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Spherical Cocrystallization of Pharmaceuticals

By Prof. Changquan Calvin Sun, Pharmaceutical Materials Science and Engineering Laboratory, University of Minnesota

The development of a quality tablet product requires overcoming deficiencies in pharmaceutical properties of an active pharmaceutical ingredient (API) to meet several performance standards. APIs with poor aqueous solubility present a challenge in tablet development for meeting the desired dissolution performance to assure adequate bioavailability. If it can be adequately controlled for robust manufacturing performance, direct compression is preferred among common manufacturing processes, because of its economy. Cocrystallization is an effective crystal engineering approach for overcoming deficiencies of APIs, e.g., solubility, tabletability, and stability. Spherical crystallization is an established particle engineering technique for improving powder properties to enable direct compression. Spherical cocrystallization holds the potential to simultaneously improve both key pharmaceutical properties and powder properties to enable direction compression of tablets with both robust manufacturability and superior in vivo performance. In this talk, examples of spherical cocrystallization of APIs and their use in developing direct compression tablet formulations will be presented.
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