Absolute bioavailability of imatinib (Glivec) orally versus intravenous infusion.
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%).
Peng
Bin
B
Clinical Pharmacology, Novartis Pharmaceuticals Corporation, 180 Park Avenue, Building 105, Room 2W212, Florham Park, NJ 07936-1080, USA.
Dutreix
Catherine
C
Mehring
Gunther
G
Hayes
Michael J
MJ
Ben-Am
Monique
M
Seiberling
Michael
M
Pokorny
Rolf
R
Capdeville
Renaud
R
Lloyd
Peter
P
D000328:Adult; D019540:Area Under Curve; D001549:Benzamides; D001682:Biological Availability; D002214:Capsules; D018592:Cross-Over Studies; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D005260:Female; D006207:Half-Life; D006801:Humans; D000068877:Imatinib Mesylate; D007262:Infusions, Intravenous; D007408:Intestinal Absorption; D008297:Male; D008657:Metabolic Clearance Rate; D008875:Middle Aged; D010865:Pilot Projects; D010879:Piperazines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D011743:Pyrimidines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D001549:Benzamides; D002214:Capsules; D004791:Enzyme Inhibitors; D010879:Piperazines; D011743:Pyrimidines; D000068877:Imatinib Mesylate