JP2002255773A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for oral cavity effectively usable for prevention of dental caries because the composition is capable of effectively inhibiting pH reduction due to acid production by oral bacteria. SOLUTION: This composition for the oral cavity is obtained by formulating a basic peptide, a fluorinated compound and a sugar alcohol.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an oral composition having an excellent caries prevention effect.

[0002]

BACKGROUND OF THE INVENTION Caries are caused by Streptococcus mutans in plaque.
The enamel ash is eluted by the acid produced by bacteria represented by Ptococcus mutans bacteria. It is said that the pH decreases with the acid production, but when the pH falls to 5.5 or lower, demineralization, that is, caries formation proceeds. Therefore, a method for suppressing a decrease in pH for the purpose of preventing caries has been studied.
Specifically, extracts such as Ginkgo biloba (JP-A-56-083416), arginine-containing oligomer peptides (JP-A-58 / 086) are disclosed by techniques such as suppression of acid production leading to a decrease in pH, and neutralization and removal of the produced acid. 53-26331), chitin / chitosan (Japanese Patent Publication No. 3-15604), histidine and calcium carbonate (Japanese Patent Application Laid-Open No. Hei 8-301742), etc., but no substance excellent in the effect of suppressing a decrease in pH has been found. .

[0003] In addition, foods and the like have been developed in which sucrose, which is a main factor of acid production, is replaced with non-fermentable sugars such as xylitol and palatinose. It is practically impossible to replace it.
It has been reported that xylitol, a non-fermentable sugar, has an acid production inhibitory effect through a bacterial metabolic pathway called a futility circuit, but the effect is not seen in the presence of sucrose ( Goran Frostell, Swe
d. Dent. J. , 8: 137-146 (198
4)). Therefore, there has been a demand for the development of a more effective pH-drop suppressing technology.

[0004]

Means for Solving the Problems and Embodiments of the Invention As a result of intensive studies to achieve the above object, the present inventor has found that by combining a basic peptide with a fluorine compound and further a sugar alcohol, it is possible to obtain The present inventors have found that an excellent effect of suppressing a decrease in pH can be obtained, and have accomplished the present invention.

Hereinafter, the present invention will be described in detail.

[0006] The oral composition of the present invention comprises a basic peptide, a fluorine compound and a sugar alcohol.

[0007] Here, a basic peptide has an isoelectric point.
Peptides that are more alkaline than the physical conditions. Preferred
1 is selected from lysine, arginine and histidine
Or two or more basic amino acids are linked two or more consecutively
Or one or more homopolymers
Is desirable. The degree of polymerization is 5-1.
00, preferably consisting of 5 to 60 amino acids
It is. A typical example is polylysine (K)_n,
Polyarginine (R)_n, Polyhistidine (H) _n(N is
Polymerization degree), DSHAKR, HEKHHSHRGY, DS
HAKRRHHGYKRKFHEKHHSHRGY and
These -COOH and -NH_TwoPharmaceutical tolerance in
Salts.

[0008] The abbreviations for the constituent amino acids of the peptide and the protective groups thereof used in the present specification are those commonly used in the field of peptides. For example, G is glycine, H is histidine, K is lysine, R is arginine, E
Is glutamic acid, D is aspartic acid, P is proline,
Q represents glutamine, A represents alanine, F represents phenylalanine, S represents serine, and Y represents tyrosine.

[0009] In the oral composition of the present invention, these peptides can be used alone or in combination of two or more kinds.
01 to 5% (mass percentage, the same applies hereinafter), particularly 0.001
~ 1.0% is preferred.

The fluorine compound used in the present invention may be either an inorganic compound or an organic compound. In particular,
For example, sodium fluoride, potassium fluoride, tin fluoride, sodium fluoride silicate, sodium monofluorophosphate, aluminum fluoride, silver fluoride, hexylamine hydrofluorate, decanolamine hydrofluoride, hydrofluoric acid And octadecenylamine hydride. Of these, sodium monofluorophosphate and sodium fluoride are particularly preferred in terms of safety, solubility, flavor and the like. The compounding amount of the fluorine ion supplying compound in the oral composition is preferably 0.002 to 1% in terms of fluorine,
It is more preferable that the content be from 0.01 to 0.2%.

The sugar alcohol used in the present invention can be used alone or in combination of one or more selected from xylitol, sorbitol, palatinose, maltitol, and erythritol. Xylitol and sorbitol are particularly preferred. The amount of the composition is 0.01 to
It is preferably 30%, more preferably 0.1 to 25%.

The composition for oral cavity of the present invention is in the form of dentifrice such as toothpaste, lubricating toothpaste, liquid dentifrice, mouthwash, mouthwash, gargle tablet, denture cleaner, chewing gum and the like. Each composition can be prepared by a usual method using other components according to the characteristics within a range that does not impair the effects of the present invention.

In the case of dentifrices, for example, abrasives, thickeners,
Various active ingredients such as binders, surfactants, sweeteners, preservatives, and the like, pigments, flavors, and the like can be blended, and can be produced by mixing these components with water. Here, as the abrasive,
Silica-based abrasives such as silica gel, precipitated silica, aluminosilicate, zirconosilicate, dibasic calcium phosphate dihydrate and anhydrate, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, tertiary magnesium phosphate , Zeolite, zirconium silicate, tribasic calcium phosphate, hydroxyapatite, quaternary calcium phosphate, octacalcium phosphate, synthetic resin abrasives and the like.

The compounding amount of these abrasives is 2% of the total composition.
６０60%, particularly preferably 8 to 45%.

