LC-coupled ESI MS for quantification of miltefosine in human and hamster plasma

Bioanalysis. 2016 Mar;8(6):533-45. doi: 10.4155/bio.16.7. Epub 2016 Feb 26.

Abstract

Background: Leishmaniasis, a fatal parasitic disease, is the second largest parasitic killer in the world and miltefosine is the first and only oral drug available for its treatment.

Results: A rapid, sensitive and simple LC-MS/MS method for miltefosine quantification in hamster and human plasma was developed and validated over the range of 2.5-400 ng/ml. The mass spectrometric detection of the drug was carried out in multiple reaction monitoring mode (m/z 408.1→125.1) using an electrospray positive ionization. The protein precipitation method was employed for sample (50 µl) cleanup.

Conclusion: The proposed method provided accurate and precise high-throughput quantification of miltefosine in plasma and was successfully applied to its oral PK study in Golden Syrian hamsters.

Keywords: HPLC–MS/MS; leishmaniasis; miltefosine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adult
  • Animals
  • Antiprotozoal Agents / blood*
  • Antiprotozoal Agents / pharmacokinetics
  • Antiprotozoal Agents / therapeutic use
  • Chromatography, High Pressure Liquid* / standards
  • Cricetinae
  • Half-Life
  • Humans
  • Leishmaniasis / drug therapy
  • Limit of Detection
  • Male
  • Phosphorylcholine / analogs & derivatives*
  • Phosphorylcholine / blood
  • Phosphorylcholine / pharmacokinetics
  • Phosphorylcholine / therapeutic use
  • Reference Standards
  • Spectrometry, Mass, Electrospray Ionization* / standards

Substances

  • Antiprotozoal Agents
  • Phosphorylcholine
  • miltefosine