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目的建立HPLC-MS法测定人血浆中茴拉西坦的活性代谢物对甲氧基苯甲酰氨基丁酸(ABA)的浓度,比较2种茴拉西坦胶囊的人体生物等效性。方法 24名健康男性志愿者单剂量交叉口服受试制剂或参比制剂200 mg,采用HPLC-MS法测定血浆中不同时间点茴拉西坦代谢物ABA的血药浓度,计算主要药代动力学参数及相对生物利用度,评价2种制剂的生物等效性。结果受试制剂和参比制剂的主要药动学参数:Cmax分别为(9.30±5.13)和(8.70±3.17)μg/ml;tmax分别为(38.41±17.89)和(39.09±19.92)min;t1/2分别为(37.21±10.51)和(38.45±9.24)min;AUC0-t分别为(555.21±157.10)和(545.39±97.22)μg/(ml.min);AUC0-∞分别为(566.24±158.01)和(554.71±100.32)μg/(ml.min)。以AUC0-t和AUC0-∞计算,受试制剂的相对生物利用度F0-t和F0-∞分别为(101.22±17.17)%和(101.52±16.63)%。2种制剂的主要药代动力学参数差异无统计学意义。结论 2种茴拉西坦胶囊具有生物等效性。
OBJECTIVE To establish a HPLC-MS method for the determination of p-anisamidobutyric acid (ABA), an active metabolite of aniracetam in human plasma, and to compare the bioequivalence of two aniracetam capsules. Methods Twenty-four healthy male volunteers were given a single dose of 200 mg of the test preparation or reference preparation. The plasma concentration of aniracetam metabolite ABA at different time points was measured by HPLC-MS. The main pharmacokinetics Parameters and relative bioavailability, bioequivalence of the two formulations was evaluated. Results The main pharmacokinetic parameters of test preparation and reference preparation were: Cmax (9.30 ± 5.13) and (8.70 ± 3.17) μg / ml respectively; tmax was (38.41 ± 17.89) and (39.09 ± 19.92) min respectively; t1 / 2 were (37.21 ± 10.51) and (38.45 ± 9.24) min respectively; AUC0-t were (555.21 ± 157.10) and (545.39 ± 97.22) μg / (ml · min), respectively; AUC0-∞ were (566.24 ± 158.01 ) And (554.71 ± 100.32) μg / (ml.min). The relative bioavailability (F0-t and F0-∞) of the tested formulations were (101.22 ± 17.17)% and (101.52 ± 16.63)%, respectively, as calculated by AUC0-t and AUC0-∞. There was no significant difference in the main pharmacokinetic parameters between the two preparations. Conclusions The two aniracetam capsules are bioequivalent.