Lee, Chun-Won Kim, Soo-Jung Youn, Yong-Suk Widjojokusumo, Edward Lee, Young-Ho Kim, Jaehoon Lee, Youn-Woo Tjandrawinata, Raymond R. 2024-01-20T18:30:43Z 2024-01-20T18:30:43Z 2021-09-04 2010-11 0896-8446 https://pubs.kist.re.kr/handle/201004/130982 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 beta-cyclodextrin (beta-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/beta-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 beta-CD hydrophobic cavity was confirmed by nuclear magnetic resonance spectroscopy (H-1 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/beta-CD physical mixtures. In addition, the resulting products prepared by SAS process have negligible amount of residual solvent. (C) 2010 Elsevier B.V. All rights reserved. English ELSEVIER SOLVENT-EXTRACTION SYSTEM ASSOCIATION CONSTANTS BETA-CYCLODEXTRIN FAMOTIDINE NAPROXEN MASKING DRUGS Preparation of bitter taste masked cetirizine dihydrochloride/beta-cyclodextrin inclusion complex by supercritical antisolvent (SAS) process Article 10.1016/j.supflu.2010.05.028 1 JOURNAL OF SUPERCRITICAL FLUIDS, v.55, no.1, pp.348 - 357 JOURNAL OF SUPERCRITICAL FLUIDS 55 1 348 357 scie scopus 000284815300045 2-s2.0-78049288532 Chemistry, Physical Engineering, Chemical Chemistry Engineering Article SOLVENT-EXTRACTION SYSTEM ASSOCIATION CONSTANTS BETA-CYCLODEXTRIN FAMOTIDINE NAPROXEN MASKING DRUGS Cetirizine dihydrochloride Inclusion complex Taste masking beta-Cyclodextrin Supercritical CO2 Supercritical antisolvent