盐酸伐昔洛韦片的人体相对生物利用度及生物等效性

The relative bioavailability and bioequivalence of valaciclovir hydrochloride tablets in healthy volunteers

目的：研究盐酸伐昔洛韦片的人体相对生物利用度和生物等效性。方法：健康志愿者20名，随机双交叉单剂量口服2种制剂的盐酸伐昔洛韦片，剂量分别为0．3g，剂间间隔为1周。分别于服药后14h内多点抽取静脉血；用高效液相色谱（HPLC）法测定血浆中阿昔洛韦的浓度。用DAS软件计算人体相对生物利用度并评价两种制剂生物等效性。结果：单剂量口服盐酸伐昔洛韦试验制剂和参比制剂后血浆阿昔洛韦的Gmax分别为（2．75±0．68）μg／ml和（2．68±0．82）μg／ml；tmax分别为（1．44±0．67）h和（1．46±0．77）h；AUC（0～14）分别为（9．53±2．00）μg／（h·ml）和（9．58±1．87）μg／（h·ml）；AUG0～inf）分别为（9．94±2．22）μg／（h·ml）和（10．12±1．92）μg／（h·ml）。AuC（0～14）的90％可信区间为94．1％～104．3％，AUC（0～inf）的90％可信区间为93．0％～102．8％，Cmax的90％可信区间为95．7％～113．9％。结论：试验制剂与参比制剂的人体相对生物利用度为（100．4±17．0）％，2种制剂具有生物等效性。

Objective：To study the relative bioavailability and bioequivalence of valaciclovir hydrochloride tablets in healthy volunteers. Methods ： A single oral dose of 0.3 g valaciclovir hydrochloride test and reference formulations were given to 20 healthy volunteers according to a randomized crossover design with an alternative interval in one week. Venous blood sampling was conducted consequently within 14 hours for detecting plasma acyclovir concentration with high performance liquid chromatography （HPLC）. The pharmacokinetics parameter was calculated completely and the bioavailability and bioequivalence of two formulations were evaluated by DAS program. Results ： After a single dose of acyclovir hydrochloride of test and reference formulations, the pharmacokinetics parameters for acyclovir were as follows： Cmax was（2. 75 ± 0.68）μg/ml and （2.68 ± 0.82）μg/ml; tmax was （1.44±0.67）h and （1.46 ± 0.77）h; AUC（0-14） was （9.53 ± 2.00） μg/（h· ml） and （9.58± 1.87）μg/（h·ml）; AUC（0-inf） was（9.94 ± 2. 11）μg/（h·ml） and（ 10.12 ± 1.92）μg/（h· ml） for test and reference formulations, respectively. The 90% confidential interval of AUC（0-14） of tested formulation was 94.1% - 104.3% while the 90% of that of AUC（0-inf） was 93.0 % - 102.8 %, and 95.7 % - 113.9 % for Cmax. Conclusion ： The relative bioavailability of test formulation to reference formulation was （100.4 ± 17.0）%, which suggests there is bioequivalence of the two agents.