1. Academic Validation
  2. Determination of Apremilast in Rat Plasma by UPLC-MS-MS and Its Application to a Pharmacokinetic Study

Determination of Apremilast in Rat Plasma by UPLC-MS-MS and Its Application to a Pharmacokinetic Study

  • J Chromatogr Sci. 2016 Sep;54(8):1336-40. doi: 10.1093/chromsci/bmw072.
Lian-Guo Chen 1 Zhe Wang 2 Shujun Wang 1 Tao Li 3 Yongyang Pan 3 Xixi Lai 4
Affiliations

Affiliations

  • 1 Wenzhou People's Hospital, Wenzhou 325000, China.
  • 2 The Second Affiliated Hospital & Yuying Children's Hospital of Wenzhou Medical University, Wenzhou 325027, China.
  • 3 Medical College of Henan University of Science and Technology, Luoyang 471003, China.
  • 4 The First Affiliated Hospital of Wenzhou Medical University, Wenzhou 325000, China laixixi-001@163.com.
Abstract

A rapid, sensitive and selective ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS-MS) was developed and validated for the determination and pharmacokinetic investigation of apremilast in rat plasma. Sample preparation was accomplished through a simple one-step deproteinization procedure with 0.2 mL of acetonitrile to a 0.1 mL plasma sample. Plasma samples were separated by UPLC on an Acquity UPLC BEH C18 column using a mobile phase consisting of acetonitrile-0.1% formic acid in water with gradient elution. The total run time was 3.0 min, and the elution of apremilast was at 1.27 min. The detection was performed on a triple quadrupole tandem mass spectrometer in the multiple reaction-monitoring mode using the respective transitions m/z 461.3 → 257.1 for apremilast and m/z 237.2 → 194.2 for carbamazepine (internal standard). The calibration curve was linear over the range of 0.1-100 ng/mL with a lower limit of quantitation of 0.1 ng/mL. The mean recovery of apremilast in plasma was in the range of 83.2-87.5%. Both intraday and interday precision were <9.6%. This method was successfully applied in the pharmacokinetic study after oral administration of 6.0 mg/kg apremilast in rats.

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