A rapid approach to the preliminary assessment of the physical stability of pharmaceutical hydrates

An insight into carvedilol solid forms: effect of supramolecular interactions on the dissolution profiles

“…However, we cannot use this endotherm as a thermodynamic characteristic of the hydrate 39 because the thermal events resulted in a complex signal in the DSC curve, with this signal being dependent on the measurement conditions. During heating, the API may have partially dissolved in the water of crystallization.…”

Enhancing the stability of active pharmaceutical ingredients by the cocrystal strategy

“…40 Pharmaceutical hydrates also have been used as clinical development candidates, but they pose unique challenges of secured stability owing to their sensitivity to the moisture level in surroundings. 26…”

“…23 Approximately one-third of all compounds used in the manufacture of medicines are able to hydrate, 24 and the potential dehydration and subsequent form change would occur at an elevated temperature, or in a variable humidity. 25,26 Such a phase transformation is not desired in the pharmaceutical industry as it might lower the dissolution rate and diminish oral bioavailability. 24 Besides, visual changes for drug products, including tablet friability and appearance, would occur at a threshold relative humidity (RH).…”

“…24 The onset temperature of dehydration could be used as an early indicator to evaluate the physical stability of pharmaceutical hydrates. 26 Unfortunately, gaps remain in predicting exactly how RH will impact physical stability despite attempts to use varied calculation models. 6 Another stability risk brought by moisture absorption is hydrolysis reactions.…”

“…40 Pharmaceutical hydrates also have been used as clinical development candidates, but they pose unique challenges of secured stability owing to their sensitivity to the moisture level in surroundings. 26 Cocrystals, however, can effectively enhance the stability of APIs, 9,12 while bringing opportunities to overcome the above limitations. 41 Suitable coformers can be selected from thousands of potential substances, especially those that have precedence as food ingredients, out of safety concern.…”