JPH06321744A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain a composition for oral cavity raising permeability of anthranilic acid-based antiinflammatory agent to bacterial plaque, sufficiently making the agent reach to the losion, adequately, exhibiting its treating effect. CONSTITUTION:One ore more anthranilic acid-based antiinflammatory agents are mixed with a polyhydric alcohol, a nonionic surfactant and >=10% water to give the objective composition for oral cavity. The composition for oral cavity is extremely effective for treating periodontal disease.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition which is capable of effectively penetrating an anthranilic acid type anti-inflammatory agent into dental plaque and exerting a sufficient therapeutic effect, and which is effective in treating periodontal diseases. .

[0002]

2. Description of the Related Art Conventionally, the problems to be solved by the invention
Non-steroidal anti-inflammatory agents such as anthranilic acid anti-inflammatory agents are effective in promoting treatment of periodontal disease.
-38030 gazette etc. are described. However, even if these drugs are applied near the affected part of the periodontal disease, they are blocked by the plaque in the periodontal pocket, the drugs do not reach the affected part sufficiently, and their therapeutic effects are not sufficiently exerted. .

Therefore, if the permeability of these drugs in dental plaque can be increased and the drugs can reach the affected area sufficiently, it is very effective for the treatment of periodontal disease.

The present invention has been made in view of the above circumstances.
It is an object of the present invention to provide an oral composition that is effective in treating periodontal diseases, since an anthranilic acid-based anti-inflammatory agent can well penetrate into dental plaque and exert a sufficient therapeutic effect.

[0005]

Means and Actions for Solving the Problems As a result of intensive studies for achieving the above-mentioned object, the present inventor has found that one or more anthranilic acid anti-inflammatory agents may contain polyhydric alcohols and non-polyhydric alcohols. Ionic surfactant, and 10% or more of water 3
When used in combination with an anthranilic acid-based anti-inflammatory agent, or with an anthranilic acid-based anti-inflammatory agent, either a polyhydric alcohol or a nonionic surfactant or 10% or more water Or, compared to the case of mixing the two,
Unexpectedly, the permeability of the anthranilic acid type anti-inflammatory drug into the plaque becomes very high, and the anti-inflammatory drug can reach the affected area sufficiently and its therapeutic effect can be sufficiently exerted. It has been found that it is possible to obtain an oral composition that is extremely effective in the treatment of diseases.

Accordingly, the present invention provides an oral composition containing one or more anthranilic acid anti-inflammatory agents,
There is provided a composition for oral cavity, which comprises a polyhydric alcohol, a nonionic surfactant, and 10% or more of water.

The present invention will be described in more detail below. The oral composition of the present invention comprises one or more anthranilic acid anti-inflammatory agents, polyhydric alcohols, and nonionic surfactants. And containing 10% or more of water,
For example, it can be used in a dosage form such as oral pasta, toothpaste, water toothpaste, mouthwash, patch and the like.

In this case, examples of the anthranilic acid type anti-inflammatory agent include diclofenac sodium, flufenamic acid, aluminum flufenamic acid, meclofenamic acid, mefenamic acid, floctafenin and the like.
The amount of the anthranilic acid-based anti-inflammatory agent blended is 0.01 to 5% (% by weight, the same applies hereinafter) of the entire composition, and particularly 0.5.
It is preferably ˜2%.

Next, examples of polyhydric alcohols include ethylene glycol, diethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol, glycerin, 1,5-pentanediol, polyethylene glycol, and the like. One or more of these may be used.

The content of these polyhydric alcohols is preferably 0.1 to 65%, especially 0.5 to 40% of the total composition, and if less than 0.1%, the content in the plaque of the drug is small. In some cases, it may not be possible to increase the penetrability, and if it exceeds 65%, the usability of the oral composition may deteriorate.

Specific examples of the nonionic surfactant include sorbitan fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, propylene glycol fatty acid ester, pentaerythritol fatty acid ester, polyoxyethylene sorbitan fatty acid ester and polyoxyethylene. Sorbit fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyethylene glycol fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene phytosterol, polyoxyethylene phytostanol, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene alkylphenyl ether, poly Oxyethylene castor oil, polyoxyethylene hydrogenated castor oil,
Examples include polyoxyethylene lanolin, polyoxyethylene lanolin alcohol, polyoxyethylene sorbit beeswax, polyoxyethylene alkylamines, polyoxyethylene fatty acid amides, polyoxyethylene alkylphenyl formaldehyde condensates, and single chain length polyoxyethylene alkyl ethers. To be done.

The content of the nonionic surfactant is preferably 0.1 to 10%, particularly 0.2 to 5% of the total composition, and if it is less than 0.1%, the plaque of the medicine is plaque. In some cases, it may not be possible to increase the permeability, and if it exceeds 10%, the irritation to oral soft tissue may become strong.

