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目的 :研究硫酸沙丁胺醇控释小丸胶囊和进口控释片及普通片在健康志愿者体内单剂量和多剂量给药后的药代动力学和生物利用度。方法 :8名健康男性志愿者自身随机交叉先后po 8mg受试硫酸沙丁胺醇控释小丸胶囊、沙丁胺醇控释片 (Volmax)或沙丁胺醇普通片 (Ventolin) ,观察其药代动力学和相对生物利用度。另 2 0名受试者自身随机交叉po受试胶囊 ( 8mg ,bid)和Volmax( 8mg ,bid) ,连服 5d ,观察峰谷波动率。用高效液相色谱法测定血药浓度。结果 :单剂量给药后Tmax分别为 ( 4.5± 0 .8)、( 5.0± 1 .5)、( 1 .8± 0 .7)h ;Cmax分别为 ( 1 4 .6± 5.5)、( 1 5.0±3 .8)、( 3 1 .0± 7.5)ng/ml;AUC0～∞ 分别为 ( 1 3 7.4± 3 1 .8)、( 1 3 9.3± 3 1 .4 )、( 1 89.2± 3 1 .3 )ng/ml·h ;MRT分别为( 1 0 .5± 0 .8)、( 1 0 .8± 1 .0 )、( 7.4± 0 .8)h。多剂量给药后第 5天的Tmax分别为 ( 5.5± 0 .8)、( 5.8± 1 .3 )h ;Cmax分别为 ( 1 4 .2± 2 .1 7)、( 1 5.2± 2 .81 )ng/ml;Cmin分别为 ( 7.7± 0 .9)、( 7.8± 1 .1 )ng/ml;AUC0～Tn分别为 ( 1 2 6.5± 1 9.9)、( 1 3 2 .3± 2 2 .1 )ng/ml·h ;峰谷波动率分别为 ( 0 .61± 0 .2 )、( 0 .66± 0 .2 )。结论 :受试胶囊相对于Ventolin和Volmax的生物利用度?
OBJECTIVE: To study the pharmacokinetics and bioavailability of salbutamol sulfate controlled release pellets, imported controlled release tablets and common tablets in healthy volunteers after single and multiple dose administration. Methods: Eight healthy male volunteers were randomized to randomize their own po 8mg salbutamol controlled release pellet capsules, albuterol controlled release tablets (Volmax) or salbutamol ordinary tablets (Ventolin) to observe the pharmacokinetics and relative bioavailability. Another 20 subjects randomized their own crossover po capsules (8mg, bid) and Volmax (8mg, bid), and even served 5d, observing the volatility of the peak. Determination of plasma concentration by high performance liquid chromatography. RESULTS: The Tmax of single dose group were (4.5 ± 0.8) days, (5.0 ± 1.5 days) and (1.8 ± 0.7 months) respectively; Cmax was (14.6 ± 5.5) 1 5.0 ± 3 .8) and (31.0 ± 7.5) ng / ml respectively; AUC0 ~ ∞ were (1 3 7.4 ± 3 1 .8), (1 3 9.3 ± 3 1 .4), (1 89.2 ± 3 1 .3) ng / ml · h; MRT were (1 0 .5 ± 0 .8), (1 0 .8 ± 1 .0), (7.4 ± 0. The Tmax of the 5th day after the multi-dose administration were (5.5 ± 0.8) days and (5.8 ± 1.3 days) respectively. The Cmax values were (14.2 ± 2.17) and (15.2 ± 2. 81) ng / ml; Cmin were (7.7 ± 0.9) and (7.8 ± 1.1) ng / ml respectively; AUC0 ~ Tn were (1 2 6.5 ± 1 9.9), (1 3 2 3 ± 2 2 .1) ng / ml · h; peak to valley fluctuations were (0.61 ± 0.2), (0.66 ± 0.2). Conclusion: The bioavailability of test capsules relative to Ventolin and Volmax?