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In vitro characterization of rosiglitazone metabolites and determination of the kinetic parameters employing rat liver microsomal fraction.

Eur J Drug Metab Pharmacokinet 2011 Sep 17;36(3):159-66. Epub 2011 Apr 17.

Departamento de Física e Química, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, 14040-903, Brazil.

Rosiglitazone (RSG), a thiazolidinedione antidiabetic drug, is metabolized by CYP450 enzymes into two main metabolites: N-desmethyl rosiglitazone (N-Dm-R) and ρ-hydroxy rosiglitazone (ρ-OH-R). In humans, CYP2C8 appears to have a major role in RSG metabolism. On the other hand, the in vitro metabolism of RSG in animals has not been described in literature yet. Read More

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September 2011
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