Oral care composition applicable for dental erosion and/or wear control

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to oral care agents. What is presented is using an oral care composition in the form of a mouthwash containing a fluoride ion source and a ternary polymer system consisting of xanthane gum, carboxymethyl cellulose and copovidone for dental erosion and/or wear control. This composition is also effective in dental caries control.

EFFECT: using fluoride ions in a combination with the ternary polymer system provides the better protection of the dental surface against dental erosion as compared to using fluoride ion only.

7 cl, 4 dwg, 5 ex

 

AREA of TECHNOLOGY

The present invention relates to compositions for the care of mouth cavity containing a triple polymer system and a source of fluoride ion, to fight (i.e. to facilitate the prevention, inhibition and/or treatment of pathological abrasion of the teeth and/or tooth wear. Such compositions are also useful in combating dental caries.

PRIOR art

Mineral teeth consists mainly of calcium hydroxyapatite, CA10(RO4)O(OH)2that may be partly replaced by anions, such as carbonate or fluoride, and cations such as zinc or magnesium. Mineral teeth may also contain Naamathite mineral phases, such as phosphate actualize and calcium carbonate.

Tooth loss can occur as a result of dental caries, representing a multifactorial disease in which bacterial acids, such as lactic acid, causing subsurface demineralization that is not fully remineralized, leading to progressive loss of tissue and, ultimately, to the formation of cavities. The presence of dental plaque biofilm is a prerequisite for caries and acid producing bacteria, such as Streptococcus mutans, can become pathogenic when the levels legkofermentiruemyh carbohydrate, such as sucrose, TPU� elevated for extended periods of time.

Even in the absence of the disease can lead to loss of dental hard tissues as a result of acid erosion and/or physical deterioration of the teeth; I believe that these processes work in synergy. Impact on dental hard tissue acid causes demineralization, which leads to softening of the surface and the decrease of the density of the mineral. In normal physiological conditions demineralized tissue independently restored due to the remineralizing effects of saliva. Saliva is supersaturated with calcium and phosphate, and in healthy people the secretion of saliva is introduced to flush the acid and raises the pH so as to shift the equilibrium toward mineral deposits.

Pathological abrasion of the teeth (acid erosion or acid wear) is a surface phenomenon that involves demineralization, and, ultimately, the complete dissolution of the tooth surface by acids of non-bacterial origin. Most often the acid is of food origin, such as citric acid from fruit or fizzy drinks, phosphoric acid from Cola-type drinks and acetic acid, for example, seasonings and vinegar. Pathological abrasion of the teeth can also be caused by repeated contact with the hydrochloric acid (Hcl) produced in the stomach that may�to ikot in the oral cavity as a result of involuntary response, such as gastroesophageal reflux, or as a result of the induced response, you may encounter of suffering from bulimia.

Wear of the teeth (i.e., the physical wear of the teeth) is caused by friction and/or abrasion. Friction occurs when the surfaces of the teeth RUB against one another, the shape of the abrasion of two bodies. Frequent dramatic example is the phenomenon which is observed in subjects with bruxism, the habit of grinding her teeth when the effort is large, and is characterized by accelerated wear, especially on occlusal surfaces. Abrasion usually occurs as a result of friction of the three bodies and the most common example is the phenomenon associated with tooth brushing toothpaste. In the case of fully mineralized enamel, levels of abrasion caused by commercially available toothpastes, minimal and have little clinical impact, or have no clinical consequences. However, if the enamel was demineralization and softened by the impact of introduced erosive agent, the enamel becomes more sensitive to the wear of the teeth. Dentin is softer than enamel and therefore more susceptible to wear. Subjects with unprotected dentin, avoid the use of abrasive toothpastes such as pastes on the basis of aluminum oxide. Besides softening de�Tina entered erotiuli agent increases the susceptibility of the fabric to wear.

Dentin is a vital tissue, which in vivo is usually covered with enamel or cement depending on the position, that is, the tooth crown vs root, respectively. Dentin has a higher organic content than enamel, and its structure is characterized by the presence of fluid-filled tubules that extend from the surface of the dentin-enamel or place of compounds of the dentin-cement to the surface of the section odontoblast/pulp. It is considered that the origin of dentin hypersensitivity refers to changes in fluid flow in open tubules (hydrodynamic theory), leading to stimulation of mechanoreceptors, which are believed, are located close to the surface section odontoblast/pulp. Not all exposed dentine is sensitive, since it is usually covered by a smear layer (smear layer); closing a mixture consisting mainly of mineral and protein derivatives of the dentin, but also contains organic components of saliva. Over time, the lumen of the tubule may gradually clog mineralized tissue. The formation of reparative dentin in response to injury or chemical irritation of the pulp is also well documented. However, the erosive agent can remove the smear layer and "clogging" of the tubule, causing currents� dentinal fluid out, what makes the dentin is much more sensitive to external stimuli such as heat, cold and pressure. As mentioned earlier, erosive agent can also make the surface of the dentin is much more sensitive to wear. In addition, dentin hypersensitivity, which increases with the diameter of the open channel, and because of increasing the diameter of tubules continue in the direction of the surface section odontoblast/pulp, degenerative dentin may lead to increased hypersensitivity, especially in cases where the wear of dentin occurs rapidly.

