Influence of administration vehicles and drug formulations on the pharmacokinetic profile of lamotrigine in rats
Autor(a) principal: | |
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Data de Publicação: | 2002 |
Outros Autores: | , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10316/101110 https://doi.org/10.1046/j.1472-8206.2002.00096.x |
Resumo: | Given that administration vehicles and drug formulations can affect drug bioavailability, their influence on the pharmacokinetic profile of lamotrigine (LTG), a newgeneration anti-epileptic drug, was studied in rats. Three different formulations administered intraperitoneally at a dose of 10 mg⁄kg were used: (1) LTG suspended in a 0.25% methylcelulose solution, (2) LTG dissolved in a 50% propylene glycol solution, and (3) LTG isethionate dissolved in distilled water. Plasma and brain homogenate levels were determined in order to evaluate vehicle-dependent drug absorption. The results demonstrated rapid absorption of LTG when it was administered as an aqueous solution, in contrast to a slower and more erratic absorption after the injection of either the lipophilic solution or the suspension. A plasma peak was achieved 15 min post-dose with the aqueous solution, with a brain peak being achieved 15 min later, while with the other formulations both plasma and brain homogenate peaks were reached 2 h after LTG administration. This study suggests that LTG isethionate dissolved in distilled water is the most suitable formulation for successful LTG pharmacokinetic studies in rats. |
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Influence of administration vehicles and drug formulations on the pharmacokinetic profile of lamotrigine in ratsdrug formulationlamotriginepharmacokinetic profileratvehicle administrationGiven that administration vehicles and drug formulations can affect drug bioavailability, their influence on the pharmacokinetic profile of lamotrigine (LTG), a newgeneration anti-epileptic drug, was studied in rats. Three different formulations administered intraperitoneally at a dose of 10 mg⁄kg were used: (1) LTG suspended in a 0.25% methylcelulose solution, (2) LTG dissolved in a 50% propylene glycol solution, and (3) LTG isethionate dissolved in distilled water. Plasma and brain homogenate levels were determined in order to evaluate vehicle-dependent drug absorption. The results demonstrated rapid absorption of LTG when it was administered as an aqueous solution, in contrast to a slower and more erratic absorption after the injection of either the lipophilic solution or the suspension. A plasma peak was achieved 15 min post-dose with the aqueous solution, with a brain peak being achieved 15 min later, while with the other formulations both plasma and brain homogenate peaks were reached 2 h after LTG administration. This study suggests that LTG isethionate dissolved in distilled water is the most suitable formulation for successful LTG pharmacokinetic studies in rats.3910-3178-31BA | MARIA MARGARIDA COUTINHO DE SEABRA CASTEL-BRANCO CAETANOinfo:eu-repo/semantics/publishedVersionBlackwell Science2002-10info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/101110http://hdl.handle.net/10316/101110https://doi.org/10.1046/j.1472-8206.2002.00096.xeng0767-39811472-8206cv-prod-143893Castel-Branco, M. M.Figueiredo, I. V.Falcão, A. C.Macedo, T. R. A.Caramona, M. M.info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2022-10-21T09:12:49Zoai:estudogeral.uc.pt:10316/101110Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T21:18:21.327350Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse |
dc.title.none.fl_str_mv |
Influence of administration vehicles and drug formulations on the pharmacokinetic profile of lamotrigine in rats |
title |
Influence of administration vehicles and drug formulations on the pharmacokinetic profile of lamotrigine in rats |
spellingShingle |
Influence of administration vehicles and drug formulations on the pharmacokinetic profile of lamotrigine in rats Castel-Branco, M. M. drug formulation lamotrigine pharmacokinetic profile rat vehicle administration |
title_short |
Influence of administration vehicles and drug formulations on the pharmacokinetic profile of lamotrigine in rats |
title_full |
Influence of administration vehicles and drug formulations on the pharmacokinetic profile of lamotrigine in rats |
title_fullStr |
Influence of administration vehicles and drug formulations on the pharmacokinetic profile of lamotrigine in rats |
title_full_unstemmed |
Influence of administration vehicles and drug formulations on the pharmacokinetic profile of lamotrigine in rats |
title_sort |
Influence of administration vehicles and drug formulations on the pharmacokinetic profile of lamotrigine in rats |
author |
Castel-Branco, M. M. |
author_facet |
Castel-Branco, M. M. Figueiredo, I. V. Falcão, A. C. Macedo, T. R. A. Caramona, M. M. |
author_role |
author |
author2 |
Figueiredo, I. V. Falcão, A. C. Macedo, T. R. A. Caramona, M. M. |
author2_role |
author author author author |
dc.contributor.author.fl_str_mv |
Castel-Branco, M. M. Figueiredo, I. V. Falcão, A. C. Macedo, T. R. A. Caramona, M. M. |
dc.subject.por.fl_str_mv |
drug formulation lamotrigine pharmacokinetic profile rat vehicle administration |
topic |
drug formulation lamotrigine pharmacokinetic profile rat vehicle administration |
description |
Given that administration vehicles and drug formulations can affect drug bioavailability, their influence on the pharmacokinetic profile of lamotrigine (LTG), a newgeneration anti-epileptic drug, was studied in rats. Three different formulations administered intraperitoneally at a dose of 10 mg⁄kg were used: (1) LTG suspended in a 0.25% methylcelulose solution, (2) LTG dissolved in a 50% propylene glycol solution, and (3) LTG isethionate dissolved in distilled water. Plasma and brain homogenate levels were determined in order to evaluate vehicle-dependent drug absorption. The results demonstrated rapid absorption of LTG when it was administered as an aqueous solution, in contrast to a slower and more erratic absorption after the injection of either the lipophilic solution or the suspension. A plasma peak was achieved 15 min post-dose with the aqueous solution, with a brain peak being achieved 15 min later, while with the other formulations both plasma and brain homogenate peaks were reached 2 h after LTG administration. This study suggests that LTG isethionate dissolved in distilled water is the most suitable formulation for successful LTG pharmacokinetic studies in rats. |
publishDate |
2002 |
dc.date.none.fl_str_mv |
2002-10 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://hdl.handle.net/10316/101110 http://hdl.handle.net/10316/101110 https://doi.org/10.1046/j.1472-8206.2002.00096.x |
url |
http://hdl.handle.net/10316/101110 https://doi.org/10.1046/j.1472-8206.2002.00096.x |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
0767-3981 1472-8206 cv-prod-143893 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.publisher.none.fl_str_mv |
Blackwell Science |
publisher.none.fl_str_mv |
Blackwell Science |
dc.source.none.fl_str_mv |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
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Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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RCAAP |
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RCAAP |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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1817550310024937472 |