空腹和餐后状态下盐酸西替利嗪片的生物等效性研究#br#

目的：评价中国健康人群空腹和餐后状态下口服盐酸西替利嗪片的生物等效性。方法：采用单剂量、随机、开放、两制剂、两周期、交叉对照的试验设计，健康受试者每周期在空腹或餐后状态下口服受试制剂和参比制剂盐酸西替利嗪片10 mg。采用经验证的液相色谱-串联质谱（LC-MS/MS）法测定西替利嗪的血浆浓度，使用WinNonlin 6.3计算药动学参数并用SAS 9.4软件进行生物等效性评价。结果：空腹状态下，受试制剂和参比制剂中西替利嗪Cmax分别为（402±84）、（379±53） ng/mL，AUC0-t分别为（2 520±491）、（2 455±480） ng·mL-1·h，AUC0-∞分别为（2 623±483）、（2 608±441） ng·mL-1·h。餐后状态下，受试制剂和参比制剂中西替利嗪Cmax分别为（221± 55）、（221±36）ng/mL，AUC0-t分别为（2 046±524）、（2 067±513） ng·mL-1·h，AUC0-∞分别为（2 142±508）、（2 165±500） ng·mL-1·h。受试制剂和参比制剂西替利嗪Cmax、AUC0-t和AUC0-∞几何均值比的90%置信区间均在80.00%～125.00%的生物等效性范围内。结论：盐酸西替利嗪片受试制剂和参比制剂在空腹和餐后状态下均具有生物等效性。

Bioequivalence study of cetirizine hydrochloride tablets under fasting and fed conditions

AIM: To evaluate the pharmacokinetics and bioequivalence of cetirizine hydrochloride tablets under fasting and fed conditions in Chinese healthy subjects. METHODS: This was a randomized, open-label, double-sequence, two-period, crossover designed study, and healthy subjects enrolled and administrated a single dose of 10 mg test and reference cetirizine hydrochloride tablets in each period under fasting or fed condition. The plasma concentrations of cetirizine were determined by a validated LC-MS/MS method. The pharmacokinetic parameters were calculated with WinNonlin 6.3 and the bioequivalence was evaluated through SAS 9.4 software. RESULTS: In the fasting condition, the major pharmacokinetic parameters of cetirizine of test and reference formulations were as follows, Cmax were (402±84) and (379±53) ng/mL, AUC0-t were (2 520±491) and (2 455±480) ng·mL-1·h, AUC0-∞ were (2 623±483) and (2 608±441) ng·mL-1·h, respectively. Subjects administrated test and reference formulations in fed condition had a Cmax of (221±55) and (221±36) ng/mL, an AUC0-t of (2 046±524) and (2067±513) ng·mL-1·h, AUC0-∞ were (2 142±508) and (2 165±500) ng·mL-1·h, respectively. The 90% confidence intervals of geometric mean ratios were all within the bioequivalence range of 80.00%-125.00%. CONCLUSION: The test formulation of cetirizine hydrochloride was bioequivalent to the reference product both under fasting and fed conditions.