Effects of biliary excretion on the disposition of felodipine and metabolites in the rat
1. After i.v. and intraduodenal administration of 3H-felodipine to rats, approx. 50% of the dose was excreted in bile in the first 6 h. Total urinary and biliary recoveries after both administration routes were similar. 2. Neither unchanged felodipine nor oxidized pyridine metabolite was detected in...
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| Veröffentlicht in: | Xenobiotica 1987, Vol.17 (10), p.1203-1214 |
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| container_title | Xenobiotica |
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| creator | Sutfin, T. A. Gabrielsson, M. Regårdh, C. G. |
| description | 1. After i.v. and intraduodenal administration of 3H-felodipine to rats, approx. 50% of the dose was excreted in bile in the first 6 h. Total urinary and biliary recoveries after both administration routes were similar.
2. Neither unchanged felodipine nor oxidized pyridine metabolite was detected in bile. Bile collection had no effect on the blood concentration-time profiles of either compound.
3. Bile collection decreased the area under the blood concentration-time curve (AUC) of total, unidentified felodipine metabolites by 30%, and their urinary recovery by 50%.
4. Of the total metabolites excreted in bile, 40% was calculated to be subject to enterohepatic recycling.
5. The dose-normalized AUC of both felodipine and pyridine metabolite were decreased after intraduodenal administration of drug, indicating pre-systemic elimination of drug, and possibly of the pyridine, in the gut. Route of administration had no effect on the AUC of total unidentified metabolites. |
| doi_str_mv | 10.3109/00498258709167412 |
| format | Article |
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2. Neither unchanged felodipine nor oxidized pyridine metabolite was detected in bile. Bile collection had no effect on the blood concentration-time profiles of either compound.
3. Bile collection decreased the area under the blood concentration-time curve (AUC) of total, unidentified felodipine metabolites by 30%, and their urinary recovery by 50%.
4. Of the total metabolites excreted in bile, 40% was calculated to be subject to enterohepatic recycling.
5. The dose-normalized AUC of both felodipine and pyridine metabolite were decreased after intraduodenal administration of drug, indicating pre-systemic elimination of drug, and possibly of the pyridine, in the gut. Route of administration had no effect on the AUC of total unidentified metabolites.</description><identifier>ISSN: 0049-8254</identifier><identifier>EISSN: 1366-5928</identifier><identifier>DOI: 10.3109/00498258709167412</identifier><identifier>PMID: 3424867</identifier><identifier>CODEN: XENOBH</identifier><language>eng</language><publisher>London: Informa UK Ltd</publisher><subject>Animals ; Antianginal agents. Coronary vasodilator agents ; Bile - metabolism ; Biological and medical sciences ; Cardiovascular system ; Chromatography, High Pressure Liquid ; Felodipine ; Male ; Medical sciences ; Nitrendipine - analogs & derivatives ; Nitrendipine - metabolism ; Nitrendipine - pharmacokinetics ; Pharmacology. Drug treatments ; Pyridines - metabolism ; Rats ; Rats, Inbred Strains</subject><ispartof>Xenobiotica, 1987, Vol.17 (10), p.1203-1214</ispartof><rights>1987 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 1987</rights><rights>1988 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c430t-1d2763796836bf0b9dd7afe0d775599d43afbd8bb86f752dc14a930b547833af3</citedby><cites>FETCH-LOGICAL-c430t-1d2763796836bf0b9dd7afe0d775599d43afbd8bb86f752dc14a930b547833af3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.3109/00498258709167412$$EPDF$$P50$$Ginformaworld$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.3109/00498258709167412$$EHTML$$P50$$Ginformaworld$$H</linktohtml><link.rule.ids>314,777,781,4010,27904,27905,27906,59626,59732,60415,60521,61200,61235,61381,61416</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=7596699$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3424867$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Sutfin, T. A.</creatorcontrib><creatorcontrib>Gabrielsson, M.</creatorcontrib><creatorcontrib>Regårdh, C. G.</creatorcontrib><title>Effects of biliary excretion on the disposition of felodipine and metabolites in the rat</title><title>Xenobiotica</title><addtitle>Xenobiotica</addtitle><description>1. After i.v. and intraduodenal administration of 3H-felodipine to rats, approx. 50% of the dose was excreted in bile in the first 6 h. Total urinary and biliary recoveries after both administration routes were similar.
2. Neither unchanged felodipine nor oxidized pyridine metabolite was detected in bile. Bile collection had no effect on the blood concentration-time profiles of either compound.
3. Bile collection decreased the area under the blood concentration-time curve (AUC) of total, unidentified felodipine metabolites by 30%, and their urinary recovery by 50%.
