are usually used as the effervescent component. The foaming reaction in the packaging material during storage causes blistering and rupture of the container, and the foaming action in the mouth, which is a characteristic function of the product, is lost. There are drawbacks. Further, the compounding amount of the organic acid in the effervescent solid preparation is large, and when the amount of the organic acid is excessive, the acidity becomes strong and the feeling of use is deteriorated.

On the other hand, for the purpose of suppressing the foaming reaction in the packaging material during storage, for example, a foamable solid composition for oral cavity using a carbonate and an organic acid coated with a hydrophobic polymer (Japanese Patent Application Laid-Open No. Hei 7-238008) ) Is disclosed, but in this case, the reactivity between the carbonate and the organic acid is reduced at the time of use, a sufficient foaming action cannot be obtained, and the sourness is not sufficiently improved. Therefore, there is a problem that a strong acidity is generated at the time of use, and it is not sufficiently satisfactory in use feeling. From the above, we have improved the quality stability during storage,
There is a demand for the development of an effervescent solid composition for oral use that has a reduced feeling of strong acidity during use and has an excellent feeling in use.

[0005]

SUMMARY OF THE INVENTION The present invention improves the quality stability of a product by suppressing the reaction between a carbonate and an organic acid during storage, and further suppresses the acidity during use. An object of the present invention is to provide an effervescent solid composition for the oral cavity with excellent feeling.

[0006]

Means for Solving the Problems The inventors of the present invention have made intensive studies to solve the above-mentioned problems, and as a result, the pH of (A) carbonate and (B) the pH at the time of dissolving in water were 3.5 to 5.5. By blending a partially neutralized organic acid that is partially neutralized to be 0 and surface-coated with a water-soluble polymer, the quality stability during storage is good, the acidity during use is suppressed, and the feeling of use is reduced. The present inventors have found that a good foamable oral solid composition can be obtained, and have accomplished the present invention. That is, according to the present invention,
(A) pH of 3.5 to 5.0 upon dissolution of carbonate and (B) water.
And a partially neutralized organic acid surface-coated with a water-soluble polymer to provide a foamable solid composition for oral cavity.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION The present invention has a pH of 3.
It is characterized by using a partially neutralized organic acid which is partially neutralized to 5 to 5.0 and is surface-coated with a water-soluble polymer. In the composition of the present invention, the reaction between the carbonate and the organic acid during storage of the preparation is suppressed, the solubility by the water in the mouth is kept high, and the acidity during use is maintained without lowering the foaming property. Is suppressed.

[0008] The carbonate (A) is not particularly limited as long as it can be used for the oral cavity and generates carbon dioxide when dissolved in the oral cavity. Examples of such a carbonate include sodium carbonate, sodium hydrogen carbonate, potassium carbonate, potassium hydrogen carbonate, ammonium carbonate, sodium sesquicarbonate and the like. Of these, sodium carbonate, sodium hydrogen carbonate and potassium carbonate are particularly preferred. These carbonates can also be used as granules by a commonly used production method. These carbonates can be used alone or as a mixture of two or more. Carbonate is 1-50% of the total amount of the composition,
In particular, it is preferably set to 5 to 40%.

(B) Partially neutralized organic acids which are partially neutralized so as to have a pH of 3.5 to 5.0 when dissolved in water and which are surface-coated with a water-soluble polymer include those conventionally known, For example, sodium or potassium partially neutralized products of organic acids such as citric acid, malic acid, and tartaric acid, and these partially neutralized organic acids are obtained by neutralizing the corresponding organic acids with sodium hydroxide or sodium carbonate by a conventional method. After the treatment, the degree of neutralization is adjusted so that the pH at the time of dissolution in water (25 ° C., 1%) becomes 3.5 to 5.0, and dried by a conventional method to obtain a powder or granules. be able to. As the water-soluble polymer for coating, conventionally known ones, for example, hydroxyethyl cellulose, hydroxypropyl cellulose,
Examples thereof include sodium carboxymethylcellulose, polyethylene glycol, and polyvinylpyrrolidone, and the average molecular weight of the polymer is usually 5,000 to 1,500.
It is about 000. The amount of the water-soluble polymer is 0.5 to 2 with respect to the amount of the partially neutralized organic acid coated on the surface.
It is preferably 0%, particularly preferably 1 to 5%. As the organic acid salt having such a surface coating, in particular, sodium partially neutralized citric acid adjusted to have a pH of 3.5 to 4.5 when dissolving citric anhydride in water is, for example, vacuum-coated. Using a machine (manufactured by Kikusui Seisakusho) etc.,
Those surface-coated with polyvinylpyrrolidone are preferred. As polyvinylpyrrolidone, those having an average molecular weight of about 40,000, for example, PVP K-30 (I.
S. (Company P) coated with 1 to 2% is particularly preferable. Such partially neutralized organic acids can be used alone or as a mixture of two or more.

