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A study of the heat-mediated phase transformations of praziquantel hydrates. Evaluation of their impact on the dissolution rate

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dc.citation.titleHeliyones
dc.citation.volume8
dc.creatorSalazar Rojas, Duvernis
dc.creatorKaufman, Teodoro Saúl
dc.creatorMaggio, Rubén Mariano
dc.date.accessioned2022-12-16T16:13:45Z
dc.date.available2022-12-16T16:13:45Z
dc.date.issued2022-11
dc.descriptionComprehensive knowledge of the critical properties of the active pharmaceutical ingredients is a requirement within the modern concept of quality. Praziquantel hemihydrate (HH) and monohydrate (MH) are new solid forms of this antihelmintic agent, which have better solubility properties than the commercial anhydrous solid form (polymorph A). The thermal stability of the hydrates was evaluated, aiming to understand any possible transformation (amorphization, change to a less soluble form). Therefore, HH and MH were prepared along with the related anhydrous solid forms A and B, and characterized employing solid-state nuclear magnetic resonance, powder X-ray diffraction, mid and near infrared spectroscopy, thermal methods and the intrinsic dissolution rate. The transformations of HH and MH under thermal stress conditions were monitored through a variable temperature infrared spectroscopy approach, assisted by multivariate curve resolution with alternating least squares (MCR-ALS), finding that HH undergoes a two-step transformation (HH→B→A) to form A, whereas MH dehydrates directly into form A. This was further confirmed by conventional calorimetric methods (differential scanning calorimetry and thermogravimetry) and powder X-ray diffractometry. The impact of changes in the stressed solid forms and their dissolution rates was also assessed. Significant differences in dissolution performance were found regarding the solid forms produced as a consequence of thermally-induced dehydration.es
dc.description.filFil: Salazar Rojas, Duvernis. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Área de Análisis de Medicamentos. Instituto de Química Rosario (IQUIR-CONICET); Argentina.es
dc.description.filFil: Kaufman, Teodoro Saúl. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Área de Análisis de Medicamentos. Instituto de Química Rosario (IQUIR-CONICET); Argentina.es
dc.description.filFil: Maggio, Rubén Mariano. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Área de Análisis de Medicamentos. Instituto de Química Rosario (IQUIR-CONICET); Argentina.es
dc.description.sponsorshipConsejo Nacional de Investigaciones Científicas y Técnicas: PUE06-IQUIR
dc.description.sponsorshipUniversidad Nacional de Rosario: BIO572, 80020190300200UR
dc.formatapplication/pdf
dc.format.extent1-10es
dc.identifier.issn2405-8440es
dc.identifier.urihttp://hdl.handle.net/2133/25041
dc.language.isoenges
dc.publisherElsevieres
dc.relation.publisherversionhttps://www.sciencedirect.com/science/article/pii/S2405844022026056#kwrds0010
dc.relation.publisherversionhttps://doi.org/10.1016/j.heliyon.2022.e11317
dc.rightsopenAccesses
dc.rights.holderSalazar Rojas, Duvernises
dc.rights.holderKaufman, Teodoro Saúles
dc.rights.holderMaggio, Rubén Marianoes
dc.rights.holderUniversidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas
dc.rights.textAttribution-NonCommercial-NoDerivatives 4.0 International (CC BY-NC-ND 4.0)es
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/*
dc.subjectChemometricses
dc.subjectHot-stage-MIRes
dc.subjectHydrateses
dc.subjectPolymorphismes
dc.subjectPraziquanteles
dc.titleA study of the heat-mediated phase transformations of praziquantel hydrates. Evaluation of their impact on the dissolution ratees
dc.typearticle
dc.typeartículo
dc.typepublishedVersion
dc.type.collectionarticulo
dc.type.versionpublishedVersiones

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