scholarly journals Structural characterisation of amorphous solid dispersions via metropolis matrix factorisation of pair distribution function data

2019 ◽  
Vol 55 (89) ◽  
pp. 13346-13349 ◽  
Author(s):  
Harry S. Geddes ◽  
Helen Blade ◽  
James F. McCabe ◽  
Leslie P. Hughes ◽  
Andrew L. Goodwin
Keyword(s):  
Distribution Function ◽  
Pair Distribution Function ◽  
Solid Dispersions ◽  
Complex Mixture ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersions ◽  
Total Scattering ◽  
Structural Characterisation ◽  
Function Data ◽  
Matrix Factorisation

We use total scattering and non-negative matrix factorisation to characterise the structure of an amorphous pharmaceutical in a complex mixture.

scholarly journals Structural Characterisation of Amorphous Solid Dispersions via Metropolis Matrix Factorisation of Pair Distribution Function Data

2019 ◽  
Author(s):  
Harry Geddes ◽  
Helen Blade ◽  
James McCabe ◽  
Leslie P. Hughes ◽  
Andrew Goodwin
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Distribution Functions ◽  
Atomistic Simulations ◽  
Amorphous Solid Dispersions ◽  
Structural Characterisation ◽  
Amorphous Pharmaceuticals ◽  
Amorphous Drug ◽  
Pair Distribution Functions ◽  
Matrix Factorisation

We measure the X-ray pair distribution functions (PDFs) of a series of felodipine:copovidone amorphous solid dispersions. Using a newly-developed Metropolis Matrix Factorisation (MMF) algorithm we extract from these data the PDF of the amorphous felodipine component in isolation. Our MMF analysis allows quantification of the degree of drug crystallinity in each sample, and structural characterisation of the amorphous drug <i>via</i>its PDF. Comparison with atomistic simulations reveals that the (in)accessibility of conformational rotamers distinguishes amorphous and crystalline felodipine, in turn suggesting design routes for stabilising the amorphous form. We discuss the conceptual importance of our results in the context of characterising not only amorphous pharmaceuticals, but complex mixtures in general.

scholarly journals Structural Characterisation of Amorphous Solid Dispersions via Metropolis Matrix Factorisation of Pair Distribution Function Data

2019 ◽  
Author(s):  
Harry Geddes ◽  
Helen Blade ◽  
James McCabe ◽  
Leslie P. Hughes ◽  
Andrew Goodwin
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Distribution Functions ◽  
Atomistic Simulations ◽  
Amorphous Solid Dispersions ◽  
Structural Characterisation ◽  
Amorphous Pharmaceuticals ◽  
Amorphous Drug ◽  
Pair Distribution Functions ◽  
Matrix Factorisation

We measure the X-ray pair distribution functions (PDFs) of a series of felodipine:copovidone amorphous solid dispersions. Using a newly-developed Metropolis Matrix Factorisation (MMF) algorithm we extract from these data the PDF of the amorphous felodipine component in isolation. Our MMF analysis allows quantification of the degree of drug crystallinity in each sample, and structural characterisation of the amorphous drug <i>via</i>its PDF. Comparison with atomistic simulations reveals that the (in)accessibility of conformational rotamers distinguishes amorphous and crystalline felodipine, in turn suggesting design routes for stabilising the amorphous form. We discuss the conceptual importance of our results in the context of characterising not only amorphous pharmaceuticals, but complex mixtures in general.

Development of novel darunavir amorphous solid dispersions with mesoporous carriers

2021 ◽  
Vol 159 ◽  
pp. 105700
Author(s):  
Sergey A. Zolotov ◽  
Natalia B. Demina ◽  
Anna S. Zolotova ◽  
Natalia V. Shevlyagina ◽  
Grigorii A. Buzanov ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersions

Effect of Carrier Type and Tween® 80 Concentration on the Release of Silymarin from Amorphous Solid Dispersions

2021 ◽  
pp. 102416
Author(s):  
Valentyn Mohylyuk ◽  
Thomas Pauly ◽  
Oleksandr Dobrovolnyi ◽  
Nathan Scott ◽  
David S. Jones ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersions

scholarly journals Enhanced Oral Bioavailability of Resveratrol by Using Neutralized Eudragit E Solid Dispersion Prepared via Spray Drying

Antioxidants ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 90
Author(s):  
Eun-Sol Ha ◽  
Du Hyung Choi ◽  
In-hwan Baek ◽  
Heejun Park ◽  
Min-Soo Kim
Keyword(s):  
Spray Drying ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Pharmaceutical Products ◽  
In Vitro Dissolution ◽  
Dependent Manner ◽  
Amorphous Solid Dispersions ◽  
Eudragit E

In this study, we designed amorphous solid dispersions based on Eudragit E/HCl (neutralized Eudragit E using hydrochloric acid) to maximize the dissolution of trans-resveratrol. Solid-state characterization of amorphous solid dispersions of trans-resveratrol was performed using powder X-ray diffraction, scanning electron microscopy, and particle size measurements. In addition, an in vitro dissolution study and an in vivo pharmacokinetic study in rats were carried out. Among the tested polymers, Eudragit E/HCl was the most effective solid dispersion for the solubilization of trans-resveratrol. Eudragit E/HCl significantly inhibited the precipitation of trans-resveratrol in a pH 1.2 dissolution medium in a dose-dependent manner. The amorphous Eudragit E/HCl solid dispersion at a trans-resveratrol/polymer ratio of 10/90 exhibited a high degree of supersaturation without trans-resveratrol precipitation for at least 48 h by the formation of Eudragit E/HCl micelles. In rats, the absolute oral bioavailability (F%) of trans-resveratrol from Eudragit E/HCl solid dispersion (10/90) was estimated to be 40%. Therefore, trans-resveratrol-loaded Eudragit E/HCl solid dispersions prepared by spray drying offer a promising formulation strategy with high oral bioavailability for developing high-quality health supplements, nutraceutical, and pharmaceutical products.

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