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目的 比较国产和进口盐酸尼卡地平 (Nic)缓释胶囊的药代动力学及生物利用度。方法 选择 12名健康志愿者随机交叉单剂量及多剂量口服两种Nic缓释胶囊 ,采用GC ECD检测 ,内标法定量测定其血药浓度。结果 两种缓释胶囊空腹给药 ,其单剂量及多剂量达稳态后经时血药浓度均呈双峰曲线 ,国产胶囊单剂量给药的主要参数 :Cmax1( 14 2± 8 2 ) μg·L-1,Cmax2 ( 16 9± 5 8) μg·L-1,Tmax1( 0 79±0 45 )h ,Tmax2 ( 5 0 8± 0 79)h ,T1/2Ke( 5 49± 2 5 3)h ,AUC0～ 2 4 ( 97 9± 2 4 8) μg·h·L-1。多剂量给药的主要参数 :Cmax( 36 7± 6 1) μg·L-1,Cmin( 7 3± 1 6 ) μg·L-1,Cav( 18 9± 3 2 ) μg·L-1,FI( 1 5 6± 0 2 6 ) ,AUC0～ 36( 341 4±48 5 ) μg·h·L-1。国产Nic缓释胶囊单剂量及多剂量给药与进口制剂比较的相对生物利用度各为 97 5 %± 19 3 %和98 2 %± 16 5 %。结论 方差分析及双单侧t检验表明 ,两种制剂具有生物等效性
Objective To compare the pharmacokinetics and bioavailability of domestic and imported nicotidine hydrochloride sustained-release capsules. Methods Twelve healthy volunteers were randomized crossover single dose and multiple doses of oral Nicorandil two sustained release capsules, using GC ECD detection, internal standard method for quantitative determination of plasma concentration. Results The fasting plasma concentration of two kinds of sustained-release capsules showed a bimodal curve after single-dose and multi-dose up to steady state. The main parameters of single-dose domestic capsules were: Cmax1 (14 2 ± 8 2) μg · L-1, Cmax2 (16 9 ± 5 8) μg · L-1, Tmax1 (0 79 ± 0 45) h, Tmax2 (58 ± 0 79) h, T1 / 2Ke ) h, AUC0 ~ 2 4 (97 9 ± 2 48) μg · h · L -1. The main parameters of multi-dose administration were Cmax 363 ± 6 1 μg · L-1, Cmin 73 ± 1 6 μg · L-1, Cav 18 9 ± 32 μg · L-1, FI (156 ± 0 2 6), AUC 0 ~ 36 (341 4 ± 48 5) μg · h · L-1. The relative bioavailabilities of domestic Nic sustained-release capsules of single and multiple doses were 97 5% ± 19 3% and 98 2% ± 16 5%, respectively. Conclusions ANOVA and two-sided t-test showed that the two preparations were bioequivalent