Plasma Concentrations of Remoxipride and the Gastrointestinal Transit of 111ln-Marked Extended-Release Coated Spheres
Identifieur interne : 000419 ( Main/Exploration ); précédent : 000418; suivant : 000420Plasma Concentrations of Remoxipride and the Gastrointestinal Transit of 111ln-Marked Extended-Release Coated Spheres
Auteurs : RBID : ISTEX:11095_1990_Article_305661.pdfEnglish descriptors
Abstract
To explore the oral absorption of remoxipride, spheres of remoxipride were labeled with indium-111 colloid before coating with a release-controlling ethylcellulose membrane. Since the labeling remained inside the coating, it was suitable as a marker. Eight healthy volunteers were given a single dose of 100 mg remoxipride in 111In-marked spheres as a multiple-unit capsule. The radioactivity and the position of the spheres (microcapsules) were followed externally for 30 hr by gamma scintigraphy. Parallel to this, plasma concentrations were drawn for 48 hr to confirm the extended dissolution and absorption of remoxipride. The hard gelatin, multiple-unit capsule released the microcapsules within the stomach. These were then rapidly emptied into the small intestine, within 0.5–1 hr. There was then an immediate distribution in the upper small intestine before collection in the lower portion, within 2–5 hr. After passing into the large intestine, there was again an extended distribution of the microcapsules. A mean Cmax of 2.7 µM remoxipride was achieved 4 hr after drug administration and a mean AUC of 26.1 µmol · L−1 hr was achieved. Judging from the absorption versus time profile, calculated according to the Wagner–Nelson method, and the scintigraphic images, it is concluded that the main absorption occurs from the small intestine. Data from four volunteers, however, indicated a comparatively good absorption also from the large intestine. Due to the good absorption properties, it is reasonable to expect a low variation in the extent of bioavailability of remoxipride after administration in an extended-release, multiple-unit capsule formulation.
DOI: 10.1023/A:1015835609333
Links toward previous steps (curation, corpus...)
Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title>Plasma Concentrations of Remoxipride and the Gastrointestinal Transit of 111ln-Marked Extended-Release Coated Spheres</title><author><name>Christina Graffner</name><affiliation wicri:level="1"><mods:affiliation>Research and Development Laboratories, Astra Läkemedel AB, S-151 85, Södertälje, Sweden</mods:affiliation><country xml:lang="fr">Suède</country><wicri:regionArea>Research and Development Laboratories, Astra Läkemedel AB, S-151 85, Södertälje</wicri:regionArea><wicri:noRegion>Södertälje</wicri:noRegion></affiliation></author><author><name>Zoltan Wagner</name><affiliation wicri:level="1"><mods:affiliation>Fyzikon AB (Ltd), S-205 12, Malmö, Sweden</mods:affiliation><country xml:lang="fr">Suède</country><wicri:regionArea>Fyzikon AB (Ltd), S-205 12, Malmö</wicri:regionArea><wicri:noRegion>Malmö</wicri:noRegion></affiliation></author><author><name>Maj-Inger Nilsson</name><affiliation wicri:level="1"><mods:affiliation>Research and Development Laboratories, Astra Alab AB, S-151 85, Södertälje, Sweden</mods:affiliation><country xml:lang="fr">Suède</country><wicri:regionArea>Research and Development Laboratories, Astra Alab AB, S-151 85, Södertälje</wicri:regionArea><wicri:noRegion>Södertälje</wicri:noRegion></affiliation></author><author><name>Erik Widerlöv</name><affiliation wicri:level="1"><mods:affiliation>Department of Psychiatry and Neurochemistry, University of Lund, S-220 06, Lund, Sweden</mods:affiliation><country xml:lang="fr">Suède</country><wicri:regionArea>Department of Psychiatry and Neurochemistry, University of Lund, S-220 06, Lund</wicri:regionArea><wicri:noRegion>Lund</wicri:noRegion></affiliation></author></titleStmt><publicationStmt><idno type="RBID">ISTEX:11095_1990_Article_305661.pdf</idno><date when="1990">1990</date><idno type="doi">10.1023/A:1015835609333</idno><idno type="wicri:Area/Main/Corpus">000922</idno><idno type="wicri:Area/Main/Curation">000922</idno><idno