盐酸伐昔洛韦片人体相对生物利用度和生物等效性研究

目的:研究2种盐酸伐昔洛韦片的药动学,评价二者的生物等效性。方法:按照两制剂双周期随机交叉试验设计。18名男性健康志愿者随机分为2组,分别单剂量口服受试制剂与参比制剂后应用HPLC法测定血浆中阿昔洛韦浓度,利用3p97程序计算药动学参数及评价二者生物等效性。结果:单剂量口服300mg盐酸伐昔洛韦受试制剂和参比制剂后,测得阿昔洛韦AUC0～24分别为(12·85±4·32)、(12·19±4·63)μg·h·mL-1,AUC0～∞分别为(14·65±5·75)、(13·27±5·03)μg·h·mL-1,Cmax分别为(3·55±0·92)、(3·71±0·97)μg·mL-1,tmax分别为(1·44±0·43)、(1·33±0·37)h,t1/2分别为(6·23±2·81)、(4·55±1·84)h。受试制剂相对生物利用度为(111·01±23·52)%。结论:受试制剂与参比制剂具有生物等效性。

Relative Bioavailability and Bioequivalence of Valaciclovir Hydrochloride Tablets in Healthy Volunteers

OBJECTIVE:To study the pharmacokinetics and relative bioavailability of two kinds of preparations of valaciclovir hydrochloride.METHODS:This was a randomized two-way cross-over study.A total of 18 healthy volunteers were randomly assigned to receive single oral dose of test valaciclovir tablets(trial group) or reference valaciclovir tablets(control group),with the plasma aciclovir concentrations determined by HPLC,the pharmacokinetics parameters calculated and the relative bioavailability evaluated using 3p97 program.RESULTS:The main pharmacokinetic parameters test and reference valaciclovir hydrochloride tablets were as follows:AUC0～ 24:(12.85± 4.32) vs.(12.19± 4.63) μg· h· mL-1;AUC0～ ∞:(14.65± 5.75) vs.(13.27± 5.03) μg· h· mL-1;Cmax:(3.55± 0.92) vs.(3.71± 0.97) μg· mL-1;tmax:(1.44± 0.43) h vs.(1.33± 0.37) h;t1/2:(6.23± 2.81) h and(4.55± 1.84) h.The relative bioavailability of the test valaciclovir tablets were(111.01± 23.52) %.CONCLUSION:The reference valaciclovir tablets and the test valaciclovir tablets were bioequivalent.