Loss of the protective layer of enamel due to erosion and/or mediated by acid wear exposes the underlying dentin, and therefore they are the main etiological factors in the development of dentin hypersensitivity.

It is argued that increasing the intake of dietary acids and waste from the ordered time of food intake accompanied by an increase in the incidence of pathological abrasion and wear of the teeth. In view of this, will be useful compositions for caring for the oral cavity that contribute to the prevention of pathological abrasion of the teeth and tooth wear.

The present invention is based on the discovery that the presence of a triple polymer system consisting of xanthan gum, carboxymetilcellulose� and copovidone in a composition for caring for the oral cavity, comprising a source of fluoride ions, enhances the effectiveness of fluoride ion in the suppression of pathological abrasion of teeth.

Oral compositions containing such a triple polymer system described in WO 2006/013081 (Glaxo Group Ltd) for use in the treatment or relief of symptoms of dry mouth through the lubrication and hydration of the oral cavity. Such compositions may contain a source of fluoride ion as an anti-caries agent. There is no indication that such compositions can counteract pathological abrasion of the teeth or the triple polymer system can increase the efficiency of the fluoride ion in the suppression of pathological abrasion of teeth.

In Van der Reijden et al. (Caries Res., 1997, 31, 216-23) described a series of experiments in vitro with the compositions of saliva substitutes containing thickeners for the study of their properties of protection against dental caries, including effects on demineralization and remineralization of enamel in vitro. Describe the impact of a number of polymeric substances on the dissolution of hydroxyapatite crystals in 50 mm acetic acid at pH 5.0, and experiment with the cyclic change of pH in which bovine enamel exposed to demineralized buffer (pH of 4.8) and remineralization buffer (pH 7.0), containing a number of dissolved polymer. These experiments suggest that such polymers, including to�Antonova gum and carboxymethylcellulose, can reduce the demineralization of enamel in vitro, and it is assumed that this may be the result of formation of adsorbed polymer layer on the enamel surface, providing protection against corrosion by acids.

In WO 00/13531 (SmithKline Beecham) describes the use of various modifying viscosity polymeric substances as inhibitors of erosion of the teeth in acidic compositions for oral administration, such as acidic beverages or acidic oral medical composition. Examples of polymers include xanthan gum, carboxymethylcellulose and polyvinylpyrrolidone.

The role of some polymeric substances in protecting against pathological abrasion of the teeth is described in WO 2004/054529 (Procter & Gamble), where the claimed method of protection against pathological abrasion of the teeth, including the introduction of a composition for caring for the oral cavity containing polymeric mineral surface active agent (i.e., a polyelectrolyte, such as polyphosphate, PCE or some carboxy-substituted polymers), where the polymeric mineral surface active agent is substantive to teeth and precipitates a layer that protects teeth from erosive damage immediately after use and for at least one hour afterwards. This means that such compositions for the care of the oral cavity may contain East�CNIC fluoride ion, although there is no indication that the presence of a polymeric mineral surface-active agent may enhance the effectiveness of fluoride in protecting against pathological abrasion of the teeth. It is also assumed that such oral compositions may contain various thickeners, including xanthan gum and carboxymethylcellulose. It is not intended that such thickeners are essential to teeth or can protect the teeth against pathological abrasion of the teeth.

In Schaad et al. (Colloids and Surfaces A: Physiochemical and Engineering Aspects 1994; 83; 285-292) described the inhibition of dissolution of the powder of hydroxyapatite adsorbed anionic polymers and it is expected that some of them can be effective agents for the prevention of dissolution of enamel or bone tissue.

In EP-A-691124 (Sara Lee) describes the products for the care of mouth cavity containing a copolymer of N-vinylpyrrolidone with acrylic acid, which lead to increased absorption of fluoride in the enamel of the tooth enamel. On page 11 describes the relative absorption efficiency of enamel fluoride from a variety of compositions containing various thickeners, where thickeners include carboxymethyl cellulose, a combination of xanthan gum and HPMC, a combination of xanthan gum and a copolymer of N-vinylpyrrolidone with acrylic acid and the combination to�antonovoi gum and a copolymer of methyl vinyl ether with maleic acid or anhydride.

In the French patent No. 2755010 (Sara Lee) describes a fluoride containing product to care for the oral cavity that contains a combination of xanthan gum and carboxylated vinyl polymer, it was found that this combination increases the effectiveness of fluoride in fighting tooth decay.

A BRIEF summary of the INVENTION

In the first aspect of the present invention proposed a composition for caring for the oral cavity to combat abnormal abrasion and/or wear of the teeth, comprising a source of fluoride ions and a triple polymer system consisting of xanthan gum, carboxymethyl cellulose and copovidone.

