In‐vivo evaluation of prolonged release bilayer tablets of anti‐Parkinson drugs in Göttingen minipigs
Identifieur interne : 000279 ( Main/Exploration ); précédent : 000278; suivant : 000280In‐vivo evaluation of prolonged release bilayer tablets of anti‐Parkinson drugs in Göttingen minipigs
Auteurs : José Paulo Sousa E Silva ; José S. Lobo ; Maria J. Bonifácio ; Rita Machado ; Amílcar Falcão [Portugal] ; Patrício Soares-Da-SilvaSource :
- Journal of Pharmacy and Pharmacology [ 0022-3573 ] ; 2011-06.
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Abstract
Objectives Patients with Parkinson's disease can benefit from controlled released levodopa dosage forms since there is a clear clinical advantage in obtaining sustained plasma concentrations. The purpose of this study was to obtain a tablet that prolonged the release of levodopa. Methods A novel bilayer tablet, consisting of an immediate release layer containing nebicapone (100 mg) and an erosion‐matrix type prolonged release layer containing levodopa (100 mg) and carbidopa (25 mg) was developed (LCN PR). A pharmacokinetic study in Göttingen minipigs was performed to evaluate this formulation. Key findings LCN PR tablets prolonged the in‐vitro release of levodopa in HCl 0.1 m for more than 3 h. In‐vivo plasma levodopa levels peaked at a later time point with LCN PR tablets as compared with that obtained with Sinemet 100/25 (2.7 vs 0.5 h). Nebicapone increased the maximum plasma concentration and area under the plasma concentration–time curve values for levodopa. Conclusions The results obtained suggested that LCN PR tablets may have decreased the number of tablets and daily intake in the treatment of patients with Parkinson's disease.
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DOI: 10.1111/j.2042-7158.2011.01278.x
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Bonifácio</name></author><author><name sortKey="Machado, Rita" sort="Machado, Rita" uniqKey="Machado R" first="Rita" last="Machado">Rita Machado</name></author><author><name sortKey="Falcao, Amilcar" sort="Falcao, Amilcar" uniqKey="Falcao A" first="Amílcar" last="Falcão">Amílcar Falcão</name></author><author><name sortKey="Soares A Ilva, Patricio" sort="Soares A Ilva, Patricio" uniqKey="Soares A Ilva P" first="Patrício" last="Soares-Da-Silva">Patrício Soares-Da-Silva</name></author></titleStmt><publicationStmt><idno type="wicri:source">ISTEX</idno><idno type="RBID">ISTEX:E4AE79B1074C08FAF420C8EBC9F426DED8F15F33</idno><date when="2011" year="2011">2011</date><idno type="doi">10.1111/j.2042-7158.2011.01278.x</idno><idno type="url">https://api.istex.fr/document/E4AE79B1074C08FAF420C8EBC9F426DED8F15F33/fulltext/pdf</idno><idno type="wicri:Area/Main/Corpus">001E12</idno><idno type="wicri:Area/Main/Curation">001B26</idno><idno type="wicri:Area/Main/Exploration">000279</idno></publicationStmt><sourceDesc><biblStruct><analytic><title level="a" type="main" xml:lang="en">In‐vivo evaluation of prolonged release bilayer tablets of anti‐Parkinson drugs in Göttingen minipigs</title><author><name sortKey="Sousa E Silva, Jose Paulo" sort="Sousa E Silva, Jose Paulo" uniqKey="Sousa E Silva J" first="José Paulo" last="Sousa E Silva">José Paulo Sousa E Silva</name><affiliation><wicri:noCountry code="subField">Faculty of Pharmacy</wicri:noCountry></affiliation></author><author><name sortKey="Lobo, Jose S" sort="Lobo, Jose S" uniqKey="Lobo J" first="José S." last="Lobo">José S. 