Rectal suppositories with analgesic action
SUBSTANCE: invention relates to medicine, in particular to drugs, and can be used for production of rectal suppositories for relieving of pain of various origin: postoperative pain, vertebrogenic radicular pain, arthritis, cancer pain, cardialgia, headache, dysmenorrhea, kidney and liver colics. Rectal suppositories proposed by authors have analgesic action and contain preparation of non-steroidal row and base, differing by fact, that preparation of non-steroidal row contains ketorolac and additionally contains amitriptyline, while base contains silicon glicerolates in 3-molar excess of glycerine composition Si(C3H7O3)4⋅3C3H8O3 and polyethylene glycol PEG-4000 with following ratio of components, calculated in g per one suppository: ketorolac 0.021÷0.031, amitriptyline 0.003÷0.008, PEG-4000 1.793÷1.804, silicon glicerolates 0.768÷0.773.
EFFECT: production of rectal suppositories.
1 cl, 2 tbl, 2 ex
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
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
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
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
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
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
SUBSTANCE: vaginal suppositories "Cervicon-DIM", containing diindolylmethane, are applied. The medication is applied for not less than 6 months in dosage 200 mg/day of diindolylmethane. The claimed method ensures durative anti-recurrence effect for not less than a year after the completion of the therapy, as well as stimulates the immune system, including general and local immunity of the vaginal mucosa.
EFFECT: invention contributes to the acceleration of epithelisation after carrying out destructive therapy concerning cervical intraepithelial neoplasia, makes it possible to reduce or eliminate the negative impact of side effects.
4 cl, 5 tbl, 5 ex, 2 dwg
SUBSTANCE: medication includes 7.0-9.0 wt % of a dried thick fraction of a product of hazel dry sublimation, 0.025-0.033 wt % of hydrochloride anaprilin, 36.0-38.0 wt % of sodium hydrocarbonate, 24.5-25.5 wt % of boric acid, 12.0-16.0 wt % of phthalic acid, 5.5-7.5 wt % of sodium carboxymethylcellulose, 0.8-1.0 wt % of sodium dodecylsulphate, 0.45-0.55 wt % of calcium stearate and 5.5-10.8 wt % of glucose.
EFFECT: invention increases the therapeutic and preventive efficiency of treatment of postnatal endometritis in cows and cow-heifers.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to an agent for treating hemorrhoid, proctitis and other proctologic inflammations. The above agent represents a suppository 1,35 - 3,65 g containing diosmin 0,3 - 0,65 g, dexpanthenol 0,05 - 0,2 g, green tea extract 0,05 - 0,2 g as active substances, and emulsifier 0,0135 - 0,1825 g and fatty acid glycerides as additives.
EFFECT: agent provides the integrated antimicrobial, local analgesic, anti-inflammatory, wound healing and adaptogenic therapeutic action.
2 cl, 3 ex
SUBSTANCE: suppositories, containing uniformly distributed in one suppository recombinant human interferon-alpha-2b in an amount of 400000-600000 IU and immunoglobulins IgA, IgM and IgG in an amount of 0.1-0.3 g, are additionally rectally introduced as the second medication to an adult patient in case of the long-term introduction of an opioid-containing medication. The dose constitutes 2-3 suppositories 2-3 times per day with the reduction of the daily dose by 1-3 suppositories in case of the reduction of pain sensation to 2-3 points by a ten-point scale and expressed sedation. If pain sensation increases to 6-8 points by the ten-point visual analogue scale, the daily dose is increased by 1-3 suppositories.
EFFECT: application of the claimed method makes it possible to ensure the prevention of the opioid dose increase and an increase of the level of antibodies to interferon-alpha in the patients' blood serum in case of the long-term application of opioids.
FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to intravaginal drug delivery system the above system (5) comprises at least one portion (1a and 1b), comprising an inner portion (2) with a cross-section diameter d2 equal to 2-10 mm, and a membrane (3) covering the inner portion, wherein the inner portion and the membrane substantially consist of the same polymer structure or various polymer structures. Besides, the intravaginal drug delivery system comprises a connector (6) permeable for a therapeutically active substances with the cross-section diameter d6 equal to 0.5-4.0mm for forming the continuous working drug delivery system. The present invention also refers to a method for making the above intravaginal drug delivery system.
EFFECT: invention provides the controlled release rate of the therapeutically active substances.
12 cl, 4 dwg, 4 ex
SUBSTANCE: agent contains the following per 1 suppository: 1.0 g glutaminic acid and 0.4 g of a 10% alcohol extract of propolis as active substances, as well as 2.0 g cacao oil, 0.15 g Cremophore CO-40 and 0.1 g PEG 400 as a base.
EFFECT: agent has high bioavailability, prolonged action, uniform release of active substances and a wide range of biological and medicinal activity.
2 cl, 1 dwg, 2 tbl, 9 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to the pharmaceutical industry, namely to an agent for treating haemorrhoid. The agent in the form of rectal suppositories for treating haemorrhoid containing 10% ethanolic extract of propolis, nicotinic acid, polyethylene glycol 1500 (PEG 1500), polyethylene glycol 4000 (PEG 4000), emulsifier T-2, Lutrol F68 and Cremophore CO-40 in certain proportions.
EFFECT: presented suppositories for treating haemorrhoid possess a wide spectrum of biological and therapeutic activities: they have the vasodilation action at the level of small vessels, improve microcirculation, promote the weak anticoagulant action, have the antioxidant, anti-edematous, spasmolytic, anti-inflammatory, regenerative and antibacterial action with the uniform release of active substances and the manifested prolonged action; they are easy to administrate with no assistance.
2 cl, 1 dwg, 2 tbl, 7 ex
SUBSTANCE: invention represents pharmaceutical composition for correction and therapy of manifestations of amyloid intoxication in patients with brain pathologies, which are characterised by the fact that it contains melatonin 3-10 mg and memantine 5-300 mg.
EFFECT: effective treatment of patients, including cases of moderate cognitive disorders.
4 cl, 2 ex, 6 tbl, 7 dwg
SUBSTANCE: invention represents an antifungal preparation in suppositories for children containing recombinant human interferon 2α and fluconazole, wherein lysozyme, Licopid and dimephosphone are additionally introduced.
EFFECT: preparation possesses the high clinical effectiveness in the fungal diseases in children that leads to reducing the length of treatment and prolonging the intercurrent period.
1 tbl, 3 ex
SUBSTANCE: invention relates to medication against HIV/AIDS transmission through sexual contact and to method of HIV-infection prevention by introduction of said medication. Medication is made in form of suppository, which includes active substance and pharmacologically acceptable base. As active substance used is fraction of humic acids, extracted from oxidised brown coal, which possesses anti-HIV activity. As base used is cocoa butter or hard confectionery fat and emulsifier. Medication is introduced intravaginally 30 minutes before sexual intercourse.
EFFECT: invention is aimed at creation of safe microbicide with anti-HIV activity based on substances, extracted from natural sources.
2 cl, 6 tbl, 7 ex
SUBSTANCE: invention relates to field of organic chemistry, namely to polymorphs of form 1 and form 2 of (-)trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolon-I-yl)-4-(1H-indol-3-yl)pyrrolidin-2,5-dione. Invention also relates to methods of obtaining said polymorphs and pharmaceutical composition on their basis.
EFFECT: novel polymorphs of (-)trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolon-I-yl)-4-(1H-indol-3-yl)pyrrolidin-2,5-dione are obtained, useful in cancer treatment.
23 cl, 26 dwg, 2 tbl, 27 ex