JPS61197510A - Composition for oral purposes - Google Patents

Abstract

PURPOSE:A composition that contains small amounts of a nitroimidazole derivative and a specific compound, thus being used for prevention of periodental diseases and stomatosis, because it causes no side-effects, even when it is given continuously, inhibits gram-negative, anaerobic microorganisms from forming volatile sulfur compounds in oral cavity. CONSTITUTION:The objective composition contains a nitroimidazole derivative such as metronidazole and extracts from leaves of camellia plant such as tea tree or camellia or sodium copper-chlorophyllin. The amount of sodium copper chlorophyllin, or the tea-leaf extract is 0.001-1.0wt% based on the composition, while the amount of the nitroimidazole derivative is 0.00001-0.1wt%. The resultant composition is used in the form of tooth paste, tooth powder, mouth wash, gingiva massage cream or local liquid or paste paint. The volatile sulfur compounds are, e.g., hydrogen sulfide, methyl mercaptan, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of the Invention The present invention relates to an oral composition effective for preventing periodontal disease and bad breath, and more particularly to an oral composition containing a nitroimidazole derivative and a camelliaceae plant leaf extract or copper chlorophyllin sodium. The present invention relates to a formulated oral composition.

Background of the Invention Among the bacteria present in the oral cavity, Fusibacterium nucleatum is a Durum-negative anaerobic bacterium.
terium nucleatum) and Bacteroides gi.
A significant increase in periodontal pockets with advanced periodontal disease has been observed, and these bacteria are also susceptible to volatile compounds such as hydrogen sulfide and methyl mercaptan.
Pounds (hereinafter abbreviated as VSC) and other harmful substances in large quantities, it is thought to be one of the causative bacteria of periodontal disease and bad breath. Therefore, it is possible to suppress the growth of Fucibacterium nucleatum and Bataeroides gingivalis, and to suppress the VS caused by these bacteria.
Suppression of C production is considered to be extremely effective in preventing periphropathy and bad breath.

It has been known that nitroimidazole derivatives such as metronidazole exhibit a specific bactericidal effect against Durum-negative aerobic bacteria.

Namely, Listgalton et al. [M Δ.

Listgar [en, et at, J, Pe
riodont, Res, 14.65-75 (1979
)], it has been reported that systemic administration of metronidazole results in the removal of the Durham-negative pneumophilic bacteria from dental plaque. Also, Hayne and Lindt [J,
He1ji and J, L1ndhe.

J, C11nical Periodontol, 6,
197-209 (1979)], metronidazole was reported to be effective in reducing plaque and gingivitis scars in dogs; furthermore, Lacier et al.
J., Loesche.

eLat, , J, Clnical Period
onLol, 8.29-44 (1981)],
Metronidazole is effective against Bacteroides asssacharol, a drowsy bacterium found in dental plaque collected from periodontal pockets.
It has been reported that this method was effective in reducing the number of bacteria (yt 1cus) and, concomitantly, in reducing the depth of periodontal pockets. Also, West German Patent Nos. 2 and 1
No. 16.214 discloses a dentifrice containing metronidazole or benzoyl metronidazole, which is effective for preventing periodontal disease or bad breath.

However, metronidazole, which is commonly marketed under the trade name Fucinol (FlagYl), has side effects such as loss of appetite, nausea, and gastrointestinal discomfort when taken in large quantities or continuously, so it is not recommended to use it indefinitely.

Summary of the Invention In view of the above-mentioned problems, the present inventors have developed a method for developing vSC using a Durham-negative anaerobic method using a low amount of a nitroimidazole derivative.
As a result of intensive research in order to obtain an oral composition that has a suppressive effect on production, we have formulated an oral composition containing a nitroimidazole derivative with a camellia plant leaf extract or sodium copper chlorophyllin. Then,
The inventors have discovered that the inhibitory effect of nitroimidazole derivatives on vSC production by Durham-negative anaerobic bacteria is enhanced, leading to the completion of the present invention.

That is, the present invention provides an oral composition characterized by containing a nitroimidazole derivative and a leaf extract of a plant of the Camellia family or sodium copper chlorophyllin.

