JPS59175412A - Dental caries preventive treatment and preventive granular medicine - Google Patents

Abstract

(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to oral science, more particularly for daily hygiene in the oral cavity, for obtaining an anti-inflammatory effect in the case of periodontal ligament diseases, and for the anesthetic effect in the case of hypersensitivity of hard tooth tissues. The present invention relates to a therapeutic and preventive granule that is used to prevent dental caries and has a caries preventive effect.

Various therapeutic and prophylactic dental preparations are available in the prior art, such as toothpastes, elixirs, gels.

Powders are known.

In some cases, powders are used as doughs because they tend to dust. However, even today, attempts are still being made to develop dry preparations for use in maintaining and caring for oral hygiene.

In the prior art, there are known granular cleaning and foaming agents for daily use for treatment and prevention that have a certain degree of preventive effect against periodontal ligament disease and dental caries (W, Milk (manufactured in Germany, Melf, Germany). Melfuran (Trademark)].

Melfuran consists of granules that have a single odor, liberate carbon dioxide, and are easily soluble in water.

This granule is the next f? 〇 Liquor with chemical composition (weight%)
Stone Acid 17 A mixture of lucicum carbonate and magnesium carbonate 8.6 and a small amount of calcium phosphate Blowing agent (sodium salt of the ether of fatty alcohol and sulfuric acid 7.7) Salt 7.9 Extract from Gum Myria 1 & Due to the special granulation process, the granules of this preparation contain all the ingredients in a predetermined proportion in concentrated form.The disadvantage of this prior art preparation is that it has an anti-caries effect. and its cleaning effect is low. Furthermore, this prior art formulation has too high an abrasive effect and the mechanical strength of the granules is very low.

The main object of the present invention is to provide therapeutic and preventive dental granule preparations that have a high caries prevention effect.

It is another object of the present invention to provide therapeutic and prophylactic dental granule preparations with low abrasive effects and high mechanical strength of the granules.

For these purposes, the abrasive, sodium tartrate bicarbonate 9
Contains foaming agents, fragrances, binders and anti-cavity ingredients,
The caries prevention ingredient is treated with dilute mineral acid on the bone tissue until the aerosol components and water-soluble proteins contained in the bone tissue are completely dissolved, the solution thus generated is separated, and this solution is used as a stabilizer. diluted with water containing citric acid or its salt,
This solution was then prepared by neutralizing and drying, and the primary components (N%), namely calcium 2-6 sodium 19-23 potassium 0.0
4-0.18 Mineral acid anion 6-10.6
Orthophosphate anion 1.5-5.0 Water-soluble protein 10-50 Magnesium 0.05-02 fluoride, mixture of trace elements including manganese, tin, zinc and 0.01-0.02 iron Citric acid complex compound (Citric acid is an anion in an amount such that the total amount is 100 °C), and the starting components are in the following proportions (wt%).

That is, 11 to 15 shots of tartaric acid.
Foaming agent 1,8-2,7 Sodium bicarbonate 42-46 Binder
0.11~0.13 fragrance material
0.8-1.2 Tooth decay prevention share
This is achieved by using granules for the treatment and prevention of dental caries consisting of an amount of 1 to 6 abrasives totaling 100%.

In order to ensure a long shelf life of the therapeutic and prophylactic granular formulations of the invention, it is advisable to add an additional 1.9 to 2.1% by weight of sodium sulfate.

The dental preparation of the present invention preferably contains dicalcium phosphate dihydrate as an abrasive.

The preparation of this invention is in the form of granules with a size of 0.15 to 1.5 mm, is white in color, and has a pleasant aroma and taste that does not change even when stored for one year. The preparation of this invention has a high caries preventive effect because it contains a component that has a caries preventive effect. The content of the caries prevention ingredient of this invention is 1.0 weight ft.
% or more than 6.0% by weight, the therapeutic and preventive effects of the granules are reduced.

The formulation of the present invention reduces caries by 35%, whereas the prior art granular formulation ``Melfuran J'' only reduces caries by 17%.

The dental formulations of this invention have good cleansing properties, as evidenced by a significant statistical fC reduction in the Oral Hygiene Index (OHI-8). The formulation of this invention has a low abrasive effect (2C)%) t-
On the other hand, it has a high cleaning effect. 6 scales are dissolved by 30% by the formulation of this invention.

