Objective  To evaluate the bioequivalence and safety of the test and reference preparations of palbociclib capsules in Chinese healthy subjects under fasting and postprandial conditions.

Methods  A single-center, randomized, open-label, two-drug, two-sequence and two-cycle crossover trial was designed. 32 healthy subjects were enrolled in the fasting trial and 28 healthy subjects were enrolled in the postprandial trial. The subjects were randomly assigned to two experimental groups (T-R group and R-T group), with a weekly administration of 125 mg each time. The concentration of palbociclib in plasma was determined by HPLC-MS/MS. The PK parameter set was obtained by Phoenix WinNonlin 8.3 software. The pharmacokinetic parameters of palbociclib capsules in each subject were calculated by noncompartmental model and statistically analyzed. The safety of clinical observation indexes of subjects was also evaluated.

Results  In the fasting and postprandial trials, 31 and 28 subjects completed two cycles of dosing, respectively. The 90% confidence intervals of the geometric mean ratios of C_max, AUC_0-t and AUC_0-∞ of the test preparation and the reference preparation were in the range of 80.00%-125.00%, and the two preparations were bioequivalent after taking palbociclib capsules under fasting and postprandial conditions. No serious adverse events occurred throughout the trial.

Conclusion  The test and reference preparations of palbociclib capsules have bioequivalence and good safety in healthy Chinese volunteers under fasting and postprandial conditions.

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