Objectives:This study assessed the pharmacokinetics, safety, and bioequivalence of generic and original palbociclib tablets in healthy Chinese subjects under fasting conditions with rabeprazole pre-treatment.
Methods:This was a single-dose, randomized, open-label, two-period crossover bioequivalence study conducted under fasting conditions with rabeprazole pre-treatment. In each trial, healthy Chinese subjects received 40 mg oral rabeprazole enteric-coated tablets once daily before breakfast for 6 days. Following an overnight fast of at least 10 h, they took the seventh dose of rabeprazole and maintained fasting. They then received a single 125 mg oral dose of either the test or reference palbociclib tablet, followed by a 14-day washout interval between periods. Blood samples were collected from 0 to 96 h post-dose in each period, and palbociclib plasma concentrations were determined using a validated method. The primary pharmacokinetic parameters were calculated using the non-compartmental method. The geometric mean ratios of the two formulations and the corresponding 90% confidence intervals were acquired for bioequivalence analysis. The safety of both formulations was also evaluated.
Results:
The 90% confidence intervals for the primary pharmacokinetic parameters of C
max
(84.53%–91.72%), AUC
0-t
(87.81%–92.49%), and
AUC0‐∞
(87.59%–92.03%) all fell within the 80.00%–125.00% bioequivalence range. No serious adverse events occurred during the study.
Conclusion:The trial confirmed that the pharmacokinetic parameters of the generic and original palbociclib tablets were bioequivalent in healthy Chinese subjects under fasting conditions with rabeprazole pre-treatment. Both formulations were safe and well tolerated.
Clinical Trial Registration:http://www.chinadrugtrials.org.cn
, identifier CTR20232617;
https://www.chictr.org.cn
, identifier ChiCTR2400084355.