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
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/52670
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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 Técnicas2025-09-29T09:43:14Zoai: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:34982025-09-29 09:43:14.835CONICET 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 application/pdf |
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) |
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CONICET Digital (CONICET) |
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Consejo Nacional de Investigaciones Científicas y Técnicas |
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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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1844613360996319232 |
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13.070432 |