Purpose

The objective of the study was to develop sublingual wafers loaded with esomeprazole magnesium trihydrate (EMT) that exhibit rapid dissolution and enhanced penetration upon administration through sublingual mucosa, thereby ensuring immediate action.

Method

Sublingual wafers containing esomeprazole magnesium trihydrate were prepared using the solvent casting method. The formulation included different concentrations of hydroxypropyl methylcellulose E-15 (HPMC E-15), sodium starch glycolate (SSG), and polyethylene glycol 400 (PEG 400), as suggested by the DESIGN EXPERT software. An optimization strategy employing desirability values was utilized to optimize the responses. The wafers underwent physical characterization and in vitro dissolution study, followed by ex vivo drug permeation assessment and histopathological evaluation.

Results

The optimized sublingual wafers exhibited disintegration time of 27.67 ± 0.92 s, folding endurance of 299.71 ± 1.67, and drug content of 92.99 ± 3.37% with a percent deviation of less than 5. In vitro release study showed 82.92 ± 4.13% drug release in the 90s, following the Korsmeyer-Peppas mechanism. Ex vivo permeation demonstrated 80.07 ± 3.04% drug diffusion in 90 s. Histopathological investigations confirmed the safety of optimized wafers on sheep’s sublingual mucosa. Short-term stability study revealed the wafer’s stability for three months at 25–27 °C and 60% relative humidity.

Conclusion

The formulation of esomeprazole magnesium trihydrate (EMT)-loaded wafer is expected to enhance patient compliance by eliminating the requirement of water intake during the treatment of peptic ulcers and the need for swallowing. Moreover, the wafer offers a rapid onset of action and quick disintegration, providing a fast and convenient treatment option.

中文翻译：

---

埃索美拉唑快速释放舌下含片：配方、优化和表征

目的

该研究的目的是开发装载有埃索美拉唑镁三水合物（EMT）的舌下糯米纸片，其在通过舌下粘膜给药后表现出快速溶解和增强的渗透性，从而确保立即发挥作用。

方法

使用溶剂浇铸法制备含有埃索美拉唑镁三水合物的舌下糯米纸囊剂。根据 DESIGN EXPERT 软件的建议，该制剂包含不同浓度的羟丙基甲基纤维素 E-15 (HPMC E-15)、羟基乙酸淀粉钠 (SSG) 和聚乙二醇 400 (PEG 400)。采用采用意愿值的优化策略来优化响应。对晶片进行物理表征和体外溶出研究，然后进行离体药物渗透评估和组织病理学评估。

结果

优化后的舌下含片崩解时间为 27.67 ± 0.92 s，耐折度为 299.71 ± 1.67，药物含量为 92.99 ± 3.37%，偏差百分比小于 5。体外释放研究显示，舌下含片的药物释放率为 82.92 ± 4.13%。 90 年代，遵循 Korsmeyer-Peppas 机制。体外渗透表明 90 秒内药物扩散率为 80.07 ± 3.04%。组织病理学研究证实了优化晶片在绵羊舌下粘膜上的安全性。短期稳定性研究表明，该晶圆在 25–27 °C 和 60% 相对湿度下可保持三个月的稳定性。

结论

埃索美拉唑镁三水合物（EMT）的配方有望通过消除消化性溃疡治疗期间的饮水需求和吞咽需求来提高患者的依从性。此外，该晶片具有快速起效和快速崩解的作用，提供了快速、方便的治疗选择。