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Pharmacokinetics, bioavailability, and metabolism of Notoginsenoside Fc in rats by liquid chromatography/electrospray ionization tandem mass spectrometry
He, Chunyong2,4; Li, Jia2,4; Xu, Niusheng1; Wang, Rufeng2,4; Li, Zeyun2; Yang, Li2,3; Wang, Zhengtao2,3
刊名Journal of pharmaceutical and biomedical analysis
2015-05-10
卷号109页码:150-7
ISSN号1873-264X
DOI10.1016/j.jpba.2015.02.038
文献子类Article
英文摘要Notoginsenoside Fc (NGFc) is a protopanaxadiol-type (PPD-type) saponin from Panax notoginseng, which has perfect anti-platelet aggregatory effect. However, its pharmacokinetics and metabolism in vivo remain unknown. In this study, a simple and sensitive liquid chromatography/electrospray ionization tandem mass spectrometry (LC-MS/MS) method was first developed for the determination of NGFc in rat plasma. After methanol-mediated protein precipitation, separation was achieved on a C18 column with MS detection operated in negative SRM mode at m/z 604.56→m/z 783.90 and m/z 799.93→m/z 637.64 for NGFc and IS, respectively. The assay was linear over the concentration range (r>0.995) with the LLOQ of 0.002μg/ml. The intra- and inter-day precisions (R.S.D.) were 2.45-12.36% and 3.67-14.22%, respectively; whereas accuracy ranged from (R.R.) 93.90% to 99.41%. The extraction recovery, stability, and matrix effect were within the acceptable limits. The validated LC-MS/MS method was successfully applied to the pre-clinical pharmacokinetic studies of NGFc in rat. After oral and intravenous administration, NGFc showed dose-independent pharmacokinetic behaviors with a t1/2 of >22h and its oral bioavailability was 0.10-0.14%. In addition, a total of 10 metabolites were detected and structurally characterized by UPLC-Q/TOF-MS technique, which suggested that deglycosylation was the major metabolic pathway for NGFc in rats.
语种英语
内容类型期刊论文
源URL[http://119.78.100.183/handle/2S10ELR8/266553]  
专题中国科学院上海药物研究所
通讯作者Yang, Li; Wang, Zhengtao
作者单位1.Thermo Fisher Scientific, Chromatography and Mass spectrometry Division, Shanghai 201206, China;
2.The MOE Key Laboratory for Standardization of Chinese Medicines and The SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China;
3.Shanghai R&D Centre for Standardization of Chinese Medicines, Shanghai 201203, China
4.Shanghai R&D Centre for Standardization of Chinese Medicines, Shanghai 201203, China;
推荐引用方式
GB/T 7714
He, Chunyong,Li, Jia,Xu, Niusheng,et al. Pharmacokinetics, bioavailability, and metabolism of Notoginsenoside Fc in rats by liquid chromatography/electrospray ionization tandem mass spectrometry[J]. Journal of pharmaceutical and biomedical analysis,2015,109:150-7.
APA He, Chunyong.,Li, Jia.,Xu, Niusheng.,Wang, Rufeng.,Li, Zeyun.,...&Wang, Zhengtao.(2015).Pharmacokinetics, bioavailability, and metabolism of Notoginsenoside Fc in rats by liquid chromatography/electrospray ionization tandem mass spectrometry.Journal of pharmaceutical and biomedical analysis,109,150-7.
MLA He, Chunyong,et al."Pharmacokinetics, bioavailability, and metabolism of Notoginsenoside Fc in rats by liquid chromatography/electrospray ionization tandem mass spectrometry".Journal of pharmaceutical and biomedical analysis 109(2015):150-7.
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