Triple polymer system facilitates the retention of fluoride on the tooth surface, thereby increasing the remineralization of teeth and increasing the resistance of teeth to acids, thus providing better protection of the surface against the effects of pathological abrasion of teeth than fluoride.

Accordingly, the compositions of the present invention are useful for increasing the efficiency of the fluoride ion in the suppression of pathological abrasion of the teeth and/or tooth wear. Such compositions can contribute both to the protection and re-hardening the enamel when exposed to food acids.

Such compositions are also useful in combating dental caries.

BRIEF DESCRIPTION�of GRAPHIC MATERIALS

Fig.1 shows obtained by dynamic mass spectrometry secondary ion image of a cross section of human enamel after exposure to solutions containing equal concentrations of sodium fluoride (a) in the presence of a triple polymer system, b) in the absence of a triple polymer system.

Fig.2 shows the average values of surface roughness (Sa) for enamel, tucked the effects of citric acid, after treatment with various solutions.

Fig.3 shows the average values of the height of the step for enamel, tucked the effects of citric acid, after treatment with various solutions.

Fig.4 shows the re-hardening artificial erosive damage to the enamel of a person through 48 h after treatment composition for rinsing the oral cavity (or toothpaste Sensodyne Pronamel).

Fig.5 shows relative values of microhardness for human enamel exposed to citric acid, after treatment with a composition for rinsing the oral cavity (or toothpaste Sensodyne Pronamel).

DETAILED description of the INVENTION

Xanthan gum may be present in amounts of from 0.001 to 1.0% based on the total weight of the composition, for example from 0.005 to 0.5%, or from 0.005 to 0.1% based on the total weight of the composition.

Carboxymethylcellulose for use in the invention is � the form of sodium salt, that is sodium carboxymethylcellulose. The carboxymethyl cellulose may be present in an amount of from 0.02 to 20% based on the total weight of the composition, for example from 0.04 to 10% or from 0.1 to 1.0% based on the total weight of the composition.

Copovidone (which is a copolymer of vinylpyrrolidone and vinyl acetate, more specifically, the copolymer of 1-vinyl-2-pyrrolidone and vinyl acetate in the ratio 3:2 by weight) may be present in an amount of from 0.1 to 20% based on the total weight of the composition, for example from 0.2 to 10% or from 0.5 to 5% based on the total weight of the composition.

Examples of a source of fluoride ions for use in the present invention include an alkali metal fluoride such as sodium fluoride, alkali metal monofluorophosphate such as sodium monofluorophosphate, tin fluoride or amine fluoride in an amount that provides from 25 to 3500 million-1fluoride ions, preferably from 100 to 1500 mn-1. A suitable source of fluoride is an alkali metal fluoride such as sodium fluoride, for example, the composition may contain from 0.05 to 0.5 wt%. Sodium fluoride, such as 0.1 wt%. (corresponds to 450 million-1fluoride ion), 0,205% of the mass. (corresponds to 927 million-1fluoride ions), 0,2542% of the mass. (corresponds to 1150 million-1fluoride ion) or 0,315% of the mass. (corresponds 1426 mn-1fluoride ion).

The compositions of the present invention �will gain the suitable agents for the manufacture of the drug, such as abrasives, surfactants, thickeners, humectants, flavoring agents, buffer agents, sweeteners, mud or coloring agents, preservatives and water, selected from agents that are typically used in the manufacture of a composition for caring for the oral cavity for such purposes. Examples of such agents are described in WO 2006/013081 (Glaxo Group Ltd) and WO 2004/054529 (Procter & Gamble), the contents of which are incorporated into this description by reference.

The compositions of the present invention is usually prepared in the form of toothpastes, sprays, mouthwashes for mouth, gels, lozenges, chewing gums, tablets, lozenges, dispersible powders, plates for the oral cavity and buccal patches. The preferred compositions are toothpastes and mouthwash.

In the compositions of the present invention may include additional active substances for the care of the oral cavity.

In addition, the compositions of the present invention may contain a desensitizing agent for combating dentine hypersensitivity. Examples desensibiliziruyuschimi agents include tubule occluding agent or agent, desensitizing the nerve, and mixtures thereof, which, for example, described in WO 02/15809. Suitable desensitizing agents include strontium salt such as strontium chloride, acetate St�once or nitrate of strontium, or potassium salt such as potassium citrate, potassium chloride, potassium bicarbonate, potassium gluconate and especially potassium nitrate.

Desensitizing potassium salt is generally from 2 to 8% based on the total weight of the composition, for example, you can use 5% of the mass. of potassium nitrate.

In another aspect of the present invention proposed composition is a mouthwash containing a source of fluoride ions and a triple polymer system, as defined above, for the suppression of pathological abrasion of the teeth and/or tooth wear.

The source of fluoride ion may be present in the composition of the mouthwash in the amount up to the maximum allowed by the rules for any specific market. For example, according to the rules of the EU mouthwash can contain up to 125 mg of fluoride ion on one container of the product. In US mouthwash for OTC (non-prescription) the application may contain no more than 225 million-1of fluoride. Typically, the composition is a mouthwash contains from 100 to 1500 mn-1the fluoride ion, for example from 150 to 1000 ppm-1or from 200 to 600 million-1, for example 225 million-1or 450 million-1the fluoride ion.

