The Preparation Of 5% Levofloxacin Hydrochloride Injection And Its Clinical Application Research On Snake

This study was performed to develop an injection which was effective and suitable for Clinical applications in snakes infected by bacterial. Drug combination susceptibility test was used to screen reagent, and the result showed that the combination of levofloxacin hydrochloride and trimethoprim caused no relative effect on Proteus penneri and E. coli in snakes, so levofloxac in hydrochloride was selected for injection preparation alone. 5% levofloxac in hydrochloride injection was prepared successfully by means of the method of rapid temperature change. The stability, quality and safety of the injection were performed. Microbiological assay was used to preliminary determination blood drug concentration changes, absorption, distribution of the injection in snakes, and levofloxacin hydrochloride injection was used in the treatment of clinical cases. The results showed that:(1) 5% levofloxacin hydrochloride injection showed significant difference on antimicrobial activity of 12 species of bacterial isolated from snakes. The minimum inhibitory concentration (MIC) to E.coli and Proteus penneri were 0.16 ?g/mL and 0.19 ?g/mL, which were higher than those of Brevibacterium casei, enterococcus faecalis, oxytocin klebsiella, pseudomonas aeruginosa, arthrobacterium, proteus (MIC ranged from 0.78 ?g/mL?3.12 ?g/mL), but MIC to salmonella, stenotrophomonas maltophilia, staphylococcus kloosii, staphylococcus lentus were lower, their ranges were 12.50 ?g/mL to 40.00 ?g/mL. The results suggested that the sensitivity of the gram-negative bacteria to levofloxacin hydrochloride injection was higher than the gram-positive bacteria in snake. The high, medium and low dose group of Levofloxacin hydrochloride injection on mice which were infected Proteus penneri had the protective effect, and showed a clear concentration-response relationship.(2) High Performance Liquid Chromatography (HPLC) method with the condition of the mobile phase:0.1% phosphoric acid and acetonitrile (85:15, V/V), the flow rate:1 mL·min-1, column temperature:30?, detection wavelength:294 nm can detect the content of levofloxacin hydrochloride injection; the average recovery was 93.68%.5% levofloxacin hydrochloride injection could save at least six months at room temperature, shading conditions.(3) 5% levofloxacin hydrochloride injection had not irritation for cobra, and the maximum dose was 600 mg/kg, the poisoning symptom of exceed this dose showed the head nystagmus, severe cases head-tilt, weakness, mouth mucus, autopsy visible intestinal hyperemia, nephropathy, such as swelling, the color of organ presented as yellow-red or yellow.(4) Fluoroquinolone are drugs acting in a concentration-dependent manner sterilize, minimum bactericidal concentration was 0.1?10 (?g/mL. A dosage of 4 mg/kg Levofloxacin hydrochloride injection i.m. in cobra would maintain a relatively higher blood drug concentration every 14 hours to medicine, but according to Cmax/MIC?10?12 or AUC0?24h/MIC?100?125, its antibacterial effect would be the best, and had a higher value of Cmax/MIC, the smaller risk of bacterial resistance. Therefore, based on the calculated Cmax/MIC, the peak blood concentration was 1.6?1.92 ?g/mL. A dosage of 10 mg/kg b.wt was recommended to treat infections caused by bacteria which the MIC of Proteus penneri was 0.16 mg/mL. Therefore, in blood and organization would achieve ideal bactericidal concentration. Levofloxacin hydrochloride injection is widely distributed in the organization with high concentration and could be used for the treatment of systemic bacterial infection.(5) The treatment effect of 5% levofloxacin hydrochloride injection for the four typical clinical cases were good, and the cure rate was more than 80%.Our results indicated that:(1) the preparation method of 5% levofloxacin hydrochloride injection was feasible and the production process was stable. (2) Using HPLC method which had high sensitivity to detect the contents of 5% levofloxacin hydrochloride injection, the result was accurate. Microbiological assay with the characteristic which was operative easily and the price lowly for determination of levofloxacin hydrochloride injection in blood and tissue drug concentration of cobra. (3) Data suggest that levofloxacin hydrochloride injection at a dosage of 10 mg/kg i.m. in snakes every 48 hours may be an effective antimicrobial.