33 results about "Probenecid" patented technology

The invention relates to a preparation method of a 4-(dipropyl sulfamoyl)-N, N-dipropyl benzamide impurity reference substance, which is characterized by comprising the following specific steps: 1, carrying out acylating chlorination reaction on probenecid and thionyl chloride under the catalysis of DMF (N, N-dimethylformamide), and distilling and concentrating to obtain an intermediate probenecid acyl chloride; 2, carrying out amidation reaction on probenecid acyl chloride and dipropylamine to obtain a product reaction solution; and 3, purification: adjusting the pH value of the reaction liquid to be alkaline by using a sodium hydroxide solution, adding purified water for extraction, taking an upper organic phase, adding hydrochloric acid, precipitating a solid, filtering, washing a filter cake by using purified water, and drying at low temperature. The sample is a white solid, the HPLC purity is greater than or equal to 98%, the content is greater than or equal to 99%, no solvent residue exists, and the technical requirement of serving as an impurity reference substance is completely met.

The invention relates to a method for removing halogenated alkyl toxic impurities in probenecid sodium, which is characterized by comprising the following steps of: 1, heating and hydrolyzing excessive halogenated alkyl under an alkaline condition to remove the halogenated alkyl toxic impurities; 2, organic solvent extraction and removal; 3, adsorption removal by a specific adsorption column; after the treatment by the method, the residue of haloalkane is reduced to be not detected from 15-100ppm, and the limit requirements of related genotoxic impurities in Chinese drug registration regulations and ICH guidance principles are completely met.

Disclosed herein are methods, compounds, and compositions for treating or preventing an inflammasome-mediated disease or condition, including an inflammasome-mediated pulmonary disease or condition.

The invention relates to a method for determining the content of di-n-propylamine impurities in probenecid sodium. The method is characterized by comprising the following steps: 1) preparing a blank solution; 2) preparing a reference solution; 3) preparing a test solution; 4) giving chromatographic conditions; 5) system applicability requirement; 6) precisely measuring the test solution and the reference solution by a determination method, respectively injecting into a gas chromatograph, recording chromatograms, and calculating the content according to an external standard method; the content of the di-n-propylamine impurity in the probenecid sodium can be effectively and accurately detected. The established gas chromatographic method for determining the probenecid sodium di-n-propylamine impurity has the advantages of strong specificity, high sensitivity, good linearity and good accuracy, and can provide research reference for quality control and evaluation of the probenecid sodium di-n-propylamine impurity.

The invention relates to a method for determining related substances of a compound preparation cefprozil and probenecid tablet, which is characterized in that the related substances are detected by high performance liquid chromatography, the related substances are impurities in the compound preparation cefprozil and probenecid, and the content of the impurity cefadroxil, other single impurities and total impurities is determined; wherein the mobile phase A is a 0.23% ammonium dihydrogen phosphate solution, and the mobile phase B is HPLC (High Performance Liquid Chromatography) grade methanol; a sample is diluted by a diluent and then is injected, the diluent is a mixed solution of a 0.23% ammonium dihydrogen phosphate solution and HPLC-grade methanol, the sample injection amount of the sample is 5 [mu] L, the concentration of cefprozil is 1.5 mg / mL, and the concentration of probenecid is 2.25 mg / ml; according to the present invention, the related substances in the cefprozil and the probenecid can be simultaneously detected, the detection cost is reduced, the method has advantages of strong specificity, high sensitivity, good reproducibility and good accuracy, has certain feasibility and practicality, is easy to popularize and apply, and can provide the research reference for the quality control and evaluation of the product.

The invention relates to a process for purifying and salifying a probenecid crude product, which is characterized in that the purpose of removing organic impurities, inorganic impurities and harmful solvent residues in the probenecid crude product is achieved by utilizing the dissolvability difference of probenecid acid and salt thereof and transferring the probenecid acid and the salt thereof in a water phase and an organic phase for many times, and a high-purity probenecid solution is obtained. And reacting the probenecid solution with a salt-forming agent to obtain the probenecid sodium. The purity of the probenecid purified by the process can reach more than 99.9% (HPLC), solid-liquid separation and intermediate drying are not needed in the purification and salification processes, continuous production can be realized, the production period is shortened, and the process is suitable for industrial production.

