JPS5835962B2 - toothpaste composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a dentifrice composition, and more particularly to a dentifrice composition that has excellent hemostatic effects.

In general, tooth brushing is used not only to clean the oral cavity, remove bad breath, and beautify teeth, but also to prevent cavities and periodontal diseases (typically pyorrhea). .

Toothpaste used to prevent cavities and periodontal diseases contains various medicinal agents, such as fluorine compounds and dextranase, and hinokitiol and aluminum to prevent periodontal diseases. Allantoin, lysozyme, azulene, common salt, vitamin E derivatives, and anti-plasmin agents such as ε-aminocaproic acid and tranexamic acid are included.

Among these, periodontal disease, especially alveolar pyorrhea, is a disease that progresses slowly but steadily without any painful or subjective symptoms.Subjective symptoms include sticky saliva, strong bad breath, and gum disease. Bleeding is said to be the most common complaint, and to prevent this bleeding, it is a good idea to add salt as a medicinal agent to your toothpaste. It is said that

However, in order to achieve the desired effect, it is necessary to incorporate a high concentration of salt, which has the disadvantage that the toothpaste has a very specific taste.

The present inventors focused on tannic acid, which has been said to have a bleeding effect since ancient times, and believed that if it was stably incorporated into toothpaste, a toothpaste with excellent hemostatic effects without the above-mentioned drawbacks could be obtained, I have done extensive research.

The structure of tannic acid is still not fully elucidated, but it is presumed to be an ester bond between the five hydroxyl groups of glucose and the free carboxyl group of galloyl gallic acid.
It has many phenolic hydroxyl groups and is extremely chemically unstable.

Therefore, if tannic acid is added to ordinary toothpaste, the toothpaste will be colored black and its commercial value will be completely lost.

However, surprisingly, this coloring caused by tannic acid, which could not be prevented when using calcium carbonate or calcium diphosphate, which are commonly used as polishing bases,
It has been found that the problem can be sufficiently suppressed by using a well-known aluminum hydroxide as a polishing base and adding ascorbic acid and a specific carboxylic acid.

The present invention was completed based on this knowledge, and uses aluminum hydroxide as the main polishing base, tannic acid as the medicinal agent, and ascorbic acid as its stabilizer.
A dentifrice composition containing a carboxylic acid selected from the group consisting of citric acid, gluconic acid, succinic acid, tartaric acid, lactic acid, malic acid and oxalic acid is provided.

The dentifrice composition of the present invention sufficiently suppresses discoloration due to the combination of tannic acid, does not exhibit a specific taste like dentifrices containing salt (and exhibits an extremely excellent hemostatic effect).

Table 1 below shows the results of examining the coloring and other properties (hardness of squeezing, texture of paste, solid-liquid separation) of various dentifrice compositions containing tannic acid.

The dentifrice composition used was prepared by blending the abrasive, citric acid, and L-ascorbic acid shown in Table 1 below according to the formulation in Example 1 below (tannic acid content: 1.0%). .

The results shown in Table 1 show that these dentifrice compositions were heated to 55°C for 1 hour.
The coloring and other properties after holding for a month were evaluated according to the following methods and criteria.

★★ In advance, a panel of three experts who standardized the evaluation criteria using standard samples squeezed out approximately 15 (1772) pieces of toothpaste from a tube on a piece of white paper, and evaluated the toothpaste's coloring, skin gloss, and solid-liquid separation. The degree was evaluated visually.

At that time, the hardness of squeezing out of the tube was also evaluated.

All evaluations were carried out in accordance with the majority opinion of the three panelists, and the coloring evaluation was performed under high fidelity natural daylight white fluorescent light.

Coloring ○: Coloring is sufficiently suppressed.

△: Coloring tolerance limit.

×: Significant coloring.

Other properties (hardness of squeezing, gloss of paste, solid-liquid separation) ○: There are no particular problems in terms of properties other than coloring.

△Two permissible limits as a product.

×: Gas generation, solidification, etc. occur, and the commercial value is greatly impaired.

As shown in Table 1, when calcium carbonate is used as a base, the coloring caused by tannic acid cannot be suppressed at all even if citric acid and L-ascorbic acid are added, and carbon dioxide gas is generated, reducing the commercial value. Not at all.

Also, when calcium diphosphate is used as a base, coloring can be suppressed to some extent when the concentrations of citric acid and L-ascorbic acid are relatively high, but solidification etc. occur, making it unsuitable as a commercial product.

On the other hand, when aluminum hydroxide is used as the base, coloring caused by tannic acid is sufficiently suppressed by adding citric acid and L-ascorbic acid, and the commercial value is not impaired.

Further, Table 2 shows the results of similar studies using other carboxylic acids.

As shown in these results, carboxylic acids other than citric acid also exhibit similar effects to citric acid.

Thus, in the dentifrice composition of the present invention, aluminum hydroxide is blended as the main polishing base.

The aluminum hydroxide to be used may be any of those commonly used as polishing bases, and its blending ratio may be at the level normally employed. %, hereinafter the same).

In the present invention, polishing bases other than calcium carbonate and calcium diphosphate, such as silicic anhydride, calcium pyrophosphate, insoluble sodium metaphosphate, silicate, and plastic powder, are used in combination with aluminum hydroxide. The polishing force may be adjusted by

As tannic acid, commonly used tannic acid obtained from pentagrams or gallic acid may be used, and its blending ratio can be selected as appropriate depending on the desired effect, but it is usually 0% based on the total amount of the composition.
．． It is preferable to mix 5 to 2.0%.

Ascorbic acid is usually 0.05 to 0.05 to the total amount of the composition.
It is preferable to mix 0.5%.

If it is blended in an amount of 0.5% or more, coloring may occur instead.

