Fleroxacin injection and its preparing method

Abstract

The present invention relates to medicine preparation, and especially fleroxacin injection and its preparation process. The fleroxacin injection is prepared with fleroxacin and aspartic acid in the weight ratio of 1 to 0.44 and water for injection, and through dissolving fleroxacin and aspartic acid in water for injection through heating to 80 deg.c and stirring, adding active carbon at 80 deg.c through stirring for 15 min, cooling, eliminating active carbon, filtering, filling, sterilizing at 105 deg.c for 30 min, inspection and packing. The fleroxacin injection has the features of raised stability, high solubility, and high permeability.

Description

Technical field [0001] The invention relates to a pharmaceutical preparation of a compound, namely fleroxacin injection and a preparation method thereof. Background technique [0002] In the prior art, fleroxacin is a quinolone antibacterial drug, its chemical name is: 6,8-difluoro-1-(2-fluoroethyl)-1,4-dihydro-7-(4-methyl) -1-piperazine)-4-oxo-3-quinoline carboxylic acid, molecular formula: C 17 H 18 N 3 O 3 F 3 . For Gram-negative bacteria, including Escherichia coli, Pneumoniae, Proteus, Salmonella typhi, Salmonella paratyphi, Shigella, Enterobacter cloacae, Enterobacter aerogenes, Citrobacter spp, and mucilage Serratia, Pseudomonas aeruginosa, Neisseria meningitidis, Haemophilus influenzae, Moracastatella, Legionella pneumophila, Neisseria gonorrhoeae, etc. have strong antibacterial effects. It also has a moderate antibacterial effect on gram-positive cocci such as Staphylococcus and Streptococcus hemolyticus. It is mainly used to inhibit bacteria's DNA gyrase for sterilizati...

AI Technical Summary

Problems solved by technology

[0004] In terms of patent applications, the Chinese Invention Patent Application Discloses a Concentrated Aqueous Solution of Gyrase Inhibitors, Patent No. ZL96116516.2, filed on September 23, 1996, which is mainly inhibited by the active compound gyrase The active compound gyrase inhibitor is 6,8-difluoro-1-(2-fluoroethyl)-1,4-dihydro -7-(4-methyl-1-piperazine)-4-oxo-3-quinolinecarboxylic acid, described acid is lactic acid or acetic acid, and its shortcoming is that this technique adopts lactic acid to make cosolvent to reach increasing fleroxacin The purpose of solubility. However, the pH value of the dissolved solution in the production process is low, and it needs to be further adjusted to the standard range with alkaline substances; insoluble substances are precipitated at low temperatures, and the content is unstable; there are many operating steps and the production process is long. (Need to keep warm for 1-4h, stand still for 10-48h), not suitable for injection production requirements

Images