The present invention relates to a method for preparing probenecid ethyl, characterized in that the specific steps are as follows: take a four-mouth reaction bottle and add probenecid, then add anhydrous ethanol, start stirring, slowly heat up until probenecid is completely dissolved, add 4a molecular sieves to the four-mouth bottle, continue to heat up to reflux, and the reaction solution gradually becomes turbid; reflux decolorization for 20-30mins, cool down after decolorization is completed; filter the reaction solution, start the freeze-drying procedure; the freeze-dried powder is a white or off-white crystalline powder, and probenecid ethyl is prepared. Its purity can reach more than 99.0% (by HPLC); the content of the impurity is further detected by H-NMR to be 98.2%, which can be used as an impurity reference.

The invention discloses a eutectic probenecid soluble microneedle as well as a preparation method and application thereof, and belongs to the technical field of microneedle preparations. The technical problem to be solved is to provide the preparation method of the deep-eutectic probenecid soluble microneedle with excellent mechanical property and better dissolution and transdermal penetration capacity. The deep-eutectic probenecid soluble microneedle disclosed by the invention improves the solubility and bioavailability of probenecid. The key point of the technical scheme is as follows: the eutectic probenecid soluble microneedle comprises the following components: probenecid, a eutectic solvent and a matrix material, wherein the eutectic solvent comprises basic amino acid and polyhydric alcohol; the molar ratio of the basic amino acid to the polyhydric alcohol is 1: (5-7.5).

Probenecid or a pharmaceutical acceptable salt thereof for use in the treatment of a neurological disorder in a subject in need thereof, wherein administration of probenecid or a pharmaceutical acceptable salt thereof controls clinical or electrographic seizures in the subject. Preferably, the neurological disorder is an epileptic disease, disorder or condition.

The present disclosure relates to combinations of valproic acid or a pharmaceutically acceptable salt thereof, a β-lactam compound or a pharmaceutically acceptable salt thereof, and probenecid or a pharmaceutically acceptable salt thereof. The present disclosure also relates to methods of treating or preventing a disease using the combinations.

The invention relates to a full-substituted 5, 5 '-bisoxazole compound which is constructed by N-(1-aryl vinyl) amide catalyzed by transition metal through a repeated cross dehydrogenation coupling strategy. Specifically, under the condition of an inert solvent, under the common promotion of a transition metal catalyst and a silver salt oxidizing agent, multi-time dehydrogenation 1, 1-bifunctionalization of olefin is realized. The method has better regioselectivity and chemical selectivity, and is worthy of noting that the invention reports the first case of simple construction of a fully-substituted 5, 5 '-biazole compound skeleton based on a multi-dehydrocyclization strategy through transition metal catalysis, and the converted substrate is wide in application range and strong in functional group tolerance. The applicant also realizes modification of drug molecules such as probenecid. Furthermore, the obtained 5, 5 '-bisoxazole molecules are subjected to fluorescence test, and the fluorescence quantum yield reaches 83.14%, which indicates that the novel skeleton has great application potential in the aspect of luminescent materials.

The present invention relates to a core-shell formulation presenting a core, said core comprising probenecid in an amount ranging from 10% to 70% in weight relative to the total weight of the core, in association with at least one pharmaceutically acceptable excipient; wherein the core is coated with a shell coating comprising triethyl citrate, a mineral charge, polyvinyl acetate, polyvinylpyrrolidone and sodium lauryl sulfate, wherein the weight ratio of polyvinyl acetate on polyvinylpyrrolidone ranges from 1.5 to 4.

To provide a composition which increases contractility of cardiac muscle without increasing the cell death in contrast to a commonly used β-agonist, isoproterenol.SOLUTION: A composition containing probenecid and administered by at least one of injection, oral administration and transdermal administration can increase the calcium concentration in a heart cell without increasing the cell death.SELECTED DRAWING: None

The present disclosure relates to a combination of valproic acid or a pharmaceutically acceptable salt thereof, a β-lactam compound or a pharmaceutically acceptable salt thereof, and probenecid or a pharmaceutically acceptable salt thereof. The present disclosure also relates to methods of treating or preventing disease using this combination.

