New solid modifications of nateglinide

被引：15

作者：

Bruni, G. ^{[1
]}

Berbenni, V. ^{[1
]}

Milanese, C. ^{[1
]}

Girella, A. ^{[1
]}

Cardini, A. ^{[2
]}

Lanfranconi, S. ^{[2
]}

Marini, A. ^{[1
]}

机构：

[1] Univ Pavia, Dipartimento Chim Fis M Rolla, CSGI, I-27100 Pavia, Italy

[2] AMSA SpA, Como, Italy

来源：

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS | 2010年 / 51卷 / 05期

关键词：

DSC; Hemihydrate form; Nateglinide; Physico chemical characterization; Polymorphism; Pseudo-polymorphism;

D O I：

10.1016/j.jpba.2009.11.019

中图分类号：

O65 [分析化学];

学科分类号：

070302 ; 081704 ;

摘要：

New modifications of the antidiabetic drug nateglinide were found and characterized by means of thermal analysis, vibrational spectroscopy and X-ray powder diffractometry. In particular it has been verified that the product obtained during the final steps of the nateglinide synthesis is the hemihydrate form which melts at about 86 degrees C provided that the adopted experimental conditions hinder the removal of the crystallization water. Otherwise, if the crystallization water is removed, the hemihydrate transforms to a new anhydrous polymorph that melts at 102.8 degrees C. The anhydrous polymorph, if stored at room temperature and humidity, gradually changes to H polymorph while, if stored in water vapour saturated atmosphere, it gets back water and reverts to the hemihydrate form. On the contrary, both an isothermal treatment at 80 degrees C and melt cooling bring to the B polymorph. (C) 2009 Elsevier B.V. All rights reserved.

引用

页码：1054 / 1059

页数：6

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