A Novel Method for Studying the Pharmacokinetics of [(14) C]Umeclidinium After Application to the Axilla or Palm of Healthy Male Subjects.

ABSTRACT: Umeclidinium (UMEC), a long-acting muscarinic antagonist approved for chronic obstructive pulmonary disease (COPD), was investigated for primary hyperhidrosis as topical therapy. This study evaluated the pharmacokinetics, safety, and tolerability of a single dose of [(14) C]UMEC applied to either unoccluded axilla (UA), occluded axilla (OA), or occluded palm (OP) of healthy males. After 8 h the formulation was removed. [(14) C]UMEC plasma concentrations (Cp) were quantified by accelerator mass spectrometry. Occlusion increased systemic exposure by 3.8-fold. Due to UMEC absorption-limited pharmacokinetics, Cp data from the OA were combined with intravenous data from a phase I study. The data were described by a two-compartment population model with sequential zero and first-order absorption

SUBMITTER: Pene Dumitrescu T 

PROVIDER: S-EPMC5351336 | biostudies-literature | 2016 Aug

REPOSITORIES: biostudies-literature