Synthesis Of Cefotaxime Magnesium And Its Antibacterial Activity In Vivo And In Vitro

Cefotaxime is the third-generation cephalosporin and is a broad-spectrum antibiotic.It is mainly used for upper respiratory tract infections,pneumonia,hepatobiliary infections,urinary tract infections,intestinal infections and other diseases caused by sensitive bacteria.It also treats blood diseases and infections.Of patients with the best clinical antibacterial effect.At present,Cefotaxime sodium is commonly used clinically,alone or in combination with sulbactam sodium,but patients with hypertension,coronary heart disease,heart failure and renal insufficiency should not use sodium salt.Excessive sodium salt intake will aggravate the heart Preload causes heart failure.Magnesium is one of the essential elements involved in the normal life activities and metabolic processes of organisms.It is reported that magnesium has a certain antibacterial activity.Therefore,in this experiment,magnesium ions were used to replace sodium ions to synthesize Cefotaxime magnesium to study its antibacterial activity in vivo and in vivo.Objectives:1.Synthesize Cefotaxime magnesium and characterize its structure to determine whether the basic structure of Cefotaxime magnesium and Cefotaxime sodium are consistent.2.Investigate the in vitro bacteriostatic effect of Cefotaxime magnesium on gram-negative and gram-positive bacteria,and compare whether the bacteriostatic effects of Cefotaxime magnesium and Cefotaxime sodium are different.3.Investigate the pharmacodynamic experiments of Cefotaxime magnesium in rats,and compare whether Cefotaxime magnesium and Cefotaxime sodium have a difference in pharmacodynamics in rats,providing a reference for further research on cefotaxime magnesium.Methods:1.Cefotaxime acid has been used as a raw material drug,and Cefotaxime magnesium was synthesized by freeze-drying method.The structure was identified by ultraviolet spectrum,infrared spectrum,atomic absorption spectrometry,nuclear magnetic resonance hydrogen spectrum,carbon spectrum and liquid chromatography-mass spectrometry.2.Determine the minimum inhibitory concentration(MIC)of Cefotaxime sodium and Cefotaxime sodium against Staphylococcus aureus and Escherichia coli by the double dilution method in a test tube,and compare the bacteriostatic effects of the two drugs by the paper diffusion method.3.The tracheal intubation method was used to inject Streptococcus pneumoniae into the rat trachea to establish a rat pneumonia model.The tail vein was injected with cefotaxime sodium and cefotaxime magnesium.The physiological state of the rat was recorded every day.The blood was collected from the abdominal aorta three days after administration.,Automatic blood analyzer to detect blood routine and enzyme-linked immunosorbent assay to detect the content of IL-6,IL-10,TNF-?,IFN-? in serum.Results:1.Compared with Cefotaxime magnesium,the basic mother nucleus structure has not changed.The reaction between Cefotaxime acid and magnesium bicarbonate is a salt formation reaction.2.The MIC of Cefotaxime sodium and Cefotaxime magnesium against S.albicans and E.coli was determined by the double dilution method.The MIC of Cefotaxime magnesium was slightly lower than that of Cefotaxime sodium.Through the paper diffusion method,compared with the diameter of the bacteriostatic ring,the diameter of the bacteriostatic ring produced by Cefotaxime magnesium for three kinds of bacteria is slightly larger than that of Cefotaxime sodium.3.Compared with the model group,the blood index and serum index of each group were significantly reduced.Blood routine results showed that the efficacy of the Cefotaxime magnesium low-dose group was higher than that of the Cefotaxime sodium low-dose group(P<0.05).The detection of inflammatory factors showed The Cefotaxime magnesium group had a better effect on the down-regulation of inflammatory factors than the Cefotaxime sodium.The respiratory frequency of the Cefotaxime magnesium group was significantly lower than that of the Cefotaxime sodium group.Conclusions:1.The basic structure of Cefotaxime and Cefotaxime sodium is the same,and the reaction is salt formation.2.Cefotaxime sodium and Cefotaxime magnesium have inhibitory effects on three kinds of bacteria,and the bacteriostatic activity of cefotaxime magnesium is stronger than that of cefotaxime sodium.3.The pharmacodynamic results show that Cefotaxime magnesium is better than Cefotaxime sodium in the treatment of pneumonia.3.It may be that the introduction of magnesium ion enhances the bacteriostatic activity of Cefotaxime.