MXPA00008697A - Desensitizing dental composition - Google Patents

Abstract

A dental composition for the treatment of dentinal hypersensitivity and in particular for the desensitization of exposed dentin, the desensitizing treatment of deep cavities, the desensitizing treatment when replacing dental layers, the stumps desensitizing treatment before placing dental prosthesis. The composition can be used as a solution or as a gel. In the first case two distinct liquid solutions for use successively on the exposed dentin are provided for. In the second case two distinct gel compounds spread successively on the exposed dentin are provided for. The first solution or the first gel compound comprises preferably three soluble potassium salts, whereas the second solution or the second gel compound comprises a calcium salt and a soluble strontium salt. In a preferred composition two solutions are provided for of which the first has solutes comprising potassium phosphate, potassium carbonate and potassium fluoride, and the second solution has solutes comprising calcium chloride and strontium chloride. For the gel composition, which may be used as toothpaste, two distinct gel compounds are provided, the first having solutes comprising potassium phosphate, potassium carbonate and potassium fluoride and the second gel compound having solutes comprising calcium chloride and strontium chloride.

Description

DESENSITIZING DENTAL COMPOSITION FIELD OF THE INVENTION The present invention relates in general to a compound for dentistry and, more precisely, relates to a dental composition for the treatment of hypersensitivity of dentin. In particular, the composition is suitable for desensitizing the exposed dentin, such as, in particular, for: • the desensitizing treatment of dental caries; • desensitizing treatment when dental layers are replaced; • the desensitizing treatment of ragones before placing dental prostheses. The composition can be used as a solution or as a gel.

DESCRIPTION OF THE PREVIOUS TECHNIQUE Dentine hypersensitivity is a problem that dentists often encounter in their patients, and it often intensifies when they take hot or cold foods, sweet or acidic foods, and when brushing their teeth. Normal dentine is covered by enamel (crown dentine or cementum (root dentine) and is not permeable.

In the sensitive areas of the teeth the enamel is often eroded or worn, and the dentin is exposed. In other cases, the gingival recession reveals the most sensitive portions of the teeth, that is, the enamel-cement joint. The absence of covering exposes the dentinal tubules. Additionally, the pulp is rich in nerves, many of which are centrifugally directed toward the dentine. The dentin is radially crossed by dentinal tubules containing dentinal fluid. Through the tubules, a nervous stimulus reaches the sensory areas of the dental pulp. A first known way to reduce the sensitivity of dentin is to close the holes of the dentinal tubules. For this purpose, natural substances are known that are able to reduce the sensitivity and close the tubules, such as tartar, collagen or mineral salts precipitated in the saliva. It is also known that chemical compounds, similar solutions, gel compounds or pastes, as well as physical treatments, are capable of mechanically obliterating the orifices of the dentinal tubules. Compounds of this class are known from GB 2239601 and WO92 / 04006. Other compounds or treatments of this kind are: • potassium oxalate and iron oxalate, which react with the ionized calcium present in the saliva and form calcium oxalate, which precipitates and obliterates the dentinal tubule orifices; • silver nitrate, which acts by the precipitation of silver compounds; • tin fluoride, which acts by the precipitation of tin compounds; • the strontium salts; • insoluble salts, such as calcium phosphate, hydroxyapatite, colloidal silica, etc., which directly obliterate the tubular orifices; • ionomeric glass cement; • certain types of resins. Other compounds, known, for example, from US-A-5603922 or from WO-A-97/06774, provide a composition useful for remineralizing lesions in dental enamel. Hypersensitivity is counteracted as a secondary effect, due to the obliteration of the dentine, due to remineralization. In any case, the obliteration of the dentinal tubules by means of soluble or insoluble salts used up to now, even if they are of simple use, is not sufficiently effective and only lasts a brief time. Furthermore, compounds such as potassium chloride or potassium nitrate or oxalate are known, capable of reducing the sensitivity of dentin by means of a depolarization effect of the nerve fibers, without obliteration of the dentinal tubules. Therefore, desensitization treatments are known which use said compounds, capable of stopping the nerve activity of the pulp, by varying the excitation capacity of the nerve fibers of the dentinal tubules. However, also in this case the effect is of short duration. New techniques, not yet used in clinical practice, use onomeric glass cement, or photoinduced resins. Desensitization is improved, but they are not easy to use and are good only for deep erosions. In addition, treatment is known using laser or ultrasound scalers, which cause the formation of extended layers and obliteration of the tubules. These treatments will give results, such as effectiveness and duration, similar to the topical treatment with the soluble or insoluble salts described above, but require expensive apparatus.

