舒林酸的多晶型：一种新多晶型物和三种新溶剂化物的分离与表征

Polymorphism of sulindac: isolation and characterization of a new polymorph and three new solvates.

作者信息

Tros de Ilarduya M C, Martín C, Goñi M M, Martínez-Ohárriz M C

机构信息

Department of Physical Chemistry, School of Pharmacy, University of Navarra, Pamplona, Spain.

出版信息

J Pharm Sci. 1997 Feb;86(2):248-51. doi: 10.1021/js9601748.

DOI:10.1021/js9601748

PMID:9040104

Abstract

The polymorphism of sulindac was investigated. Two polymorphs (I and II) and a new crystalline form (form III) of sulindac were prepared by recrystallization in different solvents. In addition, three new pseudopolymorphs (solvates) from acetone, chloroform, and benzene were obtained, with each containing 1 mol of solvent to 2 mol of sulindac. Different sulindac polymorphs and pseudopolymorphs were characterized by X-ray diffractometry, infrared spectroscopy, differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and hot-stage microscopy. The transition behavior of the crystalline forms of sulindac, their melting points, and their enthalpies were investigated by DSC. The melting of form II was observed at 184 degrees C, and form I subsequently recrystallized from this melt. Similarly, form III melts at 145 degrees C and then recrystallizes to form I. We also investigated the influence of the crystallization solvent on sulindac crystal shape.

摘要

对舒林酸的多晶型现象进行了研究。通过在不同溶剂中重结晶制备了舒林酸的两种多晶型物（I型和II型）以及一种新的晶型（III型）。此外，还获得了来自丙酮、氯仿和苯的三种新的假多晶型物（溶剂化物），每种均含有1摩尔溶剂与2摩尔舒林酸。通过X射线衍射法、红外光谱法、差示扫描量热法（DSC）、热重分析（TGA）和热台显微镜对不同的舒林酸多晶型物和假多晶型物进行了表征。通过DSC研究了舒林酸晶型的转变行为、熔点及其焓。观察到II型在184℃熔化，然后I型从该熔体中重结晶。类似地，III型在145℃熔化，然后重结晶形成I型。我们还研究了结晶溶剂对舒林酸晶体形状的影响。