STUDY OF THE POLYMORPHISM OF 3-(((3-(2-(7-CHLORO-2-QUINOLINYL)(E)-ETHENYL)PHENYL)((3-(DIMETHYLAMINO-3-OXOPROPYL)THIO)METHYL)THIO)PROPANOIC ACID (MK571) BY DSC, TG, XRPD AND SOLUBILITY MEASUREMENTS

被引：19

作者：

GHODBANE, S

MCCAULEY, JA

机构：

[1] Analytical Research Department, Merck Sharp and Dohme Research Laboratories, Rahway, NJ 07065

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 1990年 / 59卷 / 03期

关键词：

Antagonist; MK571; DSC; Leukotriene D[!sub]4[!/sub]-specific antagonist; Polymorphism; Solubility; X-ray powder diffraction;

D O I：

10.1016/0378-5173(90)90119-O

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Two polymorphs of the free acid of MK571 have been characterized unambiguously by differential scanning calorimetry (DSC), thermal gravimetric analysis (TG), X-ray powder diffraction (XRPD) and solubility measurements. These two species are designated forms I and II, respectively. The solubilities of the two crystal forms of MK571 were determined at several temperatures (5-55° C) in isopropyl alcohol (IPA) and methyl ethyl ketone (MEK). In all cases, Form II shows higher solubility than Form I which indicates that the latter is the thermodynamically stable form in this temperature range. The melting point of Form I (164° C) is higher than that of Form II (152° C), indicating that Form I is the more stable polymorph in the high temperature range. These data suggest that the two forms are monotropic polymorphs. © 1990.

引用

页码：281 / 286

页数：6

共 12 条

[1]

BYRN SR, 1982, SOLID STATE CHEM DRU, P79

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