Therefore, the composition of the present invention can suppress the production of VSC by Locodalum-negative anaerobic bacteria without any side effects even when used continuously, and is effective in preventing periodontal diseases and bad breath.

Detailed Description of the Invention Next, Table 1 shows the results of a test on the additive effects of Camellia plant leaf extract and sodium copper chlorophyllin on the inhibitory effect of nitroimidazole derivatives on vSC production by bacteria. The inhibitory effect on bacterial VSC production was expressed by the amount of the nitroimidazole derivative and the extract obtained by extracting leaves of Camelliaaceae plants or copper chlorophyllin sodium to inhibit bacterial methylmercaptan production.

Extraction procedure: After drying camellia leaves or tea leaves until the moisture content is about 1%, crush them, add a solvent such as alcohol, glycerin, ether, propylene glycol, water, etc. and use a Soxhlet extractor etc. for 10~ Extraction was carried out for 20 hours, and the resulting crude solid was carbonized to 20 mml (g) under reduced pressure.
The fraction at around 00°C is distilled into an appropriate solvent to obtain an extract.

Test method Niprene heart infusion medium (DIFCo
Fucibacterium nucleatum ATCC 25586, which had been anaerobically pre-cultured in F. nucleatum
Inoculate the infusion medium by adding 1/10 x
[[, 10%, Go, 5%)] at 37 °C for 2
Cultured for 1 day. Next, the amount of methyl mercaptan generated in the upper part of the medium was determined using a gas chromatograph. The method for measuring methyl mercaptan using gas chromatography is the Kaigan method (Journal of the Japanese Society of Periodontology, 18.1-1).
2 (1976)), Fucibacterium nucleatum ATCC 25586 was inoculated and cultured in plain heart infusion medium to which neither nitroimidazole derivatives nor additives (camellia plant leaf extract, copper chlorophyllin sodium) were added. The amount of methyl mercaptan generated in this case is assumed to be 100, and the amount of methyl mercaptan generated in the case where the nitroimidazole derivative and additives are added is expressed in %.

In Table 1, the amounts of the nitroimidazole derivatives and additives are expressed as the final concentration in the medium as weight %.

Table I Table 1 (Continued) Table 1 (Continued) As is clear from Table 1, Camellia plant leaf extract and copper chlorophyllin sodium can enhance the ■Sc production inhibitory effect of nitroimidazole derivatives. Recognize.

Therefore, in the present invention, 0.0% of the top extract of Camellia plant or copper chlorophyllin is added to the entire composition.
01~! , 0% by weight is blended.

If the amount is less than 0.001% by weight, the nitroimidazole derivative will not have a sufficient inhibitory effect on bacteria, while if it exceeds 1.0% by weight, the effect will not increase.

To obtain the leaf extract of a plant of the family Camellia family used in the present invention, any top part of a plant of the family Camellia family, such as Camellia, Camellia, and Camellia, can be used.

To obtain such an extract, the leaves of such plants are mixed with 1% moisture.
After drying to a certain degree, the mixture is crushed, refluxed with an appropriate solvent such as alcohol, glycerin, ether, or water, and then extracted. The obtained crude solid was carbonized under a reduced pressure of 20 mmHg, and the fraction at around 200° C. was distilled into an appropriate solvent and used.

The nitroimidazole derivatives used in the present invention include metronidazole, benzoyl metronidazole,
Examples include compounds having a nitroimidazole ring such as tinidazole, nimorazole, orinidazole, or mixtures thereof. The amount of these nitroimidazole derivatives in the entire composition is from o, oooi to 1% by weight.
If the amount is less than this range, a sufficient suppressive effect cannot be obtained even if the additive is added, while if it exceeds this range, there is a risk of various side effects as described above.

The oral composition of the present invention can be in the form of a toothpaste, a toothpaste such as a toothpaste, a mouthwash, a gum massage cream, a liquid or paste topical application, etc., and each is manufactured according to a conventional method. be done.

Next, two groups of 20 people each received the toothpaste of the present invention containing 0.5% by weight of fresh camellia leaf extract as described in Example 1 below, and a control toothpaste obtained by removing the camellia leaf extract from the toothpaste composition. Forty people with periodontal disease and bad breath were stratified and used continuously for two weeks. The test results were determined two weeks later by a tester with no abnormality in sense of smell who sensory-evaluated each patient's exhaled breath. The results are shown in Table 2.

