Bitterness Evaluation of H1-Receptor Antagonists Using a Taste Sensor

Abstract

The objective of this study was to evaluate an improved bitterness sensor, which, it is postulated, will allow a more precise and sensitive prediction of the bitterness of active pharmaceutical substances. The bitterness sensor, BT0, has a membrane surface with improved and optimized hydrophobicity, and was developed to enhance the hydrophobic interaction between the membrane and basic bitter substances. The bitterness of eight H 1 -receptor antagonists was measured using a multichannel tastesensing system incorporating sensor BT0. Three variables, relative value (R), change in membrane potential caused by adsorption (CPA) and adsorption ability (CPA/R), were used in the evaluation. For sample solutions of the eight H 1 -receptor antagonists, higher sensor output values of R and CPA were observed with sensor BT0, in comparison with a conventional bitterness sensor, AN0. The higher output values seem to be due to the superior hydrophobic interactions between the BT0 sensor membrane and basic bitter substances, as sensor BT0 also showed higher CPA/R values. The data suggest that sensor BT0 provides a more sensitive bitterness evaluation, being able to detect bitterness in sample solution concentrations as low as 0.01 mg/ml. The eight H 1 -receptor antagonists could be categorized into three groups by principal component analysis using data from sensor BT0. Sensor output from sensor BT0 could be used to discriminate effectively between drugs without the need for performing laborious gustatory sensation tests.

The Effect of Food Thickeners on the Bitterness and Dissolution of Amlodipine Besilate Powder When Co-Administered with Thickeners to Patients with Dysphagia

“…In this study, the CPA of membrane AN0 was used, which is suitable for the evaluation of bitterness of basic substances. The taste sensor measurements were performed as described in previous articles [13] [14] [15] [16] [17].…”

Evaluation of the Palatability of Dry Syrups and the Bitterness Intensities of Dry Syrups Mixed with Various Beverages

“…Sensor AC0, developed specifically to detect the bitterness of basic substances [14] [15] [16], was used in these experiments. The taste sensor measurements were performed to evaluate bitterness intensity for amlodipine besilate [6], solifenacin succinate [7], H 1 -receptor antagonists [9] and topiramate [17] as described in previous articles. The measurement procedure is as follows: the electrodes are dipped into the reference solution and the electric potential obtained (mV) is defined as Vr 0 .…”

“…The bitterness of active pharmaceutical ingredients in oral pharmaceutical formulations has previously been evaluated using the artificial taste sensor or "electronic tongue" [4]- [10]. There are several types of sensors which have different components of lipids and plasticizers and are sensitive to different materials: C00 is sensitive to acidic bitter materials such as diclofenac sodium, a non-steroidal anti-inflammatory drug [4]; AE1 is sensitive to astringent materials such as tannic acid; AC0 and AN0 are sensitive to basic materials such as solifenacin succinate [6] or amlodipine besilate [7] and BT0 is sensitive to hydrochloride salts, including quinine hydrochloride [9]. The bitterness of an active pharmaceutical ingredient in oral pharmaceutical formulations mixed with various foods or beverages has also been evaluated using a taste sensor [11] [12].…”

Preparation and Characterization of Orally Fast-Disintegrating Mini-Tablets Containing Diphenhydramine Hydrochloride and Aspartic or Glutamic Acid as an Umami Amino Acid

“…Sensors have been developed specifically to detect various tastes. Sensor AN0 which detects the bitterness of basic substances [8] [10] [11] [12] [13] [14] was selected for this study. Taste sensor measurements were performed as described in previous articles [8] [10]- [17].…”