The pH at the time of dissolution (B) of the present invention is 3.5 to 3.5.
The partially neutralized organic acid partially neutralized so as to be 5.0 and coated with a water-soluble polymer on the surface is dissolved in water (2
It is important that the pH (5 ° C., 1%) is 3.5 to 5.0, and more preferably 3.5 to 4.5. p
When H exceeds 5.0, the foaming amount in the mouth decreases and the feeling of use deteriorates. When the pH is less than 3.5, the feeling of use becomes extremely poor due to strong acidity and residual feeling during use, and foaming reaction occurs during storage. In addition, the swelling or rupture of the packaging material occurs, and the quality stability of the product cannot be maintained. The pH of an unneutralized organic acid such as citric acid itself when dissolved in water is slightly less than 3, which includes the above-mentioned problems.

The effervescent oral solid composition of the present invention preferably does not contain a water-insoluble solid such as an abrasive, and can be made substantially entirely water-soluble. This is a method of foaming in the mouth, washing the mouth, and discharging in order to improve the usability of the composition of the present invention and enhance the effect of improving the usability. As a result, unpleasant insoluble residues are not left in the mouth after ejection, and water rinsing after use is unnecessary, and convenience can be improved.

The foamable oral solid composition of the present invention may contain a powdered fragrance as a refreshing and aromatic component. The powdered flavor is not particularly limited in its production method, components and the like, and various powdered flavors can be used. As such, for example, dextrin,
Examples thereof include those contained in a base such as gum arabic and gelatin. On the other hand, as oily flavors, 1-menthol,
Carvone, anethole, eugenol, methyl salicylate, spearmint oil, peppermint oil, wintergreen oil, lemon oil, orange oil, grapefruit oil,
Sage oil, rosemary oil, cinnamon oil, pimento oil, cinnamon oil, perilla oil, winter green oil, clove oil, eucalyptus oil, strawberry flavor, orange flavor, lemon flavor, apple flavor, panana flavor, pineapple flavor, etc. .

The composition of the present invention may contain various auxiliary ingredients in addition to the above-mentioned perfume ingredients. The composition of the present invention may contain a fluorine-containing component. Examples of such a material include sodium fluoride, ammonium fluoride, potassium fluoride, lithium fluoride, tin fluoride, sodium monofluorophosphate, ammonium monofluorophosphate, potassium monofluorophosphate, and monofluorophosphate. Examples thereof include fluorine-containing natural products containing lithium such as lithium, seaweed, seaweeds and tea, and extracts thereof. These can be used alone or in combination of two or more.
Preferably, sodium fluoride and sodium monofluorophosphate are good. The concentration of fluorine at which these fluorine-containing components act in the oral cavity is preferably not more than 1,000 ppm, and particularly preferably 1 to 250 ppm.

The composition of the present invention can contain a surfactant. Such materials include sodium lauryl sulfate, sodium dodecyl benzene sulfonate, sodium α-sulfofatty acid alkyl ester,
Anionic surfactants such as alkyl phosphate esters, polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, sucrose fatty acid ester, polyglycerin fatty acid ester, alkyl glycosides, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester , Non-ionic surfactants such as alkyldimethylamine oxide, betaine acetate-type amphoteric surfactants such as betaine alkyldimethylaminoacetate and betaine fatty acid amidopropyldimethylaminoacetate, N-fatty acid acyl-N-carboxymethyl-N-hydroxy Examples include imidazoline-type amphoteric surfactants such as ethylethylenediamine salt, and amino acid-type surfactants such as N-fatty acid acyl-L-alginate salt. These surfactants can be used in amounts that do not interfere with the effects of the present invention. In the composition of the present invention, sugar alcohols such as xylitol, sorbitol, maltitol, mannitol, lactitol, erythritol, and palatinit can be blended as long as the effects of the present invention are not impaired.

The composition of the present invention further comprises sweeteners such as, for example, saccharin sodium, stevioside, neohesperidihydrochalcone, dipotassium glycyrrhizinate, perillartin, thaumatin, asparatylphenylalanine methyl ester, sucrose, fructose, sodium saccharinate and the like. , Bactericides such as cetylpyridinium chloride, penzalkonium chloride, benzethonium chloride, non-cationic bactericides such as triclosan, anti-inflammatory agents such as epsilon aminocaproic acid, tranexamic acid, dextranase, amylase, protease, mutanase, lysozyme , Lytic enzymes, enzymes such as litechenzymes, chlorohexidine salts, copper gluconate, hydrocholesterol, glycyrrhetin salts, glycyrrhetinic acid, chlorophyll, caropecta De, vitamins, azulene, lysozyme chloride, anti-tartar agents, anti-plaque agents, potassium nitrate, may be blended aluminum lactate and the like. In addition, the addition amount of these optional components can be a usual amount as long as the effect of the present invention is not hindered. Further, as an abrasive, calcium carbonate, magnesium carbonate, dibasic calcium hydrogen phosphate, calcium pyrophosphate, insoluble calcium metaphosphate, silicic anhydride, aluminum hydroxide and the like can be blended.

