JP2006151876A - Composition for preventing periodontal disease - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a composition for preventing periodontal diseases having excellent action for suppressing intracellular toxin activity and safe and stable for long time usage. <P>SOLUTION: The composition for preventing periodontal diseases contains cetylpyridinium chloride, lecithin and hydroxyapatite. Preferably, the composition for preventing periodontal diseases contains 0.001-0.1 mass% cetylpyridinium chloride, 0.05-5 mass% lecithin and 1-25 mass% hydroxyapatite. <P>COPYRIGHT: (C)2006,JPO&NCIPI

Description

  The present invention relates to a composition for preventing periodontal disease that can prevent periodontal disease caused by periodontal disease bacterial endotoxin.

  As pathogenic factors for periodontal diseases, adhesion factors (pilus, lectin-like ligand), endotoxin, tissue destructive enzymes (collagenase, trypsin-like enzyme), leukocyte resistance factor (capsule, superoxide desmutase, leukotriene) and There are cytotoxic metabolites (hydrogen sulfide, fatty acids) and the like. Among them, bacterial endotoxins have been confirmed to cause inflammation or periodontal bone resorption directly or indirectly against periodontal tissue.

  As a conventional technique for the prevention of periodontal diseases involving endotoxin, a pretreatment agent for periodontal tissue regeneration with a macrolide antibiotic (see Patent Document 1: JP-A-7-267867), octadecylpropyldimethylammonium fixed Endotoxin adsorption / removal agent by water-insoluble solid (Patent Document 2: Japanese Patent Laid-Open No. 8-26954), bacterial toxin neutralizer by aliphatic amine or aminocarbonyl reaction product (Patent Documents 1, 3-5: 7-267867, JP-A-7-82153, JP-A-5-271065, and JP-A-7-33679). However, when these are used as oral compositions, there are problems in the appearance of resistant bacteria, side effects, adhesion of stains to teeth, safety, and effects.

  As a conventional technique for solving this problem, an anti-endotoxin agent containing taurine as an active ingredient (Patent Document 6: see JP-A-10-158158), glutamic acid, lysozyme, cetylpyridinium chloride and benzethonium chloride An anti-endotoxin agent characterized by using two or more components in combination (Patent Document 7: see JP-A-11-12168), an oral composition comprising lactoferrin and an amino acid (Patent Document 8: JP 2001-89339 A). However, the anti-endotoxin agent containing taurine as an active ingredient was evaluated for its indirect endotoxin inhibitory activity using rabbits. In that case, since the effects of endotoxin inhibitors in the living body may affect the evaluation results, in order to evaluate the inhibitory activity of bacterial endotoxin, the endotoxin activity is directly evaluated and the inhibitory effect It is desirable to measure. An anti-endotoxin that combines two or more active ingredients selected from glutamic acid, lysozyme, cetylpyridinium chloride, and benzethonium chloride, and an oral composition that combines lactoferrin and an amino acid are directly evaluated for bacterial endotoxin inhibitory activity Met. However, it is technically difficult to stably mix lysozyme chloride and lactoferrin protein components, which are one of the active ingredients, and can be stably blended into stable blending technology and oral composition of lysozyme chloride or lactoferrin. There has been a demand for a component capable of obtaining a bacterial endotoxin inhibiting effect.

JP-A-7-267867 JP-A-8-26954 JP-A-7-82153 Japanese Patent Application Laid-Open No. 5-271055 Japanese Patent Laid-Open No. 7-33679 JP-A-10-158158 Japanese Patent Laid-Open No. 11-12168 JP 2001-89339 A

  The present invention has been made in view of the above circumstances, and has an object to provide a composition for preventing periodontal disease that has an excellent inhibitory effect on bacterial endotoxin activity and is safe and stable even when used for a long period of time. To do.

  As a result of intensive studies to achieve the above object, the present inventor has achieved excellent bacterial endotoxin activity inhibitory action in bacterial endotoxin activity inhibition tests by using cetylpyridinium chloride, lecithin and hydroxyapatite in combination. Therefore, the present inventors have found that a composition effective for the prevention of periodontal diseases can be obtained, and have made the present invention.

