安托可金(0325k_(1-1)在大鼠体内的药代动力学

The Pharmacokineticsof0325k_(1-1) in Rats

以原子吸收法测定了大鼠血浆、组织与胆汁、尿、粪便中安托可金的浓度。大鼠静注安托可金后符合二房室模型处置特征 ,分布半衰期平均为 0 .2 5± 0 .0 2h ,消除半衰期平均为 1 1 .4± 0 .57h ,中央室分布容积为 0 .1 6± 0 .0 5L/kg。静注安托可金后该药可很快向机体的各组织分布 ,大多数组织在 6min即达到较高浓度 ;其中以肾脏浓度最高 ,肝、肺、子宫、皮肤、瘤体等组织也有较高的浓度。静注给药后 ,2 4h的累积尿排泄率平均为 (77.6± 1 0 .3 ) % ,1 2 0h的累积排泄率平均为 (90 .7± 3 .80 ) % ,说明肾脏是该药的主要排泄途径 ;安托可金在粪中的排泄较少 ,1 2 0h的累积排泄率平均为 (2 .87± 0 .4 6) % ,2 4h的胆汁累积排泄率平均为(1 .0 1± 0 .2 9) % ,说明粪和胆汁不是该药的主要排泄途径。安托可金与大鼠的血浆蛋白结合率平均为 (4 0 .7± 3 .4 9) %。

The concentration of 0325k 1 1 in the plasma,tissues, bile, urine and faeces of rats has been determined by flameless atomic absorption spectrophotometry. The plasma concentration time profiles fitted to two compartments after i.v., and the distribution half life t 1/2α was 0.25±0.02 h and the elimination half life t 1/2β was 11.4±0.57 h and the distribution volume of central compartment V c was 0.16±0.05 l/kg. The distribution process of 0325k 1 1 to tissues was much quicker, and the levels at 6 min was the highest for most tissues after iv use. For all tissues studied, the kidney, liver, lung, skin and tumor tissues had higher levels than those of other tissues. More than 90% of the drug was excreted in urine after i.v. but less than 3% was found in bile or faeces. The combination rate of the drug to plasma protein was (40.7±3.49)%.