JP2979444B2 - Oral composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition for effectively and continuously inhibiting the formation of tartar.

[0002]

2. Description of the Related Art Tartar is a hard deposit with a high inorganic content generated on the tooth surface and is a major cause of gingivitis, periodontitis and the like.
Therefore, suppressing the formation of tartar is very effective in preventing and treating periodontal disease.

[0003] The formation of this tartar is thought to be due to the fact that amorphous or microcrystalline calcium phosphate is deposited on bacteria and inter-bacterial substances in plaque, and gradually becomes dense and changes to hydroxyapatite. In order to suppress the formation, it suffices to inhibit the crystal growth of hydroxyapatite. Therefore, it is desired to develop an oral composition capable of effectively suppressing the formation of hydroxyapatite.

Conventionally, various proposals have been made to prevent tartar. For example, Japanese Patent Publication No. 45-23637 and Japanese Patent Publication No. 49-27339 disclose many phosphonic acid compounds as tartar preventive agents. ing. Also.
"Arch. Oral Biol., Vo. 15, P.
893-896 (1970) "shows the effectiveness of soluble phosphate on tartar.

[0005] The present invention has also been made to solve such a problem, and it is intended to inhibit the crystal growth of hydroxyapatite and to continuously suppress the formation of tartar, thereby effectively preventing gingivitis and periodontitis. It is an object of the present invention to provide an oral composition that can be used.

[0006]

Means and Action for Solving the Problems The present inventors have
As a result of intensive studies to achieve the above object, the average polymerization ratio of D-mannuronic acid and L-guluronic acid (hereinafter referred to as average M / G ratio) was 0.2 to 1 and alginic acid or a salt thereof was averaged. It has been found that it is effective to use a water-soluble polyphosphate having a degree of polymerization of 2 to 100 in combination.

That is, alginic acid is a hydrophilic high molecular compound obtained by extracting and purifying brown algae such as kajime, alame, kelp, macrocysteis, ascophyllum, econia maxima, and lessonia by a chemical operation. It is a polymer of D-mannuronic acid [M] having β-1,4 bond and L-guluronic acid [G] having α-1,4 bond shown in the following formula. The M / G ratio is
It depends on the type and site of the raw material, the extraction method, and the like.

[0008]

Embedded image

Such alginic acid or a salt thereof has been conventionally used as a binder for toothpaste, a dental impression agent, a food stabilizer,
Properties suitable for the printing paste and the like are used. It is also known that sodium alginate suppresses the formation of plaque (Japanese Patent Laid-Open No. Hei 1-213222).
issue).

However, the present inventors have conducted comparative studies on the effects of alginic acid or its salts having different degrees of polymerization and M / G ratios on preventing bacterial adhesion and on inhibiting the crystal growth of hydroxyapatite. The average M / G ratio of the obtained alginic acid or a salt thereof is more than 1.0 and is usually in the range of 1.2 to 2.0, but the average M / G ratio is 0.2 to 1 When alginic acid or a salt thereof is used, the crystal growth of hydroxyapatite is effectively suppressed, and in alginic acid or a salt thereof having such an average M / G ratio, the average degree of polymerization is 800 to
In the case of using the one of 1500, it is found that it effectively suppresses the adhesion of bacteria to hydroxyapatite coated with saliva, and has an excellent bacterial adhesion inhibiting effect,
An oral composition containing alginic acid or a salt thereof having an average M / G ratio of 0.2 to 1 has been previously proposed (Japanese Patent Application No. 2-141).
013).

However, when the average M / G ratio is 0.2 to 1
In the oral composition containing alginic acid or a salt thereof, the calcification inhibition rate decreases with time. As a result of further study on preventing the decrease with time, the average M / G
When a water-soluble polyphosphate is further used in combination with alginic acid or a salt thereof having a ratio of 0.2 to 1, these act synergistically,
The inventors of the present invention have found that the calcification inhibition rate is remarkably prevented from decreasing over time, the effect is sustained, and the calcification inhibition rate can be increased, and the present invention has been accomplished.

Hereinafter, the present invention will be described in more detail. The oral composition according to the present invention includes dentifrices such as toothpastes and dentifrices, mouthwashes, gargle tablets, gingival massage creams, liquid or pasty topical creams. It is prepared and applied as a coating agent, troche, chewing gum and the like. As a component for preventing periodontal disease, the average M / G ratio is 0.2 to 1, preferably the average degree of polymerization is 800 to 1,50.
Alginic acid or a salt thereof having an average degree of polymerization of 2 to 100;
And a water-soluble polyphosphate.

