The method of obtaining crystalline cyclosporine in resolutional orthorhombic form

 

(57) Abstract:

The essence of the invention, the transfer crystalline cyclosporine in resolutionyou orthorhombic form. Process conditions: in a solvent with molm more than 200. ensure its dissolution at elevated temperature. 3 Taba

 

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FIELD: medicine, pharmacy.

SUBSTANCE: invention proposes new tablets with size less 3 mm with sustained-releasing the opioid analgesic drug for 30 min in the amount above 75%. Invention provides opioid for oral intake with taking into account individual necessity of patient due to selection of required amount of mictotablets by dispenser.

EFFECT: valuable properties of tablet, expanded assortment of medicinal formulations of opioid analgesics.

19 cl, 4 tbl, 4 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention proposes new tablets with size less 3 mm with sustained-releasing the opioid analgesic drug for 30 min in the amount above 75%. Invention provides opioid for oral intake with taking into account individual necessity of patient due to selection of required amount of mictotablets by dispenser.

EFFECT: valuable properties of tablet, expanded assortment of medicinal formulations of opioid analgesics.

19 cl, 4 tbl, 4 ex

FIELD: pharmacy.

SUBSTANCE: invention relates to pharmaceutical compositions in the form of cellular mechanically stable, lamellar, porous, spongy or foam-like structures and to a method for their preparing from solutions and dispersions. Method involves carrying out the following stages: a) preparing a solution or homogenous dispersion liquid and compound taken among the group including one or some pharmaceutically active compounds, one or some pharmaceutically acceptable additives and their mixtures, and the following stage b) foaming solution or homogenous dispersion at reducing pressure 30-150 torrs without boiling. Invention provides stabilizing the composition.

EFFECT: improved preparing method.

38 cl, 4 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a tablet decomposing rapidly in the buccal pocket and comprising a medicinal agent, excipient and saccharide with relatively lower melting point than that of a medicinal agent and excipient. Tablet is made by uniform mixing saccharide with low melting point with tablet mass to form bridge between particles of named medicinal agent and/or excipient through melting product followed by hardening mentioned saccharide with low melting point. Except for, invention relates to a method for making tablet decomposing rapidly in buccal pocket and comprising a medicinal agent, excipient and saccharide with relatively lower melting point than that of medicinal agent and excipient. Method involves: (a) the parent components of tablet comprising a medicinal agent, excipient and saccharide with relatively lower melting point that that of a medicinal agent and excipient are pressed under low pressure to provide the required tablet form; (b) pressed product obtained after stage (a) is heated to temperature when saccharide with low melting point is melted; (c) melted product obtained after stage (b) is cooled to temperature when melted saccharide with low melting point is hardened. Invention represents a tablet decomposing rapidly in buccal pocket and having the tablet strength providing its using in tablet-making machines for dosed formulations and giving the possibility for making tablet using common tablet-making machines, and to a method for making tablets. Except for, invention represents a tablet decomposing rapidly in buccal pocket being this table as compared with common tablets has enhanced tablet strength and improved frangibility without prolonged decomposing time in buccal pocket, and a method for tablet making.

EFFECT: improved making method.

63 cl, 4 tbl, 1 dwg, 21 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention describes sterile anesthetic composition for parenteral administration of propofol emulsified in water for injection. The composition comprise above 3 wt.-% but 6 wt.-% of less of solvent not mixing with water. Propofol is dissolved in indicated solvent. The composition is stabilized with 0.2-1.0 wt.-% of surface-active substance and has pH value level in the range 5.0-7.5. The composition with reduced pH value level allows preventing above 10-fold elevating growth of microorganisms for at least 24 h after random external pollution. Reduced fat content in composition also provides the stable analgetic effect for prolonged time and with reduced risk for the blood fat content exceeding.

EFFECT: improved and valuable properties of composition.

15 cl, 4 dwg, 4 tbl, 3 ex

FIELD: medicine, hematology, pharmacy.

SUBSTANCE: invention relates to the composition of factor VIII composed without addition of albumin and comprising the following excipients of composition in addition to factor VIII: from 4% to 10% of filling agent taken among group consisting of mannitol, glycine and alanine; from 1% to 4% of stabilizing agent taken among group consisting of sucrose, trehalose, raffinose, arginine; from 1 mM to 5 mM of calcium salt, from 100 mM to 300 mM of NaCl, and buffer agent for pH value maintenance about between 6 and 8. Alternatively, the composition can comprise from 2% to 6% of hydroxyethylstarch; from 1% to 4% of stabilizing agent taken among group consisting of sucrose, trehalose, raffinose, arginine; from 1 mM to 5 mM of calcium salt, from 100 mM to 300 mM of NaCl, and buffer agent for pH value maintenance between 6 and 8. In additional variant of realization of invention the composition can comprise: from 300 mM to 500 mM of NaCl, from 1% to 4% of stabilizing agent taken among group consisting of sucrose, trehalose, raffinose and arginine; from 1 mM to 5 mM of calcium salt, and buffer agent. The composition provides stability in the absence of albumin or other proteins.

