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Solid microcrystalline dispersion films as a new strategy to improve the dissolution rate of poorly water soluble drugs: a case study using olanzapine

Modica de Mohac, L; de Fátima Pina, M; Raimi-Abraham, BT; (2016) Solid microcrystalline dispersion films as a new strategy to improve the dissolution rate of poorly water soluble drugs: a case study using olanzapine. International Journal of Pharmaceutics , 508 (1-2) pp. 42-50. 10.1016/j.ijpharm.2016.05.012. Green open access

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Abstract

In this study, we evaluate the dissolution rate enhancement of solid microcrystalline dispersion (SMD) films of olanzapine (OLZ) formulated with four water-soluble polymers namely poly(N-vinylpyrrolidone) (PVP), poloxamer 188 (P188), poloxamer 407 (P407) and Soluplus(®) (SLP). Prepared formulations were characterised to determine particle size, morphology, hydrogen bonding interactions, thermal characteristics as well as in vitro dissolution studies conducted under sink conditions (pH 6.8). Particle size of OLZ in all formulations ranged between 42 and 58μm. Attenuated Total Reflectance Fourier Transform Infrared spectroscopy (ATR-FTIR), Differential Scanning Calorimetry (DSC) and Hot-Stage Microscopy (HSM) studies confirmed OLZ was well maintained in its crystalline state during the formulation process. In vitro dissolution studies showed immediate drug release from all formulation when compared to the drug alone. The greatest increase in in vitro dissolution rate was observed in formulations containing P188 most likely due to its enhanced hydrophilic and surfactant properties compared to the other agents used. Overall, this study successfully generated OLZ loaded SMD films with improved in vitro dissolution rates which is highly likely to result in improved oral bioavailability in vivo.

Type: Article
Title: Solid microcrystalline dispersion films as a new strategy to improve the dissolution rate of poorly water soluble drugs: a case study using olanzapine
Location: Netherlands
Open access status: An open access version is available from UCL Discovery
DOI: 10.1016/j.ijpharm.2016.05.012
Publisher version: http://dx.doi.org/10.1016/j.ijpharm.2016.05.012
Language: English
Additional information: Copyright © 2016 Elsevier B.V. All rights reserved. This manuscript version is made available under the CC-BY-NC-ND 4.0 license (http://creativecommons.org/licenses/by-nc-nd/4.0); the published version of the article is available at http://dx.doi.org/10.1016/j.ijpharm.2016.05.012
Keywords: Solid microcrystalline dispersion; Pharmaceutical film; Crystalline; Olanzapine; Polymer; PVP
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
URI: https://discovery.ucl.ac.uk/id/eprint/1493071
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