As the salt of alginic acid, sodium, potassium, lithium, ammonium, calcium, magnesium and the like are used.

In the present invention, the amount of alginic acid or a salt thereof is not particularly limited, but is usually 0.001 to 5% (% by weight, hereinafter the same) of the entire oral composition, preferably 0.02 to 5%. 2%. If the amount is less than 0.001%, the effect of inhibiting bacterial adhesion and the effect of inhibiting crystal growth of hydroxyapatite may not be sufficiently exhibited,
If it is more than 5%, problems such as excessively high viscosity of the composition may occur.

As the water-soluble polyphosphate, those having an average degree of polymerization of 2 to 100, preferably 2 to 70 are used. In this case, examples of the salt of the water-soluble polyphosphoric acid include, for example, sodium and potassium, and a sodium salt is particularly preferably used.

The amount of the water-soluble polyphosphate is preferably 0.01 to 10%, especially 0.5 to 5% of the whole composition. If the amount is less than 0.01%, the synergistic effect of the combination may not be exhibited, and if it exceeds 10%, the taste of the composition may be deteriorated.

The oral composition of the present invention may further contain, in addition to the above-mentioned components, appropriate components according to the purpose, the type of the composition and the like.

For example, in the case of dentifrices, dibasic calcium phosphate dihydrate and anhydride, monobasic calcium phosphate, tribasic calcium phosphate, calcium carbonate, calcium pyrophosphate, aluminum hydroxide, alumina, silicate anhydride are used as abrasives. One or more of aluminum silicate, insoluble sodium metaphosphate, dibasic magnesium phosphate, magnesium carbonate, calcium sulfate, polymethyl methacrylate, other synthetic resins, bentonite, zirconium silicate and the like ( Normally 20%
90%, 20% -60% for toothpaste).

In the case of paste-like compositions such as toothpaste, cellulose derivatives such as carrageenan, sodium carboxymethylcellulose, methylcellulose, hydroxyethylcellulose, sodium carboxymethylhydroxyethylcellulose, propylene glycol alginate, xanthan gum, etc. Gums such as tragacanth gum, karaya gum, arabia gum, etc., synthetic binders such as polyvinyl alcohol, sodium polyacrylate, carboxyvinyl polymer, polyvinylpyrrolidone, etc., and inorganic binders such as silica gel, aluminum silica gel, veegum, laponite, etc. or Two or more kinds may be blended (the blending amount is usually 0.3 to 5%).

Further, in the production of paste or liquid oral compositions such as dentifrices, sorbitol, ethylene glycol, propylene glycol, 1,3-butylene glycol, polyethylene glycol, polypropylene glycol, xylitol, maltitol are used as thickeners. , Lactitol and the like (compounding amount: usually 10 to 70%).

As the surfactant, one or more of an anionic surfactant, a nonionic surfactant and an amphoteric surfactant can be blended (the blending amount is usually 0.1 to 10%).
5%).

Examples of the anionic surfactant include sodium alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate; and N-type surfactants such as sodium N-lauroyl sarcosinate and sodium N-myristoyl sarcosinate.
N such as sodium acylsarcosinate, sodium dodecylbenzenesulfonate, hydrogenated coconut fatty acid sodium monoglyceride monosulfate, sodium lauryl sulfoacetate, sodium N-palmitoyl glutamate, etc.
-Acylglutamate, sodium N-methyl-N-acyltaurine, sodium N-methyl-N-acylalanine, sodium α-olefinsulfonate, sodium dioctylsulfosuccinate and the like are used.

Examples of the nonionic surfactant include sugar alcohol fatty acid esters such as sucrose fatty acid ester, maltose fatty acid ester, lactose fatty acid ester, maltitol fatty acid ester and lactitol fatty acid ester, polyoxyethylene sorbitan monolaurate, and the like.
Polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan monostearate; polyoxyethylene fatty acid esters such as polyoxyethylene hydrogenated castor oil; fatty acid diethanolamide such as lauric acid mono- or diethanolamide, myristic acid mono- or diethanolamide; sorbitan Fatty acid esters, fatty acid monoglycerides, polyoxyethylene higher alcohol ethers, polyoxyethylene polyoxypropylene fatty acid esters and the like are used.

