Novel thermal imaging method for rapid screening of drug-polymer miscibility for solid dispersion based formulation development

Alhijjaj, Muqdad, Belton, Peter, Fabian, Laszlo, Wellner, Nikolaus, Reading, Michael and Qi, Sheng (2018) Novel thermal imaging method for rapid screening of drug-polymer miscibility for solid dispersion based formulation development. Molecular Pharmaceutics, 15 (12). 5625–5636. ISSN 1543-8384

[img]
Preview
PDF (Accepted manuscript) - Submitted Version
Download (1MB) | Preview

Abstract

This study aimed to develop a rapid, simple and inexpensive screening method for selecting the best polymeric candidates possessing high active pharmaceutical ingredient (API) miscibility during the early stages of formulation development of solid dispersion based pharmaceutical products. A new thermal imaging based method, thermal analysis by structural characterization (TASC), was used as a thermoptometeric tool in conjunction with data analysis software to detect the melting point depression and post-melting dissolution of felodipine particles screened over thin spin-coated films of ten polymers commonly used in the pharmaceutical field. On the polymeric substrates the drug showed different degrees of melting point reduction, reflecting their different levels of polymer-drug miscibility. Using TASC to detect melting point depression is significantly (20-40 times) faster than the conventional DSC method without loss of the sensitivity of detection. The quantity of the material required for the screening is less than 1/1000th of the material used in conventional DSC tests which significantly reduce the material wastage. Isothermal TASC tests and IR imaging confirmed the occurrence of thermal dissolution of the drug in the polymer for more miscible pairs. The real-time stability tests validate the accuracy of the polymer-drug miscibility screening results. These results demonstrate TASC as a promising screening tool for rapidly selecting the polymeric excipients for pharmaceutical formulations development.

Item Type: Article
Faculty \ School: Faculty of Science > School of Pharmacy
Faculty of Science > School of Chemistry
Depositing User: LivePure Connector
Date Deposited: 31 Oct 2018 10:30
Last Modified: 15 Sep 2020 23:49
URI: https://ueaeprints.uea.ac.uk/id/eprint/68714
DOI: 10.1021/acs.molpharmaceut.8b00798

Actions (login required)

View Item View Item