Oral care compositions

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, namely to an oral care composition and to a method for increasing the solubility of an active ingredient recovered from magnolia extract - tetrahydrohonokiol. The oral care composition contains an active ingredient recovered from the magnolia extract - tetrahydrohonokiol, propylene glycol and an orally acceptable carrier, in a certain amount.

EFFECT: content of the certain amount of propylene glycol in the oral care composition increases the solubility of tetrahydrohonokiol that leads to improving the effectiveness of its delivery and bioavailability.

3 cl, 8 tbl, 8 ex

 

Cross-reference to related applications

The present application claims the priority of provisional patent application U.S. No. 61/307664, filed February 24, 2010, which in its entirety is incorporated herein by reference.

Background of the invention

Often unwanted interaction between the active ingredients of Magnolia extract (or synthetic analogues) and components of means of delivery used for the preparation of traditional compositions for caring for the oral cavity on the basis of the extract of Magnolia, which reduces the effectiveness of such oral compositions. It is therefore necessary to increase the solubility and positive interaction active ingredients of Magnolia extract or synthetic compounds-analogues with other components in oral compositions. It is also necessary to increase the efficiency of delivery of active ingredients of Magnolia extract or synthetic compounds-analogues in oral compositions to improve the effectiveness and bioavailability of these active ingredients.

Summary of the invention

Some embodiments of the present invention provide a method of increasing the solubility of the active ingredients found in Magnolia extract, comprising mixing a prosaw�glycol with an active ingredient. In some embodiments of the present invention one or more of the active ingredients found in Magnolia extract. In some embodiments of the present invention, at least one of the one or more active ingredients found in Magnolia extract, is selected from magnolol, honokiol, tetrahydroindole-(5,5'-DIPROPYLENE-2,2'-diol), tetrahydrocannabinol-(3',5-DIPROPYLENE-2,4'-diol), n-butylalcohol-(5,5'-demotivational-2,2'-diol) and combinations of two or more of them. Some embodiments of the present invention provide a method of increasing the solubility of the synthetic analogue of the active ingredients found in Magnolia extract, comprising mixing propylene glycol with the specified synthetic analogue. In some embodiments of the present invention the specified synthetic analogue is selected from isopropranolol, isobutylamine and dichloraniline. In some embodiments of the present invention the active ingredient and propylene glycol mixed with an orally acceptable carrier.

In other embodiments, the present invention provides an oral composition containing an active ingredient found in Magnolia extract or a synthetic analogue, propelling�ical and orally acceptable carrier.

Additional embodiments of the present invention provide a method of treating diseases or pathological conditions of the oral cavity, comprising providing a composition containing an active ingredient found in Magnolia extract or a synthetic analogue, propylene glycol and an orally acceptable carrier, and applying the specified composition in the oral cavity of a subject in need. In some embodiments of the present invention the specified composition is applied in the oral cavity daily for a period of one week. In some embodiments of the present invention the specified composition is applied in the oral cavity during the period of time up to 2 weeks. In some embodiments of the present invention the specified composition is applied in the oral cavity during the period lasting more than 2 weeks.

Detailed description

The methods and compositions according to the present invention provide advantages in comparison with the prototype compositions, providing an oral composition which is soluble, safe and highly effective against the bacterial infection and/or inflammation in a mammal subject. In addition, some embodiments of the present invention include one or more� from active ingredients of Magnolia extract.

The expression "medium" or "aqueous medium", or "orally acceptable carrier" as used in the present description, means any safe and effective materials for use according to the present invention. Such materials include water, solvents, etc., which may contain a hygroscopic agent, such as glycerin, sorbitol, xylitol, etc. Media, or orally acceptable carrier may also include additional components, intended for the care of teeth, such as thickeners, ionic active ingredients, buffering means, anticellulite tools, abrasive polishing materials, peroxide sources, bicarbonate alkali metal salts, surfactants, titanium dioxide, coloring tools, flavoring system, sweetening agents, antimicrobial agents, agents of plant origin, desensitizing agents, lightener and mixtures thereof.

All percentages and relations used in this document are based on the mass of the composition to care for the oral cavity, unless specified otherwise. All measurements were performed at 25°C, unless otherwise specified.

In the text of the present description and claims the disclosure of specific numerical values (e.g., temperature, mass % com�of onenow, etc.) aims at specifying this value plus or minus some additional value clear to persons having ordinary skills in this field that are specific to the specified variable and the degree of measurement error, usually associated with the specified value. For example, this temperature would be understood by a person having ordinary skills in the area, including up to 10% of variability given by the instrument used to measure temperature.

Some embodiments of the present invention provide a method of increasing the solubility of one or more of the active ingredients found in Magnolia extract, or their synthetic analogues in oral compositions. In some embodiments of the present invention said method comprises mixing an effective amount of propylene glycol with one or more of the active ingredients found in Magnolia extract, or their synthetic analogues. In some embodiments of the present invention, at least one of the one or more active ingredients found in Magnolia extract, is selected from magnolol, honokiol, tetrahydroindole, tetrahydrocannabinol-(3',5-DIPROPYLENE-2,4'-diol), 5,5'-di-n-butylbiphenyl-2,2'-diol, n-butylalcohol-(5,5'-demotivational-2,2'-diol). In some embodiments of the present invention synthetic anal�g of active compound of the extract of Magnolia is selected from isopropranolol, isobutylphenyl and dichloraniline. In some embodiments, the present invention is orally acceptable carrier does not contain propylene glycol as a hygroscopic means. In other embodiments, the present invention is orally acceptable carrier contains propylene glycol.

Some embodiments of the present invention include a method of manufacturing solubilizing oral composition by mixing 0.05 to 10% by mass of propylene glycol with at least one of the one or more active ingredients found in Magnolia extract, or their synthetic analogues with an orally acceptable carrier. In some embodiments of the present invention the propylene glycol is from 0.1 to 5% by weight of the composition. In other embodiments of the present invention, at least one of the one or more active ingredients found in Magnolia extract, or their synthetic analogues is present in an amount of from 0.05 to 5% by weight of the composition (preferably, 0.1 to 3% by weight of the composition).

Additional embodiments of the present invention provide an oral composition containing (i) an effective amount of propylene glycol, (ii) at least one of the one and�or more active ingredients, found in Magnolia extract, or their synthetic analogues, and (iii) an orally acceptable carrier. In some embodiments, the present invention specified oral composition is a composition for caring for the oral cavity.

In some embodiments of the present invention the specified composition is used for inhibiting excessive production of cellular mediators of inflammation in the tissues of the oral cavity in the foci of inflammation caused by infection, external toxins, or trauma in the mouth. In some embodiments of the present invention an effective amount of at least one of the one or more active ingredients found in Magnolia extract, or their synthetic analogues lowers the levels or activity of Pro-inflammatory mediators to the extent adequate to the decrease in their concentration in a mammal subject to levels, which are basal in the tissues of the oral cavity of a subject exposed to treatment without unduly suppressing the activity of intercellular mediators.

