Evaluation of taste-masking effects of pharmaceutical sweeteners with an electronic tongue system

Abstract

Electronic tongue systems have been developed for taste measurement of bitter drug substances in accurate taste comparison to development palatable oral formulations. This study was to evaluate the taste masking effect of conventional pharmaceutical sweeteners such as neohesperidin dihydrochalcone, sucrose, sucralose and aspartame. The model drugs were acetaminophen, ibuprofen, tramadol hydrochloride, and sildenafil citrate (all at 20 mM). The degree of bitterness was measured by a multichannel taste sensor system (an electronic tongue). The data was collected by seven sensors and analyzed by a statistical method of principal components analysis (PCA). The effect of taste masking excipient was dependent on the type of model drug. Changing the concentration of taste masking excipients affected the sensitivity of taste masking effect according to the type of drug. As the excipient concentration increased, the effect of taste masking increased. Moreover, most of the sensors showed a concentration-dependent pattern of the taste-masking agents as higher concentration provided higher selectivity. This might indicate that the sensors can detect small concentration changes of a chemical in solution. These results suggest that the taste masking could be evaluated based on the data of the electronic tongue system and that the formulation development process could be performed in a more efficient way.

Critical Evaluation of Laboratory Potentiometric Electronic Tongues for Pharmaceutical Analysis—An Overview

“…Since the majority of active pharmaceutical ingredients (APIs) exhibit bitter taste, various taste-masking approaches have been developed in order to reduce unpleasant sensation [38][39][40]. The efficiency of taste-masking, obtained by addition of sweeteners [41], microencapsulation [42], hot-melt extrusion [43], cations exchangers, and complexing agents [44] has been assessed with commercially available models and laboratory prototypes of electronic tongues. In all cases, the utilized devices were able to distinguish samples of different taste profiles.…”

Independent comparison study of six different electronic tongues applied for pharmaceutical analysis

“…When performing PCA excluding samples 5 and 7 and thus those samples, which neither contained caffeine citrate nor citric acid, and showed a differing pH value, the four potentiometric working e-tongues provided for pronounced discrimination between samples containing saccharin sodium (samples 4,8,9) and those without saccharin sodium (samples 1, 2, 3, 6) (Fig. 4).…”

“…Since then, multichannel taste sensor that later became a fundamental part of commercial taste sensing system by Insent had been used for quantification of basic taste sensations in large variety of samples [2][3][4]. Various studies were devoted to the application of different versions of e-tongues for the assessment of taste in pharmaceutical samples [5][6][7][8][9][10][11][12][13][14][15][16]. A variety of sensors and sensor systems were developed and applied in these research efforts, based on both, commercial [5,6,9,10,[13][14][15] or laboratory instrumentation [7,8,11,16].…”

Engineering Size and Structure of Particles in Novel Modified-Release Delivery Systems

“…Besides the foremost and simplest approach of adding sweeteners and/or flavors, other taste-masking techniques have also been developed, such as coating drug particles with polymers, forming inclusion complexes, using ion-exchange resins, producing multiparticulate taste-masking systems with lipids by hot-melting extrusion, and so forth (51)(52)(53)(54)(55)(56)(57). As a whole, modification of microparticles based on particle engineering, especially forming a core-shell or embedded structure, occupies an indispensable status.…”