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目的:比较国产和进口5-单硝酸异山梨醇酯缓释胶囊在健康人体内的药动学。方法:20名志愿者交叉随机分两组,口服50mg,GC-ECD测血药浓度,一室模型拟合或梯形法求药动学参数。结果:多剂量组连续5天服国产或进口胶囊,药动学参数C_(max)分别为(677±103)和(702±76)μg·L~(-1);T_(max)分别为(5.1±2.0)和(5.6±1.3)h;MRT分别为(11.5±0.5)和(11.4±0.7)h;AUC_(0-∞)分别为 (12121±1346)和(12352±988)μg·h·L~(-1),两者差异无显著性(P>0.05)。两种胶囊在服药16h后,血药浓度降至产生耐受性的阈值浓度以下(<300μg·L~(-1))。两种胶囊体内吸收分数和其体外相应时间的溶出率均呈显著正相关(P<0.05),单剂量和多剂量下国产对进口胶囊的相对生物利用度分别为96％±11％和98％±10％。结论:两种胶囊药动学特点相似。
Objective: To compare the pharmacokinetics of domestic and imported 5-isosorbide mononitrate sustained release capsules in healthy volunteers. Methods: Twenty volunteers were randomly divided into two groups: oral administration of 50 mg, GC-ECD blood concentration test, one-compartment model fitting or trapezoidal method for pharmacokinetic parameters. Results: The pharmacokinetic parameters C max were (677 ± 103) and (702 ± 76) μg · L -1, respectively in the multi-dose group for 5 consecutive days. The T max were (5.1 ± 2.0) and (5.6 ± 1.3) h respectively; MRT was (11.5 ± 0.5) and (11.4 ± 0.7) h respectively; AUC 0- ∞ was 12121 ± 1346 and 12352 ± 988 μg · h · L ~ (-1), no significant difference between the two (P> 0.05). After the two kinds of capsules were taken for 16h, the plasma concentration decreased to below the threshold concentration (<300μg · L -1) that produced tolerance. There was a significant positive correlation between the absorption fraction of the two capsules and the dissolution rate in vitro (P <0.05). The relative bioavailability of domestic and imported capsules at single and multiple doses were 96% ± 11% and 98%, respectively ± 10%. Conclusion: The two capsules have similar pharmacokinetic characteristics.