摘要
目的 :研究富马酸酮替芬分散片在健康人体的药代动力学特征及其生物等效性评价 .方法 :12名健康志愿受试者 ,采用标准二阶段交叉设计试验方法 ,分别单剂量po富马酸酮替芬分散片 (受试品 )和富马酸酮替芬片 (参比品 ) 2mg,以液相色谱 质谱 质谱联用法测定服药后 36h内不同时刻的血药浓度 ,计算主要药动学参数 ,并采用双单侧t检验和 90 %置信区间进行生物等效性评价 .结果 :受试者分别po受试品和参比品后 ,两者主要药动学参数tmax,cmax,t1/ 2 和AUC(0 -3 6h) 分别为 :(2 .7± 1.2 )和 (3.1± 1.4 )h;(4 0 7± 14 7)和(389± 16 8)ng/L ;(5 .5± 1.6 )和 (5 .7± 2 .6 )h ;(2 90 0± 10 4 3)和(2 76 3± 977)ng/(h·L) ,受试品的相对生物利用度为 (112±39) % .结论 :富马酸酮替芬分散片和普通片剂相比 ,具有吸收快、生物利用度较高的优点 ;统计学结果表明 ,两种制剂具有生物等效性 (P <0 .0 5 ) .
AIM: To investigate the pharmacokinetics and bioequivalence of ketotifen fumarate in healthy volunteers. METHODS: A single oral dose of the tested and control ketotifen fumarate was given respectively to 12 healthy volunteers in a randomized two-period crossover study. The serum concentration of the two drugs was determined at different time points within 36 hours following the administration by liquid chromatographic-mass spectrometric. The main pharmacokinetics parameters were calculated and the bioequivalence was evaluated by two one-side t test and 90% confidence intervals. RESULTS: The main pharmacokinetics parameters were t max : (2.7±1.2) and (3.1±1.4)h, c max : (407±147)and(389±168)ng/L, t 1/2 :(5.5±1.6)and(5.7±2.6)h, and AUC:(2900±1043)and(2763±977) ng/(h·L). The relative bioavailability of the tested drug was (112±39)%. CONCLUSION: Compared with the control, tested ketotifen fumarate has the advantages of faster absorption and higher bioavailability. The results of statistical analysis indicate that the two drugs are bioequivalent in healthy volunteers (P<0.05).
出处
《第四军医大学学报》
北大核心
2004年第18期1670-1672,共3页
Journal of the Fourth Military Medical University
关键词
富马酸酮替芬
色谱法
液相
光谱分析
质理
药代动力学
生物利用度
ketotifen fumarate
chromatography, liquid
spectrum analysis, mass
Pharmacokinetics
biological availalility
