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Pharmaceutical composition containing chondroitin sulphate and/or hyaluronidase and liposome for local application |
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IPC classes for russian patent Pharmaceutical composition containing chondroitin sulphate and/or hyaluronidase and liposome for local application (RU 2473350):
Tapentadol for treatment caused by osteoarthrosis / 2473337
Claimed is application of tapentadol for manufacturing medication for treatment of pain caused by osteoarthrosis, in which at the beginning of treatment amount of taken in tapentadol is gradually increased in order to avoid side effects (titration from 25 mg two times per day to 200 mg two times per day).
Intracellular calcium modulating compounds / 2472791
Invention relates to compounds of formula (I): where: A, J, R1, R4, X, Z are given in claim 1, and to a pharmaceutical composition containing such compounds, which modulate activity of store-operated calcium (SOC) channels. The present invention also describes methods of using such SOC channel modulators to treat diseases or conditions where inhibition of activity of SOC channels can be beneficial.
Bicyclosulphonyl acid (bcsa) and use thereof as therapeutic agent / 2472784
Invention relates to bicyclosulphonyl acid (BCSA) compounds of formula: where: where each of -Rpw, -Rpx, -RPY, and -RPZ independently denotes H or -RRS1; each -RRS1 independently denotes -F, -Cl, -Br, -I, -RA1, -CF3, -OH, -OCF3 or -ORA1; where each RA1 independently denotes C1-4alkyl, phenyl or benzyl; and additionally, two neighbouring -RRS1 groups can together form -OCH2O-, -OCH2CH2O- or -OCH2CH2CH2O-; -RAK independently denotes a covalent bond, -(CH2)- or -(CH2)2-; -RN independently denotes -RNNN, or -LN-RNNN; the rest of the values of the radicals are given in claim 1, which act as inhibitors of inhibitors of tumor necrosis factor-α converting enzyme (TACE).
Method of treating arthritis / 2472509
Invention refers to medicine, namely to arthrology and therapy, and may be used for treating arthritis in a mammal A method consists in the fact that N-(4-(4-((4'-chlor(1,1'-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulphanyl)methyl)propyl)amino)-3-nitrobenzolsulphonamide is introduced into patient in need thereof.
Method of treating baker's cyst / 2470638
Invention refers to orthopaedics, namely rheumatology, and concerns treating Baker's cyst. That is ensured by cyst puncture, aspiration of its content, and introduction of the non-steroid anti-inflammatory preparation xefocam in its cavity; and then the enzymatic preparation longidaza is introduced in a paraarticular space.
1-cyanocyclopropyl derivatives as cathepsin k inhibitors / 2470023
Claimed invention relates to compounds of formula (I) where values of substituents are given in description, possessing inhibiting activity with respect to cathepsin K as well as to pharmaceutical compositions for treating diseases, associated with cysteine protease activity and to methods of inhibiting cathepsin K in mammals, requiring such treatment by introduction of efficient amount of compound to mammal.
Aminonicotinic acid and isonicotinic acid derivatives as dhodg (dihydroorotate dehydrogenase) inhibitors / 2469024
Present invention refers to new compounds of formula (I) and its pharmaceutically acceptable salts possessing dihydroorotate dehydrogenase inhibitory ability, to a based pharmaceutical composition, to application thereof in preparing a drug compound and to a combined preparation containing the presented compounds and the other active compound (I) in effective amounts wherein both groups G1 mean CRC, G2 mean a nitrogen atom or group CRd, of the groups G3 and G4 mean a nitrogen atom and the other one means group CH, M means a hydrogen atom or a pharmaceutically acceptable cation, while R1, R2, Ra, Rb, Rc and Rd have the values specified in the patent claim.
