Influence of Solvent Composition on the Performance of Spray-Dried Co-Amorphous Formulations

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Standard

Influence of Solvent Composition on the Performance of Spray-Dried Co-Amorphous Formulations. / Mishra, Jaya; Rades, Thomas; Löbmann, Korbinian; Grohganz, Holger.

In: Pharmaceutics, Vol. 10, No. 2, 12.04.2018, p. 1-13.

Research output: Contribution to journalJournal articlepeer-review

Harvard

Mishra, J, Rades, T, Löbmann, K & Grohganz, H 2018, 'Influence of Solvent Composition on the Performance of Spray-Dried Co-Amorphous Formulations', Pharmaceutics, vol. 10, no. 2, pp. 1-13. https://doi.org/10.3390/pharmaceutics10020047

APA

Mishra, J., Rades, T., Löbmann, K., & Grohganz, H. (2018). Influence of Solvent Composition on the Performance of Spray-Dried Co-Amorphous Formulations. Pharmaceutics, 10(2), 1-13. https://doi.org/10.3390/pharmaceutics10020047

Vancouver

Mishra J, Rades T, Löbmann K, Grohganz H. Influence of Solvent Composition on the Performance of Spray-Dried Co-Amorphous Formulations. Pharmaceutics. 2018 Apr 12;10(2):1-13. https://doi.org/10.3390/pharmaceutics10020047

Author

Mishra, Jaya ; Rades, Thomas ; Löbmann, Korbinian ; Grohganz, Holger. / Influence of Solvent Composition on the Performance of Spray-Dried Co-Amorphous Formulations. In: Pharmaceutics. 2018 ; Vol. 10, No. 2. pp. 1-13.

Bibtex

@article{20f228b983454f1d81024087bcb6e153,
title = "Influence of Solvent Composition on the Performance of Spray-Dried Co-Amorphous Formulations",
abstract = "Ball-milling is usually used to prepare co-amorphous drug–amino acid (AA) mixtures. In this study, co-amorphous drug–AA mixtures were produced using spray-drying, a scalable industrially preferred preparation method. The influence of the solvent type and solvent composition was investigated. Mixtures of indomethacin (IND) and each of the three AAs arginine, histidine, and lysine were ball-milled and spray-dried at a 1:1 molar ratio, respectively. Spray-drying was performed at different solvent ratios in (a) ethanol and water mixtures and (b) acetone and water mixtures. Different ratios of these solvents were chosen to study the effect of solvent mixtures on co-amorphous formulation. Residual crystallinity, thermal properties, salt/partial salt formation, and powder dissolution profiles of the IND–AA mixtures were investigated and compared to pure crystalline and amorphous IND. It was found that using spray-drying as a preparation method, all IND–AA mixtures could be successfully converted into the respective co-amorphous forms, irrespective of the type of solvent used, but depending on the solvent mixture ratios. Both ball-milled and spray-dried co-amorphous samples showed an enhanced dissolution rate and maintained supersaturation compared to the crystalline and amorphous IND itself. The spray-dried samples resulting in co-amorphous samples were stable for at least seven months of storage.",
author = "Jaya Mishra and Thomas Rades and Korbinian L{\"o}bmann and Holger Grohganz",
year = "2018",
month = apr,
day = "12",
doi = "10.3390/pharmaceutics10020047",
language = "English",
volume = "10",
pages = "1--13",
journal = "Pharmaceutics",
issn = "1999-4923",
publisher = "MDPI AG",
number = "2",

}

RIS

TY - JOUR

T1 - Influence of Solvent Composition on the Performance of Spray-Dried Co-Amorphous Formulations

AU - Mishra, Jaya

AU - Rades, Thomas

AU - Löbmann, Korbinian

AU - Grohganz, Holger

PY - 2018/4/12

Y1 - 2018/4/12

N2 - Ball-milling is usually used to prepare co-amorphous drug–amino acid (AA) mixtures. In this study, co-amorphous drug–AA mixtures were produced using spray-drying, a scalable industrially preferred preparation method. The influence of the solvent type and solvent composition was investigated. Mixtures of indomethacin (IND) and each of the three AAs arginine, histidine, and lysine were ball-milled and spray-dried at a 1:1 molar ratio, respectively. Spray-drying was performed at different solvent ratios in (a) ethanol and water mixtures and (b) acetone and water mixtures. Different ratios of these solvents were chosen to study the effect of solvent mixtures on co-amorphous formulation. Residual crystallinity, thermal properties, salt/partial salt formation, and powder dissolution profiles of the IND–AA mixtures were investigated and compared to pure crystalline and amorphous IND. It was found that using spray-drying as a preparation method, all IND–AA mixtures could be successfully converted into the respective co-amorphous forms, irrespective of the type of solvent used, but depending on the solvent mixture ratios. Both ball-milled and spray-dried co-amorphous samples showed an enhanced dissolution rate and maintained supersaturation compared to the crystalline and amorphous IND itself. The spray-dried samples resulting in co-amorphous samples were stable for at least seven months of storage.

AB - Ball-milling is usually used to prepare co-amorphous drug–amino acid (AA) mixtures. In this study, co-amorphous drug–AA mixtures were produced using spray-drying, a scalable industrially preferred preparation method. The influence of the solvent type and solvent composition was investigated. Mixtures of indomethacin (IND) and each of the three AAs arginine, histidine, and lysine were ball-milled and spray-dried at a 1:1 molar ratio, respectively. Spray-drying was performed at different solvent ratios in (a) ethanol and water mixtures and (b) acetone and water mixtures. Different ratios of these solvents were chosen to study the effect of solvent mixtures on co-amorphous formulation. Residual crystallinity, thermal properties, salt/partial salt formation, and powder dissolution profiles of the IND–AA mixtures were investigated and compared to pure crystalline and amorphous IND. It was found that using spray-drying as a preparation method, all IND–AA mixtures could be successfully converted into the respective co-amorphous forms, irrespective of the type of solvent used, but depending on the solvent mixture ratios. Both ball-milled and spray-dried co-amorphous samples showed an enhanced dissolution rate and maintained supersaturation compared to the crystalline and amorphous IND itself. The spray-dried samples resulting in co-amorphous samples were stable for at least seven months of storage.

U2 - 10.3390/pharmaceutics10020047

DO - 10.3390/pharmaceutics10020047

M3 - Journal article

C2 - 29649124

VL - 10

SP - 1

EP - 13

JO - Pharmaceutics

JF - Pharmaceutics

SN - 1999-4923

IS - 2

ER -

ID: 195004913