【摘要】 目的 :研究阿司匹林缓释片健康人体的药物动力学及相对生物利用度。方法 :以阿司匹林肠溶片为标准参比制剂 ,12名健康男性受试者 ,分别进行单剂量和多剂量用药试验 ,均采用随机交叉口服单剂量 (15 0mg)和多剂量 (15 0mg ,qd× 5 )阿司匹林缓释片和肠溶片 ,HPLC法测定用药后不同时间血浆中水杨酸浓度 ,用 3P87软件处理药 时数据。结果 :单剂量用药后 ,两制剂的体内过程均符合一房室开放模型 ,血药浓度分别在用药后 (5 .5± 0 .5 )h和 (5 .4± 0 .8)h达峰值 (3.8± 0 .4)mg·L-1和(9 .5± 1.8)mg·L-1,药 时曲线下面积 (AUC0→∞)分别为 (6 6 .5± 12 .6 )mg·L-1和 (6 4.5± 8.9)mg·h·L-1,缓释片的相对生物利用度为 (10 3.5± 12 .3) % ;多剂量用药血药浓度达稳态后 ,峰浓度 (Cmax)分别为 (3.8± 0 .5 )mg·L-1和 (9.7± 1.5 )mg·L-1,谷浓度 (Cmin)分别为 (1.2 5± 0 .2 7)mg·L-1和 (0 .49± 0 .2 5 )mg·L-1。两者血药浓度波动系数FI分别为 0 .86± 0 .2 3和 1.73±0 .16。结论 :阿司匹林缓释片在健康人体内具有明显的缓释特征。更多还原

【Abstract】 OBJECTIVE:To study the pharmacokinetics and relative bioavailability of aspirin sustaried release tablets in health volunteers.METHODS:Twelve male health volunteers orally took a single and multiple doses of the tablets and enteric coating tablets in an open randomized crossover study.Plasma concentrations of salicylic acid were tested by HPLC.RESULTS:The plasma concentration time curves of these two drugs appeared to fit oral first order absorption and one compartment open model after a single oral dose.The peak levels in plasma averaged ( 3.8 ± 0.4 ) and ( 9.5 ± 1.8 )mg·L -1 at ( 5.5 ± 0.5 ) and ( 5.4 ± 0.8 )h and the AUC were ( 66.5 ± 12.5 ) and ( 64.5 ± 8.9 )mg·h·L -1 ,respectively.The relative bioavailabilety of sustarned realease tablets was ( 103.5 ± 12.3 )%.Following multiple dosing mean steady state, C max values were ( 3.8 ± 0.5 ) and ( 9.7 ± 1.5 )mg·h·L -1 and C min were ( 1.25 ± 0.27 )mg·L -1 and ( 0.49 ± 0.25 )mg·L -1 ,respectively.The peak to through fluctuation index(FI) for the two formulations were 0.86 ± 0.23 and 1.73 ± 0.16 respectively.CONCLUSIONS:The sustarned release tablets had an obvious slow release characteristics. [更多还原