39 results about "Cefuroximum" patented technology

The invention discloses a preparation method of cefuroxime axetil. The method comprises the following steps: completely dissolving cefuroxime acid in dimethylformamide, and carrying out esterification reaction with 1-bromethylacetate under the catalytic action of cupric chloride; and hydrolyzing with ethyl acetate and sodium chloride solution, extracting, carrying out vacuum distillation, crystallizing with cyclohexane, carrying out vacuum filtration, and drying to obtain high-purity cefuroxime axetil. The cupric chloride, which has the advantages of no toxicity, no harm and high catalytic efficiency, is preferably used as the catalyst; the cyclohexane for crystallization is easy to recover and reutilize, thereby lowering the production cost; and meanwhile, the method has the advantages of mild and controllable reaction conditions, short production cycle and lower energy consumption, and is suitable for industrial production.

The invention relates to a pharmaceutical composition of cefuroxime axetil for suspension for pharmaceutical purposes and a preparation method thereof. The pharmaceutical composition of the cefuroxime axetil for suspension disclosed by the invention comprises 100 parts by weight of cefuroxime axetil (calculating according to the weight of cefuroxime), 50-250 parts by weight of cane sugar and 400-650 parts by weight of stearic acid. The invention further provides the method for preparing the composition. According to the pharmaceutical composition for suspension disclosed by the invention, the bitter taste of the cefuroxime axetil is effectively covered up; and the pharmaceutical composition is applied to adults, more importantly, the problem for difficultly taking medicines of children, old people and patients suffering from dysphagia is solved, and the compliance of medicine taking patients is greatly increased.

The invention relates to a novel crystal form of cefuroxime acid and a preparation method thereof. In X ray powder diffraction, the novel crystal form of cefuroxime acid has characteristic peaks at diffraction angles 2 theta of 8.06, 9.96, 10.44, 11.84, 12.82, 16.34, 19.02, 20.02, 21.86, 23.22, 25.46, 25.98, 33.12, 34.24 and 36.40 degrees. The preparation method comprises the following steps of adding cefuroxime raw materials into an acetonitrile mixed solvent to obtain a solution having a concentration of 0.1 to 0.2g / ml, stirring at a temperature of 25 to 35 DEG C for complete dissolution, continuously stirring for 30 to 60 minutes, carrying out filtration and decoloration, transferring filtrate to a crystallizer, adding a hydrochloric acid solution into the crystallizer to adjust a pH value of the mixed solution to 3-4, cooling to a temperature of 10 to 15 DEG C, adding cefuroxime acid seed crystals into the crystallizer, carrying out crystallization for 1 to 2 hours, adding water as a solventing-out agent into the crystallizer, sequentially cooling to a temperature of 0 to 5 DEG C, carrying out crystallization for 1 to 3 hours, filtering, washing filter cake by a washing solvent, and drying to obtain products. The novel crystal form of cefuroxime acid has HPLC content above 99.3%, avoids crystal accumulation, has large particle sizes, wherein a main particle size is more than 100 microns, and also has uniform particle size distribution and a single-cycle mole yield above 88% in crystallization.

The invention relates to a preparation method of cefuroxime axetil. The preparation method comprises the following steps: (1) reacting de-ammoniated formyl cephalosporanic acid with diphenyl diazomethane to generate acetyl-diphenyl methyl cephalosporanate; (2) reacting diphenyl methyl de-ammoniated formyl cephalosporanate with trichloroacetic isocyanate to generate diphenyl methyl cefuroxime ester; (3) hydrolyzing diphenyl methyl cefuroxime ester to obtain cefuroxime acid; (4) reacting cefuroxime acid with 1-acetoxyl-bromoethane to generate cefuroxime axetil. During the preparation process, the carboxyl group is protected by diphenyl diazomethane, the generation of impurities is reduced, and the product quality is improved.

