An UPLC-MS/MS method for quantification of D-pinitol in rat plasma and its application to a pharmacokinetic and...

D-pinitol could be a potential therapeutic agent for the treatment of diabetes mellitus (DM) type II. In this work, a sensitive and rapid ultra performance liquid chromatography coupled with tandem mass spectrometry method was firstly developed and validated for the determination and pharmacokinetic study of D-pinitol in rat plasma. D-pinitol and 5,7-dihydroxychromone (Internal Standard, IS) were completely separated on a BEH C18 column. The plasma samples were deproteinated with acetonitrile: ethanol (1:1). The MRM transitions for D-pinitol was m/z 179.125 → 105.049, and for IS was m/z 195.085 → 109.031. The method linearity ranges was 5-200 ng/mL. The precision, accuracy, recovery, matrix effect, stability under different conditions, were all within the required criteria. After intragastric (50 mg/kg) administration of D-pinitol to the rats, the maximum plasma concentration (C_max) was 77.8 ± 19.5 ng/mL. The time to reach the maximum plasma concentration (T_max) was 2.2 ± 0.98 h. Apparent distribution volume (V_z) was 1557.5 ± 1329.1 L/kg and the plasma centration time curve (AUC_0-t) was 1265.5 ± 479.3 µg/L*h. After intravenous (5.0 mg/kg) administration, V_z was 325.2 ± 107.8 L/kg and AUC_(0-t) was 693.0 ± 89.9 µg/L*h. Our study indicated D-pinitol had a slow elimination phase and might be the high affinity binding to blood protein in vivo, which are helpful for its further drug development and clinical application.