Comparison of intramuscular and intravenous pharmacokinetics of ginsenosides in humans after dosing XueShuanTong, a lyophilized extract of Panax notoginseng roots.
Comparison of intramuscular and intravenous pharmacokinetics of ginsenosides in humans after dosing XueShuanTong, a lyophilized extract of Panax notoginseng roots.
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服用三七冻干提取物血栓通后人参皂苷在人体肌肉注射和静脉注射药代动力学的比较。
DOI：
10.1016/j.jep.2020.112658
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发表时间：
2020-02
期刊：
影响因子：
--
通讯作者：
Li C.
中科院分区：
文献类型：
--
作者：
Zhang H-Y.;Niu W.;Olaleye O.E.;Du F-F.;Wang F-Q.;Huang Y-H.;Yuan L.;Li Y-F.;Liu G-P.;Xu F.;Yang J-L.;Li C.
民族药理学相关性中药中许多生物活性成分的口服生物利用度较差。在中国，除了口服外，草药也可配制成肠外给药。与静脉途径不同，对草药化合物的肌肉内药代动力学知之甚少。为了促进草药的合理使用，更好地了解这种肌肉内药代动力学是很重要的。研究目的：血栓通（三七根的冻干提取物，广泛用于缺血性心脑血管病的治疗）的生物活性成分主要有20(S)-原人参二醇型人参皂苷Rg1、Rd和20(S)-原人参二醇型人参皂苷Rg1、Re和20(S)-原人参二醇型三七皂苷r1；这些皂苷很难被胃肠道吸收。本研究旨在比较血栓通给药后人参皂苷的肌内和静脉药代动力学。方法采用血栓通150 mg/人肌肉注射和1.5 h静脉滴注两种剂量下人参皂苷的药代动力学方法，采用液相色谱/质谱法对血浆和尿液进行分析。结果与静脉给药一样，肌内给药后，未改变的皂苷是主要的循环形式，其代谢产物检测较差。相对于静脉注射数据，这些人参皂苷的肌肉内生物利用度为100%-112%。与静脉输注相似，肌注后20(S)-原人参二醇型人参皂苷的终末半衰期（46 ~ 106 h）明显高于20(S)-原人参二醇型人参皂苷（1.1 ~ 1.4 h）。结论从药动学角度看，肌内给药可替代静脉给药。
Ethnopharmacological relevanceMany 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 studyBioactive constituents of XueShuanTong (a lyophilized extract ofPanax notoginsengroots, extensively used in treatment of ischemic heart and cerebrovascular diseases) predominantly comprise ginsenosides Rb1and Rd of 20(S)-protopanaxadiol-type and ginsenosides Rg1, and Re, and notoginsenoside R1of 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.MethodsPharmacokinetics 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.ResultsLike 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).ConclusionsIntramuscular route might be an effective alternative to intravenous route for XueShuanTong, from the pharmacokinetic perspective.
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影响因子：
4.4
作者：
Guo, Hong;Adah, Dickson;Hu, Limin
通讯作者：
Hu, Limin
影响因子：
6.6
作者：
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通讯作者：
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Xueshuantong对瞬态和永久性大鼠脑缺血模型注射（冻干）的神经保护作用。
DOI：
10.1155/2015/134685
发表时间：
2015
期刊：
Evidence-based complementary and alternative medicine : eCAM
影响因子：
--
作者：
Wang X;Wang S;Wang J;Guo H;Dong Z;Chai L;Hu L;Zhang Y;Wang H;Chen L
通讯作者：
Chen L
DOI：
10.1002/0471462993
发表时间：
2002-04
期刊：
--
影响因子：
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作者：
S. Gad
通讯作者：
S. Gad
DOI：
10.1002/9780470571224.pse038
发表时间：
2010-03
期刊：
Journal of Physics: Conference Series
影响因子：
--
作者：
M. Bermejo;I. González-Álvarez
通讯作者：
M. Bermejo;I. González-Álvarez