Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques

Rosmarinic acid (RA) is a phenolic compound that presents well-documented anti-inflammatory, antioxidant and antitumor activities, and based on its pharmacological potential and poor bioavailability, several solid dosage forms have been developed to RA delivery. Therefore, in literature, there are n...

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Autores: Veras, Kleyton Santos, Fachel, Flávia Nathiely Silveira, Pittol, Vanessa, Garcia, Keth Ribeiro, Bassani, Valquiria Linck, Santos, Venina dos, Henriques, Amelia Teresinha, Teixeira, Helder Ferreira, Koester, Leticia Scherer
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2019
País:Brasil
Institución:Universidade Federal do Rio Grande do Sul (UFRGS)
Repositorio:Repositório Institucional da UFRGS
Idioma:inglés
OAI Identifier:oai:www.lume.ufrgs.br:10183/206428
Acceso en línea:http://hdl.handle.net/10183/206428
Access Level:acceso abierto
Palabra clave:Farmácia
Ácido rosmarínico
Rosmarinic acid
Excipient
Compatibility
TG
ssNMR
IST
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spelling 2020-03-04T04:20:21Z20191319-0164http://hdl.handle.net/10183/206428001110276Rosmarinic acid (RA) is a phenolic compound that presents well-documented anti-inflammatory, antioxidant and antitumor activities, and based on its pharmacological potential and poor bioavailability, several solid dosage forms have been developed to RA delivery. Therefore, in literature, there are no reports about RA compatibility with excipients. In this regard, the aim of the present study was to evaluate, for the first time, the compatibility of RA with excipients commonly used in solid dosage forms at a 1:1 (RA: excipient) ratio using differential scanning calorimetry (DSC), thermogravimetry (TG), Fourier-transform infrared (FTIR), solid-state nuclear magnetic resonance (ssNMR), and isothermal stress testing (IST) coupled with liquid chromatography (LC). The excipients selected were hydroxypropyl methylcellulose (HPMC), microcrystalline cellulose (MCC), lactose monohydrate (LAC), polyvinylpyrrolidone (PVP), talc (TALC), croscarmellose sodium (CCS), and magnesium stearate (MgSTE). According to DSC results, physical interactions were found between RA and HPMC, LAC, CCS, and MgSTE. The TG analyses confirmed the physical interactions and suggested chemical incompatibility. FTIR revealed physical interaction of RA with TALC and MgSTE and the ssNMR confirmed the physical interaction showed by FTIR and excluded the presence of chemical incompatibility. By IST, the greatest loss of RA content was found to CCS and MgSTE (>15%), demonstrating chemical incompatibilities with RA. High temperatures used in DSC and TG analyses could be responsible for incompatibilities in binary mixtures (BMs) with HPMC and LAC, while temperature above 25 C and presence of water were factors that promote incompatibilities in BMs with CCS and MgSTE. Overall results demonstrate that RA was compatible with MCC and PVP.application/pdfengSaudi Pharmaceutical Journal. Riad (Arábia Saudita). Vol. 27, no. 8 (Dec. 2019), p. 1138-1145FarmáciaÁcido rosmarínicoRosmarinic acidExcipientCompatibilityTGssNMRISTCompatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniquesEstrangeiroinfo:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UFRGSinstname:Universidade Federal do Rio Grande do Sul (UFRGS)instacron:UFRGSVeras, Kleyton SantosFachel, Flávia Nathiely SilveiraPittol, VanessaGarcia, Keth RibeiroBassani, Valquiria LinckSantos, Venina dosHenriques, Amelia TeresinhaTeixeira, Helder FerreiraKoester, Leticia SchererTEXT001110276.pdf.txt001110276.pdf.txtExtracted Texttext/plain41046http://www.lume.ufrgs.br/bitstream/10183/206428/2/001110276.pdf.txtdd6ec41870851e7d9c36bc0ec2af4482MD52ORIGINAL001110276.pdfTexto completo (inglês)application/pdf1043589http://www.lume.ufrgs.br/bitstream/10183/206428/1/001110276.pdff21290999e242ae28db74bda63495224MD5110183/2064282020-03-05 04:18:06.008448oai:www.lume.ufrgs.br:10183/206428Repositório InstitucionalPUBhttps://lume.ufrgs.br/oai/requestlume@ufrgs.bropendoar:2020-03-05T07:18:06Repositório Institucional da UFRGS - Universidade Federal do Rio Grande do Sul (UFRGS)false
dc.title.pt_BR.fl_str_mv Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques
title Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques
