JPS6141893B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a dentifrice composition, and more particularly, to a dentifrice composition that stably contains allantoin or an allantoin derivative in a dentifrice composition that uses a base that elutes calcium ions, such as calcium carbonate or calcium phosphate. Allantoin and allantoin derivatives (hereinafter simply referred to as allantoin) have the effect of removing necrotic tissue, are themselves low-toxic, non-irritating, and have anti-irritant and anti-allergic properties, so they are used as medicinal agents in pharmaceuticals and cosmetics. It is widely used in dentifrice compositions for the purpose of preventing alveolar pyorrhea and gingivitis. Conventionally, when allantoin is added to a dentifrice composition, it has been considered desirable to use a base that does not elute calcium ions, such as aluminum hydroxide or calcium pyrophosphate; When using a base that elutes calcium ions, such as calcium carbonate and calcium phosphate, which are often used in
The effective amount of allantoin (the amount of soluble allantoin) decreases significantly over time, and the effect of allantoin is impaired. This is thought to be because allantoin forms some kind of bond with calcium ions eluted from the base over time, forming an insoluble or poorly soluble substance. The present inventors have conducted intensive research to stably incorporate allantoin into dentifrice compositions using bases that elute calcium ions, which are often used in ordinary dentifrice compositions. They discovered that allantoin can be stabilized by coexisting with a polyphosphate, and have completed the present invention. That is, the present invention provides an allantoin-containing dentifrice composition using a base that elutes calcium ions, which is characterized in that it contains a compound selected from monofluorophosphates and polyphosphates as an allantoin stabilizer. Even if the dentifrice composition of the present invention uses a base that elutes calcium ions, the decrease in the amount of effective allantoin over time is significantly suppressed, and it is extremely effective in preventing alveolar pyorrhea and gingivitis. Demonstrates excellent effects. The mechanism of action of allantoin stabilization by monofluorophosphate or polyphosphate is not clear, but they are adsorbed onto the particle surface of a base material such as calcium carbonate or calcium phosphate, as if coating the base material. It becomes a shape,
In order to suppress the elution of calcium ions from the base material, the amount of calcium ions eluted into the dentifrice system is significantly suppressed, and the small amount of calcium ions eluted is absorbed into the monofluorophosphate and polyphosphate dissolved in the dentifrice system. This is presumed to be due to the fact that the ion form is not lost due to the chelation effect of the acid salt, and the bond with allantoin is weakened, thereby suppressing allantoin from becoming insoluble or hardly soluble. The monofluorophosphate used in the present invention has the general formula: M ₂ PO ₃ F (wherein M is sodium,
Refers to an alkali metal such as potassium or an ammonium cation. (same below), preferably
Examples include sodium monofluorophosphate, and it is preferably blended in an amount of 0.05% (weight %, the same applies hereinafter) or more to the dentifrice composition. In addition, since the physical properties of the toothpaste composition will deteriorate if added in a large amount, 0.05 to 2%,
Preferably 0.1-0.76% (approximately 130-0.76% as fluorine)
Approximately 1000ppm) range is desirable. In addition, as polyphosphates, pyrophosphate (M ₄ P ₂ O ₇ or M ₂ H ₂ P ₂ O ₇ ), tripolyphosphate (M ₅ P ₃ O ₁₀ ), trimetaphosphate (M ₃ P ₃ O ₉ ), tetrametaphosphate ( _{M4P4O12 )} , hexametaphosphate ( _M6P6O18 ), insoluble metaphosphate [( _{MPO3 ) o ] ,} or a mixture thereof. It is preferable to add 0.05% or more to the product. Note that if added in a large amount, the physical properties of the toothpaste composition will deteriorate, and if it is filled into an aluminum tube without an inner surface coating, corrosion of the inner surface of the aluminum tube will be accelerated. %, preferably in the range of 0.05 to 2% for sodium tripolyphosphate and 0.1 to 4% for insoluble sodium metaphosphate. Examples of the base used to elute calcium include calcium carbonate, dicalcium phosphate (dihydrate, anhydride), and the like. Examples of allantoin include allantoin and allantoin derivatives such as aluminum allantoinate, and the blending ratio thereof is appropriately selected depending on the formulation of the dentifrice composition, but is usually preferably in the range of 0.05 to 2%. The dentifrice composition of the present invention can be manufactured according to a conventional method,
It can be in the form of toothpaste, toothpaste ointment, water toothpaste, and the like. Other ingredients to be used may be those used in ordinary dentifrice compositions, such as foaming agents such as sodium alkyl sulfate such as sodium lauryl sulfate, sodium acylsarcosine, α-olefin sulfonate, sucrose fatty acid ester; As a binder, sodium carboxymethyl cellulose, carrageenan, sodium alginate, bentonite, silicic anhydride, etc.;
Glycerin, sorbitol, propylene glycol, sodium pyrrolidone carboxylate, polyethylene glycol, and the like are used as wetting agents. Next, the present invention will be explained in more detail with reference to Examples, but the present invention is not limited thereto. Example 1 A toothpaste was prepared according to a conventional method using the following formulation. Ingredients % Calcium carbonate 40.0 Silicic anhydride 1.5 Sodium carboxymethyl cellulose 1.2 Carrageenan 0.3 Glycerin 10.0 Sorbitol 15.0 Sodium lauryl sulfate 1.5 Sodium satucharin 0.1 Preservatives 0.1 Allantoin chlorohydroxyaluminum 0.1 Sodium monofluorophosphate 0.76 Purified water 28.44 Flavor 1.0 Example 2 A toothpaste was prepared according to the conventional method using the following formulation. Component percentage Calcium second phosphate Calcimethylcellulose sodium 1.2 Calcimethylcello sodium 1.2 Glicinan 0.0 Solbitol 15.0 Sacrillyl sodium 1.5 Satsukarin sulfate 0.1 Preservatory 0.1 Preservatory 0.1 Alantorohydroxial minium 0.1 Sodium fluorinate 0.76 purified water 28.44 fragrance 1.0 3 A toothpaste was prepared according to the conventional method using the following recipe. Ingredients % Calcium carbonate 40.0 Silicic anhydride 1.5 Sodium carboxymethyl cellulose 1.2 Carrageenan 0.3 Glycerin 10.0 Sorbitol 15.0 Sodium lauryl sulfate 1.5 Sodium satucharyl 0.1 Preservatives 0.1 Allantoin 0.1 Sodium pyrophosphate 0.5 Purified water 21.7 Flavor 1.0 Example 4 Next by prescription A toothpaste was prepared according to a conventional method. Ingredients % Dicalcium phosphate dihydrate 41.5 Sodium carboxymethyl cellulose 1.2 Carrageenan 0.3 Glycerin 10.0 Sorbitol 15.0 Sodium lauryl sulfate 1.5 Sodium saccharin 0.1 Preservative 0.1 Allantoin 0.1 Sodium pyrophosphate 0.2 Purified water 29.0 Flavor 1.0 In Examples 1 and 2 above Table 1 below shows the results of a test on the change over time in the amount of effective allantoin in the obtained dentifrice composition. The test was conducted by measuring the effective allantoin amount in the toothpaste composition sample over each day, taking the effective allantoin amount immediately after production as 100%, and calculating the percentage (%) of the effective allantoin amount remaining over each day. Summer. As a control, dentifrice compositions in which sodium monofluorophosphate was removed from the formulations of Examples 1 and 2 were used (Comparative Examples 1 and 2). The effective amount of allantoin was measured as follows. Accurately weigh approximately 1 g of the sample, add 50 ml of 0.01M barium chloride solution (Japanese Pharmacopoeia analytical standard solution, the same applies hereinafter), and
After stirring for 30 minutes at °C, centrifugation (10000 r.pm, 20
minutes). Add 70 ml of ether to this supernatant liquid, shake it, remove the aqueous layer, volatilize the ether in the aqueous layer, and dilute to 50 ml to use as a sample solution. Separately, accurately weigh 0.5 mg of allantoin chlorhydroxyaluminum (cosmetic primordium), dilute to 50 ml with 0.01M barium chloride solution, and use this as the standard solution. Subject 70 μl each of the sample solution and standard solution to high performance liquid chromatography, and calculate the peak height (HT) of the sample solution and the peak height (HS) of the standard solution, which have the same retention time as the peak of the standard solution. and calculate the effective amount of allantoin (mg) using the following formula. Effective amount of allantoin (mg) = amount of allantoin chlorhydroxyaluminum in standard solution (mg) x HT/HS

