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

Abstract

Aims: The present study was undertaken to determine the absolute systemic availability of budesonide from three different devices for nasal administration: 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 intravenous dose of 400 microg, and as three, single-dose, intranasal administrations: pressurized aerosol 800 microg, aqueous pump spray 400 microg, and powder 800 microg. Blood was sampled for 10 h after each administration and budesonide was assayed in plasma by liquid chromatography plus mass spectrometry.

Results: The mean [95% CI] systemic availability of budesonide with reference to the metered dose was: 13 [10; 15]%, 29 [23; 37]%, and 20 [16; 23]%, and the maximum plasma concentration (Cmax) was attained at (tmax) 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 aqueous pump spray and powder than from the pressurized aerosol.

Figure 1

Plasma concentration profile of budesonide after intravenous administration of 400 μg over 8 min (mean and s.e.mean).

Figure 2

Plasma concentration profiles of budesonide after single-dose nasal administrations of pressurized aerosol 800 μg (–––), aqueous pump spray (—) 400 μg, and powder 800 μg (.....). Data have been normalised to metered doses with the pMDI formulation. (mean and s.e.mean).