JPS644485B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a toothpaste containing at least one compound selected from guaiazulene and its sulfonate and an aluminum salt. Guaiazulene and its sulfonate (hereinafter referred to as "azulene compounds") used in the present invention
) is expressed by the following general formula. In the formula, R represents a hydrogen atom or _-SO3M . M
represents an alkali metal or an alkaline earth metal, such as Na, K, Ca, Mg, etc. Azulene compounds have anti-inflammatory, anti-allergic, antibacterial, and tissue-regenerating properties, and have been confirmed to be effective in the treatment and prevention of oral diseases, particularly stomatitis, lip mucositis, and periodontitis. It is widely used as an agent. Therefore, it is clear that the inclusion of azulene compounds having such properties in toothpaste is beneficial for the prevention and treatment of oral diseases. However, azulene compounds have the disadvantage that they are gradually decomposed and discolored by light and oxygen in the air. For this reason, even if an azulene compound is blended into regular toothpaste, it will be decomposed by light and air, changing the color tone of the product and reducing its medicinal efficacy.
To prevent this, complicated operations such as light shielding and oxygen removal are required. Therefore, an object of the present invention is to provide an azulene compound-containing toothpaste that is stable against light and oxygen. Another object of the present invention is to provide an azulene compound-containing toothpaste that is effective in preventing or treating various oral diseases. As a result of intensive research in view of the above-mentioned purpose, the present inventor obtained the knowledge that adding an aluminum salt to a toothpaste containing an azulene compound stabilizes the azulene compound blended in the toothpaste, and was able to complete the present invention. Ivy. The toothpaste of the present invention is characterized in that the azulene compound and aluminum salt are blended into a regular toothpaste. Specific examples of the azulene compound used in the present invention include the following compounds. Guaiazulene Sodium guaiazulene sulfonate Potassium guaiazulene sulfonate Calcium guaiazulene sulfonate Magnesium guaiazulene sulfonate Specific examples of the aluminum salt used in the present invention include the following compounds. Aluminum lactate, aluminum phosphate, aluminum sulfate, potassium aluminum sulfate, allantoin hydroxychloraluminum, aluminum stearate, aluminum chloride Among the above aluminum salts, particularly preferred are aluminum phosphate and aluminum lactate. The amount of azulene compound added to dentifrice is limited by formulation issues such as product viscosity and uniformity, but generally 0.001 to 5.0% by weight is appropriate;
Particularly preferred is 0.01 to 2.0% by weight. In addition, the amount of aluminum salt added to stabilize the azulene compound may be appropriately determined by considering the amount of the azulene compound added, the viscosity of the product, the uniformity, etc., but in general, 0.01 to 10% by weight is suitable. It is. In particular, when the amount of the azulene compound added is 0.01 to 2.0% by weight, the amount of the aluminum salt added is preferably in the range of 0.1 to 5.0% by weight. The dentifrice composition of the present invention is completely the same as a general dentifrice composition except that it contains an azulene compound and an aluminum salt. Therefore, it may contain abrasives, wetting agents, binders, surfactants, etc. that are commonly used as base materials. The present invention will be explained in more detail below using test examples and examples. In addition, all "%" is weight%.
In the test examples, the residual rate of the azulene compound was measured as follows. 15 g of toothpaste was extracted with methanol, the extract was concentrated under reduced pressure to 25ml, and the absorbance of this solution at 575 nm was measured using a spectrophotometer to determine the residual rate of azulene in the toothpaste. Test Example 1 A toothpaste with the following formulation was prepared by adding 0.02% each of guaiazulene and sodium guaiazulene sulfonate, and 2.0% of aluminum lactate, and compared with a toothpaste without aluminum lactate. These toothpastes were stored at a temperature of 40°C and a humidity of 75%, and changes in azulene compounds over time were investigated. The one without aluminum lactate has a survival rate of 79% after 14 days.
