Physico-chemical property impact of pharmaceutical co-crystals

ORGN 86

Magali B. Hickey, Mhickey1@tpius.jnj.com, Matthew L. Peterson, Julius F. Remenar, jremenar@tpius.jnj.com, and Örn Almarsson, oalmarss@tpius.jnj.com. Pharmaceutical Chemistry, TransForm Pharmaceuticals, 29 Hartwell Ave., Lexington, MA 02421
Co-crystals are emerging as interesting and underexploited compositions in the pharmaceutical industry. Co-crystals of drug products have been prepared by several techniques, including crystallization from solution and mechanical grinding. The co-crystals often display different physical properties from the active pharmaceutical ingredient (API) such as modified dissolution, enhanced bioavailability and altered physical stability. The co-crystal of carbamazepine and saccharin was found to be less hygroscopic than the parent drug and showed an improved dissolution profile compared to the marketed product (Tegretol®). The co-crystal of celecoxib (active drug in Celebrex®) and nicotinamide exhibits increased kinetic solubility relative to the API and improved stability relative to the sodium salt of celecoxib. This presentation will demonstrate how a molecular self-assembly approach can be used to prepare co-crystals with the aim of identifying new pharmaceutical materials, which can modify physical properties and performance.