JP3152467B2 - 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 having an excellent effect on the prevention and treatment of dentin hypersensitivity, and having a stable and good feeling of use.

[0002]

2. Description of the Related Art Dentin hypersensitivity refers to dentin being exposed due to loss of tooth enamel or cementum due to caries, tooth attrition, wear and gingival regression. Symptoms that become hypersensitive to extraneous stimuli, and the pain caused by the stimuli is a significant obstacle to daily eating habits. For this reason, many proposals have been made for the prevention and treatment of dentin hypersensitivity. For example, effective drugs for dentin hypersensitivity include formaldehyde, fluoride, zinc chloride, silver nitrate, potassium nitrate, citrate, and strontium salts (Dental Medicine Journal: 3,116-149, 1984, J. Pe).
riodontol .: 10,351-363, 1983), aluminum lactate, etc. (JP-A-61-36212, JP-A-61-36212).
155312) has been proposed. Further, potassium nitrate and fluorine, strontium acetate and fluorine, etc.
7215) is also disclosed. However, these drugs do not have a sufficiently effective dentin hypersensitivity inhibitory effect and an excellent feeling in use, and it has been desired to develop an oral composition free of such defects. Furthermore, despite the fact that the frequency of occurrence of root surfaces and dentin caries increases due to exposure of dentin, no oral composition having such a root surface and dentin caries inhibiting action has been proposed.

[0003]

Means for Solving the Problems Accordingly, the present inventors have conducted intensive studies to obtain an oral composition having an excellent dentin hypersensitivity inhibitory action and a feeling of use.
By combining at a certain concentration and a certain mixing ratio,
The present inventors have found that an oral composition having not only a synergistic effect of suppressing dentin hypersensitivity and an excellent feeling in use but also an effect of suppressing the root surface and dentin caries can be obtained. Was. That is, the present invention is an oral composition containing a water-soluble aluminum compound and a fluoride, and has a fluorine concentration of 100 to 2000 ppm,
The molar ratio of fluorine and aluminum is F: Al =
The present invention provides an oral composition characterized by having a pH of from 1: 0.3 to 1: 3 and a pH of from 5 to 10.

The water-soluble aluminum compound used in the present invention is not particularly limited as long as it is water-soluble, but aluminum lactate, aluminum gluconate, aluminum tartrate,
Carboxylic acid compounds such as aluminum citrate and the like, aluminum chloride, aluminum allantoin and the like can be used. Generally, aluminum lactate, aluminum allantoin and the like are preferred.

As the fluoride, monofluorophosphate, tin fluoride, sodium fluoride, sodium silicon fluoride, ammonium fluoride and the like may be used. Sodium.
Fluoride is blended in the composition such that the fluorine concentration becomes 100 to 2000 ppm. If it is less than 100 ppm, the desired effect cannot be obtained, and if it is more than 2000 ppm, safety is a problem. Generally, it is preferably 800 to 1600 ppm.

In the oral composition of the present invention, the fluoride and the water-soluble aluminum compound are converted to a molar ratio of fluorine and aluminum, whereby F: Al = 1: 0.3 to
It is blended at a blending ratio of 1: 3. When the ratio of aluminum to fluorine is 0.3 or less, the effect of suppressing the root surface and dentin caries is low, and when it is 3 or more, the feeling of use is poor. Preferably, F: Al = 1: 1.

The pH of the oral composition of the present invention is pH 5-1.
0, preferably 5 to 8. When the pH is 5 or less,
This is because the feeling of use is poor and if the pH is 10 or more, there is irritation.

[0008] The oral composition of the present invention can be produced by a conventional method, and includes dentifrice (eg, toothpaste, lubricating dentifrice, liquid dentifrice, mouthwash), and paste-like composition (eg, oral pasta). , Gum massage cream, etc.), liquid oral fresheners and the like. Further, in addition to the above-mentioned components, ordinary effective base materials may be used depending on the form of the composition. For example, sorbitol, glycerin and the like can be used as a lubricant, and the compounding amount thereof is 10 to 60%, preferably 20 to 50% based on the whole composition.
%. Furthermore, surfactants, flavors, binders, sweeteners and the like can be added.

