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目的:比较在空腹条件下,国产左乙拉西坦注射液与原研药左乙拉西坦片给药时的药代动力学参数,并观察两者在健康受试者中的安全性与耐受性。方法:利用已经建立的高效液相色谱质谱(HPLC-MS/MS)分析法测定健康受试者两周期给药前后血浆样本中的左乙拉西坦药物浓度。结果:受试者分别静脉注射左乙拉西坦注射液和口服左乙拉西坦片后,左乙拉西坦的主要药代动力学参数如下:t1/2分别为(7.70±0.85)、(7.81±0.88)h;Tmax分别为(0.70±0.10)、(0.90±0.80)h;Cmax分别为(51.64±9.59)、(40.83±9.13)ng/m L;AUC0-t分别为(385.69±65.45)、(394.24±64.68)ng·m L-1·h;AUC0-∞分别为(390.85±66.40)、(400.13±65.89)ng·m L-1·h。以左乙拉西坦片的AUC0-t计算左乙拉西坦注射液平均相对生物利用度为(98.1±9.4)%。试验期间未发生严重程度为重度的不良事件。结论:左乙拉西坦注射液和左乙拉西坦片的药代动力学参数无统计学差异且两种制剂在健康受试者中的安全性较好。
OBJECTIVE: To compare pharmacokinetic parameters of domestic levetiracetam injection with natriuretic tablets before and after fasting, and observe the safety and resistance of both in healthy subjects By sexual. METHODS: The concentration of levetiracetam in plasma samples before and after two-cycle administration in healthy subjects was determined using established HPLC-MS / MS analysis. RESULTS: The main pharmacokinetic parameters of levetiracetam after intravenous levodocis injection and oral levetiracetam tablets were as follows: t1 / 2 = (7.70 ± 0.85), (7.81 ± 0.88) h, Tmax were (0.70 ± 0.10) and (0.90 ± 0.80) h respectively; Cmax was (51.64 ± 9.59) and (40.83 ± 9.13) ng / m L, respectively; AUC0-t was (385.69 ± 65.45), (394.24 ± 64.68) ng · m L-1 · h; AUC0-∞ were (390.85 ± 66.40) and (400.13 ± 65.89) ng · m L-1 · h, respectively. The average relative bioavailability of levetiracetam injection was (98.1 ± 9.4)% based on the AUC0-t of levetiracetam tablets. No serious adverse events occurred during the trial. Conclusion: The pharmacokinetic parameters of levetiracetam injection and levetiracetam tablets are not statistically different, and the safety of the two preparations in healthy subjects is good.