Preparation And Application Of Apramycin Sulfate Injection

Apramycin is a broad-spectrum antibiotic for aminoglycoside for animals.It has good antibacterial effect on Gram-negative bacteria,Gram-positive bacteria,Treponemaum and some mycoplasma.It is widely used in veterinary medicine.Due to the poor stability of the injection and more irritating of the product,most of the commercially available products are soluble powder,premix,injection products rarely.Objective:In this study,a stable,safe and efficient type of apramycin injection was prepared by screening and optimizing the preparation of apramycin injection of sulfuric acid.And evaluate its clinical efficacy,the clinical recommended dose,provide the basis for its application in clinical practice.Method:Screening accessories.The optimum production conditions were determined by orthogonal test.The stability of the prepared injections was observed and evaluated by the influencing factor test,the accelerated test,and the long-term test.The minimal inhibitory concentration and minimum bactericidal concentration of five drugs?Escherichia coli,Salmonella,Staphylococcus aureus,Streptococcus suis,Pasteurella multocida?were tested with commercially available apramycin injection as control group.The LD₅₀ was determined by UDP.Evaluation of homemade drug safety by muscle irritation test,heat source test and hemolytic test in vitro.Based on the preliminary clinical diagnosis and etiological diagnosis of diarrhea piglets,the natural cases were determined to be Escherichia coli diarrhea.After the diagnosis of diarrhea piglets were grouped,each group of 20,set dose of 0.3mg/kg,0.2mg/kg,0.1mg/kg of homemade apramycin sulfate injection as high,medium and low dose group,set the dosage is 0.2mg/kg of commercially available Apramycin sulfate injection for drug cont-rol group,set the given 0.2mg/kg physiological saline as blank control group,observe and evaluate the clinical curative effect of drugs.Result:The optimum preparation materials of homemade apramycin sulfate injection were sodium sulfite,citric acid and disodium ethylenediaminetetraacetate.The optimum prep-aration conditions were solvent temperature 40 degrees,sterilization time 30 min,sterilization Temperature 120 degrees.The results of stability test showed that the self-made injection was allowed to stand for 12 months under the condition of temperature 25±2 degrees and humidi-ty 65±5%,the PH range was 5.04-5.44,the content range was 100.2%-107.8%,both in the“People's Republic of China Veterinary Pharmacopoeia”2010 Editionon the quality control of the injection of apramycin sulfate?quality standards:PH should be 4.5-6.5,the cotent should be marked the amount of 90.0%-110.0%?,the results show that it has a high stability.The minimum inhibitory concentrations of homemade injection against Escherichia coli,Sal-monella,Staphylococcus aureus,Streptococcus and Pasteurella multocida were 0.08?g/ml,0.62?g/mL,0.06?g/mL,0.31?g/mL,0.31?g/mL,the minimum bactericidal concentrations were 2.5?g/mL,25?g/mL,100?g/mL,200?g/mL,50?g/mL.The LD₅₀ of the self-made injection was 857.8 mg/kg?95%confidence interval was 700-920mg/kg?.No muscle irritation and heat source,no hemolytic reaction.The clinical efficacy test showed that the therapeutic effect of homemade apramycin injection on diarrhea piglets was dose-dependent,and the cure rate of piglets in high dose group and middle dose group was higher than that in drug control group,but there was no significant difference?P>0.05?,indicating that the effect of self-made injection is better than commercial products,the clinical recommended dose of0.3mg/kg.Conclusion:The preparation of the selected materials and optimize the production process is reasonable.And the stability is good,no adverse reactions were found,and the curative effect on the disease caused by sensitive bacteria was significant.Therefore,the preparation can be used for clinical treatment.