Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study

Autores
Costa, Emanuel D.; Priotti, Josefina; Orlandi, Silvina; Leonardi, Darío; Lamas, Maria Celina; Nunes, Teresa G.; Diogo, Hermínio P.; Salomon, Claudio Javier; Ferreira, M. João
Año de publicación
2016
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
The saturation solubility of PVP:PZQ physical mixtures (PMs) and solid dispersions (SDs) prepared from ethanol (E/E) or ethanol/water (E/W) by the solvent evaporation method at 1:1, 2:1 and 3:1 ratio (w/w) was determined. The presence of PVP improves the solubility of PZQ (0.31 ± 0.01 mg/mL). A maximum of 1.29 ± 0.03 mg/mL of PZQ in solution was achieved for the 3:1 SD (E/E). The amount of PZQ in solution depends on the amount of polymer and on the preparation method. Solid-state NMR (ssNMR) and DSC were used to understand this behavior. Results show that PMs are a mixture of crystalline PZQ with the polymer, while SDs show different degrees of drug amorphization depending on the solvent used. For E/W SDs, PZQ exists in amorphous and crystalline states, with no clear correlation between the amount of crystalline PZQ and the amount of PVP. For E/E SDs, formulations with a higher percentage of PZQ are amorphous with the components miscible in domains larger than 3 nm (1H ssNMR relaxation measurements). Albeit its higher saturation solubility, the 3:1 E/E PVP:PZQ sample has a significant crystalline content, probably due to the water introduced by the polymer. High PVP content and small crystal size account for this result.
Fil: Costa, Emanuel D.. Universidade de Lisboa; Portugal
Fil: Priotti, Josefina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; Argentina
Fil: Orlandi, Silvina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; Argentina
Fil: Leonardi, Darío. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; Argentina
Fil: Lamas, Maria Celina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; Argentina
Fil: Nunes, Teresa G.. Universidade de Lisboa; Portugal
Fil: Diogo, Hermínio P.. Universidade de Lisboa; Portugal
Fil: Salomon, Claudio Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; Argentina
Fil: Ferreira, M. João. Universidade de Lisboa; Portugal
Materia
DSC
PHARMACEUTICAL FORMULATIONS
POLY(VINYLPYRROLIDONE)
PRAZIQUANTEL
SOLID-STATE NMR
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/52670
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/52670
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR studyCosta, Emanuel D.Priotti, JosefinaOrlandi, SilvinaLeonardi, DaríoLamas, Maria CelinaNunes, Teresa G.Diogo, Hermínio P.Salomon, Claudio JavierFerreira, M. JoãoDSCPHARMACEUTICAL FORMULATIONSPOLY(VINYLPYRROLIDONE)PRAZIQUANTELSOLID-STATE NMRhttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1The saturation solubility of PVP:PZQ physical mixtures (PMs) and solid dispersions (SDs) prepared from ethanol (E/E) or ethanol/water (E/W) by the solvent evaporation method at 1:1, 2:1 and 3:1 ratio (w/w) was determined. The presence of PVP improves the solubility of PZQ (0.31 ± 0.01 mg/mL). A maximum of 1.29 ± 0.03 mg/mL of PZQ in solution was achieved for the 3:1 SD (E/E). The amount of PZQ in solution depends on the amount of polymer and on the preparation method. Solid-state NMR (ssNMR) and DSC were used to understand this behavior. Results show that PMs are a mixture of crystalline PZQ with the polymer, while SDs show different degrees of drug amorphization depending on the solvent used. For E/W SDs, PZQ exists in amorphous and crystalline states, with no clear correlation between the amount of crystalline PZQ and the amount of PVP. For E/E SDs, formulations with a higher percentage of PZQ are amorphous with the components miscible in domains larger than 3 nm (1H ssNMR relaxation measurements). Albeit its higher saturation solubility, the 3:1 E/E PVP:PZQ sample has a significant crystalline content, probably due to the water introduced by the polymer. High PVP content and small crystal size account for this result.Fil: Costa, Emanuel D.. Universidade de Lisboa; PortugalFil: Priotti, Josefina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; ArgentinaFil: Orlandi, Silvina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; ArgentinaFil: Leonardi, Darío. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; ArgentinaFil: Lamas, Maria Celina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; ArgentinaFil: Nunes, Teresa G.. Universidade de Lisboa; PortugalFil: Diogo, Hermínio P.. Universidade de Lisboa; PortugalFil: Salomon, Claudio Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; ArgentinaFil: Ferreira, M. João. Universidade de Lisboa; PortugalElsevier Science2016-09info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/52670Costa, Emanuel D.; Priotti, Josefina; Orlandi, Silvina; Leonardi, Darío; Lamas, Maria Celina; et al.; Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study; Elsevier Science; International Journal Of Pharmaceutics; 511; 2; 9-2016; 983-9930378-5173CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0378517316307384info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ijpharm.2016.08.009info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-15T14:36:29Zoai:ri.conicet.gov.ar:11336/52670instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-10-15 14:36:30.009CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study
title Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study
spellingShingle Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study
Costa, Emanuel D.
DSC
PHARMACEUTICAL FORMULATIONS
POLY(VINYLPYRROLIDONE)
PRAZIQUANTEL
SOLID-STATE NMR
title_short Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study
title_full Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study
title_fullStr Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study
title_full_unstemmed Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study
title_sort Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study
dc.creator.none.fl_str_mv Costa, Emanuel D.
