正常大鼠体内女贞子红景天苷制备物药代动力学表征研究

Pharmacokinetic characterization of salidroside extract from Ligustri Lucidi Fructus in rats

目的建立超高效液相色谱法,PDA检测器同时测定大鼠血清中红景天苷及酪醇的含量分析方法,以研究女贞子红景天苷制备物药代动力学表征及其类药特性。方法采用UPLCPDA色谱法,ACQUITY UPLC H-CLASS T3色谱柱(50 mm×2.1 mm,1.8μm);流动相:乙腈—水(3︰97),流速0.3 m L/min;柱温25℃。结果入血成分红景天苷Cmax19.29μg/m L、Tmax0.5 h、T1/23.28 h、K0.21,酪醇Cmax0.32μg/m L、Tmax0.75 h,血药浓度比值(酪醇︰红景天苷)最大为2.99︰100,为体外含量比值的9.65倍。结论所建方法简便经济、稳定易行;以入血成分体内外浓度、含量比值动态变化与药代动力学表征关联分析,揭示了女贞子红景天苷制备物类药特性。

Objective The concentration of salidroside and tyrosol in serum of rats is determined by using UPLC-PDA to investigate the pharmacokinetic parameters and characters of salidroside extract pre-pared from Ligustri Lucidi Fructus. Methods UPLC-PCA was performed on ACQUITY UPLC H-CLASS T3 column（50 mm ×2. 1 mm,1. 8 μm） with salicin as the internal standard. The mobile phase was aceto-nitrile：water solution （3∶ 97, v/v） at a flow rate of 0. 3 mL/min. The temperature of column was 25℃. Results The pharmacokinetics parameters of salidroside in rat including Cmax , Tmax , T1/2 and K were 19. 29 μg/mL, 0. 5 h, 3. 28 h, 0. 21, respectively. The pharmacokinetics parameters of tyrosol in rat in-cluding Cmax , Tmax were 0. 32μg/mL and 0. 75 h, respectively. The maximum content ratio of tyrosol / sal-idroside in vivo was 2. 99/100, which was 9. 65 times higher than the ratio in vitro. Conclusion The es-tablished method showing stability was easy to execute, which revealed the drug-like characters of salidro-side extract from Ligustri Lucidi Fructus.