Moxifloxacin aqueous solution type injection

Abstract

The invention discloses a moxifloxacin aqueous solution type injection which contains moxifloxacin or pharmaceutically acceptable salt, weak acid sodium salt or phosphoric acid sodium salt and water for injection, wherein the content of the moxifloxacin is 0.8-4 percent (g / ml), and the molar concentration of the weak acid sodium salt or the phosphoric acid sodium salt is 0.0002-1mol / L. The moxifloxacin aqueous solution type injection product has strong dissolubility, human body acceptable pH value, easier control of product quality, stability in a storage period, good compatibility with clinical common isotonic solution, low production cost, small volume and convenient transportation and storage.

Description

technical field [0001] The invention relates to moxifloxacin aqueous solution type injection and belongs to the field of pharmaceutical preparations. Background technique [0002] Moxifloxacin (Moxifloxacin, MOX) (see the structure figure 1 ) is an 8-methoxyfluoroquinolone antibacterial drug with broad-spectrum activity and bactericidal effect commonly used clinically, mainly used for Gram-positive bacteria, Gram-negative bacteria, anaerobic bacteria, acid-fast bacteria and atypical microorganisms ( Such as Mycoplasma, Chlamydia and Legionella) infection. Due to the widespread clinical application of quinolone antibiotics in recent years, the problem of bacterial resistance to quinolones has become increasingly serious. The 8-methoxy part of moxifloxacin has high activity and low selectivity for Gram-positive bacteria and drug-resistant mutations, and the bulky 7-position diazo heterocyclic substituent can prevent the activity efflux, which is the fluoroquinolone resistanc...

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Problems solved by technology

[0004] The moxifloxacin sodium chloride solution described in Chinese patent ZL00811427.7 has the problem of poor solubility of moxifloxacin hydrochloride

However, we found in the stability test that the moxifloxacin solution added with aspartic acid or glycine was placed at 60°C for 10 days, and the color of the solution turned brown

[0007] On the other hand, world patent WO2007037330, Chinese patent application 200410053321.4, Chinese patent application 200510093595.0, and Chinese patent application 200510092828.5 disclose freeze-dried preparations containing moxifloxacin or quinolones, but those skilled in the art can easily understand that freeze-dried preparations cannot Autoclave sterilization, compared with the injection solution, has a lower level of sterility assurance, higher production costs, and needs to be reconstituted with a solvent before use, which is inconvenient to use

[0008] Therefore, the prior art has the problems of poor water solubility of moxifloxacin, poor operability of production control, high production cost or unstable product quality when additives are used

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