Method of treating inflammatory-degenerative arthropathies / 2468839
Invention refers to medicine, namely traumatology, orthopaedics and rehabilitation, and may be used for treating inflammatory-degenerative arthropathies. The therapy is three-staged. The first stage involves at least one course of the integrated therapy aiming at inflammatory response suppression and pain syndrome arrest. The second stage involves at least one session of focused extracorporeal shock wave therapy to create microcavities buried in a interarticular cartilage. At the third stage, the created microcavities buried in the interarticular cartilage are filled with a modelling compound by interarticular electrophoresis followed by stabilising the modelling compound. The modelling compound is represented by a mixture of 15 portions of fine biopolymer gel, 65 portions of hyaluronic acid, 15 portions of animal's articular cartilage extracts and 5 portions of Dimexidum solution. The modelling compound is stabilised by non-invasive exposure to pulse high-power IR laser at wave length 785 nm and heated to 44 Celsius degree.
New application of il-1β compounds / 2468817
Presented group of inventions refers to medicine. What is presented is application of IL-1β binding antigen for producing a drug preparation for treating juvenile rheumatoid arthritis in a patient, containing at least one antigen-binding centre which involves a first domain having an amino acid sequence specified in SEQ ID NO:1, and a second domain having an amino acid sequence specified in SEQ ID NO:2. What is presented is a pharmaceutical composition containing said antibody in a combination with pharmaceutically acceptable excipients, solvents or carriers introduced parenterally.
Composition for local use and its applications / 2467759
Claimed invention relates to pharmaceutical industry, in particular to composition for prevention or therapeutic treatment of inflammatory and/or degenerative condition. Composition for local application for prevention or therapeutic treatment of inflammatory and/or degenerative condition, including (i) woundwort or obtained from woundwort compound or its analogue or derivative, and (ii) tannic acid or its analogue or derivative. Method of prevention or therapeutic treatment of inflammatory and/or degenerative condition (versions). Application of composition for local application for production of medication for prevention or therapeutic treatment of inflammatory and/or degenerative condition. Set, including in two or more containers (i) tannic acid or its analogue or derivative and (ii) woundwort or obtained from woundwort compound or its analogue or derivative or any their combination. Set, including container, which includes composition for local application.
Composition for activated nanoparticles plga, loaded with active substance for targeted nanotherapy of cancer / 2473331
Claimed invention includes compositions and methods for obtaining activated polymer nanoparticles for targeted delivery of medication. Nanoparticle includes biocompatible polymer and amphiphilic stabilising agent, non-covalently bound with linker, which includes, at least, one elecrophile, selectively reacting with any nucleophile on targeting substance, and places targeting substance on external surface of biodegradable nanoenvelope, active substance being loaded into nanoenvelope. Biocompatible po;ymer includes one or several polyesters, selected from group, containing polylactic acid, polyglycolic acid, copolymer of lactic and glycolic acids and their combinations. Amphiphilic stabilising agent includes polyol. Active substance represents anti-cancer medication, preferably, curcumin.
Antituberculous composition and method for preparing it / 2472512
Invention refers to pharmaceutics and medicine and concerns a therpaeutic composition of antituberculous preparations with a phospholipid transport system consisting of fatty acid salt, herbal phosphatidylcholine (73-94%), maltose and an antituberculous agent specified in rifamycin, protionamide, rifabutin and rifapentine, and method for preparing it.
Pharmaceutical composition for treating cytostatic myelosuppression / 2471490
Invention refers to a pharmaceutical composition for treating cytostatic myelosuppression. The declared composition containing 0.4-4 wt % of oxidised dextran of molecular weight 35-70 kDa as a leukopoiesis stimulator, a liposome-forming agent - phosphatidyl choline in the amount of 1.0-4.0 wt %, a liposome stabiliser representing polyethylene glycol of molecular weight 1500-4000 Da in the amount of 0.4-4 wt % and a pharmaceutically acceptable excipient. The pharmaceutical composition may be presented in the form of a nanoliposome emulsion of liposome size 150-800 nm.
