关键词: Particle interaction methods Polymer coatings Reduced mucoadhesion Rheological measurements Solid oral dosage forms Swallowing safety

Mesh : Adhesiveness Administration, Oral Dose-Response Relationship, Drug Drug Delivery Systems Hydrogen-Ion Concentration Hypromellose Derivatives Mucus / chemistry Nephelometry and Turbidimetry Particle Size Polyethylene Glycols Polymers / chemistry Povidone / chemistry Rheology Static Electricity

来  源:   DOI:10.1016/j.colsurfb.2018.02.012

Abstract:
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.
摘要:
固体口服剂型(SODF)是物理学家在初级和次级护理中通常开出的药物载体,因为它们对患者最方便,便于治疗管理。关于SODF在口食管转运过程中意外粘连的担忧仍然存在,尤其是在多患患者中,卧床不起的病人和吞咽困难的病人。因此,在SODF的开发过程中应该考虑这个因素,考虑到吞咽问题的患者,应更多地注意适当的表面条件的设计。这项工作的目的是估计涂层技术中常用的不同药物聚合物的低粘膜粘附强度,因为这种特性被认为对口食管转运过程中SODF的粘膜粘附特性有影响。在使用基于粒子相互作用的体外方法的方法中,聚乙二醇等级(PEG)显示出最低的相互作用力,表明比羟丙基甲基纤维素(HPMC)更有利的体内性能,被发现具有最高的粒子相互作用。应优选具有较低浓度的聚合物和低分子量等级的涂料配方。此外,当针对不良粘膜粘附聚合物时,应采用流变测量。
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