However, the residual rates of 2.0% addition remained 98% and 97% even after 6 months, indicating that the azulene compound was sufficiently stabilized. The toothpaste formulation and test results are shown in Tables 1 and 2, respectively. Table 1 Toothpaste prescription Calcium hydrogen phosphate 40.0 Glycerin 15.0 D-sorbitol solution 10.0 Sodium carboxymethylcellulose 0.1 Sodium saccharin 0.06 Sodium lauryl sulfate 1.8 Methyl benzoate 0.1 Fragrance 0.9 Regular water Appropriate amount 100.0%

[Table] Test Example 2 0.02% sodium guaiazulene sulfonate was added to the toothpaste shown in Table 1, and various amounts of aluminum lactate were added thereto, and changes over time were investigated under conditions of 40°C and 75% humidity. The results are shown in Table 3.

[Table] It can be seen that the azulene compound is stable at 0.10 to 5.00%. Test Example 3 Next, the stability was investigated by varying the amount of sodium guaiazulene sulfonate added. 1st
Using the table toothpaste, add a specified amount of azulene compound to 2.0% aluminum lactate, and add 40% of azulene compound.
Changes in azulene compounds over time were investigated under conditions of ℃ and 75% humidity. The results are shown in Table 4.

[Table] Test Example 4 0.02% sodium guaiazulene sulfonate was added to the toothpaste shown in Table 1, and 2% of various aluminum salts were added thereto, and the changes over time of the azulene compound were investigated under conditions of 40°C and 75% humidity. Ta. The results are shown in Table 5.

[Table] Example 1 Dibasic calcium phosphate 45.0g Glycerin 15.0g Sorbit (70% aqueous solution) 10.0g Carboxymethylcellulose 1.0g Methylparaben 0.1g Aluminum lactate 1.0g Sodium guaiazulene sulfonate 0.05g Sodium saccharin 0.1g Sodium lauryl sulfate 1.8g Fragrance Material: 0.9g Make total amount to 100g with water. Example 2 Sodium chloride 10.0g Dicalcium phosphate 35.0g Glycerin 18.5g Propylene glycol 2.5g Sodium carboxymethylcellulose 1.0g Methylparaben 0.1g Aluminum lactate 1.5g Sodium guaiazulene sulfonate 0.1g Sodium lauryl sulfate 1.5g Fragrance 0.9g Total amount 100g with water shall be. Example 3 Sodium chloride 10.0g Calcium pyrophosphate 33.0g Silicic anhydride 3.0g Glycerin 25.0g Carboxymethylcellulose 1.09 Methylparaben 0.1g Aluminum lactate 0.5g Sodium guaiazulene sulfonate 0.02g Sodium lauryl sulfate 1.0g Fragrance 0.9g Make the total amount to 100g with water . Example 4 Dibasic calcium phosphate 32.0g Silicic anhydride 5.0g Glycerin 15.0g Sorbit (70% aqueous solution) 10.0g Sodium alginate 0.6g Carrageenan 0.5g Alkylolamide 2.0g Sodium saccharin 0.1g Sodium lauryl sulfate 1.5g Sodium lauroylsarcosine 0.3 g Aluminum lactate 5.0g Sodium guaiazulene sulfonate 0.1g Flavor 0.9g Add water to bring the total amount to 100g. Example 5 Sodium chloride 10.0g Dicalcium phosphate 35.0g Glycerin 18.0g Propylene glycol 4.0g Sodium alginate 0.5g Carrageenan 0.5g Methylparaben 0.1g Sodium lauryl sulfate 1.5g Aluminum phosphate 2.0g Sodium guaiazulene sulfonate 0.05g Fragrance 0.9g Water The total amount is 100g. Example 6 Calcium pyrophosphate 30.0g Silicic anhydride 2.0g Glycerin 25.0g Sodium carboxymethylcellulose 