Chemical degradation kinetics of fibrates: bezafibrate, ciprofibrate and fenofibrate
Autor(a) principal: | |
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Data de Publicação: | 2016 |
Outros Autores: | , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Brazilian Journal of Pharmaceutical Sciences |
Texto Completo: | https://www.revistas.usp.br/bjps/article/view/128352 |
Resumo: | Fibrates are drugs used for the treatment of hypertriglyceridemia and for the prevention of atherosclerosis. Three drugs in the fibrate class, ciprofibrate, fenofibrate and bezafibrate, were chosen for this study because their raw materials are readily available and because scientific publications on these compounds is limited. To evaluate their intrinsic stability, the drugs were exposed to a test condition (temperature, oxidation, UV light exposure, hydrolysis at different pH values and metal ions in solution) and then were subjected to analysis by HPLC. The samples were run on a C18 column, with a flow rate of 1.0 mL min-1 in a mobile phase consisting of methanol: 0.01 % phosphoric acid v/v (80:20), with variable detection wavelengths in the UV spectra. The analysis methodology showed satisfactory performance parameters. The three drugs were very unstable, degrading in each of the conditions evaluated. The test conditions of acid and basic hydrolysis showed the most significant degradation. The results demonstrated that the drugs in this class are unstable. Based on these experimentally determined degradation kinetics, it is easy to understand and emphasize the importance of the lack of liquid dosage forms on the market for fibrates because of their instability. |
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Brazilian Journal of Pharmaceutical Sciences |
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Chemical degradation kinetics of fibrates: bezafibrate, ciprofibrate and fenofibrate Fibrates are drugs used for the treatment of hypertriglyceridemia and for the prevention of atherosclerosis. Three drugs in the fibrate class, ciprofibrate, fenofibrate and bezafibrate, were chosen for this study because their raw materials are readily available and because scientific publications on these compounds is limited. To evaluate their intrinsic stability, the drugs were exposed to a test condition (temperature, oxidation, UV light exposure, hydrolysis at different pH values and metal ions in solution) and then were subjected to analysis by HPLC. The samples were run on a C18 column, with a flow rate of 1.0 mL min-1 in a mobile phase consisting of methanol: 0.01 % phosphoric acid v/v (80:20), with variable detection wavelengths in the UV spectra. The analysis methodology showed satisfactory performance parameters. The three drugs were very unstable, degrading in each of the conditions evaluated. The test conditions of acid and basic hydrolysis showed the most significant degradation. The results demonstrated that the drugs in this class are unstable. Based on these experimentally determined degradation kinetics, it is easy to understand and emphasize the importance of the lack of liquid dosage forms on the market for fibrates because of their instability. Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2016-09-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/12835210.1590/s1984-82502016000300019Brazilian Journal of Pharmaceutical Sciences; Vol. 52 Núm. 3 (2016); 545-553Brazilian Journal of Pharmaceutical Sciences; v. 52 n. 3 (2016); 545-553Brazilian Journal of Pharmaceutical Sciences; Vol. 52 No. 3 (2016); 545-5532175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/128352/125224Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso)info:eu-repo/semantics/openAccessOliveira, Marcelo Antonio deSilva, Gerliane Damázio daCampos, Michele Soares Tacchi2017-03-16T17:54:51Zoai:revistas.usp.br:article/128352Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2017-03-16T17:54:51Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false |
dc.title.none.fl_str_mv |
Chemical degradation kinetics of fibrates: bezafibrate, ciprofibrate and fenofibrate |
title |
Chemical degradation kinetics of fibrates: bezafibrate, ciprofibrate and fenofibrate |
spellingShingle |
Chemical degradation kinetics of fibrates: bezafibrate, ciprofibrate and fenofibrate Oliveira, Marcelo Antonio de |
title_short |
Chemical degradation kinetics of fibrates: bezafibrate, ciprofibrate and fenofibrate |
title_full |
Chemical degradation kinetics of fibrates: bezafibrate, ciprofibrate and fenofibrate |
title_fullStr |
Chemical degradation kinetics of fibrates: bezafibrate, ciprofibrate and fenofibrate |
title_full_unstemmed |
Chemical degradation kinetics of fibrates: bezafibrate, ciprofibrate and fenofibrate |
title_sort |
Chemical degradation kinetics of fibrates: bezafibrate, ciprofibrate and fenofibrate |
author |
Oliveira, Marcelo Antonio de |
author_facet |
Oliveira, Marcelo Antonio de Silva, Gerliane Damázio da Campos, Michele Soares Tacchi |
author_role |
author |
author2 |
Silva, Gerliane Damázio da Campos, Michele Soares Tacchi |
author2_role |
author author |
dc.contributor.author.fl_str_mv |
Oliveira, Marcelo Antonio de Silva, Gerliane Damázio da Campos, Michele Soares Tacchi |
description |
Fibrates are drugs used for the treatment of hypertriglyceridemia and for the prevention of atherosclerosis. Three drugs in the fibrate class, ciprofibrate, fenofibrate and bezafibrate, were chosen for this study because their raw materials are readily available and because scientific publications on these compounds is limited. To evaluate their intrinsic stability, the drugs were exposed to a test condition (temperature, oxidation, UV light exposure, hydrolysis at different pH values and metal ions in solution) and then were subjected to analysis by HPLC. The samples were run on a C18 column, with a flow rate of 1.0 mL min-1 in a mobile phase consisting of methanol: 0.01 % phosphoric acid v/v (80:20), with variable detection wavelengths in the UV spectra. The analysis methodology showed satisfactory performance parameters. The three drugs were very unstable, degrading in each of the conditions evaluated. The test conditions of acid and basic hydrolysis showed the most significant degradation. The results demonstrated that the drugs in this class are unstable. Based on these experimentally determined degradation kinetics, it is easy to understand and emphasize the importance of the lack of liquid dosage forms on the market for fibrates because of their instability. |
publishDate |
2016 |
dc.date.none.fl_str_mv |
2016-09-01 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/128352 10.1590/s1984-82502016000300019 |
url |
https://www.revistas.usp.br/bjps/article/view/128352 |
identifier_str_mv |
10.1590/s1984-82502016000300019 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/128352/125224 |
dc.rights.driver.fl_str_mv |
Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso) info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso) |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
dc.source.none.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences; Vol. 52 Núm. 3 (2016); 545-553 Brazilian Journal of Pharmaceutical Sciences; v. 52 n. 3 (2016); 545-553 Brazilian Journal of Pharmaceutical Sciences; Vol. 52 No. 3 (2016); 545-553 2175-9790 1984-8250 reponame:Brazilian Journal of Pharmaceutical Sciences instname:Universidade de São Paulo (USP) instacron:USP |
instname_str |
Universidade de São Paulo (USP) |
instacron_str |
USP |
institution |
USP |
reponame_str |
Brazilian Journal of Pharmaceutical Sciences |
collection |
Brazilian Journal of Pharmaceutical Sciences |
repository.name.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP) |
repository.mail.fl_str_mv |
bjps@usp.br||elizabeth.igne@gmail.com |
_version_ |
1800222912845709312 |