Pharmacokinetics Study of Cefoselis Sulfate in Rabbits

OBJECTIVE:To study pharmacokinetics of cefoselis sulfate in rabbit.METHODS:15 rabbits were randomly divided into high-dose group(75 mg·kg -1 ),medium-dose group(150 mg·kg -1 )and low-dose group(300 mg·kg -1 ).3 groups were given medicine via ear vein.Blood sample and urine sample were collected before administration.Then blood samples were collected at 5 min,10 min,15 min,30 min,45 min,60 min,80 min,100 min,120 min,150 min,180 min,240 min and 360 min after administration.The urine samples were collected at 0～2 h,2～4 h,4～6 h,6～8 h,8～12 h after administration.The concentrations of cefoselis in blood samples and urine samples were determined by HPLC.The pharmacokinetic parameters were calculated. RESULTS:Pharmacokinetics of cefoselis in rabbits conformed to one-compartment mode.Main pharmacokinetic parameters were as follows:t 1/2 :(0.87±0.03)h,(0.88±0.04)h and(0.86±0.04)h;c max :(210.54±28.92)mg·L -1 ,(362.66±47.86)mg·L -1 and (805.46±61.11)mg·L -1 ;AUC (0～6 h) :(288.52±38.79)mg·h·L -1 ,(495.12±64.78)mg·h·L -1 and(1 095.81±75.34)mg·h·L -1 , respectively.The accumulative urinary excretion at 12 h was up to average value with accumulative excretion rate of 68.44%～ 72.29%.CONCLUSION:The pharmacokinetics of cefoselis sulfate(75～300 mg·kg -1 )in rabbit conforms to linear relationship and first-order kinetics.