Pharmaceutical composition for treating alcoholism, drug addiction and chemical abuse with improved naltrexone release profile / 2471478
Invention refers to medicine and pharmacy, namely addictology and may be used for treating human addiction to alcohol, drugs and toxic substances. An intramuscularly injected prolonged-release pharmaceutical composition contains naltrexone as an active substance. Additionally, the composition contains a pharmaceutically acceptable solvent and excipients differing by the fact that the active substance is included in first and second microsphere fractions of polylactide coglycolide. The first microsphere fraction is characterized by the relation of lactide and glycolide monomer links 50 mole %:50 mole % and microsphere size 0.4 to 7 mcm. The second microsphere fraction is characterized by the relation of lactide and glycolide monomer links 75 mole %:25 mole % and microsphere size 20 to 90 mcm. A weight ratio of the first fraction of 0.01 to 0.15, while a weight ratio of the second fraction is 0.99 to 0.85.
Device for producing liposomal preparations / 2470624
Invention refers to biotechnology and may be used in medicine, cosmetology, veterinary science, plant growing etc. A device for producing liposomal preparations comprises a mixing chamber with a non-magnetic body which integrates magnetic working members total volume of which makes 0.5-4% of the volume of the mixing chamber; the body adjoins a system of electromagnetic coils connected to an alternating current source; inlet pipes are non-magnetic and inserted into a lower portion of a body of the mixing chamber, while an outlet pipe is provided at an upper portion of the body. An aqueous medium container and a lipid ingredient (a lipid solution in a water-soluble organic solvent) container are connected to the outlet pipes of the mixing chamber.
Pharmaceutical composition for transdermal application for increase of drug activity and decrease of side effects / 2469706
Phospholipid emulsion contains lecithin with the phosphatidylcholine content min. 60%, ethanol, water and diclofenac sodium in the amounts specified in the patent claim. The phospholipid emulsion represents liposomes (nanosomes) of a mean diameter of 20 to 500 nm. The composition is used for the liposomal introduction of biologically active substances and/or drugs into a human body. The emulsion nanosomes may additionally contain one or more substances specified in a group: carotinoids, flavonoids, vitamins, resveratrol, vitamin-like substances, cartilage protectors, amino acids, preserving agents.
Method and composition for treatment of inflammatory disorders / 2468797
Invention relates to homogenous pharmaceutical composition for treatment of inflammatory disorders, which contains mixture of steroid anti-inflammatory or anti-histamine active ingredient in pharmaceutically acceptable water carrier with liposome. As steroid anti-inflammatory ingredient used is budesonide or fluticasone or their pharmaceutically acceptable salt, and antihistamine preparation is represented by azelastine or its pharmaceutically acceptable salt, concentration of active ingredient in water carrier is, in fact, equal inside and outside liposomic structures and varies ±20% when concentration of active ingredient inside and outside liposomic structures is compared. Polar lipid is swellable in water and represents phospholipid or glycosphingolipid. Invention also relates to method of composition obtaining, which lies in joint mixing of polar lipid, water phase and said active ingredient and mixture homogenising. Invention also relates to method of treating inflammatory disorders, including introduction of claimed composition to individuum, suffering from or sensitive to said disorders.
Nucleic acid complex and composition for nucleic acid delivery / 2465009
Group of inventions refers to medicine and represents a complex of nucleic acid and strongly branched cyclic dextrin representing glucan of a degree of polymerisation 50-5000, containing an internal branched cyclic structural fragment formed by alpha-1,4-glucoside bonds and at least one alpha-1,6-glucoside bonds and an external branched structural fragment bound to the internal branched cyclic structural fragment. The group of inventions also involves a composition containing of the diacylphosphatidylcholine, at least one compound specified in cholesterol, and a primary aliphatic amine, as well as the use and the method for cell delivery.
