Pharmacokinetics and dose proportionality of beclomethasone from three strengths of a CFC-free beclomethasone dipropionate metered-dose inhaler

Biopharm Drug Dispos. 1997 Oct;18(7):635-43. doi: 10.1002/(sici)1099-081x(199710)18:7<635::aid-bdd53>3.0.co;2-y.

Abstract

As part of a development program to offer alternatives to chlorofluorocarbon (CFC) containing metered-dose inhalers, beclomethasone dipropionate has been formulated in a CFC-free system at three strengths: 50, 100, and 200 micrograms/actuation ex valve. To measure serum levels and dose proportionality of the beclomethasone derived from beclomethasone dipropionate, 13 mild to moderate asthmatic patients received a single dose of eight inhalations from each strength according to a double-blind crossover design. Seven patients were studied over 4 h and six patients over 12 h. For the total doses of 400, 800, and 1600 micrograms studied over 12 h, Cmax and AUC increased in a ratio of 1:1.8:3.1. A good correlation was seen between the fine-particle mass delivered and the in vivo performance of the three strengths. From a clinical point of view, the predictable increases in serum levels with an increase in dose will permit the clinician to effectively titrate a patient with this product.

Publication types

  • Clinical Trial
  • Controlled Clinical Trial

MeSH terms

  • Administration, Inhalation
  • Adult
  • Anti-Asthmatic Agents / administration & dosage
  • Anti-Asthmatic Agents / pharmacokinetics*
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / pharmacokinetics*
  • Area Under Curve
  • Asthma / blood
  • Asthma / drug therapy
  • Beclomethasone / administration & dosage
  • Beclomethasone / blood
  • Beclomethasone / pharmacokinetics*
  • Chlorofluorocarbons
  • Cross-Over Studies
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Female
  • Half-Life
  • Humans
  • Male
  • Middle Aged
  • Nebulizers and Vaporizers / standards*

Substances

  • Anti-Asthmatic Agents
  • Anti-Inflammatory Agents
  • Chlorofluorocarbons
  • Beclomethasone