BRIEF DESCRIPTION OF THE INVENTION It is an object of the present invention to provide a dental composition for dentin desensitization, which has good mechanical obliteration properties of the dentine tubules, in addition to depolarizing the properties of the nerve dentinal fibers, and which is capable of obtaining good effectiveness and long-lasting, and also make it easy to use. According to a first aspect of the invention, this objective is achieved by the composition whose characteristics consist of at least two solutions to be used successively on the exposed dentine. A second aspect of the invention provides at least two different compounds in gel, to be used successively on the exposed dentine. The characteristics of said solutions and said gel compounds consist in that they comprise a first and a second solution, or a first and a second gels, suitable to be mixed topically; wherein: • in the first solution are present a first solute consisting of potassium phosphate, and at least one second solute, selected from potassium carbonate, potassium fluoride, potassium oxalate; and • in the second solution are present a first solute, selected from a calcium salt and at least a second solute selected from a strontium salt, a silver salt, a barium salt, a zinc salt; so that a crystalline complex is formed, comprising: • a plurality of insoluble salts, which have obliteration properties on the dentinal tubules, obtained by means of a double-change reaction of the first and second soluble of the first and second solution; • a soluble potassium salt, which has a depolarizing effect on dentin. The weight ratio, preferred, for the first solution, is as follows: Potassium phosphate 0.5-20% Potassium carbonate 0.5-10% Potassium fluoride 0.1-5% Sodium methylparaben 0.1% Deionized water 64.9-98.8%. The preferred weight ratio for the second solution is as follows: Calcium chloride 0.5-20% Strontium chloride 0.5-11% Sodium benzoate 0.2% Deionized water 68.8-98.8% General weight ratio, preferred, for the first compound, it is as follows: Potassium phosphate 0.5-10% Potassium carbonate 0.5-5% Potassium fluoride 0.1-0.5% Sorbitol 30-45% Colloidal silica 15-30% Glucolol 5-10% Carboxymethylhydroxy ethylcellulose 0.5- 1.5% Sodium lauryl sulfate 1-1.5% Sodium benzoate 0.3-0.8% Sodium saccharinated 0.3-0.5% Mint fragrance c. s. Color Cl 42051, XCI 19140 c. s. Purified water c.s.p.100 ml The preferred, general weight ratio for the second compound is as follows: Strontium chloride 0.5-10% calcium chloride 0.5-10% sorbitol 30-45% colloidal silica 15-30% glycerol 5-10% carboxymethylhydroxyethylcellulose 0.5-1.5 % sodium lauryl sulfate 1.1-5% sodium benzoate 0.3-0.8% Sodium saccharinated 0.3-0.5% mint fragrance cs color CI16255, CI47005 q.s. purified water c.s.p. 100 ml The combined use of the two preferred solutions, or of the two preferred gel compounds, successively has the result, after an immediate double exchange reaction, of six insoluble salts: calcium phosphate calcium carbonate • fluoride of calcium strontium phosphate strontium strontium fluoride and a soluble salt, that is, potassium chloride. According to a sudden reaction, a "crystalline complex" is formed by said six insoluble salts, which surprisingly has the shown desensitization properties in short term (15 minutes and long term (6-12 months) .The formation of potassium chloride It helps to increase the desensitization properties, increasing a nerve depolarization effect, in fact, potassium chloride is obtained after a double change reaction and is present in solution inside the dentinal tubule when the "crystalline complex" is formed that obliterates the tubule orifices.That way a greater amount of potassium is present for a longer time, with respect to the depolarization compounds according to the prior art, which do not obliterate the dentinal tubules, thus allowing the dentinal fluid (whose flow is always centrifugal) and then also the potassium ions, to leave the dentinal tubules. The use of an induced crystallization to obliterate the dentinal tubules with the formation of a "crystalline complex", together with the formation (always inside the tubules) of a compound with depolarizing properties of the nerve fibers, is new in the dental field, and is used with excellent results, in accordance with the present invention. If the composition according to the invention is prepared with potassium phosphate, potassium carbonate and potassium fluoride (for the first solution) in amounts of more than 20, 10 and 5%, respectively, for the first solution; and with calcium chloride and strontium chloride in amounts of more than 20 and 11%, respectively, for the second solution, a desensitization having the same good properties described above is obtained, but less convenient to use. In fact, at the time of the union of both solutions, when the formation of the six insoluble salts occurs, an opalescent gel compound will be obtained, less manageable and less spread on the surface to cure. It is also advisable that the two solutions are spread with different brushes, so that the two solutions or gels are not in contact before reaching the patient's mouth. Similarly, the composition with potassium phosphate, potassium carbonate and potassium fluoride, in amounts of more than 10, 5 and 0.5% for the first compound in gel, and with calcium chloride and strontium chloride in amounts of more of 10% for both salts, in the second gel compound, a desensitizing composition is obtained that can be used and that has the same properties described above, but less suitable for a toothpaste, because its organoleptic aspect would be less acceptable . The composition according to the present invention will be clearer with the following non-limiting examples.

