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目的:考察国产奥卡西平片的人体相对生物利用度和生物等效性。方法:20名健康男性志愿者,分别随机交叉单剂量口服奥卡西平试验药和对照药0.3 g。用高效液相色谱法测定血浆中奥卡西平的活性代谢产物10-羟基卡马西平(MHD)的浓度,用DAS2.0软件计算药动学参数并进行生物等效性评价。结果:MHD的线性范围为0.1～10.0μg·ml~(-1),定量下限为0.1μg·ml~(-1)。20名健康志愿者单剂量口服试验药和对照药后,MHD的C_(max)分别为(4.32±0.40)μg·ml~(-1)和(4.59±0.94)μg·ml~(-1);t_(max)分别为(4.54±0.70)h和(4.33±0.77)h;t_(1/2)分别为(14.53±4.34)h和(15.25±3.21)h;AUC_(0～72)分别为(76.23±15.09)μg·ml~(-1)·h和(75.29±13.14)μg·ml~(-1)·h。试验制剂与参比制剂的相对生物利用度F=(105.6±19.1)%。两者AUC_(0～72),C_(max),t_(max)差异均无统计学意义。结论:两种制剂生物学等效。
OBJECTIVE: To investigate the relative bioavailability and bioequivalence of oxcarbazepine tablets in China. Methods: Twenty healthy male volunteers were randomized to receive a single oral dose of oxcarbazepine 0.3 g. The concentration of 10-hydroxycarbamazepine (MHD), the active metabolite of oxcarbazepine in plasma, was determined by HPLC. The pharmacokinetic parameters were calculated by DAS2.0 software and bioequivalence was evaluated. Results: The linear range of MHD was 0.1 ~ 10.0μg · ml ~ (-1) and the limit of quantification was 0.1μg · ml ~ (-1). The Cmax of MHD were (4.32 ± 0.40) μg · ml -1 and (4.59 ± 0.94) μg · ml -1 in 20 healthy volunteers after a single oral dose of test drug and control drug respectively. ; t_ (max) were (4.54 ± 0.70) h and (4.33 ± 0.77) h respectively; t 1/2 was (14.53 ± 4.34) h and (15.25 ± 3.21) h respectively; AUC_ (0 ~ 72) (76.23 ± 15.09) μg · ml -1 · h and (75.29 ± 13.14) μg · ml -1 · h, respectively. The relative bioavailability of the test formulation to the reference formulation was F = (105.6 ± 19.1)%. There was no significant difference between AUC_ (0 ~ 72), C_ (max), t_ (max). Conclusion: Both preparations are bioequivalent.