Compositions for treating dental hypersensitivity

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions concerns oral care compositions effective for treating dental hypersensitivity, and a method of treating using them. The composition contains a compound of formula I: M1-A-M2-B-M1; wherein M1 and M3 represent potassium (K); M2 represents Ti or titanium (Ti) oxide; A and B independently represent C2-C6 dibasic acid; and at least one orally acceptable solvent. The oral care composition has pH falling within the range of 2.0 to 7.0. There are also presented a version of the composition, which contains at least one additional desensitising agent, and a method of treating sensitive teeth with the use of this composition.

EFFECT: using the group of inventions provides the effective dental desensitisation by creating a protective barrier on the tooth surface and/or sealing the effective dental tubules effectively.

11 cl, 8 tbl, 12 dwg

 

Deepak Sharma (Deepak Sharma)

Field of the INVENTION

The present invention relates to such compositions for the treatment of sensitive teeth, which have a relationship to the dentin and effectively seal open dentinal tubules.

Background of the INVENTION

Many people suffer from sensitive teeth, and this condition is often called increased dentinal sensitivity, which is a common problem among the adult population. It is defined as ongoing pain that occurs in the naked dentin, typically in response to chemical, thermal, tactile or osmotic stimuli that cannot be explained any other defects or diseases of the teeth. Erosion of the exposed surface (enamel) of the tooth and/or gingival recession often leads to exposure of dentinal tubules, creating lines of communication between the oral cavity and nerve fibers in the pulp. It has been shown in-vivo that the dentin has a gradient of pressure of liquid in the outward direction. Violation or increasing the current of fluid occurs in response to tactile, thermal (heat or cold) and osmotic stimuli (large amounts of sugar, etc.), and it is assumed, leads to the response of mechanoreceptors nerve fibers in the pulp, which is felt as pain. For the treatment of hypertonic� tooth sensitivity are used desensibilization nerves and substances occluding dentinal tubules. Special toothpastes containing potassium nitrate and/or biostable, amorphous calcium phosphate, etc., are regularly used by consumers suffering from increased dentinal sensitivity. Other occluding material that is also used to treat tooth sensitivity is potassium oxalate. However, none of these occluding substances is not completely effective to reduce dentinal sensitivity, since the effective blockage of the dentinal tubules is dependent on various variables. Thus, there remains a need for compositions for the treatment of sensitive teeth, which have high affinity to dentin and effectively sealed dentinal tubules.

BRIEF description of the INVENTION

It is established that the above-mentioned goal can be achieved by selecting special compounds that form a protective barrier for teeth and/or effectively clog Nude dentinal tubules, thereby reducing the sensitivity of the teeth. In some embodiments of the present invention proposed a composition for caring for the oral cavity that contains:

a) at least one compound of the formula I

M1-A-M2 -B-M3(I)

where: M1and M3represent independently a monovalent or divalent metal; M2- polyvalent metal or a metal oxide; A and B are independently selected from the group consisting of C2-C6dibasic, and tribasic chetyrehspalnyh acids;

(b) alternatively, flavoring;

c) alternatively, the sweetener;

(d) alternatively, a buffer of pH; and

e) at least one orally acceptable solvent,

moreover, the composition for caring for the oral cavity has a pH of greater than (or at least equal) to 2.0 (or about 2).

In other embodiments, the compositions of the present invention relate to compositions for caring for the oral cavity that contains:

a) at least one compound of the formula I

M1-A-M2-B-M3(I)

where: M1and M3represent independently a monovalent or divalent metal; M2- polyvalent metal or a metal oxide; A and B are independently selected from the group consisting of C2-C6dibasic, and tribasic chetyrehspalnyh acids; and

(b) at least one orally acceptable solvent,

the composition with almost no�holds water.

In other embodiments, the compositions of the present invention relate to compositions for caring for the oral cavity that contains:

a) at least one compound of the formula I

M1-A-M2-B-M3(I)

where: M1and M3represent independently a monovalent or divalent metal; M2- polyvalent metal or a metal oxide; A and B are independently selected from the group consisting of C2-C6dibasic, and tribasic chetyrehspalnyh acids;

(b) at least one additional desensibilization; and

c) at least one orally acceptable solvent.

In another embodiment of the compositions of the present invention relate to a method for treating sensitive teeth comprising at least two sequential use on sensitive teeth composition containing:

a) at least one compound of the formula I

M1-A-M2-B-M3(I)

where: M1and M3represent independently a monovalent or divalent metal; M2multivalent meth�ll or a metal oxide; A and B are independently selected from the group consisting of C2-C6dibasic, and tribasic chetyrehspalnyh acids; and

(b) at least one orally acceptable solvent,

moreover, the application should be made at intervals of not more than (or less than) 12 (or about 12 hours.

In other embodiments, the compositions of the present invention relate to a method of plugging dentinal tubules of teeth comprising at least two successive applying to the teeth a composition containing:

a) at least one compound of the formula I

M1-A-M2-B-M3(I)

where: M1and M3represent independently a monovalent or divalent metal; M2- polyvalent metal or a metal oxide; A and B are independently selected from the group consisting of C2-C6dibasic, and tribasic chetyrehspalnyh acids; and

(b) contacting the teeth with the composition for a period of at least (or longer than) 10 (or about 10) seconds

the tubules are plugged at least (or greater than) about 5%.

In other embodiments, the compositions of the present invention relate to a method of plugging dentinal ka�of alceu teeth comprising at least two sequential applying to the teeth a composition containing:

a) at least one compound of the formula I

M1-A-M2-B-M3(I)

where: M1and M3represent independently a monovalent or divalent metal; M2- polyvalent metal or a metal oxide; A and B are independently selected from the group consisting of C2-C6dibasic, and tribasic chetyrehspalnyh acids; and

(b) contacting the teeth with the composition in the presence of calcium for at least 20 seconds,

thus, the connection forms on the teeth or near the precipitate with calcium, such that at least (or greater than) 30% (or about 30%) of the formed precipitate remains on the teeth after dispersion with ultrasound for 2 (or about 2) minutes.

In other embodiments, the compositions of the present invention relate to a method for the deposition of precipitate on the teeth and/or dentinal tubules of teeth comprising at least two successive applying to the teeth a composition containing:

a) at least one compound of the formula I

M 1-A-M2-B-M3(I)

where: M1and M3represent independently a monovalent or divalent metal; M2polyvalent metal or a metal oxide; A and B are independently selected from the group consisting of C2-C6dibasic, and tribasic chetyrehspalnyh acids; and

(b) contacting the teeth with the composition in the presence of calcium for at least (or longer than) 20 (or about 20) seconds

where M2present in the precipitate at a concentration of at least (or greater than) 5% (or about 5%) of the deposited precipitate.

Brief description of figures

Fig.1 shows an image of the cut dentin treatment must be performed, using scanning electron microscope after 7 treatments with 0.5% composition of potassium oxalate and demonstrates a minimum precipitation of oxalate on the cut surface of the dentin and/or plugging dentinal tubules after treatment.

Fig.2 shows an image of the cut dentin treatment must be performed, using scanning electron microscope after 14 treatments with 0.5% composition of potassium oxalate and demonstrates a minimum precipitation of oxalate on the cut surface of the dentin and/or plugging dentinal tubules after treatment.

