失眠模型下女贞子红景天苷制备物药代动力学分析研究

摘要

目的：阐明女贞子红景天苷制备物作为治疗失眠病症药物的药代动力学表征特性。方法采用超高效液相色谱法, PDA检测器, 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 mL/min；柱温25℃。结果失眠模型下,入血成分红景天苷Cmax20．24μg/mL、Tmax0．5 h、T1/22．53 h、K0．27,酪醇Cmax0．49μg/mL、Tmax0．75 h,血药浓度比值(酪醇∶红景天苷)最大值为3．90∶100,为体外含量比值的12．58倍。结论在失眠模型下,女贞子红景天苷制备物体内主要入血成分为红景天苷和酪醇,且表征出药代协同性；与正常状态比较,表现出体内成分生物利用度增加的药物亲和性。%Objective To study the pharmacokinetic characterization of Salidroside drug which was prepared from Fructus Ligustri Lucidi as a drug for insomnia treatment. Methods The drug content was measured by UPLC with PDA detector. Analyzes was performed on an ACQUITY UPLC H-CLASS T3 (50 mm × 2. 1 mm, 1. 8 μm) column with salicin as the internal standard. The mobile phase was acetoni-trile:water solution (3:97, v/v) at a flow rate of 0. 3 mL/min. The temperature of column was 25℃. Re-sults The Cmax, Tmax, T1/2, and K of salidroside were 20. 24μg/mL, 0. 5 h, 2. 53 h, and 0. 27 in in-somnia rats, respectively;and the Cmax, Tmax of tyrosol were 0. 49μg/mL and 0. 75 h respectively in in-somnia rats. The maximum content ratio of tyrosol / salidroside was 3. 90/100, which was 12. 58 times higher than that in vitro. Conclusion Salidroside and tyrosol were the main components of salidroside drug into the blood and they exhibited a synergistic effect for absorption in the insomnia model rats. The bioavailability of drug was increased in insomnia model rats when compared with the health rats.