Cediranib Maleate—From Crystal Structure Toward Materials Control
| Autor: | Anna Pettersen, Martin F. Jones, Ronald John Roberts, Simon N. Black, Helen P. Wheatcroft, Ian Michael Mcfarlane |
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| Rok vydání: | 2020 |
| Předmět: |
Active ingredient
Materials science Cediranib Maleate Maleates Pharmaceutical Science 02 engineering and technology Crystal structure 021001 nanoscience & nanotechnology 030226 pharmacology & pharmacy law.invention Crystal 03 medical and health sciences Crystallography 0302 clinical medicine Pharmaceutical Preparations law Phase (matter) Quinazolines Particle Size Crystallization 0210 nano-technology Salt formation Phase diagram |
| Zdroj: | Journal of Pharmaceutical Sciences. 109:1509-1518 |
| ISSN: | 0022-3549 |
| DOI: | 10.1016/j.xphs.2019.12.017 |
| Popis: | Cediranib maleate is an active pharmaceutical ingredient (API) in phase III of development within AstraZeneca's oncology portfolio. Analysis of the crystal structure of this API confirmed that the selected salt form was robust. The salt formation step had to be redesigned to avoid an unwanted metastable polymorph. A solvate with a twist appeared during later development and was avoided using insights gained from its crystal structure. Differences between predicted and experimental aspect ratios correlate with weaker crystal interactions. Acceptable variability in particle size was defined and accommodated. The "Matwall" is introduced as a tool for building control of API performance from the crystal structure upward. |
| Databáze: | OpenAIRE |
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