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Pharmacokinetics and disposition of monoterpene glycosides derived from Paeonia lactiflora roots (Chishao) after intravenous dosing of antiseptic XueBiJing injection in human subjects and rats

文献类型：期刊论文

作者Cheng, Chen5,6; Lin, Jia-zhen4,6; Li, Li6; Yang, Jun-ling6; Jia, Wei-wei6; Huang, Yu-hong3; Du, Fei-fei6; Wang, Feng-qing6; Li, Mei-juan6; Li, Yan-fen3
刊名ACTA PHARMACOLOGICA SINICA
出版日期2016-04
卷号37期号:4页码:530-544
关键词herbal injection XueBiJing Paeonia lactiflora roots Chishao monoterpene glycosides paeoniflorin pharmacokinetics disposition
ISSN号1671-4083
DOI10.1038/aps.2015.103
文献子类Article
英文摘要Aim: Monoterpene glycosides derived from Paeonia lactiflora roots (Chishao) are believed to be pharmacologically important for the antiseptic herbal injection XueBiJing. This study was designed to characterize the pharmacokinetics and disposition of monoterpene glycosides. Methods: Systemic exposure to Chishao monoterpene glycosides was assessed in human subjects receiving an intravenous infusion and multiple infusions of XueBiJing injection, followed by assessment of the pharmacokinetics of the major circulating compounds. Supportive rat studies were also performed. Membrane permeability and plasma-protein binding were assessed in vitro. Results: A total of 18 monoterpene glycosides were detected in XueBiJing injection (content levels, 0.001-2.47 mmol/L), and paeoniflorin accounted for 85.5% of the total dose of monoterpene glycosides detected. In human subjects, unchanged paeoniflorin exhibited considerable levels of systemic exposure with elimination half-lives of 1.2-1.3 h; no significant metabolite was detected. Oxypaeoniflorin and albiflorin exhibited low exposure levels, and the remaining minor monoterpene glycosides were negligible or undetected. Glomerular-filtration-based renal excretion was the major elimination pathway of paeoniflorin, which was poorly bound to plasma protein. In rats, the systemic exposure level of paeoniflorin increased proportionally as the dose was increased. Rat lung, heart, and liver exposure levels of paeoniflorin were lower than the plasma level, with the exception of the kidney level, which was 4.3-fold greater than the plasma level; brain penetration was limited by the poor membrane permeability. Conclusion: Due to its significant systemic exposure and appropriate pharmacokinetic profile, as well as previously reported antiseptic properties, paeoniflorin is a promising XueBiJing constituent of therapeutic importance.
WOS关键词HUMAN INTESTINAL BACTERIA ; SYSTEMIC EXPOSURE ; MASS-SPECTROMETRY ; PC12 CELLS ; MAJOR CONSTITUENTS ; IMPROVES SURVIVAL ; SEVERE SEPSIS ; SEPTIC SHOCK ; ALBA EXTRACT ; IN-VIVO
资助项目National Science & Technology Major Project of China 'Key New Drug Creation and Manufacturing Program'[2009ZX09304-002] ; National Science & Technology Major Project of China 'Key New Drug Creation and Manufacturing Program'[2011ZX09201-201-23] ; National Science Foundation of China for Distinguished Young Scholars[30925044] ; National Basic Research Program of China[2012CB518403] ; National Natural Science Foundation of China[81503345] ; China Postdoctoral Science Foundation[2014M560169]
WOS研究方向Chemistry ; Pharmacology & Pharmacy
语种英语
CSCD记录号CSCD:5676381
WOS记录号WOS:000373504400010
出版者ACTA PHARMACOLOGICA SINICA
源URL[http://119.78.100.183/handle/2S10ELR8/276091]  
专题上海药物代谢研究中心
科研与新药推进处
通讯作者Li, Chuan
作者单位1.Tianjin Chasesun Pharmaceut Co Ltd, Tianjin 301700, Peoples R China;
2.Fudan Univ, Shanghai Canc Ctr, Lab Phase Clin Trials 1, Shanghai 200032, Peoples R China
3.Tianjin Univ Tradit Chinese Med, Affiliated Hosp 2, Tianjin 300150, Peoples R China;
4.Univ Chinese Acad Sci, Shanghai 201203, Peoples R China;
5.China Acad Chinese Med Sci, Inst Chinese Materia Med, Beijing 100700, Peoples R China;
6.Chinese Acad Sci, Shanghai Inst Materia Med, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Cheng, Chen,Lin, Jia-zhen,Li, Li,et al. Pharmacokinetics and disposition of monoterpene glycosides derived from Paeonia lactiflora roots (Chishao) after intravenous dosing of antiseptic XueBiJing injection in human subjects and rats[J]. ACTA PHARMACOLOGICA SINICA,2016,37(4):530-544.
APA Cheng, Chen.,Lin, Jia-zhen.,Li, Li.,Yang, Jun-ling.,Jia, Wei-wei.,...&Li, Chuan.(2016).Pharmacokinetics and disposition of monoterpene glycosides derived from Paeonia lactiflora roots (Chishao) after intravenous dosing of antiseptic XueBiJing injection in human subjects and rats.ACTA PHARMACOLOGICA SINICA,37(4),530-544.
MLA Cheng, Chen,et al."Pharmacokinetics and disposition of monoterpene glycosides derived from Paeonia lactiflora roots (Chishao) after intravenous dosing of antiseptic XueBiJing injection in human subjects and rats".ACTA PHARMACOLOGICA SINICA 37.4(2016):530-544.

入库方式： OAI收割

来源：上海药物研究所

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