JP2002012536A - Oral composition - Google Patents

Abstract

(57) [Summary] (Modified) [Problem] Since plaque causes periodontal disease such as dental caries, gingivitis and alveolar pyorrhea, the search for an active ingredient that suppresses the formation and adhesion of plaque is needed. Various dextranases have been put to practical use because of their high plaque suppression efficiency and high safety. Among them, the present invention provides an oral composition having a more effective plaque suppression effect. SOLUTION: An oral composition comprising a polylysine and a non-cationic bactericide selected from halogenated diphenyl ether, halogenated salicylanilide, halogenated carbanilide and phenol compound. The non-cationic fungicide is triclosan and / or isopropylmethylphenol.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an oral composition having a high plaque inhibiting effect.

[0002]

BACKGROUND OF THE INVENTION Conventionally, plaque causes periodontal diseases such as dental caries, gingivitis and alveolar pyorrhea, and is therefore an effective ingredient for suppressing the formation and adhesion of plaque. Various searches have been carried out, among which dextranase has a high plaque-suppressing effect and high safety, and is therefore being put to practical use. Development is desired.

[0003]

Means for Solving the Problems and Embodiments of the Invention The present inventor has conducted intensive studies to meet the above-mentioned demands. As a result, polylysine, halogenated diphenyl ether, halogenated salicylanilide, halogenated carbanilide and phenol have been studied. It has been found that the use of a non-cationic fungicide selected from compounds gives an excellent plaque-suppressing effect.

Conventionally, oral compositions containing polylysine have been proposed in Japanese Patent Application Laid-open No. Sho 61-76411, in which polylysine is used as a stabilizer for dextranase, and Japanese Patent Application Laid-Open No. 10-298048 discloses polylysine. The effect of inhibiting the adhesion of Actinomyces viscosus bacteria has been shown, and it has been proposed to use polylysine as an endotoxin neutralizing agent for periodontal disease bacteria. There is no proposal to use it as an active ingredient for suppressing the formation of. The present inventor has reported that the combination of this polylysine and a non-cationic bactericide can be used for Streptococcus mutans (Streptococcus mutans).
Ans) has been found to effectively inhibit plaque formation, and the present invention has been accomplished.

Hereinafter, the present invention will be described in more detail.
The composition for oral cavity of the present invention is a mixture of polylysine and a non-cationic fungicide selected from halogenated diphenyl ethers, halogenated salicylanilides, halogenated carbanilides and phenol compounds.

Here, polylysine includes poly-D-lysine, poly-DL-lysine, and poly-L-lysine, which can be used as hydrochloride and hydrobromide, and having a molecular weight of about 500 to 300,000. it can.

In the composition of the present invention, polylysine is
Any one or two or more of the above can be used in combination, and the amount of polylysine is preferably 0.001 to 10% (mass percentage, the same applies hereinafter) of the composition, and more preferably 0.01 to 1%. If the amount is less than 0.001%, the effect of inhibiting bacterial adhesion may not be sufficiently exhibited, and if it is more than 10%, an adverse effect on flavor may be caused.

[0008] The non-cationic fungicide is selected from any of halogenated diphenyl ether, halogenated salicylanilide, halogenated carbanilide and phenolic compounds. As the halogenated diphenyl ether, triclosan, 2,2′-dihydroxy-5,
5′-dibromo-diphenyl ether and halogenated salicylanilide include 4 ′, 5-dibromosalicylanilide, 3,4 ′, 5-trichlorosalicylanilide,
2,3,3 ', 5-tetrachlorosalicylanilide,
3 ', 5-dibromo-3'-trifluoromethylsalicylanilide and halogenated carbanilide include 3-
Trifluoromethyl-4,4'-dichlorocarbanilide, and phenolic compounds include isopropylmethylphenol. Of these, halogenated diphenyl ethers and phenol compounds are preferred,
Particularly, triclosan and isopropylmethylphenol are preferable. The amount of the non-cationic fungicide is preferably 0.001 to 5% of the composition, more preferably 0.01 to 5%.
~ 1%. If the amount is less than 0.001%, the effect of inhibiting bacterial adhesion may not be sufficiently exhibited, and if the amount is more than 5%, an adverse effect on flavor may be caused.

