JPH05262629A - Composition for oral cavity application - Google Patents

Abstract

PURPOSE:To provide an oral cavity composition having excellent inhibitive effect on the resorption of the alveolar bone caused by endotoxin of pathogenic bacteria of periodontosis and effective for the prevention and treatment of periodontosis. CONSTITUTION:The objective oral cavity composition having excellent inhibitive effect on the resorption of the alveolar bone can be produced by compounding an immunomodulator, especially lobenzarit or its nontoxic salt (e.g. disodium salt) useful as an immunomodulator, especially a slow-acting curative medicine for articular rheumatism in an amount of preferably 0.000001-5wt.% (especially 0.005-1wt.%) as an active component to an oral cavity composition such as an agent for implanting in the periodontal pocket, a gel preparation for oral cavity, an ointment to be applied to oral mucosa, a tape for pasting to gingiva, pasta for oral cavity, dentifrice, mouth wash and chewing gum. The composition is applied once to several times a day to the diseased part.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition effective for the prevention and treatment of periodontal disease. More specifically, the bone resorption by endotoxin of periodontopathic bacteria which is the main cause of alveolar bone resorption. The present invention relates to a composition for oral cavity, which has an effect of suppressing

[0002]

BACKGROUND OF THE INVENTION Periodontal disease is caused by plaques formed by periodontopathic bacteria.
It is a disease that causes inflammation of periodontal tissues, gingiva and periodontal ligament, and eventually leads to resorption of alveolar bone, resulting in tooth loss.

Conventionally, prevention of inflammation of connective tissue of periodontal tissue,
For the treatment, plaque suppression by anti-plaque agents and anti-inflammatory agents are used. In addition, as other preventive and therapeutic methods, methods of actively suppressing resorption of alveolar bone that supports teeth have been studied, for example, use of indomethacin, which is a prostaglandin synthesis inhibitor, has been studied ( J.
of Periodont. Res. 1983 (1
8) 110-117).

However, the effect is not sufficient,
Further development of more effective alveolar bone resorption inhibitor is desired.

The present invention has been made in view of the above circumstances.
An object of the present invention is to provide an oral composition capable of suppressing bone resorption caused by endotoxin of periodontopathic bacteria which is a main cause of alveolar bone resorption.

[0006]

Means for Solving the Problems and Actions The inventors of the present invention have conducted extensive studies to achieve the above object, and as a result, found that lobenzarit or a non-toxic salt thereof has an excellent alveolar bone resorption inhibiting effect.

[0007] That is, lobenzarit or a salt thereof is conventionally known as an immunomodulator and is used as a slow-acting therapeutic agent for rheumatoid arthritis. However, the present inventors have surprisingly found that lobenzarit or a salt thereof is alveolar bone. Strongly suppresses bone resorption by endotoxin of periodontopathic bacteria, which is the main cause of absorption, and found to be useful as an active ingredient for preventing or treating periodontal disease, which led to the present invention. Is.

The present invention will be described in more detail below. The oral composition of the present invention contains lobenzarit or a non-toxic salt thereof (eg, disodium salt) as an active ingredient for preventing or treating periodontal disease. Then, it can be prepared and applied to a suitable dosage form such as periodontal pocket insertion agent, oral gel preparation, oral mucoadhesive ointment, gingival adhesive tape preparation and oral pasta preparation. In addition, toothpaste, mouthwash, chewing gum and the like may be incorporated with lobenzarit or a salt thereof.

In this case, it is appropriate that the content of the above-mentioned active ingredient in the oral composition is 0.000001 to 5% (weight%, the same applies hereinafter), particularly 0.005 to 1%. The dose may be once to several times per day as the number of times of administration to the affected area.