In some embodiments of the present invention, at least one of the one or more active ingredients found in Magnolia extract, or their synthetic analogues will be present in the amount required DL� create a desired therapeutic or prophylactic effect in a subject representing a human or lower animal, which is active substance is administered, without undesirable side effects (such as toxicity, irritation or allergic response), in accordance with the reasonable risks and benefits, when they are used according to the present invention. The specific safe and effective amount of active ingredients will change depending on such factors as the particular condition being treated, the physical condition of the subject, the nature of the combination therapy (if such conduct), specific compounds, specific metered-dose form of media to be used and the desired dosage regimen. Qualified specialists in this field will be able to determine a safe and effective amount of active ingredient required for use in the above compositions and methods, using the instructions provided in this document.

In highly sensitive tissue high concentrations of substances extracted from Magnolia, can cause irritation and exacerbate inflammation, and not weaken it. Since the possibility of additional inflammation depends on the condition of the individual subject and his reaction to irritants, and other variables related to treatment, preferably a�ablate the subject of one or more of the active ingredients found in Magnolia extract, or their synthetic analogues at concentrations that do not cause any irritation. The term "non-irritating" means oral contact of the composition with the oral cavity of a mammal subject does not increase irritability, soreness, redness, or a hard tissue in the oral cavity and enhances or worsens the condition of inflammation.

In addition, the concentration of the specified one or more active ingredients found in Magnolia extract, or their synthetic analogues in oral compositions will vary depending on the form of delivery, dosage, final useful effects, the nature of the pathology and/or individual therapeutic requirements of the subject (one or more), to whom they are administered, and therefore the number is expected to present the active ingredient can change the way it recognizes a qualified specialist in this field. In addition, the concentration of active ingredients is usually depends on the form of oral compositions. For example, solutions for rinsing the mouth usually have a relatively low concentration of the active ingredient, while the means for brushing your teeth, gels or tooth powders have a higher concentration to achieve the same delivered dose, as with the easier dispel�remote. Similarly, the confectionery compositions with drugs usually have a relatively high concentration of the active ingredient, to make it possible for sufficient dispersion when dissolved or chewed.

The term "confectionery composition", as used herein, refers to chewing gum, and pills, pills, and lozenges that dissolve in the mouth. Saliva dissolves the material that it is made of candy or chewing gum and contributes to prolonged contact with the surfaces of the oral cavity, so that when using this product active ingredient in the form of lozenges, tablets, pills and chewing gum adequately delivered to the desired surface in the oral cavity.

As used herein, the expression "the Magnolia extract" or "Magnolia extract" means an extract from the dried bark of plants of the family Magnoliaceae, such as Magnolia officinalis (hereinafter in this document called "Magnolia") or synthetic or semi-synthetic equivalent of such an extract or its active component. In certain embodiments of the present invention the oral composition comprises one or more active ingredients selected from an extract of Magnolia, or obtained by traditional synthetic methods. In other embodiments, the OSU�of estline present invention, the oral composition comprises an extract of Magnolia. Preferably, the extracts from Magnolia bark (the bark of Magnolia officinalis) contain active compounds including magnolol, honokiol, tetrahydroindole-(5,5'-DIPROPYLENE-2,2'-diol) and tetrahydrocannabinol-(3',5-DIPROPYLENE-2,4'-diol), which in tests in vitro have demonstrated their antibacterial properties against a typical oral bacteria S. miitans, F. nucleatum, V. parvula, A. naslundii, P. Gingivitis. It should be noted that any plant of the family Magnoliaceae is suitable for extraction of active ingredients used in embodiments of the present invention.

In some embodiments, the implementation of the present invention, the extract contains effective antimicrobial against the concentration of the compounds selected from the group consisting of magnolol, honokiol, tetrahydroindole, tetrahydrocannabinol-(3',5-DIPROPYLENE-2,4'-diol), isopropranolol, isobutylamine and n-butylmagnesium-(5,5'-demotivational-2,2'-diol) and combinations of two or more of them. In other embodiments of the present invention the oral composition comprises one or more active ingredients selected from the group consisting of magnolol, honokiol, tetrahydroindole, tetrahydrocannabinol-(3',5-DIPROPYLENE-2,4'-diol), n-butylalcohol-(5,5'-demotivational-2,2'-diol) and combinations of two or more of them, the number�as, effective for influencing the condition of the oral cavity of a mammal subject, caused by bacterial infection and/or inflammation.

In some embodiments of the present invention, the Magnolia extract can be obtained through extraction. In one method of extraction of the dried powdered Magnolia bark in powder form sequentially brought into contact with ethanol, methylene chloride and cyclohexane, at each stage forming a concentrated paste, the latter pasty form dissolved in hot petroleum ether at about 50-60°C and then dried in vacuum at finite extraction yielding an extract containing from about 5 to about 10% by weight honokiol and from about 15 to about 25% by weight magnolol.

In another method of extracting the Magnolia extract is prepared from the dried bark of the plant Magnolia, subjecting it to extraction with a suitable solvent. Preferred solvents include methanol, ethanol, methylene chloride, hexane, cyclohexane, pentane, petroleum ether, chloroform, hydrochloric acid, ethylene dichloride and hydrofluroalkane, such as 1,1,1,2-Tetrafluoroethane or HFA-13A. Usually one portion of plant tissue (based on dry material) was extracted with 5-50 parts of solvent (preferably, 1530 parts), using an extraction apparatus where the solvent is in contact with the bark, forming a concentrated paste, which is then subjected to one or more additional extraction stages with different solvents for further concentration initially obtained paste over an extended period of time, preferably, from about 6 hours to about 1-2 days (more preferably, within 1 day). In one simplified method of extraction of the dried powdered Magnolia bark in powder form are brought into contact with hydrofluroalkane (such as 1,1,1,2-Tetrafluoroethane (HFA-13A)) for education at the final extraction of the concentrated extract containing from 5 to 50% honokiol and from 5 to 50% of magnolol.

In still one other method of extracting the Magnolia extract is isolated by supercritical fluid extraction (SFE) using carbon dioxide (CO2). Supercritical fluids are gases with properties intermediate between the properties of "normal" gas phase and fluid properties. Changing the pressure, regulate the properties of supercritical fluids, depending on the pressure applied, may change from a more gas-like behavior to behavior that is more characteristic of the liquid. As the supercritical fluid used races�foretell, which is readily available, inexpensive and environmentally safe (CO2and H2O). Carbon dioxide is non-toxic, explosion-proof, easily accessible and easily removed from the extracted products. Operating temperatures for SFE are typically low to moderate. Thus, SFE produces products, almost free of solvent and, in addition, eliminates the possibility of any adverse reactions.

