JPH0995457A - Composition for oral cavity containing sodium chloride and magnesium chloride - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for oral cavity, excellent in feeling of use and effective in preventing periodontal diseases by blending a quaternary ammonium salt type cationic antimicrobial agent or an antiplasmin agent as an active ingredient with sodium chloride and magnesium chloride and thereby masking the bitterness thereof. SOLUTION: This composition for oral cavity is obtained by blending a quaternary ammonium salt type cationic antimicrobial agent selected from the group consisting of cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride and decalinium chloride or an antiplasmin agent such as tranexamic acid or ε-aminocaproic acid with sodium chloride and magnesium chloride. Furthermore, the magnesium chloride is blended at (1/1000) to (1/5) expressed in terms of weight ratio based on the sodium chloride in this prescription.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for oral cavity which is excellent in feeling of use and is effective for prevention and treatment of periodontal disease.

[0002]

2. Description of the Related Art Conventionally, quaternary ammonium salt type cationic antibacterial agents have been effective in suppressing plaque formation and preventing periodontal disease, and antiplasmin agents have excellent anti-inflammatory and hemostasis effects. It is known to be effective for the prevention of periodontal disease, and its incorporation into oral compositions has been studied and proposed. However, since they have a bitter taste, they need to be improved in order to be used in practice. In order to improve the bitterness of quaternary ammonium salt type cationic antibacterial agents, it has been conventionally practiced to increase the amount of sweeteners such as saccharin and dipotassium glycyrrhizinate, and sweetening polyhydric alcohols such as glycerin and sorbit. There is. Further, JP-A-5-931 proposes to use a stevia sweetener. In order to improve the bitterness of the antiplasmin agent, carvone and 1-menthol are used in combination (Japanese Patent Publication No. 61-92323), and aldecht fragrance, menthone, isomentone and pulegone are also used (JP-A-62-277314). No.), triclosan and l-menthyl acetate (JP-A-4-139117).

However, among these technologies, Stevia,
Dipotassium glycyrrhizinate has a problem that it has a unique bitterness. In addition, saccharin causes a decrease in the antibacterial activity of the cationic antibacterial agent, the flavor of the fragrance component is limited, and the polyhydric alcohols have a problem that the stickiness is increased and the usability is poor.

[0004]

The object of the present invention is to solve the above-mentioned problems, to provide a quaternary ammonium salt type cationic antibacterial agent which has an excellent feeling of use and is effective in the prevention and treatment of periodontal diseases. It is intended to provide an oral composition containing an antiplasmin agent.

[0005]

Means for Solving the Problems As a result of intensive studies to achieve the above object, the present inventors have combined sodium chloride and magnesium chloride together with a quaternary ammonium salt type cationic antibacterial agent or an antiplasmin agent. By doing so, it was found that the bitterness of the cationic antibacterial agent or antiplasmin agent was masked, and the present invention was completed.

[0006] That is, the present invention provides a composition for oral cavity, which comprises a quaternary ammonium salt type cationic antibacterial agent or antiplasmin agent, sodium chloride and magnesium chloride. is there. According to the present invention, these bitternesses are masked without impairing the effect of the quaternary ammonium salt type cationic antibacterial agent or antiplasmin agent used, the feeling of use is good, and excellent prevention against periodontal disease is provided. An oral composition showing a therapeutic effect can be provided.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION Examples of the quaternary ammonium salt type cationic antibacterial agent used in the present invention include cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride and decalinium chloride. In particular, cetylpyridinium chloride is preferable because of its antibacterial action and feeling of use. The quaternary ammonium salt type cationic antibacterial agent is usually
It is preferable that about 0.005 to 0.2% (% by weight, the same applies hereinafter) based on the total weight of the composition.

As the antiplasmin agent used in the present invention,
For example, tranexamic acid and ε-aminocaproic acid. Above all, tranexamic acid is preferable because of its anti-inflammatory effect and feeling of use. The antiplasmin agent is usually preferably added in an amount of about 0.005 to 0.2% based on the total weight of the composition.

In the present invention, a quaternary ammonium salt type cation and an antiplasmin agent may be used in combination,
The ratio can be appropriately selected, but usually the ratio of the weight ratio of the quaternary ammonium salt type cation is 1:10 to 10: 1, and the total amount of both is 0 based on the total weight of the composition. It is particularly preferable to add the compounding agent so as to be about 0.01 to 0.2%.

