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Characteristics of indomethacin-saccharin (IMC-SAC) co-crystals prepared by an anti-solvent crystallization process
- Authors
- Chun, Nan-Hee; Wang, In-Chun; Lee, Min-Jeong; Jung, Yun-Taek; Lee, Sangkil; Kim, Woo-Sik; Choi, Guang J.
- Issue Date
- Nov-2013
- Publisher
- ELSEVIER
- Keywords
- Co-crystal; Indomethacin; Saccharin; Anti-solvent crystallization; Mechanism; Dissolution rate
- Citation
- EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, v.85, no.3, pp 854 - 861
- Pages
- 8
- Journal Title
- EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
- Volume
- 85
- Number
- 3
- Start Page
- 854
- End Page
- 861
- ISSN
- 0939-6411
1873-3441
- Abstract
- The creation of co-crystals of various insoluble drug substances has been extensively investigated as a promising approach to improve their pharmaceutical performance. In this study, co-crystal powders of indomethacin and saccharin (IMC-SAC) were prepared by an anti-solvent (water) addition and compared with co-crystals by evaporation method. No successful synthesis of a pharmaceutical co-crystal powder via an anti-solvent approach has been reported. Among solvents examined, methanol was practically the only one that resulted in the formation of highly pure IMC-SAC co-crystal powders by anti-solvent approach. The mechanism of a preferential formation of IMC-SAC co-crystal to IMC was explained with two aspects: phase solubility diagram and solution complexation concept. Accordingly, the anti-solvent approach can be considered as a competitive route for producing pharmaceutical co-crystal powders with acceptable properties. (C) 2013 Elsevier By. All rights reserved.
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