JPH0720870B2 - Hyperesthesia inhibitor - Google Patents

Description

TECHNICAL FIELD The present invention relates to a topical agent for suppressing hypersensitivity of teeth.

2. Description of the Related Art Tooth hypersensitivity of teeth is caused by various systemic or local causes, and tooth pain is a major symptom. There are various causes, for example, local ones such as tooth wear, tooth surface loss due to tooth cutting, gingival retraction, and tooth root exposure due to gingival resection, and various other causes.

Among the hypersensitivity inhibitors used today, there are silver preparations and fluoride preparations which are applied topically to suppress the pain symptoms of teeth. However, silver preparations have the drawback of blackening teeth, and fluoride preparations have the disadvantage that the appearance of the effect is uncertain and it takes time before the effect appears. Therefore, a hypersensitivity inhibitor that can replace them has been desired.

Zinc salt has long been known to have an excellent inhibitory effect on tooth hypersensitivity, and previously zinc chloride was widely used as a hypersensitivity inhibitor, but it has a high effective concentration. It cannot be used today because its use concentration cannot be adjusted to a high level and its irritation and corrosive effects on gingiva and pulp are intense.

Means for Solving the Problems The present invention eliminates the above-mentioned drawbacks of conventional hypersensitivity inhibitors, and provides a hyposensitivity inhibitor which is hypoallergenic and can be used safely and effectively without adversely affecting tissues. To do.

That is, the present invention, zinc salt as zinc ions 0.3 ~ 10 wt%, aluminum salts as aluminum ions 0.02 ~.
It relates to a hypersensitivity inhibitor containing 1% by weight and 0.3-2% by weight of anionic surfactant.

The present inventors have paid attention to the hypersensitivity suppressing effect of the zinc salt and have made various studies. However, if a small amount of an aluminum salt and an anionic surfactant were mixed with the zinc salt in the process, these would be synergistic. It has been found that a remarkable hypersensitivity-suppressing effect can be obtained without causing irritation and tissue damage due to zinc salt.

The zinc salt used in the present invention is not particularly limited as long as it has an effect of suppressing hypersensitivity, and various salts which have been conventionally effective for this purpose can be used, but zinc sulfate and zinc chloride are particularly preferable. Preferred examples include zinc sulfate, zinc acetate, zinc acetate, and zinc nitrate. A hydrate of the zinc salt may be used.

The aluminum salt used in the present invention remarkably enhances the inhibitory effect of the above zinc salt, and various inorganic or organic aluminum salts can be effectively used. In particular, aluminum chloride, aluminum sulfate, aluminum lactate, alum. , Aluminum acetate and the like and hydrates thereof can be mentioned as preferable ones.

In the present invention, it is essential to use an anionic surfactant together with the above-mentioned zinc salt and aluminum salt, whereby the perceptual suppressing effect of the mixture of both salts can be further enhanced. As the anionic surfactant, various ones can be used, for example, alkyl sulfates such as sodium lauryl sulfate and sodium cetyl sulfate, triethanolamine lauryl sulfate, lauroyl sarcosine sodium, polyoxyethylene lauryl ether sulfate triethanolamine and the like. Can be mentioned as a preferable example.

The hypersensitivity inhibitor of the present invention is used as an inhibitor for hypersensitivity caused by various local causes. Since this kind of hypersensitivity has various causes and the period until the disappearance of the symptoms is not constant, it is necessary to provide home care guidance in case of long-term symptoms in addition to clinical treatment by the dentist. . Therefore, the blending concentration of each of the above components is appropriately selected according to the usage mode. Zinc ion /
The proportion of aluminum ions is about 50/1 to 5/1, preferably about 8/1.

When the inhibitor of the present invention is used for rapid action, the zinc salt is 3 to 10% by weight as zinc ion, the aluminum salt is 0.2 to 1% by weight as aluminum ion, and the anionic surfactant is 0.3 to 2% by weight. Is good.

When the inhibitor of the present invention is used for a long period of time, it is preferable to use a zinc salt and an aluminum salt at a mixing ratio of 1/10 the concentration of the fast-acting preparation. That is, it is preferable that the zinc salt is 0.3 to 1% by weight as zinc ion and the aluminum salt is 0.02 to 0.1% by weight as aluminum ion. The blending ratio of the anionic surfactant is preferably 0.3 to 2.0% by weight as in the case of the fast-acting preparation.

The inhibitor of the present invention can take a dosage form for various treatments depending on the treatment mode, and for example, for dentist treatment, an aqueous solution, a jelly agent, a paste agent, an ointment, etc. are suitable,
For aftercare, dentifrice, jelly, or film for topical tooth application is suitable.

In addition to the above-mentioned essential components, various additives for formulation can be used in the inhibitor of the present invention, if necessary.

Examples will be given below to explain the present invention in more detail. In the following examples, all% represent% by weight.

Example 1 A conventional dentifrice base was mixed with zinc sulfate heptahydrate 2% (0.45% as zinc ion), aluminum chloride hexahydrate 0.5% (aluminum ion 0.06%) and sodium lauryl sulfate 1.5%, A hypersensitivity inhibitor for the dentifrice formulation was obtained.

Example 2 Zinc sulphate 1.5% (0.7 as zinc ion) in a conventional dentifrice
2%) Aluminum chloride hexahydrate 0.2% (0.02% as aluminum ion) and sodium lauryl sulfate 0.03%
Were mixed to obtain a hypersensitivity inhibitor for the dentifrice formulation.