Stable crystalline chloride modifications dotap / 2463291
Invention refers to enantiomerically pure (2S)- or (2R)-N,N,N-trimethyl-2,3-bis[[(9Z)-1-oxo-9-octadecenyl]oxy]-1-propanamide chloride (DOTAP chloride) which possess the transfection properties and can find application in medicine and pharmaceutics for intracellular transportation of pharmaceutically active compounds. The invention also refers to a pharmaceutical composition and the use of enantiomerically pure (2S)- or (2R)-DOTAP chloride as an ingredient for preparing drugs.
Phospholipid nanoform for oral application (sachet) and method for preparing it (versions) / 2463057
Invention refers to medicine, pharmacology and concerns an oral granulated dosage form in sachets containing phospholipids in the form of particles of small (20-30 nm) diameter, glycyrrhizic acid and its salt (including sodium glycerrhizinate), as well as carbohydrate (including maltose) and excipients (granulation, anti-clotting and powder), as well as to a method for preparing it by mixing fat and water phases of herbal phospholipids and acceptable carbohydrate to prepare an emulsion, cooling to 50°C and passing through a microfluidiser for 4-5 cycles under pressure 2000 atm.
Ointment for treating bitten wounds / 2473329
Invention relates to pharmaceutical industry, to creation of wound-healing ointment. Ointment for treatment of bitten wounds includes lidocaine hydrochloride, sea-buckthorn oil, water-free lanolin, medicinal purified Vaseline, metronidazole, clindamycin, rifampicin and trombolisin.
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FIELD: medicine, pharmaceutics. SUBSTANCE: present invention refers to medicine, namely to a pharmaceutical composition for local application. The composition contains chondroitin sulphate, hyaluronidase, glucosamine hydrochloride, liposome and pharmaceutically acceptable carriers and excipients in the amounts specified in the patent claim. The composition may additionally contain capsaicin. EFFECT: pharmaceutical composition according to the invention is characterised by fast skin penetration of the ingredients. 3 cl, 4 ex
The present invention relates to medicine, namely to pharmaceutical compositions for topical application containing chondroitin sulfate and/or hyaluronidase and liposomes. Recently, liposomes are most often used as carriers for various biologically active substances such as vitamins, antibiotics, fruit acids and other in medicine. In the range of liposomal drugs are ointments, creams and gels for the treatment of various diseases. Chondroitin sulfate is a structural analogue of hyaluronic acid of natural origin and has contractualism, moisturizing, regenerating and anti-inflammatory action. Chondroitin sulfate stimulates the biosynthesis glucosamine, slowing degeneration in the cartilage tissue, promotes regeneration of the cartilage surfaces of the joints, increases mobility of joints and muscles, promotes skin hydration. Liposomes can be single layer or multilayer, can have different sizes. Components of liposomal membranes can be charged lipids (PA, dipalmitoylphosphatidyl acid, phosphatidylserine, diacetilactis or its acetate, stearylamine, dimyristoylphosphatidylcholine-glycerol), sterols - cholesterol and its esters, isoprenoids, tocopherol, fatty acid, glycolipid is (gangliosides and cerebrosides), and also, under certain conditions, some proteins, diazotrophy alcohol (Abstract. Development of the basic biotechnological production processes and quality management system lipid cosmetic products http://www.fos.ru/biology/7369_1.html). The known properties of liposomes, described in the article "LIPOSOMES" (LIEBERSON. LIPOSOMES - Sorovskie educational journal, No. 10, 1998, retrieved from the Internet 10.11.2011, <URL:http://www.pereplet.ru/nauka/Soros/pdf/9810_002.pdf) on page 5 indicates that the inclusion of drugs in liposomes can significantly improve their therapeutic efficacy (left column, second paragraph from the bottom). It also indicates that the problem of drug delivery to the desired location can be solved by topical application of liposomal drugs. Known drug Lydasum is a drug containing hyaluronidase. Hyaluronidase found in the various tissues of the body, causes the breakdown of hyaluronic acid to glucosamine and glucuronic acid, and thereby reduces its viscosity, increases the permeability of the tissue and provides the movement of fluids in the interstitial spaces. Describes