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<p>Betulinic acid (BA) is a plant-derived pentacyclic triterpenoid with various biological properties. Studies have identified that the deprotonated molecular ion of BA could not generate any product ions by an LC-ESI/MS/MS. In this study, BA reacted with <i>p</i>-toluenesulfonyl isocyanate (PTSI) to produce an ionizable and fragmentary derivative for LC-ESI/MS/MS detection in a negative mode. Thus, we developed and validated an UPLC-ESI/MS/MS method to quantitate BA in rat plasma. The calibration curve was linear over the concentration range of 5–1280 ng/mL for BA, with a lower limit of detection of 1 ng/ml. This validated method was successfully applied to a pharmacokinetic study of BA in rat plasma after intravenous administration of BA.</p>

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A UPLC-ESI/MS/MS Method for the Determination of Betulinic Acid and Its Application to the Pharmacokinetic Study in Rat Plasma

  • 期刊论文

  • 发表日期：

    2025年6月1日

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  • Xinxin Liu,
  • Qiang Zhang,
  • Zijia Wang,
  • Yonghong Jiang,
  • Yang Wang,
  • Huixi Zou,
  • Xiufeng Yan,
  • Zhiwei Hu,
  • Ziming Wang

摘要

Betulinic acid (BA) is a plant-derived pentacyclic triterpenoid with various biological properties. Studies have identified that the deprotonated molecular ion of BA could not generate any product ions by an LC-ESI/MS/MS. In this study, BA reacted with p-toluenesulfonyl isocyanate (PTSI) to produce an ionizable and fragmentary derivative for LC-ESI/MS/MS detection in a negative mode. Thus, we developed and validated an UPLC-ESI/MS/MS method to quantitate BA in rat plasma. The calibration curve was linear over the concentration range of 5–1280 ng/mL for BA, with a lower limit of detection of 1 ng/ml. This validated method was successfully applied to a pharmacokinetic study of BA in rat plasma after intravenous administration of BA.