College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan, PR China.
Department of Pharmacy, Jinan Maternity and Child Care Hospital, Jinan, PR China.
Pharm Biol. 2021 Dec;59(1):525-531. doi: 10.1080/13880209.2021.1913188.
Thonningianin A is an ellagitannin substance and displays multiple pharmacological activities.
This study investigated the pharmacokinetic characteristics of thonningianin A after oral administration in rats using a fully validated liquid chromatography tandem mass spectrometry (LC-MS/MS) method.
A sensitive and selective LC-MS/MS assay was developed for quantifying thonningianin A. Eighteen Wistar rats were randomly divided into three groups ( = 6), which were given at a single dose of 10, 20, or 40 mg/kg thonningianin A by gavage. Blood samples (200 µL) were collected from the orbit vein at designated time points and analyzed using the LC-MS/MS method to measure the levels of thonningianin A.
Thonningianin A and internal standard (IS) were eluted at 1.5 and ∼3.0 min, respectively. The selected reaction mode transitions monitored were 873.2 > 300.3 and 819.3 > 610.6 for thonningianin A and the IS, respectively. The calibration range was 10-1200 ng/mL. The intra- and the inter-day accuracy and precision met the acceptance criteria. No carryover and matrix effect were observed. The plasma concentrations of thonningianin A increased rapidly after oral administration of three dosages and reached the mean peak concentrations () within 0.61-0.83 h. Meanwhile, AUC/AUC of the three dosage groups was more than 89.0% (10 mg/kg), 95.7% (20 mg/kg), and 97.0% (40 mg/kg).
The present method is the first report in terms of the simple precipitation procedure, high sensitivity, and high-throughput efficiency. This validated assay was successfully applied to determine the pharmacokinetic behaviours of thonningianin A in rats. This study should be helpful for providing references for understanding the action mechanism and further application of .
Thonningianin A 是一种鞣花单宁物质，具有多种药理活性。
本研究采用完全验证的液相色谱-串联质谱（LC-MS/MS）法研究 Thonningianin A 灌胃给药后的药代动力学特征。
建立了一种灵敏、选择性的 LC-MS/MS 测定方法用于定量 Thonningianin A。18 只 Wistar 大鼠随机分为三组（每组 6 只），分别灌胃给予 10、20 或 40mg/kg Thonningianin A。在指定时间点从眶静脉采集 200µL 血样，采用 LC-MS/MS 法测定 Thonningianin A 的浓度。
Thonningianin A 和内标（IS）分别在 1.5 和 ∼3.0min 洗脱。监测的选择反应模式转换为 Thonningianin A 和 IS 的 873.2 > 300.3 和 819.3 > 610.6。校准范围为 10-1200ng/mL。日内和日间精密度和准确度均符合要求。未观察到拖尾和基质效应。三种剂量给药后，Thonningianin A 的血浆浓度迅速升高，在 0.61-0.83h 内达到平均峰浓度（）。同时，三个剂量组的 AUC/AUC 均大于 89.0%（10mg/kg）、95.7%（20mg/kg）和 97.0%（40mg/kg）。
本方法是首次报道采用简单沉淀法、高灵敏度和高通量效率。该验证后的方法成功应用于测定大鼠体内 Thonningianin A 的药代动力学行为。本研究有助于为了解其作用机制和进一步应用提供参考。
