应用于微型片剂的凝胶膜包衣用于掩味和改善吞咽性

文献信息

中文摘要

凝胶膜包衣（GFC）技术作为一种改善口服固体制剂吞咽性和掩味的策略已受到关注；然而，由于其高比表面积和制造限制，将其应用于微型片剂仍具有挑战性。本研究旨在使用标准薄膜包衣设备，开发一种简单且可放大的微型片剂GFC处方。以聚乙烯醇/聚乙二醇接枝共聚物（PVAPEG）作为基础聚合物，并筛选各种增稠剂以优化凝胶形成、崩解行为和表面粘附。对处方的最大挤出应力、崩解时间、溶出性能、药代动力学、感官特性和稳定性进行了评价。在所测试的处方中，黄原胶（XG）在降低粘附与控制崩解之间提供了最佳平衡。与未包衣处方相比，含PVAPEG和XG的GFC微型片剂显著改善了吞咽性和掩味效果，同时保持与参比产品相当的快速药物溶出。与市售产品的生物等效性得到确认，加速稳定性研究证明该处方具有优异的稳定性。这些发现表明，基于PVAPEG和XG的GFC微型片剂代表了一种稳健且可放大的处方策略，可在不损害药学性能的情况下提高患者可接受性。

英文摘要

Gelation film-coating (GFC) technology has attracted attention as a strategy to improve the swallowability and taste masking of oral solid dosage forms; however, its application to mini-tablets remains challenging because of their high specific surface area and manufacturing limitations. This study aimed to develop a simple and scalable GFC formulation for mini-tablets using standard film-coating equipment. A poly(vinyl alcohol)/polyethylene glycol graft copolymer (PVAPEG) was used as the base polymer, and various thickening agents were screened to optimize the gel formation, disintegration behavior, and surface adhesion. The formulations were evaluated in terms of maximum extrusion stress, disintegration time, dissolution performance, pharmacokinetics, sensory characteristics, and stability. Among the tested formulations, xanthan gum (XG) provided an optimal balance between reduced adhesion and controlled disintegration. GFC mini-tablets containing PVAPEG and XG significantly improved swallowability and bitterness masking compared to uncoated formulations, while maintaining rapid drug dissolution comparable to that of the reference product. Bioequivalence with the marketed product was confirmed, and accelerated stability studies demonstrated excellent stability of the formulation. These findings indicate that GFC mini-tablets based on PVAPEG and XG represent a robust and scalable formulation strategy that enhances patient acceptability without compromising the pharmaceutical performance.