61 results about "Benzbromarone" patented technology

The invention relates to a medicinal composition for treating hyperuricemia, which comprises Febuxostat or derivate thereof, benzbromarone and a pharmaceutically acceptable medicinal carrier, whereinthe ratio in weight portion of the Febuxostat or derivate thereof to the benzbromarone to the pharmaceutically acceptable medicinal carrier is 1:1-4:0.5-100. The medicinal composition can provide extremely beneficial effects of treating the hyperuricemia. Pharmacological tests prove that the medicinal composition has obviously synergistic action, can quickly reduce the concentration of purine trione in blood serum, remarkably improves effect of treating the hyperuricemia, greatly reduces medicament dosage of single component simultaneously, and effectively reduces toxic and side effect of medicament.

The invention relates to the field of drug synthesis and in particular relates to a method for preparing benzbromarone. The method for preparing benzbromarone is characterized by comprising the steps of carrying out an acetylation reaction, a Friedel-Craft reaction, a hydrolysis reaction and the like to prepare the benzbromarone by using 3,5-dibromo-4-hydroxybenzoic acid and 2-ethyl benzofuran as raw materials. The preparation method disclosed by the invention has the advantages of being simple and safe to operate, convenient for post-treatment, high in product purity, low in economic cost, small in environment pollution, easier to realize industrialization and the like.

The dispersive allopurinol and benzbromarone tablet has allopurinol and benzbromarone in the ratio of 5, and can disintegrate completely in 100 ml water at 20 deg.c within 3 min and through No. 2 sieve. It has the functions of treating various kinds of hyperuricemia and its clinical complications, especially gout with symptom, as well as various diseases resulting in raised uric acid in blood.

The invention discloses a method for preparing benzbromarone tablets. By the method, the dissolution of the benzbromarone tablets can be obviously improved. The method comprises the following steps of: treating a benzbromarone raw material by a jet milling method until the particle size D50 is 5mu m; combining part of dodecyl sodium sulfate and Tween-80 in a prescription with the micronized raw material through a fluidized bed; and pelletizing and tabletting the obtained material and other auxiliary materials. The dissolution of the prepared tablets is obviously improved.

The invention relates to benzbromarone of crystal form B applied in the field of chemical pharmacy, and its preparation method. In the X-ray powder diffraction pattern represented by 2theta angles of the benzbromarone of crystal form B, the error range of the 2theta angles is +/-0.2, and the benzbromarone of crystal form B has a basic X-ray powder diffraction pattern; and in the differential scanning calorimetry pattern of the benzbromarone of crystal form B, a maximum endothermic peak exists when the heating speed is 10DEG C/min, and the maximum endothermic peak begins at 150.54DEG C, reaches the top at 151.62DEG C and ends at 153.82DEG C, the melting point is 151.66DEG C; when 10ml of trichloromethane is added to 1.0g of the benzbromarone of crystal form B at 25DEG C, a very small amount of the benzbromarone of crystal form B is not dissolved, and the obtained solution is not clear; and 25ml of N,N-dimethyl formamide is added to the 1.25g of benzbromarone of crystal form B, the benzbromarone of crystal form B is complete dissolved, and the obtained solution is clear. The benzbromarone of crystal form B has good stability, and the preparation method has the advantages of simplicity, low cost, simple post-treatment, high product purity and few relevant substances.

The invention discloses a composite western medicine formula for treating gout. The composite western medicine is prepared from, by weight per granule, 0.2-0.5 g of sucralfate, 0.01-0.2 g of diclofenac sodium, 0.01-0.1 g of magnesium oxide, 0.1-0.3 g of benzbromarone and 0.2-1.5 g of chitin. According to the composite western medicine formula for treating the gout, the good gout treatment using effect is achieved; the activity of xanthine oxidase can be inhibited by using the benzbromarone, and therefore the concentration of uric acid in human blood is effectively lowered; by using the sucralfate, a layer of a protective film is formed to cover the ulcer surface, the effect of protecting the gastric mucosa is achieved, the using side effects of medicine on patients suffering from gastric ulcer and the like are effectively reduced, and meanwhile the effects of eliminating inflammation and relieving pain are obvious; by using the chitin, the effects of activating cells in a human body, preventing cell aging, promoting a newly-born cell band, adsorbing harmful heavy metal ions in the body, promoting human body detoxifying and the like can be achieved; gout patients can be effectively treated, and use is very convenient.

