Synthesis and Evaluation of Taste-Masked Ionic Liquid Salts of Loratadine

Abstract

Objective: To synthesize and evaluate taste-masked ionic liquid (IL) salts of loratadine.
 Methods: In the present work, pharmaceutically active IL salts of loratadine using selected counter-ions were synthesized. The synthesized IL salts were characterized using melting point, Ultraviolet (UV) spectroscopy, Fourier Transform Infra-Red (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC), and X-ray Diffraction (XRD). These salts were also evaluated for solubility, dissolution, and palatability studies.
 Results: All synthesized IL salts of loratadine exhibited melting points below 100 °C. UV spectral data and FTIR data confirmed the formation of new salt forms with selected counter-ions. The absence of sharp melting point peaks during DSC studies revealed the amorphous nature of new salt forms. During XRD studies, loratadine-indomethacin IL salt yields completely amorphous compound while the intensity of characteristic peaks of loratadine was found to be reduced with other counter-ions. Solubility studies revealed that the solubility of loratadine is reduced from 35.85 mg/ml to 3.63 mg/ml, 15.39 mg/ml, 5.31 mg/ml, and 3.71 mg/ml in case of IL-1, IL-2, IL-3, and IL-4, respectively. Dissolution studies further confirmed this finding. Except for oleate, all the IL salts were found to be palatable by subjects with the score ranging from 2.5 to 2.8, which is the standard range for palatability.
 Conclusion: Results obtained in the present work indicated that IL salts of loratadine can be synthesized successfully using selected counter-ions. This approach can be used to mask the bitter taste of pure loratadine and thus can be used for the development of drug products intended for children.

Enhancement of Loratadine Dissolution by Surface Solid Dispersion: The Potential Use of Co-Processed Excipients as on-Surface Carriers

“…The spectral analysis of plain drug showed many characteristic bands, band at wave number 1700 cm -1 due to the C=O stretching, bands at 1437 cm -1 , 1225 cm -1 and 1105 cm -1 due to C-O stretching, and bands from 3000 cm -1 to 2880 cm -1 corresponds to C-H stretching [38][39][40].…”