基于LC-MS/MS技术研究黄芩苷在脑、血微透析探针体内外回收率  

Analysis on microdialysis probe recovery of baicalin in vitro and in vivo based on LC-MS/MS

作　　者：陈腾飞[1] 刘建勋[1] 张颖[1] 林力[1] 宋文婷[1] 姚明江[1] 

机构地区：[1]中国中医科学院西苑医院基础医学研究所,中药药理北京市重点实验室,北京100091

出　　处：《中国中药杂志》2017年第11期2168-2174,共7页China Journal of Chinese Materia Medica

基　　金：国家重点基础研究发展计划(973)项目(2015-CB554405);中国中医科学院科技创新团队项目(YS1303);国家自然科学基金面上项目(81673587)

摘　　要：为进一步研究黄芩苷的入脑行为及脑细胞间液药代动力学,对黄芩苷在脑、血微透析探针的体内外回收率及其稳定性进行了研究。采用LC-MS/MS测定脑、血微透析液中黄芩苷的浓度,计算探针回收率;分别采用增量法、减量法考察不同流速(0.50,1.0,1.5,2.0,3.0μL·min^(-1))对探针体外回收率的影响;采用增量法考察不同浓度(50.00,200.0,500.0,1 000μg·L^(-1))、探针使用次数(0,1,2)对体外回收率的影响;采用减量法考察在大鼠体内探针回收率稳定性及流速对回收率的影响,并与体外结果进行比较。在同一浓度下,黄芩苷的脑、血探针体外回收率均随着流速的增加而降低;在同一流速下,探针回收率与黄芩苷的浓度无关;使用后并经过恢复处理的脑、血探针,在使用2次后,探针的回收率没有明显的变化;增量法和减量法所测得的体外回收率基本相同;减量法测得的体内回收率与体外结果相近,且脑、血探针体内回收率在10 h内的稳定性均良好。研究结果表明减量法能够作为研究黄芩苷体内回收率的测定方法,微透析技术能够用于黄芩苷在脑细胞间液药代动力学、血液药代动力学的同步研究。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 baiealin 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 baiealin 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 phar-macokinetic study of baicalin, and can be used to study probe recovery in vivo at the same time.

关 键 词：黄芩苷 LC-MS/MS 微透析 回收率 脑细胞间液 

分 类 号：R285[医药卫生—中药学]