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An Overview of the Pharmacokinetics of Cilomilast (Ariflo®), a New, Orally Active Phosphodiesterase 4 Inhibitor, in Healthy Young and Elderly Volunteers
Author(s) -
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
Publication year - 2001
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/009127000104100904
Subject(s) - pharmacokinetics , dosing , tolerability , bioavailability , medicine , pharmacology , oral administration , absorption (acoustics) , adverse effect , physics , acoustics
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 C max and t 1/2 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 .