Systemic exposure to rosiglitazone is unaltered by food
MI Freed, A Allen, DK Jorkasky, RA DiCicco - European journal of clinical …, 1999 - Springer
MI Freed, A Allen, DK Jorkasky, RA DiCicco
European journal of clinical pharmacology, 1999•SpringerObjective: 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 unaffected …
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 unaffected …
Abstract
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 AUC0–inf and Cmax.
Results: Single oral doses of rosiglitazone were safe and well tolerated. Overall exposure to rosiglitazone was unaffected by food. The geometric mean ratio of AUC(0–inf) in the fed:fasted regimens was 0.94 (95% CI: 0.82, 1.06); t1/2 was unaffected. Absorption of rosiglitazone in the fed state was more gradual and sustained than in the fasted state. Cmax was reduced by approximately 20% (point estimate 0.80; 95% CI 0.65 to 0.97) and tmax 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.
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