Bioavailability of fluticasone propionate and mometasone furoate aqueous nasal sprays

Eur J Clin Pharmacol. 2004 Jun;60(4):265-8. doi: 10.1007/s00228-004-0763-y. Epub 2004 Apr 28.

Abstract

Objectives: To compare the systemic exposure for intranasal mometasone furoate (MF) and fluticasone propionate (FP) aqueous nasal sprays (ANS) in terms of serum and urinary cortisol parameters and plasma pharmacokinetics.

Methods: Twelve healthy subjects completed this three-way, cross-over study. They received FPANS (50 microg/spray), MFANS (50 microg/spray) or placebo ANS, eight sprays per nostril every 8 h for 4 days. Cortisol measurements were made at baseline and day 4. FP and MF plasma concentrations were also measured on day 4.

Results: MFANS produced similar mean plasma AUC (123 pmol/l h) to FPANS (112 pmol/l h). Despite the use of high doses, necessary to generate adequate pharmacokinetic data, only minor reductions in cortisol parameters were found, with no difference between FPANS and MFANS.

Conclusions: FP and MF have similar and very low systemic bioavailability when administered intranasally using a high-dose regimen. It is therefore unlikely that therapeutic doses of intranasal FP or MF will produce dissimilar or significant degrees of systemic exposure or systemic effects.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Administration, Intranasal
  • Adrenal Cortex Hormones / administration & dosage
  • Adrenal Cortex Hormones / pharmacokinetics*
  • Adult
  • Aerosols
  • Androstadienes / administration & dosage
  • Androstadienes / pharmacokinetics*
  • Area Under Curve
  • Biological Availability
  • Cross-Over Studies
  • Female
  • Fluticasone
  • Humans
  • Hydrocortisone / blood
  • Hydrocortisone / urine
  • Male
  • Mometasone Furoate
  • Pregnadienediols / administration & dosage
  • Pregnadienediols / pharmacokinetics*

Substances

  • Adrenal Cortex Hormones
  • Aerosols
  • Androstadienes
  • Pregnadienediols
  • Mometasone Furoate
  • Fluticasone
  • Hydrocortisone