JPH0710726A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain the subject composition excellent in suppressive effect on dental calculus development and also excellent in safety and feel when used. CONSTITUTION:This composition for oral cavity comprises a macromolecular compound having a condensed phosphate or phosphoric ester and a tannin or a hydrolyzate thereof. This composition, which is effective for preventing and suppressing dental calculus development and periodontosis, is very useful in terms of oral cavity hygienics.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for the oral cavity which has an excellent effect of suppressing the formation of tartar and an excellent safety.

[0002]

2. Description of the Related Art Conventionally, the problems to be solved by the invention
Although much attention has been paid to tartar as it impairs the aesthetics of the tooth, its removal has been a tedious task, which is regarded only by a professional and requires considerable labor.

However, in recent years, it has been confirmed that calculus deposition can be easily suppressed by using oral compositions such as dentifrice and mouthwash containing a tartar formation inhibitor, and these products are useful for oral hygiene. It started to be highly evaluated. In addition, recent studies have started to think that tartar promotes the accumulation of plaque and may be involved in the progression of periodontal disease. Under such circumstances, the development of a technology and a product having a better tartar control effect greatly contributes to the prevention of oral diseases.

At present, two approaches have been studied as a means for preventing tartar, roughly classified as follows.
The first method is a physicochemical method that suppresses the crystal growth of apatite, which is a major mineral component in tartar, and various active ingredients having an adsorbing action on apatite have been proposed as shown below. These active ingredients have various problems.

(1) Condensed inorganic phosphate (JP-A-1-20
No. 7227, No. 1-254618, No. 2-4708) Since condensed phosphate has a high effect of suppressing the crystal growth of apatite, a high calculus-preventing effect was expected, but it was easy due to phosphatase in the oral cavity. It is decomposed into orthophosphoric acid and its effect is not always sufficient.

(2) Natural or synthetic polymer compounds having a phosphoric acid group (ester), a sulfuric acid group (ester) or a carboxyl group (JP-A 64-71808, JP-A 1-17)
No. 2316, No. 2-56414, No. 4-217613.
No. 2-62819). As such, a homopolymer or copolymer obtained by polymerizing a monomer of an unsaturated carboxylic acid, a peptide obtained by polymerizing an amino acid, etc. have been reported. However, the safety of these synthetic polymer compounds is a problem in practical application, and many careful studies are required to overcome them. In addition, hydrolysates of naturally-occurring polymer compounds and phosphoric acid groups (esters)
There are also proposals for the introduction of sulphate and sulfuric acid groups (esters), but these natural substances have relatively few problems in terms of safety, but there are concerns about stable supply as raw materials due to variations in lots. . Furthermore, although these compounds are all excellent in chemical stability, their effectiveness has not yet been determined. Furthermore, since the phosphate ester undergoes hydrolysis by phosphatase similarly to the condensed inorganic phosphate salt, a sufficient effect cannot always be expected.

(3) Organic phosphate (Japanese Patent Laid-Open No. 1-2650)
No. 13, No. 2-56414) The derivative is PC such as ethanehydroxydiphosphonate [(HO) (CH ₃ ) C (PO ₄ H ₂ ) ₂ ].
Many types of molecules having a -P bond have been reported.
Although these substances are not decomposed by phosphatase, they have not been widely used because of the possibility of inhibiting bone formation.

(4) Polyvalent metal salt (JP-A-56-7707)
No. 64-6212 and JP-A-3-220116.) As the polyvalent metal salt, zinc, magnesium, aluminum and the like have been reported. Due to their strong cationic nature, it is difficult to stabilize and formulate them into formulations such as toothpaste containing a large amount of anionic substances and negatively charged bases, and many of them are required to ensure compatibility with fluorine. Needs consideration.

(5) Zeolite (JP-A-55-2411)
Since the zeolite is originally a solid, the reachability to the deep part of the plaque where tartar is formed and the staying property in the affected area are not sufficient as compared with the dissolved substance, and a certain effect of suppressing tartar is expected. Can not.

