Freeze dry powdered injection of moxlfloxacin or its salts and preparation process thereof

Abstract

The invention provides a moxfloxacin for injection or freeze dried powder injection of its salts, and its preparation process, which is prepared from moxifloxacin or its salts, excipient, pH modifier and water for injection through freeze drying.

Description

technical field [0001] The invention relates to a freeze-dried powder injection of moxifloxacin or its salt for injection with broad-spectrum antibacterial effect and a preparation method thereof, which solves the problem of instability and easy occurrence of moxifloxacin solution due to the need to add an isotonic regulator. Subvisible particles, and easy to form amorphous particles during storage and other technical problems. Background technique [0002] Moxifloxacin (moxifloxacin) is a fourth-generation novel extended-spectrum quinolone antibacterial drug, and its structure is as follows: [0003] [0004] 1-cyclopropyl-7-([S,S]-2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-8-methanol Oxy-4-oxo-3-quinolonecarboxylic acid [0005] In addition to maintaining strong anti-gram-negative bacteria activity, this new type of quinolone drug also has strong antibacterial activity against gram-positive bacteria and other atypical pathogenic bacteria. For Moraxella c...

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Problems solved by technology

Application No. 00811427.7 patent discloses moxifloxacin / sodium chloride preparation, using sodium chloride as an isotonic regulator, although subvisible particles are reduced, subvisible particles are still prone to appear in varying degrees, especially in storage Temperature is higher, under the condition that there is certain iron content in the solution (drug is easily brought into a certain amount of iron because of contact with container, production line etc. in the production process), as in embodiment 1, under the solution iron content 540ppb, store at 40 ℃ After 4 weeks, the number of particles with a particle size greater than 25 μm was 0.13 / ml, and after storage for 8 weeks, the number of particles with a particle size greater than 25 μm was 0.17 / ml; in Example 2, the solution was stored at 25°C for 95 weeks Afterwards, the number of particles with a particle size greater than 25 μm was 0.16 grains / ml, which must strictly control the storage conditions of moxifloxacin sodium chloride preparations such as low temperature, and also limit the validity period to some extent

In addition, in the presence of sodium chloride, the solubility of moxifloxacin hydrochloride is too poor, and it is necessary to use a narrow concentration of active compounds and isotonic regulators to obtain a certain concentration of moxifloxacin solution, which brings great challenges to industrial preparation and production. inconvenient

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