Format

Send to

Choose Destination
J Ethnopharmacol. 2020 Feb 6;253:112658. doi: 10.1016/j.jep.2020.112658. [Epub ahead of print]

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

Author information

1
Graduate School, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China. Electronic address: 791750458@qq.com.
2
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China. Electronic address: niuwei@simm.ac.cn.
3
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China. Electronic address: oeolaleye@simm.ac.cn.
4
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China. Electronic address: dufeifei@simm.ac.cn.
5
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China. Electronic address: wfq@simm.ac.cn.
6
Second Affiliated Hospital, Tianjin University of Traditional Chinese Medicine, Tianjin, 300250, China. Electronic address: hyh101@126.com.
7
Idorsia (Shanghai) Pharmaceuticals Co., Ltd., Shanghai, 201203, China. Electronic address: lei.yuan@idorsia.com.
8
Second Affiliated Hospital, Tianjin University of Traditional Chinese Medicine, Tianjin, 300250, China. Electronic address: liyanfen2008@163.com.
9
Guangxi Wuzhou Pharmaceutical (Group) Co., Ltd, Wuzhou, Guangxi Zhuang Autonomous Region, 543000, China. Electronic address: lgp3808@126.com.
10
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China. Electronic address: fangxu@simm.ac.cn.
11
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China. Electronic address: yangjl@simm.ac.cn.
12
Graduate School, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China. Electronic address: chli@simm.ac.cn.

Abstract

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 Rb1 and Rd of 20(S)-protopanaxadiol-type and ginsenosides Rg1, and Re, and notoginsenoside R1 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.

KEYWORDS:

Ginsenoside; Intramuscular; Intravascular; Panax notoginseng roots; Pharmacokinetics; Sanqi; XueShuanTong

PMID:
32035876
DOI:
10.1016/j.jep.2020.112658

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center