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Comparison of intramuscular and intravenous pharmacokinetics of ginsenosides in humans after dosing XueShuanTong, a lyophilized extract of Panax notoginseng roots

文献类型：期刊论文

作者Zhang, Hai-Yan1,5; Niu, Wei1; Olaleye, Olajide E.1; Du, Fei-Fei1; Wang, Feng-Qing1; Huang, Yu-Hong2; Yuan, Lei3; Li, Yan-Fen2; Liu, Guan-Ping4; Xu, Fang1
刊名JOURNAL OF ETHNOPHARMACOLOGY
出版日期2020-05-10
卷号253页码:7
ISSN号0378-8741
关键词Ginsenoside Pharmacokinetics Intramuscular Intravascular XueShuanTong Panay notoginseng roots Sanqi
DOI10.1016/j.jep.2020.112658
通讯作者Yang, Jun-Ling(yangjl@simm.ac.cn) ; Li, Chuan(chli@simm.ac.cn)
英文摘要Ethnopharmacological relevance: Many bioactive constituents of Chinese herbal medicines have poor oral bioavailability. Besides oral administration, herbal medicines in China are also prepared for parenteral administration. Unlike for intravenous route, little is known about the intramuscular pharmacokinetics of herbal compounds. To facilitate rational use of herbal medicine, it is important to better understand such intramuscular pharmacokinetics. Aim of the study: Bioactive constituents of XueShuanTong (a lyophilized extract of Panax notoginseng roots, extensively used in treatment of ischemic heart and cerebrovascular diseases) predominantly comprise ginsenosides Rb-1 and Rd of 20(S)-protopanaxadiol-type and ginsenosides Rg(1), and Re, and notoginsenoside R-1 of 20(S)-protopanaxatriol-type; these saponins are poorly absorbed from the gastrointestinal tract. This study aimed to compare intramuscular and intravenous pharmacokinetics of these ginsenosides after dosing XueShuanTong. Methods: Pharmacokinetics of ginsenosides was assessed in human volunteers receiving an intramuscular injection or 1.5-h intravenous infusion of XueShuanTong, both at 150 mg/person, and the plasma and urine samples were analyzed by liquid chromatography/mass spectrometry. Results: Like after intravenous administration, the unchanged saponins were the major circulating forms after intramuscular administration, while their metabolites were poorly detected. These ginsenosides exhibited intramuscular bioavailability of 100%-112%, relative to the respective intravenous data. Similar to that after intravenous infusion, the 20(S)-protopanaxadiol-type ginsenosides after the intramuscular injection exhibited notably longer terminal half-lives (46-106 h) than the 20(S)-protopanaxatriol-type ginsenosides (1.1-1.4 h). Conclusions: Intramuscular route might be an effective alternative to intravenous route for XueShuanTong, from the pharmacokinetic perspective.
WOS关键词ABSORPTION ; CONSTITUENTS ; INJECTION ; SAPONINS ; EXPOSURE ; SINGLE ; RD
资助项目National Key R&D Program of China[2018YFC1704500] ; National Natural Science Foundation of China[81673582] ; National Science and Technology Major Project of China Key New Drug Creation and Manufacturing Program[2017ZX09301012-006] ; National Science and Technology Major Project of China Key New Drug Creation and Manufacturing Program[2012ZX09101201-005] ; Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12050306]
WOS研究方向Plant Sciences ; Pharmacology & Pharmacy ; Integrative & Complementary Medicine
语种英语
出版者ELSEVIER IRELAND LTD
WOS记录号WOS:000523597600033
源URL[http://119.78.100.183/handle/2S10ELR8/280812]  
专题新药研究国家重点实验室
通讯作者Yang, Jun-Ling; Li, Chuan
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 501 Haike Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China
2.Tianjin Univ Tradit Chinese Med, Affiliated Hosp 2, Tianjin 300250, Peoples R China
3.Idorsia Shanghai Pharmaceut Co Ltd, Shanghai 201203, Peoples R China
4.Guangxi Wuzhou Pharmaceut Grp Co Ltd, Wuzhou 543000, Guangxi Zhuang, Peoples R China
5.Tianjin Univ Tradit Chinese Med, Grad Sch, Tianjin 300193, Peoples R China
推荐引用方式
GB/T 7714		 Zhang, Hai-Yan,Niu, Wei,Olaleye, Olajide E.,et al. Comparison of intramuscular and intravenous pharmacokinetics of ginsenosides in humans after dosing XueShuanTong, a lyophilized extract of Panax notoginseng roots[J]. JOURNAL OF ETHNOPHARMACOLOGY,2020,253:7.
APA Zhang, Hai-Yan.,Niu, Wei.,Olaleye, Olajide E..,Du, Fei-Fei.,Wang, Feng-Qing.,...&Li, Chuan.(2020).Comparison of intramuscular and intravenous pharmacokinetics of ginsenosides in humans after dosing XueShuanTong, a lyophilized extract of Panax notoginseng roots.JOURNAL OF ETHNOPHARMACOLOGY,253,7.
MLA Zhang, Hai-Yan,et al."Comparison of intramuscular and intravenous pharmacokinetics of ginsenosides in humans after dosing XueShuanTong, a lyophilized extract of Panax notoginseng roots".JOURNAL OF ETHNOPHARMACOLOGY 253(2020):7.

入库方式： OAI收割

来源：上海药物研究所

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