46 results about "Edaravone" patented technology

The invention belongs to the technical field of biological medicine, and discloses a pharmaceutical composition for treating metabolic diseases, a preparation method and application, and the pharmaceutical composition comprises edaravone or pharmaceutically acceptable salts thereof and dextroborneol. The weight ratio of the edaravone to the dextroborneol is (10: 1)-(1: 1). The invention finds that the combination of edaravone and dextroborneol shows remarkable curative effects in the aspects of improving cognitive function, reducing blood fat, relieving fatty liver and recovering cardiac function and / or overall metabolic homeostasis; meanwhile, the pharmaceutical composition disclosed by the invention has a remarkable comprehensive treatment effect on metabolic diseases or complications (such as metabolic syndrome) of the metabolic diseases and / or vascular cognitive impairment complicated with the metabolic syndrome.

The application discloses a kind of pharmaceutical composition, organ preservation fluid and its application, the pharmaceutical composition includes seduxian and edaravone.The mass ratio of seduxian and edaravone is 1:0.0001-10000.The cell protection effect of the pharmaceutical composition of the application is good, seduxian and edaravone show synergistic effect, help to obtain excellent curative effect, and reduce drug dosage, help to improve clinical drug safety.

A pharmaceutical composition, an organ preservation solution, and their applications are disclosed, wherein the pharmaceutical composition comprises cedutinib and edaravone. The mass ratio of cedutinib to edaravone is 1:0.0001-10000. The pharmaceutical composition of the present invention exhibits good cell protection effects, and cedutinib and edaravone demonstrate a synergistic effect, contributing to excellent therapeutic efficacy, reducing drug dosage, and improving clinical drug safety.

The invention relates to the technical field of pharmaceutical preparations, in particular to a concentrated solution for injection of edaravone dextroborneol and a preparation method of the concentrated solution. According to the invention, the sulfonic acid antioxidant and the amino acid antioxidant are compounded and added into the edaravone dextroborneol injection solution, so that a synergistic effect is generated on inhibition of compound oxidative degradation of edaravone dextroborneol, and the prepared edaravone dextroborneol injection concentrated solution has high stability in accelerated and long-term stability tests; related substances grow slowly, the content of main components is not obviously reduced, the appearance of the solution is almost unchanged, and the validity period of the product is obviously prolonged. The preparation method provided by the invention is stable in process and easy for industrial production, and ensures the consistency of batch-to-batch quality through the combination of nitrogen charging protection and a specific antioxidant system.

The invention belongs to the technical field of biological medicines, and particularly discloses a self-assembled nano preparation coated with a macrophage membrane as well as a preparation method and application of the self-assembled nano preparation. According to the nano preparation, nano particles formed by self-assembly of epigallocatechin gallate (EGCG), ferric chloride (FeCl3) and edaravone (EDV) serve as a core, and the outer layer of the nano preparation is coated with a macrophage membrane. The preparation method is a one-pot method and comprises the following steps: mixing and self-assembling EGCG, FeCl3 and EDV in a phosphate buffer solution, carrying out centrifugal purification, and carrying out ultrasonic fusion with a macrophage membrane. The nano preparation is uniform in particle size, has excellent free radical scavenging capacity and antioxidant activity, can effectively pass through a blood-brain barrier and target a cerebral ischemia reperfusion injury area, and shows a remarkable effect in preparation of drugs for treating cerebral arterial thrombosis.

Provided is an edaravone suspension for oral administration that can reduce the burden on ALS patients and caregivers and exhibit an ALS treatment effect equivalent to that of an injection.SOLUTION: An edaravone suspension for human oral administration including edaravone particles, a dispersant, and water is provided.SELECTED DRAWING: None

An edaravone suspension for human oral administration includes edaravone particles, a dispersant, and water.

The present application relates to a kind of cytidine choline dextrohydrotalcid derivatives and its preparation method and application, belong to biological medicine technical field.The present application is aimed at solving the technical problems of low blood-brain barrier penetration rate and limited treatment effect of existing edaravone dextrohydrotalcid compound preparation.The present application prepares a dextrohydrotalcid derivative (C-B) with boronic acid structure, then it is compounded with cytidine choline in specific pH buffer system, and forms cytidine choline dextrohydrotalcid derivative (C-D-B).The present application can effectively improve the efficiency of drug crossing blood-brain barrier by using the dynamic covalent characteristics of boronic ester bond and free radical responsiveness.The experimental results show that, compared with existing combination drug, the derivative of the present application can significantly reduce the infarction area of cerebral ischemia model animal, reduce cell damage and active oxygen level, and promote vascular regeneration, and show better treatment effect on ischemic brain injury.

