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Open AccessArticle

Investigation of Dissolution Mechanism and Release Kinetics of Poorly Water-Soluble Tadalafil from Amorphous Solid Dispersions Prepared by Various Methods

1
Department of Organic Technology, University of Chemistry and Technology, Prague, Technická 5, 166 28 Prague 6, Czech Republic
2
Department of Metals and Corrosion Engineering, University of Chemistry and Technology, Prague, Technická 5, 166 28 Prague 6, Czech Republic
3
Department of Polymers, University of Chemistry and Technology, Prague, Technická 5, 166 28 Prague 6, Czech Republic
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(8), 383; https://doi.org/10.3390/pharmaceutics11080383
Received: 2 July 2019 / Revised: 24 July 2019 / Accepted: 30 July 2019 / Published: 2 August 2019
(This article belongs to the Special Issue Recent Progress in Solid Dispersion Technology)
The aims of this study were to investigate how the release of tadalafil is influenced by two grades of polyvinylpyrrolidone (Kollidon® 12 PF and Kollidon® VA 64) and various methods of preparing solid dispersions (solvent evaporation, spray drying and hot-melt extrusion). Tadalafil is poorly water-soluble and its high melting point makes it very sensitive to the solid dispersion preparation method. Therefore, the objectives were to make a comparative evaluation among different solid dispersions and to assess the effect of the physicochemical nature of solid dispersions on the drug release profile with respect to the erosion-diffusion mechanism. The solid dispersions were evaluated for dissolution profiles, XRD, SEM, FT-IR, DSC, and solubility or stability studies. It was found that tadalafil release was influenced by polymer molecular weight. Therefore, solid dispersions containing Kollidon® 12 PF showed a faster dissolution rate compared to Kollidon® VA 64. Tadalafil was released from solid dispersions containing Kollidon® 12 PF because of the combination of erosion and diffusion mechanisms. The diffusion mechanisms were predominant in the initial phase of the experiment and the slow erosion was dissolution-controlling at the second stage of the dissolution. On the contrary, the tadalafil release rate from solid dispersions containing Kollidon® VA 64 was controlled solely by the erosion mechanism. View Full-Text
Keywords: solid dispersion; tadalafil; Wood’s apparatus; intrinsic dissolution rate; Weibull dissolution model; dissolution rate solid dispersion; tadalafil; Wood’s apparatus; intrinsic dissolution rate; Weibull dissolution model; dissolution rate
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MDPI and ACS Style

Školáková, T.; Slámová, M.; Školáková, A.; Kadeřábková, A.; Patera, J.; Zámostný, P. Investigation of Dissolution Mechanism and Release Kinetics of Poorly Water-Soluble Tadalafil from Amorphous Solid Dispersions Prepared by Various Methods. Pharmaceutics 2019, 11, 383.

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