Gatifloxacin freeze-dried powder injection and preparing method thereof

Abstract

The invention provides a gatifloxacin freeze-dried powder injection and a preparation method thereof. The method includes weighing the raw and auxiliary materials according to the formula and placing them in a sterile container, adding water for injection at a temperature of 70-80°C, keeping warm and stirring evenly, and then adding lactic acid solution, and mixing the raw and auxiliary materials to obtain a pH value of 4.0±0.5 after stirring solution; then add activated carbon for needles, stir evenly and let it stand, then filter for decarbonization to obtain the filtrate after decarbonization; dilute the decarbonized filtrate with water for injection to the configured amount, stir well and pass through 0.45 μm, 0.22 μm Composite microporous membrane filtration, the obtained filtrate is bottled and the gas outlet is reserved; the obtained filtrate in the bottle is freeze-dried: first pre-freeze at -40°C for 2-4 hours, and then freeze at -40°C ~ 10 Dry under reduced pressure and vacuum for 24-28 hours under the condition of ℃, and finally dry at 35 ℃ and high temperature for 6-8 hours.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a preparation method of gatifloxacin freeze-dried powder for injection. Background technique [0002] Gatifloxacin (Gatifloxacin) is a newly synthesized fourth-generation quinolone antibacterial drug, which was researched and developed by Japan's Kyorin Company. At present, the U.S. company Bristol-Myers Squibb has obtained the drug in Canada and Brazil. , Mexico, Argentina and other countries. In June 1999, the application for the marketing of oral and intravenous injection preparations of this product was submitted to the US FDA in June 1999, and it was approved in December 1999. It is clinically used to treat bacterial infections of the respiratory system, urinary system and gynecological diseases. The clinical dosage is 400mg / d orally or intravenously. This product has a different structure from quinolone antibacterial drugs such as ciprofloxacin and ofloxacin. The C7 positi...

AI Technical Summary

Problems solved by technology

[0012] The prior art shows that gatifloxacin is slightly soluble in water, so the preparation of freeze-dried powder injection usually adds Injection water, add lactic acid solution, stir evenly, so that gatifloxacin is easy to dissolve, and then add sodium hydroxide The pH value of the solution is adjusted, which makes the process cumbersome. First, lactic acid is used to dissolve gatifloxacin, and then hydrogen is added. The sodium chloride solution is adjusted to the required pH value, and the clarity and stability of the prepared gatifloxacin freeze-dried powder injection are not stable. Well, the clarity of the freeze-dried powder injection is not good, and the main drug content is low, while the content of related substances is high, In order to improve the above-mentioned properties of gatifloxacin freeze-dried powder injection, researchers of the present invention, through long-term experimental research, research The researchers found that under the conditions of 70-80°C water for injection and a certain concentration of lactic acid solution, the solubility of gatifloxacin Good performance, combined with an appropriate freeze-drying process, the performance of the prepared freeze-dried powder injection is good, and the preparation method is simple, Therefore, the present invention is proposed

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