Lyophilized drug nanosuspensions

FIELD: pharmacology.

SUBSTANCE: present invention relates to a lyophilized (also known as freeze-dried) drug nanosuspension comprising of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile or its stereoisomeric form or its pharmaceutically acceptable salt and a steric stabiliser, which is a solid at room temperature, and polyvinyl pyrrolidone.

EFFECT: according to the present invention the composition of the lyophilized drug nanosuspension has an acceptable stability of grain-size composition in storage, including long-term storage.

25 cl, 6 dwg, 7 tbl, 2 ex

 



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new aminotetraline derivatives of formula (I) and their physiologically tolerable salts. In formula

,

A means a benzene ring or a ring specified in a group consisting of a 5-merous ring

,

R means the group R1-W-A1-Q-Y-A2-X1-; R1 means hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl-C1-C4-alkyl, halogenated C1-C6-alkyl, tri-(C1-C4-alkyl)-silyl-C1-C4-alkyl, C1-C6-alkoxy-C1-C4-alkyl, amino-C1-C4-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl, an optionally substituted phenyl, C1-C6-alkoxy, di-C1-C6-alkylamino, an optionally substituted 5 or 6-merous heterocyclyl containing 1-3 heteroatoms specified in nitrogen and/or oxygen or sulphur; W means a bond; A1 means a bond; Q means -S(O)2- or -C(O)-; Y means -NR9- or a bond; A2 means C1-C4-alkylene, or a bond; X1 means -O-, C1-C4-alkylene, C2-C4-alkynylene; R2 means hydrogen, halogen, or two radicals R2 together with the ring atom to which they are attached form a benzene ring; R3 means hydrogen. The other radical values are specified in the patent claim. The invention also refers to intermediate products for preparing the compounds of formula (I).

EFFECT: compounds possess the properties of glycine transporter inhibitors, particularly GlyT1 and can find application in treating neurological and psychiatric disorders, such as dementia, bipolar disorder, schizophrenia, etc or for managing pain related to glycerinergic or glutamatergic neurotransmission dysfunction.

20 cl, 2 tbl, 326 ex

FIELD: medicine.

SUBSTANCE: invention represents a pharmaceutical composition for treating the HIV infection in the form of a solid dosage form, containing at least one HIV protease inhibitor in a therapeutically effective amount specified in a group of nelfinavir, sacvinavir, tipranavir, darunavir, indinavir, ritonavir, lopinavir, palinavir or fosamprenavir, and pharmaceutically acceptable additives differing by the fact that as the pharmaceutically acceptable additives it contains at least one water-insoluble polymer from 0.39 to 28 wt % of the total dosage form, surfactants, excipients up to 100% of the total dosage form, as well as a method of treating the HIV infection.

EFFECT: pharmaceutical composition according to the invention possesses the improved technological properties and improved bioavailability as compared to a prototype therapeutic agent.

10 cl, 4 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, particularly to a composition for treating or preventing the human immunodeficiency virus (HIV) or hepatitis C. The herbal composition used for treating or preventing the patients infected by the HIV or hepatitis C viruses and containing a herbal ingredient with tannin agents and catechin, and a pharmaceutically acceptable carrier; the herbal ingredient is Agrimonia Eupatoria (GAFT) and/or gambier (Uncaria gambir). A method for preparing the herbal composition for treating or preventing the patients infected by the HIV or hepatitis C viruses.

EFFECT: composition is effective for treating or preventing the patients infected by the HIV or hepatitis C viruses.

12 cl, 6 dwg, 2 tbl

FIELD: medicine.

SUBSTANCE: invention relates to the field of biotechnology and cell technology. The claimed invention is aimed at the creation of pluripotent, multipotent and/or self-renewing cells, which are able to start differentiating in a culture into various types of cells and are capable of further differentiation in vivo. The claimed invention is also aimed at the creation of populations of the required differentiating cells, which can be transplanted to patients, genetic modification of endogenic cells and treatment of patients, suffering from diseases, intensity of which can be reduced by means of the said methods.

EFFECT: invention also claims methods of prevention, treatment or retardation of a disease, associated with an infection of immunodeficiency virus.

17 cl, 1 dwg, 13 ex

FIELD: medicine.

SUBSTANCE: invention refers to medical and molecular genetics. There are described genetic constructs expressing RNA sequences and genes coding proteins possessing the antiviral activity on human immunodeficiency virus. The genetic constructs contain a sequence coding the human TRIM5a modified protein. The invention can be used in scientific investigations.

EFFECT: presented constructs enable providing the higher expression of the modified gene of the human TRIM5a.