The effervescent solid composition for oral cavity of the present invention can be used in the form of tablets, pills, granules, powders, dentifrices and the like, though not particularly limited.

The method for directly containing the foamable oral solid composition of the present invention into the oral cavity is most suitable. However, even after adding a small amount of water, the method for including it in the oral cavity can provide a sufficient effect. .

[0018]

The effervescent oral solid composition of the present invention is an effervescent oral solid composition which has good quality stability during storage and has an excellent feeling in use while suppressing acidity during use.

[0019]

EXAMPLES The present invention will be specifically described below with reference to comparative examples and examples, but the present invention is not limited to these examples.

Examples 1 to 5, Comparative Examples 1 to 4 [Evaluation of feeling of use] For the foamable solid mouthwash shown in Table 1, the subject 1
Sensory evaluation was performed on the feeling of use by 0 persons. (1) 1 g of the sample described in Table 1 is contained in the mouth, rinsed with a foam foamed by the moisture of saliva for 30 seconds, and exhaled. (2) The sourness during and after use is 5
The evaluation was performed on a scale, and the average score of 10 persons was obtained. “Sourness during and after use” 5: No sourness is felt. 4: Sourness is slightly felt, but there is no problem in use. 3: Sourness is slightly felt, but within the allowable limit for use. 2: Feels sour and difficult to use. 1: A considerable amount of acidity is felt and cannot be used. II. 1 g of the effervescent solid mouthwash shown in Table 1 was filled in a polyethylene-laminated aluminum foil bag-shaped container, sealed, and stored in a constant temperature bath at 40 ° C. for one month. did. “Swelling of container after storage at 40 ° C. for 1 month” ：: Almost no swelling Δ: Slightly swelling X: Very swelling

[0021]

[Table 1]

The specific contents of the components shown in the table are as follows. (1) PVP coating / partially neutralized citric acid (pH
3.8) p of aqueous solution when dissolved at 1% concentration in water at 25 ° C
The product obtained by partially neutralizing citric acid with sodium carbonate so that H becomes 3.8 was converted to polyvinylpyrrolidone (ISP).
Co., Ltd., "PVP K = 30"). In this case, the amount of the coating is 2% with respect to the whole coating. (2) PVP coating, partially neutralized malic acid (pH
3.8) p of aqueous solution when dissolved at 1% concentration in water at 25 ° C
Malic acid was partially neutralized with sodium carbonate so that H became 3.8, and then polyvinylpyrrolidone (I.S.P.
Co., Ltd., "PVP K = 30"). In this case, the amount of the coating is 2% with respect to the whole coating. (3) PVP coating / citric anhydride (pH 2.
5) p of aqueous solution when dissolved at 1% concentration in water at 25 ° C
This shows a coating of citric anhydride having an H of 2.5 with polyvinylpyrrolidone (“PVP K = 30”, manufactured by ISP). In this case, the amount of the coating is 2% with respect to the whole coating. (4) Citric anhydride (pH 2.5) p of an aqueous solution when dissolved at a concentration of 1% in water at 25 ° C.
2 shows citric anhydride in which H is 2.5. (5) Malic acid (pH 2.5) p of an aqueous solution when dissolved at a concentration of 1% in water at 25 ° C
Shows malic acid where H is 2.5.

From the results in Table 1, it is found that Examples 1 to 5 according to the present invention were used.
It can be seen that the foamable oral solid composition of No. 5 has significantly improved quality stability in which the foaming reaction during the storage period in the container has been suppressed. Also, it can be seen that a high feeling of use can be obtained by improving the acidity.

Examples of the formulation of the effervescent solid composition of the present invention are shown in Examples 6 to 12.

Example 6 Sodium Bicarbonate 16 (%) Partially Neutralized Sodium Citrate 20 (Partially Neutralized with Sodium Carbonate, PVP K-30 2% Coating) Sodium Fluoride 0.2 Xylitol 45 Powder Flavor (30% (Including menthol) 3 Saccharin sodium 0.1 Sucrose stearic acid ester 1 Lactite Residual total 100% A foamable solid composition for the oral cavity was prepared in which a total of 1 g was contained in a polyethylene laminated aluminum foil bag.

Example 7 Sodium hydrogencarbonate (granules) 25 (%) Partially neutralized citric acid 40 (partially neutralized with sodium carbonate, PVP K-30 2% coating) Stevia extract 0.1 Sodium monofluorophosphate 0 2.5 Powdered flavor (containing 30% menthol) 2.5 Powdered flavor (containing 20% lemon oil) 1 Xylitol 28 Sucrose stearate 2 Corn starch Residual total 100% A total of 1 g was contained in a polyethylene laminated aluminum foil bag. An effervescent solid oral composition was prepared.

