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Pharmacokinetics of chlorofluorocarbon and hydrofluoroalkane metered‐dose inhaler formulations of beclomethasone dipropionate
Author(s) -
Brian J. Lipworth,
CM Jackson
Publication year - 1999
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1046/j.1365-2125.1999.00098.x
Subject(s) - chlorofluorocarbon , cmax , inhaler , pharmacokinetics , crossover study , inhalation , chemistry , beclometasone dipropionate , pharmacology , metered dose inhaler , anesthesia , asthma , medicine , respiratory disease , alternative medicine , organic chemistry , pathology , lung , placebo
Aims To compare the pharmacokinetic profile of Beclazone TM (beclomethasone dipropionate) in its chlorofluorocarbon (CFC)‐based and CFC‐free formulations.Methods Ten healthy adults received a single 1000 μg nominal dose (ex‐valve) of beclomethasone dipropionate from a CFC inhaler (BEC‐CFC) or from a CFC‐free inhaler containing hydrofluoroalkane (HFA)‐134a (BEC‐HFA) in an open‐label, randomized, two‐way, crossover study. Blood samples were collected predose and over 12 h after inhalation. Comparisons were made of maximum plasma concentration of beclomethasone 17‐monopropionate (17‐BMP) (C max ), and area under the plasma concentration vs time curve (AUC).Results The t max was significantly (P<0.05) earlier with BEC‐HFA and plasma levels were significantly higher following administration of BEC‐HFA than BEC‐CFC. Geometric mean values for AUC were 1.5 fold greater (90% CI 1.3–1.9) and for C max were 1.9 fold greater (90% CI 1.6–2.6) following BEC‐HFA than BEC‐CFC.Conclusions Our data in healthy volunteers would not be consistent with the manufacturers’ recommendation for a microgram equivalent (1:1) nominal dose switch between these HFA and CFC formulations. Further well designed trials are required in asthmatic patients to properly define their respective dose–response relationships for antiasthmatic and systemic adverse effects.