Chen Teng-Fei, Liu Jian-Xun, Zhang Ying, Lin Li, Song Wen-Ting, Yao Ming-Jiang
Institute of Basic Medical Sciences, Xiyuan Hospital, China Academy of Chinese Medical Sciences, Beijing Key Laboratory of Pharmacology of Chinese Material Medica, Beijing 100091, China.
Zhongguo Zhong Yao Za Zhi. 2017 Jun;42(11):2168-2174. doi: 10.19540/j.cnki.cjcmm.20170307.001.
To further study the brain behavior and the pharmacokinetics of baicalin in intercellular fluid of brain, and study the recovery rate and stability of brain and blood microdialysis probe of baicalin in vitro and in vivo. The concentration of baicalin in brain and blood microdialysates was determined by LC-MS/MS and the probe recovery for baicalin was calculated. The effects of different flow rates (0.50, 1.0, 1.5, 2.0，3.0 μL•min⁻¹) on recovery in vitro were determined by incremental method and decrement method. The effects of different drug concentrations (50.00, 200.0, 500.0, 1 000 μg•L⁻¹) and using times (0, 1, 2) on recovery in vitro were determined by incremental method. The probe recovery stability and effect of flow rate on recovery in vivo were determined by decrement method, and its results were compared with those in in vitro trial. The in vitro recovery of brain and blood probe of baicalin was decreased with the increase of flow rate under the same concentration; and at the same flow rate, different concentrations of baicalin had little influence on the recovery. The probe which had been used for 2 times showed no obvious change in probe recovery by syringe with 2% heparin sodium and ultrapure water successively. In vitro recovery rates obtained by incremental method and decrement method were approximately equal under the same condition, and the in vivo recovery determined by decrement method was similar with the in vitro results and they were showed a good stability within 10 h. The results showed that decrement method can be used for pharmacokinetic study of baicalin, and can be used to study probe recovery in vivo at the same time.
为进一步研究黄芩苷在脑间质液中的脑内行为及药代动力学，以及黄芩苷脑和血液微透析探针在体外和体内的回收率及稳定性。采用液相色谱-串联质谱法测定脑和血液微透析液中黄芩苷的浓度，并计算黄芩苷的探针回收率。采用增量法和减量法测定不同流速（0.50、1.0、1.5、2.0、3.0 μL•min⁻¹）对体外回收率的影响。采用增量法测定不同药物浓度（50.00、200.0、500.0、1 000 μg•L⁻¹）及使用次数（0、1、2次）对体外回收率的影响。采用减量法测定探针回收率稳定性及流速对体内回收率的影响，并与体外试验结果进行比较。相同浓度下，黄芩苷脑和血液探针的体外回收率随流速增加而降低；相同流速下，不同浓度黄芩苷对回收率影响较小。经2%肝素钠和超纯水先后冲洗的探针使用2次后，探针回收率无明显变化。相同条件下，增量法和减量法获得的体外回收率大致相等，减量法测定的体内回收率与体外结果相似，且在10 h内具有良好的稳定性。结果表明，减量法可用于黄芩苷的药代动力学研究，同时可用于研究体内探针回收率。
