Details

Autor(en) / Beteiligte

• Kosoglou, Teddy
• Hubbell, James
• Kantesaria, Bhavna
• Hanson, Mary E.
• Cutler, David L.

Titel

An evaluation of the systemic bioavailability of mometasone furoate (MF) after oral inhalation from a MF/formoterol fumarate metered-dose inhaler versus an MF dry-powder inhaler in healthy subjects

Ist Teil von

• Clinical pharmacology in drug development, 2014-05, Vol.3 (3), p.229-234

Ort / Verlag

United States: Blackwell Publishing Ltd

Erscheinungsjahr

2014

Quelle

Wiley-Blackwell Journals

Beschreibungen/Notizen

• Purpose This randomized, open‐label, multiple‐dose, two‐period, crossover study compared the systemic bioavailability of mometasone furoate (MF) administered from a metered‐dose inhaler containing MF and formoterol fumarate (F) (MF/F‐MDI) versus MF administered from a single‐ingredient dry‐powder inhaler (MF‐DPI). Methods Healthy, non‐smoking adults, 18–65 years with body mass index 18–29 kg/m2 (N = 12) received MF 800 µg/F 20 µg via MF/F‐MDI or MF 800 µg via MF‐DPI twice daily for 5 days separated by a 7‐day period. MF pharmacokinetics (AUC(0–12 hour), Cmax, and Tmax) were measured at Day 1 and 5 after each treatment. Safety and tolerability were assessed. Results Systemic exposure to MF based on AUC(0–12 hour) was ∼25% lower following MDI versus DPI administration. The Day 5 geometric mean ratio (MDI/DPI) estimates (90% confidence intervals [CI]) for AUC(0–12 hour) and Cmax were 0.747 (0.61, 0.91) and 0.606 (0.49, 0.75), respectively. The accumulation index (R) value for MF was higher following MDI (3.81‐fold) versus DPI administration (2.34‐fold) indicative of prolonged absorption. The most common adverse events were tremor, headache, and catheter site pain. Conclusions Systemic exposure to MF was lower following multiple‐dose MF/F‐MDI administration versus MF‐DPI administration. The magnitude of this difference is not considered to be clinically important. MF/F‐MDI was safe and generally well tolerated.