The invention provides a cefuroxime sodium crystal compound and a composition powder injection thereof, and relates to the fields of medicament and preparation method technology of medicament, and cefuroxime sodium crystal compound composition belongs to a new crystal type-amorphous. The crystal form of cefuroxime sodium is amorphous and the preparation method thereof is as follows: reacting cefuroxime acid with sodium bicarbonate to obtain a solution and adding active carbon to discolor it, and then quick-freezing for 2 hours at -40-50 DEG C after sterile filtration using a filter membrane with aperture of 0.45 mu m and 0.22 mu m, followed by vacuum drying (drying temperature below 15 DEG C, vacuum degree 10-20 Pa, time 30-35 hours). The components of the cefuroxime sodium composition powder injection are: 95-100 parts of cefuroxime sodium crystal compound and 5-10 parts of mannitol. The component is packaged into bottles of 0.25 g, 0.75 g, 1.5 g, 2.25 g or 2.5 g as power injection preparation for clinic injection. The cefuroxime sodium crystal compound has the advantages of a simple preparation method, good stability, high solubility and dissolving quickly in water, and is convenient for clinical use.

The invention discloses a cefuroxime axetil pharmaceutical composition which is a capsule. Every 1000 capsules are prepared by the following components in percentage by weight: 80 g to 180 g of cefuroxime axetil, 10 g to 80 g of superfine silica powder, 20 g to 120 g of carboxymethyl starch sodium and 0.5 g to 9 g of lauryl sodium sulfate; in addition, the invention further discloses a preparation method of the cefuroxime axetil pharmaceutical composition. The cefuroxime axetil pharmaceutical composition has the characteristics of good stability, high dissolution rate, simple formula and high relative bioavailability, and is better suitable for industrial production.

The invention discloses a preparation method of high-purity cefuroxime acid which is an intermediate for synthesizing second-generation cephalosporins cefuroxime sodium and cefuroxime axetil. The preparation method comprises the following steps: based on 7-aminocephalosporanic acid (7-ACA) as a raw material, carrying out an N-acylation reaction on the 7-ACA and furoyl acetylchoride at the 7-position; at a low temperature, hydrolyzing 3-acetyl with a sodium hydroxide solution, crystallizing, filtering and drying so as to obtain the intermediate 3-deformamido cefuroxime acid (DCC); quantitatively adding the DCC in a tetrahydrofuran solvent, dropwise adding chlorosulfonyl isocyanate for a nucleophilic addition reaction so as to generate chlorosulfonyl cefuroxime acid, and adding purified water for hydrolysis so as to prepare a cefuroxime acid reaction liquid; adding sodium bicarbonate for salifying; removing by-reactant lactone and other unsaponifiable impurities in the reaction liquid with a ternary compound extracting agent of dichloromethane, ethyl acetate and tetrahydrofuran, layering, and adding hydrochloric acid in a water phase for acidification; adding the ternary compound extracting agent to extract and separate out the cefuroxime acid; and removing water-soluble impurities, crystallizing and filtering a distilled organic phase, and then drying so as to obtain the high-purity cefuroxime acid with the purity of more than or equal to 99%.

The invention provides a method for synthesizing 3-decarbamoyl-acetyl-cefuroxin acid compound, comprising: using 2-(2-furyl)-2-oxo-acetaldehyde, 7-aminocephalosporanic acid , and methoxyamine as a raw material; under the joint action of the first catalyst, the oxidizing agent and the second catalyst, the raw material is reacted in a reaction solvent; Cefuroxime Acid Compound. Using the method of the invention, the process steps are simple, the by-product is mainly water, there will not be a large amount of remaining waste, and the cost of subsequent treatment and environmental protection pressure are low.

The invention relates to a cefuroxime sodium raw material, an injection and a preparation method thereof, belonging to the technical field of medicine. The cefuroxime sodium raw material of the present invention is passed in a specific solvent environment, with a special dropping rate, dropwise adding cefuroxime acid solution and a 95% ethanol solution of sodium acetate trihydrate prepared according to a specific mixed solvent ratio and a specific concentration at the same time Prepared. The product quality and stability of cefuroxime sodium for injection prepared from this raw material through special process control has been significantly improved, especially the production of related substance 2 has been reduced, and the product quality has been strictly controlled, thereby ensuring the safety and effectiveness of the drug.