In this composition, mouthwash source of fluoride ion may be an alkali metal fluoride such as sodium fluoride.

Suitably the composition is a mouthwash �will win xanthan gum in amounts of from 0.005 to 0.02% based on the total weight of the composition.

Appropriate composition mouthwash contains carboxymethylcellulose in an amount of from 0.1 to 0.4% based on the total weight of the composition.

Appropriate composition mouthwash contains copovidone in an amount of from 0.5 to 1.5% based on the total weight of the composition.

Such an arrangement mouthwash can advantageously be used in conjunction with fluoride toothpaste, in particular with fluoride toothpaste, which has a higher efficiency, for example of the type described in WO 2006/100071, which are included in this description by reference, and suitably contains an alkali metal fluoride as the fluoride source, an amphoteric surfactant or maloine surface-active substance, which represents metallatria methyl coquillart, or a mixture thereof as a surfactant, and abrasive for the teeth on the basis of silicon dioxide as an abrasive substance, composition, having the value of the relative abrasiveness against dentin (RDA) from 20 to 60 and a pH in the range of 6.5 to 7.5 and containing orthophosphate buffer, a water soluble salt With10-18alkylsulfate and calcium salt.

Thus, in another aspect, the present invention includes a scheme of care for the oral cavity to combat pathological stonemont�Yu teeth and/or tooth wear, includes daily use of the composition of the present invention mouthwash and fluoride toothpaste. Appropriately each of mouthwash and fluoride toothpaste is used at least twice a day in accordance with the scheme to care for the oral cavity according to the present invention.

With the aim of improving adherence for care by the consumer in the present invention also proposes a kit for caring for the oral cavity to combat abnormal abrasion and/or wear of the teeth, containing the composition according to the present invention mouthwash, fluoride toothpaste, and instructions for their use in the scheme of care for the oral cavity according to the present invention.

The compositions of the present invention can be produced by mixing the ingredients in the appropriate relative amounts in any order that is convenient, and, if necessary, regulation of pH to obtain the desired value, for example from 4.0 to 9.5, such as from 5.5 to 9.0, for example from 6.0 to 8.0, or from 6.5 to 7.5.

The present invention also provides a method of combating pathological abrasion of the teeth and/or tooth wear which comprises applying an effective amount of a composition as defined above, to a subject in need of it.

The present invention also proposed the use of high�ka fluoride ions and a triple polymer system, consisting of xanthan gum, carboxymethyl cellulose and copovidone in the manufacture of a composition for caring for the oral cavity to fight with pathological abrasion of the teeth and/or tooth wear.

The invention is additionally illustrated by the following examples.

Example 1

Dynamic mass spectrometry of secondary ions (DSIMS)

Dynamic mass spectrometry of secondary ions is a semiquantitative method that makes it possible for fast elemental depth profiling with depth resolution in the nanometer scale and sensitivity in the parts per billion and chemical maps with submicron detail. Before DSIMS used to study the composition of the enamel and to determine the degree of inclusion of fluoride in the enamel surface in humans. In such a study, using DSIMS, investigated the effect of the presence of a triple polymer system on the inclusion of fluoride in the surface of human enamel containing artificial erosive damage. In this experiment, a triple polymer system consisting of a 0.75% copovidone, 0.2% carboxymethyl cellulose and 0.01% of xanthan gum, it's all calculated on the total weight of the composition.

Inserted in the acrylic resin samples of human enamel with a size of ~2×2 mm, smooth polished, using paper with silicon carbide grit 1200 and 2400. Then� the samples were divided into one of four groups for treatment (n=5):1) deionized water, 2) the triple polymer system in deionized water 3) a solution of fluoride 300 million-1(the fluoride source=sodium fluoride) and 4) triple polymer system with 300 million-1fluoride (the fluoride source=sodium fluoride), each solution to processing has a pH falling in the range of from about 6.5 to 7.0. Artificial erosive damage created in the enamel by dipping the samples for 5 minutes in a 1.0% solution of citric acid, pH 3.8. Then, after washing enamel deionized water, the samples were placed under stirring for 1 minute in one of the mixtures described above. The final washing stage was performed (using deionized water) prior to analysis DSIMS. Distribution of fluoride incorporated into enamel/held-on enamel was determined using DSIMS. Mode depth profiling was used at the initial stage to determine the relative concentrations of fluoride in the first few microns of the surface. This was accompanied by the production of a vertical sectioning of samples, which are then inserted in epoxy resin and polished. The obtained cross sections were coated with gold and the distribution of fluoride was studied using DSIMS-visualization on the enamel to a depth of ~200 µm. Data were obtained from different plots (by size of 200 μm ×160 μm and 100 μm ×80 μm) of each sample.