Examples of zwitterionic surfactants include N-alkyldiaminoethylglycine such as N-lauryldiaminoethylglycine and N-myristyldiaminoethylglycine, N-alkyl-N-carboxymethylammonium betaine, 2-alkyl-1-. Hydroxyethylimidazoline betaine sodium and the like are used.

The oral composition of the present invention further comprises menthol, carvone, anethole, methyl salicylate, eugenol, isoeugenol, limonene, ocimene, n-
Decyl alcohol, citronellol, α-terpineol, methyl acetate, citronellyl acetate, cineol, linalool, ethyl linalool, crocodile, thymol, spearmint oil, peppermint oil, lemon oil,
Perfume such as orange oil, sage oil, rosemary oil, cinnamon oil, pimento oil, laurel oil, perilla oil, winter green oil, clove oil, eucalyptus oil or the like, alone or in combination, from 0 to 10
%, Preferably about 0.5 to 5%, and sweeteners such as saccharin sodium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartin, thaumatin, asparatyl phenylalanine methyl ester, p-methoxycinnamic aldehyde, etc. To 1%, preferably 0.01 to 0.5%).

In the present invention, as active ingredients, cationic bactericides such as chlorhexidine, benzethonium chloride, benzalkonium chloride, cetylpyridinium chloride, and decalinium chloride;
Phenolic compounds such as triclosan, hinokitiol, and biosol; enzymes such as dextranase, mutanase, lysozyme, amylase, protease, lytic enzyme, and superoxide dismutase; and alkali metal monofluorocarbons such as sodium monofluorophosphate and potassium monofluorophosphate. Phosphate, sodium fluoride,
Fluorides such as stannous fluoride, tranexamic acid, epsilon aminocaproic acid, aluminum chlorohydroxyl allantoin, dihydrocholestanol, glycyrrhizic acids, glycyrrhetinic acid, bisabolol, glycerophosphate, chlorophyll, vitamin C, ascorbic acid 2-phosphate, One or more active ingredients such as vitamin C derivatives such as 2-0-glucosyl ascorbic acid and sodium chloride may be blended.

[0027]

The oral composition of the present invention has an average M / G ratio of 0.2 to 1, preferably an average degree of polymerization of 800 to 1,
500 alginic acid or a salt thereof and an average degree of polymerization of 2 to 10
By mixing with a water-soluble polyphosphate of 0, hydroxyapatite crystal growth is inhibited and calculus formation is particularly continuously suppressed, which is very effective in preventing gingivitis and periodontitis.

[0028]

EXAMPLES Next, the effects of the present invention will be specifically described with reference to experimental examples.

[Experimental example] Experiment for increasing the sustained effect of the calcification inhibitory effect Calcification reaction solution (0.7 mM CaCl ₂ , 2.59 mM
KH ₂ PO ₄ , 50 mM NaCl, pH 7.4) 1
20 ml of sodium alginate (average degree of polymerization 1260) and sodium tripolyphosphate 1 shown in Table 1
ppm, and the mixture was kept warm at 37 ° C., and a solution of hydroxyapatite powder (Central Glass) 60 m
g, and the pH was measured after 30 minutes, 1 hour, and 2 hours. The calcification inhibition rate was determined by the following equation. Table 1 shows the results.

[0030]

(Equation 1) A: pH change of control solution B: pH change of drug added solution

[0031]

[Table 1]

From the results shown in Table 1, when sodium alginate having an M / G ratio of 0.2 to 1 and polyphosphate are used in combination,
It can be seen that the calcification suppression effect is maintained for a long time.

Hereinafter, examples will be described, but the present invention is not limited to the following examples.

Example 1 Toothpaste Aluminum hydroxide 45.0% Gelling silica 2.0 Sorbit 25.0 Sodium carboxymethylcellulose 0.5 Sodium alginate 0.5 (Average degree of polymerization 1440, M / G ratio 1) 1.0) Sodium polyphosphate (n = 3) 1.0 Sucrose monopalmitate 1.0 Sodium lauryl sulfate 1.5 Saccharin sodium 0.2 Ethanol 0.1 Sodium benzoate 0.1 Triclosan 0.1 Fragrance 1.0 Water balance 100.0%