Example 8 15% sodium bicarbonate Partially neutralized citric acid 40 (partially neutralized with sodium carbonate, PVP K-30 2% coating) Powdered alcohol (including 30% ethanol) 5 Saccharin sodium 0.1 Cetylpyridinium chloride 0.01 Sorbit 15 Lauryl glycoside 1 Powdered flavor (including 30% menthol) 2.5 Sodium fluoride 0.05 Xylitol Residual total 100% Solid foam mouthwash with 1 g of total amount contained in polyethylene laminated aluminum foil bag An agent was prepared.

Example 9 Sodium hydrogen carbonate 30 (%) Partially neutralized citric acid 42 (Partially neutralized with sodium carbonate, PVP K-30 2% coating) Stevia extract 0.2 Maltitol 15 Powder flavor (30% menthol) 2.5 Xylitol 10 Dye (Blue No. 1) 0.002 Dextrin Residual Total 100% A solid foam mouthwash containing a total of 1 g in a polyethylene-laminated aluminum foil bag was prepared.

Example 10 Sodium hydrogen carbonate 25 (%) Partially neutralized citric acid 20 (Partially neutralized with sodium carbonate, PVP K-30 2% coating) Partially neutralized malic acid 15 (Partially neutralized with sodium carbonate , PVP K-30 2% coating) Stevia extract 0.15 xylitol 30 powder flavor (including 30% menthol) 3.5 dextranase 0.1 α-cyclodextrin 2 PVP K-30 Residual amount Total 100% 1 g of the components are mixed, and the diameter is 15 mm by a tableting machine.
Tablets were prepared.

Example 11 Sodium Bicarbonate 10 (%) Partially Neutralized Citric Acid 20 (Partially Neutralized with Sodium Carbonate, PVP K-30 2% Coating) Sodium Dihydrogen Phosphate 60 Sodium Lauryl Sulfate 0.2 Powder Fragrance (including 30% menthol) 3.0 Dye (Blue No. 1) 0.005 Methyl paraben 0.05 Mannitol Residual total 100% The above total components (1 g) were mixed to prepare a powder toothpaste.

[Procedure amendment]

[Submission date] April 11, 2001 (2001.4.1
1)

[Procedure amendment 1]

[Document name to be amended] Statement

[Correction target item name] Full text

[Correction method] Change

[Correction contents]

[Document Name] Statement

[Title of the Invention] Foamable solid composition for oral cavity

[Claims]

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a partially neutralized solubilized carbonate and water having a pH of 3.5 to 5.0 when dissolved in water.
The present invention also relates to an effervescent oral solid composition containing a partially neutralized organic acid whose surface is coated with a water-soluble polymer.

[0002]

2. Description of the Related Art Conventionally, a solid foamable oral composition is a solid preparation containing a carbonate and an organic acid as a foaming component, and has an excellent refreshing sensation when placed directly in the oral cavity. There are known oral compositions (for example, JP-A-3-279321). In addition, an oral composition containing a foaming component, a heat absorbing agent and 1-menthol to obtain an excellent refreshing sensation, and a solid preparation containing a large amount of a heat absorbing agent to enhance the refreshing sensation (JP-A-7-238008) Gazette) is also known.

[0003] In the form of such an effervescent solid preparation, solid carbonates and organic acids are usually used as the effervescent component. The foaming reaction in the packaging material during storage causes blistering and rupture of the container, and the foaming action in the mouth, which is a characteristic function of the product, is lost. There are drawbacks. Further, the compounding amount of the organic acid in the effervescent solid preparation is large, and when the amount of the organic acid is excessive, the acidity becomes strong and the feeling of use is deteriorated.

On the other hand, for the purpose of suppressing the foaming reaction in the packaging material during storage, for example, a foamable solid composition for oral cavity using a carbonate and an organic acid coated with a hydrophobic polymer (Japanese Patent Application Laid-Open No. Hei 7-238008) ) Is disclosed, but in this case, the reactivity between the carbonate and the organic acid is reduced at the time of use, a sufficient foaming action cannot be obtained, and the sourness is not sufficiently improved. Therefore, there is a problem that a strong acidity is generated at the time of use, and it is not sufficiently satisfactory in use feeling. From the above, we have improved the quality stability during storage,
There is a demand for the development of an effervescent solid composition for oral use that has a reduced feeling of strong acidity during use and has an excellent feeling in use.

[0005]

SUMMARY OF THE INVENTION The present invention improves the quality stability of a product by suppressing the reaction between a carbonate and an organic acid during storage, and further suppresses the acidity during use. An object of the present invention is to provide an effervescent solid composition for the oral cavity with excellent feeling.

