吡喹酮在绒山羊体内药代动力学的研究

Pharmacokinetics Study of Praziguantel after Oral Administration in Cashmere Goat

应用反相高效液相色谱法测试了 6只健康绒山羊以每千克体重 10 0mg剂量口服给药后吡喹酮在体内的血药浓度 ,并进行了药代动力学研究 ,应用非线性最小二乘法处理 ,实验数据参数用一室模型描述。在口服给药后 ,经过短暂的迟滞期 [Lagtime =(0 2 3987± 0 0 95 39)h],血药浓度迅速上升 ,吸收相很快完成[t1/ 2ka=(0 33899± 0 192 94)h],达峰时间tp=(1 6 45 6 8± 0 43788)h ,之后是一缓慢的消除相 [t1/ 2kel=(6 2 3789± 0 70 6 2 7)h],表观分布容积Vd=(2 3 6 8130± 13 16 197)L/kg ,机体清除率CLB =[(2 6 2 3 46±1 473 10 )mg/(kg·h) ],药时曲线下面积AUC =[(5 0 0 73 2 7± 2 6 12 482 ) μg/(mL·h) ],最高血药浓度Cmax=(4 89990± 2 830 6 4) μg/mL。对吡喹酮在绒山羊体内血药浓度实测值与理论值进行卡平方检验 ,结果表明二者之间没有显著性差异 (P >0 0 5 )。

The drug concentration of plaziquantel in plasma were determined by high performance liquid chromatography(HPLC)and the pharmacokinetics of praziquantel were determined after oral administration of 100 mg/kg of body weight to six cashmere goats using nonlinear least squares regression methods.Data obtained were best described by one compartment open model.After dosing there is a short lagtime [Lagtime=(0 239?87±0 095?39)h].Then plasma concentration of praziguantel increased rapidly And the absorption phase was quickly completed [ t 1/2ka =( 0 338?99± 0 192?94)h].The time of peak ( t p) is described as t p=(1 645?68±0 437?88)h.After peak, there is long clearance phase [ t 1/2kel =(6 237?89±0 706?27)h].The apparent volume of distribution V d=(23 681?30±13 161?97)L/kg.The mean body clearance rate CLB=[( 2 623?46± 1 473?10)mg/(kg·h)].The area under curve of concentration time AUC=[( 50 073?21± 26 124?82)μg/(mL·h)].The maximal plasma concentration C max =(4 899?90± 2 830?64)μg/mL . No significant difference was found between the measured values and theoretically predicted values in the plasma concentration of praziquantel ( P >0 05).