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采用液相色谱-串联质谱法研究大鼠体内重楼皂苷 II 和重楼皂苷 VII 的药代动力学特征。

Pharmacokinetics profiles of polyphyllin II and polyphyllin VII in rats by liquid chromatography with tandem mass spectrometry.

机构信息

Tianjin Key Laboratory for Modern Drug Delivery and High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China.

Tasly Academy, Tasly Holding Group Co. Ltd, Beichen District, Tianjin, China.

出版信息

Biomed Chromatogr. 2021 Jun;35(6):e5083. doi: 10.1002/bmc.5083. Epub 2021 Feb 17.

DOI:10.1002/bmc.5083
PMID:33544400
Abstract

Polyphyllin II (PII) and polyphyllin VII (PVII) are the main active ingredients in Paris Polyphylla with an excellent antitumor effect in vitro and in vivo. In this study, a rapid and precise LC-MS/MS method was developed and validated for the separation and simultaneous determination of PII and PVII in rat plasma, tissues, feces and urine using ginsenoside Rg3 as the internal standard. Positive linearity ranged from 1 to 1,000 ng/ml in samples. At the same time, intra- and inter-day precisions were in range of 1.8-12.0%. The accuracy ranged from 95.9 to 100.8%. Mean extraction recoveries of PII and PVII ranged from 86.6 to 96.4%. The analytical method has been successfully applied to the pharmacokinetic studies of PII and PVII in rats after their i.v. administration. After entering systemic circulation, PII and PVII were rapidly distributed in organs, mainly including liver, lung and spleen. Their elimination rate was slow. All of these data provided a theoretical basis for the application of PII and PVII in the treatment of liver- and lung-related diseases.

摘要

重楼皂苷 II(PII)和重楼皂苷 VII(PVII)是七叶一枝花中的主要活性成分,具有良好的体外和体内抗肿瘤作用。本研究建立并验证了一种快速、准确的 LC-MS/MS 法,用于同时分离和测定大鼠血浆、组织、粪便和尿液中 PII 和 PVII 的含量,以人参皂苷 Rg3 为内标。样品中 PII 和 PVII 的线性范围为 11000ng/ml。同时,日内和日间精密度均在 1.8%12.0%范围内。准确度在 95.9%100.8%之间。PII 和 PVII 的平均提取回收率在 86.6%96.4%之间。该分析方法已成功应用于 PII 和 PVII 静脉注射给药后在大鼠体内的药代动力学研究。进入体循环后,PII 和 PVII 迅速分布于各器官,主要包括肝、肺和脾。其消除率较慢。所有这些数据为 PII 和 PVII 在治疗肝肺相关疾病中的应用提供了理论依据。

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