The oral composition of the present invention can be prepared and applied as a dentifrice such as toothpaste, liquid dentifrice, mouthwash, mouthwash, liniment, chewing gum, artificial saliva and the like. Appropriate components according to the type of product and the like can be blended. For example, for dentifrices, abrasives, binders,
Thickeners, surfactants, sweeteners, preservatives, flavors, coloring agents,
Various active ingredients other than those described above can be blended in a usual dose, and can be produced by mixing these ingredients with water.

Here, as the abrasive, precipitated silica,
Silica-based abrasives such as silica gel, aluminosilicate and zirconosilicate, dibasic calcium phosphate dihydrate and anhydrate, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, tertiary magnesium phosphate, zeolite , Zirconium silicate, synthetic resin-based abrasives and the like are preferably used.

As the thickener, glycerin, sorbitol, propylene glycol, polyethylene glycol,
Xylit, maltit, lactit, and the like are preferably used.

As the surfactant, an anionic surfactant, a cationic surfactant, a nonionic surfactant and the like can be blended, and specific examples thereof include sodium lauryl sulfate, sodium α-olefin sulfonate, and N-acyl sulfonate. Cosinate, N-acyl glutamate, 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine, N-acyl taurate, sucrose fatty acid ester, alkylol amide, polyoxyethylene hydrogenated castor oil, polyglycerin Fatty acid esters, pluronics, polyoxyethylene sorbitan monostearate and the like are preferably used.

As a sweetener, saccharin sodium,
Examples include stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, and perillartin.

Examples of the preservative include p-hydroxybenzoate, sodium benzoate and the like.

As the fragrance, terpenes such as l-menthol, carvone, anethole, limonene and the like, and derivatives thereof are preferable. As the colorant, blue No. 1, yellow No. 4, titanium dioxide and the like are preferable.

Various active ingredients include sodium fluoride, potassium fluoride, ammonium fluoride, and primary fluoride.
Fluorides such as tin and sodium monofluorophosphate,
Water-soluble phosphoric acid compounds such as potassium phosphate and sodium salt of orthophosphoric acid, allantoinchlorohydroxyaluminum,
Hinokitiol, ascorbic acid, lysozyme chloride, glycyrrhizic acid and salts thereof, sodium chloride, tranexamic acid, epsilon aminocaproic acid, dl-tocopherol acetate, azulene, glycyrrhetinic acid, copper chlorophyllin sodium, copper compounds such as copper gluconate, aluminum lactate, chloride Strontium, potassium nitrate, berberine, hydroxamic acid and derivatives thereof, sodium tripolyphosphate, zeolite, dextranase, mutanase, amylase, methoxyethylene-maleic anhydride copolymer, polyvinylpyrrolidone, epidihydrocholesterine, dihydrocholesterol, zinc citrate , Touki, bakaku, clove, rosemary, ogon,
Extracts such as safflower, α-bisabolol, chlorhexidine salts, cetylpyridinium chloride, benzethonium chloride, trichlorocarbanilide and the like.

[0017]

The oral composition of the present invention provides a high plaque inhibiting effect.

[0018]

EXAMPLES Hereinafter, the present invention will be described in detail with reference to Experimental Examples, Examples and Comparative Examples, but the present invention is not limited to the following Examples.

[Experimental Example] A bacterial adhesion test using hydroxyapatite beads was performed by the following method. Hydroxyapatite beads (Asahi Kogaku) (hereinafter abbreviated as HA) 5
mg was weighed in a polystyrene multiwell, and KCl buffer (50 mM KCl, 1 mM KH ₂ PO ₄ , 1 mM
After washing with CaCl ₂ , 0.1 mM MgCl ₂ , pH 6.0), the centrifugal supernatant of human whole saliva (12,000 rpm / 2)
(0 minute) 125 μL was added and reacted for 90 minutes. Next, the HA was washed with KCl buffer, and 125 μl of each drug solution was added.
L. and S. cerevisiae cultured in a medium containing 3H-thymidine. muta
A solution in which a bacterial solution containing nsingbrit was mixed was added and reacted for 60 minutes. Washing the HA with KCl buffer,
The radioactivity of the bacteria attached to HA was measured by a liquid scintillation counter. Table 1 shows the results.