The invention discloses a method for simultaneous determination of benzbromarone, allopurinol and probenecid in health food, which comprises the following steps: (1) sample pretreatment; (2) standard solution preparation; (3) benzbromarone, allopurinol and probenecid content determination. In the method, a sample to be determined is purified by QuEChERS Extract after extraction with ammonia water-acetonitrile, and positive and negative ion-exchange scanning is performed by a HPLC-MS/MS method to solve the technical difficulty that the difference in the chemical properties of the benzbromarone, allopurinol and probenecid is large, so that simultaneous extraction and determination is difficult to realize, and also solve the problems that the health food matrix interference is serious, and the recovery rate is low; the method for online simultaneous determination of the content of the benzbromarone, allopurinol and probenecid in anti-gout health food is established, which fills the technical gap in simultaneous determination of the content of the benzbromarone, allopurinol and probenecid in the anti-gout health food.

The invention discloses a traditional Chinese medicine composition for treating gouty arthritis. An active ingredient of the traditional Chinese medicine composition for treating the gouty arthritis is prepared from the following raw material medicines in parts by weight: 30-60 parts of rhizoma smilacis glabrae, 20-40 parts of radix astragali, 5-10 parts of radix platycodonis, 10-30 parts of rhizoma alismatis, 20-40 parts of semen plantaginis and 15-40 parts of herba epimedii. The traditional Chinese medicine composition for treating the gouty arthritis, disclosed by the invention, has the advantages of simple composition, good safety, no obvious toxic and side effects on lever and kidney, and obvious effect of reducing uric acid level and protecting the kidney. The traditional Chinese medicine composition for treating the gouty arthritis, disclosed by the invention, has the advantages that effect of the traditional Chinese medicine composition in reducing the uric acid level and improving inflammatory marks is equivalent to the effect of uric-acid-lowering drug benzbromarone; and the effect of the traditional Chinese medicine composition in improving glomerular filtration rate issuperior to the effect of the uric-acid-lowering drug benzbromarone.

The invention provides a process for preparing a key intermediate 2-ethyl-3-p-hydroxybenzoyl-benzofuran of benzbromarone. The process comprises the following steps of: (1) by taking 2-ethyl-3-p-methoxybenzoyl-benzofuran as a raw material and alkylbenzene as a reaction solvent, reacting the raw material with the reaction solvent in the presence of an acidic catalyst by a certain quantity; (2) after cooling by using ice water, adding a bit of diluted hydrochloric acid and separating out the water layer, performing decompression distillation on the organic layer so as to recover the solvent, and then concentrating the organic layer until the organic layer is dry; (3) adding a diluted basic liquid to the organic layer concentrated liquid obtained in the step (2), separating out the water layer, adding diluted hydrochloric acid to the water layer for adjusting the pH to the range from 1 to 4, and then adding haloalkane for extraction, and slowly distilling the extract until the extract becomes dry, thereby obtaining solid; and (4) performing recrystallization separation on the solid obtained in the step (3) by using petroleum ether, thus obtaining the 2-ethyl-3-p-hydroxybenzoyl-benzofuran of benzbromarone. The yield is over 90% and the liquid phase content is greater than or equal to 98%. The process is easy to control, greatly reduced in cost, and convenient for realizing industrial mass production.

