Azithromycin composition for injection and preparation method thereof

Abstract

The invention relates to an azithromycin composition for injection and a preparation method thereof. The composition consists of azithromycin, organic acid/sodium salt, freeze-drying excipient and a stabilizer in a weight ratio of (10-60):(2-15):(0-50):(0-50). According to a chemical reaction method, azithromycin and organic acid react to prepare a water soluble salt, so that the solubility of the azithromycin is increased, and the stability of the composition is improved. The preparation method comprises the following steps of: preparing the azithromycin into the water soluble salt, adding water to dissolve the water soluble salt, regulating pH, adding and dissolving the freeze-drying excipient and the stabilizer, then adding active carbon for discoloring, filtering and decarburizing, and sub-packaging after refined filtration; cooling to -40 DEG C within 0.5 hour, preserving the heat and freezing for 3 hours, vacuumizing to 13.33Pa, gradually increasing to -10 DEG C from -40 DEG C within 14 hours, and continuously drying for 5 hours at 35 DEG C. the composition prepared by the preparation method disclosed by the invention is accurate in dosage, stable in quality and high in purity.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a composition of azithromycin for injection and a preparation method thereof. Background of the invention [0002] Azithromycin is the first new azolide antibiotic researched and developed by Pliva Company of Yugoslavia Croatia. It was launched in Yugoslavia in 1988 and in the United States in 1992, and then it was promoted worldwide. [0003] Azithromycin is a derivative of macrolide antibiotic erythromycin, which is effective for respiratory tract infection, urinary tract infection, skin infection, soft tissue infection and infection in other parts of the human body. Compared with erythromycin, azithromycin has a wider antibacterial spectrum, high bioavailability, long half-life, less frequent administration, and less gastrointestinal irritation. [0004] Azithromycin is the first preparation of a new type of azolide antibiotics. Its mechanism of action is the same a...

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Problems solved by technology

For example, patent CN200510014275.1 uses hydrochloric acid and lactobionic acid as cosolvents. Since azithromycin is insoluble in water, it is unstable under strong acid (hydrochloric acid, sulfuric acid) conditions and is easily decomposed and destroyed during the preparation process. The process conditions are also very harsh, resulting in The cost of azithromycin freeze-dried agent remains high

Patent CN95106702.8 uses lactic acid and acetic acid as cosolvents to prepare lactic acid and azithromycin acetate salts, but the solubility of azithromycin acetate salts decreases after being heated at 105 for 5 hours, and the color of azithromycin lactic acid salts will de

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