Example 3 A conventional gel base was mixed with 2.5% zinc sulfate heptahydrate (0.57% as zinc ions) 0.5% aluminum chloride hexahydrate (0.06% as aluminum ions) and 0.1% sodium lauryl sulfate. , A hypersensitivity inhibitor of the dosage form of jelly was obtained.

Example 4 Non-adhesive layer based on polyvinylpyrrolidone containing zinc sulfate heptahydrate 2% (0.45% as zinc ions) aluminum chloride hexahydrate 0.5% (0.06% as aluminum ions) and sodium lauryl sulphate 0.5%. Thus, a bilayer film-like hypersensitivity inhibitor comprising a vinyl acetate polymer layer as a hydrophobic layer for preventing dissolution by saliva or the like was obtained.

Example 5 Zinc sulfate heptahydrate 20% (4.5% as zinc ion) Aluminum chloride hexahydrate 5% (as aluminum ion
0.56%) and sodium lauryl sulfate (0.5%) were dissolved in distilled water to obtain a hypersensitivity inhibitor for the dosage form of the aqueous solution.

Example 6 A conventional gel base was mixed with 20% zinc sulfate heptahydrate (4.5% as zinc ion), 5% aluminum chloride hexahydrate (0.56% as aluminum ion) and 0.5% sodium lauryl sulfate. , A hypersensitivity inhibitor of the dosage form of jelly was obtained.

Example 7 Zinc chloride 15% (as zinc ion 7.
2%) Aluminum chloride hexahydrate 3% (0.34% as aluminum ion) and sodium lauryl sulfate 0.5%
Were mixed to obtain a hypersensitivity inhibitor of the jelly dosage form.

Example 8 Zinc sulfate heptahydrate 24% (zinc ion 5.5%), aluminum chloride hexahydrate 5% (aluminum ion 0.56%), sodium lauryl sulfate 2%, plastibase 70% and sodium polyacrylate. The mixture was mixed with 30% base to obtain an ointment hypersensitivity inhibitor.

Example 9 Zinc sulfate heptahydrate 24% (zinc ion 5.5%), aluminum chloride hexahydrate 5% (aluminum ion 0.56%), sodium lauryl sulfate 2% from Macrogol 400 and Macrogol 4000. Mixed with the base
An ointment hypersensitivity inhibitor was obtained.

Example 10 Zinc sulfate heptahydrate 2 was added to an ethanol solution of copar resin.
% (0.45% as zinc ion) 0.5% aluminum chloride hexahydrate (0.06% as aluminum ion) and 0.5% sodium lauryl sulfate were mixed to obtain a hyperesthesia inhibitor.

Example 11 An anti-collagenase test and a rabbit blood coagulation test were carried out as follows for the preparation of Example 5 as an in vitro test for investigating the hypersensitivity suppressing effect from the protein fixing action of teeth.

1) Anti-collagenase test by agar plate Mix collagen treated with sample solution dissolved in Noble Agar 0.25 and 7.6 ml of physiological saline solution, inner diameter 52m
Pour into a petri dish of m. After solidifying, 2 holes with a diameter of 8 mm
Place 0.1 ml of collagenase solution (5 mg / ml, 0.05 M Tris-HCl buffer pH 7.2 dissolved) in one side and 0.05 M in the other
Add 0.1 ml of Tris-HCl buffer (pH 7.2) and incubate at 37 ° C. After 24 hours, the diameter of the transparent portion that was decomposed by collagenase was measured.

2) Rabbit blood coagulation test Take 0.5 ml of rabbit blood in a Spitz tube and add 0.1 ml of sample to it.
In addition, after shaking well, measure the time until blood does not drop even if the tube is inverted, for 3 minutes.

The results of the anti-collagenase test and the rabbit blood coagulation test are shown in Table 1 below.

Example 12 The effect of the hyperesthesia inhibitor dentifrice obtained in Example 1 was applied to hypersensitivity patients twice a day for 2 weeks continuously. The results are shown in Table 2 below.

Evaluation method Severe pain ………… 3 points, moderate pain …… 2 points Mild pain ………… 1 point If there is no pain… 0 points Pain difference between the first visit day and the second week is 3 points… excellent effect 2 points ... effective,
1 point ... Somewhat effective, 0 point ... Ineffective, and the effective rate was calculated as above.

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Claims (4)

[Claims] 1. A zinc salt is 0.3 to 10% by weight as zinc ion and an aluminum salt is 0.02 to 0.02 as aluminum ion.
A hypersensitivity inhibitor containing 1% by weight and 0.3 to 2% by weight of an anionic surfactant. 2. A zinc salt is 0.3 to 10% by weight as zinc ion, and an aluminum salt is 0.2 to 10% as aluminum ion.
The hypersensitivity inhibitor according to claim 1, which comprises 1% by weight and 0.3 to 2% by weight of an anionic surfactant. 3. A zinc salt is 0.3 to 1% by weight as zinc ion, and an aluminum salt is 0.02 to as aluminum ion.
The hypersensitivity inhibitor according to claim 1, which comprises 0.1% by weight and 0.3 to 2% by weight of an anionic surfactant. 4. The zinc salt is selected from zinc sulfate, zinc chloride, zinc acetate and zinc nitrate, the aluminum salt is selected from aluminum chloride, aluminum sulfate, aluminum lactate, alum and aluminum acetate, and the anionic surfactant is lauryl. The hyperesthesia inhibitor according to any one of claims 1 to 5, which is selected from alkyl sulfates such as sodium sulfate and sodium cetyl sulfate, triethanolamine lauryl sulfate, sodium lauroyl sarcosine and triethanolamine polyoxyethylene lauryl ether sulfate.