吲达帕胺多晶型及假多晶型的固态研究与特性鉴定。

Solid state investigation and characterization of the polymorphic and pseudopolymorphic forms of indapamide.

机构信息

Nadkarni Sacasa Research Laboratory, Department of Chemistry, St. Xavier's College, Mumbai 400001, India. p d

出版信息

J Pharm Biomed Anal. 2010 Feb 5;51(3):532-40. doi: 10.1016/j.jpba.2009.09.003. Epub 2009 Sep 11.

DOI:10.1016/j.jpba.2009.09.003

PMID:19796901

Abstract

Solid state investigation and polymorphic screening of indapamide, a diuretic drug generally used for the treatment of hypertension was carried out. Substantial differences were obtained in the solid state properties of crystals confirming the existence of a polymorphic and three pseudopolymorphic forms of indapamide. Detailed methods of preparation of the polymorphs and pseudopolymorphs are described. X-ray powder diffraction (XRPD), diffuse reflectance infrared Fourier transform (DRIFT) spectroscopy, differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) were employed for the characterization of different crystalline forms of indapamide. The stoichiometric ratio of solvents associated with the drug molecules in the pseudopolymorphic forms were calculated using TGA, nuclear magnetic resonance (NMR) spectroscopy and headspace gas chromatographic (HS-GC) analysis.

摘要

对利尿剂吲达帕胺（通常用于治疗高血压）的固态研究和多晶型筛选进行了研究。晶体的固态性质存在明显差异，证实了吲达帕胺存在多晶型和三种假多晶型形式。详细描述了多晶型和假多晶型的制备方法。X 射线粉末衍射（XRPD）、漫反射红外傅里叶变换（DRIFT）光谱、差示扫描量热法（DSC）和热重分析（TGA）用于吲达帕胺不同晶型的表征。使用 TGA、核磁共振（NMR）光谱和顶空气相色谱（HS-GC）分析计算了假多晶型中与药物分子结合的溶剂的化学计量比。