Typical transverse image �to enable enamel samples shown in Fig.1. Samples, processed or only water or a triple polymer system in water, showed a lack of fluoride in the samples at any depth (data not shown). Samples treated with one or a solution of a fluoride, or a fluoride solution, containing a triple polymer system showed fluoride containing strip on the enamel surface, approximately 60 μm in depth in both cases (Fig.1A and b). However, the enamel treated with the triple polymer system and a fluoride contained significantly more fluoride in the top 6 μm, the surface of the fabric (Fig.1A and b) than the enamel treated with one fluoride. See Fig.1, which shows obtained by dynamic mass spectrometry secondary ion image of a cross section of human enamel after exposure to solutions containing equal concentrations of sodium fluoride (a) in the presence of a triple polymer system b) in the absence of a triple polymer system.

Example 2

The white light interferometry (3DP)

Method of white light interferometry provides a quick visualization of the surface topography and determination of the roughness parameters in a non-contact method, which can be obtained by the resolution of the height in the nanometer scale. In this study, the effects of artificial erosive agent on the enamel of the person observed using white light interferometry Investigated the influence of pre-treatment of enamel with a solution contains only the triple polymer system, and the system in combination with fluoride. In this experiment, a triple polymer system consisting of a 0.75% copovidone, 0.2% carboxymethyl cellulose and 0.01% of xanthan gum, it's all calculated on the total weight of the composition.

Samples of human enamel were polished and divided into one of four groups for treatment (n=5):1) deionized water, (2) fluoride 300 million-1(sodium fluoride) 3) triple polymer system with 300 million-1fluoride and 4) triple polymer system in deionized water, where each solution for treatment has a pH in the range of from about 6.5 to 7.0. The samples were incubated for 1 min in solutions for processing and then washed with deionized water. Before exposure to acid sample surface is partially masked with tape to get a reference point that allows you to measure any loss of underlying tissue. During the phase of erosion, the samples were immersed in 1.0% solution of citric acid, pH 3.8, for 5 minutes. The surface topography of the samples was investigated using a white light interferometer ADE PhaseShift MicroXAM. Data received from multiple sections (200 μm × 160 μm and 100 μm × 80 μm) of each sample. After removal of the mask with tape samples performed additional measurements to determine whether there has been any loss of underlying tissue during the experimental�.

The results of this study are summarized in Fig.2 and 3. Measurement of Sa (surface roughness) and Sz (ten-point height) of the enamel treated with deionized water showed that the acidic agent significantly increased the surface roughness of the samples (Fig.2). However, the analysis of samples that have been treated with solutions containing fluoride and/or triple polymer system showed that these solutions for pretreatment provided protection against surface changes observed after pre-treatment with water only. The enamel treated with the triple polymer system in combination with fluoride, had the lowest values of Sa, indicating an additional protective effect of these two agents when used in combination against any one of these agents (Fig.2).

Profilometric measurements made along the surface of the section of the treated plot/tape disguised plot showed that the loss of underlying tissue from samples treated with various solutions reflect a General trend in the values of surface roughness, shown in detail above (Fig.3). The most significant average loss of the main fabric was measured for the samples treated only with deionized water, and approximately 20 microns. The average loss of fabric for samples, about�Botanik solution contains only the triple polymer system was approximately 2.5 μm, and for samples treated with solutions containing only fluoride or combination of fluoride and a triple polymer system was less than 1 µm (Fig.3).

Example 3

Re-hardening the enamel softened by acid

Artificial erosive damage received of polished human enamel, inserted in the acrylic resin. Damage obtained by bringing into contact of the inserted samples for 30 minutes with 1.0% wt./mass. the citric acid solution, pH 3.8. The original hardness of each subject to erosion of the sample was determined using microindenter Struers Duramin Microindenter, equipped with a diamond tip Vickers. Hardness values were expressed as numbers of the Vickers hardness (VHN). Load 1,961 N was applied to the samples with a dwell time of 20 seconds. Then the samples randomizable and were divided into 4 groups for treatment (n=6).

Six samples of enamel were placed at 120 C in one of two compositions for rinsing the mouth, or water, or mix 1:3 wt./mass. the slurry obtained from improved fluoride toothpaste (1450 mn-1F). Improved fluoride toothpaste is described in W02006/100071 and sold as Sensodyne Pronamel. Two compositions for rinsing the mouth was a Colgate Plax Sensitive (225 million-1 F) and ProRinse (450 million-1F), that is being tested for rinsing the oral cavity for use in the present invention, such as those described in WO 2006/013081 having a pH of 7.0 and containing 0.1% of sodium fluoride and a triple polymer system consisting of a 0.75% copovidone 0.2% carboxymethyl cellulose and 0.01% of xanthan gum, it's all calculated on the total weight of the composition. Segment to handle toothpaste Sensodyne Pronamel was included in the analysis as a reference to provide verification during the study. Then the samples were removed and placed in containing mucin artificial saliva. Re-hardening of the sample was determined using microindentation after 24 h and 48 h. For each sample was obtained by six notches in each moment of time.