40 cl, 4 dwg, 3 tbl, 13 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a pharmaceutical composition in a tabletted dosage form which contains the first layer containing ritonavir and a polymer in a ratio of 1:1 - 1:6, and the second layer containing darunavir. The first layer is produced by hot extrusion, and the second layer - by direct extrusion or wet granulation. Also, the invention refers to a method for preparing the above pharmaceutical composition, and to a method of treating HIV or AIDS involving administering the above composition.

EFFECT: invention enables overcoming the incompatibility of ritonavir and darunavir, and also provides an optimum dissolution profile of both the active substances.

17 cl, 2 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a pharmaceutical composition for HIV-1 replication inhibition containing a compound of Formula

,

wherein n is equal to 1 or 2; Ar means phenyl substituted by one substitute specified in a group consisting of OH and NO2, or by two substitutes OR, or thienyl; R1 is specified in a group consisting of R6, C(O)N(R6)2, and C1-C6 alkyl substituted by OR; R2 means H or C1-C6 alkyl; R6 is independently in each specific case specified in H and C1-C6 alkyl; each R independently represents C1-C8 alkyl; or its pharmaceutically acceptable salt, or a compound 1G3, or its pharmaceutically acceptable salt. Also, the invention refers to a method of treating an individual either HIV-1 infected or suffering a high risk of HIV-1 infection involving administration of the above composition, to a method for HIV-1 virus replication inhibition.

EFFECT: what is prepared is the new pharmaceutical composition possessing effective biological properties 1G3.

11 cl, 6 tbl, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to improved method of obtaining pyridine compounds (AA),(BB) and (CC) of respective formulas:

,

,

.

said compounds possess inhibiting action with respect to HIV-integrase. method consists in carrying out the following stages: P-1) bromination of compound of formula (I-I) with obtaining bromine-compound of formula (II-II)

,

where value R represents -CHO, -CH(OH)2, -CH(OH)(OR4), -CH(OH)-CH2OH or -CH(OR5)(OR6); P1 represents benzyl; P3 represents H or protective group of carboxyl; R4 represents lower alkyl; R5 and R6 independently represent lower alkyl or R5 and R6 can represent alkyl and be connected with formation of 5-, 6- or 7-member ring, P-2) formation of side chain of 2,4-di-fluorophenyl-CH2-NH-C(O)- with application of reagents 2,4-di-fluorophenyl-CH2-NH2 and carbon monoxide, stage of formation of Q ring by means of respective amine, selected from 3-amino-butan-1-ol, 2-amino-propan-1-ol and 2-pyrrolidinyl methylamine, and stage of debenzylation with obtaining compound of formula (AA), (BB) or (CC), where said stage P-2 is carried out after formation of Q ring.

EFFECT: method makes it possible to simplify obtaining target compounds due to carrying out regioselective bromination at the first stage.

6 cl, 3 ex, 7 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to use of nucleoside derivatives - 1,2,5-oxadiazoles of general structural formula I where R1 and R2 are selected from phenylsulphonyl, substituted with one or more halogen atoms, nitro groups, carboxy groups, alkyl halides, CH3, OCH3, OCF3; X is selected from N or N→O; or R1 and R2 form a group, where R', R", R'" and R'''' are independently selected from hydrogen; halogens; nitro groups, hydroxy group, carboxy group, CH3; CH2Br; OCH3; phenylsulphonyl; phenylthio group; or the following groups: R' and R" can also be merged into one of the following common rings for inhibiting human immunodeficiency virus (HIV) replication. The invention also relates to a pharmaceutical composition based on compounds of formula I and a method of inhibiting HIV-1 subtypes A and B integrase, including forms which are resistant to raltegravir.

EFFECT: detecting novel activity in compounds of formula I, which can be used in medicine as HIV replication inhibitors.

3 cl, 5 tbl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula or , where Ar1 represents phenyl group, optionally substituted with one or several identical or non-identical halogen atoms; R1 represents hydrogen atom; R4, R5, R6a, R6b represent hydrogen atoms; Y, Z independently represent linear C1-4 alkylene group, optionally substituted with one linear C1-4 alkyl group; Ar2 stands for condensed with benzene 5-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, substituted with one linear C1-4 alkyl group, or derivative of 5- or 6-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, condensed with heteroaromatic 6-memebered ring, containing one or two nitrogen atoms, substituted with one linear C1-4 alkyl group, linear C1-4 alkoxygroup or group -NR7R8, where R7 and R8 independently stand for hydrogen atom, linear or branched C1-4 alkyl group, or R7 and R8 together with nitrogen atom form group of general formula , where R2, R3 represent linear C1-4 alkyl groups, A stands for group -CHR12, oxygen atom or group -NR9, where R12 and R9 stand for hydrogen atom or linear C1-4 alkyl group, m has value 1 or 2, n has value 1 or 2, o has value 0 or 1, p has value 0 or 1, Q stands for group -O-, group -N--H or group -N--CO-R10, where R10 stands for linear C1-4 alkyl group or -NH-R11 group, where R11 represents linear C1-4 alkyl group; and to their salts. Invention also relates to methods of obtaining therein and to based on them pharmaceutical composition, possessing antagonistic activity with respect to receptor CCR3.