[0006]

Means for Solving the Problems The inventors of the present invention have made intensive studies to solve the above-mentioned problems, and as a result, the pH of (A) carbonate and (B) the pH at the time of dissolving in water were 3.5 to 5.5. By blending a partially neutralized organic acid that is partially neutralized to be 0 and surface-coated with a water-soluble polymer, the quality stability during storage is good, the acidity during use is suppressed, and the feeling of use is reduced. The present inventors have found that a good foamable oral solid composition can be obtained, and have accomplished the present invention. That is, according to the present invention,
(A) pH of 3.5 to 5.0 upon dissolution of carbonate and (B) water.
And a partially neutralized organic acid surface-coated with a water-soluble polymer to provide a foamable solid composition for oral cavity.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION The present invention has a pH of 3.
It is characterized by using a partially neutralized organic acid which is partially neutralized to 5 to 5.0 and is surface-coated with a water-soluble polymer. In the composition of the present invention, the reaction between the carbonate and the organic acid during storage of the preparation is suppressed, the solubility by the water in the mouth is kept high, and the acidity during use is maintained without lowering the foaming property. Is suppressed.

[0008] The carbonate (A) is not particularly limited as long as it can be used for the oral cavity and generates carbon dioxide when dissolved in the oral cavity. Examples of such a carbonate include sodium carbonate, sodium hydrogen carbonate, potassium carbonate, potassium hydrogen carbonate, ammonium carbonate, sodium sesquicarbonate and the like. Of these, sodium carbonate, sodium hydrogen carbonate and potassium carbonate are particularly preferred. These carbonates can also be used as granules by a commonly used production method. These carbonates can be used alone or as a mixture of two or more. Carbonate is 1-50% of the total amount of the composition,
In particular, it is preferably set to 5 to 40%.

(B) Partially neutralized organic acids which are partially neutralized so as to have a pH of 3.5 to 5.0 when dissolved in water and which are surface-coated with a water-soluble polymer include those conventionally known, For example, sodium or potassium partially neutralized products of organic acids such as citric acid, malic acid, and tartaric acid, and these partially neutralized organic acids are obtained by neutralizing the corresponding organic acids with sodium hydroxide or sodium carbonate by a conventional method. After the treatment, the degree of neutralization is adjusted so that the pH at the time of dissolution in water (25 ° C., 1%) becomes 3.5 to 5.0, and dried by a conventional method to obtain a powder or granules. be able to. As the water-soluble polymer for coating, conventionally known ones, for example, hydroxyethyl cellulose, hydroxypropyl cellulose,
Examples thereof include sodium carboxymethylcellulose, polyethylene glycol, and polyvinylpyrrolidone. The average molecular weight of the polymer is usually 5,000 to 1,500.
It is about 000. The amount of the water-soluble polymer is 0.5 to 2 with respect to the amount of the partially neutralized organic acid coated on the surface.
It is preferably 0%, particularly preferably 1 to 5%. As the organic acid salt having such a surface coating, in particular, sodium partially neutralized citric acid adjusted to have a pH of 3.5 to 4.5 when dissolving citric anhydride in water is, for example, vacuum-coated. Using a machine (manufactured by Kikusui Seisakusho) etc.,
Those surface-coated with polyvinylpyrrolidone are preferred. As polyvinylpyrrolidone, those having an average molecular weight of about 40,000, for example, PVP K-30 (I.
S. (Company P) coated with 1 to 2% is particularly preferable. Such partially neutralized organic acids can be used alone or as a mixture of two or more.

The pH at the time of dissolution (B) of the present invention is 3.5 to 3.5.
The partially neutralized organic acid partially neutralized so as to be 5.0 and coated with a water-soluble polymer on the surface is dissolved in water (2
It is important that the pH (5 ° C., 1%) is 3.5 to 5.0, and more preferably 3.5 to 4.5. p
When H exceeds 5.0, the foaming amount in the mouth decreases and the feeling of use deteriorates. When the pH is less than 3.5, the feeling of use becomes extremely poor due to strong acidity and residual feeling during use, and foaming reaction occurs during storage. In addition, the swelling or rupture of the packaging material occurs, and the quality stability of the product cannot be maintained. The pH of an unneutralized organic acid such as citric acid itself when dissolved in water is slightly less than 3, which includes the above-mentioned problems.

The effervescent oral solid composition of the present invention preferably does not contain a water-insoluble solid such as an abrasive, and can be made substantially entirely water-soluble. This is a method of foaming in the mouth, washing the mouth, and discharging in order to improve the usability of the composition of the present invention and enhance the effect of improving the usability. As a result, unpleasant insoluble residues are not left in the mouth after ejection, and water rinsing after use is unnecessary, and convenience can be improved.