The results of the study re-curing are summarized in Fig.4. Hardness values of enamel were normalized relative to values obtained after softening the enamel acid. Thus, the data in the later time points show the re-hardening of the enamel. All enamel samples became solid again during the period when they were exposed to artificial saliva, and processing or composition for rinsing the mouth, or toothpaste Sensodyne Pronamel resulted in statistically greater re-hardening than treatment with water and one eve of another time. In addition, after 24 hour remineralization treatment or toothpaste Sensodyne Pronamel or ProRinse resulted in statistically greater re-hardening compared to rinsing with mouthwash Colgate Plax Sensitive. However, after 48 h of incubation in artificial saliva, there was no difference between the degree of remineralization after treatment with one of two compositions for rinsing the mouth or toothpaste.

Example 4

Protection against the effects of acid erosion

The study included the impact on human enamel 1% citric acid (pH 3.8), then 2 minutes of processing one of the two aforementioned compositions for rinsing of the mouth (used in the study of re-curing), water or toothpaste Sensodyne Pronamel. The samples were washed with water between treatments and exposure to acid. The study of acid erosion consisted of 10, 20 and 30 minutes, and microhardness measurement was performed at each time point after washing the samples with distilled water again. At all time points for each sample of the enamel gets six notches. Each treatment was performed on six separate samples.

The study results softening are summarized in Fig.5. Hardness values of enamel were normalized with respect to the individual source values microti�achievements, thus the data at a later point in time reflect the softening of the enamel. After 10-minute exposure acid composition Prorinse provided statistically greater protection against softening the enamel surface than any of the other treatments. After a 20-minute exposure to acid treatment for rinsing the oral cavity Prorinse and toothpaste Sensodyne Pronamel resulted in statistically lower softening of the enamel than treatment with water, but definitely less softening than treatment with a rinsing mouthwash Colgate Plax Sensitive. By the time the 30-minute erosion composition for rinsing the oral cavity Prorinse provided statistically greater protection against softening the surface than the water treatment, and definitely more protection against softening than rinsing with mouthwash Colgate Plax Sensitive.

1. The use of a composition for caring for the oral cavity in the form of a liquid mouthwash, containing a source of fluoride ions and a triple polymer system consisting of xanthan gum, carboxymethyl cellulose and copovidone for the suppression of pathological abrasion of the teeth and/or tooth wear.

2. Use of the composition according to claim 1, wherein the source of fluoride ion is a fluoride of an alkali metal.

3. Use of the composition according to claim 1, wherein the xanthan gum is present in an amount of from 0.001 to 1.0% in �calculating the total weight of the composition.

4. Use of the composition according to claim 1, wherein the carboxymethylcellulose is present in an amount of from 0.02 to 20% based on the total weight of the composition.

5. Use of the composition according to claim 1, wherein the copovidone is present in an amount of from 0.1 to 20% based on the total weight of the composition.

6. Use of the composition according to any one of claims. 1-5 containing desensitizing agent.

7. Use of the composition according to claim 6, where the desensitizing agent is a salt of strontium or potassium salt.



 

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6 ex

FIELD: chemistry.

SUBSTANCE: composition of preparation for teeth cleaning contains effective quantity of arginine in free form or in form of salt; abrasive substance, containing (i) natural sodium carbonate (NSC) with the average size of particles 3-7 mcm and moisture absorption 12-25 g/100 g and (ii) precipitated calcium carbonate (PCC) with the average particle size 1-5 mcm and water absorption higher than 25 g/100 g. Ratio of natural calcium carbonate to precipitated calcium carbonate constitutes from 1:2 to 1:3. Composition has pellicle cleaning ratio (PCR), at least, 70 and value of abrasivity of isotope-labelled dentin (RDA) lower than 140. Method of oral cavity care includes application of effective quantity of said composition in oral cavity of individual requiring it.

EFFECT: effective teeth cleaning and strengthening without injuring abrasive action, which makes it possible to apply it, in particular, for individuals with increased teeth sensitivity.

13 cl, 2 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: composition contains a) surface-active substances, including a salt of C10-16 alcohol ethoxylate sulphate, a betaine surface-active substance and alkylpolyglicoside, and b) a fatty C12-18 acid, constituting at least 15% of the total composition weight.

EFFECT: composition, possessing an increased viscosity and capable of producing a stable foam, is created.

10 cl, 1 tbl, 4 ex, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine, particularly to cosmetology, and describes a method for stabilising an anhydrous antiperspirant composition involving: (a) preparing a mixture of at least one substance having the antiperspirant action, containing a metal salt, and an anhydrous carrier for at least one substance possessing the antiperspirant action, wherein dissolved is at least one substance having the antiperspirant action, a carrier containing an eutectic mixture of carbamide and trimethylglycine; (b) heating this mixture for preparing the eutectic mixture of at least one substance having the antiperspirant action, and the anhydrous carrier.

EFFECT: invention can be used to reduce the body perspiration; the compositions can be applied by hands or with a package.

