Polymorphism of Dehydro-Aripiprazole, the Active Metabolite of the Antipsychotic Drug Aripiprazole (Abilify)
| Autor: | Magali B. Hickey, Jacob T. Trotta, Renato A. Chiarella, Mark A. Oliveira, Julius F. Remenar, Tarek A. Zeidan, Orn Almarsson |
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| Rok vydání: | 2013 |
| Předmět: |
Thermogravimetric analysis
Transition temperature Infrared spectroscopy General Chemistry Condensed Matter Physics chemistry.chemical_compound Crystallography Differential scanning calorimetry chemistry Polymorphism (materials science) Organic chemistry General Materials Science Methanol Active metabolite Powder diffraction |
| Zdroj: | Crystal Growth & Design. 13:2036-2046 |
| ISSN: | 1528-7505 1528-7483 |
| Popis: | Crystal form exploration of dehydro-aripiprazole (dAPZ), the active metabolite of the antipsychotic drug aripiprazole (APZ), elucidated five polymorphs (I, II, III, IV, and V), two methanol solvates, and a monohydrate. The forms were characterized by thermal microscopy, differential scanning calorimetry (DSC), thermal gravimetric analysis (TGA), single and powder X-ray diffraction (SCXRD and PXRD), and infrared spectroscopy. DSC analysis showed monotropic relationships among polymorphs I, II, III, and IV and enantiotropic relationships for the two form pairs I ↔ V and II ↔ V. Solvent-mediated conversion experiments indicated that Form V is the thermodynamically stable form in the temperature range 5–60 °C and Form I is the stable form at ≥70 °C, where a transition temperature lies between 60 and 70 °C. Two polymorphs of the methanol solvate (SMeOH1 and SMeOH2) were crystallized from methanol solutions in 1:1 dAPZ/methanol molar ratio. SMeOH2 is the thermodynamically stable form of the two methanol solvate... |
| Databáze: | OpenAIRE |
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