the use of lidz (in combination with anti-inflammatory drugs) in rheumatoid arthritis by electrophoresis: 64 UE lidz was dissolved in 30 ml of distilled water was added 4-5 drops of 0.1 molar hydrochloric KIS is the notes and was injected with a forked electrode (anode) on two of the joint. The drug is available in powder form in vials of 64 ITEMS. Known gel Assawan™, which consists of: escin, "essential" phospholipids and heparin sodium salt and used phlebitis, thrombophlebitic and hemorrhoids (Mashkovsky PPM Medicines. - 15-ed., Rev., Corr. and extra - M.: New Wave, 2006. - s-462). Known ointment handaxe™containing chondroitin sulfate and dimethyl sulfoxide, which is used in degenerative diseases of joints and spine (arthrosis, osteochondrosis), as well as bruises, contusions and sprains. Also known cream Artrozan containing chondroitin sulfate, plant extracts and vitamins, which is used with the aim of gradual resorption of excess deposits of calcium salts, reduce pain and restore joint mobility. The disadvantage of these tools is that they do not have a high absorbability. Well-known cosmetic composition, which comprises chondroitin sulfate, hyaluronidase, liposomes (of unknown composition), for the implementation of transepidermal migration of chondroprotective, extracts of juniper, the Martini (EN 2004121471 A, 10.01.2006) for daily care of skin with the purpose of regeneration and hydration. From RU 2376011 C1-known remedy for the treatment of peripheral joints and allow the student with an active transdermal migration of several protective agents, such as chondroitin sulfate, glucosamine hydrochloride and acetylglucosamine. At the same time more effective transdermal transport is achieved through the use of liposomal concentrate containing phospholipids of soybean. Pharmaceutical compositions containing chondroitin sulfate and/or hyaluronidase, and liposomes for topical use are not described. Thus, the present invention is to create a pharmaceutical composition for topical application containing chondroitin sulfate and/or hyaluronidase and liposomes with rapid penetration through the skin. According to the present invention proposed a pharmaceutical composition for topical application containing chondroitin sulfate and/or hyaluronidase and pharmaceutically acceptable carriers or excipients, characterized in that it further comprises liposomes. However, the rapid penetration through the skin is ensured not only by the liposomes, and hyaluronidase. As liposomes can be used Dragosomes® (Symrise) representing bilayer liposomes with a diameter of 200 nm on the basis of cholesterol and lecithin, as well as Corneosphere® (Kobo) in the form of structured multilayer liposomes based on hydrogenated lecithin and modified amylopectin. As the preferred waples is of the claimed invention proposed pharmaceutical composition, above, additionally containing glucosamine hydrochloride. Most preferred is a pharmaceutical composition, which has the following composition, wt.%:
As one of the preferred embodiments of the claimed invention proposed pharmaceutical composition specified above, optionally containing capsaicin. Most preferred is a pharmaceutical composition, which has the following composition, wt.%:
The technical result of the present invention to provide a pharmaceutical composition based on chondroitin sulfate and/or hyaluronidase and liposomes, which has the ability to rapidly penetrate the skin and, accordingly, rapid absorption. Hyaluronidase increases tissue permeability and enhances the action of liposomes and chondroitin sulfate. Additional advantages are ease of application and ease of dispensing. The pharmaceutical composition of the present invention are generally made by using common methods, using solid or liquid pharmaceutically acceptable carriers or excipients selected from emulsifiers, dispersing agents, preservatives, flavoring agents, pH regulators, polymeric carriers and other excipients, which are suitable for preparation of compositions for local application. The pharmacy is practical composition of the present invention can be prepared in the form of a gel, creams, ointments and the like. The rapid penetration through the skin due to the binding of chondroitin sulfate with liposomes containing hydrogenated lecithins in combination with cholesterol. In the first preferred embodiment of the composition based on chondroitin sulfate and/or hyaluronidase and liposomes