Preparation of bitter taste masked cetirizine dihydrochloride/β-cyclodextrin inclusion complex by supercritical antisolvent (SAS) process

Title
Preparation of bitter taste masked cetirizine dihydrochloride/β-cyclodextrin inclusion complex by supercritical antisolvent (SAS) process
Authors
이춘원김수정윤용석Edward Widjojokusumo이영호김재훈이윤우Raymond R. Tjandrawi
Keywords
Cetirizine dihydrochloride; Inclusion complex; Taste masking; β-Cyclodextrin; Supercritical CO2; Supercritical antisolvent
Issue Date
2010-11
Publisher
The Journal of supercritical fluids
Citation
VOL 55, NO 1, 348-357
Abstract
Rapid-disintegrating tablets (RDT) provide many advantages, such as rapid onset of action and assisting those patients who have difficulty swallowing. An important consideration in the formulation of RDT is masking the bitter taste of the drug to ensure patient compliance. The purpose of this study was to evaluate the possibility of inclusion complexation as a means of formulating taste masked cetirizine dihydrochloride (CTZ) rapid-disintegrating tablets. The inclusion complex between CTZ and β-cyclodextrin (β-CD) was prepared using a supercritical antisolvent (SAS) process, where dimethylsulfoxide (DMSO) was used as a liquid solvent and carbon dioxide (CO2) as a supercritical antisolvent. Compared to large, irregular shaped products of freeze-drying method, small, spherically shaped, uniformly sized CTZ/β-CD inclusion complex products were successfully prepared by the SAS process. Concerning the structure of the complex, space conformation of the phenyl ring and chlorophenyl ring of CTZ in the β-CD hydrophobic cavity was confirmed by nuclear magnetic resonance spectroscopy (1H NMR) and two-dimensional rotating frame overhauser effect spectroscopy (2D ROESY) studies. The obtained inclusion complex products prepared by both freeze-drying method and SAS process have the same efficacy in regards to dissolution characteristics and show the effective taste masking as compared to pure CTZ and CTZ/β-CD physical mixtures. In addition, the resulting products prepared by SAS process have negligible amount of residual solvent.
URI
http://pubs.kist.re.kr/handle/201004/38418
ISSN
0896-8446
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KIST Publication > Article
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