Document Detail

Theophylline cocrystals prepared by spray drying: physicochemical properties and aerosolization performance.
MedLine Citation:
PMID:  23297166     Owner:  NLM     Status:  MEDLINE    
The purpose of this work was to characterize theophylline (THF) cocrystals prepared by spray drying in terms of the physicochemical properties and inhalation performance when aerosolized from a dry powder inhaler. Cocrystals of theophylline with urea (THF-URE), saccharin (THF-SAC) and nicotinamide (THF-NIC) were prepared by spray drying. Milled THF and THF-SAC cocrystals were also used for comparison. The physical purity, particle size, particle morphology and surface energy of the materials were determined. The in vitro aerosol performance of the spray-dried cocrystals, drug-alone and a drug-carrier aerosol, was assessed. The spray-dried particles had different size distributions, morphologies and surface energies. The milled samples had higher surface energy than those prepared by spray drying. Good agreement was observed between multi-stage liquid impinger and next-generation impactor in terms of assessing spray-dried THF particles. The fine particle fractions of both formulations were similar for THF, but drug-alone formulations outperformed drug-carrier formulations for the THF cocrystals. The aerosolization performance of different THF cocrystals was within the following rank order as obtained from both drug-alone and drug-carrier formulations: THF-NIC>THF-URE>THF-SAC. It was proposed that micromeritic properties dominate over particle surface energy in terms of determining the aerosol performance of THF cocrystals. Spray drying could be a potential technique for preparing cocrystals with modified physical properties.
Amjad Alhalaweh; Waseem Kaialy; Graham Buckton; Hardyal Gill; Ali Nokhodchi; Sitaram P Velaga
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2013-01-08
Journal Detail:
Title:  AAPS PharmSciTech     Volume:  14     ISSN:  1530-9932     ISO Abbreviation:  AAPS PharmSciTech     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-26     Completed Date:  2013-08-12     Revised Date:  2014-01-09    
Medline Journal Info:
Nlm Unique ID:  100960111     Medline TA:  AAPS PharmSciTech     Country:  United States    
Other Details:
Languages:  eng     Pagination:  265-76     Citation Subset:  IM    
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MeSH Terms
Calorimetry, Differential Scanning
Chromatography, Gas
Microscopy, Electron, Scanning
Particle Size
Powder Diffraction
Theophylline / chemistry*
Reg. No./Substance:
0/Aerosols; C137DTR5RG/Theophylline

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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