Novel Thermal Imaging Method for Rapid Screening of Drug–Polymer Miscibility for Solid Dispersion Based Formulation Development

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 1/1000 th 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.

Analytical and Computational Methods for the Estimation of Drug-Polymer Solubility and Miscibility in Solid Dispersions Development

“…TASC technique is based on the algorithm that converts any change in the sample appearance during heating into a quantified signal, i.e., TASC curve [59]. Suitability of TASC as a technique for fast screening of the drug-polymer miscibility by evaluating the melting point depression has been demonstrated for felodipine and ten commonly used polymers in solid dispersion formulations [60]. Fast analysis, high sensitivity, and the requirement of a small amount of sample make this technique very attractive in the early stage of solid dispersion formulation development; however, further studies are necessary to confirm the usefulness of this technique.…”

An Image is Everything: A Tutorial on Choosing and Using the Components of a Dynamic Data Capture System

“…TASC was invented by Professor Mike Reading, working in the Department of Chemical Sciences at the University of Huddersfield in the UK, in 2017 [6]. Subsequent studies, with co-workers in the School of Pharmacy at the University of East Anglia in Norwich, Norfolk, UK, reported how TASC could be applied successfully to estimating drug-polymer miscibility and to the screening of drug-polymer combinations [7,8].…”

Vanadium Pentaoksida (V2O5) : Termodinamika Molecular dan Interaksi Ion dalam Larutan

“…Proses ini dapat dinamakan dengan cara pembentukan mineral evaporit (157)(158)(159)(160)(161)(162). Pada vanadium pentaoksida memiliki titik lebur (163)(164)(165)(166)…”