JPS59175423A - Cariostatic agent - Google Patents

Abstract

PURPOSE:To provide a safe cariostatic agent absolutely free of side effect, by using a synthetic perfumery as it is, or combining the perfumery properly with a flavoring agent such as carboxylic acid, lactone, etc., i.e. a food flavor. CONSTITUTION:The objective cariostatic agent contains (A) one or more synthetic perfumes selected from cresyl acetate, cyclamen aldehyde, isoeugenol, methyleugenol, heriotropin, ethyl salicylate, n-decanal and p-methylacetophenone, or contains the component (A) in combination with one or more components selected from (B) one or more carboxylic acids selected from caprylic acid, lauric acid, myristic acid, palmitic acid, stearic acid, etc. and (C) one or more lactones selected from d-decalactone, d-dodecalactone, d-undecalactone, d-tridecalactone, etc. EFFECT:Excellent effect can be attained by the use of a slight amount of the agent.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an anti-caries agent, that is, an oral agent for preventing caries or inhibiting its progression.

In recent years, the prevalence of tooth decay, or dental caries, has increased significantly and has developed into a major social problem.

On the other hand, research into the cause of 1st eclipse is progressing, and the current theory is that sucrose in food undergoes changes due to the action of 1st eclipse-causing bacteria, producing insoluble and sticky glucan. It is said that there is something to do. Due to the glucans produced in this way, bacteria that cause tooth decay adhere to the tooth surface and multiply to form dental plaque. Using this plaque as a base, the bacteria within it generate acid through sugar fermentation, and the acid produces 1
The eclipse progresses. 1. To prevent cavities, there are methods to increase the resistance of teeth, methods to eliminate sucrose or use sweeteners in place of sucrose, methods to decompose insoluble glucan produced from sucrose, or methods to block the production of glucan. Possible methods include eradicating nodule-causing bacteria. Each of the above methods has its advantages and disadvantages, but since the essence of ayu caries is an infection caused by bacteria that cause caries, the most effective way to prevent nodules is to eradicate the nodule-causing bacteria that cause this. Conceivable. The above bacteria include Streptococcus mutans
and Streptococcus sandeis (5treptococcus
ccus Sanguis). In order to prevent nodules, many attempts have been made to eliminate such bacteria that cause cavities. For example, antibiotics such as penicillin and erythromycin, cell wall lytic enzymes that lyse the cell walls of bacteria that cause Ayu erosion, and fungicides such as cyclohexidine are sometimes used. However, these have the problem of disrupting the natural bacterial balance by disturbing the oral and intestinal flora, and causing side effects. Since the problem of such side effects has not been solved, it is not suitable for widespread use. Therefore, the reality is that there is no definitive method for preventing nodules, and no preventive method has been established that is superior to the physical method of cleaning with a towel after meals. be.

In view of these circumstances, the inventors of the present invention have conducted a series of studies with the aim of preventing caries, and were inspired by the fact that certain fragrances have antibacterial effects. Over a long period of time, he conducted a series of research studies on a huge number of fragrances that could be used as agents. As a result, synthetic fragrances! , -1 or by appropriately combining a synthetic flavoring agent with a flavoring agent (food flavoring agent) such as a carboxylic acid or lactone, an excellent bactericidal effect on bacteria that causes caries can be obtained, and this invention has been achieved. . That is, the gist of the present invention is an anti-corrosion agent characterized by comprising only a synthetic fragrance, or a synthetic fragrance and at least one of the following anti-nodulation components A and B.

A: Carboxylic acid 13: Lactone As described above, the greatest feature of the present invention is that it uses an extremely safe fragrance ingredient with no side effects as an anti-corrosion agent.

Next, this invention will be explained in detail.

