56 results about "Nintedanib" patented technology

The invention includes dry powder nintedanib formulation for dispersion and inhalation administration including salts thereof, indolinone derivative or salts thereof and in fixed dose combinations with carrier agents and other active ingredients. The aerosol delivery combination formulation may be administered as an inhaled aerosol over a few actuations or by two or more actuations. Each dose may be administered one or more times daily on a regular or interval daily dosing regimen. The special formulation parameters of the invention include the selection of the salt for complexation with the form of nintedanib used for an isolated dry powder along with particle size distributions and combination with a force control agent for improved aerosol delivery. Methods of the invention include therapeutically effective doses of the described invention used to treat interstitial lung disease.

Compositions and methods of using nintedanib for treating indications with abnormal neovascularization in the front part of the eye are disclosed.

The present invention relates to a combination therapy of pexidartinib and nintedanib for use in the prevention or treatment of pulmonary fibrosis, in particular to a combination therapy of pexidartinib and nintedanib for use in the prevention or treatment of pulmonary fibrosis.

A pharmaceutical composition for prevention or treatment of a disease or disorder characterized by chronic inflammation, associated with angiogenesis and fibrosis. The pharmaceutical composition includes a multi-target inhibitor, multi-phase modulator, or multi-kinase inhibitor, such as axitinib, nintedanib, pirfenidone, riociguat, sorafenib, sunitinib, lenvatinib, regorafenib, ponatinib, or pazopanib.

A preparation method of the methacrylated gelatin with the dual functions comprises the following steps: firstly, preparing collagen methylated polymethacrylate, then mixing 5% of collagen methylated polymethacrylate, 0.2% of trimethylbenzoyl phosphonate, 10 mg / ml of a herba houttuyniae extract and 20 micrograms / ml of nifedimab, and carrying out uniform mixing, so as to obtain the methacrylated gelatin with the dual functions, the collagen methylated polymethacrylate and the trimethylbenzoyl phosphonate, the herba houttuyniae extract, the nifedimab and the collagen methylated polymethacrylate, the herba houttuyniae extract and the nifedimab. The methacrylated gelatin is prepared under ultraviolet irradiation, and the loose cross-linked network structure of the methacrylated gelatin can realize continuous release of drugs, so that the demand of continuous and stable drug delivery is met; in addition, the gelatin methacrylamide, the herba houttuyniae extract and the nintedanib are combined to relieve hemorrhagic intestinal adhesion and can regulate inflammation and anti-fibrosis functions.

The present application provides a kind of nintedanib solution for inhalation and preparation method and application, the inhalation solution includes active substance, solvent and auxiliary material, the single dose specification of the inhalation solution is 1-5ml, and the active substance in single dose specification is 2.41-12.04mg / ml nintedanib ethanesulfonic acid;The solvent is sterile injection solution water;The auxiliary material includes isotonicity regulator and pH regulator and can also include antioxidant;The addition amount of the isotonicity regulator is to make the inhalation solution have the weight molal osmotic concentration of 240-400mOsmol / kg;The addition of the pH regulator is to make the pH value of the inhalation solution preparation 3.0-4.0.The inhalation nintedanib solution of the present application can provide a kind of nintedanib for inhalation with convenient, safe and effective, and good stability of drug dosage form and drug delivery system in combination with liquid atomization device.

The application belongs to the technical field of nintedanib preparation development, and particularly relates to a nintedanib suspension preparation, a preparation method thereof and application of the nintedanib suspension preparation in treatment of pulmonary fibrosis. A phospholipid material is dissolved in an organic solvent under the condition of 50-70 DEG C to obtain solution A; an inorganic salt is dissolved in water for injection to obtain solution B; nintedanib ethanesulfonic acid is dissolved in water for injection to obtain solution C; an osmotic pressure regulator is dissolved in water for injection to obtain solution D; solution A and solution B are mixed by microfluidic to obtain suspension E; the organic solvent in the suspension E is removed by tangential flow membrane filtration, then solution C is added and kept for a period of time, and solution D is added as needed and mixed; the suspension can be filtered by a sterilization filter to obtain the nintedanib suspension preparation. The nintedanib prepared in the application is in a stable physical state, has excellent slow-release effect, is suitable for low-dose inhalation administration in the lung, and is helpful to improve the treatment effect and reduce side effects.