EXAMPLE 1.1 A composition for desensitizing exposed dentin, which uses two solutions for spreading them successively, comprises: potassium phosphate, potassium carbonate and potassium fluoride for the first solution, and calcium chloride and strontium chloride for the second solution, with the following reason by weight: Solution No. 1: Potassium phosphate 16% Potassium carbonate 5% Potassium fluoride 3% Methylparaben sodium 0.1% Deionized water 75.9% Solution No. 2: Calcium chloride 16% Strontium chloride 10.6% Sodium benzoate 0.2 % Deionized water 73.2% The preferred spreading method is as follows for desensitizing treatment: After having isolated the surgical area with cotton or similar elements, and after ablation of the dental plaque by means of low speed electric brushing, it is cleaned the surface to be treated by means of cotton pellets moistened with a disinfectant liquid (such as 5% hypochloride solution) sodium). The surface is then dried with an air jet for about 15 seconds. The drying action must substantially dehydrate the outer layer of the exposed dentin. Then, by means of a brush or cotton pellets or spongy elements, rubbed gently, the first solution is spread for about 20 seconds. Immediately afterwards the second solution is spread on the same dental surface and in the same way. When the hypersensitivity is high, the same treatment can be repeated. The action of said composition, which reacts, forms a crystalline complex that obliterates deeply the orifices of dentinal tubules, is double In fact, the first solution is spread over the dehydrated dentin causing, by capillarity, the filling of the dentinal tubules. Added to this is the nervous depolarization of potassium chloride, which is always formed within the tubules through a double exchange reaction. As an alternative to the composition of Example 1 above, in the same manner, the following exemplification compositions can be used. In these compositions only two potassium salts are present in the first solution, and the crystalline complex will be formed by four insoluble salts only. The suitable potassium salts are still present.

