盐酸伐昔洛韦片的药动学及相对生物利用度

Pharmacokinetics and relative bioavailability study of valaciclovir hydrochloride tablets in Chinese healthy volunteers

目的:研究盐酸伐昔洛韦片在健康人体的药动学和相对生物利用度。方法:采用两制剂双周期交叉对照的研究方法,以HPLC法测定18例健康志愿者单剂量口服盐酸伐昔洛韦片600mg后血浆中阿昔洛韦的浓度变化,采用DAS2.0软件计算药动学参数。结果:阿昔洛韦的线性范围为0.201～12.884mg.L-1(r=0.9999),日内和日间RSD均小于6.0%。供试制剂与参比制剂的主要药动学参数tmax分别为(1.5±0.6)h和(1.9±0.7)h;Cmax分别为(2.7±0.5)mg.L-1和(2.8±0.7)mg.L-1;t1/2分别为(3.0±0.6)h和(3.3±0.9)h;AUC0-t分别为(10.6±1.9).和(10.6±2.4)mg.L-1.h;AUC0-∞分别为(11.5±2.0)mg.L-1.h-1和(11.7±2.6)mg.L-1.h。两种盐酸伐昔洛韦片主要药动学参数间差异均无显著性(P>0.05)。供试制剂对参比制剂的相对生物利用度为(101.9±14.9)%。结论:供试制剂和参比制剂具有生物等效性。

OBJECTIVE To study the pharmacokinetics and relative bioavailability of valaciclovir hydrochloride tablets and evaluate its bioequivalence. METItODS A single oral dose 600 mg of valaciclovir hydrochloride tablets was given to 18 healthy volunteers in an open randomized cross over study. The concentration of aciclovir in plasma was determined by HPLC. The pharmacokinetic parameters were calculated by DAS 2. 0 software. RESULTS The calibration curve of aciclovir was linear in the range of 0. 201-12. 884 mg·L^-1 （r= 0. 999 9） ,and an intra-day and inter-day RSD of 〈6. 0% was observed. The main pharmacokinetic parameters were as follows：tmax were （1. 5±0. 6） and （1.9±0. 7） h;Cmax were （2. 7 ± 0.5） and （2. 8 ± 0. 7） mg·L^-1 ,t1/2 were （3.0 ±0. 6） and （3.3 ± 0. 9） h; AUG0-t were （10.6 ±1.9） and （10.6 ± 2. 4） mg· L^-1 · h. The relative bioavailability of the test preparations compared with the reference preparations was （101.9 ± 14. 9）%. There was no statistically significant difference in parameters tmax,t1/2,C AUG0-t and AUG0-∞ between the two products （P〉0. 05）. CONCLUSION The two valaciclovir hydrochloride tablets are bioequivalent.