[Table] As is clear from Table 1, allantoin is stabilized by adding sodium monofluorophosphate. The following Table 2 shows the results of testing the relationship between the amount of sodium monofluorophosphate blended and the change over time in the amount of effective allantoin. The test was conducted according to the formulation of Example 1, using dentifrice compositions containing sodium monofluorophosphate at various concentrations, and calculating the residual rate of effective allantoin in the same manner as in Table 1.

[Table] As is clear from Table 2, sodium monofluorophosphate significantly stabilizes allantoin at a blending amount of 0.05% or more. Table 3 below shows the results of tests conducted in the same manner as in Table 2 for dentifrice compositions containing sodium pyrophosphate at various concentrations according to the formulation of Example 4.

[Table] As is clear from Table 3, sodium pyrophosphate also significantly stabilizes allantoin at 0.05% or more.

Claims (1)

[Scope of Claims] 1. A dentifrice composition characterized in that a dentifrice composition containing allantoin or an allantoin derivative using a base that elutes calcium ions is blended with a compound selected from monofluorophosphates and polyphosphates. . 2. The dentifrice composition according to claim 1, which contains the compound in an amount of 0.05% by weight or more. 3. The dentifrice composition of claim 1 or 2, wherein the compound is sodium monofluorophosphate. 4 Sodium monofluorophosphate 0.1-0.76
The dentifrice composition according to claim 3, which contains % by weight. 5. The toothpaste according to claim 1 or 2, wherein the compound is selected from pyrophosphate, tripolyphosphate, trimetaphosphate, tetrametaphosphate, hexametaphosphate, insoluble metaphosphate and mixtures thereof. Composition. 6. The dentifrice composition according to claim 5, which contains 0.05 to 2% by weight of sodium pyrophosphate.