Priotti, Josefina
Orlandi, Silvina
Leonardi, Darío
Lamas, Maria Celina
Nunes, Teresa G.
Diogo, Hermínio P.
Salomon, Claudio Javier
Ferreira, M. João
author Costa, Emanuel D.
author_facet Costa, Emanuel D.
Priotti, Josefina
Orlandi, Silvina
Leonardi, Darío
Lamas, Maria Celina
Nunes, Teresa G.
Diogo, Hermínio P.
Salomon, Claudio Javier
Ferreira, M. João
author_role author
author2 Priotti, Josefina
Orlandi, Silvina
Leonardi, Darío
Lamas, Maria Celina
Nunes, Teresa G.
Diogo, Hermínio P.
Salomon, Claudio Javier
Ferreira, M. João
author2_role author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv DSC
PHARMACEUTICAL FORMULATIONS
POLY(VINYLPYRROLIDONE)
PRAZIQUANTEL
SOLID-STATE NMR
topic DSC
PHARMACEUTICAL FORMULATIONS
POLY(VINYLPYRROLIDONE)
PRAZIQUANTEL
SOLID-STATE NMR
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv The saturation solubility of PVP:PZQ physical mixtures (PMs) and solid dispersions (SDs) prepared from ethanol (E/E) or ethanol/water (E/W) by the solvent evaporation method at 1:1, 2:1 and 3:1 ratio (w/w) was determined. The presence of PVP improves the solubility of PZQ (0.31 ± 0.01 mg/mL). A maximum of 1.29 ± 0.03 mg/mL of PZQ in solution was achieved for the 3:1 SD (E/E). The amount of PZQ in solution depends on the amount of polymer and on the preparation method. Solid-state NMR (ssNMR) and DSC were used to understand this behavior. Results show that PMs are a mixture of crystalline PZQ with the polymer, while SDs show different degrees of drug amorphization depending on the solvent used. For E/W SDs, PZQ exists in amorphous and crystalline states, with no clear correlation between the amount of crystalline PZQ and the amount of PVP. For E/E SDs, formulations with a higher percentage of PZQ are amorphous with the components miscible in domains larger than 3 nm (1H ssNMR relaxation measurements). Albeit its higher saturation solubility, the 3:1 E/E PVP:PZQ sample has a significant crystalline content, probably due to the water introduced by the polymer. High PVP content and small crystal size account for this result.
Fil: Costa, Emanuel D.. Universidade de Lisboa; Portugal
Fil: Priotti, Josefina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; Argentina
Fil: Orlandi, Silvina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; Argentina
Fil: Leonardi, Darío. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; Argentina
Fil: Lamas, Maria Celina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; Argentina
Fil: Nunes, Teresa G.. Universidade de Lisboa; Portugal
Fil: Diogo, Hermínio P.. Universidade de Lisboa; Portugal
Fil: Salomon, Claudio Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; Argentina
Fil: Ferreira, M. João. Universidade de Lisboa; Portugal
description The saturation solubility of PVP:PZQ physical mixtures (PMs) and solid dispersions (SDs) prepared from ethanol (E/E) or ethanol/water (E/W) by the solvent evaporation method at 1:1, 2:1 and 3:1 ratio (w/w) was determined. The presence of PVP improves the solubility of PZQ (0.31 ± 0.01 mg/mL). A maximum of 1.29 ± 0.03 mg/mL of PZQ in solution was achieved for the 3:1 SD (E/E). The amount of PZQ in solution depends on the amount of polymer and on the preparation method. Solid-state NMR (ssNMR) and DSC were used to understand this behavior. Results show that PMs are a mixture of crystalline PZQ with the polymer, while SDs show different degrees of drug amorphization depending on the solvent used. For E/W SDs, PZQ exists in amorphous and crystalline states, with no clear correlation between the amount of crystalline PZQ and the amount of PVP. For E/E SDs, formulations with a higher percentage of PZQ are amorphous with the components miscible in domains larger than 3 nm (1H ssNMR relaxation measurements). Albeit its higher saturation solubility, the 3:1 E/E PVP:PZQ sample has a significant crystalline content, probably due to the water introduced by the polymer. High PVP content and small crystal size account for this result.
publishDate 2016
dc.date.none.fl_str_mv 2016-09
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/52670
Costa, Emanuel D.; Priotti, Josefina; Orlandi, Silvina; Leonardi, Darío; Lamas, Maria Celina; et al.; Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study; Elsevier Science; International Journal Of Pharmaceutics; 511; 2; 9-2016; 983-993
0378-5173
CONICET Digital
CONICET
url http://hdl.handle.net/11336/52670
identifier_str_mv Costa, Emanuel D.; Priotti, Josefina; Orlandi, Silvina; Leonardi, Darío; Lamas, Maria Celina; et al.; Unexpected solvent impact in the crystallinity of praziquantel/poly (vinylpyrrolidone) formulations. A solubility, DSC and solid-state NMR study; Elsevier Science; International Journal Of Pharmaceutics; 511; 2; 9-2016; 983-993
0378-5173
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0378517316307384
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ijpharm.2016.08.009
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
application/pdf
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dc.publisher.none.fl_str_mv Elsevier Science
publisher.none.fl_str_mv Elsevier Science
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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