The foamable oral solid composition of the present invention may contain a powdered fragrance as a refreshing and aromatic component. The powdered flavor is not particularly limited in its production method, components and the like, and various powdered flavors can be used. As such, for example, dextrin,
Examples thereof include those contained in a base such as gum arabic and gelatin. On the other hand, as oily flavors, 1-menthol,
Carvone, anethole, eugenol, methyl salicylate, spearmint oil, peppermint oil, wintergreen oil, lemon oil, orange oil, grapefruit oil,
Sage oil, rosemary oil, cinnamon oil, pimento oil, cinnamon oil, perilla oil, winter green oil, clove oil, eucalyptus oil, strawberry flavor, orange flavor, lemon flavor, apple flavor, panana flavor, pineapple flavor, etc. .

The composition of the present invention may contain various auxiliary ingredients in addition to the above-mentioned perfume ingredients. The composition of the present invention may contain a fluorine-containing component. Examples of such a material include sodium fluoride, ammonium fluoride, potassium fluoride, lithium fluoride, tin fluoride, sodium monofluorophosphate, ammonium monofluorophosphate, potassium monofluorophosphate, and monofluorophosphate. Examples thereof include fluorine-containing natural products containing lithium such as lithium, seaweed, seaweeds and tea, and extracts thereof. These can be used alone or in combination of two or more.
Preferably, sodium fluoride and sodium monofluorophosphate are good. The concentration of fluorine at which these fluorine-containing components act in the oral cavity is preferably not more than 1,000 ppm, and particularly preferably 1 to 250 ppm.

The composition of the present invention can contain a surfactant. Such materials include sodium lauryl sulfate, sodium dodecyl benzene sulfonate, sodium α-sulfofatty acid alkyl ester,
Anionic surfactants such as alkyl phosphate esters, polyoxyethylene hydrogenated castor oil, polyoxyethylene alkyl ether, sucrose fatty acid ester, polyglycerin fatty acid ester, alkyl glycosides, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester , Non-ionic surfactants such as alkyldimethylamine oxide, betaine acetate-type amphoteric surfactants such as betaine alkyldimethylaminoacetate and betaine fatty acid amidopropyldimethylaminoacetate, N-fatty acid acyl-N-carboxymethyl-N-hydroxy Examples include imidazoline-type amphoteric surfactants such as ethylethylenediamine salt, and amino acid-type surfactants such as N-fatty acid acyl-L-alginate salt. These surfactants can be used in amounts that do not interfere with the effects of the present invention. In the composition of the present invention, sugar alcohols such as xylitol, sorbitol, maltitol, mannitol, lactitol, erythritol, and palatinit can be blended as long as the effects of the present invention are not impaired.

The composition of the present invention further comprises sweeteners such as, for example, saccharin sodium, stevioside, neohesperidihydrochalcone, dipotassium glycyrrhizinate, perillartin, thaumatin, asparatyl phenylalanine methyl ester, sucrose, fructose, sodium saccharinate and the like. , Bactericides such as cetylpyridinium chloride, penzalkonium chloride, benzethonium chloride, non-cationic bactericides such as triclosan, anti-inflammatory agents such as epsilon aminocaproic acid, tranexamic acid, dextranase, amylase, protease, mutanase, lysozyme , Lytic enzymes, enzymes such as litechenzymes, chlorohexidine salts, copper gluconate, hydrocholesterol, glycyrrhetin salts, glycyrrhetinic acid, chlorophyll, caropecta De, vitamins, azulene, lysozyme chloride, anti-tartar agents, anti-plaque agents, potassium nitrate, may be blended aluminum lactate and the like. In addition, the addition amount of these optional components can be a usual amount as long as the effect of the present invention is not hindered. Further, as an abrasive, calcium carbonate, magnesium carbonate, dibasic calcium hydrogen phosphate, calcium pyrophosphate, insoluble calcium metaphosphate, silicic anhydride, aluminum hydroxide and the like can be blended.

The effervescent solid composition for oral cavity of the present invention can be used in the form of tablets, pills, granules, powders, dentifrices and the like, though not particularly limited.

The method for directly containing the foamable oral solid composition of the present invention into the oral cavity is most suitable. However, even after adding a small amount of water, the method for including it in the oral cavity can provide a sufficient effect. .

[0018]

The effervescent oral solid composition of the present invention is an effervescent oral solid composition which has good quality stability during storage and has an excellent feeling in use while suppressing acidity during use.

[0019]

EXAMPLES The present invention will be specifically described below with reference to comparative examples and examples, but the present invention is not limited to these examples.