EFFECT: valuable properties of compositions.

35 cl, 11 tbl, 7 ex

FIELD: biotechnology, veterinary medicine.

SUBSTANCE: invention relates to the development of biological preparation for prophylaxis and treatment of colibacillosis (escherichiosis) and for control of carriage of escherichious infections pathogens in animals and poultries also. Also, invention can be used in producing curative fodders and ecologically pure human foodstuffs. Biopreparation for prophylaxis and treatment of escherichiosis in animals and poultries comprises strains of bacteriophages Phagum Escherichia coli Ec022-DEP and/or Phagum Escherichia coli Ec021-DEP, and/or Phagum Escherichia coli Ex0782-DEP, and/or Phagum Escherichia coli Ec0781-DEP, and/or Phagum Escherichia coli EPZ-1-DEP, and/or Phagum Escherichia coli EPZ-2-DEP, and/or Phagum Escherichia coli EG-5-DEP, and/or Phagum Escherichia coli BC-1-DEP, and/or Phagum Escherichia coli M78-DEP, and/or Phagum Escherichia coli Sheksna 2k-DEP taken in the effective amount. The biopreparation comprises also antiseptic, for example, quinosol and a stabilizing agent. Protein (for example, soybean protein), vegetable meal, organic polymer, milk, serum, albumin can be used as a stabilizing agent. Among organic polymers can be used: dextran, polyglucin, starch, polyvinylpyrrolidone. The biopreparation can be dried by lyophilization, granulated and placed in polymeric matrix. The biopreparation has no toxic properties on animals, it shows good hygroscopicity and can be good dispersed in water. The biopreparation can be used in liquid and dry prescription formulations and in different methods of its administrations: both by subcutaneous, intraperitoneal, intramuscular injections and as an aerosol, by administration of phage particles into lung compartments including applying as curative fodder and supplement to fodder, and by applying on surface of cutaneous integuments. Invention provides enhancing the effectiveness of treatment of animals and poultries with gastroenteric infections due to reducing treatment period, expanding spectrum of lytic effect of the biopreparation, resistance to effect of digestive tract enzymes and convenience in using.

EFFECT: valuable veterinary properties of biopreparation.

9 cl, 5 tbl, 7 ex

FIELD: biotechnology, veterinary medicine.

SUBSTANCE: invention relates to the development of biological preparation for prophylaxis and treatment of colibacillosis (escherichiosis) and for control of carriage of escherichious infections pathogens in animals and poultries also. Also, invention can be used in producing curative fodders and ecologically pure human foodstuffs. Biopreparation for prophylaxis and treatment of escherichiosis in animals and poultries comprises strains of bacteriophages Phagum Escherichia coli Ec022-DEP and/or Phagum Escherichia coli Ec021-DEP, and/or Phagum Escherichia coli Ex0782-DEP, and/or Phagum Escherichia coli Ec0781-DEP, and/or Phagum Escherichia coli EPZ-1-DEP, and/or Phagum Escherichia coli EPZ-2-DEP, and/or Phagum Escherichia coli EG-5-DEP, and/or Phagum Escherichia coli BC-1-DEP, and/or Phagum Escherichia coli M78-DEP, and/or Phagum Escherichia coli Sheksna 2k-DEP taken in the effective amount. The biopreparation comprises also antiseptic, for example, quinosol and a stabilizing agent. Protein (for example, soybean protein), vegetable meal, organic polymer, milk, serum, albumin can be used as a stabilizing agent. Among organic polymers can be used: dextran, polyglucin, starch, polyvinylpyrrolidone. The biopreparation can be dried by lyophilization, granulated and placed in polymeric matrix. The biopreparation has no toxic properties on animals, it shows good hygroscopicity and can be good dispersed in water. The biopreparation can be used in liquid and dry prescription formulations and in different methods of its administrations: both by subcutaneous, intraperitoneal, intramuscular injections and as an aerosol, by administration of phage particles into lung compartments including applying as curative fodder and supplement to fodder, and by applying on surface of cutaneous integuments. Invention provides enhancing the effectiveness of treatment of animals and poultries with gastroenteric infections due to reducing treatment period, expanding spectrum of lytic effect of the biopreparation, resistance to effect of digestive tract enzymes and convenience in using.

EFFECT: valuable veterinary properties of biopreparation.

9 cl, 5 tbl, 7 ex

FIELD: agriculture, animal husbandry, organic chemistry.