The subject invention provides pharmaceutical compositions comprising combinations of probenecid or a pharmaceutically acceptable salt thereof, and one or more carboxylic acid aldose reductase inhibit

Disclosed herein are methods, compounds, and compositions for treating or preventing inflammasome-mediated diseases or conditions, including inflammasome-mediated lung diseases or conditions.

The present disclosure provides a combination of a beta-lactam compound and probenecid and uses thereof. The present disclosure relates to a bilayer tablet comprising a second layer comprising a beta-lactam compound or a pharmaceutically acceptable salt thereof; and a first layer, the first layer comprising probenecid or a pharmaceutically acceptable salt thereof. The present disclosure also relates to methods of treating or preventing disease using the bilayer tablets.

The invention belongs to the technical field of veterinary drugs for poultry, and discloses a probenecid solution for poultry and application thereof, and the probenecid solution is prepared from probenecid, a cosolvent, an antioxidant, a complexing agent, a stabilizer and the balance of water according to a specific proportion. The prepared probenecid solution has the characteristics of rapid and complete absorption after oral administration, is used for drinking water for poultry, and has the advantages of accurate dosage, easiness in administration, good safety and convenience in use. The probenecid solution solves the problems that the existing probenecid solution is poor in stability and inconvenient to orally take by poultry by adjusting the proportion of the raw material components and specifically adding specific auxiliary substances. The product disclosed by the invention is suitable for preparing the poultry anti-gout medicine.

Compositions and methods of treating a coronavirus infection in a subject are provided. The methods generally include administering to the subject an effective amount of a probenecid, metabolite or analog thereof, or a pharmaceutically acceptable salt thereof. The methods can be therapeutic and / or prophylactic. The amount of probenecid, metabolite or analog thereof, or a pharmaceutically acceptable salt thereof can be effective, for example, to reduce viral replication, reduce one or more symptoms of a disease, disorder, or illness associated with the virus, or a combination thereof. In preferred embodiments, the virus is a severe acute respiratory syndrome-associated coronavirus, such as SARS-CoV-2 or SARS-CoV, a Middle East respiratory syndrome-associated coronavirus, such as MERS-CoV, or a coronavirus that causes the common cold.

The present disclosure relates to bilayer tablets comprising a second layer comprising a β-lactam compound or a pharmaceutically acceptable salt thereof; and a first layer comprising probenecid or a pharmaceutically acceptable salt thereof. The present disclosure also relates to methods of treating or preventing a disease using the bilayer tablets.

The invention belongs to the technical field of veterinary drugs for poultry, and discloses a preparation method of a probenecid solution for poultry, and the probenecid solution prepared by adding raw materials such as probenecid, a cosolvent, an antioxidant, a complexing agent, a stabilizer and the like according to a specific adding sequence and carrying out a specific temperature dissolving and filtering process has the characteristics that the pH value is still stable after long-term storage, and the probenecid solution has the characteristics of high stability, high stability and the like. And when the water is used for drinking water for poultry, the dosage is accurate, the administration is easy, the safety is good, and the use is convenient. The probenecid solution solves the problems that the existing probenecid solution is poor in stability and inconvenient to orally take by poultry by adjusting the proportion of the raw material components and specifically adding specific auxiliary substances. The product disclosed by the invention is suitable for preparing the poultry anti-gout medicine.

The present disclosure relates to combinations of a β-lactam compound or a pharmaceutically acceptable salt thereof and probenecid or a pharmaceutically acceptable salt thereof. The present disclosure also relates to methods of treating or preventing a disease via administering to subjects in need thereof a β-lactam compound or a pharmaceutically acceptable salt thereof and probenecid or a pharmaceutically acceptable salt thereof.

Disclosed herein are methods, compounds, and compositions for treating or preventing inflammasome-mediated dermatological diseases or conditions.