[0009]

Next, the present invention will be described in more detail with reference to experimental examples and examples. In the experimental examples, the effect of suppressing the hypersensitivity to dentin, the effect of suppressing the root surface and dentin caries, and the feeling of use of the oral composition of the present invention were evaluated. Experimental Example 1 (Evaluation of Dentin Hypersensitivity Inhibition) When the surface layer of the tooth was rapidly lost, that is, when the enamel and cementum were rapidly worn away and the underlying dentin surface was exposed, It is said that quality hyperesthesia occurs.
Dentin has countless thin empty tubes called dentin tubules,
It is said that when dentin is exposed, physicochemical stimuli easily reach the pulp through the dentin tubules, causing transient painful symptoms. Therefore, obstructing exposed dentin tubules is important for preventing and treating hyperesthesia. Therefore, the method of Pashley et al. (J. Dent.
s. 57, 187-193, 1987) were used to evaluate the degree of stenosis and occlusion of dentinal tubules by various drugs.

Method A block was cut out from the root of a cow and polished to produce a thin section, which was used as a sample. The sample was fixed, immersed in the medicine shown in Table 1 at room temperature for 15 minutes, physiological saline was flowed before and after the treatment, and the amount of physiological saline per unit time passing through the sample was measured. However, all drugs were adjusted to pH 6.5.

(Equation 1)

[0011]

Table 1 Chemical name Aluminum content (%) Fluorine content (ppm) Reduction rate (%) Aluminum lactate 0.02 500 53 0.1 0 50 0.1 50 51 0.1 500 75 0.1 1000 95 95. 2 1000 92 Aluminum Gluconate 0.1 0.43 0.1 500 70 0.1 1000 90 0.15 500 82 0.2 1000 85 Aluminum Tartrate 0.1 0.31 0.1 500 78 0.1 1000 90 0.0 2 1000 88 Aluminum citrate 0.03 1000 70 0.1 0 40 0.1 500 78 0.1 1000 92 0.2 1000 90 According to the above results, fluoride was compounded compared to the case of water-soluble aluminum alone. In particular, the effect is improved, especially when F: Al = 1: 0.3 to 1: 3 and the fluoride concentration is in the range of 100 to 2000 ppm. Have effect was observed.

Experimental Example 2 (Evaluation of root surface and dentin caries inhibiting action) It is known that dentin is softer and lower in acid resistance than enamel, so that caries is easily generated. Therefore, it has been pointed out that cariousness is likely to occur in exposed dentin that causes hyperesthesia. In recent years, it has been recognized that the effect of inhibiting dental caries can be evaluated by an in vitro remineralization evaluation method using teeth. This remineralization evaluation method is to treat enamel or dentin sections of bovine teeth with acid (cavities) and drugs (dentifrice, etc.), and to increase or decrease (increase remineralization) the amount of minerals in the teeth caused by the treatment. , The decrease is referred to as demineralization). The dentin caries suppression effect was evaluated using the method.

Method The root dentin of bovine teeth was cut out in a block shape, embedded in acrylic resin, and then the surface of the tooth was polished. After polishing,
The polished surface layer was treated with 0.1 M lactic acid (pH 4.5) for 48 hours to artificially produce a decalcified layer. Half of the surface layer of the decalcified block was coated with a water-insoluble polymer solution, and immersed in a chemical solution (twice a day) and artificial saliva described later, alternately, for 10 days. After the tooth block was cut and polished to a thickness of 100 μm, the amount of remineralization was calculated based on the following equation by performing image processing on the X-rayed film (JM Ten Cate, J. Dent Res .: 69, 6
14-619, 1990, JR Mellberg, J. Dent.
Res .: 65, 959-962, 1986).

(Equation 2)

[0014]

Table 2 Chemical solution (w / w%) Aluminum lactate MFP Remineralization amount (%) 0 3 10 4 0 0.35 20 1 0.35 32 1 0.7 74 According to the above test results, aluminum lactate It was found that while only a caries solution had almost no caries suppressing effect, a strong caries suppressing effect was obtained with the chemical solution of the present invention to which aluminum lactate and fluoride were added.