As a thickener, glycerin, propylene glycol, polyethylene glycol, etc., as a binder, sodium carboxymethylcellulose, hydroxyethylcellulose, carrageenan, carbopol, guar gum, montmorillonite, gelatin, etc .; Surfactants, cationic surfactants, nonionic surfactants and the like can be blended. Specifically, sodium lauryl sulfate, sodium α-olefin sulfonate, N-acyl sarcosinate, N-acyl glutamate, 2- Alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, N-acyl taurate, sucrose fatty acid ester, alkylol amide, polyoxyethylene sorbitan monostearate,
Pluronics, etc., as sweeteners, saccharin sodium, stevioside, stevia extract, paramethoxycinamic aldehyde, neohesperidyl dihydrochalcone, perillartin, etc., as preservatives, parabenzoic acid esters, sodium benzoate, etc. , Dextranase, mutanase, amylase, lysozyme chloride, water-soluble phosphate compounds such as potassium and sodium orthophosphates, allantochlorohydroxyaluminum, hinokitiol, ascorbic acid, glycyrrhizic acid and its salts, sodium chloride, tranexamic acid , Epsilon aminocaproic acid, dl-tocopherol acetate, α-bisabolol, isopropylmethylphenol, chlorohexidine salts, cetylpyridinium chloride, azulene, Chirurechin acid, sodium copper chlorophyllin, copper compounds such as copper gluconate, aluminum lactate, strontium chloride, potassium nitrate, berberine,
Hydroxamic acid and its derivatives, sodium tripolyphosphate, zeolite, methoxyethylene, maleic anhydride copolymer, polyvinylpyrrolidone, epidihydrocholesterine, benzethonium chloride, dihydrocholesterol, trichlorocarbanilide, zinc citrate, touki soft extract, oakaku Extracts, extracts, cloves, rosemary, ogre, safflower and the like, fragrances such as l-menthol, carvone, anethole, terpenes such as limonene or derivatives thereof, and coloring agents, blue No. 1, yellow No. 4, Titanium dioxide and the like are exemplified. In addition, the compounding amount of these components can be made into a usual amount.

The oral composition of the present invention has a pH of 6.
It is preferably adjusted to 0 to 9.0, especially 6.0 to 7.0.

[0017]

EFFECT OF THE INVENTION The oral composition of the present invention is capable of effectively preventing a decrease in pH due to acid production by oral bacteria, and can be effectively used for the prevention of dental caries.

[0018]

EXAMPLES Hereinafter, the present invention will be described specifically with reference to experimental examples and examples, but the present invention is not limited to the following examples. In addition, in each example, all% are mass percentages.

[Experimental Example] The suppression of pH drop by mutans bacteria, the causative bacteria, was evaluated by the following method.

[0020] Streptococcus mutans cultivated in Brain Heart Infusion medium
mutans 10449 was washed three times with PBS (300
(0 rpm, 10 min), and then suspended in PBS.
A centrifugal supernatant (10000 rpm, 20 min) of a three-fold diluted dentifrice having the composition shown in Table 1 was added to 1 ml of the bacterial suspension adjusted to a turbidity (550 nm) of 0.2 and an initial pH of 7.0.
1 was added. A sucrose solution was added to a final concentration of 1%, and the pH after 1 hour was measured. Table 2 shows the results.

[0021]

[Table 1]

[0022]

[Table 2]

[0023]

[Table 3]

From the above results, it was confirmed that the combination of a basic peptide, a fluorine compound and a sugar alcohol statistically significantly improved the effect of suppressing a decrease in pH and was effective in preventing dental caries.

[0025] [Example 3] Dentifrice Ingredient Amount (%) anhydrous silicic acid 15 Sodium lauryl sulfate 1.0 Sorbitol 20 Xylitol 5 Xanthan gum 0.5 Sodium alginate 0.5 Sodium saccharin 0.1 Sodium monofluorophosphate 0 .1 HEKHHSHRGY 0.01 Perfume 1.0 Purified water Balance total 100

[0026] [Example 4] Dentifrice Ingredient Amount (%) calcium phosphate 25 5 sodium lauryl sulfate anhydrous silicic acid 1.0 Glycerin 10 Xylitol 10 Sodium carboxymethyl cellulose 0.8 Carrageenan 0.5 Sodium saccharin 0.1 stannous fluoride 0.1 DSHAKR 0.05 Perfume 1.0 Purified water Balance total 100

Example 5 Mouthwash Component Ingredient Content (%) Ethanol 10 DSHAKRHHGYKRKFHEKHHSHRGY 0.1 Polyoxyethylene (60E0) Hydrogenated Castor Oil 0.5 Sorbitan Saccharin Sodium 0.2 Sodium Fluoride 0.1 Xylitol 5 Preservative Agents and fragrances 0.8 distilled water balance total 100

Example 6 Oral Pasta Component Blended Amount (%) White Vaseline 10 Stearic Alcohol 8 Propylene Glycol 5.6 Sodium Lauryl Sulfate 0.6 Ethyl Parahydroxybenzoate 0.01 Sodium Monofluorophosphate 0.5 (K) ₁₁ 0.1 Xylitol 3 Carboxymethylcellulose 16 Distilled water Balance total 100

Example 7 Gum Component Blended Amount (%) Gum Base 20 Flavor 1 Saccharum 20 Sorbitol 20 Xylitol 10 Powdered Sugar 20 Trisodium Citrate 1.5 Sodium Monofluorophosphate 0.5 (R) ₄₆ 0. 1 water balance total 100

Continued on front page F-term (reference) 4C083 AB172 AB471 AB472 AC072 AC122 AC131 AC132 AC302 AC432 AC482 AC782 AC862 AC902 AD272 AD302 AD352 AD411 AD412 CC41 EE32

Claims (1)

[Claims] 1. An oral composition comprising a basic peptide, a fluorine compound and a sugar alcohol.