type="wicri:Area/Main/Exploration">000419</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Absorption</term><term>Extended release</term><term>Gamma scintigraphy</term><term>Multiple-unit capsule</term><term>Remoxipride</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="eng">To explore the oral absorption of remoxipride, spheres of remoxipride were labeled with indium-111 colloid before coating with a release-controlling ethylcellulose membrane. Since the labeling remained inside the coating, it was suitable as a marker. Eight healthy volunteers were given a single dose of 100 mg remoxipride in 111In-marked spheres as a multiple-unit capsule. The radioactivity and the position of the spheres (microcapsules) were followed externally for 30 hr by gamma scintigraphy. Parallel to this, plasma concentrations were drawn for 48 hr to confirm the extended dissolution and absorption of remoxipride. The hard gelatin, multiple-unit capsule released the microcapsules within the stomach. These were then rapidly emptied into the small intestine, within 0.5–1 hr. There was then an immediate distribution in the upper small intestine before collection in the lower portion, within 2–5 hr. After passing into the large intestine, there was again an extended distribution of the microcapsules. A mean Cmax of 2.7 µM remoxipride was achieved 4 hr after drug administration and a mean AUC of 26.1 µmol · L−1 hr was achieved. Judging from the absorption versus time profile, calculated according to the Wagner–Nelson method, and the scintigraphic images, it is concluded that the main absorption occurs from the small intestine. Data from four volunteers, however, indicated a comparatively good absorption also from the large intestine. Due to the good absorption properties, it is reasonable to expect a low variation in the extent of bioavailability of remoxipride after administration in an extended-release, multiple-unit capsule formulation.</div></front></TEI><mods xsi:schemaLocation="http://www.loc.gov/mods/v3 file:///applis/istex/home/loadistex/home/etc/xsd/mods.xsd" version="3.4" istexId="a0b429c16119ce303f6c9af1db65bfb697e267c5"><titleInfo lang="eng"><title>Plasma Concentrations of Remoxipride and the Gastrointestinal Transit of 111ln-Marked Extended-Release Coated Spheres</title></titleInfo><name type="personal"><namePart type="given">Christina</namePart><namePart type="family">Graffner</namePart><role><roleTerm type="text">author</roleTerm></role><affiliation>Research and Development Laboratories, Astra Läkemedel AB, S-151 85, Södertälje, Sweden</affiliation></name><name type="personal"><namePart type="given">Zoltan</namePart><namePart type="family">Wagner</namePart><role><roleTerm type="text">author</roleTerm></role><affiliation>Fyzikon AB (Ltd), S-205 12, Malmö, Sweden</affiliation></name><name type="personal"><namePart type="given">Maj-Inger</namePart><namePart type="family">Nilsson</namePart><role><roleTerm type="text">author</roleTerm></role><affiliation>Research and Development Laboratories, Astra Alab AB, S-151 85, Södertälje, Sweden</affiliation></name><name type="personal"><namePart type="given">Erik</namePart><namePart type="family">Widerlöv</namePart><role><roleTerm type="text">author</roleTerm></role><affiliation>Department of Psychiatry and Neurochemistry, University of Lund, S-220 06, Lund, Sweden</affiliation></name><typeOfResource>text</typeOfResource><genre>Original Paper</genre><originInfo><publisher>Kluwer Academic Publishers-Plenum Publishers, New York</publisher><dateValid encoding="w3cdtf">2004-08-27</dateValid><copyrightDate encoding="w3cdtf">1990</copyrightDate></originInfo><language><languageTerm type="code" authority="iso639-2b">eng</languageTerm></language><physicalDescription><internetMediaType>text/html</internetMediaType></physicalDescription><abstract lang="eng">To explore the oral absorption of remoxipride, spheres of remoxipride were labeled with indium-111 colloid before coating with a release-controlling ethylcellulose membrane. Since the labeling remained inside the coating, it was suitable as a marker. Eight healthy volunteers were given