Graz University of Technology, Inffeldgasse 13, 8010 Graz, Austria.
Graz University of Technology, Inffeldgasse 13, 8010 Graz, Austria; Capsugel, Rijksweg 11, 2880 Bornem, Belgium.
Colloids Surf B Biointerfaces. 2018 May 1;165:9-17. doi: 10.1016/j.colsurfb.2018.02.012. Epub 2018 Feb 9.
Solid oral dosage forms (SODF) are drug vehicles commonly prescribed by physicists in primary and secondary cares, as they are the most convenient for the patient and facilitate therapy management. Concerns regarding unintended adhesion of SODF during oro-esophageal transit remain, especially in multimorbid patients, bedridden patients and patients suffering from dysphagia. Hence, this factor should be considered during the development of SODF, and more attention should be given on the design of appropriate surface conditions considering patients with swallowing problems. The aim of this work was to estimate the low mucoadhesion strength of different pharmaceutical polymers frequently used in coating technologies, since this property is thought to have impact on the mucoadhesive profile of SODF during oro-esophageal transit. In an approach using in vitro methods based on particle interactions, polyethylene glycol grades (PEG) showed the lowest interaction forces suggesting a more favorable in vivo performance than hydroxypropyl methylcellulose (HPMC), which was found to have the highest particle interaction. Preference should be given to coating formulations with lower concentrations of polymer and grades with low molecular weight. In addition, rheological measurements should be adopted when targeting poor mucoadhesive polymers.
固体制剂(SODF)是初级和二级保健医生常用的药物载体,因为它们对患者最方便,并且有利于治疗管理。人们仍然担心 SODF 在经口-食管传递过程中意外黏附,尤其是在多系统疾病患者、卧床患者和吞咽困难患者中。因此,在 SODF 的开发过程中应考虑这一因素,并应更加关注考虑吞咽问题患者的适当表面条件的设计。本工作旨在评估经常用于包衣技术的不同药用聚合物的低黏膜黏附强度,因为该性质被认为对 SODF 在经口-食管传递过程中的黏膜黏附特性有影响。在基于粒子相互作用的体外方法中,聚乙二醇(PEG)等级显示出最低的相互作用力,表明在体内性能上比羟丙基甲基纤维素(HPMC)更有利,HPMC 被发现具有最高的粒子相互作用。应优先选择聚合物浓度较低和分子量较低的包衣配方。此外,当针对黏附性差的聚合物时,应采用流变学测量。