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目的 :比较国产和进口单硝酸异山梨酯缓释胶囊的人体药动学和相对生物利用度。方法 :采用单次和多次给药的 4周期双交叉设计 ,气相色谱 电子捕获检测法 (GC ECD)测定 2 2名健康男性志愿者血浆中单硝酸异山梨酯的浓度。结果 :单次 (2 5mg)口服国产和进口单硝酸异山梨酯缓释胶囊后的药动学参数分别为 :Tmax为 (5 .7±s 0 .5 )h和 (5 .8±1 .0 )h ,Cmax为 (2 3 6± 62 ) μg·L-1和 (2 42± 62 )μg·L-1,T1/ 2 为 (8.3± 1 .6)h和 (8.4± 2 .1 )h ,AUC0 3 6为 (3 .7± 0 .9)mg·h·L-1和 (3 .6±0 .9)mg·h·L-1,AUC0 ∞ 为 (4 .0± 0 .9)mg·h·L-1和 (3 .8± 0 .8)mg·h·L-1,平均滞留时间MRT为 (1 1 .5±0 .8)h和 (1 1 .4± 0 .7)h。多次 (2 5mg,6d)口服国产和进口单硝酸异山梨酯缓释胶囊后的稳态药动学参数分别为 :Tmax 为 (5 .2± 0 .7)h和 (5 .4±0 .9)h,Cmax为(3 1 4± 67) μg·L-1和 (3 1 0± 5 8) μg·L-1,Cmin为(63± 1 4) μg·L-1和 (65± 1 6) μg·L-1,稳态血药浓度均值Cav为 (1 87± 3 8) μg·L-1和 (1 83± 3 8) μg·L-1,AUC0 3 6h为 (5 .0± 1 .0 )mg·h·L-1和 (4 .9± 1 .0 )mg·h·L-1,波动度DF为 (1 3 4± 2 0 )%和 (1 3 4± 1 8) %。单次和多次口服国产与进口单硝酸异山梨酯
OBJECTIVE: To compare human pharmacokinetics and relative bioavailability of domestic and imported isosorbide mononitrate sustained-release capsules. Methods: The concentration of isosorbide mononitrate in plasma of 2 2 healthy male volunteers was determined by four-cycle double crossover design and gas chromatography electron capture detection (GC ECD) in single and multiple administrations. Results: The pharmacokinetic parameters of domestic and imported isosorbide mononitrate single oral sustained-release capsules after oral administration (25mg) were as follows: Tmax was (5 .7 ± s 0. 5) h and (5 ± 8) (8 ± 6) μg · L-1 and (42 ± 62) μg · L-1 for Cmax and (8.3 ± 16) h and (8.4 ± 2.1) ) h, AUC0 3 6 was (3.7 ± 0.9) mg · h · L-1 and (3.6 ± 0.9) mg · h · L-1, and AUC0 ∞ was (4.0 ± 0 .9) mg · h · L-1 and (3.8 ± 0.8) mg · h · L-1, respectively. The mean MRT was (11.5 ± 0.8) h and (11.4 ± 0 .7) h. The steady-state pharmacokinetic parameters of domestic and imported isosorbide mononitrate sustained-release capsules after oral administration (25mg, 6d) for several times were as follows: Tmax was (5.2 ± 0.7) h and (5.4 ± 0 .9) h, Cmax was (31.4 ± 67) μg · L-1 and (31 ± 5 8) μg · L-1, and Cmin was 63 ± 14 μg · L- ± 1 6) μg · L-1. The mean plasma concentration of Cav was (1887 ± 38) μg · L-1 and (1883 ± 38) μg · L-1, .0 ± 1 .0) mg · h · L-1 and (4.9 ± 1.0) mg · h · L-1, respectively. The volatility DF was (1 34 ± 2 0)% and ± 1 8)%. Single and multiple oral domestic and imported isosorbide mononitrate