Purpose <p>Benzydamine hydrochloride (BZD) is a nonsteroidal anti-inflammatory drug commonly used for the relief of acute sore throat. Currently, BZD is available in lozenges, oromucosal solutions, and sprays. This study aimed to develop and evaluate pastilles as an immediate-release dosage form for the local delivery of BZD in the oral cavity.</p> Methods <p>First, blank-loaded pastilles were formulated using various types and concentrations of sweeteners, to investigate their effects on the physical and mechanical properties, which were characterized by weight variation, friability, and texture profile analysis, along with different concentrations of gelatin. After characterization, BZD was loaded into the optimal formulation and evaluated for its physical, mechanical, and chemical properties using FT-IR and DSC, as well as BZD content, release profile, cytotoxicity and stability.</p> Results <p>The results found that sweeteners and gelatin influenced the pastille characteristics. Among the formulations, pastilles containing 15% w/w erythritol and 12.5% w/w gelatin exhibited optimal physical and mechanical properties suitable for oral use. BZD was successfully loaded into the pastille with acceptable content uniformity and demonstrated a rapid release profile, indicating an immediate-release pattern that was faster than that of the marketed lozenges. The cytotoxicity test indicated that BZD-loaded pastilles were biocompatible with oral cells. Furthermore, BZD was stable throughout the preparation process and storage at 30 ± 2&#xa0;°C for at least three months.</p> Conclusions <p>These findings suggest that BZD-loaded pastilles are a promising immediate-release formulation for local delivery in the oral cavity.</p>

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Development and Evaluation of Benzydamine Hydrochloride-Loaded Pastilles for Local Delivery in the Oral Cavity

  • Wipada Samprasit,
  • Praneet Opanasopit,
  • Benchawan Chamsai

摘要

Purpose

Benzydamine hydrochloride (BZD) is a nonsteroidal anti-inflammatory drug commonly used for the relief of acute sore throat. Currently, BZD is available in lozenges, oromucosal solutions, and sprays. This study aimed to develop and evaluate pastilles as an immediate-release dosage form for the local delivery of BZD in the oral cavity.

Methods

First, blank-loaded pastilles were formulated using various types and concentrations of sweeteners, to investigate their effects on the physical and mechanical properties, which were characterized by weight variation, friability, and texture profile analysis, along with different concentrations of gelatin. After characterization, BZD was loaded into the optimal formulation and evaluated for its physical, mechanical, and chemical properties using FT-IR and DSC, as well as BZD content, release profile, cytotoxicity and stability.

Results

The results found that sweeteners and gelatin influenced the pastille characteristics. Among the formulations, pastilles containing 15% w/w erythritol and 12.5% w/w gelatin exhibited optimal physical and mechanical properties suitable for oral use. BZD was successfully loaded into the pastille with acceptable content uniformity and demonstrated a rapid release profile, indicating an immediate-release pattern that was faster than that of the marketed lozenges. The cytotoxicity test indicated that BZD-loaded pastilles were biocompatible with oral cells. Furthermore, BZD was stable throughout the preparation process and storage at 30 ± 2 °C for at least three months.

Conclusions

These findings suggest that BZD-loaded pastilles are a promising immediate-release formulation for local delivery in the oral cavity.