The application relates to the technical field of stem cells, and specifically discloses a drying protective agent and a cell drying process of mesenchymal stem cells. The drying protective agent provided by the application comprises the following components in the following contents: EGCG: 5-45 mg / 100 mL, hydroxytetrahydro pyrimidine: 400-520 mg / 100 mL, vitamin C: 350-500 mg / 100 mL, edaravone: 0.02-0.3 mg / 100 mL, quercitrin: 0.10-0.35 mg / 100 mL, aspartic acid: 180-280 mg / 100 mL, tetrahydro pyrimidine: 400-500 mg / 100 mL, trehalose: 10-60 g / 100 mL, dextran: 20-50 g / 100 mL, maltose: 25-40 g / 100 mL and 2,3,4,6-tetraacetyl-d-glucose: 30-60 mg / 100 mL, and the solvent is a phosphate buffer solution PBS; the application also provides a cell drying process, which comprises the following steps: cold-heat cycle treatment and drying; wherein the cold-heat cycle treatment adopts the aforementioned drying protective agent. The drying protective agent provided by the application can avoid damage of mesenchymal stem cells in the drying process, so that the survival rate of the mesenchymal stem cells after rehydration is improved.

The invention discloses solid particles of edaravone and dextroborneol prepared by a wet granulation process and a solid oral quick-release preparation prepared from the solid particles. The solid particles comprise edaravone, dextroborneol, polyethylene glycol and other pharmaceutic adjuvants. According to the present invention, the dextroborneol and the polyethylene glycol are co-dissolved in the absolute ethyl alcohol, and the wet granulation is performed with the edaravone and the pharmaceutical excipients, such that the process feasibility is significantly improved, and the particles with different particle sizes can be prepared according to the absolute ethyl alcohol use amount so as to prepare the oral quick-release tablets with different dosage forms, the dissolving-out speed of the prepared solid particle dextroborneol is obviously improved, and the stability of edaravone is also improved at the same time.

The invention relates to a solid water-dispersible pharmaceutical composition for use in the treatment of a disease, said treatment comprising dispersing said pharmaceutical composition into an aqueous liquid to produce an enteraliy administrable liquid containing at least 0.5 gram of said pharmaceutical composition and at least 0.3 g / 1 of edaravone, followed by enteral administration of said enteraliy administrable liquid to a human patient in an amount to provide a dose of 30-300 mg of edaravone, said pharmaceutical composition comprising: 2-50 weight % of 3-methyl-l-phenyl-2-pyrazolin-5-one (edaravone); and 3-50 weight % of a water-soluble alkalizing agent. This solid composition containing edaravone can be easily dispersed in an aqueous liquid to prepare an aqueous solution of edaravone that can be ingested by a patient. The solid composition of the invention provides the advantage that when the composition is introduced into water the edaravone dissolves very rapidly and the enteraliy administrable liquid thus obtained has a high oral bioavailability.

A method of treating an oxidative stress disease includes orally or intragastrically administering, to a subject in need thereof, a pharmaceutical composition including edaravone with a time interval from a consumption of a meal by the subject in need thereof to an administration of the pharmaceutical composition to the subject in need thereof. The time interval is 8 hours or longer after the consumption of a high-fat meal, the time interval is 4 hours or longer after the consumption of a standard meal, or the time interval is 2 hours or longer after the consumption of a light meal.

This invention relates to the fields of pharmaceuticals and nanomedicine, specifically disclosing the preparation of a dual-targeting liposome drug delivery system and its application in stroke. The dual-targeting liposome drug delivery system comprises neutrophils, artemisinin, edaravone, and liposomes. The liposomes co-load artemisinin and edaravone, and their surfaces are modified with sialic acid derivatives and phosphatidylserine to form liposome nanomedicines. The neutrophils act as carriers, transporting the drug across the brain border (BBB) ​​and targeting it to the ischemic brain region. This dual-targeting strategy achieves precise two-stage drug delivery to the ischemic brain region. This delivery system can inhibit NLRP3 inflammasome activation, reduce pyroptosis, and promote microglial polarization towards the M2 anti-inflammatory phenotype, thereby effectively treating cerebral ischemia-reperfusion injury or ischemic stroke.

