Co-Crystal Screening of Diclofenac
In the pharmaceutical industry, co-crystals are becoming increasingly valuable as crystalline solids that can offer altered/improved physical properties of an active pharmaceutical ingredient (API) without changing its chemical identity or biological activity. In order to identify new solid forms of...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2011-08-01
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| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1999-4923/3/3/601/ |
| _version_ | 1811262410938384384 |
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| author | John Desper Christer B. Aakeröy Angela B. Grommet |
| author_facet | John Desper Christer B. Aakeröy Angela B. Grommet |
| author_sort | John Desper |
| collection | DOAJ |
| description | In the pharmaceutical industry, co-crystals are becoming increasingly valuable as crystalline solids that can offer altered/improved physical properties of an active pharmaceutical ingredient (API) without changing its chemical identity or biological activity. In order to identify new solid forms of diclofenac—an analgesic with extremely poor aqueous solubility for which few co-crystal structures have been determined—a range of pyrazoles, pyridines, and pyrimidines were screened for co-crystal formation using solvent assisted grinding and infrared spectroscopy with an overall success rate of 50%. The crystal structures of three new diclofenac co-crystals are reported herein: (diclofenac)∙(2-aminopyrimidine), (diclofenac)∙(2-amino-4,6-dimethylpyrimidine), and (diclofenac)∙(2-amino-4-chloro-6-methylpyrimidine). |
| first_indexed | 2024-04-12T19:24:46Z |
| format | Article |
| id | doaj.art-3de5d32a13a9495e878c25e5bd5c909f |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-12T19:24:46Z |
| publishDate | 2011-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-3de5d32a13a9495e878c25e5bd5c909f2022-12-22T03:19:30ZengMDPI AGPharmaceutics1999-49232011-08-013360161410.3390/pharmaceutics3030601Co-Crystal Screening of DiclofenacJohn DesperChrister B. AakeröyAngela B. GrommetIn the pharmaceutical industry, co-crystals are becoming increasingly valuable as crystalline solids that can offer altered/improved physical properties of an active pharmaceutical ingredient (API) without changing its chemical identity or biological activity. In order to identify new solid forms of diclofenac—an analgesic with extremely poor aqueous solubility for which few co-crystal structures have been determined—a range of pyrazoles, pyridines, and pyrimidines were screened for co-crystal formation using solvent assisted grinding and infrared spectroscopy with an overall success rate of 50%. The crystal structures of three new diclofenac co-crystals are reported herein: (diclofenac)∙(2-aminopyrimidine), (diclofenac)∙(2-amino-4,6-dimethylpyrimidine), and (diclofenac)∙(2-amino-4-chloro-6-methylpyrimidine).http://www.mdpi.com/1999-4923/3/3/601/diclofenacco-crystalshydrogen bondingcrystallographyIR spectroscopy |
| spellingShingle | John Desper Christer B. Aakeröy Angela B. Grommet Co-Crystal Screening of Diclofenac Pharmaceutics diclofenac co-crystals hydrogen bonding crystallography IR spectroscopy |
| title | Co-Crystal Screening of Diclofenac |
| title_full | Co-Crystal Screening of Diclofenac |
| title_fullStr | Co-Crystal Screening of Diclofenac |
| title_full_unstemmed | Co-Crystal Screening of Diclofenac |
| title_short | Co-Crystal Screening of Diclofenac |
| title_sort | co crystal screening of diclofenac |
| topic | diclofenac co-crystals hydrogen bonding crystallography IR spectroscopy |
| url | http://www.mdpi.com/1999-4923/3/3/601/ |
| work_keys_str_mv | AT johndesper cocrystalscreeningofdiclofenac AT christerbaakeroy cocrystalscreeningofdiclofenac AT angelabgrommet cocrystalscreeningofdiclofenac |