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

Abstract

Katewongsa, et al.: Cetirizine Dihydrochloride and β-Cyclodextrin Complex by Ethanol KneadingCetirizine 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 1 H-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 had 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.

Development and evaluation of pH sensitive semi-interpenetrating networks: assessing the impact of itaconic acid and aloe vera on network swelling and cetirizine release

“…The DSC thermogram of blank hydrogels showed a melting peak of IA at approximately 160°C ( Figure 6 ) as reported previously ( Kirimura et al, 2011 ) and poly (acrylamide) above 300°C. Pure CTZ HCl exhibited a melting peak at approximately 201.3°C, followed by a degradation peak at approximately 220°C and is in agreement with previous studies ( Katewongsa et al, 2017 ; Afzal et al, 2018 ). CTZ HCl peaks diminished in drug-loaded hydrogels (F5) indicating dispersion of the drug in an amorphous form.…”

Review of Applications of Cyclodextrins as Taste-Masking Excipients for Pharmaceutical Purposes

“…FTIR, DSC, PXRD, 1 H MR, [75] Cetirizine dihydrochloride α-, β-, and γ-cyclodextrin No detailed information provided. FTIR, UV-VIS, HPLC [76] Cetirizine dihydrochloride α-, β-, and γ-cyclodextrin…”

“…In [84], the authors showed how arundic acid Even in the form of physical mixture with API, β-CD exhibits some taste-masking properties that are greatly improved when the complex is being administrated. Adapted from [75], licensed under CC BY 3.0 (Creative Commons Attribution License 3.0).…”

Formulation, optimization and evaluation of mucoadhesive microspheres of captopril

“…The pure drug, polymer mix and formulation were subjected to Fourier transform infrared (FTIR) studies. The pure drug, polymer and formulation was mixed with small quantity of IR grade potassium bromide and scanned in the range of 4000-400 cm −1 using an FTIR JASCO instrument (Jasco Corporation, Tokyo, Japan) [8].…”