Details

Autor(en) / Beteiligte

• Zussman, Barry D.
• Benincosa, Lisa J.
• Webber, Dawn M.
• Clark, David J.
• Cowley, Hugh
• Kelly, John
• Murdoch, Robed D.
• Upward, James
• Wyld, Peter
• Port, Andreas
• Fuder, Hermann

Titel

An Overview of the Pharmacokinetics of Cilomilast (Ariflo®), a New, Orally Active Phosphodiesterase 4 Inhibitor, in Healthy Young and Elderly Volunteers

Ist Teil von

• Journal of clinical pharmacology, 2001-09, Vol.41 (9), p.950-958

Ort / Verlag

Oxford, UK: Blackwell Publishing Ltd

Erscheinungsjahr

2001

Quelle

MEDLINE

Beschreibungen/Notizen

• The oral pharmacokinetics of cilomilast (Ariflo®) were investtigated in five separate studies in healthy volunteers. Cilomilast was rapidly absorbed, and pharmacokinetics were dose proportional after single and repeat dosing. The elimination half‐life was 7 to 8 hours; accordingly steady state was reached on the 3rd day of dosing. The degree of accumulation following repeat twice‐daily dosing was predictable from the data following a single dose. Although systemic exposure (AUC) was, on average, 21% higher in elderly (65–84 years) compared with young subjects, values for Cmax and t1/2 were similar, and no difference in tolerability was noted. Single and repeat doses of cilomilast up to and including 15 mg (dosed before or taken between meals) were well tolerated. Dosing with food reduced the rate of absorption without affecting total bioavailability. Hence, tolerability was optimal in the fed state; repeat doses up to and including 30 mg twice daily after meals were well tolerated following dose titration.