74 results about "Probenecid" patented technology

An improved stable pharmaceutical composition for controlled release of an active ingredient comprises a betalactam antibiotic such as cephalexin, cefaclor or their pharmaceutically acceptable hydrates, salts or esters as active ingredient, a calcium salt and a mixture of hydrophilic polymers selected from the group consisting of at least one sodium alginate and one xanthan gum and with or without hydroxypropyl methylcellulose, said composition optionally containing probenecid. The composition may also contain one or more of a water soluble and / or water dispersible diluent, wherein the quantities of the hydrophilic polymers and water soluble and / or water dispersible diluents are such that the therapeutically effective active ingredient is released at a rate suitable for once or twice daily administration of the pharmaceutical composition.

Described herein are inventions is directed to methods of treating a cardiac dysfunction and symptoms of cardiac dysfunction in a subject that includes administering an amount of probenecid effective to treat a symptom of cardiac dysfunction. The probenecid may be administered in at least one of an injection, orally, or transdermally. The amount of probenecid is sufficient to result in an improved performance on a standardized 6 minute walk test, an improved New York Heart Association (NYHA) classification, a lower diuretic dose requirement, a lower serum BNP levels, a normalization of serum sodium concentrations, and combinations thereof In an embodiment, probenecid is administered over a period of about 8 hours to about 24 hours. Probenecid may be used for short term treatments, i.e., less than a week, or it may be administered in a long term manner, i.e., over a period of weeks, months, or even years. Probenecid may be administered in an amount sufficient to treat the symptoms of cardiac dysfunction.

The invention relates to a medicinal composition for treating hyperuricemia, which comprises Febuxostat or derivate thereof, probenecid and a pharmaceutically acceptable medicinal carrier, wherein theratio in weight portion of the Febuxostat or derivate thereof to the probenecid to the pharmaceutically acceptable medicinal carrier is 1:10-200:0.5-100. 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 trionein 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.

A fast disintegrating controlled release oral composition comprising a core material containing cefuroxime axetil present as controlled release form, the cefuroxime axetil being provided with an outer coating of a copolymer selected from aqueous dispersions of enteric methacrylic acid and methacrylic acid esters anionic copolymers having carboxyl group as the functional group or mixtures thereof and an inner coating of a sustained-release copolymer selected from aqueous dispersions of acrylate and methacrylate pH independent copolymers having quaternary ammonium group as a functional group or mixtures thereof, and optionally probenecid. Additionally, the coating composition may contain plasticizers. The composition is suitable for once daily administration.

The present invention relates to a compound injection preparation formed from probenecid sodium and benzylpenicillin antibiotics, belonging to the field of chemical pharmaceutical technology. The benzylpenicillin antibiotics include amoxicillin sodium and piperacillin sodium. The amoxicillin sodium and piperacillin sodium are mixed according to ratio of 1:3 and 1:5 through a conventional preparation process.

The present disclosure relates to a pharmaceutical composition, a health functional food composition, and a method for preventing or treating a brain disease or diabetes. The pharmaceutical composition, health functional food composition, and method includes at least one active ingredient that is chlorhexidine, thioguanosine, mebendazole, fenbendazole, colchicine, farnesol, trimethobenzamide hydrochloride, disulfuram, azathioprine, mebeverine hydrochloride, zaprinast, tosufloxacin hydrochloride, efavirenz, thiostrepton, probenecid, entacapone, harmine hydrochloride, flunisolide, thimerosal, hexestrol, sulfaquinoxaline sodium salt, monensin sodium salt, raloxifene hydrochloride, 2-chloropyrazine, or topotecan.

Disclosed is a method for preparing compound beta lactam sodium salt / sodium benemid for injection, which comprises dissolving 1-10 weight parts of probecid into 1-100 parts of water, charging sodium ion-containing alkaline solution, adjusting pH to 6-11 for reaction into salts, filtering and degerming through microporous filtering film, asepsis drying, or filtering with microporous filtering film and charging 10-100 parts of absolute ethyl alcohol or waterless acetone for evolution of solid body, carrying out asepsis dehydration obtain the end product, mixing sodium salt of beta-lactams with the obtained sodium benemid by the proportion of 10:1-1:10 and dissolving into 1-100 parts of water.

