58 results about "Edaravone" patented technology

The invention provides a preparation method of an edaravone and dextroborneol injection, the injection comprises edaravone, dextroborneol, propylene glycol and sodium pyrosulfite, in the preparation process, the propylene glycol accounting for 60%-85% of the prescription dosage and water accounting for 5%-25% of the prescription dosage are injected into a liquid preparation tank according to the volume ratio, the mixture is heated to 50-60 DEG C, edaravone is added and stirred to be dissolved, and the edaravone and dextroborneol injection is prepared. The preparation method comprises the following steps: dissolving propylene glycol in the remaining prescription dosage, adding dextroborneol which is dissolved by propylene glycol in the remaining prescription dosage in advance, uniformly stirring, adding water which is close to a constant volume, cooling to 25 DEG C or below, adding sodium pyrosulfite, adjusting the pH value to 4.0-5.0, and fixing the volume to a full volume. According to the preparation method of the edaravone dextroborneol injection, auxiliary materials in a specific proportion are matched with the preparation steps, the problem that raw material medicines are extremely easy to separate out in the preparation process is solved, the requirement of the preparation process for an industrial liquid preparation tank is low, industrial operation is convenient, and the preparation cost is low.

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 provides multifunctional hydrogel carrying neural stem cells. The multifunctional hydrogel mainly comprises the following components: chitosan, beta-sodium glycerophosphate, edaravone, nerve growth factors and the neural stem cells, the invention also provides a method for preparing the multifunctional hydrogel, which comprises the following steps: preparing temperature-sensitive hydrogel by taking a chitosan solution and a beta-sodium glycerophosphate solution as matrixes, preparing an edaravone-nerve growth factor mixed solution, and preparing the edaravone-nerve growth factor composite hydrogel. Sequentially adding a neural stem cell suspension and the mixed solution into a hydrogel system to obtain the multifunctional hydrogel carrying the neural stem cells. The multifunctional hydrogel disclosed by the invention realizes high-efficiency integration of three core functions of temperature-sensitive positioning, drug sustained-release microenvironment regulation and control and cell proliferation and differentiation support, and can remarkably promote spinal cord injury repair.

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 belongs to the technical field of medicines, and particularly relates to an alpha-lipoic acid phenothiazine derivative as well as a preparation method and application thereof. The structural formula of the alpha-lipoic acid phenothiazine derivative is as shown in formula 1. The invention provides an alpha-lipoic acid phenothiazine derivative, and research finds that the alpha-lipoic acid phenothiazine derivative shows good anti-inflammatory activity which is slightly superior to that of alpha-lipoic acid. Moreover, the effect of the pharmaceutical composition is better than that of a positive drug edaravone clinically used in cerebral arterial thrombosis at present, and the pharmaceutical composition can be further developed into a treatment drug applied to ferroptosis related diseases. .

The invention relates to the technical field of sustained-release preparation, in particular to a microcrystalline sustained-release preparation and a preparation method thereof.The sustained-release preparation comprises a core composed of edaravone rodlike microcrystals and a shell composed of 2-4 double layers, the shell comprises at least one polyethylene glycol-polylysine copolymer inner layer, and the polyethylene glycol-polylysine copolymer inner layer is a polyethylene glycol-polylysine copolymer outer layer. And at least one outer layer of hyaluronic acid modified with a CD44 targeting peptide. The CD44 targeting peptide modified by the shell layer can specifically recognize a CD44 receptor on the surface of an inner ear hair cell, so that the binding efficiency of a preparation, a round window membrane and a target cell is remarkably improved, the diffusion of a drug to non-target tissues is reduced, and the local drug concentration is improved.

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.

The present invention relates to liquid pharmaceutical compositions of edaravone. More specifically, stable solutions of edaravone for enteral administration are provided, wherein the composition is stable for extended period of time. The present invention further relates to stable solutions of edaravone, methods for their administration, processes for their production, and use of these compositions for treatment of diseases treatable by edaravone.

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 discloses an edaravone film quick-release preparation composition which comprises edaravone or pharmaceutically acceptable salts, prodrugs, metabolites, solvates, crystals or deuterated substances of edaravone and auxiliary materials. The weight percentage of the edaravone or the pharmaceutically acceptable salt, prodrug, metabolite, solvate, crystal or deuterated substance is 1%-60%. The edaravone oral cavity soluble film quick release preparation is used for sublingual administration, and has the characteristics of quick disintegration and good taste.

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.