Next, the second method is a method for biochemically suppressing the growth of plaque itself, which is also a place for the formation of tartar, and the following method has been specifically proposed. (6) Insoluble glucan-degrading enzyme (JP-A-50-5824)
(3) Insoluble glucan-degrading enzymes, such as dextranase and mutanase, can dissolve the substrate portion of plaque and suppress the growth of tartar. However, it is difficult to stabilize and mix these enzymes in the preparation, and a special stabilization technique is required.

By the way, in the above method, it is said that the decomposition of condensed inorganic phosphate into orthophosphate by the oral phosphatase is suppressed by the anti-enzymatic action of the fluoride contained as a caries preventive agent. There is. Therefore, in order to confirm this point, the present inventor has adopted fluorine (NaF) as 35%.
The inhibitory effect was examined at the laboratory level at a concentration of up to 0 ppm (assuming that 1000 ppm in toothpaste was diluted about 3 times when used), but such inhibitory effect was not found. could not. In fact, even a preventive agent containing fluorine containing condensed inorganic phosphate as an active ingredient for preventing tartar cannot be said to have a sufficient effect level, and therefore, it is considered that the effect of suppressing the decomposition of fluoride is not sufficient.

Under these circumstances, the main preventive agents on the market do not lose their preventive effects, for example, about 5% for dentifrices.
Therefore, it is necessary to blend the condensed inorganic phosphate in a considerably high concentration, which has a considerable adverse effect on the formulation and usability.

Therefore, it is desired to develop a higher quality oral composition excellent in the effect of preventing tartar formation.

The present invention has been made in view of the above circumstances.
It is an object of the present invention to provide an oral composition that is excellent in the effect of suppressing tartar formation and excellent in safety.

[0015]

Means and Actions for Solving the Problems The present inventor has conducted extensive studies in order to achieve the above object, and as a result, tannins or hydrolysates thereof are effective as an additive for suppressing phosphatase activity. By using a tannin or a hydrolyzate thereof in combination with a condensed phosphate or a polymer compound having a phosphate ester, the phosphatase activity in the oral cavity is suppressed and the condensed phosphate or the orthophosphate of the phosphate ester is suppressed. The present inventors have found that the decomposition into calculus is prevented and that the effect of suppressing tartar is sufficiently exerted over a long period of time, and thus the present invention has been accomplished.

In this case, various phosphatase activities exist in the oral cavity, but it is considered that acid phosphatase, alkaline phosphatase, pyrophosphate degrading enzyme, etc. decompose the condensed inorganic phosphate. Since the human oral phosphatase is difficult to separate and purify, its detailed characteristics are not clear, but the phosphatase activity from other species or tissues has been studied in detail. According to it, (1) certain chemical substances (so-called enzyme inhibitors), (2) polyvalent metal salts, (3) protein denaturants,
(4) It is known that chelating agents and the like suppress the activity. Probably, human oral phosphatase also has similar properties. Therefore, in order to suppress the phosphatase activity, these substances may be used, but the safety to humans and the compatibility with the active ingredients in the preparation (eg pyrophosphate, fluoride, bactericide, etc.) are ensured. However, not all of them can be used. Then, as a result of diligent studies, it was confirmed that tannins or hydrolysates thereof are useful enough to satisfy them.

