A sensitive validated high-performance liquid-chromatographic method for analysis of cilostazol in human plasma (in vitro) has been developed, and it was applied to determine pharmacokinetics of cilostazol in male albino rabbit. Cilostazol was extracted from human plasma (in vitro) by acetonitrile, and efficient chromatographic elution was achieved on a C18 column (250 × 4.60 mm i.d., 0.5 μm particle size) with an isocratic mobile phase [acetonitrile-50 mM acetate buffer (pH 5.0, glacial acetic acid)-water (50:20:30)] at flow rate of 1.5 mL min−1. Quantification was carried out by photo-diode array (PDA) detection at 248 nm. The linearity of the method was excellent over the range 0.2–2 μg mL-1 with low limits of detection (0.005 μg mL-1) and quantification (0.05 μg mL-1). The extraction recovery of the drug from plasma was consistently good (73.45–78.64%), with low relative standard deviation (0.44–1.65%). Robustness studies confirmed that peak area was unaffected by small changes in temperature, mobile phase (composition and pH). The maximum concentration (Cmax) in rabbit (in vivo) was determined 1.620 μg mL-1 at tmax (0.51 h) with 0.63% RSD by validated bioanalytical method.
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