22 cl, 3 dwg, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a compound of formula such as below , wherein Z is oxygen; Y is hydrogen or a sequence as follows: -O-C(R4)-V-(C=O)-R5; V is oxygen; R1 and R4 are identically or independently hydrogen or a C1-4 alkyl; R2 and R5 are identically or independently a C1-10 alkyl.

EFFECT: these compounds can be applicable in therapy for treating pathologies or disorders related to the presence of Propionibacterium acnes, eg acne-like skin disorders.

5 cl, 2 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed is emulsified composition for improvement of skin condition, which contains (A) 0.001-10 wt % of organic compound, which has two or more hydroxyl groups, inorganic value 220-450 and organic value 300-1000; (B) 0.001-10 wt % of organic compound, which has one hydroxyl group, inorganic value 100-200 and organic value 280-700; (C) 0.001-10 wt % of organic substance, represented by formula (2), in which R1 is C4-C30 hydrocarbon group; Z is methylene group, methane group or oxygen atom; X1, X2, X3 are hydrogen atom, hydroxyl group or acetoxy group; X4 is hydrogen atom, acetyl group or glyceryl group; each of R2 and R3 is hydrogen atom, hydroxyl group, hydroxymethyl group or acetoxymethyl group; R4 is C5-C60 hydrocarbon group; and R5 is hydrogen atom or hydrocarbon group, containing in total 1-30 carbon atoms; (D) (D) 0.00012-10 wt % of at least one compound, selected from group, consisting of non-ionic surface-active substance, which has polyoxyethylene group and HLB 10 or higher, ionic surface-active substance and sphingosine salt; (E) 0.003-15 wt % of at least one compound, selected from group, consisting of sugar alcohol, selected from group, consisting of erythritol, threitol, xylitol and mannitol, disaccharide and trisaccaride, and (F) water.

EFFECT: emulsion composition preserves water in skin for long time.

13 cl, 1 dwg, 18 tbl, 64 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the chemical-pharmaceutical industry and represents an agent for preventing or reducing pigmentation, containing a compound presented by the following formula (1) its stereoisomer and/or its pharmacologically acceptable salt, wherein: R1 represents a hydrogen atom or an alkyl group with a linear or branched chain having 1-4 carbon atoms; R2 represents a hydrogen atom or an unsubstituted aliphatic hydrocarbon group having 1-4 carbon atoms; R3 represents an unsubstituted aromatic group having 5-15 carbon atoms, substituted by an alkyl group having 1-6 carbon atoms, by an alkoxy group containing an alkyl chain having 1-6 carbon atoms, or by a phenyl group; R3 also represents an aromatic group having 5-15 carbon atoms; n is equal to 1 or 2, and m represents an integer falling within 0 to 3.

EFFECT: preparing the agent for preventing or reducing pigmentation.

10 cl, 10 ex, 6 tbl

Hair care product // 2553347

FIELD: cosmetology.

SUBSTANCE: hair care product is made in the form of gel, shampoo, lotion. All embodiments comprise aqueous vegetable extracts, phosphonate complex containing potassium-sodium salts of oxyethylidenebisphosphonic acid or their mixture with trisodium salt hexahydrate of phosphonformic acid and a cosmetically acceptable base.

EFFECT: hair care product is recommended for use in medicinal and cosmetic purposes for all ages for prevention and treatment of dystrophic changes in hairy part of the head.

5 cl

FIELD: cosmetology.

SUBSTANCE: cosmetic product contains an aqueous solution of trace elements in amounts close to the daily demand of the human body, succinic acid which provides a high level of energy production (ATP), and also a bioregulatory complex obtained from hair follicles of calves, which stimulates proliferation of dormant cells of hair follicles.

EFFECT: increased efficiency of cosmetic product for complete prevention of hair loss caused by a wider range of reasons, and for partial or complete restoration of hair.

5 ex

FIELD: chemistry.

SUBSTANCE: invention relates to application of dry extract of aronia melanocarpa as hypolipidemic agent. Claimed extract is obtained by double extraction with 95% ethanol, acidified with hydrochloric acid, at heating on water bath.

EFFECT: claimed invention ensures obtaining agent with expressed ability to reduce level of triacylglycerols, total cholesterol and cholesterol in atherogenic lipoproteins of low density in blood serum.

3 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: drops possessing antiviral and immunomodulatory effects characterised by the fact that they represent a 95% ethanol infusion of wild strawberry leaves and fruit specified in: red raspberry fruit, mountain ash fruit, bilberry fruit, blood-red hawthorn fruit, cinnamon rose fruit; 15-25 mg of the substance in 1 ml of the infusion.

EFFECT: drops possess pronounced antiviral and immunomodulatory effects.

15 tbl, 5 ex

FIELD: food industry.

SUBSTANCE: invention relates to a polyphenol grape extract, a compound for oral administration, a food product, beverage, a taste additive, a nutraceutical product, a revitalising composition and therapeutic remedy including the said grape extract. According to the invention, the grape extract contains nearly 5-15 wt % of monomers, nearly 5-20 wt % of dimers, nearly 3-10 wt % of trimers, nearly 2-10 wt % of tetramers and nearly 2-10 wt % of pentamers.

