7 results about "Avibactam sodium" patented technology

The application relates to a compound cefoperazone and avibactam powder injection and a preparation method thereof. The compound powder injection is obtained by uniformly mixing cefoperazone hydrochloride and avibactam sodium, tabletting and crushing. When the powder injection is prepared into an injection solution, the powder injection is easy to disperse and dissolve, is convenient to use, ensures the content of cefoperazone, is not prone to produce beta-lactamase bacterial drug resistance, and has a good market application prospect.

The application belongs to the technical field of pharmaceutical preparations, and particularly relates to a pharmaceutical composition of avibactam sodium and a preparation method thereof. The pharmaceutical composition comprises the following components: avibactam sodium, 2-(5-(2-oxoazetidin-1-yl)thiophene-2-yl)benzo[d]thiazole-6-carboxylic acid; the mass ratio of the avibactam sodium and the 2-(5-(2-oxoazetidin-1-yl)thiophene-2-yl)benzo[d]thiazole-6-carboxylic acid is 1:(2-3). The pharmaceutical composition has a significant synergistic antibacterial effect.

The invention belongs to the technical field of chemical synthesis of medicines, and particularly relates to a preparation method of avibactam sodium. According to the method, (2S, 5R)-trans-5-hydroxypiperidine-2-formic acid is taken as a starting raw material, hydroxyl in the (2S, 5R)-trans-5-hydroxypiperidine-2-formic acid is efficiently and selectively converted into hydroximido by adopting an electrochemical method, the condition is mild, the method is environment-friendly, and the pollution problem caused by using an equivalent metal reducing agent or an oxidizing agent in a traditional chemical method is avoided; after O-benzyl oxime ether is constructed, a (2S, 5R) absolute configuration required by avibactam sodium is constructed and maintained through stereoselective reduction and efficient amination. From (2S, 5R)-trans-5-hydroxypiperidine-2-formic acid to avibactam sodium, the route design is ingenious, the steps are shorter, and a novel, simple and efficient synthesis route is provided for synthesis of avibactam sodium.

The invention discloses a chemical synthesis method of avibactam sodium, which comprises the following steps: with (2S)-5-[(benzyloxy) imino] piperidine-2-carboxylic acid ethyl ester as a starting material, carrying out selective reduction under the action of a hand-shaped inducer and a reducing agent to construct 5-site chiral carbon, and carrying out oxalic acid resolution to obtain high-purity oxalate, and then carrying out five-step reaction, namely intramolecular ureization, acylase catalytic hydrolysis amidation, debenzylsulfonic acid esterification salification and sodium ion exchange, so as to obtain the avibactam sodium. According to the method, the chiral inducer is adopted to induce selective reduction, and the acylase catalytic ammonolysis process is optimized, so that the content of isomer impurities in the product is remarkably reduced, and the purity and the overall yield of the product are improved. Wherein the acylase catalytic ammonolysis reaction conditions are mild, and the process safety risk is greatly reduced while the energy consumption is reduced.

This invention discloses an intermediate product of ceftazidime and avibactam sodium for injection and its preparation method, relating to the field of pharmaceutical manufacturing technology. It solves the problems of high energy consumption and poor uniformity, stability, and controllability of sterile powder mixing during large-scale production. The preparation method of the intermediate product includes adding ceftazidime and avibactam sodium to a mixer at a certain weight ratio, controlling the mixing speed of the mixer at 13-17 rpm and the mixing time at 20-60 min. By precisely controlling the combination of key process parameters—mixing speed and time—this invention effectively overcomes the problem of uneven mixing caused by the difference in physical properties of the two powders, ensuring that the RSD of the mixing uniformity is stably controlled within a high standard range of ≤5.0%.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a pharmaceutical composition of avibactam sodium and a preparation method of the pharmaceutical composition. The medicine composition is prepared from the following components: avibactam sodium and 2-(5-(2-oxo azetidine-1-yl) thiophene-2-yl) benzo [d] thiazole-6-carboxylic acid, and the medicine composition is prepared from the following components: the avibactam sodium and the 2-(5-(2-oxo azetidine-1-yl) The mass ratio of the avibactam sodium to the 2-(5-(2-oxo azetidine-1-yl) thiophene-2-yl) benzo [d] thiazole-6-carboxylic acid is 1 to (2 to 3). The pharmaceutical composition has a remarkable synergistic antibacterial effect.

The invention discloses an aztreonam and avibactam sodium freeze-dried preparation for injection and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. Comprising the following steps: pre-cooling a freeze dryer plate layer to 5 DEG C; the method comprises the following steps: filling a freeze-drying solution containing aztreonam and avibactam sodium into a penicillin bottle, and putting the penicillin bottle filled with the freeze-drying solution into a box; the temperature is reduced to-35 DEG C to-50 DEG C within 2-6 hours, and the temperature is kept for 2-6 hours for freezing; the vacuum degree is reduced to 0.0-0.5 mbar, the temperature is increased to-25 DEG C to-5 DEG C within 2-8 hours, and heat preservation is conducted for 50-80 hours; raising the temperature to 20-30 DEG C in 2-8 hours, vacuumizing for 0.0-0.4 mbar, and keeping for 2-6 hours, raising the temperature to 40-50 DEG C in 0.5-2 hours, vacuumizing for 0.0-0.4 mbar, and keeping for 4-8 hours, and raising the temperature to 40-50 DEG C in 0.5-2 hours, vacuumizing for 0.0-0.4 mbar, and keeping for 4-8 hours; the concentration of aztreonam in the freeze-drying solution is 1.5 g / mL, the concentration of avibactam sodium is 0.5 g / mL, and the concentration of L-arginine in the solution is 0.09-0.135 g / mL. Through a conventional freeze-drying process, the prepared freeze-dried product has few appearance defects, the water content is lower than 1%, and the freeze-dried product has good re-dissolvability, does not have dendritic crystals during re-dissolution and has good stability and safety.