Determination of Deltaline in Rat Plasma by UPLC-MS/MS and its Application to Pharmacokinetics

A sensitive and simple UPLC-MS/MS method was developed to detect deltaline in rat plasma, and its pharmacokinetics in rats was investigated. Precipitation method with acetonitrile was used for preparation samples. A BEH C18 column was used for chromatographic separation, mobile phase was acetonitrile-0.1% formic acid with gradient elution. Multiple reaction monitoring (MRM) mode with positive electrospray ionization (ESI)ionization was applied, 508.3 -> 110.0 and 285.1 -> 193.3 for deltaline and IS. Linearity of deltaline (0.5-500 ng/mL) in rat plasma was acceptable (r > 0.995), and the lower limit of quantification (LLOQ) was 0.5 ng/mL. Accuracy of method was between 91.2 and 109.3%, precision was lower than 13%, and matrix effect was between 103.7 and 108.7%. The UPLC-MS/MS method was successfully applied in the pharmacokinetics of deltaline in rats after oral and intravenous administration. The absolute bioavailability of the deltaline was 2.0% in rats.