Influence of preparation methods on solid state supersaturation of amorphous solid dispersions: a case study with itraconazole and eudragit e100.

Pharmaceutical Research
Sandrien JanssensGuy Van den Mooter

Abstract

The present study aims to determine the drug / polymer miscibility level as a function of the preparation method for an amorphous solid dispersion model system containing itraconazole and eudragit E100. This value was compared to the theoretical crystalline drug solubility in the amorphous polymer and the miscibility of the amorphous drug in the amorphous polymer. The amorphous solid dispersions were prepared via spray drying and film casting in order to evaluate the influence of the solvent drying rate. The experimental miscibility level was estimated using XRPD, MDSC, FT-IR, HPLC and TGA. The solubility and miscibility were estimated using the Flory-Huggins mixing theory and experimental drug in monomer solubility data. The experimental miscibility level was found to be 27.5% w/w for spray-dried and 15% for film-casted solid dispersions. FT-IR measurements confirmed the absence of saturable interactions like hydrogen bonds, and analysis of the mixed glass transition temperatures suggested low adhesion forces in the amorphous mixture. The solubility analysis rendered a positive FH interaction parameter, a crystalline solubility of approximately 0.012% w/w and an amorphous drug-polymer miscibility of approximately 7.07% w/w. Th...Continue Reading

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Citations

May 23, 2012·Pharmaceutical Research·Ravikiran Panakanti, Ajit S Narang
Jul 27, 2012·Therapeutic Delivery·Monica VialpandoGuy Van den Mooter
Aug 12, 2014·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Ziyi YangSheng Qi
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Jul 15, 2015·Drug Development and Industrial Pharmacy·Sundeep ChaurasiaBrahmeshwar Mishra
Jun 28, 2011·Drug Development and Industrial Pharmacy·Marjana DürriglJelena Filipović-Grčić
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May 3, 2014·Journal of Pharmaceutical Sciences·Mohammed ManiruzzamanDennis Douroumis
Jul 16, 2015·Journal of Pharmaceutical Sciences·Yan He, Chris Ho
Jul 18, 2015·Journal of Pharmaceutical Sciences·Joel HellrupDenny Mahlin
Feb 13, 2015·Pharmaceutical Research·Sujinda KeratichewanunJittima Chatchawalsaisin
Aug 14, 2012·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Xue-Qing Wang, Qiang Zhang
Jul 24, 2012·International Journal of Pharmaceutics·Amrit PaudelGuy Van den Mooter
Nov 24, 2011·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Mohammed ManiruzzamanDennis Douroumis
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Oct 21, 2016·The Journal of Pharmacy and Pharmacology·Hisham Al-ObaidiGraham Buckton

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