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<p>The taste of a drug impacts the compliance of patients for oral administration. In this study, the bitter taste of diclofenac sodium (DS) was masked with purolite A430MR through ion exchange. The DS-A430MR complexes (DACs) were prepared at a 1:1 (<i>w/w</i>) drug to resin through a simple aqueous binding process. The key factors affecting release behaviors were identified by optimized experiments. The taste masking effect of the DACs was evaluated by human taste panel studies and simulated saliva release. The physical characterization proved successful preparation of DACs. The released experiments demonstrated that the pH values, types, and strengths of counter ions were important factors affecting the DS release from the DACs. The simulated saliva release profiles demonstrated that the DS concentration in oral cavity was lower than its bitterness threshold. The bitter taste of DS was almost completely masked by the IERs, which provided guidance for the development of palatable oral preparations using IERs.</p> Graphical Abstract <p><b>Schematic illustration.</b> A schematic diagram of the formation of DACs and drug exchange processes <i>in vivo</i>.</p> <p></p>

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Preparation and Characterization of Diclofenac Sodium-Purolite A430MR Complexes for Taste Masking

  • 期刊论文

  • 发表日期：

    2025年6月3日

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  • Genyang Ye,
  • Qun Wang,
  • Yibo Shang,
  • Yibo Li,
  • Rui Yang,
  • Boyu Jing,
  • Qiang Fu

摘要

The taste of a drug impacts the compliance of patients for oral administration. In this study, the bitter taste of diclofenac sodium (DS) was masked with purolite A430MR through ion exchange. The DS-A430MR complexes (DACs) were prepared at a 1:1 (w/w) drug to resin through a simple aqueous binding process. The key factors affecting release behaviors were identified by optimized experiments. The taste masking effect of the DACs was evaluated by human taste panel studies and simulated saliva release. The physical characterization proved successful preparation of DACs. The released experiments demonstrated that the pH values, types, and strengths of counter ions were important factors affecting the DS release from the DACs. The simulated saliva release profiles demonstrated that the DS concentration in oral cavity was lower than its bitterness threshold. The bitter taste of DS was almost completely masked by the IERs, which provided guidance for the development of palatable oral preparations using IERs.

Graphical Abstract

Schematic illustration. A schematic diagram of the formation of DACs and drug exchange processes in vivo.