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电子舌引导的掩味口服液的合理开发。

Rational development of taste masked oral liquids guided by an electronic tongue.

机构信息

Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University Duesseldorf, Universitaetsstr. 1, 40225 Duesseldorf, Germany.

出版信息

Int J Pharm. 2010 Nov 15;400(1-2):114-23. doi: 10.1016/j.ijpharm.2010.08.042. Epub 2010 Sep 9.

Abstract

Human taste testing is often associated with ethical concerns, organizational and validation issues. Electrochemical sensor array systems, so called electronic tongues, offer an alternative to assess the taste of multi-component liquid formulations. Therefore, it should be investigated how an electronic tongue can be implemented in the rational development of taste masked formulations. Taste masking of bitter tasting quinine hydrochloride (QH) in a liquid formulation was carried out by screening sweetening agents (sucrose, glucose, fructose, mannitol, sucralose, sodium saccharin, acesulfame potassium, and monoammonium glycyrrhizinate), strong and weak cation ion exchange (IE) resins (Amberlite™ IRP69, Amberlite™ IRP88, and Indion 234), and soluble complexing agents (α-, β-, hydroxypropyl-β-, sulfobutyl ether-β- and γ-cyclodextrin and maltodextrin). Amberlite™ IRP88 showed the best binding capacity for quinine (1.9 g quinine/1 g IE). The addition of sulfobutyl ether-β-cyclodextrin (SBE-β-CD) could significantly reduce the bitter taste of QH (79% reduction of free QH). The SBE-β-CD formulation was further improved by adding sodium saccharin as secondary taste masking agent. It could also be shown that presence of strawberry flavor and the preservative domiphen bromide does not affect evaluation of taste masking efficiency. The introduced stepwise approach was shown to be applicable to rationally develop novel taste masked formulations.

摘要

人类味觉测试通常与伦理问题、组织和验证问题有关。电化学传感器阵列系统,即所谓的电子舌,为评估多组分液体配方的味道提供了一种替代方法。因此,应该研究如何在合理开发掩味配方中实施电子舌。通过筛选甜味剂(蔗糖、葡萄糖、果糖、甘露醇、三氯蔗糖、糖精钠、安赛蜜钾和单铵甘草酸)、强阳离子和弱阳离子离子交换(IE)树脂(Amberlite™IRP69、Amberlite™IRP88 和 Indion 234)以及可溶性络合剂(α-、β-、羟丙基-β-、磺丁基醚-β-和 γ-环糊精和麦芽糊精),对盐酸奎宁(QH)在液体配方中的苦味进行掩味处理。Amberlite™IRP88 对奎宁的结合能力最强(1gIE 可结合 1.9g 奎宁)。添加磺丁基醚-β-环糊精(SBE-β-CD)可显著降低 QH 的苦味(游离 QH 减少 79%)。通过添加糖精钠作为二级掩味剂,进一步改善了 SBE-β-CD 配方。还可以证明,草莓味香精和防腐剂溴米那福的存在并不影响对掩味效率的评价。所引入的逐步方法适用于合理开发新型掩味配方。

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