| Investigation of a potential food effect on the pharmacokinetics of roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor, in healthy subjects. | |
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MedLine Citation:
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PMID: 16988203 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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This open, randomized, single-dose crossover study investigated effects of a high-fat meal on the pharmacokinetics of roflumilast and its major active N-oxide metabolite. Twelve healthy subjects received oral roflumilast 500 microg (2 x 250 microg) after overnight fasting and after breakfast. Blood was sampled up to 54 hours for pharmacokinetic profiling of roflumilast and N-oxide. Geometric mean ratios (fed/fasted) for point estimates (PE) and 90% confidence intervals (CI) were calculated for AUC(0-last), AUC(0-infinity), and C(max) of both compounds. After the meal, roflumilast C(max) (PE, 0.59; 90% CI, 0.49-0.70) was modestly reduced; N-oxide C(max) (PE, 0.95; 90% CI, 0.90-1.01) was unchanged. Roflumilast t(max) was delayed in fed state (2.0 +/- 0.4 hours) versus fasted state (1.0 +/- 0.2 hours); N-oxide t(max) was unaltered. No significant food effect on roflumilast AUC(0-last) (PE, 1.04; 90% CI, 0.90-1.21), AUC(0-infinity) (PE, 1.12; 90% CI, 1.00-1.25), and respective N-oxide AUCs (PE, 0.91; 90% CI, 0.79-1.04; PE, 0.99; 90% CI, 0.92-1.06) occurred. Because roflumilast N-oxide is the major contributor to roflumilast's overall pharmacologic effects, these findings suggest that roflumilast can be taken with or without food. |
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Authors:
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Bernhard Hauns; Robert Hermann; Andreas Hünnemeyer; Rolf Herzog; Dieter Hauschke; Karl Zech; Thomas D Bethke |
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Publication Detail:
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Type: Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of clinical pharmacology Volume: 46 ISSN: 0091-2700 ISO Abbreviation: J Clin Pharmacol Publication Date: 2006 Oct |
Date Detail:
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Created Date: 2006-09-21 Completed Date: 2007-03-13 Revised Date: 2007-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0366372 Medline TA: J Clin Pharmacol Country: United States |
Other Details:
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Languages: eng Pagination: 1146-53 Citation Subset: IM |
Affiliation:
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Department of Clinical Pharmacology, ALTANA Pharma AG, Byk-Gulden-Str. 2, D-78467 Konstanz, Germany. bernhard.hauns@altanapharma.com |
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| MeSH Terms | |
Descriptor/Qualifier:
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3',5'-Cyclic-AMP Phosphodiesterases
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antagonists & inhibitors* Administration, Oral Adult Aminopyridines / administration & dosage, blood, metabolism, pharmacokinetics* Area Under Curve Benzamides / administration & dosage, blood, metabolism, pharmacokinetics* Cross-Over Studies Cyclic Nucleotide Phosphodiesterases, Type 4 Cyclopropanes / administration & dosage, blood, metabolism, pharmacokinetics Dietary Fats / administration & dosage*, adverse effects, pharmacokinetics Fasting Female Food-Drug Interactions* Half-Life Headache / diagnosis, epidemiology Humans Male Phosphodiesterase Inhibitors / administration & dosage, adverse effects, pharmacokinetics* |
| Chemical | |
Reg. No./Substance:
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0/Aminopyridines; 0/Benzamides; 0/Cyclopropanes; 0/Dietary Fats; 0/Phosphodiesterase Inhibitors; 0/roflumilast; 0/roflumilast N-oxide; EC 3.1.4.17/3',5'-Cyclic-AMP Phosphodiesterases; EC 3.1.4.17/Cyclic Nucleotide Phosphodiesterases, Type 4 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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