a single dose of 100 mg remoxipride in 111In-marked spheres as a multiple-unit capsule. The radioactivity and the position of the spheres (microcapsules) were followed externally for 30 hr by gamma scintigraphy. Parallel to this, plasma concentrations were drawn for 48 hr to confirm the extended dissolution and absorption of remoxipride. The hard gelatin, multiple-unit capsule released the microcapsules within the stomach. These were then rapidly emptied into the small intestine, within 0.5–1 hr. There was then an immediate distribution in the upper small intestine before collection in the lower portion, within 2–5 hr. After passing into the large intestine, there was again an extended distribution of the microcapsules. A mean Cmax of 2.7 µM remoxipride was achieved 4 hr after drug administration and a mean AUC of 26.1 µmol · L−1 hr was achieved. Judging from the absorption versus time profile, calculated according to the Wagner–Nelson method, and the scintigraphic images, it is concluded that the main absorption occurs from the small intestine. Data from four volunteers, however, indicated a comparatively good absorption also from the large intestine. Due to the good absorption properties, it is reasonable to expect a low variation in the extent of bioavailability of remoxipride after administration in an extended-release, multiple-unit capsule formulation.</abstract><subject lang="eng"><topic>remoxipride</topic><topic>extended release</topic><topic>gamma scintigraphy</topic><topic>multiple-unit capsule</topic><topic>absorption</topic></subject><relatedItem type="series"><titleInfo type="abbreviated"><title>Pharm Res</title></titleInfo><titleInfo><title>Pharmaceutical Research</title><subTitle>An Official Journal of the American Association of Pharmaceutical Scientists</subTitle><partNumber>Year: 1990</partNumber><partNumber>Volume: 7</partNumber><partNumber>Number: 1</partNumber></titleInfo><genre>Archive Journal</genre><originInfo><dateIssued encoding="w3cdtf">1990-01-01</dateIssued><copyrightDate encoding="w3cdtf">1990</copyrightDate></originInfo><subject usage="primary"><topic>Biomedicine</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Biochemistry, general</topic><topic>Medical Law</topic><topic>Biomedical Engineering</topic></subject><identifier type="issn">0724-8741</identifier><identifier type="issn">Electronic: 1573-904X</identifier><identifier type="matrixNumber">11095</identifier><identifier type="local">IssueArticleCount: 23</identifier><recordInfo><recordOrigin>Plenum Publishing Corporation, 1990</recordOrigin></recordInfo></relatedItem><identifier type="doi">10.1023/A:1015835609333</identifier><identifier type="matrixNumber">Art10</identifier><identifier type="local">305661</identifier><accessCondition type="use and reproduction">MetadataGrant: OpenAccess</accessCondition><accessCondition type="use and reproduction">AbstractGrant: OpenAccess</accessCondition><accessCondition type="restriction on access">BodyPDFGrant: Restricted</accessCondition><accessCondition type="restriction on access">BodyHTMLGrant: Restricted</accessCondition><accessCondition type="restriction on access">BibliographyGrant: Restricted</accessCondition><accessCondition type="restriction on access">ESMGrant: Restricted</accessCondition><part><extent unit="pages"><start>54</start><end>58</end></extent></part><recordInfo><recordOrigin>Plenum Publishing Corporation, 1990</recordOrigin><recordIdentifier>11095_1990_Article_305661.pdf</recordIdentifier></recordInfo></mods></record>Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=IndiumV1/Data/Main/Exploration
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 000419 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 000419 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien
|wiki= *** parameter Area/wikiCode missing ***
|area= IndiumV1
|flux= Main
|étape= Exploration
|type= RBID
|clé= ISTEX:11095_1990_Article_305661.pdf
|texte= Plasma Concentrations of Remoxipride and the Gastrointestinal Transit of 111ln-Marked Extended-Release Coated Spheres
}}
| This area was generated with Dilib version V0.5.81. |  |