Evaluation of Predictive Models for Stable Solid Solution Formation

• Published in: Journal of pharmaceutical sciences Vol. 100; no. 2; pp. 667 - 680
• Main Authors: Albers, Jessica, Matthée, Karin, Knop, Klaus, Kleinebudde, Peter
• Format: Journal Article
• Language: English
• Published: Hoboken Elsevier Inc 01.02.2011; Wiley Subscription Services, Inc., A Wiley Company; Wiley; American Pharmaceutical Association; Elsevier Limited
• Subjects: amorphous; Biological and medical sciences; crystallinity; Crystallization; Drug Carriers - chemistry; extrusion; General pharmacology; glass transition; Medical sciences; melting point depression; Models, Chemical; Pharmaceutical Preparations - chemistry; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Phase Transition; solid solution; solid state; Solubility; solubility parameter; Solutions - chemistry; thermal analysis; Thermodynamics; Transition Temperature; melting point depression; amorphous; solid solution; extrusion; crystallinity; glass transition; solubility parameter; solid state; thermal analysis; Mood disorder; Evaluation; Pharmaceutical technology; Depression; Crystallinity; Glass transition; Solid state; Solubility parameter; Extrusion; Thermal analysis; Melting point; Solution
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.22313

The objective of this study was to evaluate predictive models for stable solid solution formation and to find a quick and successful approach for miscibility screenings. The results show that the interpretation of the chemical structure and the crystallinity by X-ray powder diffraction measurements as well as the determination of melting point depressions and melting enthalpies are beneficial tools to predict the miscibility of drugs and carriers. A combined approach of prediction tools is highly appropriate, as no single technique may yield all the required information. Nevertheless, the evaluation of the melting behavior via differential scanning calorimetry has the highest impact.