The invention discloses a medicine for relieving side effects of gastrointestinal tracts caused by nintedanib, a medicine for preventing or treating pulmonary fibrosis and application of stachyose, and belongs to the technical field of medicines. The medicine taking the stachyose as the active ingredient can effectively relieve gastrointestinal tract side effects caused by the nintedanib, for example, intestinal mucosa lesions caused by the nintedanib can be obviously relieved, for example, intestinal mucosa tissue structure abnormity, intestinal cell proliferation activity reduction, intestinal cell apoptosis increase, intestinal tissue inflammatory factor gene expression level up-regulation and the like.

The invention discloses a method for measuring the delivery rate and the total delivery amount of nintedanib lipidosome, and relates to the technical field of detection of pharmaceutical preparations, and the method comprises the following steps: placing filter paper into a filter paper device, connecting an atomizer by using an adapter, and setting a respiration simulator as an adult mode; pouring the to-be-detected Nintedanib liquid medicine into an atomizer, starting the respiration simulator, working for 60 seconds, synchronously starting and stopping the compressor during the period, taking out the filter paper to obtain a first piece, replacing the filter paper with new filter paper, continuously atomizing until no smoke, and taking down to obtain a second piece; a test solution is obtained through treatment, the test solution and the reference solution are injected into a chromatograph, the result of the first test solution is the delivery rate, and the result of the second test solution is the total amount; according to the method for determining the delivery rate and the total delivery amount of the nintedanib liposome, atomized medicine can be accurately and effectively extracted, the recovery rate is high, the detection method is simple in mobile phase, convenient to operate and good in accuracy, the problem of accurate detection of main components in the delivery of the nintedanib liposome medicine is solved, and the accuracy of a detection result is improved.

The invention discloses a pharmaceutical composition for inhibiting tumor drug resistance and application thereof. The pharmaceutical composition comprises an exosome inhibitor, nintedanib and gemcitabine, the exosome inhibitor, the nintedanib and the gemcitabine are used in a combined manner, so that the cell viability of the CTS can be remarkably reduced, and the proportion of apoptotic cells in the CTS can be remarkably increased; the pharmaceutical composition interferes with the mutual transformation process between normal fibroblasts and CAFs, and inhibits secretion and release of EVs and reduces formation of new CAFs while restoring the CAFs existing in TME to normal fibroblasts, thereby successfully reversing the drug resistance of tumors.

The present invention relates to a pharmaceutical formulation containing nintedanib or a pharmaceutically acceptable salt thereof and a methacrylic acid copolymer, wherein the formulation provides an excellent dissolution rate of 90% or more after 180 minutes under the conditions of the Korean Pharmacopoeia dissolution method II (paddle method) at 50 rpm in a test solution of pH 4.5.

The application discloses a compound inhalation powder aerosol and a preparation method thereof. The compound inhalation powder aerosol comprises apremilast or a pharmaceutically acceptable salt thereof and an efficacy enhancing substance, wherein the efficacy enhancing substance is nintedanib or a pharmaceutically acceptable salt thereof; and the amount of the efficacy enhancing substance is 0.1-10 times the amount of the apremilast or the pharmaceutically acceptable salt thereof. In the compound inhalation powder aerosol, the drug exposure of apremilast is greatly improved under the action of nintedanib, and a significant enhancement effect is exhibited. Meanwhile, nintedanib further improves efficacy. The powder aerosol is used for pulmonary inhalation administration, and apremilast or the pharmaceutically acceptable salt thereof and nintedanib or the pharmaceutically acceptable salt thereof are used for treating lung diseases, so that the drugs can be directly delivered to effective sites, the administration dose can be further effectively reduced or the drug utilization rate can be improved, the deposition rate can be improved, and the treatment effect can be greatly improved.

This invention provides a method for treating ocular indications involving abnormal neovascularization. [Solution] The present invention provides a method comprising the step of administering an effective amount of nintedanib or a pharmaceutically acceptable salt thereof in the form of a topical eye drop or implant to the eye of a subject.

The present invention concerns the compounds of formula (I)wherein R1, R2, R3, X, and Y are as described in the description, and their use as antagonists of the LPA1 receptor, in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s); such as especially pirfenidone and / or nintedanib, in the prevention and / or treatment of fibrotic diseases. The invention further relates to pharmaceutical compositions comprising the compounds of formula (I) in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s) such as pirfenidone or nintedanib.

