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J Clin Pharmacol ; 44(2): 158-62, 2004 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-14747424

RESUMO

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%).


Assuntos
Inibidores Enzimáticos/farmacocinética , Piperazinas/farmacocinética , Pirimidinas/farmacocinética , Adulto , Área Sob a Curva , Benzamidas , Disponibilidade Biológica , Cápsulas , Estudos Cross-Over , Inibidores Enzimáticos/administração & dosagem , Inibidores Enzimáticos/sangue , Feminino , Meia-Vida , Humanos , Mesilato de Imatinib , Infusões Intravenosas , Absorção Intestinal , Masculino , Taxa de Depuração Metabólica , Pessoa de Meia-Idade , Projetos Piloto , Piperazinas/administração & dosagem , Piperazinas/sangue , Pirimidinas/administração & dosagem , Pirimidinas/sangue
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