As sodium chloride to be used, any of those known to be used in oral compositions can be used, and as magnesium chloride, purified one having a purity of 95% or more can be used. Alternatively, bittern obtained as a by-product in producing salt from seawater containing a large amount of magnesium chloride may be used. Magnesium chloride is
Those coated on the sodium chloride crystal surface,
It may be encapsulated or may be added separately from sodium chloride. Sodium chloride is 0.5-5%
Especially, the concentration of sodium chloride is particularly preferably in the range of 0.5 to 5% based on the total weight of the composition, because the effect of masking is particularly high, and salty taste tends to increase at higher concentration. Further, magnesium chloride is preferably blended in a weight ratio of 1/1000 to 1/5 with respect to sodium chloride. If the mixing ratio of sodium chloride and magnesium chloride is less than this range, sweetness and mellowness will not occur, and if it is more than this range, the bitterness of magnesium chloride itself will tend to appear. Thus, it has been found that when the mixing ratio of sodium chloride and magnesium chloride is set in this way, an oral composition having a good feeling in use and having a high preventive and therapeutic effect on periodontal disease can be obtained.

The oral composition of the present invention is prepared according to a conventional method.
It can be made into various dosage forms, for example, a solid-liquid composition such as toothpaste, powdered toothpaste, water toothpaste, mouthwash, mouthwash, etc., and if desired, the effect of the present invention Abrasives, foaming agents, flavoring agents, wetting agents, binders, sweeteners, preservatives and various medicinal ingredients that are usually used in this type of composition can be appropriately blended within a range that does not impair. . Particularly, in the present invention, from the viewpoint of efficiently exhibiting the action of the quaternary ammonium salt type cationic antibacterial agent and the antiplasmin agent, a liquid composition such as a toothpaste, a mouthwash and a mouth refreshing agent can be prepared. preferable.

[0012]

EXAMPLES Next, the present invention will be described in more detail with reference to examples, but the present invention is not limited thereto. Examples 1 to 65 and Comparative Examples 1 to 23 Mouth washes were prepared according to the formulations shown in Tables 1 to 10, and taste tests were conducted by the following methods. Mouthwash Component Ingredient (%) Ethanol 7.0 Glycerin 13.0 Antibacterial agent (shown in Tables 1-10) Antiplasmin agent (shown in Tables 1-10) Masking agent (shown in Tables 1-10) Fragrance 0 .3 Purified water balance 100.0

[0013]

[Table 1]

[0014]

[Table 2]

[0015]

[Table 3]

[0016]

[Table 4]

[0017]

[Table 5]

[0018]

[Table 6]

[0019]

[Table 7]

[0020]

[Table 8]

[0021]

[Table 9]

[0022]

[Table 10]

Taste Test Method About 20 ml of mouthwash was rinsed for about 30 seconds, and the degree of bitterness remaining in the mouth after being contained in the mouth was sensory-evaluated according to the following evaluation criteria in four stages. The evaluation results are shown by rounding off the average score of 10 panelists. Evaluation criteria No bitterness ... 0 Almost no bitterness ... 1 Some bitterness ... 2 Some bitterness ... 3 The results are shown in Tables 1-10.

As is clear from these results, while the oral composition according to the present invention exhibits an excellent bitterness masking effect, the oral compositions given as Comparative Examples are insufficient in bitterness masking, The usability is inferior.

Example 66 A toothpaste was produced by a conventional method according to the following formulation. Ingredients Amount (%) Calcium carbonate 35.0 Silica anhydride 3.0 Sorbit 25.0 Sodium saccharin 0.05 Sodium carboxymethyl cellulose 1.5 Sodium lauryl sulfate 2.0 Cetylpyridinium chloride 0.05 Sodium chloride 15.0 Nigari Contained sodium chloride * 20.0 Fragrance 0.9 Purified water Balance 100.0 *: Sodium chloride crystals containing 2% magnesium chloride. That is, 10.0% sodium chloride and 0.4% magnesium chloride are contained in 20.0%.