The tannin-like substance is a general term widely existing in the natural world and chemically given to substances having astringency, astringency, leather tanning, protein denaturation and the like.
Its chemical structural commonality is the presence of polyphenol groups. A variety of substances that correspond to tannin-like substances have been found depending on the combination of the type of plant used as the raw material for obtaining this and its extraction method, but it is difficult to define this with a specific chemical formula. Is. Currently, tannic acid (didepside of gallic acid or m-galloyl gallic acid) described in the Japanese Pharmacopoeia is listed as a standard substance of tannin-like substances. Known techniques for tannin-like substances are:
Many proposals have been made such as specifying the raw material, specifying the extraction / purification method (or specifying the combination thereof), or having a specific structural formula. Further, it is characterized by containing a tannin-like substance, which has a protein denaturing action (for example, hemostasis action: see JP-A-56-139423, collagenase activity inhibiting action: JP-A-4-66524).
No.), caries preventive action (Journal of the Japan Conservation Society of Dentistry 1
Also proposed is a composition for the oral cavity to which 1992, 35, p. 15), and a technique for preventing discoloration of tannin-like substances (described in JP-A-59-225109). However, the present inventors found for the first time that tannins or hydrolysates thereof are effective as an additive that suppresses the phosphatase activity associated with the decomposition of condensed phosphate or phosphate ester-containing polymers that are tartar-preventing agents. It is a thing.

On the other hand, as a mixture of phenols (a substance having phenol or polyphenol, such as thymol) not derived from tannin, for example, US Pat.
Japanese Patent No. 45667 discloses an oral composition for preventing tartar, which contains tripolyphosphate as an active ingredient, a diphenyl ether derivative as a water-insoluble, noncationic antibacterial agent, and a fluoride as a phosphatase activity inhibitor against tripolyphosphate. Is listed. Here, diphenyl ether is limited to non-water-soluble, non-cationic substances such as triclosan, but these substances are generally distinguished from tannin-like substances from the viewpoint of their discovery, chemical properties, and applications. The tannins of the present invention or a hydrolyzate thereof are in a completely different category.

Furthermore, as described above, the fluoride (N
aF) is within the range we have investigated (350 pp as F)
In m), the inhibitory effect on the phosphatase activity is not detected.

The present invention will be described in more detail below. The oral composition of the present invention comprises a polymer compound having a condensed phosphate or phosphate ester and a tannin or a hydrolyzate thereof in combination. For example, it can be prepared as a dentifrice, a mouthwash, a coating agent, a chewing gum and the like.

In the composition of the present invention, examples of the condensed phosphate include pyrophosphoric acid, tripolyphosphoric acid, tetrapolyphosphoric acid, hexametaphosphoric acid and the like. Examples of the polymer compound having a phosphoric acid ester include phosphorylated starch, casein, phosphorylated chitin, phosphorylated chitosan and the like.

The compounding amount of the polymer compound having a condensed phosphate or a phosphoric acid ester is 0.01 to 15 of the total composition.
% (% By weight, the same applies below), particularly 0.5 to 8%, more preferably 1 to 5%, and if it is less than 0.01%, the tartar inhibiting activity may not be exhibited.
If it exceeds%, abnormal irritation to the oral mucosa and taste buds, or compositional problems may occur.

Next, as the tannins used in the present invention, for example, natural products such as plants such as arame, swordfish, and clove, those extracted from other natural products, and chemical structures similar to tannins are used. Examples include chemically synthesized products and tannin hydrolysates (for example, tannic acid and gallic acid). Regarding the method of hydrolyzing tannins, a method of using an acid as a catalyst is generally used, but any method other than that using an enzyme or the like can be used as long as an equivalent hydrolyzate can be obtained. Absent.

The amount of tannin or its hydrolyzate to be added is 0.001 to 3%, especially 0.01 to 1% of the total composition.
%, More preferably 0.05 to 0.2%, and if the amount is less than 0.001%, the phosphatase activity inhibitory effect may not be obtained, and if it exceeds 3%, the preparation is colored and astringent. , Bitterness may occur.

Further, in addition to the above-mentioned essential components, other optional components can be added to the composition of the present invention. Specifically, abrasives, binders, thickeners, surfactants, fragrances, In addition to sweeteners and the like, various active ingredients such as various enzymes, tranexamic acid, glycyrrhizinic acid, copper gluconate and the like can be added. In addition, the compounding amount of the optional components can be a usual amount within a range that does not impair the effects of the present invention.

