Determination of metabolite of nicergoline in human plasma by high-performance liquid chromatography and its application in pharmacokinetic studies

Abstract

AbstractA fast, simple and sensitive high performance liquid chromatographic (HPLC) method has been developed for determination of 10α-methoxy-6-methyl ergoline-8β-methanol (MDL, a main metabolite of nicergoline) in human plasma. One-step liquid–liquid extraction (LLE) with diethyl ether was employed as the sample preparation method. Tizanidine hydrochloride was selected as the internal standard (IS). Analysis was carried out on a Diamonsil ODS column (150mm×4.6mm, 5μm) using acetonitrile–ammonium acetate (0.1mol/L) (15/85, v/v) as mobile phase at detection wavelength of 224nm. The calibration curves were linear over the range of 2.288–73.2ng/mL with a lower limit of quantitation (LLOQ) of 2.288ng/mL. The intra- and inter-day precision values were below 13% and the recoveries were from 74.47% to 83.20% at three quality control levels. The method herein described was successfully applied in a randomized crossover bioequivalence study of two different nicergoline preparations after administration of 30mg in 20 healthy volunteers