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

doi:10.1016/j.jep.2020.112658

	Comparison of intramuscular and intravenous pharmacokinetics of ginsenosides in humans after dosing XueShuanTong, a lyophilized extract of Panax notoginseng roots
	Zhang, Hai-Yan 1,2; Niu, Wei 2; Olaleye, Olajide E.2; Du, Fei-Fei 2; Wang, Feng-Qing 2; Huang, Yu-Hong 3; Yuan, Lei 4; Li, Yan-Fen 3; Liu, Guan-Ping 5; Xu, Fang 2
刊名	JOURNAL OF ETHNOPHARMACOLOGY
	2020-05-10
卷号	253 页码:7
关键词	Ginsenoside Pharmacokinetics Intramuscular Intravascular XueShuanTong Panay notoginseng roots Sanqi
ISSN号	0378-8741
DOI	10.1016/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.
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关键词	ABSORPTION ; CONSTITUENTS ; INJECTION ; SAPONINS ; EXPOSURE ; SINGLE ; RD
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
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/280812]
专题	中国科学院上海药物研究所
通讯作者	Yang, Jun-Ling; Li, Chuan
作者单位	1.Tianjin Univ Tradit Chinese Med, Grad Sch, Tianjin 300193, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 501 Haike Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China 3.Tianjin Univ Tradit Chinese Med, Affiliated Hosp 2, Tianjin 300250, Peoples R China 4.Idorsia Shanghai Pharmaceut Co Ltd, Shanghai 201203, Peoples R China 5.Guangxi Wuzhou Pharmaceut Grp Co Ltd, Wuzhou 543000, Guangxi Zhuang, 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.