盐酸伐昔洛韦片的人体药动学及生物等效性研究

Studies on Pharmacokinetics and Bioequivalence of Valaciclovir Hydrochloride Tablets

目的:研究单剂量口服盐酸伐昔洛韦片的药动学特征,并评价2种制剂的生物等效性。方法:采用双周期交叉试验方法,18名健康志愿者分别单剂量口服2种盐酸伐昔洛韦片600mg,采用高效液相色谱法测定血浆中药物浓度,计算药动学参数,并进行统计分析。结果:盐酸伐昔洛韦片受试制剂与参比制剂的主要药动学参数tmax分别为(1.69±0.25)、(1.72±0.26)h,Cmax分别为(3.34±0.58)、(3.40±0.49)μg·mL-1,t1/2分别为(2.73±0.31)、(2.97±0.33)h,AUC0～14分别为(11.22±2.21)、(11.12±1.90)μg·h·mL-1,AUC0～∞分别为(11.76±2.15)、(11.61±1.86)μg·h·mL-1。受试制剂相对于参比制剂的生物利用度为(101.06±11.72)%。结论:2种制剂具有生物等效性。

OBJECTIVE： To study pharmacokinetics of valacielovir hydrochloride tablets and to evaluate the bioequivalence of test and reference tablets. METHODS： In a two-period cross-over design test, 18 healthy volunteers were given a single oral dose of 600 mg test valaciclovir hydrochloride and 600 mg reference formulations respectively. Plasma concentrations of acyclovir were determined by HPLC method. The pharmacokinetic parameters of the two formulations were calculated and analyzed statistically. RESULTS： The main pharmacokinetic parameters of test vs. reference valacyclovir hydrochloride tablets were as follows： tmax （1.69 ±0.25）h vs. （1.72 ± 0.26）h, Cmax（3.34±0.58） μg·mL^-1 vs. （3.40 ＋±0.49）μg·mL^-1, t1/2（2.73 ± 0.31）h vs. （2.97 ± 0.33）h, AUC0-14 （11.22±2.21） μg·h·mL^-1 vs. （11.12±1.90）μg·h·mL^-1, AUC0-∞（11.76±2.15）μg·h·mL^-1 vs. （11.61 ± 1.86）μg·h·mL^-1, respectively. As compared with reference formulation, the relative bioavailability of test formulation was （101.06± 11.72）%. CONCLU- SION： The two preparations are bioequivalent.