additionally contains glucosamine hydrochloride, which reinforces the main effect of chondroitin sulfate and linking hyaluronidase with liposomes ensures the stability of the enzyme, in addition, hyaluronidase increases tissue permeability and improves penetration of the components of the composition. In another preferred embodiment the composition is based on chondroitin sulfate and/or hyaluronidase and liposomes additionally contains capsaicin, which has more distracting distracting effect and helps to reduce pain, vasodilatation and improve the penetration of the components of the composition. The present invention is illustrated by the following examples. EXAMPLE 1 Pharmaceutical composition in the form of a cream based on chondroitin sulfate and/or hyaluronidase and liposomes has the following composition:
The above composition is prepared by the following method. In demineralized water by heating to 80°C mix: chondroitin sulfate, carbomer, emulsifier, glucosamine hydrochloride, then cooled to 30°C and add liposomes, hyaluronidase and preservative. The resulting homogenized cream and vacuum. EXAMPLE 2 Farmacevticheskaja composition in the form of a cream based on chondroitin sulfate and/or hyaluronidase and capsaicin has the following composition: /tr>
The above composition is prepared as in EXAMPLE 1, characterized in that it additionally uses capsaicin, which is added during the cooling of the cream in a random order. The resulting homogenized cream and vacuum. EXAMPLE 3 Evaluation of stability of hyaluronidase in compositions for local application Since the main drawback of enzymes is their instability during long-term storage of finished dosage forms based on them within the expiration date was the comparative assessment of the conservation activity of hyaluronidase during storage in solution and in the form of a composition for topical use (for example cream). The hyaluronidase activity was determined by the following method. 2 tubes were made in 0.5 ml of water was added in the first 0.1 ml, and the second 0.2 ml of substrate hyaluronic acid. In each tube was made of 0.1 ml of 1%solution of bovine serum albumin (BSA, M=67000 Yes) firm "Serva" (With The A) and added 0.2 ml of 15%aqueous solution of acetic acid. For a working dose took the minimum number of substrate, forming a clearly defined mutiney clot adding acetic acid. The results are shown in the following table.
As can be seen from the table, the introduction of the enzyme hyaluronidase in compositions for topical application allows to obtain a stable pharmaceutical composition for local application. Despite the fact that with the introduction of this enzyme in the composition of these songs is a minor loss of enzyme activity, etc is further stored for 1 year hyaluronidase does not change its activity. EXAMPLE 4 Study of the pharmaceutical composition with chondroitin sulfate and liposomes on the ability of rapid penetration into the skin. For this purpose, we compared the ability of rapid skin penetration composition according to the present invention on the basis of chondroitin sulfate and a control composition containing chondroitin sulfate without liposomes. The tests were carried out on rabbits. The above composition was applied on the inner surface of the rabbit ear. Absorption was determined by the amount of chondroitin sulfate, remaining on the skin of the rabbit after 10 minutes after application of the compositions, expressed in percentage of the initial amount of chondroitin sulfate in the composition. Results: the control composition is 50% of the remaining chondroitin sulfate; the composition of the present invention is 10% of the remaining chondroitin sulfate. Thus, the pharmaceutical composition according to this invention has the ability to rapidly penetrate the skin, providing a more rapid manifestation of therapeutic effect of the active substances of the composition. 1. Pharmaceutical composition for topical application, haraktrizuyutsya the fact that it contains chondroitin sulfate, hyaluronidase, glucosamine hydrochloride, liposomes and a pharmaceutically acceptable carriers and excipients in the following autosizecomponents, wt.%:
2. The pharmaceutical composition according to claim 1, characterized in that it further comprises capsaicin. 3. The pharmaceutical composition according to claim 2, characterized in that it has the following composition, wt.%:
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