There have been reports here and there that certain fragrance compounds have antibacterial effects. However, there are no reports regarding the antibacterial activity of Nacala against Streptococcus mutans, which has the strongest nodulation effect. Therefore, the present inventors first
As a step, we measured the antibacterial activity against S. mutans using synthetic fragrances that have been reported to have an antibacterial effect or are relatively widely used. The antibacterial activity was determined by adding the above synthetic fragrance to a 5% alcohol solution as the test component) and adding it to a heart infusion medium containing 5% sucrose at a ratio of 1/100 to 1/l O00. (5
Alcohol solution ((test component)) concentration is 1/100~
After the medium had solidified, mutans bacteria (Streptococcus mutans RIMD 3125001) was punctured and incubated at 37°C.
The cells were cultured for 72 hours or more, and the growth of the bacteria in the medium and on the surface of the medium was observed and measured. Those having anti-Streptococcus mutans activity are shown in Table 1 below. Having anti-Streptococcus mutans activity means that no growth of Streptococcus mutans is observed when the test components are added at a ratio of 171,000 parts and cultured at 37°C for 72 hours or more. Then, the concentration of the test component was diluted rapidly, and the minimum concentration at which anti-Streptococcus mutans activity was observed (
The reciprocal of the effective growth inhibitory concentration), for example, the concentration of the test component is 1/
When the value was 1000, the reciprocal of 1000 was shown as the anti-mutans activity value. Similar experiments were conducted using Atsuboku extract, the active ingredient of Atsubaku extract, Magnolia nigra, and erythromycin, an antibiotic that has a bactericidal effect against Streptococcus mutans, and are shown in Table 1. The synthetic fragrances listed in Table 1 exhibit excellent anti-Streptococcus mutans activity equivalent to or superior to that of Koboku extract (see JP-A-57-85319), which is known as an anti-candy agent.

Since synthetic fragrances are extremely rich in anti-Streptococcus mutans activity, we expanded our search to the field of flavoring agents such as carboxylic acids and lactones to investigate substances with anti-Streptococcus mutans activity. The results are shown in Table 2 below. The carboxylic acids and lactones listed in Table 2 had extremely high anti-Streptococcus mutans activity.

Next, the fragrance ingredients shown in Tables 1 and 2 above were mixed and their anti-mutans activity was investigated.

The results are shown in Table 3 below, and the anti-Streptococcus mutans activity values were higher than the arithmetic mean of the anti-Streptococcus mutans activity values of the fragrance ingredients in Tables 1 and 2, respectively. This shows that a great synergistic effect can be achieved by mixing the fragrance ingredients shown in Tables 1 and 2. That is, in general, fragrance ingredients are rarely used alone, and various ingredients are mixed to create a mixed fragrance with a desired fragrance, and the resulting mixture is used.

Therefore, it is extremely effective in practice that the large synergistic effects shown in Table 3 can be obtained by mixing and using the fragrance ingredients shown in Tables 1 and 2.

As described above, the anti-nodulation agent of the present invention does not cause any side effects because it is composed of highly safe flavor ingredients that are widely and actually used in the food industry and the like. In other words, the anti-nodulation agent of this invention has a slightly lower anti-nodulation effect than the antibiotic erythromycin, but since the anti-nodulation agent of this invention is not an antibiotic, it does not cause side effects (in vivo microflora) that are seen with antibiotics. (disturbance of bacteria, emergence of resistant bacteria), and there is no problem at all even if used continuously for a long period of time. Moreover, since the anti-nodulation agent of the present invention is comprised of a wide range of flavoring ingredients such as synthetic fragrances, carboxylic acids, and sifton, appropriate flavoring ingredients can be combined to impart any desired flavor to the product to which the anti-nodulation agent is added. It becomes possible to grant.

This effect is clinically practical, considering that anti-nodulation agents can be administered for a fairly long period of time, and that to prevent nodules, it is desirable to administer them to infants from around 1 year of age, when tooth development begins. Moreover, it is extremely useful.

Furthermore, since the anti-nodulation agent of the present invention can stimulate the growth of S. mutans at an extremely low concentration, a large anti-nodulation effect can be obtained with a small amount of use.

As described above, the anti-nodule agent of the present invention is a fragrance ingredient that can have an excellent anti-nodule effect even when used in a small amount, so it can be used in gargles, troches, and toothpastes.

