New pharmaceutical composition containing nsaid and cyclodextrin

FIELD: medicine.

SUBSTANCE: invention refers to medicine and consists in liquid composition for treating sore throat, containing 1–5 % wt/vol. of flurbiprofen; 5–10 % wt/vol. of cyclodextrin; up to 5 % wt/vol. of buffer agents and 80–90 % wt/vol. of water.

EFFECT: technical result consists in physically and chemically pure stable solution of flurbiprofen of sufficient concentration, solution has no undesirable taste and does not contain alcohol as auxiliary solvent.

21 cl, 5 ex, 2 tbl, 5 dwg

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to a novel chemical substance - 4,10-bis((±)-5-benzoyl-2,3-dihydro-1H-pyrrolo[1,2-a]pyrrole-1-carbonyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,03,11,05,9]dodecane The invention also relates to a method of its obtaining, which consists in the acylation of 2,6,8,12-tetraacetyl-2,4,6,8,10,12- hexaazatetracyclo [5,5,0,03,11,05,9]dodecane by chloranhydride 5-benzoyl-2,3-dihydro-1H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid.

EFFECT: novel compound, which has analgetic activity, is obtained.

2 cl, 1 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to novel heterocyclic compounds of general formula (I) or enantiomers, diastereomers or pharmaceutically acceptable salts thereof, where Y is: phenyl or a heteroaryl selected from thiazolyl, pyridyl, pyrimidinyl, 1,3,5-triazinyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl and 1,3,4-thiadiazolyl; wherein the phenyl or heteroaryl is optionally substituted with one substitute selected from fluorine, chlorine, bromine, iodine, C1-4alkyl, trifluoromethyl, C1-4alkoxy, C1-4alkylthio, nitro and cyano; r=1-2; R2 is absent or is an oxo-group; Z is: (a) phenyl substituted with NRaRb; where Ra is: H or C1-4alkyl; where Rb is: C1-4alkyl, cycloalkyl, phenyl, furanylmethyl, or phenyl(C1-2alkyl); and wherein the phenyl or the furanyl are optionally substituted with iodine; alternatively, Ra and Rb are taken together with the nitrogen atom to which they are bonded to form a 5-8 member heterocyclyl, which is optionally condensed to a benzene ring; (b) biphenyl-3-yl or biphenyl-4-yl; where the interior phenyl ring, attached to the carbonyl in formula (I) is optionally substituted with a fluorine atom; and where the terminal phenyl ring is optionally substituted with a substitute selected from trifluoromethyl, C1-4alkoxy, chlorine, dichloro, fluorine, and iodine; (c) phenyl substituted with a substitute selected from C5-8cycloalkyl, -NHC(=O)cyclohexyl, phenyloxy, phenylcarbonyl, phenyl(C1-3)alkyl, phenyl(C1-3)alkoxy, pyrrolyl, pyrazolyl, imidazolyl, isoindol-2-yl-l,3-dione, 2,3-dihydro-isoindol-2-yl; l-(tert- butoxycarbonyl)piperidin-4-yloxy, and 1-(tert-butoxycarbonyl)piperidin-4-yl; (d) phenyl substituted with 1-2 substitutes independently selected from: C1-6alkyl, C1-4alkoxy, iodine, chlorine and nitro; (e) phenyl(C1-2)alkyl; where the phenyl is optionally substituted with 1 or 2 substitutes independently selected from iodine, fluorine, C1-6alkyl, phenyl and NRcRd; where Rc: H or C1-4alkyl; where Rd is: C1-4alkyl or C1-6cycloalkyl(C1-4)alkyl; and where the C1-2alkyl of phenyl(C1-2)alkyl is optionally substituted with phenyl; (f) phenyl(C2-4)alkenyl; where the phenyl is optionally substituted with a substitute selected from C1-4alkyl, C1-4alkoxy, trifluoromethyl, trifluoromethylthio and phenyl; (g) naphthyl; where the naphthyl is optionally substituted with one C1-4alkoxy substitute; (h) fluorenyl or xanthenyl; where the fluorenyl or xanthenyl is optionally substituted with an oxo group; (i) C5-8cycloalkyl; where the C5-8cycloalkyl is optionally substituted with one C1-6alkyl substitute; (j) benzene ring-condensed C5-8cycloalkyl or benzene ring-condensed C5-8cycloalkyl(C1-4)alkyl; where said C5-8cycloalkyl fragment is optionally substituted with 1-4 methyl groups; (k) bicyclo[2.2.2]octyl-1-yl; where the bicyclo[2.2.2]octyl-l-yl is optionally substituted with C1-6alkyl; (1) a heteroaryl or benzene ring-condensed heteroaryl selected from benzooxazolyl, quinolinyl, benzimidazolyl, pyridinyl, indolyl, thienyl, furanyl, pyrazolyl, oxazolyl, benzothienyl and benzofuranyl; where the heteroaryl or benzene ring-condensed heteroaryl is optionally substituted with 1 or 2 substitutes independently selected from C1-4alkyl, trifluoromethyl, C5-8cycloalkyl, phenyl, phenyl(C1-2)alkoxy, phenyl(C2-4)alkynyl and dichlorophenoxy; and where the phenyl substitute in the heteroaryl is further optionally substituted with C1-4alkyl, C1-4alkoxy or trifluoromethyl; (m) l,5-diphenyl-lH-pyrazol-3-yl; where the pyrazol-3-yl is optionally substituted with a methyl group; and where each of the phenyl groups of the 1,5-diphenyl substitutes is also optionally substituted with substitutes selected from chlorine, dichloro or aminosulphonyl; (n) 1,2,3,4-tetrahydroquinolin-6-yl; where the 1,2,3,4-tetrahydroquinolin-6-yl is optionally substituted with phenyl or trifluoromethyl-substituted phenyl; and (o) benzene ring-condensed heterocyclyl(C2-4)alkenyl; where the benzene ring-condensed heterocyclyl is attached to the C2-4alkenyl via the benzene ring; and where benzene ring-condensed heterocyclyl is further optionally substituted with C5-6cycloalkyl; taking into account constraining conditions indicated in claim 1. The invention also relates to a pharmaceutical composition based on the compound of formula (I), a method of producing said pharmaceutical composition, a method of treating said pathological conditions and use of the compound of formula (I).

