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Journal ArticleDOI

Influence of Polymeric Additive on the Physical Stability and Viscoelastic Properties of Aripiprazole.

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TLDR
Due to the better stabilization effect and the more favorable rheological properties, KVA proved to be a better polymeric excipient for extrusion of amorphous aripiprazole.
Abstract
In this article, we investigated aripiprazole + Kollidon VA64 (ARP/KVA) and aripiprazole + Soluplus (ARP/SOP) amorphous solid dispersions. Thermal properties of all prepared systems have been examined by means of differential scanning calorimetry (DSC). Compositions revealing the recrystallization tendency were subsequently investigated by means of broadband dielectric spectroscopy (BDS). On the basis of dielectric data, the physically stable drug-polymer concentrations have been found. Finally, these systems have been investigated by rheology, which enables us to determine the minimal temperature required for dissolving the drug in the polymeric matrix, as well as the temperature dependence of the sample viscosity. Our investigations have shown that the amorphous form of the investigated antipsychotic drug might be effectively stabilized by both employed polymers. However, due to the better stabilization effect and the more favorable rheological properties, KVA proved to be a better polymeric excipient for extrusion of amorphous aripiprazole.

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Journal ArticleDOI

Orodispersible films containing ball milled aripiprazole-poloxamer®407 solid dispersions.

TL;DR: This research aimed at developing ODFs containing an antipsychotic drug - aripiprazole (ARP) found that co-processing led to an over 100-fold increase in drug solubility in comparison with pure drug.
Journal ArticleDOI

Review of melt crystallization in the pharmaceutical field, towards crystal engineering and continuous process development

TL;DR: In this article, the advances of melt crystallization in the pharmaceutical field towards crystal engineering and continuous process development are summarized, and critical concerns and opportunities for further research and perspectives are proposed.
Journal ArticleDOI

Dielectric Study on the Well-Resolved Sub-Rouse and JG β-Relaxations of Poly(methylphenylsiloxane) at Ambient and Elevated Pressures

TL;DR: In this article, the dielectric behavior of poly(methylphenylsiloxane) was revisited to investigate the well-resolved α′- and β-relaxations found on the low and high-frequency flanks of the segmental (α) re...
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Compression-Induced Phase Transitions of Bicalutamide

TL;DR: The formation of solid dispersions with the amorphous drug dispersed in the polymeric matrix improves the dissolution characteristics of poorly soluble drugs and exhibits improved wettability and dissolution enhanced by 2.5- to 11-fold in comparison with the crystalline drug.
References
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Journal ArticleDOI

Improving drug solubility for oral delivery using solid dispersions.

TL;DR: The historical background and definitions of the various systems including eutectic mixtures, solid dispersions and solid solutions, as well as the production, the different carriers and the methods used for the characterization of solid dispersion are outlined.
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Pharmaceutical Applications of Hot-Melt Extrusion: Part I

TL;DR: The pharmaceutical applications of hot-melt extrusion, including equipment, principles of operation, and process technology, are reviewed and the physicochemical properties of the resultant dosage forms are described.
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Drug polymorphism and dosage form design: a practical perspective.

TL;DR: If there is no particular medical benefit, there is less justification for accepting the risks of intentional development of a metastable crystalline or amorphous form and laboratory work which provides assurance that the largest possible form change will have no substantive effect on product quality or bioavailability is provided.
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Solid state amorphization of pharmaceuticals.

TL;DR: The purpose of this short review paper is to illustrate the possibility to amorphize one compound by several different routes and to rationalize the observed transformations using the concepts of effective temperature introduced in nonequilibrium physics.
Journal ArticleDOI

Hot melt extrusion (HME) for amorphous solid dispersions: Predictive tools for processing and impact of drug–polymer interactions on supersaturation

TL;DR: The highest dissolution rate and supersaturation of poorly water soluble drugs could be attributed to drug-polymer interactions occurred during HME.
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