27 results about "Bumetanide" patented technology

The application discloses a kind of bumetanide tablets, raw materials include bumetanide 1 according to mass ratio;Corn starch 81~85;Lactose 50~54;Agar 0.1~0.3;Povidone K304~6;Polysorbate 80, 0.1~0.2;Silicon dioxide 3~4.5;Talcum powder 2~3.3;Magnesium stearate 0.3~0.7.Its preparation method includes the following steps: pretreatment, premixing, granulation, wet granulation, drying, dry granulation, total mixing, tabletting and packaging.The application introduces the synergistic system of trace agar and polysorbate 80 in the prescription.Agar, as a natural hydrophilic colloid, can form a hydrophilic network structure during the granulation process, and synergistically act with polysorbate 80, greatly improving the wettability and dispersibility of the slurry to ultrafine bumetanide, preventing drug agglomeration, so that the drug can be more evenly distributed in the granules during the subsequent drying and tabletting process.

The present invention relates to a pharmaceutical composition for use in the treatment of both low-grade and high-grade glioblastoma in a human subject. The composition comprises a synergistic combination of the following active agents: R-Ketorolac, Bumetanide, and Niflumic acid. This specific combination is designed to exert a synergistic therapeutic effect against glioblastoma by targeting multiple molecular pathways involved in tumor progression, inflammation, and ion transport. In a further aspect of the invention, there is provided a method for selecting a subpopulation of glioblastoma subjects who are responsive to the aforementioned treatment. This method comprises identifying genetic profiles predictive of a favorable therapeutic response to the combined administration of R-Ketorolac, Bumetanide, and Niflumic acid.

The application provides a preparation method of bumetanide, taking p-chlorobenzoic acid as a starting material, performing chlorosulfonation, nitration, and ammonolysis to obtain a key intermediate of 3-(N-(tert-butyl) sulfamoyl)-4-chloro-5-nitrobenzoic acid, then performing phenoxylation, nitro reduction, n-butylation, and tert-butyl removal, and finally obtaining the bumetanide. Compared with the synthesis process of the prior art, the method has less side reactions, low cost, high yield, high safety, and is beneficial to industrial production.

A method and formulations are developed for enhancing solubility and improving the permeability of bumetanide across a mucosal membrane. The formulation includes bumetanide in various water-cosolvent mixtures, which include at least one of an alcohol, polyether, glyceride, pyrrolidone, or any combination thereof. In some embodiments, the formulation has a pH of about 3.5 to about 8.0. In some embodiments, the formulation enhances the solubility and permeability of the bumetanide. Also disclosed is a use of the formulation for rapidly achieving effective bumetanide plasma concentration leading to diuresis. In some embodiments, the formulation can be administered to a subject conveniently without injection in the treatment of edema associated with heart failure or other conditions.

The present disclosure provides methods of treating Alzheimer's Disease (AD) and rescuing cognitive deficits associated with AD in a subject having an apoE4 / 4 genotype, by administering a therapeutically effective amount of the loop-diuretic bumetanide to the subject. Also disclosed are kits for performing the method, including one or more doses of a bumetanide formulation; and which may also include instructions for treating a patient having an apoE4 / 4 genotype by administering bumetanide, and / or instructions and reagents for testing / identifying a subject having an apoE4 / 4 genotype.

The present invention relates to a pharmaceutical composition comprising, as active ingredients, ibudilast and bumetanib for use in the treatment of autism spectrum disorder (ASD) wherein said treatment induces a patient's electroencephalogram (EEG) to produce a favorable alteration.

The present application provides a kind of pharmaceutical composition, the composition comprises therapeutically effective amount of bucumidol, one or more specific antioxidants and other necessary one or more pharmaceutically acceptable pharmaceutical adjuvant, the specific antioxidant is selected from one or more of the following: lipid-soluble vitamin C derivative, or phenolic antioxidant.In addition, a method for improving the stability of bucumidol pharmaceutical composition is also disclosed.The technical scheme of the present application effectively solves the problem of the generation and growth of N-nitroso-bumetanide and other related substances in the production and storage of bucumidol solid preparation, significantly improves the stability of the drug and the safety of drug use.

The invention relates to pharmaceutical composition comprising ibudilast and bumetanide as active ingredients for use in the treatment of autism spectrum disorder (ASD), wherein the treatment induces favorable changes in the EEG of the patient.