The invention relates to a benzbromarone crystal form A applicable to the field of chemical pharmacy and a preparation method thereof. In an X-ray powder diffraction pattern represented by a 2theta angle, the error range of the 2theta angle is +/- 0.2. The benzbromarone crystal form A has the basic X-ray powder diffraction pattern. In the differential scanning calorimetry pattern, when the heating speed is 10 DEG C per minute, the benzbromarone crystal form A has a maximal endothermic peak, and the melting point value of the benzbromarone crystal form A is 152.23 DEG C. The method comprises the following steps: under the condition of 25 DEG C, taking 1.0g of benzbromarone crystal form A, and adding 10ml of trichloromethane, wherein the solid is completely dissolved, and the solution is clear; taking 1.25g of benzbromarone crystal form A, and adding 25ml of N,N-dimethylformamide, wherein the solid is slightly insoluble, and the solution is not clear; and crystallizing from a single solvent acetone to obtain the benzbromarone crystal form A. The crystal form has the advantages of high stability, simple preparation method, low cost, simple after-treatment, high product purity and fewer related substances.

The invention relates to the field of medicines, in particular to a compound allopurinol dispersible tablet. The tablet is prepared by the following steps of: respectively sieving 100g of allopurinol, 20g of benzbromarone, 22g of sodium starch glycolate and 4g of superfine silica gel powder by a sieve of 80 meshes; putting 104g of microcrystalline cellulose in an oven at the temperature of 80 DEG C, baking for 2 hours, and sieving by the sieve of 80 meshes for later use; taking the prescription amounts of allopurinol and benzbromarone, and uniformly mixing by an equivalent amount increasing method; taking the prescription amounts of sodium starch glycolate and microcrystalline cellulose and half of the prescription amount of superfine silica gel powder, adding into the mixture of allopurinol and benzbromarone by the equivalent amount increasing method, and uniformly mixing; taking the mixture, using water as an adhesive to make damp mass, sieving by a sieve of 24 meshes to granulate, drying for 3 hours at the temperature of 60-70 DEG C, and arranging particles by a sieve of 22 meshes; uniformly mixing the left half of the prescription amount of superfine silica gel powder with the particles and tabletting, and the weight of each tablet is 0.25g.

The invention discloses a preparation method for benzbromarone (formula I). The preparation method comprises the following steps: using (4- hydroxyphenyl)-(2-ethylbenzofuran-3-yl) ketone (formula II)as a raw material, using crown ether-bromine as a brominating agent, and preparing the benzbromarone in a room temperature through a bromination reaction. A by-product HBr is absorbed by diluted alkali solution for salifying, and used for preparing the crown ether-bromine. The beneficial effect is that the crown ether-bromine is used as the brominating agent, a utilization ratio of bromine is high, generated impurities are less, the reaction conditions are moderate, and crown ether and HBr can be recycled.

The invention provides a compound preparation for treating hyperuricemia and gout. Specifically, the invention provides a composition, which comprises (a) a first active ingredient, wherein the first active ingredient is a 1,2,4-triazole compound or a pharmaceutically acceptable salt thereof; and (b) a second active ingredient, wherein the second active ingredient is benzbromarone or a pharmaceutically acceptable salt thereof. The first active ingredient and the second active ingredient can synergistically play a role in treating hyperuricemia and gout and reduce side effects.

The invention discloses a drug for treating cirrhosis with ascites, a preparation method thereof and an application; the drug is prepared from, by weight, 7-15 parts of catechinic acid, 1-5 parts of benzbromarone, 11-19 parts of chitin, 3-7 parts of usnic acid. The drug is prepared by mixing and grinding benzbromarone and chitin; sieving through 120 meshes; adding 3.7 times of deionized water by mass of the both; then raising temperature to 81-83 DEG C, and stirring for 36-39 min under the temperature; preparing a mixture A; placing usnic acid and catechinic acid in a mixture A, then performing ultrasound treatment on the mixture for 28 min at 56 DEG C; stirring the mixture until dry at 61 DEG C, and prilling the mixture. The total effective rate for treating the cirrhosis with ascites is 98% above, and the drug can improve liver function of patients, correct hypoproteinemia and rapidly remove ascites, while reduce complication. The raw materials are simple and easy to acquire, the preparation technique is simple, the production cost is low, the treatment effect is good, and visible effect is quick; the drug is free from toxic and side effects, and applicable to large-scale production and popularization.