  Accordingly, the present invention provides a composition for preventing periodontal disease, comprising cetylpyridinium chloride, lecithin and hydroxyapatite. In this case, 0.001 to 0.1% by mass of cetylpyridinium chloride, 0.05 to 5% by mass of lecithin, and 1 to 25% by mass of hydroxyapatite are preferably contained. It is preferable to contain lecithin and hydroxyapatite in a mass ratio of 0.001 to 0.005: 0.05 to 0.2: 1.

  ADVANTAGE OF THE INVENTION According to this invention, it has the outstanding inhibitory effect of bacterial endotoxin activity, and is safe and stable even if it is used for a long period of time, and can be used effectively for prevention of periodontal disease.

  The composition for preventing periodontal disease of the present invention contains cetylpyridinium chloride, lecithin and hydroxyapatite in combination as an effective ingredient for preventing periodontal disease.

Cetylpyridinium chloride used in the present invention has a bactericidal effect on oral bacteria, an inhibitory effect on plaques, and an improvement effect on gingivitis, and is therefore widely used as a bactericidal agent in oral compositions. Lecithin is widely distributed in the living bodies of plants, animals and microorganisms, and is extracted and separated from these living bodies to produce products. Mainly, soybean lecithin and egg yolk lecithin are commercially available. Such lecithin is widely used as an emulsifier in oral compositions, particularly chewing gum. The lecithin used in the present invention is particularly preferably derived from soybean. Hydroxyapatite is used in oral compositions as a remineralization accelerator for tooth enamel. The hydroxyapatite used in the present invention is preferably a high-purity hydroxyapatite containing at least 90% (mass%, the same shall apply hereinafter), desirably 95% or more of Ca ₁₀ (PO ₄ ) ₆ (OH) ₂ . Specifically, there is “Sekisui Pamicron” manufactured by Sekisui Plastics Co., Ltd. The hydroxyapatite particle size used in the present invention may be any particle size, but when used in an appropriate amount, this component has a particle size that can be satisfactorily cleaned without harming the tooth surface. Preferably used. The average particle size of such hydroxyapatite is preferably about 1 to 100 μm, more preferably 2 to 50 μm, and still more preferably 3 to 20 μm. The average particle size is a value measured by a particle size analyzer model 7990-20 manufactured by LEEDS & North Rup.

  In the composition of the present invention, the amount of cetylpyridinium chloride is preferably 0.001 to 0.1%, particularly preferably 0.005 to 0.05% of the composition. If the blending amount is less than 0.001%, a satisfactory effect may not be obtained, and if it exceeds 0.1%, a problem may occur in flavor. The amount of lecithin is preferably 0.05% to 5%, particularly 0.1 to 1% of the composition. If the blending amount is less than 0.05%, a satisfactory effect may not be obtained, and if it exceeds 5%, a problem may occur in flavor. The compounding amount of hydroxyapatite is 1 to 25% of the whole composition, more preferably 2 to 20%, and still more preferably 3 to 15%. If the blending amount is less than 1%, a satisfactory effect may not be obtained, and if it exceeds 25%, the composition may be too hard.

  Further, in the composition of the present invention, the content ratio of cetylpyridinium chloride A, lecithin B, and hydroxyapatite C is within a range not exceeding the above concentration as A: B: C = 0.001 to 0.005: It is preferably 0.05 to 0.2: 1, particularly preferably 0.001 to 0.004: 0.05 to 0.2: 1.

  In the composition of the present invention, components used in normal oral compositions and food compositions other than those described above can be used depending on the type, and the amount of these components added is determined according to the present invention. The amount can be adjusted within the range that does not interfere with the effect.

  For example, if it is a dentifrice composition, an abrasive, a thickener, a binder, a surfactant, a sweetener, an antiseptic, various active ingredients, a colorant, a fragrance, etc. can be blended. Silica-based abrasives such as precipitated silica, silica gel, aluminosilicate, zirconosilicate, dicalcium phosphate dihydrate and anhydrous, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, triphosphate Magnesium, zeolite, zirconium silicate, synthetic resin-based abrasive and the like are preferably used.