Fig.3 presents from�a reflection of the cut dentin treatment must be performed, using scanning electron microscope after 21 treatment with 0.5% composition of potassium oxalate and demonstrates a minimum precipitation of oxalate on the cut surface of the dentin and/or plugging dentinal tubules after treatment.

Fig.4 shows an image of the cut dentin treatment must be performed, using scanning electron microscope after 28 treatments with 0.5% composition of potassium oxalate and demonstrates a minimum precipitation of oxalate on the cut surface of the dentin and/or plugging dentinal tubules after treatment.

Fig.5 shows an image of the cut dentin treatment must be performed, using scanning electron microscope after 7 treatments with 0.5% composition of potassium oxalate, titanium oxide, indicating the strong precipitation of oxalate of titanium oxide on the cut surface of the dentin and/or virtually complete blockage of dentinal tubules after treatment.

Fig.6 shows an image of the cut dentin treatment must be performed, using scanning electron microscope after 14 treatments with 0.5% composition of potassium oxalate, titanium oxide, indicating the strong precipitation of oxalate of titanium oxide on the cut surface of the dentin and/or virtually complete blockage of dentinal tubules after treatment./p>

Fig.7 shows an image of the cut dentin treatment must be performed, using scanning electron microscope after 21 treatment with 0.5% composition of potassium oxalate, titanium oxide, indicating the strong precipitation of oxalate of titanium oxide on the cut surface of the dentin and/or virtually complete blockage of dentinal tubules after treatment.

Fig.8 shows an image of the cut dentin treatment must be performed, using scanning electron microscope after 28 treatments with 0.5% composition of potassium oxalate, titanium oxide, indicating the strong precipitation of oxalate of titanium oxide on the cut surface of the dentin and/or virtually complete blockage of dentinal tubules after treatment.

Fig.9 shows an image of the cut dentin treatment must be performed, using scanning electron microscope after treatment with a composition comprising the same ingredients that were used for the treatment of dentin slices in Fig.1-8, but with their no potassium oxalate or potassium oxalate, titanium oxide and there is no difference in the precipitation on the cut surface of the dentin and/or blockage of the dentinal tubules before and after treatment composition.

Fig.10 shows an image of the cut dentin treatment must be performed, obtained using scanning electron �of icroscope after 28 treatments composition includes the same ingredients that were used for the treatment of dentin slices in Fig.1-8, but with their no potassium oxalate or potassium oxalate, titanium oxide and there is no difference in the precipitation on the cut surface of the dentin and/or blockage of the dentinal tubules before and after treatment composition.

Fig.11 shows obtained by scanning electron microscope image of a cut dentin treatment must be performed, who has been 28 treatments composition containing 0.5% potassium oxalate (composition B), and then the dispersion with ultrasound for 2 minutes using an ultrasonic disperser under normal impulse.

Fig.12 presents obtained by scanning electron microscope image of a cut dentin treatment must be performed, who has been 28 treatments composition containing 0.5% potassium oxalate titanium oxide (composition D), and then the dispersion with ultrasound for 2 minutes using an ultrasonic disperser at normal pulse. Compare these images of the dentin slices in Fig.11 and 12 with the corresponding images after 28-day treatment shown in Fig.4 and 8, illustrate the increased stability of the precipitates formed by composition with potassium oxalate titanium oxide in comparison with compositional�her containing potassium oxalate.

Detailed description of the invention

The compositions according to the present invention can include, consist of, or consist primarily of essential elements and features of the invention described in this document and any additional or used for the selection of ingredients, components or features of the invention described herein.

All documents are fully incorporated herein by reference, is included only to the extent they do not conflict with these technical requirements.

All percentage concentrations, parts and ratios are based on total weight of the composition according to the present invention, if not specified. All these weight related to listed ingredients are based on the active level and, therefore, do not include carriers or by-products that may be included in commercially available materials, unless you specify otherwise.

The term "safe and effective dose" as used herein means that dose of a compound or composition of local or systemic action, sufficient to bring significant benefits, for example, to cause a reduction in tooth sensitivity, but low enough to avoid serious side effects, i.e. to provide a reasonable relationship �claim/benefit within the sound judgment of a specialist in this field.

The term "corked" or "clogging" as used herein means that the open holes in the dentinal tubules or openings in the dentinal tubules partially, substantially or completely closed.

The compositions of the present invention contain at least one compound of the formula I

M1-A-M2-B-M3(I)

where: M1and M3represent independently a monovalent or divalent metal; M2- polyvalent metal or the oxides of this metal; A and B are independently selected from the group consisting of a dibasic, tribasic and chetyrehspalnyh acid (C2-C6; alternatively, from dibasic and tribasic acids (C2-C4; alternatively, from dibasic and tribasic acids (C2-C3; or, alternatively, from a dibasic acid, C2.

Examples of suitable monovalent metals include, among others, Na, K and Li; alternatively, Na or K; or alternatively, K.

Examples of suitable divalent metals include, among others, Mg, Ca, Sr, Ba and Zn; Mg, Ba and Zn; or, alternatively, Mg.

Examples of suitable divalent metals include, among others, Ti, V, Cr, Mn, Fe, Co, Ni, Cu, Tc, Re, Os, Ir, Hg, Ce, Sn, Eu, Yb, Pa, and U; as �Ariant, Ti, Sn, Mn and Fe; or, alternatively, Ti.

Examples of suitable metal oxides include, among others, the corresponding oxides of Ba, Ti, V, Cr, Mn, Fe, Co, Ni, Cu, Tc, Re, Os, Ir, Hg, Ce, Sm, Eu, Yb, Pa, and U; as a variant, the corresponding oxides of Ba, Ti, Sr, Sn, Zr, Mn and Fe; alternatively, the corresponding oxides of Ba, Ti, Sr, Sn, Zr; or, alternatively, the corresponding Ti oxide.

In some embodiments, M1and/or M3independently selected from the group consisting of Na, K and Li. As an option, and M1and M3represent K.

In some embodiments, M2selected from the group consisting of Ti, Sr, Sn, Mg, Ca, Mn, and Zr. Alternatively, M2selected from the group consisting of oxides of Ti, Sr, Sn, Mg, Ca, Mn, and Zr. In other embodiments, M2selected from the group consisting of Ti or Ti oxide.

Examples of suitable dibasic acids include, among others, oxalic acid, succinic acid, methylethanol acid, diglycolic acid, glutaric (i.e. pentandiol) acid, 3,5,5-trimethylpentanediol acid, hexanediol acid, 3, 5,5-trimethylhexanoic acid, 2,4,4-trimethylhexane acid, decandiol acid, undecadienal acid, dodecadienol acid, 1,4-cyclohexanecarbonyl acid, cyclohexane-1,4-acetoacetic acid, maleic acid, Tarakanova acid, taconova acid, Shmarov�Yu acid, oxalic acid, terephthalic acid, phthalic acid and isophthalic acid, xiantao acid, malonic acid, adipic acid, sabotinova acid and tartaric acid, optionally, oxalic acid, succinic acid or oxalic acid.

Examples of suitable tribasic acids include, among others, citric acid.

Examples of suitable tribasic acids include, among others, 1,1,2,2-atinternational acid; 1,1,2,3-propanetricarboxylic acid; 1,1,4,4-butanetetracarboxylic acid; 1,2,4, 5-benzotriazolyl acid and ethylenediaminetetraacetic acid, or, alternatively, 1,1,2,2-atinternational acid.