[Example 2] Toothpaste Precipitable silica 25.0% Sorvit 25.0 Glycerin 25.0 Polyvinylpyrrolidone 0.8 Sodium alginate 0.4 (Average degree of polymerization 1260, M / G ratio 0.52) Polyline Sodium acid salt (n = 3) 1.0 Sodium pyrophosphate 2.0 Lauroyl polyglycerin ester 1.0 Polyoxyethylene (60 mol) 0.5 Sorbitan monolaurate Saccharin sodium 0.2 Ethyl parahydroxybenzoate 0.1 Chlorhexidine Hydrochloride 0.1 Triclosan 0.05 Fragrance 1.0 Water Balance 100.0%

Example 3 Toothpaste 20.0% dibasic calcium phosphate dihydrate 20.0% dibasic calcium phosphate dihydrate 20.0 gelling silica 2.0 sorbite 20.0 propylene glycol 2.5 carboxy Sodium methylcellulose 0.5 Sodium alginate 0.3 (average degree of polymerization 840, M / G ratio 0.91) Sodium pyrophosphate 3.0 Sodium polyphosphate (n = 63) 0.5 Lauryl diethanolamide 1.0 Lauryl sulfate Sodium 1.5 Lauroyl sarcosine sodium 0.3 Saccharin sodium 0.1 Ethyl parahydroxybenzoate 0.1 Fragrance 0.8 Water Residue 100.0%

Example 4 Oral Pasta Cetanol 5.0% Squalane 20.0 Precipitable Silica 5.0 Sodium Alginate 1.0 (Average Degree of Polymerization 1160, M / G Ratio 0.85) Sodium Polyphosphate (n) = 3) 2.0 Polyoxyethylene (40 mol) hydrogenated castor oil 0.1 Sorbitan monooleate 1.0 Sodium lauryl sulfate 0.2 Glycyrrhetinic acid 0.1 Saccharin sodium 0.6 Triclosan 0.3 Perfume 0.6 Water balance 100.0%

Example 5 Oral Pasta Liquid Paraffin 15.0% Cetanol 7.0 Glycerin 20.0 Sodium Alginate 1.0 (Average Degree of Polymerization 1000, M / G Ratio 0.52) Sodium Polyphosphate (n = 53) 2.0 Sorbitan monopalmitate 0.6 Polyoxyethylene (40 mol) 5.0 Sorbitan monostearate Sodium lauryl sulfate 0.1 Saccharin sodium 0.5 Benzethonium chloride 0.1 Perfume 0.5 Water Balance 100. 0%

Example 6 Mouthwash Sorbit 10.0% Ethanol 5.0 Sodium Alginate 0.2 (Average Degree of Polymerization 800, M / G Ratio 0.21) Sodium Polyphosphate (n = 3) 3.0 Poly Oxyethylene (60 mol) hydrogenated castor oil 0.1 sucrose monopalmitate 0.2 sodium lauryl sulfate 0.05 saccharin sodium 0.2 benzethonium chloride 0.05 fragrance 0.6 water balance 100.0%

Example 7 Oral Lozenges Lactose 96.0% Sodium Alginate 1.5 (Average Degree of Polymerization 800, M / G Ratio 0.21) Sodium Polyphosphate (n = 3) 1.0 Polyoxyethylene ( 60 mol) monostearate 0.2 chlorhexidine gluconate 0.02 stevia extract 0.2 fragrance 0.02 hydroxyethylcellulose balance 100.0%

[Example 8] Chewing gum gum base 20.0% sugar 15.0 isomaltose 20.0 palatinose 20.0 corn syrup 12.0 starch syrup 11.9 sodium alginate 0.5 (average degree of polymerization 840, M / G Ratio 0.91) Sodium polyphosphate (n = 3) 1.0 Fragrance 0.6 Total 100.0%

Example 9 Candy Sugar 30.0% Isomaltose 10.0 Palatinose 10.0 Maltose 10.0 Syrup Cane 23.0 Organic Acid 2.0 Sodium Alginate 0.5 (Average Degree of Polymerization 1440, M / G Ratio 1.0) Sodium polyphosphate (n = 14) 2.0 Fragrance 0.5 Water Balance 100.0%

──────────────────────────────────────────────────続 き Continued on the front page (58) Field surveyed (Int.Cl. ⁶ , DB name) A61K 7/16

Claims (1)

(57) [Claims] An alginic acid having an average weight ratio of D-mannuronic acid and L-guluronic acid of 0.2 to 1 or a salt thereof, and a water-soluble polyphosphate having an average degree of polymerization of 2 to 100. An oral composition characterized by comprising: