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Co-crystalline solid solution affords a high-soluble and fast-absorbing form of praziquantel
Date
2023
Abstract
Praziquantel (PZQ) is a chiral class-II drug, and it is used as a racemate for the treatment of schistosomiasis. The knowledge of several cocrystals with dicarboxylic acids has prompted the realization of solid solutions of PZQ with both enantiomers of malic acid and tartaric acid. Here, the solid form landscape of such a six-component system has been investigated. In the process, two new cocrystals were structural-characterized and three non-stoichiometric, mixed crystal forms identified and isolated. Thermal and solubility analysis indicates a fourfold solubility advantage for the newly prepared solid solutions over the pure drug. In addition, a pharmacokinetic study was conducted in rats, which involved innovative mini-capsules for the oral administration of the solid samples. The available data indicate that the faster dissolution rate of the solid solutions translates in faster absorption of the drug and helps maintain a constant steady-state concentration.
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Publisher
American Chemical Society
Citation
Molecular Pharmaceutics, 2023, 20, 4,pp. 2009–2016
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Funding Information
The work of M.L. and C.C. was supported by SFI-SIRG grant number 15/sirg/3577. The work of FR was funded by the Erasmus+ Traineeship Programme
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Type
Article
Rights
https://creativecommons.org/licenses/by-nc-sa/4.0/