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 128 publications

(63 citation statements)

References 68 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…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

View full text Add to dashboard Cite

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/).

show abstract

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

View full text Add to dashboard Cite

show abstract

“…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

View full text Add to dashboard Cite

“…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

View full text Add to dashboard Cite

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.

show abstract

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

Cited by 128 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

Contact Info

Product

Resources

About