An arylalkylamine ferroptosis inhibitor based on an edaravone structure, and a preparation method therefor and a use thereof. The structural formula of the ferroptosis inhibitor is as shown in the following formula I, formula II, or formula III: formula I, formula II, formula III. The ferroptosis inhibitor has strong ROS scavenging ability and an inhibitory effect on lipid peroxidation, can inhibit ferroptosis caused by an ferroptosis inducer, and can reduce cerebral ischemia and nerve damage caused by cerebral ischemia, and alleviate symptoms of neurological diseases such as Parkinson's syndrome. On the basis of the ferrostain-1 / edaravone structure, the provided arylalkylamine ferroptosis inhibitor can exert a synergistic effect by means of multiple effects to treat ferroptosis-related diseases and can also expand the use of edaravone, thereby providing a candidate compound for subsequent drug research and development.

The invention belongs to the technical field of pharmaceutical analysis, and discloses a method for simultaneously detecting sodium hydrogen sulfite and cysteine hydrochloride and application. Taking the concentrated solution for injection of edaravone dextroborneol, and detecting the content of an oxidizing agent by adopting high performance liquid chromatography; the oxidizing agent is sodium hydrogen sulfite and cysteine hydrochloride; a mobile phase of the high performance liquid chromatography is a 0.035% sodium heptanesulfonate solution and methanol in a volume ratio of (18-22): (78-82). According to the method, a normal-phase-mode universal chromatographic column is selected, and a proper amount of ion pair reagent is added into a reversed-phase chromatographic mobile phase, so that the retention of a sample can be enhanced, and the peak pattern can be improved. The method has remarkable advantages in specificity, linear range and repeatability, has the advantages of high specificity, high precision, high accuracy and the like, and provides an important method detection reference basis for antioxidant quality control of a concentrated solution product for edaravone dextroborneol injection.

A method of treating an oxidative stress disease includes orally or intragastrically administering, to a subject in need thereof, a pharmaceutical composition including edaravone with a time interval from a consumption of a meal by the subject in need thereof to an administration of the pharmaceutical composition to the subject in need thereof. The time interval is 8 hours or longer after the consumption of a high-fat meal, the time interval is 4 hours or longer after the consumption of a standard meal, or the time interval is 2 hours or longer after the consumption of a light meal.

The application provides a preparation method of a medicinal injection, and the injection contains edaravone 2 mg / ml, dextrohydrotalcid 0.5 mg / ml, propylene glycol 0.08 ml / ml and sodium pyrosulfite 1.0 mg / ml. In the preparation process, the prescription amount of 60%-85% propylene glycol and the prescription amount of 5%-25% water are first injected into a preparation tank in a volume ratio, heated to 50-60 DEG C, and then edaravone is added and stirred to dissolve, and then dextrohydrotalcid dissolved in the remaining prescription amount of propylene glycol is added, and then water close to the constant volume is added, and then the temperature is reduced to below 25 DEG C, and then sodium pyrosulfite is added, and then the pH value is adjusted to 4.0-5.0, and then the constant volume is adjusted to the full amount. The preparation method of the edaravone dextrohydrotalcid injection solves the problem that the raw material is easily precipitated in the preparation process by matching the specific proportion of the auxiliary materials with the preparation steps, and the preparation process has low requirements on the industrialization preparation tank, is convenient for industrialization operation, and has low manufacturing cost.

The invention discloses an edaravone structure-based aromatic alkylamine ferroptosis inhibitor as well as a preparation method and application thereof. The structural formula of the ferroptosis inhibitor is shown as a formula I, a formula II or a formula III. The ferroptosis inhibitor has relatively strong ROS (reactive oxygen species) removal capability and a lipid peroxidation inhibition effect; ferroptosis caused by a ferroptosis inducer can be inhibited; cerebral ischemia and nerve injury caused by cerebral ischemia can be relieved, and symptoms of neurological diseases such as Parkinson's syndrome and the like can be relieved. Therefore, based on the ferrostain-1 / edaravone structure, the aromatic alkylamine ferroptosis inhibitor provided by the invention can play a synergistic effect through multiple effects to treat ferroptosis related diseases, can also expand the application of edaravone, and provides a candidate compound for subsequent drug research and development.

