Pharmacokinetics and tissues distribution of rosiglitazone in rats

Abstract

Abstract: A simple, rapid and selective HPLC method was developed and validated to determinate rosiglitazone in rat plasma, tissues and cerebrospinal fluid. Samples were prepared, with a higher extraction recovery (96.72% in plasma， 95.63% in tissues and 90.67% in cerebrospinal fluid), based on a simple methanol protein precipitation. Assay of rosiglitazone was achieved on a reversed-phase C₁₈ column (250 mm× 4.6 mm, 5 μm) with a mobile phase consisting of acetonitrile and 20 mmol/L ammonium acetate pH 6.0 (53∶47, v/v) at a flow rate of 0.6 mL/min. The method was applied to study pharmacokinetics, distribution of rosiglitazone in rats after a single intragastric administration. The rosiglitazone was rapidly absorbed (Tmax 0.5～1 h) with an elimination half-life of 2.5 hours. The highest levels of the drug were observed in liver and fat while the lowest levels in the brain and spleen. The method was also used for the determination of rosiglitazone in cerebrospinal fluid. The result showed that rosiglitazone can be detected in cerebrospinal fluid, thus providing direct evidence that rosiglitazone can permeate cross blood brain barrier.

Key words: rosiglitazone, HPLC-UV, pharmacokinetics, tissues distribution, cerebrospinal fluid

CLC Number:

R965

ZHANG Ling-hong, DUAN Ya-le, LI Yu-bo, WAN Xue-mei, ZHAO Zheng. Pharmacokinetics and tissues distribution of rosiglitazone in rats[J]. Journal of East China Normal University(Natural Sc, 2011, 2011(4): 104-114.

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