盐酸伐昔洛韦缓释片家犬药动学研究  

Pharmacokinetics of valaciclovir HCl sustained release tablets in dogs

作　　者：许小红[1] 李铜铃[1] 王玮[1] 李莉[1] 孙健[1] 

机构地区：[1]四川大学华西药学院,成都610041

出　　处：《中国新药杂志》2004年第5期414-416,共3页Chinese Journal of New Drugs

摘　　要：目的:研究盐酸伐昔洛韦缓释片(HVSRT)与盐酸伐昔洛韦片(HVT)在家犬体内药动学,为人体生物利用度研究提供依据和参考。方法:以市售HVT为参比制剂,采用反相高效液相色谱法测定血浆中阿昔洛韦浓度,按单剂量、多剂量给药方案研究并计算药动学参数。结果:HVRST与HVT单剂量给药后,血浆中阿昔洛韦的Tmax分别为(3.5±1.1)和(2.3±1.4)h,Cmax分别为(3.81±1.46)和(4.24±1.51)μg·mL-1,MRT分别为(5.4±1.6)和(4.6±0.8)h,AUC0-(?)分别为(25.53±8.96)和(26.22±8.92)μg·h·mL-1,AUC0-∞分别为(29.42±7.15)和(29.41±1.89)μg·h·mL-1,HVSRT相对生物利用度F(0-Tn)为(97.02±12.54)%。HVRST和HVT多剂量给药达稳态后,血浆中阿昔洛韦的Cmax分别为(4.51±0.91)和(7.07±2.36)μg·mL-1,Cmin分别为(1.20±0.32)和(0.58±0.15)μg·mL-1,FI分别为(135.2±14.3)%和(481.3±101.3)%。结论:HVSRT与HVT生物等效,且HVRST具有明显的缓释特征,能持久地维持比HVT更平稳的血药浓度。Objective:To study the pharmacokinetics of VHSRT (valaciclovir HCl sustained re-lease tablets) in dogs. Methods: VHT (valaciclovir HCl talets) available from market was adopted as reference preparation in the self-control, randomized and crossover study. RP-HPLC was adopted to measure the plasma level of aciclovir and the pharmacokinetic parameters were calculated based on single oral dose and multi-oral dose regimen.Results:Pharmacokinetic parameters of plasma aciclovir calculated based on single oral dose for VHSRT and VHT were respectively:Tmax=(3.5±1.1) and (2.3±1.4)h;Cmax=(3.81±1.46) and (4.24±1.51)μg·mL-1;MRT=(5.4±1.6) and (4.6±0.8)h; AUC0-t=(25.53±8.96) and (26.22±8.92)μg·h·mL-1;AUC0-∞= (29.42±7.15) and (29,41±1. 89)μg·h·mL-1. The bioavailability for VHSRT F(0--Tn) was (97.02±12.54) % . Pharmacokinetic parameters of plasma aciclovir calculated based on multi-oral doses for VHSRT and VHT were respectively: Cmax= (4.51±0.91) and(7.07±2.36)μg·mL-1;Cmin=(1.20±0.32) and (0.58±0. 15)μg·mL-1 and FI= (135.2±14.3)% and (481. 3±101. 3)% . Conclusion: VHSRT and VHT are bioequivalent and VHSRT shows a significant sustained release property in dogs.

关 键 词：盐酸伐昔洛韦 缓释片 反相高效液相色谱 生物利用度 

分 类 号：R969.1[医药卫生—药理学] R978.7[医药卫生—药学]