The oral composition of the present invention can be prepared by a conventional method, but it is desirable to adjust its pH to a neutral range of 5 to 9, especially 6 to 8.

[0027]

EFFECTS OF THE INVENTION The oral composition of the present invention has an excellent inhibitory effect on calculus formation and is excellent in safety, and is effective in preventing plaque formation and periodontal disease and preventing the progress thereof. Very useful for oral hygiene.

[0028]

EXAMPLES The present invention will be specifically described below by showing experimental examples and examples, but the present invention is not limited to the following examples. In addition,% in each example is% by weight.

[Experimental Example] The effect of suppressing the decomposition reaction of condensed phosphate by phosphatase was evaluated by the following method. That is, sodium pyrophosphate was used as the substrate, reagent grade alkaline phosphatase was used as the degrading enzyme, and the activity inhibitors (tannic acid or Na
A buffer solution in which F) was dissolved was allowed to act for 20 minutes at 37 ° C., and then the decomposition product, orthophosphate, was quantified. A blank containing only sodium pyrophosphate was used as a blank, and the degradation inhibiting activity was evaluated by comparing the amount of substrate degradation. The results are shown in Tables 1 and 2.

From the results shown in Tables 1 and 2, it was confirmed that tannic acid effectively suppressed the decomposition reaction of sodium pyrophosphate by phosphatase as compared with fluorine.

[0031]

[Table 1]

[0032]

[Table 2]

[Example 1] Dentifrice Silica 30% Glycerin 20 Carboxymethylcellulose 1.0 Sodium lauryl sulfate 1.0 Perfume 1.0 Saccharin 0.1 Sodium pyrophosphate 5.5 Tannic acid 0.1 SnF ₂ 0.41 Sn ₂ P ₂ O ₇ 0.5 Purified water Residual 100.0%

[Example 2] Dentifrice Silica 30% Solbit 30 Carboxymethylcellulose 0.5 Hydroxyethylcellulose 0.5 Sodium lauryl sulfate 1.0 Perfume 1.0 Saccharin 0.1 Sodium tripolyphosphate 1.5 Tannic acid 0.1 Alame extract 0.05 NaF 0.22 Sn ₂ P ₂ O ₇ 0.5 Purified water Residual 100.0%

Example 3 Dentifrice Dicalcium Phosphate Dihydrate 30% Glycerin 25 Carboxymethyl Cellulose 1.2 Sodium Lauryl Sulfate 1.0 Perfume 1.0 Saccharin 0.1 Sodium Tetrapolyphosphate 2.0 Tannic Acid 05 Ougon Extract 0.02 Clove Extract 0.01 Sodium Monofluorophosphate 0.76 Purified Water Residual 100.0%

[Example 4] Dentifrice Calcium carbonate 30% Glycerin 15 Sorbit 15 Carboxymethyl cellulose 1.0 Sodium lauryl sulfate 1.0 Perfume 1.0 Saccharin 0.1 Sodium pyrophosphate 3.0 Tetrapolyphosphate sodium 2.0 Phosphorylated starch 1.0 Tannic acid 0.1 Alame extract 0.01 NaF 0.22 Sn ₂ P ₂ O ₇ 1.0 Purified water Residual 100.0%

[Example 5] Dentifrice Aluminum hydroxide 25% Glycerin 25 Carboxymethylcellulose 1.0 Sodium lauryl sulfate 1.0 Perfume 1.0 Saccharin 0.1 Sodium tripolyphosphate 2.0 Phosphorylated chitin 1.0 Tannic acid 0.1 Ougon Extract 0.01 SnF ₂ 0.41 Sn ₂ P ₂ O ₇ 1.0 Purified Water Residual 100.0%

