JPS59175426A - Cariostatic agent - Google Patents

Abstract

PURPOSE:To provide a cariostatic agent free from the side effects such as the disturbance of the microflora in the body, the emergence of resistant microorganisms, etc., administrable continuously for a long period, and effective at a low concentration, by using a carboxylic acid used as a flavoring material or the carboxylic acid and a lactone as essential component. CONSTITUTION:The objective agent contains, as active component, a carboxylic acid used as a flavoring material, such as caprylic acid, lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, linoleic acid, rosin acid, vanillic acid, undecanoic acid, undecylenoic acid or enantoic acid, or a mixture of the above carboxylic acid and a lactone used as a flavoring material, e.g. d-decalactone, d-dodecalactone, d-undecalactone, d-tridecalactone, d-tetradecalactone, etc. as another cariostatic component. A high synergistic effect can be attained by the combined use of the above components.

Description

DETAILED DESCRIPTION OF THE INVENTION This invention relates to anti-nodular agents, ie, oral agents that prevent caries or arrest its progression.

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

On the other hand, research into the cause of eclipse 1 is progressing, and the current theory is that sucrose in food undergoes changes due to the action of eclipse-causing bacteria, producing insoluble and sticky glucan. It is said that there is something to do. The glucan thus produced causes nodule-causing bacteria to adhere to the tooth surface and multiply, forming dental plaque. Using this plaque as a base, microorganisms within it ferment sugar and produce silicic acid, which causes caries to progress. To prevent caries, there are methods to increase tooth resistance, methods to eliminate sucrose or use a sweetener instead of sucrose, and methods to decompose insoluble glucan produced from sucrose or to block the production of glucan. Alternatively, methods for eradicating caries-causing bacteria may be considered.

Each of the above methods has advantages and disadvantages, but since the essence of nodule is an infection caused by the bacteria that causes caries, we believe that eradicating the nodule-causing bacteria is the most effective way to prevent nodule. It will be done. The above bacteria include Streptococcus Mutans.
tans) and Strebtococcus sanguis (5tr
eptococcus Sanguis). Many attempts have been made to eliminate such nodule-causing bacteria in order to prevent nodules. For example, the use of antibiotics such as penicillin and erythromycin, cell wall lytic enzymes that dissolve the cell walls of nodule-causing bacteria, and bactericidal agents such as cyclohexidine is gaining momentum. However, these have the problem of disrupting the natural bacterial balance by disturbing the oral and intestinal flora, and causing side effects. It has not been widely used until the problem of side effects has been resolved. Therefore, the reality is that there is no definitive way to prevent nodules, and no preventive method has been established that is superior to the physical method of cleaning with clothes after meals. .

In view of the above circumstances, the present inventors conducted a series of studies aimed at preventing nodules, and were inspired by the fact that certain fragrances have antibacterial effects. Over a long period of time, we have carried out a series of research on a huge number of fragrances that are used as fragrances. As a result, we found that using carboxylic acid, which is used as a flavoring agent (food flavoring) as it is, or combining this carboxylic acid with lactone, which is also used as a flavoring agent, has an excellent sterilizing effect on bacteria that cause caries. This invention was achieved by discovering that it can be obtained. That is, this invention:
The gist thereof is an anti-knot agent characterized by comprising only a carboxylic acid or a carboxylic acid and the following anti-knot component.

Anti-nodulation component: lactone As described above, the greatest feature of the present invention is that it uses an extremely safe fragrance component with no side effects as a nodulation agent.

Next, this invention will be explained in detail.

Heretofore, there have been reports that natural essential oils and some of the active ingredients of natural essential oils have antibacterial effects against Escherichia coli, Shigella, and the like. However, there are almost no reports on the antibacterial properties of flavoring agents such as carboxylic acids.

Therefore, as a first step, the present inventors measured the antibacterial activity against Streptococcus mutans using carboxylic acids, which are relatively widely used. The antibacterial activity was determined by adding a 1/100 to 1/1000 ratio of carboxylic acid to a heart infusion medium containing 5 parts sucrose (5 parts alcohol solution as the test component). The alcohol solution ((test component)) concentration is 1/lo.

