Study On Production Technology Optimization Of Levofloxacin Lactate And Sodium Chloride Injection

Levofloxacin lactate is the third generation broad-spectrum antibacterial of quinolones. It’s no cross-resistance effects with other antimicrobial agents, so it can be used widely in clinical applications. However, the visible particles of levofloxacin lactate and sodium chloride injection can be effected with many factors, the product qualification ratio was low.The visible particle detection indicated that many white spots appeared in the injection after exposed to room temperature for long time.Thus, the visible particles do not meet the national drug standards. Therefore, the improvements on the production technology is needed to keep the quality of the levofloxacin lactate and sodium chloride injection and ensure the patients’safety.On the basis of the references and the complete analysis of the visible particles influence factors, we carried out the corresponding studies by choosing the quantity of active carbon as well as the pH and the metal complexes, which can improve the visible particles of the injection. This paper put forward an effective method of controlling the visible particle creatively. The orthogonal test results scientifically and efficiently indicated that the best technological conditions are as follows:the closed loop time is20minutes at the temperature of40℃with the EDTA-2Na concentration is0.2‰, the Ingredients can temperature is40℃and the quantity of active carbon is3%. Based on the above conditions, the obtained levofloxacin lactate and sodium chloride injection was satisfied and met the test stardards and the Chinese Pharmacopeia.The results of the preliminary stability tests were as follows:the preparations were stable enough after10days expose to light (45001x) and high temperature (60℃), respectively. While, the related substances increased slightly, the drug content decreased under high temperature (60℃) and light (45001x) for10days. These results indicated that the levofloxacin lactate and sodium chloride injection was stable to humidity and light, was unstable to high temperature.The accelerated testing (40℃, RH75%) results showed that the related substances and the optical isomers increased slightly, and the drug content decreased slightly. Other indicators are almost unchanged, are in line with regulations.For long-term testing, the samples were investigated under room temperature (25℃, RH60%) for12months, the results showed that the preparations were stable enough under this long-term testing condition.Through process optimization of the levofloxacin lactate, Some correlative conclusions about the drug content, the related substance and the optical isomers were obtained. The suitability test was also carried out. Results show that optimized process can improve the production stability, the visible particle met the standards of China Pharmacopoeia. In addition,the result also showed that the levofloxacin lactate injection was unstable to light and heat. Need to be stored no more than20℃.