Source: Annual Congress 2001 - Asthma
Disease area: Airway diseases

Abstract

Roflumilast (ROF) is a new selective PDE4 inhibitor for the treatment of COPD and asthma. We investigated the pharmacokinetic (PK) characteristics of ROF after oral and iv administration.
In an open, randomized, 2-period cross-over study 12 healthy male subjects (age: 25-44 y) received a single oral dose of 500 mcg ROF and 150 mcg iv as 15 min short-term infusion. Plasma concentrations of ROF and metabolite were measured by HPLC. PK data are given below as georn. means with 68% range. [TABLE] The absolute bioavailability was 79% (69 - 92%). Vital signs, ECG, clinical laboratory and adverse events (AE) were recorded. No relevant changes were observed. The medication was safe and well tolerated.
In conclusion, the high absolute bioavailability and the long t_1/2 of ROF after oral intake favours a once daily administration mode.

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K. Zech, M. David, M. Seiberling, C. Weimar, T. Bethke, W. Wurst (Konstanz, Freiburg). High oral absolute bioavailability of roflumilast, a new, orally active, once daily PDE4 inhibitor. Eur Respir J 2001; 16: Suppl. 31, 256

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