Title:Recent Advancements in Pharmaceutical Cocrystals, Preparation Methods, and their Applications
Volume: 27
Issue: 44
Author(s): Deeksha Manchanda, Arun Kumar and Arun Nanda*
Affiliation:
- Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak (Haryana),India
Keywords:
Pharmaceutical cocrystals, drug-drug cocrystals, supramolecular synthon, solubility enhancement, cocrystallization, active
pharmaceutical ingredient (API).
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.