mercaptopurine and isonicotinamide

6-Mercaptopurine (6-MP) is a clinically important antitumor drug. The commercially available form was provided as monohydrate and belongs to BCS class II category. Co-crystallization screening by reaction crystallization method (RCM) and monitored by powder X-ray diffraction led to the discovery of a new co-crystal formed between 6-MP and isonicotinamide (co-crystal 1). Co-crystal 1 was thoroughly characterized by X-ray diffraction, FT-IR and Raman spectroscopy, and thermal analysis. Noticeably, the in vitro and in vivo studies revealed that co-crystal 1 possesses improved dissolution rate and superior bioavailability on animal model.

Topics: Animals; Antimetabolites, Antineoplastic; Crystallization; Crystallography, X-Ray; Mercaptopurine; Models, Molecular; Niacinamide; Powder Diffraction; Spectroscopy, Fourier Transform Infrared; Spectrum Analysis, Raman; X-Ray Diffraction