The invention discloses a method for screening uric acid-lowering small molecule compounds for promoting uric acid excretion based on a patch clamp technology. The method comprises the following stepsof: constructing recombinant plasmids for expressing a GLUT9 gene; instantaneously transfecting the recombinant plasmids to an HEK293T cell; after 18-24 hours, recording the change of a current whenthe GLUT9 cells are expressed to transport uric acid by utilizing a patch clamp technology; and verifying the reliability of the model through positive drugs, namely benzbromarone and probenecid, andnegative drugs, namely RDEA3170 and allopurinol. The method is simple, convenient and rapid to operate; the result is stable, reliable and good in reproducibility; compared with an existing method fordetecting isotope uptake by using xenopus oocytes, the method has the advantages that the consumed time is shorter, the cost is lower, and high-throughput screening of the GLUT9 inhibitor can be achieved.

The invention discloses a method for preparing benzbromarone. According to the method, 3, 5-dibromo-4-hydroxybenzoic acid is used as a raw material, dihydropyran is used as a hydroxyl protection reagent to prepare benzbromarone, and dihydropyran hydroxyl protection and hydroxyl deprotection are realized through explored optimized process conditions so that the purposes of reducing the generation of byproducts in the reaction process, increasing the yield and reducing the cost are achieved.

The invention discloses a Chinese and western medicine composition for curing liver cirrhosis ascites, and a preparation method and an application of the Chinese and western medicine composition. The Chinese and western medicine composition comprises the following materials in parts by weight: 7-15 parts of aminophylline, 1-5 parts of benzbromarone, 11-19 parts of L-carnitine, and 3-7 parts of taurine. The benzbromarone and the L-carnitine are mixed, grinded, and screened by a 120-mesh sieve; deionized water, whose mass is 3.7 times the total mass of both the benzbromarone and the L-carnitine, is added, the temperature is raised to 81-83 DEG C, and the benzbromarone, the L-carnitine and the deionized water are stirred at the temperature for 36-39 minutes to obtain a mixture A; the taurine and the aminophylline are added into the mixture A, ultrasonic treatment is carried out at the temperature of 56 DEG C for 28 minutes, the mixture is then stirred at the temperature of 61 DEG C to dry, and pelletizing is implemented to obtain the Chinese and western medicine composition. The total effective rate of the Chinese and western medicine composition for curing liver cirrhosis ascites is up to more than 98%, the liver function of a patient is improved, the hypoproteinemia is corrected, the ascites is rapidly eliminated, and meanwhile, the complication is reduced. The materials are simple and easy to get, the preparation process is simple, the production cost is low, the curative effect is good, and the Chinese and western medicine composition becomes effective rapidly, has no toxic or side effects, and is suitable for large-scale production and popularization.

The invention discloses a preparation method and application of a pseudo-positive drug X-333 with uric acid reducing and gout resisting effects, and the preparation method of the pseudo-positive drug X-333 with the uric acid reducing and gout resisting effects comprises the following steps: (1) weighing gCMC-Na, adding water to boil to completely dissolve the gCMC-Na, cooling to room temperature, transferring into a volumetric flask, and measuring the content of the gCMC-Na in the volumetric flask; diluting with purified water to the maximum scale line; (2) preparing hypoxanthine: weighing xanthine, and dissolving the xanthine in a CMC-Na solution; (3) preparation of benzbromarone: weighing 0.05 to 0.1 g of benzbromarone, and dissolving the benzbromarone in the CMC-Na solution; (4) preparing a spartina parviflora extract solution; (5) preparing a licorice extract solution; and (5) preparing the quasi-positive medicine X-333, so as to prepare a solid product of the quasi-positive medicine X-333. The medicine is high in safety and obvious in medicine effect, and the medicine prepared according to the formula can be taken for a long time.