SUBSTANCE: antiseptic ointment comprises cationic surface-active substance, lower glycols, polyethylene glycols, water and ethylene glycol monophenolic ester and higher polyethylene glycols taken in the definite ratio of components. As cationic surface-active substance ointment comprises N-alkyl-N-alkoxycarbonylmethylhexahydroazipinium chloride or alkyldimethylbenzylammonium chloride, or cetylpyridinium bromide, or cetylpyridinium chloride, or 1,2-ethylenebis-(N-methylcarbdecyloxymethyl)ammonium dichloride, or ethylhexadecyldimethylammonium chloride, or chlorhexidine; as lower glycol ointment comprises 1,2-propylene glycol or polyethylene glycol-300, or polyethylene glycol-400; as higher polyethylene glycol ointment comprises polyethylene glycol-1500 or polyethylene glycol-3000, or polyethylene glycol-4000, or polyethylene glycol-6000. Ointment elicits the high antibacterial activity, broad spectrum of bactericidal effect and low irritating effect with respect to udder skin. Invention can be used for sanitary-hygienic treatment of udder of lactating cows for prophylaxis and rapid healing external damages of udder and nipples (arising cracks), prophylaxis of mastitis, enhancing milk purity by microbiological indices.

EFFECT: valuable antiseptic properties of ointment.

2 cl, 1 tbl, 22 ex

FIELD: pharmacology, fluorinated quinolone-based drug, in particular ofloxacine for injections.

SUBSTANCE: claimed composition contains therapeutically acceptable amount of ofloxacine and trilon-B, sodium chloride, water for injections as additives.

EFFECT: high therapeutic effectiveness; non-crystallized active agent for a long-time storage.

1 ex

FIELD: biochemistry.

SUBSTANCE: method relates to new cyclopeptides of general formula cyclo(R1-Arg-Ile-Lys-Pro-His-R2) selected from group containing: P11: cyclo(DPhe-Pro-Gln-Ile-Met-Arg-Ile-Lys-Pro-His-Gln-Gly-Gln-His-Ile-Gly-Glu) (SEQ ID NO:5), P16: cyclo(Arg-Ile-Lys-Pro-His-Gln-Gly (SEQ ID NO:8), P17: cyclo(Pro-Arg-Ile-Lys-Pro-His-Gln-Gly) (SEQ ID NO:9), P19: cyclo(Gln-Ile-Met-Arg-Ile-Lys-Pro-His-Gln-Gly-Gln-His-Ile-Gly-Glu) (SEQ ID NO:10), P20: cyclo(Dphe-Pro-Gln-Ile-Met-Arg-Ile-Lys-Pro-His-Gln-Gly-Gln-His-Ile-Gly) (SEQ ID NO:11), P23: cyclo(DPhe-Pro-Arg-Ile-Lys-Pro-His-Gln) (SEQ ID NO:13), P24: cyclo(Gly-Arg-Ile-Lys-Pro-His) (SEQ ID NO:25), as well as P11, P20 and P23 with DPhe substituted by DTyr. Cyclopeptides are useful in systems for angiogenesis inhibition. System includes substrate with cyclopeptides attached by organic spacer arm optionally containing group cleavable by any fermentation system.

EFFECT: angiogenesis inhibiting cyclopeptides.

23 cl, 4 dwg, 2 tbl, 2 ex

FIELD: organic chemistry, amino acids.

SUBSTANCE: invention proposes agonists of somatostatin of the formula (I): X-A1-cyclo-(D-Cys-A3-A4-Lys-A6-A7)-A8-Y or its pharmaceutically acceptable salt wherein X represents hydrogen atom (H); A1 represents L-Cpa, L-Phe, L-Trp or L-Nal; A3 represents L-3-Pal or L-4-Pal; A4 represents D-Trp; A6 represents -NH-(CHR1)n-CO- wherein n = 2, 3 or 4; A7 represents L- or D-Cys; A8 represents D- or L-isomer of amino acid taken among the group consisting of Nal, Phe, Cpa and Trp; Y represents NH2; R1 represents hydrogen atom (H), and Cys in A3 is bound by disulfide bong in A wherein this disulfide bond is formed by thiol groups of each Cys residue.

EFFECT: valuable biological properties of compounds.

9 cl, 2 ex

FIELD: organic chemistry, polypeptides.

