Winters C S, Shields L, Timmins P, York P
Department of Pharmacy, University of Bradford, West Yorkshire, U.K.
J Pharm Sci. 1994 Mar;83(3):300-4. doi: 10.1002/jps.2600830308.
The solid-state characterization of gliclazide, for which no analytical standard was previously available, has been completed by extensive structural and physical analytical examination. The crystal and molecular structure for gliclazide was determined by single-crystal X-ray diffraction. Gliclazide crystallizes in the monoclinic space group P2(1)/n, with the unit cell dimensions a = 10.828(2) A, b = 14.342(19) A, c = 11.005(6) A, and with beta = 106.97(2) degrees, V = 1635(12) A3, and Z = 4. The gliclazide molecule is articulated in an open extended conformation about the sulphonylurea nucleus. Two gliclazide molecules form a complex with one calcium atom to facilitate the transport of calcium ions across the pancreatic beta cells necessary for the stimulation of insulin secretion. The only conformation that allows for the close apposition of the tolyl groups, and therefore the formation of the gliclazide:calcium complex, is the extended conformer.
格列齐特的固态表征此前尚无分析标准，现已通过广泛的结构和物理分析检测完成。格列齐特的晶体和分子结构通过单晶X射线衍射确定。格列齐特以单斜空间群P2(1)/n结晶，晶胞参数a = 10.828(2) Å，b = 14.342(19) Å，c = 11.005(6) Å，β = 106.97(2)°，V = 1635(12) ų，Z = 4。格列齐特分子围绕磺酰脲核呈开放伸展构象。两个格列齐特分子与一个钙原子形成复合物，以促进钙离子穿过胰腺β细胞的运输，这对于刺激胰岛素分泌是必要的。唯一允许甲苯基紧密并置从而形成格列齐特 -钙复合物的构象是伸展构象体。
