Abstract |
Hydrofluoroalkane-134a (HFA) beclomethasone dipropionate (BDP) was formulated in a metered-dose inhaler (MDI) to deliver a particle size of 1.1 microm compared with 35 microns for currently marketed chlorofluorocarbon (CFC)-BDP products. Two phase I single-dose human deposition studies were conducted using 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-actuator 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. The pattern of deposition within the lung showed that HFA-BDP was spread diffusely throughout the lung airways, whereas CFC-BDP was confined to the central airways with little, if any, peripheral airway deposition. A second study with asthmatics (n=16) confirmed that 56% of the HFA-BDP dose was deposited in the airways, with 33% in the oropharynx. In conclusion, hydrofluoroalkane-134a-beclomethasone dipropionate deposition was much greater in the airways than chlorofluorocarbon- beclomethasone dipropionate, with a concomitant reduction in oropharyngeal deposition. The increased lung deposition efficiency of the hydrofluoroalkane propellant has led to a reduction in the amount of beclomethasone dipropionate needed to achieve a similar efficacy. The penetration of the hydrofluoroalkane to the small airways may provide asthma treatment not afforded by conventional chlorofluorocarbons.
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Authors | C L Leach, P J Davidson, R J Boudreau |
Journal | The European respiratory journal
(Eur Respir J)
Vol. 12
Issue 6
Pg. 1346-53
(Dec 1998)
ISSN: 0903-1936 [Print] England |
PMID | 9877489
(Publication Type: Comparative Study, Journal Article)
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Chemical References |
- Aerosol Propellants
- Chlorofluorocarbons
- Glucocorticoids
- Hydrocarbons, Fluorinated
- Betamethasone
- apaflurane
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Topics |
- Adolescent
- Adult
- Aerosol Propellants
- Asthma
(drug therapy, metabolism)
- Betamethasone
(administration & dosage, pharmacokinetics)
- Chlorofluorocarbons
- Female
- Glucocorticoids
(administration & dosage, pharmacokinetics)
- Humans
- Hydrocarbons, Fluorinated
- Lung
(metabolism)
- Male
- Middle Aged
- Nebulizers and Vaporizers
- Oropharynx
(metabolism)
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