Primarty Study On The Toxicity And Pharmacodynamics Of Domestic Cefquinome Sulfate

Cefquinome,the design and development of Hoechst Aktiengesellschaft Gemany at 80's in the 20 century.It was the first fourth-generation cephalosp antibiotics special and good antibiotic effect,low toxicity,low residue,high safety for animal,this drug was first approved in 1993.It has been approved for using for the treatment of respiratory tract infection of cattle and pigs caused by bacterial infections,as well as dairy cow and sows mammitis,study on the toxicity and pharmacodynamics of domestic cefquinome sulfate,To provide a reference in clinical application.1 Study on the toxicity of domestic cefquinome sulfateThis paper was designed to investigate general toxicity and special toxicity of domestic cefquinome sulfate in mice.Acute toxic effect and accumulative toxic effect tolerance test and tolerance test of cefquinome sulfate were detected by modified Kaber method and accumulative coefficient method respectively.Sub-chronic toxicity high(1/2LD₅₀),middle (1/4LD₅₀)and low(1/8LD₅₀) three dose groups,meantime establishing blank group,were treated with intraperitoneal injection for consecutively 28 days.Sperm structural test and micronucleus test of cefquinome sulfate were carried out in mice to evaluate its mutagenic toxicity.It was tested out that the mouse oral LD₅₀ of cefquinome Sulfate was higher than 5000 mg/kg.LD₅₀ was 844.03mg/kg after intraperitoneal injection of its suspension and 95%confidence interval was 802.05～887.56 mg/kg.Cefquinome sulfate is practical nontoxicity. The accumulative coefficient K was higher than 5,no death occurred.Blood routine detetion results show that a slight decrease of red blood cells count and platelet in high dose group,but compared with the control group,the difference is not so obvious(p＞0.05).Blood biochemistry indexs results showed that a slight increase of urea nitrogen and creatinine in high dose group.But the difference is not so obvious(p＞0.05).Other groups showed that measurement values were all in the normal range.Histopathologic examination also showed there were no abnormalities except renal capsule in the high dose group.It showed that cefquinome sulfate had little effect on blood routine and blood biochemistry indexs.Sperm structural test and Micronucleus test results were negative.Its showed that cefquinome sulfate had no mutagenicity and teratogenicity effect.The results showed that toxicity of domestic cefquinome Sulfate is slight and extensive safe extension.It is safety in clinical.2 Study on the antibacterial activities of domestic cefquinome sulfate in vitroThe antibacterial activities of domestic cefquinome sulfate and other antibiotics in vitro against clinical strains and standard strains were studied,the result showed that cefquinome sulfate had very high activities to clinical strains and standard strains in vitro.Antibacterial activities of cefquinone sulfate in vitro against E.coli,S.suis and A.pleuropneumoniae were (0.063μg/mL,0.016μg/mL,0.016μg/mL) stronger than ceftiofur sodium(0.25μg/mL,0.032μg/mL,0.125μg/mL) and amoxicillin sodium(2μg/mL,0.25μg/mL,0.5μg/mL), (0.5μg/mL) weaker than amoxicillin sodium(0.063μg/mL) against S.aureu,almost had no effect of mediums of different pH value and different bacterial inoculation amount on MIC of cefquinome sulfate.The killing curves of cefquinome sulfate against four standard strains showed that had a good killing rate,sterilization effect of cefquinome sulfate against E.coli,S.suis and A.pleuropneumoniae better than S.aureu,the killing rates weren't positively correlative with the drug concentrations(4,2,1MIC),as well as that it is Antibiotics that didn't depend on drug concentration.3 Study on pharmacodynamics of domestic cefquinome sulfate in chickens infected artificially by E.coliTherapeutic effect of domestic cefquinome sulfate has been investigated in chickens infected artificially by E.coli.Two hundreds and forty one-day-old sanhuang broilers were randomly alloted into eight groups after 25 days of breeding,three dose of cefquinome sulfate such as low(0.5mg/kg),medium(1mg/kg) and high dose groups(2mg/kg),ceftiofur sodium(1mg/kg),amoxicillin sodium(10mg/kg),ampicillin sodium(20mg/kg),the healthy and infection control groups were designed.The results showed that cefquinome sulfate can effectively control the infection caused by E.coli at the dose of medium and high dose groups.The effective rates were 93.3%and 90.0% respectively.The relative weight increase rates were 90.24%and 83.37% respectively.The compound can alleviate the symptom and prevent the discreasing weight and reduce the mortality rate of the broiler chicken infected with E.coli.The effect was superior to the control drug ceftiofur sodium,amoxicillin sodium and ampicillin sodium.All the results showed that the drug was perspective and recommend ability in the veterinary clinic.The dose of 1mg/kg for 25 days in chicken is suitable in clinic.