论文部分内容阅读
目的研究健康受试者单次和多次口服阿德福韦酯片后的药动学过程。方法 12名中国男性健康受试者单次po和多次po 10 mg阿德福韦酯片;采用液相色谱-串联质谱联用法(LC-MS/MS)测定阿德福韦酯活性代谢物阿德福韦的血药浓度。用DAS2.0程序计算主要药动学参数,并进行统计分析。结果健康志愿者单次和多次口服阿德福韦酯片10 mg后,阿德福韦的ρmax分别为(24±9)和(24±8)μg.L-1,tmax分别为(1.3±0.7)和(1.5±0.6)h,t1/2分别为(7.4±1.2)和(8.5±2.1)h,AUC0-24h分别为(210±54)和(213±73)μg.h.L-1,AUC0-∞分别为(236±64)和(250±90)μg.h.L-1。多次po阿德福韦酯片后ρsasv为(8.90±3.06)μg.L-1,DF为(2.52±0.66)。结论阿德福韦酯片单次与多次口服的主要药动学参数无显著性差异,体内药物无蓄积现象,耐受性良好。
Objective To study the pharmacokinetics of adefovir dipivoxil tablets in healthy subjects after single or multiple oral administration. Methods 12 Chinese male healthy subjects were treated with single po and multiple po 10 mg adefovir dipivoxil tablets. The active metabolites of adefovir dipivoxil were determined by liquid chromatography-tandem mass spectrometry (LC-MS / MS) Adefovir plasma concentration. The main pharmacokinetic parameters were calculated using the DAS 2.0 program and statistically analyzed. Results After a single or multiple oral administration of adefovir dipivoxil 10 mg in healthy volunteers, the ρmax of adefovir were (24 ± 9) and (24 ± 8) μg.L-1, respectively, with tmax of 1.3 ± 0.7, and 1.5 ± 0.6 h respectively, and the values of t1 / 2 were (7.4 ± 1.2) and (8.5 ± 2.1) h, respectively. The AUC0-24h were (210 ± 54) and , AUC0-∞ were (236 ± 64) and (250 ± 90) μg.hL-1, respectively. After multiple po po adefovir dipivoxil tablets ρsasv was (8.90 ± 3.06) μg.L-1, DF was (2.52 ± 0.66). Conclusions Adefovir dipivoxil tablets have no significant difference in the main pharmacokinetic parameters between single and multiple oral injections. The in vivo drug does not accumulate and is well tolerated.