Systemic exposure to rosiglitazone is unaltered by food

Objective: To evaluate the effect of food on the bioavailability and pharmacokinetics of the insulin sensitizer rosiglitazone. Methods: In a randomized, open-label, period-balanced, single-dose, crossover study, rosiglitazone 2 mg was administered to 12 healthy male volunteers either in the fasting state or following a standard high-fat breakfast. The primary end points of the study were AUC(0-inf), and C-max. Results: Single oral doses of rosiglitazone were safe and well tolerated. Overall exposure to rosiglitazone was un- affected by food. The geometric mean ratio of AUC((0-inf)) , in the fed:fasted regimens was 0.94 (95% CI: 0.82, 1.06); t(1/2) was unaffected. Absorption of rosiglitazone in the fed state was more gradual and sustained than in the fasted state. C-max was reduced by approximately 20% (point estimate 0.80; 95% CI 0.65 to 0.97) and t(max) was modestly delayed in the fed state. Conclusion: These data support dosing guidelines that will permit the administration of rosiglitazone without regard to meals for treatment of type 2 diabetes mellitus.