It not only adds flavor to chewing gum, but also has an anti-knot effect. Moreover, its use does not cause any side effects unlike those of conventional antibiotics, and it is highly practical as it can withstand long-term continuous use. Moreover, the anti-nodulation agent of this invention contains substances already known to have antibacterial effects, and these have antibacterial effects against pathogenic bacteria such as Escherichia coli and Shigella. However, there is nothing known about its antibacterial effect against special bacteria such as Streptococcus mutans (which does not belong to any of the streptococcal classifications). It can be said that it can produce excellent effects that cannot be foreseen.

(Hereafter, extra white) Table 2 Next, examples will be described.

The following examples were carried out using the mixtures in Table 3, which give excellent synergistic effects when mixed.

[Example 1] When the Streptococcus mutans activity was determined for the mixture of Qi 1 listed in Table 3, the effective growth-inhibiting concentration against the Streptococcus mutans was 1/4000 (anti-Streptococcus mutans activity 4oooo). )Met. Even when a 5-thialcohol solution of the &l mixture was added to a 10-thiol sucrose solution at a ratio of 1/4000 and put into the mouth, no discomfort or irritation was felt at all.

[Example 2] The effective growth-inhibiting concentration against S. mutans was investigated using the mixture in column 2 of Table 3. The effective growth-inhibiting concentration was 1/6000 (anti-mutans activity 6
000). Even when a 5-thiol alcohol solution of this mixture was added to a 10-thiol sucrose solution at a ratio of 176,000 and taken in the mouth, no discomfort or irritation was felt at all.

[Example 3] The effective growth-inhibiting concentration against Streptococcus mutans was determined for the mixture 3 in Table 3. The effective growth inhibitory concentration of this substance is 1/6000 (anti-Streptococcus mutans activity 6
000). Even when a 5-thialcohol solution of this mixture was added to a 10% sucrose solution at a ratio of 1/6000 and placed in the mouth, no discomfort or irritation was felt at all.

[Example 4] Using the mixture of patient 4 in Table 3, the effective growth-inhibiting concentration of this mixture against S. mutans was determined. As a result, the effective growth-inhibiting concentration was 176,000 (anti-Streptococcus mutans activity 6,000). Even when a 5% alcohol solution of this product was added to a 10% sucrose solution at a ratio of 1/6000 and placed in the mouth, no discomfort or irritation was felt at all.

Patent applicant Kanebo Foods Co., Ltd. Agent: Patent Attorney Yukihiko Nishifuji Procedural amendment (voluntary) May 23, 1982 Commissioner of the Patent Office 1. Display of incident 1981 Patent Application No. 51201 2 Name of the invention anti-knot agent 3. Person who makes corrections Relationship to the case Patent applicant 7. Contents of correction (1) Table 1 on page 10 of the specification is corrected as follows.

Note (2) In the third line of the substance name column in the left frame of Table 2 on page 11 of the specification, "mystilic acid" is corrected to "r-myristic acid."

(3) In the 5th line of the substance name column in the left frame of Table 2 on page 11 of the specification, "stearic acid" is corrected to "stearic acid."

Claims (4)

[Claims] (1) An anti-ayu caries agent characterized by comprising only a synthetic fragrance or a synthetic fragrance and at least one of the following anti-ayu cariogenic ingredients A and B. A: Carboxylic acid B: Lactone (2) Synthetic fragrances include talesylbuscetate, cyclamen aldehyde, ineugenol, methyleugenol, heliothrobin, and ethyl salicylate. 2. The anti-acillus caries agent according to claim 1, which is at least one synthetic fragrance selected from the group consisting of n-decaol and P-methylacetophenone. (3) The carboxylic acid of anti-corrosion component A is capric acid. Lauric acid, myristic acid, valmitic acid, stearic acid, oleic acid, linoleic acid, rosin acid. Vanillic acid, undecanoic acid, undecanoic acid and! The anti-sweetfish corrosion agent according to claim 1, which is at least one carboxylic acid selected from the group consisting of nando acids. (4) The lactone of the anti-sweetfish corrosion ingredient B is d-decalactone,
2. The anti-corrosion agent according to claim 1, which is at least one lactone selected from the group consisting of d-dodecalactone, d-undecalactone, d-)ridecalactone, and d-tetradecalactone.