In addition, SFE-extracted products, usually absent natural contaminants that may be present in other methods of extraction. For example, such compounds as arisekola acid, and alkaloids such as manokaran and tubocurarine, are maintained at low concentrations (e.g., typically less than 0.0002%). Thus, in those embodiments of the present invention, in which Magnolia is extracted by SFE, the extract is substantially free from chemical changes caused by heat and water, residues from solvent and other artifacts.

The terms "extracting" or "extraction" of some solid or liquid material, as used herein, means contacting said material with some suitable material, such as a solvent, for the removal of substances (one or more) which is extracted from said material. Such extraction can be performed by conventional means, known to a qualified specialist in the art, for example, using an extraction apparatus such as a Soxhlet apparatus, which retains the solid material in a holder and allows the solvent to flow through the material; or mixing the solvent with the specified material and then separating the liquid and solid phases or two immiscible liquid phases, as by filtration or sedimentation and decanting.

The Magnolia extract according to the present invention, obtained by different methods of extraction, maybe 2-95% consist of magnolol. In some embodiments of the present invention magnolol may be present in the extract at a concentration of from 5 to 50%. In other embodiments of the present invention magnolol may be present in the extract at a concentration of from 30 to 50%. In certain embodiments, the present invention honokiol may be present in the extract at a concentration of from 2 to 95%. In additional embodiments, the present invention honokiol may be present in the extract at a concentration of from 5 to 50%. In another group of embodiments of the present invention honokiol may be present in the extract at a concentration of from 30 to 50%.

Inappointed embodiments of the present invention is preferred, to the active ingredients of Magnolia extract contained either magnolol or honokiol or both of these compounds. Magnolol and honokiol are nonionic hydroxybiphenyl compounds, the structure of which is as follows:

In addition to this, tetrahydroindole-(5,5'-DIPROPYLENE-2,2'-diol) and tetrahydrocannabinol-(3',5-DIPROPYLENE-2,4'-diol) are hydrogenated analogues of magnolol and honokiol, respectively; they are often found in extracts of Magnolia, and therefore they can be included in the oral composition. In addition, the oral composition may be included 5,5'-demotivational-2,2'-diol (homolog of magnolol); expert with ordinary skills in the art can realize the synthesis of this compound by traditional organic synthesis. The structure of tetrahydropyrrolo-(5,5'-DIPROPYLENE-2,2'-diol), tetrahydrocannabinol-(3',5-DIPROPYLENE-2,4'-diol) and 5,5'-di-n-butylbiphenyl-2,2'-diol (homolog of magnolol) is shown below.

Orally acceptable carriers, intended for use according to the present invention, include traditional and well-known carriers used in the manufacture of toothpastes, tooth powders, sieves�political pastes, solutions for rinsing the mouth, lozenges for sucking, chewing gums, dragees, etc.; hereinafter in this document they are described more fully. Preferably, the orally acceptable carrier did not cause irritation, swelling or pain and, as a rule, made no allergic or adverse reactions, such as upset stomach, nausea or dizziness. The selection of specific component carrier depends on the desired product form, including means for cleaning teeth, toothpastes, tooth powders, pastes, solutions for rinsing the mouth, lollipops for sucking, chewing gum, gels, dyes, confectionery, etc.

The term "solution for rinsing the oral cavity" in the present invention relates to oral compositions which are substantially liquid in nature, such as a liquid for rinsing of a mouth spray or mouthwash. In this drug orally acceptable carrier usually has a water phase containing water or a mixture of water and alcohol. In addition, in various embodiments of the present invention, the oral carrier comprises a hygroscopic agent and a surfactant as described below. Typically, the ratio of the mass of water to mass of alcohol is in the range from 1:1 to 20:1(preferably, from 3:1 to 10:1 and, more preferably, from 4:1 to 6:1). The total amount of water-alcohol mixture in the preparation of this type is usually from 70 to 99.9% by weight of the drug. In various embodiments of the present invention the specified alcohol is typically ethanol or isopropanol.

As recognized by qualified experts in the art, orally acceptable carrier according to the present invention may also contain a variety of other conventional active ingredients, known qualified specialists in this field of technology, including funds against deposits of plaque, whitening agents, antibacterial agents, the means for controlling the deposition of Tartar (anticellulite medium), anti-caries substances affecting the sensitivity, etc., Preferably, the carrier does not substantially reduce the effectiveness of anti-inflammatory and antibacterial active ingredients found in Magnolia extract, or their synthetic analogues.

The pH of such liquid and other preparations of oral compositions according to the present invention is generally from 4.5 to 10. The pH can be adjusted with acid (e.g. citric acid or benzoic acid) or base (e.g. sodium hydroxide) or buffered connection, for example, citrate, benzoate, carbonate, or sodium bicarbonate, disodium phosphate, sodium or odnozamesheng phosphate sodium).

In various embodiments of the present invention the aqueous oral composition (e.g., mouthwash) comprises a hygroscopic agent. Specified hygroscopic agent, typically is a mixture of hygroscopic substances, such as glycerin and sorbitol, and a polyhydric alcohol, such as hexyleneglycol or polyethylene glycol, although the optimum is the use of polyethylene glycol as a hygroscopic funds in addition to its use for increasing the solubility of the active ingredient. The content of hygroscopic means is typically in the range from 5 to 40% and preferably from 10 to 30%.

Surfactants suitable for the compositions according to the present invention include anionic, nonionic and zwitterionic surfactants. A surfactant is typically present in the aqueous oral compositions according to the present invention in an amount of from 0.01% to 5% and preferably in an amount of from 0.5% to 2.5%.

Oral composition according to the present invention, optionally, may include other materials, such as, for example, cleaning products, vkusomyatka, sweeteners, adhesive means, surfactants, foam modulators, abrasives, tools, pH modifier, hygroscopic substances, moisturizers, drugs affecting the mouth feel, coloring tools, preservatives, source of fluoride ions, stimulants salivation, emollients, viscosity modifiers, diluents, emulsifiers, nutrients, and combinations thereof. A variety of components that can be added to the oral composition include, for example, a sweetener such as saccharin or sodium saccharinate), alcohols (such as ethanol), sources of fluoride ions (such as sodium fluoride), as well as glycerin, sorbitol, polyethylene glycols, poloxamine polymers (such as POLOXOMER®407, PLURONIC®F108 available from BASF Corporation), alkylpolyglycoside (APG), Polysorbate, PEG40, castor oil, menthol, etc. it is Clear that although the basic characteristics of each of the above categories of materials may differ, but there may be some common characteristics and any given material may serve many purposes in two or more of such categories of materials. Preferably, such materials carriers are selected based on compatibility with the active ingredients found in Magnolia extract, or their synthetic analogues, as well as with other ingredients com�osili.

