Lung deposition of fluticasone propionate/formoterol administered via a breath-triggered inhaler

Introduction: Inhaled drug efficacy is dependent on adequate pulmonary drug deposition. A scintigraphic study was undertaken to assess in vivo pulmonary deposition for a novel fluticasone propionate/formoterol (FP/FORM) breath-triggered inhaler (BTI; Flutiform ® K-haler ® ). Aims & Objectives: To determine total lung deposition and regional distribution pattern for FP/FORM BTI in healthy subjects and patients with asthma and COPD. Methods: Healthy, asthmatic and COPD subjects (N=12 per group) received a single dose of 2 puffs technetium-99 ( 99m Tc)-labelled FP/FORM BTI 125/5 µg. Two-dimensional gamma scintigraphy was used to assess the drug deposition pattern. Prior 99m Tc transmission scans defined regions of interest and attenuation correction factors. Results: The radiolabel and radiolabelled drug conformed to release specifications for the unlabelled product. Of 36 subjects, 35 provided post-dose scintigraphic data. Mean ages were 35.7 (healthy), 44.5 (asthma) and 61.7 years (COPD). The corresponding mean FEV 1 % predicted values were 109.8%, 77.4% and 43.2%, respectively. Whole lung deposition was, on average, 26.6% (healthy), 44.7% (asthma), 39.0% (COPD) of the delivered dose. The respective mean penetration indices (peripheral:central ratio) were 0.44, 0.31 and 0.30. Conclusions: Lung deposition with FP/FORM BTI compares favourably with other combination inhalers. The BTI’s deposition fraction of ~40% in asthma and COPD echoes ex vivo measurements for the same formulation via a pressurised metered-dose inhaler (pMDI). Both results reflect the high fine particle dose of ~40% within the BTI and pMDI. EudraCT number: 2015-000744-42. Funded by: Mundipharma Research Ltd.