The invention discloses application of high mangiferin and aglycon thereof in preparation of a medicament for preventing and treating hyperuricemia and in particular relates to application of high mangiferin and aglycon thereof in preparation of a medicament for preventing and treating hyperuricemia as well as gout and lithangiuria brought by the hyperuricemia, and a medicine application way. The high mangiferin and aglycon thereof provided by the invention can be used for obviously reducing the concentration of serum uric acid in an animal for experiment and have the serum uric acid inhibition effect similar to that of a xanthine oxidase inhibition medicament allopurinol; and simultaneously, the high mangiferin and aglycon thereof provided by the invention can be used for obviously improving the concentration of uric acid in urine and have the uric acid excretion promoting function similar to that of a uric acid excretion promoting medicament probenecid. The high mangiferin and aglycon thereof provided by the invention are efficient, low in toxicity and high in safety, thus the high mangiferin and aglycon thereof are wide in application prospect.

The invention discloses a probenecid sustained-release tablet and a preparation method. The probenecid sustained-release tablet is composed of, by weight, 40-50 parts of probenecid, 30-35 parts of sodium bicarbonate, 20-25 parts of core pellet, 3-5 parts of sustained-release material, 0.3-0.6 part of plasticizer, 0.1-0.3 part of porogen, 10-15 parts of filler, 0.5-1.0 of lubricating agent, 15-20 parts of disintegrant and 2-5 parts of coating material. The preparation method includes the steps of material preparation, preparation of pellet containing core, preparation of sustained-release pellets, tabletting and coating. Sodium bicarbonate is added in the formula, so that urate can be prevented from forming urinary stone in the urinary tract by taking the probenecid sustained-release tablet with a lot of water for treating chronic gout. Sodium bicarbonate can neutralize excessive gastric acid and has stomach-invigorating and antiacid effect when improving effect of penicillins. The probenecid sustained-release tablet is taken 1-2 times a day, so that compliance of patients is increased.

The present invention is directed to methods for treating hyperuricemia and related disorders, comprising co-therapy with canagliflozin and probenecid.

The invention relates to a medicinal composition for treating gout. The composition consists of febuxostat crystals, probenecid and a pharmaceutically acceptable medicinal carrier of which the ratio of part by weight is 1:10-200:0.05-100. When the ratio of the febuxostat crystals to the probenecid is 1 to 33.3, the inhibition ratio is improved by 155.6 percent compared with the total inhibition rate of the febuxostat crystals and the probenecid which are singly used; and when the ratio of the febuxostat crystals to the probenecid is 1 to 100, the inhibition ratio is improved by 113.3 percent compared with the total inhibition ratio of the febuxostat crystals and the probenecid which are singly used. Pharmacological tests show that the composition has obvious synergetic effect, can quickly reduce the concentration of uric acid in blood serum, obviously improves gout treatment effect, greatly reduces the dosage of each single component at the same time and effectively reduces the toxic and side effects of the medicament.

A compound powder injection or freeze-dried powder injection is prepared from the sodium (or potassium) salt of probenecid and the beta-lactam kind of antibiotics including penicillin G, ampicillin, ancef, cefuroxime, cefotaxime and cefoxitin. It can elongate the half life of antibiotic, increase the AUC and plasma level and prevent the generation of drug-resistant bacteria.

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 relates to a pharmaceutical composition used for preventing and treating colibacillosis in livestock and poultry. Every 100 g of the pharmaceutical composition comprises 2 to 10 g of ceftiofur hydrochloride, 0.25 to 10 g of tazobactam sodium, 5 to 10 g of probenecid sodium, 0.1 to 0.5 g of dexamethasone sodium phosphate and 2 to 15 g of beta-cyclodextrin, with the balance being pharmaceutically acceptable accessories. The pharmaceutical composition has the advantages of reasonable composition, low cost, a remarkable curative effect on clinical pathogenic escherichia coli, especially on drug-resistant intractable escherichia coli, a simple preparation method, stable properties and convenience in large scale intensive production.

The invention relates to a Beta-lactam antibiotic compound preparation for animals, which contains probenecid. Calculated by weight percentage, the preparation is composed of 1 to 20 percent of probenecid , 5 to 20 percent of Beta-lactam antibiotic, 5 to 40 percent of cosolvent, and acceptable vector in pharmacy which is added until the preparation is 100 percent. The preparation can be orally administrated , and can be dissolved in water to be drunk by livestock and fowl. The invention has a broad antifungal spectrum, shows a strong antibacterial activity, is convenient to be used clinically, has good safety, and is applicable to treating light to moderate infection. The used practice shows that the preparation can reduce the dosage of the Beta-lactam antibiotic in clinical practice, can reduce the occurrence possibilities of drug resistance, and can also save the treatment cost with good using effect.