Among the substances that can be used in the present invention, flavoring materials include any material or mixture of materials, existing to improve the taste of the composition. You can use any orally acceptable natural or synthetic flavoring substance, such as flavoring oils, flavoring aldehydes, esters, alcohols, and similar materials and combinations thereof. Flavorings include vanillin, sage, marjoram, parsley oil, peppermint oil curly, cinnamon oil, wintergrove oil (methyl salicylate), peppermint oil, clove oil, Bay oil, anise oil, eucalyptus oil, citrus oil, fruit oils and essences, including oils and essences derived from lemon, orange, lime, grapefruit, apricot, banana, grape, Apple, strawberry, cherry, pineapple, etc., flavoring substances derived from beans and nuts (such as coffee, cocoa, Cola, peanut, almond, etc.), adsorbed and encapsulated flavoring substances and their mixtures. In addition, the term "flavouring substance" as used herein covers the ingredients, which create a feeling of flavoring and/or other sensory effect in the mouth, including cooling and warming effects. Such ingredients include menthol, methylacetate, Mantellate, camphor, eucalyptus oil, eucalyptol, Anya�ol, eugenol, Cassia, Oksanen, [alpha]-irison, propylgallate, thymol, linalool, benzaldehyde, cinnamic aldehyde, N-ethyl-p-Mentana-3-carboxamid, N,2,3-trimethyl-2-isopropylmalonic, 3-1-methoxypropane-1,2-diol, acetal, cinnamic aldehyde and glycerol (CGA), acetal Menton with glycerol (MGA) and mixtures thereof. One or more of flavouring substances optionally present in a total quantity from 0.01% to 5%; optionally in various embodiments of the present invention in an amount of from 0.05 to 2%, from 0.1% to 2.5% and from 0.1 to 0.5%.

Among the substances that can be used in the present invention, the sweeteners include dextrose, Polydextrose, sucrose, maltose, dextrin, dried invert sugar, mannose, xylose, ribose, fructose, levulose, galactose, corn syrup, partially hydrolyzed starch, hydrogenated starch hydrolysate, sorbitol, mannitol, xylitol, maltitol, isomalt, aspartame, neotame, saccharin and its salts, energy, intense sweeteners-based dipeptides, cyclamate, dihydrochalcone and mixtures thereof.

Drugs affecting the mouth feel, include materials which when used in the composition give a sense of the desirable texture or other sensation.

Among the substances that can be used in the present invention, colorants include pigments, dyes, lacquers and means�ment special luster or reflectivity (such as materials, giving a pearly luster). In various embodiments of the present invention the colouring agent used to create a white or light coloured coating on the surface of the teeth, as an indicator of locations on a dental surface that have been effectively contacted by the composition, and/or to change the appearance of the composition (in particular color and/or opacity) to increase its attractiveness to the consumer. You can use any orally acceptable the colorant including a dye FD&C and pigments, talc, mica, magnesium carbonate, calcium carbonate, magnesium silicate, magnesium aluminosilicate, silica, titanium dioxide, zinc oxide, red, yellow, brown and black iron oxides, ferric synergistic ammonium, dye manganese violet, ultramarine, titaniumalloy mica, bismuth oxychloride, and mixtures thereof. One or more coloring agents, optionally present in a total quantity amounting to from 0.001% to 20%, e.g., 0.01% to 10% or 0.1% to 5%.

In some embodiments of the present invention the oral composition according to the present invention may contain optional abrasive material used, for example, as polishing agents. You can use any orally acceptable abrasive, but the type, the degree of granular�STI (particle size) and amount of abrasive should be selected so as to tooth enamel not subjected to excessive abrasion during normal use of the composition. Suitable optional abrasives include silica (e.g. precipitated silica or mixed with alumina, insoluble phosphates, calcium carbonate, and mixtures thereof. To insoluble phosphates useful as abrasives include orthophosphate, polymetaphosphate and pyrophosphates. Typical examples are the dihydrate dicalciumphosphate, calcium pyrophosphate, tricalcium phosphate, polymetaphosphate calcium and insoluble polymetaphosphate sodium.

In some embodiments of the present invention the compositions according to the present invention optionally contain a means for controlling the deposition of Tartar (anticellulite tool). Among the substances that can be used in the present invention, the means controlling the deposition of Tartar, include salts of any of them, for example, their salts with alkali metals and ammonium: phosphates and polyphosphates (for example pyrophosphates), polyaminopropyl acid (AMPS), polyaluminosilicate, poliolefinas, diphosphonates (such as azacycloheptane-2,2-diphosphonates - for example, azacycloheptane-2,2-difosfonovoy acid, N-methylacetophenone-2,3-difosfonovoy acid, ethane-1-hydroxy-1,1-difosfonovoy acid (EHDP) and ethane-1-amino-1,1-�ifastnet), phosphonocrotonate acid. Applicable inorganic phosphate and polyphosphate salts include monobasic, dibasic and tribasic sodium phosphates, sodium tripolyphosphate and metropolitical sodium, mono-, di-, tri - and tetranitromethane, trimetaphosphate sodium, sodium hexametaphosphate and mixtures thereof.

In other embodiments of the present invention an oral composition according to the present invention optionally contain a source of fluoride ions, applicable, for example, as anti-caries funds. You can use any orally acceptable source of fluoride ions, including fluoride and monophosphate potassium, sodium and ammonium, fluoride tin (II) fluoride India, amine fluorides, such as olaflur (N'-octadecyltrimethylammonium-N,N,N'-Tris(2-ethanol)-dihydrofluoride) and mixtures thereof. One or more sources of fluoride ions, optionally is present in amounts that provide oral compositions clinically effective amount of soluble fluoride ions.

In additional embodiments of the present invention an oral composition according to the present invention optionally contain a stimulant salivation - for example, to moisturize your dry mouth. You can use any orally acceptable stimulator salivation, including, without limitation, food to�slots, such as citric, lactic, malic, succinic, ascorbic, adipic, fumaric and tartaric acid, and mixtures thereof. One or more of stimulants salivation, optionally, present in the total number of effectively stimulating salivation.

In other embodiments of the present invention an oral composition according to the present invention optionally contain a nutrient. Suitable nutrients include vitamins, minerals, amino acids and mixtures thereof. Vitamins include vitamins C and D, thiamine, Riboflavin, calcium Pantothenate, nicotinic acid, folic acid, nicotinamide, pyridoxine, cyanocobalamin, p-aminobenzoic acid, bioflavonoids, and mixtures thereof. Nutritional supplements include amino acids (such as L-tryptophan, L-lysine, methionine, threonine, levocarnitine and L-carnitine), lipotropic substances (such as choline, Inositol, betaine, and linoleic acid), and mixtures thereof.

In some embodiments, the present invention provides a method of treating conditions associated with the presence of oral bacteria, including the provision of oral composition according to any one of the above-described embodiments of the present invention and the application of specified oral composition in the oral cavity of a mammal subject. In some embodiments, us�Mr sage of the invention said method includes the repeated recurrence of applying specified song as long while the subject has not achieved the desired antibacterial and/or anti-inflammatory effects.

