JP2604807B2 - Toothpaste composition - Google Patents

Description

Description: FIELD OF THE INVENTION The present invention relates to a dentifrice composition, and more particularly, it is suitable for inhibiting plaque formation and preventing gingivitis by preventing the bactericidal activity of triclosan-containing dentifrice over time. Dentifrice compositions.

2. Description of the Related Art Conventionally, it has been established that plaque deposited on teeth is an important factor as a cause of gingivitis. Means for removing such plaque include physical oral cleaning by brushing or the like, but it takes a long time,
It is very difficult to remove sufficiently.

In order to compensate for this, various oral preparations such as dentifrices to which a bactericide has been added have been studied, and they are reported to have an antiplaque effect. In particular, it is known that cationic bactericides are effective in suppressing plaque formation,
It has poor compatibility with other dentifrice components, and has not yet completed a highly marketable dentifrice.

In recent years, it has been proposed to incorporate a non-cationic bactericide having excellent compatibility with the dentifrice component into the dentifrice in order to solve such a drawback. Among them, it has been reported that dentifrices containing triclosan, a typical non-cationic bactericide, have an excellent antiplaque effect (JP-A-60-239409).
No. 60-239410).

However, such triclosan-containing dentifrices have an excellent bactericidal activity at an early stage, but have a problem that the bactericidal activity decreases with time.

Means for Solving the Problems While the present inventors have been conducting various studies on such triclosan-containing dentifrices, surprisingly, by using triclosan in combination with a specific binder and a surfactant, the bactericidal activity is improved. The present inventors have found that toothpaste that can be stably maintained for a long period of time can be obtained, and the present invention has been completed.

That is, the present invention provides (a) one or two kinds of binders selected from the group consisting of hydroxyethyl cellulose, carrageenan and sodium carboxymethyl cellulose having a degree of etherification of 1.0 or less; A dentifrice comprising a combination of one or more surfactants selected from the group consisting of amino acids or salts thereof, amidobetaine-type amphoteric surfactants and fatty acid alkanolamides, and (c) triclosan. It provides a composition. The dentifrice composition of the present invention does not decrease the bactericidal activity of the compounded triclosan over time, exhibits an extremely excellent plaque formation inhibitory action, and is extremely useful in preventing gingivitis.

Hydroxyethylcellulose used as a binder in the present invention, carrageenan and sodium carboxymethylcellulose having a degree of etherification of 1.0 or less may be used alone or in combination of two or more, and may be used in an amount of 0.1 to 0.1% based on the total amount of the composition.
It is blended at a ratio of 5.0% by weight.

The N-long-chain acylamino acid or a salt thereof, an amidobetaine-type amphoteric surfactant and a fatty acid alkanolamide used as a surfactant in the present invention may also be used alone or in combination with 2 or more.
More than one kind may be used in combination, and may be blended at a ratio of 0.1 to 5.0% by weight based on the total amount of the composition.

The N-long-chain acyl amino acid used is such that the constituent amino acids are, for example, N-methyl-β-alanine, L-glutamic acid, sarcosine, etc., and the acyl group has 8 to 18 carbon atoms.
Fatty acid residues, for example, acyl groups such as lauric acid, myristic acid, stearic acid, and coconut oil fatty acids, or mixtures thereof. Examples of the salt include a monosodium salt and a monotriethanolamine salt.
Examples of such N-long-chain acylamino acids or salts thereof include sodium N-lauroylglutamate, sodium N-lauroylsarcosine and the like.

The amidobetaine-type amphoteric surfactant used has a fatty acid residue having an acyl group of 8 to 18 carbon atoms, for example, coconut oil fatty acid,
It is of bovine fatty acids and the like. Examples of these amidobetaine-type amphoteric surfactants include coconut oil fatty acid amidopropyldimethylaminoacetic acid betaine, bovine fatty acid amidopropyl, dimethylaminoacetic acid betaine, and the like.

The fatty acid alkanolamide used has a constituent fatty acid having 8 to 18 carbon atoms, for example, lauric acid, myristic acid, palmitic acid, coconut oil fatty acid, bovine fatty acid and the like, and the alkanol has 1 to 3 carbon atoms. For example, ethanol, isopropanol and the like. Examples of these fatty acid alkanolamides include lauric acid diethanolamide, myristic acid diethanolamide, palmitic acid diethanolamide, coconut oil fatty acid diethanolamide, bovine fatty acid diethanolamide, and the like.

If the amounts of the binder and the surfactant used are outside the above ranges, sufficient day-to-day stability of the sterilizing power of triclosan cannot be obtained.