spellingShingle Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques
Veras, Kleyton Santos
Farmácia
Ácido rosmarínico
Rosmarinic acid
Excipient
Compatibility
TG
ssNMR
IST
title_short Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques
title_full Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques
title_fullStr Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques
title_full_unstemmed Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques
title_sort Compatibility study of rosmarinic acid with excipients used in pharmaceutical solid dosage forms using thermal and non-thermal techniques
dc.creator.none.fl_str_mv Veras, Kleyton Santos
Fachel, Flávia Nathiely Silveira
Pittol, Vanessa
Garcia, Keth Ribeiro
Bassani, Valquiria Linck
Santos, Venina dos
Henriques, Amelia Teresinha
Teixeira, Helder Ferreira
Koester, Leticia Scherer
author Veras, Kleyton Santos
author_facet Veras, Kleyton Santos
Fachel, Flávia Nathiely Silveira
Pittol, Vanessa
Garcia, Keth Ribeiro
Bassani, Valquiria Linck
Santos, Venina dos
Henriques, Amelia Teresinha
Teixeira, Helder Ferreira
Koester, Leticia Scherer
author_role author
author2 Fachel, Flávia Nathiely Silveira
Pittol, Vanessa
Garcia, Keth Ribeiro
Bassani, Valquiria Linck
Santos, Venina dos
Henriques, Amelia Teresinha
Teixeira, Helder Ferreira
Koester, Leticia Scherer
author2_role author
author
author
author
author
author
author
author
dc.subject.por.fl_str_mv Farmácia
Ácido rosmarínico
topic Farmácia
Ácido rosmarínico
Rosmarinic acid
Excipient
Compatibility
TG
ssNMR
IST
dc.subject.eng.fl_str_mv Rosmarinic acid
Excipient
Compatibility
TG
ssNMR
IST
description Rosmarinic acid (RA) is a phenolic compound that presents well-documented anti-inflammatory, antioxidant and antitumor activities, and based on its pharmacological potential and poor bioavailability, several solid dosage forms have been developed to RA delivery. Therefore, in literature, there are no reports about RA compatibility with excipients. In this regard, the aim of the present study was to evaluate, for the first time, the compatibility of RA with excipients commonly used in solid dosage forms at a 1:1 (RA: excipient) ratio using differential scanning calorimetry (DSC), thermogravimetry (TG), Fourier-transform infrared (FTIR), solid-state nuclear magnetic resonance (ssNMR), and isothermal stress testing (IST) coupled with liquid chromatography (LC). The excipients selected were hydroxypropyl methylcellulose (HPMC), microcrystalline cellulose (MCC), lactose monohydrate (LAC), polyvinylpyrrolidone (PVP), talc (TALC), croscarmellose sodium (CCS), and magnesium stearate (MgSTE). According to DSC results, physical interactions were found between RA and HPMC, LAC, CCS, and MgSTE. The TG analyses confirmed the physical interactions and suggested chemical incompatibility. FTIR revealed physical interaction of RA with TALC and MgSTE and the ssNMR confirmed the physical interaction showed by FTIR and excluded the presence of chemical incompatibility. By IST, the greatest loss of RA content was found to CCS and MgSTE (>15%), demonstrating chemical incompatibilities with RA. High temperatures used in DSC and TG analyses could be responsible for incompatibilities in binary mixtures (BMs) with HPMC and LAC, while temperature above 25 C and presence of water were factors that promote incompatibilities in BMs with CCS and MgSTE. Overall results demonstrate that RA was compatible with MCC and PVP.
publishDate 2019
dc.date.issued.fl_str_mv 2019
dc.date.accessioned.fl_str_mv 2020-03-04T04:20:21Z
dc.type.driver.fl_str_mv Estrangeiro
info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10183/206428
dc.identifier.issn.pt_BR.fl_str_mv 1319-0164
dc.identifier.nrb.pt_BR.fl_str_mv 001110276
identifier_str_mv 1319-0164
001110276
url http://hdl.handle.net/10183/206428
dc.language.iso.fl_str_mv eng
language eng
dc.relation.ispartof.pt_BR.fl_str_mv Saudi Pharmaceutical Journal. Riad (Arábia Saudita). Vol. 27, no. 8 (Dec. 2019), p. 1138-1145
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv reponame:Repositório Institucional da UFRGS
instname:Universidade Federal do Rio Grande do Sul (UFRGS)
instacron:UFRGS
instname_str Universidade Federal do Rio Grande do Sul (UFRGS)
instacron_str UFRGS
institution UFRGS
reponame_str Repositório Institucional da UFRGS
collection Repositório Institucional da UFRGS
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