The invention belongs to the field of animal husbandry and veterinary medicine, and discloses a method for detecting the content of probenecid in a poultry probenecid solution, the content of probenecid in the probenecid solution is determined by adopting a high performance liquid chromatography, the mobile phase of the high performance liquid chromatography is a sodium dihydrogen phosphate solution and acetonitrile which are equal in volume, and the mobile phase of the high performance liquid chromatography is acetonitrile. The sodium dihydrogen phosphate solution contains glacial acetic acid with the mass fraction of 1%. According to the method, the probenecid content in the probenecid solution for poultry can be accurately, qualitatively and quantitatively determined.

To provide an ATP production promoter useful for preventing or treating diseases associated with decreased ATP production, particularly renal impairment. [Solution] The present invention comprises an ATP production promoter containing a component having URAT1 inhibitory activity. Preferably, the component having URAT1 inhibitory activity is at least one selected from the group consisting of benzbromarone, probenecid, dotinurad, recinurad, and berinurad. The present invention is expected to be useful as a preventive and therapeutic agent for diseases of decreased ATP production, and is particularly useful as a therapeutic and / or preventive agent for nephrotic syndrome, chronic glomerulonephritis, chronic tubulointerstitial nephritis, chronic pyelonephritis, amyloid kidney, familial juvenile hyperuricemia nephropathy, autosomal dominant tubulointerstitial kidney disease, nephronoplasia, renovascular hypertension, renal vein thrombosis, renal arteriovenous fistula, renal tubular acidosis, Gitelman syndrome, Bartter syndrome, Fanconi syndrome, Lowe syndrome, Alport syndrome, kidney and ureteral stones, and chronic renal failure.

The present invention discloses a compound comprising quercetin and probenecid derived from the Japanese blueberry tree, as well as its preparation method and application. The compound comprising quercetin and probenecid derived from the Japanese blueberry tree of the present invention has a structural formula as shown in Formula (I): #imgabs0# The compound comprising quercetin and probenecid derived from the Japanese blueberry tree of the present invention is synthesized through a series of chemical reaction steps, including solvent dissolution, heating and stirring, vacuum concentration, extraction, and silica gel column chromatography. The derivative of the quercetin and probenecid derived from the Japanese blueberry tree of the present invention exhibits enhanced biological activity and therapeutic effects through structural modification. The compound of the present invention has a significant effect on lowering blood uric acid, blood sugar, and serum total cholesterol, and increasing serum total protein levels in experimental mice.

The present invention relates to probenecid or a pharmaceutically acceptable salt thereof for use in the treatment of neurological disorders in a subject in need thereof wherein administration of probenecid or a pharmaceutically acceptable salt thereof controls clinical or electrographic seizures in said subject. Preferably, the neurological disorder is an epileptic disease, disorder or condition.

The present invention relates to a core-shell particulate formulation presenting a core comprising probenecid in an amount ranging from 10% to 70% in weight relative to the total weight of the core, in association with at least one pharmaceutically acceptable excipient, wherein the core is coated with a shell coating composition comprising triethyl citrate, a mineral charge, polyvinyl acetate, polyvinylpyrrolidone and sodium lauryl sulfate, characterized in that the weight ratio of polyvinyl acetate on polyvinylpyrrolidone ranges from 1.5 to 4.

The invention relates to a preparation method for salifying and freeze-drying probenecid, which is characterized by comprising the following steps: reacting probenecid and a salt-forming agent in injection water to form salt, adding a pH regulator to regulate the pH value, adding absolute ethyl alcohol, adsorbing and decolorizing with activated carbon, filtering, and freeze-drying to obtain the product, the probenecid comprises probenecid, sodium hydroxide and sodium carbonate according to a molar ratio of 1: 1: 0.01, a solvent is injection water containing 3%-5% of ethanol, and freeze-drying comprises pre-freezing, annealing, heating to melt small ice crystals, and re-freezing. The probenecid sodium freeze-dried powder is good in appearance property, stable in salt forming rate, controllable in pH and capable of improving the redissolution time, the product freeze-drying process efficiency is improved, and it is guaranteed that the product quality is controllable. The process is simple and suitable for industrial production.