Is the amorphous fraction of a dried nanosuspension caused by milling or by drying? A case study with Naproxen and Cinnarizine

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Pieterjan Kayaert, Guy Van den Mooter

Abstract

One of the benefits of nanocrystals is their positive effect on the solubility and dissolution rate without alterations to the solid state. Up to now, amorphization of nanocrystals after milling or drying has only rarely been described. The results we present in this article prove that amorphization occurs in some specific cases. This conclusion is based on careful investigation of two different drugs and one polymeric stabilizer. Milling is often mentioned as the prime suspect for solid-state alterations; however, milling proved to be an unlikely cause as the water present in the nanosuspensions acts as a plasticizer that triggers recrystallization. The cause of amorphization can instead be found in the interplay between drug and stabilizer after drying. If a drug is soluble in the stabilizer in the solid state, an amorphous solid dispersion is formed at the interface. Calculations show that the total amount of amorphous material is rather low, but even a small amount could have an influence on both chemical and physical stability or influence the bioavailability if uncontrolled crystallization occurs during storage. In general, those results prove that in depth testing and characterization of the solid state of a dried nanocr...Continue Reading

References

Feb 21, 2003·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Elaine Merisko-LiversidgeEugene R Cooper
Sep 2, 2004·Nature Reviews. Drug Discovery·Barrett E Rabinow
Jul 4, 2006·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Colin W Pouton
Aug 15, 2008·Journal of Pharmaceutical Sciences·A De GussemeM Descamps
Sep 23, 2008·Journal of Pharmaceutical Sciences·Bernard Van EerdenbrughGuy Van den Mooter
Oct 29, 2008·Molecular Pharmaceutics·J F Willart, M Descamps
Apr 1, 2009·Journal of Controlled Release : Official Journal of the Controlled Release Society·Morten AllesøJaakko Aaltonen
Apr 2, 2009·Journal of Pharmaceutical Sciences·I ColomboM Grassi
Jul 7, 2009·International Journal of Pharmaceutics·Puneet SharmaSanjay Garg
Sep 30, 2009·International Journal of Pharmaceutics·Jiao YangJohn Doney
Mar 9, 2010·Drug Discovery Today·Huabing ChenJinming Gao
May 25, 2010·Carbohydrate Research·J F WillartM Descamps

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Citations

Nov 21, 2015·Archives of Pharmacal Research·Jianwen LiYongjun Wang
Sep 26, 2012·Drug Development and Industrial Pharmacy·Steffi ThomasCheng Shu Chaw
Aug 8, 2014·Journal of Pharmaceutical Sciences·William Wei Lim ChinRajeev Gokhale
Jan 8, 2013·International Journal of Pharmaceutics·Ana M CerdeiraBruno Gander
Jan 21, 2015·International Journal of Pharmaceutics·Mirja PaloNiklas Sandler
Aug 21, 2013·Journal of Controlled Release : Official Journal of the Controlled Release Society·Yancai WangDianrui Zhang
Aug 10, 2013·International Journal of Pharmaceutics·Xin-Jiang TangJian-Qing Gao
Jul 30, 2014·Pharmaceutical Development and Technology·Junlin WangJianping Liu
Mar 15, 2015·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·A BitterlichA Kwade
Oct 12, 2014·International Journal of Pharmaceutics·Ramona BaumgartnerEva Roblegg
Dec 3, 2014·International Journal of Pharmaceutics·Xin-Jiang TangJian-Qing Gao
Mar 13, 2014·International Journal of Pharmaceutics·Sumit Kumar, Diane J Burgess
Oct 1, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Christine PetzoldtMartin Philipp Feth
Aug 7, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Carlos E Figueroa, Sonali Bose
Apr 7, 2019·Expert Review of Clinical Pharmacology·Kabir SardanaAastha Gupta
Feb 23, 2018·Pharmaceutical Research·Simone AleandriMartin Kuentz
Aug 24, 2018·Pharmaceutics·Maria Rosa GigliobiancoPiera Di Martino
Jan 17, 2015·Crystal Growth & Design·Heike M A EhmannOliver Werzer

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