EFFECT: obtaining novel heterocyclic compounds having MGL inhibiting activity.

21 cl, 5 tbl, 11 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents a pharmaceutical composition for control of pain accompanying individual's joint diseases containing hyaluronic acid, which is cross-linked by cycling a double bond in a group of cinnamic acid in partially amidated hyaluronic acid presented by formula (1) to form a cyclobutane cycle, wherein in the above formula, Ar represents a phenyl group, n is equal to an integer 2 or 3; HA represents a carboxy residue of hyaluronic acid, and m represents a relation of amidation of hyaluronic acid to all the carboxyl groups and is equal to 3-50% in relation to all the carboxyl groups, and a pharmaceutically acceptable carrier, wherein the pharmaceutical composition represents a product for injection, wherein the pharmaceutical composition represents the product for injection, wherein the amount of the cross-linked hyaluronic acid makes 1 wt % at the total amount of the product for injection, wherein a single dose of the product for injection makes 2-3 ml, wherein the pharmaceutical composition represents a single-use preparation, which is administered every 13 weeks and more.

EFFECT: invention provides the extremely long analgesic action after the single administration, earlier onset of the analgesic action.

15 cl, 1 dwg, 5 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely to a method for preparing a medicinal product possessing choleretic activity. The medicinal product possessing choleretic activity and prepared by extracting an elevated part of Lomatogonium carinthiacum in 96% ethanol twice at room temperature, them in 40% ethanol with an extractant added in an amount equal to a discharged one, twice; the filtered aqueous-alcoholic extracts are combined; the extraction cake is extracted in purified water; the aqueous extract is filtered; the aqueous residues of the aqueous-alcoholic extracts are combined with the aqueous extract, concentrated, dried in a vacuum drying cabinet to produce the dry extract in the certain environment.

EFFECT: medicinal product prepared as described above possesses the evident choleretic activity.

11 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: using a polyphenolic complex produced by extracting milled ash berry in 40% ethanol, condensing the alcohol-water extract, adding 95% ethanol, centrifuging the residue, filtering and condensing the supernatant in the certain environment, as an agent possessing anti-inflammatory action.

