Preparation of bitter taste masked cetirizine dihydrochloride/β-cyclodextrin inclusion complex by supercritical antisolvent (SAS) process
- Preparation of bitter taste masked cetirizine dihydrochloride/β-cyclodextrin inclusion complex by supercritical antisolvent (SAS) process
- 이춘원; 김수정; 윤용석; Edward Widjojokusumo; 이영호; 김재훈; 이윤우; Raymond R. Tjandrawi
- Cetirizine dihydrochloride; Inclusion complex; Taste masking; β-Cyclodextrin; Supercritical CO2; Supercritical antisolvent
- Issue Date
- The Journal of supercritical fluids
- VOL 55, NO 1, 348-357
- 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.
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