Lung deposition of hydrofluoroalkane-134a beclomethasone is greater than that of chlorofluorocarbon fluticasone and chlorofluorocarbon beclomethasone : a cross-over study in healthy volunteers

Chest. 2002 Aug;122(2):510-6. doi: 10.1378/chest.122.2.510.

Abstract

Study objectives: To compare the lung deposition of radiolabeled hydrofluoroalkane-134a beclomethasone dipropionate (HFA-BDP) with chlorofluorocarbon fluticasone propionate (CFC-FP) and chlorofluorocarbon beclomethasone (CFC-BDP).

Design: Six-day, open-label, nonrandomized, crossover study.

Setting: Clinical research laboratory.

Participants: Nine healthy, nonsmoking, adult volunteers.

Interventions: On each study day, participants inhaled one or two puffs of 99mTc-labeled HFA-BDP, CFC-FP, or CFC-BDP. All products delivered 50 micro g per puff ex-valve. Subjects used a respiratory training and monitoring device to meet predefined, standardized inhalation patterns. Immediately after inhalation of radiolabeled study drug, planar gamma camera images were obtained.

Measurements and results: Radiolabeled HFA-BDP had a higher deposition in the lungs (53% ex-actuator) compared with CFC-FP (12 to 13%) and CFC-BDP (4%). Conversely, CFC-FP and CFC-BDP had a much higher distribution to the oropharynx (72 to 78%, and 82%, respectively) than HFA-BDP (29%). HFA-BDP was deposited evenly throughout the lungs, while CFC-FP and CFC-BDP deposition was primarily in the large central and intermediate airways. Andersen particle size sampling gave mass median aerodynamic diameters for HFA-BDP, CFC-FP, and CFC-BDP of 0.9 micro m, 2.0 micro m, and 3.5 micro m, respectively.

Conclusions: Lung deposition was greater with HFA-BDP compared with CFC-FP and CFC-BDP. Deposition values appeared to be related to the particle size distribution of each inhaler, with the smaller particles of HFA-BDP providing the greatest lung deposition and least oropharyngeal deposition.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase I
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Inhalation
  • Administration, Topical
  • Adult
  • Aerosol Propellants / pharmacokinetics*
  • Aerosols
  • Androstadienes / pharmacokinetics*
  • Anti-Inflammatory Agents / pharmacokinetics*
  • Beclomethasone / pharmacokinetics*
  • Chlorofluorocarbons / pharmacokinetics*
  • Cross-Over Studies
  • Female
  • Fluticasone
  • Glucocorticoids
  • Humans
  • Hydrocarbons, Fluorinated / pharmacokinetics*
  • Lung / diagnostic imaging
  • Lung / metabolism*
  • Male
  • Middle Aged
  • Particle Size
  • Radionuclide Imaging
  • Radiopharmaceuticals / pharmacokinetics
  • Technetium

Substances

  • Aerosol Propellants
  • Aerosols
  • Androstadienes
  • Anti-Inflammatory Agents
  • Chlorofluorocarbons
  • Glucocorticoids
  • Hydrocarbons, Fluorinated
  • Radiopharmaceuticals
  • Technetium
  • Fluticasone
  • Beclomethasone
  • apaflurane