Syntheses and pharmacokinetics properties of an iloperidone pharmaceutical cocrystal

Abstract

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.