Pharmacokinetics and pharmacodynamics of ciclesonide and its active principle after inhalative and intravenous administration in healthy subjects
R. Nave, T. D. Bethke, M. Seiberling, V. W. Steinijans, K. Zech (Konstanz, Freiburg, Germany)
Source: Annual Congress 2002 - Asthma and COPD: pharmacology
Session: Asthma and COPD: pharmacology
Session type: Thematic Poster Session
Number: 749
Disease area: Airway diseases
Abstract Objectives: Ciclesonide (CIC) is a novel topical glucocorticosteroid currently under development for the treatment of asthma. The present study investigated the bioavailability of CIC and its active principle (CIC-AP) after inhalation of CIC as compared to intravenous administration of CIC to healthy subjects. Pharmacodynamics (cortisol in serum) was compared to corresponding placebo formulations. Methods: Open, randomized, change-over study design with 12 healthy male subjects (median age: 30y) who received the following treatments: I) Inhaled placebo on day 1 in one period and a dose of 1600μg CIC via a HFA-driven MDI on day 2; II) Intravenous placebo on day 1 in the other period and 800μg CIC as intravenous infusion on day 2. Serum concentrations of CIC and CIC-AP were determined by LC/MS/MS (LLOQ: 25ng/l). Results: The mean volume of distribution was 2.9 l/kg and the total clearance was 2.0 l/h/kg for the parent compound following intravenous administration. Absolute bioavailability of CIC and systemic availability of CIC-AP after inhalation was 18 (13-24)% and 50 (35-73)%, respectively. Changes in serum cortisol mesors were statistically non-significant at the 5% level. Conclusions: Pharmacokinetic results indicate a high lung deposition rate of the active principle. After inhalative or intravenous administration of ciclesonide no suppression of cortisol in serum was observed.
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R. Nave, T. D. Bethke, M. Seiberling, V. W. Steinijans, K. Zech (Konstanz, Freiburg, Germany). Pharmacokinetics and pharmacodynamics of ciclesonide and its active principle after inhalative and intravenous administration in healthy subjects. Eur Respir J 2002; 20: Suppl. 38, 749
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