EFFECT: obtained are novel compounds and based on them pharmaceutical compositions, which can be applied in medicine for obtaining medication, intended for treating asthma, allergic rhinitis, atopic dermatitis, eczema, inflammatory intestinal diseases, ulcerous colitis, Crohn's disease, allergic conjunctivitis, multiple sclerosis or HIV-infection and AIDS-associated diseases.

14 cl, 3 tbl, 26 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine and deals with histidine-trehalose composition, stable after storage, containing antibody T1h, histidine buffer, trehalose and non-ionic surface-active substance.

EFFECT: invention provides reduction of quantity of highly molecular weight proteins (HMWP) by approximately 20% by weight with respect to initial quantity of HMWP in histidine-trehalose composition within five weeks.

4 cl, 5 ex, 27 dwg

FIELD: medicine.

SUBSTANCE: pharmaceutical composition in form of lyophilisate for preparation of solution for parenteral application for tuberculosis treatment represents lyophilisate of prothionamide salt, which includes in composition additional substances, and in case of addition of pharmaceutically acceptable diluents is applicable for intravenous introduction. Pharmaceutical composition is obtained by dissolution of prothionamide substance in pharmaceutically acceptable acid, taken in equimolar ratio or with up to 20% excess, sterile filtering of solution, pouring in reservoirs and lyophilic drying. Finished medication is provided with pH corrector (sodium hydrocarbonate solution).

EFFECT: medication is stable in storage and is applied for preparation of solution for intravenous drip-feed.

9 cl, 2 ex

FIELD: medicine.

SUBSTANCE: pharmaceutical composition in form of lyophilisate with complexiant for preparation of solution for parenteral application to treat tuberculosis represents complex in form of prothionamide lyophilisate, which includes in composition water-soluble derivatives of β-cyclodextrine, and in case of addition of pharmaceutically acceptable diluent applicable for intravenous introduction. Pharmaceutical composition is obtained by dissolution of prothionamide substance in pharmaceutically acceptable acid (such as chloromethane, sulphuric, ascorbic, citric, etc.) in equimolar ratio or with up to 20% excess, obtaining complex with cyclodextrine derivative in equimolar ratio or with excess of cyclodextrine derivative up to 20%, sterile filtering of solution, pouring into reservoirs and lyophilic drying. As diluent applied is solution of sodium chloride, glucose and other pharmaceutically acceptable solutions. Finished medication is provided with pH corrector (sodium hydrocarbonate solution).

EFFECT: medication is stable in storage and is applied for preparation of solution for intravenous drip-feed.

11 cl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of lyophilisation of a composition, which contains purified antithrombin III (AT III) and a crystallised substance, selected from alanine, mannitol, glycine or NaCl. The claimed method includes freezing the composition at a temperature from -52°C to -60°C for 6-15 hours, annealing the composition at -30°C for 1 hour, re-freezing the composition at a temperature from -52°C to -60°C for 2-15 hours at keeping the product temperature between -48°C and -52.7°C for 4-10 before lyophilisation and drying the composition with obtaining a lyophilised cake. The invention also relates to a pharmaceutical set, which contains the said lyophilised cake and a liquid reagent.

EFFECT: invention provides obtaining the lyophilised composition, containing AT III, which preserves its activity and stability.

14 cl, 24 dwg, 5 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to pharmaceutics and medicine, and concerns protein and peptide stabilisation formulation which contains a hydrophilic polymer, a mixture of polyalcohol and sugar, wherein a weight ratio of polyalcohol to sugar makes from 2:1 to 5:1 (wt %), a detergent, and wherein the formulation is free from stabilising proteins. A composition and a kit for treating a disease or a composition caused by hyperactive cholinergic innervation of muscles or endocrine glands in a patient, and contain the above formulation and peptide, protein or a mixture thereof.

EFFECT: group of inventions provides the better protein stability in the absence of stabilising proteins.

13 cl, 4 ex

FIELD: chemistry.

