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一种用于定量大鼠血浆中淫羊藿苷A的简单且选择性的液相色谱-串联质谱法及其在药代动力学研究中的应用。

A simple and selective LC-MS/MS method for quantification of ikarisoside A in rat plasma and its application to a pharmacokinetic study.

作者信息

Cong Yue, Wang Rui, Zhang Chen, Lin Hai

机构信息

Department of Ocular Fundus Disease, the Second Hospital of Jilin University, Changchun, China.

Department of Hematology, the First Hospital of Jilin University, Changchun, China.

出版信息

Biomed Chromatogr. 2018 Aug;32(8):e4245. doi: 10.1002/bmc.4245. Epub 2018 Apr 23.

DOI:10.1002/bmc.4245
PMID:29575004
Abstract

Ikarisoside A is a natural flavonoid isolated from Epimedium plants. To further evaluate its medicinal potential, a sensitive and robust LC-MS/MS method was developed and validated for the assay of ikarisoside A in rat plasma. Orientin was used as an internal standard. The electrospray ionization was operated in its negative ion mode while ikarisoside A and IS were measured by selected reaction monitoring using precursor-to-product ion transitions of m/z 499.1 → 353.0 and m/z 446.9 → 327.6, respectively. This LC-MS/MS method had good sensitivity (LLOQ = 1.5 ng/mL), accuracy (both intra- and inter-day RE ≤ ±11.9%) and precision (both intra- and inter-day RSD ≤8.5%). The pharmacokinetics of ikarisoside A was subsequently profiled in Sprague-Dawley rats. Following oral administration (35 mg/kg), ikarisoside A reached maximum plasma concentration (C , 207.6 ± 96.7 ng/mL) attained at 1.10 ± 0.42 h. Following oral administration, the clearance and terminal half-life were 42.9 ± 26.5 L/h/kg and 3.15 ± 0.80 h by oral route, respectively.

摘要

淫羊藿苷A是从淫羊藿属植物中分离得到的一种天然黄酮类化合物。为了进一步评估其药用潜力,建立并验证了一种灵敏且可靠的LC-MS/MS方法,用于测定大鼠血浆中的淫羊藿苷A。异荭草苷用作内标。电喷雾电离在负离子模式下运行,而淫羊藿苷A和内标分别通过选择反应监测,采用m/z 499.1 → 353.0和m/z 446.9 → 327.6的母离子到子离子跃迁进行测定。该LC-MS/MS方法具有良好的灵敏度(LLOQ = 1.5 ng/mL)、准确度(日内和日间RE均≤ ±11.9%)和精密度(日内和日间RSD均≤8.5%)。随后在Sprague-Dawley大鼠中研究了淫羊藿苷A的药代动力学。口服给药(35 mg/kg)后,淫羊藿苷A在1.10 ± 0.42小时达到最大血浆浓度(Cmax,207.6 ± 96.7 ng/mL)。口服给药后,清除率和末端半衰期分别为42.9 ± 26.5 L/h/kg和3.15 ± 0.80小时。

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