The invention provides a Chinese patent medicine for treating gout. The compound preparation capable of reducing concentration of serum uric acid and treating gout is characterized by being prepared from the following components in percentage by weight: 30 percent of rhizoma smilacis glabrae, 15 percent of yam rhizome, 10 percent of benzbromarone, 10 percent of eleutheroside, 5 percent of picroside, 10 percent of triptolide, 10 percent of croceic acid and 10 percent of cordycepic acid, and the eight medicinal materials are mixed according to the proportion to prepare a tablet. The tablet or pill is orally taken for 0.5-1.0g each time, and is taken three times a day with warm boiled water after meals, and is taken continuously for 2-3 weeks.

The invention discloses a western medicine composition for treatment of gout. The western medicine composition is prepared from, by weight in per pill, 0.2-0.5 g of sucralfate, 0.01-0.2 g of NaHCO3, 0.01-0.1 g of MgO, 0.1-0.3 g of benzbromarone, 0.2-1.5 g of analginum, 0.1-2.0 g of ketoprofen, 0.05-0.1 g of prednisone acetate, 0.05-0.2 g of eugenol and 0.05-0.1 g of naproxen. The western medicinecomposition has reasonable medicine combination and raw material coordination, can effectively treat the gout, is quick to work and is short in treatment course, and satisfies use demands at present.

The invention discloses a formula of a tablet candy with an auxiliary uric acid reducing function. The formula comprises the following raw materials in parts by weight: 80-220 parts of sorbitol, 85-255 parts of marine fish oligopeptide powder (containing goose carnosine), 175-525 parts of acerola cherry powder, 15-45 parts of turmeric, 40-110 parts of chitosan oligosaccharide, 5-20 parts of a grape seed extract, 42-125 parts of poria cocos powder, 80-180 parts of microcrystalline cellulose and 2-7 parts of magnesium stearate. Most of existing medicines (such as allopurinol, benzbromarone and febuxostat) for reducing uric acid have side effects and can cause harm to human bodies after being used for a long time. The tablet candy adopts natural and healthy animal and plant components, and the marine fish oligopeptide powder containing goose carnosine, turmeric, chitosan oligosaccharide, the grape seed extract and poria cocos powder are combined for use to achieve the effect of reducing uric acid, so that the safety is high; and through a reasonable formula proportion, the product achieves a good taste, and meanwhile, on the premise of ensuring the effects, consumers can enjoy the tablet candy better and the compliance is high.

The invention belongs to the technical field of new medical application, and particularly relates to an application of benzbromarone as an FXR agonist. A homogeneous time-resolved fluorescence experiment, a transcriptional activation experiment and a quantitative PCR experiment prove that the benzbromarone can effectively excite a FXR receptor, and can be applied to medicines for treating FXR receptor mediated bile blockage, gall-stone, diabetes, non-alcoholic fatty liver disease, atherosclerosis and inflammation.

The invention belongs to the technical field of organic synthesis, and particularly relates to a preparation method of benzbromarone. According to the method disclosed by the invention, polystyrene-loaded aluminum trichloride is used as a catalyst to carry out Friedel-Crafts acylation reaction, so that the catalytic effect is good, and the catalyst can be recycled, in the demethylation reaction process, aluminum trichloride is adopted to replace common pyridine hydrochloride, so that the reaction temperature can be reduced, and the yield can be increased, in the bromination reaction, sodium sulfide and hydrogen peroxide are adopted to replace bromine, so that the technical problems of strong corrosivity of bromine, great harm to human bodies and environmental pollution are solved, and meanwhile, the yield can be further improved.

The invention belongs to the field of medicines, and discloses a lansoprazole tablet composition, which contains the active components i.e., lansoprazole and benzbromarone with the weight ratio being1:(3 to 5). The invention discloses combined application of the lansoprazole and the benzbromarone on remarkably reducing an experimental hyperuricemia mice blood uric acid level, and the lansoprazoletablet composition has an effect on treating gout.