Tissue distribution, pharmacokinetics and identification of roscovitine metabolites in rat

The pharmacokinetics, biodistribution and the metabolic pathway of roscovitine were investigated in Sprague-Dawley rats after a single intravenous dose of 25 mg/kg. Blood, lungs, kidney, liver, testis, adipose tissue, spleen and brain were removed at different time-points. Plasma and tissue samples...

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Bibliographic Details
Published in:European journal of pharmaceutical sciences 2005-05, Vol.25 (1), p.91-103
Main Authors: Vita, Marina, Abdel-Rehim, Mohamed, Olofsson, Susanne, Hassan, Zuzana, Meurling, Lennart, Sidén, Åke, Sidén, Mabel, Pettersson, Tommy, Hassan, Moustapha
Format: Article
Language:English
Subjects:
Animals
Area Under Curve
Biological and medical sciences
cdk inhibitors
Chromatography, High Pressure Liquid
Drug metabolism
General pharmacology
HPLC
Magnetic Resonance Spectroscopy
Mass Spectrometry
Medical sciences
Medicin och hälsovetenskap
NMR
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Purines - pharmacokinetics
Rats
Rats, Sprague-Dawley
Tissue Distribution
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Summary:The pharmacokinetics, biodistribution and the metabolic pathway of roscovitine were investigated in Sprague-Dawley rats after a single intravenous dose of 25 mg/kg. Blood, lungs, kidney, liver, testis, adipose tissue, spleen and brain were removed at different time-points. Plasma and tissue samples were analyzed using high performance liquid chromatography. The metabolites were identified using liquid chromatography/tandem mass spectrometry and nuclear magnetic resonance spectroscopy. Roscovitine (MW = 354) was cleared rapidly from circulation and highly distributed to the tissues. The elimination half-life of roscovitine in plasma and tissues was short (
ISSN:0928-0987
1879-0720
DOI:10.1016/j.ejps.2005.02.001