The term "inflammation" of the oral tissues, as used herein, refers to a local protective reactions caused by damage to or destruction of the tissue and serves to destroy, dilute or isolate as the damaging agent and injured tissue. In the acute form it is characterized by pain, heat, redness, swelling and loss of functionality. Chronic inflammation is a slow process, primarily characterized by the formation of new connective tissue. Chronic inflammation is often a continuation of acute inflammation or is an extended less pronounced form of inflammation (such as the inflammation associated with periodontitis or gingivitis); it usually causes permanent tissue damage. Histologically, inflammation is involved a complex series of events, including dilatation of arterioles, capillaries and venules with increased permeability and increased blood flow, exudation of fluids, including plasma proteins, and leukocyte migration into the inflammatory focus. Inflammation corresponds to elevated levels of Pro-inflammatory cellular mediators or substances released from cells, for example, as a result of the interaction of antigen with antibody or re�functions of antigen with a sensitized lymphocyte.

In various embodiments of the present invention applying or contacting is carried out by rinsing, coating, processing, brush or layering with the use of suitable coating materials. In some embodiments of the present invention the contacting also includes accidental contact when eating or chewing. In various embodiments of the present invention the coating composition comprises applying applicating device that helps to maintain a sufficient contact time of Magnolia extract containing anti-inflammatory active ingredient, processed cloth, giving the opportunity to pharmacological way to inhibit the increased production of one or more of inflammatory mediators such as PGE2and TNF-α.

In certain embodiments of the present invention the oral composition is not intended for ingestion, and for retention in the oral cavity for a time sufficient for the existence of the desirable action. In other embodiments of the present invention, particularly those where the oral composition to provide a product designed for Pets, such as pet food, feed additives for domesticanimals (for example, a treat) or razzhevyvanie toys, small concentrations of oral compositions can zaputyvaetsja without harm to the animal. Preferably, the specific materials and compositions to be used according to the present invention are pharmaceutically or cosmetically acceptable.

Some embodiments of the present invention provide an oral composition containing from about 0.05 to about 10% by weight propylene glycol, from about 0.05 to about 5% by weight of one or more of the active ingredients found in Magnolia extract, or their synthetic analogues and orally acceptable carrier.

Some embodiments of the present invention provide an arrangement in which at least one of the one or more active ingredients is tetrahydropyrrolo. In some embodiments of the present invention, at least one of the one or more active ingredients is tetrahydrocannabinol. In other embodiments of the present invention, at least one of the one or more active ingredients is a 5,5'-di-n-butylbiphenyl-2,2'-diol.

Some embodiments of the present izobreteny� provide a method of treating diseases or pathological conditions of the oral cavity, includes the provision of compositions containing from about 0.05 to about 10% by weight propylene glycol, from about 0.05 to about 5% by weight of one or more of the active ingredients found in Magnolia extract, or their synthetic analogues and orally acceptable carrier and application of the specified composition in the oral cavity of a subject in need.

In some embodiments of the present invention, the disease or pathological state of the oral cavity is a disease or pathological condition of the teeth, oral mucosa, gums or tongue. Such diseases or pathological conditions include caries, gingivitis, periodontitis, and cosmetic conditions, such as yellowing and odor.

The present invention will be described in more detail with specific examples. The following examples are presented for purposes of illustration and are not intended to limit the scope of the present invention any way. Qualified specialists in the art will easily recognize those non-critical parameters that you can change or modify, yielding essentially the same results.

Examples

Oral compositions having the ingredients listed in the tables below to monopolizing the following way. Sodium fluoride and any other salt is dispersed in water. Hygroscopic substances (for example, glycerin and sorbitol) are added to the mixture in the traditional mixer with vigorous stirring. The mixture obtained as a result of this, are intensively mixed to form a homogeneous phase of the gel. This gel phase are added a pigment such as TiO2and any acid or any base (e.g., NaOH) required to bring the pH to 6-7. Then add organic thickeners, carrageenan and SMS. These ingredients are stirred until then, until a homogeneous phase. Then this mixture was transferred to a high-speed vacuum mixer, add silica abrasives and a silica thickener. Thereafter, the mixture was stirred at high speed for about 5-30 minutes in a vacuum of approximately 20 to 50 mm Hg (preferably, at about 30 mm Hg). Weigh flavoring oil and then add extracts of Magnolia or their active ingredients. This perfume oil and active ingredients of Magnolia was added to the mix. Last add a surfactant such as sodium lauryl sulfate (SLS). The product obtained by this procedure is solubilizing, stable, efficient, homogeneous, semi-solid, extrudable paste or gel�.

Example 1

Table 1 shows solubilization and effective oral composition containing propylene glycol and tetrahydrocannabinol (one of the active ingredients found in Magnolia extract).

Table 1
IngredientNumber (%)
Purified water29
Sorbitol19,45
Glycerin20
Sodium CMC type 12 according to the USP1,1
Iota-carragenan0,4
Sodium saccharin in the United States Pharmacopoeia0,3
Sodium fluoride0,24
Zeodent-1158,5
Zeodent-1653
Sylodent XWA65010
Titanium dioxide0,5
Powder sodium lauryl sulfate-N 1,5
Flavoring1
Propylene glycol4,5
Tetrahidrocannabinol0,5
Total100

Example 2

Table 2 shows solubilization and effective oral composition containing propylene glycol and 5,5'-di-n-butylbiphenyl-2,2'-diol (structural analogue of magnolol, one of the active ingredients found in Magnolia extract).

Table 2
IngredientNumber (%)
Purified water29
Sorbitol19,45
Glycerin20
Sodium CMC type 12 according to the USP1,1
Iota-carragenan0,4
Sodium saccharin in the United States Pharmacopoeia0,3
Fluoride on�Riya 0,24
Zeodent-1158,5
Zeodent-1653
Sylodent XWA65010
Titanium dioxide0,5
Powder sodium lauryl sulfate-NF1,5
Flavoring1
Propylene glycol4,5
5,5'-di-n-butylbiphenyl-2,2'-diol0,5
Total100

Example 3

Table 3 shows solubilization and effective oral composition containing propylene glycol and synthetic honokiol (one of the active ingredients found in Magnolia extract).

Table 3
IngredientNumber (%)
Purified water32,51
Sorbitol19,45
Glycerin20
Sodium CMC type 12 according to the USP1,1
Iota-carragenan0,4
Sodium saccharin in the United States Pharmacopoeia0,3
Sodium fluoride0,24
Zeodent-1158,5
Zeodent-1653
Zeodent-10510
Titanium dioxide0,5
Powder sodium lauryl sulfate-NF1,5
Flavoring1
Propylene glycol1
Synthetic honokiol0,5
Total100

Example 4

Table 4 shows solubilization and effective oral composition containing propylene glycol and natural honokiol (one of the active ingredients found in Magnolia extract).