The content of water is 10% or more of the total composition,
In particular, it is preferably 20 to 90%, and if it is less than 10%, the permeability of the drug in plaque cannot be increased,
If it exceeds 95%, the anthranilic acid anti-inflammatory agent cannot be stably mixed.

The oral composition of the present invention may further contain various appropriate optional components in addition to the above-mentioned components depending on the dosage form and the like. Further, in addition to the above anti-inflammatory agents, for example, chlorhexidine or its hydrochloride, which is a drug that can be expected to have a plaque inhibiting effect by bactericidal action, thimerosal, protein silver, chloramine, iodoglycerin, iodoform, boric acid, paraformaldehyde, phenol, hexyl. Resorcin, benzalkonium chloride, benzethonium chloride, chlorhexidine gluconate, phenododecium bromide, decalinium chloride, cetylpyridinium chloride, ofloxacin, popidone iodine, benzylpenicillin, ampicillin, carpenicillin, acetylkitasamycin, amoxicillin, pacitracin, cephalotin sodium, Cephaloridine, cephalexin, erythromycin, chloramphenicol, polymyxin B sulfate, fradiomycin sulfate, gentamicin sulfate , Lysozyme chloride, amylase, dextranase, protease, etc., which have plaque-dissolving action, and procaine hydrochloride, oxyprocaine hydrochloride, tetracaine hydrochloride, chloroprocaine hydrochloride, ethyl aminobenzoate, which have local anesthetic action , Dibucaine, dibucaine hydrochloride, lidocaine, lidocaine hydrochloride, cocaine hydrochloride, thecaine, and the like, and antihistamines such as diphenhydramine hydrochloride, chlorpheniramine maleate, and clemastine can be blended as active ingredients.

[0015]

INDUSTRIAL APPLICABILITY The oral composition of the present invention has a very high permeability of an anthranilic acid anti-inflammatory agent into dental plaque, and the drug can sufficiently reach the affected area, and its therapeutic effect is sufficiently exerted. It is, therefore, very effective in the treatment of periodontal diseases.

[0016]

EXAMPLES The present invention will be specifically described below with reference to Examples and Comparative Examples, but the present invention is not limited to the following Examples. In addition,% in each example is% by weight.

[Examples and Comparative Examples] Oral compositions having the compositions shown below were prepared and a drug permeability test was conducted by the following method. The results are shown in Tables 2, 4, 8 and 11. Penetrance Penetration Test of Drugs Porphyromonas gingivalis 38 in THB medium supplemented with hemin and menadione at a concentration of 5 μg / ml each
One strain was cultured at 37 ° C. for 3 days in an anaerobic box whose gas was replaced with N ₂ : CO ₂ : H ₂ = 80: 10: 10.

The cells were washed twice with distilled water and suspended in distilled water so that the number of cells was 5 × 10 ¹⁰ cells / ml. Diameter 1
cm, height 7 cm, and a column with a glass plate with several holes at the bottom, place a Millipore filter with a diameter of 9 mm,
A suspension of bacteria was layered so that the height was 2 mm. A filter paper having a diameter of 9 mm was placed on the upper portion thereof and left at room temperature for 3 hours. Oral pasta and toothpaste have a sample amount of 0.1
g of the patch was cut to a diameter of 6 mm, and samples were laminated on the filter paper. 3 artificial saliva on top of it
After being laminated at 37 ° C for 16 hours, the liquid that passed through the column was collected, and the nonsteroidal anti-inflammatory agent contained in this liquid was quantified by high performance liquid column chromatography,
The comparison of drug concentration in the two samples was expressed as drug penetration ratio.

From the results of Tables 2, 4, 8 and 11, the oral composition of the present invention containing both the polyhydric alcohol and the nonionic surfactant together with the anthranilic acid anti-inflammatory agent and 10% or more of water. (Example) is more permeated in the plaque of the anthranilic acid anti-inflammatory agent than the case where both the polyhydric alcohol and the nonionic surfactant are not added or the case where either one is added (Comparative Example). It was confirmed to be excellent.

[0020]

[Table 1]

[0021]

[Table 2]

[0022]

[Table 3]

[0023]

[Table 4]

[0024]

[Table 5]

[0025]

[Table 6]

[0026]

[Table 7]

[0027]

[Table 8]

[0028]

[Table 9]

[0029]

[Table 10]

[0030]

[Table 11]

Continuation of the front page (51) Int.Cl. ⁵ Identification number Office reference number FI technical display location A61K 47/10 Z 7433-4C

Claims (1)

[Claims] 1. A composition for oral cavity containing one or more kinds of anthranilic acid type anti-inflammatory agents, and polyhydric alcohols, a nonionic surfactant, and 10% or more of water. A composition for oral cavity characterized by the above.