摘要
8头体重32.9±4.3kg(平均值土标准差)的健康长白×约克夏杂种猪,随机交叉设计试验,按10mg/kg静注或50mg/kg内服吡喹酮,给药间隔时间为2周。以乙醚萃取法提取血浆中的药物,反相高效液相色谱法测定血浆吡喹酮的浓度。非线性最小二乘法计算机程序拟合静注及内服的药时数据,分别适合二室开放模型及一级吸收一室开放模型。静注给药的动力学参数是:t1/2α0.31±0.08h,t1/2β1.50±0.57h,Vd(area)3.09±1.19 I/kg,Cl_B24.57±8.57ml/kg/min,AUC 7.48±2.36μg/ml·h。内服给药的动力学参数是:C_(max)0.27±0.21μg/ml,t_(max)0.97±0.50h,t1/2Ka 0.53±0.31h,t1/2 Ke 1.07±0.38h,tlag 0.07±0.08h,AUC 0.91±1.14μg/ml·h,F 3.20±5.7％。猪内服吡喹酮后,生物利用度很低的原因可能是吡喹酮在肝内有极强的首过效应。
The disposition and absorption pharmacokinetics of praziquantel were studied in younger cross-over pigs (n=8). Single doses of praziquantel were given as an iv bolus (l0mg/kg) and po (50mg/kg) into the same swine with a 14 day rest period between treaments. Blood samples were collected at different intervals after iv or po administration. The plasma concentration of praziquantel was determined by HPLC. The iv pharmacokinetics could be described by a two-compartment model with a tl/2α of 0.31±0.08 (X±SD) hour and a t1/2β of 1.50±0.57 hour. The total body clearance of praziquantel was 24.57±8.57ml/kg/min and the volume of distribution was 3.09±1.19 1/kg. Following po administration, the peak plasma drug concentration was 0.27±0.21μg/ml and occured at 0.97±0.50 hour. The oral bioavailability of praziquantel was observed to be 3.20±5.07%.
出处
《畜牧兽医学报》
CAS
CSCD
北大核心
1993年第2期170-174,共5页
ACTA VETERINARIA ET ZOOTECHNICA SINICA
关键词
吡喹酮
药物
动力学
猪
利用率
Praziquantel, HPLC, Pharmacokinetics, Bioavailability, Pigs