Table 4
IngredientNumber (%)
Purified water33,96
Sorbitol20
Glycerin20
Sodium CMC type 12 according to the USP1,1
Iota-carragenan0,4
Sodium saccharin in the United States Pharmacopoeia0,3
Sodium fluoride0,24
Zeodent-1157,5
Zeodent-1653
Sylodent XWA 6509
Titanium dioxide0,5
Powder sodium lauryl sulfate-NF1,5
Flavoring1
Honokiol0,5
Propylene glycol1
Total100

Example 5

Table 5 below describes data demonstrating the effect of propylene glycol on the solubility of the extract of Magnolia in the liquid drug.

Table 5
IngredientPreparation 5APreparation 5BPreparation 5C
Water41,0440,95To 40.07
Sorbitol25,8025,4225,42
Glycerin24,7624,3924,39
Sodium fluoride0,300,290,29
Sodium sulphate0,620,610,61
Copolymer Gantrez2,802,752,75
Sodium hydroxide0,750,740,74
Sodium saccharin0,380,370,37
Sodium lauryl sulfate1,871,84Of 1.82
Flavoring1,301,281,23
The Magnolia extract (purity >98%)0,390,380,37
Propylene glycol0,981,94
Total100100100
The appearance of drug isThe separation of the phases, creamy top layerTranslucent, but homogeneousClean and clear

Example 6

Table 6 below describes data demonstrating the effect of propylene glycol on the solubility of m�of golola in the liquid drug.

Table 6
IngredientPreparation 6AThe drug 6BPreparation 6C
Water39,1039,1137,43
Sorbitol24,0424,0423,73
Glycerin23,0723,0722,77
Sodium fluoride0,280,280,27
Sodium sulphate0,580,580,57
Copolymer Gantrez2,602,602,56
Sodium hydroxide0,700,700,69
Sodium saccharin0,350,36Sodium lauryl sulfate2,211,721,7
Flavoring1,201,161,18
Magnolol0,590,590,58
Propylene glycol5,285,288,18
Furanol (additional surfactants)0,51
Total100100100
The appearance of drug isThe separation of the phases, creamy top layerThe separation of the phases, creamy top layerTranslucent, but homogeneous

Example 7

Table 7 below describes data demonstrating the effect of propylene glycol on the solubility of butylmagnesium in the liquid drug.

Table 7
IngredientPreparation 7APreparation 7BThe drug 7CThe drug 7D
Water40,8640,2339,4938,00
Sorbitol25,9225,5625,0724,11
GlycerinAre 24.8824,5324,0623,14
Sodium fluoride0,300,290,290,28
Sodium sulphate0,630,620,60,58
Copolymer Gantrez2,802,762,712,61
Sodium hydroxide0,75 0,740,730,70
Sodium saccharin0,370,370,360,35
Sodium lauryl sulfateTo 1.861,871,801,72
Flavoring1,261,211,181,15
Mucilaginosa0,380,370,370,37
Propylene glycol1,463,347,00
Total100100100100
The appearance of drug isVery cloudyVery cloudyCloudyClean and clear

Example 8

Tables� 8, below describes data demonstrating the effect of propylene glycol on the solubility of papilionaceae in the liquid drug.

Table 8
IngredientPreparation 8APreparation 8BPreparation 8CThe drug 8D
Water40,8640,2639,4638,00
Sorbitol25,9225,5425,0524,12
Glycerin24,8724,5124,0423,15
Sodium fluoride0,300,290,290,28
Sodium sulphate0,620,620,600,58
Copolymer Gantrez2,0 2,762,712,61
Sodium hydroxide0,750,740,730,7
Sodium saccharin0,370,360,360,35
Sodium lauryl sulfateTo 1.861,83To 1.791,73
Flavoring1,271,261,241,16
Papilionacea0,380,370,380,35
Propylene glycol1,463,356,97
Total100100100100
The appearance of drug is Very cloudyClean and clearClean and clearClean and clear

Each patent, patent and printed publication referred to in this patent document are thereby incorporated by reference in their entirety.

As recognized by qualified experts in the art, in embodiments of the present invention, described herein, can be made of numerous changes and modifications without deviation from the essence of the present invention. It is assumed that all such variations fall within the scope of formula of the present invention.

1. Composition for caring for the oral cavity that contains:
from 0.1 to 5% by weight of propylene glycol;
from 0.1 to 3% by weight of active ingredient, selected from an extract of Magnolia, representing tetrahydrocannabinol; and orally acceptable carrier.

2. A method of increasing the solubility of the active ingredients found in Magnolia extract, representing tetrahydrocannabinol, in a composition for caring for the oral cavity according to claim 1, comprising mixing propylene glycol with the active ingredient.

3. A composition according to claim 1 for use in a method of treating or preventing diseases or pathological status�States of the oral cavity, wherein said method comprises applying the specified composition in the oral cavity, where the specified composition is applied daily for a period of not less than one week.



 

Same patents:

FIELD: medicine.

SUBSTANCE: invention relates to medicine and is intended for oral cavity care. Compositions include a multi-layered film and an orally acceptable carrier. The carrier contains the first flavouring agent, with the second flavour being contained in the present central layer of the multi-layered film, located between two external surface layers. The first and second flavouring agents can be similar or different. Each film layer can include a film-forming polymer, for instance, hydroxypropylmethylcellulose. The external layers can include a substance, modulating the release of the flavouring agent, for instance, polyvinylacetate or hydroxymethylcellulose. The carrier can be a means for teeth cleaning or a liquid for mouth rinsing.

EFFECT: obtaining the composition for oral cavity care.

22 cl, 3 dwg, 4 tbl, 11 ex

FIELD: medicine.

SUBSTANCE: vaseline-lanolin (2:1) based ointment 74.0 g is added with a 40% herbal alcoholate 25 ml of the following composition (in the mixture of a herbal raw material: alcohol base - 1:5), weight fractions: nodding catchfly herb - 3 weight fractions, pot marigold blossom - 1 weight fraction, spiraea herb - 1 weight fraction, with the ointment added with clove oil 1.0 ml. The prepared ointment is applied on inflamed periodontal and oral mucosal tissues for 20 minutes 2-3 times a day for 14 days; the patient is advised not to drink or eat for 1 hour.

EFFECT: method enables increasing clinical effectiveness by combining high antimicrobial, immunomodulatory, anti-allergic and keratoplastic activity and ease of use.

3 ex

FIELD: medicine.

SUBSTANCE: on completion of the antibacterial course, sodium hyaluronate in the form of a gel is single administered by means of a syringe with a needle of 2 cm long or more under an oral mucosa along a transitory fold into the points within projections of apexes of dental roots 1.4, 2.4, 3.6, 4.6 and into a point on the mid-line of projections of apexes of anterior roots of upper and lower jaw respectively. The needle is brought under the mucosa on the lower jaw by transecting the projections of an alveolar counterfort line. On the upper jaw - by transecting the projections of the upper counterfort line. While removing the needle from the mucosa, the syringe content is squeezed out. Sodium hyaluronate is administered into both jaws in an amount of 3.0 to 4.4 ml.