4. Of the total metabolites excreted in bile, 40% was calculated to be subject to enterohepatic recycling.
5. The dose-normalized AUC of both felodipine and pyridine metabolite were decreased after intraduodenal administration of drug, indicating pre-systemic elimination of drug, and possibly of the pyridine, in the gut. Route of administration had no effect on the AUC of total unidentified metabolites.</description><subject>Animals</subject><subject>Antianginal agents. Coronary vasodilator agents</subject><subject>Bile - metabolism</subject><subject>Biological and medical sciences</subject><subject>Cardiovascular system</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Felodipine</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Nitrendipine - analogs & derivatives</subject><subject>Nitrendipine - metabolism</subject><subject>Nitrendipine - pharmacokinetics</subject><subject>Pharmacology. Drug treatments</subject><subject>Pyridines - metabolism</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><issn>0049-8254</issn><issn>1366-5928</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kF1rFDEUhoNY6rr6A7wQciHejU0mmWSC3pRSP6DQmwreDfk4YVMykzXJov33Zpm1IEIhEMj7vIecB6E3lHxglKgLQrga-2GURFEhOe2foQ1lQnSD6sfnaHPMuwbwF-hlKfeEEEH7_hydM97zUcgN-nHtPdhacPLYhBh0fsDw22aoIS24nboD7ELZpxLWJ489xOTCPiyA9eLwDFWbFEOFgsNayLq-QmdexwKvT_cWff98fXf1tbu5_fLt6vKms5yR2lHXS8GkEiMTxhOjnJPaA3FSDoNSjjPtjRuNGYWXQ-8s5VoxYgYuR9YytkXv17n7nH4eoNRpDsVCjHqBdCiTlEc1jd0iuoI2p1Iy-Gmfw9z2nSiZjjan_2y2ztvT8IOZwT02Tvpa_u6U62J19FkvNpRHTA5KCKUa9mnFwuJTnvWvlKObqn6IKf_tsKd-8fGf-g50rDurM0z36ZCXpveJHf4A3J2h6Q</recordid><startdate>1987</startdate><enddate>1987</enddate><creator>Sutfin, T. A.</creator><creator>Gabrielsson, M.</creator><creator>Regårdh, C. G.</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>1987</creationdate><title>Effects of biliary excretion on the disposition of felodipine and metabolites in the rat</title><author>Sutfin, T. A. ; Gabrielsson, M. ; Regårdh, C. G.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c430t-1d2763796836bf0b9dd7afe0d775599d43afbd8bb86f752dc14a930b547833af3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Animals</topic><topic>Antianginal agents. Coronary vasodilator agents</topic><topic>Bile - metabolism</topic><topic>Biological and medical sciences</topic><topic>Cardiovascular system</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Felodipine</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Nitrendipine - analogs & derivatives</topic><topic>Nitrendipine - metabolism</topic><topic>Nitrendipine - pharmacokinetics</topic><topic>Pharmacology. Drug treatments</topic><topic>Pyridines - metabolism</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sutfin, T. A.</creatorcontrib><creatorcontrib>Gabrielsson, M.</creatorcontrib><creatorcontrib>Regårdh, C. G.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Xenobiotica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Sutfin, T. A.</au><au>Gabrielsson, M.</au><au>Regårdh, C. G.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effects of biliary excretion on the disposition of felodipine and metabolites in the rat</atitle><jtitle>Xenobiotica</jtitle><addtitle>Xenobiotica</addtitle><date>1987</date><risdate>1987</risdate><volume>17</volume><issue>10</issue><spage>1203</spage><epage>1214</epage><pages>1203-1214</pages><issn>0049-8254</issn><eissn>1366-5928</eissn><coden>XENOBH</coden><abstract>1. After i.v. and intraduodenal administration of 3H-felodipine to rats, approx. 50% of the dose was excreted in bile in the first 6 h. Total urinary and biliary recoveries after both administration routes were similar.
2. Neither unchanged felodipine nor oxidized pyridine metabolite was detected in bile. Bile collection had no effect on the blood concentration-time profiles of either compound.
3. Bile collection decreased the area under the blood concentration-time curve (AUC) of total, unidentified felodipine metabolites by 30%, and their urinary recovery by 50%.
4. Of the total metabolites excreted in bile, 40% was calculated to be subject to enterohepatic recycling.
5. The dose-normalized AUC of both felodipine and pyridine metabolite were decreased after intraduodenal administration of drug, indicating pre-systemic elimination of drug, and possibly of the pyridine, in the gut. Route of administration had no effect on the AUC of total unidentified metabolites.</abstract><cop>London</cop><pub>Informa UK Ltd</pub><pmid>3424867</pmid><doi>10.3109/00498258709167412</doi><tpages>12</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0049-8254 |
| ispartof | Xenobiotica, 1987, Vol.17 (10), p.1203-1214 |
| issn | 0049-8254 1366-5928 |
| language | eng |
| recordid | cdi_pascalfrancis_primary_7596699 |
| source | MEDLINE; Taylor & Francis; Taylor & Francis Medical Library - CRKN |
| subjects | Animals Antianginal agents. Coronary vasodilator agents Bile - metabolism Biological and medical sciences Cardiovascular system Chromatography, High Pressure Liquid Felodipine Male Medical sciences Nitrendipine - analogs & derivatives Nitrendipine - metabolism Nitrendipine - pharmacokinetics Pharmacology. Drug treatments Pyridines - metabolism Rats Rats, Inbred Strains |
| title | Effects of biliary excretion on the disposition of felodipine and metabolites in the rat |
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