In some embodiments, the compound of formula I is selected from the group consisting of potassium oxalate, titanium oxide (“WHO”) (also referred to as titanium oxalate, potassium), potassium citrate, titanium oxide, titanium-calcium oxalate and potassium calcium titanium oxalate, alternatively, potassium oxalate, titanium oxide (“WHO”), potassium citrate, titanium oxide or, alternatively, potassium oxalate, titanium oxide (“WHO”).

The compositions of the present invention include, based on the total weight of the composition, from 0.01% (or about 0.01%) to 10.0% (or about 10.0%); alternatively, from 0.1% (or about 0.1%) to 7.0% (or about 7.0%); or, alternatively, from 1% (or about 1%) to 5.0% (Il� about 5.0%) at least one compound of formula I.

In some embodiments, compositions comprise an orally acceptable solvent. Orally acceptable solvents include, among others, water; ethanol; n-propanol; or polyhydric alcohols such as glycerin, sorbitol and polyethylene glycol; and any mixtures thereof and can be present in concentrations from 0.1% to 99.9%; alternatively, from about 1% to about 90%; or alternatively from about 10% to 75% of the orally acceptable solvent.

In some other embodiments, the compositions according to the present invention substantially does not contain water. The term "substantially free" as used herein means a composition with a water content of less than 5% (or about 5%; alternatively, less than 3% (or 3%); alternatively, less than 1% (or about 1%); alternatively, less than 0.5% (or about 0.5%); as a variant - zero (or anhydrous).

In some embodiments, the compositions of the present invention have a pH value equal to at least 2 (or about 2); alternatively from 2.5 (or about 2.5) to 7.0 (or about 7.0); alternatively, ranging from 3.5 (or about 3.5) to 6.0 (or approximately 6.0); or, alternatively, from 3.2 (or about 3.2) to 4.5 (or about 4.5).

In some embodiments, the pH for the compositions of the present invention create (app is buffering) using traditional acid-salt systems. Usually�s buffer systems include phosphoric acid and phosphate salts, or citric acid and sodium citrate. Suitable for use in the present invention combinations of acids/acid salts include citric acid-sodium citrate, phosphoric acid-metafictionally sodium, primary sodium acid phosphate, secondary sodium acid phosphate, acetic acid-sodium acetate, succinic acid-sodium succinate, Aconitum acid-aconitate sodium and benzoic acid-benzoic acid sodium at doses up to about 1% weight percent; alternatively, from about 0.05 percent weight percent to 0.75% weight percent of the composition; and/or, optionally, about 0.1% percent by weight to 0.5% weight percent of the composition.

Additional components

In some embodiments, compositions according to the present invention further comprise other desensibilization that reduce the sensitivity of teeth. Examples of additional desensibilization include, among others, potassium citrate, potassium chloride, potassium nitrate, citric acid, salts of citric acid, strontium chloride, and mixtures thereof. Also suitable are biologically active glass materials described in U.S. patents 5735942; 5891233; 6086374; 6244871; 6338751; and 6365132, each of which in virtue of this reference is fully included in the present application, and phosphorus�peptides, described in the U.S. patents 5015628; 5981475; 6448374; and 6780844, each of which in virtue of this reference is fully included in the present application.

In some embodiments, additional desensibilization is potassium nitrate. In some embodiments, the additional concentration of desensitizer to reduce tooth sensitivity is 0.1% (or about 0.01%) to 10% (or about 10%); alternatively, from 0.1% (or about 0.1%) to 8% (or about 8%); or, alternatively, from 1% (or about 1%) to 7% (or about 7%) by weight of the composition.

The sources of fluoride ions are well known as anti-caries active substances in the compositions for the care of the oral cavity and may also be included in compositions according to the present invention. Fluoride ions are present for this purpose in a number of compositions for caring for the oral cavity, specifically, in toothpastes. Among the patents disclosing the use of such toothpastes include U.S. patents 3538230; 3689637; 3711604; 3911104; 3935306; and 4040858, each of which is entirely included in the present application by reference.

The application of fluoride ions to the tooth enamel protects the teeth against caries. As sources of soluble fluoride in the compositions of the instant action, you can use a wide range of materials containing fluoride ions. Examples of materials, soda�containing fluoride ions, described in U.S. patent No. 3535421 issued by Briner et al. October 20, 1970; and U.S. patent No. 3678154 issued to Widder et al. July 18, 1972, both patents are entirely incorporated in this application by reference. In some embodiments, sources of fluoride ions for the purposes of the present invention include dottorato tin, monitoringstate, sodium fluoride, potassium fluoride and ammonium fluoride. In other embodiments of included sodium fluoride. In some embodiments, the compositions of the present invention provide from about 50 to 10,000 ppm; alternatively, from about 100 to 3000 parts per million of fluoride ions in aqueous solutions that contact the surface of the teeth.

In the compositions of the present invention can also be used phosphates. Among the phosphates include pyrophosphates, polyphosphates, polyphosphonates and mixtures thereof. Pyrophosphates are among the products that are best known for use in dentistry. The ion source of pyrophosphato coming to teeth, are protostoria salt. Protostoria salts suitable for use in existing formulations include protostoria salt of di-alkali metal, protophormia salt tetralone metals and mixtures thereof. Dihydrogenphosphate dynatree (Na2H2P2O7), tetrasodium pyrophosphate (Na4 P2O7) and potassium pyrophosphate (K4P2O7in non hydrated and hydrated form are the preferred types of compounds. In some embodiments, the pyrophosphate salt is tetrasodium pyrophosphate.

Protostoria salts described in more detail in publications Kirk & Othmer, "encyclopedia of clinical technology", third edition, volume 17, Wiley-Interscience (1982), incorporated in this application in its entirety by reference along with all references included in the publication of Kirk & Othmer. Additional substances that prevent the formation of Tartar, include pyrophosphates or polyphosphates disclosed in U.S. patent 4590066; polyacrylates and other polycarboxylates, for example, disclosed in the U.S. patents 3429963; 4304766; and 4661341; polyepoxide the succinates (salt of succinic acid), for example, disclosed in U.S. patent 4846650; ethylenediaminetetraacetic acid, disclosed in British patent No. 490384 of 15 February 1937; nitrilotriacetic acid and related compounds disclosed in U.S. patent 3678154; polyphosphonate disclosed in the U.S. patents 3737533; 3988443; and 4877603; all of these patents are incorporated in this application in its entirety by reference. In some embodiments, the phosphates include pyrophosphates, potassium and sodium; sodium tripolyphosphate; difo�methanesulphonate, such as ethane-1-hydroxy-1,1-diphosphonate, 1-azacycloheptane-1,1-diphosphonate and linear alkilirovanny; tricalcium phosphate, linear carboxylic acids; sodium citrate zinc and mixtures of any of the above-mentioned phosphates. In some embodiments, the phosphate is tricalcium phosphate plus sodium lauryl sulfate, as described in application for U.S. patent 20080187500 A1, published August 7, 2008 Karlinsey, Robert L., and this publication is incorporated in this application in its entirety by reference.

Phosphates included in compositions according to the present invention, may be present in concentrations from about 0.01% to 10%; alternatively, from about 0.1% to 7%; and, optionally, from about 0.5% to 5%.

