Caira M R, Easter B, Honiball S, Horne A, Nassimbeni L R
Department of Chemistry, University of Cape Town, Western Cape, South Africa.
J Pharm Sci. 1995 Nov;84(11):1379-84. doi: 10.1002/jps.2600841121.
Five forms of the drug alprazolam have been identified by thermal analysis and X-ray powder diffraction (XRD). The single crystal X-ray structures of two of these species, a polymorph 1 and a dihydrate 2, were determined. The dihydrate crystallized from a solution of alprazolam in methanol containing traces of water. Species 3 and 4 are nonstoichiometric solvates with ethanol and acetonitrile, respectively. The differential scanning calorimetric curves for the solvates 2-4 are similar, showing a desolvation endotherm, followed by an exotherm associated with recrystallization, and a final endotherm for the fusion of alprazolam. The solvates 3 and 4 were shown to be isomorphous by XRD. The products of desolvation of 2-4 were identified by their XRD traces. Solvates 2 and 3 yield polymorph 1 on desolvation, whereas solvate 4 yields a different polymorph.
通过热分析和X射线粉末衍射（XRD）已鉴定出药物阿普唑仑的五种晶型。确定了其中两种晶型的单晶X射线结构，一种是多晶型物1，另一种是二水合物2。二水合物是从含有微量水的阿普唑仑甲醇溶液中结晶出来的。物种3和4分别是与乙醇和乙腈形成的非化学计量溶剂化物。溶剂化物2 - 4的差示扫描量热曲线相似，显示出一个去溶剂化吸热峰，接着是一个与重结晶相关的放热峰，以及阿普唑仑熔化的最终吸热峰。通过XRD显示溶剂化物3和4是同构的。通过它们的XRD图谱鉴定了2 - 4去溶剂化的产物。溶剂化物2和3去溶剂化后生成多晶型物1，而溶剂化物4生成一种不同的多晶型物。
