盐酸伐昔洛韦在人体内的药动学和相对生物利用度

Pharmacokinetics and relative bioavailability of valaciclovir in healthy volunteers

目的研究伐昔洛韦在正常人体内药动学和相对生物利用度。方法20名健康志愿者单剂量交叉口服伐昔洛韦300mg和参比片,用高效液相色谱(HPLC)法检测受试者血药浓度,并计算两者的药动学参数。结果受试药与参比药的血药浓度水平一致。其主要药动学参数t1/2分别为(3.81±0.66)h和(4.15±0.74)h;Tmax分别为(1.48±0.58)h和(1.38±0.56)h,Cmax分别为(1.86±0.50)mg/L和(2.07±0.62)mg/L,AUC分别为(7.51±1.71)mg.h/L和(7.03±0.98)mg.h/L,两制剂的药动学参数相近。用AUC估算的伐昔洛韦试验药相对生物利用度为98.0%±11.8%。结论伐昔洛韦片和参比片的AUC、Cmax经方差分析和双向单侧t检验表明两制剂生物等效;Tmax经非参数法检验表明两种制剂差异无统计学意义(P>0.05)。

Objective To study the pharmacokinetics and relative bioavailability of valaciclovir in healthy volunteers. Methods A single oral dose of 300 mg test valaciclovir or reference drug was given to 20 volunteers according to a randomized crossover study. The drug concentration in plasma was analyzed by HPLC method. Results The main pharmacokinetic parameters of valaciclovir were as follows： t1/2（3.81±0.66）hand （4.15±0.74）h, Tmax（1.48±0.58）hand （1.38±0.56）h, Cmax （1. 86 ± 0. 50） mg/L and （2.07± 0.62） mg/L, AUC0-12 （7.51 ±1.71） mg · h/L and 7.03 ± 0.98 mg·h/L for test and reference drug, respectively. The relative bioavailability of the test drug was 98.0% ± 11.8%. Conclusions Statistical analysis shows that the two preparations were bioequivalent.