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目的在中国健康成年男性志愿者中比较研究国产和进口佐米曲坦片剂的药动学参数,评估两者的生物等效性。方法24名健康男性受试者随机交叉给药,分别单剂口服国产和进口佐米曲坦片7.5mg。以HPLC测定血药浓度,应用3P97软件计算两者的药动学参数并考察其生物等效性。结果受试者按自身前后交叉设计分别应用国产片剂(试验制剂)和进口片剂(参比制剂)7.5mg后,药-时曲线符合一房室模型,主要药动学参数:tmax分别为(2.48±0.40)和(2.50±0.36)h;ρmax分别为(13.22±2.55)和(13.06±3.24)μg.L-1;AUC0-t分别为(59.52±19.99)和(63.60±17.98)μg.h.L-1;t1/2ke分别为(2.16±0.62)和(2.31±0.50)h;国产片剂对于进口片剂的相对生物利用度为(94.8±13.0)%,两种片剂的AUC0-t及ρmax经双向单侧t检验表明,AUC0-t和ρmax90%置信区间分别为89.1%～97.7%和95.1%～104.0%,根据本试验结果,可判定两种制剂生物等效。结论国产与进口佐米曲坦片剂为生物等效制剂。
Objective To compare the pharmacokinetic parameters of domestic and imported zolmitriptan tablets in healthy adult male volunteers in China to evaluate their bioequivalence. Methods Twenty-four healthy male subjects were randomized to receive oral administration of 7.5 mg of domestic and imported Zolmitriptan tablets. The plasma concentration was determined by HPLC. The pharmacokinetic parameters of the two drugs were calculated by 3P97 software and the bioequivalence was evaluated. Results Subjects were designed according to their own cross-sectional design using domestic tablets (test preparation) and imported tablets (reference preparation) 7.5mg, the drug-time curve in line with a ventricular model, the main pharmacokinetic parameters: tmax were (2.48 ± 0.40) and (2.50 ± 0.36) h respectively; ρmax was (13.22 ± 2.55) and (13.06 ± 3.24) μg.L-1, respectively; AUC0-t was (59.52 ± 19.99) and (63.60 ± 17.98) μg (2.16 ± 0.62) and (2.31 ± 0.50) h, respectively. The relative bioavailability of domestic tablets to imported tablets was (94.8 ± 13.0)%. The AUC0- t and ρmax showed that the confidence intervals of AUC0-t and ρmax90% were 89.1% -97.7% and 95.1% -104.0%, respectively. According to the results of this test, the bioequivalence of the two preparations could be judged. Conclusion Domestic and imported zolmitriptan tablets as bioequivalent formulations.