化学学报 ›› 2007, Vol. 65 ›› Issue (24): 2817-2820. 上一篇    下一篇

研究论文

那格列奈的多晶型与溶解度

李钢*,1, 徐群为2, 李瑞2, 程永科1, 黄长高1   

  1. (1南京师范大学分析测试中心 南京 210097)
    (2南京医科大学药学院 南京 210009)
  • 投稿日期:2007-03-28 修回日期:2007-07-18 发布日期:2007-12-28
  • 通讯作者: 李钢

Polymorphism and Solubility of Nateglinide

LI Gang*,1; XU Qun-Wei2; LI Rui2; CHENG Yong-Ke1; HUANG Chang-Gao1   

  1. (1 Testing & Analysis Center, Nanjing Normal University, Nanjing 210097)
    (2 College of the Medicine, Nanjing Medicine University, Nanjing 210009)
  • Received:2007-03-28 Revised:2007-07-18 Published:2007-12-28
  • Contact: LI Gang

分别对那格列奈B, H和S三种晶型的溶解度、溶解热进行了测定和计算. 结果表明: 那格列奈的S晶型与临床使用的H晶型溶解度均明显大于B晶型. B, H和S三种晶型的溶解热分别为42.84, 28.44 和29.14 kJ•mol-1. 此外, 我们还新发现了不同于B, H, S晶型的X2晶型, 并且制备出了无定型的那格列奈.

关键词: 那格列奈, 多晶型, 溶解度, 糖尿病, X射线粉末衍射

The solubility values of three forms of nateglinide have been measured at different temperatures, and their enthalpies have been calculated. The results indicated that the solubility values of both S-form and H-form are large than that of B-form clearly. Moreover, a new X2-form of nateglinide was found and its amorphous form was prepared.

Key words: nateglinide, polymorphism, solubility, diabetes, X-ray powder diffraction