【摘要】 本文报告头孢唑肟在犬体内的组织浓度及药代动力学。静注及肌注剂量均为20mg/kg,药物浓度以微生物杯碟法测定。 根据F检测、γ₁²值及AIC值判别房室模型,肌肉和静脉注射的药代动力学分别符合开放型一室和二室模型。肌注后0.5小时血药浓度达峰值,为55.40±7.68μg/ml。静脉注射后平均即刻血浓度为201.92±19.34μg/ml,肌注与静注后血浆半衰期分别为2.11±0.42和1.94±0.49小时,总表观分布容积分别为0.37±0.06和0.32±0.04L/kg。生物利用度为89.03±11.15％,犬血清蛋白结合率为19.4％。 6只犬分为两组,分别单次肌注或静注头孢唑肟20mg/kg,测定1小时后各组织浓度。结果显示,静脉注射组的各平均组织浓度略高于肌肉注射组。肾脏浓度最高,按递减顺序其他组织为肝、子宫或前列腺、肺、小肠、胰、心、骨骼肌和脾脏。胆汁浓度低于血清浓度,脑组织浓度最低。静注与肌注后脑脊液平均浓度为1.22±0.67和0.64±0.19μg/ml。更多还原

【Abstract】 The pharmacokinetics and tissue concentration of ceftizoxime after im and iv administration were determined in 6 healthy dogs. The drugs were given in a dose of 20 mg/kg to each test animal. Drug concentration was bioassayed by the disk-plate diffusion technique.Based on the F-, γ₁²-and AIC-values,the pharmacokinetics after iv bolus injection conformed to a first-order two-compartment open model) while the pharmacokinetics after im injection conformed to the one-compartment open model. The mean peak concentration in serum samples after im injection was 55.40±7.68μg/ml at 0.5 hr. After iv bolus injection, the mean peak level was 201.92 ± 19.34μg/ml. Serum half-lives after iv and im injection were 1.94±0.49 and 2.11±0.42hr respectively. The value of Vd were 0.37 ±0.06 and 0.32 ± 0.04 L/kg. Binding of CZX to dog serum protein was 19.4%.Three dogs of each group wee given ceftizoxime in a single dose of 20mg/kg intramuscularly or intravenously. Tissue level were determined 1 hr after administration.The average concentration of different tissue were higher in the iv group than those in the im group. The concentration in the kidney tissue was the highest, followed in decreasing order by hepatic, uterine, prostatic, pulmonary, small intestinal, pancreatic cardiac, muscular and splenic tissue. The concentration in the bile was lower than that in th serum, and was lowest in the brain tissue. The average concentration in CSF after iv and im injection was1.22 ± 0.67 and 0.64± 0.19μg/ml respectively.更多还原