The present application relates to the technical field of medicine, and particularly relates to an anti-pulmonary fibrosis prodrug compound and a preparation method and application thereof. The prodrug compound is a novel prodrug, and the structure comprises: a) an active drug unit selected from pirfenidone and nintedanib; b) a lung targeting unit selected from diphenyl chloroiodonium salt and a mimic thereof 521; and c) a linker unit which is a responsive linkage sensitive to a biomarker specifically overexpressed in a pulmonary fibrosis microenvironment. The prodrug is stable in the systemic circulation and has no activity or low activity, and can be actively targeted to a pulmonary fibrosis lesion; under the specific stimulation of the PFM, the linker is broken, and the original drug molecule is accurately released, so that the concentration of the drug in the lesion site is significantly increased, the toxic side effects caused by systemic exposure are reduced, and the anti-pulmonary fibrosis effect is enhanced.

The invention discloses application of nintedanib in preparation of a medicine for treating plant migration and plant mineralization, and belongs to the technical field of biological medicine. The research shows that the nintedanib has the effects of reducing deposition of extracellular matrix of an allogeneic kidney transplantation model mouse, improving renal tubular atrophy, relieving mouse CD206 + macrophage infiltration and reducing rejection injury degree and immune infiltration degree of kidney grafts after being administered under the administration dosage without generating liver and kidney toxicity and intestinal side effects; the lesion process of mouse chronic transplanted kidney rejection is obviously slowed down, and the damage of excessively activated inflammatory cells to the transplanted kidney is reduced. The results show that nintedanib can delay the progress of chronic transplantation renal fibrosis.

The invention relates to a crystal form of a novel nintedanib derivative as shown in a formula (I), a preparation method of the crystal form, and medical application of a medicinal preparation containing the crystal form. The invention further provides application of the compound shown in the formula (I) in preparation of drugs for treating systemic sclerosis related pulmonary interstitial diseases, idiopathic pulmonary fibrosis and non-small cell lung cancer. The compound has the advantages of being remarkable in stability and long-acting.

The invention relates to the technical field of biological medicines, in particular to application of surface-engineered mitochondria for activating mitochondrial autophagy in preparation of a medicine for treating pulmonary fibrosis. According to the present invention, the antibody is covalently coupled to the PLL modified exogenous mitochondrial surface to construct the Ab-mito with characteristics of positive electricity and targeting function, such that the efficient mitochondrial transplantation to the recipient cell is promoted, the problems of poor selectivity and low efficiency confronted by the existing mitochondrial delivery research are overcome, and the new direction is provided for the pulmonary fibrosis treatment. The treatment effect of the traditional Chinese medicine composition on pulmonary fibrosis is equivalent to that of a clinical medicine nintedanib, and the method is simpler and more effective.

The invention relates to the use of a tyrosine kinase inhibitor, specifically nintedanib or one of the pharmaceutically acceptable salts thereof, for the treatment of Castleman disease or the prevention or treatment of one of its complications.

The invention provides a pharmaceutical composition of a nintedanib solution for inhalation. The pharmaceutical composition comprises a first container and a second container, the first container is filled with a first solution, and the first solution contains nintedanib or pharmaceutically acceptable salt thereof and does not contain a nonionic osmotic pressure regulator; the second container is filled with a second solution, and the second solution contains an ionic osmotic pressure regulator and a nonionic osmotic pressure regulator. The medicinal composition disclosed by the invention is simple in component, stable in preparation, capable of avoiding generation of genotoxic impurities, high in safety, lower in irritation to respiratory mucosa and capable of improving the compliance of a patient.

The invention relates to the technical field of medicine, in particular to an ethanesulfonic acid nintedanib sublingual tablet and a preparation method thereof.The ethanesulfonic acid nintedanib sublingual tablet contains ethanesulfonic acid nintedanib, a carrier material, a filling agent, a disintegrating agent, a flavoring agent and a lubricating agent, and the ethanesulfonic acid nintedanib sublingual tablet is prepared by setting the specific proportion of the raw materials and the auxiliary materials. Compared with an original research medicine, namely a nintedanib ethanesulfonate soft capsule, the problem that the bioavailability is low due to the liver first-pass effect is effectively solved, the medicine provided by the invention is good in taste, excellent in stability, rapid in disintegration and rapid in dissolution rate, and each detection item meets the quality standard. And meanwhile, the clinical use compliance of a patient is also improved.