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Bonifácio</name><affiliation><wicri:noCountry code="subField">São Mamede do Coronado</wicri:noCountry></affiliation></author><author><name sortKey="Machado, Rita" sort="Machado, Rita" uniqKey="Machado R" first="Rita" last="Machado">Rita Machado</name><affiliation><wicri:noCountry code="subField">São Mamede do Coronado</wicri:noCountry></affiliation></author><author><name sortKey="Falcao, Amilcar" sort="Falcao, Amilcar" uniqKey="Falcao A" first="Amílcar" last="Falcão">Amílcar Falcão</name><affiliation wicri:level="1"><country xml:lang="fr">Portugal</country><wicri:regionArea>Faculty of Pharmacy and Centre for Neuroscience and Cell Biology (CNC), University of Coimbra</wicri:regionArea><wicri:noRegion>University of Coimbra</wicri:noRegion></affiliation></author><author><name sortKey="Soares A Ilva, Patricio" sort="Soares A Ilva, Patricio" uniqKey="Soares A Ilva P" first="Patrício" last="Soares-Da-Silva">Patrício Soares-Da-Silva</name><affiliation><wicri:noCountry code="subField">University of Porto</wicri:noCountry></affiliation><affiliation><wicri:noCountry code="subField">São Mamede do Coronado</wicri:noCountry></affiliation></author></analytic><monogr></monogr><series><title level="j">Journal of Pharmacy and Pharmacology</title><idno type="ISSN">0022-3573</idno><idno type="eISSN">2042-7158</idno><imprint><publisher>Blackwell Publishing Ltd</publisher><pubPlace>Oxford, UK</pubPlace><date type="published" when="2011-06">2011-06</date><biblScope unit="volume">63</biblScope><biblScope unit="issue">6</biblScope><biblScope unit="page" from="780">780</biblScope><biblScope unit="page" to="785">785</biblScope></imprint><idno type="ISSN">0022-3573</idno></series><idno type="istex">E4AE79B1074C08FAF420C8EBC9F426DED8F15F33</idno><idno type="DOI">10.1111/j.2042-7158.2011.01278.x</idno><idno type="ArticleID">JPHP1278</idno></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0022-3573</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Sinemet</term><term>carbidopa</term><term>levodopa</term><term>nebicapone</term></keywords></textClass><langUsage><language ident="en">en</language></langUsage></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Objectives Patients with Parkinson's disease can benefit from controlled released levodopa dosage forms since there is a clear clinical advantage in obtaining sustained plasma concentrations. The purpose of this study was to obtain a tablet that prolonged the release of levodopa. Methods A novel bilayer tablet, consisting of an immediate release layer containing nebicapone (100 mg) and an erosion‐matrix type prolonged release layer containing levodopa (100 mg) and carbidopa (25 mg) was developed (LCN PR). A pharmacokinetic study in Göttingen minipigs was performed to evaluate this formulation. Key findings LCN PR tablets prolonged the in‐vitro release of levodopa in HCl 0.1 m for more than 3 h. In‐vivo plasma levodopa levels peaked at a later time point with LCN PR tablets as compared with that obtained with Sinemet 100/25 (2.7 vs 0.5 h). Nebicapone increased the maximum plasma concentration and area under the plasma concentration–time curve values for levodopa. Conclusions The results obtained suggested that LCN PR tablets may have decreased the number of tablets and daily intake in the treatment of patients with Parkinson's disease.</div></front></TEI><affiliations><list><country><li>Portugal</li></country></list><tree><noCountry><name sortKey="Bonifacio, Maria J" sort="Bonifacio, Maria J" uniqKey="Bonifacio M" first="Maria J." last="Bonifácio">Maria J. Bonifácio</name><name sortKey="Lobo, Jose S" sort="Lobo, Jose S" uniqKey="Lobo J" first="José S." last="Lobo">José S. Lobo</name><name sortKey="Machado, Rita" sort="Machado, Rita" uniqKey="Machado R" first="Rita" last="Machado">Rita Machado</name><name sortKey="Soares A Ilva, Patricio" sort="Soares A Ilva, Patricio" uniqKey="Soares A Ilva P" first="Patrício" last="Soares-Da-Silva">Patrício Soares-Da-Silva</name><name sortKey="Sousa E Silva, Jose Paulo" sort="Sousa E Silva, Jose Paulo" uniqKey="Sousa E Silva J" first="José Paulo" last="Sousa E Silva">José Paulo Sousa E Silva</name></noCountry><country name="Portugal"><noRegion><name sortKey="Falcao, Amilcar" sort="Falcao, Amilcar" uniqKey="Falcao A" first="Amílcar" last="Falcão">Amílcar Falcão</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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