关键词: 西替利嗪, 药动学, 生物等效性, 液相色谱-串联质谱

Abstract: 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.

Key words: cetirizine, pharmacokinetic, bioequivalence, LC-MS/MS