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Pharmacokinetics of radiopharmaceuticals.

Identifieur interne : 004F23 ( Main/Exploration ); précédent : 004F22; suivant : 004F24

Pharmacokinetics of radiopharmaceuticals.

Auteurs : RBID : pubmed:1304681

English descriptors

Abstract

The pharmacokinetics of various radiopharmaceuticals following i.v. administration in mice and rats has been studied and compared. Before injection the radiochemical purity (RP) of the compounds were determined by HPLC and PAGE. In all cases RP-s were higher than 90%. The biodistribution of 99mTc labelled anti CEA IgG was studied in mice bearing human colon carcinoma xenografts. Animals with different tumour weights showed different blood kinetic and tumor uptake. The pilot clinical study of the 99mTc labelled anti melanoma Fab and 111-In-DTPA labelled anti melanoma F(ab')2 showed differences in the pharmacokinetic parameters. (99mTc labelled: comp.A. 84.6%; T1/2:0.6 h, 111-In-labelled: comp.A.: 46%, T1/2 1.5 h.) The various isonitrile derivatives synthetized in our laboratory were labelled with 99mTc and the biodistribution were tested in rats. The kinetic study showed that all the three molecules have different half lives in the heart and liver (T1/2 for heart ranged 5.1-18.6 h, for liver T1/2:1.2-2.5 h). Reversed phase HPLC study of the collected bile showed the 15-100% of injected compounds are metabolized during hepatic excretion. Literature data and our recent observations confirm that the knowledge of pharmacokinetics of radiolabelled compounds both in research, development and clinical practice is of basic importance.

PubMed: 1304681

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Le document en format XML

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<title xml:lang="en">Pharmacokinetics of radiopharmaceuticals.</title>
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<name sortKey="J Noki, G A" uniqKey="J Noki G">G A Jánoki</name>
<affiliation wicri:level="1">
<nlm:affiliation>Frédérick Joliot Curie National Institute for Radiobiology and Radiohygiene, Budapest, Hungary.</nlm:affiliation>
<country xml:lang="fr">Hongrie</country>
<wicri:regionArea>Frédérick Joliot Curie National Institute for Radiobiology and Radiohygiene, Budapest</wicri:regionArea>
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<name sortKey="Kerekes, A" uniqKey="Kerekes A">A Kerekes</name>
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<term>Animals</term>
<term>Antibodies, Monoclonal (immunology)</term>
<term>Bile (metabolism)</term>
<term>Carcinoembryonic Antigen (immunology)</term>
<term>Chromatography, High Pressure Liquid</term>
<term>Chromatography, Thin Layer</term>
<term>Colonic Neoplasms (metabolism)</term>
<term>Electrophoresis, Polyacrylamide Gel</term>
<term>Indium Radioisotopes (diagnostic use)</term>
<term>Male</term>
<term>Melanoma (immunology)</term>
<term>Mice</term>
<term>Mice, Inbred Strains</term>
<term>Neoplasms, Experimental (metabolism)</term>
<term>Pentetic Acid (pharmacokinetics)</term>
<term>Radioisotopes (pharmacokinetics)</term>
<term>Rats</term>
<term>Rats, Inbred Strains</term>
<term>Technetium (pharmacokinetics)</term>
<term>Tissue Distribution</term>
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<term>Indium Radioisotopes</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="immunology" xml:lang="en">
<term>Antibodies, Monoclonal</term>
<term>Carcinoembryonic Antigen</term>
</keywords>
<keywords scheme="MESH" qualifier="immunology" xml:lang="en">
<term>Melanoma</term>
</keywords>
<keywords scheme="MESH" qualifier="metabolism" xml:lang="en">
<term>Bile</term>
<term>Colonic Neoplasms</term>
<term>Neoplasms, Experimental</term>
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<keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en">
<term>Pentetic Acid</term>
<term>Radioisotopes</term>
<term>Technetium</term>
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<term>Animals</term>
<term>Chromatography, High Pressure Liquid</term>
<term>Chromatography, Thin Layer</term>
<term>Electrophoresis, Polyacrylamide Gel</term>
<term>Male</term>
<term>Mice</term>
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<term>Rats</term>
<term>Rats, Inbred Strains</term>
<term>Tissue Distribution</term>
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<front>
<div type="abstract" xml:lang="en">The pharmacokinetics of various radiopharmaceuticals following i.v. administration in mice and rats has been studied and compared. Before injection the radiochemical purity (RP) of the compounds were determined by HPLC and PAGE. In all cases RP-s were higher than 90%. The biodistribution of 99mTc labelled anti CEA IgG was studied in mice bearing human colon carcinoma xenografts. Animals with different tumour weights showed different blood kinetic and tumor uptake. The pilot clinical study of the 99mTc labelled anti melanoma Fab and 111-In-DTPA labelled anti melanoma F(ab')2 showed differences in the pharmacokinetic parameters. (99mTc labelled: comp.A. 84.6%; T1/2:0.6 h, 111-In-labelled: comp.A.: 46%, T1/2 1.5 h.) The various isonitrile derivatives synthetized in our laboratory were labelled with 99mTc and the biodistribution were tested in rats. The kinetic study showed that all the three molecules have different half lives in the heart and liver (T1/2 for heart ranged 5.1-18.6 h, for liver T1/2:1.2-2.5 h). Reversed phase HPLC study of the collected bile showed the 15-100% of injected compounds are metabolized during hepatic excretion. Literature data and our recent observations confirm that the knowledge of pharmacokinetics of radiolabelled compounds both in research, development and clinical practice is of basic importance.</div>
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<Day>06</Day>
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<Month>11</Month>
<Day>21</Day>
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<Year>1992</Year>
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<Title>Acta physiologica Hungarica</Title>
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<ArticleTitle>Pharmacokinetics of radiopharmaceuticals.</ArticleTitle>
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<AbstractText>The pharmacokinetics of various radiopharmaceuticals following i.v. administration in mice and rats has been studied and compared. Before injection the radiochemical purity (RP) of the compounds were determined by HPLC and PAGE. In all cases RP-s were higher than 90%. The biodistribution of 99mTc labelled anti CEA IgG was studied in mice bearing human colon carcinoma xenografts. Animals with different tumour weights showed different blood kinetic and tumor uptake. The pilot clinical study of the 99mTc labelled anti melanoma Fab and 111-In-DTPA labelled anti melanoma F(ab')2 showed differences in the pharmacokinetic parameters. (99mTc labelled: comp.A. 84.6%; T1/2:0.6 h, 111-In-labelled: comp.A.: 46%, T1/2 1.5 h.) The various isonitrile derivatives synthetized in our laboratory were labelled with 99mTc and the biodistribution were tested in rats. The kinetic study showed that all the three molecules have different half lives in the heart and liver (T1/2 for heart ranged 5.1-18.6 h, for liver T1/2:1.2-2.5 h). Reversed phase HPLC study of the collected bile showed the 15-100% of injected compounds are metabolized during hepatic excretion. Literature data and our recent observations confirm that the knowledge of pharmacokinetics of radiolabelled compounds both in research, development and clinical practice is of basic importance.</AbstractText>
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<DescriptorName MajorTopicYN="N">Male</DescriptorName>
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