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采用 Smartseal 30D 和 ReadyMix 对微囊化苦味药物进行掩味比较评价。用于儿科剂型。

Comparative taste-masking evaluation of microencapsulated bitter drugs using Smartseal 30D and ReadyMix for paediatric dosage forms.

机构信息

Faculty of Engineering and Science, University of Greenwich, Medway Campus, ME4 4TB, Chatham Maritime, Kent, UK.

Cubi-Tech Extrusion Limited, Unit 3, Sextant park, Neptune Close, Rochester, Kent, ME2 4LU, UK.

出版信息

AAPS PharmSciTech. 2021 Apr 21;22(4):141. doi: 10.1208/s12249-021-02002-0.

Abstract

The taste of drug substances plays a key role in the development of paediatric formulations with suitable organoleptic properties. The aim of the study was to evaluate the taste masking effectiveness of Smartseal 30D and ReadyMix on a range of bitter drug substances such as diphenhydramine HCl (DPD), ibuprofen lysine (IBU-LS), and phenylephrine HCl (PPH) for the development of paediatric dosage forms. The drugs were microencapsulated in the polymer carriers at 10-20% loadings using spray-drying processing. Spray drying of drug formulations was optimized in terms of percent yield and encapsulation efficiency followed by physicochemical characterization in order to identify the drugs' physical state in the polymer microparticles. The in vivo taste masking efficiency was evaluated using human test panel and showed noticeable reduction of drug's bitterness at all loadings in comparison to the bulk substances.

摘要

药物的味道在儿科制剂的开发中起着关键作用,具有合适的感官特性。本研究的目的是评估 Smartseal 30D 和 ReadyMix 对一系列苦味药物(如盐酸苯海拉明(DPD)、赖氨酸布洛芬(IBU-LS)和盐酸苯肾上腺素(PPH))的掩味效果,以开发儿科剂型。使用喷雾干燥工艺,将药物以 10-20%的载药量包埋在聚合物载体中。对药物配方的喷雾干燥进行了优化,以获得产率和包封效率,然后对其进行物理化学特性分析,以确定药物在聚合物微球中的物理状态。通过人体测试小组评估了体内掩味效率,与原料药相比,在所有载药量下均能显著降低药物的苦味。

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