EFFECT: polyphenolic complex possesses pronounced anti-inflammatory action.

1 dwg, 9 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical composition, containing compound of formula or for prevention or treatment of diseases, associated with oxidative stress, selected from group, consisting of MELAS (mitochondrial myopathy, encephalopathy, lactic acidosis and stroke episodes), MERRF syndrome (myoclonic epilepsy with ragged red fibres) or Kearns-Sayre syndrome, arrhythmia, cardioplegia or myocardium infarction. in formula (1) na stands for 1 or 2, Aa represents 5-membered heteroaryl or heterocycle, each of which has 2 heteroatoms, selected from N, O and S, Rla represents R5a-Xa-Ba-X′a-, Ba represents direct bond, Xa and X′a independently on each other represent direct bond or -OC(O)-, R5a represents hydrogen or 6-9-membered monocyclic or condensed cyclic heterocycle or heteroaryl, each of which has from 1 to 3 heteroatoms, selected from N, O and S, and is optionally substituted with oxo or C1-C6-alkyl, R2a represents -(CR8aR9a)pa-Ya-R7a, pa stands for number from 0 or 1, Ya represents direct bond or -O-, R7a represents hydrogen or phenyl, R3a, R8a, R9a, R10a represent hydrogen, R4a represents -(CH2)pa-Da-R10a-, Da represents C5-cycloalkyl or 6-membered heterocycle, which has 1 heteroatom, selected from N, S and O. Radical values for formula (2) are give in invention formula.

EFFECT: obtaining compositions for prevention or treatment of diseases, associated with oxidative stress.

19 dwg, 5 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing 9-aryl-6,8,20-trioxa-13-azapentacyclo-[11.8.0.01,10.02,7.014,19]heneicosa-9,14,16,18-tetraene-11,12,21-triones (IIa-d), which includes reacting 3-aroyl-1H-pyrrolo[2,1-c][1,4]benzoxazine-1,2,4-triones (Ia-d) with 3,4-dihydro-2H-pyran in a medium of an inert aprotic solvent, followed by separation of the end products. In general formula (I) Ar=Ph (a, d), C6H4Br-4 (b), C6H4OMe-4 (c), R=H (a-c), Cl (d).

EFFECT: obtaining 9-aryl-6,8,20-trioxa-13-azapentacyclo-[11,8,0,01,10,02,7,014,19]heneicosa-9,14,16,18-tetraene-11,12,21-triones.

2 cl, 1 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention refers to a new compound, namely to 2-[(2-methylphenyl)imino]-9-oxo-7-phenyl-8-(3-phenyl-2-quinoxalinyl)-1,6-dioxaspiro[4,4]none-3,7-diene-3,4-dicarboxylic acid dimethyl ester of formula possessing antinociceptive activity, and a method for producing it consisting in synthesis of 4-(3-phenylquinoxalin-2-yl)-5-phenylfurane-2,3-dione, acetylene dicarboxylic acid dimethyl ester and o-methylphenylisonitrile.

EFFECT: preparing the new compound.

2 cl, 1 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound, represented by the following formula

,

or its pharmaceutically acceptable salt. In claimed formula each symbol has values, determined in formula of invention. Versions of formula [I] compound and particular compounds are also objects of invention. In addition, invention relates to pharmaceutical composition, ITK inhibitor and means for treatment or prevention of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection and other diseases and methods of treating said diseases.

EFFECT: claimed compounds inhibit induced T-cellular kinase (ITK).

32 cl, 86 tbl, 387 ex

FIELD: medicine.

SUBSTANCE: application of a compound of the general formula 1 or its spatial isomers as analgesic means is claimed.

EFFECT: compounds have high efficiency, low toxicity, can be applied in medicine.

4 tbl 8 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely represents a method for the therapy of respiratory symptom. The method involves administering a liquid composition containing a gel former and/or a mucoactive polymer, a non-menthol cooling substance; and contacting the oral mucosa with the liquid composition. The invention also describes liquid compositions applicable in the method for the therapy of a respiratory disease.

EFFECT: implementing the method provides improving the cooling properties of the cooling agent N-(4-cyanomethylphenyl)-n-menthane carboxamide in the liquid composition by combining the non-menthol cooling substance with the gel former.