The invention belongs to the technical field of organic chemical synthesis and specifically discloses a water-phase synthetic method of probenecid. The water-phase synthetic method comprises the following steps: firstly, preparing diazotization reaction liquor by reacting aminobenzoic acid, hydrochloric acid and sodium nitrite; secondly, feeding liquid-state sulfur dioxide into diluted hydrochloric acid aqueous liquor to obtain a sulfonyl chlorinazation reagent; thirdly, enabling the two reaction liquor to generate sulfonyl chlorinazation reaction to obtain p-carboxyl benzene sulfonyl chloride; and finally, preparing a probenecid pure product by reacting the p-carboxyl benzene sulfonyl chloride with dipropyl amine through acidifying. The synthetic process adopts a water-phase synthetic technology, changes a reaction path, reduces production of byproducts, and avoids use of an organic solvent and a virulent agent; and product yield is ideal (91%, in terms of para aminobenzoic acid), and purity is high (98%). The novel synthetic process is developed for being beneficial to enlarged implementation of industrialization.

The present invention provides an inhalation-type pharmaceutical composition for gout and preparation method thereof, comprising a first gas and an atomized medicine. The first gas comprises hydrogen. The gas volume concentration of hydrogen in the inhalation-type pharmaceutical composition is between 2 to 96%. The atomized medicine is selected from a group comprising colchicine, allopurinol, probenecid, sulfinpyrazone, and any combination thereof. The inhalation-type pharmaceutical composition of the present invention can remove harmful radicals in the body of the patient through the use of hydrogen while also increases the absorption effect of the medicine for the patient by using an atomized medicine. At the same time, because the use of the small amount of the vaporized pharmaceutical liquid can indirectly reduce the side effects on the user.

The invention discloses a preparation method of compound nano lipidosome capable of improving the bioavailability of catechin. The method comprises the following steps: 1) adding 100mg to 150mg of catechin and 1.0g to 2.0g of tween80 into 20ml of 0.05mol / L phosphate buffer (PBS, pH7.0) so as to obtain a mixture, and stirring the mixture at the temperature of 40-60 DEG C to obtain a catechin PBS solution; 2) weighing and dissolving 100mg to 200mg of probenecid, 0.1g to 0.5g of lecithin and 100mg to 500mg of cholesterol in 10ml to 20ml of dichloromethane so as to obtain a mixture I, injecting the mixture I into the catechin PBS solution obtained in step 1) by utilizing a syringe at the temperature of 40-60 DEG C so as to obtain a mixture II, and stirring the mixture II at a constant temperature to obtain a suspension; 3) evaporating the suspension in a rotating state to remove the dichloromethane; carrying out the ultrasonic treatment on the mixture by utilizing the ultrasonic of 350W to 400W for 8min to 12min to obtain the catechin compound nano lipidosome.

The invention discloses a preparation method of a water-soluble probenecid salt. The preparation method comprises the following steps in sequence: reacting probenecid with an alkaline matter in water to obtain the probenecid salt; separating out the probenecid salt from the reaction liquid by controlling the temperature and pH (Potential of Hydrogen) of reaction liquid; and filtering and drying, so as to obtain the probenecid salt. The preparation method is completely carried out under a water phase, no other organic solvents are adopted, no 'three wastes' are brought basically, and the solvent recovery processes are reduced; the production cost and environmental pollution are greatly reduced through the preparation method, and the requirement on clean production is met; the probenecid salt is obtained in a crystallization mode instead of the mode of drying the solvent by distilling, so that other reaction product residues can be avoided, and the production quality and yield of the probenecid salt can be obviously improved.

The invention belongs to the field of the medicines for animals and discloses a painless synergistic amoxicillin powder injection for animals and a preparation method thereof. The powder injection comprises the following components in parts by weight: 48-52 parts of amoxicillin or amoxicillin sodium (active ingredient), 10-30 parts of a cosolvent, 1-3 parts of an analgetic, 5-8 parts of probenecid sodium and 1-2 parts of an antifebrile anti-inflammatory analgesic. The preparation method of the powder injection comprises the following steps of: in parts by weight, evenly mixing 1-3 parts of analgetic, 5-8 parts of probenecid sodium and 1-2 parts of antifebrile anti-inflammatory analgesic together, and then evenly mixing the mixture with 48-52 parts of amoxicillin or amoxicillin sodium (active ingredient) and 10-30 parts of cosolvent, thereby obtaining the painless synergistic amoxicillin powder injection. The amoxicillin powder injection prepared by the preparation method provided by the invention solves the problems of strong injection pricking stress, poor effects of anti-inflammation and analgesia, and heat elimination and defervescence, ingestion reduction after the administration of the drug, and the like; and the product is highly required in clinical application, and is wide in market prospect and huge in social benefit.

