A kind of fluoroquinolone pharmaceutical composition

Abstract

The invention provides a fluoroquinolone pharmaceutical composition, each 100ml pharmaceutical composition contains: fluoroquinolone 10g-30g, cosolvent 0.1g-20g, water 0g-60g, and the balance is an organic solvent, wherein the cosolvent is A pharmaceutically acceptable acidic cosolvent. The fluoroquinolone drug content in the fluoroquinolone pharmaceutical composition provided by the invention is greatly improved, greatly increasing the therapeutic effect of a single administration; using an organic solvent as the main solvent, compared with conventional enrofloxacin injection, it reduces the intramuscular injection irritation; the prepared fluoroquinolone pharmaceutical composition has stable properties and no crystallization during long-term storage; the preparation method is simple and easy to operate, and is easy to realize industrialized large-scale production.

Description

technical field [0001] The invention relates to a veterinary fluoroquinolone pharmaceutical composition. Background technique [0002] Fluoroquinolones have obvious after-drug effects on Gram-positive bacteria and Gram-negative bacteria, and it is concentration-dependent, that is, the higher the drug concentration, the longer the after-drug effect. With the increasing dosage of clinical use, the concentration of enrofloxacin injection has gradually developed from the initial 0.5% (g / ml) to the current 10% (g / ml). Because enrofloxacin has very little solubility in water and is easily soluble in sodium hydroxide solution, the prior art mainly adopts the method of adding co-solvent sodium hydroxide to increase the concentration of enrofloxacin in the preparation of enrofloxacin injection. Solubility in water, taking into account the stability of the product and the best conditions for enrofloxacin to produce bactericidal effect, control the pH value to 9.5-10.5 (Chinese Veteri...

AI Technical Summary

Problems solved by technology

However, it has been found in production practice that this method has problems such as high preparation difficulty, poor product stability and frost resistance when preparing high-concentration (i.e. 5%-10% (g / ml)) enrofloxacin injection: With the increase of enrofloxacin concentration, the amount of sodium hydroxide required to completely dissolve it in water also increases, and it is very difficult to control the pH value of the injection at 9.5-10.5; even if the pH value of the injection is increased to 11.5 , the product is also extremely unstable, and crystals will precipitate after 1-2 hours of refrigeration at 0°C, and the crystals cannot be redissolved when the temperature rises, which is extremely inconvenient to use in the cold winter conditions in the north

And because its pH value is on the high side, it is very irritating when injected, and causes great stress to animals during administration, especially for sick young animals, and the stress can lead to sudden death

At the same time, the high pH value of the injection will lead to necrosis at the injection site, affect the quality and appearance of carnivorous animals, and easily cause drug residues

At present, it is also reported that it is made into acidic or neutral injection, but all of them have the defects of low content or complicated preparation process, which is not convenient for production.

[0003] For ciprofloxacin lactate injection, the existing technology can prepare 10% content, but the 10% content also has problems such as difficult preparation, poor product stability and frost resistance: and further increase in concentration will cause stability problems such as crystallization, At the same time, using the existing technology to increase the content of ciprofloxacin and enrofloxacin injection to more than 15%, especially to about 30% and low irritation is a clinical demand

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