血塞通（三七冻干根提取物）给药后人参皂苷在人体内肌内和静脉药代动力学比较。
Comparison of intramuscular and intravenous pharmacokinetics of ginsenosides in humans after dosing XueShuanTong, a lyophilized extract of Panax notoginseng roots.
机构信息
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.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
出版信息
J Ethnopharmacol. 2020 May 10;253:112658. doi: 10.1016/j.jep.2020.112658. Epub 2020 Feb 6.
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 and Rd of 20(S)-protopanaxadiol-type and ginsenosides Rg, and Re, and notoginsenoside R 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.
民族药理学相关性
许多中药的生物活性成分的口服生物利用度较差。除了口服给药外，中国的草药还可用于肠胃外给药。与静脉途径不同，人们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，了解这种肌肉内药代动力学非常重要。
研究目的
血塞通（一种广泛用于治疗缺血性心脏和脑血管疾病的三七根冻干提取物）的生物活性成分主要包括 20(S)-原人参二醇型的人参皂苷 Rb 和 Rd 以及人参皂苷 Rg、Re 和三七皂苷 R，这些皂苷类化合物从胃肠道吸收较差。本研究旨在比较血塞通给药后这些皂苷类化合物的肌肉内和静脉内药代动力学。
方法
通过液相色谱/质谱法分析接受肌肉内注射或 1.5 小时静脉输注血塞通（均为 150mg/人）的志愿者的血浆和尿液样本，评估皂苷类化合物的药代动力学。
结果
与静脉给药后一样，肌肉内给药后未改变的皂苷类化合物是主要的循环形式，而其代谢产物则难以检测到。这些人参皂苷类化合物的肌肉内生物利用度为 100%-112%，相对于各自的静脉数据。与静脉输注后相似，肌肉内注射后 20(S)-原人参二醇型人参皂苷类化合物的半衰期明显较长（46-106 小时），而 20(S)-原人参三醇型人参皂苷类化合物的半衰期较短（1.1-1.4 小时）。
结论
从药代动力学角度来看，肌肉内途径可能是血塞通的一种有效替代静脉途径。
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