As is clear from Table 2, the toothpaste of the present invention was more effective in preventing bad breath than the control product, and had no side effects on patients.

EXAMPLES The present invention will be explained in more detail below with reference to Examples. In addition, in the examples, all % is weight %.

Example 1 A toothpaste was manufactured according to a conventional method using the following composition.

Composition Amount (%) Calunium diphosphate 50 ・Sorbitol dihydrate 10 Glycerin 10 Sodium lauryl sulfate 2.0 Carboxymethylcellulose 1.0 Fragrance
1.0 Metronidazole 0.05 Camellia leaf extract 0.5 Satucalin sodium 0.1 Paraben
0.2 water Total balance too, oo% The obtained toothpaste had a very good effect in preventing bad breath and had no side effects.

Example 2 A toothpaste was manufactured according to a conventional method using the following composition.

Composition Amount (%) Calcium carbonate 50 Sorbit 20 Propylene glycol 5 Sodium lauroyl sarcosone 0.5 Sydisaccharide fatty acid ester 06 Carboxymethyl cellulose 1.5 Fragrance
1.0 Metronidazole
0.03 Sodium copper chlorophyllin 0.02
Satucalin sodium 0.1 Sodium benzoate 0.3 Water
Total balance: 100.00% The obtained toothpaste has a very good halitosis prevention effect,
There were no side effects at all.

Example 3 A toothpaste was manufactured according to a conventional method using the following composition.

Composition Amount (%) Silicic anhydride
15 Sorbit (70% solution) 65 Polyacrylic acid 1. O carrageenan 0.2 Sodium lauryl sulfate
1.0 Fragrance 1.0
Metronidazole 0.05 Tea leaf extract O9l Saccharin sodium
0.2 Methyl paraoxybenzoate 0.3 Water Total balance 1
00.00% The obtained toothpaste has a very good halitosis prevention effect,
There were no side effects at all.

Example 4 A mouthwash was manufactured according to a conventional method using the following composition.

Composition Amount (%) Ethanol 15 Glycerin
lO Sorbit (70% solution) 20 Polyoxyethylene (80 mol) 0.05 Hydrogenated castor oil metronidazole 0.05 Camellia leaf extract 0.1 Zatukarin sodium
0.1 fragrance 2.
0 water remaining total
too, oo% The obtained mouthwash had a very good halitosis preventive effect and had no side effects at all.

Example 5 A mouthwash was manufactured according to a conventional method using the following composition.

Composition Amount (%) Ethanol 5 Glycerin 1O Polyoxyethylene (80 mol) 0.5 Hydrogenated castor oil Monooleic acid polyokino 0.5 Ethylene sorbicun benzoyl metronibuzole 0.05 Camellia leaf extract OI Zasocalin sodium
0.05 Fragrance 05
Water Remaining total 1. Oo, OO The obtained mouth water had a very good halitosis prevention effect and had no side effects.

Example 6 Oral pasta was produced according to a conventional method using the following composition.

Composition Amount (%) Liquid paraffin 15 Setanol 10 Glycerin
15 P, (1, E, (40) Sorbitan 5.
0 Monostearate metronidazole 0.05 Copper white lophyllin sodium 0.2 Valley fee
08 Zatucarinosodium 1.0 water
Total remaining 10
0.00% The obtained oral pasta had a very good halitosis prevention effect and had no side effects at all.

Claims (5)

[Claims] (1) An oral composition characterized by containing a nitroimidazole derivative and a leaf extract of a plant of the Camellia family or copper chlorophyllin sodium. (2) The oral composition according to item 1 above, wherein the leaf extract of a plant of the Camellia family is a camellia leaf or a tea leaf extract. (3) The oral composition according to item 1 above, wherein the amount of the leaf extract of a plant belonging to the Camellia family or sodium copper chlorophyllin is 0.001 to 1.0% by weight. (4) The oral composition according to item 1 above, wherein the nitroimidazole derivative is metronidazole. (5) The amount of nitroimidazole derivative is 0.000
The oral composition according to item 1 above, which has a content of 1 to 0.1% by weight.