[Example 6] Dentifrice Silica 30% Sorbit 30 Carboxymethylcellulose 1.0 Sodium lauryl sulfate 1.0 Perfume 1.0 Saccharin 0.1 Phosphorylated starch 2.0 Tannic acid 0.1 Lame extract 0. 01 Clove extract 0.01 SnF ₂ 0.41 Sn ₂ P ₂ O ₇ 1.0 Purified water Residual 100.0%

[Example 7] Dentifrice Silica 30% Solbit 30 Carboxymethylcellulose 1.0 Sodium lauryl sulfate 1.0 Perfume 1.0 Saccharin 0.1 Phosphorylated starch 1.0 Phosphorylated chitin 1.0 Tannic acid 0. 1 Arame extract 0.01 Ougon extract 0.01 NaF 0.22 Purified water Residual 100.0%

[Example 8] Dentifrice Silica 30% Glycerin 25 Carboxymethyl cellulose 1.0 Sodium lauryl sulfate 1.0 Perfume 1.0 Saccharin 0.1 Sodium pyrophosphate 5.5 Phosphorylated starch 1.0 Tannic acid 0.1 1 Lame extract 0.01 Clove extract 0.01 SnF ₂ 0.41 Sn ₂ P ₂ O ₇ 0.5 Purified water Residual 100.0%

[Example 9] Dentifrice Silica 30% Glycerin 25 Carboxymethylcellulose 1.0 Sodium lauryl sulfate 1.0 Fragrance 1.0 Saccharin 0.1 Sodium tripolyphosphate 2.5 Phosphorylated starch 1.0 Tannic acid 1 Lame extract 0.01 SnF ₂ 0.41 Sn ₂ P ₂ O ₇ 1.0 Purified water Residual total 100.0%

[Example 10] Dentifrice Silica 30% Glycerin 25 Carboxymethylcellulose 1.0 Sodium lauryl sulfate 1.0 Perfume 1.0 Saccharin 0.1 Sodium pyrophosphate 5.5 5.5 Gallic acid / H ₂ O 0.1 NaF 0.22 Purified water Residual 100.0%

[Example 11] Mouthwash Ethanol 20% Saccharin 0.05 Perfume 1.0 Lauryl diethanolamide 0.3 Sodium pyrophosphate 2.0 Tannic acid 0.04 Thymol 0.02 NaF 0.05 Sn ₂ P ₂ O ₇ 0.05 Purified water Residual 100.0%

Example 12 Mouthwash Ethanol 15% Saccharin 0.05 Perfume 1.0 Sodium pyrophosphate 2.0 Phosphorylated starch 0.5 Tannic acid 0.03 Lame extract 0.01 Thymol 0.03 SnF ₂ 0.1 Sn ₂ P ₂ O ₇ 0.05 Purified water Residual 100.0%

[Example 13] Mouthwash Ethanol 10% Saccharin 0.05 Perfume 1.0 Sodium tripolyphosphate 1.0 Phosphorylated chitin 0.5 Tannic acid 0.03 Ougon extract 0.01 Thymol 0.02 NaF 0 0.011 Purified water Residual 100.0%

Example 14 Mouthwash Ethanol 15% Saccharin 0.01 Perfume 0.5 Sodium tetrapolyphosphate 1.0 Phosphorylated starch 0.3 Phosphorylated chitin 0.3 Tannic acid 0.02 Lame extract 0 .01 Clove extract 0.01 Thymol 0.01 Sodium monofluorophosphate 0.2 Purified water Residual 100.0%

Example 15 Mouthwash Ethanol 10% Saccharin 0.02 Perfume 0.5 Sodium pyrophosphate 1.0 Phosphorylated starch 0.5 Tannic acid 0.03 Lame extract 0.01 Thymol 0.01 SnF ₂ 0.04 Purified water Residual total 100.0%

Claims (1)

[Claims] 1. An oral composition comprising a polymer compound having a condensed phosphate or a phosphoric acid ester, and a tannin or a hydrolyzate thereof in combination.