Journal
CRYSTAL GROWTH & DESIGN
Volume 13, Issue 12, Pages 5261-5266Publisher
AMER CHEMICAL SOC
DOI: 10.1021/cg4010104
Keywords
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Funding
- National Natural Science Foundation of China [21075051, 21275064, 30973587, 81102383]
- Program for New Century Excellent Talents in University [NCET-10-0433]
- National Basic Research Program of China (973 Program) [2012CB821700]
- Major International (Regional) Joint Research Project of NSFC [21120102034]
- NSFC [20831002]
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The crystal engineering strategy was used to facilitate the supramolecular synthesis of a new crystalline phase of iloperidone, an atypical psychotropic drug with known problems related to poor dissolution and absorption profile. The novel crystal forms Jilin University China-Cocrystal-1 (JUC-C1), Jilin University China-Cocrystal-2 (JUC-C2), and Jilin University China-Cocrystal-3 (JUC-C3) of iloperidone with 3-hydroxybenzoic acid (3-HBA), 2,3-dihydroxybenzoic acid (2,3-DHBA), and 3,5-dihydroxybenzoic acid (3,5-DHBA) were obtained using the reaction crystallization method (RCM). The dissolution and pharmacokinetics studies were performed to exploit this atypical psychotropic drug. In the dissolution experiment, JUC-C1, JUC-C2, and JUC-C3 (JUC-C1-3) showed a much faster dissolution rate than the original active pharmaceutical ingredient (API) in simulated gastric fluid media (pH = 1.2). Furthermore, pharmacokinetic behavior of JUC-C1-3 and API was investigated to evaluate the effectiveness of this strategy for enhancing the oral absorption of iloperidone. The in vitro and in vivo studies revealed that JUC-C2 possessed an excellent dissolution behavior and improved pharmacokinetic profile.
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