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

作者: Chun-Won Lee , Soo-Jung Kim , Yong-Suk Youn , Edward Widjojokusumo , Young-Ho Lee

DOI: 10.1016/J.SUPFLU.2010.05.028

关键词: DissolutionNuclear Overhauser effectSolventNuclear magnetic resonance spectroscopySupercritical fluidCyclodextrinProton NMRNuclear chemistryChemistryScientific methodChromatography

摘要: 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 RDT is masking bitter taste drug to ensure patient compliance. The purpose this study was evaluate possibility inclusion complexation a means formulating masked cetirizine dihydrochloride (CTZ) rapid-disintegrating tablets. complex between CTZ β-cyclodextrin (β-CD) prepared using supercritical antisolvent (SAS) process, where dimethylsulfoxide (DMSO) used liquid solvent carbon dioxide (CO 2 ) antisolvent. Compared large, irregular shaped products freeze-drying method, small, spherically shaped, uniformly sized CTZ/β-CD were successfully by SAS process. Concerning structure complex, space conformation phenyl ring chlorophenyl β-CD hydrophobic cavity confirmed nuclear magnetic resonance spectroscopy ( 1 H NMR) two-dimensional rotating frame overhauser effect (2D ROESY) studies. obtained both method process same efficacy regards dissolution characteristics show effective compared pure physical mixtures. In addition, resulting negligible amount residual solvent.

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