Examples 1 to 5, Comparative Examples 1 to 4 [Evaluation of feeling of use] For the foamable solid mouthwash shown in Table 1, the subject 1
Sensory evaluation was performed on the feeling of use by 0 persons. (1) 1 g of the sample described in Table 1 is contained in the mouth, rinsed with a foam foamed by the moisture of saliva for 30 seconds, and exhaled. (2) The sourness during and after use is 5
The evaluation was performed on a scale, and the average score of 10 persons was obtained. “Sourness during and after use” 5: No sourness is felt. 4: Sourness is slightly felt, but there is no problem in use. 3: Sourness is slightly felt, but within the allowable limit for use. 2: Feels sour and difficult to use. 1: A considerable amount of acidity is felt and cannot be used. II. 1 g of the effervescent solid mouthwash shown in Table 1 was filled in a polyethylene-laminated aluminum foil bag-shaped container, sealed, stored in a 40 ° C constant temperature bath for one month, and then evaluated for swelling of the container in three steps. did. “Swelling of container after storage at 40 ° C. for 1 month” ：: Almost no swelling Δ: Slightly swelling X: Very swelling

[0021]

[Table 1]

The specific contents of the components shown in the table are as follows. (1) PVP coating / partially neutralized citric acid (pH
3.8) p of aqueous solution when dissolved at 1% concentration in water at 25 ° C
The partially neutralized citric acid with sodium carbonate so that H becomes 3.8 was converted to polyvinylpyrrolidone (ISP).
Co., Ltd., "PVP K = 30"). In this case, the amount of the coating is 2% with respect to the whole coating. (2) PVP coating, partially neutralized malic acid (pH
3.8) p of aqueous solution when dissolved at 1% concentration in water at 25 ° C
Malic acid was partially neutralized with sodium carbonate so that H became 3.8, and then polyvinylpyrrolidone (I.S.P.
Co., Ltd., "PVP K = 30"). In this case, the amount of the coating is 2% with respect to the whole coating. (3) PVP coating / citric anhydride (pH 2.
5) p of aqueous solution when dissolved at 1% concentration in water at 25 ° C
This shows a coating of citric anhydride having an H of 2.5 with polyvinylpyrrolidone (“PVP K = 30”, manufactured by ISP). In this case, the amount of the coating is 2% with respect to the whole coating. (4) Citric anhydride (pH 2.5) p of an aqueous solution when dissolved in water at 25 ° C. at a concentration of 1%
2 shows citric anhydride in which H is 2.5. (5) Malic acid (pH 2.5) p of an aqueous solution when dissolved at a concentration of 1% in water at 25 ° C
Shows malic acid where H is 2.5.

From the results in Table 1, it is found that Examples 1 to 5 according to the present invention were used.
It can be seen that the foamable oral solid composition of No. 5 has significantly improved quality stability in which the foaming reaction during the storage period in the container has been suppressed. Also, it can be seen that a high feeling of use can be obtained by improving the acidity.

Examples of the formulation of the effervescent solid composition of the present invention are shown in Examples 6 to 12.

Example 6 Sodium Bicarbonate 16 (%) Partially Neutralized Sodium Citrate 20 (Partially Neutralized with Sodium Carbonate, PVP K-30 2% Coating) Sodium Fluoride 0.2 Xylitol 45 Powder Flavor (30% (Including menthol) 3 Saccharin sodium 0.1 Sucrose stearic acid ester 1 Lactite Residual total 100% A foamable solid composition for the oral cavity was prepared in which a total of 1 g was contained in a polyethylene laminated aluminum foil bag.

Example 7 Sodium hydrogencarbonate (granules) 25 (%) Partially neutralized citric acid 40 (partially neutralized with sodium carbonate, PVP K-30 2% coating) Stevia extract 0.1 Sodium monofluorophosphate 0 2.5 Powdered flavor (containing 30% menthol) 2.5 Powdered flavor (containing 20% lemon oil) 1 Xylitol 28 Sucrose stearate 2 Corn starch Residual total 100% A total of 1 g was contained in a polyethylene laminated aluminum foil bag. An effervescent solid oral composition was prepared.

Example 8 15% sodium bicarbonate Partially neutralized citric acid 40 (partially neutralized with sodium carbonate, PVP K-30 2% coating) Powdered alcohol (including 30% ethanol) 5 Saccharin sodium 0.1 Cetylpyridinium chloride 0.01 Sorbit 15 Lauryl glycoside 1 Powdered flavor (including 30% menthol) 2.5 Sodium fluoride 0.05 Xylitol Residual total 100% Solid foam mouthwash with 1 g of total amount contained in polyethylene laminated aluminum foil bag An agent was prepared.

Example 9 Sodium hydrogen carbonate 30 (%) Partially neutralized citric acid 42 (Partially neutralized with sodium carbonate, PVP K-30 2% coating) Stevia extract 0.2 Maltitol 15 Powder flavor (30% menthol) 2.5 Xylitol 10 Dye (Blue No. 1) 0.002 Dextrin Residual Total 100% A solid foam mouthwash containing a total of 1 g in a polyethylene-laminated aluminum foil bag was prepared.

