Syntheses and pharmacokinetics properties of an iloperidone pharmaceutical cocrystal

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Author(s)
Zhang, Ting-Ting
Wang, Hai-Tao
Jia, Jiang-Tao
Cui, Xiao-Qiang
Li, Qin
Zhu, Guang-Shan
Griffith University Author(s)
Year published
2014
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We report here a pharmaceutical cocrystal, which was composed of iloperidone with 3, 5-pyridinedicarboxlic acid by crystal engineering strategy. It was characterized by single crystal X-ray and powder X-ray diffraction, which demonstrated that the cocrystal with high purity was obtained. Pharmacokinetics (PK) study of Jilin Uni- versity China-Cocrystal 10 (JUC-C10) was performed to evaluate the advantages of this strategy for enhancing the oral absorption of the original active pharmaceutical ingredient (API) of iloperidone. The in vivo study of Beagle dogs revealed that the plasma concentration of JUC-C10 reached the maximum ...
View more >We report here a pharmaceutical cocrystal, which was composed of iloperidone with 3, 5-pyridinedicarboxlic acid by crystal engineering strategy. It was characterized by single crystal X-ray and powder X-ray diffraction, which demonstrated that the cocrystal with high purity was obtained. Pharmacokinetics (PK) study of Jilin Uni- versity China-Cocrystal 10 (JUC-C10) was performed to evaluate the advantages of this strategy for enhancing the oral absorption of the original active pharmaceutical ingredient (API) of iloperidone. The in vivo study of Beagle dogs revealed that the plasma concentration of JUC-C10 reached the maximum concentration and effec- tive blood level earlier than the original API after oral administration, which suggested that JUC-C10 exhibited a more rapid absorption profile and could thus achieve a rapid onset of action.
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View more >We report here a pharmaceutical cocrystal, which was composed of iloperidone with 3, 5-pyridinedicarboxlic acid by crystal engineering strategy. It was characterized by single crystal X-ray and powder X-ray diffraction, which demonstrated that the cocrystal with high purity was obtained. Pharmacokinetics (PK) study of Jilin Uni- versity China-Cocrystal 10 (JUC-C10) was performed to evaluate the advantages of this strategy for enhancing the oral absorption of the original active pharmaceutical ingredient (API) of iloperidone. The in vivo study of Beagle dogs revealed that the plasma concentration of JUC-C10 reached the maximum concentration and effec- tive blood level earlier than the original API after oral administration, which suggested that JUC-C10 exhibited a more rapid absorption profile and could thus achieve a rapid onset of action.
View less >
Journal Title
Inorganic Chemistry Communications
Volume
39
Copyright Statement
© 2014 Elsevier Inc. This is the author-manuscript version of this paper. Reproduced in accordance with the copyright policy of the publisher. Please refer to the journal's website for access to the definitive, published version.
Subject
Inorganic chemistry
Inorganic chemistry not elsewhere classified
Other chemical sciences