EXAMPLE 1.2 Solution No. 1: Potassium phosphate 16% Potassium oxalate 6% Sodium methylparaben 0.1% Deionized water c.s.p. 100 ml Solution No. 2: Calcium chloride 16% Strontium chloride 10% Sodium benzoate 0.2% Deionized water 73.8% EXAMPLE 1.3 Solution No. 1: Potassium phosphate 16% Potassium carbonate 5% Methylparaben sodium 0.1% Deionized water c.s.p. 100 ml Solution No. 2: Calcium chloride 16% Barium chloride 10% Sodium benzoate 0.2% Deionized water 73.8% EXAMPLE 1.4 Solution No. 1: Potassium phosphate 16% Potassium carbonate 5% Methylparaben sodium 0.1% Deionized water c.s.p. 100 ml Solution No. 2: Calcium chloride 16% Silver chloride 10% Sodium benzoate 0.2% Deionized water 73.8% EXAMPLE 1.5 Solution No. 1: Potassium phosphate 16% Potassium carbonate 5% Methylparaben sodium 0.1% Deionized water c.s.p. 100 ml Solution No. 2: Calcium chloride 16% Zinc chloride 10% Sodium benzoate 0.2% Deionized water 73.8% EXAMPLE 1.6 Solution No. 1: Potassium phosphate 16% Potassium carbonate 5% Methylparaben sodium 0.1% Deionized water 78.9% Solution No. 2: Calcium chloride 16% Strontium chloride 10.6% Sodium benzoate 0.2% Deionized water 73.2% EXAMPLE 2 A desensitizing composition for use as toothpaste, which sequentially uses two gel compounds comprising potassium phosphate, potassium carbonate and potassium fluoride for the first compound in gel and calcium chloride and strontium chloride for the second gel compound , in the following weight ratio: Gel Compound No. 1: Potassium Phosphate 8% potassium carbonate 3.5% Potassium fluoride 0.4% Sorbitol 30% Colloidal silica 15% Glycerol 5% Sodium lauryl sulfate 1.5% Carboxymethylhydroxyethylcellulose 1% Benzoate sodium 0.5% Sodium saccharinated 0.4% Mint fragrance cs Color Cl 42051, Cl 19140 c.s. Purified water c.s.p. 100 ml Gel compound No. 2: Calcium chloride 7% Strontium chloride 6% Sorbitol 30% Colloidal silica 15% Glycerol 5% Sodium lauryl sulfate 1.5% Carboxymethylhydroxyethylcellulose 1% Sodium benzoate 0.5% Sodium saccharinate 0.4% Mint fragrance q.s. Color Cl 16255, Cl 47005 c.s. Purified water c.s.p.- 100 ml This composition is used in the following manner for the desensitizing treatment: • An amount of gel compound No. 1, substantially equal to the volume of two peas, is poured into the toothbrush. • Compound No. 1 is spread on both dental arches, brushing from top to bottom, for about two minutes. • friction is prolonged over areas that are sensitive to hot or cold foods, to acidified or sweet substances; • without rinsing, after having spread the same amount of gel compound No. 2 on the brush, the same tooth surface is brushed again, as described above for the first gel compound; • after the two compounds have been mixed in gel on the dental surface, an instantaneous reaction of double change occurs, with formation of the "crystalline complex", which comprises the six insoluble salts and potassium chloride; • Then rinse your mouth with water. The description of the specific modalities will completely reveal the invention, according to the conceptual point of view, so that others, when applying current knowledge, are able to modify and / or adapt for different applications said modalities without further investigation and without departing from the invention; and therefore, it should be understood that these adaptations and modifications will have to be considered as equivalent to the specific modalities. The means and materials for implementing the different functions described herein could have a different nature without, for that reason, departing from the scope of the invention. It should be understood that the phraseology or terminology used here is intended to describe, and not to limit.

Claims (11)

1. - A dental composition for desensitizing the exposed dentin, characterized in that it comprises a first and a second liquid or gel solution, suitable to be mixed topically; wherein: in the first solution are present a first solute consisting of potassium phosphate and at least one second solute selected from potassium carbonate, potassium fluoride, potassium oxalate; and in the second solution are present a first solute selected from a calcium salt and at least a second solute selected from a strontium salt, a silver salt, a barium salt or a zinc salt; so as to form a crystalline complex comprising: a plurality of insoluble salts having obliterating properties on the dentinal tubules, obtained by reaction of double change of the first solute and the second solute of the first and second solutions; a potassium salt that has a depolarizing effect on dentin.

2. Composition according to claim 1, further characterized in that, in the second liquid solution, the first solute is selected from calcium chloride or calcium acetate, and the second solute is selected from strontium chloride, strontium acetate, silver chloride, barium chloride and zinc chloride.

3. Composition according to claim 1, further characterized in that, in the second gel compound, the first solute is calcium chloride and the second solute is strontium chloride.

4. Composition according to the claims 1 or 2, further characterized in that it comprises a solvent and a bacteriostatic preservative compound.

