Determination of talinolol in human plasma by high performance liquid chromatography–electrospray ionization mass spectrometry: Application to pharmacokinetic study

A rapid and sensitive method for determination and screening in human plasma of talinolol is described using propranolol as the internal standard. The analytes in plasma were extracted by liquid–liquid extraction using methyl t-butyl ether. After removed and dried the upper organic phase, the extracts were reconstituted with a fixed volume of buffer of ammonium acetate and acetonitrile (60:40, v/v). The extracts were analyzed by a HPLC coupled to electrospray ionization mass spectrometry (HPLC–MS/ESI). The HPLC separation of the analytes was performed on a Phenomenex C18 (250 mm × 4.6 mm, 5 μm, USA) column, with a flow rate of 0.85 mL/min. The complete elution was obtained within 5.5 min. The calibration curve was linear in the 1.0–400.0 ng/mL range for talinolol, with a coefficient of determination of 0.9996. The average extraction recovery was above 83%. The methodology recovery was between 101% and 102%. The limit of detection (LOD) was 0.3 ng/mL for talinolol. The intraday and inter-day coefficients of variation were less than 6%. This HPLC–MS/ESI procedure was used to assess the pharmacokinetics of talinolol. A single oral 50 mg dose of talinolol tablet was administered to 12 healthy Chinese volunteers, the main pharmacokinetic data are as follows: Cmax was 147.8 ± 63.8 ng/mL; tmax was 2.0 ± 0.7 h; t1/2 was 12.0 ± 2.6 h. The method is accurate, sensitive and simple for the pharmacokinetic study of talinolol.