The invention relates to an environmentally-friendly preparation method of an intermediate of cefuroxime acid. The method comprises the following steps: preparing an SMIA acyl chloride solution by utilizing triphosgene, preparing a D-7-ACA solution, and performing a condensation reaction on the SMIA acyl chloride solution and D-7-ACA solution to obtain DCC. The environmentally-friendly preparationmethod of the intermediate of the cefuroxime acid provided by the invention greatly reduces the amount of a chloride salt and a phosphate salt, and does not use high-boiling-point class-2 solvent dimethylacetamide (DMAC) difficult to recover and soluble in water, thereby greatly reducing environmental pressure, greatly reducing production costs, and steadily improving the product quality; the reaction for preparing the acyl chloride from the triphosgene is thorough, and the prepared acyl chloride has high purity, so that the prepared intermediate DCC also has higher purity; and the high-boiling-point class-2 solvent DMAC is not used; therefore the produced cefuroxime acid has a lower residual solvent, a residual solvent of bulk drug cefuroxime sodium and cefuroxime axetil produced by theintermediate of the cefuroxime acid is greatly reduced, the quality of the final product is better improved, and the yield is increased.

The invention relates to a cefuroxime lysine compound. The cefuroxime lysine contains 98-99.99% by weight of cefuroxime lysine and 0.01-2% of trans-cefuroxime acid, and the molecular formula of the trans-cefuroxime acid is as shown in formula I. The obtained cefuroxime lysine disclosed by the invention has very strong stability which is higher than that of the prior art; and the impurity content and the polymer content are lower than those of the cefuroxime lysine in the prior art, thus the cefuroxime lysine is very suitable for clinical applications.

The invention discloses a method for determining high-molecular polymers in cefuroxime axetil tablets, which comprises the following steps: the chromatographic conditions include a high-efficiency gel chromatographic column, the detector is UV, and the mobile phase is 0.03 mol / L lithium halide at 25- 35% N,N-dimethylformamide solution containing monoalcohols with 3 to 8 carbon atoms. The method of the present invention has better solution stability, can effectively prevent the degradation of the cefuroxime axetil component to be tested, and ensure the stability of the sample, so that the high molecular polymer in the cefuroxime axetil tablet can be more accurately controlled, and the product can be guaranteed. Quality, prevention of allergic reactions caused by polymers, and better protection of drug safety for patients.

The invention discloses a cefuroxime axetil composition which comprises the following components in parts by weight: 1 part of cefuroxime axetil, 1-15 parts of a low-melting-point wax material, 5-8 parts of filler, 0-0.6 part of a disintegrating agent, 0-0.15 part of a binder and 0-0.08 part of a corrigent. The invention further discloses a preparation method of the cefuroxime axetil composition. The cefuroxime axetil composition obtained can better cover bitter taste of the medicine and is good in dissolution rate, so that the medication compliance of patients is further improved.

The invention discloses a cefuroxime magnesium compound, composition, preparation method and application. The preparation method comprises: providing a cefuroxime-containing compound, providing a magnesium compound; making the cefuroxime-containing compound and the magnesium The compound is chemically reacted; the product of the chemically reacted cefuroxime magnesium compound is obtained. In this way, the present invention can provide technical support for realizing large-scale industrial production, and can improve the stability of cefuroxime salt.

The invention relates to the technical field of pharmaceutical synthesis, in particular to a method for recovering cefuroxime acid from cefuroxime acid waste residue liquid. Dissolving cefuroxime acid waste residue liquid in a solvent, filtering, adding a polymer-loaded catalyst to the filtrate, reacting, and distilling under reduced pressure to obtain cefuroxime acid. The present invention directly converts trans isomer by-products into cis products, which not only solves the environmental protection problems caused by waste residues, but also improves the product yield. The cis products in the reaction process are not destroyed, and can be completely recovered by the reaction system. The reaction process is simple, no other reaction raw materials are consumed in the middle, the process is simple, and the production cost is low.