EFFECT: grape extract reduces blood pressure with patients suffering from prehypertonic condition or metabolic syndrome.

27 cl, 4 dwg, 8 tbl, 7 ex

FIELD: medicine.

SUBSTANCE: minor amputation of the foot with the further necrectomy is performed. After the application of an antimicrobial bandage and drainage, the wound is hermetised from the environment by the creation of a negative pressure above the wound in a combination with drug treatment. The reatment is performed in two steps. At the first step the wound with the antimicrobial bandage and drainage is first hermetised from above with an adhesive film, with the creation and support of the negative pressure not lower than 80 mm Hg. Urokinase 500000 U is additionally introduced daily intravenously by drop infusion per 100 ml of physiological solution, Vessel-Due-F in a dose of 600 LU per 100 ml of physiological solution and VAP 20 - alprostadil in a dose of 40 mcg per 100 ml of physiological solution. In addition Antistax in capsules is introduced to the patient. At the second stage active 24-hour vacuum aspiration with the change of the negative pressure from 10 to 80 mm Hg within a day is carried out. Additionally introduced is Vessel-Due-F in a dose of 1 capsule with 250 LU 2 times per day between meals and Antistax. At the first and second stages Antistax is introduced in a dose of 2 capsules in the morning 30-40 minutes before meal, daily. Duration of each stage constitutes not less than 7 days.

EFFECT: increase of the treatment efficiency due to the complete and timely purification of the wound from pathological exudates, elimination of the progression of the purulent-necrotic process, increase of the regenerative activity of tissues, activation of local immunity, recovery of microcirculation and oxygenation of the affected tissues.

2 cl, 2 ex

FIELD: chemistry.

SUBSTANCE: group of inventions relates to nanoparticles for encapsulating biologically active compounds. The nanoparticle contains a casein matrix, a basic amino acid and a metal selected from a group including a divalent metal, a trivalent metal and combinations thereof. Disclosed is a method of producing nanoparticles, which includes preparing an aqueous solution of a casein source and a basic amino acid and adding to the prepared solution an aqueous solution of a metal selected from a group including a divalent metal, a trivalent metal and combinations thereof to obtain a suspension containing formed nanoparticles. Another version of the method of producing nanoparticles includes mixing an aqueous solution of a casein source and a basic amino acid with a solution of a biologically active compound and adding to the obtained mixture an aqueous solution of a metal selected from the group to obtain a suspension containing formed nanoparticles. Nanoparticles obtained using said methods are used in combination with a carrier to prepare food products, as well as in pharmaceutics and cosmetics.

EFFECT: invention enables to obtain nanoparticles with high stability and low polydispersity.

40 cl, 17 dwg, 13 tbl, 11 ex

FIELD: chemistry.

SUBSTANCE: group of inventions relates to a two-phase mouth wash liquid and a method for use thereof. The disclosed two-phase mouth wash liquid contains a hydrophilic phase, a hydrophobic phase, a hydrotrope and a preservative, wherein the preservative contains (i) sodium benzoate and (ii) potassium sorbate and/or methylisothiazolinone (MIT), and the hydrotrope component contains glycerine and/or propylene glycol. The mouth wash liquid contains (a) 0.05-0.11 wt % sodium benzoate and (b) 0.05-0.2 wt % potassium sorbate and/or 0.0005-0.01 wt % MIT. The hydrophilic phase of the mouth wash liquid can additionally contain cetylpyridinium chloride in amount of 0.01-0.1 wt %, wherein the disclosed method of improving oral health includes using an effective amount of said liquid in the mouth of a subject to reduce the level of cariogenic bacteria.

EFFECT: use of said combination of preservatives coupled with said hydrotrope provides good resistance to microbial contamination without any adverse effect on taste properties or appearance of the mouth was liquid.

12 cl, 1 ex

FIELD: medicine.

SUBSTANCE: combined phyto- and physiotherapy is conducted. The phytotherapy involves administering Prolit Super 2 capsules two times a day (at 8 and 14 o'clock) for one month; the physiotherapy provides rectal electrical stimulation by means of AndroGyn for 8 minutes a day, 15 procedures in the therapeutic course.

EFFECT: invention enables improving the sexual function and prostatic microcirculation, and can be used in ambulance situation.

1 dwg, 1 ex

FIELD: medicine, oncology, amino acids.

SUBSTANCE: invention relates, in particular, to the development of an antitumor preparation based on natural substances. Invention relates to an amino acid preparation comprising at least one modified essential amino acid obtained by treatment of amino acid by ultraviolet radiation (UV) at wavelength 250-350 nm for 12-80 h at temperature 15-30oC or with ozone at temperature 15-25oC. The modified amino acid has no toxicity for health cells. Also, invention relates to a method for preparing such preparation. Invention provides the development of an antitumor preparation based on modified amino acids and expanded assortment of antitumor preparations being without cytotoxicity for normal cells.

EFFECT: valuable medicinal antitumor properties of preparation.

8 cl, 4 tbl, 2 dwg, 4 ex

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