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Abstract：
Oral drug therapy is generally provided in the form of solid oral dosage forms (SODF) that have to be swallowed and move throughout the oro-esophageal system. Previous studies have provided evidence that the oro-esophageal transit of SODF depends on their shape, size, density, and surface characteristics. To estimate the impact of SODF surface coatings during esophageal transit, an in vitro system was implemented to investigate the gliding performance across an artificial mucous layer. In this work, formulations comprised of different slippery-inducing agents combined with a common film forming agent were evaluated using the artificial mucous layer system. Xanthan gum (XG) and polyethylene glycol 1500 (PEG) were applied as film-forming agents, while carnauba wax (CW), lecithin (LE), carrageenan (CA), gellan gum (GG) and sodium alginate (SA), and their combination with sodium lauryl sulfate (SLS), were applied as slippery-inducing components. All tested formulations presented lower static friction (SF) as compared to the negative control (uncoated disc, C, F0), whereas only CW/SLS-based formulations showed similar performance to F0 regarding dynamic friction (DF). The applied multivariate analysis approach allowed a higher level of detail to the evaluation and supported a better identification of excipients and respective concentrations that are predicted to improve in vivo swallowing safety.
摘要：
口服药物治疗通常以固体口服剂型(SODF)的形式提供,其必须被吞咽并在整个口食管系统中移动。以前的研究提供了证据，表明SODF的口食管运输取决于它们的形状，尺寸,密度,和表面特征。为了评估食管转运过程中SODF表面涂层的影响，实施了体外系统来研究在人造粘液层的滑动性能。在这项工作中,使用人工粘液层系统评估了由不同的滑脱诱导剂与普通成膜剂组合组成的制剂。黄原胶（XG）和聚乙二醇1500（PEG）作为成膜剂，而巴西棕榈蜡（CW），卵磷脂（LE），角叉菜胶（CA），结冷胶（GG）和海藻酸钠（SA），以及它们与十二烷基硫酸钠（SLS）的组合，作为滑溜诱导成分应用。与阴性对照(未涂覆的圆盘，C,F0),而只有基于CW/SLS的配方在动态摩擦（DF）方面表现出与F0相似的性能。所应用的多变量分析方法允许对评估进行更高水平的细节,并支持更好地鉴定预测改善体内吞咽安全性的赋形剂和相应浓度。
