Compositions for treating neoplastic diseases

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely to a solid pharmaceutical composition for oral administration on the basis of taxane. The solid pharmaceutical composition for oral administration contains amorphous taxane, a hydrophilic carrier and a surfactant (sodium dodecylsulphate (SDS)), with specific weight proportions of taxane and the carrier with taxane, the carrier and the surfactant found in a solid dispersion. The use of the composition for preparing a drug for treating a neoplastic disease. A method for preparing the pharmaceutical composition.

EFFECT: pharmaceutical composition is characterised by higher solubility and higher dissolution rate of taxane.

16 cl, 21 dwg, 18 tbl, 5 ex

 

The text descriptions are given in facsimile form.

1. Solid pharmaceutical composition for oral administration containing amorphous Texan, hydrophilic carrier and a surfactant, with Texan, carrier and surfactant are in the form of a solid dispersion, and the weight ratio taxane to carrier is between 2.5:97.5 weight./weight. and 15:85 wt./weight.

2. To the position according to claim 1, characterized in that the amorphous Texan obtained using the method of solvent evaporation or lyophilization method.

3. The composition according to claim 1, characterized in that the medium is selected from polyvinylpyrrolidone (PVP), polyethylene glycol (PEG), polyvinyl alcohol (PVA), crosspovidone (PVP-CL), copolymer of polyvinylpyrrolidone and polyvinyl acetate (PVP-PVA), methyl cellulose, hydroxypropylcellulose, karboksimetiltselljulozy, azettftalat cellulose phthalate of hydroxypropylmethylcellulose; polyacrylates, polymethacrylates, sugars, polyols, and their polymers, such as mannitol, sucrose, sorbitol, dextrose, and chitosan; and cyclodextrins.

4. The composition according to claim 1, characterized in that the medium is selected from polyvinylpyrrolidone (PVP) and cyclodextrin.

5. The composition according to claim 1, characterized in that the medium is selected from PVP-R17, PVP-K25, PVP-K30, PVP-K60, PVP-K90 and PVP K120.

6. The composition according to claim 1, characterized in that the surfactant is a sodium dodecyl sulphate (SDS).

7. The composition according to claim 1, characterized in that the weight ratio taxane to carrier is between about 2.5:97.5 weight./weight. and about 1:9 weight./weight.

8. The composition according to claim 1, characterized in that the weight ratio taxane to carrier is between about 5:95 wt./weight. and about 1:9 weight./weight.

9. The composition according to claim 1, characterized in that the amorphous Texan receive is by lyophilization.

10. The composition according to claim 9, characterized in that the amorphous Texan obtained by lyophilization of a solution taxane in a capsule for oral administration.

11. The composition according to claim 1, characterized in that it further comprises an inhibitor of CYP3A4.

12. The composition according to p. 11, characterized in that the inhibitor of CYP3A4 represents ritonavir.

13. The composition according to claim 1, characterized in that taxon represents docetaxel.

14. Composition according to any one of claims 1 to 13 for use in therapy.

15. The use of a composition according to any one of claims 1 to 13 for the preparation of drugs for the treatment of neoplastic disease.

16. A method of obtaining a composition according to any one of claims 1 to 13, comprising the stage of:
dissolution taxane, hydrophilic polymer carrier and a surfactant in a solvent, with the weight ratio taxane to carrier is between 2.5:97.5 weight./weight. and 15:85 wt./weight.;
and lyophilization solution or the application of the method of evaporating the solvent to the solution to obtain a composition.



 

Same patents:

FIELD: medicine.

SUBSTANCE: what is involved is simulating moderate growth inhibition of tumour and metastases in Lewis lung carcinoma with prolonged cyclophosphanine-induced leukopenia in mice by intraperitoneal introduction of cyclophosphane in 1/3 ADR - 3 times, 83.3 mg/kg each on 6th, 12th and 18th post-transplantation days. On the 3rd day after each introduction, peripheral blood is analysed (total leukocyte count, leukogram) - the lowest WBC count is determined. The clinical effectiveness is assessed at the end of the experiment on the 21st post-transplantation day as shown by tumour weight, a percentage of growth inhibition, a metastasis rate, the number of lung metastases, a metastasis inhibition index.

EFFECT: new biological model of carcinoma with comorbid prolonged leukopenia enables weighing the contribution of substances of different nature to the anti-cancer clinical effectiveness and to the elimination of white blood cell toxicity when the above substances are included into the therapy.

