喷昔洛韦注射剂在中国健康人体内的药代动力学

Pharmacokinetics of penciclovir injection in Chinese healthy volunteers

目的:考察喷昔洛韦注射剂在中国健康人体内的药代动力学。方法:10名健康志愿者单剂量静脉输注10mg/kg的喷昔洛韦,应用高效液相色谱-荧光检测法测定生物样品中的药物浓度,并采用Win-NonLin程序进行非房室模型拟合,计算药代动力学参数。结果:计算得到的药代动力学参数如下:ke为(0.37±0.05)/h,t1/2为(1.91±0.26)h,Cmax为(9.8±1.6)mg/L,AUC0-t为(19.1±2.8)mg.L-1.h,AUC0-∞为(19.6±2.9)mg.L-1.h,Vd为(1.4±0.4)L/kg,CL为(0.52±0.08)L.h.kg-1。给药后12h尿中喷昔洛韦累积排泄率约为70%。结论:喷昔洛韦静脉输注后在人体内分布广泛,主要经过肾脏迅速排泄。

AIM： To study the pharmaeokineties of peneielovir injection in Chinese healthy volunteers. METHODS： 10 healthy volunteers were infused a single dose of 10 mg/kg of penciclovir. The concentrations of penciclovir in plasma and urine were determined by HPLC-FLD. Pharmacokinetic parameters were conformed to a non-compartment model analyzed by WinNonLin program.RESULTS： The main pharmacokinetic parameters were as follows： the ke was （0.37 ± 0.05） /h; the t1/2 was （1.91 ±0.26） h; the Cmax was （9.8± 1.6） mg/L; the AUC0-t was （19.1 ±2.8） mg·L^-1·h; the AUC0-∞ was （19.6±2.9） mg·L^-1·h; the Vd was （1.4±0.4） Llkg; the CL was （ 0.52 ± 0.08 ） L·h·kg^-1 About 70% of peneielovir was excreted into urine within 12 h. CONCLUSION： Peneielovir is widely distributed and rapidly excreted, predominantly by the kidney.