Example 10 Sodium hydrogen carbonate 25 (%) Partially neutralized citric acid 20 (Partially neutralized with sodium carbonate, PVP K-30 2% coating) Partially neutralized malic acid 15 (Partially neutralized with sodium carbonate , PVP K-30 2% coating) Stevia extract 0.15 xylitol 30 powder flavor (including 30% menthol) 3.5 dextranase 0.1 α-cyclodextrin 2 PVP K-30 Residual amount Total 100% 1 g of the components are mixed, and the diameter is 15 mm by a tableting machine.
Tablets were prepared.

Example 11 Sodium Bicarbonate 10 (%) Partially Neutralized Citric Acid 20 (Partially Neutralized with Sodium Carbonate, PVP K-30 2% Coating) Sodium Dihydrogen Phosphate 60 Sodium Lauryl Sulfate 0.2 Powder Fragrance (including 30% menthol) 3.0 Dye (Blue No. 1) 0.005 Methyl paraben 0.05 Mannitol Residual amount 100% The above total components (1 g) were mixed to prepare a powder toothpaste.
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[Procedure amendment]

[Submission date] April 24, 2001 (2001.4.2
4)

[Procedure amendment 1]

[Document name to be amended] Statement

[Correction target item name] 0003

[Correction method] Change

[Correction contents]

[0003] In such effervescent solid preparation, and mustard its dosage form, usually as a foaming component, if and solid carbonate and organic acid is used, the preparation of the solid formulation by these components, the formulation The foaming reaction in the packaging material during storage causes blistering and rupture of the container, and the foaming action in the mouth, which is a characteristic function of the product, is lost. There are drawbacks. Further, the compounding amount of the organic acid in the effervescent solid preparation is large, and when the amount of the organic acid is excessive, the acidity becomes strong and the feeling of use is deteriorated.

[Procedure amendment 2]

[Document name to be amended] Statement

[Correction target item name] 0009

[Correction method] Change

[Correction contents]

(B) Partially neutralized organic acids which are partially neutralized so as to have a pH of 3.5 to 5.0 when dissolved in water and which are surface-coated with a water-soluble polymer include those conventionally known, For example, sodium or potassium partially neutralized products of organic acids such as citric acid, malic acid, and tartaric acid, and these partially neutralized organic acids are obtained by neutralizing the corresponding organic acids with sodium hydroxide or sodium carbonate by a conventional method. After the treatment, the degree of neutralization is adjusted so that the pH at the time of dissolution in water (25 ° C., 1%) becomes 3.5 to 5.0, and dried by a conventional method to obtain a powder or granules. be able to. As the water-soluble polymer for coating, conventionally known ones, for example, hydroxyethyl cellulose, hydroxypropyl cellulose,
Sodium carboxymethylcellulose, polyethylene glycol, polyvinyl pyrrolidone, and the like, the average molecular weight of the polymer, usually, 5, 000-1, 50
0, it is about 000. The amount of the water-soluble polymer was 0.5 to the amount of the surface-coated partially neutralized organic acid.
-20%, particularly preferably 1-5%. As such a surface-coated organic acid salt, in particular,
The sodium partially neutralized citric acid adjusted to have a pH of 3.5 to 4.5 when dissolving citric anhydride in water is coated with polyvinylpyrrolidone using, for example, a vacuum coating machine (manufactured by Kikusui Seisakusho) or the like. Coated ones are preferred. The polyvinyl pyrrolidone, having an average molecular weight of about 40, 000, for example, PVP K-3
0 (manufactured by ISP) is particularly preferably coated with 1 to 2%. Such partially neutralized organic acids can be used alone or as a mixture of two or more.

 ──────────────────────────────────────────────────続 き Continuation of the front page (72) Inventor Ken Yamada 1-3-7 Honjo, Sumida-ku, Tokyo Inside Lion Corporation (72) Inventor Takao Yokoo 1-3-7 Honjo, Sumida-ku, Tokyo F-term in Lion Corporation (reference) 4C083 AA112 AB282 AB311 AB312 AB472 AC102 AC132 AC301 AC302 AC342 AC482 AC692 AC782 AC792 AC862 AD071 AD212 AD222 AD242 AD252 AD472 AD532 BB36 CC41 DD15 DD17 DD21 EE01 EE03 EE06

Claims (3)

[Claims] 1. A partially neutralized organic acid which is partially neutralized so that the pH at the time of dissolving (A) carbonate and (B) water is 3.5 to 5.0, and is surface-coated with a water-soluble polymer. A solid composition for an effervescent oral cavity, comprising: 2. The composition of claim 1, wherein said partially neutralized organic acid is partially neutralized citric anhydride and said water-soluble polymer is polyvinylpyrrolidone. 3. The composition of claim 1 or claim 2, wherein the composition is substantially water-soluble without water-insoluble solids.