国产与进口替扎尼定片人体药动学和相对生物利用度比较

目的 :比较国产与进口替扎尼定片在正常人体内的药动学与相对生物利用度。方法 :18名男性志愿者随机交叉单次口服国产或进口替扎尼定片4mg后 ,采用高效液相色谱 (HPLC)法测定血药浓度 ,用 3p97软件包计算两者的药动学参数与相对生物利用度。结果 :国产片和进口片口服吸收的药 时曲线符合一房室模型。Tmax分别为 (1.3±s 0 .5 )h和 (1.2± 0 .4 )h ;Cmax 分别为 (10± 7) μg·L- 1和(10± 6 ) μg·L- 1;AUC0 10 分别为 (16± 11) μg·h·L- 1和 (17± 12 ) μg·h·L- 1;T12 β分别为 (1.1± 0 .6 )h和 (0 .9± 0 .4 )h。国产片相对于进口片的生物利用度为 (94± 14 ) % ,经配对t检验、方差分析、双单侧t检验及 (1 2α)置信区间法统计分析 ,各药动学参数无显著差异 (P >0 .0 5 )。结论 :国产片与进口片生物等效。

Pharmacokinetics and relative bioavailability of domestic vs imported tizanidine tablets in human body

AIM: To compare pharmacokinetics and the relative bioavailability of domestic and imported tizanidine(TZND) tablets in normal human body. METHODS: A single oral domestic TZND tablet or imported tablet 4 mg was given to 18 healthy male volunteers in randomized self-crossover study. Plasma concentration of tizanidine was measured by high performance liquid chromatography. The pharmacokinetic parameters as well as relative bioavailability were measured by 3p97. RESULTS: The concentration-time curves of domestic TZND tablet and imported TZND tablet conformed to one compartment open model. The T _ max were (1.3± s 0.5) h and (1.2±0.4) h, C _ max (10±7)μg·L -1 and (10±6)μg·L -1, AUC_ 0-10 (16±11)μg·h·L -1 and (17±12)μg·h·L -1, T _ 12β (1.1±0.6) h and (0.9±0.4) h,respectively. There was no significant difference between the two kinds of tablets in the T _ max, C _ max,AUC_ 0-t, T _ 12β . The relative bioavailability of domestic TZND tablets was (94±14)% compared with imported TZND tablet. CONCLUSION: The results of the statistical analysis shows that the two kinds of tablets are bioequivalent.