An Investigation into the Relationship between Xanthan Gum Film Coating Materials and Predicted Oro-Esophageal Gliding Performance for Solid Oral Dosage Forms

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.

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A review of in vitro and in vivo methods and their correlations to assess mouthfeel of solid oral dosage forms

Drug Discovery Today ◽

10.1016/j.drudis.2020.12.015 ◽

2020 ◽

Author(s):

Abdullah Asiri ◽

Justyna Hofmanová ◽

Hannah Batchelor

Keyword(s):

Dosage Forms ◽

Oral Dosage ◽

Solid Oral Dosage Forms ◽

Oral Dosage Forms

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Multi-Analytical Framework to Assess the In Vitro Swallowability of Solid Oral Dosage Forms Targeting Patient Acceptability and Adherence

Pharmaceutics ◽

10.3390/pharmaceutics13030411 ◽

2021 ◽

Vol 13 (3) ◽

pp. 411

Author(s):

Abdul Latif Ershad ◽

Ali Rajabi-Siahboomi ◽

Shahrzad Missaghi ◽

Daniel Kirby ◽

Afzal Rahman Mohammed

Keyword(s):

Hydroxypropyl Methylcellulose ◽

Analytical Framework ◽

Dosage Forms ◽

Oral Dosage ◽

Surface Erosion ◽

World Population ◽

Swallowing Problems ◽

Solid Oral Dosage Forms ◽

Oral Dosage Forms

A lack of effective intervention in addressing patient non-adherence and the acceptability of solid oral dosage forms combined with the clinical consequences of swallowing problems in an ageing world population highlight the need for developing methods to study the swallowability of tablets. Due to the absence of suitable techniques, this study developed various in vitro analytical tools to assess physical properties governing the swallowing process of tablets by mimicking static and dynamic stages of time-independent oral transitioning events. Non-anatomical models with oral mucosa-mimicking surfaces were developed to assess the swallowability of tablets; an SLA 3D printed in vitro oral apparatus derived the coefficient of sliding friction and a friction sledge for a modified tensometer measured the shear adhesion profile. Film coat hydration and in vitro wettability was evaluated using a high-speed recording camera that provided quantitative measurements of micro-thickness changes, simulating static in vivo tablet–mucosa oral processing stages with artificial saliva. In order to ascertain the discriminatory power and validate the multianalytical framework, a range of commonly available tablet coating solutions and new compositions developed in our lab were comparatively evaluated according to a quantitative swallowability index that describes the mathematical relationship between the critical physical forces governing swallowability. This study showed that the absence of a film coat significantly impeded the ease of tablet gliding properties and formed chalky residues caused by immediate tablet surface erosion. Novel gelatin- and λ-carrageenan-based film coats exhibited an enhanced lubricity, lesser resistance to tangential motion, and reduced stickiness than polyvinyl alcohol (PVA)–PEG graft copolymer, hydroxypropyl methylcellulose (HPMC), and PVA-coated tablets; however, Opadry® EZ possessed the lowest friction–adhesion profile at 1.53 a.u., with the lowest work of adhesion profile at 1.28 J/mm2. For the first time, the in vitro analytical framework in this study provides a fast, cost-effective, and repeatable swallowability ranking method to screen the in vitro swallowability of solid oral medicines in an effort to aid formulators and the pharmaceutical industry to develop easy-to-swallow formulations.

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