The dental formulation of this invention is used as follows: Remove the granules from the container onto a damp toothbrush.During tooth brushing, the granules come into contact with water and the formulation is rapidly heated with the evolution of carbon dioxide. dissolve. At the same time, intense foaming occurs, which fixes the diacid fly, carbon on the tooth and gingival surfaces, thus causing plaque dissolution. and clinically tested on patients. 3% of caries prevention ingredients
The aqueous solution was tested against a control. The test used 1-month-old Wistar rats (
40 mice were used for the test solution and the other 40 mice were used as controls) and carried out at °C. Animals at 10°C were fed the caries-inducing diet 5Tephan® 580 and the test solution was applied to the teeth for 3 minutes each day over a 4-week study period. After the experiment was completed, the teeth were removed and tested using a generally accepted method. Caries index was measured according to the following.The obtained data are shown in Table 1.

Below is a blank space for applying a 3% solution of the caries prevention ingredient of this invention to children aged 7 to 100.
1.5 according to the dosing schedule twice a month for children
When used for more than a year, the caries prevention efficiency is 44.1-53.7% according to the relative decrease of increase in DMF-T index, and 402-58.0 according to DM, F-8 index. %, and according to the data of the CRT test, the acid resistance of enamel increases considerably.The effectiveness of the 3-chi solution, which is an anti-caries ingredient, in the early stage of dental caries treatment is high, and the positive effect of the treatment, i.e. mineral deficiency. Disappearance or reduction of spots was observed in 72.4-84% of cases, stabilization of course in 14-31.9%, and no treatment effect was observed in cases 2-8. .

The effect of the 3% solution of the anti-caries component of this invention in the treatment of hypersensitivity of hard tooth tissues was good, and the well-enhanced sensation of the tooth neck was eliminated in 23.2 to 36.4 cases. .

Clinical trials on caries prevention ingredients? , from the viewpoint of researching the preventive effect on children and pregnant women, and from the viewpoint of researching the efficiency in conservative treatment of nested mineral defects in tooth enamel. ○Anti-caries prevention ingredient is 1.5-3% of the administration solution. used in the form of

176 children aged 7-8 were selected according to the results of epidemiological tests and divided into two groups.

81 people in the first group were treated with anti-cavity solution, and 9 in the second group.
Five people served as a control group.

The solution was applied after pre-brushing the teeth with a sanitary toothpaste. The teeth were then isolated from saliva with a lignin tampon and dried with a blast of air. The solution was applied to all tooth surfaces by placing a well-dissolved main ball on a flexible plastic spoon. The application time was 10 minutes for 6 jaws. After application, children were instructed not to eat or drink anything for 2 hours. All subsequent biweekly applications were performed as described above.

Preliminary observation of the oral cavity shows that the DMF-T value of cavities is 1.1.
A relatively uniform level of 2±0.13 to 1.30±0.13 was observed.

The results of the application of the anti-caries solution are shown in Table 2.

From this table, it can be seen that the increase in tooth decay in the first group of children is due to DM
44.7% each based on F-T and DMF-8
and 49.5% lower.

In an analysis of the caries-preventing effect of the test component on tooth types, it was confirmed that it was effective on first molars that had already been developed and on incisors that had protruded during the observation period.

A solution of the test component was used to treat mineral defects in the teeth of 81 students aged 7-14.

The students were divided into two subgroups according to the type of mineral deficiency.

Namely.

Group 3a (total 42 students): students with slowly progressing mineral deficiencies, and Group 3b (total 39 students): students with rapidly progressing mineral deficiencies.

For students in group 3a, in a total of 229 teeth;
For students in group 3b, there were a total of 248
Mineral substance deficiency was observed in each case (Table 3). Control groups are shown as Group 1a and Group 1b in the table corresponding to the aforementioned groups.

In order to obtain a positive effect on dental treatment with a solution of the test component, ViIO should be applied 15 times in Group 3a (1).
average) and in the 1!3b group it was necessary to perform 20-25 applications.

Remineralization treatment was more effective in treating slowly progressing mineral deficiency processes. Small spots (2-
(2- and 3-) decreased and disappeared more rapidly than the larger ones. Conservative treatment of rapidly progressing mineral defects in the teeth of students in group 3b was ineffective.

However, a linear relationship was observed between the treatment effect and the size of the spots (Table 4).