In some embodiments, the compositions of the present invention include essential oils. Essential oils are volatile aromatic oils that are synthetic or derived from plants by distillation, extraction or extraction. Essential oils usually pass the smell or flavor of the plant from which they are derived. When used in a composition means for brushing your teeth according to the present invention the essential oils have protivovirusnym action. Some essential oils also act as flavoring agents. Essential oils according to the present �the turbine zobretenie include, among others, thymol, menthol, methyl salicylate (wintergrove oil) and eucalyptol.

Thymol, with the chemical formula 5-methyl 2-(1-methylethyl) phenol, is obtained from the essential oil of Thymus vulgaris Labiatae and Monarda punctata Labiatae. Thymol is a white crystalline powder with an aromatic odor and taste. Thymol is soluble in organic solvents but only slightly soluble in deionized water.

Menthol is isolated mainly from Mentha arvensis oil. In commercial form menthol is available in the form of crystals of L-menthol, obtained with the help of the technological process, including the cooling oil. Fractional distillation of mint oil, which typically contains from about 40% to 65% of menthol, represents another important source of menthol. Also available synthetic sources of L-menthol.

Eucalyptol obtained from a eucalyptus tree. With camphor smell and cooling taste, this essential oil is then combined with other essential oils such as menthol, in the composition of medicinal substances with a sweet filler for the purpose of giving the latter treatment modality. The combination of menthol with eucalyptol widely used. Specifically, preferred embodiments utilize a combination of menthol with eucalyptol include according to the present invention for cleaning teeth, such as dental �asty or gels.

Methyl salicylate is the main ingredient in many essential oils, constituting about 99% of oil in Wintergreen (Gaultheria procumbens) and birch globalistas (Betula lenta). Methyl salicylate, which has a characteristic refreshing flavor, is widely used in liquids for mouth rinses, chewing gums and other oral and pharmaceuticals.

Doses of essential oils that can be used in the compositions according to the present invention comprise from 0.001 (or about 0.001) to 1% (or about 1%) of thymol, of 0.001 (or about 0.001) to 1% (or about 1%) methyl salicylate, 0,001 (or about 0.001) to 15% (or 15%) of menthol and 0.001 (or about 0.001) to 1% (or about 1%), eucalyptol, and these doses have clinical efficacy, necessary for suppression of gingivitis. As a variant, the composition according to the present invention contains about of 0.064% thymol, about is 0.060% methyl salicylate, about 0,042% menthol and about 0.092% eucalyptol, and these doses have clinical efficacy required to suppress gingivitis.

Alternatively, or in addition to essential oils of the composition according to the present invention can also include having antimicrobial efficacy of a substance selected from the group consisting of polyphenols (e.g., triclosan), zinc salts, tin fluoride, chlorhexidine�and, the hexetidine treatment, sanginario, benzalkonium chloride, salicylanilide, domiphen bromide, cetylpyridinium chloride, tetraterpene chloride (TPC), N-tetradecyl-4-ethylpyridine chloride (TDEPC), octenidine, delmopinol, Octafinal and other piperidine derivatives, preparations lowland, ionic substances zinc/tin, antibiotics such as Augmentin, amoxicillin, tetracycline, doxycycline, minocycline and metronidazole, and analogues and salts of these substances, essential oils including eugenol, geraniol, carvacrol, citral, hinokitiol, catechin, hydrogen peroxide, salts of chlorite metals or any combination of all of these substances.

Can also be used a mixture of any of the above substances.

The compositions according to the present invention can also contain a surfactant selected from anionic, nonionic, amphoteric, betaine, cationic surfactants and mixtures thereof. Suitable anionic surfactants include alkylsulfate, alkylamine sulfates, sulfosuccinates, isetionate, acylamide, alcelaphinae the carboxylates and alkyl phosphates in which the alkyl group has from 6 to 30 carbon atoms. Suitable cationic surfactants include cetylpyridinium chloride. The total dose of surfactant (s), which are suitable for use in compositions according to the present invention, can include, based on the total weight of all composite�, from about 1% to 50%; alternatively, from about 5% to 40%; or alternatively, from about 8% to 25%.

Types of nonionic surfactants that are suitable for use in the present invention include acid or etexilate amides, ethoxylate of monoglycerides, ethoxylate ether of sorbitol fatty alcohols and alkyl polyglycoside. These nonionic surfactants can be used in the compositions according to the present invention in doses based on the total weight of the composition, from about 0.0% to 30%, for example from about 0.1% to 20% and from 0.1% to 15%.

Classes of amphoteric surfactants that are suitable for use in the present invention include alkylenediamines, alcelaphinae (mono - or di-), alkylamidoamines (mono - or di-), alkylamidoamines (mono - or di-), N-alkyl-β-aminopropionic acid, alkylaminocarbonyl and the phosphorylated imidazoline. These amphoteric surfactants can be used in the compositions of the present invention in doses based on the total weight of the composition, from about 0.1% to 20%, for example from about 0.1% to 15% and from 0.1% to 10%.

Types of betinov, which are suitable for use in the present invention include alkylbetaine, alkylamidoamines, alkylsulfanyl and alkylimidazole in which the alkyl group has from 6 to 30 atoms coal�ode, this is the preferred number of carbon atoms from 10 to 14. These betamovie surfactants can be used in the compositions of the present invention in doses based on the total weight of the cleaning composition, from about 0.1% to 15%, for example from about 0.1% to 10% and from 0.1% to 8%.

Classes of cationic surfactants that are suitable for use in the present invention include alkyl Quaternary compounds (mono-, di - or tri-), benzyl Quaternary compounds (e.g., cetylpyridinium chloride), Quaternary ether compounds, ethoxylated Quaternary compounds, alkyl amines and mixtures thereof in which the alkyl group has from 6 to 30 carbon atoms, with the preferred number of carbon atoms from 8 to 22. These cationic surfactants can be used in the compositions of the present invention in doses based on the total weight of the cleaning composition, from about 0.01% to 20%, for example from about 0.05% to 15% and from 0.1% to 10%.

The compositions according to the present invention may also include one or more additional ingredients, including, non-exclusively, thickening agent, humectants, chelating agents, and additives such as flavorings, preservatives and the like.

Commercially available thickening agents, which are able to give the appropriate visco�th compositions suitable for use in the present invention. Non-exclusive examples of suitable thickening agents include: mono - or dietery 1) of polyethylene glycol according to the formula: HO-(CH2CH2O)zH, where z is an integer from 3 to 200; and 2) fatty acids containing from 16 to 22 carbon atoms; fatty acid esters of ethoxylated polyols; ethoxylated derivatives of mono - and diapirov fatty acids and glycerol; hydroxyethylcellulose; alkylaryl; hydroxyalkyl-alkylaryl; and mixtures thereof. Among the preferred thickening agents include the ether of polyethylene glycol and, more preferably, distearate PEG-150, which can be purchased in the company Stepan Company, Northfield, Illinois, or in the company Comiel, S. p.A. Bologna, Italy, under the trade name “PEG 6000 DS”.

In some embodiments, the thickeners can be included in compositions according to the present invention at concentrations of from about 0.01% to 10%, alternatively from 0.1 to 5%, or alternatively from 0.2% to 2.0%.

