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Co-Crystalline Solid Solution Affords a High-Soluble and Fast-Absorbing Form of Praziquantel

Cappuccino C.
•
Spoletti E.
•
Renni F.
altro
Lusi M.
2023
  • journal article

Periodico
MOLECULAR PHARMACEUTICS
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.
DOI
10.1021/acs.molpharmaceut.2c00984
WOS
WOS:000946785600001
Archivio
https://hdl.handle.net/11368/3058780
info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-85149805305
https://pubs.acs.org/doi/10.1021/acs.molpharmaceut.2c00984
Diritti
open access
license:creative commons
license:creative commons
license uri:http://creativecommons.org/licenses/by/4.0/
license uri:http://creativecommons.org/licenses/by/4.0/
FVG url
https://arts.units.it/bitstream/11368/3058780/1/acs.molpharmaceut.2c00984.pdf
Soggetti
  • chirality

  • malic acid

  • mini-capsule

  • mixed crystal

  • praziquantel

  • solid solution

  • tartaric acid

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