14 cl, 2 tbl, 5 dwg

FIELD: medicine.

SUBSTANCE: treating tonsillopharyngitis in children is ensured by Panavir Inlight spray gel 1 oropharyngeal irrigation 2 times a day after meal daily for 5 days.

EFFECT: method enables treating more effectively by the anti-viral and cytoprotective action of the preparation, reducing a toxic load with no complications and applicability.

4 ex

FIELD: medicine.

SUBSTANCE: pathogenetic treatment of chronic tonsillitis and/or hypertrophy of palatine tonsils in preschool children suffering from lymphoproliferative syndrome is ensured by the palatine tonsils debridement. An interleukin-1β(IL-1β) level is measured in the palatine tonsils washing. If the measured value is less than 5.8 pg/ml, recombinant interleukin-1β (IL-1β) is to be administered orally by phonophoresis with the use of the Tonsillor MM apparatus. Two courses of 10 procedures every 14 days are performed. The clinical effectiveness is assessed if observing a positive dynamics of IL-1β measured in the palatine tonsils washing 17 and 41 days after the beginning of the immunomodulatory therapy.

EFFECT: higher clinical effectiveness ensured by the differentiated selection of children for carrying out the immunomodulatory therapy, reducing a rate of infectious involvements of the palatine tonsils in the declared group of patients by the pathogenetically reasoned application of recombinant IL-1β.

3 cl, 2 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: palatal tonsils are daily sanitated with antibacterial preparations selected in accordance with the bacteriological examination of oral smears for pathogenic microflora and antibiotic sensitivity with the tonsil lacunae washed for 10 days. Pre-anaesthesia is followed by the tonsil lacunae exposure to an ultrasonic disintegrator at a depth of a probe working area at an amplitude of 23-26 mc every second day for 5 days. That is followed by paratonsil administration of polyoxidonium in an adult dose of 6 mg every second day for 5 days; the therapeutic course is performed once a year.

EFFECT: method enables higher clinical effectiveness in chronic tonsillitis.

2 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to a composition for treating throat pain in the form of dispersible tablets. The claimed composition contains an endothermic cooling substance, representing xylitol, in an amount of 1-10 wt/wt % and an active substance, which contains menthol and 2,4-dichlorobenzyl alcohol and amylmetacresole.

EFFECT: invention ensures relief of symptoms, associated with throat pain, and ensures a cooling effect.

5 cl, 1 tbl

FIELD: medicine.

SUBSTANCE: method involves drug and irrigation therapy, laser therapy covering a sub-mandibular region; the novel is that drug therapy represents administering the hydrogel sterile material 'Coletex-gel-DNK-L' or 'Coletex-gel-ADL' 1-3 ml into each tonsil lacunas. Laser therapy additionally covers a projection of the common carotid artery, the carotid sinus, internal and external jugulars, the vagus nerve and the upper cervical sympathetic ganglion; these regions and the sub-mandibular region are pre-coated with the sterile textile tissue 'Coletex-AND' or 'Coletex ADL'. The exposure is performed in the infrared band series from both sides at a frequency of 1000 to 1500 Hz, output power 10 to 20 mW, length of exposure 2 to 8 min; after the procedure, the used tissue is left for 6-8 hours; the course consists of 3-10 daily procedures.

EFFECT: sequence of therapeutic procedures enables regaining a structural balance of the immune regulation that provides the central determination of eliminating the immunological reactivity disorders specific for children suffering chronic tonsillitis, eliminating manifested autonomic nervous system imbalance, providing the higher clinical effectiveness.

FIELD: medicine.

SUBSTANCE: starch or sorbite photosensitiser powder is administered into a laryngeal pharynx that is further exposed to laser light. The laser light exposure is performed at wave length 0.685 mcm, powder 18-20 mWt, energy density 18-28.8 J/cm2.

EFFECT: implementing the method provides the reliable laryngeal fixation of the photosensitiser, maintains the constant concentration of the photosensitiser for the whole therapeutic session, and thereby faster reduction of the inflammatory process.

