Department of Pharmacology, School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing, China.
J Pharm Pharmacol. 2010 Mar;62(3):360-7. doi: 10.1211/jpp.62.03.0011.
The aim was to investigate the pharmacokinetic interaction between puerarin and edaravone, and the effect of borneol on the brain distribution kinetics of puerarin in rats.
A reversed-phase high performance liquid chromatography method was developed and validated for the simultaneous determination of puerarin and edaravone in rat plasma. The detection method was successfully applied to compare the pharmacokinetic interaction and brain distribution kinetics of puerarin and edaravone using in-situ microdialysis sampling in rats after intravenous administration and co-administration with a single dose.
The method gave good linearity and no endogenous material interfered with the two target compounds and internal standard peaks. The limit of detection of puerarin and edaravone was 0.03 and 0.05 microg/ml, respectively. The average recovery of the two compounds from rat plasma was >94%. The precision of the test was determined to be within 10%. The combination of puerarin and edaravone reduced drug elimination rates, gave a wider distribution, and the disposition of both drugs in rats was optimized. The distribution of puerarin in brain tissues was significantly increased and its elimination was noticeably slower with borneol pretreatment.
The results provide important information for the improved combined use of puerarin and edaravone with borneol pretreatment in clinical practice.
研究葛根素与依达拉奉的药代动力学相互作用，以及冰片对葛根素在大鼠脑内分布动力学的影响。
建立并验证了一种反相高效液相色谱法，用于同时测定大鼠血浆中的葛根素和依达拉奉。该检测方法成功应用于大鼠静脉注射后原位微透析采样，比较了单剂量给药和联合给药时葛根素和依达拉奉的药代动力学相互作用和脑内分布动力学。
该方法具有良好的线性，无内源性物质干扰两种目标化合物和内标峰。葛根素和依达拉奉的检测限分别为 0.03 和 0.05 microg/ml。两种化合物从大鼠血浆中的平均回收率均大于 94%。该试验的精密度确定在 10%以内。葛根素和依达拉奉的联合使用降低了药物消除率，使分布更广泛，优化了两种药物在大鼠体内的处置。冰片预处理可显著增加葛根素在脑组织中的分布，明显减慢其消除速度。
研究结果为临床实践中葛根素与依达拉奉联合使用并配合冰片预处理提供了重要信息。
