Systemic availability of budesonide after nasal administration of three different formulations: pressurized aerosol, aqueous pump spray, and powder

Aims The present study was undertaken to determine the absolute systemic av ailability of budesonide from three different devices for nasal administrat ion: pressurized aerosol, aqueous pump spray, and powder. Methods Sixteen healthy, non-smoking, volunteers participated in this open, randomized, and crossover study. All subjects received budesonide as an in travenous dose of 400 mu g, and as three, single-dose, intranasal administr ations: pressurized aerosol 800 mu g, aqueous pump spray 400 mu g, and powd er 800 mu g. Blood was sampled for 10 h after each administration and budes onide was assayed in plasma by Liquid chromatography plus mass spectrometry . Results The mean [95% CI] systemic availability of budesonide with referenc e to the metered dose was: 13 [10; 15]%, 29 [23; 37]%, and 20 [16; 23]%, an d the maximum plasma concentration (C-max) was attained at (t(max)) 2.0, 0. 7, and 0.4 h after administration for the pressurized aerosol, aqueous pump spray, and powder, respectively. Conclusions The uptake of budesonide was more rapid and more complete, and the systemic availability of the drug was significantly higher from the aqu eous pump spray and powder than from the pressurized aerosol.