The other components of the oral composition of the present invention are
It may be a commonly used ingredient depending on the dosage form, for example, as a excipient, an auxiliary agent, cellulose such as methyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, a lower alkyl ether compound, polyvinylpyrrolidone, vinyl such as polyvinyl alcohol. Compounds, polysaccharides such as pullulan and starch, and their derivatives, polyoxyalkylenes such as polyacrylamide, polyoxyethylene oxide, and high molecular weight polyethylene glycol, carboxyvinyl polymers, carboxymethyl cellulose, salts such as carboxymethyl cellulose calcium, alginic acid, sodium alginate , Ammonium alginate, salts such as triethanolamine alginate, tragacanth gum, methacrylic acid, styrene or vinyl ether Copolymerized copolymers and salts thereof such as monomers, polypeptides such as gelatin, guar gum,
Higher fatty acids such as gum arabic, chitin, chitosan, shellac, stearic acid and palmitic acid, water-insoluble polymer compounds such as ethyl cellulose, Eudragit E, L,
PH-sensitive polymer compounds such as S, higher alcohols such as cetanol, surfactants of lipophilic surfactants such as HLB1-8, inorganic powders such as titanium oxide, liquid paraffin, white petrolatum, collagen, and atelocollagen. It is illustrated.

These substances can be used alone or in combination of two or more, and the type can be appropriately selected according to the dosage form.

Further, known ingredients can be used in toothpaste, mouthwash and the like.

[0013]

INDUSTRIAL APPLICABILITY The oral composition containing lobenzarit or a non-toxic salt thereof of the present invention as an active ingredient can exert an excellent inhibitory effect on alveolar bone resorption by endotoxin of periodontopathic bacteria.

[0014]

EXAMPLES The present invention will be specifically described below by showing experimental examples and examples, but the present invention is not limited to the following examples.

[Experimental Example] The skull of a newborn (6 days old) BALB / c mouse was excised, divided into two, and each was placed in 2 ml of a medium for culturing α-MEM cells for 24 hours in a CO ₂ incubator. It was pre-cultured in. afterwards,
Porphyromonas gingival (porphyromonas gingival) was attached to one of the divided skulls.
is) 381 strain or Actinobacillus actinomycetemcomitans (Actinobacillus ac)
Add endotoxin (LPS, 1 μg / ml each) separated and prepared from tinomycetemcomitans) Y4,
The other skull has the same amount of endotoxin and lobenzarit 2N
a was added so as to have a concentration shown in Table 1 below, and the cells were cultured in a CO ₂ incubator for 48 hours. The Ca ²⁺ released in each medium was measured by Corning 940. The results are shown in Table 1. The results show the amount of Ca released when the mouse skull was stimulated with LPS.

[0016]

[Table 1]

From the results shown in Table 1, lobenzalit.2Na
It was found that at a very low concentration, the bone resorption activity of LPS stimulation of periodontopathic bacteria can be strongly suppressed.

[Example 1] Periodontal pocket insertion agent Lobenzarit 2Na 1% Polyvinylpyrrolidone 65 Sodium polyacrylate 20 Polyethylene glycol 400 10 Water residual 100%

[Example 2] Periodontal pocket insertion agent Robenzalit 2Na 0.5% Polyvinylpyrrolidone 65 Carboxyvinyl polymer 10 Sodium polyacrylate 10 Glycerin 10 Water Residual 100%

[Example 3] Periodontal pocket insertion agent Lobenzarit 2Na 0.2% Polyvinyl alcohol 45 Carboxymethylcellulose 20 Methylcellulose 20 Water Residual 100%

[Example 4] Periodontal pocket insertion agent Robenzalit 2Na 1% Polyvinyl alcohol 50 Sodium alginate 15 Hydroxypropylmethylcellulose 10 Collagen 5 Propylene glycol 10 Leftovers Total 100%

Example 5 Oral Pasta Lobenzalit 2Na 0.1% Cetanol 10 Squalane 20 Precipitable Silica 5 Polyoxyethylene (40 mol) Hydrogenated Castor Oil 0.1 Sorbitan Monooleate 1.0 Sodium Lauryl Sulfate 0.2 Glycyrrhetinic acid 0.1 Sodium saccharin 0.6 Eugenol 0.1 Perfume 0.6 Water Residual 100%

[Example 6] Lozenge Lobenzarit 2Na 0.5% Gum Arabic 20 Fructose 20 Glucose 20 Maltose 30 Water Residual 100%

[Example 7] Oral massage cream Lobenzarit 2Na 1% White petrolatum 10 Stearyl alcohol 10 Propylene glycol 4 Polyethylene glycol 4000 25 Polyethylene glycol 400 40 Ethanol 10 Total 100%

Claims (1)

[Claims] 1. An oral composition comprising lobenzarit or a non-toxic salt thereof.