1 ex, 1 tbl

FIELD: medicine.

SUBSTANCE: what is involved is simulating moderate growth inhibition of tumour and metastases in Lewis lung carcinoma with prolonged cyclophosphanine-induced leukopenia in mice by intraperitoneal introduction of cyclophosphane in 1/3 ADR - 3 times, 83.3 mg/kg each on 6th, 12th and 18th post-transplantation days. On the 3rd day after each introduction, peripheral blood is analysed (total leukocyte count, leukogram) - the lowest WBC count is determined. The clinical effectiveness is assessed at the end of the experiment on the 21st post-transplantation day as shown by tumour weight, a percentage of growth inhibition, a metastasis rate, the number of lung metastases, a metastasis inhibition index.

EFFECT: new biological model of carcinoma with comorbid prolonged leukopenia enables weighing the contribution of substances of different nature to the anti-cancer clinical effectiveness and to the elimination of white blood cell toxicity when the above substances are included into the therapy.

1 ex, 1 tbl

FIELD: biotechnologies.

SUBSTANCE: single-thread RNA is described with common formula G1XmGn or C1XmCn, which is modified with lipid. The single-thread RNA may act as immunogen, inducing the inherent immune response. The pharmaceutical composition is described. The invention may be used to treat infectitious diseases, allergies or cancer diseases.

EFFECT: improved composition properties.

22 cl, 15 dwg, 24 ex

FIELD: chemistry.

SUBSTANCE: disclosed are anti-5T4 antibodies, nucleic acids which encode variable regions of such antibodies, antibody/drug conjugates, a method of delivering a drug using such a conjugate, as well as a method of treating a subject with cancer which is characterised by 5T4 antibody expression, by administering the disclosed conjugate.

EFFECT: present invention can further be used in therapy of 5T4-associated diseases.

42 cl, 8 ex, 15 tbl, 15 dwg

FIELD: chemistry.

SUBSTANCE: disclosed is a single-chain multi-specific binding protein for binding or modulating activity of one or more biding partner molecules. The protein contains from the N-terminal to the C-terminal: a first binding domain derived from variable regions of a light and a heavy immunoglobulin chain; a constant sub-region derived from immunoglobulin containing a hinge or hinge-like domain, a CH2-domain and a CH3-domain; scorpion linker peptide, where said peptide contains an amino acid sequence from the immunoglobulin hinge or a type II C-lectin protein stalk region; and a second binding domain derived from variable regions of a light and a heavy immunoglobulin chain. The invention describes an encoding nucleic acid, as well as an expression vector based thereon and a host cell for vector based protein expression. The invention discloses a pharmaceutical composition for treating cell proliferation disorders based on a single-chain protein and a protein dimer for binding or modulating activity of one or more binding partner molecules based on two single-chain binding proteins.

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31 cl, 61 dwg, 14 tbl, 19 ex

FIELD: chemistry.

SUBSTANCE: disclosed are peptides which are isolated from the FOXM1 protein and are capable of activating cytotoxic (killer) human T cells by forming an antigen-presenting complex with a HLA-A2 molecule. Disclosed are compositions which contain the disclosed peptides, use of a peptide to produce an agent for inducing cancer immunity, treating and preventing cancer, and for producing antibodies which selectivity bind the disclosed peptides. The invention describes an exosome and an isolated antigen-presenting cell, which present a complex of the disclosed peptide with a HLA-A2 molecule, for inducing cytotoxic T cells, methods of inducing a antigen-presenting cell and a cytotoxic T cell, as well as a method of damaging FOXM1 and HLA-A2 expressing cells.

EFFECT: invention can further be used in treating tumours that are characterised by high FOXM1 expression.

14 cl, 2 ex, 1 dwg, 1 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to a novel azacytidine analogue of formula (I): where R is H, R5C(O); R1 is or where the crossing dashed line denotes the formed bond joining R1 to a molecule of formula (I); R2 and R3 are independently OH or H provided that R2 and R3 are not OH at the same time; R4 is H or R5C(O) provided that R and R4 are not H at the same time; and R5 is C3-C26 alkenyl, or a pharmaceutical salt thereof.

EFFECT: compounds have anti-cancer and anti-inflammatory activity.

