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.

D-松醇可能是治疗II型糖尿病（DM）的潜在治疗剂。在这项工作中，首先开发了灵敏，快速的超高效液相色谱-串联质谱联用方法，并被验证用于大鼠血浆中D-松醇的测定和药代动力学研究。D-松醇和5,7-二羟基色酮（内标，IS）在BEH C18色谱柱上完全分离。血浆样品用乙腈：乙醇（1：1）脱蛋白。D-松醇的MRM跃迁为m / z 179.125→105.049，IS为m / z195.085→109.031。该方法的线性范围为5–200 ng / mL。在不同条件下的精密度，准确性，回收率，基质效应，稳定性均在要求的标准之内。在大鼠胃内（50 mg / kg）施用D-松醇之后，最大血浆浓度（C _max）为77.8±19.5 ng / mL。达到最大血浆浓度（T _max）的时间为2.2±0.98 h。表观分布体积（V _z）为1557.5±1329.1 L / kg，血浆浓缩时间曲线（AUC _0-t）为1265.5±479.3 µg / L * h。静脉内（5.0 mg / kg）给药后，V _z为325.2±107.8 L / kg和AUC _（0-t）为693.0±89.9μg/ L * h。我们的研究表明，D-松醇的消除阶段较慢，可能与体内血蛋白具有高亲和力结合，这有助于其进一步的药物开发和临床应用。