The present application relates to a preparation method of bumetanide, and belongs to the technical field of pharmaceutical chemistry. The present application takes 4-chlorobromobenzene as a starting material, and is subjected to sulfonylation, nitration, ammonolysis, substitution, cyanation, nitro reduction, alkylation, and finally acidification to obtain bumetanide. In the synthetic route of the present application, the carboxyl group does not need to be protected, but a cyano group which does not need functional group protection is introduced, and finally the cyano group is directly hydrolyzed into a carboxyl group to obtain bumetanide. The present application has few side reactions, the intermediates can be precipitated in water, greatly reducing the solvent cost, being easier to purify, the quality of the intermediates and bumetanide being easy to control, reducing the production risk, and being more beneficial to industrial mass production.

This invention discloses a highly stable bumetanide solid dosage form comprising bumetanide, an antioxidant, a pH adjuster, a filler, a binder, a disintegrant, a surfactant, a lubricant, and a flow aid. It can solve the problem of N-nitrosobumetanide impurities and other impurities being generated during the production and storage of the dosage form, while maintaining good dissolution behavior.

The invention relates to an aqueous bumetanide-containing liquid comprising: • 0.1-5 wt.% bumetanide; • 0.1-10 wt.% of amine-functional polymer; and • 65-99 wt.% water; wherein the aqueous bumetanide-containing liquid has a pH at 25°C in the range of 4.5 to 8.0. The aqueous bumetanide-containing liquid of the present invention achieves excellent bioavailability upon transmucosal administration. In addition, diuresis is achieved much faster by transmucosal administration of the aqueous bumetanide-containing liquid than by oral administration of known oral bumetanide formulations.

To provide a therapy for patients with autism spectrum disorder (ASD), targeting a subgroup of specific patients sharing a common etiology.SOLUTION: The present invention relates to a pharmaceutical composition comprising ibudilast and bumetanide for use in the treatment of autism spectrum disorder (ASD), where the composition is administered to a patient showing an overactivation of an NF-κB pathway.SELECTED DRAWING: None

The invention provides a bumetanib injection and a preparation method thereof, and particularly relates to the field of medicines. Comprising 1 mg of bumetanib, 5-10 g of glucose, a proper amount of sodium hydroxide and the balance of water for injection, the volume is fixed to 100 ml, and the pH is 5.0-6.0. The preparation method comprises the following steps: S1, weighing bumetanib according to the prescription dosage, stirring the bumetanib and 20% of water for injection according to the prescription dosage at 20-30 DEG C for 10-20 minutes, and dissolving the bumetanib to obtain a solution A; s2, adding the prescription amount of glucose into 70% of the prescription amount of water for injection, stirring and dissolving to obtain a solution BS3, mixing the solution A and the solution B, and adding a sodium hydroxide pH regulator with the concentration of 0.05 mol / L; adjusting the pH to a target value; s4, fixing the volume of the solution obtained in S3 to 100% of the total volume, stirring for 10-20 minutes after fixing the volume, and detecting that the pH value is within a target range; s5, filtering by using a 0.22 mu m PES filter membrane, filling nitrogen and filling, wherein the residual oxygen content is less than or equal to 3.0%; s6, sterilizing for 10-15 minutes at the temperature of 110-130 DEG C after filling and sealing, so as to obtain a target product. According to the invention, bumetanib infusion medication can be realized, the medication safety is improved, and the product stability is good.

The application provides a preparation method of bumetanide, and relates to the technical field of biological medicine synthesis. 4-chloro-3-nitro-5-sulfonamidobenzoic acid, an alkaline reagent, phenol and water are mixed to perform a phenoxylation reaction, the obtained 3-nitro-4-phenoxy-5-sulfonamidobenzoic acid is mixed with a reducing agent and palladium carbon to perform a reduction reaction, the obtained 3-amino-4-phenoxy-5-sulfonamidobenzoic acid is mixed with n-butyl aldehyde, sodium triacetoxyborohydride and an organic solvent to perform a reductive amination reaction, and then bumetanide is obtained. The preparation method provided by the application has a high total yield of products. Moreover, the preparation method provided by the application has the advantages of wide raw material sources, simple synthesis process route, mild reaction conditions, few by-products, high product quality, low cost and suitability for industrial production. As shown in the test results of examples, the total yield of bumetanide prepared by the preparation method provided by the application is more than 37.5%.

