摘要
目的：研究盐酸伐昔洛韦片在健康人体的药代动力学和相对生物利用度，为临床合理用药提供依据．方法：采用双周期、单中心、开放、自身交叉对照的研究方法，18例健康志愿者随机分为两组，单次，交叉口服盐酸伐昔洛韦片600mg后，以HPLC法测定血浆中阿昔洛韦的浓度，采用BAPP2．0软件进行数据处理，计算药代动力学参数．结果：HPLC法测定阿昔洛韦的线性范围为0．1～4．0μg/mL（r=0．9999），日内和日间RSD均小于7．00％．试验与参比制剂的药时曲线可用一室模型拟合，两者主要药代动力学参数Tmax分别为（1．50±0．40），（1．40±0．40）h；Cmax分另4为（2．70±0．68），（2．87±0．75）μg／mL．t1/2分别为（3．00±0．65），（3．28±0．67）h；AUC0-14分别为（9．07±2．43），（9．71±2．70）μg·h／mL．两种盐酸伐昔洛韦片主要药动学参数间均无显著性差异（P〉0．05）．供试制剂对参比制剂的相对生物利用度为（96．4±23．7）％．结论：供试制剂和参比制剂具有生物等效性．
AIM： To study the pharmacokinetics and relative bioavailability of valaciclovir hydrochloride tablets and evaluate its bioequivalence. METHODS： A single oral dose 600 mg of 2 valaciclovir hydrochloride tablets was given to 18 healthy volunteers in an open randomized crossover study. The concentration of acyclovir in plasma was determined by HPLC at different time points within 14 h following administration. The pharmacokinetic parameters were calculated by BAPP 2.0 software and the bioequivalence was evaluated by two one-sided t test and 90% confidence intervals. RESULTS： The calibration curve of acyclovir was linear in the range of 0.1 - 4.0 μg/mL （ r = 0. 9999 ） , and an intra-day and inter-day RSD of 〈 7.00% was observed. The concentration-time curve after administration was best fitted to a one compartment open model, and main pharmacokinetic parameters were as follows ： Tmax were （ 1.50 ± 0.40 ） and （ 1.40 ±0.40） h; Cmax were （2.70±0.68） and （2.87±0.75） μg/ mL; t1/2 were （3.00±0.65） and （3.28±0.67） h; AUC0 -14 were 9.07 ± 2.43 and 9.71±2.70μg ·h/mL. The relative bioavailability of the test preparations compared with the reference preparations was （ 96.4±23.7 ） %. There was no statistically singnificant difference in parameters Tax, t1/2, Tmax MRT, AUC0-14 and AUC0-14 between the 2 products （P 〉 0. 05）. CONCLUSION： The 2 valaciclovir hydrochloride tablets were bioequivalent.
出处
《第四军医大学学报》
北大核心
2006年第18期1726-1728,共3页
Journal of the Fourth Military Medical University
关键词
盐酸伐昔洛韦片
阿昔洛韦
色谱法
高压液相
药代动力学
生物利用度
valaciclovir hydrochlofide tablet
acyclovir
chromatography, high pressure liquid
pharmacokinetics
biological availability
