口服国产及进口盐酸特比萘芬片的药动学

Study on pharmacokinetics of domestic and imported terbinafine tablets

目的:研究盐酸特比萘芬片剂国产与进口产品在健康志愿者体内的药动学。方法:男性健康受试者10 名,随机分成二组,采用单剂量双周期交叉试验设计,分别口服国产及进口特比萘芬片剂,以高效液相色谱法测定其血药浓度。结果:结果国产及进口特比萘芬的AUC0→T分别为(10.8±1.0),(11.6±1.9)mg·L-1·h;AUC0→∞分别为(15.0±2.1),(15.6±3.4) mg·L-1·h;Cmax为(1.8±0.4),(1.9±0.7) mg·L-1,Tmax为(2.0±0.9),(2.3±1.1) h、Ke分别为(0.047±0.017),(0.058±0.026)h-1;t1/2 分别为(16.9±7.5),(15.6±9.4)h;国产特比萘芬的相对生物利用度为AUC0→T为(94.3±10.3)%,AUC0→∞(99.5±22.1)%。结论:经方差、双单侧及90%可信限区间法统计分析表明,盐酸特比萘芬片剂国产与进口产品在健康志愿者体内的药动学参数(AUC、Cmax)差异无显著性。

OBJECTIVE To study the pharmacokinetics of terbinafine tablets in healthy volunteers. METHODS Ten male volunteers were administrated with domestic and imported terbinafine tablets 500 mg respectively in random crossover study. Plasma concentration was detected by reverse-phase HPLC. RESULTS The pharmacokinetics parameters of domestic terbinafine and imported terbinafine were as follows: AUC_ 0→T =( 10.8 ± 1.0 ) mg · L -1 ·h and ( 11.6 ± 1.9 ) mg · L -1 ·h;AUC_ 0→∞ =( 15.0 ± 2.1 ) mg · L -1 ·h and ( 15.6 ± 3.4 ) mg · L -1 ·h; C _ max =( 1.8 ± 0.4 ) mg · L -1 and ( 1.9 ± 0.7 ) mg · L -1 、 T _ max =( 2.0 ± 0.9 ) h and ( 2.3 ± 1.1 ) h; K _e=( 0.047 ± 0.017 )h -1 、( 0.058 ± 0.026 )h \{-1\}、 t _ 1/2 =( 16.9 ± 7.5 ) h and ( 15.6 ± 9.4 ) h. The relative bioavailability of domestic terbinafine tablets was ( 94.3 ± 10.3 ) % ( AUC_ 0→T ) and ( 99.5 ± 22.1 ) % ( AUC_ 0→∞ ). CONCLUSION The pharmacokinetic parameters(AUC、 C _ max ) of domestic terbinafine tablets and imported terbinafine tablets were of no statistical difference.