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目的:评价盐酸特比萘芬片在健康人体的相对生物利用度和生物等效性。方法:20名健康受试者随机交叉单剂量口服盐酸特比萘芬片受试制剂(T)和参比制剂(R),采用液质联用分析方法(LC-MS/MS)测定血浆中特比萘芬浓度。结果:20名健康受试者口服受试制剂和参比制剂后的主要药代动力学参数为:Tmax分别为(1.7±0.6)和(2.2±0.7)h;Cmax分别为(1 590±489)和(1 266.6±432.8)ng·mL-1;t1/2分别为:(21.6±3.6)和(21.0±10.1)h;AUC0～t分别为(8 272.2±2 280.6)和(8 138.9±2 424.0)ng·h·mL-1。受试制剂的AUC0～t或Cmax的90%置信区间对应于参比制剂相应参数的93.44%～111.87%或112.83%～141.91%范围内;受试制剂相对于参比制剂的相对生物利用度为(105.5±26.3)%。结论:受试制剂与参比制剂的生物利用度相当,但受试制剂峰浓度增加,达峰时间提前,没有增加不良反应,疗效也未见降低。
OBJECTIVE: To evaluate the relative bioavailability and bioequivalence of terbinafine hydrochloride tablets in healthy volunteers. Methods: Twenty healthy subjects were randomized to receive a single dose of terbinafine hydrochloride test formulation (T) and a reference formulation (R). LC-MS / MS was used to determine plasma Terbinafine concentration. RESULTS: The main pharmacokinetic parameters of 20 healthy subjects after oral administration of the test preparation and the reference preparation were Tmax (1.7 ± 0.6) and (2.2 ± 0.7) h, respectively, and Cmax were (1 590 ± 489) (21.6 ± 3.6) and (21.0 ± 10.1) h, respectively. The AUC0 ~ t were (8 272.2 ± 2 280.6) and (8 138.9 ± 2 424.0) ng · h · mL-1. The 90% confidence intervals of AUC0 ~ t or Cmax of the tested formulations corresponded to 93.44% ~ 111.87% or 112.83% ~ 141.91% of the corresponding parameters of the reference formulation; the relative bioavailability of the tested formulations relative to the reference formulation was (105.5 ± 26.3)%. Conclusion: The bioavailability of the test preparation and the reference preparation is similar, but the peak concentration of the test preparation increases, the peak time is advanced, the adverse reaction is not increased, and the curative effect is not reduced.