Evaluating suspension formulations of theophylline cocrystals with artificial sweeteners

Page view(s)
58
Checked on May 30, 2024
Evaluating suspension formulations of theophylline cocrystals with artificial sweeteners
Title:
Evaluating suspension formulations of theophylline cocrystals with artificial sweeteners
Journal Title:
Journal of Pharmaceutical Sciences
Keywords:
Publication Date:
05 October 2017
Citation:
Aitipamula, S.; Wong, A. B. H.; Kanaujia, P., Evaluating suspension formulations of theophylline cocrystals with artificial sweeteners. Journal of Pharmaceutical Sciences 2018, 107 (2), 604-611.
Abstract:
Pharmaceutical cocrystals have garnered significant interest as potential solids to address issues associated with formulation development of drug substances. However, studies concerning the understanding of formulation behavior of cocrystals are still at the nascent stage. We present results of our attempts to evaluate suspension formulations of cocrystals of an antiasthmatic drug, theophylline, with 2 artificial sweeteners. Stability, solubility, drug release, and taste of the suspension formulations were evaluated. Suspension that contained cocrystal with acesulfame showed higher drug release rate, while a cocrystal with saccharin showed a significant reduction in drug release rate. The cocrystal with saccharin was found stable in suspension for over 9 weeks at accelerated test condition; in contrast, the cocrystal with acesulfame was found unstable. Taste analysis using an electronic taste-sensing system revealed improved sweetness of the suspension formulations with cocrystals. Theophylline has a narrow therapeutic index with a short half-life which necessitates frequent dosing. This adversely impacts patient compliance and enhances risk of gastrointestinal and cardiovascular adverse effects. The greater thermodynamic stability, sweetness, and sustained drug release of the suspension formulation of theophylline-saccharin could offer an alternative solution to the short half-life of theophylline and make it a promising formulation for treating asthmatic pediatric and geriatric patients.
License type:
http://creativecommons.org/licenses/by-nc-nd/4.0/
Funding Info:
This work was funded by the Science and Engineering Research Council of A*STAR (Agency for Science, Technology and Research), Singapore.
Description:
ISSN:
0022-3549
1520-6017
Files uploaded:

File Size Format Action
fy17-062-cfs-manu-evaluating-suspension.pdf 1.04 MB PDF Open