Disclosed is an application of Teruravone in the preparation of a drug for treating the amyotrophic lateral sclerosis disease. Teruravone can significantly increase the survival rate of TDP-43 M337V stably transfected cells and reduce the LDH leakage rate, and has a potency superior to that of Edaravone, indicating that Teruravone possesses stronger neuroprotective activity. Preliminary clinical trials indicate that after oral administration of Teruravone to an ALS patient for 3 months, the Norris Scale score and the neurofilament light chain protein level in the blood remained generally stable, and the decline in ALSFRS-R score was significantly slowed. Thus, the clinical effect of delaying the disease course of ALS is achieved, and no serious adverse effects were observed.

This invention, entitled "A Pharmaceutical Composition, Formulation, Preparation Method, and Application for Alleviating Cerebral Ischemia-Reperfusion Injury," belongs to the field of pharmaceutical technology. The technical problem to be solved is to improve the efficacy of drugs in preventing and / or treating cerebral ischemia-reperfusion injury. The key technical solution is a pharmaceutical composition for alleviating cerebral ischemia-reperfusion injury, comprising sinapic acid and a second therapeutic agent, wherein the second therapeutic agent comprises at least one of edaravone, citicoline, and tetramethylpyrazine.

A composition of the present disclosure contains edaravone and is used for causing a change in expression level of a gene product in a target. The gene product is a gene product of one or more genes selected from KAZALD1, SBK1, SCN2A, UBE2L6, ALPL, NTM, PTTG1, ITGB4, HAUS4, DCTD, MT2A, ASF1B, FCSK, MAST1 and FAIM2. The composition is also suitably used as a pharmaceutical. The composition is also suitably used for treating or preventing a neurodegenerative disease. The neurodegenerative disease is suitably amyotrophic lateral sclerosis (ALS). The present disclosure also provides a method for evaluating responsiveness of edaravone based on an expression level of the gene product or a change in the expression level.

The invention belongs to the technical field of chromatography-mass spectrometry detection, and relates to a method for simultaneously detecting concentrations of riluzole and edaravone. The invention establishes an analysis method for simultaneously detecting riluzole and edaravone based on liquid chromatography-tandem mass spectrometry (LC-MS / MS) for the first time. Mass spectrum response signals of the two drugs are remarkably improved by optimizing key conditions such as mass spectrum ion source parameters, collision energy and declustering voltage. Experimental results show that the quantitation limits of riluzole and edaravone in the method provided by the invention are as low as 1 ng / mL, the monitoring requirement under low blood concentration can be met, and the method is particularly suitable for pharmacokinetic research and trace concentration monitoring of patients taking medicine for a long time.

Provided in the present disclosure is the use of edaravone and a pharmaceutically acceptable salt thereof in the prevention and / or treatment of acute high-altitude illnesses caused by acute high-altitude hypobaric hypoxia. The acute high-altitude illnesses include, for example, acute mountain sickness (AMS), high-altitude cerebral edema (HACE), and high-altitude pulmonary edema (HAPE). Additionally provided in the present disclosure is the use of edaravone and a pharmaceutically acceptable salt thereof in the prevention and / or treatment of high-altitude pulmonary hypertension (HAPH) and inflammatory responses caused by acute high-altitude hypobaric hypoxia.

The invention discloses a composition for treating acute ischemic stroke and a preparation method of the composition. The composition is prepared from 80 mg / ml-2. 20 mg / ml of edaravone, 0.48 mg / ml-0. 52 mg / ml of dextroborneol, 0.06 ml / ml-0. 10 ml / ml of propylene glycol, 0.80 mg / ml-1. 20 mg / ml of sodium pyrosulfite and the balance of water for injection, and the pH value of the composition is 3.5-5.5. According to the present invention, the liquid preparation process is optimized and improved, and the step-by-step preparation and mixing process of dissolving edaravone by using 35-45% of the prescription amount of propylene glycol (heating) and dissolving dextroborneol by using the remaining prescription amount of propylene glycol (room temperature) is adopted, such that the drug dissolving effect is ensured, the liquid preparation time can be substantially shortened, the liquid preparation efficiency can be substantially improved, and the industrial production benefit can be well met.

An inhibitor of aggregation of TDP-43 comprising a combination of at least one compound selected from the group consisting of cycloserine and terizidone and their salts, and edaravone. An inhibitor of the aggregation of TDP-43, which contains at least one compound selected from the group consisting of cycloserine and terizidone, and salts thereof, in combination with edaravone. An inhibitor of aggregation of TDP-43 comprising edaravone in combination with at least one compound selected from the group consisting of cycloserine and terizidone and their salts.

