LAPSE:2021.0200
Published Article
LAPSE:2021.0200
Impact of Hot-Melt-Extrusion on Solid-State Properties of Pharmaceutical Polymers and Classification Using Hierarchical Cluster Analysis
Ioannis Partheniadis, Miltiadis Toskas, Filippos-Michail Stavras, Georgios Menexes, Ioannis Nikolakakis
April 16, 2021
The impact of hot-melt extrusion (HME) on the solid-state properties of four methacrylic (Eudragit® L100-55, Eudragit® EPO, Eudragit® RSPO, Eudragit® RLPO) and four polyvinyl (Kollidon® VA64, Kollicoat® IR, Kollidon® SR, and Soluplus®) polymers was studied. Overall, HME decreased Tg but increased electrostatic charge and surface free energy. Packing density decreased with electrostatic charge, whereas Carr’s and Hausner indices showed a peak curve dependency. Overall, HME reduced work of compaction (Wc), deformability (expressed as Heckel PY and Kawakita 1/b model parameters and as slope S′ of derivative force/displacement curve), and tablet strength (TS) but increased elastic recovery (ER). TS showed a better correlation with S′ than PY and 1/b. Principal component analysis (PCA) organized the data of neat and extruded polymers into three principal components explaining 72.45% of the variance. The first included Wc, S′ and TS with positive loadings expressing compaction, and ER with negative loading opposing compaction; the second included PY, 1/b, and surface free energy expressing interactivity with positive loadings opposing tap density or close packing. Hierarchical cluster analysis (HCA) assembled polymers of similar solid-state properties regardless of HME treatment into a major cluster with rescaled distance Cluster Combine Index (CCI) < 5 and several other weaker clusters. Polymers in the major cluster were: neat and extruded Eudragit® RSPO, Kollicoat® IR, Kollidon® SR, Soluplus®, and extruded Eudragit® L100-55. It is suggested that PCA may be used to distinguish variables having similar or dissimilar activity, whereas HCA can be used to cluster polymers based on solid-state properties and pick exchangeable ones (e.g., for sustain release or dissolution improvement) when the need arises.
Keywords
classification, dendrograms, factor analysis, hot-melt extrusion, Polymers, powders
Suggested Citation
Partheniadis I, Toskas M, Stavras FM, Menexes G, Nikolakakis I. Impact of Hot-Melt-Extrusion on Solid-State Properties of Pharmaceutical Polymers and Classification Using Hierarchical Cluster Analysis. (2021). LAPSE:2021.0200
Author Affiliations
Partheniadis I: Department of Pharmaceutical Technology, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece [ORCID]
Toskas M: Department of Pharmaceutical Technology, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Stavras FM: Department of Pharmaceutical Technology, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Menexes G: Laboratory of Agronomy, School of Agriculture, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece [ORCID]
Nikolakakis I: Department of Pharmaceutical Technology, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece [ORCID]
Journal Name
Processes
Volume
8
Issue
10
Article Number
E1208
Year
2020
Publication Date
2020-09-25
Published Version
ISSN
2227-9717
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Original Submission
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PII: pr8101208, Publication Type: Journal Article
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LAPSE:2021.0200
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doi:10.3390/pr8101208
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Apr 16, 2021
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