SUBSTANCE: invention relates to new antagonists of urotensin-II. Invention represents group of cyclic polypeptides of the general formula: (R1)a-AA1-cyclo-[AA2-AA3-AA4-AA5-AA6-Cys]-AA7-R2 wherein AA1 means L-isomer of aromatic amino acid; AA2 means L- or D-isomer of Cys; AA3 means L-isomer of aromatic amino acid; AA4 means L- or D-isomer of Trp; AA5 means L- or D-isomer of Lys, N-Me-Lys or Orn; AA6 means L- or D-isomer of Val, Thr, Leu, Ile, Tle, Nle or aromatic amino acid; AA7 means L- or D-isomer of Val, Thr, Leu, Ile, Tle, Abu, Nle or aromatic amino acid; R1 means hydrogen atom (H), lower alkyl, lower alkanoyl or lower acyl; a = 1 or 2; R2 means hydroxyl; group (OH), OR3, N(R3)2 or NHR3 wherein R3 means H, lower alkyl or arylalkyl. These cyclic polypeptides are used as antagonists of urotensin-II.

EFFECT: valuable biological properties of compounds.

24 cl, 1 tbl, 2 ex

FIELD: medicine, hormones, chemistry of peptides.

SUBSTANCE: invention describes compound of the formula: cyclo-[{4-NH2-C2H4-NH-CO-O-)-Pro}-Phg-D-Trp-Lys-Tyr-(4-Bzl)-Phe] being not obligatory in protected form, or its pharmaceutically acceptable salt of complex. Compound possesses the inhibitory activity on release of the growth hormone and insulin.

EFFECT: valuable medicinal properties of peptide.

9 cl, 2 ex

FIELD: chemical technology.

SUBSTANCE: invention relates to variants of a method for synthesis of a mixture (E)- and (Z)-isomers of ISATX247. By one variant acetyl-ciclosporin is heated with the first compound chosen from group consisting of triarylphosphine, trialkylphosphine, arylalkylphosphine and triarylarsine for preparing an intermediate substance that is stirred with the second compound chosen from group consisting of acetaldehyde, formaldehyde, deuterium-labeled formaldehyde, 2-chlorobenaldehyde and benzaldehyde. Mixture of (E)- and (Z)-isomers of acetyl-1,3-diene is prepared that is treated with a base and mixture of (E)- and (Z)-isomers of ISATX247 is prepared. Other variant for preparing mixture of (E)- and (Z)-isomers of ISATX247 represents interaction of acetyl-ciclosporin A aldehyde that is prepared by oxidation of acetyl-ciclosporin A, with phospholide by Wittig reaction followed by treatment of the prepared mixture with a base. Also, invention relates to a method for synthesis of mixture of (E)- and (Z)-isomers of ISATX247 enriched with E-isomers or Z-isomer, and to a method for synthesis of the preliminary assigned isomeric mixture of (E)- and (Z)-isomers of ISATX247 by mixing materials enriched with (E)- and (Z)-isomers.

EFFECT: improved method of synthesis.

77 cl, 7 tbl, 16 dwg, 39 ex

FIELD: chemistry.

SUBSTANCE: invention concerns biochemistry, particularly biologically active peptides with stress-protection effect, which can be applied in medicine and pharmaceutics. The invention extends the range of safe substances stress resistance of an organism to include cyclopeptides I and II featuring the following aminoacid sequence: Cyclo(Gly1-Lys2-Val3-Leu4-Lys5-Lys6-Arg7-Arg8)n, where n = 2-3.

EFFECT: extension of the range of safe substances enhancing stress resistance of an organism.

5 tbl, 5 ex

FIELD: chemistry, pharmacology.

SUBSTANCE: invention relates to compositions, that include isomers mixture of cyclosporine A analogue, modified by 1,3-diene substitute in 1st amino acid residue, where isomers represent isomers E- and Z-: , . Invention also relates to compositions application in medicine production, and to method of immunosuppression realization.

EFFECT: pharmaceutical compositions have immunosuppressive activity.

77 cl, 7 tbl, 17 dwg, 39 ex

FIELD: medicine.

SUBSTANCE: method provides interaction of cells of a medullary carcinoma of a thyroid gland with agonist SSTR2 representing bond of the formula of cyclo [Tic-Tyr-D-Trp-Lys-Abu-Phe].

EFFECT: reduction of rate of proliferation of cells of thyroid gland medullary carcinoma.

3 cl, 8 dwg, 2 tbl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention refers to the method for preparation of the cyclic somostatin analogues of formula I and to the intermediates used in the claimed method. The method is implemented by the cyclisation of somostatin having formula II where R1 is -C2-C6 alkylene -NR3R4, R3 and R4 independently of each other are H or acyl, R2 is , where R5 is phenyl, R11 and R12 independently of each other are amino protective groups. If R1 contains the amino end-group the latter is also protected with amino protective group, if necessary the amino protective group(s) is (are) eliminated and thus obtained compound of formula I is reduced in free or salt form.

EFFECT: improvement of method for preparation of somostatin peptides.

6 cl, 4 ex

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