Miniaturized screening of polymers for amorphous drug stabilization (SPADS): Rapid assessment of solid dispersion systems

Wyttenbach, Nicole; Janas, Christine; Siam, Monira; Lauer, Matthias E.; Jacob, Laurence; Scheubel, Emmanuel; Page, Susanne

doi:10.1016/j.ejpb.2013.01.009

Cited by 57 publications

(38 citation statements)

References 38 publications

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“…Screen Polymers for Amorphous Drug Stabilization (SPADS) is one such approach widely used to identify polymers that can generate and maintain supersaturation and stabilize an amorphous drug in the formulation matrix. Wyttenbach et al (2013) presented the workflow and experimental aspects of the SPADS approach with seven different polymers and four drugs.…”

Section: Commonly Used Polymers To Stabilize Amorphous Pharmaceuticalsmentioning

confidence: 99%

“…The use of conventional methods such as hot-melt extrusion, rotary evaporation, spray-drying, or freeze-drying during the preliminary screening stage could be time and resource intensive. In an attempt to cut down the time and resources, miniaturized methods have been developed to efficiently screen the polymers that facilitate amorphous formulation (Wyttenbach et al 2013). A comprehensive overview of various miniaturized assays was outlined by Shah et al (2012).…”

Section: Commonly Used Polymers To Stabilize Amorphous Pharmaceuticalsmentioning

confidence: 99%

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Excipients That Facilitate Amorphous Drug Stabilization

Wei

Dattachowdhury

Vangara

et al. 2015

Excipient Applications in Formulation Design and Drug Delivery

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The importance of the amorphous state in studying bioavailability of poorly water-soluble drugs cannot be over-emphasized. The higher free energy and therefore the apparent high solubility of the amorphous phase are some of the advantages for promoting the amorphous phase, as compared to its crystalline counterpart. It is well known that the amorphous phase is thermodynamically unstable. This might result in the conversion of the metastable form to its stable crystalline form during storage. This conversion might also lead to product failure during storage owing to the poor dissolution properties of the crystalline form. Excipients can play a key role in preventing such a transformation during storage as well as maximizing the therapeutic efficacy of the amorphous material. This book chapter intends to highlight the delivery issues pertaining to amorphous drugs with a special emphasis on the most commonly used excipients in stabilizing amorphous drug substances in formulations.

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Section: Commonly Used Polymers To Stabilize Amorphous Pharmaceuticalsmentioning

confidence: 99%

Section: Commonly Used Polymers To Stabilize Amorphous Pharmaceuticalsmentioning

confidence: 99%

Excipients That Facilitate Amorphous Drug Stabilization

Wei

Dattachowdhury

Vangara

et al. 2015

Excipient Applications in Formulation Design and Drug Delivery

View full text Add to dashboard Cite

show abstract

“…While the earlier-described approaches focus on the assessment of the supersaturation potential of the polymer, there are some methods describing the evaluation of amorphous drug stabilization in the solid state (van Eerdenbrugh and Taylor 2010;Lauer et al 2011;Weuts et al 2011). Wyttenbach et al (2013) present an interesting strategy to identify amorphous solid dispersions (ASD) with maximum supersaturation and solid-state stability. The authors employed three different miniaturized assays (SPADS dissolution assay, FTIR microspectroscopy-based SPADS interaction assay, and atomic force microscopy-based SPADS imaging assay), combined in a two-step experimental flow to determine both the supersaturation potential and the stability of amorphous compositions thus formed with different drug-polymer combinations (Fig.…”

Section: Screening Criteria and Selectionmentioning

confidence: 99%

“…The authors employed three different miniaturized assays (SPADS dissolution assay, FTIR microspectroscopy-based SPADS interaction assay, and atomic force microscopy-based SPADS imaging assay), combined in a two-step experimental flow to determine both the supersaturation potential and the stability of amorphous compositions thus formed with different drug-polymer combinations (Fig. 1.5;Wyttenbach et al 2013).…”

Section: Screening Criteria and Selectionmentioning

confidence: 99%

Melt Extrusion in Drug Delivery: Three Decades of Progress

Shah

Repka

2013

AAPS Advances in the Pharmaceutical Sciences Series

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This chapter appraises the role of melt extrusion as a solubilization and bioavailability enhancement technique. The introductory chapter highlights major aspects of hot melt extrusion (HME) technology as applied in the pharmaceutical industry, particularly processing techniques, material considerations, recent innovative applications of melt extrusion in drug delivery system design, and a review of current HME-based formulations (marketed or under commercial development). The chapter also focuses on key development aspects of HME processes, such as material sparing screening approaches, process formulation relationships, and stability evaluation of prototype formulations, which emphasize the clinical and biological significance of this technique. In addition, it displays the journey and evolution of this important processing technology into an established pharmaceutical manufacturing platform. The chapter describes several case studies wherein melt extrusion has been utilized to develop commercial drug products.Early-stage development in melt extrusion encompasses various critically interdependent areas involving process considerations, stability assessment of prototype formulations, and performance evaluation (with respect to intended applications) of prototype formulations. Processing ConsiderationsProcessing considerations is a rather broad terminology covering material properties, instrument considerations, and process-formulation interplay. Systematic research over the last couple of decades has revealed that critical product quality attributes are directly dependent on both "formulation" and the "process" employed. It is important to note that the interplay between these determines the finished product attributes. Material PropertiesAll of the materials used in melt extrusion (drugs, carriers, processing aids, release modifiers, etc.) should meet certain minimal pharmaceutical criteria, which

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“…In addition, glass solutions provide an environment in which the solid state of the drug is altered to give rise to enhanced solubility and dissolution rate. Owing to the potential for the successful formulation of a poorly water-soluble drug, the study of miscibility of drug with polymer has increasingly become a topic of interest in both academic and industrial research (Djuris et al 2013;Wyttenbach et al 2013). However, many real pharmaceutical formulation cases are particularly challenging because the drug loading in a singlephase amorphous glass solution needs to be relatively high for the required drug dose to be achieved.…”

Section: Drug-polymer Miscibility: Theoretical Approachesmentioning

confidence: 99%