Chan, SY;
Qi, S;
Craig, DQ;
(2015)
An investigation into the influence of drug-polymer interactions on the miscibility, processability and structure of polyvinylpyrrolidone-based hot melt extrusion formulations.
International Journal of Pharmaceutics
, 496
(1)
pp. 95-106.
10.1016/j.ijpharm.2015.09.063.
Preview |
Text
Revised Sam1 2009.pdf Download (2MB) | Preview |
Abstract
While hot melt extrusion is now established within the pharmaceutical industry, the prediction of miscibility, processability and structural stability remains a pertinent issue, including the issue of whether molecular interaction is necessary for suitable performance. Here we integrate the use of theoretical and experimental drug-polymer interaction assessment with determination of processability and structure of dispersions in two polyvinylpyrrolidone-based polymers (PVP and PVP vinyl acetate, PVPVA). Caffeine and paracetamol were chosen as model drugs on the basis of their differing hydrogen bonding potential with PVP. Solubility parameter and interaction parameter calculations predicted a greater miscibility for paracetamol, while ATR-FTIR confirmed the hydrogen bonding propensity of the paracetamol with both polymers, with little interaction detected for caffeine. PVP was found to exhibit greater interaction and miscibility with paracetamol than did PVPVA. It was noted that lower processing temperatures (circa 40°C below the Tg of the polymer alone and Tm of the crystalline drug) and higher drug loadings with associated molecular dispersion up to 50% w/w were possible for the paracetamol dispersions, although molecular dispersion with the non-interactive caffeine was noted at loadings up to 20% w./w. A lower processing temperature was also noted for caffeine-loaded systems despite the absence of detectable interactions. The study has therefore indicated that theoretical and experimental detection of miscibility and drug-polymer interactions may lead to insights into product processing and extrudate structure, with direct molecular interaction representing a helpful but not essential aspect of drug-polymer combination prediction.
| Type: | Article |
|---|---|
| Title: | An investigation into the influence of drug-polymer interactions on the miscibility, processability and structure of polyvinylpyrrolidone-based hot melt extrusion formulations. |
| Location: | Netherlands |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1016/j.ijpharm.2015.09.063 |
| Publisher version: | http://dx.doi.org/10.1016/j.ijpharm.2015.09.063 |
| Language: | English |
| Additional information: | After an initial embargo period, this article is made available under a Creative Commons Attribution Non-commercial Non-derivative 4.0 International license (CC BY-NC-ND 4.0). This license allows you to share, copy, distribute and transmit the work for personal and non-commercial use providing author and publisher attribution is clearly stated. Further details about CC BY licenses are available at http://creativecommons.org/ licenses/by/4.0 |
| Keywords: | HME, Hot melt extrusion, Melting point depression, Polyvinylpyrrolidone, Solid dispersion, Solubility parameter |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics |
| URI: | https://discovery.ucl.ac.uk/id/eprint/1471688 |
Archive Staff Only
 |
View Item |
