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

Abstract

AimsThe 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 mg, and as three, single-dose, intranasal administrations: pressurized aerosol 800 mg, aqueous pump spray 400 mg, and powder 800 mg. 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 (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 aqueous pump spray and powder than from the pressurized aerosol.

Budesonide quantification by HPLC coupled to atmospheric pressure photoionization (APPI) tandem mass spectrometry. Application to a comparative systemic bioavailability of two budesonide formulations in healthy volunteers

“…This is the first method developed to assess the budesonide quantification in human plasma applied to a pharmacokinetics study using LC-MS/MS with a photoionization source. This method offers the advantage over those previously reported using LC-MS/MS ( [12,15,[20][21][22]), showing a low validated LLOQ (7.5 pg ml −1 ) associated with a faster chromatographic run time (4.0 min). Two other methods use LC-MS/MS to quantify budesonide showed a slight lower LLOQ of 6.5 pg ml −1 using a APCI ionization source [11] and 5 pg ml −1 using a Turboionspray ionization source [14].…”

Development of Budesonide Microparticles Using Spray-Drying Technology for Pulmonary Administration: Design, Characterization, In Vitro Evaluation, and In Vivo Efficacy Study

“…ICSs appear to have a place in the management of severe chronic obstructive pulmonary disease (COPD), perhaps by decreasing and reducing the frequency of exacerbations and improve quality of life in patients with COPD (3). Budesonide (BUD) has a high ratio of topical anti-inflammatory to systemic activity and is one of the most extensively used inhaled glucocorticoids (4). BUD decreases airway hyper-responsiveness and reduces the number of inflammatory cells and mediators present in airways of patients with asthma.…”

Expanding choices in intranasal steroid therapy: Summary of a Roundtable Meeting

“…In an open-label, randomized, crossover trial with budesonide, Thorsson et al 26 found drug uptake to be "more rapid and more complete" and systemic bioavailability significantly higher from the aqueous pump spray and powder inhaler than the pressurized metered-dose inhaler (MDI). In a second clinical comparison of the same drug delivered by aqueous spray or an MDI to patients with AR, both devices produced good results and there was no effect on urinary cortisol excretion.…”