Abstract
A randomised, open-label, single dose four-period crossover study was performed in
healthy male human subjects to compare the pharmacokinetics of formoterol fumarate
(CAS 43229-80-7) after inhalation from two different hydrofluoro -alkane (HFA) pressurised
metered dose inhaler (pMDI) formulations at two dose levels, 12 and 24 μg. This is
the first stud which has evaluated two HFA formulations of formoterol. Fourteen subjects
were randomised, of which 13 completed the study. Each subject received in separate
periods a single dose of 12 μg or 24 μg of each formulation. Blood samples for determination
of formoterol plasma concentrations were taken pre-administration of study treatments
and subsequently at 2, 5, 10, 20, 30, 45, 60, 90 min and 2, 3, 4, 6, 8, 12, 24 and
36 h post-administration of the study treatments. The pharmacokinetic profiles of
both the formulations were similar in shape and dose-related increase in formoterol
plasma concentration was seen at all time points for both the test and reference formoterol
HFA formulations between the dose levels 12 μg and 24 μg. Overall the findings indicate
that treatment with the test formoterol HFA preparation has lung absorption pattern
and systemic exposure comparable to the already licensed reference formoterol HFA
preparation.
Key word
Bronchodilator - CAS 43229-80-7 - CAS 73573-87-2 - Formoterol, bioavailability inhalation,
pharmacokinetic - Hydrofluoroalkane