The invention discloses a probenecid purification method, comprising the steps of: reacting a crude probenecid product and an alkaline substance in water until the probenecid is dissolved completely; cooling an obtained solution to carry out low-temperature crystallization, and stirring till complete crystallization; filtering, dissolving the obtained filter cakes with water, and then, adding acid to regulate the obtained solution to be acidic; and filtering, washing the obtained filter cakes with water, and then filtering and drying to obtain a pure probenecid product. According to the invention, by utilization of chemical principles of crystallization and filtration, the purpose of purifying the probenecid in a water environment is achieved by alkaline dissolution and acidification operation. The probenecid purification method is simple to operate and free from utilization of organic solvents, so that the production cost and environment pollution are reduced greatly, and the requirement for clean production is met.

The invention relates to a pharmaceutical composition for preventing and treating chicken bursal disease and nephrotic bronchitis and a preparation method thereof. The pharmaceutical composition comprises the following active ingredients by weight percentage: 5-20% of hypericum perforatum extractive, 10-30% of radix isatidis extractive, 20-30% of radix astragali extractive; 2-5% of probenecid, 5-8% of taurine, 10-30% of paracetamol, and the balance of auxiliary ingredients. The invention has low cost and convenient use, and can be directly added into feed and drinking water for animals without toxic side effect or medicine residue, and is an efficient pharmaceutical composition for preventing and curing the chicken bursal disease and the nephrotic bronchitis with a higher curative rate.

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 present invention relates to a method for activation of TRPV2 (transient receptor potential vanilloid 2) using probenecid, more precisely a method for selecting a candidate for TRPV2 blocker using probenecid. Probenecid of the present invention works on TRPV2 specifically so that it facilitates the isolation of sensory neurons expressing TRPV2. Therefore, probenecid of the invention can be effectively used for the studies on TRPV2 mechanisms and the development of a TRPV2 based anodyne.

The invention relates to a synthesis and preparation method for probenecid sodium and probenecid potassium. The method is characterized by comprising the following steps: heating water bath to reach 75 to 80 DEG C to completely dissolve probenecid in absolute ethyl alcohol; then dropping a mixed solution of sodium hydroxide or potassium hydroxide or absolute ethyl alcohol which is dissolved in advance at 70 DEG C at speed of 5ml per minute; further reacting for 15 minutes after dropping; slowly cooling to reach 50 to 60 DEG C; replacing a reflux condensing pipe by a distilling condensing pipe; heating the water bath to reach 90 to 95 DEG C; condensing until the volume is 1 / 5 of original volume; pouring out the reactant while hot; standing for more than 4 hours at cold condition; leaching to obtain rough products of probenecid sodium and probenecid potassium; and further refining to obtain the products probenecid sodium and probenecid potassium. According to the synthesis and preparation method, the absolute ethyl alcohol is adopted as the solvent, so that more crystals are separated after cooling when the reaction is finished, and the yield can reach over 80% after condensing; and the technical means for purifying and recrystallizing the probenecid sodium (potassium) is easy to operate, and suitable for industrial production.

The invention discloses a chronic low-perfusion PD (Parkinson's disease) mouse model as well as a preparation method and device thereof. Probenecid and MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) are administrated jointly to a mouse with bilateral common carotid artery coarctation, and the chronic low-perfusion PD mouse model is obtained. The provided method is simple and safe to operate; the success rate is high; the cognitive disorder simulation performance of the obtained mouse model is typical.

The invention relates to enteric long-acting compound amoxicillin powder for veterinary use and a preparation method thereof. Every 100g of the enteric long-acting compound amoxicillin powder for veterinary use comprises the following components by weight: 8-10g of amoxicillin, 2-3g of potassium clavulanate, 8-10g of probenecid, 20-40g of beta-cyclodextrin, 10-20g of micropowder silica gel, 1-5% of acrylic resin and the balance of glucose. The main drug amoxicillin of the preparation is kept stable in a strong acid environment in the upper portion of the stomach and is not damaged by the strong acid; when the pH of the lower portion of the stomach is close to 6, amoxicillin is released after an enteric material is dissolved; potassium clavulanate can reduce degradation of beta-lactamase generated by sensitive bacteria, and probenecid can prolong discharge of amoxicillin in kidneys, so that the blood concentration is effectively prolonged. According to the product, the bioavailability of amoxicillin is improved greatly, the treatment course of livestock diseases is shortened, the treatment cost of farmers is lowered, and a high quality preventing drug is provided for animal husbandry.