In addition, as carboxylic acids, as mentioned above, citric acid,
Examples include gluconic acid, succinic acid, tartaric acid, lactic acid, malic acid, and oxalic acid, and these can be used alone or in combination of two or more.

Although the blending ratio can be selected as desired, it is usually blended in an amount of 0.05 to 1.0% based on the total amount of the composition.

If a large amount is added, the pH of the composition will decrease, and one of the ingredients
It is preferable to use the above-mentioned blending ratio in view of the fact that the binder, which is the main component, is likely to decompose and the stability of the composition is likely to be impaired.

The dentifrice composition of the present invention can be prepared as toothpaste, powdered toothpaste, or
It can be in a dosage form such as a liquid toothpaste.

Other ingredients may be those normally added to these ingredients, such as wetting agents such as glycerin and Sorbi-/1, foaming agents such as sodium lauryl sulfate, sodium acylsarcosine, and sucrose fatty acid esters, sodium carboxymethyl cellulose, carrageenan, Contains binders such as sodium alginate and bentonite, sweeteners, and flavoring agents.

The dentifrice composition of the present invention further includes sodium monofluorophosphate, stannous fluoride, ε-aminocaproic acid, aluminum allantoinate, chlorhexidine, salt, tranexamic acid, vitamin E derivatives, chlorophyll,
Medicinal agents such as dextranase and polyvinylpyrrolidone may be added.

Next, the present invention will be explained in more detail with reference to Examples.

Example 1 Toothpaste was obtained in a conventional manner according to the following recipe.

Ingredients % Aluminum hydroxide 45.0 Sodium carboxymethyl cellulose 0.5 Carrageenan 0.5 Glycerin
10.0 Sorbitol
10.0 water
29.1 Sucrose fatty acid ester
2.0 Sodium lauroyl sarcosine 0.5 Flavoring 0.8 Tannic acid 1.0 Sodium saccharin 0.2 Citric acid 0.2 L-ascorbic acid 0.2 Using the obtained toothpaste, the hemostatic effect is as follows. conducted a test.

(1) Selection of subjects We selected 20 men between the ages of 20 and 50 who had a significant bleeding reaction even when at rest, and 10 men from each group were selected so that they would evenly include people with the same degree of bleeding from their gums. They were divided into two groups: an experimental group and a control group.

(2) Measurement of bleeding amount Subjects in the experimental group used the toothpaste of Example 1, and subjects in the control group used a toothpaste with the formulation of Example 1 except for tannic acid, and were given special flushing instructions. do not do it,
The subjects were instructed to brush their teeth after every meal using the same toothbrush, and they continued to brush their teeth for 4 weeks.

During this period, at the beginning of the test, 1 week later, 2 weeks later, and 4 weeks later, each subject was asked to lick one portion of Hemmer Combi Stakes (urinalysis test strips manufactured by Miles Samm Co.) for 30 seconds. The amount of occult blood in saliva was measured in comparison with a colorimetric table.

The amount of occult blood for each subject is shown in Table 3 below, and the results of the significance test for oral changes are shown in Table 4* below.

The values in Table 3 are divided into occult blood levels from 1 to 10: -: 0, ±: 0.5, 10:1, 10 to 10:1.
．． 5, 10:2, 10~10+10:2.5 points, 110:3.

As is clear from Tables 3 and 4, when the tannic acid-containing toothpaste of the present invention is continuously used, the amount of bleeding decreases from about 2 weeks onwards, and an excellent hemostatic effect is exhibited.

Example 2 A toothpaste was obtained according to the following recipe according to a conventional method.

Ingredients % Aluminum hydroxide 45.0 Sodium carboxymethylcellulose 0.5% Carrageenan 0.5 Glycerin 80 Sorbitol
12. O water
286 silicic anhydride
1.5 Sodium lauryl sulfate
1,5 Flavor 0.8 Tannic acid 1.0 Saccharin sodium 0.1 Citric acid 0.3 L-ascorbic acid 0,2 Example 3 A toothpaste is obtained according to the conventional method using the following formulation.

Ingredients % Aluminum hydroxide 50.0 Sodium carboxymethyl cellulose 0.6 Carrageenan 0.4 Glycerin
130 vine beet
7,0 water
22.7 Silicic anhydride
1.5 sucrose fatty acid ester
1.8 Sodium lauroyl sarcosinate 0.5** Ingredients Flavoring Sodium saccharin tannate di-L-tartrate L-Ascorbic acid % 0.7 1.0 0.1 0.4 0.3 Example 4 According to the following recipe, according to the conventional method Get toothpaste.

Ingredients % Aluminum hydroxide 50.0 Sodium carboxymethyl cellulose 0.6 Carrageenan 0.4 Glycerin
13.0 Sorbitol
7.0 water
24.9 Sodium lauryl sulfate 1.5 Fragrance 0.
9 Tannic acid 1.0 Satucalin sodium 0.1 di-
Tartaric acid 0.4 L-Ascorbic acid 0.2 A panel of five experts evaluated the flavor of toothpaste obtained by changing the concentration of tannic acid in the formulation of Example 1.
Shown in the table.

As shown in Table 5, The amount of tannic acid If it exceeds 2.0%, the usability deteriorates significantly.

Claims (1)

[Scope of Claims] 1 A dentifrice composition using aluminum hydroxide as the main polishing base contains 0.5 to 2.0% by weight of tannic acid, 0.05 to 0.5% by weight of ascorbic acid, citric acid, and gluconate. 0.05 to 1 carboxylic acid selected from the group consisting of acid, co-phosphoric acid, tartaric acid, lactic acid, malic acid and oxalic acid
．． A toothpaste composition characterized in that it contains 0% by weight. 2. The composition of item 1 above, wherein the carboxylic acid is citric acid or tartaric acid.