After the medium had solidified, mutans bacteria (Streptococcus mutans RIMD 8125001) was punctured and inoculated to 37
The cells were cultured at °C for 72 hours or more, and the growth of 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. Anti-Streptococcus mutans activity means that the test ingredient has 171,000
Streptococcus mutans was added at a ratio of 50% and cultured at 37°C for 72 hours or more, and no growth of Streptococcus mutans was observed. Then, the concentration of the test component is gradually diluted.For example, if the concentration of the test component is 1/1000, is shown as the anti-Streptococcus mutans activity value. Similar experiments were conducted using Atsuboku extract, Magnolol, which is an active ingredient of Atsubaku extract, and erythromycin, an antibiotic that has a bactericidal effect against Streptococcus mutans, and are shown in Table 1. The carboxylic acids listed in Table 1 are known as Koboku extract (Japanese Patent Application Laid-Open No. 57-8531), which is known as an anti-caries agent.
9) shows an excellent anti-Streptococcus mutans activity that is equivalent to or better than that of Streptococcus mutans.

Since carboxylic acids are extremely rich in anti-Streptococcus mutans activity, we expanded our search to include lactones, which are used as flavoring agents like carboxylic acids, to investigate substances with anti-Streptococcus mutans activities. . The results are shown in Table 2 below, and the lactones listed in the table had extremely high anti-minitans activity.

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

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 greater synergistic effect can be obtained by mixing the fragrance ingredients shown in Tables 1 and 2. That is, in general, flavoring agents such as carboxylic acids are rarely used alone, and various components are mixed to create a desired fragrance and then used. Therefore, it is extremely effective in practice that the large synergistic effects shown in Table 8 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 a highly safe flavoring ingredient that is widely used in the food industry and other areas to remove knots. 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. Furthermore, the anti-nodulation agent of the present invention is composed of a wide range of flavoring ingredients such as carboxylic acids and lactones, and can be combined with appropriate flavoring ingredients to impart any desired flavor to the product to which the anti-nodulation agent is added. It becomes like a vine. 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.

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

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

It can flavor chewing gum and the like and at the same time exhibit 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.

(Hereafter, extra white) Table 3 Next, examples will be described.

The following examples were carried out using the mixtures shown in Table 3, which give excellent synergistic effects upon mixing.

[Example 1] When the Streptococcus mutans activity was determined using the mixture of Magnetic 1 listed in Table 3, the effective growth-inhibiting concentration against Streptococcus mutans was 1/4000 (anti-Streptococcus mutans activity 4000). )Met. Even when a 5% alcohol solution of this &1 mixture was added to a 10% 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 inhibitory concentration against Streptococcus mutans was investigated using the mixture in column 2 of Table 3.
00). Even when a 5% alcohol solution of this mixture was added to a 10% sucrose solution at a ratio of l/4000 and put into the mouth, no discomfort or irritation was felt at all.

Patent applicant Kanebo Foods Co., Ltd. Representative Patent attorney Yukihiko Nishifuji Procedural amendment (spontaneous) 1. Indication of the case Patent Application No. 51202 of 1982 2. Name of the invention Anti-nodulation agent 3. Case of the person making the amendment No patent applicant 7. Contents of the amendment (1) In the fifth line of the substance name column of Table 1 on page 10 of the specification, "stearic acid" is corrected to "stearic acid."

(2) Supplement the attached power of attorney.

8. List of attached documents

Claims (2)

[Claims] (1) An anti-knot agent characterized by comprising only a carboxylic acid or a carboxylic acid and the following anti-knot ingredient. Anti-corrosion ingredient: lactone (2) The carboxylic acid is capric acid or lauric acid. Myristic acid, valmitic acid, stearic acid, oleic acid, linoleic acid, rosin acid, vanillic acid. The lactone of the anti-nodulation agent 5(3) anti-nodulation component according to claim 1, which is at least one carboxylic acid selected from the group consisting of undecanoic acid, undecanoic acid and ena/tonic acid, is d-decalactone. , d-dodecalactone,
d-Undecalactone d-) Ridecalactone and d-
The anti-nodulation agent according to claim 1, which is at least one lactone selected from the group consisting of tetradecalactone.