Cetirizine Dihydrochloride, beta-Cyclodextrin Inclusion Complex by Ethanol Kneading for Taste Masking

Abstract

Cetirizine dihydrochloride has a very unpleasant bitter taste. To mask the bitter taste, complexation with β-cyclodextrin using ethanol as a kneading solvent was investigated and evaluated by Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, thermogravimetric analysis, simultaneous X-ray diffractometry-differential scanning calorimetry measurement and 1H-nuclear magnetic resonance spectroscopy. Taste was evaluated by human volunteers using an unstructured line scale. The basic characterization of the prepared tablets including in vivo disintegration time and drug dissolution was studied. Fourier transform infrared spectroscopy, differential scanning calorimetry and powder X-ray diffractometry data confirmed the inclusion complex formation. Thermogravimetric analysis, simultaneous X-ray diffractometry-differential scanning calorimetry measurements revealed the reduction of crystalline β-cyclodextrin due to the displacement of water molecules from complex formation. Proton nuclear magnetic resonance spectroscopy indicated an intermolecular interaction between protons of cetirizine dihydrochloride with the cavity of β-cyclodextrin. The prepared complex showed an unstructured line scale with apparent low average rating of 1.70. The inclusion complex-loaded fast disintegrating tablet prepared with direct compression has short disintegration time and good taste with an unstructured line scale with average rating of 0.28. Cetirizine dihydrochloride, β-cyclodextrin inclusion complex was successfully prepared by kneading method using ethanol as solvent. The inclusion complex-loaded fast disintegrating tablet had good taste and good perception in the mouth.