[0020]

[Table 1]

Polylysine is S. cerevisiae, a causative bacterium. mu
It was confirmed that the bacterium exhibited an excellent effect of suppressing bacterial adhesion to tansingbrit.

Example 1, Comparative Examples 1 to 3 Toothpastes shown in Table 2 were prepared by a conventional method, and the plaque inhibiting effect was evaluated by the following method. Table 3 shows the results.

[0023]

[Table 2]

1 week old (male) golden hamster
Each group consisted of 10 animals. mutans10449 strain was infected. For infection, the strain was transformed into 4 mL of BHI medium (manufactured by BBL).
After inoculating one platinum loop into the hamster and culturing it at 36 ° C. for 20 hours under anaerobic conditions, 0.1 mL of this bacterial solution was dropped into the mouth of each hamster for 3 days. The colonization of the bacteria of each hamster was confirmed using MS agar medium (manufactured by Difuco) containing 0.1% streptomycin. After confirming the colonization of the bacteria as described above, a solution obtained by extracting the toothpaste shown in Table 2 with three times the amount of water was administered for 5 weeks. The administration method was such that 0.1 mL of hamster was administered twice a day into the mouth. As a feed during the experiment, a caries-inducing powder feed Diet2000 (manufactured by CLEA Japan) was used. Drinking water has a pore size of 0.2μ.
m-ion-exchanged water filtered through a membrane filter was used. The condition of plaque adherence to each hamster was evaluated by the method of Shimada et al. (11 hygiene inspection technology courses) for 12 molars and expressed as the total score. Criterion 0: No plaque is exuded, and the contents of the pits and fissures are only stained in dots or lines 1: 1: Less than 1/3 area covered with exuded plaque 2 : One-third or more and less than two-thirds covered with stained plaque. 3: Two-thirds or more covered with stained plaque.

[0025]

[Table 3]

From these results, it was found that the combination of polylysine and a non-cationic bactericide (triclosan) synergistically increases the plaque control effect.

[0027]

[Table 4]

Example 10 Mouthwash Ethanol 10.0% Glycerin 20.0 Polyoxyethylene hydrogenated castor oil 0.05 Fragrance 0.8 Polylysine hydrobromide 0.1 Triclosan 0.05 Sodium fluoride 0.23 Water Remaining total 100.0%

Example 11 Mouthwash Ethanol 10.0% Glycerin 20.0 Polyoxyethylene hydrogenated castor oil 0.03 Fragrance 0.8 Polylysine hydrobromide 0.1 3,4 ′, 5-Trichlorosalicylanilide 0 .05 Sodium fluoride 0.35 Water Total remaining 100.0%

Example 12 Gum Gum Base 20.0% Syrup 5.0 Glycerin 2.5 Sorbit 71.4 Polylysine Hydrochloride 0.07 Triclosan 0.03 Flavor 1.0 Total 100.0%

Example 13 Artificial Saliva Sodium Fluoride 0.2% Potassium Chloride 0.15 Sodium Chloride 0.09 Magnesium Chloride 0.005 Calcium Chloride 0.01 Sodium Carboxymethylcellulose 0.05 Polylysine Hydrochloride 0.02 3 -Trifluoromethyl-4,4'-dichlorocarbanilide 0.01 Perfume 0.8 Water Remaining 100.0% All of the compositions for oral cavity of the above Examples also have a good plaque formation inhibitory effect.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61P 1/02 A61P 1/02 31/04 31/04 F term (Reference) 4C083 AB032 AB222 AB292 AB332 AB342 AB442 AB472 AC102 AC122 AC132 AC432 AC471 AC472 AC642 AC692 AC782 AC811 AC812 AC862 AD092 AD112 AD302 AD352 AD411 AD412 BB48 CC41 DD23 DD27 EE32 EE36 4C084 AA19 MA57 NA05 ZA672 ZB352 ZC751 4C086 AA01 AA02 FA03 MA02 MA04 A05 MA05 A05 MA02 ZA67 ZB35 ZC75

Claims (2)

[Claims] 1. An oral composition comprising polylysine and a non-cationic bactericide selected from halogenated diphenyl ethers, halogenated salicylanilides, halogenated carbanilides and phenol compounds. 2. The non-cationic bactericide is triclosan and / or isopropylmethylphenol.
The oral composition according to any one of the preceding claims.