1.0g Methylparaben 0.1g Sodium saccharin 0.1g Sodium lauryl sulfate 1.0g Sodium lauroylsarcosinate 0.3g Aluminum phosphate 0.5g Sodium guaiazulene sulfonate 0.005g Fragrance Material: 0.9g Make total amount to 100g with water. Example 7 Dibasic calcium phosphate 40.0g Silicic anhydride 5.0g Polyethylene glycol 400 5.0g Glycerin 20.0g Carboxymethyl cellulose 0.3g Carrageenan 0.8g Sodium lauryl sulfate 1.5g Aluminum stearate 0.1g Sodium guaiazulene sulfonate 0.05g Flavor 1.0g With water The total amount is 100g. Example 8 Sodium chloride 5.0g Calcium pyrophosphate 30.0g Silicic anhydride 5.0g Glycerin 19.0g Sorbit (70% aqueous solution) 6.0g Sodium lauryl sulfate 1.5g Sodium lauroylsarcosine 0.2g Sodium carboxymethyl cellulose 1.0g Methylparaben 0.1g Sodium saccharin 0.1g Potassium aluminum sulfate 0.05g Sodium guaiazulene sulfonate 0.1g Flavor 0.9g Make total amount 100g with water. Example 9 Dibasic calcium phosphate 30.0g Aluminum hydroxide 10.0g Glycerin 25.0g Sodium carboxymethyl cellulose 1.0g Sodium lauryl sulfate 1.2g Methylparaben 0.1g Allantoin hydroxychloraluminum
0.2g Sodium guaiazulene sulfonate 0.01g Flavor 0.9g Make total amount to 100g with water. Example 10 Aluminum hydroxide 35.0g Silicic anhydride 5.0g Glycerin 25.0g Carboxymethylcellulose 0.7g Carrageenan 0.3g Methylparaben 0.1g Sodium satucalin 0.1g Sodium lauryl sulfate 1.8g Aluminum lactate 5.0g Sodium guaiazulene sulfonate 1.0g Flavor 0.9g Add water to make a total volume of 100g. Example 11 Aluminum hydroxide 30.0g Sodium chloride 5.0g Glycerin 20.0g Sorbit (70% aqueous solution) 5.0g Sodium carboxymethylcellulose 1.0g Sodium saccharin 0.1g Methylparaben 0.1g Sodium lauryl sulfate 1.5g Aluminum lactate 2.0g Sodium guaiazulene sulfonate 0.2 g Flavor 0.9g Add water to make total amount 100g. Example 12 Dibasic calcium phosphate 34.0g Silicic anhydride 2.0g Glycerin 19.0g Propylene glycol 5.0g Carrageenan 0.5g Sodium alginate 0.6g Alkylolamide 2.0g Methylparaben 0.05g Sodium lauryl sulfate 1.8g Sodium lauroylsarcosinate 0.3g Aluminum chloride 1.0g Guaiazulene 0.01g Flavor 0.9g Add water to make a total of 100g. Example 13 Calcium pyrophosphate 40.0g Silicic anhydride 1.0g Aluminum hydroxide 3.0g Glycerin 18.0g Sorbit (70% aqueous solution) 6.0g Sodium carboxymethylcellulose 1.0g Methylparaben 0.1g Sodium lauryl sulfate 1.8g Allantoin hydroxychloraluminum
0.5g Guaiazulene 0.1g Flavor 0.9g Make total amount to 100g with water. Example 14 Sodium chloride 5.0g Calcium carbonate 35.0g Silicic anhydride 2.0g Glycerin 15.0g Propylene glycol 5.0g Carboxymethyl cellulose 1.0g Sodium lauryl sulfate 1.5g Aluminum phosphate 5.0g Guaiazulene 0.1g Fragrance 0.9g Add water to bring the total amount to 100g . Example 15 Calcium pyrophosphate 20.0g Sodium chloride 5.0g Silicic anhydride 2.0g Glycerin 25.0g Sodium carboxymethylcellulose 1.2g Ethylparaben 0.1g Sodium saccharin 0.1g Sodium lauryl sulfate 1.8g Sodium lauroylsarcosinate 0.5g Aluminum lactate 1.0g Guaiazulene 0.5g Fragrance 0.9g Make total amount to 100g with water. Example 16 Dicalcium phosphate 32.0g Sodium chloride 5.0g Silicic anhydride 2.0g Glycerin 10.0g Polyethylene glycol 400 15.0g Sodium carboxymethyl