HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

An LC-MS/MS method for the determination of five erectile dysfunction drugs and their selected metabolites in hair.

Abstract
The abuse of sildenafil and its analogous, accelerated by their inappropriate or illegal distribution, is a serious social issue globally. However, no studies have been conducted to monitor these drugs simultaneously in hair, which can provide valuable information on chronic drug use. In the present study, an LC-MS/MS method was developed for the simultaneous determination in hair of five erectile dysfunction drugs having a high risk for abuse (mirodenafil, sildenafil, tadalafil, udenafil and vardenafil) and their selected metabolites (SK3541, desmethylsildenafil, DA8164 and desethylvardenafil). The novel method was fully validated after optimizing matrix effects and extraction efficiency. The optimized sample preparation included acidic methanol extraction followed by solid phase extraction using C18 mixed mode strong cation exchange polymeric cartridges. The prepared samples were analyzed by LC-MS/MS with electrospray ion source in the positive ionization mode. The validation results proved the method to be selective, sensitive, accurate and precise, with acceptable linearity within calibration ranges. LODs ranged from 0.05 (DA8164) to 1 ng/10 mg hair (tadalafil). LOQs were 1 ng/10 mg hair except for DA8164 and vardenafil, of which they were 2.5 ng/10 mg hair. No significant variations were observed by different sources of matrices in both human and rat hair, except for tadalafil, for which a stable isotope-labeled internal standard was effective. The animal study suggested hair pigmentation was a major factor for the incorporation of the drugs and metabolites into hair. However, a wide variation of the sildenafil-to-desmethylsildenafil ratios was observed in human hair samples. The developed method will be very useful for monitoring the abuse of erectile dysfunction drugs for both legal and public health aspects.
AuthorsSooyeun Lee, Boyeon Choi, Jihyun Kim, Sanghwan In, Seungkyung Baeck, Seung Min Oh, Kyu Hyuck Chung
JournalJournal of chromatography. B, Analytical technologies in the biomedical and life sciences (J Chromatogr B Analyt Technol Biomed Life Sci) Vol. 978-979 Pg. 1-10 (Jan 26 2015) ISSN: 1873-376X [Electronic] Netherlands
PMID25531864 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2014 Elsevier B.V. All rights reserved.
Chemical References
  • Phosphodiesterase 5 Inhibitors
  • Piperazines
  • Sulfonamides
  • Urological Agents
Topics
  • Animals
  • Chromatography, Liquid (methods)
  • Erectile Dysfunction (drug therapy)
  • Hair (chemistry)
  • Humans
  • Limit of Detection
  • Linear Models
  • Male
  • Phosphodiesterase 5 Inhibitors (analysis, therapeutic use)
  • Piperazines (analysis, therapeutic use)
  • Rats
  • Rats, Zucker
  • Reproducibility of Results
  • Sulfonamides (analysis, therapeutic use)
  • Tandem Mass Spectrometry (methods)
  • Urological Agents (analysis, therapeutic use)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: