Moxifloxacin hydrochloride injection pharmaceutical composition and its preparation and quality control method

Abstract

The invention relates to a moxifloxacin hydrochloride injection pharmaceutical composition and a preparation method and a quality control method thereof. The moxifloxacin hydrochloride injection pharmaceutical composition comprises moxifloxacin hydrochloride, aspartic acid, sodium calcium edetate, an optional acidifying or alkalizing agent and water for injection. The quality control method is a method for determining content of RR isomers in the moxifloxacin hydrochloride injection pharmaceutical composition. The moxifloxacin hydrochloride injection pharmaceutical composition and the preparation method and the quality control method thereof have the superior advantages specified in the description.

Description

technical field [0001] The present invention relates to a preparation of an injection containing moxifloxacin hydrochloride as the main medicinal component, a preparation method and application thereof, and a quality control method of the moxifloxacin hydrochloride injection pharmaceutical composition. technical background [0002] Fluoroquinolones are fully synthetic antibacterial drugs that have developed very rapidly in the past two decades. They mainly act on the helicase and topoisomerase of bacterial DNA. They have the characteristics of broad antibacterial spectrum, strong antibacterial effect, and high safety. It is widely used clinically to treat respiratory, urinary tract, skin and soft tissue, ENT, gynecology, tuberculosis and other infections caused by Gram-positive bacteria, negative bacteria, and anaerobic bacteria. According to the chemical structure, antibacterial effect and in vivo process of quinolones, they can be divided into first, second, third and four...

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Problems solved by technology

Chinese patent 00811427.7 records that the water preparation of moxifloxacin hydrochloride and glucose has poor stability due to iron ions

[0019] CN103543230A (201210236984.4) discloses a method for the separation and determination of moxifloxacin hydrochloride and its enantiomers, which is characterized in that it includes: 1) selection of reference substances: moxifloxacin hydrochloride racemate, moxifloxacin hydrochloride; 2) Sample preparation: take moxifloxacin hydrochloride racemate, add mobile phase to dissolve and dilute, and prepare a moxifloxacin hydrochloride racemate solution of 1 μg / ml to 20 μg / ml; take moxifloxacin hydrochloride, add mobile phase to dissolve and dilute, and prepare 0.4mg / ml~1mg / ml moxifloxacin hydrochloride solution; 3) Chromatographic conditions: high performance liquid chromatography, the chromatographic column used is a reversed-phase chromatographic column, and the mixed aqueous solution of copper sulfate and chiral reagent is the water phase, The mixture of aqueous phase and organic phase is the mobile phase, the column temperature is: 20°C ~ 45°C; the flow rate is: 0.6ml / min ~ 1.4ml / min; the detection wavelength is: 270 ~ 310nm; 4) Determination: separate precision measurement Take 2 μl to 50 μl of the moxifloxacin hydrochloride racemate solution and the moxifloxacin hydrochloride solution, inject them into a liquid chromatograph, and record the chromatograms, but it is unclear whether this method is suitable for testing the formulation of the injection solution of the present invention

However, the inventors have also found that the above-mentioned CN102895178A contains amino acids, such as aspartic acid-containing injections, which are stored in a slightly low temperature environment (such an environment is easy to encounter, for example, it is often encountered in some circulation links) There will be slight opalescence later, although it is not clear whether this will affect the safety of the product, but it is known to those skilled in the art that it still needs to be avoided as a marketed drug.

The inventor found through further research that this opalescence can be avoided by using activated carbon adsorption in the injection preparation process; however, unfortunately, the new problem caused by the use of activated carbon adsorption is that when using activated carbon adsorption, Shows a significant adsorption of active ingredients, resulting in a significant loss of active ingredients in the finished product, which needs to be overcome by increasing the amount of feed

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