In the gaa group, a positive treatment effect, i.e., disappearance of spots, was observed in 193 out of 229 teeth (84% ± 2.4%), whereas in the control group, it was observed in 100 out of 270 teeth (36 %±2.4%) positive treatment effects were observed.

The stabilization process affected 31 teeth (14%) in group 3a.
In the control group, it was observed in 87 teeth (31%±2.8%).

Enlargement of spots and shape of cavities were observed in only 5 out of 229 teeth (2% of teeth) in the F3a group, but in 92 out of 279 teeth (33 teeth) in the control group.
% ± 2.8%) of teeth were observed.

The difference between the m 3 a group and the 1a group (control group) was statistically significant (Table 4).

In the treatment of rapidly progressing mineral defects in group 3b, a positive treatment effect occurred in 155 out of 248 teeth (63 teeth ± 3.0%), whereas in the control group, 30
Spontaneous disappearance was observed only in 33 out of 5 teeth (11 teeth ± 18%). 60 of students in group 3b
The mineral loss process was stabilized in real teeth (24 ± 2.7%). Mineral defect plaques [and cavities were formed] on 33 teeth of students in Group 3b.

There were statistically significant differences between the characteristics of Group 3b and Group 1b (control group) (Table 4).

As a result, the average positive effect in the treatment of rapid and slow mineralization processes in tooth enamel is 73%.
It was Section 5.

Margin below Table 3 Mineral deficiency spots of various sizes in Group 3 and Group 1 (control)? Number of Teeth The solution of the ingredient having an anti-caries effect according to the present invention was tested on pregnant women. Epidemiological studies have shown that pregnant women with IC
It was found that focal mineral defects in tooth enamel increased with increasing gestational age.

In order to test the preventive effect against such phenomena, 6
Nine pregnant women (Group 1) K were treated with the solution of the ingredient having a caries-preventing effect according to the present invention. Sixty-four pregnant women were the target group (group 2).

In both groups of pregnant women (1 to 3 months of gestation), tooth damage due to focal mineral defects was relatively the same, i.e. 29-30% had damage to an average of 1.8 ± 0.3 teeth.
,Met.

At the end of pregnancy, focal mineral defects of tooth enamel in the control group were 64% of cases with an average of 5.23±0.7 teeth damaged.

By using the ingredient having a caries-preventing effect of this invention in the first group of pregnant women, it is possible to not only prevent the formation of new focal lesions on the enamel, but also stabilize the process of the already existing lesions. (no enlargement of mineral defect foci or formation of cavities was observed).

Granules of this invention were tested. The granules of this invention, pseudo-granules, and known composition "Melfuran" were tested on 100 1-month-old Weister rats (25 rats each). 25 of
animals were used as controls).

All animals were given the caries-inducing diet Nutephan-58 (1 dose), and the teeth of the animals were brushed for 1.5 minutes with the respective formulations (sham granules, "Melfuran granules" and the formulation of this invention) over the 4-week experimental period. .

The polishing effect was evaluated according to medical indicators using 18 extracted human teeth. The polishing effect of pseudogranules was considered to be the highest.

Four groups of 30 students each with approximately similar backgrounds were formed to fully evaluate the detergent effect of the drug. 0OHI-8 where students brushed their teeth daily under control using the study formulation.
Evaluation was performed using the standard method with a rigid index [Green (G
reene) J-Ct Vermilion (Verm
illion) J, E, The simplif
iedoral hygien 1ndex, J, A
mer, Dent, Ann.

1964, 68, 1.7-13].

Silness-L has the effect of dissolving dental plaque.
oe) was evaluated by the index. For this purpose, preliminary tests have shown that a suitable degree of solid deposits have been formed on the enamel, and that the initial Sirnes-Thurot index is the same and approximately 0.
．． In order to accurately evaluate the amount of settled M in dental plaque, 30 subjects were selected.
) (made in France) was used.

The results of this test are shown in Table 5.

A comparative test between the granule "Melfuran" and the formulation of this invention revealed that the latter was twice as effective in preventing cavities as the former.
It was shown that the polishing effect was 20% lower and the plaque dissolution effect was 30% higher.

As is clear from the above test results, the dental preparation of the present invention is superior to the dental preparation "Melfuran" in all characteristics.

The formulation of this invention is manufactured as follows. The abrasive and anti-caries ingredients are mixed with the moistened binder and foaming agent. The mixture is disintegrated and thoroughly mixed with sodium monobicarbonate tartrate, and flavor, and granulated.

