Estimation of the Solubility of Metastable Polymorphs: A Critical Review

被引：73
作者：
Nicoud, Lucrece [1 ]
Licordari, Filippo [1 ]
Myerson, Allan S. [1 ]
机构：
[1] MIT, 77 Massachusetts Ave, Cambridge, MA 02139 USA
来源：
CRYSTAL GROWTH & DESIGN | 2018年 / 18卷 / 11期
基金：
瑞士国家科学基金会;
关键词：
DIFFERENTIAL SCANNING CALORIMETRY; L-GLUTAMIC ACID; CHLORAMPHENICOL PALMITATE; PHASE-TRANSFORMATIONS; SECONDARY NUCLEATION; DISSOLUTION BEHAVIOR; THERMODYNAMIC RULES; MOLECULAR-CRYSTALS; AQUEOUS SOLUBILITY; THERMAL-PROPERTIES;
D O I：
10.1021/acs.cgd.8b01200
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Solubility measurements of metastable poly morphs are often complicated by solvent-mediated transformation toward more stable forms. In this review, we first summarize potential experimental methods to estimate the solubility of metastable polymorphs. Then, we discuss a methodology based on a thermodynamic model, which allows solubility predictions from (i) solubility data of the stable form, and (ii) solid-state properties of the stable and metastable forms.
引用
收藏
页码：7228 / 7237
页数：10
相关论文
共 72 条
[1]   STATISTICAL THERMODYNAMICS OF LIQUID-MIXTURES - NEW EXPRESSION FOR EXCESS GIBBS ENERGY OF PARTLY OR COMPLETELY MISCIBLE SYSTEMS [J].
ABRAMS, DS ;
PRAUSNITZ, JM .
AICHE JOURNAL, 1975, 21 (01) :116-128
[2]   Continuous Crystallization of Paracetamol (Acetaminophen) Form II: Selective Access to a Metastable Solid Form [J].
Agnew, Lauren R. ;
McGlone, Thomas ;
Wheatcroft, Helen P. ;
Robertson, Amy ;
Parsons, Anna R. ;
Wilson, Chick C. .
CRYSTAL GROWTH & DESIGN, 2017, 17 (05) :2418-2427
[3]   Controlled production of the elusive metastable form II of acetaminophen (paracetamol): a fully scalable templating approach in a cooling environment [J].
Agnew, Lauren R. ;
Cruickshank, Dyanne L. ;
McGlone, Thomas ;
Wilson, Chick C. .
CHEMICAL COMMUNICATIONS, 2016, 52 (46) :7368-7371
[4]   DISSOLUTION BEHAVIOR OF POLYMORPHS OF CHLORAMPHENICOL PALMITATE AND MEFENAMIC ACID [J].
AGUIAR, AJ ;
ZELMER, JE .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1969, 58 (08) :983-+
[5]  
[Anonymous], 2001, CRYSTALLIZATION
[6]   Sulfathiazole polymorphism studied by magic-angle spinning NMR [J].
Apperley, DC ;
Fletton, RA ;
Harris, RK ;
Lancaster, RW ;
Tavener, S ;
Threlfall, TL .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1999, 88 (12) :1275-1280
[7]   Ritonavir: An extraordinary example of conformational polymorphism [J].
Bauer, J ;
Spanton, S ;
Henry, R ;
Quick, J ;
Dziki, W ;
Porter, W ;
Morris, J .
PHARMACEUTICAL RESEARCH, 2001, 18 (06) :859-866
[8]   CHARACTERIZATION OF POLYMORPHISM OF GEPIRONE HYDROCHLORIDE [J].
BEHME, RJ ;
BROOKE, D ;
FARNEY, RF ;
KENSLER, TT .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1985, 74 (10) :1041-1046
[9]  
BORKA L, 1971, ACTA PHARM SUEC, V8, P365
[10]   An evaluation of thermodynamic models for the prediction of drug and drug-like molecule solubility in organic solvents [J].
Bouillot, Baptiste ;
Teychene, Sebastien ;
Biscans, Beatrice .
FLUID PHASE EQUILIBRIA, 2011, 309 (01) :36-52
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