Effect of pressure up to 5.5 GPa on dry powder samples of chlorpropamide form-A

被引:49
作者
Boldyreva, Elena V.
Dmitriev, Vladimir
Hancock, Bruno C.
机构
[1] Novosibirsk State Univ, Novosibirsk 630090, Russia
[2] RAS, SB, Inst Solid State Chem, Novosibirsk 630128, Russia
[3] Pfizer Inc, Groton, CT 06340 USA
[4] European Synchrotron Radiat Facil, Swiss Norwegian Beamlines, F-38043 Grenoble, France
基金
俄罗斯基础研究基金会;
关键词
pressure; polymorphism; polymorphic transformation; X-ray powder diffraction; chlorpropamide;
D O I
10.1016/j.ijpharm.2006.07.019
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effect of pressure up to 5.5 GPa on a dry powder sample of chlorpropamide (4-chloro-N-((propylamino)-carbonyl)-benzenesulfonamide), form-A (sp. gr. P2(1)2(1)2(1), a = 9.066 angstrom, b = 5.218 angstrom, c = 26.604 angstrom), was studied in situ in a Merrill-Bassett diamond anvil cell using high-resolution Xray powder diffraction (a synchrotron radiation source at SNBLESRF, Grenoble). No evidence of the polymorphic transformation of chlorpropamide form-A to form-C was observed. The A-C polymorphic transition on tabletting previously reported by Otsuka et al. (1989) is therefore likely to be due to local heating effects. Similarly, the phase transitions of form-A reported by Cao (2002) to be induced by pressure applied to a sample in its saturated ethanol solution (at 0.9 and at 2.0 GPa) would appear to be solvent-mediated. In the dry sample, a phase transition may be supposed to occur at pressures above 4 GPa, but this requires further studies. (c) 2006 Elsevier B.V. All rights reserved.
引用
收藏
页码:51 / 57
页数:7
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