Application of Cocrystallization Approach in Drug Development: Recent Patents Review.

BACKGROUND: Cocrystals of active pharmaceutical ingredient has been of interest in the field of pharmaceutical research due to their potential for tailoring the physicochemical properties of pharmaceutical molecules. The increase in number of cocrystals screening experiments being reported and simultaneously the draft guidelines issued from regulatory bodies on pharmaceutical cocrystals provide the evidence of the acceptance of cocrystals in the drug development. This review presents the numerous patents addressing the key properties of an active pharmaceutical ingredient namely solubility and stability towards varied environmental conditions, being modified using suitable coformer and appropriate cocrystallization technique.

METHODS: A literature review was conducted to summarize the reported articles as well as patents that have been published and/or granted for work related to cocrystallization of an active pharmaceutical ingredient (API). Efforts have been made to include examples for various types of objectives undertaken by the researchers to cocrystallize an API.

RESULTS: The summary of the various cocrystallization techniques reported in peer reviewed journals shows that a majority of the articles till date prefer and explore the slow solvent crystallization technique compared to solid-state mediated processes. Amongst all the patents summarized in the review article, 37 patents have been published along with the improvement in physicochemical properties of the API whereas 35 patents have been reported only for the process of preparation of the API.

CONCLUSION: The contents of the review very well highlight the ever increasing scope for the cocrystallization technique of an API, the varied methodologies applied for cocrystallization and the properties that can be improved by cocrystallization.