Improving the dissolution and bioavailability of 6-mercaptopurine via co-crystallization with isonicotinamide. Issue 5 (1st March 2015)

• Record Type: Journal Article
• Authors: Wang, Jian-Rong; Yu, Xueping; Zhou, Chun; Lin, Yunfei; Chen, Chen; Pan, Guoyu; Mei, Xuefeng
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 5(2015)
• Page Start: 1042
• Page End: 1045
• Publication Date: 2015-03-01
• Subjects: 6-Mercaptopurine -- Pharmaceutical co-crystal -- Crystal structure -- Bioavailability; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.01.022
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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-crystal1 ). Co-crystal1 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-crystal1 possesses improved dissolution rate and superior bioavailability on animal model.