Please use this identifier to cite or link to this item: http://hdl.handle.net/2440/126328
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Type: Journal article
Title: Design of inhalable solid dosage forms of budesonide and theophylline for pulmonary combination therapy
Author: Leng, D.
Kissi, E.O.
Lobmann, K.
Thanki, K.
Fattal, E.
Rades, T.
Foged, C.
Yang, M.
Citation: AAPS PharmSciTech, 2019; 20(3):137-1-137-11
Publisher: American Association of Pharmaceutical Scientists
Issue Date: 2019
ISSN: 1530-9932
1530-9932
Statement of
Responsibility: 
Donglei Leng, Eric Ofosu Kissi, Korbinian Löbmann, Kaushik Thanki, Elias Fattal, Thomas Rades ... et al.
Abstract: Corticosteroid resistance poses a major challenge to effective treatment of chronic obstructive pulmonary diseases. However, corticosteroid resistance can be overcome by co-administration of theophylline. The aim of this study was to formulate the corticosteroid budesonide with theophylline into inhalable dry powders intended for pulmonary combination therapy. Four types of spray-dried powders were prepared: (i) budesonide and theophylline co-dissolved and processed using a 2-fluid nozzle spray drier, (ii) budesonide nanocrystals and dissolved theophylline co-dispersed and processed using a 2-fluid nozzle spray drier, (iii) dissolved budesonide and dissolved theophylline processed using a 3-fluid nozzle spray drier, and (iv) budesonide nanocrystals and dissolved theophylline processed using a 3-fluid nozzle spray drier. Spray drying from the solutions resulted in co-amorphous (i) and partially amorphous powders (iii), whereas spray drying of the nanosuspensions resulted in crystalline products (ii and iv). Even though budesonide was amorphous in (i) and (iii), it failed to exhibit any dissolution advantage over the unprocessed budesonide. In contrast, the dissolution of budesonide from its nanocrystalline formulations, i.e., (ii) and (iv), was significantly higher compared to a physical mixture or unprocessed budesonide. Furthermore, the spray-dried powders obtained from the 2-fluid nozzle spray drier, i.e., (i) and (ii), exhibited co-deposition of budesonide and theophylline at the same weight ratio in the aerodynamic assessment using the New Generation Impactor. In contrast, the depositions of budesonide and theophylline deviated from the starting weight ratio in the aerodynamic assessment of spray-dried powders obtained from the 3-fluid nozzle spray drier, i.e., (iii) and (iv). Based on these results, the powders spray-dried from the suspension by using the 2-fluid nozzle spray drier, i.e., (ii), offered the best formulation properties given the physically stable crystalline solid-state properties and the co-deposition profile.
Keywords: Pulmonary administration; spray drying; inhalable dry powder; 2-fluid nozzle; 3-fluid nozzle
Rights: © 2019 American Association of Pharmaceutical Scientists
RMID: 0030125785
DOI: 10.1208/s12249-019-1344-9
Appears in Collections:Medicine publications

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