Commercially available humectants suitable for use in the present invention because of its moisturizing properties, in addition to the use as potential solvents, as noted above. The humectant may be present in amounts from about 0% to 10%, preferably from 0.5% to 5%, more preferred�Stateline, from 0.5% to 3%, based on the total weight of the composition. Non-exclusive examples of suitable humectants include: 1) water soluble liquid polyols selected from the group consisting of glycerin, propylene glycol, hexyleneglycol, butyleneglycol, dipropyleneglycol and mixtures thereof; 2) the pag by the formula: HO-(R”O)b-H, where R” is alkylenes group with 2-3 carbon atoms and b is an integer in the range from 2 to 10; 3) polyethylene glycol ether of methylglucose by the formula CH3-C6H10O5-(OCH2CH2)c-OH, where c is an integer in the range from 5 to 25; 4) urea; and 5) mixtures thereof, with glycerine being the preferred humectant.

In some embodiments, the humectants can be included in compositions according to the present invention at concentrations from about 0.1% to 40%, alternatively from 1.0 to 30%, or alternatively from 5% to 25%.

In some embodiments, the chelating agents can be included in compositions of the present invention. Examples of suitable chelating agents include those agents that are able to protect and preserve the compositions of the present invention. As an option, in addition to potential use as chetyrehosnuju acid in the compound (s) of formula I, ethylenediaminetetraacetic acid (“EDB�”) can be used as a chelating agent. In some embodiments, the chelating agent is tetranitro EDTA, commercially available Dow Chemical Company, Midland, Michigan, under the trade name “Versene 100XL”, which may be present in amounts, based on the total weight of the composition, is from about 0 to 0.5%; and, optionally, from 0.05% to 0.25%.

Suitable preservatives include benzoic acid sodium and Polysorbate and are present in the composition in an amount, based on the total weight of the composition may range from about 0 to 0.2% and preferably from 0.05% to 0.10%.

The compositions of the present invention can be in the form of liquids and means for rinsing the mouth, cleaning teeth, pastes, such as toothpastes, powders, such as dentifrices, gels, pills, medicinal lozenges, microcapsules, sprays, lacquers or strips (such as remineralizers strips disclosed in the publication of U.S. patent 20070128130 Kropt et al., published June 7, 2007, which is hereby incorporated into the present application in its entirety by reference, either peroxide or superoxide strips for teeth whitening, as disclosed in the publication of U.S. patent 20080003248 Georgiades et al., published January 3, 2008, and in U.S. patent 6949240 issued WEBERS et al. September 27, 2005, both of which patent are incorporated into the present application in its entirety �through the links) coatings for such strips and the like. Speaking of the above listed funds, the compositions of the present invention can also be applied using conventional devices to care for the oral cavity, including toothbrushes, floss, interdental floss, dental spray guns or sprayers and dental syringe pen, described in the publication of U.S. patent 20080044363, Montgomery, issued February 21, 2008, which is hereby incorporated into the present application in its entirety by reference.

The compositions of the present invention may also be suitable as a coating or as impregnating substances for impregnation dental devices selected from the group consisting of toothbrushes (manual or mechanical), the bristles of the toothbrush, interdental thread, toothpicks and the like. The compositions of the present invention may also be useful as coatings or impregnating substances for dental composite materials, dental fillings and the like.

The method of use of compositions of the present invention

The invention illustratively disclosed herein, can be applied in the absence of any component, ingredient, or step which is not disclosed here, specifically.

In some embodiments, the compositions of the present invention are applied to sensitive teeth with �on at least two sequential applications; as a variant, with at least (or greater than) and 7 (or about 7) consecutive applications; or, alternatively, 14 (or nearly 14) consecutive applications; or, alternatively, 21 (or about 21) consecutive applications; or, alternatively, 28 (or about 28) consecutive applications.

When applied to the sensitive tooth (or teeth) in some embodiments, the composition is left in contact with sensitive teeth for a period of at least (or longer than) 10 (or about 10) seconds; alternatively, 20 (or about 20) seconds; alternatively, 30 (or about 30) seconds; alternatively, 50 (or about 50) seconds; or 60 (or about 60) seconds.

In some embodiments, the time interval between consecutive applications should be no more than (or less than) 12 (or about 12 hours; alternatively, 8 (or about 8) hours; alternatively, a 4 (or about 4) hours; alternatively, a 2 (or about 2) hours or, alternatively, one (or near one) hour.

In some embodiments, the compositions of the present invention is applied to sensitive teeth so that the compounds of formula I form on the teeth the deposition of precipitates containing calcium, such that at least (or greater than) 5% (or about 5%) of the dentinal tubules of the teeth occluded; alternatively, 25% (or about 25%) of the dentinal tubules occluded; in�stage configuration, 40% (or 40%) of the dentinal tubules occluded; alternatively, 60% (or about 60%) of the dentinal tubules occluded; alternatively, 75% (or about 75%) of the dentinal tubules occluded; 85% (or 85%) of the dentinal tubules occluded; 95% (or 95%) of the dentinal tubules occluded.

In some embodiments, M2formula I is present in the deposition of precipitate formed by the compound (s) of formula I and calcium in a concentration of at least (or greater than) 5% (or about 5%); 10% (or about 10%), alternatively, 20% (or 20%); or, alternatively, 35% (or about 35%).

After the formation of the teeth is provided such stability adjournment (s) precipitate containing the compound of formula I and calcium that at least (or greater than) 5% (or about 5%); 30% (or about 30%); 35% (or 35%); alternatively, 50% (or 50%); 75% (or 75%); or, alternatively, 90% (or about 90%) remains on the teeth after ultrasonic treatment for 2 (or about 2) minutes using ultrasonic sonicator CD-4800 digital ultrasonic cleaner [CD-4800] produced by Best And More Electronics [Shenzhen] Co., Ltd., China) at the normal pulse frequency of about 42 kHz. At this frequency, sonicator usually provides more force, �eat in normal use, ultrasonic or manual toothbrushes. The phrase “deposition of (I) precipitates" as used herein means the deposition, which is formed on the teeth and/or clog the tubules of the teeth by precipitation of the compound (s) of formula I with calcium present in the fluids of the oral cavity after application of compositions containing compound (I) of formula I, as disclosed in the present application. To initiate or facilitate the formation of deposits (th) precipitates with compound (s) of formula I may also separate the addition of calcium in the oral cavity in the form of water soluble salts of calcium before or after the addition of the compositions of the present invention containing compound (I) of formula I. Examples of water-soluble calcium salts include, among others, calcium chloride, calcium nitrate, calcium bromide, dihydrogenphosphate calcium and mixtures thereof. The amount of water-soluble calcium salts must exceed, in molar proportions, the amount of compound (s) of formula I contained in the compositions of the present invention.

Below are some examples to further illustrate the invention and the method of its realization.

Examples

The compositions of the present invention described in following examples illustrate specific examples of application in practice of the compositions of the present invention, but are not limited to these examples. Other Modific�tion can be performed by a person skilled in the art without departing from the scope of the present invention and a retreat from its essence.

Preparation of the compositions of funds for mouthwash

Compositions were prepared liquid funds mouthwash, and evaluated the effectiveness of clogging the dentin compositions based on potassium oxalate, titanium oxide (KTO). The method of preparation is described as follows.

