Artykuł w czasopiśmie
Brak miniatury
Licencja
CC-BYCC-BY - Uznanie autorstwa
 

Mechanochemical Synthesis and Physicochemical Characterization of Previously Unreported Praziquantel Solvates with 2-Pyrrolidone and Acetic Acid

Uproszczony widok
dc.abstract.enTwo new solvates of the widely used anthelminthic Praziquantel (PZQ) were obtained through mechanochemical screening with different liquid additives. Specifically, 2-pyrrolidone and acetic acid gave solvates with 1:1 stoichiometry (PZQ-AA and PZQ-2P, respectively). A wide-ranging characterization of the new solid forms was carried out by means of powder X-ray diffraction, differential scanning calorimetry, FT-IR, solid-state NMR and biopharmaceutical analyses (solubility and intrinsic dissolution studies). Besides, the crystal structures of the two new solvates were solved from their Synchrotron-PXRD pattern: the solvates are isostructural, with equivalent triclinic packing. In both structures acetic acid and 2-pyrrolidone showed a strong interaction with the PZQ molecule via hydrogen bond. Even though previous studies have shown that PZQ is conformationally flexible, the same syn conformation as the PZQ Form A of the C=O groups of the piperazinone-cyclohexylcarbonyl segment is involved in these two new solid forms. In terms of biopharmaceutical properties, PZQ-AA and PZQ-2P exhibited water solubility and intrinsic dissolution rate much greater than those of anhydrous Form A.
dc.affiliationUniwersytet Warszawski
dc.contributor.authorDemitri, Nicola
dc.contributor.authorChierotti, Michele R.
dc.contributor.authorHasa, Dritan
dc.contributor.authorZanolla, Debora
dc.contributor.authorVoinovich, Dario
dc.contributor.authorJones, William
dc.contributor.authorArhangelskis, Mihails
dc.contributor.authorGigli, Lara
dc.contributor.authorPerissutti, Beatrice
dc.date.accessioned2024-01-25T11:26:31Z
dc.date.available2024-01-25T11:26:31Z
dc.date.copyright2021-10-02
dc.date.issued2021
dc.description.accesstimeAT_PUBLICATION
dc.description.financePublikacja bezkosztowa
dc.description.number10
dc.description.versionFINAL_PUBLISHED
dc.description.volume13
dc.identifier.doi10.3390/PHARMACEUTICS13101606
dc.identifier.issn1999-4923
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/112229
dc.identifier.weblinkhttps://www.mdpi.com/1999-4923/13/10/1606/pdf
dc.languageeng
dc.pbn.affiliationchemical sciences
dc.relation.ispartofPharmaceutics
dc.relation.pages1606
dc.rightsCC-BY
dc.sciencecloudnosend
dc.subject.enpraziquantel
dc.subject.ensolvates
dc.subject.enacetic acid
dc.subject.en2-pyrrolidone
dc.subject.enmechanochemistry
dc.subject.enliquid-assisted grinding
dc.titleMechanochemical Synthesis and Physicochemical Characterization of Previously Unreported Praziquantel Solvates with 2-Pyrrolidone and Acetic Acid
dc.typeJournalArticle
dspace.entity.typePublication