Determination of the Solubility of Crystalline Low Molar Mass Compounds in Polymers by Differential Scanning Calorimetry

被引：4
|
作者：
Rager, Timo [1 ]
机构：
[1] Solvias AG, Dept Solid State Dev, CH-4303 Kaiseraugst, Switzerland
来源：
JOURNAL OF PHARMACEUTICAL SCIENCES | 2014年 / 103卷 / 06期
关键词：
amorphous; calorimetry (DSC); liquidus; mathematical model; polymeric drug carrier; solid dispersion; solid solution; solubility; stability; thermodynamics; AMORPHOUS MOLECULAR DISPERSIONS; SOLID DISPERSIONS; PHASE-BEHAVIOR; DRUG SOLUBILITIES; MELT EXTRUSION; WATER; BIOAVAILABILITY; INDOMETHACIN; ANTIOXIDANTS; ADVANTAGE;
D O I：
10.1002/jps.23957
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A mathematical equation has been derived to calculate the liquidus for a binary system consisting of an amorphous polymer and a crystalline low molar mass compound. The experimental input to this equation is an interaction enthalpy, which is derived from the variation of the melting enthalpy with composition in differential scanning calorimetry (DSC) experiments. The predictive power of the equation has been tested with mixtures of acetylsalicylic acid, carbamazepine, or intraconazole with poly(ethylene glycol) as well as mixtures of carbamazepine with poly(acrylic acid), poly(hydroxystyrene), or poly(vinylpyrrolidone). It has been confirmed that the evaluation of the melting enthalpy in DSC is a suitable method to identify the preferred solute-polymer combinations for thermodynamically stable molecular dispersions. (c) 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci
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页码：1673 / 1679
页数：7
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