In a container for the preparation of the composition was added and mixed until dissolved water, KTO, benzoic acid and poloxamer. After dissolution poloxamer added alcohol, n-propanol, sorbitol, water and benzoic acid sodium, then mixing them to dissolve. Checked the pH and found it to be equal to 4.2.

To this mixture was added menthol, thymol, eucalyptol, methyl salicylate, mixing until a homogeneous condition. After a homogeneous solution was added sodium saccharin and FDC green No. 3 (1% solution, adjustable according to the degree of purity). Drug composition was mixed until uniform. The final pH of the composition was equal to 4.2.

The composition of the liquid formulations of funds mouthwash are presented in table 1.

Table 1
IngredientABCD% weight percentage% weight percentage% weight percentage% weight percentage% weight percentage
Alcohol USP22,65322,65322,65322,65322,653
Menthol USP0,0320,0320,0320,0320,032
Thymol NF0,0640,0640,0640,0640,064
Methyl salicylate NF0,0660,0660,0660,0660,066
Eucalyptol USP0,0920,0920,0920,0920,092
n-Propanol0,500 0,5000,5000,5000,500
Mint flavor N & A0,0850,0850,0850,0850,085
Poloxamer 4070,2500,2500,2500,2500,250
Benzoic acid, USP0,1200,1200,1200,1200,120
Benzoic acid sodium0,0350,0350,0350,0350,035
Potassium oxalate (KO)0,1000,50,0000,0000,000
Potassium oxalate, titanium oxide (KTO)0,0000,0000,100 0,5000,000
Saccharin sodium USP0,1170,1170,1170,1170,117
FD&C green No. 30,0010,0010,0010,0010,001
The sorbitol solution USP20,00020,00020,00020,00020,000
Distilled water, USP55,88555,48555,88555,48555,985
Total100,000100,000100,000100,000100,000
pH4,24,24,24,24,2

Preparation of samples of dentin and the claim�stvennoi saliva

The efficiency of trapping of dentin compounds and compositions based on the KTO was demonstrated as follows.

The dentin slices (polished and untreated) were obtained from Dental product testing, unit Thermametric technologies Inc., Indianapolis, Indiana, USA. The dentin slices were protravlivanie for complete removal of smear layer (or a layer of sawdust formed by the cutting of the dentin or enamel) by soaking slices of dentin in 6% citric acid during the time interval to 2 minutes and then were rinsed and subjected to sonication in deionized water.

Potassium oxalate (KO) was obtained from the company Fluka, St. Louis, Missouri (part number: 430462/1). Potassium oxalate, titanium oxide (KTO) dehydrate were obtained from Sigma, St. Louis, Missouri (batch No. 51740).

Artificial saliva was prepared using the traditional equipment and protocols used in the laboratory according to a conventional method and had a composition shown in Table 2.

Table 2
IngredientConcentration
Sodium chloride0,381 g/l
Dehydrate Chloe�East calcium 0,213 g/l
Primary acid phosphate potassium0,738 g/l
Potassium chloride1,114 g/l
Gastric mucus2.20 g/l
pH 7,0

Control and analysis of method comparison

All samples of the etched dentin slices (total of 10) were arranged in random order and divided into five treatment groups. In order to control blockage of tubules and surface deposition under the action of the compositions KTO were performed scanning electron microscopy (SEM) and chemical analysis of surfaces using electronic dispersion spectroscopy (EDS). Five treatment groups included:

Group 1: treatment with composition A

Group 2: treatment with composition B

Group 3: treatment with composition C

Group 4: treatment with composition D

Group 5: treatment with composition E (i.e. not KTO and not KO)

The processing scheme for groups 1-5 were as follows.

1. Processing samples of slices in each group with 20 ml of the appropriate therapeutic compositions with shaking for 30 seconds.

2. Rinsing samples of slices in each group using deionized H2O within 1 minute.

3. Dip samples of slices in artificial saliva between treatments, and a day was made not more than two treatments.

4. Repeat steps 1-3 until you run 28 treatments.

5. The dentin samples were analyzed using SEM and/or EDS after 7, 14, 21 and 28 treatments. Before analysis the sections were rinsed with deionized H2O for 3 minutes and subjected to air drying for analysis by SEM.

Data obtained by analysis of EMF for 2 samples of slices (slice 1 and slice 2), are summarized in tables 3 and 4 below.

B
Table 3
EMF after 7 treatments
CompositionS (%)K (%)P (%)Ca (%)Ti (%)
ASlice 139,05,412,543,1x
Slice 237,96,213,542,4x
Slice 116,99,317,256,6x
Slice 217,79,718,054,6x
CSlice 15,712,021,734,626,0
Slice 24,612,419,635,228,2
DSlice 1x11,628,028,332,1
Slice 2x12,525,7a 33.328,5
ESlice 148,2x of 13.038,8x
Slice 247,7x13,239,1x

the 15.4
Table 4
EMF after 14 treatments
CompositionS (%)K (%)P (%)Ca (%)Ti (%)
ASlice 130,68,412,548,5x
Slice 229,59,011,350,2x
BSlice 16,813,516,060,5x
Slice 28,718,457,5x
CSlice 11,810,2to 27.426,326,7
Slice 22,111,729,425,828,4
DSlice 1x18,722,126,432,8
Slice 2x20,917,730,0of 31.4
ESlice 147,5x13,638,9x
Slice 248,1x12,739,2x

After 7 treatments the samples treated with 0.5% KTO (composition D) demonstrate the highest degree of affinity to the etched dentin surface, as is evident from the decrease of the percentage of sulphur found in the EMF readings (usually EDS spectra etched surfaces of dentin contain about 45-50% sulfur). The percentage detected reduced sulfur as sulfur on the cut surface of the dentin is covered or masked by deposition on the surface that occur after treatment with composition KTO. Although sulfur is not completely absent, its percentage decreases dramatically in the sample treated with 0.1% KTO (composition C). After 14 treatments, the percentage of detected sulfur remains low in the sample treated with 0.5% KTO (composition D), and decreased more significantly in the sample treated with 0.1% KTO (composition C).

Scanning electron microscopy performed on these samples indicate the beginning or the formation of surface precipitation on the surface of the dentin samples treated with composition D, the degree of blockage of tubules increases with the number of treatments.

To obtain semi-quantitative comparison of the effectiveness of blockage of the dentinal tubules of different compositions were analyzed EMF, image classification and races�et blockage of tubules in percent. Methods and calculations for data analysis EMF, image classification and receive a percentage of occluded tubules were performed in accordance with methods described in the work of the West NX, Addy M, Hughes, J. (1998) J. Oral Rehabil, 25, 885 and confirmed by the methods described in the work of Lee SY, Kwon HK, Kim BI (2008) J. Oral Rehabil, 35, 847. Based on the above analysis of the EDS data, the percentage of occluded tubules was determined for compositions A-E at 7, 14, 21 and 28 treatments and are summarized in table 5.

Table 5
The percentage of occluded tubules
Composition7 treatments14 treatments21 treatments28 treatments
A5%15%25%40%
B20%35%45%60%
C25%35%55%75%
D 40%65%85%>99%
E0%5%5%5%

Comparing the analyzed data to Miroshnikov obtained before and after treatment using scanning electron microscopy at various time points of the processing cycle and at different concentrations KTO (as shown in table 5 and Fig.1-4 (processing KO), 5-8 (processing KTO) and 9-10 (treatment without oxalate)), clearly demonstrates the increased surface precipitation leading to increased blockage of tubules and increase its efficiency.

