Wang Jian-Rong, Yu Xueping, Zhou Chun, Lin Yunfei, Chen Chen, Pan Guoyu, Mei Xuefeng
Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; Nano Science and Technology Institute, University of Science and Technology of China, Suzhou, Jiangsu 215123, China.
Bioorg Med Chem Lett. 2015 Mar 1;25(5):1036-9. doi: 10.1016/j.bmcl.2015.01.022. Epub 2015 Jan 17.
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.
6-巯基嘌呤（6-MP）是一种临床上重要的抗肿瘤药物。市售形式为一水合物，属于BCS II类。通过反应结晶法（RCM）进行共结晶筛选并通过粉末X射线衍射监测，发现了6-MP与异烟酰胺之间形成的一种新的共晶体（共晶体1）。通过X射线衍射、傅里叶变换红外光谱和拉曼光谱以及热分析对共晶体1进行了全面表征。值得注意的是，体外和体内研究表明，共晶体1在动物模型上具有提高的溶解速率和优异的生物利用度。