Triclosan used as the fungicide of the present invention is 2 ',
It is a commercially available fungicide having a broad spectrum of chemical names 4,4'-trichloro-2-hydroxydiphenyl ether, and has excellent bactericidal activity against bacteria forming plaque. Triclosan is usually 0.001 to the total amount of the composition
To 5% by weight, preferably 0.005 to 1% by weight. If the amount is less than 0.001% by weight, sufficient bactericidal activity is not exhibited, and if it is more than 5% by weight, it has irritation to the oral mucosa and poses a practical problem.

The dentifrice composition of the present invention can be made into toothpaste, powdered toothpaste, and the like according to a conventional method.

Further, the dentifrice composition of the present invention may contain appropriate components as necessary, for example, dibasic calcium phosphate anhydrous or dihydrate, calcium carbonate, calcium pyrophosphate, calcium sulfate, insoluble sodium metaphosphate, amorphous silica Abrasives such as crystalline silica, aluminosilicate, aluminum hydroxide, aluminum oxide and resin; thickeners such as polyethylene glycol, sorbitol, glycerin and propylene glycol; essential oils such as peppermint and spearmint; l-menthol, Gabon, eugenol ,
Flavors such as anethole and other flavoring materials, saccharin sodium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartin, p-methoxycinnamic aldehyde, thaumatin and other sweeteners and preservatives, and chlorhexidine or its salts, lysozyme chloride, dextranase , Lytic enzyme, mutanase, sorbic acid, alexidine, hinokitiol, cetylpyridinium chloride, alkyl glycine, alkyl diaminoethyl glycine salt, allantoin, ε-aminocaproic acid, tranexamic acid, azulene, vitamin E, sodium monofluorophosphate, sodium fluoride Active ingredients such as stannous fluoride, water-soluble primary or secondary phosphates, quaternary ammonium compounds, and sodium chloride in a range that does not impair the effects of the present invention. It can be formulated.

Examples Next, the present invention will be described in more detail with reference to Examples and Test Examples.

Examples 1 to 16 and Test Examples 1 to 77 Toothpastes were prepared according to the following formulation according to a conventional method.

Ingredients Amount (% by weight) Binder (described in Tables 1 to 20) 1.5 Surfactant (described in Tables 1 to 20) 1.5 Triclosan 0.5 Silicic anhydride 20.0 Sorbit (70% aqueous solution) 60.0 Saccharin sodium 0.2 Flavor 0.9 Purification A suitable amount of the toothpaste thus obtained was filled in a laminate tube, and the bactericidal activity of the toothpaste on the first day of production was measured by the following measurement method. 3
It was left for a month and the bactericidal activity was measured again by the same method.

Preparation of Sample About 6 g of each toothpaste was collected and uniformly suspended in a 35% polyethylene glycol 400 aqueous solution. Then 150
After centrifugation at 00 rpm for 15 minutes, the obtained supernatant was diluted with a 35% aqueous solution of polyethylene glycol 400 so that the concentrations of triclosan were 0.1%, 0.05% and 0.02%, respectively.

In addition, since the bactericidal activity of the dentifrice composition may be reduced from the first day of production, triclosan is dissolved in a 35% polyethylene glycol 400 aqueous solution without using triclosan together with other components such as a binder and a surfactant, 0.1%, 0.05% and 0.02
The concentration in% was used as a standard for measuring the minimum bactericidal concentration (%, hereinafter abbreviated as MBC).

Measurement method 10 ⁸ ~10 ⁹ CFU / ml of S. mutans in each preparation sample 10 ml (Streptococcus mutans) bacteria suspension
0.1 ml was added, and a bactericidal reaction was performed at 37 ° C. for 15 minutes in a hot water bath. After the reaction, a loop of the sample was collected and applied to a trypticase soy agar (TSA) plate containing 0.5% polyoxyethylene monooleate and 0.07% lecithin,
The cells were cultured at 37 ° C. for 2 days under anaerobic conditions (N ₂ / H ₂ / CO ₂ = 85/10/5), and MBC was measured.

 The standard MBC was 0.05%.

The results are shown in Tables 1 to 20. The overall evaluation in the table was evaluated according to the following criteria. However, for a dentifrice composition in which the MBC on the first day of production (hereinafter abbreviated as MBC on the first day) has already been higher than the standard, the MBC after 3 months has passed (hereinafter referred to as “day M C”)
(Abbreviated as BC) was not measured and is indicated by-in the table.

○… The first day MBC is below the standard MBC (0.05%), and
The daily MBC is below the standard MBC.

×: One or both of first day and daily MBC is larger than control MBC.

As shown in Tables 1 to 20, only toothpaste in which triclosan was combined with the above-mentioned specific binder and surfactant showed good day-to-day stability of the sterilizing power of triclosan.

