Physical stability of pharmaceutical formulations: solid-state characterization of amorphous dispersions

Guo, Ya-Fang; Shalaev, Evgenyi; Smith, Scott R.

doi:10.1016/j.trac.2013.06.002

Cited by 129 publications

(63 citation statements)

References 68 publications

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“…The recrystallization of amorphous drugs in SD may lead to a reduced dissolution rate and consequently a lower bioavailability [19,20]. The data generated by SM content analysis and XRD of SM-SD were presented in Table 1 and Fig.…”

Section: Stabilitymentioning

confidence: 99%

Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids

Yang

Zhao

Feng

et al. 2015

Asian Journal of Pharmaceutical Sciences

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Available online xxxKeywords: Silymarin Solution-enhanced dispersion by supercritical fluids Solid dispersion Dissolution Bioavailability a b s t r a c tThe objective of this study was to improve the dissolution and bioavailability of silymarin (SM). Solid dispersions (SDs) were prepared using solution-enhanced dispersion by supercritical fluids (SEDS) and evaluated in vitro and in vivo, compared with pure SM powder.The particle sizes, stability, and contents of residual solvent of the prepared SM-SDs with SEDS and solvent evaporation (SE) were investigated. Four polymer matrix materials were evaluated for the preparation of SM-SD-SEDS, and the hydrophilic polymer, polyvinyl pyrrolidone K17, was selected with a ratio of 1:5 between SM and the polymer. Physicochemical analyses using X-ray diffraction and differential scanning calorimetry indicated that SM was dispersed in SD in an amorphous state. The optimized SM-SD-SEDS showed no loss of SM after storage for 6 months and negligible residual solvent (ethanol) was detected using gas chromatography. In vitro drug release was increased from the SM-SD-SEDS, as compared with pure SM powder or SM-SD-SE. In vivo, the area under the rat plasma SM concentration-time curve and the maximum plasma SM concentration were 2.4-fold and 1.9-fold higher, respectively, after oral administration of SM-SD-SEDS as compared with an aqueous SM suspension. These results illustrated the potential of using SEDS to prepare SM-SD, further improving the biopharmaceutical properties of this compound. © 2014 Shenyang Pharmaceutical University. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/ licenses/by-nc-nd/4.0/).

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Section: Stabilitymentioning

confidence: 99%

Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids

Yang

Zhao

Feng

et al. 2015

Asian Journal of Pharmaceutical Sciences

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“…The long-term stability of amorphous formulations has been investigated in several studies [2][3][4]. The maximum amount of API that can be dissolved in a polymeric excipient without recrystallization is the API solubility in the polymer and thus depends on the phase behavior of the resulting API/polymer formulation.…”

Section: Introductionmentioning

confidence: 99%

Influence of humidity on the phase behavior of API/polymer formulations

Prudic

Luebbert

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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“…Evgenyi Shalaev, Allergan, presented a panorama of new characterization tools for understanding amorphous structure and properties. The standard characterization methods for solid state properties include XRPD (crystallinity), DSC (mobility, crystallinity), and water/solvent content, and are amongst many that are used across the pharmaceutical industry (Guo et al 2013). The limitation of conventional XRPD for amorphous/crystalline physical mixtures is that it has only an approximately 1% detection limit for crystalline material.…”

Section: New Tools For Amorphous Form Characterizationmentioning

confidence: 99%

New directions in pharmaceutical amorphous materials and amorphous solid dispersions, a tribute to Professor George Zografi – Proceedings of the June 2016 Land O’Lakes Conference

Newman¹,

Hastedt

2017

AAPS Open

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The University of Wisconsin-Madison June Land O'Lakes Conference on Research and Development is held every year and is recognized worldwide as a premier teaching conference for pharmaceutical scientists. The conference held in June 2016 was a tribute to the ground-breaking work of Emeritus Professor and Dean George Zografi of School of Pharmacy, University of Wisconsin-Madison. This paper provides a summary of the wide range of topics in the areas of amorphous drugs, amorphous solid dispersions, mesophases, mesoporous supports, cocrystals, and related themes that were covered at this conference.

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Physical stability of pharmaceutical formulations: solid-state characterization of amorphous dispersions

Cited by 129 publications

References 68 publications

Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids

Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids

Influence of humidity on the phase behavior of API/polymer formulations

New directions in pharmaceutical amorphous materials and amorphous solid dispersions, a tribute to Professor George Zografi – Proceedings of the June 2016 Land O’Lakes Conference

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