Elsevier

The Lancet

Volume 354, Issue 9187, 16 October 1999, Pages 1357-1358
The Lancet

Research Letters
Differences in lung bioavailability between different propellants for fluticasone propionate

https://doi.org/10.1016/S0140-6736(99)03581-3Get rights and content

Summary

The lung bioavailability (as adrenal suppression) of fluticasone propionate was about two-fold greater with chlorofluorocarbons than hydrofluoroalkane as propellant. Direct switching between formulations on a μg equivalent may therefore be inadvisable.

References (3)

  • AM Wilson et al.

    24 hour and fractionated profiles of adrenocortical activity in asthmatic patients receiving inhaled and intranasal corticosteroids

    Thorax

    (1999)
There are more references available in the full text version of this article.

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    Dempsey et al. [22] in healthy volunteers had previously demonstrated that the use of VM spacer with CFC–FP via pMDI increased the suppression of OUCC by nearly 1.9-fold, as compared to a value of 1.66-fold greater suppression with HFA–FP in the present study. In this regard a greater degree OUCC suppression with CFC vs. HFA–FP has been previously documented [26,27] when using pMDI alone in either healthy volunteers or asthmatics. There are only limited in vitro and in vivo data on the relative respirable dose delivery of inhaled SM via spacer devices [28,29].

  • Airway and systemic effects of hydrofluoroalkane formulations of high-dose ciclesonide and fluticasone in moderate persistent asthma

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    It has previously been shown that the systemic bioavailability of the hydrofluoroalkane FP suspension formulation is significantly lower than that of the chlorofluorocarbon FP suspension formulation for the same nominal dose.21 Moreover, the degree of HPA axis suppression is significantly lower with the hydrofluoroalkane FP formulation than with the chlorofluorocarbon FP formulation.22–24 Thus, although the nominal dose of hydrofluoroalkane FP was high at 2,000 μg, its lower systemic bioavailability would in part, along with reduced airway caliber, explain the lower-than-expected magnitude of adrenal suppression.

  • Lung deposition of hydrofluoroalkane-134a beclomethasone is greater than that of chlorofluorocarbon fluticasone and chlorofluorocarbon beclomethasone: A cross-over study in healthy volunteers

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    The two products have been licensed on a dose-equivalent basis for switching between formulations. However, a study by Wilson et al14 demonstrated that the lung bioavailability and, by implication, lung deposition of CFC-FP was about twofold greater than that of HFA-FP at the same dose, as assessed by markers of adrenal suppression. The use of CFC-FP rather than HFA-FP in the current study, therefore, provided the more stringent comparator.

  • Therapeutic ratio of hydrofluoroalkane and chlorofluorocarbon formulations of fluticasone propionate

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    Other studies2122 have showed FP to produce less adrenal suppression in asthmatic patients compared to healthy subjects, and that the degree of suppression is related to airflow obstruction.23 Indeed, when comparing the magnitude of suppression of overnight urinary cortisol/creatinine level with CFC-FP1000 in patients in the present study (33% vs placebo) with that in healthy volunteers (66% vs placebo),8 it is evident that lung bioavailability is reduced in association with reduced small airways calibre, as evidenced by the 61% mean predicted FEF25–75 in our patients. It is also worth pointing out that there is an apparent discrepancy between the comparable in vitro impactor profiles for respirable dose delivery and the difference in lung bioavailability from pharmacokinetics when comparing the two formulations.56

  • Adrenal suppression with inhaled corticosteroids

    2001, Annals of Allergy, Asthma and Immunology
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