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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