Definition of substantively for deposits formed precipitates

To determine substantively (or the ability of the precipitate to remain on the surface of the dentin) precipitate KTO deposited on samples of dentine slices in the loop processing, the following tasks have been completed. Slices of dentin treated with composition B (0,5% KO) and composition (D (0,5% KTO), after 28 treatments were subjected to dispersion with ultrasound for 2 minutes (the time may be about 2 minutes) using ultrasonic sonicator CD-4800 with normal heart rate (about 42 kHz). Comparing images processed sonic�Orom slices (Fig.11 and 12) with the corresponding images after 28-day treatment, shown in Fig.4 and 8, demonstrates that the deposition of precipitates obtained by KTO, proved to be more resistant to sonication (about 92% of the precipitate obtained by KTO, remained on the sample cutoff) than the precipitates obtained by KO (about 38% of the precipitate obtained by KO, remained on the sample slice), indicating that the deposition of precipitates obtained by KTO, provide enhanced stability in comparison with the deposits of precipitates obtained by KO. In the absence of theoretical restrictions can be assumed that this improved the stability of the deposits of precipitates formed by the compounds of formula I, not only provides an increased degree of reduction of tooth sensitivity, but longer duration of the effect.

In tables 6 and 7 shows examples of F-O illustrating additional examples of liquids for rinsing of a mouth on the basis of the compositions of the present invention. Examples F-O can be prepared using the methods described above for examples A-E.

Table 6
FGHI J
% weight percentage% weight percentage% weight percentage% weight percentage% weight percentage
Alcohol USP22,65322,65322,65322,65322,653
Menthol USP0,0320,0320,0320,0320,032
Thymol NF0,0640,0640,0640,0640,064
Methyl salicylate NF0,0660,0660,0660,0660,066
Eucalyptol USP0,0920,0920,0920,0920,092
n-Propanol0,500 0,5000,5000,5000,500
Mint flavor N & A0,0850,0850,0850,0850,085
Poloxamer 4070,2500,2500,2500,2500,250
Benzoic acid, USP0,1200,1200,1200,1200,120
Sodium benzoate0,0350,0350,0350,0350,035
Potassium citrate, titanium oxide0,1000,5---
Titanium-calcium oxalate--0,1000,500-
Potassium oxalate, titanium oxide2,00
Saccharin sodium USP0,1170,1170,1170,1170,117
FD&C green No. 30,0010,0010,0010,0010,001
The sorbitol solution USP20,00020,00020,00020,00020,000
Distilled water USP55,88555,48555,88555,48553,485
Total100,00100,00100,00100,00100,000
pH4,2 4,24,24,2

Table 7
KLMNO
% weight percentage% weight percentage% weight percentage% weight percentage% weight percentage
Alcohol USP22,65322,65322,65322,65322,653
Menthol USP0,0320,0320,0320,0320,032
Thymol NF0,0640,0640,0640,0640,064
Methyl salicylate NF0,0660,0660,0660,066
Eucalyptol USP0,0920,0920,0920,0920,092
Mint flavor N & A0,0850,0850,0850,0850,085
Poloxamer 4070,2500,2500,2500,2500,250
Benzoic acid, USP0,1200,1200,1200,1200,120
Sodium benzoate0,0350,0350,0350,0350,035
Potassium oxalate, titanium oxide0,1000,5000,51,0 2,0
Nitrate potassium2,42,43,03,03,0
Saccharin sodium USP0,1170,1170,1170,1170,117
FD&C green No. 30,0010,0010,0010,0010,001
The sorbitol solution USP20,00020,00020,00020,00020,000
Distilled water, USP53,21052,81052,21052,71051,710
Total100,00100,00100,00100,00100,000
pH4,2 4,24,24,24,2

Table 8 shows examples of P-S illustrating examples of means for cleaning teeth on the basis of the compositions of the present invention. Examples of P-S can be prepared using conventional mixing technology tools for cleaning teeth. Example S illustrates the anhydrous dentifrice as variant implementation of the present invention.

Table 8
IngredientsPQRS
(weight percent %)(weight percent %)(weight percent %)(weight percent %)
Water15,0012,5010,00---
99.7% glycerin, USP23,0023,0023,0028,00
Carboxymethylcellulose sodium0,600,600,600,60
Sorbitol (70%)24,9624,9624,9629,96
Saccharin sodium0,200,200,200,20
Sucralose0,800,800,800,80
Sodium fluoride0,240,240,240,24
The silicon hydroxide20,0020,0020,0020,00
Nitrate potassium0,005,005,005,00
The titanium oxalate, potassium (KTO)5,002,505,00 5,00
Synthetic amorphous silicon dioxide6,506,506,506,50
Lauroylsarcosinate sodium1,001,001,001,00
Lauryl glucoside1,001,001,001,00
Cocamidopropylbetaine0,500,500,500,50
Flavoring1,201,201,201,20
Total100,00100,00100,00100,00

1. Composition for caring for the oral cavity that contains:
a) at least one compound of the formula I
M1-A-M2-B-M3(I)
where: M1and M3are potassium (K); M2represents Ti or titanium oxide (Ti); A and B represent Soboh� independently C 2-C6dibasic acid; and
(b) at least one orally acceptable solvent;
where the composition is to care for the oral cavity has a pH in the range from 2.0 to 7.0.

2. A composition according to claim 1, wherein the compound of formula I is potassium oxalate, titanium oxide.

3. A composition according to claim 1, further comprising a buffer pH.

4. A composition according to claim 3, wherein the buffer pH is a combination of acid and acid salt selected from the group consisting of citric acid-sodium citrate, phosphoric acid-metaphosphoric sodium, the primary acidic sodium phosphate, secondary acidic sodium phosphate, acetic acid-sodium acetate, succinic acid-sodium succinate sodium, amanitowoc acid-aconitate sodium and benzoic acid-benzoic acid sodium.

5. A composition according to claim 1, further comprising a flavoring.

6. A composition according to claim 1, further comprising a sweetener.

7. A composition according to claim 1, wherein the composition is in the form of liquid or rinses mouth for cleaning teeth, paste, powder, gel, tablets, medicinal lozenges, microcapsules, strips or coatings of the strip.

8. A composition according to claim 1, wherein the composition is a coating or impregnating substance for dental devices selected from the group consisting of toothbrushes, the bristles subnoise, interdental filaments and toothpicks.

9. Composition for caring for the oral cavity that contains:
a) at least one compound of the formula I
M1-A-M2-B-M3(I)
where: M1and M3are potassium (K); M2represents Ti or titanium oxide (Ti); A and B independently represent C2-C6dibasic acid;
(b) at least one additional desensibilization; and
c) at least one orally acceptable solvent.

10. A composition according to claim 9, where the additional desensibilization selected from the group consisting of potassium citrate, potassium chloride, potassium nitrate, citric acid, salts of citric acid, chloride of strontium, bioactive glass materials, phosphopeptides and mixtures thereof.

11. A method of treating sensitive teeth comprising the step of contacting sensitive teeth with a composition for caring for the oral cavity according to claim 9 for at least 10 seconds.



