Theophylline cocrystals prepared by spray drying: Physicochemical properties and aerosolization performance

Alhalaweh, Amjad, Kaialy, Waseem, Buckton, Graham, Gill, Hardyal, Nokhodchi, Ali and Velaga, Sitaram P (2013) Theophylline cocrystals prepared by spray drying: Physicochemical properties and aerosolization performance. AAPS PharmSciTech, 14 (1). pp. 265-276. ISSN 1530-9932

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Abstract

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. © 2013 American Association of Pharmaceutical Scientists.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science > QD Chemistry
Depositing User: Tom Gittoes
Date Deposited: 17 Dec 2014 13:35
Last Modified: 17 Dec 2014 13:35
URI: http://sro.sussex.ac.uk/id/eprint/51753
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