Objective To investigate the pharmacokinetics and relative bioavailability of praziquantel injection in buffaloes in contrast to praziquantel tablet. Methods A single oral administration of praziquantel tablet at a dose of 20 mg/kg or intramuscular administration of praziquantel injection at a dose of 10 mg/kg was performed in six healthy adult buffalos according to a twoperiod crossover design. The praziquantel concentration in plasma was determined by a high performance liquid chromatography (HPLC) method. The pharmacokinetic parameters were calculated by non-compartmental analysis. Results The main pharmacokinetic parameters of praziquantel tablet were as follows: Tmax = (0.60±0.29)h, Cmax = (0.57±0.37)μg/ml, T1/2β = (0.70±0.42)h, AUC = (0.80±0.70) (μg/ml)·h. The main pharmacokinetic parameters of praziquantel injection were as follows: Tmax = (0.65± 0.49)h, Cmax = (3.82±1.17)μg/ml, T1/2β = (1.00±0.73)h, AUC = (1.61±0.89) (μg/ml)·h. The relative bioavailability of praziquantel injection was 402.5% in contrast to praziquantel tablet. Conclusion The praziquantel injection has pharmacokinetic characteristics of rapid absorption, high bioavailability and extensive distribution, and the clinical recommended dosage of praziquantel injection is 10 mg/kg.
［摘要］目的 研究吡喹酮注射液在水牛体内的药物动力学特征及其与吡喹酮片之间的相对生物利用度。方法 选用 6头健康成年水牛, 采用两周期随机交叉实验设计, 单剂量内服吡喹酮片 (20 mg/kg)或肌注吡喹酮注射液 (10 mg/kg), 高效液相色谱法 (HPLC)测定水牛血浆中吡喹酮浓度, 进行非房室模型分析, 计算药动学参数。结果 水牛内服吡喹酮片的峰时 (Tmax)为 (0.60±0.29)h, 峰浓度 (Cmax)为 (0.57±0.37)μg/ml, 消除半衰期 (T1/2β)为 (0.70±0.42)h, 药-时曲线下面积 (AUC)为 (0.80±0.70) (μg/ml)·h。水牛肌注吡喹酮注射液的 Tmax 为 (0.65±0.49)h, Cmax 为 (3.82±1.17)μg/ml, T1/2β 为 (1.00± 0.73)h, AUC为 (1.61±0.89) (μg/ml)·h。吡喹酮注射液相对于吡喹酮片的生物利用度为402.5%。结论 吡喹酮注射液肌注给药后在水牛体内具有吸收迅速, 生物利用度高, 体内分布广的药物动力学特征, 临床推荐给药剂量为10 mg/kg。 ［关键词］吡喹酮注射液; 药物动力学; 水牛; 相对生物利用度.
Keywords: Buffalo; Pharmacokinetics; Praziquantel injection; Relative bioavailability.