Example 17 Toothpaste was prepared according to a conventional method according to the following formulation.

Ingredients Compounding amount (% by weight) Hydroxyethylcellulose 1.0 Sodium N-lauroylglutamate 1.0 Triclosan 0.5 Dibasic calcium phosphate dihydrate 40.0 Sorbit (70% aqueous solution) 15.0 Saccharin sodium 0.2 Fragrance 0.9 Adjusted to purified water 100 Example 18 The following formulation A toothpaste was prepared according to a conventional method.

Ingredients Compounding amount (% by weight) Hydroxyethylcellulose 1.0 Coconut oil fatty acid amidopropyl 1.0 N-lauroyl sarcosine sodium 0.2 Triclosan 0.5 Aluminum hydroxide 40.0 Silicic anhydride 10.0 Concentrated glycerin 10.0 Stevia extract 0.5 Perfume 0.9 Adjusted to purified water 100 Example 19 Next A toothpaste was prepared according to the conventional method in accordance with the conventional method.

Ingredients Compounding amount (% by weight) Hydroxyethyl cellulose 1.0 N-lauroyl sarcosine sodium 0.3 Diethanolamide laurate 0.5 Triclosan 0.5 Calcium carbonate 40.0 Sorbit (70% aqueous solution) 15.0 Saccharin sodium 0.2 Chlorhexidine gluconate 0.05 Allantoin 0.05 Perfume 0.9 Adjust to purified water 100 Implement Example 20 Toothpaste was prepared according to a conventional method according to the following formulation.

Ingredient Content (% by weight) Carboxymethylcellulose 1.0 Sodium (degree of etherification 0.8) N-lauroylglutamic acid 1.0 sodium Triclosan 0.5 dibasic calcium phosphate dihydrate 40.0 sorbit (70% aqueous solution) 15.0 saccharin sodium 0.2 Perfume 0.9 Purified water 100 Adjustment Example 21 A toothpaste was prepared according to the following formulation according to a conventional method.

Ingredient Content (% by weight) Carboxymethyl cellulose 0.4 Sodium (degree of etherification 0.7) Hydroxyethyl cellulose 0.4 Carrageenan 0.2 Coconut oil fatty acid amidopropyl 1.0 N-lauroyl sarcosine sodium 0.2 Triclosan 0.5 Aluminum hydroxide 40.0 Silicic anhydride 10.0 Concentrated glycerin 10.0 Stevia extract 0.5 Fragrance 0.9 Adjusted to purified water 100 Example 22 Toothpaste was prepared according to a conventional method according to the following formulation.

Ingredients Amount (wt%) Carboxymethylcellulose 0.6 Sodium (degree of etherification 1.0) Hydroxyethylcellulose 0.6 N-lauroylsarcosine sodium 0.3 Lauric acid diethanolamide 0.5 Triclosan 0.5 Calcium carbonate 40.0 Sorbit (70% aqueous solution) 15.0 Saccharin sodium 0.2 Chlorhexidine gluconate 0.05 Allantoin 0.05 Perfume 0.9 Adjusted to purified water 100 The germicidal activity of the toothpastes obtained in Examples 17 to 22 thus obtained was measured on the first day of production and after 3 months, and comprehensively evaluated.

 Table 21 shows the results.

As is clear from Table 21, the bactericidal activity of the toothpastes of Examples 17 to 22 was stable over time, and the bactericidal activity was the same as that on the first day of production even after 3 months.

Effects of the Invention As described above, the dentifrice composition of the present invention can stably maintain its bactericidal activity over a long period of time by combining triclosan with a specific binder and a surfactant, It has an excellent effect on inhibiting plaque formation and preventing gingivitis.

 ──────────────────────────────────────────────────続 き Continuation of the front page (56) References JP-A-62-89614 (JP, A) JP-A-60-239409 (JP, A) JP-A-60-239410 (JP, A) JP-A 62-896410 126116 (JP, A) JP-A-63-258404 (JP, A) JP-A-63-233909 (JP, A) JP-A-55-164617 (JP, A) JP-A-56-36408 (JP, A) JP-A-60-75415 (JP, A)

Claims (1)

(57) [Claims] (1) one or two binders selected from the group consisting of (a) hydroxyethylcellulose, carrageenan and sodium carboxymethylcellulose having a degree of etherification of 1.0 or less; (b) N-long-chain acylamino acid or A dentifrice composition comprising a salt thereof, one or more surfactants selected from the group consisting of amidobetaine-type amphoteric surfactants and fatty acid alkanolamides, and (c) triclosan. .