Experimental Example 3 (Evaluation of feeling of use) Toothpaste having the formulation shown in Table 3 was prepared, and the feeling of use was organoleptically evaluated by 15 expert panelists. Evaluation criteria ○: There is no problem in usability △: There is some problem in usability ×: There is a problem in usability

[0016]

[Table 3] Raw material name Compounding amount (%) ABCD FGH silica 20 20 20 20 20 20 20 20 Carboxymethyl 22 22 22 22 22 Sodium cellulose Sodium lauryl sulfate 1.5 1.5 1.5 1.5 1.5 1.5 1.5 1.5 Sodium saccharin 0.1 0.1 0.1 0.1 0.1 0.1 0.1 0.1 Aluminum lactate 1.0 1.0 1.0 5.0 1.0 1.0 3.0 2.0 Monofluorophosphoric acid 0.7 0.7 0.7 0.7 2.5 0.7 0.7 1.5 Sodium glycerin 20 20 20 20 35 5 5-Sorbitol 20 20 20 10-50 5 20 Fragrance 1.0 1.0 1.0 1.0 1.0 1.0 1.0 1.0 Water Remaining Remaining Remaining Remaining Remaining Remaining Remaining Remaining Remaining pH 4.5 6.5 8.0 6.5 6.5 6.5 6.5 6.5 Feeling × × ○ × × × × △ ○ From the above results, the fluorine concentration is 100 to 2000 ppm. When F: Al = 1: 0.3 to 1: 3,
For the first time, it was found that a remarkable astringent feeling and metallic taste were suppressed, and a composition excellent in use feeling was obtained.

The following examples show specific compositions of the compositions. In addition, all "%" are weight%. Example 1 Toothpaste Ingredient Content (%) Silica 20.0 Sorbitol 30.0 Glycerin 8.0 Sodium Carboxymethylcellulose 1.6 Sodium Saccharin 0.1 Fragrance 1.0 Aluminum Lactate 1.0 Sodium Lauryl Sulfate 1.2 Monofluoro Sodium phosphate 0.7 Water adjusted to 100% (pH adjusted to 6.5)

Example 2 Mouthwash Ingredients Content (%) Ethyl alcohol 15.0 Glycerin 10.0 Ascorbic acid 0.03 Aluminum lactate 1.5 Polyoxyethylene hydrogenated castor oil (60 EO) 1.0 Saccharin sodium 0 .05 Sodium fluoride 0.2 Fragrance 0.3 Water adjusted to 100% (Adjusted to pH 6.5)

Example 3 Toothpaste Ingredients Amount (%) Dibasic calcium phosphate 40.0 Sorbitol 30.0 Sodium carboxymethylcellulose 1.5 Saccharin sodium 0.1 Fragrance 0.9 N-Lauroyl sarcosine sodium 0.5 Sucrose fatty acid ester 0.5 Aluminum lactate 2.0 Sodium fluoride 0.3 Water adjusted to 100% (Adjusted to pH 8.0)

Example 4 Oral Pasta Ingredients Compounding Amount (%) Glyceryl Monostearate 10.0 Glycerin 15.0 Hydroxyethylcellulose 5.0 Cetyl Alcohol 3.0 Sorbitan Monooleate 5.0 Fragrance 1.0 Aluminum Lactate 1.0 5 Sodium monofluorophosphate 1.5 Adjusted to 100% water (Adjusted to pH 5.5)

[0021]

According to the present invention, it is possible to obtain a composition for the oral cavity which has not only an effect of suppressing hypersensitivity to dentin but also an effect of suppressing dental root surfaces and dentin caries.

──────────────────────────────────────────────────続 き Continued on front page (58) Field surveyed (Int.Cl. ⁷ , DB name) A61K 7/18

Claims (1)

(57) [Claims] 1. An oral composition containing aluminum lactate and fluoride, wherein the fluorine concentration is 100 to 160.
0 ppm, the mixing ratio of fluorine and aluminum is F: Al = 1: 0.7-1: 2.8 in molar ratio, and the pH is 5
A composition for oral cavity, which is 10 to 10.