Pharmacokinetics and Bioequivalence of 2 Immediate ‐Release Tofacitinib Tablet Formulations in Chinese Healthy Volunteers Under Fasting and Fed Conditions

AbstractThe purpose of this study was to evaluate the bioequivalence of a generic immediate ‐release tofacitinib tablet versus a brand‐named immediate‐release tofacitinib tablet under fasting and fed conditions, and the food effect on pharmacokinetic profiles of the both formulations. This randomized, open‐label, 2‐period, crossover, bioequivalence study included 52 healthy Chine se subjects (fasting cohort: n = 26; fed cohort: n = 26). The subjects were assigned to receive a single 5‐mg dose of generic or brand‐named tofacitinib. Blood samples were collected at predosing and up to 14 hours after dosing. Tofacitinib concentrations in plasma were analyzed by high‐perfor mance liquid chromatography–tandem mass spectrometry. Safety was monitored. There were no significant differences in maximum plasma concentration, area under the plasma concentration–time curve from time zero to time t (AUC0 ‐t), AUC from time zero to infinity (AUC0 ‐∞), and terminal elimination half ‐life between the test and reference formulations (allP> .05); high ‐fat food had no significant effect on AUC0 ‐t, AUC0 ‐∞, or terminal elimination half ‐life of immediate‐release tofacitinib tablets (allP> .05). The 90% confidence intervals of the test/reference ratios of log ‐transformed maximum plasma concentration, AUC0 ‐t, and AUC0 ‐∞ were within the range of 80% to 125% under both fasting and fed conditions. No serious adverse events were reported. The 2 ...
Source: Clinical Pharmacology in Drug Development - Category: Drugs & Pharmacology Authors: Tags: Original Manuscript Source Type: research