EFFECT: method enables increasing the jaw bone density within counterforts, as well as soft and bone tissues of periodontium.

4 tbl, 16 dwg, 3 ex

FIELD: medicine.

SUBSTANCE: invention refers to dentistry and concerns treating chronic generalised periodontitis. Implementing the above method is ensured by a complex preparation in the form of an ointment of the following composition: Vaselin - lanolin base (1:1) - 88.5 g, 70% ipecac infusion - 5.0 g, 70% scholar tree - 5.0 g, Ecdysterone - 0.02 g; eucalyptus oil - 1.0 g. The oil is applied as a therapeutic periodontal applicate on a gingival surface following application anaesthesia with 10% lidocaine, chairside oral hygiene, drug-induced treatment of the gingival margin with 1% Iodinolum and separation of salivary glands in the oral cavity, once a day for 2 hours for 4 weeks; the patients are recommended not to eat or drink for two hours. The preparation composition particularly provides capillary-reinforcing, anti-inflammatory, reparative and anaesthetic action.

EFFECT: method of treating is easy to use, physiologically-friendly, and provides the complete recovery.

2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) : or a salt thereof, wherein R1 and R5 are independently selected from H, OH and alkoxy; R2-R4 and R6-R8 are independently selected from H, OH, F, Cl, Br and I; R9 and R10 are C2-C8 alkenyl; under the condition that at least one of R1, R5 and R7 is OH or alkoxy; at least one of R2-R4, R6 and R8 is F, Cl, Br or I; and R2 and R6 are Cl. The invention also relates to an antibacterial composition and treatment methods.

EFFECT: improved properties.

18 cl, 7 ex, 10 tbl

FIELD: medicine.

SUBSTANCE: agent for treating inflammatory periodontal and oral mucosal diseases associated with Helicobacter infection contains silicone glycerohydrogel of Si(C3H7O3)4·6C3H8O3·24H2O and bismuthate tripotassium dicitrate of formula [HOC(CH2COO)2COO]2K3Bi in the following proportions, wt %: bismuthate tripotassium dicitrate 1.0-2.5; silicone glycerohydrogel - the rest up to 100. The method of treating inflammatory periodontal and oral mucosal diseases consists in a combination of systemic standard anti-Helicobacter therapy and a local effect of the above agent on the involved region. Particularly, treating periodontitis is ensured by applying the agent on the gingival surface and introducing it into the gingival pockets once a day for 10 min; the therapeutic course makes 5-6 days. The oral mucosal diseases are treated by applying the agent 0.1 mm thick with a glass spatula on the involved oral mucosa 2 times a day; the therapeutic course is 12 days.

EFFECT: formulation of the agent provides achieving the high therapeutic effect; the dosage form is easy to be applied locally.

4 cl, 2 dwg, 1 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: method includes the preparation of a carious cavity, opening the tooth cavity, creation of an access to root canals, extension of their orifice. Removal of a decayed material from the root canals and their drug treatment are carried out. After that, performed are: wide opening of the apical tooth orifice, mechanical and drug removal of periapical pathological exudative formations in the focus of periapical inflammation through the root canal. Before filling the canal with a filling material the gel "Lamifaren" is introduced into the focus of periapical destruction. Such introduction is performed three times after a day under temporary stopping. The gel "Lamifaren" is introduced inside in a dose of 50 g 2 times per day for 30 days.

EFFECT: application of the invention accelerates bone tissue regeneration due to the active release of an active substance calcium alginate, provides stable remission due to local and systemic detoxifying effect.

2 ex

FIELD: medicine.

SUBSTANCE: treatment is two-staged; at the first stage, gingival pockets are rinsed with a stream of 1.5% hydrogen peroxide in a cannula delivered through the gingival pockets around the teeth. If observing the exposed furcation of premolars and molars, the cannula is brought under the root furcation. Thereafter, the gingival pockets are similarly rinsed with an aqueous tincture of garden sage herb for 3-5 days, then with an aqueous tincture of camomile blossom for 3-5 days, an aqueous tincture of plantain leaves daily for the following 3-5 days; each rinsing procedure is followed by applications of cotton drains impregnated with the respective aqueous herbal tincture introduced by the cannula on gingival mucous membranes for 1 hour; that is combined with prescribing oral baths with the respective aqueous herbal tincture introduced by the cannula daily 5-7 times a day. The second stage involves instillations of Normoflorin-B or Bifidumbacterin in the cannula delivered through the gingival pockets around the teeth, brought under the furcation if observing the exposed furcation of premolars and molars; the gingival mucous membranes are laid with cotton drains with the above preparation for 2 hours daily for 5-10 days.

EFFECT: method enables providing the higher clinical effectiveness.

2 cl, 1 ex

FIELD: medicine.

SUBSTANCE: at the first stage, after removing supra- and sub-gingival dental calculus and granulations, cleaning the teeth professionally, rinsing gingival pockets by stream infusions of 1.5% hydrogen peroxide in a cannula delivered through the gingival pockets around the teeth, brought under root furcation if observing the exposed furcation of premolars and molars; the preparation "Calsept" is administered within the frontal teeth for 5-7 days daily into the gingival pockets bringing the cannula similarly around the teeth, whereas the preparation "Calsept-Iodo" is administered within the distal teeth; the dentist recommends that the patient does not eat for 2 hours thereafter. The second stage involves administering a preparation containing bifidus bacteria, e.g. Normoflorin-B or Bifidumbacterin by instillations in a cannula delivered through the gingival pockets around the teeth, brought under the furcation if observing the exposed furcation of premolars and molars; gingival mucous membranes are laid with cotton drains with the preparation for 2 hours daily for 5-10 days.

EFFECT: using the method provides increasing the therapeutic effect ensured by the antibacterial effect, odontotropic and anaesthetic action, bone tissue recovery, action of the therapeutic preparation in difficult-to-access anatomic formations.

2 cl, 1 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: therapeutic agent contains anastrozole, poly(lactic-co-glycolic acid), polyvinyl alcohol and D-mannitol. The therapeutic agent represents sub-micron particles and can be presented in the form of capsules, granules, powder, as well as a suspension for injections.

EFFECT: using the developed therapeutic agent enables achieving the therapeutic effect with lower therapeutic doses and making the antitumour therapy more comfortable for the patient.

2 cl, 1 tbl, 2 dwg, 3 ex

FIELD: medicine.

SUBSTANCE: invention refers to a pharmaceutical composition containing a compound presented by formula (I) , wherein R1 represents a hydrogen atom, C1-6 alkyl group or C3-8 cycloalkyl group; while R2 represents a hydrogen atom or a methoxyl group, or its pharmaceutically acceptable salt, or solvate; and alkaline earth carbonate, wherein the content of the compound presented by formula (I), or its salt or solvate makes 0.25 to 50 wt %, and the content of alkaline earth carbonate makes 1 to 60 wt % in relation to total weight of the composition, respectively.