2 cl, 4 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely otorhinolaryngology, phoniatrics and physiotherapy and may be used for the integrated treatment of aggravated chronic laryngitis. Starting from the 4-5th day from the aggravation, a standard drug therapy is additionally combined with an endolaryngeal injection of specific pyobacteriophague 1 ml and further exposure to low-frequency vibration covering 3 fields of the larynx and phonopaedic breathing exercises. The low-frequency vibration starts at a first filed comprising side neck surfaces at frequency 20 Hz per 1 filed with a vibratode advanced smoothly upward at 2-3 mm/sec with undisplaced skin and rectangularly up to a mandibular angle, and then downwards to a posterior triangle of neck for 1-2 minutes from each side; the patient does the phonopaedic breathing exercises and pronounces expiratory 'M'; that is followed by the vibrational exposure covering a projection of intersection of a thyroid cartilage plate and a border of sternocleidomastoid muscle (m.sternocleidomastoideus) at a thyroid cartilage notch at frequency 40 Hz and 60 Hz for 1-2 minutes from both sides according to the stable technique; the patient does the phonopaedic breathing exercises and pronounces expiratory vowels 'U', 'O', 'A'; that is followed by vibration of a collar at frequency 30-40 Hz with the vibratode advanced from a paravertebral line to a shoulder joint for 2-3 minutes from each side; the technique is labile. The course performs 8-10 combined daily procedures.

EFFECT: method enables higher clinical effectiveness ensured by the integrated effect on the patient's immune system in a combination with the drainage, anti-inflammatory, and trophic stimulating effects.

11 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, and aim at treating compensated non-specific chronic tonsillitis. A method involves a stress-protective therapy, a diet therapy, a vitamin therapy, a probiotic therapy, an antioxidant therapy, a therapy with prebiotic-like drugs, a local immunocorrecting and topical eradication therapy.

EFFECT: method is high effective in treating compensated non-specific chronic tonsillitis; it provides normalising an epigenetic regulation of gene expression and oxidation-reduction processes in the human body, creating conditions for relieving the micro-environmental disorder and recovering a colonisation resistance of the upper airway mucosa, an eradication of bacterial and viral infectious agents with underlying recovering an eubiosis of the upper airway mucosa, normalizing the gastrointestinal function, blocking the lipopolysaccharide effects of gram-negative bacteria, eliminating the aggravations within one year completely in the majority of patients.

9 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, namely to a method for preparing a therapeutic hydrogel material involving mixing an aqueous solution of sodium alginate and a drug preparation, dispersing a cross-linking agent that is presented by calcium sulphate in glycerol in the concentration of 0.8-2.5%, mixing the dispersion with the prepared mixture of sodium alginate with the drug preparation in ratio 1-2:4-6, placing the prepared product into a tiling pattern and keeping it till form-stable, conducting gamma sterilisation; the formation process involves the mechanical stability measurements with the diametral compression of the formed hydrogel; the hydrogel is considered to be formed once a thickness of the formed hydrogel varies with the diametral compression by 10-30%.

EFFECT: invention provides the wider medical variation of the drug concentrations, preparing high-thixotropy soft hydrogel materials (tablets) easy to administer, including through rectum, preparing the materials that preserve its all their physical-technical and mechanical properties after the gamma sterilisation along with the sterility.

4 cl, 10 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents a pharmaceutical composition for control of pain accompanying individual's joint diseases containing hyaluronic acid, which is cross-linked by cycling a double bond in a group of cinnamic acid in partially amidated hyaluronic acid presented by formula (1) to form a cyclobutane cycle, wherein in the above formula, Ar represents a phenyl group, n is equal to an integer 2 or 3; HA represents a carboxy residue of hyaluronic acid, and m represents a relation of amidation of hyaluronic acid to all the carboxyl groups and is equal to 3-50% in relation to all the carboxyl groups, and a pharmaceutically acceptable carrier, wherein the pharmaceutical composition represents a product for injection, wherein the pharmaceutical composition represents the product for injection, wherein the amount of the cross-linked hyaluronic acid makes 1 wt % at the total amount of the product for injection, wherein a single dose of the product for injection makes 2-3 ml, wherein the pharmaceutical composition represents a single-use preparation, which is administered every 13 weeks and more.

EFFECT: invention provides the extremely long analgesic action after the single administration, earlier onset of the analgesic action.

15 cl, 1 dwg, 5 tbl, 1 ex

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