Example 67 A toothpaste was produced according to the following formulation by a conventional method. Ingredients Ingredient (%) Calcium hydrogen phosphate 35.0 Silicic anhydride 3.0 Sorbit 25.0 Propylene glycol 5.0 Sodium carboxymethyl cellulose 1.0 Carrageenan 0.5 Sodium lauryl sulphate 1.5 Tranexamic acid 0.05 Sodium chloride 15.0 Magnesium chloride 2.0 Dipotassium glycyrrhizinate 0.05 Sodium saccharin 0.1 Perfume 0.9 Purified water Residual total 100.0

Example 68 A toothpaste was produced according to the following formulation by a conventional method. Ingredients Amount (%) Silica Anhydrous 20.0 Glycerin 10.0 Sorbit 35.0 Carboxymethyl Cellulose Sodium 1.0 Xanthan Gum 0.5 Sodium Lauryl Sulfate 1.5 Benzethonium Chloride 0.01 Vitamin E Acetate 0.05 Sodium Chloride 10.0 Magnesium chloride 1.0 Sodium saccharin 0.2 Perfume 0.9 Purified water balance Total 100.0

Example 69 A liquid dentifrice was produced according to the following formulation by a conventional method. Ingredients Blending amount (%) Glycerin 15.0 Ethanol 10.0 Polyoxyethylene hydrogenated castor oil 0.5 ε-Aminocaproic acid 0.05 Sodium chloride 2.0 Magnesium chloride 0.2 Citric acid 0.16 Trisodium citrate 0.32 Saccharin sodium 0.02 Fragrance 0.3 Purified water Balance 100.0

Example 70 A liquid dentifrice was produced according to the following formulation by a conventional method. Ingredients Blending amount (%) Sorbit 10.0 Ethanol 10.0 Polyoxyethylene hydrogenated castor oil 0.5 Cetylpyridinium chloride 0.05 Sodium chloride 1.0 Magnesium chloride 0.1 Sodium hydrogen phosphate 0.06 Phosphoric acid Sodium dihydrogen 0.01 Aluminum allantoinate 0.1 Sodium saccharin 0.02 Perfume 0.25 Purified water Residual total 100.0

Example 71 A liquid dentifrice was produced according to the following formulation by a conventional method. Ingredients Content (%) Glycerin 10.0 Ethanol 10.0 Polyoxyethylene polyoxypropylene block copolymer 1.0 Tranexamic acid 0.05 Sodium chloride 3.0 Magnesium chloride 0.2 Vitamin E Nicotinate 0.2 Triclosan 0.2 1 Citric acid 0.16 Trisodium citrate 0.32 Stevia extract 0.05 Perfume 0.2 Purified water Residual total 100.0

Example 72 A mouthwash was manufactured according to the following formulation by a conventional method. Ingredients Content (%) Glycerin 10.0 Polyoxyethylene hydrogenated castor oil 1.0 Benzethonium chloride 0.02 Sodium chloride 0.5 Magnesium chloride 0.05 Sodium fluoride 0.03 Stevia extract 0.05 Citric acid 0.0 16 Trisodium citrate 0.32 Perfume 0.2 Purified water Balance 100.0

Example 73 A mouthwash was manufactured according to the following formulation by a conventional method. Ingredients Amount (%) Glycerin 13.0 Ethanol 7.0 Polyoxyethylene hydrogenated castor oil 0.4 Tranexamic acid 0.05 Nigari-containing sodium chloride * 1.5 Malic acid 0.01 Sodium malate 0.14 Saccharin sodium 0 .03 Fragrance 0.25 Purified water balance 100.0 *: Sodium chloride crystal containing 1% magnesium chloride. Therefore, 1.5% contains 1.485% sodium chloride and 0.015% magnesium chloride.

[0033]

According to the present invention, even if a quaternary ammonium salt type cationic antibacterial agent or antiplasmin agent is added,
It is possible to provide an oral composition in which the bitterness is masked, the feeling of use is good, and the preventive and therapeutic effects on periodontal disease are excellent.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification code Internal reference number FI Technical display area A61K 47/02 A61K 47/02 L // (A61K 31/14 31: 195) (A61K 31/44 31: 195)

Claims (6)

[Claims] 1. An oral composition comprising a quaternary ammonium salt type cationic antibacterial agent or antiplasmin agent, sodium chloride and magnesium chloride. 2. The oral composition according to claim 1, wherein the quaternary ammonium salt type cationic antibacterial agent is one or more selected from cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride and decalinium chloride. . 3. The oral composition according to claim 1, wherein the antiplasmin agent is tranexamic acid. 4. The oral composition according to claim 1, wherein the antiplasmin agent is ε-aminocaproic acid. 5. The composition for oral cavity according to claim 1, wherein the mixing ratio of magnesium chloride is 1/1000 to 1/5 by weight ratio with respect to sodium chloride. 6. The oral composition according to claim 1, which is a liquid composition.