15 cl, 6 tbl, 7 dwg, 15 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) or (I'): Z-X1-(-CH2-CH2-O-)n-Yp-D (I), D-Yp-(-CH2-CH2-O-)n-X1-Z (l'), where: Z is a reactive carboxylic ether selected from a group consisting of N-succinimidyl, N-sulphosuccinimidyl, N-phthalimidyl, N-sulphophthalimidyl, 2-nitrophenyl, 4-nitrophenyl, 2,4-dinitrophenyl, 3-sulpho-4-nitrophenyl, 3-carboxy-4-nitrophenyl and a trifluorophenyl ester, or haloacetamide; D is maytansinoid; X is an aliphatic structural unit; Y is an aliphatic structural unit linked to the maytansinoid through a thioether bond; where said aliphatic structural unit, represented by X or Y, is a simple or branched alkyl group with 1-20 carbon atoms in the chain, a cyclic alkyl group having 3-10 carbon atoms, a simple or branched alkenyl group, having 2-15 carbon atoms in the chain or a simple or branched alkynyl group, having 2-15 carbon atoms in the chain; 1 equals 0 or 1; p equals 0 or 1; and n is an integer from 1 to 2000. The invention also relates to a conjugate of a cell-binding agent, and cytotoxic maytansinoid, where the cell-binding agent is an antibody.

EFFECT: obtaining compounds and conjugates, as well as pharmaceutical compositions based thereon, which can be used in medicine to treat tumours, autoimmune diseases, graft rejection, graft-versus-host disease, viral infections and parasitic infections.

20 cl, 38 dwg, 10 ex

FIELD: medicine, pharmaceutics.

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EFFECT: there are produced new compounds and composition on their basis which can find application in medicine for treating cancer expressing Pim-1 kinase.

13 cl, 5 dwg, 9 tbl, 9 ex

FIELD: medicine, pharmaceutics.

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EFFECT: preparing the specific compounds and pharmaceutical composition containing the above compounds effective for kinase inhibition.

18 cl, 393 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to medicine and describes a solid pharmaceutical composition applicable for oral administration and containing: S1P receptor modulator which represents 2-amino-2-[2-(4-octylphenylethyl)]propane-1,3-diol in the free form or in the form of a pharmaceutically acceptable salt or a phosphate thereof and monocrystalline cellulose in the absence of a sugar alcohol.

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9 cl, 40 ex, 11 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of medicine, namely to pharmaceutical industry and deals with solid pharmaceutical composition, possessing high physical strength. Claimed invention also presents method of manufacturing solid pharmaceutical composition. Claimed pharmaceutical composition contains 7 varicoloured types of granules in form of capsule. Granules contain, wt %: nikotinamide 1-35; pyridoxine 0.1-8; calcium pantitenate 0.1-15, thiamin 0.1-30; tryptophan 1-30; tocoferol 0.5-5; ascorbic acid 0.1-50; 5-hydroxyanthranyl acid 0.01-10; Riboflavin 0.1-10; folic acid 0.1-6; cyanocobalomin 0.001-6; isoleucin 0.5-10; leucin 0.5-15; lysine 0.5-20; phenylalanine 0.1-5; threonine 0.1-5.0; valin 0.1-8.0; methionine 0.1-15; lactose 1-4.0; ergocalcioferol 1-95.0 and auxiliary substances for obtaining granules.

EFFECT: claimed composition possesses excellent properties of medication release and digectionin application composition possesses hepatoprotective hypolipidemic immunostimulating and normalising kidney activity action.

2 cl. 2 ex. 5 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a pharmaceutical composition for the correction of cerebrovascular disease accompanying cardiovascular diseases which contains the active ingredients presented by atorvastating or pharmaceutically acceptable salt thereof and nicergolin in the therapeutically effective amounts.

EFFECT: pharmaceutical composition is characterised by high stability and bioavailability.

8 cl, 8 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, and represents an oral dosage form in the form of capsule, containing: 1) pomalidomide in the amount of 0.1 to 3 wt % of total weight; 2) a binding agent or an excipient in the amount of 90 to 99 wt % of total weight wherein the binding agent or the excipient represent starch, mannitol or their mixture.

EFFECT: invention provides stability of the declared dosage form.

