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

Autores
Salazar Rojas, Duvernis Maria; Kaufman, Teodoro Saul; Maggio, Ruben Mariano
Año de publicación
2022
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Comprehensive 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.
Fil: Salazar Rojas, Duvernis Maria. 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
Fil: Kaufman, Teodoro Saul. 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
Fil: Maggio, Ruben Mariano. 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
Materia
CHEMOMETRICS
HOT-STAGE-MIR
HYDRATES
POLYMORPHISM
PRAZIQUANTEL
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:11336/216903
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/216903
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rateSalazar Rojas, Duvernis MariaKaufman, Teodoro SaulMaggio, Ruben MarianoCHEMOMETRICSHOT-STAGE-MIRHYDRATESPOLYMORPHISMPRAZIQUANTELhttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1Comprehensive 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.Fil: Salazar Rojas, Duvernis Maria. 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; ArgentinaFil: Kaufman, Teodoro Saul. 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; ArgentinaFil: Maggio, Ruben Mariano. 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; ArgentinaElsevier2022-11info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/216903Salazar Rojas, Duvernis Maria; Kaufman, Teodoro Saul; Maggio, Ruben Mariano; A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rate; Elsevier; Heliyon; 8; 11; 11-2022; 1-102405-8440CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S2405844022026056info:eu-repo/semantics/altIdentifier/doi/10.1016/j.heliyon.2022.e11317info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T09:49:21Zoai:ri.conicet.gov.ar:11336/216903instacron: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:34982025-09-03 09:49:21.296CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rate
title A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rate
spellingShingle A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rate
Salazar Rojas, Duvernis Maria
CHEMOMETRICS
HOT-STAGE-MIR
HYDRATES
POLYMORPHISM
PRAZIQUANTEL
title_short A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rate
title_full A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rate
title_fullStr A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rate
title_full_unstemmed A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rate
title_sort A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rate
dc.creator.none.fl_str_mv Salazar Rojas, Duvernis Maria
Kaufman, Teodoro Saul
Maggio, Ruben Mariano
author Salazar Rojas, Duvernis Maria
author_facet Salazar Rojas, Duvernis Maria
Kaufman, Teodoro Saul
Maggio, Ruben Mariano
author_role author
author2 Kaufman, Teodoro Saul
Maggio, Ruben Mariano
author2_role author
author
dc.subject.none.fl_str_mv CHEMOMETRICS
HOT-STAGE-MIR
HYDRATES
POLYMORPHISM
PRAZIQUANTEL
topic CHEMOMETRICS
HOT-STAGE-MIR
HYDRATES
POLYMORPHISM
PRAZIQUANTEL
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv Comprehensive 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.
Fil: Salazar Rojas, Duvernis Maria. 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
Fil: Kaufman, Teodoro Saul. 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
Fil: Maggio, Ruben Mariano. 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
description Comprehensive 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.
publishDate 2022
dc.date.none.fl_str_mv 2022-11
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/11336/216903
Salazar Rojas, Duvernis Maria; Kaufman, Teodoro Saul; Maggio, Ruben Mariano; A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rate; Elsevier; Heliyon; 8; 11; 11-2022; 1-10
2405-8440
CONICET Digital
CONICET
url http://hdl.handle.net/11336/216903
identifier_str_mv Salazar Rojas, Duvernis Maria; Kaufman, Teodoro Saul; Maggio, Ruben Mariano; A study of the heat-mediated phase transformations of praziquantel hydrates: Evaluation of their impact on the dissolution rate; Elsevier; Heliyon; 8; 11; 11-2022; 1-10
2405-8440
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S2405844022026056
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.heliyon.2022.e11317
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
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
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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score 13.13397

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