Cl. Leach et al., Improved airway targeting with the CFC-free HFA-beclomethasone metered-dose inhaler compared with CFC-beclomethasone, EUR RESP J, 12(6), 1998, pp. 1346-1353
Hydrofluoroalkane-134a (HFA) beclomethasone dipropionate (BDP) was formulat
ed in a metered-dose inhaler (MDI) to deliver a particle size of I,I pm com
pared with 3.5 microns for currently marked chlorofluorocarbon (CFC)-BDP pr
oducts. Two phase I single-dose human deposition studies were conducted usi
ng technetium 99m-radiolabelled BDP in a press-and-breathe actuator without
an add-on spacer.
A healthy volunteer study (n=6) showed that 55-60% of the HFA-BDP ex-actuat
or dose was deposited in the lungs, with 29-30% deposited in the oropharynx
.. CFC-BDP deposition was 4-7% in the lungs and 90-94% in the oropharynx. T
he pattern of deposition within the lung showed that HFA-BDP was spread dif
fusely throughout the lung airways, whereas CFC-BDP was confined to the cen
tral airways with little, if any, peripheral airway deposition. A second st
udy with asthmatics (n=16) confirmed that 56% of the HFA-BDP dose was depos
ited in the airways, with 33% in the oro-pharynx.
In conclusion, hydrofluoroalkane-134a-beclomethasone dipropionate depositio
n was much greater in the airways than chlorofluorocarbon-beclomethasone di
propionate, with a concomitant reduction in oropharyngeal deposition. The i
ncreased lung deposition efficiency of the hydrafluoroalkane propellant has
led to a reduction in the amount of bedomethasone dipropionate needed to a
chieve a similar efficacy. The penetration of the hydrofluoroalkane to the
small airways may provide asthma treatment not afforded by conventional chl
orofluorocarbons.