 

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FIELD: chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely to novel pyridine derivatives of the general formula

and to their pharmaceutically acceptable salts, where R1 stands for (C1-6) alkyloxy, CN or halogen, R2 stands for a hydrogen atom, R3 stands for a hydrogen atom or (C1-6) alkyl, R4, R5, R6, R7 are similar or different and stand for a hydrogen atom or halogen. The invention also relates to the cosmetic application of the formula (I) compound.

EFFECT: novel pyridine derivatives, useful in the treatment of diseases associated with a receptor of androgens, are obtained.

9 cl, 1 tbl, 16 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to health-promoting compositions and methods for preparing them. A method for preparing the composition of non-living lactic acid bacilli, possessing an ability of specific binding to Streptococcus mutans, involves the following stages: heating a cell suspension of lactic acid bacillus or a mixture of lactic acid bacilli possessing an ability of specific binding to Streptococcus mutans from an initial temperature of less than 40°C to a pasteurisation temperature of 75 to 85°C with a temperature variation within the range of 0.5 to 2°C/min, keeping the heated suspension at a pasteurisation temperature of 20 to 40 minutes and cooling the suspension to a final temperature of less than 40°C within the range of 0.5 to 2°C/min. The specific binding the cell suspension of the lactic acid bacillus or the mixture of lactic acid bacilli to Streptococcus mutans is stable to heat treatment and/or resistant to proteases and/or calcium-dependent and/or is observed within the range of pH values falling within the range of 4.5 and 8.5, and/or in the saliva environment.

EFFECT: invention enables producing the agent preventing or delaying the caries lesion formation.

9 cl, 4 ex

FIELD: medicine.

SUBSTANCE: 0.5% dihydroquercetin is instilled into the rectum of a patient with temporary colostomy until he/she starts feeling intestinal inflation. The procedure is performed twice a day, daily up until the restorative surgery.

EFFECT: method reduces a rate and a degree of colitis manifestations by the local antioxidant, anti-inflammatory effect, unfolding the excluded colon.

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetic industry and represents a cosmetic product which has the following composition in each specific case calculated using the total composition: at least 0.1 wt % of at least one hydrophilic softening product, 2 to 40 wt % of at least one surfactant specified in a group of fatty alcohol ethoxylates, fatty alcohol ether sulphates and salts of sulphated and/or sulphonated fatty acids, 30 to 90 wt % of water, 1 to 30 wt % of one or more abrasives with the total ingredients making 10%; the product contains at least 0.1 wt % of at least one hydrophilic softening product with a hydrophilic-lipophilic balance ≥8 and flour thermally treated by saturated vapour; the flour is natural flour of shell or kernels characterized by a light absorption at wave length 660 nm of less than 1 prepared by reacting the flour 1 g with a solution prepared of water 10 ml and 0.1% aqueous methylene blue 1 ml.

EFFECT: invention provides the lower effect on viscosity, possesses the high cleaning action and high tolerability.

16 cl, 5 ex, 3 tbl

Foaming detergent // 2543713

FIELD: chemistry.

SUBSTANCE: invention relates to aqueous foaming composition for hands, containing castor oil maleate in amount from 0.1 to 1% of composition weight, PEG-7 glyceryl cocoate in amount from 0.05 to 0.3% of composition weight, glycerol in amount from 0.5 to 6% of composition weight, PEG-6 of glycerides of caprylic/capric acid in amount from 0.05 to 1% of composition weight and SAS. Glycerol is present in amount greater than amount of castor oil maleate or glyceryl cocoate PEG-7, and said composition has viscosity from 1 to 100 mPa·s (sP).

EFFECT: obtaining aqueous foaming composition for hands, which is capable of providing foam stability, has lower tendency for flowing and soiling when applied and creates more pleasant sensations for skin.

7 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to oral care compositions containing a basic amino acid or its salt. The presented oral care composition promoting the dentine defect closure in the oral cavity contains arginine in the free form or in the form of a salt, and an abrasive substance representing synthetic amorphous silica and containing small particle fractures making at least approximately 5% of total weight of the composition, wherein the particles of the small particle fracture having d50 from 3 to 4 mcm. What is also presented is a method of treating sensitive teeth in the oral cavity involving using the oral treatment with this composition, as well as using arginine as a part of the oral care composition and for producing a therapeutic agent, wherein the above composition and agent contain the above abrasive material containing the small particle fracture.

EFFECT: group of inventions provide the effective dentin defect closure in the patient's oral cavity.

8 cl, 1 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing technetium-99m labelled nanocolloid for radionuclide diagnosis. The disclosed method includes preparing a starting suspension of a nanocolloid in 0.1% sodium dodecylbenzene sulphate and passing said suspension through a filter with pore diameter of 100 nm, adding a technetium-99m eluate, then adding 0.20-0.25 mg ascorbic acid, 2.5-4.0 mg gelatine and 0.02-0.03 mg tin (II) chloride dihydrate per 1 ml of the mixture. The obtained mixture is heated in a water bath at 70-80°C for 30 minutes, cooled to room temperature in an ultrasonic bath and then subjected to sterilisation filtration. The nanocolloid used is iron-carbon particles whose surface is chemically modified with arenediazonium tosylate.

EFFECT: invention enables to obtain technetium-99m labelled nanocolloid, for which not less than 80% of particles have a size in the range of 20-100 nm, relative content of particles with a size smaller than 20 nm is not more than 6% and radiochemical purity is higher than 90% and is maintained for not less than 4 hours.

1 dwg, 4 ex

FIELD: medicine.

SUBSTANCE: rejuvenating effect is ensured by exposing high-molecular hyaluronic acid to gamma-radiation to preparing a stable low-molecular hyaluronic acid, which is used as a prescribed ingredient alongside with synthesised matrix peptide of specific amino acid sequence.

EFFECT: prescribed combination of low-molecular hyaluronic acid and matrix peptides of the developed cosmetic product enables achieving the pronounced aesthetic effect by a physiological mechanism of stimulation of developing proper hyaluronic acid in the skin.

2 dwg, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents an oral care composition, which contains 5 - 95 wt % of an orally acceptable carrier; and a film, wherein the above film contains 10 - 60 wt % of the film of an odour control active ingredient (a zinc-containing compound), 2 - 5 wt % of the film of a mucoadhesive polymer (polyacrylic acid or polyacrylate, polyalkylacrylate, polyvinylpyrrolidone, poly(acrylate)/polyvinylpyrrolidone copolymer, chitosan, 20 - 30 wt % of the film of one or more release controlling polymers (polyvinyl acetate or hydroxyethyl cellulose), 25 - 50 wt % of the film of a polymeric base (hydroxypropyl methyl cellulose, methyl cellulose, hydroxypropyl cellulose and a copolymer thereof) and a flavouring agent, wherein the above film is integrated into the above orally acceptable carrier and makes 0.1 - 5 wt % of the orally acceptable carrier.

EFFECT: invention provides creating the agent able to keep the breath fresh for a long period of time.

5 cl, 5 ex, 7 tbl, 6 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry and represents a foaming personal care composition containing: - a carrier; - an oil phase containing at least one terpene alcohol, which has a cyclic structure; - at least partially fluorinated compound; and - a stabilising agent, wherein the mass ratio of at least partially fluorinated compound and terpene alcohol makes from 2:1 to 4:1.

EFFECT: composition possesses higher stability and provides initial foaming and a longer positive skin effects, including cleansing and moistening.

16 cl, 12 tbl, 14 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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