Transformation pathways of cocrystal hydrates when coformer modulates water activity

Journal of Pharmaceutical Sciences
Adivaraha JayasankarNaír Rodríguez-Hornedo

Abstract

An important attribute of cocrystals is that their properties can be tailored to meet required solubility and stability specifications. But before such practical uses can be realized, a better understanding of the factors that dictate co-crystal behavior is needed. This study attempts to explain the phase behavior of anhydrous/hydrated cocrystals when the coformer modulates both water activity and co-crystal solubility. Stability dependence on solution composition and water activity was studied for theophylline-citric acid (THP-CTA) anhydrous and hydrated cocrystals by both suspension and vapor equilibration methods. Eutectic points and associated water activities were measured by suspension equilibration methods to determine stability regions and phase diagrams. The critical water activity for the anhydrous-hydrate co-crystal was found to be 0.8. It is shown that (a) both water and coformer activities determine phase stability, and (b) excipients that alter water activity can profoundly affect the hydrate/anhydrous eutectic points and phase stability. Vapor phase stability studies demonstrate that cocrystals of highly water soluble coformers, such as citric acid, are predisposed to conversions due to moisture uptake and deliqu...Continue Reading

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Citations

Dec 5, 2012·International Journal of Pharmaceutics·Ranjit ThakuriaNaír Rodríguez-Hornedo
Jun 21, 2016·Chemical & Pharmaceutical Bulletin·Ken-Ichi IzutsuEtsuo Yonemochi
Jul 11, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Mingyu LiuYan Xie
Dec 6, 2018·Chemical Communications : Chem Comm·Rafael BarbasAntonio Frontera
Nov 19, 2011·Drug Development and Industrial Pharmacy·Luis PadrelaSitaram P Velaga
Feb 8, 2011·Chemical & Pharmaceutical Bulletin·Keiji YamamotoKunikazu Moribe
Apr 4, 2021·Pharmaceutics·Heiner VeithGabriele Sadowski
Jul 3, 2021·Pharmaceutics·Isabela Fanelli Barreto BiscaiaPaulo Renato Oliveira

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