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 University 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 effective 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.
We report here a pharmaceutical cocrystal, which was composed of iloperidone with 3, 5-pyridinedicarboxlic acid by crystal engineering strategy. The in vivo study of Beagle dogs revealed that the plasma concentration of JUC-C10 reached to the maximum concentration and effective blood level earlier than the original API after oral administration. [Display omitted]
•In our work, JUC-C10 with high purity was obtained in a mild condition.•The dissolution and pharmacokinetic studies were conducted to evaluate the pharmaceutical characteristics of original API and JUC-C10.•The great improvement of absorption illustrated that JUC-C10 would be a favored candidate for the pharmaceutical industry.