20%吡喹酮注射剂在水牛体内的药代动力学研究  被引量:1

Pharmacokinetics of 20%praziquantel injection in water buffalo after intramuscular and oral administration

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作  者:孙雨[1] 卜仕金[1] 赵丹[1] 王柄樟[1] 汤仁想[1] 周明荣[1] 

机构地区:[1]扬州大学兽医学院药理与毒理实验室,江苏扬州225009

出  处:《中国兽医学报》2011年第3期402-406,共5页Chinese Journal of Veterinary Science

基  金:中国农业科学院上海兽医研究所资助项目

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。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.

关 键 词:吡喹酮 水牛 高效液相色谱 药代动力学 

分 类 号:S859.7[农业科学—临床兽医学]

 

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