中国药理学通报2012，Vol.28Issue(7)：1005-1010,6.DOI:10.3969/j.issn.1001-1978.2012.07.028
黄芩苷及三七总皂苷配伍脑脊液药代动力学研究
Pharmacokinetic studies of baicalin and compatibility of baicalin-Panax Notoginsenosides in rat cerebrospinal fluid
摘要
Abstract
Aim To establish a HPLC-MS-MS method for the determination of baicalin in rat cerebrospinal fluid ( CSF ) and investigate the pharmacokinetics of ba -icalin and compatibility with Panax Notoginsenosides (PNS) . Methods After baicalin and compatibility of BA -PNS were given by intravenous administration , the concentration of baicalin in rat CSF was determined by HPLC-MS-MS. Chromatographic separation was performed on an Agilent Eclipse XDB-C18 (4. 6 mm ×150 mm, 5 μm) within 7 min,with the mobile gradi- entphase of acetonitrile ; 1 mmol · L-1 ammonium acetate ( containing 0. 1 % formic acid ) : 0. 1 % ammonia. The target ion transitions were m/z 445/269 ( baicalin [ M - 1 ] - ) and m/z 237/194 ( Carbamazepine [ M + 1] ). Results Calibration curves were linear over the concentration range from 5 ~ 200 μg · L for baicalin, with the recovery rates between 87. 15% ~ 92.73%. The pharmacokinetic parameters after a sin-gle dose of baicalin and baicalin -PNS were as follows; Cmax: (189. 67 ± 20. 13 ), (237. 00 ± 51. 86) μg ·L-l; AUCo0-1: (6612. 96 ± 1023. 65 ), (5466. 63 ± 267.06) μg · min · L-1; AUC0-∞ (6930.43 ±1060.41), (5682.13 ± 412. 79) μg · min · L-1; T1/2:(108. 84 ±45. 67), (102. 54 ±38. 37) min; CL:(15. 39 ±2. 60), (18.32 ±0.88) L· min-l · kg-1. Conclusion The method is proved to be accurate andconvenient to determine baicalin in rat cerebrospinal fluid. Baicalin can pass through blood -brain barrier and enter the cerebrospinal fluid. The pharmacokinetic parameters of baicalin have not changed , so PNS has no effect on the CSF pharmacokinetic of baicalin.关键词
黄芩苷/三七总皂苷/配伍/脑脊液/药代动力学/HPLC-MS/MSKey words
baicalin/ Panax Notoginsenosides / compatibility / cerebrospinal fluid/ pharmacokinetics/ HPLC-MS/MS分类
医药卫生引用本文复制引用
杨雁芳,李智,王磊,王永炎,张文生..黄芩苷及三七总皂苷配伍脑脊液药代动力学研究[J].中国药理学通报,2012,28(7):1005-1010,6.基金项目
国家自然科学基金资助项目(No 81072723) （No 81072723）
国家"重大新药创制"科技重大专项(No 2012ZX09103-201) （No 2012ZX09103-201）
北京市支持中央在京高校共建项目(No 403105) （No 403105）
