ArticleACS omega2025
Paliperidone Acid-Based Cocrystal for Improving Biopharmaceutical Properties: In Vitro and In Vivo Evaluation.
Article in ACS omega, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
1 citing paper in PubMed.
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Authors and funding
9 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Although it is an effective and well-tolerated antipsychotic, paliperidone is practically insoluble and suffers from low oral bioavailability. The current work aims to develop paliperidone cocrystals using different short-chain acids as coformers to improve biopharmaceutical properties. The formulation showed higher solubility and was characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy. In addition, the dissolution rate and oral bioavailability study were assessed in comparison with the pure drug. A cocrystal formulation containing paliperidone and oxalic acid (as coformers) in a 1:2 molar ratio exhibited the highest solubility (9831 ± 113 μg/mL) among screened coformers. Cocrystal structural features evidenced the formation of hydrogen bonds between paliperidone and coformers, while solid-state analyses verified their existence in the less crystalline state. Additionally, the cocrystal showed a faster dissolution rate when compared with the pure drug. Furthermore, the in vitro dissolution pattern of the cocrystal was further mirrored in its higher improvement of bioavailability (2.66-fold) and plasma retention when compared to the drug suspension. These results suggest that the cocrystal provides a feasible solution to unwanted biopharmaceutical properties of paliperidone.
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Registered trials
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