cellulose 1.0g Satucharin sodium 0.1g Aluminum phosphate 1.0g Guaiazulene 0.05g Flavor 0.9g Total amount with water The weight shall be 100g. Example 17 Calcium pyrophosphate 15.0g Crystalline cellulose 10.0g Sodium chloride 5.0g Glycerin 25.0g Carboxymethyl cellulose 1.5g Sodium saccharin 0.05g Sodium lauryl sulfate 1.8g Aluminum lactate 2.0g Guaiazulene 0.01g Flavor 0.9g Dilute to 100g with water . Example 18 Calcium carbonate 40.0g Silicic anhydride 3.0g Glycerin 20.0g Sodium carboxymethylcellulose 1.0g Sodium saccharin 0.1g Aluminum chloride 0.1g Guaiazulene 0.01g Flavor 0.9g Add water to bring the total amount to 100g. Example 19 Dicalcium phosphate 20.0g Crystalline cellulose 10.0g Silicic anhydride 2.0g Sodium chloride 5.0g Sodium carboxymethyl cellulose 1.0g Glycerin 20.0g Methylparaben 0.1g Sodium lauryl sulfate 2.0g Aluminum lactate 1.5g Guaiazulene 0.1g Fragrance 0.9g Water The total amount is 100g. Example 20 Calcium pyrophosphate 37.0g Silicic anhydride 5.0g Glycerin 25.0g Satucalin sodium 0.1g Methylparaben 0.05g Sodium lauroylsarcosine 0.3g Sodium lauryl sulfate 1.8g Aluminum phosphate 2.0g Guaiazulene 0.05g Fragrance 0.9g Dilute to 100g with water do. Example 21 Silicic anhydride 20.0g Glycerin 25.0g Sorbit (70% aqueous solution) 5.0g Carboxymethylcellulose 1.2g Satucharin sodium 0.1g Methylparaben 0.05g Aluminum lactate 1.0g Sodium guaiazulene sulfonate 0.05g Sodium lauryl sulfate 1.0g Fragrance 0.9g Add water to make a total volume of 100g. Example 22 Dibasic calcium phosphate 43.0g Silicic anhydride 5.0g Glycerin 19.0g Sodium carboxymethylcellulose 1.2g Methylparaben 0.1g Aluminum lactate 1.0g Potassium guaiazulene sulfonate 0.1g Sodium lauryl sulfate 0.9g Fragrance 0.9g Make the total amount to 100g with water. Example 23 Calcium pyrophosphate 42.0g Silicic anhydride 5.0g Glycerin 19.0g Sorbit (70% aqueous solution) 6.0g Carboxymethylcellulose 1.0g Aluminum lactate 2.0g Potassium guaiazulene sulfonate 0.1g Fragrance 0.9g Sodium lauryl sulfate 1.0g Total amount with water 100g shall be. Example 24 Dibasic calcium phosphate 35.0g Sodium chloride 5.0g Glycerin 20.0g Sodium carboxymethylcellulose 1.0g Methylparaben 0.05g Aluminum lactate 1.5g Magnesium guaiazulene sulfonate 0.3g Sodium lauryl sulfate 0.8g Sodium lauroylsarcosine 0.3g Fragrance 0.9g Total volume with water The weight shall be 100g.

Claims (1)

[Scope of Claims] 1. A toothpaste containing at least one of guaiazulene and its sulfonate represented by the following general formula and an aluminum salt. In the formula, R represents a hydrogen atom or _-SO3M (M represents an alkali metal or an alkaline earth metal). 2. The toothpaste according to claim 1, wherein R is a hydrogen atom. 3. The toothpaste according to claim 1, wherein R is _-SO3Na . 4. The toothpaste according to claim 1, wherein R is _-SO3K . 5. The toothpaste according to claim 1, comprising 0.01 to 2.0% by weight of at least one of guaiazulene and its sulfonate, and 0.1 to 5.0% by weight of an aluminum salt. 6. The toothpaste according to claim 5, wherein the aluminum salt is aluminum lactate. 7. The toothpaste according to claim 5, wherein the aluminum salt is aluminum phosphate.