文献类型：期刊文献

英文题名：Development and validation of a UPLC-MS/MS method for determination of Sarsasapogenin-AA22 in rat plasma and its application to a pharmacokinetic study

作者：Pei, Lixia[1];Ge, Songlan[1,2];Ye, Yiyi[1];Jiang, Ziwei[1];Liang, Xiaoqiang[1];Zhao, Wenshu[1];Ma, Lei[2]

机构：[1]Shanghai Univ Tradit Chinese Med, Longhua Hosp, Shanghai, Peoples R China;[2]East China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Sch Pharm, Shanghai, Peoples R China

年份：2018

卷号：32

期号：10

外文期刊名：BIOMEDICAL CHROMATOGRAPHY

收录：;EI(收录号：20232414233866);WOS:【SCI-EXPANDED(收录号:WOS:000445175600012)】；

基金：Three-year plan of action (2018-2020) to further accelerate the development of Chinese Medicine in Shanghai; National Natural Science Foundation of China, Grant/Award Number: 81303187; Science and Technology Innovation Project of Longhua Hospital, Grant/Award Number: KY1736

语种：英文

外文关键词：diosgenin; LC; MS; MS; pharmacokinetics; sarsasapogenin-AA22

摘要：A sarsasapogenin derivative, sarsasapogenin-AA22 (AA22), with cyclobutylamine at the 3-hydroxyl position of sarsasapogenin, has great neuroprotective activity in PC12 cells and NO production inhibitory activity in RAW264.7 cell lines. A method was developed to determine AA22 in rat plasma which was further applied to evaluate the pharmacokinetics of AA22 after taking a single dose of AA22. Liquid chromatography tandem mass spectrometry was used in the method, while diosgenin was used as internal standard. A simple protein precipitation based on acetonitrile was utilized. A simple sample cleanup promoted the throughput of the method considerably. The method was validated over the range of 1-1000ng/mL with a correlation coefficient>0.99. The lower limit of quantification was 1ng/mL for AA22 in plasma. Intra- and inter-day accuracies for AA22 were 92-111 and 100-103%, respectively, and the inter-day precision was <15%. After a single oral dose of 25mg/kg of AA22, the mean peak plasma concentration of AA22 was 2114 +/- 362ng/mL at 6h. The area under the plasma concentration-time curve was 196,098 +/- 69,375hng/mL, and the elimination half-life was 8.7 +/- 2.2h.