The application discloses a preparation process of bumetanide. 4-chloro-3-nitro-5-sulfamoylbenzoic acid is used as a starting material, and nucleophilic substitution is carried out with phenol in potassium hydroxide aqueous solution to obtain a compound with a structural formula Int01; in a methanol-water mixed solvent, palladium-carbon is used as a catalyst, and ammonium formate is used as a hydrogen source for transfer hydrogenation, so that the nitro group on the compound with the structural formula Int01 is reduced to an amino group, and a compound with a structural formula Int02 is obtained; the compound with the structural formula Int02 is subjected to reductive amination with n-butyl aldehyde and sodium triacetoxyborohydride to obtain a crude bumetanide product; after the crude bumetanide product is refined in an acetic acid and cyclohexane system, decolorization is carried out in methanol-water by using activated carbon, and crystallization is carried out to obtain a pure bumetanide product; and the pure bumetanide product is mixed with mannitol, an alkaline adjusting agent and taurine to obtain a finished product.

The present disclosure provides a method of edema in a subject in need thereof. The method includes administering to the subject a pharmaceutical composition comprising bumetanide using a nasal delivery device, wherein the plume generated by the nasal delivery device is characterized by the total volume administered per actuation, the average droplet size, the spray pattern, or the plume geometry.

To provide a pharmaceutical composition and a kit for treating autism spectrum disorder (ASD) that exhibit measurable physiological effects in a patient.SOLUTION: A pharmaceutical composition comprising ibudilast and bumetanide as active ingredients for use in the treatment of autism spectrum disorder (ASD) is provided. The treatment induces favorable changes in the EEG of the patient.SELECTED DRAWING: None

A pharmaceutical composition comprising ibudilast and bumetanide as active ingredients for use in the treatment of autism spectrum disorder (ASD), wherein the treatment induces favourable changes in t

A pharmaceutical composition comprising ibudilast and bumetanide for use in the treatment of autism spectrum disorder (ASD), wherein the composition is administered to a patient showing an overactivat

The present invention relates to bumetanide derivatives of formula (I) as well as pharmaceutical compositions comprising these compounds for use in the treatment or prevention of neurological diseases / disorders involving Na+—K+-2Cl−—cotransporters (NKCCs), such as stroke, traumatic brain injury (TBI), spinal cord injury (SCI), peripheral nerve injury (PNI), brain edema, or glioma, and particularly for use in the treatment or prevention of stroke. The invention likewise relates to a method of treating or preventing a neurological disease or disorder involving an NKCC, such as stroke, TBI, SCI, PNI, brain edema, or glioma, the method comprising administering a compound of formula (I) to a subject in need thereof.

The present invention features methods and compositions for the intranasal, sublingual, and subcutaneous administration of bumetanide for the treatment of subjects suffering from edema refractory to oral diuretics.

The application discloses a high-stability solid preparation of bumetanide, which comprises the following components: bumetanide, an antioxidant, a pH regulator, a filling agent, a binder, a disintegrant, a surfactant, a lubricant and a flow aid. The high-stability solid preparation of bumetanide can solve the generation of N-nitroso-bumetanide impurities and other impurities during the production and storage of the preparation, and meanwhile, good dissolution behavior is maintained.

The invention relates to a preparation method of bumetanib. Specifically, the invention discloses a method for preparing bumetanib by taking a compound with a higher atom utilization rate as a raw material in an inert solvent, introducing a sulfonyl chloride group into the compound and then carrying out a three-step substitution reaction. The method disclosed by the invention is simple to operate, the number of steps is obviously reduced, a noble metal catalyst is not needed, the cost is low, the method is environment-friendly, and industrial production is easy.

Described herein is Bumetanide Dibenzylamide, methods for synthesizing Bumetanide Dibenzylamide, pharmaceutical compositions thereof, and methods of dosing Bumetanide Dibenzylamide for treating epilepsy or other indication for which bumetanide is effective.

This invention discloses a method for preparing a bumetanide nasal administration formulation and its application in the treatment of epilepsy, belonging to the field of pharmaceutical technology. The nasal administration formulation is a bumetanide nasal spray and / or a bumetanide dry powder inhaler. The drug is used for immediate administration intervention within 30 minutes after an epileptic seizure in non-medical settings, including at home, outdoors, or during transport. In this invention, the bumetanide nasal spray or dry powder inhaler does not require intravenous puncture or operation by professional medical personnel. Patients or their families can administer the drug directly through the nasal cavity within 30 minutes after an epileptic seizure at home, outdoors, or during transport, breaking through the dependence of traditional intravenous injection on medical settings and equipment, and buying valuable time for neuronal resuscitation.

The present invention relates to bumetanide, or a salt or a solvate or an analog thereof, for use in treating autism spectrum disorders in specific subpopulations of patients.

The present invention relates to a pharmaceutical composition comprising ibudilast and bumetanide for use in the treatment of autism spectrum disorder (ASD) wherein the composition is to be administered to a patient exhibiting excessive activation of the NF-[kappa] B pathway.