  As the thickener, glycerin, sorbit, propylene glycol, polyethylene glycol, xylit, maltite, lactit and the like can be blended.

  As the binder, sodium carboxymethyl cellulose, hydroxyethyl cellulose, carrageenan, sodium alginate, xanthan gum, carbopol, guaia gum, montmorillonite, gelatin and the like can be blended.

  As the surfactant, an anionic surfactant, a cationic surfactant other than the cetylpyridinium chloride, a nonionic surfactant, and the like can be blended. Specifically, sodium lauryl sulfate, α-olefin sulfonic acid Sodium, N-acyl sarcosinate, N-acyl glutamate, 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine, N-acyl taurate, sucrose fatty acid ester, alkylol amide, polyoxyethylene Hardened castor oil, polyglycerin fatty acid ester, polyoxyethylene sorbitan monostearate and the like can be blended.

  As sweeteners, sodium saccharin, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, perilartine and the like can be blended, and as preservatives, paraoxybenzoate, sodium benzoate and the like can be blended.

  Various active ingredients include fluorides such as sodium fluoride, potassium fluoride, ammonium fluoride, stannous fluoride, sodium monofluorophosphate, and water-soluble phosphate compounds such as potassium salt and sodium salt of orthophosphoric acid. Allantochlorohydroxyaluminum, lysozyme chloride, glycyrrhizic acid and its salts, sodium chloride, epsilon aminocaproic acid, α-bisabolol, isopropylmethylphenol, chlorohexidine salts, benzethonium chloride, benzalkonium chloride, azulene, water-soluble azulene, glycyrrhetinic acid, Copper compounds such as dipotassium glycyrrhizinate, copper chlorophyllin sodium and copper gluconate, aluminum lactate, strontium chloride, potassium nitrate, berberine, hydroxamic acid and its derivatives, tripolylysate Sodium acid, zeolite, dextranase, mutanase, amylase, methoxyethylene, maleic anhydride copolymer, polyvinyl pyrrolidone, epidihydrocholesterin, dihydrocholesterol, trichlorocarbanilide, zinc citrate, soft extract of Japanese cherry, clove, rose Extracts such as Marie, Ogon, and safflower can be blended.

  Examples of the colorant include blue No. 1, yellow No. 4, titanium dioxide, alumina oxide and the like. In addition, a fragrance | flavor etc. can be mix | blended.

  The composition of the present invention is most effective when used as a toothpaste, liquid toothpaste or foam toothpaste, and can also be applied to troches, chewing gums, gummies and candies.

  Moreover, in this invention, the composition can be used by the normal usage method and use frequency according to the kind of composition.

  EXAMPLES Hereinafter, although an experiment example and an Example are shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example. In addition, all% in each example is the mass%.

[Experimental example]
In Vitro Endotoxin Activity Inhibition Test An in vitro endotoxin activity inhibition test was carried out by the following method, using a modified end space method (Seikagaku Corporation).
After incubating porphyromonas gingivalis endotoxin (hereinafter abbreviated as Pg LPS) 2 μg / ml and 1 ml of various drugs shown in Table 1 for 30 minutes at 37 ° C. The LPS was diluted to 10 to 50 pg / ml, and the endotoxic activity suppression rate by the end-spacey method was determined as P.P. g. The inactivation rate was evaluated. The results are shown in Table 1.

Cetylpyridinium chloride: Wako Pure Chemical Industries, Ltd.
Soy lecithin: Hydroxyapatite manufactured by Honen Corporation: Sekisui Plastics Co., Ltd.

From the above results, by combining the three of cetylpyridinium chloride, soybean lecithin and hydroxyapatite, P.I. g. It was observed that a synergistic effect of inactivation rate was obtained.
Examples in which the active ingredient according to the present invention is blended in various compositions will be shown below as examples.

