Effect of formulation parameters on hydrofluoroalkane-beclomethasone dipropionate drug deposition in humans

J Allergy Clin Immunol. 1999 Dec;104(6):S250-2. doi: 10.1016/s0091-6749(99)70041-2.

Abstract

Chlorofluorocarbon metered dose inhalers (MDIs) and dry powder inhalers currently deliver drug that deposits primarily in the oropharynx and secondarily in the large central airways. Chlorofluorocarbon-beclomethasone dipropionate (CFC-BDP) MDIs deliver more than 90% of the drug in the oropharynx and less than 10% in the lungs. The elimination of chlorofluorocarbons from MDIs provided the opportunity to more optimally target corticosteroids directly to all inflammatory sites. Hydrofluoroalkane-BDP (HFA-BDP) MDIs (QVAR(trade mark)) deliver 50% to 60% of the drug to the lungs with approximately 30% delivered to the mouth. Additionally, the amount of drug delivered to the lungs is distributed throughout the large, intermediate, and small airways. Radiolabeled deposition studies have shown that the HFA-BDP MDI is a "forgiving" aerosol in that even the extreme discoordinated use of the press and breathe MDI still resulted in more than 30% lung deposition. The breath-actuated Autohaler inhaler provided the same lung deposition as an optimally used press and breathe MDI. The dose delivered from either the press and breathe HFA-BDP MDI or the Autohaler was consistent across a wide range of inspiratory flows (eg, flows of 26-137 L/min). Clinical studies have shown that the improvements in lung deposition of HFA-BDP result in equivalent efficacy at approximately one half of the total daily dose compared with current CFC-BDP products.

MeSH terms

  • Beclomethasone / metabolism*
  • Chemistry, Pharmaceutical*
  • Humans
  • Hydrocarbons, Fluorinated / metabolism*
  • Nebulizers and Vaporizers / standards
  • Particle Size
  • Patient Education as Topic

Substances

  • Hydrocarbons, Fluorinated
  • Beclomethasone
  • apaflurane