| Abstract: | 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 1–1000 ng/mL with a correlation coefficient > 0.99. The lower limit of quantification was 1 ng/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 25 mg/kg of AA22, the mean peak plasma concentration of AA22 was 2114 ± 362 ng/mL at 6 h. The area under the plasma concentration–time curve was 196,098 ± 69,375 h ng/mL, and the elimination half‐life was 8.7 ± 2.2 h. |
