苯扎贝特缓释片在犬体内的药动学  

Pharmacokinetics of bezafibrate sustained-release tablets in dogs

作　　者：李昂[1,2] 褚扬[2] 王相阳[2] 万梅绪[2] 马晓慧[2] 赵锦花[2] 郭治昕[1,2] 闫希军[1,2] 

机构地区：[1]天津中医药大学,天津300193 [2]天津天士力研究院,天津300410

出　　处：《中国医院药学杂志》2011年第5期348-351,共4页Chinese Journal of Hospital Pharmacy

基　　金：国家科技重大新药创制专项资助项目(编号:2008ZX09401-006)

摘　　要：目的:研究单剂量和多剂量口服苯扎贝特缓释片在Beagle犬体内的药动学特征。方法:4只Beagle犬单剂量和多剂量口服苯扎贝特缓释片后,不同时间点采集血样。采用高效液相色谱法测定其血药浓度,应用Topfit2.0软件计算其主要药动学参数。结果:苯扎贝特缓释片给药后主要药动学参数如下:单剂量Cmax为(19.8±6.7)mg.L-1,tmax为(2.3±0.8)h,AUC0-τ为(80.0±35.8)mg.h.L-1,t1/2为(8.5±1.5)h;多剂量Cmax为(21.5±6.0)mg.L-1,tmax为(2.8±1.1)h,AUC0-τ为(114.3±63.0)mg.h.L-1,t1/2为(8.8±4.5)h。结论:本法灵敏度高,简便,分析速度快,专属性强,可用于犬血浆中苯扎贝特的测定。苯扎贝特缓释片口服给药符合二房室模型,多次给药无明显蓄积现象。OBJECTIVE To investigate the pharmacokinetics of bezafibrate sustained-release tablets in beagle dogs after single-dose and multi-dose oral administration. METHODS Blood samples were collected at a series of time point after single-dose and multi-dose oral administration of bezafibrate sustained-release tablets to four Beagle dogs, then bezafibrate concentrations were determined by HPLC and the main pharmacokinetic parameters were calculated using Top/it 2. 0 pharmacokinetic software. RESULTS The pharmacokinetie parameters of single-dose were as follows： the Cmax was （19. 8 ± 6. 7） mg· L^-1, tmax was （2. 3 ± 0. 8） h, AUC0-τ, was （80. 0 ± 35.8） mg·h·L ^-1, t1/2 was （8. 5 ± 1.5） h, respectively; The parameters after multi-dose： Cmax was （21.5 ± 6. 0） mg·L^-1, tmax was （2. 8 ± 1. 1 ） h, AUC0-τ was （ 114. 3 ±63.0） mg· h · L^- 1, h/2 was （8.8 ± 4. 5 ） h, respectively. CONCLUSION This method is highly sensitive, rapid, simple and specific enough for determining the concentrations of bezafibrate in dog plasma. The pharmacokinetic results show that bezafibrate sustained-release tablets are fitted to two- compartment model. There is no accumulation of bezafibrate after multi-doses in Beagle dogs.

关 键 词：苯扎贝特缓释片 药动学 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学]