22 cl, 7 ex, 6 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to chemical-pharmaceutical industry and represents a pharmaceutical composition containing: {1S-[1α,2α,3β(1S*,2R*),5β]}-3-(7-{[2-(3;4-difluorophenyl)cyclopropyl]amino)-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol; an excipient representing mixed mannitol and dibasic calcium phosphate dihydrate; a binding agent representing hydroxypropyl cellulose; a disintegrant representing sodium starch glycolate; and one or more lubricating agents.

EFFECT: invention provides preparing the composition of the active compound possessing high stability and high bioavailability of the active agent.

12 cl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics and medicine, namely a stable pharmaceutical composition of a water-soluble salt of vinorelbine. The composition contains approximately 56 wt % of a diluent, approximately 2.5 wt % of a binding agent, approximately 5 wt % of a disintegrant, approximately 0.25 wt % of a flow agent and approximately 0.5 wt % of a lubrication agent. The water-soluble salt of vinorelbine is preferentially vinorelbine ditartrate.

EFFECT: pharmaceutical composition is preferentially presented in the form of a gelatine capsule or a tablet.

5 cl, 6 ex, 12 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: pharmaceutical composition applicable for oral administration contains an S1P receptor agonist and mannitol with the composition representing a solid dosage form. Mannitol has a particle specific surface area 1 to 7 m2/g, and the S1P receptor agonist is specified from 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol (FTY720), its pharmaceutically acceptable salt and FTY720-phosphate.

EFFECT: compositions under the invention are characterised by a high level of distribution uniformity of said S1P receptor agonist, and applicable for oral administration in the solid dosage form, eg in the form of a tablet or a capsule.

14 cl, 39 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: method for preparing a pharmaceutical composition consists in mixing an S1P receptor agonist - 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or its pharmaceutically acceptable salt with sugar alcohols; the mixture is milled and/or granulated, and then mixed with an oil agent. The method under invention is implemented on high-speed automated equipment and enables producing the compositions with high-level distribution uniformity of 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or its pharmaceutically acceptable salt in the composition applicable for oral administration of said S1P receptor agonist.

EFFECT: preparing the pharmaceutically acceptable salt in the composition applicable for oral administration of said S1P receptor agonist.

15 cl, 39 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a pharmaceutical composition for treating and/or preventing depressions. The pharmaceutical composition contains an active substance presented by a selective serotonin reuptake inhibitor (SSRI) specified in a group of fluoxetine, paroxetine, citalopram, escitalopram, sertraline, fluvoxamine differing by the fact that as an active substance, it additionally contains N-acetyl-5-methoxytryptamine (melatonin) in the following proportions, mg: selective serotonin reuptake inhibitor (SSRI) - 10-30 mg, melatonin - 3-8 mg. The pharmaceutical composition may be presented by a solid dosage form - a tablet, a film-coated tablet, a capsule, by a soft dosage form - a rectal suppository.

EFFECT: pharmaceutical composition provides treating depressions and has a number of additional therapeutic properties: easing falling asleep and relieving sleeping disorders, recovering circadian rhythm and seasonal rhythm with reducing a risk of side effects of SSRI.

3 cl, 14 tbl, 7 ex

FIELD: medicine.

SUBSTANCE: invention describes a method for stabilising a sensitive ingredient for biological absorption in the oral intake in a therapeutic composition involving the stages of combining pregelatinised starch with at least one sensitive ingredient, and mixing the sensitive ingredient with pregelatinised starch. Pregelatinised starch is used in the amount of 5% to 80% of composition weight. The sensitive ingredient is specified in vitamin C, phenylephrine and their combinations. The sensitive ingredient is used in the amount of 0.1% to 20% of composition weight. Said sensitive ingredient is uniformly distributed in pregelatinised starch and adsorbed on pregelatinised starch.

EFFECT: stability of said sensitive ingredients and maintenance of their activity and availability for biological absorption in the oral intake of the therapeutic composition.

17 cl, 15 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine, namely to a lyophilised formulation containing an influenza vaccine, an aqueous solution prepared by lyophilisation and containing (i) he influenza vaccine, (ii) a hydrophobic amino acid, and (iii) arginine and an acid addition salt thereof; it also concerns a method for preparing the lyophilised formulation containing the influenza vaccine to be desalted.

EFFECT: group of inventions provides preparing the lyophilised formulation wherein the influenza vaccine exhibits improved stability.

15 cl, 3 tbl

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