| Bioequivalence evaluation reflects the biological standard of drugs, provides conclusive proof for clinical curative effect, and determine whether the active components of the same drugs in two different preparations or products of the same ingredients in two manufacturers can replace each other when used in clinic on animals (FDA,2001). Speeding up application and approval process of new drugs, it has very important significance to reduce the cost of research and development of new drugs. Ceftiofur is the third generation of cephalosporin antibiotics, widely used abroad in treatment of espiratory disease in pigs, cattle, sheep and chicken.At present our country has developed ceftiofur hydrochloride suspension injection, in order to compare the efficacy and safety of domestic ceftiofur hydrochloride with similar foreign products in the clinical application of vet, subject to the domestic ceftiofur hydrochloride suspension injection for the tested drug, its speed and Jie Ling (EXCENEL) in biological bioequivalence evaluation pigs, domestic ceftiofur hydrochloride and quick solution spirit on the pharmacokinetics of pigs were analyzed, providing reference for veterinary clinical rational drug use.In this experiment,24healthy Landrace x large white cross barrows (long white boars), body weight of30±5kg, according to a2x2crossover design, a single dose of intramuscular injection of ceftiofur hydrochloride injection and quick solution spirit, respectively after administration of0.13h,0.5h,1H,2h,4h,5h,8h,12h,24h,48h,72h,96h,120h,144H precaval vein blood3-4mL, implantation of centrifugal heparin sodium anticoagulation tube,3000r/min centrifugal10min after taking the plasma. Plasma samples were two sulfur erythritol extraction and ProElut PLS SPE cartridge followed by high performance liquid chromatography (HPLC) was detected, quantified by external standard method, the regression equation is y=23.09x+15.37, correlation coefficient r=0.9996. Measured the recovery rate is greater than80%, the variation coefficient was less than8%LOD, the detection limit was0.05μg/mL, the limit of quantification of LOQ was0.1μg/mL, meet the need for a bioequivalence study using the method of drug concentration in blood.The data of drug concentration using3P97software for processing, the two kinds of ceftiofur injection products is very similar in the pharmacokinetics of pigs, are in line with the absorption of the two compartment open model. Domestic ceftiofur hydrochloride and quickly solve the plasma concentration-time curve in the area under the spirit of AUC0-mean was376.7±117.8μg·h/mL and390.5±124.6μg·h/mL, the relative bioavailability of96.5%; the average measured peak concentrations of Cmax were34.6±5.5μg/mL and36.1±6.2μg/mL; the mean measured peak time of Tmax were1.27±0.18h and1.26±0.21h. In the multivariate analysis of variance (ANOVA), two one-sided t test and90%confidence interval method for statistical tests, showed that domestic5%ceftiofur hydrochloride injection solution and velocity of spirit in pigs are bioequivalent, providing a basis for the further study of the domestic preparation. |
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