5. Composition according to claim 4, further characterized in that the solutes are: potassium phosphate, potassium carbonate and potassium fluoride for the first solution; calcium chloride and strontium chloride for the second solution, and are mixed with said solvent and said preservative compound, according to the following ratio in general weight: Solution No. 1: potassium phosphate 0.5-20% potassium carbonate 0.5-10 % potassium fluoride 0.5-5% conservative 0.1% solvent 64.9-98.4%; Solution No. 2: calcium chloride 0.5-20% strontium chloride 0.5-10% preservative 0.2% solvent 69.8-98.8%.

6. Composition according to claims 4 or 5, further characterized in that the solvent is deionized water and the preservative compound is methylparaben sodium for solution 1 and sodium benzoate for solution 2.

7. Composition according to claim 6, characterized in that the solutes, the solvent and the preservative compound are mixed in the following weight ratio: Solution No. 1: potassium phosphate 16% potassium carbonate 5% potassium fluoride 3% methylparaben sodium 0.1% deionized water 75.9 % Solution No. 2: calcium chloride 15% strontium chloride 10.6% sodium benzoate 0.2% deionized water 74.2%.

8. Composition according to claim 4, further characterized in that: in the first liquid solution, said at least second solute is potassium oxalate; and in the second liquid solution, the first solute is selected from chloride or calcium acetate, and the second solute is selected from strontium chloride or acetate, silver chloride, barium chloride, zinc chloride; and said solvent is deionized water, and the preservative is methylparaben sodium for the first solution and sodium benzoate for the second solution.

9. Composition according to claim 3 for use as gel toothpaste, capable of desensitizing the exposed dentine; characterized in that the solutes are present potassium phosphate, potassium carbonate and potassium fluoride for the first compound in gel, and calcium chloride and strontium chloride for the second compound in gel, and the other compounds, according to the following reason general in weight: Compound in gel No. 1: potassium phosphate 0.5-10% potassium carbonate 0.5-5% potassium fluoride 0.1-0.5% sorbitol 30-45% colloidal silica 15-30% glycerol 5-10% carboxymethylhydroxyethylcellulose 0.5 -1.5% lau ri Isu Sodium sodium 1-1.5% sodium benzoate 0.3-0.8% sodium saccharinated 0.3-0.5% mint fragrance cs color Cl 42051, Cl 19140 c.s. purified water c.s.p. 100 ml; Compound No. 2: strontium chloride 0.5-10% calcium chloride 0.5-10% sorbitol 30-45% colloidal silica 15-30% glycerol 5-10% carboxymethylhydroxyethylcellulose 0.5-1.5% sodium lauryl sulfate 1-1.5% sodium benzoate 0.3-0.8% sodium saccharinated 0.3-0.5% mint fragrance cs color Cl 16255, Cl 47005 c.s. purified water c.s.p. 100 ml.

10. Composition according to claim 8, further characterized in that the solutes and other compounds are mixed in the following weight ratio: Gel Compound No. 1: potassium phosphate 8% potassium carbonate 3.5% potassium fluoride 0.4 % sorbitol 30% colloidal silica 15% glycerol 5% lauri Isu If ato de sodio 1.5% carboxymethylhydroxyethylcellulose 1% sodium benzoate 0.5% saccharinated sodium 0.4% mint fragrance cs color Cl 42051, Cl 19140 c.s. purified water c.s.p. 100 ml; Compound in gel No. 2: calcium chloride 7% strontium chloride 6% sorbitol 30% colloidal silica 15% glycerol 5% sodium lauryl sulfate 1.5% carboxymethylhydroxyethylcellulose 1% sodium benzoate 0.5 sodium saccharine 0.4% mint fragrance q.s. color Cl 16255, Cl 47005 c.s. purified water c.s.p. 100 ml.

11. A method for preparing a dental desensitizing composition, characterized in that it comprises the steps of: preparing a first liquid solution or gel solution, comprising a first solute consisting of potassium phosphate and at least one second solute selected from carbonate of potassium, potassium fluoride, potassium oxalate; and preparing a second liquid solution or gel solution, comprising a first solute selected from a chloride or an acetate salt; topically mixing the first and second solutions, thereby forming a crystalline complex comprising a plurality of nonsoluble salts, obtained by double-shifting reaction, of the above-mentioned salts potassium chloride or acetate; said insoluble salts having obliterating properties of the dentin tubules, and a soluble potassium salt having a depolarizing effect on the dentine.