Pharmacokinetic and bioequivalence study of apremilast tablets in healthy Chinese subjects under fasting and fed conditions.

Apremilast is a pioneering oral selective phosphodiesterase-4 inhibitor for the treatment of psoriasis. To evaluate and compare the pharmacokinetic properties and bioavailability of apremilast tablets manufactured by Nanjing Haijing Pharmaceutical Company (Nanjing, China) with apremilast tablets certified by Celgene Europe B.V. (Utrecht, The Netherlands), we conducted a randomized, open-label, single-dose, two-period, crossover study in healthy Chinese subjects under fasted and fed conditions. Eligible subjects were randomly assigned to receive reference or test apremilast tablets in the first treatment period and the other formulation in the second period. Serial blood samples were collected for pharmacokinetic analysis. Adverse events were recorded. A total of 28 healthy subjects were enrolled in the fasting cohort and 36 subjects in the fed cohort. The 90% confidence intervals of the geometric mean ratios of the test to reference formulations were 91.56 - 106.18% for Cmax, 96.08 - 108.18% for AUC0-t, and 96.02 - 107.67% for AUC0-∞ in the fasting cohort, and 95.15 - 107.05% for Cmax, 105.13 - 113.45% for AUC0-t, and 104.80 - 111.91% for AUC0-∞ in the fed cohort, all of which were within the bioequivalence range of 80.00 - 125.00%. There were no serious adverse events. The results showed that the test and reference apremilast tablets were bioequivalent and well tolerated in healthy Chinese subjects under fasting and fed conditions.