黄牛静注、肌注和内服吡喹酮的药动学与生物利用度  

Pharmacokinetics and Bioavailability of Praziquantel in Cattle after Oral,Intramuscular and Intravenous Administration

作　　者：操继跃[1] 刘恩勇[2] 赵俊龙[1] 李克斌[2] 窦树龙[1] 

机构地区：[1]华中农业大学畜牧兽医学院,湖北武汉430070 [2]湖北省畜牧局血防所,湖北武汉430060

出　　处：《中国兽医学报》2001年第6期612-614,共3页Chinese Journal of Veterinary Science

摘　　要：6头成年健康黄牛按 10 mg/ kg剂量单次快速静注吡喹酮 ,另 6头成年健康黄牛根据交叉试验设计法按 10 mg/kg剂量单次肌注、30 mg/ kg剂量内服吡喹酮进行药动学与生物利用度试验。利用高效液相色谱法测定血浆中吡喹酮原药的质量浓度 ,其检测限为 2 5μg/ L。房室模型分析表明 ,静注给药后的药时数据符合无吸收二室开放模型 ,其分布半衰期 (t1 / 2α)、消除半衰期 (t1 / 2β)、表观分布容积 (Vd)、总体清除率 (Cl B)、药时曲线下面积 (AUC)分别为 (0 .2 5± 0 .0 3)h、(1.2 8± 0 .2 0 ) h、(2 .11± 0 .38) L/ kg、(1.14± 0 .10 ) L/ (kg·h)和 (8.79± 0 .74) m g/ (L· h)。肌注的药时数据符合有吸收一室开放模型 ,主要药动学参数吸收半衰期 (t1 / 2 ka)、消除半衰期 (t1 / 2 ke)、药时曲线下面积 (AU C)、达峰时间(tmax)、峰浓度 (Cmax)和生物利用度 (F)分别为 (0 .40± 0 .17) h、(4 .6 5± 0 .91) h、(6 .85± 1.0 2 ) mg/ (L· h)、(1.33±0 .5 2 ) h、(0 .83± 0 .0 8) mg/ L 和 77.93%。内服给药后符合有吸收一室开放模型 ,吸收不规则 ,其药动学参数 t1 / 2 ka、t1 / 2 ke、AU C、tmax、Cmax和 F分别为 (1.0 8± 0 .13) h、(6 .81± 1.2 6 ) h、(8.5 1± 1.78) mg/ (L· h)、(4 .33± 1.36 ) h、The pharmacokinetics and bioavailability of a widespectrum antiparasitic, praziquantel, were studied in healthy adult cattle after intravenous,intramuscular and oral administration. The drug was given to 6 cattle at a dosage of 10 mg/kg b.w. intravenously, and another 6 cattle were administered the drug at a dosage of 10 mg/kg b.w. intramuscularly and 30 mg/kg b.w. orally by a single two-period cross over design method. Plasma praziquantel concentrations were determined by high-performance liquid chromatography, with a limit of detection of 25 μg/mL in plasma. The plasma drug concentration versus time data were fitted to a two-compartment model following a single intravenous injection of praziquantel in cattle. The main pharmacokinetic parameters were as follows: distribution half-life(t 1/2α) (0.25±0.03) h, elimination half-life(t 1/2β) (1.28±0.20) h, total body clearance(Cl B) (1.14±0.10) L/(kg·h), apparent distribution volume(Vd) (2.11±0.38) L/kg, the area under curve(AUC) (8.79±0.74) mg/(L·h), respectively. The drug concentration-time data were fitted to a one-compartment open model after a single intramuscular administration. The main pharmacokinetic parameters were as follows: absorption half-life(t 1/2ka) (0.40±0.17) h, elimination half-life(t 1/2ke) (4.65±0.91) h, AUC (6.85±1.02) mg/(L·h), the peak of plasma concentration(C max) (0.83±0.08) mg/L,the time to reach C max(t max) (1.33±0.52) h, the bioavailability(F) 77.93%,respectively. Plasma praziquantel pharmacokinetic parameters were calculated using a one-compartment open model after a single oral administration. The pharmacokinetic parameters were as follows: t 1/2ka (1.08±0.13) h, t 1/2ke (6.81±1.26) h, AUC (8.51±1.78) mg/(L·h), C max (0.70±0.08) mg/L,t max (4.33±1.36) h, and F 32.31%,respectively. The drug was well-absorbed into blood after i.m. dosing, but poorly absorbed after orally dosing in cattle. The bioavailability following i.m. dosing was higher 2.5 times as that following orally dos

关 键 词：黄牛 吡哇酮 药动学 生物利用度 静脉注射 肌肉注射 内服 

分 类 号：S858.23[农业科学—临床兽医学] S853.76[农业科学—兽医学]