Tiwari Roshan V, Polk Ashley N, Patil Hemlata, Ye Xingyou, Pimparade Manjeet B, Repka Michael A
Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, University, Mississippi, 38677, USA.
Department of Psychology, The University of Mississippi, University, Mississippi, 38677, USA.
AAPS PharmSciTech. 2017 Feb;18(2):341-348. doi: 10.1208/s12249-015-0447-1. Epub 2015 Nov 16.
Developing a pediatric oral formulation with an age-appropriate dosage form and taste masking of naturally bitter active pharmaceutical ingredients (APIs) are key challenges for formulation scientists. Several techniques are used for taste masking of bitter APIs to improve formulation palatability; however, not all the techniques are applicable to pediatric dosage forms because of the limitations on the kind and concentration of the excipients that can be used. Hot-melt extrusion (HME) technology is used successfully for taste masking of bitter APIs and overcomes some of the limitations of the existing taste-masking techniques. Likewise, analytical taste assessment is an important quality control parameter evaluated by several in vivo and in vitro methods, such as the human taste panel, electrophysiological methods, electronic sensor, and animal preference tests to aid in selecting a taste-masked formulation. However, the most appropriate in vivo method to assess the taste-masking efficacy of pediatric formulations remains unknown because it is not known to what extent the human taste panel/electronic tongue can predict the palatability in the pediatric patients. The purpose of this study was to develop taste-masked caffeine citrate extrudates via HME and to demonstrate the wide applicability of a single bottle-test rat model to record and compare the volume consumed of the taste-masked solutions to that of the pure API. Thus, this rat model can be considered as a low-cost alternative taste-assessment method to the most commonly used expensive human taste panel/electronic tongue method for pediatric formulations.
开发具有适合儿童剂型且能掩盖天然苦味活性药物成分(API)味道的儿科口服制剂,是制剂科学家面临的关键挑战。有几种技术用于掩盖苦味API的味道以提高制剂的适口性;然而,由于可使用的辅料种类和浓度有限,并非所有技术都适用于儿科剂型。热熔挤出(HME)技术已成功用于掩盖苦味API的味道,并克服了现有掩味技术的一些局限性。同样,分析味觉评估是一个重要的质量控制参数,可通过多种体内和体外方法进行评估,如人体味觉小组、电生理方法、电子传感器和动物偏好测试,以帮助选择掩味制剂。然而,评估儿科制剂掩味效果的最合适体内方法仍然未知,因为尚不清楚人体味觉小组/电子舌在多大程度上能够预测儿科患者的适口性。本研究的目的是通过HME开发掩味的柠檬酸咖啡因挤出物,并证明单瓶试验大鼠模型在记录和比较掩味溶液与纯API消耗体积方面的广泛适用性。因此,对于儿科制剂而言,该大鼠模型可被视为一种低成本的替代味觉评估方法,以取代最常用但昂贵的人体味觉小组/电子舌方法。