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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 adult healthy buffaloes were randomized to a crossover design. The pharmacokinetics of praziquantel injection intramuscularly and praziquantel tablet were given respectively. Praziquantel injection at a single dose of 10 mg / kg intramuscular injection, praziquantel tablets at a single dose of 20 mg / kg administered. The HPLC method was used to determine the concentration of praziquantel in plasma. The detection limits and the limits of quantification were 0.01 mg / L and 0.062 5 mg / L, respectively. The main pharmacokinetic parameters of praziquantel injection were single-dose intramuscular injection and plasma concentration-time data in accordance with the first-order absorption one-compartment open model. The main kinetic parameters were p (t 1/2) (0.45 ± 0.029) h, t_ (1/2) (5.04 ± 0.10) h, T_ (peak) (1.72 ± 0.029) h and C_ (max) (0.87 ± 0.006) mg / L and V ± 0.010) L / kg, AUC (7.99 ± 0.005) mg · L -1 · h -1. The single-dose oral administration of praziquantel tablets was consistent with the open-chamber model with absorption and its main kinetic parameters were: Lagtime (0.13 ± 0.010) h, t 1/2 (ka) (0.76 (0.31 ± 0.076) h, T_ (peak) (3.84 ± 0.026) h, C_ (max) (0.51 ± 0.006) mg / L, (c) (26.07 ± 1.221) L / kg and AUC (7.99 ± 0.005) mg · L -1 · h -1. The relative bioavailability of intramuscular injection was (232 ± 12.9)%. The results showed that intramuscular injection of 20% praziquantel injection absorbed rapidly and completely, with high bioavailability; praziquantel absorption widely distributed in the body.