The application relates to the technical field of medicines, and discloses application of a tetra-substituted pyrrole derivative in preparation of a product for treating neurodegenerative diseases. The application provides application of the tetra-substituted pyrrole derivative or a pharmaceutically acceptable salt thereof in preparation of the product for treating neurodegenerative diseases. The tetra-substituted pyrrole derivative has high cell safety, and the neuroprotective effect on glutamic acid damage is far higher than that of atrasentan, edaravone and riluzole which are standard clinical drugs; not only can the tetra-substituted pyrrole derivative effectively correct TDP-43 nuclear and cytoplasmic mislocation, but also has the ability of removing insoluble pathological aggregates which atrasentan does not have; the tetra-substituted pyrrole derivative can more effectively inhibit the co-localization of TDP-43 and stress granule protein G3BP1, and intervene in the formation of pathological granules from the source; on a whole animal model, the tetra-substituted pyrrole derivative successfully converts the advantages at the cell level into significant survival benefits, and significantly prolongs the life span of a disease model fruit fly.

The invention relates to an edaravone oral instant film as well as a preparation method and application thereof, and belongs to the technical field of medicines. The invention relates to an edaravone oral instant film. The edaravone oral instant film is prepared from the following raw materials: edaravone, a film forming material and phospholipid, the phospholipid is one or more of soybean phospholipid, lecithin or hydrogenated soybean phospholipid, and the film-forming material is one or more of hydroxypropyl methyl cellulose, polyvinyl alcohol, polyethylene glycol or polyvinylpyrrolidone; the weight ratio of the edaravone to the film-forming material to the phospholipid is 1: (1-5): (1-5). The oral cavity instant film provided by the invention not only meets the requirement that the dissolution rate of the oral cavity instant film is greater than 30% under a non-leakage groove condition, but also can form nanoparticles which can remarkably penetrate through soft palate mucosa after meeting water, and is delivered into the brain through a trigeminal nerve path, so that the bioavailability and local drug concentration of edaravone are remarkably improved, and the oral cavity instant film is suitable for clinical application. Wide application prospects are realized in the application of treating nervous system diseases.

This invention belongs to the field of chemical medicine, specifically relating to a phenylpropanoid compound, its preparation method, and its application. The phenylpropanoid compound specifically refers to the compound, solvate, optically pure isomer, stereoisomer, or pharmaceutically acceptable salt thereof, or mixtures thereof, represented by general formula (Ⅰ), wherein X is selected from O or N; R1, R2, R3, R4, and R5 are the same or different, and are independently selected from hydrogen, hydroxyl, halogen, alkoxy, and alkylthio groups; R 13 Selected from hydrogen or C1-C4 alkyl, or R 13 Connect R5 to form a loop; R 14 The compounds are selected from cycloalkyl groups with 5-6 substituted carbon atoms. The phenylpropanoid compounds synthesized in this invention exhibit significant inhibitory effects on glioma cells, and their inhibitory effect is superior to that of the positive control drugs temozolomide and the original chlorogenic acid. Simultaneously, some of the synthesized phenylpropanoid compounds significantly improve neuronal cell survival rates, and their protective effect is superior to that of the positive control drug edaravone, demonstrating potential for treating stroke.

The application provides a time-sequential drug controlled-release multifunctional intracranial stent and a preparation method, relates to the technical field of vascular stents, and comprises a stent base made of a Fe-based metal material; and, from inside to outside on the surface of the stent base, a bottom coating layer composed of iron oxide nanotubes, wherein the surface of the iron oxide nanotubes is modified by polydopamine and loaded with rapamycin; a middle coating layer formed by the complex of beta-rich silk fibroin and sodium heparin; and a surface coating layer formed by the complex of silk fibroin and edaravone; wherein the setting positions of the surface coating layer, the middle coating layer and the bottom coating layer correspond to the time sequence of drug release in each coating layer, so that the corresponding drugs are released at different stages after the stent base is placed in a blood vessel, so as to adapt to the pathological evolution process in the blood vessel repair process. The application solves the problems of cerebral ischemia-reperfusion injury and vascular restenosis after the current vascular stent is placed in a cerebral blood vessel.