As abrasives, chalk, dicalcic phosphate dihydrate, and other materials can be used.

Preference is given to using dicalcium phosphate dihydrate. As blowing agents, sodium lawalyl sulfate, sodium lawalyl sarcosinate and the like can be used. Preference is given to using gelatin as binder. The granules formed are sieved. For long-term storage, the granules can be dusted with sodium sulfate powder. The granules thus obtained are placed in a container. The shelf life is one year. To explain the invention in more detail, some specific examples of the dental compositions of the invention are described below.

Example 1 A therapeutic and prophylactic preparation comprising the following composition u) with anti-caries effect was produced.

Anti-cavity ingredient dicalcic phosphate dihydrate having the following composition (% by weight) 31.90 Gelatin
012 Sodium Lacryl Sulfate 2,00 Tartaric Acid
12.95 Sodium Sulfate 2.00 Flavor 1.00 Sodium Bicarbonate
The therapeutic and preventive dental granule preparation of the present invention having a caries-preventing effect is produced in the following manner.

Dicalcium phosphate dihydrate and anti-cavity ingredients are mixed with moist gelatin and sodium hydryl sulfate; the resulting mixture is disintegrated; and tartaric acid.

Thoroughly mix with sodium bicarbonate, and flavor, and granulate at °C. The granules are sprinkled with sodium sulfate for long-term storage. The granules thus produced are packed into containers.

Storage period: 1 year Diameter of granules: 0.8 mm Mechanical strength of granules: 6.0 kg/cn 1 Example 2 A therapeutic and preventive dental preparation having a caries-preventing effect and consisting of the following composition C) was produced.

Dental caries prevention ingredient dicalcic acid phosphate dihydrate having the following composition (weight 5I%) 36.79 Zekugun 0.11
Lawalyl Sodium Sulfate 1.
80 Tartaric acid 13.00 Sodium sulfate 2.10 Flavor and raw materials 1.20 Sodium bicarbonate
A formulation is manufactured by the method of JPY 1 with a total weight of 100.00.

Granule diameter 1.1 mm Granule mechanical strength 8.8 kg/cr7L Example 3
A therapeutic and preventive dental preparation having an anti-caries effect and consisting of the following composition (9) was produced.

Anti-cavity ingredient consisting of the following composition (i! (Jt%)) Dicalcium phosphate dihydrate 34.90 Gelatin 0.13 Sodium quaryl sulfate 2.27 Tartaric acid 1100 Sodium sulfate 1.90 Scent v
% fee 0.80 sodium bicarbonate worm
A preparation having the above composition was prepared in the same manner as in the case of Keiyo 1, in which the total amount was 10D,00.

Diameter of granules: 1.44 mm Mechanical strength of granules: 9.5 kg/i Example 4 A therapeutic and preventive dental preparation having the following composition (#) d and having an anti-caries effect was produced.

Dental caries prevention ingredient dicalcic acid phosphate dihydrate having the following composition (wt%) 33.45 Gelatin
0.12 Sodium lauryl sulfate 2.25 Tartaric acid
12.55 Sodium sulfate 1.70 Flavoring agent 0.95 Sodium bicarbonate
A preparation having the above composition was produced by the same method as in Keiyo 1, in which the total concentration was 100°00.

Diameter of granules: 0.95 mm Mechanical strength of granules: 3.8 kg/c 4 examples: 5° A therapeutic and preventive dental preparation having an anti-caries effect and having the following composition (&) was manufactured.

Margin below: Dental caries prevention ingredient dicalcium phosphate dihydrate having the following composition (wt%) 32.75 Gelatin
0.12 Sodium lacryl sulfate 2.19 Tartaric acid
12.20 Sodium sulfate 2.05 Flavoring agent 0.90 Sodium bicarbonate
A preparation having the above composition was produced by the same method as Meal 1, in which the whole was ioo and oo. Diameter of granules: 0.7 mm Mechanical strength of granules: 2.3 kg/C Shoulder example 6゜Cavity prevention effect: Therapeutic and prophylactic dental preparations consisting of the following composition (also: J.

The following composition (wt%) contains gelatin, a caries prevention ingredient
0.11 Lawalyl Sodium Sulfate 190 Tartaric Acid
13.00 Fragrance 1 ingredient 0.95 Sodium bicarbonate 9
The formulation of the present invention was obtained according to the method of Meal 1 in which the total weight was 100.00.

