An in-vitro-in-vivo taste assessment of bitter drug: comparative electronic tongues study.

Abstract

The efficiency of the Astree e-tongue and Taste Sensing system TS5000Z for the evaluation of the taste masking effect of hot melt extruded formulations was investigated in this study. Hot melt extrusion (HME) processing was optimized using Randcastle single screw extruder (USA) to manufacture extrudates with desirable characteristics. Cationic model drug propranolol HCl (PRP) was processed with the anionic polymers - Eudragit L100 (L100) and Eudragit L100-55 (Acryl-EZE). Solid state of the drug in polymer matrices was evaluated by scanning electron microscopy (SEM), differential scanning calorimetry, particle size analysis, Fourier transform infrared (FTIR) and Nuclear magnetic resonance (NMR) analysis. In-vitro taste masking efficiency of the two polymers was performed by using two different e-tongues (Astree e-tongue and TS5000Z). The results obtained from both e-tongues were further compared and contrast to find out the sensor outputs in all formulations. Solid state analysis of the extruded formulations revealed the presence of amorphous PRP. Both e-tongues were able to detect the taste masking variations of the extrudates and were in good agreement with the in-vivo results obtained from a panel of six healthy human volunteers (R(2) > 0.84). However, each e-tongue sensor demonstrated different sensitivity, suggesting a careful consideration of the experimental findings during melt extrusion, is necessary for the development of taste-masked formulations. Furthermore, FTIR spectroscopy and NMR studies revealed possible drug polymer intermolecular interactions as the mechanism of successful taste masking. HME can effectively be used to manufacture taste-masked extruded formulations, while both e-tongues demonstrated satisfactory taste analysis for the development of taste-masked formulations.