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International journal of pharmaceutics · 2026

Improving the palatability of Platycodonic Radix for pediatric use: Integrating LC-MS-based bitter component profiling with an HP-β-Cyclodextrin/xylitol taste-masking strategy.

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Zhou Zhiqing, Zhang Shiman, Fang Can, Cheng Hong, Yasheng Mayire, Yuan Jinfeng, Cai Wangyan, Fang Zihan, Wu Fei, Wang Youjie, Xue Zheng, Zhang Xinguang

Аннотация

Platycodonic Radix (PR) is a key herb in traditional Chinese prescriptions for pediatric respiratory disorders. However, its intense bitterness and persistent throat astringency reduce treatment compliance. This study established a mechanism-informed taste-masking strategy integrating chemical profiling, sensory evaluation, and formulation optimization. PR sensory characteristics were first quantified using human panels and an electronic tongue. Subsequently, PR water extracts were characterized by non-targeted profiling based on liquid chromatography-mass spectrometry (LC-MS). Putative bitter constituents were further screened using BitterX-assisted TAS2R molecular docking. The optimized formulation was then validated in two representative pediatric formulas containing the classical "PR-Glycyrrhiza uralensis Fisch." herb pair. LC-MS tentatively identified 308 compounds in PR decoctions, mainly carbohydrates and glycosides. Docking results indicated that platycodigenin, polygalacic acid, lactone-type platycodins, luteolin, and lignans show high affinity for human bitter taste receptors TAS2R14, TAS2R44, and TAS2R47, confirming a multi-component basis for PR bitterness. Among the excipients tested, 2-Hydroxypropyl-β-cyclodextrin (HP-β-CD) and xylitol were most effective. Mechanistically, HP-β-CD primarily suppressed residual bitterness and astringency, whereas xylitol improved initial mouthfeel. An optimized combination of 6.5 % HP-β-CD plus 10 % xylitol (w/w relative to PR) successfully transformed PR decoctions from "difficult to accept" to "sweet with no lingering bitterness", a shift corroborated by electronic tongue DFA plots. This strategy improved palatability in two representative pediatric formulas without altering the herbal composition. These findings demonstrate that 6.5 % HP-β-CD plus 10 % xylitol effectively alleviates both initial bitterness and throat irritation, offering a practical, non-destructive solution to enhance pediatric medication adherence in traditional phytotherapy.

Предметные рубрики MeSH

ИП Урсолов Владлен Сергеевич

ИНН 500118482352 · ОГРНИП 314500117700049

Реквизиты и контакты