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Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

General Review Article

Recent Advancements in Pharmaceutical Cocrystals, Preparation Methods, and their Applications

Author(s): Deeksha Manchanda, Arun Kumar and Arun Nanda*

Volume 27, Issue 44, 2021

Published on: 14 April, 2021

Page: [4477 - 4495] Pages: 19

DOI: 10.2174/1381612827666210415104411

Price: $65

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Abstract

The issue of poor aqueous solubility is a major hurdle in pharmaceutical dosage form design. A large number of active molecules in the research and development pipeline possess poor aqueous solubility and, hence, are not suitable for further development. Therefore, the pharmaceutical industry is continuously in search of techniques to tackle the issue of poor solubility. Cocrystallization has gained popularity as one such technique for the modulation of physicochemical properties of an active pharmaceutical ingredient (API). Pharmaceutical cocrystals consist of an API non-covalently linked to a crystal former or coformer that plays an important role in imparting the desired properties to the cocrystal. Cocrystallization of an API with a suitable coformer not only enhances solubility but also helps in improving physicochemical properties such as stability, bioavailability, mechanical properties, etc., without changing the pharmacological activity of the API. The past decade has experienced enormous growth in cocrystal research which paved the way for drug-drug, higherorder, and nano-sized cocrystals, and further exploration of the applications of cocrystals is still going on. Recently FDA and EMA have released regulatory guidelines for pharmaceutical cocrystals, which grant them a status similar to that of polymorphs and salts, which in turn opens a wider prospect for pharmaceutical cocrystals in terms of intellectual property.

Keywords: Pharmaceutical cocrystals, drug-drug cocrystals, supramolecular synthon, solubility enhancement, cocrystallization, active pharmaceutical ingredient (API).


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