The present invention relates to the technical field of biomedicine and discloses use of a hypoxanthine derivative in the preparation of a drug for treating renal fibrosis and / or kidney disease. By assaying pharmacological activities of structurally modified and altered hypoxanthine derivatives for treating renal fibrosis and / or kidney disease, the pharmacological activities of such compounds were tested in animal disease models, and data on activities for preventing and treating renal fibrosis and / or kidney disease were provided. It is proven that the hypoxanthine derivatives have good activities, and the effects are significantly superior to those of clinically commonly used positive drugs nintedanib and losartan, and the effects are also significantly superior to those of hypoxanthine derivatives A, B, and C and other hypoxanthine derivatives in the prior art. The hypoxanthine derivative of the present invention can provide a novel skeleton for the screening of novel compounds for the preparation of a drug for treating renal fibrosis and / or kidney disease.

This invention relates to a combination therapy of dacomitinib and nintedanib for the prevention or treatment of pulmonary fibrosis.

A medicament for treating a cutaneous scar, comprising a combination of Nintedanib and Propranolol.

Formulations and intravitreal implants containing nintedanib can be used in methods for the treatment of back-of-the-eye diseases.

This invention relates to a combination therapy of pexidartinib and nintedanib for the prevention or treatment of pulmonary fibrosis.

The invention relates to the field of cell therapy, in particular to application of NK cells in preparation of drugs for treating fibrosis diseases. The invention discloses application of NK (natural killer) cells in preparation of medicines for treating fibrosis diseases, and compared with nintedanib or pirfenidone, the NK cells have equivalent or even better effects in treatment of pulmonary fibrosis diseases, are higher in safety and do not cause side effects such as hepatotoxicity or renal toxicity. Also disclosed is a method of treating a subject suffering from a fibrotic disease by administering one or more NK cells to the subject.

The invention relates to the technical field of biological medicines, and discloses an application of an inoxanthine derivative in preparation of a medicine for treating peritoneal diseases, the pharmacological activity of the compound is tested in various animal disease models by detecting the pharmacological activity of the inoxanthine derivative subjected to structure modification and transformation in treatment of peritoneal diseases, and the application of the inoxanthine derivative in preparation of the medicine for treating peritoneal diseases is provided. The invention also provides data of activity of preventing and treating different types of peritoneal diseases, which proves that the compound has good activity, the effect is obviously superior to that of a clinically common drug nintedanib, and the effect is also obviously superior to that of hypoxanthine derivatives A, B and C and other hypoxanthine derivatives in the prior art. The hypoxanthine derivative provided by the invention can provide a novel skeleton for screening a novel compound for preparing a medicine for treating peritoneal diseases, and lays a theoretical foundation for developing a novel lead compound.

The invention discloses a light-operated biological hybrid micro-robot drug-loaded delivery carrier and preparation and application thereof, and the light-operated biological hybrid micro-robot drug-loaded delivery carrier is composed of polymer nanoparticles carrying anti-fibrosis drugs and flexible living microorganisms, wherein 0.1-1 mg of the anti-fibrosis drug can be loaded on each flexible living microorganism with the order of magnitude of 1 * 10 < 5 >-1 * 10 < 6 >; the anti-fibrosis drug in the polymer nanoparticles loaded with the anti-fibrosis drug is nintedanib, the polymer is a polylactic acid-glycolic acid copolymer, and the mass ratio of the polylactic acid-glycolic acid copolymer to the nintedanib is (10: 1)-(20: 1). The ratio of lactide to glycolide in the polylactic acid-glycolic acid copolymer is 30: 70-50: 50, and the molecular weight of the polylactic acid-glycolic acid copolymer is 38000-54000. According to the photo-biological hybrid micro-robot, flexible living microalgae and a micro-robot drug delivery system are combined to achieve light-operated accurate regulation and control, light-operated permeation enhancement is achieved, drug retention time is prolonged, and good biocompatibility and safety are achieved.