李钢, 陈家英, 吕光烈, 徐群为. 那格列奈的多晶结构与药效测定J. 药学学报, 2005, 40(10): 958-960.
引用本文: 李钢, 陈家英, 吕光烈, 徐群为. 那格列奈的多晶结构与药效测定J. 药学学报, 2005, 40(10): 958-960.
LI Gang, CHEN Jia-ying, Lü Guang-lie, XU Qun-wei. Determination of the nateglinide polymorphism structure and the drug effectDetermination of the nateglinide polymorphism structure and the drug effectJ. Acta Pharmaceutica Sinica, 2005, 40(10): 958-960.
Citation: LI Gang, CHEN Jia-ying, Lü Guang-lie, XU Qun-wei. Determination of the nateglinide polymorphism structure and the drug effectDetermination of the nateglinide polymorphism structure and the drug effectJ. Acta Pharmaceutica Sinica, 2005, 40(10): 958-960.

那格列奈的多晶结构与药效测定

Determination of the nateglinide polymorphism structure and the drug effectDetermination of the nateglinide polymorphism structure and the drug effect

  • 摘要: 目的测定那格列奈的多晶结构和药效,给出晶格参数和动物试验数据。方法X射线粉末衍射法测定物相和晶格参数;腹腔注射葡萄糖致使小鼠形成高血糖血症。小鼠分成对照组、模型组、H晶型治疗组和S晶型治疗组。测定给药20,40和60 min后小鼠的血糖值。结果那格列奈有3种晶型,B-,H-和S-型结构。H晶型为三斜晶系,晶格参数a=1.769 9(7) nm,b=2.719 1(8) nm,c=1.267 0(6) nm,α=61.75(3)°,β=73.11(6)°,γ=66.77(7)°,V=4.895 nm3Z=10。S晶型为正交晶系,晶格参数a=2.317 8(6) nm,b=2.533 2(5) nm,c=0.653 1(2) nm,α=β=γ=90°,V=3.835 nm3Z=8。小鼠模拟降糖试验表明:与H晶型一样,S晶型也能有效地降低血糖值,特别是用药40 min后效果更加明显。结论H晶型为三斜晶系,S晶型为正交晶系,用S晶型给药40 min后效果更加明显。

     

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