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Cocrystals by design: A rational coformer selection approach for tackling the API problems

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journal contribution
posted on 2023-05-12, 10:08 authored by Maan Singh, Harsh BaruaHarsh Barua, Vaskuri G. S. Sainaga Jyothi, Madhukiran R. Dhondale, Amritha G. Nambiar, Ashish K. Agrawal, Nalini R. Shastri, Dinesh Kumar

Active pharmaceutical ingredients (API) with unfavorable physicochemical properties and stability present a significant challenge during their processing into final dosage forms. Cocrystallization of such APIs with suitable coformers is an efficient approach to mitigate the solubility and stability concerns. A considerable number of cocrystal-based products are currently being marketed and show an upward trend. However, to improve the API properties by cocrystallization, coformer selection plays a paramount role. Selection of suitable coformers not only improves the drug’s physicochemical properties but also improves the therapeutic effectiveness and reduces side effects.Numerous coformers have been used till date to prepare pharmaceutically acceptable cocrystals. The carboxylic acid-based coformers, such as fumaric acid, oxalic acid, succinic acid, and citric acid, are the most commonly used coformers in the currently marketed cocrystal-based products. Carboxylic acid-based coformers are capable of forming the hydrogen bond and contain smaller carbon chainwith the APIs. This review summarizes the role of coformers in improving the physicochemical and pharmaceutical properties of APIs, and deeply explains the utility of afore-mentioned coformers in API cocrystal formation. The review concludes with a brief discussion on the patentability andregulatory issues related to pharmaceutical cocrystals.


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Pharmaceutics, 2023, 15, ( 4), 1161



Other Funding information

The authors are grateful to the Indian Institute of Technology (Banaras Hindu University), Varanasi for providing infrastructure facilities. Singh, M and Kumar, D acknowledges funding from SERB, India under grant number SRG/2021/002389. Dhondale, MR acknowledges funding from PMRF, India under grant number 1102018.

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