Oswaldo Cruz Foundation, Sizenando Nabuco Street, 100, Rio de Janeiro, RJ, Brazil.
Material Department, National Institute of Technology, Rio de Janeiro, RJ, Brazil.
AAPS PharmSciTech. 2021 Dec 14;23(1):22. doi: 10.1208/s12249-021-02162-z.
The assessment of drug taste is crucial for pediatric treatments so that formulations can be developed to enhance their effectiveness. In this study, in vivo and in vitro methods were applied to evaluate the taste of tablets of three drugs administered to children without taste-masking excipients to treat tropical diseases, namely artesunate-mefloquine (ASMQ), praziquantel (PZQ), and benznidazole (BNZ). In the first method, a model of rat palatability was adapted with recirculation to ensure sample dispersion, and the data were analyzed using ANOVA (single factor, 95%). The taste assessment results (in vivo) indicated an aversion to the three medicines, denoted by the animals retracting themselves to the bottom of the box after the first contact with the drugs. For the placebo samples, the animals behaved normally, indicating that taste perception was acceptable. The second method was based on the in vitro analysis of capacitance data from a homemade impedimetric electronic tongue. Consistent with the in vivo taste assessment results, the data points obtained with PZQ, ASMQ, and BNZ were far away from those of their placebos in a map built with the multidimensional projection technique referred to as Interactive Document Mapping (IDMAP). A combined analysis of the results with the two methods allowed us to confirm the bitterness of the three drugs, also pointing to electronic tongues as a promising tool to replace in vivo palatability tests.
药物味觉评估对于儿科治疗至关重要,以便可以开发出增强其疗效的配方。在这项研究中,应用体内和体外方法评估了三种无掩味赋形剂用于治疗热带病的儿童药物片剂的味觉,即青蒿琥酯-甲氟喹(ASMQ)、吡喹酮(PZQ)和苯并咪唑(BNZ)。在第一种方法中,适应了大鼠味觉模型的再循环以确保样品分散,并使用方差分析(单因素,95%)分析数据。味觉评估结果(体内)表明对三种药物的厌恶,动物在第一次接触药物后缩回箱子底部表示。对于安慰剂样本,动物行为正常,表明味觉感知可接受。第二种方法基于自制阻抗电子舌的电容数据的体外分析。与体内味觉评估结果一致,用多维投影技术(称为交互式文档映射(IDMAP))构建的图谱中,来自 PZQ、ASMQ 和 BNZ 的数据点远离其安慰剂的点。两种方法的结果综合分析证实了这三种药物的苦味,也指出电子舌是替代体内味觉测试的有前途的工具。