【摘要】 4头成年健康水牛采用随机交叉实验设计,分别进行吡喹酮注射剂肌注和吡喹酮片内服给药的药动学试验。吡喹酮注射剂按10 mg/kg的剂量单次肌注,吡喹酮片按20 mg/kg的剂量单次内服给药。采用高效液相色谱法测定血浆中吡喹酮的质量浓度,方法最低检测限和定量限分别为0.01 mg/L和0.062 5 mg/L。吡喹酮注射剂单剂量肌注给药,血药浓度-时间数据符合一级吸收一室开放模型,其主要动力学参数分别为:t_1/2（ka）（0.45±0.029）h,t_1/2（ke）（5.04±0.10）h,T_（peak）（1.72±0.029）h,C_（max）（0.87±0.006）mg/L,V（c）（8.58±0.010）L/kg,AUC（7.99±0.005）mg·L^-1·h^-1。吡喹酮片单剂量口服给药血药浓度-时间数据符合有吸收一室开放模型,其主要动力学参数分别为:Lagtime（0.13±0.010）h,t_1/2（ka）（0.76±0.11）h,t_1/2（ke）（1.31±0.076）h,T_（peak）（3.84±0.026）h,C_（max）（0.51±0.006）mg/L,V（c）（26.07±1.221）L/kg,AUC（7.99±0.005）mg·L^-1·h^-1。肌注相对生物利用度为（232±12.9）%。研究结果表明,20%吡喹酮注射剂肌注给药吸收迅速且完全,具有较高的生物利用度;吡喹酮吸收后在体内广泛分布。更多还原

【Abstract】 Four water buffalos were administered the drug at a dosage of 10 mg/kg b.w.intramuscularly and 30 mg/ kg body weight,orally by a single two-period cross over design method.Plasma praziquantel concentrations wes determined by high-performance liquid chromatography,with a limit of detection of 0.01 mg/L in plasma.The drug concentration-time date were fitted to a one-compartment open model after a single intramuscular administration.The main pharmacokinetic parameters were as follows:absorption half-life t₍1/2（ka）（0.45±0.029） h,elimination half-life t_1/2（ke）（5.04±0.110） h,T_（peak）（1.72±0.029） h,C_（max）（0.87±0.00.6） mg/L,AUC（7.99±0.005） mg·L（-1）·h^-1, respectively.Plasma praziquantel pharmacokinetic parameters were calculated using a one-compartment open model after a single oral administration,as follows:Lagtime（0.13±0.010） h,t_1/2（ka）（0.76±0.11） h,t₍1/2（（ke））（1.31±0.076） h,T_（peak）（3.84±0.026） h,C_（max）（0.51±0.006） mg/L,AUC（7.99±0.005） mg·L^-1·h^-1,respectively. The drug was well-adsorbed into blood after i.m.dosing,but poorly absorbed after orally dosing in cattle.The results suggest that intramuscular administration is a reasonable route in treatment,of water buffalo schistosomiasis.更多还原