Lung deposition of hydrofluoroalkane-134a beclomethasone is greater than that of chlorofluorocarbon fluticasone and chlorofluorocarbon beclomethasone : a cross-over study in healthy volunteers.
OBJECTIVE
To compare the lung deposition of radiolabeled hydrofluoroalkane-134a beclomethasone dipropionate (HFA-BDP) with chlorofluorocarbon fluticasone propionate (CFC-FP) and chlorofluorocarbon beclomethasone (CFC-BDP).


METHODS
Six-day, open-label, nonrandomized, crossover study.


METHODS
Clinical research laboratory.


METHODS
Nine healthy, nonsmoking, adult volunteers.


METHODS
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.


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.
Leach
Chet L
CL
3M Pharmaceuticals, St. Paul, MN, USA. cleach@inhale.com
Davidson
Patricia J
PJ
Hasselquist
Bruce E
BE
Boudreau
Robert J
RJ
D000280:Administration, Inhalation; D000287:Administration, Topical; D000328:Adult; D000335:Aerosol Propellants / Q000493:pharmacokinetics*; D000336:Aerosols; D000730:Androstadienes / Q000493:pharmacokinetics*; D000893:Anti-Inflammatory Agents / Q000493:pharmacokinetics*; D001507:Beclomethasone / Q000493:pharmacokinetics*; D017402:Chlorofluorocarbons / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D005260:Female; D000068298:Fluticasone; D005938:Glucocorticoids; D006801:Humans; D006845:Hydrocarbons, Fluorinated / Q000493:pharmacokinetics*; D008168:Lung / Q000000981:diagnostic imaging / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D010316:Particle Size; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D013667:Technetium; D005466:Fluorocarbons
D000335:Aerosol Propellants; D000336:Aerosols; D000730:Androstadienes; D000893:Anti-Inflammatory Agents; D001507:Beclomethasone; D017402:Chlorofluorocarbons; D000068298:Fluticasone; D005938:Glucocorticoids; D006845:Hydrocarbons, Fluorinated; D019275:Radiopharmaceuticals; D013667:Technetium; C094049:apaflurane; D005466:Fluorocarbons