title: Characteristics of indomethacin-saccharin (IMC-SAC) co-crystals prepared by an anti-solvent crystallization process.
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.
authors: Dept. of Biomedical Science, Soon Chun Hyang University, Asan, Republic of Korea.
authors: Nan-Hee
authors: NH
authors: Chun
authors: In-Chun
authors: IC
authors: Wang
authors: Min-Jeong
authors: MJ
authors: Lee
authors: Yun-Taek
authors: YT
authors: Jung
authors: Sangkil
authors: S
authors: Lee
authors: Woo-Sik
authors: WS
authors: Kim
authors: Guang J
authors: GJ
authors: Choi
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003460:Crystallization; D007213:Indomethacin / Q000737:chemistry*; D000432:Methanol / Q000737:chemistry; D011208:Powders; D012439:Saccharin / Q000737:chemistry*; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D014867:Water / Q000737:chemistry; D014961:X-Ray Diffraction
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D011208:Powders; D012997:Solvents; D014867:Water; D012439:Saccharin; D007213:Indomethacin; D000432:Methanol
keywords: Anti-solvent crystallization; Co-crystal; Dissolution rate; Indomethacin; Mechanism; Saccharin