[Example 1] Toothpaste cetylpyridinium chloride 0.01% by mass
Soy lecithin 0.5
Hydroxyapatite 5
Calcium carbonate 45
Sorbit 24
Carrageenan 0.7
Sodium alginate 0.3
Saccharin sodium 0.1
Gelatin 0.2
Lauric acid diethanolamide 0.8
Propylene glycol 4
Fragrance 1
Lauroyl sarcosine sodium 0.4
Sodium monofluorophosphate 0.75
Purified water balance
100.0 mass% in total

[Example 2] Toothpaste cetylpyridinium chloride 0.01% by mass
Soy lecithin 0.5
Hydroxyapatite 5
Silica 20
Sorbit 60
Saccharin sodium 0.15
Gelatin 0.3
Lauric acid diethanolamide 1.5
Propylene glycol 5
Fragrance 1.5
Lauroyl sarcosine sodium 0.5
Sodium fluoride 0.2
Xanthan gum 0.5
Polyethylene glycol # 4000 0.5
Purified water balance
100.0 mass% in total

[Example 3] Toothpaste cetylpyridinium chloride 0.01% by mass
Soy lecithin 0.5
Hydroxyapatite 5
Modified aluminum hydroxide 50
Carrageenan 0.5
Xanthan gum 0.5
Saccharin sodium 0.14
Propylene glycol 5
Fragrance 1
Myristoyl sarcosine sodium 0.3
Sodium fluoride 0.5
Glycerin 20
Silicic anhydride 5
Titanium oxide 0.5
Sodium carboxymethylcellulose 0.1
Purified water balance
100.0 mass% in total

[Example 4] Liquid dentifrice cetylpyridinium chloride 0.01% by mass
Soy lecithin 0.5
Hydroxyapatite 5
Precipitated silica 20
Butyl paraoxybenzoate 0.01
Xanthan gum 0.2
Sodium polyacrylate 0. l5
Propylene glycol 2
Sorbit 35
Glycerin 25
Saccharin sodium 0.1
Fragrance 1
Dye (Brilliant Blue) 0.001
Decaglyceryl monolaurate 4
Purified water balance
100.0 mass% in total

[Example 5] Foam dentifrice cetylpyridinium chloride 0.01% by mass
Soy lecithin 0.5
Hydroxyapatite 5
Polyoxyethylene (60) hydrogenated castor oil 1
2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine 0.06
Glycerin (85%) 10
Propylene glycol 1
Xanthan gum 0.1
Polyvinylpyrrolidone 0.5
Xylitol 1
Citric acid 0.08
Sodium citrate 0.2
Sodium benzoate 0.3
Methylparaben 0.2
Fragrance 0.5
Purified water balance
100.0 mass% in total

[Example 6] Troche cetylpyridinium chloride 0.01% by mass
Soy lecithin 0.5
Hydroxyapatite 5
Gum arabic 6
Fragrance 1
Sodium monofluorophosphate 0.05
Lauroyl sarcosine sodium 0.01
Glucose 36
Palatinose 36
Purified water balance
100.0 mass% in total

[Example 7] Chewing gum cetylpyridinium chloride 0.01% by mass
Soy lecithin 0.5
Hydroxyapatite 5
Gum base 20
Fragrance 1
Sodium monofluorophosphate 0.1
Lauroyl sarcosine sodium 0.01
Calcium carbonate 2
Minamata 15
Powdered sugar 55
Purified water balance
100.0 mass% in total

[Example 8] Gummy cetylpyridinium chloride 0.01% by mass
Soy lecithin 0.5
Hydroxyapatite 5
Sugar 40.2
Minamata 44.8
Gelatin 8.0
Citric acid 1.0
Fragrance 0.49
100.0 mass% in total

[Example 9] Candy cetylpyridinium chloride 0.01% by mass
Soy lecithin 0.5
Hydroxyapatite 5
Sugar 50.0
Minamata 33.0
Organic acid 2.0
Fragrance 0.2
Purified water balance
100.0 mass% in total

Claims (3)

  A composition for preventing periodontal disease, comprising cetylpyridinium chloride, lecithin and hydroxyapatite.   A composition for preventing periodontal disease comprising 0.001 to 0.1% by mass of cetylpyridinium chloride, 0.05 to 5% by mass of lecithin, and 1 to 25% by mass of hydroxyapatite. The composition for preventing periodontal disease according to claim 2, comprising cetylpyridinium chloride, lecithin and hydroxyapatite in a mass ratio of 0.001 to 0.005: 0.05 to 0.2: 1.