EFFECT: composition exhibits excellent solubility; it is storage-stable or even long-term storage-stable, and applicable as a preventive or therapeutic agent for treating a tumour.

10 cl, 7 dwg, 10 tbl, 19 ex

FIELD: medicine.

SUBSTANCE: invention provides a solid hypolipidemic dosage form containing rosuvastatin or its pharmaceutically acceptable salt in an amount of 3 to 15%, processing additives and a pharmaceutically acceptable excipient containing microcrystalline cellulose, lactose monohydrate, polyvinylpyrrolidone and croscarmellose sodium. The above excipient represents granulate in an amount of 79 to 95 wt % of the dosage form containing absorbed moisture within the range of 0.5% to 1.5%. What is also described is a method for preparing the dosage form.

EFFECT: uniform distribution of the active substance and storage stability of the dosage form of rosuvastatin.

11 cl, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing metribuzin microcapsules. Said method is characterised by mixing aqueous polyvinyl alcohol solution with metribuzin and E472c, stirring the mixture until dissolution of components of the reaction mixture and then adding methyl carbinol as a first precipitant and isopropanol as a second precipitant, filtering the obtained microcapsule suspension, washing with isopropanol and drying.

EFFECT: invention provides a simple process of producing metribuzin microcapsules in a water-soluble polymer, and increases mass output.

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, more specifically to an implanted device comprising a biologically compatible, biologically degradable polymer mixed with TMC278 (rilpivirine) and with one or more release-enhancing agents specified in a group consisting of poloxamers, polysorbates and a combination of dimethylsulphoxide (DMSO) and poly(vinylpyrrolidone) (PVP).

EFFECT: device provides the extended release of the active ingredient for long periods of time.

17 cl, 3 dwg, 5 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compositions for local application for the prevention and treatment of local eye pathologies, in particular inflammatory keratites and conjunctivitis and the dry eye syndrome, which contain as active ingredients polyunsaturated fatty acids of the omega-3 and omega-6 type, namely, EPA (eicosapentaenoic acid), DHA (docosahexaenoic acid) and GLA (γ-linolenic acid), mixed with vitamin E acetate and combined into a stable composition in a hydrogel, that is in the disperse form in a water solution, containing one or more gel-forming polymers. The claimed compositions are especially recommended for application as artificial tears.

EFFECT: invention provides an increased efficiency of the prevention and treatment of eye pathologies.

15 cl, 15 tbl, 3 dwg, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a percutaneously absorbable layer having a base and an adhesive layer which is placed on the base and which comprises an adhesive agent and a therapeutic ingredient. The adhesive agent contains a mixture of resins containing 100 portions by weight of an acrylic copolymer (A) and 0.1 to 30 portions by weight of an acrylic copolymer (B) or 0.05 to 2 portions by weight of a low-molecular polyamine compound having at least two amino groups in one molecule and non-polymerising with a polymer or an oligomer formed. The adhesive layer additionally contains an organic acid. The acrylic copolymer (A) represents an acrylic copolymer, which contains acrylic ester of (meth)acrylic acid as a main monomer ingredient and contains 3 to 45 wt % of diacetone acrylamide as a target monomer ingredient, but free from a free carboxylic group. The acrylic copolymer (B) represents an acrylic copolymer, which contains acrylic ester of (meth)acrylic acid as a main monomer ingredient and contains a primary amino group and/or carboxyhydrazidase group on side chains, but free from a free carboxylic group.

EFFECT: reducing the aging period of the adhesive layer considerably.

7 cl, 8 tbl, 39 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claim describes prolonged release formulations containing an active ingredient presented by octreotide or its pharmaceutically acceptable salt and three various linear polymers of poly(lactide-co-glycolic acid) (PLGA). The first PLGA has the lactide:glycolic acid relation of 65:35; the second PLGA has the lactide:glycolic acid relation of 75:25; the third PLGA has the lactide:glycolic acid relation of 85:15. The octrotide composition containing three various linear polymers of PLGA is characterized by the plasma octreotide concentration of low variability over the period of time making more than three months.

EFFECT: composition is applicable for the prolonged supporting therapy of the patients suffering acromegalia and for treating diarrhoea and congestions associated with malignant carcinoids and tumours producing vasoactive intestinal peptides (VIPoma-like tumours).

18 cl, 4 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: ulcer region is coated with macroporous hydrogel with the concentration of lightly cross-linked acrylic polymer 0.2-0.6 wt %, gel viscosity 45-85 poises at pH from 7.0 to 7.8. The wound floor is coated with a layer 2-4mm thick, and the wound edges - 1.5-3 mm, while a periulcerous region - 1-3 mm thick.

EFFECT: healing trophic ulcer 5-15 days later and no recurrence for 1-2 years as shown by patient's follow-up.

3 ex

FIELD: chemistry.

SUBSTANCE: group of inventions relates to a composite organic substance powder for use in medicine, a suspension for use in medicine in which the composite powder is dispersed in water and a method producing the composite powder. In the composite powder, the surface of particles of a poorly water-soluble crystalline organic substance are partially or completely coated with a carboxyvinyl polymer and the average diameter of particles coated with the carboxyvinyl polymer, obtained by calculating the BET specific surface is in the range of 50-400 nm. The method of producing the composite powder includes mixing a poorly water-soluble crystalline organic substance powder, a physiologically acceptable salt, a physiologically acceptable polyol and a carboxyvinyl polymer, pulverising the organic substance powder and removing the salt and the polyol after the pulverisation.

EFFECT: invention enables to obtain a medicinal preparation with a low degree of contamination with a pulverisation medium and with improved bioavailability.

6 cl, 8 dwg, 2 tbl, 38 ex

Abt-263 capsule // 2550956

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutics, in particular, described is a capsule, containing a capsule envelope, which includes an encapsulated liquid solution of N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)3-(morpholin-4-yl)-1-(phenylsulphanyl)methyl)propyl)-amino)-3-((trifluoromethyl)sulphonyl)benzenesulphonamide (ABT-263) or its bis-hydrochloride salts in a non-ethanol carrier. As filling agents used are: a phospholipid, a solubilising agent for the phospholipid, selected from glycols, glycolides, glycerides and their mixtures, a surface-active substance of a non-phospholipid type and a sulphur-containing antioxidant in an amount, effective for the reduction of oxidising ABT-263 degradation in storage. The sulphur-containing antioxidant is selected from sulphites, bisulphites, metabisulphites and thiosulphites and their mixtures. A method of the capsule obtaining is also described. The capsule is used for treating a disease, characterised by the overexpression of one or several anti-apoptotic proteins of the Bcl-2 family, for instance, cancer.

EFFECT: invention provides a long storage term for the said capsule.

33 cl, 3 dwg, 20 tbl, 14 ex

Up!