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Absolute Bioavailability of Imatinib (Glivec®) Orally versus Intravenous Infusion

From the Novartis Pharmaceuticals, Florham Park, New Jersey (B. Peng, M. Hayes, M. Ben-Am); Novartis Pharma AG, Basel, Switzerland (C. Dutreix, G. Mehring, R. Capdeville, P. Lloyd); and Swiss Pharma Contract, Allschwil, Switzerland (M. Seiberling, R. Pokorny).

The purpose of this study was to investigate the absolute bioavailability of a single oral dose of imatinib (Glivec®), 400 mg (capsules vs. oral solution), compared with imatinib, 100 mg (intravenous [i.v.] infusion), in healthy subjects. Twelve subjects received a single treatment in each treatment period: a 400-mg oral dose of imatinib in capsule form or as a solution or a 100-mg i.v. infusion of imatinib. Plasma imatinib concentrations were measured following each treatment; pharmacokinetic parameters and absolute bioavailability were determined. Absolute bioavailability values (compared with i.v. infusion) for the imatinib capsule and oral solution were 98.3% and 97.2%, respectively. Both the rate and extent of imatinib absorption, as measured by C_max, partial AUC, and total AUC, were similar for the oral solution and the imatinib capsule intended for the market. The 400-mg oral dose of imatinib, as a capsule or a solution, was completely absorbed and was almost completely bioavailable (> 97%).

Key Words: Imatinib • STI571 • bioavailability • oral solution • capsule • pharmacokinetics

Address for reprints: Bin Peng, MD, PhD, Clinical Pharmacology, Novartis Pharmaceuticals Corporation, 180 Park Avenue, Building 105, Room 2W212, Florham Park, NJ 07936-1080.

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