34 results about "Cefbuperazone" patented technology

The invention discloses a synthetic method of cefoperazone acid. The method comprises the steps of: reacting raw materials of 7-ACA and 1-methyl-5-mercapto tetrazole under the catalysis of boron trifluoride acetonitrile to obtain 7-ACT; dissolving the 7-ACT in a mixed solution of acetonitrile and N,O-(bis) trimethylsilyl acetamide to obtain a 7-ACT amino alkylate solution; mixing HO-EPCP, an organic solvent and a catalyst, adding phosphorus oxychloride for reaction at the temperature of -25 to -20 DEG C, wherein when the residue amount of HO-EPCP in the reaction solution is no more than 0.5%, the reaction is complete, so as to prepare a HO-EPCP acyl chloride solution; mixing and reacting 7-ACT amino alkylate solution with HO-EPCP acyl chloride solution, adding an aqueous solution of sodium bicarbonate after the reaction, standing foe stratification, filtering a lower layer material, adding water, crystallizing, filtering, washing and drying to obtain the cefoperazone acid. The method has the advantages of simpleness, high yield and stable intermediate.

The invention belongs to the technical field of medicine, and specifically relates to a composition of cefoperazone sulbactam sodium and lysine, and also provides a preparation method of the composition injection, and is used for the treatment of cefoperazone drug-resistant patients. Use in medicine for infectious diseases caused by β-lactamase-producing bacteria sensitive to this product.

The invention discloses a composite pharmaceutical composition of cefoperazone sodium and tazobactam sodium. The composite pharmaceutical composition is an injection, and is prepared from the following components in parts by weight: 3.5-4.5 parts of cefoperazone sodium, 1 part of tazobactam sodium, 0.5-1 part of ambroxol hydrochloride, 0-6 parts of excipient, 0-10 parts of isotonic agent, 0-1 part of antioxidant, a proper amount of citric acid-sodium citrate and 20 parts of injection water. The composite preparation of the cefoperazone sodium and the tazobactam sodium disclosed by the invention is stable in quality and significant in curative effect, not only can three active ingredients be evenly mixed, but also the composite pharmaceutical composition is excellent in stability, good in solubleness and good in clinical use safety.

The invention relates to a synthesis method of cefbuperazone, and the synthesis method comprises the following steps: (1) protecting 7beta-amino-7alpha-methoxy-3-[(1-methyl-1H-tetrazol-5-yl)S-methyl]-3-cephalosporin-en-4-carboxylic acid diphenyl methyl ester (7-MAC) with an amino group protective agent to obtain 7-MAC silane; (2) reacting cefbuperazone lateral chain with a halide to obtain cefbuperazone lateral chain acyl halide; (3) reacting 7-MAC silane with cefbuperazone lateral chain acyl halide to obtain an intermediate product, namely cefbuperazone diphenyl methyl ester; and (4) removing the protective group from cefbuperazone diphenyl methyl ester to obtain cefbuperazone, wherein the amino group protective group is hexamethyl disilylamine, trimethyl chlorosilane, N,O-bis(trimethylsilyl) acetamide or N,N-bis(trimethylsilyl)-2,2,2-trifluoroacetamide. The synthesis method is easy for realization and has the advantages of simple and reasonable synthesis route design, mild reaction conditions, simple, safe and controllable reaction process and high yield of cefbuperazone, and the intermediate product is easy to separate and purify.

The invention provides a preparation method for cefbuperazone. The preparation method comprises the steps of performing an acylchloriration reaction on D-alpha-(4-ethyl-2 ,3-dioxo-piperazine-carboxamido)-beta-(S) hydroxybutyric acid and oxalyl chloride in the presence of copper toluenesulfonate at a temperature of 5 DEG C; then distilling a reaction product under a reduced pressure after the acylchloriration reaction; adding methylene dichloride; and distilling again under the reduced pressure. The preparation method for the cefbuperazone can increase a conversion rate of intermediate products and improve purity of a final product of the cefbuperazone.

A cefbuperazone pharmaceutical composition has the advantages of high uniformity, strong delamination resistance, fast dissolution speed, good fluidity, etc., and the product obtained by subpackaging meets the requirements of the Pharmacopoeia on the difference in powder injection bottle weight, solution clarity, and the like.

The invention relates to a medicinal composition of cefoperazone sodium and tazobactam sodium. The medicinal composition comprises the following components in part by weight: 4 to 8 parts of cefoperazone sodium and 1 part of tazobactam sodium, wherein the tazobactam sodium is measured by a powder X-ray diffraction measuring method, and characteristic diffraction peaks are shown at the positions of 6.9 degrees, 10.5 degrees, 11.4 degrees, 16.6 degrees, 19.2 degrees, 22.7 degrees, 27.0 degrees, 29.7 degrees and 33.5 degrees in an X-ray powder diffraction map expressed by a diffraction angle of between 2 theta+ / -0.2 degree. The medicinal composition has the advantages of high stability, low relevant substance content, controllable quality and the like, and the administration safety of patients is improved. The invention also relates to a method for preparing the tazobactam sodium with the technical characteristics of the characteristic diffraction peaks.

The invention provides a cefoperazone sodium and sulbactam sodium composition, which comprises the following raw materials in parts by weight: 9-10 parts of cefoperazone sodium, 1 part of sulbactam sodium and 0.05-0.07 part of glutathione. The glutathione is added to the composition, so that the composition has relatively good antibacterial effect. Furthermore, a little of sulbactam sodium is utilized, so that accumulation of the sulbactam sodium in a body is reduced; and the production cost is reduced. In addition, by a novel sulbactam sodium crystal, the composition provided by the invention has relatively good stability.

The invention discloses a method for preparing 4-ethyl-2,3-dioxypiperazine-1-formate. In the method, 1-ethyl-2,3-dioxypiperazine and chloro-formate are used as raw materials and reacted in an organic solvent system in the presence of an acid binding agent to form 4-ethyl-2,3-dioxypiperazine-1-formate, wherein the molar ratio of the 1-ethyl-2,3-dioxypiperazine to the acid binding agent to the chloro-formate is 1:1.0-3.0:1.0-2.0; the chloro-formate is methyl chloroformate or ethyl chloroformate; and the 4-ethyl-2,3-dioxypiperazine-1-formate is 4-ethyl-2,3-dioxypiperazine-1-methyl formate or 4-ethyl-2,3-dioxypiperazine-1-ethyl formate. The method greatly reduces cost, simplifies process, reduces byproducts, improves product purity and reduces solvent separation processes; and the prepared product can be used as an intermediate for piperacillin and cefoperazone and is suitable for industrial production.