SUBSTANCE: highly dispersive pharmaceutical composition contains from 5 to 100 mg of budesonide per 1 g of β-glycine. Composition is characterised by bulk density 0.008-0.035 g/cm3 and consists of porous spherical agglomerates with diameter to 50 mcm and separate fragments, formed in the process of destruction of agglomerates, which represent complex of joined into perforated layers separate particles. Composition is obtained by method, based on dispersing into tank with liquid nitrogen solutions of initial substances in mixed solvent tetrahydrofurane-water, in which concentration of tetrahydrofurane constitutes 20-25 wt %, solvents are removed from obtained by dispersion mixture of solid phases in dry nitrogen flow under pressure 100 Pa until pressure drop less than 2 Pa by step-by-step temperature increase in the interval from -196°C to -5°C to decompose clathrate hydrate formed in the system tetrahydrofurane-water and to remove components of used mixture of solvents by sublimation, then from -5°C to +30°C to remove residual moisture, with application of initial substances budesonide and α-glycine in mixed solvent tetrahydrofurane-water with ratio budesonide from 0.25 to 0.9 mg/g of solvent, α-glycine from 8 to 50 mg/g of solvent.

EFFECT: improved method of composition obtaining.

2 cl, 5 dwg, 2 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: as medications composition includes beclomethazone dipropionate and salbutamol, with beta-glycine serving as carrier. Composition is obtained by dispersing solutions of initial medications in mixed solvent into tank with liquid nitrogen with further removal of solvents from obtained by dispersion mixture solid phases in dry nitrogen flow under pressure 600±20 mtorr to pressure drop less than 8 mtorr with stopping nitrogen supply by step-by-step increase of temperature: in the interval from -196°C to -15°C, then from -15°C to +30°C. As initial substances used are: beclomethazone dipropionate 1.9-5.1 wt %, salbutamol 1.9-10.2 wt %, alpha-glycin to 100%. Composition of mixed solvent includes tetrahydrofurane 5-15 wt %, tert-butyl alcohol 15-5 wt %, water 77-80 wt %.

EFFECT: invention provides obtaining highly dispersed pharmaceutical composition of salbutamol and beclomethazone dipropionate.

2 cl, 10 dwg, 3 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of pharmaceutics and represents method of treating prostate cancer, which includes introduction to patient of composition, which contains degarelix lyophilisate or its pharmaceutically acceptable salt and excipient, dissolved in solvent, in initial dose 200-300 mg of degarelix in concentration 20-80 mg of degarelix per ml of solvent with the following after 14-56 days after initial dose supporting dose 320-55 mg of degarelix in concentration 50-80 mg of degarelix per ml of solvent, possibly with one or more than one following additional supporting dose 320-550 mg of degarelix in concentration 50-80 mg of degarelix per ml of solvent, introduced with interval from 56 days to 112 days between each supporting dose.

EFFECT: invention provides long release of degarelix from obtained depot of medication without increase of occurrence of side effects.

11 cl, 1 ex, 2 dwg, 4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to pharmaceutical compositions based on botulinum toxin and is intended for diagnostic or therapeutic introduction to a subject. A lyophilised or dried in vacuum composition contains botulinum toxin, stabilised with a non-protein excipient; a compound, selected from the group, consisting of the first monosaccharide, the first disaccharide, the first trisaccharide and the first alcohol, obtained by the reduction of the first monosaccharide; and a compound, selected from the group, consisting of the second monosaccharide, the second disaccharide, the second trisaccharide, the second alcohol and amino acid. In the other aspect the pharmaceutical composition contains botulinum toxin, stabilised with the non-protein excipient; polyethyleneglycol and a compound, selected from the group, consisting of monosaccharide, disaccharide, trisaccharide and amino acid. The pharmaceutical composition can contain botulinum toxin, stabilised with the non-protein excipient, polyvinylpyrrolidone; and disaccharide. The pharmaceutical composition of botulinum toxin, which does not contain an animal protein, includes botulinum toxin; a compound, selected from the group, consisting of the first monosaccharide, the first disaccharide, the first trisaccharide and amino acid.

EFFECT: application of the group of inventions provides the stable pharmaceutical composition for diagnostic or therapeutic introduction to a subject.

6 cl, 8 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: invention represents a medicinal preparation storage system comprising a chamber (3) accommodating at least two lyophilised active and/or additive substances (W1, W3, W5, W7) together in at least one chamber (3).

EFFECT: improving the system.

6 cl, 2 dwg

FIELD: medicine.

SUBSTANCE: group of inventions refers to medicine, namely to ophthalmology, and can be used for treating dry eye syndrome. That is ensured by administering an effective amount of a compound of formula I and/or II or its pharmaceutically acceptable salt form to a patient. What is also presented is a pharmaceutical composition.

EFFECT: group of inventions provides the effective treatment of dry eye syndrome in a patient by JAK path inhibition.

6 cl, 1 tbl, 10 ex

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