Granule diameter 1.20 mm Granule mechanical strength 9.0 kg/c? Patent Applicant Lysisky Medi Twin Sugii Institute (1 other person) Patent Application Agent Akira Aoki Patent Attorney Kazuyuki Nishidate Patent Attorney Kazuyuki Fukumoto Batersky Institute Stomatology Soviet Union Moscow Ulitsa Timura Frunze 16 Procedural Amendment March 90, 1980 Director General of the Patent Office Kazuo Wakasugi 1, Indication of Case 1981 Patent Application No. 044535 2, Invention Name of therapeutic and prophylactic granular preparations with anti-caries effect 3 Relationship with the amended person's case Name of patent applicant Lidzhisky Meditsinsky Institute (1 other person) 4. Agent (3 other people) 5 , Subject of amendment (1) Column 1 of claims 1 of the specification (2) Column 6 of "Detailed Description of the Invention" of the specification, Contents of amendment (1) The scope of claims is amended as shown in the attached sheet do.

(2)■ Correct the phrase "aerial component" on page 5, line 5 of the specification to "inorganic component."

■ On page 24, line 8, "fragrance" is corrected to "flavoring agent."

7. List of Attached Documents Amended Claims l Circular 2, Claim 1 Comprising an abrasive, sodium tartrate monobicarbonate, a foaming agent, a flavoring agent, a binder, and a caries-preventing ingredient, the caries-preventing ingredient However, the bone tissue is treated with dilute mineral acid until the inorganic components and water-soluble proteins contained in the bone tissue are completely dissolved, the solution thus produced is separated, and this solution is treated with citric acid or its stabilizer as a stabilizer. It was prepared by diluting with salt-containing water, then neutralizing and drying the solution, and containing the following components (wt%): Calcium 2-6 Sodium 19-23 Calcium Um
004~0.18 Mineral acid anion 6~
10.6 Orthophosphate anion 1.5-5
．． 0 Bath protein] 0. ~5.0 Magnesium 0.05~0.2 Fluorine, Manganese,
A mixture of trace elements including tin, zinc and 0.01 to 0.02 iron contains an amount of citric acid complex compound (citrate anion as a total of 100 ions), and the starting components are in the following proportions (% by weight): ), i.e. tartaric acid 11-15 foams
Agent 1.8-2.7 Sodium bicarbonate 42-46 Binding agent
0.11~o, 13 flavoring
0.8-1.2 Dental caries prevention ingredient 1-6 Abrasive A granule for dental caries treatment and prevention consisting of an amount of 100% as a whole.

2.Additionally 1.9-2 to ensure long-term storage
, 1% by weight of sodium sulfate.

3. Granules for treatment and prevention according to claim 1, which uses dicalcium phosphate dihydrate as the abrasive.

Claims (1)

[Scope of Claims] The caries-preventing component is obtained by treating the bone tissue with dilute mineral acid until the aerosol components and water-soluble proteins contained in the bone tissue are completely dissolved, and separating the resulting solution. This solution is diluted with water containing citric acid or its salt as a stabilizer,
Then neutralize this solution. It is prepared by drying at ℃ and the primary component (wt%) is calcium
2-6 Sodium 19-23 Calcium 0.
04-0.18 Mineral acid anion 6-10.
6 Orthophosphate anion 1.5-5.0 Water-soluble protein 10. ~5.0 Magnesium
A mixture of trace elements containing 0.05 to 0.2 fluorine, manganese, tin, zinc, and 0.01 to 0.02 iron.Contains an amount of citric acid complex (as an ion with a total of 100 citric acid anions). , and the starting components are in the following proportions (wt%): tartaric acid 11-15
Foaming agent 1.8-2.7 Sodium bicarbonate 42-46 Binding agent 0.11-0.13 Flavoring agent
0.8-1.2 Dental caries prevention ingredient 1-6 Abrasive A granule for dental caries treatment and prevention consisting of an amount of 100% as a whole. 2.Additionally 1.9-2 to ensure long-term storage
．． The therapeutic and prophylactic granules according to claim 1, containing 1 part by weight of sodium sulfate. 3. Granules for treatment and prevention according to claim 1, which uses C. dicalcium phosphate dihydrate as the abrasive.